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Dexlansoprazole, Uses, Dosage, Side Effects, Interactions

Dexlansoprazole is the R-isomer of lansoprazole and a substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity. As a weak base, dexlansoprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting the pump’s activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.

Dexlansoprazole is a proton pump inhibitor and R-enantiomer of lansoprazole. Its dual-delivery system is intended for extended plasma concentration and therapeutic effects, in comparison to other single-release proton pump inhibitors. Capsule formulation of dexlansoprazole also allows dosing at any time of the day without regard to meals.

Mechanism of action of Dexlansoprazole

H/K ATPase is involved in the secretion of hydrochloric acid, hydrolyzing ATP and exchanging H+ ions from the cytoplasm for K+ ions in the secretory canaliculus, which results in HCl secretion into the gastric lumen. Dexlansoprazole inhibits this effect of H/K ATPase by demonstrating a high degree of activation in the acidic environment. After passing through the liver and reaching the gastric parietal cells activated by a meal, PPIs undergo protonation in the acidic pH environment, followed by conversion to sulphenamide which represents the active form of the drug. Sulphenamide inhibits the activity of the proton pump and hence the transport of hydrogen ions into the gastric lumen via covalent binding to the SH groups of the cysteine residues of H/K ATPase

Dexlansoprazole is a substituted which inhibits the secretion of hydrochloric acid in the stomach by specific blockade of the proton pumps of the parietal cells.

Dexlansoprazole is converted to its active form in the acidic environment in the parietal cells where it inhibits the H+, K+-ATPase enzyme, i.e. the final stage in the production of hydrochloric acid in the stomach. The inhibition is dose-dependent and affects both basal and stimulated acid secretion. In most patients, freedom from symptoms is achieved within 2 weeks. As with other proton pump inhibitors and H2 receptor inhibitors, treatment with esomeprazole reduces acidity in the stomach and thereby increases gastrin in proportion to the reduction in acidity. The increase in gastrin is reversible. Since esomeprazole binds to the enzyme distal to the cell receptor level, it can inhibit hydrochloric acid secretion independently of stimulation by other substances (acetylcholine, histamine, gastrin). The effect is the same whether the product is given orally or intravenously.

Indications of Dexlansoprazole

Dexlansoprazole is used to treat conditions caused by too much acid production in the stomach, such as:

To treat symptoms of GORD such as heartburn and acid regurgitation
Gastroesophageal reflux disease (GERD)
Erosive esophagitis (acid-related damage to the esophagus, the tube that connects your mouth to your stomach)
Gastric (stomach) ulcers or duodenal ulcers , Duodenal ulcers occur in your duodenum. This is the first part of your small intestine. It is the part connected to your stomach.
Conditions where your stomach makes too much acid, such as Zollinger-Ellison Syndrome
Ulcers in the upper part of the intestine (duodenal ulcer) or stomach (gastric ulcer).
Ulcers which are infected with bacteria called ‘Helicobacter pylori’. If you have this condition, your doctor may also prescribe antibiotics to treat the infection and allow the ulcer to heal.
Ulcers caused by medicines called NSAIDs (Non-Steroidal Anti-Inflammatory Drugs). Pentoprazole 20 mg capsules can also be used to stop ulcers from forming if you are taking NSAIDs.
Too much acid in the stomach caused by a growth in the pancreas (Zollinger-Ellison syndrome).
Treatment of duodenal ulcers
Benign gastric ulcers
Gastroesophageal reflux disease (GERD),
Heartburn and other symptoms associated with GERD,
Erosive esophagitis, and long-term treatment of pathological hypersecretory conditions
Multiple endocrine adenomas,
Systemic mastocytosis.
Indicated for healing all grades of erosive esophagitis (EE), maintaining and healing of EE and relief of heartburn, and treating heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD).

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Contra Indications of Dexlansoprazole

Clostridium difficile infection
Inadequate Vitamin B12
Low amount of magnesium in the blood
Severe liver disease
Interstitial Nephritis
Subacute cutaneous lupus erythematosus
Systemic Lupus Erythematosus
Osteoporosis
Broken Bone
Allergies to Proton Pump Inhibitors

Taking a proton pump inhibitor such as dexlansoprazole may increase your risk of bone fracture in the hip, wrist, or spine. This effect has occurred mostly in people who have taken the medicine long term or at high doses, and in those who are age 50 and older. It is not clear whether dexlansoprazole is the actual cause of an increased risk of fracture.

Dosage of Dexlansoprazole

Strengths: 30 mg, 60mg,

Erosive Esophagitis

Healing of Erosive Esophagitis (EE): 60 mg orally once a day
Duration of therapy: Up to 8 weeks
Maintenance dose: 30 mg orally once a day
Duration of therapy: Up to 6 months.

Gastroesophageal Reflux Disease

30 mg orally once a day
Duration of therapy: 4 weeks

Pediatric Erosive Esophagitis

12 years and older

Healing of EE: 60 mg orally once a day
Duration of therapy: Up to 8 weeks
Maintenance dose: 30 mg orally once a day
Duration of therapy: Up to 6 months

Pediatric Gastroesophageal Reflux Disease

12 years and older: 30 mg orally once a day
Duration of therapy: 4 weeks

Side Effects of Dexlansoprazole

The most common

More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
difficulty with moving
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
decreased amount of urine

Rare

Anxiety
change in vision
seizures
abnormal or fast heart rate
tremors
weight loss
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
a headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities

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Drug Interactions of Dexlansoprazole

Dexlansoprazole may interact with following drugs, suppliments, & may change the efficacy of drugs

“azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
bisphosphonates (e.g., alendronate, etidronate)
carbamazepine
carvedilol
celecoxib
certain tyrosine kinase inhibitors (e.g., bosutinib, dasatinib, nilotinib)
chlorpropamide
cilostazol
citalopram
clobazam
clopidogrel
clozapine
cyclosporine
diazepam
escitalopram
fluoxetine
iron salts (e.g., ferrous fumarate, ferrous sulphate)
losartan
methotrexate
methylphenidate
montelukast
multivitamins with iron, folate
mycophenolate
phenobarbital
phenytoin
other proton pump inhibitors (e.g., esomeprazole, lansoprazole)
“statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
tizanidine
tricyclic antidepressants (e.g.amitriptyline, clomipramine, desipramine, trimipramine)
trimethoprim
warfarin
zafirlukast

Pregnancy Catagory of Dexlansoprazole

FDA Pregnancy Category B

Pregnancy

This medication falls into category B. There are no well-done studies that have been done in humans with dexlansoprazole. In animal studies, pregnant animals were given this medication, and the babies did not show any medical issues related to this medication.

Lactation

Tell your doctor if you are breastfeeding or planning to breastfeed. It is not known if dexlansoprazole passes into your breast milk. You and your doctor should decide if you will take dexlansoprazole or breastfeed. You should not do both. Talk to your doctor about the best way to feed your baby if you take dexlansoprazole.

Dexlansoprazole Usage

Take dexlansoprazole exactly as prescribed by your doctor.
Do not change your dose or stop taking dexlansoprazole without talking to your doctor first.
You can take dexlansoprazole capsules with or without food.
Dexlansoprazole orally disintegrating tablets should be taken on an empty stomach, 30 minutes before a meal.
Swallow dexlansoprazole capsules whole.
If you have trouble swallowing dexlansoprazole capsules or tablets whole, you may take or give them as follows:

Take dexlansoprazole capsules with applesauce

Place 1 tablespoon of applesauce into a clean container.
Carefully open the capsule and sprinkle the granules onto the applesauce.
Swallow the applesauce and granules right away. Do not chew the granules. Do not save the applesauce and granules for later use.

Take dexlansoprazole capsules with water using an oral (by mouth) syringe:

Place 20 mL of water into a clean container.
Carefully open the capsule and empty the granules into the container of water.
Use an oral syringe to draw up the water and granule mixture.
Gently swirl the syringe to keep the granules from settling.
Give the mixture into the mouth right away. Do not save the water and granule mixture for later use.
Refill the syringe with 10 mL of water and swirl gently. Give the water into the mouth.
Repeat the previous step.

For people who have a nasogastric (NG) tube that is size 16 French or larger, dexlansoprazole capsules may be given as follows:

Place 20 mL of water into a clean container.
Carefully open the capsule and empty the granules into the container of water.
Use a 60 mL catheter-tip syringe to draw up the water and granule mixture.
Gently swirl the syringe to keep the granules from settling.
Connect the catheter-tip syringe to the nasogastric tube.
Give the mixture right away through the nasogastric tube into the stomach. Do not save the water and granule mixture for later use.
Refill the syringe with 10 mL of water and swirl gently. Flush the nasogastric tube with the water.
Repeat the previous step.

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Giving dexlansoprazole orally disintegrating tablet with water using an oral syringe:

Put 1 tablet in an oral syringe and draw up 20 mL of water into the oral syringe.
Gently swirl the oral syringe to mix the tablet and the water.
After the tablet is mixed in the water, place the tip of the oral syringe in your mouth. Give the medicine right away. Do not save the tablet and water mixture for later use.
Refill the syringe with about 10 mL of water and swirl gently. Place the tip of the oral syringe in your mouth and give the medicine that is left in the syringe.
Repeat the previous step.

For people who have an NG tube that is size 8 French or larger, dexlansoprazole orally disintegrating tablet may be given as follows:

Put 1 tablet in a catheter-tip syringe and draw up 20 mL of water.
Gently swirl the catheter-tip syringe to mix the tablet and the water.
After the tablet is mixed in the water, swirl the catheter-tip syringe gently in order to keep the particles from settling.
Connect the catheter-tip syringe to the NG tube.
Give the mixture right away through the NG tube that goes into the stomach. Do not save the tablet and water mixture for later use.
Refill the catheter-tip syringe with about 10 mL of water and swirl gently. Flush the NG tube with water.
Repeat the previous step.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of dexlansoprazole at the same time.

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