Optirel
Esomeprazole 40 mg
DESCRIPTION
OPTIREL Capsules in anenteric-coated pellet formulation of Esomeprazole Magnesium trihydrate due to its acidlabile nature. Esomeparazole (OPTIREL) is the S-isomer of omeprazole, whichinhibits the gastric acid secretion more effectively than omeprazole, which inhibits the gastric acid secretion more effectively than omeprazole. Chemically Esomeprazole is bis(5-methoxy-2-[(S)]-[4-methoxy-3, 5-dimethyl-2-pyridinyl)methyl] suifinyl]-1h- benzimidazole-1-yl) magnesium trihydrate. Esomeprazole (OPTIREL) acts by binding irreversibly to the H/K AT Pas in the
PHARMACOKINETICS
pEAK PLASMA LEVELS OF eSOMEPRAZOLE (OPTIREL) are achieved approximately after 1.5 hour of oral administration. At repeated once daily dosing with 40mg. the systemic bio-availability in approximately 90% compared to 64% after a single dose of 40mg. Esomeprazole is 97% bound to plasma proteins. Esomeprazole is extensively metabolized in the liver by the cytochome P450 (CYP)enzyme system. The metabolites of Esomeprazole lack anti-secretory activity. The plasma elimination half life of Esomeprazole is approximately 1 to 1.5 hour less than 1% of parent drug is excreted in the urine approximately 80% of oral dose of Essomeprazole is excreted as inactive metabolites in the urine and the
INDICATIONS: OPTIREL (Esomeprazole) is indicated for.
- Gastroesophageal Reflux Disease (GERD).
- Symptomatic treatment of Gastroesophageal Refulx Disease (GERD) without Esophagitis.
- Treatment of Erosive Retube Esophagitis.
- Long-term management of patients with healed esophagitis to prevent relapse.
- As triple therapy OPTIREL plus Amoxycillin and Clarithromycin for the treatment of patients with H.pylri infection and duodenal ulcer disease (active or history of within the past 5 year).
- Healing of duodenal ulcer associated with helicobacter pylori infection.
- Prevention of relapse of peptic ulcers in patients with helicobacter pylori asociated ulcers.
CONTRAINDICATIONS
OPTIREL (Esomeprazole) is contraindicated in patients with known hypersensitivity to any component of the formulation or to substituted benzimidazoles.
POSSIBLE ADVERSE EFFETS
The most frequently occurring adverse effects with OPTIREL (Esomeprazole) therapy include, diarrhea, nausea, flatulence, abdominal pain, constipation and dry mouth. Other side effects include Cardiovascular: Hypertension & tachycardia Gastrointestinal: Stomatitis and gastrointestinal candidiasis. Nervous System/Psychiatric: Confusion, depression, dizziness, nervousness, insomnia, parenthesis, somnolence, vertigo, agitation, aggression & hallucination. Endocrine: Gynaecomastia. Hematologic Leukopenia, thrombocytopenia, agranulocytosis & pancytopenia. Hepatic: increased liver enzymes, hepatitis with or without jaundice & hepatic failure. Dermatologic: Rash, photosensitivity, toxic epidermal necrolysis (TEN). Stevens-Johnson syndrome, erythema multiform & alopecia, Besides these other adverse effects include malaise, hypersensitivity reaction like fever, bronchospasm, interstitial nephritis, increased sweating peripheral edema, blurred
DRUG INTERACTIONS
- Co-administration of Esomeprazole decreases the absorption of ketoconazole & intraconazole due to decreased intragastric acidity during treatment with esomeprazole.
- Co-administration of Esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the levels of esomeprazole and 14 hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major esomeprazole metabolizing enzyme, so co-administration of esomeprazole with other drugs metabolized by CYP2C19 enzyme such as diazepam, citalopram, imipramine clomipramine, phenytoin, etc., results in increase plasma concentration of these drugs & needs reduction of such drugs.
WARNINGS
Use in pregnancy: there are no well-controlled and adequate studies in pregnant women. Esomeprazole should be used during pregnancy, only if clearly needed Use in Lactation: Esomeprazole is likely to be excreted in human milk, so Esomeprazole should be used only if clearly needed. Pediatric Use: Safety & effectiveness of the drug has not been established in pediatric patients. Use in Elderly: No dosage adjustment required in elderly patients. Use in Renal Failure: In cases of severe renal failure the drug should be used with caution. Use in Hepatic Failure: Since the drug is extensively metabolized by hepatic cytochromic enzymes, so the drug should be used with caution in
DOSAGE AND ADMINISTRATION
OPTIREL Capsules should be swallowed whole and should be taken at least one hour before meals. Adult dosage guidelines for OPTIREL (Esomeprazole) Capsules are given below:-
RECOMMENDED ADULT DOSAGE GUIDELINES:
- Gastro esophageal Reflux Disease (GERD) 20-40 mg Once daily for 4-8 weeks (An additional 4-8 weeks treatment may be considered if symptoms persist or esophagitis does not heal).
- Maintenance of healing erosive esophagitis 20 mg Once daily (controlled studies do not extend beyond 6 months).
- Symptomatic treatment of Gastro esophageal Reflux Disease (GERD) without Esophagitis 20-40 mg Once daily for 4 weeks (An additional 48 weeks treatment may be considered if symptoms persist and do mot resolves completely).
- H.Pylori eradication to reduce the risk of duodenal ulcer reoccurrence 40 mg Once daily for 10 days.
- The drug should be sold/used under strict medical supervision/advice.
STORAGE PRECATUIONS
Store in a cool, dry place below 30°C. Keep al medicine out of the reach of children
PRESENTAION
OPTIREL Capsules 20 & 40mg are available in packing containing 14 capsules. Respectively.