Cimetidine (HCl)
Cimetidine (HCl) is a histamine H2 receptor blocking agent. It conatins a substituted imidazole ring. Cimetidine approved for clinical use in 1977 by the Food and Drug Aministration and after five years of clinical experience of cimetidine in 25 million patients, cimetidine is considered the prototype drug for ulcer therapy.
Primary Characteristics
Cimetidine (HCl) is also known as Cimetidine.
It is of Synthetic origin and belongs to Imidazole Guanidine.
It belongs to H2-antagonist pharmacological group on the basis of mechanism of action and also classified in Antineoplastic Agent, Plant Derivative pharmacological group.
Molecular Weight: 288.8 · pKa: 7.1 · Solubility in Water: slightly soluble · Solubility in Alcohol: soluble · Non-proprietary name: Cimetidine (HCl).

Pharmacokinetics
Absorption: Cimetidine (HCl) has an oral bioavailability is 92.5% (±2.5%), pre-systemic (first-pass) metabolism accounts for 37% (±13%).
Distribution: Cimetidine (HCl) has a volume of distribution is 0.8-1.2 l/kg. plasma protein binding is 13-25%.
Elimination: it is metabolised via 25-40% (hepatic), plasma half-life is 1-3 hr, renal excretion is 50-80%.
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Indications
Cimetidine (HCl) is primarily indicated in conditions like Acid-related dyspepsia, Aspiration prophylaxis, Benign gastric and duodenal ulceration, Degradation of pancreatic enzyme suppliments, Duodenal ulcer, Dyspepsia, Gastric acid reduction (surgical procedures), Gastric ulceration, Mendelsons syndrome prophylaxis, NSAID associated ulceration, NSAID-induced ulcer prophylaxis, Peptic ulcer, Prohylaxis of stress ulceration, Prophylaxis of acid aspiration in obstetric patients, Reflux oesophagitis, Risk of acid aspiration in obstetric patients, Short-bowel syndrome, Stress ulcers prevention, Surgical procedures, To reduce degradation of pancreatic enzyme supplements, Zollinger-ellison syndrome.
Cimetidine (HCl) is also indicated for secondary conditions like Benign gastric ulcer, Esophagitis, Gastritis, GI bleeding, Heart burn, Pancreatic insufficiency.
Contraindications
Cimetidine (HCl) is contraindicated in conditions like Hypersensitivity.
Dosage
Cimetidine (HCl)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 800 mg | 800 mg | Every 24h | PO | For 6 weeks. given at bed time. |
| Paediatric Dosage (20kg) | ||||
| 20 mg/kg | 20 mg/kg | — | Oral | in divided doses |
| Neonatal Dosage (3kg) | ||||
| 20 mg/kg | 20 mg/kg | — | oral | in divided doses |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Cimetidine (HCl) in overdosage may give rise to further complications which include Granulocytopenia , Agranulocytosis , Jaundice , Jaundice , Interstitial nephritis , Thrombocytopenia , Tachycardia , Impotence , Stevens johnson syndrome , Acute pancreatitis , Aplastic anemia , Reversible confusion state , Gynacomastia , Aplastic anemia, Fever , Aplastic anemia , Acute pancreatitis , Sinus bradycardia , Stevens johnson syndrome , reversible on stoping treatment.
Cimetidine (HCl) produces potentially life-threatening effects which include Cardiac arrhythmia, Heart block. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Cimetidine (HCl) are no significant adverse effects gave been associated with gross deluberate overdosing.
Cimetidine (HCl) is known to cause more or less tolerable side effects which are usually transient. These include Agitation , Alopecia, Arthralgia, Confusion, Depression, Diarrhea, Dizziness, Fever, Hallucination , HDL chlosterol level increase, Headache, Myalgia, plasma creatinine level increase, Rashes , Sr parathyroid hormone increase, Tiredness .
Warnings / Precautions
Interference in Pathology
Cimetidine (HCl) may interfere in the diagnosis of Interfere with Gastric Juice Haemoccult Testing , treatment ingestion, faecal test donot seem to be affecrted.
Available Brands
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Single Ingredient
Storage Conditions
Drug Classification
- 1.17.1.2 — Anti-peptic ulcerants
Manufacturers
Manufacturers of Cimetidine (HCl) in Pakistan: