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OXYCODON E
Overview Click to edit Master subtitle style

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Various names (UNESCO)

Oxycodon (Dutch) (French) (Spanish)

Oxycodone Oxicodona

Arabic) (Chinese) (Russian)

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History
Freund

and Speyer (University of Frankfurt) first synthesized oxycodone from thebaine in 1916, a few years after the German pharmaceutical company Bayer stopped the mass production of heroin, with hope that a thebaine -derived drug would retain the analgesic effects of morphine and heroin with less dependence. clinical use = 1917, first introduced to the US market in May 1939.

1st

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History
The

International Narcotics Control Board estimates that 11.5 tons (23,000lbs) of oxycodone were manufactured worldwide in 1998, by 2007 this figure had grown to 75.2 tons (150,400lbs). all countries, the United States had the highest total consumption of oxycodone in 2007 at 51.6 tons (103,200lbs) or 82% of the world total. In addition, the U.S. had the highest per capita consumption of oxycodone, followed by Canada in 2006, 2007 and

Of

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Australia
The By

illegal use of OxyContin began in Australia in the early 2000s. 2007, 51% of a national sample of injection drug users in Australia had reported using oxycodone, and 27% had injected it in the last six months

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Pharmaceutics
Class:

Phenanthrene derivative from poppy derived

Synthesized

thebaine

Developed Available

in Germany 1916

as IV, single or multi-compound oral preparations (paracetamol/NSAIDs) = Purdue Pharmas brand for time release oxycodone

Oxycontin

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Pharmacodynamics
Uses:

moderate to severe acute or chronic pain to other opiates

Alternative MOA:

1997 Australian research on rats suggested main site is Kappa receptors (KOP) - 2b-opioid agonist disputed as effect seems to be similar to MOP agonist studies: depend on situation KOP in diabetic mice, 1-opioid receptor in non-DM

Japanese

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Pharmacokinetics
A:

oral peak plasma level in 1h, Oxycontin peak plasma level in 3h

Oxycodone

can be administered orally, intranasally, IV, IM, SC, PR of oral administration of oxycodone averages 6087%, with rectal administration yielding the same results; intranasal varies between individuals with a mean of 46%.

Bioavailability

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Pharmacokinetics
D:

skeletal muscle, liver, intestinal tract, lungs, spleen, and brain. Conventional oxycodone reduces pain within 10-15 min, Oxycontin within 1 hour

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Pharmacokinetics
M:

liver cyt-p450 to active metabolites: and oxycodol; oxymorphone, then and oxymorphol and noroxymorphone; and noroxycodone, then and noroxycodol and noroxymorphone (Ndesmethyloxycodone). Drug opioid effect on brain appears to be from oxycodone itself urine and sweat accumulate in renal failure

Excretion:

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Dosage
Oxycodone

is approximately 1.52 times as potent as morphine when administered orally. 1015mg of oxycodone produces an analgesic effect similar to 10mg of morphine when administered intramuscularly. as a parenteral dose, morphine is approximately up to 50% more potent than oxycodone.

However,

Therefore,

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Dosage
There

are no comparative trials showing that oxycodone is more effective than any other opioid. palliative care, morphine remains the gold standard; however, oxycodone can be useful as an alternative opioid if a patient has troublesome adverse effects with morphine

In