Usage
Dexlansoprazole is prescribed for the following medical conditions:
- Healing of all grades of erosive esophagitis (EE): This condition involves damage to the esophagus caused by stomach acid reflux.
- Maintenance of healed EE and relief of heartburn: To prevent recurrence of erosive esophagitis and manage associated heartburn.
- Treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD): For patients experiencing heartburn due to GERD without esophageal damage.
It is classified as a proton pump inhibitor (PPI).
Dexlansoprazole’s mechanism of action involves inhibiting the H+/K+-ATPase enzyme (proton pump) in gastric parietal cells. This blocks the final step of gastric acid production, thereby reducing the amount of acid in the stomach.
Alternate Names
Dexlansoprazole is also known by the brand name Dexilant. There do not seem to be other alternate names, international variations, or regional variations of the name.
How It Works
Pharmacodynamics: Dexlansoprazole reduces gastric acid secretion by irreversibly inhibiting the H+/K+-ATPase enzyme system located on the secretory surface of gastric parietal cells. This action effectively blocks the final step in gastric acid production. The dual delayed-release formulation of Dexilant provides two peaks of drug release, resulting in prolonged acid suppression.
Pharmacokinetics:
- Absorption: Dexlansoprazole exhibits two peaks of absorption after oral administration, one occurring within 1-2 hours and another within 4-5 hours. Food may slightly delay absorption but does not clinically affect efficacy.
- Metabolism: Extensively metabolized in the liver primarily by CYP2C19 and CYP3A4 enzymes into inactive metabolites.
- Elimination: Primarily eliminated via hepatic metabolism with subsequent biliary excretion. No parent drug is recovered in urine.
Mode of Action: Dexlansoprazole irreversibly binds to the H+/K+-ATPase enzyme, inhibiting its activity and reducing acid secretion. It does not bind to other receptors or modulate neurotransmitters.
Elimination Pathways: Primarily hepatic metabolism followed by biliary excretion.
Dosage
Standard Dosage
Adults:
- Healing of EE: 60 mg once daily for up to 8 weeks.
- Maintenance of healed EE and relief of heartburn: 30 mg once daily for up to 6 months.
- Symptomatic Non-Erosive GERD: 30 mg once daily for 4 weeks.
Children (12-17 years):
- Healing of EE: 60 mg once daily for up to 8 weeks.
- Maintenance of healed EE and relief of heartburn: 30 mg once daily for up to 16 weeks (information provided in the sources indicated up to 6 months for adults, and up to 4 months as per MIMS).
- Symptomatic Non-Erosive GERD: 30 mg once daily for 4 weeks.
Dexlansoprazole is not recommended for children under 12 years of age.
Special Cases:
- Elderly Patients: Dosage adjustment may be necessary based on individual requirements. A daily dose of 60 mg should not be exceeded unless clinically indicated.
- Patients with Renal Impairment: No dosage adjustment is necessary.
- Patients with Hepatic Dysfunction:
Mild impairment: no adjustment is needed. Moderate impairment: 30 mg once daily should be considered, with a maximum of up to 8 weeks of treatment for EE. Severe impairment: not recommended.
- Patients with Comorbid Conditions: Consider underlying conditions and potential drug interactions when determining the dosage.
Clinical Use Cases
Dexlansoprazole’s usage in the listed clinical scenarios generally falls under its established indications for GERD and erosive esophagitis. The specific dosage should be determined based on patient-specific factors and the severity of the condition. There are no specific dosing recommendations for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations indicated in the sources. The general dosage guidelines should be followed, taking into account potential drug interactions and the patient’s condition.
Dosage Adjustments
Dosage adjustments may be required based on factors such as age, hepatic impairment, and concomitant medications. Monitor renal and liver function during long-term therapy.
Side Effects
Common Side Effects:
Diarrhea, stomach pain, nausea, vomiting, gas, upper respiratory infection, headache.
Rare but Serious Side Effects:
Clostridium difficile infection, vitamin B12 deficiency, hypomagnesemia, severe allergic reactions, bone fractures (hip, wrist, spine), cutaneous lupus erythematosus (CLE), systemic lupus erythematosus (SLE), fundic gland polyps, acute interstitial nephritis.
Long-Term Effects:
Potential for bone loss and fractures with prolonged use, especially at higher doses.
Adverse Drug Reactions (ADR):
Anaphylaxis, severe skin reactions (DRESS), acute interstitial nephritis.
Contraindications
- Known hypersensitivity to dexlansoprazole or any component of the formulation.
- Concomitant use with rilpivirine.
Drug Interactions
Dexlansoprazole interacts with numerous medications, including:
- Methotrexate
- Digoxin
- Warfarin
- Tacrolimus
- Certain antiretroviral medicines (e.g., rilpivirine, nelfinavir, saquinavir)
- St. John’s Wort
- Rifampin
Consult a comprehensive drug interaction resource for a complete list. Monitor patients closely for potential interactions.
Pregnancy and Breastfeeding
Data on dexlansoprazole use during pregnancy are limited. Use only if clearly needed. It is unknown if dexlansoprazole passes into breast milk. Consult a physician to weigh the risks and benefits of using this drug during breastfeeding or consider safer alternatives.
Drug Profile Summary
- Mechanism of Action: PPI, inhibits H+/K+-ATPase.
- Side Effects: Diarrhea, stomach pain, nausea; rarely C. difficile, B12 deficiency, hypomagnesemia, fractures.
- Contraindications: Hypersensitivity, rilpivirine.
- Drug Interactions: Methotrexate, digoxin, warfarin, tacrolimus, antiretrovirals.
- Pregnancy & Breastfeeding: Limited data; use with caution.
- Dosage: Adults/Children (12+): EE healing: 60mg QD up to 8 weeks; EE maintenance: 30 mg QD up to 6/16 months/weeks; GERD: 30mg QD up to 4 weeks.
- Monitoring Parameters: Magnesium levels, vitamin B12 levels, bone density (long-term use), signs of adverse reactions.
Popular Combinations
No specific popular combinations are described in the provided sources.
Precautions
- Pre-screening for allergies, metabolic disorders, organ dysfunction is recommended.
- Caution in patients with risk factors for osteoporosis and vitamin B12 deficiency.
- Monitor liver function in patients with hepatic impairment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Dexlansoprazole?
A: Adults/Children(12+): 60 mg once daily for up to 8 weeks for EE; 30 mg once daily for up to 6/16 months/weeks for maintenance of healed EE, and up to 4 weeks for GERD. Dosages should be adjusted for moderate hepatic impairment (30 mg maximum). Not recommended in severe hepatic impairment. Not established for use in children below 12 years.
Q2: What are the common side effects of Dexlansoprazole?
A: Common side effects include diarrhea, stomach pain, nausea, vomiting, gas, upper respiratory infections, and headache.
Q3: What are the serious side effects of Dexlansoprazole?
A: C. difficile infection, vitamin B12 deficiency, hypomagnesemia, severe allergic reactions (including anaphylaxis and DRESS), bone fractures, cutaneous and systemic lupus erythematosus, and fundic gland polyps are rare but serious side effects.
Q4: What are the contraindications for Dexlansoprazole?
A: Contraindications include known hypersensitivity to dexlansoprazole or its components and concomitant use with rilpivirine.
Q5: How should Dexlansoprazole be administered?
A: Dexlansoprazole capsules should be swallowed whole. They can also be opened and the granules sprinkled on applesauce and swallowed immediately without chewing. Administer without regard to food.
Q6: Does Dexlansoprazole interact with other medications?
A: Yes, Dexlansoprazole can interact with several medications, including methotrexate, digoxin, warfarin, tacrolimus, and some antiretrovirals. Always consult a comprehensive drug interaction resource before co-prescribing.
Q7: Can Dexlansoprazole be used during pregnancy or breastfeeding?
A: Data on use during pregnancy is limited, use only if clearly needed. It is unknown if it is excreted in breast milk; weigh benefits and risks or consider alternatives.
Q8: Are there any precautions for elderly patients taking Dexlansoprazole?
A: Due to reduced clearance, dosage adjustment may be necessary for elderly patients. Do not exceed 60 mg daily unless clinically indicated.
Q9: How does hepatic impairment affect Dexlansoprazole dosing?
A: No adjustment is needed for mild impairment. 30mg maximum daily dose is advised for moderate hepatic impairment. It is not recommended for patients with severe hepatic impairment.
