INSTRUCTION

for medical use of the preparation

LOCID 20 

 

Composition.

Active substance: omeprazole;

1 capsule contains omeprazole 20 mg;

Auxiliary substances: corn starch, sucrose, spherical sugar, magnesium carbonate, talc, sodium phosphate, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, methacrylic acid copolymer (1:1), polyethylenglyol 6000, colloidal silicon dioxide, sodium hydroxide, titanium dioxade Е171.

Medicinal form. Capsules.
Pharmacotherapeutical group.  Drugs for treatment of peptic ulcer. Proton pump inhibitors. Omeprazole. АТС code А02В С01

Clinical characteristics. 

Indications.

• peptic gastric ulcer;
• peptic duodenal ulcer;
• gastroesophageal reflux disease (GERD);
• chronic gastritis with increased acid-forming function of the stomach in the acute stage;
• functional dyspepsia;
• for eradication of Helicobacter pylori (in combination with antibacterial agents);
• Zollinger-Ellison syndrome.

Contraindications.

Hypersensitivity to the components of the preparation; pregnancy and lactation. It is not recommended to indicate the preparation to children under 12 years old.

Way of introduction and doses. 

The preparation is used in adults and children over 12 years old internally:

• peptic gastric ulcer in case of absence of Helicobacter pylori – 1 capsule twice a day for 2 – 4 weeks;
• peptic duodenal ulcer in case of absence of Helicobacter pylori – 1 capsule twice a day for 2 – 6 weeks;
• GERD - 1 capsule twice a day for 4 – 8 weeks; supportive therapy for GERD - 1 capsule once a day for up to 12 months;
• chronic gastritis with increased acid-forming function of the stomach in the acute stage - 1-2 capsules a day for 2 – 3 weeks;
• functional dyspepsia - 1-2 capsules a day for 2 – 3 weeks;
• for eradication of Helicobacter pylori – 1 capsule twice a day (in combination with antibacterial agents (amoxicilline, clarithromycin, tetracycline, furasolidone, metronidazole) and bismuth preparations);
• Zollinger-Ellison syndrome – the initial dose of the preparation is 3 capsules a day, the dose is increased if necessary;the dose is adjusted individually.

Side effects.

In case of short-term use of the preparation side effects occur rarely. They are usually low-grade and of short duration. Severe side effects appear very seldom.

Changes from the side of skin: seldom – rash and/or itching. In single cases there appears inhenced photosensitivity, erythema multiforme, alopecia. 

Disturbance from the side of musculoskeletal system: In single cases – pain in muscles and ligaments, muscle weakness, pain in joints.

From the side of the central and peripheral nervous system:  headache, seldom - giddiness, paresthesia, sleepiness, insomnia, vertigo. In single cases – reversible syncope, agitation, depression or hallucination.

Gastro-intestinal disorders: diarrhea, constipation, abdominal pain, nausea, vomiting and flatulence. In single cases – dry mouth, stomatitis andgastro-intestinal candidosis. 

Disturbance from the side of liver: seldom – increase of the level of liver enzymes. In single cases – encephalopathy at severe diseases of liver, hepatitis. 

Disturbance from the side of endocrine system: In single cases – hyponatremia.

Disturbance from the side of blood-vascular system and lymphatic system: In single cases -  thrombocytopenia, eukopenia, agranulocytosis and pancytopenia. 

Other: seldom – general weakness. Allergic reactions: urticaria (seldom), in single cases – Quincke's edema, fever, bronchospasm, interstitial nephritis, anaphylactic shock. In single cases – excessive sweating, periferal edema, impaired sight, taste abnormality, decrease of sodium concentration in blood.

Overdose. 

In case of Locid 20 overdose there appear symptoms typical for its side effects. Omeprazole in day dose of 360 mg is well tolerated. All symptoms observed in the context of omeprazole overdose have short-termed character. 

There is no specific antidote. Omeprazole binds to the blood plasma proteins, and consequently slowly excretes during dialysis. In case of overdose there should be taken measures for excretion of unabsorbed omeprazole from the gastro-intestinal tract, the treatment is symptomatic and supportive.
Use in pregnancy and lactation.

Omeprazole can be used during pregnancy and lactation only in case of clinical need and when the potential benefit prevails over the risk for the fetus.

Omeprazole is excreted in breast milk, so the therapy with the preparation is indicated by the doctor. If the treatment is important for the mother, the breast-feeding is discontinued.

Children.

The preparation is contraindicated for children under 12 years old.
Peculiarities of administration.  

When indicating Locid 20 to gastric ulcer patients it is necessary to exclude the possibility of malignant disease as omeprazole can mask its symptoms and postpone the diagnosis.  

The preparation should be taken before meals. 

The ability to influence the reaction time when driving and working with other mechanisms.

There are no reports about influence of the preparation on the ability to drive and operate machines.

Interaction with other drugs and other forms of interaction.  

Locid 20 can prolong the half-life and the duration of the activity of the preparations metabolized in liver via oxidation with participation of cytochrome Р450 enzyme systems. Omeprazole can increase the concentration in blood plasma of diazepam, phenytoin, nifedipine, warfarin, aminopyrine, disulfiram.  As a rule, when omeprazole is used in recommended doses, such increase is not clinically significant. However, it is recommended to control the state of the patient at the beginning of the treatment and after it, adjust the dose of the preparation, if needed.

When used concomitantly omeprazole and clarithromycin have increased plasma concentrations.

Omeprazole can prevent the assimilation of medicinal preparations in those cases when the acidity of the stomach medium is the important factor for their bioavailability.. 

As a result of decreased stomach acidity the absorbtion of ampicillin, ketoconazole and iron preparations may change.

When used concomitantly antacids, amoxicillin, digoxin, theofillin, lidocaine, quinidine, metoprolol do not demonstrate clinically significant interaction.

Pharmacological properties. 

Pharmacodynamics. Omeprazole is a specific proton pump inhibitor of parietal mucous cells of the stomach. After intake it causes the reversible inhibition of gastric juice secretion. Omeprazole, a racemate blend of two active enantiomers, decreases acidic gastric secretion by the mechanism of acting on the targets.

Omeprazole is a weak base that is concentrated and turns into an active form in strong-acidic medium of the intracellular longitudinal coombs of the parietal cells, where it inhibits enzyme Н+/К+-ATPase – proton pump.

This influence on the final stage of the acid-forming is dose-dependent and provides highly effective inhibition both basal and stimulated acid secretion irrespective of the stimulus type.

Oral intake of omeprazole causes quick and effective inhibition of acid secretion both during the day and at night. The maximal effect is achieved in 4 days of treatment.

In duodenal ulcer patients mean inhibition of acidic gastric secretion by 80 % is achieved in 24 hours. In 24 hours after omeprazole intake, the decrease of peak acid production after stimulation with pentagastrine is approximately 70 %.

Due to the decrease of acid secretion and intragastric acidity by omeprazole in gastrointestinal reflux patients the time of acid action in esophagus decreases and normalizes in double-dependent way.

Inhibition of acid secretion is tightly connected with omeprazole AUC, but not with its plasma concentration at the certain period of time.

During treatment with omeprazole tachyphylaxis has not been observed. 

70-95 % of all peptic ulcer patients, including duodenal ulcer and gastric ulcer, were infected by Helicobacter pylori. Eradication of Helicobacter pylori with omeprazoleу in combination with antibiotics causes quick relief of the symptoms, high frequency of healing of any mucus damages and long-term remission of digestive ulcers. It also decreases the level of complications, as well as gastro-intestinal bleedings.

Decreased acidity in the stomach usually may increase the index of intragastric bacteria. The use of compounds that inhibit acid-forming may somewhat increase the risk of gastrointestinal salmonellosis and/or Helicobacter infections.

Pharmacokinetics. 

Usually omeprazole is absorbed in small intestine during 3-6 h. Systemic bioavailability of the single oral dose is nearly 35 % and increases up to 60 % after repeated daily intake. Concomitant food intake does not influence the bioavailability.

Binding of omeprazole with plasma proteins is about 95 %. In elderly patients and those with liver dysfunction the volume of distribution is somewhat decreased.

Omeprazole is metabolized mainly in liver with cytochrome Р450 enzyme system. The main volume of the exchange is done by polymorphous specific isoforms CYP2C19 (S- mephenytoin hydroxylase). They are responsible for formation of hydroximeprasole – the main plasma metabolite. Due to the fact that omeprazole inhibits competitively CYP2C19, there is a risk of metabolic interaction of omeprazole and other substances metabolized with the help of CYP2C19. This risk increases in people having low level of CYP2C19 (“mephenytoin polymorphism”; 3-5 % of Asian race individuals).

None of the metabolites influences the acidic secretion.

70-80 % of taken oral dose is excreted in metabolized form with urine, the other part – with bile and faeces. 

Omeprazole half-life of from plasma is usually less than one hour and does not change during long-term treatment.

General plasma clearance is within 0.3 and 0.6 l/min. 

Systemic bioavailability in patients with renal dysfunction doe not change, the excretion slows proportionally to the decrease of creatinine clearance.

In patients with hepatic dysfunction AUC (area under the curve “concentration - time”) increases. However, at the dose regimen of once a day it does not cause the accumulation of omeprazole.

Pharmaceutical characteristics.

Main physical and chemical properties: hard gelatine capsules with grey frame and pink cup, content of capsules – white or nearly white pellets (granules).

Shelf life: 3 years.

Storage conditions. Keep out of the reach of children in dry place at temperature below 30єC. 

Packing. 10 capsules in a blister; 10 blisters in a carton.  

Manufacturer. Flamingo Pharmaceuticals Ltd.

Legal address. Flamingo Pharmaceuticals Ltd. 7/1, Corporate Park, Sion-Trombai Road, Chembur, Mumbai – 400071, India.

Name and address of the marketing company.

 Ananta Medicare Ltd.

Suite 1, 2 Station Court, Imperial Wharf, Townmead Road, Fulham, London, United Kingdom.

Category of dispensing. On prescription.