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Oxycodone-an opioid pain killer

Oxycodone is a semisynthetic opioid synthesized from thebaine, an opioid alkaloid found in the Persian poppy, and one of the many alkaloids More

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Description

Oxycodone is a semisynthetic opioid synthesized from thebaine, an opioid alkaloid found in the Persian poppy, and one of the many alkaloids

Generic Name

Oxycodone-an opioid pain killer

Chemical names

Oxycodone; Dihydrohydroxycodeinone; Dihydrone; Dihydroxycodeinone; Oxycodeinone

Brand names

IUPAC name

(1S,5R,13R,17S)-17-hydroxy-10-methoxy-4-methyl-12-oxa-4-azapentacyclo[9.6.1.0¹,¹³.0?,¹?.0?,¹?]octadeca-7(18),8,10-trien-14-one

Pharmacokinetics

Actions

Oxycodone, a semisynthetic opiate agonist derived from the opioid alkaloid, thebaine, is similar to other phenanthrene derivatives such as hydrocodone and morphine. This is available in combination with acetaminophen or aspirin to control restless leg and pain and Tourette syndromes. Oxycodone acts as a weak agonist at mu, kappa, and delta opioid receptors within the central nervous system (CNS). It affects primarily on mu-type opioid receptors, 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 cAMP and adenylate cyclase 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 somatostatin, vasopressin, glucagon and insulin. Opioids close N-type voltage-operated calcium channels (kappa-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (mu and delta receptor agonist). This results in hyperpolarization and reduced neuronal excitability.

Dosage/Dosage form

Therapeutic uses

For the treatment of diarrhoea, pulmonary oedema and for the relief of moderate to moderately severe pain.

Adverse effects/Side effects

Interaction

  • Oxycodone can interact with Nalbuphine, buprenorphine, butorphanol and pentazocine.
  • Do not drink wine or grapefruit juice, don’t eat grapefruit while taking Oxycodone.

Contraindications

Oxycodone is contraindicated in patients who are allergic to narcotic analgesics, paralytic ileus patients, asthmatic patients and individuals with alcohol or substance abuse history. 

Storage

Store at 20-25°C.

Information

Molecular weight

315.3636

Molecular formula

C18H21NO4

CAS number

76-42-6

Precautions

  • Do not drive vehicles or operate heavy machineries that need utmost mental alertness.
  • Should not be used in patients with hypotension, spinal curvature, hepatic or renal disorders, COPD, adrenal gland disorders, enlarged prostate, mental illness, urination problems, seizure, gallbladder diseases and thyroid dysfunctions.
  • Oxycodone may impair thinking and alertness.