Esopep leaflets

ESOPEP Capsules (20, 40mg)
Esomeprazole Magnesium Trihydrate Pellets (Vision Specs.)
COMPOSITION: Each capsule contains:
Esomeprazole Magnesium Trihydrate Pellets eq. To Esomeprazole
(Vision Specs.) .20 & 40 mg respectively.
DESCRIPTION: ESOPEP Capsule in an enteric-coated pellet formulation of esomeprazole Magnesium due to
its acid labile nature. Esomeprazole (ESOPEP) is the S-isomer of omeprazole, which inhibits the gastric acid
secretion more effectively than omeprazole. Chemically esomeprazole is bis (5-methoxy-2-[(S)-[(4-methoxy-3,
5-dimethyle-2-pyridinyl) methyl] sulfinyl] 1H-benzimidazole-1-y) magnesium trihydrate. Esomeprazole
(ESOPEP) acts by binding irreversibly to the H /K ATPase in the proton pump, which dramatically decrease the
secretion of HCI in the stomach & alters gastric pH.
PHARMACOLOGY: Peak plasma levels of Esomeprazole (ESOPEP) are achieved approximately after 1.5
hours of oral administration. At repeated once daily dosing with 40 mg. The systemic bioavailability is
approximately 90% compared to 64% after a single dose of 40 mg. Esomeprazole is 97% bound to plasma
proteins. Esomeprazole is extensively metabolized in the liver by the cytochrome P450. (CYP) enzyme system.
The metabolites of esomeprazole lack antisecretory activity. The plasma elimination half life of esomeprazole is
approximately 1-1.5 hours Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral
dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive
metabolites in the feces.
INDICATIONS: ESOPEP (Esomeprazole) is indicated for:
Gastroesophageal Reflux Disease GERD.
Treatment of Erosive Reflux Esophagitis.
Long-term management of patients with healed esophagitis to prevent relapse.
Symptomatic treatment of Gastroesophageal Reflux Disease (GERD) without Esophagitis.
As triple therapy Esomeprazole plus Amoxycillin and Clarithromycin for the treatment of patients with H, pylori infection and duodenal ulcer disease (active or history of within the past 5 years).
Healing of duodenal ulcer associated with helicobacter pylori infection.
Prevention of relapse of peptic ulcers in patients with helicobacter pylori associated ulcers.
CONTRAINDICATIONS: ESOPEP (Esomeprazole) is contraindicated in patients with known hypersensitivity to
any content of the formulation or to substituted benzimidazoles.
POSSIBLE ADVERSE EFFECTS: The most frequently occurring adverse events with 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, paresthesia,
somnolence, vertigo, agitation, aggression & hallucinations Endocrine: Gynaecomastia. Haemotologic:
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 multiforme & alopecia. Besides these, other adverse effects
include malaise, hypersensitivity reactions like fever, bronchospasm, interstitial nephritis, increased sweating,
peripheral edema, blurred vision, taste disturbance & hyponatraemia.
DRUG INTERACTIONS:
Co-administration of Esomeprazole decreases the absorption of ketoconazole & itraconazole due to decreased intragastric acidity during treatment with esomeprazole.
Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increase in the levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major esomeprazole metabolizing enzyme, so coadministration of esomeprazole with other drugs metabolized by CYP2C19 enzyme such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc, results in increased plasma concentration of these drug & needs dose reduction of such drugs.
WARNINGS: Use in Pregnancy: There are no well-controlled & 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 patients with hepatic insufficiency.
DOSAGE AND ADMINISTRATION: ESOPEP Capsules should be swallowed whole and should be taken at
least one hour before meals. Adult dosage guidelines for ESOPEP (Esomeprazole) Capsules are given in table
below.
RECOMMENDED ADULT DOSAGE GUIDELINES
INDICATIONS
FREQUENCY
Once daily for 4-8 weeks (An additional 4-8 week treatment may be considered if symptoms persist or esophagitis does not heal).
Maintenance of healing erosive esophagitis Symptomatic treatment of Gastroesophageal Once daily for 4 weeks (An additional 4-8 Reflux Disease (GERD) without Esophagitis week treatment may be considered if symptoms persist or do not resolve completely).
H-pylori eradication to reduce the risk of The drug should be used under strict medical supervision.
PRESENTATION: ESOPEP Capsules 20 & 40 mg are available in packing containing 2x7 capsules,
respectively.
Complete Medical Information available only for doctors on-request.
ISO 9001 : 2000 Certified Company
Manufactured for:
Plot No.: 204-205, Industrial Triangle,Kahuta Road, Islamabad-Pakistan.

Source: http://www.globalpharmaceuticalspk.com/pdf/Esopep%20Leaflet.pdf