Cisapride

Oral
Disorders associated with reduced gastrointestinal motility, Gastro-oesophageal reflux disease, Non-ulcer dyspepsia

Reduce initial dose in patients with renal impairment.

Reduce dose to ½ in patients with hepatic impairment.

Should be taken on an empty stomach. Take 15 min before meals. Avoid grapefruit juice.

Hypersensitivity. GI haemorrhage, obstruction or perforation; patients on oral or parenteral azole antifungals; erythromycin, clarithromycin and troleandomycin. Premature neonates with gestational age ≤3 mth. History of irregular heart beat, abnormal ECG, heart disease, pulmonary disease, dehydration or persistent vomiting. Pregnancy.

Elderly; renal or hepatic impairment. Patients in whom increase in GI motility could be harmful. Lactation.

Abdominal cramps, borborygmi and loose stools (transient); rarely require discontinuation of therapy. Headache and lightheadedness (rare). Hypersensitivity, convulsions, frequent urination.

PO: C

Sedative effects of benzodiazepines and alcohol may be enhanced. Prothrombin time in patients on anticoagulants may be increased. Effect antagonised by anticholinergic drugs. Avoid cisapride with antiallergics, antibacterials, antidepressants, antifungals, antinauseants, antipsychotics and protease-inhibitors. Cisapride increases the GI absorption of cimetidine and ranitidine. Grapefruit juice increases bioavailability of cisapride, avoid concomitant use.

Food increases the bioavailability.

Description:
Mechanism of Action: Cisapride increases GI motility by enhancing the release of acetylcholine at the myenteric plexuses in the gut plain muscle. It increases lower oesophageal sphincter pressure, shortens gastric transit time, reduces oesophageal reflux and facilitates healing of oesophageal ulcers. It also increases small intestine activity.
Onset: 30-60 minutes.
Duration: 7-10 hr.
Pharmacokinetics:
Absorption: Readily absorbed in the GI tract; peak plasma concentrations after 1-2 hr (oral).
Distribution: Enters breast milk (small amounts); protein-binding: 98%.
Metabolism: Extensively hepatic; converted to norcisapride.
Excretion: Urine and faeces (as metabolites); 10 hr (elimination half-life).

Store below 25°C.

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