Peringatan Keamanan

Coma, respiratory depression, circulatory collapse, and pulmonary edema. Seizures occur more frequently in patients with propoxyphene intoxication than in those with opiate intoxication. LD50=230mg/kg (orally in rat, Emerson)

Dextropropoxyphene

DB00647

small molecule approved illicit investigational withdrawn

Deskripsi

Dextropropoxyphene is an opioid analgesic manufactured by Eli Lilly and Company. It is used in the symptomatic treatment of mild pain. It displays antitussive and local anaesthetic actions. Due to the risk of cardiac arrhythmias and overdose, possibly leading to death, dextropropoxyphene has been withdrawn from the market in Europe and the United States. The drug is often referred to as the general form, "propoxyphene", however only the dextro-isomer (dextropropoxyphene) has any analgesic effect. The levo-isomer appears to exhibit a very limited antitussive effect.

Struktur Molekul 2D

Berat 339.4712
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 6-12 hours
Volume Distribusi * 16 L/kg
Klirens (Clearance) * 2.6 L/min

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Hepatic

Rute Eliminasi

The major route of metabolism is cytochrome CYP3A4 mediated N-demethylation to norpropoxyphene, which is excreted by the kidneys. In 48 hours, approximately 20% to 25% of the administered dose of propoxyphene is excreted via the urine, most of which is free or conjugated norpropoxyphene.

Interaksi Makanan

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

Interaksi Obat

1276 Data
Buprenorphine Dextropropoxyphene may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Dextropropoxyphene.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Dextropropoxyphene.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Dextropropoxyphene.
Hydrocodone Dextropropoxyphene 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 Dextropropoxyphene.
Magnesium sulfate The therapeutic efficacy of Dextropropoxyphene can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Dextropropoxyphene may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Dextropropoxyphene may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Dextropropoxyphene.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Dextropropoxyphene.
Orphenadrine Dextropropoxyphene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Dextropropoxyphene 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 Dextropropoxyphene.
Pramipexole Dextropropoxyphene may increase the sedative activities of Pramipexole.
Ropinirole Dextropropoxyphene may increase the sedative activities of Ropinirole.
Rotigotine Dextropropoxyphene may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Dextropropoxyphene.
Sodium oxybate Dextropropoxyphene may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Dextropropoxyphene 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 Dextropropoxyphene.
Thalidomide Dextropropoxyphene may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Dextropropoxyphene may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Alvimopan The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Alvimopan.
Desmopressin The risk or severity of hyponatremia can be increased when Dextropropoxyphene is combined with Desmopressin.
Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Dextropropoxyphene.
Codeine The risk or severity of adverse effects can be increased when Codeine is combined with Dextropropoxyphene.
Hydromorphone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Dextropropoxyphene.
Oxycodone The risk or severity of adverse effects can be increased when Oxycodone is combined with Dextropropoxyphene.
Naltrexone The therapeutic efficacy of Dextropropoxyphene can be decreased when used in combination with Naltrexone.
Sufentanil The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Sufentanil.
Levorphanol The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Remifentanil.
Diphenoxylate The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Diamorphine.
Bezitramide The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Bezitramide.
Ethylmorphine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Dihydromorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Nicomorphine.
Meptazinol The therapeutic efficacy of Dextropropoxyphene can be decreased when used in combination with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Carfentanil, C-11.
Meperidine The risk or severity of adverse effects can be increased when Meperidine is combined with Dextropropoxyphene.
Alfentanil The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Alfentanil.
Benzhydrocodone The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Benzhydrocodone.
Naloxegol The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Naloxegol.
Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Dextropropoxyphene.
Succinylcholine The risk or severity of bradycardia can be increased when Succinylcholine is combined with Dextropropoxyphene.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Dextropropoxyphene.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Dextropropoxyphene.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Dextropropoxyphene.
Colchicine The metabolism of Colchicine can be decreased when combined with Dextropropoxyphene.
Fentanyl The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Fentanyl.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Dextropropoxyphene.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Dextropropoxyphene.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Dextropropoxyphene.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Dextropropoxyphene.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Dextropropoxyphene.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Dextropropoxyphene.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Dextropropoxyphene.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Dextropropoxyphene.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Dextropropoxyphene.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Dextropropoxyphene.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Dextropropoxyphene.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Dextropropoxyphene.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Dextropropoxyphene.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Dextropropoxyphene.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Dextropropoxyphene.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Dextropropoxyphene.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Dextropropoxyphene.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Dextropropoxyphene.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Dextropropoxyphene.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Dextropropoxyphene.
Mirabegron The serum concentration of Dextropropoxyphene can be increased when it is combined with Mirabegron.
Mirtazapine Dextropropoxyphene may increase the serotonergic activities of Mirtazapine.
Fluvoxamine The risk or severity of serotonin syndrome can be increased when Dextropropoxyphene is combined with Fluvoxamine.
Citalopram The risk or severity of serotonin syndrome can be increased when Dextropropoxyphene is combined with Citalopram.
Duloxetine The risk or severity of serotonin syndrome can be increased when Dextropropoxyphene is combined with Duloxetine.
Sertraline The risk or severity of serotonin syndrome can be increased when Dextropropoxyphene is combined with Sertraline.
Sibutramine The risk or severity of serotonin syndrome can be increased when Dextropropoxyphene is combined with Sibutramine.
Zimelidine The risk or severity of serotonin syndrome can be increased when Dextropropoxyphene is combined with Zimelidine.

Target Protein

Mu-type opioid receptor OPRM1
Delta-type opioid receptor OPRD1
Kappa-type opioid receptor OPRK1
Liver carboxylesterase 1 CES1
NMDA receptor GRIN1

Referensi & Sumber

Synthesis reference: Carl R. White, "Synthesis and purification of d-propoxyphene hydrochloride." U.S. Patent US4661625, issued April, 1973.
Artikel (PubMed)
  • PMID: 12818953
    Coda BA, Rudy AC, Archer SM, Wermeling DP: Pharmacokinetics and bioavailability of single-dose intranasal hydromorphone hydrochloride in healthy volunteers. Anesth Analg. 2003 Jul;97(1):117-23, table of contents.
  • PMID: 10690289
    Ulens C, Daenens P, Tytgat J: Norpropoxyphene-induced cardiotoxicity is associated with changes in ion-selectivity and gating of HERG currents. Cardiovasc Res. 1999 Dec;44(3):568-78.
  • PMID: 6249436
    Tyers MB: A classification of opiate receptors that mediate antinociception in animals. Br J Pharmacol. 1980 Jul;69(3):503-12.

Contoh Produk & Brand

Produk: 72 • International brands: 6
Produk
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    Tablet • 65 mg • Oral • Canada • Approved
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  • Balacet 325
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Balacet 325
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Darvocet A500
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  • Darvocet A500
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Darvocet N100
    Tablet, film coated • - • Oral • US • Approved
Menampilkan 8 dari 72 produk.
International Brands
  • Abalgin — DLF
  • Dacoton — Standard
  • Deprancol — Parke Davis
  • Depronal — Pfizer
  • Dolene
  • Doloxene — Aspen Pharmacare

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