Prilosec 10 mg Capsules

Brand Name

The medication is marketed under the brand name Prilosec, a widely acknowledged label in the realm of gastrointestinal acid control and healing.

International Nonproprietary Name (INN)

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

Form of Release

Prilosec is available as delayed-release oral capsules and packets for oral suspension. Capsules come in strengths of 10 mg, 20 mg, and 40 mg, while suspension packets match these doses, offering flexible administration options for various patient needs.

Composition

Each delayed-release capsule of Prilosec contains omeprazole magnesium as the primary active substance, with dosages of 10 mg, 20 mg, or 40 mg (equivalent to omeprazole base). The formulation includes several inactive ingredients, such as disodium hydrogen phosphate, which acts as a stabilizer, and microcrystalline cellulose, providing structural support. Additional excipients like hydroxypropyl methylcellulose serve as binders, while the enteric coating comprises methacrylic acid copolymer, triethyl citrate, and gelatin to ensure release in the intestine. The suspension includes xylitol and sodium bicarbonate, enhancing palatability and stability.

Pharmacologic Properties

Pharmacodynamics

Prilosec 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 promotes healing of acid-damaged tissues. Its action provides prolonged acid suppression, lasting up to 24 hours, making it more effective than H2-receptor antagonists for chronic conditions.

The medication also facilitates Helicobacter pylori eradication when combined with antibiotics, optimizing the gastric environment for bacterial clearance. Clinical studies demonstrate its ability to heal duodenal ulcers in 90–95% of patients within 2–4 weeks, with significant symptom relief in gastroesophageal reflux disease (GERD). It does not alter gastric motility or endocrine function directly, focusing on acid control. This targeted mechanism supports its efficacy in managing acid-related disorders.

Pharmacokinetics

Following oral administration, Prilosec is absorbed in the small intestine due to its enteric coating, with peak plasma concentrations reached within 0.5 to 3.5 hours. Bioavailability increases with repeated dosing, ranging from 30–40% initially to 60–70% at steady state, though food reduces absorption by about 50%. The drug binds to plasma proteins at approximately 95%, distributing primarily to the bloodstream and gastric mucosa.

Metabolism occurs extensively in the liver via cytochrome P450 enzymes CYP2C19 and CYP3A4, converting omeprazole into inactive hydroxy and sulfone metabolites. The half-life ranges from 0.5 to 1 hour, though its antisecretory effect persists longer due to enzyme binding. Elimination is predominantly urinary, with 77% excreted as metabolites and less than 20% via feces, reflecting minimal biliary clearance.

Indications for Use

Prilosec is prescribed for the treatment of active duodenal ulcers in adults, promoting healing and relieving pain within 2–4 weeks. It is also indicated for erosive esophagitis due to GERD, addressing esophageal damage and symptoms like heartburn, and for maintenance therapy in healed esophagitis to prevent relapse. The medication manages symptomatic GERD without erosions, providing relief from acid reflux discomfort.

In combination with antibiotics, it eradicates Helicobacter pylori in patients with peptic ulcers, reducing recurrence risk. It treats gastric ulcers and hypersecretory conditions like Zollinger-Ellison syndrome by controlling excessive acid production. Over-the-counter use targets occasional heartburn or acid indigestion, making it versatile for both prescription and self-care applications.

Contraindications

Prilosec is contraindicated in patients with known hypersensitivity to omeprazole, substituted benzimidazoles, or any formulation component, such as sodium bicarbonate in suspension, where reactions could range from rash to anaphylaxis. It is also prohibited in those requiring immediate acid suppression unavailable via oral delayed-release forms.

Use with nelfinavir or rilpivirine 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, such as acute interstitial nephritis, unless benefits outweigh risks. Infants under 1 year are excluded from use due to limited safety data.

Method of Administration and Dosage

Administration Guidelines

The capsules should be taken orally, swallowed whole with water, ideally 30–60 minutes before a meal to optimize acid suppression. They should not be opened or crushed, as this disrupts the enteric coating. Suspension packets require mixing with water for immediate consumption, with apple juice as an alternative for children. Consistent morning dosing enhances efficacy.

Dosage for Adults and Children

For adults with active duodenal ulcers, the typical dose of Prilosec is 20 mg once daily for 4–8 weeks. Erosive esophagitis uses 20–40 mg once daily for 4–8 weeks, with maintenance at 20 mg daily. Symptomatic GERD requires 20 mg daily for 4 weeks. Helicobacter pylori eradication involves 20 mg twice daily with antibiotics for 10 days. Hypersecretory conditions start at 60 mg daily, adjustable up to 120 mg in divided doses. Children aged 2–16 with GERD use 5–20 mg daily based on weight (e.g., 5 mg for 5–10 kg, 10 mg for 10–20 kg, 20 mg for over 20 kg) for up to 12 weeks; ages 1–2 use 5–10 mg daily.

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 10 mg, guided by response. Treatment duration aligns with clinical improvement, avoiding unnecessary extension beyond recommended periods.

Side Effects

Prilosec may cause a variety of side effects, though many patients experience only mild reactions with short-term use. Common issues include headache, diarrhea, or abdominal pain, often resolving without intervention. Nausea, constipation, or flatulence are also reported, typically transient as the body adjusts.

Less frequent effects include dizziness, fatigue, or rash, linked to systemic exposure. Rare but serious reactions, such as hypomagnesemia, Clostridium difficile infection, or vitamin B12 deficiency with prolonged use, warrant monitoring. Acute interstitial nephritis or severe cutaneous reactions (e.g., toxic epidermal necrolysis) require immediate cessation and medical attention. Regular follow-ups help manage these risks effectively.

Overdose

Symptoms of Overdose

Excessive intake of Prilosec is unlikely to cause acute toxicity due to its wide therapeutic index, with symptoms limited to amplified side effects like confusion, drowsiness, or gastrointestinal distress. Doses up to 560 mg 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

Prilosec alters gastric pH, reducing absorption of pH-dependent drugs like ketoconazole or digoxin, potentially decreasing efficacy, requiring spacing by 1–2 hours. It inhibits CYP2C19, increasing levels of diazepam, phenytoin, or warfarin, necessitating 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 omeprazole 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 reduces bioavailability significantly, making pre-meal dosing critical for optimal effect, though suspension tolerates mixing with certain liquids.

Special Precautions

Use During Pregnancy and Breastfeeding

Prilosec is Category C 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, typically resolving within hours.

Considerations for Elderly and Pediatric Populations

Elderly patients tolerate Prilosec well, with no significant efficacy differences, though monitoring for long-term effects like bone health 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.