Product Information
Registration Status: ActiveMETOCLOPRAMIDE INJECTION BP 5mg/ML is approved to be sold in Singapore with effective from 1990-11-14. It is marketed by PFIZER PTE LTD, with the registration number of SIN05202P.
This product contains Metoclopramide 5mg/ml in the form of INJECTION. It is approved for INTRAVENOUS, INTRAMUSCULAR use.
This product is manufactured by PFIZER (PERTH) PTY LTD in AUSTRALIA.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A dopamine D2 antagonist that is used as an antiemetic.
Indication
For the treatment of gastroesophageal reflux disease (GERD). It is also used in treating nausea and vomiting, and to increase gastric emptying.
Mechanism of Action
Metoclopramide inhibits gastric smooth muscle relaxation produced by dopamine, therefore increasing cholinergic response of the gastrointestinal smooth muscle. It accelerates intestinal transit and gastric emptying by preventing relaxation of gastric body and increasing the phasic activity of antrum. Simultaneously, this action is accompanied by relaxation of the upper small intestine, resulting in an improved coordination between the body and antrum of the stomach and the upper small intestine. Metoclopramide also decreases reflux into the esophagus by increasing the resting pressure of the lower esophageal sphincter and improves acid clearance from the esophagus by increasing amplitude of esophageal peristaltic contractions. Metoclopramide's dopamine antagonist action raises the threshold of activity in the chemoreceptor trigger zone and decreases the input from afferent visceral nerves. Studies have also shown that high doses of metoclopramide can antagonize 5-hydroxytryptamine (5-HT) receptors in the peripheral nervous system in animals.
Pharmacokinetics
- Absorption
- Rapidly and well absorbed (oral bioavailability 80±15.5%).
- Distribution
- * 4.4±0.65 L/kg
- Metabolism
- Hepatic
- Elimination
Clearance
* 0.67 +/- 0.14 L/hr/kg [infants (0.9-5.4 months) with gastroesophageal reflux (GER)]
Toxicity
Oral, mouse LD50: 280 mg/kg. Signs of overdose include drowsiness, disorientation, and extrapyramidal reactions.
Active Ingredient/Synonyms
2-methoxy-4-amino-5-chloro-N,N-(dimethylaminoethyl)benzamide | 2-methoxy-5-chloroprocainamide | 4-amino-5-chloro-2-methoxy-N-(β-diethylaminoethyl)benzamide | 4-amino-5-chloro-N-(2-(diethylamino)ethyl)-o-anisamide | Metoclopramida | Metoclopramidum | Metoclopramide |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.