Percolone - General Information
Semisynthetic derivative of codeine that acts as a narcotic analgesic more potent and addicting than codeine. [PubChem]
Pharmacology of Percolone
Percolone, a semisynthetic opiate agonist derived from the opioid alkaloid, thebaine, is similar to other phenanthrene derivatives such as hydrocodone and morphine. Percolone is available in combination with aspirin or acetaminophen to control pain and restless leg and Tourette syndromes.
Percolone for patients
Drug Dependence: Oxycodone can produce drug dependence of the morphine type, and therefore, has the potential for being abused. Psychic dependence, physical dependence and tolerance may develop upon repeated administration of this drug, and it should be prescribed and administered with the same degree of caution appropriate to the use of other oral narcotic-containing medications. Like other narcotic-containing medications, this drug is subject to the Federal Controlled Substances Act.
Usage in Ambulatory Patients: Oxycodone may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks such as driving a car or operating machinery. The patient using this drug should be cautioned accordingly.
Interaction with Other Central Nervous System Depressants: Patients receiving other narcotic analgesics, general anesthetics, phenothiazines, other tranquilizers, sedative-hypnotics or other CNS depressants (including alcohol) concomitantly with oxycodone hydrochloride may exhibit an additive CNS depression. When such combined therapy is contemplated, the dose of one or both agents should be reduced.
Usage in Pregnancy: Safe use in pregnancy has not been established relative to possible adverse effects on fetal development. Therefore, this drug should not be used in pregnant women unless, in the judgment of the physician, the potential benefits outweigh the possible hazards.
Usage in Children: This drug should not be administered to children.
Head Injury and Increased Intracranial Pressure: The respiratory depressant effects of narcotics and their capacity to elevate cerebrospinal fluid pressure may be markedly exaggerated in the presence of head injury, other intracranial lesions or a pre-existing increase in intracranial pressure. Furthermore, narcotics produce adverse reactions which may obscure the clinical course of patients with head injuries.
Acute Abdominal Conditions: The administration of this drug or other narcotics may obscure the diagnosis or clinical course in patients with acute abdominal conditions.
Special Risk Patients: This drug should be given with caution to certain patients such as the elderly, or debilitated, and those with severe impairment of hepatic or renal function, hypothyroidism, Addison's disease and prostatic hypertrophy or urethral stricture.
Hypersensitivity to oxycodone.
Additional information about Percolone
Percolone Indication: For the treatment of diarrhoea, pulmonary oedema and for the relief of moderate to moderately severe pain.
Mechanism Of Action: Percolone acts as a weak agonist at mu, kappa, and delta opioid receptors within the central nervous system (CNS). Percolone primarily affects mu-type opioid 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 (kappa-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (mu and delta receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Drug Interactions: Cimetidine Cimetidine increases the effect of the narcotic
Citalopram Increased risk of serotonin syndrome
Escitalopram Increased risk of serotonin syndrome
Fluoxetine Increased risk of serotonin syndrome
Fluvoxamine Increased risk of serotonin syndrome
Sertraline Increased risk of serotonin syndrome
Paroxetine Increased risk of serotonin syndrome
Naltrexone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals
Food Interactions: Not Available
Generic Name: Oxycodone
Synonyms: Dihydrohydroxycondeinone; Dihydrohydroxycodeinone; Dihydrone; Oxycodone Hydrochloride; Oxicodona [Inn-Spanish]; Oxycodone Hcl; Oxycodonum [Inn-Latin]
Drug Category: Narcotics; Antitussives; Analgesics, Opioid; Opiate Agonists
Drug Type: Small Molecule; Illicit; Approved
Other Brand Names containing Oxycodone: Combunox; Dihydroxycodeinone; Dinarkon; Diphydrone; Endocet; Endodan; Endone; Eubine; Eucodal; Eucodalum; Eukodal; Eutagen; Oxanest; Oxicon; Oxicone; Oxikon; Oxycodeinone; Oxycodon; Oxycon; Oxycontin; Pancodine; Percobarb; Percodan; Roxicodone; Supendol; Tecodin; Tekodin; Thecodine; Thekodin; OxyIR; OxyNorm; Percolone; OxyFAST; Supeudol;
Absorption: Well absorbed with an oral bioavailability of 60% to 87%
Toxicity (Overdose): Symptoms of overdose include respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, bradycardia, hypotension, and death.
Protein Binding: 45%
Half Life: 4.5 hours
Dosage Forms of Percolone: Tablet, extended release Oral
Chemical IUPAC Name: 4, 5-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one
Chemical Formula: C18H21NO4
Oxycodone on Wikipedia: https://en.wikipedia.org/wiki/Oxycodone
Organisms Affected: Humans and other mammals