Peringatan Keamanan

Patients experiencing an overdose may present with respiratory depression, sleepiness, stupor, coma, skeletal muscle flaccidity, cold sweat, constricted pupils, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring, and death.Label Overdose should be treated by maintaining airway, ventilation, and oxygenation.Label Oxygen and vasopressor treatment may be necessary to treat circulatory shock and pulmonary edema and defibrillation may be required for cardiac arrest of arrhythmia.Label Naloxone, nalmefene, or naltrexone may be used to counteract the effects of opioids but patients should be monitored in case further doses are required.Label

The intraperitoneal LD50 in mice is 320mg/kg, the oral LD50 is 426mg/kg.MSDS The oral lowest dose causing toxic effects in humans is 0.14mg/kg and subcutaneously in rats it is 1.53mg/kg.MSDS

Oxycodone is pregnancy category B according to the FDA.Label There is a paucity of data regarding oxycodone use in pregnancy, though animal studies show no teratogenic effects.Label Rats given oxycodone during lactation showed smaller offspring, though after lactation, they recovered to normal size.Label Oxycodone is excreted in breast milk and so patients should not breastfeed while taking oxycodone due to risk of sedation and respiratory depression in infants.Label

No studies on the carcinogenicity of oxycodone have been performed.Label Oxycodone was genotoxic at 50mcg/mL with metabolic activation and at 400mcg/mL without.Label It was also clastogenic with metabolic activation at ?1250mcg/mL.Label Oxycodone was not found to be genotoxic in other tests.Label Oxycodone does not affect reproduction and fertility in rats at doses of up to 8mg/kg/day.Label

Oxycodone

DB00497

small molecule approved illicit investigational

Deskripsi

Oxycodone is a semisynthetic opioid analgesic derived from thebaine in Germany in 1917.A178696 It is currently indicated as an immediate release product for moderate to severe pain and as an extended release product for chronic moderate to severe pain requiring continuous opioid analgesics for an extended period.Label The first oxycodone containing product, Percodan, was approved by the FDA on April 12, 1950.L6460

Struktur Molekul 2D

Berat 315.3636
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent elimination half life of oxycodone is 3.2 hours for immediate release formulations and 4.5 hours for extended release formulations.[Label] Noroxycodone has a half life of 5.8 hours, oxymorphone has a half life of 8.8 hours, noroxymorphone has a half life of 9 hours.[A178639]
Volume Distribusi 2.6L/kg.[Label]
Klirens (Clearance) Total plasma clearance is 1.4L/min in adults.[Label]

Absorpsi

Oxycodone has an oral bioavailability of 60% to 87% that is unaffected by food.Label The area under the curve is 135ng/mL\*hr, maximum plasma concentration is 11.5ng/mL, and time to maximum concentration is 5.11hr in patients given a 10mg oral immediate release dose of oxycodone.Label

Metabolisme

Oxycodone's hepatic metabolism is extensive and completed by 4 main reactions. CYP3A4 and 3A5 perform N-demethylation, CYP2D6 performs O-demethylation, unknown enzymes perform 6-keto-reduction, and unknown enzymes perform conjugation.A178639 Oxycodone is metabolized by CYP3A4 and CYP3A5 to noroxycodone and then by CYP2D6 to noroxymorphone.A178639 Noroxycodone and noroxymorphone are the primary circulating metabolites.Label Noroxycodone can also be 6-keto-reduced to alpha or beta noroxycodol.A178639 Oxycodone can be metabolized by CYP2D6 to oxymorphone and then by CYP3A4 to noroxymorphone.A178639 Oxymorphone can also be 6-keto-reduced to alpha or beta oxymorphol.A178639 Oxycodone can also be 6-keto-reduced to alpha and beta oxycodol.A178639 The active metabolites noroxycodone, oxymorphone, and noroxymorphone can all be conjugated before elimination.A178639

Rute Eliminasi

Oxycodone and its metabolites are eliminated in the urine.Label Unbound noroxycodone makes up 23% of the dose recovered in urine and oxymorphone makes up <1%.Label Conjugated oxymorphone makes up 10% of the recovered dose.Label Free and conjugated oxycodone makes up 8.9% of the recovered dose, noroxymorphone makes up 14%, and reduced metabolites make up 18%.Label

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. Food does not significantly affect absorption.

Interaksi Obat

1301 Data
Buprenorphine The therapeutic efficacy of Oxycodone can be decreased when used in combination with Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
Hydrocodone Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
Magnesium sulfate The therapeutic efficacy of Oxycodone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Oxycodone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
Orphenadrine Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
Pramipexole Oxycodone may increase the sedative activities of Pramipexole.
Ropinirole Oxycodone may increase the sedative activities of Ropinirole.
Rotigotine Oxycodone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Oxycodone.
Sodium oxybate Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
Thalidomide Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Alvimopan The therapeutic efficacy of Oxycodone can be decreased when used in combination with Alvimopan.
Desmopressin The risk or severity of hyponatremia can be increased when Oxycodone is combined with Desmopressin.
Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Oxycodone.
Codeine The risk or severity of adverse effects can be increased when Codeine is combined with Oxycodone.
Hydromorphone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Oxycodone.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Oxycodone is combined with Dextropropoxyphene.
Sufentanil The risk or severity of adverse effects can be increased when Oxycodone is combined with Sufentanil.
Levorphanol The risk or severity of adverse effects can be increased when Oxycodone is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Oxycodone is combined with Remifentanil.
Diphenoxylate The risk or severity of adverse effects can be increased when Oxycodone is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Oxycodone is combined with Oxymorphone.
Dezocine The therapeutic efficacy of Oxycodone can be decreased when used in combination with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Oxycodone is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Oxycodone is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Oxycodone is combined with Diamorphine.
Bezitramide The risk or severity of adverse effects can be increased when Oxycodone is combined with Bezitramide.
Ethylmorphine The risk or severity of adverse effects can be increased when Oxycodone is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Oxycodone is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Oxycodone is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Oxycodone is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Oxycodone is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Oxycodone is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Oxycodone is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Oxycodone is combined with Dihydromorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Oxycodone is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Oxycodone is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Oxycodone is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Oxycodone is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Oxycodone is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Oxycodone is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Oxycodone is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Oxycodone is combined with Nicomorphine.
Meptazinol The therapeutic efficacy of Oxycodone can be decreased when used in combination with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Oxycodone is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Oxycodone is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Oxycodone is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Oxycodone is combined with Carfentanil, C-11.
Alfentanil The risk or severity of adverse effects can be increased when Oxycodone is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Oxycodone is combined with Fentanyl.
Benzhydrocodone The risk or severity of adverse effects can be increased when Oxycodone is combined with Benzhydrocodone.
Meperidine The risk or severity of adverse effects can be increased when Meperidine is combined with Oxycodone.
Naloxegol The therapeutic efficacy of Oxycodone can be decreased when used in combination with Naloxegol.
Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Oxycodone.
Succinylcholine The risk or severity of bradycardia can be increased when Succinylcholine is combined with Oxycodone.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Oxycodone.
Voriconazole The risk or severity of adverse effects can be increased when Voriconazole is combined with Oxycodone.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Oxycodone.
Furazolidone Furazolidone may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Procaine Procaine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Tranylcypromine Tranylcypromine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Phenelzine Phenelzine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Minaprine Minaprine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Selegiline Selegiline may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Procarbazine Procarbazine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Moclobemide Moclobemide may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Isocarboxazid Isocarboxazid may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Rasagiline Rasagiline may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Pargyline Pargyline may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Clorgiline Clorgiline may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Iproniazid Iproniazid may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Nialamide Nialamide may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Safinamide Safinamide may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Hydracarbazine Hydracarbazine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Pirlindole Pirlindole may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Toloxatone Toloxatone may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Benmoxin Benmoxin may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Mebanazine Mebanazine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Octamoxin Octamoxin may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Pheniprazine Pheniprazine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Phenoxypropazine Phenoxypropazine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Pivhydrazine Pivhydrazine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Safrazine Safrazine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Caroxazone Caroxazone may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Harmaline Harmaline may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Brofaromine Brofaromine may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Oxycodone.
Mirabegron The serum concentration of Oxycodone can be increased when it is combined with Mirabegron.

Target Protein

Mu-type opioid receptor OPRM1
Kappa-type opioid receptor OPRK1
Delta-type opioid receptor OPRD1

Referensi & Sumber

Synthesis reference: Bao-Shan Huang, Yansong Lu, Ben-Yi Ji, Aris P Christodoulou, "Preparation of oxycodone from codeine." U.S. Patent US6008355, issued March, 1990.
Artikel (PubMed)
  • PMID: 26227254
    DePriest AZ, Puet BL, Holt AC, Roberts A, Cone EJ: Metabolism and Disposition of Prescription Opioids: A Review. Forensic Sci Rev. 2015 Jul;27(2):115-45.
  • PMID: 8249052
    Leow KP, Wright AW, Cramond T, Smith MT: Determination of the serum protein binding of oxycodone and morphine using ultrafiltration. Ther Drug Monit. 1993 Oct;15(5):440-7.
  • PMID: 28526158
    Ruan X, Mancuso KF, Kaye AD: Revisiting Oxycodone Analgesia: A Review and Hypothesis. Anesthesiol Clin. 2017 Jun;35(2):e163-e174. doi: 10.1016/j.anclin.2017.01.022. Epub 2017 Mar 14.
  • PMID: 20852623
    Andrade A, Denome S, Jiang YQ, Marangoudakis S, Lipscombe D: Opioid inhibition of N-type Ca2+ channels and spinal analgesia couple to alternative splicing. Nat Neurosci. 2010 Oct;13(10):1249-56. doi: 10.1038/nn.2643. Epub 2010 Sep 19.

Contoh Produk & Brand

Produk: 949 • International brands: 2
Produk
  • Act Oxycodone CR
    Tablet, extended release • 5 mg • Oral • Canada • Approved
  • Act Oxycodone CR
    Tablet, extended release • 10 mg • Oral • Canada • Approved
  • Act Oxycodone CR
    Tablet, extended release • 20 mg • Oral • Canada • Approved
  • Act Oxycodone CR
    Tablet, extended release • 40 mg • Oral • Canada • Approved
  • Act Oxycodone CR
    Tablet, extended release • 80 mg • Oral • Canada • Approved
  • Apo-oxycodone CR
    Tablet, extended release • 40 mg • Oral • Canada • Generic • Approved
  • Apo-oxycodone CR
    Tablet, extended release • 5.0 mg • Oral • Canada • Generic • Approved
  • Apo-oxycodone CR
    Tablet, extended release • 20.0 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 949 produk.
International Brands
  • Oxanest
  • OxyIR

Sekuens Gen/Protein (FASTA)

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