Bioprazol

(Omeprazolum)
Hard gelatine capsules, 20 mg

Composition of the drug

One capsule of a white colour contains 20 mg of omeprazole in form of granules for inestinal absorption and the following excipients: sucrose, glucose, lactose, starch, hydroxypropylmethylcellulose, hydroxypropylcellulose, hydroxy-propylmethylcellulose phthalate, dibasic sodium phosphate, sodium laurylsulfate, diethyl phthalate and in the external part, gelatine and titanium dioxide

Mode of action

The Bioprazol^® preparation contains omeprazole that inhibits activity of the proton pump (H+/K+?ATP-ase), responsible for both principal and stimulated secretory action of parietal cells of the stomach mucous membrane. By inhibiting secretion of the gastric juice, that is acidic, the drug raises pH of the stomach content and prevents irritation of the mucous membrane of the gastrointestinal tract by acids. Omeprazole does not act on acetylcholine and histamine receptors. It is absorbed in the small intestine. 95 % of the active ingredient binds to the plasma proteins. The drug is metabolised in the liver and excreted mostly with urine, and to a lesser extend - with the faeces. Half-life time of omeprazole in the organism is approximately 1.5 hour. A single dose of omeprazole inhibits secretion of hydrochloric acid in the stomach for approximately 24 hours.

Indication to use

• chronic peptic ulcer disease of the stomach and/or duodenum, also co-existing with a Helicobacter pylori infection,

• reflux oesophagitis,

• Zollinger ? Ellison syndrome.

Counter-indications

Hypersensitivity to omeprazole or other constituents of the preparation.

Warnings and recommended precautions

Because the treatment with omeprazole can relieve symptoms of the stomach cancer and therefore, cause a delay in diagnosing the stomach cancer, the neoplastic nature of the disease has to be excluded before initiating the treatment of an ulcer disease.
In patients with liver insufficiency the daily dose of the drug should be reduced due to possible increase of concentration of the drug in the blood serum and extension of its half-life time.
Renal insufficiency does not significantly affect blood concentration of the drug thus no dosage adjustment is necessary.
Tobacco smoking is a reason of lower efficacy of the therapy.

Using the drug in pregnancy and lactation

In pregnancy, the Bioprazol^® preparation may be used only in cases, when according to the doctor's opinion benefit for the mother supersedes a potential risk for the foetus.
Using the drug by breast-feeding mothers is not recommended.

Influence of the drug on ability to drive vehicles, operate machines and psychophysical aptitude

Omeprazole does not impair psychophysical aptitude, does not affect ability to drive mechanical vehicles and operate machines.
The patients should exercise caution due to possible adverse reactions such as dizziness and blurred vision.

Interactions with other drugs

Oeprazole is metabolised in the liver with participation of the cytochrome P 450. Therefore, interaction with certain drugs is a potential risk. Omeprazole can reduce elimination rate of diazepam, phenytoin and varfarine. Monitoring patients taking varfarine, phenytoin or diazepam and dosage reduction, if necessary, is recommended. Simultaneous administering omeprazole and clarithromycin increases concentration of these drugs in blood serum and therefore, it is applied in treating Helicobacter pylori infections. There is a report concerning an increase of digoxine concentration in blood by 10% in case of simultaneous administration of omeprazole.
No interactions with other drugs, in particular with the drugs neutralising the gastric juice and with non-steroidal anti-inflammatory drugs.
Omeprazole can affect bioavailability of the drugs, absorption of which depends on pH of the gastric juice, such as ketoconazole?, ampicylin esters and iron salts.
Decrease of ketoconazole absorption resulted from a change of pH in the stomach was observed during omeprazole therapy.

Dosage and method of application

• Chronic peptic ulcer disease of the duodenum or stomach and reflux oesophagitis: the recommended dose of omeprazole is 20 mg (1 capsules) once per day for 4 weeks. In case of insufficient response to the therapy in some patients (e.g. in tobacco smokers) the therapy should be extended up to 8 weeks.

• Zollinger ? Ellison syndrome: the treatment should begin with a dose of 60 mg once per day. Further treatment should be decided individually according to the patient?s response. In some patients with intensive symptoms, weakly responding to other method of treatment, a standard supportive treatment with a dose of 20 mg to 120 mg per day could be efficient. In case of dosage exceeding 80 mg per day omeprazole should be given in two divided doses.

• Helicobacter pylori infections: a three-component therapy is applied in treating infections caused by Helicobacter pylori bacteria. It involves simultaneous administration of 40 mg of omeprazole once per day or 20 mg twice daily and:

- clarithromycin (250 mg two times per day) and metronidazole (400 mg two times per day) for 1 week; or

- amoxyciline (500 mg three times per day) and metronidazole (400 mg three times per day) for 1 week.

In a two-component therapy of a Helicobacter pylori infection omeprazole is administered in a dose of 40 mg once per day or amoxyciline (20 mg two times per day) and clarithromycin in a dose of 500 mg three times per day or amoxyciline in a dose of 750 to 1000 mg two times per day for 2 weeks.

Children

The Bioprazol^® preparation may not be given to children up to 4 years of age. If it is necessary to give the drug to children over 4 years of age with reflux oesophagitis, recommended dosage is as follows:

• children of the body weight from 10 kg to 20 kg ? 10 mg,

• children of the body weight over 20 kg ? 20 mg.

Senile patients

No dosage adjustment is necessary for the older patients.

Patients with hepatic failure

Bioavailability of omeprazole and half-life of the drug in the plasma are increased in patients with hepatic failure. Therefore, the drug is administered in doses from 10 to 20 mg per day.

Patients with renal insufficiency

There is no need of dosage adjustment in patients with renal insufficiency.

Mode of application

The capsule should be swallowed as a whole. Patients with swallowing disorders should open the capsule and suspend its content in e.g. fruit juice or in any other acidic liquid and drink the suspension.
Before swallowing the capsule, it should not be chewed or crushed.

Overdosage

Single cases of omeprazole overdosage in humans were reported. In a single dose of 160 mg the drug was well tolerated.
Observed symptoms of overdosage were: blurred vision, disorientation, drowsiness, excessive perspiration, reddening of the face, headache, nausea, vomiting, dryness in mouth, tachycardia. The symptoms were of transient nature

Adverse reactions

The drug is well tolerated. Adverse reactions, if observed, are mild and transient. The following disorders were reported during taking omeprazole:

• gastrointestinal system: diarrhoea, constipation, flatulence, pain in the epigastrium, nausea, vomiting, dryness in mouth, yeast infections in the mouth and in the gastrointestinal tract,

• osteo-muscular system: muscular and articular pains, weakness of muscles,

• central nervous system: headache and dizziness, irritability, anxiety, agitation or apathy, paraesthesia, drowsiness, insomnia, balance disorders,

• skin: rash, urticaria, erythema multiforme, hair loss, Stevens and Johnson syndrome, Lyell syndrome,

• urinary system: inflammation of urinary tract, interstitial inflammation of kidneys, haematuria, proteinuria,

• liver: increase of activity of hepatic enzymes, hepatitis with or without jaundice, encephalopathy in patients diagnosed with a severe hepatic failure before the treatment, hepatic insufficiency,

• hormone system: gynaecomastia,

• circulatory system: a decrease of the count of neutrophilic lymphocytes (neutropenia), reduction of blood platelets (thrombocytopenia), lack of granulocytes (agranulocytosis), aplastic anaemia, decrease of the count of all blood cells (pancytopenia),

• other: hypersensitivity to light, ill-being, hypersensitivity, acute circumscribed oedema, fever, bronchospasm, anaphylactic shock), blurred vision, taste disorders, hyponatraemia.

Furthermore, sporadic cases of bradycardia and tachycardia, blood pressure increase were reported.

Any connection of the above specified symptoms with the use of omeprazole is not unequivocally proven.

Available packaging

Plastic containers comprising 14 or 28 capsules.