* Adults. NSAID associated peptic ulceration: - Acute treatment: 150 mg twice daily for 8 to 12 weeks, or 300mg nocte.

Transcription

1 Trade Name Aciloc 75 mg & 300 mg Film-coated tablets Generic Name Ranitidine Composition Each Aciloc 300 mg film-coated tablet contains: - Active ingredient: Ranitidine hydrochloride 336 mg equivalent to 300 mg Ranitidine - Inactive ingredients: Croscarmellose sodium, Magnesium stearate, Microcrystalline Cellulose, Methocel E-15, Ethyl cellulose, Titanium dioxide, Green colour-s12947, Dibutyl phthalate, Docusate sodium. Each Aciloc 75 mg film-coated tablet contains: - Active ingredient: Ranitidine hydrochloride 84 mg equivalent to 75 mg Ranitidine Inactive ingredients: Croscarmellose sodium, Magnesium stearate, Microcrystalline Cellulose, Methocel E-15, Ethyl Cellulose, Titanium dioxide, Green colour-s12947, Dibutyl phthalate, Docusate sodium. Pharmaceutical form Film-coated Tablets Pharmacological action Ranitidine is a specific rapidly acting histamine H2-antagonist. It inhibits basal and stimulated secretion of gastric acid, reducing both the volume and the acid and pepsin content of the secretion. Ranitidine has a relatively long duration of action and so a single 75 mg dose effectively suppresses gastric acid secretion for 12 h. Pharmacokinetics Absorption: The bioavailability of oral ranitidine is consistently about 50% absorption of ranitidine after oral administration is rapid and peak plasma concentrations are usually achieved 2 hours after administration. Peak concentrations in plasma, normally in the range 300 to 550 nanograms/ml, occur 2 to 3 h after oral administration of a 150 mg dose. Concentrations of ranitidine in plasma are proportional to oral dose up to and including 300 mg. Metabolism: Ranitidine is not extensively metabolized. After oral dosing, 6% of the dose being excreted in urine as the N-oxide, 2% as the S-oxide, 2% desmethylranitidine and 1 to 2% as the furoic acid analogue. Elimination:

2 60-70% of an oral dose was excreted in urine and 26% in faeces. The elimination half-life is 2 to 3 h. Indications Aciloc 300 mg film-coated tablets are indicated for: - Duodenal ulcer and benign gastric ulcer, including that associated with non-steroidal antiinflammatory agents. - Prevention of non-steroidal anti-inflammatory drug (including aspirin) associated duodenal ulcers, especially in patients with a history of peptic ulcer disease. - Duodenal ulcer associated with Helicobacter pylori infection. - Post-operative ulcer. - Reflux oesophagitis. - Symptom relief in gastro-oesophageal reflux disease. - Zollinger-Ellison Syndrome. - Chronic episodic dyspepsia, characterized by pain (epigastric or retrosternal) which is related to meals or disturbs sleep. - Prophylaxis of stress ulceration in seriously ill patients. - Prophylaxis of recurrent hemorrhage from peptic ulcer. - Prophylaxis of Mendelsons syndrome. Aciloc 75 mg film-coated tablets are indicated for: Symptomatic relief and prevention of heartburn associated with consuming food and drink, indigestion, and hyperacidity. Dosage and administration # Aciloc 300 mg film-coated tablets: * Adults Duodenal ulcer and benign gastric ulcer: 150 mg twice daily or 300 mg nocte (at night), in most cases of duodenal ulcer or benign gastric ulcer healing occurs within 4 weeks. Healing usually occurs after a further 4 weeks in those not healed after the initial 4 weeks. - Long term: For the long-term management of duodenal or benign gastric ulcer the usual dosage regimen is 150 mg nocte, smoking is associated with a higher rate of duodenal ulcer relapse, and such patients should be advised to stop smoking. In those who fail to comply with such advice a dose of 300 mg nocte provides additional therapeutic benefit over the 150 mg dosage regimen. NSAID associated peptic ulceration: 150 mg twice daily for 8 to 12 weeks, or 300mg nocte. - Prophylaxis:

3 150 mg twice daily may be given concomitantly with non-steroidal anti-inflammatory drug therapy. Duodenal ulcers associated with Helicobacter pylori Infection: 300 mg before bedtime or 150 mg twice daily may be given with the oral amoxicillin 750 mg three times daily and, metronidazole 500 mg three times. Postoperative ulcer: 100 mg twice daily, most cases heal within 4 weeks, extended for another 4 weeks for those not fully healed. Gastro-Oesophageal Reflux Disease: 150 mg twice daily or 300 mg nocte is administered for up to a period of 8, or if necessary, 12 weeks. In patents with moderate to severe oesophagitis, the dosage of Aciloc may be increased 150 mg four times daily for up to 12 weeks. - Long-term management: 150 mg twice daily. - Symptom relief: 150 mg twice daily for two weeks. This regimen may be continued for a further two weeks in those patients in whom the initial response is inadequate. Zollinger-Ellison syndrome: 150 mg three times daily, but this may be increased as necessary. Doses up to 6 grams per day have been well tolerated. Chronic episodic dyspepsia: 150 mg twice daily for up to 6 weeks. Anyone not responding or relapsing shortly afterwards should be investigated. Prophylaxis of Mendelsons syndrome: 150 mg 2 hours before anaesthesia, and preferably 150 mg the previous evening. In obstetric patients in labor 150 mg every 6 h. Prophylaxis of hemorrhage from stress ulceration in seriously ill patient: 150 mg twice daily may be substituted for the injection once oral feeding commences. * Renal Impairment: In patients with creatinine clearance less than 50 ml /min, it is recommended that the orally dose of Aciloc should be 150 mg/day. # Aciloc 75 mg film-coated tablets:

4 * Adults (including elderly) and children 16 years of age and older: Swallow one Aciloc 75 mg tablet whole, with a drink of water, as soon as you have symptoms. If symptoms persist for more than one hour or return, take another tablet. For prevention of acid indigestion, indigestion, hyperacidity and heartburn associated with consuming food and drink, swallow one tablet with water, half to one hour beforehand. Contraindications Aciloc is contra-indicated in patients known to have hypersensitivity to any component of the preparation. Side effects The following convention has been utilized for the classification of undesirable effects: very common (> 1/10), common (> 1/100, < 1/10), uncommon (> 1/1000, < 1/100), rare (> 1/10,000, < 1/1000), very rare (< 1/10,000), adverse event frequencies have been estimated from spontaneous reports from post-marketing data. - Very rare: Blood count changes (leucopenia, thrombocytopenia). These are usually reversible. Agranulocytosis or pancytopenia, sometimes with marrow hypoplasia or marrow aplasia, anaphylactic shock, Depression, Reversible mental confusion, hallucinations, Headache (sometimes severe) and dizziness, Reversible involuntary movement, Reversible blurred vision, Vasculitis, Diarrhoea, Acute pancreatitis, Hepatitis (hepatocellular, hepatocanalicular or mixed) with or without jaundice, these were usually reversible, Erythema multiforme, alopecia, Musculoskeletal symptoms such as arthralgia and myalgia, Acute interstitial nephritis, Reversible impotence, breast symptoms in men. - Rare: Hypersensitivity reactions (urticaria, angioneurotic oedema, fever, bronchospasm, hypotension and chest pain). Transient and reversible changes in liver function tests. Skin rash. Drug interactions Ranitidine, at blood levels produced by standard recommended doses, does not inhibit the hepatic Cytochrome P450-linked mixed function oxygenase system. Accordingly, Aciloc in usual therapeutic doses does not potentiate the actions of drugs which are inactivated by this enzyme: these include diazepam, lignocaine, phenytoin, propranolol, theophylline, warfarin. There is no evidence of an interaction between oral ranitidine and amoxicillin and metronidazole. If high doses (2 g) of sucralfate are co-administered with oral ranitidine the absorption of the later may be reduced. This effect is not seen if sucralfate is taken after an interval of 2 h. Pregnancy and Lactation Ranitidine crosses the placenta and is excreted in human breast milk, thus Aciloc should only be used during pregnancy or during nursing if considered essential. Precautions and Warnings The possibility of malignancy should be excluded before commencement of therapy in patients with gastric ulcer and patients of middle age and over with new or recently changed dyspeptic symptoms, as treatment with Aciloc may mask symptoms of gastric carcinoma.

5 In patients such as the elderly, persons with chronic lung disease, diabetes or the immunocompromised, there may be an increased risk of developing community acquired pneumonia. Ranitidine should be avoided in patients with a history of acute porphyria. Regular supervision of patients who are taking non-steroidal anti-inflammatory drugs, concomitantly with oral Aciloc is recommended, especially in the elderly and in those with a history of peptic ulcer. Aciloc tablets are not recommended for children under 1 6 years of age. Patient Instructions Keep out of reach of children. Package and storage Aciloc 300 mg film-coated tablets: A carton box containing one, two or three AL/AL blisters each of 10 tablets + leaflet Aciloc 75 mg film-coated tablets: A carton box containing one, two or three AL/AL blisters each of 1 0 tablets + leaflet Store in a dry place at temperature not exceeding 30C. Company Produced by: SIGMA Pharmaceutical Industries - Egypt - S.A.E.