Percodan: profile and news

The Health Report: Xanax Is NOT a Painkiller, Charlie Sheen! May 12, 2006
...to opiates in any way. "Percodan, Vicodin, OxyContin, and heroin are opiates. Not Xanax. "Benzodiazepines do not produce euphoria ... - DeadBrain.us (satire)

Defense seeks new trial in 1981 murder May 1, 2006
3, 1978, Rodwell enlisted the help of Frank Holmes, formerly of Burlington, and a third person to set up Rose and steal about 1,000 Percodan painkillers worth ... - Lowell Sun,

Acclaimed photographer teams with former OxyContin addict to film ... Apr 29, 2006
He talks openly about how he began experimenting with marijuana at 15, started taking pills including Percodan and Percocet at 16, stealing from his ... - ChronicleHerald.ca,

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