Treatment of symptoms of gastroesophageal reflux (eg heartburn and acid reflux) in adult patients.
Composition:
1 capsule contains 20 mg of Omeprazole (and 163 mg of sucrose and 8 mg of lactose).
Action:
Omeprazole, which is a racemic mixture of two enantiomers, is a specific inhibitor of the proton pump (H+/ K+ ATPase) in the parietal cells of the gastric mucosa. It reduces the secretion of hydrochloric acid in the stomach, both basal and stimulated. Omeprazole is not stable in an acidic environment and is therefore administered orally in the form of capsules filled with coated pellets. Absorption of omeprazole is rapid and Cmax occurs about 1-2 hours after administration. The bioavailability of omeprazole after a single oral administration is approximately 40%. Multiple administration once a day increases the bioavailability to about 60%. Omeprazole binds to plasma proteins in approximately 97%. It is completely metabolised by the cytochrome P450 system, mainly CYP2C19 (to hydroxyomeprazole) and partly by CYP3A4 (to the omeprazole sulfone). Almost 80% of an orally administered dose is excreted as metabolites in the urine; the remaining part with faeces. T0,5 is <1 h. In patients with hepatic impairment the metabolic rate is reduced. In slow metabolisers (who do not have active CYP2C19 isoenzyme), the mean AUC is 5-10 times higher than in fast metabolisers (those with active CYP2C19 isozymes), mean C valuesmax they are also 3-5 times larger; however, these data do not give any consequences regarding the dosage of omeprazole.
Contraindications:
Hypersensitivity to the active substance, substituted benzimidazoles or any of the excipients. Do not use with nelfinavir.
Precautions:
In patients with suspected or diagnosed peptic ulcer disease, as well as any disturbing symptoms (eg, significant unintentional weight loss, recurrent vomiting, swallowing difficulties, bloody vomiting or tarry stools), the cancerous background of the disease should be excluded, as omeprazole treatment may alleviate the symptoms of cancer and delay its diagnosis. Patients should be advised to report the following cases: history of peptic ulcer or gastrointestinal surgery; treatment of dyspepsia or heartburn symptoms that have lasted for more than 4 weeks; jaundice, liver dysfunction or disease; onset of new symptoms or change in the nature of previously observed symptoms in patients> 55 years. Patients with long-term recurrent symptoms of indigestion or heartburn should undergo regular medical check-ups. Do not use omeprazole preventively. Treatment with omeprazole may cause a slight increase in the risk of gastrointestinal infections with such bacteria asSalmonella spp. And Campylobacter spp. Omeprazole, as a CYP2C19 inhibitor, may interact with drugs metabolised by this isoenzyme - be careful. Co-administration of omeprazole and Clopidogrel should be avoided. The use of omperazole with atazanavir is not recommended (reduction of atazanavir exposure). Due to the content of sucrose and lactose, the drug should not be used in patients with fructose or galactose intolerance, sucrase-isomaltase deficiency or Lapp lactase deficiency, malabsorption of glucose-galactose.
Pregnancy and lactation:
The preparation can be used during pregnancy. Omeprazole passes into breast milk, but there is no risk of adverse effects on the child when using the drug at therapeutic doses.
Side effects:
Common: headache, diarrhea, constipation, abdominal pain, nausea, vomiting, bloating. Uncommon: insomnia, dizziness, paresthesia, drowsiness, labyrinth-like dizziness, increased liver enzymes, dermatitis, pruritus, rash, urticaria, malaise, peripheral edema. Rare: leukopenia, thrombocytopenia, hypersensitivity reactions (e.g.fever, angioneurotic edema and anaphylactic reaction / shock), hyponatremia, agitation, confusion, depression, taste disorders, blurred vision, bronchospasm, dryness or inflammation of the oral mucosa, gastrointestinal candidiasis, hepatitis with or without jaundice, alopecia, hypersensitivity to light, joint pain, muscle pain, interstitial nephritis, increased sweating. Very rare: agranulocytosis, pancytopenia, hypomagnesaemia, aggression, hallucinations, hepatic failure, encephalopathy in patients with pre-existing liver disease, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, muscle weakness, gynecomastia.
Dosage:
Orally. Adults: 1 capsule once a day for 14 days. In order to achieve relief of symptoms, it may be necessary to use the medicine for another 2-3 days. In the majority of patients, heartburn disappears completely within 7 days. After complete relief of symptoms, treatment should be discontinued.Special groups of patients. No dosage adjustment is necessary for elderly patients or patients with renal impairment. The metabolism of omeprazole in patients with hepatic impairment is impaired, resulting in an increase in AUC; omeprazole does not tend to accumulate when given once a day.Way of giving. The drug should be taken in the morning, before a meal. The capsules should be swallowed whole with half a glass of water. Do not chew or crush capsules. In the case of patients with swallowing disorders, the capsule can be opened and dissolved in non-carbonated water, mixed with fruit juice or apple sauce. The prepared suspension should be drunk immediately (or within 30 minutes) and always stir immediately before drinking and drink half a glass of water. Do not mix with milk or sparkling water. Do not chew the pellets.
(C)
