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ByRx Harun

What Is Antacids? -Uses, Dosage, Side Effects, Interaction

What Is Antacids?/Antacids are a group of drugs that have been on the market for many years. They were initially first-line defense against peptic ulcer disease; however, the discovery of proton pump inhibitors revolutionized the treatment of peptic ulcer disease. Currently, antacid use is restricted to the relief of mild intermittent gastroesophageal reflux disease (GERD) associated heartburn. The estimated prevalence of heartburn at least once per week in North America ranges from 18% to 28%, with 25% adults reporting heartburn daily.

Antacids are medications that do not require a prescription; in other words, they are self-prescribed. Antacids are a combination of various compounds with various salts of calcium, magnesium, and aluminum as the active ingredients. The antacids act by neutralizing the acid in the stomach and by inhibiting pepsin, which is a proteolytic enzyme. Each of these cationic salts has a characteristic pharmacological property that determines its clinical use.

Mechanism of Action of Antacids

The antacids reduce the acid reaching the duodenum by neutralizing the acid present in the stomach. The main objectives are:

  • Alleviating pain
  • Relieving pylorospasms
  • Avoid digestion and corrosion by acid chyme

The salts’ mechanism of neutralization of acid varies, and each salt has a different mechanism with the ultimate goal of acid neutralization.

Aluminum Hydroxide

The formulation of aluminum hydrochloride and water results in the neutralization of the acid in the stomach. It is also known to inhibit pepsin activity. Aluminum hydroxide is complexed with a sulfated polysaccharide sucrose octasulfate to form sucralfate. This complex does not have a significant buffering action against the acid or has no effect on the pepsin secretion and does not alter the gastric acid production in any way. Nevertheless, it is known to heal chronic ulcers and prevent acute mucosal damage induced chemically by reducing access to pepsin and acid. Sucralfate, like its aluminum hydroxide component, is known to stimulate angiogenesis and granulation tissue formation.

Aluminum hydroxide is also useful in hyperphosphatemia due to its ability to bind phosphate in the gastrointestinal (GI) tract and subsequently prevent the absorption of phosphate.

Calcium Salts

Calcium salts neutralize gastric acidity resulting in increased gastric and duodenal bulb pH; they additionally inhibit the proteolytic activity of pepsin if the pH is greater than 4 and increase lower esophageal sphincter tone. The calcium released from calcium carbonate is known to increase peristalsis in the esophagus, pushing the acid into the stomach and provide relief from symptoms of heartburn. The calcium salts also form combined insoluble compounds with dietary phosphate and prevent the absorption of later.

The acid-neutralizing mechanism of the antacids is well understood, as mentioned above. In addition to this, other mechanisms add to the ulcer healing properties of this class of drugs. The exact mechanism is still unclear, but it is believed to be a combination of:

  • Ability to promote angiogenesis
  • Bind to bile acids
  • Inhibit peptic activity
  • Suppress Helicobacter pylori growth

Indications of Antacids

Antacids have therapeutic use for the following:

  • Heartburn symptoms in GERD
  • Duodenal and gastric ulcers
  • Stress gastritis
  • Pancreatic insufficiency
  • Non-ulcer dyspepsia
  • Diarrhea caused by bile-acid
  • Biliary reflux
  • Constipation
  • Osteoporosis
  • Urinary alkalinization
  • Phosphate binding in chronic renal failure

Contraindications of Antacids

The absolute contraindication is hypersensitivity to any component of the formulation. Also, antacid agents require caution in patients with:

  • Renal  failure
  • Heart failure
  • Edema
  • Cirrhosis
  • Low-sodium diets
  • Uremia
  • GI hemorrhages
  • Hyperparathyroidism
  • Renal calculus
  • Achlorhydria

Dosage of Antacids

The dose for antacids depends upon the age of the patient, the purpose of administration (neutralization of acid or off-label use), and the presence of other comorbidities like renal or hepatic impairment. As all the forms of these medications are available as over the counter medication, the dosing recommendation varies by product/and or manufacturer.

Aluminum Hydroxide (Antacid)
  • Oral: Usually taken daily after meals and at bedtime at a dose of  640 mg up to 5 to 6 times a day with a maximum dose of 3840 mg per 24 hours.
  • Suspension  The dose for suspension form is 320 mg/5 mL (473 mL). The suspension is to be shaken before use and is to be followed by water.
Hyperphosphatemia
  • Oral:  Use is reserved for patients with serum phosphorus levels greater than 7 mg/dl. It is to be taken with meals at a dose of 300  to 600 mg three times a day, with use limited to a short period (4 weeks).
Calcium Carbonate (Antacid)

It is used up to a maximum dose of 8000 mg per day up to 2 weeks with 1 to 4 tablets for symptomatic relief.

Hyperphosphatemia

The total dose is not to exceed 2000 mg per day.

Adverse Effects of Antacids

Adverse effects are prominent in the infant and the elderly populations. The chronic use of antacids in this population is not a recommendation due to safety concerns.

Aluminum Hydroxide

Aluminum use is associated with an increased risk of toxicity in individuals with renal failure and infants. It presents as:

  • Osteopenia
  • Microcytic anemia
  • Neurotoxicity
  • Osteomalacia
  • Constipation
  • Fecal impaction
  • Nausea
  • Vomiting
  • Abdominal cramps
  • Hypomagnesemia
  • Hypophosphatemia
Calcium Carbonate

The adverse reactions often seen with this  group of antacids are:

  • Abdominal pain
  • Anorexia
  • Constipation
  • Acid rebound
  • Nausea
  • Vomiting
  • Flatulence
  • Xerostomia
  • Headache
  • Hypercalcemia
  • Hypophosphatemia
  • Milk-alkali syndrome

Pregnancy and Breastfeeding

Antacids containing aluminum salts are safe to be used in pregnant women as well as for women during labor for aspiration prophylaxis.  The information regarding the use of aluminum-containing antacids in breastfeeding females has not been studied, but aluminum is known to be endogenous to breast milk. In the case of calcium-containing antacids, excessive use is to be avoided in pregnant women as calcium crosses the placenta. The amount of calcium reaching the fetus is dependent on the physiological changes in the mother. Maternal calcium intake also affects the amount of calcium excreted in breast milk; the currently prevailing opinion is that the use of calcium-containing antacids is safe during breastfeeding.

Monitoring

The average therapeutic dose of antacid is 10 to 15 mL (1 tablespoon or one package content) of liquid or 1 to 2 tablets 3 to 4 times a day. Periodic monitoring of calcium and phosphorus plasma concentrations is a suggested practice in patients on chronic therapy.

Toxicity

No information is available regarding toxicities caused by aluminum- and calcium-containing antacids. However, antacids are to be used cautiously in the high-risk population mentioned above.

References

ByRx Harun

What Is Influenza Vaccines? – Indications, Contraindication

What Is Influenza Vaccines? /Influenza Vaccines belong to the Orthomyxoviridae RNA virus family and classify into three distinct types based on their major antigenic differences; influenza A, influenza B and influenza C.  Influenza viruses cause the annual human epidemics, seasonal and pandemic. Seasonal influenza epidemics caused by influenza A and B viruses result in 3–5 million severe cases and thousands of deaths globally each year. Influenza pandemics caused by influenza A virus emerge at unpredictable intervals. The influenza A virus will cause epidemics and pandemics because of its spread from migrating birds, pigs, horses, and humans. Transmission can be human to human from fomites, coughing and sneezing. Pandemics are responsible for increased morbidity and mortality, compared with seasonal influenza. Four such pandemics have occurred in the past century, during 1918, 1957, 1968, and 2009. Influenza B causes only human to human spread with a particular emphasis on the fact that no other hosts are involved, therefore, not involved in pandemics. Influenza C is a mild disease. It causes seasonal episodes of influenza such as Northern infections when they happen from September to March while Southern infections happen from May to September. Due to the variation in viruses responsible for infections in these two seasons; it needs two different sets of vaccines. Influenza generally has an incubation period of 2 days, ranging from 1 to 4 days.

FDA-approved indications

  1. Prevention of Influenza A in persons aged 6 months and above
  2. Prevention of Influenza B in persons aged 6 months and above

The Centers for Disease Control and Prevention (CDC) recommends administration of an annual influenza vaccine for all persons above 6 months of age.

The vaccination is the most effective method for prevention and control of influenza. It is most effective in children greater than 2 years old and healthy adults. The efficacy of the seasonal influenza vaccine ranges between 10% and 60%. The lowest efficacy occurs when vaccine strains are not well matched to circulating strains. Both the trivalent and quadrivalent vaccines are FDA approved.

Regarding immunization in pregnancy, a randomized controlled trial conducted in South Africa has shown that when pregnant women receive the influenza vaccine, it halves their risk of developing influenza while reducing the risk of their infants (up to 24 weeks) contracting the illness.

Data shows the trivalent influenza vaccine provides protection in HIV-infected adults without severe immunosuppression while the effectiveness in HIV-infected children aged <5 years is somewhat uncertain. In certain groups, including the elderly, immune-compromised individuals and infants, the influenza vaccine is less effective, but it is beneficial by reducing the incidence of severe disease, like bronchopneumonia, and reduces hospital admission and mortality.

Mechanism of Action of Influenza Vaccines

Influenza viruses express two types of antigens; hemagglutinin (HA) and neuraminidase (NA). Influenza A virus has 18 HA, and 11 NA subtypes, and these antigens are critical for the virulence of the organism. The trimeric hemagglutinin glycoprotein acts by promoting attachment of the virus to the host cell surface resulting in infusion and thereby releasing virions into the cytoplasm.

Differently combined H and N antigens are seen in influenza A, which in turn undergo antigenic drifts and shifts resulting in antigenic variation, and thereby the necessity for vaccine strain types to vary accordingly. Antigenic drifts are genetic changes occurring in the virus due to various actions of polymerases leading to gradual antigenic changes in both HA and NA producing new variant strains. An antigenic shift takes place when the currently circulating virus disappears and gets replaced by a new subtype with novel glycoproteins to which antibodies against the previously circulating subtype do not cross-react.

The influenza vaccine conveys immunity against the influenza virus by stimulating the production of antibodies specific to the disease. Antibodies to NA act by aggregating viruses on the cell surface effectively and reducing the amount of virus released from infected cells.  Regarding the induction of immunity, the surface HA protein of the influenza virus contains two structural elements, head and stalk wherein the head is the primary target of antibodies that confer protective immunity against influenza viruses.

Flu shots offer protection against three or four strains of the flu virus. Trivalent flu vaccines provide protection against two influenza A strains, H1N1 and H3N2, and one influenza B strain. Quadrivalent flu vaccines protect against the same strains as the trivalent vaccine as well as an additional strain of influenza B.

The mechanism of immune protection is more complicated, as while primarily humoral, cell-mediated immunity also plays an essential role in immunity to influenza. After vaccination, it takes two weeks to build up an immune response against the flu. The effectiveness of a vaccine depends on several host factors such as age, underlying health status, genetic status and furthermore on antigenic matches between the vaccine and circulating viruses.

Contraindications of Influenza Vaccines

  • History of allergy or hypersensitivity to any component of the vaccine (i.e., egg protein allergy)
  • Infants less than 6 months of age
  • High fever
  • Guillain–Barre Syndrome

Administration of Influenza Vaccines

Flu shots are available in several forms:

  • Intramuscular vaccine
  • High-dose vaccine (> 65 years)
  • Intradermal vaccine (18 to 64years)
  • Egg-free vaccine (>4 years)
  • Nasal spray (2 to 49years)
  • Needle-free vaccine as a jet injector (18 to 64 years)

Dosage

  • Age 6 months to 3 years;

0.25 – 0.5 ml: 2 doses 4 weeks apart.

  • Age 3 to 8 years:

Not previously vaccinated: 2 doses, 0.5 ml 4 weeks apart.

Vaccinated previous season; 0.5 ml one or two doses 4 weeks apart.

  • Age 9 years and above:

Single dose;  0.5 ml

Adverse Effects of Influenza Vaccines

  • Injection site reactions
  • Fever
  • Irritability
  • Drowsiness
  • Myalgia
  • Nasal spray
    • Upper respiratory symptoms
    • Fever, headache, vomiting
    • Lower respiratory symptoms

  • Rare

    • Allergic reaction
    • Urticaria/Anaphylaxis

Monitoring

CDC and FDA continuously monitor vaccine safety and will inform health officials, health care providers, and the public when necessary.

CDC uses three systems vaccine safety monitoring:

  • The Vaccine Adverse Event Reporting System (VAERS): an early warning system that helps CDC and FDA monitor problems following vaccination.  Anyone can report possible vaccine side effects to VAERS.
  • The Vaccine Safety Data link (VSD): a collaborative effort between the CDC and nine other health care organizations, which allows ongoing monitoring and proactive searches of vaccine-related data.
  • The Clinical Immunization Safety Assessment (CISA) Project: a partnership between CDC and several medical centers that conduct clinical research on vaccine-associated health risks.

Inactivated flu vaccine and pneumococcal vaccine administered at the same time may show an increased risk for febrile seizures.

Toxicity

The vaccine does not manifest any dose-dependent toxicity.

The toxicity regarding carcinogenicity and infertility have undergone extensive study and shown to be negative.

The components of the influenza vaccine are:

  • Formaldehyde used to inactivate toxins from viruses and bacteria.
  • Thimerosal safeguards against contamination, and it is only present in multi-dose vials.
  • Aluminum salts act as adjuvants and impart stronger immune response.
  • Gelatin is present as a stabilizer.
  • Antibiotics, such as gentamicin or neomycin are present in the flu vaccine to keep bacteria from growing.

Toxicity due to the components of the vaccine is not present due to the inconspicuous amounts in the vaccine.

References

ByRx Harun

Influenza Vaccines – Uses, Dosage, Side Effect, Interaction

Influenza Vaccines belong to the Orthomyxoviridae RNA virus family and classify into three distinct types based on their major antigenic differences; influenza A, influenza B and influenza C.  Influenza viruses cause the annual human epidemics, seasonal and pandemic. Seasonal influenza epidemics caused by influenza A and B viruses result in 3–5 million severe cases and thousands of deaths globally each year. Influenza pandemics caused by influenza A virus emerge at unpredictable intervals. The influenza A virus will cause epidemics and pandemics because of its spread from migrating birds, pigs, horses, and humans. Transmission can be human to human from fomites, coughing and sneezing. Pandemics are responsible for increased morbidity and mortality, compared with seasonal influenza. Four such pandemics have occurred in the past century, during 1918, 1957, 1968, and 2009. Influenza B causes only human to human spread with a particular emphasis on the fact that no other hosts are involved, therefore, not involved in pandemics. Influenza C is a mild disease. It causes seasonal episodes of influenza such as Northern infections when they happen from September to March while Southern infections happen from May to September. Due to the variation in viruses responsible for infections in these two seasons; it needs two different sets of vaccines. Influenza generally has an incubation period of 2 days, ranging from 1 to 4 days.

FDA-approved indications

  1. Prevention of Influenza A in persons aged 6 months and above
  2. Prevention of Influenza B in persons aged 6 months and above

The Centers for Disease Control and Prevention (CDC) recommends administration of an annual influenza vaccine for all persons above 6 months of age.

The vaccination is the most effective method for prevention and control of influenza. It is most effective in children greater than 2 years old and healthy adults. The efficacy of the seasonal influenza vaccine ranges between 10% and 60%. The lowest efficacy occurs when vaccine strains are not well matched to circulating strains. Both the trivalent and quadrivalent vaccines are FDA approved.

Regarding immunization in pregnancy, a randomized controlled trial conducted in South Africa has shown that when pregnant women receive the influenza vaccine, it halves their risk of developing influenza while reducing the risk of their infants (up to 24 weeks) contracting the illness.

Data shows the trivalent influenza vaccine provides protection in HIV-infected adults without severe immunosuppression while the effectiveness in HIV-infected children aged <5 years is somewhat uncertain. In certain groups, including the elderly, immune-compromised individuals and infants, the influenza vaccine is less effective, but it is beneficial by reducing the incidence of severe disease, like bronchopneumonia, and reduces hospital admission and mortality.

Mechanism of Action of Influenza Vaccines

Influenza viruses express two types of antigens; hemagglutinin (HA) and neuraminidase (NA). Influenza A virus has 18 HA, and 11 NA subtypes, and these antigens are critical for the virulence of the organism. The trimeric hemagglutinin glycoprotein acts by promoting attachment of the virus to the host cell surface resulting in infusion and thereby releasing virions into the cytoplasm.

Differently combined H and N antigens are seen in influenza A, which in turn undergo antigenic drifts and shifts resulting in antigenic variation, and thereby the necessity for vaccine strain types to vary accordingly. Antigenic drifts are genetic changes occurring in the virus due to various actions of polymerases leading to gradual antigenic changes in both HA and NA producing new variant strains. An antigenic shift takes place when the currently circulating virus disappears and gets replaced by a new subtype with novel glycoproteins to which antibodies against the previously circulating subtype do not cross-react.

The influenza vaccine conveys immunity against the influenza virus by stimulating the production of antibodies specific to the disease. Antibodies to NA act by aggregating viruses on the cell surface effectively and reducing the amount of virus released from infected cells.  Regarding the induction of immunity, the surface HA protein of the influenza virus contains two structural elements, head and stalk wherein the head is the primary target of antibodies that confer protective immunity against influenza viruses.

Flu shots offer protection against three or four strains of the flu virus. Trivalent flu vaccines provide protection against two influenza A strains, H1N1 and H3N2, and one influenza B strain. Quadrivalent flu vaccines protect against the same strains as the trivalent vaccine as well as an additional strain of influenza B.

The mechanism of immune protection is more complicated, as while primarily humoral, cell-mediated immunity also plays an essential role in immunity to influenza. After vaccination, it takes two weeks to build up an immune response against the flu. The effectiveness of a vaccine depends on several host factors such as age, underlying health status, genetic status and furthermore on antigenic matches between the vaccine and circulating viruses.

Contraindications of Influenza Vaccines

  • History of allergy or hypersensitivity to any component of the vaccine (i.e., egg protein allergy)
  • Infants less than 6 months of age
  • High fever
  • Guillain–Barre Syndrome

Administration of Influenza Vaccines

Flu shots are available in several forms:

  • Intramuscular vaccine
  • High-dose vaccine (> 65 years)
  • Intradermal vaccine (18 to 64years)
  • Egg-free vaccine (>4 years)
  • Nasal spray (2 to 49years)
  • Needle-free vaccine as a jet injector (18 to 64 years)

Dosage:

  • Age 6 months to 3 years;

0.25 – 0.5 ml: 2 doses 4 weeks apart.

  • Age 3 to 8 years:

Not previously vaccinated: 2 doses, 0.5 ml 4 weeks apart.

Vaccinated previous season; 0.5 ml one or two doses 4 weeks apart.

  • Age 9 years and above:

Single dose;  0.5 ml

Adverse Effects of Influenza Vaccines

  • Injection site reactions
  • Fever
  • Irritability
  • Drowsiness
  • Myalgia
  • Nasal spray
    • Upper respiratory symptoms
    • Fever, headache, vomiting
    • Lower respiratory symptoms

  • Rare

    • Allergic reaction
    • Urticaria/Anaphylaxis

Monitoring

CDC and FDA continuously monitor vaccine safety and will inform health officials, health care providers, and the public when necessary.

CDC uses three systems vaccine safety monitoring:

  • The Vaccine Adverse Event Reporting System (VAERS): an early warning system that helps CDC and FDA monitor problems following vaccination.  Anyone can report possible vaccine side effects to VAERS.
  • The Vaccine Safety Data link (VSD): a collaborative effort between the CDC and nine other health care organizations, which allows ongoing monitoring and proactive searches of vaccine-related data.
  • The Clinical Immunization Safety Assessment (CISA) Project: a partnership between CDC and several medical centers that conduct clinical research on vaccine-associated health risks.

Inactivated flu vaccine and pneumococcal vaccine administered at the same time may show an increased risk for febrile seizures.

Toxicity

The vaccine does not manifest any dose-dependent toxicity.

The toxicity regarding carcinogenicity and infertility have undergone extensive study and shown to be negative.

The components of the influenza vaccine are:

  • Formaldehyde used to inactivate toxins from viruses and bacteria.
  • Thimerosal safeguards against contamination, and it is only present in multi-dose vials.
  • Aluminum salts act as adjuvants and impart stronger immune response.
  • Gelatin is present as a stabilizer.
  • Antibiotics, such as gentamicin or neomycin are present in the flu vaccine to keep bacteria from growing.

Toxicity due to the components of the vaccine is not present due to the inconspicuous amounts in the vaccine.

References

ByRx Harun

Insulin Therapy – Types and Indications, Contraindications

Insulin therapy is the cornerstone of management of T1D as beta-cell dysfunction or destruction progressively leads to absolute insulin deficiency. Physiologic insulin replacement that aims to mimic normal pancreatic insulin secretion is the preferred method of treatment of T1D patients. Basal insulin is the background insulin required to suppress hepatic glucose production overnight and between meals. Prandial (bolus or meal-time) insulin replacement, provides enough insulin to dispose of glucose after eating. Such a therapeutic insulin regimen providing both basal and bolus insulin allows flexibility of dosing. Older twice-daily combination of regular and NPH regimens generally should not be used in T1D as they are less effective since the time-action profile of these two standard insulins does not readily allow for the clear separation of basal and prandial insulin action. However, it may be necessary to use such regimens in patients who cannot otherwise afford insulin. It also should be pointed out that for newly diagnosed patients with T1D, transient use of once- or twice-daily basal injections is sometimes adequate.

Types of Insulin Therapy

Principles of Management of T1DM

Management of T1D involves a multidisciplinary framework that includes the following:

  • Physiologic insulin replacement using basal-bolus therapy, either as MDI or CSII
  • Blood glucose monitoring with SMBG and/or CGM with the development of individualized A1c goals
  • Patient education
  • A supportive team of providers including endocrinologists, nurses, CDEs, psychologists, dietitians, social workers, other specialists such as cardiologists, nephrologists, psychiatrists as well as family members, social support groups, etc.

Types of Insulin Therapy

Selecting the appropriate insulin depends largely on the desired time course of insulin action.

Insulin products are categorized according to their action profiles:

  • Rapid-acting –  e.g., insulin lispro, insulin aspart, and insulin glulisine (genetically engineered insulin analogues)
  • Short-acting –  regular (soluble) insulin
  • Intermediate-acting – NPH (isophane)
  • Long-acting – e.g., insulin glargine, insulin detemir, and insulin degludec (genetically engineered insulin analogues)
  • Pre-mixed insulin
  • Inhaled insulin

A general principle to bear in mind is the longer the time to peak, the broader the peak and the longer the duration of action. Additionally, the breadth of the peak and the duration of action will be extended with increasing dose. Figures 9 and 10 should therefore be considered a conceptual representation of insulin action curves.

Rapid-Acting Insulin

  • The genetically engineered insulin analogs have a rapid onset in 15-30 minutes, peak in 30-90 minutes, and an effective duration of 4 to 5 hours when injected subcutaneously because they do not self-aggregate in solution as human (regular) insulin does. Insulin lispro differs from human insulin by an amino acid exchange of lysine and proline at positions B28 and B29. The substitution of aspartic acid for proline at position B28 characterizes insulin aspart.
  • Insulin glulisine differs from human insulin in that the B3 asparagine is replaced by lysine, and B29 lysine is replaced by glutamic acid. These modifications in the primary structure of human insulin increase the rapidity of the breakdown of insulin hexamers in the analogs and thus result in more rapid absorption. When administered before meals, rapid-acting insulins used as part of multiple daily injections or with CSII, resemble physiologic insulin increases stimulated by food. Doses can be adjusted proportionately to food consumed; in patients with gastroparesis or poor appetite, insulin can be injected halfway through or after the meal.

Short-Acting Insulin

  • Regular insulin is structurally similar to endogenous human insulin. It consists of dissolved zinc-insulin crystals which self aggregate in the subcutaneous tissue and results in a delayed onset of action of 30 to 60 minutes, a peak of 2 to 3 hours, and an effective duration of 6 to 8 hours. Proper use requires injection at least 20 to 30 minutes prior to meals to match insulin availability and carbohydrate absorption. Use of regular insulin is associated with greater hypoglycemia risk [39]. Regular insulin acts almost instantly when injected intravenously.

Intermediate-Acting Insulin

  • Neutral protamine Hagedorn (NPH) insulin, developed in the 1950s, is a combination of recombinant human insulin with protamine which results in crystal formation. When injected subcutaneously, precipitated crystals of NPH insulin are released slowly resulting in a longer duration of action compared to regular insulin.
  • The action of NPH varies quite widely within the same patient as well as between patients. Its onset of action occurs 2 to 4 hours from the time of injection, with a peak effect lasting 6 to 10 hours, and an effective duration of 10 to 16 hours. Due to this peak effect, NPH insulin acts as a basal and prandial insulin, necessitating that patients eat a meal at the time the insulin is peaking. NPH typically requires twice a day dosing [40].

Long-Acting or Basal Insulin

  • Long-acting insulin analogs were created by modifying the amino acid sequence on the beta chain of insulin [41]. They exhibit much-improved pharmacokinetics and pharmacodynamics without a peak effect and maintain a longer duration of action. Improved absorption rates result in significantly decreased inter-individual and intra-individual variability with improvement in glycemic control and reduced hypoglycemia risk.
  • Insulin glargine (U-100): Insulin glargine is modified human insulin produced by the substitution of glycine for asparagine at position A21 of the insulin molecule and by the addition of two arginine molecules at position B30. These changes result in an insulin molecule that is less soluble at the injection site forming a precipitate in the subcutaneous tissue to form a depot from which insulin is slowly released after injection and is slowly released into the circulation. It has no pronounced peak and a longer duration of action of about 20 to 24 hours in most patients, allowing for once daily dosing. In clinical practice, many patients with T1DM may benefit from twice-daily injections. Insulin glargine is solubilized in acidic pH and should not be mixed with rapid-acting insulins as the kinetics of both insulins will be altered. Insulin glargine shows a greater reduction in A1C and decreased hypoglycemia in patients with T1DM [42].

Pre-mixed insulins

  • Premixed insulins are mixtures of prandial and intermediate-acting insulins (the same prandial insulin attached to protamine so that it becomes intermediate-acting). In the US, insulin lispro protamine mixtures are available in two forms: 75% insulin lispro protamine suspension and 25% insulin lispro injection (75/25) and 50% insulin lispro protamine suspension and 50% insulin lispro injection (50/50).
  • Available preparations of insulin aspart protamine mixtures include 50/50 and 70/30 suspensions. A variety of other ratios are available in Europe. These insulins are typically administered before breakfast and dinner. This alleged twice-daily dosing is the primary advantage of these insulins. In general, use of premixed insulins restricts adjustment of doses and meal timing.
  • Therefore, premixed insulins are not recommended for adult patients with T1D, where intensive regimens with the ability to make adjustments in the premeal short-acting insulin bolus are better suited for glycemic control. Premixed insulin in T1D could have benefits for some patients who do not adhere to an intensive insulin regimen.

U-500 insulin

  • U-500 insulin is highly concentrated regular insulin, administered 2-3 times a day without basal insulin. Due to its concentration, the action is prolonged and variable. In T1D, use is primarily limited to individuals with significant insulin resistance (requiring >200 units of insulin a day). Caution should be used while prescribing this insulin as confusion may occur among clinicians, pharmacists, nurses, and patients who are unfamiliar with its use. Recently,
  • U-500 insulin became available in a pen delivery system allowing patients to administer insulin by 5 units increments up to a maximum of 300 units at a time. Units to be delivered are clearly readable through the pen “dose window” which should minimize or eliminate confusion when administering this highly concentrated insulin formulation.

Inhaled insulin

  • Currently, one form of inhaled insulin is available in the market. Afrezza was approved by the FDA in 2014. This is a drug-device combination that contains powdered human insulin in single-use dose cartridges delivered via a small inhaler. When inhaled, it dissolves immediately on contact with the alveolar surface of the lung and is rapidly absorbed into the systemic circulation, reaching a peak within 15 minutes.
  • Thus Afrezza acts similarly to rapid-acting insulin analogs but with a much faster peak of action and shorter duration of action. Prior to the initiation of its use, patients should be screened for underlying lung disease with spirometry. Follow-up spirometry is recommended after 6 months’ use, and annually thereafter.
  • The main advantages of inhaled insulin are avoidance of injections, faster onset of action, less weight gain and less hypoglycemia [50]. Dosing is not flexible as cartridges are available in fixed doses (4, 8 and 12 units). Afrezza is contraindicated in patients with chronic lung disease such as asthma or chronic obstructive pulmonary disease (COPD).

Table 1Currently Available Insulin Preparations

Insulin Preparation Onset of action (h) Peak Action (h) Effective duration of action (h) Maximum duration(h)
Rapid-acting analogues
Insulin lispro (Humalog) ¼ – ½ ½-1 ½ 3-4 4-6
Insulin aspart (NovoLog) ¼ – ½ ½ -1 ¼ 3-4 4-6
Insulin glulisine (Apidra ¼ – ½ ½ -1 ¼ 3-4 4-6
Inhaled insulin (Afrezza) seconds 12-17 min 2-3 2-3
Short-acting
Regular (soluble) ½ – 1 2-3 3-6 6-8
Intermediate-acting
NPH (isophane 2-4 6-10 10-16 14-16
Long-acting analogue
Insulin glargine (Lantus) 0.5-1.5 8-16 18-20 20-24
Insulin glargine U-300 (Toujeo) 0.5-1.5 none 24 30
Insulin detemir (Levemir) 0.5-1.5 6-8 14 ~20
Insulin degludec (Tresiba) 0.5-1.5 none 24 40

Labeled indications

  • Insulin, regular is the mainstay therapy in the management of Diabetes Mellitus type 1 and type 2 (in some cases) to improve glycemic control.

Off-Label indications

  • Use for hormonal resuscitation in cadaveric organ recovery
  • For toxicity of calcium channel blockers and beta-blockers
  • The mainstay treatment of diabetic ketoacidosis and hyperosmolar hyperglycemic state
  • Treatment of Gestational diabetes mellitus when refractory to non-pharmacologic treatment such as nutrition
  • Adjunct therapy for hyperglycemia in the critically ill

Contraindications of Insulin therapy

Regular insulin is contraindicated in patients with hypersensitivity to the drug due to the potential to cause an allergic reaction.

Side Effects of Insulin therapy

A useful and detailed way to classify the adverse effects of insulin is by separating and organizing the by organ systems:

  • Cardiovascular side effects include peripheral edema
  • Dermatologic side effects include pruritus and erythema at the injection site
  • Hypersensitivity side effects include hypersensitivity reaction and anaphylaxis
  • Local injection site adverse effects include lipoatrophy and hypertrophy
  • Endocrine and metabolic side effects include hypokalemia, weight gain, and hypoglycemia

References

ByRx Harun

Ubiquinone – Uses, Dosage, Side Effects, Interactions

Ubiquinone/Ubidecarenone also called coenzyme Q10, is a 1,4-benzoquinone. From his name (Q10), the Q refers to the constitutive quinone group, and 10 is related to the number of isoprenyl subunits in its tail. It is a powerful antioxidant, a lipid-soluble and an essential cofactor in mitochondrial oxidative phosphorylation.[rx] The ubidecarenone is the coenzyme destined for mitochondrial enzyme complexes involved in oxidative phosphorylation in the production of ATP. It is fundamental for cells that have a high metabolic demand.[rx] Ubidecarenone is sold as a dietary supplement and is not FDA approved as a drug thus, it is not meant to treat, cure or prevent any disease. FDA does not approve these dietary supplements before sold nor regulate the manufacturing process.[rx]

Coenzyme Q, also known as ubiquinone, is a coenzyme family that is ubiquitous in animals and most bacteria (hence the name ubiquinone). In humans, the most common form is Coenzyme Q10 or ubiquinone-10. CoQ10 is not approved by the U.S. Food and Drug Administration (FDA) for the treatment of any medical condition;[1 however, it is sold as a dietary supplement.

Mechanism of Action of Ubiquinone

Ubidecarenone is an essential cofactor in the mitochondrial electron transport chain. Its functions are the acceptance of electrons from the complex I and II and this activity is vital for the production of ATP. It acts as a mobile redox agent shuttling electrons and protons in the electron transport chain.[rx] Ubidecarenone also presents antioxidant activity in mitochondria and cellular membranes, protecting against peroxidation of lipid membranes as well as inhibiting the oxidation of LDL-cholesterol.[rx]

Ubidecarenone has roles in many physiological processes including sulfide oxidation, regulation of mitochondrial permeability transition pore and translocation of protons and calcium ions across biological membranes. Studies have shown its beneficial effect in treating cancer, statin myopathy, congestive heart failure and hypertension.

Indications of Ubiquinone

  • The diet supplements containing ubidecarenone are indicated, as stated in the product label, to assist individuals with cardiovascular complaints including congestive heart failure and systolic hypertension. In the product, ubidecarenone is used to increase the cardiac input as well as for the prevention of several other diseases like Parkinson, fibromyalgia, migraine, periodontal disease and diabetes, based on preclinical studies.[rx] It is important to highlight that these products are not FDA approved and it is recommended to use under discretion.
  • Migraine
  • Essential dietary elements or organic compounds that are required in only small quantities for normal physiologic processes to occur.
  • Organic substances that are required in small amounts for maintenance and growth, but which cannot be manufactured by the human body

Specific Function of Ubiquinone

  • Accessory subunit of the mitochondrial membrane respiratory chain NADH dehydrogenase (Complex I), that is believed not to be involved in catalysis. Complex I functions in the transfer of electrons from NADH to the respiratory chain. The immediate electron acceptor for the enzyme is believed to be ubiquinone.
  • Flavoprotein (FP) subunit of succinate dehydrogenase (SDH) that is involved in complex II of the mitochondrial electron transport chain and is responsible for transferring electrons from succinate to ubiquinone (coenzyme Q). It can act as a tumor suppressor.
  • A transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins.
  • Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
  • Binds LDL, the major cholesterol-carrying lipoprotein of plasma, and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clathrin-coated pits. (Microbial infection) Acts as a receptor for the hepatitis C virus in hepatocytes, but not through direct interaction with viral proteins (PubMed:10535997, PubMed:12615904). Acts as a receptor for vesicular stomatitis virus (PubMed:23589850). In the case of HIV-1 infection, it may function as a receptor for extracellular Tat in neurons, mediating its internalization in uninfected cells (PubMed:11100124).
  • Binds VLDL and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clathrin-coated pits. Binding to Reelin induces tyrosine phosphorylation of Dab1 and modulation of Tau phosphorylation (By similarity).

Contraindications of Ubiquinone

Absolute contraindications have not been identified.

  • low blood pressure
  • liver problems
  • blockage of a bile duct

Allergies

  • Vitamin E Analogues
  • Omega-3(N-3)Polyunsaturated Fatty Acids
  • Ubidecarenone (Coenzyme Q10)

Dosage of Ubiquinone

Strengths: 60 mg; 100 mg; 200 mg; 30 mg; 50 mg; 400 mg; 30 mg/5 mL; 10 mg; 30 mg/mL; 10 mg/mL; 90 mg/mL; 100 mg/mL; 90 mg; 300 mg.

Dietary Supplement

Oral: 30 to 200 mg/day

Side Effects of Ubiquinone

The Most Common 

  • Stomach upset
  • Decreased appetite
  • Diarrhea
  • Increased levels of liver enzymes in the blood
  • Nausea

Common

  • Allergies
  • Low blood pressure
  • very low blood pressure–dizziness, severe weakness, feeling like you might pass out.

Rare

  • upset stomach, nausea, vomiting, loss of appetite;
  • diarrhea;
  • skin rash; or
  • low blood pressure.

Drug Interactions of Ubiquinone

  • anisindione
  • dicumarol
  • warfarin
  • Alendronic acid
  • Atorvastatin
  • Anagliptin
  • Alogliptin
  • Baclofen
  • Canagliflozin
  • Captopril

Pregnancy Category

Information regarding safety and efficacy in pregnancy and lactation is lacking.

References

  1. https://clinicaltrials.gov/ct2/about-site/terms-conditions#Usehttps://clinicaltrials.gov/
  2. https://www.ncbi.nlm.nih.gov/mesh/68014451https://www.ncbi.nlm.nih.gov/mesh/67024989http://www.nlm.nih.gov/mesh/meshhome.htmlhttps://www.ncbi.nlm.nih.gov/mesh/68018977https://www.ncbi.nlm.nih.gov/mesh/68014815
  3. https://pubchem.ncbi.nlm.nih.gov
  4. https://www.whocc.no/atc_ddd_index/
  5. https://www.drugbank.ca/drugs/DB09270
  6. https://pubchem.ncbi.nlm.nih.gov/compound/Coenzyme-Q10
  7. https://pubchem.ncbi.nlm.nih.gov/substance/310265165
  8. https://en.wikipedia.org/wiki/Coenzyme_Q10
  9. https://www.drugs.com/international/ubidecarenone.html
  10. https://www.drugs.com/npp/ubiquinone.html
  11. https://www.medicinenet.com/coenzyme_q10_ubiquinone_ubidecarenone-oral/article.htm
  12. https://www.webmd.com/drugs/2/drug-77955/ubidecarenone
ByRx Harun

Coenzyme Q10 – Uses, Dosage, Side Effects, Interactions

Coenzyme Q10/Ubidecarenone also called coenzyme Q10, is a 1,4-benzoquinone. From his name (Q10), the Q refers to the constitutive quinone group, and 10 is related to the number of isoprenyl subunits in its tail. It is a powerful antioxidant, a lipid-soluble and an essential cofactor in mitochondrial oxidative phosphorylation.[rx] The ubidecarenone is the coenzyme destined for mitochondrial enzyme complexes involved in oxidative phosphorylation in the production of ATP. It is fundamental for cells that have a high metabolic demand.[rx] Ubidecarenone is sold as a dietary supplement and is not FDA approved as a drug thus, it is not meant to treat, cure or prevent any disease. FDA does not approve these dietary supplements before sold nor regulate the manufacturing process.[rx]

Coenzyme Q, also known as ubiquinone, is a coenzyme family that is ubiquitous in animals and most bacteria (hence the name ubiquinone). In humans, the most common form is Coenzyme Q10 or ubiquinone-10. CoQ10 is not approved by the U.S. Food and Drug Administration (FDA) for the treatment of any medical condition;[1 however, it is sold as a dietary supplement.

Mechanism of Action of Coenzyme Q10

Ubidecarenone is an essential cofactor in the mitochondrial electron transport chain. Its functions are the acceptance of electrons from the complex I and II and this activity is vital for the production of ATP. It acts as a mobile redox agent shuttling electrons and protons in the electron transport chain.[rx] Ubidecarenone also presents antioxidant activity in mitochondria and cellular membranes, protecting against peroxidation of lipid membranes as well as inhibiting the oxidation of LDL-cholesterol.[rx]

Ubidecarenone has roles in many physiological processes including sulfide oxidation, regulation of mitochondrial permeability transition pore and translocation of protons and calcium ions across biological membranes. Studies have shown its beneficial effect in treating cancer, statin myopathy, congestive heart failure and hypertension.

Indications of Coenzyme Q10

  • The diet supplements containing ubidecarenone are indicated, as stated in the product label, to assist individuals with cardiovascular complaints including congestive heart failure and systolic hypertension. In the product, ubidecarenone is used to increase the cardiac input as well as for the prevention of several other diseases like Parkinson, fibromyalgia, migraine, periodontal disease and diabetes, based on preclinical studies.[rx] It is important to highlight that these products are not FDA approved and it is recommended to use under discretion.
  • Migraine
  • Essential dietary elements or organic compounds that are required in only small quantities for normal physiologic processes to occur.
  • Organic substances that are required in small amounts for maintenance and growth, but which cannot be manufactured by the human body

Specific Function

  • Accessory subunit of the mitochondrial membrane respiratory chain NADH dehydrogenase (Complex I), that is believed not to be involved in catalysis. Complex I functions in the transfer of electrons from NADH to the respiratory chain. The immediate electron acceptor for the enzyme is believed to be ubiquinone.
  • Flavoprotein (FP) subunit of succinate dehydrogenase (SDH) that is involved in complex II of the mitochondrial electron transport chain and is responsible for transferring electrons from succinate to ubiquinone (coenzyme Q). It can act as a tumor suppressor.
  • A transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins.
  • Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
  • Binds LDL, the major cholesterol-carrying lipoprotein of plasma, and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clathrin-coated pits. (Microbial infection) Acts as a receptor for the hepatitis C virus in hepatocytes, but not through direct interaction with viral proteins (PubMed:10535997, PubMed:12615904). Acts as a receptor for vesicular stomatitis virus (PubMed:23589850). In the case of HIV-1 infection, it may function as a receptor for extracellular Tat in neurons, mediating its internalization in uninfected cells (PubMed:11100124).
  • Binds VLDL and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clathrin-coated pits. Binding to Reelin induces tyrosine phosphorylation of Dab1 and modulation of Tau phosphorylation (By similarity).

Contraindications

Absolute contraindications have not been identified.

  • low blood pressure
  • liver problems
  • blockage of a bile duct

Allergies

  • Vitamin E Analogues
  • Omega-3(N-3)Polyunsaturated Fatty Acids
  • Ubidecarenone (Coenzyme Q10)

Dosage of 

Strengths: 60 mg; 100 mg; 200 mg; 30 mg; 50 mg; 400 mg; 30 mg/5 mL; 10 mg; 30 mg/mL; 10 mg/mL; 90 mg/mL; 100 mg/mL; 90 mg; 300 mg.

Dietary Supplement

Oral: 30 to 200 mg/day

Side Effects

The Most Common 

  • Stomach upset
  • Decreased appetite
  • Diarrhea
  • Increased levels of liver enzymes in the blood
  • Nausea

Common

  • Allergies
  • Low blood pressure
  • very low blood pressure–dizziness, severe weakness, feeling like you might pass out.

Rare

  • upset stomach, nausea, vomiting, loss of appetite;
  • diarrhea;
  • skin rash; or
  • low blood pressure.

Drug Interactions

  • anisindione
  • dicumarol
  • warfarin
  • Alendronic acid
  • Atorvastatin
  • Anagliptin
  • Alogliptin
  • Baclofen
  • Canagliflozin
  • Captopril

Pregnancy Category

Information regarding safety and efficacy in pregnancy and lactation is lacking.

References

  1. https://clinicaltrials.gov/ct2/about-site/terms-conditions#Usehttps://clinicaltrials.gov/
  2. https://www.ncbi.nlm.nih.gov/mesh/68014451https://www.ncbi.nlm.nih.gov/mesh/67024989http://www.nlm.nih.gov/mesh/meshhome.htmlhttps://www.ncbi.nlm.nih.gov/mesh/68018977https://www.ncbi.nlm.nih.gov/mesh/68014815
  3. https://pubchem.ncbi.nlm.nih.gov
  4. https://www.whocc.no/atc_ddd_index/
  5. https://www.drugbank.ca/drugs/DB09270
  6. https://pubchem.ncbi.nlm.nih.gov/compound/Coenzyme-Q10
  7. https://pubchem.ncbi.nlm.nih.gov/substance/310265165
  8. https://en.wikipedia.org/wiki/Coenzyme_Q10
  9. https://www.drugs.com/international/ubidecarenone.html
  10. https://www.drugs.com/npp/ubiquinone.html
  11. https://www.medicinenet.com/coenzyme_q10_ubiquinone_ubidecarenone-oral/article.htm
  12. https://www.webmd.com/drugs/2/drug-77955/ubidecarenone
ByRx Harun

Ubidecarenone – Uses, Dosage, Side Effects, Interactions

Ubidecarenone also called coenzyme Q10, is a 1,4-benzoquinone. From his name (Q10), the Q refers to the constitutive quinone group, and 10 is related to the number of isoprenyl subunits in its tail. It is a powerful antioxidant, a lipid-soluble and an essential cofactor in mitochondrial oxidative phosphorylation.[rx] The ubidecarenone is the coenzyme destined for mitochondrial enzyme complexes involved in oxidative phosphorylation in the production of ATP. It is fundamental for cells that have a high metabolic demand.[rx] Ubidecarenone is sold as a dietary supplement and is not FDA approved as a drug thus, it is not meant to treat, cure or prevent any disease. FDA does not approve these dietary supplements before sold nor regulate the manufacturing process.[rx]

Coenzyme Q, also known as ubiquinone, is a coenzyme family that is ubiquitous in animals and most bacteria (hence the name ubiquinone). In humans, the most common form is Coenzyme Q10 or ubiquinone-10. CoQ10 is not approved by the U.S. Food and Drug Administration (FDA) for the treatment of any medical condition;[1 however, it is sold as a dietary supplement.

Mechanism of Action

Ubidecarenone is an essential cofactor in the mitochondrial electron transport chain. Its functions are the acceptance of electrons from the complex I and II and this activity is vital for the production of ATP. It acts as a mobile redox agent shuttling electrons and protons in the electron transport chain.[rx] Ubidecarenone also presents antioxidant activity in mitochondria and cellular membranes, protecting against peroxidation of lipid membranes as well as inhibiting the oxidation of LDL-cholesterol.[rx]

Ubidecarenone has roles in many physiological processes including sulfide oxidation, regulation of mitochondrial permeability transition pore and translocation of protons and calcium ions across biological membranes. Studies have shown its beneficial effect in treating cancer, statin myopathy, congestive heart failure and hypertension.

Indications

  • The diet supplements containing ubidecarenone are indicated, as stated in the product label, to assist individuals with cardiovascular complaints including congestive heart failure and systolic hypertension. In the product, ubidecarenone is used to increase the cardiac input as well as for the prevention of several other diseases like Parkinson, fibromyalgia, migraine, periodontal disease and diabetes, based on preclinical studies.[rx] It is important to highlight that these products are not FDA approved and it is recommended to use under discretion.
  • Migraine
  • Essential dietary elements or organic compounds that are required in only small quantities for normal physiologic processes to occur.
  • Organic substances that are required in small amounts for maintenance and growth, but which cannot be manufactured by the human body

Specific Function

  • Accessory subunit of the mitochondrial membrane respiratory chain NADH dehydrogenase (Complex I), that is believed not to be involved in catalysis. Complex I functions in the transfer of electrons from NADH to the respiratory chain. The immediate electron acceptor for the enzyme is believed to be ubiquinone.
  • Flavoprotein (FP) subunit of succinate dehydrogenase (SDH) that is involved in complex II of the mitochondrial electron transport chain and is responsible for transferring electrons from succinate to ubiquinone (coenzyme Q). It can act as a tumor suppressor.
  • A transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins.
  • Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
  • Binds LDL, the major cholesterol-carrying lipoprotein of plasma, and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clathrin-coated pits. (Microbial infection) Acts as a receptor for the hepatitis C virus in hepatocytes, but not through direct interaction with viral proteins (PubMed:10535997, PubMed:12615904). Acts as a receptor for vesicular stomatitis virus (PubMed:23589850). In the case of HIV-1 infection, it may function as a receptor for extracellular Tat in neurons, mediating its internalization in uninfected cells (PubMed:11100124).
  • Binds VLDL and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clathrin-coated pits. Binding to Reelin induces tyrosine phosphorylation of Dab1 and modulation of Tau phosphorylation (By similarity).

Contraindications

Absolute contraindications have not been identified.

  • low blood pressure
  • liver problems
  • blockage of a bile duct

Allergies

  • Vitamin E Analogues
  • Omega-3(N-3)Polyunsaturated Fatty Acids
  • Ubidecarenone (Coenzyme Q10)

Dosage of 

Strengths: 60 mg; 100 mg; 200 mg; 30 mg; 50 mg; 400 mg; 30 mg/5 mL; 10 mg; 30 mg/mL; 10 mg/mL; 90 mg/mL; 100 mg/mL; 90 mg; 300 mg.

Dietary Supplement

Oral: 30 to 200 mg/day

Side Effects

The Most Common 

  • Stomach upset
  • Decreased appetite
  • Diarrhea
  • Increased levels of liver enzymes in the blood
  • Nausea

Common

  • Allergies
  • Low blood pressure
  • very low blood pressure–dizziness, severe weakness, feeling like you might pass out.

Rare

  • upset stomach, nausea, vomiting, loss of appetite;
  • diarrhea;
  • skin rash; or
  • low blood pressure.

Drug Interactions

Pregnancy Category

Information regarding safety and efficacy in pregnancy and lactation is lacking.

References

  1. https://clinicaltrials.gov/ct2/about-site/terms-conditions#Usehttps://clinicaltrials.gov/
  2. https://www.ncbi.nlm.nih.gov/mesh/68014451https://www.ncbi.nlm.nih.gov/mesh/67024989http://www.nlm.nih.gov/mesh/meshhome.htmlhttps://www.ncbi.nlm.nih.gov/mesh/68018977https://www.ncbi.nlm.nih.gov/mesh/68014815
  3. https://pubchem.ncbi.nlm.nih.gov
  4. https://www.whocc.no/atc_ddd_index/
  5. https://www.drugbank.ca/drugs/DB09270
  6. https://pubchem.ncbi.nlm.nih.gov/compound/Coenzyme-Q10
  7. https://pubchem.ncbi.nlm.nih.gov/substance/310265165
  8. https://en.wikipedia.org/wiki/Coenzyme_Q10
  9. https://www.drugs.com/international/ubidecarenone.html
  10. https://www.drugs.com/npp/ubiquinone.html
  11. https://www.medicinenet.com/coenzyme_q10_ubiquinone_ubidecarenone-oral/article.htm
  12. https://www.webmd.com/drugs/2/drug-77955/ubidecarenone
ByRx Harun

Selumetinib – Shrinks Tumors, Provides Clinical Benefit NF1

Selumetinib/Findings from a phase 2 clinical trial show that the drug selumetinib improves outcomes for children with the genetic disorder neurofibromatosis type 1 (NF1). In the trial, selumetinib shrank the inoperable tumors that develop with NF1 called plexiform neurofibromas, and children experienced reduced pain, improved function, and better overall quality of life after receiving the treatment.

The trial was led by intramural researchers in the Center for Cancer Research (CCR) at the National Cancer Institute (NCI), part of the National Institutes of Health. Results of the trial were published March 18, 2020, in the New England Journal of Medicine.

“Until now, no effective medical therapies have existed for children with NF1 and plexiform neurofibromas, and it’s been a long journey to find a drug that can help them,” said Brigitte Widemann, M.D., lead author of the study, and chief of CCR’s Pediatric Oncology Branch, which developed and coordinated the trial. “While this is not yet a cure, this treatment is shrinking tumors and it’s making children feel better and have a better quality of life.”

The trial was sponsored by the NCI Cancer Therapy Evaluation Program (CTEP) and conducted by the NIH intramural program. Drugmaker AstraZeneca provided the study drug under a Cooperative Research and Development Agreement with NCI and supported correlated studies that were part of the trial. The company worked closely with the researchers on the New Drug Application to gather the data that has been submitted by the company to the U.S. Food and Drug Administration (FDA). In addition, the Neurofibromatosis Therapeutic Acceleration Program (NTAP) provided funding to support patient enrollment at participating sites.

The trial enrolled 50 children ages 3 to 17 years with NF1-related plexiform neurofibromas in 2015 and 2016. The most common symptoms from the tumors were disfigurement, limitations on strength and range of motion, and pain. The children received selumetinib orally twice a day in 28-day cycles continuously, and assessments were performed at least every four cycles. The researchers used a novel approach to assess outcomes tailored to each patient’s specific tumor-related symptoms, something no prior clinical trial directed at NF1 neurofibromas had done before.

Dr. Brigitte Widemann with Travis Carpenter, who received selumetinib for NF1 at NIH.

As of March 2019, 35 children, or 70%, had a confirmed partial response (≥ 20% volumetric tumor shrinkage), and most of them maintained that response for more than a year. After a year on the treatment, children and parents reported lower levels of pain and clinically meaningful improvement in interference of pain in daily function, overall quality of life, strength, and range of motion.

“One of the most surprising findings of this trial was the impact the treatment had on pain,” said Andrea M. Gross, M.D., of CCR, first author of the study. “It even helped patients who had been living with chronic, debilitating pain come off pain medications, which was not something we anticipated. So that was a really exciting finding.”

Five children stopped receiving selumetinib because of side effects possibly related to the drug, and six children had disease progression. The most frequent side effects included nausea and vomiting, diarrhea, and rashes.

The new study confirmed results of an earlier phase 1 trial that demonstrated for the first time that the drug could shrink large tumors. Dr. Widemann and her team have been studying selumetinib for NF1 since 2011. The drug works by blocking a protein called MEK that is part of the RAS signaling pathway, which is overly active in patients with NF1, leading to the growth of tumors. FDA granted orphan drug designation to selumetinib for the treatment of NF1 in 2018, and in 2019, the drug received FDA breakthrough therapy designation.

Plexiform neurofibromas have proven hard to treat. The tumors can grow quickly and become very large—up to 20% of a child’s body weight. Surgery to remove the tumors is often not feasible because the tumors can be intertwined with healthy nerves and tissue. Tumors that have been partially removed by surgery also tend to grow back, especially in young children.

Dr. Widemann had been doing trials with different medications for NF1 since 2001 and was excited when she saw the first tumors shrink. She and her team are grateful to the many different groups and programs that have worked together to reach this point, including the NCI intramural and extramural programs, NTAP, and the Children’s Tumor Foundation, all of which she said made this work possible. Most of all, however, the researchers want to thank the children and families who participated in the trial.

“There’s a lot more to be done. Even though these children have tumor shrinkage, many still have disabling tumors,” Dr. Widemann said. “But these findings are a big step forward and inspire us to work even harder towards additional progress in NF1 therapies.”

The trial was conducted at the NIH Clinical Center in Bethesda, Maryland, as well as three participating sites: Children’s Hospital of Philadelphia, Cincinnati Children’s Hospital Medical Center, and Children’s National Hospital in Washington, D.C. Both the Children’s Hospital of Philadelphia and Cincinnati Children’s Hospital received additional funding for the trial from NTAP.

About the National Cancer Institute (NCI): NCI leads the National Cancer Program and NIH’s efforts to dramatically reduce the prevalence of cancer and improve the lives of cancer patients and their families, through research into prevention and cancer biology, the development of new interventions, and the training and mentoring of new researchers. For more information about cancer, please visit the NCI website at cancer.gov or call NCI’s contact center, the Cancer Information Service, at 1-800-4-CANCER (1-800-422-6237).

About the National Institutes of Health (NIH): NIH, the nation’s medical research agency, includes 27 Institutes and Centers and is a component of the U.S. Department of Health and Human Services. NIH is the primary federal agency conducting and supporting basic, clinical, and translational medical research, and is investigating the causes, treatments, and cures for both common and rare diseases. For more information about NIH and its programs, visit www.nih.gov.

ByRx Harun

Bioflavonoid – Uses, Dosage, Side Effects, Interactions

Bioflavonoid /Hesperidin is a disaccharide derivative that consists of hesperetin substituted by a 6-O-(alpha-L-rhamnopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage. It has a role as a mutagen. It is a disaccharide derivative, a member of 3′-hydroxyflavanones, a dihydroxyflavanone, a monomethoxyflavanone, a flavanone glycoside, a member of 4′-methoxyflavanones and a rutinoside. It derives from a hesperetin.

Hesperidin is an abundant and inexpensive by-product of Citrus cultivation and is the major flavonoid in sweet orange and lemon. In young immature oranges, it can account for up to 14% of the fresh weight of the fruit. Hesperidin is an abundant and inexpensive by-product of Citrus cultivation and is the major flavonoid in sweet orange and lemon. In young immature oranges, it can account for up to 14% of the fresh weight of the fruit due to vitamin C deficiency such as bruising due to capillary fragility was found in early studies to be relieved by crude vitamin C extract but not by purified vitamin C. The bioflavonoids, formerly called “vitamin P“, were found to be the essential components in correcting this bruising tendency and improving the permeability and integrity of the capillary lining. These bioflavonoids include hesperidin, citrin, rutin, flavones, flavonols, catechin, and quercetin. Of historical importance is the observation that “citrin”, a mixture of two flavonoids, eriodictyol, and hesperidin, was considered to possess a vitamin-like activity, as early as in 1949. Hesperidin deficiency has since been linked with abnormal capillary leakiness as well as pain in the extremities causing aches, weakness and night leg cramps. Supplemental hesperidin also helps in reducing edema or excess swelling in the legs due to fluid accumulation. As with other bioflavonoids, hesperidin works best when administered concomitantly with vitamin C. No signs of toxicity have been observed with normal intake of hesperidin. Hesperidin was first discovered in 1827, by Lebreton, but not in a pure state and has been under continuous investigation since then (PMID: 11746857).

Another Name

  • (S)-(−)-hesperidin
  • Cirantin
  • Ciratin
  • Hesperetin 7-O-rutinoside
  • Hesperidin
  • Hesperidina
  • Hesperidoside
  • Bioflavonoid,
  • Bioflavonoid Complex,
  • Bioflavonoid Concentrate,
  • Bioflavonoid Extract,
  • Bioflavonoide,
  • Bioflavonoide d Agrume,
  • Bioflavonoïdes d’Agrumes,
  • Citrus Bioflavones,
  • Citrus Bioflavonoid,
  • Citrus Bioflavonoids,
  • Citrus Bioflavonoid Extract,
  • Citrus Flavones,
  • Citrus Flavonoids,
  • Complexe de Bioflavonoides,
  • Concentré de Bioflavonoides,
  • Extrait de Bioflavonoïdes,
  • Extrait de Bioflavonoides d’Agrumes,
  • Flavonoid,
  • Flavonoïde, Hesperidin Methyl Chalcone,
  • Hesperidina, Hesperidine, Trimethylhesperidin-chalcon


Mechanism of Action of Bioflavonoid

Hesperetin reduces or inhibits the activity of acyl-coenzyme A cholesterol acyltransferase genes (ACAT1 and ACAT2) and it reduces microsomal triglyceride transfer protein (MTP) activity. Hesperetin also seems to upregulate the LDL receptor. This leads to the reduced assembly and secretion of apoB-containing lipoproteins and enhanced reuptake of those lipoproteins, thereby lowering cholesterol levels. Hesperetin is a cholesterol-lowering flavonoid found in a number of citrus juices. It appears to reduce cholesteryl ester mass and inhibit apoB secretion by up to 80%. Hesperetin may have antioxidant, anti-inflammatory, anti-allergic, hypolipidemic, vasoprotective and anticarcinogenic actions.

Indications of Bioflavonoid

  • For lowering cholesterol  – and, possibly, otherwise favorably affecting lipids. In vitro research also suggests the possibility that hesperetin might have some anticancer effects and that it might have some anti-aromatase activity, as well as an activity again.
  • Beneficial effects on blood vessels – It’s touted as a natural remedy for a number of health problems, including allergies, hemorrhoids, high blood pressure, hot flashes, hay fever, sinusitis, symptoms associated with menopausal changes, premenstrual syndrome, and varicose veins. Hesperidin is also said to improve circulation, reduce inflammation, and help fight cancer.
  • Poor circulation can cause the legs to swell (chronic venous insufficiency or CVI) – Taking a particular product containing hesperidin methyl chalcone, butcher’s broom, and vitamin C by mouth seems to relieve the symptoms of poor circulation in the legs. Also, taking a different product containing hesperidin and diosmin by mouth for 2-6 months seems to improve CVI symptoms, although taking the drug Venoruton might be more effective for treating this condition.
  • Hemorrhoids – Some research suggests that taking hesperidin and diosmin improves symptoms of anal hemorrhoids. It may also prevent hemorrhoids from coming back after they have healed and may help in an emergency worsening of hemorrhoids.
  • Leg sores caused by weak blood circulation (venous leg ulcer) – Taking a specific product containing hesperidin and diosmin by mouth for 2 months seems to improve the healing of small venous stasis ulcers when used along with compression dressings.
  • High cholesterol – Some research shows that taking hesperidin does not affect cholesterol.
  • Obesity – Some research shows that taking glucosyl hesperidin for 12 weeks does not reduce body weight in people that are modestly overweight.
  • Diabetes – Early research suggests that taking one tablet of a specific product containing hesperidin and diosmin by mouth for 45 days decreases blood sugar levels and improves blood sugar control in women with type 2 diabetes. Other research suggests that taking hesperidin each day might lower blood pressure by a small amount in people with diabetes.
  • High blood pressure – Early research suggests that taking hesperidin by mouth or drinking orange juice containing hesperidin can decrease diastolic blood pressure (the bottom number) but does not decrease systolic blood pressure (the top number) in people with or without high blood pressure.
  • Swelling in the arms or legs caused by damage to the lymph system (lymphedema) – Early research suggests that taking a specific product containing butcher’s broom root extract, hesperidin methyl chalcone, and vitamin C by mouth for 90 days reduces swelling in the upper arm and forearm and improves mobility and heaviness in women with swelling of the arm after breast cancer treatment. However, other research shows that taking a different product containing hesperidin and diosmin by mouth does not reduce arm swelling in women following breast cancer surgery.
  • Rheumatoid arthritis (RA) – Early research suggests that drinking a beverage containing alpha-glucosyl hesperidin for 12 weeks improves symptoms of RA.
  • Varicose veins

Contraindications of Bioflavonoid

  • a high amount of oxalic acid in the urine
  • iron metabolism disorder causing increased iron storage
  • sickle cell anemia
  • anemia from pyruvate kinase and G6PD deficiencies

Allergies

  • Ascorbic Acid (Vitamin C)
  • Rutin Analogues
  • Hesperidin

Side Effects Of Bioflavonoid

The most common

Common

  • unusual bruising,
  • unexplainable bruises
  • bruises that grow in size
  • nosebleeds
  • bleeding gums
  • bleeding from cuts that take a long time to stop
  • heavier than normal menstrual or vaginal bleeding
  • pink or brown urine
  • red or black stools
  • coughing up blood
  • vomiting blood

Less common

Dosage of Bioflavonoid

The following doses have been studied in scientific research

BY MOUTH

  • For poor circulation that can cause the legs to swell (chronic venous insufficiency or CVI) – A specific combination product containing hesperidin methyl chalcone 150 mg, butcher’s broom root extract 150 mg, and ascorbic acid 100 mg has been used. Also, a combination of 100-150 mg of hesperidin with 900-1350 mg of diosmin taken daily for 2-6 months has been used.
  • For hemorrhoids – A combination of 150 mg of hesperidin plus 1350 mg of diosmin twice daily for 4 days, followed by 100 mg of hesperidin and 900 mg of diosmin twice daily for 3 days has been used. Also, a combination of 50 mg of hesperidin plus 450 mg of diosmin twice daily for 3 months has been used to prevent the return of hemorrhoids.
  • For sores caused by weak blood circulation (venous leg ulcer) – A combination of 100 mg of hesperidin and 900 mg of diosmin daily for up to 2 months has been used.

Drug Interactions of Bioflavonoid

Hesperidin might decrease blood pressure. Taking hesperidin along with medications used to lower high blood pressure might cause your blood pressure to go too low.

  • nifedipine (Adalat, Procardia), verapamil (Calan, Isoptin, Verelan), diltiazem (Cardizem), isradipine (DynaCirc), felodipine (Plendil), amlodipine (Norvasc), and others.
  • etoposide, paclitaxel, vinblastine, vincristine, vindesine, ketoconazole, itraconazole, amprenavir, indinavir, nelfinavir, saquinavir, cimetidine, ranitidine, diltiazem, verapamil, corticosteroids, erythromycin, cisapride (Propulsid), fexofenadine (Allegra), cyclosporine, loperamide (Imodium), quinidine, and others.
  • aspirin, clopidogrel (Plavix), diclofenac (Voltaren, Cataflam, others), ibuprofen (Advil, Motrin, others), naproxen (Anaprox, Naprosyn, others), dalteparin (Fragmin), enoxaparin (Lovenox), heparin, warfarin (Coumadin), and others.
  • include alprazolam (Xanax), clonazepam (Klonopin), diazepam (Valium), lorazepam (Ativan), midazolam (Versed), temazepam (Restoril), triazolam (Halcion), and others.
  • pentobarbital (Nembutal), phenobarbital (Luminal), secobarbital (Seconal), thiopental (Pentothal), fentanyl (Duragesic, Sublimaze), morphine, propofol (Diprivan), and others.

Pregnancy Category of Bioflavonoid

Pregnancy and breast-feeding

  • Hesperidin is POSSIBLY SAFE for pregnant or breast-feeding women when taken by mouth with diosmin.

Bleeding disorder

Hesperidin might slow blood clotting and increase the risk of bleeding. In theory, hesperidin might make bleeding disorders worse.  Hesperidin might lower blood pressure. In theory, taking hesperidin might make blood pressure become too low in people who already have low blood pressure. Hesperidin might prolong bleeding. There is concern that hesperidin might increase the risk of bleeding during and after surgical procedures. Stop taking hesperidin at least 2 weeks before a scheduled surgery.

References

ByRx Harun

Daflon – Uses, Dosage , Side Effects

Daflon/Diosmin is a disaccharide derivative that consists of diosmetin substituted by a 6-O-(alpha-L-rhamnopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage. It has a role as an antioxidant and an anti-inflammatory agent. It is a glycosyloxyflavone, a rutinoside, a disaccharide derivative, a monomethoxyflavone, and a dihydroxyflavanone. It derives from a diosmetin.

Diosmin is a semisynthetic drug indicated for the treatment of venous disease. Diosmin is a flavone that can be found in the plant Teucrium gnaphalodes. Diosmin is available as prescription medicine in several European countries and is available as a nutritional supplement in the United States and the rest of Europe. It should be noted that clinical studies have been inconclusive and no articles have been published pertaining to its use in the treatment of vascular disease. When used in rats, diosmin has been effective at mitigating hyperglycemia, and may also have antineutrino degenerative properties.

Another Name

  • Barosmin
  • Buchu Resin
  • Daflon
  • Diosmin
  • Resin, Buchu
  • Venosmine
  • Diosmin
  • Diosmina
  • Diosmine
  • Diosminum

Mechanism of Action of Diosmin

Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phases I and II xenobiotic chemical metabolizing enzyme gene. Diosmin is a semisynthetic drug indicated for the treatment of venous disease. Diosmin is a flavone that can be found in the plant Teucrium gnaphalodes. Diosmin is available as prescription medicine in several European countries and is available as a nutritional supplement in the United States and the rest of Europe. It should be noted that clinical studies have been inconclusive and no articles have been published pertaining to its use in the treatment of vascular disease. When used in rats, diosmin has been effective at mitigating hyperglycemia, and may also have antineutrino degenerative properties.

Indications of Diosmin

  • Venous Insufficiency – general or unspecified but usually of the legs; coordinate IM with the specific vein (IM) or organ /‌blood supply (IM) if pertinent cope NoteImpaired venous blood flow or venous return (venous stasis), usually caused by inadequate venous valves. Venous insufficiency often occurs in the legs, and is associated with EDEMA and sometimes with VENOUS STASIS ULCERS at the ankle.
  • Hemorrhoidal; hemorrhoidal disease; hemorrhoids – Swollen veins in the lower part of the RECTUM or ANUS. Hemorrhoids can be inside the anus (internal), under the skin around the anus (external), or protruding from inside to outside of the anus. People with hemorrhoids may or may not exhibit symptoms that include bleeding, itching, and pain.\
  • Edema – general prefer specifics; coordinate IM with organ/diseases term (IM); egg-white edema: coordinate IM with OVALBUMIN (NIM if indexed at all); EPH (Edema, Proteinuria, Hypertension)  gestosis, EPH & do not index under EDEMA unless it is particularly discussedScope NoteAbnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.
  • Diosmin is a dietary supplement – used to aid the treatment of hemorrhoids and venous diseases, i.e., chronic venous insufficiency including spider and varicose veins, leg swelling (edema), stasis dermatitis and venous ulcers. The mechanism of action of Diosmin and other phlebotomists is undefined, and clinical evidence of benefit is limited. Diosmin is not recommended for treating the rectal mucosa, skin irritations, or wounds, and should not be used to treat dermatitis, eczema, or urticaria. Diosmin is not recommended for use in children or women during pregnancy.[rx]
  • Chronic venous insufficiency
  • Diabetes
  • Hemorrhoids
  • High blood pressure
  • Lymphedema (swelling of the arms)
  • Premenstrual syndrome
  • Ulcerative colitis
  • Varicose veins

Contraindications of Diosmin

The gel formulation is contraindicated for application to mucosa, dermal irritations, or wounds, and it should not be used to treat dermatitis, eczema, or urticaria. Diosmin is not recommended for use in children.

Dosage of Diosmin

For venous insufficiency, the dosage is 2 tablets daily. For acute hemorrhoidal attack, the dosage is 6 tablets daily for 4 days, followed by 4 tablets daily over the next 3 days.[rx] For chronic venous disease, the dosage is 2 tablets a day for at least 2 months.[rx]

BY MOUTH

  • For the treatment of internal hemorrhoids – 1350 mg of diosmin plus 150 mg of hesperidin twice daily for 4 days followed by 900 mg of diosmin and 100 mg of hesperidin twice daily for 3 days. Some researchers also try 600 mg of diosmin three times daily for 4 days, followed by 300 mg twice daily for 10 days, in combination with 11 grams of psyllium daily. However, this lower diosmin dose does not seem to be as effective.
  • For prevention of relapse internal hemorrhoids – 450 mg of diosmin plus 50 mg of hesperidin twice daily for 3 months of therapy.
  • For the treatment of leg wounds due to blood flow problems (venous stasis ulcers) – the combination of 900 mg of diosmin and 100 mg of hesperidin daily has been used for up to 2 months.

Side Effects of Diosmin

Diosmin is safe for most people when used short-term for up to 6 months. It can cause some side effects such as stomach and abdominal pain, diarrhea, dizziness, headache, skin redness and hives, muscle pain, blood problems, and altered heart rate.

In some 10% of users, diosmin causes mild gastrointestinal disorders or skin irritations (hives, itching), stomach pain, nausea, heart arrhythmias, or anemia.[rx] Preliminary research indicates no evidence of toxicity.[rx] The US Food and Drug Administration (FDA) concluded in 2001 that there was inadequate evidence on which to base an expectation of safety. As of 2013, the FDA did not revise this position.[rx]

Drug Interactions of Diosmin

We currently have no information about DIOSMIN Interactions.

Pregnancy Category of Diosmin

Pregnancy and breast-feeding

  • Not enough is known about the use of diosmin during pregnancy and breast-feeding. Stay on the safe side and avoid use.

Bleeding disorders

  • Diosmin might make bleeding disorders worse. If you have a bleeding disorder, don’t use diosmin.

References

ByRx Harun

Barosmin – Uses, Dosage, Side Effects

Barosmin/Diosmin is a disaccharide derivative that consists of diosmetin substituted by a 6-O-(alpha-L-rhamnopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage. It has a role as an antioxidant and an anti-inflammatory agent. It is a glycosyloxyflavone, a rutinoside, a disaccharide derivative, a monomethoxyflavone, and a dihydroxyflavanone. It derives from a diosmetin.

Diosmin is a semisynthetic drug indicated for the treatment of venous disease. Diosmin is a flavone that can be found in the plant Teucrium gnaphalodes. Diosmin is available as prescription medicine in several European countries and is available as a nutritional supplement in the United States and the rest of Europe. It should be noted that clinical studies have been inconclusive and no articles have been published pertaining to its use in the treatment of vascular disease. When used in rats, diosmin has been effective at mitigating hyperglycemia, and may also have antineutrino degenerative properties.

Another Name

  • Barosmin
  • Buchu Resin
  • Daflon
  • Diosmin
  • Resin, Buchu
  • Venosmine
  • Diosmin
  • Diosmina
  • Diosmine
  • Diosminum

Mechanism of Action of Diosmin

Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phases I and II xenobiotic chemical metabolizing enzyme gene. Diosmin is a semisynthetic drug indicated for the treatment of venous disease. Diosmin is a flavone that can be found in the plant Teucrium gnaphalodes. Diosmin is available as prescription medicine in several European countries and is available as a nutritional supplement in the United States and the rest of Europe. It should be noted that clinical studies have been inconclusive and no articles have been published pertaining to its use in the treatment of vascular disease. When used in rats, diosmin has been effective at mitigating hyperglycemia, and may also have antineutrino degenerative properties.

Indications of Diosmin

  • Venous Insufficiency – general or unspecified but usually of the legs; coordinate IM with the specific vein (IM) or organ /‌blood supply (IM) if pertinent cope NoteImpaired venous blood flow or venous return (venous stasis), usually caused by inadequate venous valves. Venous insufficiency often occurs in the legs, and is associated with EDEMA and sometimes with VENOUS STASIS ULCERS at the ankle.
  • Hemorrhoidal; hemorrhoidal disease; hemorrhoids – Swollen veins in the lower part of the RECTUM or ANUS. Hemorrhoids can be inside the anus (internal), under the skin around the anus (external), or protruding from inside to outside of the anus. People with hemorrhoids may or may not exhibit symptoms that include bleeding, itching, and pain.\
  • Edema – general prefer specifics; coordinate IM with organ/diseases term (IM); egg-white edema: coordinate IM with OVALBUMIN (NIM if indexed at all); EPH (Edema, Proteinuria, Hypertension)  gestosis, EPH & do not index under EDEMA unless it is particularly discussedScope NoteAbnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.
  • Diosmin is a dietary supplement – used to aid the treatment of hemorrhoids and venous diseases, i.e., chronic venous insufficiency including spider and varicose veins, leg swelling (edema), stasis dermatitis and venous ulcers. The mechanism of action of Diosmin and other phlebotomists is undefined, and clinical evidence of benefit is limited. Diosmin is not recommended for treating the rectal mucosa, skin irritations, or wounds, and should not be used to treat dermatitis, eczema, or urticaria. Diosmin is not recommended for use in children or women during pregnancy.[rx]
  • Chronic venous insufficiency
  • Diabetes
  • Hemorrhoids
  • High blood pressure
  • Lymphedema (swelling of the arms)
  • Premenstrual syndrome
  • Ulcerative colitis
  • Varicose veins

Contraindications of Diosmin

The gel formulation is contraindicated for application to mucosa, dermal irritations, or wounds, and it should not be used to treat dermatitis, eczema, or urticaria. Diosmin is not recommended for use in children.

Dosage of Diosmin

For venous insufficiency, the dosage is 2 tablets daily. For acute hemorrhoidal attack, the dosage is 6 tablets daily for 4 days, followed by 4 tablets daily over the next 3 days.[rx] For chronic venous disease, the dosage is 2 tablets a day for at least 2 months.[rx]

BY MOUTH

  • For the treatment of internal hemorrhoids – 1350 mg of diosmin plus 150 mg of hesperidin twice daily for 4 days followed by 900 mg of diosmin and 100 mg of hesperidin twice daily for 3 days. Some researchers also try 600 mg of diosmin three times daily for 4 days, followed by 300 mg twice daily for 10 days, in combination with 11 grams of psyllium daily. However, this lower diosmin dose does not seem to be as effective.
  • For prevention of relapse internal hemorrhoids – 450 mg of diosmin plus 50 mg of hesperidin twice daily for 3 months of therapy.
  • For the treatment of leg wounds due to blood flow problems (venous stasis ulcers) – the combination of 900 mg of diosmin and 100 mg of hesperidin daily has been used for up to 2 months.

Side Effects of Diosmin

Diosmin is safe for most people when used short-term for up to 6 months. It can cause some side effects such as stomach and abdominal pain, diarrhea, dizziness, headache, skin redness and hives, muscle pain, blood problems, and altered heart rate.

In some 10% of users, diosmin causes mild gastrointestinal disorders or skin irritations (hives, itching), stomach pain, nausea, heart arrhythmias, or anemia.[rx] Preliminary research indicates no evidence of toxicity.[rx] The US Food and Drug Administration (FDA) concluded in 2001 that there was inadequate evidence on which to base an expectation of safety. As of 2013, the FDA did not revise this position.[rx]

Drug Interactions of Diosmin

We currently have no information about DIOSMIN Interactions.

Pregnancy Category of Diosmin

Pregnancy and breast-feeding

  • Not enough is known about the use of diosmin during pregnancy and breast-feeding. Stay on the safe side and avoid use.

Bleeding disorders

  • Diosmin might make bleeding disorders worse. If you have a bleeding disorder, don’t use diosmin.

References

ByRx Harun

Diosmin Cream For Hemorrhoid and Piles

Diosmin Cream For Hemorrhoid and Piles/Diosmin is a disaccharide derivative that consists of diosmetin substituted by a 6-O-(alpha-L-rhamnopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage. It has a role as an antioxidant and an anti-inflammatory agent. It is a glycosyloxyflavone, a rutinoside, a disaccharide derivative, a monomethoxyflavone, and a dihydroxyflavanone. It derives from a diosmetin.

Diosmin is a semisynthetic drug indicated for the treatment of venous disease. Diosmin is a flavone that can be found in the plant Teucrium gnaphalodes. Diosmin is available as prescription medicine in several European countries and is available as a nutritional supplement in the United States and the rest of Europe. It should be noted that clinical studies have been inconclusive and no articles have been published pertaining to its use in the treatment of vascular disease. When used in rats, diosmin has been effective at mitigating hyperglycemia, and may also have antineutrino degenerative properties.

Another Name

  • Barosmin
  • Buchu Resin
  • Daflon
  • Diosmin
  • Resin, Buchu
  • Venosmine
  • Diosmin
  • Diosmina
  • Diosmine
  • Diosminum

Mechanism of Action of Diosmin

Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phases I and II xenobiotic chemical metabolizing enzyme gene. Diosmin is a semisynthetic drug indicated for the treatment of venous disease. Diosmin is a flavone that can be found in the plant Teucrium gnaphalodes. Diosmin is available as prescription medicine in several European countries and is available as a nutritional supplement in the United States and the rest of Europe. It should be noted that clinical studies have been inconclusive and no articles have been published pertaining to its use in the treatment of vascular disease. When used in rats, diosmin has been effective at mitigating hyperglycemia, and may also have antineutrino degenerative properties.

Indications of Diosmin

  • Venous Insufficiency – general or unspecified but usually of the legs; coordinate IM with the specific vein (IM) or organ /‌blood supply (IM) if pertinent cope NoteImpaired venous blood flow or venous return (venous stasis), usually caused by inadequate venous valves. Venous insufficiency often occurs in the legs, and is associated with EDEMA and sometimes with VENOUS STASIS ULCERS at the ankle.
  • Hemorrhoidal; hemorrhoidal disease; hemorrhoids – Swollen veins in the lower part of the RECTUM or ANUS. Hemorrhoids can be inside the anus (internal), under the skin around the anus (external), or protruding from inside to outside of the anus. People with hemorrhoids may or may not exhibit symptoms that include bleeding, itching, and pain.\
  • Edema – general prefer specifics; coordinate IM with organ/diseases term (IM); egg-white edema: coordinate IM with OVALBUMIN (NIM if indexed at all); EPH (Edema, Proteinuria, Hypertension)  gestosis, EPH & do not index under EDEMA unless it is particularly discussedScope NoteAbnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.
  • Diosmin is a dietary supplement – used to aid the treatment of hemorrhoids and venous diseases, i.e., chronic venous insufficiency including spider and varicose veins, leg swelling (edema), stasis dermatitis and venous ulcers. The mechanism of action of Diosmin and other phlebotomists is undefined, and clinical evidence of benefit is limited. Diosmin is not recommended for treating the rectal mucosa, skin irritations, or wounds, and should not be used to treat dermatitis, eczema, or urticaria. Diosmin is not recommended for use in children or women during pregnancy.[rx]
  • Chronic venous insufficiency
  • Diabetes
  • Hemorrhoids
  • High blood pressure
  • Lymphedema (swelling of the arms)
  • Premenstrual syndrome
  • Ulcerative colitis
  • Varicose veins

Contraindications of Diosmin

The gel formulation is contraindicated for application to mucosa, dermal irritations, or wounds, and it should not be used to treat dermatitis, eczema, or urticaria. Diosmin is not recommended for use in children.

Dosage of Diosmin

For venous insufficiency, the dosage is 2 tablets daily. For acute hemorrhoidal attack, the dosage is 6 tablets daily for 4 days, followed by 4 tablets daily over the next 3 days.[rx] For chronic venous disease, the dosage is 2 tablets a day for at least 2 months.[rx]

BY MOUTH

  • For the treatment of internal hemorrhoids – 1350 mg of diosmin plus 150 mg of hesperidin twice daily for 4 days followed by 900 mg of diosmin and 100 mg of hesperidin twice daily for 3 days. Some researchers also try 600 mg of diosmin three times daily for 4 days, followed by 300 mg twice daily for 10 days, in combination with 11 grams of psyllium daily. However, this lower diosmin dose does not seem to be as effective.
  • For prevention of relapse internal hemorrhoids – 450 mg of diosmin plus 50 mg of hesperidin twice daily for 3 months of therapy.
  • For the treatment of leg wounds due to blood flow problems (venous stasis ulcers) – the combination of 900 mg of diosmin and 100 mg of hesperidin daily has been used for up to 2 months.

Side Effects of Diosmin

Diosmin is safe for most people when used short-term for up to 6 months. It can cause some side effects such as stomach and abdominal pain, diarrhea, dizziness, headache, skin redness and hives, muscle pain, blood problems, and altered heart rate.

In some 10% of users, diosmin causes mild gastrointestinal disorders or skin irritations (hives, itching), stomach pain, nausea, heart arrhythmias, or anemia.[rx] Preliminary research indicates no evidence of toxicity.[rx] The US Food and Drug Administration (FDA) concluded in 2001 that there was inadequate evidence on which to base an expectation of safety. As of 2013, the FDA did not revise this position.[rx]

Drug Interactions of Diosmin

We currently have no information about DIOSMIN Interactions.

Pregnancy Category of Diosmin

Pregnancy and breast-feeding

  • Not enough is known about the use of diosmin during pregnancy and breast-feeding. Stay on the safe side and avoid use.

Bleeding disorders

  • Diosmin might make bleeding disorders worse. If you have a bleeding disorder, don’t use diosmin.

References

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