Nexium 20 mg Capsules

Brand Name

The medication is marketed under the brand name Nexium, a widely recognized label in the field of gastrointestinal acid-related disorder management.

International Nonproprietary Name (INN)

The active ingredient in this product is identified globally as esomeprazole, a name standardized for consistency across international pharmacological practices.

Form of Release

Nexium is available as delayed-release oral capsules, delayed-release oral tablets, and packets for oral suspension, with an intravenous formulation for specific use. Capsules come in strengths of 20 mg and 40 mg, tablets match these doses, and the suspension packets offer 2.5 mg, 5 mg, 10 mg, 20 mg, or 40 mg, while the injectable form provides 20 mg or 40 mg per vial.

Composition

Each delayed-release capsule or tablet of Nexium contains esomeprazole magnesium as the primary active substance, with dosages of 20 mg or 40 mg (equivalent to esomeprazole base). The formulation includes several inactive ingredients, such as glyceryl monostearate, which acts as a stabilizer, and microcrystalline cellulose, providing structural support. Additional excipients like hydroxypropyl cellulose serve as binders, while the enteric coating comprises methacrylic acid copolymer, polysorbate 80, and triethyl citrate to ensure intestinal release. The suspension includes citric acid and maltodextrin, and the intravenous solution contains sodium hydroxide for pH adjustment, ensuring efficacy across all forms.

Pharmacologic Properties

Pharmacodynamics

Nexium belongs to the proton pump inhibitor (PPI) class, exerting its effects by irreversibly inhibiting the hydrogen/potassium adenosine triphosphatase (H+/K+ ATPase) enzyme in gastric parietal cells. This blockade suppresses gastric acid secretion, reducing both basal and stimulated acid output, which elevates intragastric pH and facilitates healing in acid-damaged tissues. Its S-isomer structure enhances potency and duration compared to racemic PPIs, providing acid control for up to 24 hours per dose.

The medication also supports Helicobacter pylori eradication when combined with antibiotics, reducing ulcer recurrence by creating an optimal pH environment. Clinical studies demonstrate its ability to heal erosive esophagitis in 90–95% of patients within 4–8 weeks, with superior symptom relief in gastroesophageal reflux disease (GERD). It does not affect gastric motility or pepsin secretion significantly, focusing on acid suppression. This targeted mechanism underpins its efficacy in managing acid-mediated conditions.

Pharmacokinetics

Following oral administration, Nexium is absorbed in the small intestine due to its enteric coating, with peak plasma concentrations reached within 1 to 2 hours. Bioavailability increases with repeated dosing, reaching 64–90% due to reduced first-pass metabolism, and food delays absorption without altering extent. The drug binds to plasma proteins at approximately 97%, distributing primarily to the bloodstream and gastric mucosa.

Metabolism occurs extensively in the liver via cytochrome P450 enzymes CYP2C19 and CYP3A4, converting esomeprazole into inactive hydroxy and desmethyl metabolites. The half-life ranges from 1 to 1.5 hours, though its antisecretory effect persists longer due to enzyme binding. Elimination is predominantly urinary, with 80% excreted as metabolites and less than 20% via feces, reflecting minimal biliary clearance.

Indications for Use

Nexium is prescribed for the treatment of erosive esophagitis due to GERD in adults and children over 1 year, healing esophageal erosions and relieving symptoms like heartburn. It is also indicated for maintenance therapy in healed GERD to prevent relapse, offering sustained acid control. The medication manages symptomatic GERD without erosions, addressing persistent reflux discomfort.

In combination with antibiotics, it eradicates Helicobacter pylori in patients with duodenal ulcers, promoting healing and preventing recurrence. It treats Zollinger-Ellison syndrome and other hypersecretory states by controlling excessive acid production. Intravenous use is indicated for acute GERD or bleeding ulcers when oral administration is not feasible. These applications highlight its versatility in acid-related care.

Contraindications

Nexium is contraindicated in patients with known hypersensitivity to esomeprazole, substituted benzimidazoles, or any formulation component, such as polysorbate 80, where reactions could range from rash to anaphylaxis. It is also prohibited in those requiring immediate acid suppression unavailable via oral delayed-release forms, unless intravenous use is an option.

Use with atazanavir or nelfinavir is restricted due to reduced antiviral efficacy from elevated gastric pH. Severe liver dysfunction does not strictly contraindicate it, but caution is warranted. The medication should not be used in patients with a history of severe PPI-related adverse events, like acute interstitial nephritis, unless benefits outweigh risks. Pregnancy and breastfeeding limit its use unless clearly necessary.

Method of Administration and Dosage

Administration Guidelines

The capsules or tablets should be taken orally, swallowed whole with water, typically 1 hour before a meal to optimize acid suppression. They should not be chewed or crushed, as this disrupts the enteric coating. Suspension packets require mixing with water and immediate consumption, while intravenous doses are administered by healthcare professionals over 10–30 minutes. Consistent timing enhances efficacy.

Dosage for Adults and Children

For adults with erosive GERD, the typical dose of Nexium is 20–40 mg once daily for 4–8 weeks, extendable if needed. Maintenance therapy uses 20 mg daily, adjustable to 40 mg for severe cases. Symptomatic GERD requires 20 mg daily for 4 weeks. Helicobacter pylori eradication involves 40 mg once daily with antibiotics for 10 days. Zollinger-Ellison syndrome starts at 40 mg twice daily, up to 240 mg daily. Children aged 12–17 with GERD use 20–40 mg daily for up to 8 weeks; ages 1–11 use 10–20 mg daily based on weight (e.g., 10 mg for 10–20 kg, 20 mg for over 20 kg).

Dose Adjustment in Specific Conditions

No adjustment is needed for renal impairment, as excretion is primarily metabolic. Mild to moderate liver dysfunction allows standard dosing, but severe cases cap doses at 20 mg daily due to altered metabolism. Elderly patients or those with mild symptoms may start at 20 mg, guided by response. Intravenous dosing mirrors oral regimens for acute needs, with oral transition as soon as feasible.

Side Effects

Nexium may cause a range of side effects, though many patients experience only mild reactions with short-term use. Common issues include headache, abdominal pain, or diarrhea, often resolving spontaneously. Nausea, constipation, or flatulence are also reported, typically transient as the body adjusts.

Less frequent effects include dizziness, dry mouth, or rash, linked to systemic exposure. Rare but serious reactions, such as hypomagnesemia, Clostridium difficile infection, or vitamin B12 deficiency, may occur with prolonged use, warranting monitoring. Acute interstitial nephritis or severe cutaneous reactions (e.g., erythema multiforme) require immediate cessation and medical attention. Regular follow-ups mitigate these risks effectively.

Overdose

Symptoms of Overdose

Excessive intake of Nexium is unlikely to cause acute toxicity due to its wide therapeutic index, with symptoms limited to amplified side effects like drowsiness, confusion, or gastrointestinal distress. Doses up to 280 mg daily have shown no consistent severe pattern, reflecting rapid metabolism.

First Aid Measures

In case of overdose, medical consultation is advised, though emergency measures are rarely needed. No specific antidote exists, so treatment focuses on supportive care, such as hydration for diarrhea or rest for fatigue. Monitoring is recommended until symptoms resolve, typically within 24 hours, given the drug’s short half-life.

Drug Interactions

Effects on Other Medications

Nexium alters gastric pH, reducing absorption of pH-dependent drugs like ketoconazole or digoxin, potentially decreasing efficacy. It inhibits CYP2C19, increasing levels of diazepam, phenytoin, or warfarin, requiring monitoring or adjustments. Co-use with clopidogrel may reduce antiplatelet effect due to metabolic competition, while methotrexate toxicity risk rises at high doses.

Drugs like rifampin, a CYP3A4 inducer, may lower esomeprazole levels, though this is rarely significant. Patients should report all medications to their healthcare provider to manage these interactions, especially in long-term therapy.

Compatibility with Alcohol and Food

Moderate alcohol use does not directly impair efficacy but may worsen GERD symptoms, suggesting limited intake during therapy. Food delays absorption slightly but enhances tolerability, making pre-meal dosing a practical strategy for optimal effect.

Special Precautions

Use During Pregnancy and Breastfeeding

Nexium is Category B in pregnancy, with no clear fetal harm in limited data, used cautiously if benefits outweigh risks, typically for severe GERD. It passes into breast milk minimally, so short-term use is generally safe with monitoring for infant effects, guided by medical advice.

Women of childbearing age should confirm non-pregnant status before starting and use contraception during therapy to avoid unintended fetal exposure.

Impact on Driving and Operating Machinery

The medication may cause dizziness or drowsiness in some patients, suggesting caution with driving or machinery until tolerance is clear. Most individuals resume normal activities once adjusted, but initial use warrants observation for these effects.

Considerations for Elderly and Pediatric Populations

Elderly patients tolerate Nexium well, with no significant efficacy differences, though long-term monitoring for bone health or nutrient deficiencies is key. Children over 1 year can use age- and weight-adjusted dosing safely, while those under 1 lack established safety data, limiting use to older pediatric groups.