28/30 Salvation Road, Opebi-Ikeja, Lagos; 47 Morison Cres, Oregun Ikeja, Lagos
Tel: 01-8045232, 3451454-5
Cadila Pharma Ltd, 244, Glodasar, Ahmedabad-380050, India.
Dosage Form, Composition & NAFDAC Registration Number (NRN)
Tablet (NRN: 04-1763): Ranitidine HCl U.S.P. 334.8 mg equivalent to Ranitidine 300 mg.
How to identify the Product: Film-coated tablet
Pack size: 4’s; 10’s.
Ranitidine is a competitive inhibitor of histamine at histamine H2-receptor sites, including receptors on the gastric cells. Aciloc inhibits both day time and nocturnal basal gastric acid secretions as well as gastric acid secretion stimulated by food, histamine and pentagastrin.
In healthy subjects and duodenal ulcer patients, Ranitidine did not significantly alter serum gastrin, pancreatic or mucus secretion. Pepsin secretion is not decreased but its output is reduced in proportion to the decrease in volume of gastric ulcer. Serum prolactin secretion is not increased in recommended doses. Aciloc does not have anti-androgenic effects in animals or human and studies to date suggest it does not affect serum gonadotrophin, FSH, GH, count or motility or morphology of sperms and hepatic metabolism of drugs.
Pharmacokinetics: Aciloc is well absorbed after oral administration and the peak plasma concentrations are achieved within 1 to 2 hours. Absorption is not significantly impaired by the administration of food or antacids. After a 150 mg oral dose, mean peak plasma concentrations are about 400 mcg/ml. Reported bioavailability after single doses has varied between 40-80% (average 50%). Ranitidine undergoes significant first pass metabolism after oral administration. The elimination half life is about 2.5-3 hours.
Aciloc is absorbed very rapidly after IM injection within 15 minutes or less following a 50 mg I.M. dose. Absorption from IM sites is virtually complete with a bioavailability of 90% to 100% compared with I.V. administration.
The principal route of excretion of Aciloc (tablet and injection) is urine, the N-oxide being the principal metabolite (4%). Other metabolites are the S-oxide (1%) and desmethyl ranitidine (1%). The remainder of the administered dose is found in stool. The serum protein binding of ranitidine averages 15%.
Following oral, I.M. or I.V. injections, serum concentrations of Aciloc are estimated to be 36 to 94 mg/ml which is necessary to inhibit 50% of stimulated gastric acid secretion.
Treatment of proven duodenal ulcer and gastric ulcer; Treatment of hypersecretory conditions - ZE syndrome, mastocytosis, post-operative ulcer etc; Reflux oesophagitis. Aciloc is also indicated for the long term prevention of ulcer recurrence.
The IV or IM injection is indicated where oral treatment is inappropriate.
Known hypersensitivity to the drug.
Symptomatic response to Aciloc therapy does not preclude the presence of gastric malignancy. Since Ranitidine is excreted primarily by the kidneys, dosage should be adjusted in patients with impaired renal function. Caution should be observed in patients with hepatic dysfunction since Ranitidine is metabolised in the liver.
Treatment with a H2-antagonist may cause symptoms associated with carcinoma of the stomach and therefore may delay diagnosis of the condition. Accordingly, if gastric ulcer is suspected the possibility of malignancy should be excluded before therapy with ranitidine tablets or injection is instituted.
Pregnancy and Reproduction: Studies performed in animals have revealed no evidence of impaired fertility or harm to the foetus due to ranitidine. However, there are no well controlled studies in pregnant women. Therefore, Ranitidine should be used in pregnancy only if clearly needed. Ranitidine is secreted in human milk and it should be used with caution in nursing mothers.
Paediatric Usage: Safety and effectiveness in children have not been established.
In various short term and longer studies in the treatment of peptic ulcers, ranitidine has been well tolerated with side effects occurring only in a minority of patients. Minor side effects reported are usually confined to rash, headache, dizziness, diarrhoea and tiredness. Rare cases of reversible mental confusion have been reported, especially in severely ill, elderly patients. Local pain, burning or itching has been reported at the site of injection.
Dosage & Administration
Oral: The usual oral, adult dose of Aciloc 300 is once daily at bed time in the treatment of duodenal ulcer and benign gastric ulcer.
Treatment should be continued for 4 to 8 weeks, the duration in which most of the ulcers heal. Maintenance treatment to prevent recurrence of the ulcer in some patients is recommended in the dose of 150 mg tablet at bedtime for 6 months to 1 year.
Parenteral: In some hospitalized patients with pathological hypersecretory conditions or intractable duodenal ulcers, or in patients who are unable to take oral medication, Aciloc may be administered parenterally according to the following recommendations:
IM injection: 50 mg (2 ml) every 6-8 hours.
IV injection: 50 mg (2 ml) every 6-8 hours. Dilute Aciloc injection, 50 mg in 0.9% Sodium Chloride Injection or other compatible
I.V. solution to a total volume of 20 ml and inject over a period of not less than five minutes.
IV infusion: 50 mg (2 ml) every 6-8 hours. Dilute Aciloc 50 mg, in 100 ml of 5% Dextrose Injection or other compatible I.V. solution and infuse at the rate of 25 mg per hour for 2 hours.
Tablet: Store below 25oC. Protect from light. Injection: Store Below 30°C. Do not freeze. Protect from light.