Cimetidine

Indications
 Oral
Benign gastric and duodenal ulceration
Adult: Initially, 800 mg as a single daily dose given at bedtime for at least 4 wk for duodenal ulcers and 6 wk for gastric ulcers. Maintenance: 400 mg once daily at bedtime or bid.
CrCl (ml/min)Dosage Recommendation
30-50200 mg 4 times daily.
15-30200 mg tid.
0-15200 mg bid.

Oral
Stress ulceration of upper gastrointestinal tract
Adult: 200-400 mg every 4-6 hr.
CrCl (ml/min)Dosage Recommendation
30-50200 mg 4 times daily.
15-30200 mg tid.
0-15200 mg bid.

Oral
Prophylaxis of acid aspiration during general anaesthesia
Adult: 400 mg is given orally 90-120 minutes before induction of anaesthesia or at the start of labour and up to 400 mg may be given every 4 hr if necessary.
CrCl (ml/min)Dosage Recommendation
30-50200 mg 4 times daily.
15-30200 mg tid.
0-15200 mg bid.

Oral
Gastro-oesophageal reflux disease
Adult: 400 mg 4 times daily or 800 mg bid for 4-8 wk.
CrCl (ml/min)Dosage Recommendation
30-50200 mg 4 times daily.
15-30200 mg tid.
0-15200 mg bid.

Oral
Zollinger-Ellison syndrome
Adult: 300-400 mg 4 times daily, increase dose if necessary.
CrCl (ml/min)Dosage Recommendation
30-50200 mg 4 times daily.
15-30200 mg tid.
0-15200 mg bid.

Oral
Non-ulcer dyspepsia
Adult: Up to 200 mg 4 times daily.
CrCl (ml/min)Dosage Recommendation
30-50200 mg 4 times daily.
15-30200 mg tid.
0-15200 mg bid.

Oral
Prophylaxis of nocturnal heartburn
Adult: 100 mg at night.
CrCl (ml/min)Dosage Recommendation
30-50200 mg 4 times daily.
15-30200 mg tid.
0-15200 mg bid.

Oral
Pancreatic insufficiency
Adult: 800-1600 mg daily in 4 divided doses, to be taken 60-90 minutes before meals.
CrCl (ml/min)Dosage Recommendation
30-50200 mg 4 times daily.
15-30200 mg tid.
0-15200 mg bid.

Intravenous
Stress ulceration of upper gastrointestinal tract
Adult: 200 mg every 4-6 hr.

Special Populations: Renal impairment: Dose reduction based on creatinine clearance.
Contraindications
 Hypersensitivity, lactation.
Warnings / Precautions
 Impaired renal and hepatic function. Age >50 yr; CV impairment. Pregnancy.
Adverse Reactions
 Diarrhoea, dizziness, tiredness, rash, headache, CNS disturbances, arthralgia, myalgia, gynaecomastia, alopoecia, blood dyscrasias, nephritis, hepatitis, pancreatitis, granulocytopenia, hypersensitivity reactions.
Overdose Reactions
 Overdosage may lead to respiratory failure and tachycardia that may be controlled by assisted respiration and admin of a β-blocker.
Drug Interactions
 Absorption reduced by antacids. May potentiate anticoagulants, phenytoin, theophylline, benzodiazepines, β-blockers, lidocaine. Procainamide clearance is reduced. Reduced absorption of ketoconazole and itraconazole. May enhance gastric mucosal irritation when taken with ethanol. Avoid concurrent use with clopidogrel.
See Below for More cimetidine Drug Interactions
Food Interactions
 Absorption delayed.
Mechanism of Actions
 Cimetidine competitively inhibits histamine at H2-receptors of the gastric parietal cells resulting in decreased gastric acid secretion, gastric volume and hydrogen ion concentration. It is a potent inhibitor of metabolism in the hepatic mixed-function oxidase systems. It is also used in patients with pancreatic insufficiency to reduce the breakdown of pancreatic enzyme supplements.
Onset: 1 hr.
Duration: 4-6 hr.
Absorption: Readily absorbed from the GI tract; peak plasma concentrations after 1-3 hr. Food delays the rate and slightly decreases extent of absorption.
Distribution: Widely distributed in the body; crosses the placental barrier and appears in breast milk. Protein-binding: 20%.
Metabolism: Partially hepatic; converted to the sulfoxide and to hydroxymethylcimetidine.
Excretion: Urine (as unchanged); 2 hr (elimination half-life).
Administration
 Should be taken with food.
ATC Classification
 A02BA01 - cimetidine ; Belongs to the class of H2-receptor antagonists. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Available As
  • Cimetidine 200 mg
  • Cimetidine 400 mg
  • Cimetidine 600 mg

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