Losec


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omeprazole

(o-mep-ra-zole) ,

Losec

(trade name),

PriLOSEC

(trade name),

PriLOSEC OTC

(trade name)

Classification

Therapeutic: antiulcer agents
Pharmacologic: proton pump inhibitors
Pregnancy Category: C

Indications

GERD/maintenance of healing in erosive esophagitis.Duodenal ulcers (with or without anti-infectives for Helicobacter pylori).Short-term treatment of active benign gastric ulcer.Pathologic hypersecretory conditions, including Zollinger-Ellison syndrome.Reduction of risk of GI bleeding in critically ill patients.OTC: Heartburn occurring ≥twice/wk.

Action

Binds to an enzyme on gastric parietal cells in the presence of acidic gastric pH, preventing the final transport of hydrogen ions into the gastric lumen.

Therapeutic effects

Diminished accumulation of acid in the gastric lumen with lessened gastroesophageal reflux.
Healing of duodenal ulcers.

Pharmacokinetics

Absorption: Rapidly absorbed following oral administration; immediate release formulation contains bicarbonate to prevent acid degradation.
Distribution: Good distribution into gastric parietal cells.
Protein Binding: 95%.
Metabolism and Excretion: Mostly metabolized by the liver via the cytochrome P450 (CYP) system (primarily CYP2C19 isoenzyme, but also the CYP3A4 isoenzyme) (the CYP2C19 enzyme system exhibits genetic polymorphism; genetic implication 15–20% of Asian patients and 3–5% of Caucasian and Black patients may be poor metabolizers and may have significantly ↑ omeprazole concentrations and an ↑ risk of adverse effects); inactive metabolites are excreted in urine (77%) and feces.
Half-life: 0.5–1 hr (↑ in liver disease to 3 hr).

Time/action profile (antisecretory effects)

ROUTEONSETPEAKDURATION
PO-delayed releasewithin 1 hrwithin 2 hr72–96 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Lactation: Discontinue omeprazole or discontinue breast feeding.
Use Cautiously in: Liver disease (dose ↓ may be necessary); Obstetric / Lactation / Pediatric: Safety not established in pregnant or breast-feeding women, or children <1 yr;Patients using high-doses for >1 year (↑ risk of hip, wrist, or spine fractures).

Adverse Reactions/Side Effects

Central nervous system

  • dizziness
  • drowsiness
  • fatigue
  • headache
  • weakness

Cardiovascular

  • chest pain

Gastrointestinal

  • pseudomembranous colitis (life-threatening)
  • abdominal pain (most frequent)
  • acid regurgitation
  • constipation
  • diarrhea
  • flatulence
  • nausea
  • vomiting

Fluid and Electrolyte

  • hypomagnesemia (especially if treatment duration ≥3 mo)

Dermatologic

  • itching
  • rash

Musculoskeletal

  • bone fracture

Miscellaneous

  • allergic reactions

Interactions

Drug-Drug interaction

Omeprazole is metabolized by the CYP450 enzyme system and may compete with other agents metabolized by this system.↓ metabolism and may ↑ effects of antifungal agents, diazepam, digoxin, flurazepam, triazolam, cyclosporine, phenytoin, saquinavir, tacrolimus, and warfarin.May ↓ absorption of drugs requiring acid pH, including ketoconazole, itraconazole, ampicillin, iron salts, and digoxin.Has been used safely with antacids.May significantly ↓ effects of atazanavir and nelfinavir (concurrent use not recommended).May ↑ risk of bleeding with warfarin (monitor INR/PT).Voriconazole may ↑ levels.May ↓ the antiplatelet effects of clopidogrel ; avoid concurrent use.May ↑ levels of cilostazol ; consider ↓ dose of cilostazol from 100 mg twice daily to 50 mg twice daily.Rifampin may ↓ levels and may ↓ response; avoid concurrent use.Hypomagnesemia ↑ risk of digoxin toxicity.May ↑ levels of tacrolimus and methotrexate.St. John's wort may ↓ levels and may ↓ response; avoid concurrent use.

Route/Dosage

Oral (Adults) GERD/erosive esophagitis—20 mg once daily. Duodenal ulcers associated with H. pylori—40 mg once daily in the morning with clarithromycin for 2 wk, then 20 mg once daily for 2 wk or 20 mg twice daily with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 10 days (if ulcer is present at beginning of therapy, continue omeprazole 20 mg daily for 18 more days); has also been used with clarithromycin and metronidazole. Gastric ulcer—40 mg once daily for 4–6 wk. Reduction of the risk of GI bleeding in critically ill patients—40 mg initially, then another 40 mg 6–8 hr later, followed by 40 mg once daily for up to 14 days. Gastric hypersecretory conditions—60 mg once daily initially; may be increased up to 120 mg 3 times daily (doses >80 mg/day should be given in divided doses); OTC—20 mg once daily for up to 14 days.
Oral (Children 1–16 yr and 5–9 kg) GERD/erosive esophagitis—5 mg once daily.
Oral (Children 1–16 yr and 10–19 kg) GERD/erosive esophagitis—10 mg once daily.
Oral (Children 1–16 yr and ≥20 kg) GERD/erosive esophagitis—20 mg once daily.

Availability (generic available)

Delayed-release capsules: 10 mg, 20 mgRx, OTC, 40 mg
Delayed-release powder for oral suspension peach-mint: 2.5 mg/packet, 10 mg/packet
In combination with: metronidazole and clarithromycin in a compliance package (Losec 1-2-3 M); with amoxicillin and clarithromycin in a compliance package (Losec 1-2-3-A) (both in Canada only); with sodium bicarbonate (Zegerid [OTC]; see combination drugs).

Nursing implications

Nursing assessment

  • Assess patient routinely for epigastric or abdominal pain and frank or occult blood in the stool, emesis, or gastric aspirate.
  • Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of pseudomembranous colitis. May begin up to several weeks following cessation of therapy.
  • Lab Test Considerations: Monitor CBC with differential periodically during therapy.
    • May cause ↑ AST, ALT, alkaline phosphatase, and bilirubin.
    • May cause serum gastrin concentrations to ↑ during first 1–2 wk of therapy. Levels return to normal after discontinuation of omeprazole.
    • Monitor INR and prothrombin time in patients taking warfarin.
    • May cause hypomagnesemia. Monitor serum magnesium prior to and periodically during therapy.

Potential Nursing Diagnoses

Acute pain (Indications)

Implementation

  • Do not confuse Prilosec (omeprazole) with Prozac (fluoxetine) or Pristiq (desvenlafaxine). Do not confuse omeprazole with fomepizole.
  • Oral: Administer doses before meals, preferably in the morning. Capsules should be swallowed whole; do not crush or chew. Capsules may be opened and sprinkled on cool applesauce, entire mixture should be ingested immediately and followed by a drink of water. Do not store for future use.
    • Powder for oral suspension: Administer on empty stomach, as least 1 hr before a meal. For patients with nasogastric or enteral feeding, suspend feeding for 3 hr before and 1 hr after administration. Empty packet contents into a small cup containing 1–2 tablespoons of water. Do not use other liquids or foods. If administered through a nasogastric tube, suspend in 20 mL of water. Stir well and drink immediately. Refill cup with water and drink again.
    • May be administered concurrently with antacids.

Patient/Family Teaching

  • Instruct patient to take medication as directed for the full course of therapy, even if feeling better. Take missed doses as soon as remembered but not if almost time for next dose. Do not double doses.
  • May cause occasional drowsiness or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
  • Advise patient to avoid alcohol, products containing aspirin or NSAIDs, and foods that may cause an increase in GI irritation.
  • Advise patient to report onset of black, tarry stools; diarrhea; abdominal pain; or persistent headache to health care professional promptly.
  • Instruct patient to notify health care professional of onset of black, tarry stools; diarrhea; abdominal pain; or persistent headache or if fever and diarrhea develop, especially if stool contains blood, pus, or mucus. Advise patient not to treat diarrhea without consulting health care professional.
  • Advise female patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Decrease in abdominal pain or prevention of gastric irritation and bleeding. Healing of duodenal ulcers can be seen on x-ray examination or endoscopy.
  • Decrease in symptoms of GERD and erosive esophagitis. Therapy is continued for 4–8 wk after initial episode.

Losec

A brand name for OMEPRAZOLE.
References in periodicals archive ?
En la LOSEC se senala que las empresas comunales seguiran las fases del ciclo productivo comunal, las que "deberan estar avaladas y previamente aprobadas por la respectiva instancia del Poder Popular, en articulacion con los integrantes de la organizacion socio productiva" (LOSEC, articulo 27)
Secondly, it criticised AZ for having withdrawn marketing authorisations for Losec in Denmark, Sweden and Norway in order to make the marketing of generic medicinal products more difficult and to prevent parallel imports.
Naturally, the generic drug manufacturers had their eyes on the market, eagerly looking forward to the expiration of the Losec patent.
A complaint was first made to the European Commission in 1999 that AstraZeneca were abusing European competition law in obtaining extension of their patent protection for Losec and denying market access to generic equivalents by various means.
Commission powers allow for fines against big companies guilty of impeding fair competition and an inquiry found that from 1993 until 2000, AstraZeneca breached EU competition rules 'by blocking or delaying the market access for generic versions of Losec and preventing parallel imports of Losec'.
Losec pioneered a new generation of medicines to treat stomach ulcers and other acid-related diseases - so-called proton pump inhibitors.
The European Commission said today (31 July) that preliminary findings suggested that the Anglo-Swedish pharmaceutical group AstraZeneca could have misused the patent system and other regulatory procedures for the marketing of its product Losec.
The company is likely to have been impacted by the launch in December of a generic version of key ulcer drug Losec in the United States and the unwinding of one-off buying patterns seen in the third quarter.
That said, this year does have its challenges, most notably in the form of the loss of patent protection for its wonder drug Losec.
Bentley's Omeprazole Belmac is the generic version of AstraZeneca's Prilosec and Losec brands, the largest-selling drug product worldwide.
Shares were already trading low, he added, due to market pessimism about the imminent expiry of key patents for the anti-ulcer drug Losec.
They are proton pump inhibitors or PPIs such as Losec and Zoton which may need to be taken long-term.