Vitamin A Acid – Uses, Dosage, Side Effects, Interaction

Indications of Tretinoin

Antineoplastic Agents Keratolytic Agents

• Isotretinoin is a vitamin A derivative used in the treatment of severe acne and some forms of skin, head and neck cancer.
• Tretinoin gel and cream are indicated for topical application in the treatment of acne vulgaris. The safety and efficacy of the long-term use of this product in the treatment of other disorders have not been established.
• Tretinoin is used topically as a 0.05 or 0.1% cream for palliative therapy to improve dermatologic changes (e.g., fine wrinkling, mottled hyperpigmentation, roughness) associated with photodamage.
• Tretinoin has been used topically for the treatment of flat warts. The drug also has been used with topical fluorouracil for the temporary, initial combination therapy of multiple actinic (solar) keratoses on areas other than the head and neck (e.g., hands, arms).
• In concentrations of 0.1-0.3%, tretinoin has been used topically for the treatment of other skin conditions such as psoriasis, ichthyosis congenital, ichthyosis Vulgaris, lamellar ichthyosis, keratosis palmaris et plantaris, epidermolytic hyperkeratosis, senile comedones, senile keratosis, keratosis follicularis (Darier’s disease), and basal cell carcinomas.
• Acne Vulgaris
• FAB classification M3 Acute promyelocytic leukemia
• Solar Lentigines
• Facial fine wrinkling
• Moderate Melasma
• Mottled hyperpigmentation
• Severe Melasma
• Severe, recalcitrant Cystic acne
• Tactile roughness of facial skin
• Photoaging of the Skin
• Necrobiosis Lipoidica Diabeticorum
• Lichen Sclerosus
• For the topical treatment of acne vulgaris, flat warts and other skin conditions (psoriasis, ichthyosis congenital, ichthyosis Vulgaris, lamellar ichthyosis, keratosis palmaris et plantaris, epidermolytic hyperkeratosis, senile comedones, senile keratosis, keratosis follicularis (Darier’s disease), and basal cell carcinomas.);
• For palliative therapy to improve fine wrinkling, mottled hyperpigmentation, roughness associated with photodamage.
• Tretinoin is used to induce remission in people with acute promyelocytic leukemia who have a mutation translocation 160 and/or the presence of the PML/RARα gene) and who don’t respond to anthracyclines or can’t take that class of drug.

Contraindications Of Tretinoin

• glucose-6-phosphate dehydrogenase (G6PD) deficiency
• deficiency of the blood enzyme cytochrome b5 reductase
• significant anemia
• liver problems
• Anemia from Pyruvate Kinase and G6PD Deficiencies
• Absolute contraindications to the use of dapsone are prior hypersensitivity to dapsone or its derivatives including agranulocytosis and hypersensitivity syndrome. Deaths from agranulocytosis, aplastic anemia, and other blood dyscrasias have been reported with dapsone administration.
• Relative contraindications to the use of dapsone include allergy to sulfonamide antibiotics, significant cardiopulmonary disease, significant liver or renal function impairment, or pre-existing peripheral neuropathy.
• For the treatment of women who are pregnant, dapsone is a category C drug. Therefore, it should be used with caution only if benefits outweigh risks.
• According to the American Academy of Pediatrics, dapsone is listed as a “maternal medication usually compatible with breastfeeding.
• Allergies to tretinoin

Dosage of Tretinoin

 Strengths: 0.05%; 0.025%; 0.02%; 0.1%; 0.04%; 0.01%; 0.06%; 0.08%; cream 0.1%; cream 0.05%; cream 0.025%; gel 0.025%; gel 0.01%; 0.0375%; 0.075%

Acne

• Recommended dose: Apply a thin layer to the entire affected area once a day at bedtime

Dermatoheliosis

• Recommended dose: Apply a pea-sized amount to the entire affected area once a day at bedtime
• Duration of therapy: 48 weeks (0.05% cream/emollient cream) and 52 weeks (0.02% cream)

Pediatric Dose for Acne

12 years and older

• Recommended dose: Apply a thin layer to the affected area once a day at bedtime

Side Effects Of Tretinoin

More common

• itching, dryness, redness, scaling, or peeling of the skin
• Burning, itching, stinging, scaling, or redness of the skin
• chapping or slight peeling of the skin (mild)
• darkening of the skin
• lightening of normal skin color
• lightening of treated areas of dark skin
• redness of skin (mild)
• unusual dryness of skin (mild)
• unusually warm skin (mild)
• numbing or tingling sensation in the hands or feet
• signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities)
• signs of infections (e.g., fever or chills, sore throat)
• signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
• unusual tiredness or weakness
• Back, leg, or stomach pains
• bluish fingernails, lips, or skin
• difficult breathing
• fever
• loss of appetite
• pale skin
• skin rash
• unusual tiredness or weakness

Common

• Hematologic: Hemolytic anemia, methemoglobinemia, leukopenia, and agranulocytosis
• Cutaneous hypersensitivity reactions: Mebilliform eruption, exfoliative erythroderma, drug-induced lupus erythematosus, and toxic epidermal necrolysis
• Neurologic: Peripheral neuropathy, predominantly motor loss
• Psychiatric: Psychosis and insomnia
• Eyes: Blurred vision
• Ear, nose, and throat: Tinnitus and vertigo
• Cardiac: Tachycardia
• Pulmonary: Pulmonary Eosinophilia
• Hepatic: Hepatitis, dapsone syndrome, cholestatic jaundice, and hypoalbuminemia without proteinuria
• Gastrointestinal: Nausea, vomiting, abdominal pain, anorexia, and pancreatitis
• Renal: Nephrotic syndrome, albuminur
• signs of anemia (low red blood cells; e.g., dizziness, pale skin, unusual tiredness or weakness, shortness of breath)
• signs of infection (fever, severe chills, sore throat, mouth ulcers)
• signs of an allergic reaction (e.g., rash, hives, swelling of the lips or face, difficulty breathing)

Rare

• severe vomiting
• signs of methemoglobinemia (e.g., headache, fatigue, dizziness, shortness of breath, grey or bluish skin colour, especially of lips, mouth and nail beds)
• signs of pancreatitis (e.g., abdominal pain on the upper left side, back pain, nausea, fever, chills, rapid heartbeat, swollen abdomen)
• Itching, dryness, redness, scaling, or peeling of the skin, or loss of hair
• mood or other mental changes
• numbness, tingling, pain, burning, or weakness in hands or feet
• sore throat
• unusual bleeding or bruising
• yellow eyes or skin
• blurred vision
• dizziness
• fast heartbeat
• fatigue
• headache
• loss of appetite
• nausea or vomiting
• skin rash or itch
• trouble sleeping

Drug Interaction of Vitamin A Acid

There may be an interaction between tretinoin and any of the following

• aminolevulinic acid
• aminolevulinic acid topical
• benzoyl peroxide topical
• benzoyl peroxide
• medications that increase the skin’s sensitivity to sunlight (e.g., isotretinoin, sulfamethoxazole, trimethoprim, minocycline, ciprofloxacin)
• medicated or abrasive soaps and cleansers
• other skin-applied medications
• erythromycin
• isotretinoin
• methoxsalen
• methyl aminolevulinate topical
• resorcinol topical
• salicylic acid topical
• sulfur topical
• verteporfin
• other topical medications to treat acne
• products with high concentrations of alcohol, astringents, spices, or lime
• skin preparations containing sulfur, resorcinol, or salicylic acid
• soaps and cosmetics with a strong drying effect

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

• stop taking one of the medications,
• change one of the medications to another,
• change how you are taking one or both of the medications, or
• leave everything as is.

Pregnancy Category of Vitamin A Acid

FDA Pregnancy Category – C

Pregnancy

This medication is not recommended for use during pregnancy. Women who may become pregnant should use an effective method of birth control while they are using this medication. If you become pregnant while using this medication, stop using it immediately and contact your doctor.

Breast-feeding

It is not known if tretinoin passes into breast milk. If you are a breast-feeding mother and are using this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of using this medication have not been established for children less than 12 years of age. Topical tretinoin is not recommended for this age group.

What form(s) does this medication come in?

Cream

0.01%
Each gram of cream contains 0.01% tretinoin in a bland, hydrophilic base. Nonmedicinal ingredients: butylated hydroxytoluene, isopropyl myristate, polyoxyl (40) stearate, purified water, sorbic acid, stearic acid, stearyl alcohol, and xanthan gum.

0.025%
Each gram of cream contains 0.025% tretinoin in a bland, hydrophilic base. Nonmedicinal ingredients: butylated hydroxytoluene, isopropyl myristate, polyoxyl (40) stearate, purified water, sorbic acid, stearic acid, stearyl alcohol, and xanthan gum.

0.05%
Each gram of cream contains 0.05% tretinoin in a bland, hydrophilic base. Nonmedicinal ingredients: butylated hydroxytoluene, isopropyl myristate, polyoxyl (40) stearate, purified water, sorbic acid, stearic acid, stearyl alcohol, and xanthan gum.

0.1%
Each gram of cream contains 0.1% tretinoin in a bland, hydrophilic base. Nonmedicinal ingredients: butylated hydroxytoluene, isopropyl myristate, polyoxyl (40) stearate, purified water, sorbic acid, stearic acid, stearyl alcohol, and xanthan gum.

Gel

0.01%
Each gram of gel contains 0.01% tretinoin. Nonmedicinal ingredients: butylated hydroxytoluene, undenatured ethanol, and hydroxypropyl cellulose.

0.025%
Each gram of gel contains 0.025% tretinoin. Nonmedicinal ingredients: butylated hydroxytoluene, undenatured ethanol, and hydroxypropyl cellulose.

References

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