Product Information
Registration Status: ActiveOXYCONTIN 5MG PROLONGED RELEASE TABLET is approved to be sold in Singapore with effective from 2005-07-04. It is marketed by MUNDIPHARMA PHARMACEUTICALS PTE LTD, with the registration number of SIN13076P.
This product contains Oxycodone 5mg in the form of TABLET, FILM-COATED, EXTENDED-RELEASE. It is approved for ORAL use.
This product is manufactured by Bard Pharmaceuticals 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
Oxycodone is a semisynthetic derivative of codeine that acts as a narcotic analgesic more potent and addicting than codeine. An extended-release (ER) form of oxycodone (Xtampza ER) was approved for the management of daily, around-the-clock pain management in April, 2016.
Indication
For the treatment of diarrhoea, pulmonary oedema and for the relief of moderate to moderately severe pain.
Mechanism of Action
Oxycodone acts as a weak agonist at mu, kappa, and delta opioid receptors within the central nervous system (CNS). Oxycodone primarily affects mu-type opioid receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as oxycodone also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (kappa-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (mu and delta receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Pharmacokinetics
- Absorption
- Well absorbed with an oral bioavailability of 60% to 87%
- Distribution
- * 2.6 L/kg
- Metabolism
- Hepatic
- Elimination
Clearance
* 0.8 L/min [adults]
Toxicity
Symptoms of overdose include respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, bradycardia, hypotension, and death.
Active Ingredient/Synonyms
(-)-14-Hydroxydihydrocodeinone | 4,5-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one | 4,5alpha-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one | 4,5α-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one | Dihydro-14-hydroxycodeinone | Dihydrohydroxycodeinone | Dihydroxycodeinone | Oxicodona | Oxycodone | Oxycodonum | Oxycodone |
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.