Brands, Medical Use, Clinical Data
Drug Category
- Narcotics
- Antitussives
- Analgesics, Opioid
- Opiate Agonists
Dosage Forms
Brands / Synonyms
Codeinone, Dihydrohydroxy-; Combunox; Dea No. 9143; Dihydrohydroxycodeinone; Dihydrohydroxycondeinone; Dihydrone; Dihydroxycodeinone; Dinarkon; Diphydrone; ENDOCET; ENDODAN; Endone; Eubine; Eubine [France]; Eucodal; Eucodalum; Eukodal; Eutagen; Ossicodone [Dcit]; Oxanest; Oxicodona [Inn-Spanish]; Oxicon; Oxicone; Oxikon; Oxycet; Oxycodeinone; Oxycodon; Oxycodone; Oxycodone and Acetaminophen; Oxycodone and Aspirin; Oxycodone Hcl; Oxycodone Hydrochloride; Oxycodone [Usan:Ban:Inn]; Oxycodonum [Inn-Latin]; Oxycon; Oxycontin; Oxyir; Pancodine; Percobarb; Percocet; Percodan; Roxicet; Roxicodone; Roxilox; Supendol [Canada]; Tecodin; Tekodin; Thecodine; Thekodin; Tylox
Indications
For the treatment of diarrhoea, pulmonary oedema; For the relief of moderate to moderately severe pain
Pharmacology
Oxycodone, a semisynthetic opiate agonist derived from the opioid alkaloid, thebaine, is similar to other phenanthrene derivatives such as hydrocodone and morphine. Oxycodone is available in combination with aspirin or acetaminophen to control pain and restless leg and Tourette syndromes.
Mechanism of Action
Oxycodone acts as a weak agonist at OP1, OP2, and OP3 opiate receptors within the central nervous system (CNS). Oxycodone primarily affects OP3 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 (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Absorption
well absorbed from OxyContin® tablets with an oral bioavailability of 60% to 87%
Toxicity
respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, bradycardia, hypotension, and death.
Biotrnasformation / Drug Metabolism
Hepataic
Contraindications
Hypersensitivity to oxycodone.
Drug Interactions
The CNS depressant effects of oxycodone hydrochloride may be additive with that of other CNS depressants..
|
