Product Information
Registration Status: ActiveMST CONTINUS TABLET 10mg is approved to be sold in Singapore with effective from 1991-04-03. It is marketed by MUNDIPHARMA PHARMACEUTICALS PTE LTD, with the registration number of SIN05506P.
This product contains Morphine 10mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by BARD PHARMACEUTICALS LTD in UNITED KINGDOM.
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
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle. In January, 2017, morphine was approved for the treatment of chronic pain.
Indication
For the relief and treatment of severe pain.
Mechanism of Action
The precise mechanism of the analgesic action of morphine is unknown. However, specific CNS opiate receptors have been identified and likely play a role in the expression of analgesic effects. Morphine first acts on the mu-opioid receptors. The mechanism of respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension and to electrical stimulation. It has been shown that morphine binds to and inhibits GABA inhibitory interneurons. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream.
Pharmacokinetics
- Absorption
- Bioavailability is approximately 30%.
- Distribution
- * 1 to 6 L/kg
- Metabolism
- Primarily hepatic (90%), converted to dihydromorphinone and normorphine. Also converted to morphine-3-glucuronide (M3G) and morphine-6-glucuronide. Virtually all morphine is converted to glucuronide metabolites; only a small fraction (less than 5%) of absorbed morphine is demethylated.
- Elimination
Clearance
* 20 – 30 mL/min/kg [Adult] * 1852 +/- 116 mL/min [Chinese] * 1495 +/- 80 mL/min [Caucasian]
Toxicity
LD50 = 461 mg/kg (rat, oral), 600 mg/kg (mouse, oral). Human lethal dose by ingestion is 120-250 mg of morphine sulfate. Symptoms of overdose include cold, clammy skin, flaccid muscles, fluid in the lungs, lowered blood pressure, "pinpoint" or dilated pupils, sleepiness leading to stupor and coma, slowed breathing, and slow pulse rate.
Active Ingredient/Synonyms
(−)-morphine | (5alpha,6alpha)-17-methyl-7,8-didehydro-4,5-epoxymorphinan-3,6-diol | (5alpha,6alpha)-didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol | (5R,6S,9R,13S,14R)-4,5-epoxy-N-methyl-7-morphinen-3,6-diol | (5α,6α)-17-methyl-7,8-didehydro-4,5-epoxymorphinan-3,6-diol | (5α,6α)-didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol | (7R,7AS,12bs)-3-methyl-2,3,4,4a,7,7a-hexahydro-1H-4,12-methano[1]benzofuro[3,2-e]isoquinoline-7,9-diol | anhydrous morphine | morfina | Morphia | Morphin | Morphinum | Morphium | Morphine |
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.