H2 RECEPTOR BLOCKER

1.Ranitidone

2.cimetidine

3.Nizaridone

RANITIDINE

INDICATION:

Ranitidine is indicated in the short-term treatment of active duodenal and active benign gastric ulcer; maintenance
therapy for duodenal and gastric ulcer patients at reduced dosage; treatment of gastroeosophageal reflux and
pathological hypersecretory conditions e.g. Zollinger-Ellison syndrome.

DOSAGE/DIRECTION OF USE

Adult: Duodenal Ulcer and Benign Gastric Ulcer: Treatment: 150 mg twice a day or 300 mg at bedtime for 4 to 8
weeks. Maintenance: 150 mg at bedtime.
Gastric Hypersecretory Conditions:Treatment: 150 mg three times a day; the dosage being adjusted as needed
and therapy continued as long as clinically indicated. Doses up to 6 grams per day have been used in severe cases.
Gastroeosophageal reflux: Treatment: 150 mg twice to four times a day for up to 8 weeks.

Contraindocation

Ranitidine is contraindicated in patients with known hypersensitivity to the drug.

Dosage overdose

There has been limited experience with overdosage. Reported acute ingestions of up to 18 g orally have been
associated with transient adverse effects similar to those encountered in normal clinical experience. In addition,
abnormalities of gait and hypotension have been reported.
If overdosage occurs, the usual measures to remove the absorbed material from gastrointestinal tract by induction of
emesis and/or gastric lavage should be employed. Ranitidine may be removed from plasma by haemodialysis.
In addition to clinical monitoring, specific treatment and supportive care should be instituted.

Adverse effect

Gastrointestinal: Constipation, diarrhoea, nausea/vomiting, abdominal discomfort/pain and rare reports of

pancreatitis.

Central Nervous System: Rarely malaise, dizziness, somnolence, insomnia and vertigo. Rare cases of reversible
mental confusion, agitation, depression and hallucinations have been reported, predominantly in severely ill elderly
patients. Rare cases of reversible blurred vision suggestive of a change in accommodation have been reported. Rare
reports of reversible involuntary motor disturbances have been received

Use in Lactation: Ranitidine is distributed into breast milk and could possibly suppress gastric acidity, inhibit drug
metabolism and cause CNS stimulation in the nursing baby. Caution should be exercised when ranitidine is
administered to a nursing mother.
Cimetidine

Dosage:

Benign gastric and duodenal ulceration, Zollinger-Ellison syndrome

Adult: Intermittent infusion: 300 mg 6-8 hrly infused over 15-20 min. Max: 2400 mg/day. Continuous infusion: 37.5
mg/hr (900 mg/day). A 150 mg IV loading dose may be given in patients requiring rapid elevation of gastric pH.

Oral
Prophylaxis of gastrointestinal haemorrhage from stress ulceration

Adult: 200-400 mg 4-6 hrly.

Oral
Benign gastric and duodenal ulceration

Adult: 800 mg daily at bedtime or 400 mg bid for at least 4 wk for duodenal ulcers, 6 wk for gastric ulcers and 8 wk
for NSAID-associated ulcers. May increase to 400 mg 4 times daily if necessary. Maintenance: 400 mg daily at
bedtime or bid.

Over Dosage:

Symptoms: Dizziness, bradycardia, CNS depression, vomiting. Management: Induce vomiting and/or gastric lavage,
followed by symptomatic and supportive treatment.

Adverse Drug Reaction:

Diarrhoea, other GI disturbances, dizziness, headache, tiredness, myalgia, arthralgia, rashes, altered LFTs,
reversible confusional states. Rarely, hypersensitivity reactions and fever, reversible alopecia, blood disorders (e.g.
agranulocytosis, leucopenia, and thrombocytopenia), acute pancreatitis, interstitial nephritis, hallucinations and
depression, CV disorders (e.g. bradycardia, tachycardia, heart block), transient hypotension, gynaecomastia and
impotence.
Potentially Fatal: Rarely, hepatotoxicity, cardiac arrest and arrhythmias due to rapid IV inj.

Mechanism Of Action

Description: 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 also used in patients w/
pancreatic insufficiency to reduce the breakdown of pancreatic enzyme supplements.
Onset: 1 hr.
Duration: 4-5 hr.
Pharmacokinetics:
Absorption: Readily absorbed from the GI tract. Food delays the rate and slightly decreases extent of absorption.
Bioavailability: Approx 60-70%. Time to peak plasma concentration: Approx 1-3 hr.
Distribution: Widely distributed; enters breast milk, crosses the placental barrier. Volume of distribution: Approx 1
L/kg. Plasma protein binding: Approx 20%.
Metabolism: Partially hepatic, converted to sulfoxide and hydroxymethylcimetidine.
Nizatidine

DOSAGE

Adult : PO Benign gastric and duodenal ulceration; NSAID-associated ulceration300 mg at bedtime or in 2

divided doses for 4-8 wk. Maintenance: 150 mg at bedtime. GERD 150-300 mg bid for up to 12 wk. Dyspepsia 75
mg/day. Max: 150 mg/day for up to 2 wk.

Dosage Details:

Oral
Benign gastric and duodenal ulceration, NSAID-associated ulceration

Adult: 300 mg at bedtime or in 2 divided doses for 4-8 wk. Maintenance: 150 mg at bedtime.

Oral
Dyspepsia

Adult: 75 mg daily, repeated if needed, up to a max of 150 mg daily for up to 2 wk.

Oral
Gastro-oesophageal reflux disease

Adult: 150-300 mg bid for up to 12 wk.

Child: ≥12 yr 150 mg bid for up to 8 wk.

Averse Drug Reaction:

Headache, dizziness, insomnia, abnormal dreams, somnolence, asthenia, anxiety, excessive sweating, diarrhoea,
nausea and/or vomiting, abdominal pain/discomfort, constipation, flatulence, dyspepsia, dry mouth, anorexia, tooth
disorder, urticaria, rash, pruritus, exfoliative dermatitis, anaemia, rhinitis, pharyngitis, sinusitis, reversible
hepatocellular injury, diaphoresis, myalgia, fever. Rarely, asymptomatic ventricular tachycardia, thrombocytopenic
purpura, decreased libido, gynaecomastia, reversible cholestatic or mixed cholestatic-hepatocellular injury w/
jaundice

Overdosage:

Symptoms: Lacrimation, salivation, emesis, miosis, and diarrhoea. Management: Symptomatic and supportive
treatment. Activated charcoal, emesis or lavage may reduce absorption

Mechanism Of Action:

Description: Nizatidine is a histamine H2-receptor antagonist. It blocks histamine H2-receptors on gastric parietal
cells resulting in decreased gastric acid secretion, gastric volume and hydrogen ion concentration.
Pharmacokinetics:
Absorption: Readily absorbed from the GI tract. Bioavailability: >70%; slightly increased by food. Time to peak
plasma concentration: Approx 0.5-3 hr.
Distribution: Widely distributed; enters breast milk. Volume of distribution: 0.8-1.5 L/kg. Plasma protein binding:
Approx 35%.
Metabolism: Partly hepatic. Converted to nizatidine N-2-oxide, nizatidine S-oxide, and N-2-monodesmethylnizatidine
(60% of the activity).