Oxycodone is a pain reliever, a semi-synthetic opioid derived from thebaine . Designed in 1916 in Germany [1] [2] . He was one of several new semi-synthetic opioids created in an attempt to improve existing opioids: morphine , diacetylmorphine (heroin) and codeine [3] .
| Oxycodone | |
|---|---|
 | |
 | |
| Chemical compound | |
| IUPAC | (5 R , 9 R , 13 S , 14 S ) -4,5Ξ±-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one |
| Gross formula | C 18 H 21 NO 4 |
| Molar mass | 315.364 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| Classification | |
| ATX | |
| Pharmacokinetics | |
| Bioavailable | 100% (intravenously); Up to 87% (oral) |
| Metabolism | In the liver: primarily CYP3A , secondarily CYP2D6 |
| The half-life. | 3-4.5 h |
| Excretion | Urine (19% unchanged) |
| Dosage Forms | |
| tablets, capsules, solution | |
| Route of administration | |
| orally, intramuscularly, intravenously, intranasally, subcutaneously, transdermally, rectally, epidural | |
| Other names | |
| Oxycodone, OxyContin | |
Oxycodone is usually prescribed to relieve moderate to severe pain .
Content
- 1 Physico-chemical properties
- 2 Getting
- 3 Effect of the substance and effects of intoxication
- 3.1 Effect of oxycodone
- 3.2 Duration and symptoms of poisoning
- 4 Medical applications
- 5 Links
- 6 notes
Physico-chemical properties
Oxycodone is a solid, although there are forms in the form of solutions, capsules. Soluble in ethyl alcohol , chloroform , insoluble in water and diethyl ether . Oxycodone hydrochloride is dissolved in the following proportions:
- water - insoluble
- ethanol - 1:60
- chloroform - 1: 600
- diethyl ether - insoluble
Getting
Oxycodone is obtained from natural sources of opioids by synthesis through thebaine. The main reaction for the preparation of oxycodone is the Diels-Alder reaction .
Effect of the substance and effects of intoxication
Oxycodone Action
Oxycodone is a powerful pain reliever. In their effectiveness, 10 mg of oxycodone (oral) is equivalent to:
- Morphine sulfate
- orally - 20 mg;
- intramuscularly - 33 mg;
- codeine - 30 mg orally;
- oxycodone - 5 mg, intramuscularly.
After repeated doses of the drug, physical and mental dependence occurs [4] [5] . With abuse, signs of poisoning are similar to taking codeine . Oxycodone can only partially suppress withdrawal symptoms in people taking any other opiate / opioid. Oxycodone can be found in the placenta , and is also found in small doses in breast milk. However, no inherent pathological changes in the newborns have been identified. Among the metabolic products there is noroxycodone, however, the metabolism of oxycodone itself is not well understood, as well as other semi-synthetic opiates. [6]
Duration and symptoms of poisoning
When using oxycodone orally:
- its action begins in 10-15 minutes;
- the maximum effect occurs after 30-60 minutes;
- the total duration of action is from 3 to 6 hours.
The toxic range is from 0.6 to 10 mg / ml. With intoxication , respiratory depression, bradycardia , fainting , drowsiness, euphoria / dysphoria , disorientation, nausea , vomiting , miosis , and urinary retention are observed. There may be rashes, hives and itching on the skin. A person can fall into a coma , arrhythmia , acidosis will appear. In extreme cases, intoxication can lead to vascular insufficiency and cardiac arrest , after which death occurs.
Medical Use
Oxycodone has been used in medicine since 1917. It is used to treat moderate to severe pain in acute or chronic pain. The controlled release of tablets for oral administration is used for cancer and other chronic pains and the drug must be taken every 12 hours. The remaining forms of the drug are usually used to treat moderate pain. In 2001, the European Palliative Therapy Association recommended oral oxycodone as an alternative to morphine .
Oxycodone is used as an anesthetic in combination with aspirin or paracetamol . It is used as an anesthetic, which is a substitute for morphine , diamorphine or hydrocodone . Oxycodone is not used as an antitussive. Effective for acute pain. Also used in oncology .
Links
Notes
- β Patent No. 296916 (Germany)
- β Sneader W. Drug discovery: a history. - Hoboken, NJ: Wiley, 2005 .-- P. 119. - ISBN 0-471-89980-1 .
- β Kalso E; Kalso, E. Oxycodone (English) // Journal of Pain and Symptom Management : journal. - 2005. - Vol. 29 , no. 5S . - P. S47 β S56 . - DOI : 10.1016 / j.jpainsymman.2005.01.010 . - PMID 15907646 .
- β The family that built the empire on pain (Russian) , InoSMI.Ru (December 30, 2017). Date of treatment December 29, 2017.
- β An epidemic that kills Americans brings billions to a specific family (Rus.) . Date of treatment December 29, 2017.
- β In Guilty Plea, OxyContin Maker to Pay $ 600 Million - The New York Times