oxycodone_HCl: profile and news

Watson Pharmaceuticals Reports First Quarter 2006 Results May 9, 2006
The decrease in gross margin versus both prior periods was due primarily to the sales of oxycodone HCl controlled-release tablets, a distributed generic ... - Yahoo! News (press release)

Up to $5,000 Reward Offered for Information Leading to Arrest of ... May 3, 2006
The cash reward is donated by pharmaceutical company Purdue Pharma LP, the distributor of OxyContinÂ® (oxycodone HCl controlled- release) Tablets, the Marion ... - Yahoo! News (press release)

First-Ever Systematic Analysis of Internet Chatter Yields ... May 4, 2006
Stephen Butler, Ph.D. and Nathaniel Katz, MD, MS, specifically analyzed Internet chatter about three target dugs: OxyContin(R) (oxycodone HCl controlled-release ... - PR Newswire (press release),

Forest Laboratories Signs Grants Manager Agreement With Fast Track ... Apr 19, 2006
...with alcohol dependence who are abstinent at treatment initiation in combination with psychosocial support; and Combunoxâ„¢ (Oxycodone HCl and Ibuprofen), an ... - Market Wire (press release)

Other information

Indication
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.

Drug Category
Narcotics; Antitussives; Analgesics, Opioid; Opiate Agonists; ATC:N02AA05

Brand Names/Synonyms
Codeinone, Dihydrohydroxy-; Combunox; Dea No. 9143; Dihydrohydroxycodeinone; Dihydrohydroxycondeinone; Dihydrone; Dihydroxycodeinone; Dinarkon; Diphydrone; ENDOCET; ENDODAN; Endone; Eubine; Eubine [France]; Eucodal; Eucodalum; Eukodal; Eutagen; HSDB 3142; Ossicodone [Dcit]; Oxanest; Oxicodona [Inn-Spanish]; Oxicon; Oxicone; Oxikon; Oxycet; Oxycodeinone; Oxycodon; Oxycodone; Oxycodone Hcl; Oxycodone Hydrochloride; Oxycodone [Usan:Ban:Inn]; Oxycodonum [Inn-Latin]; Oxycon; Oxycontin; PERCOCET; Pancodine; Percobarb; Percocet; Percodan; Roxicet; Roxicodone; Roxilox; Supendol [Canada]; Tecodin; Tekodin; Thecodine; Thekodin; Tylox

Dosage Forms
Tablet; Suppository

Absorption
well absorbed from OxyContin® tablets with an oral bioavailability of 60% to 87%

Interactions
Interactions for Oxycodone:

The CNS depressant effects of oxycodone hydrochloride may be additive with that of other CNS depressants..

Chemical IUPAC Name
4, 5-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one

Chemical Formula
C18H21NO4

Half Life
4.5 hours

Drug Type
Approved Drug

# Accession No
APRD00387

CAS Registry Number
76-42-6