Peringatan Keamanan

Generally, pholcodine is significantly less toxic than codeine. Nonetheless, it is important to consider the significant depressive respiratory effect.L1202

Pholcodine

DB09209

small molecule approved illicit

Deskripsi

Pholcodine formula is 3-o-morpholinoethylmorphine and it is classified as an antitussive which is defined as an opioid cough suppressant. It belongs to the opioid family of compounds and it is widely used.A31738 Pholcodine activity is the suppression of unproductive cough and it also has a mild sedative effect with little or no analgesic effects.A31742 Pholcodine is not prescribed in the United States where it is classed as a Schedule I drug. It is categorized as Class B drug in the UK and officially taken out of the shelves in 2008. Pholcodine is not approved in Canada.

Struktur Molekul 2D

Berat 398.4953
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) After oral administration of 60 mg of pholcodine, the half-life in plasma, saliva and urine are 45, 55 and 45 hours respectively.[A31738]
Volume Distribusi The reported volume of distribution depends on the pharmacokinetic model and it can be of 265L based on a one-compartment model to 3207L in a two-compartment model.[A31747]
Klirens (Clearance) After oral administration of 60 mg of pholcodine, the clearance rate was reported to be 126 ml/min.[A31738]

Absorpsi

After oral administration of 60 mg of pholcodine, the Tmax and Cmax are reported to be 1.3 hours and 26.3 ng/ml. In the same administration, the AUC in plasma and saliva are reported to be 1.67 and 6.61 mg h/l respectively. The absorption of pholcodine is reported to represent approximately 88% of the administered dose.A31738

Metabolisme

The metabolism of pholcodine seems to be very slowA31747 and due to the elimination profile, it is thought that most of the administered dose undergoes metabolism. There is some evidence in preclinical trials that indicate that morphine is a minor metabolite of pholcodine and that it accounts for 1% of the administered dose.A31738

Rute Eliminasi

After oral administration of pholcodine, the serum concentration peaks and declines in a monoexponential manner. The percent of the dose excreted unchanged is of approximately 25-30%. Part of the administered dose is composed by metabolites that can be recovered in urine. From the administered dose, the fecal excretion corresponds to the 5% of the administered dose as unchanged pholcodine.A31738

Interaksi Obat

751 Data
Linezolid Pholcodine may increase the serotonergic activities of Linezolid.
Furazolidone Pholcodine may increase the serotonergic activities of Furazolidone.
Procaine Pholcodine may increase the serotonergic activities of Procaine.
Tranylcypromine Pholcodine may increase the serotonergic activities of Tranylcypromine.
Phenelzine Pholcodine may increase the serotonergic activities of Phenelzine.
Minaprine Pholcodine may increase the serotonergic activities of Minaprine.
Selegiline Pholcodine may increase the serotonergic activities of Selegiline.
Procarbazine Pholcodine may increase the serotonergic activities of Procarbazine.
Moclobemide Pholcodine may increase the serotonergic activities of Moclobemide.
Isocarboxazid Pholcodine may increase the serotonergic activities of Isocarboxazid.
Rasagiline Pholcodine may increase the serotonergic activities of Rasagiline.
Pargyline Pholcodine may increase the serotonergic activities of Pargyline.
Clorgiline Pholcodine may increase the serotonergic activities of Clorgiline.
Iproniazid Pholcodine may increase the serotonergic activities of Iproniazid.
Nialamide Pholcodine may increase the serotonergic activities of Nialamide.
Safinamide Pholcodine may increase the serotonergic activities of Safinamide.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline Pholcodine may increase the serotonergic activities of 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Methylene blue Pholcodine may increase the serotonergic activities of Methylene blue.
Hydracarbazine Pholcodine may increase the serotonergic activities of Hydracarbazine.
Pirlindole Pholcodine may increase the serotonergic activities of Pirlindole.
Toloxatone Pholcodine may increase the serotonergic activities of Toloxatone.
Benmoxin Pholcodine may increase the serotonergic activities of Benmoxin.
Mebanazine Pholcodine may increase the serotonergic activities of Mebanazine.
Octamoxin Pholcodine may increase the serotonergic activities of Octamoxin.
Pheniprazine Pholcodine may increase the serotonergic activities of Pheniprazine.
Phenoxypropazine Pholcodine may increase the serotonergic activities of Phenoxypropazine.
Pivhydrazine Pholcodine may increase the serotonergic activities of Pivhydrazine.
Safrazine Pholcodine may increase the serotonergic activities of Safrazine.
Caroxazone Pholcodine may increase the serotonergic activities of Caroxazone.
Harmaline Pholcodine may increase the serotonergic activities of Harmaline.
Brofaromine Pholcodine may increase the serotonergic activities of Brofaromine.
Cyclosporine Cyclosporine may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Pholcodine which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Pholcodine which could result in a higher serum level.

Target Protein

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

Referensi & Sumber

Artikel (PubMed)
  • PMID: 3190994
    Chen ZR, Bochner F, Somogyi A: Pharmacokinetics of pholcodine in healthy volunteers: single and chronic dosing studies. Br J Clin Pharmacol. 1988 Oct;26(4):445-53.
  • PMID: 23283141
    Florvaag E, Johansson SG: The Pholcodine Case. Cough Medicines, IgE-Sensitization, and Anaphylaxis: A Devious Connection. World Allergy Organ J. 2012 Jul;5(7):73-8. doi: 10.1097/WOX.0b013e318261eccc.
  • PMID: 9804079
    Murata A, Taniguchi Y, Hashimoto Y, Kaneko Y, Takasaki Y, Kudoh S: Discrimination of productive and non-productive cough by sound analysis. Intern Med. 1998 Sep;37(9):732-5.
  • PMID: 3741728
    Findlay JW, Fowle AS, Butz RF, Jones EC, Weatherley BC, Welch RM, Posner J: Comparative disposition of codeine and pholcodine in man after single oral doses. Br J Clin Pharmacol. 1986 Jul;22(1):61-71.

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