Peringatan Keamanan

Mild adverse effects include nausea, vomiting, diarrhea, headache, and dizziness L1893.

LD50 in rats is 535 mg/kg L1895.

Reported effects in humans in case of overdose include gastrointestinal disturbance, central nervous system effects, and superficial skin reactions. In one study, serum aspartate aminotransferase (AST) and serum alanine-aminotransferase (ALT) values were increased in approximately 2% of patients L1906.

Pyrantel should be used with caution in patients with severe malnutrition or anemia. Supportive therapy is recommended for anemic, dehydrated, or malnourished patients before administration of the drug L1898.

Pyrantel pamoate has been placed in pregnancy category C. This refers to the fact that animal studies have revealed adverse effects on the fetus (teratogenic/embryocidal, or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus L1894.Data on the use of pyrantel pamoate in pregnant women are quite limited. In mass treatment programs for which the World Health Organization (WHO) has observed that the benefits of treatment outweigh the risks, WHO allows the use of pyrantel pamoate in the 2nd and 3rd trimesters of pregnancy, due to the fact that the effects of pyrantel on birth outcome are uncertain. The risk of treatment in pregnant women already known to have an infection needs to be balanced with the risk of disease progression if treatment were to be omitted L1894. Individuals with liver disease are more susceptible to the toxicity in cases of pyrantel overexposure L1894, L1897.

There are no data regarding the presence of pyrantel in breast milk. Pyrantel is poorly absorbed from the GI tract; therefore, excretion into breast milk may be minimal. Some experts recommend that a single dose of pyrantel therapy may be given to breastfeeding women L1893.

Pyrantel

DB11156

small molecule approved vet_approved

Deskripsi

Pyrantel is a pyrimidine-derivative anthelmintic agent for the oral treatment of various parasitic worm infections including ascariasis, hookworm infections, enterobiasis (pinworm infection), trichostrongyliasis, and trichinellosis L1904.

Pyrantel was initially described in 1965 by researchers from Pfizer who sought cyclic amidines with suitable pharmacokinetic properties (specifically, duration of action) for use as an anthelmintic drug. Pyrantel is mainly available in formulations for dogs and cats as the embonate salt, containing a 34.7% pyrantel base L1900.

Pyrantel is on the World Health Organization's List of Essential Medicines, which are the safest and most effective medicines required in a functioning health system L1901, L1902.

A depolarizing neuromuscular-blocking agent causing longstanding nicotinic receptor activation, resulting in spastic paralysis of susceptible nematodes (worms). Pyrantel has shown to be effective after a single dose L1905.

In humans, it is administered as pyrantel pamoate A32282,A32283,L1893,L1898.

Struktur Molekul 2D

Berat 206.31
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In pigs, following intravenous administration, pyrantel exhibited a half-life of 1.75 +/- 0.19 h [A32291].
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Pyrantel is poorly absorbed from the GI tract of humans L1893, L1908. Peak serum concentrations occur 1–3 hours after a single dose L1904.

Metabolisme

Pyrantel is administered orally. The poor solubility of the pamoate salt offers the advantage of reduced absorption from the gastrointestinal tract and allows the drug to reach and act against parasites in the large intestine. Metabolism of pyrantel is rapid L1991. The absorbed drug is partly metabolized in the liver L1907.

Rute Eliminasi

Approximately 50% of an oral dose is excreted unchanged in feces; 7% excreted in urine as unchanged drug and metabolites L1904.

Interaksi Obat

1389 Data
Buprenorphine Pyrantel 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 Pyrantel.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Pyrantel.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Pyrantel.
Hydrocodone Pyrantel 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 Pyrantel.
Magnesium sulfate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Pyrantel may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Pyrantel may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Pyrantel.
Mirtazapine Pyrantel may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Pyrantel.
Orphenadrine Pyrantel may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Pyrantel 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 Pyrantel.
Pramipexole Pyrantel may increase the sedative activities of Pramipexole.
Ropinirole Pyrantel may increase the sedative activities of Ropinirole.
Rotigotine Pyrantel may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Pyrantel.
Sodium oxybate Pyrantel may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Pyrantel 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 Pyrantel.
Thalidomide Pyrantel may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Pyrantel may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Capreomycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Capreomycin.
Botulinum toxin type B The therapeutic efficacy of Pyrantel can be increased when used in combination with Botulinum toxin type B.
Botulinum toxin type A The therapeutic efficacy of Pyrantel can be increased when used in combination with Botulinum toxin type A.
Cyclosporine The therapeutic efficacy of Pyrantel can be increased when used in combination with Cyclosporine.
Doxycycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Doxycycline.
Lymecycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Lymecycline.
Piperacillin The therapeutic efficacy of Pyrantel can be increased when used in combination with Piperacillin.
Framycetin The therapeutic efficacy of Pyrantel can be increased when used in combination with Framycetin.
Clomocycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Clomocycline.
Quinine The therapeutic efficacy of Pyrantel can be increased when used in combination with Quinine.
Tigecycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Tigecycline.
Oxytetracycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Oxytetracycline.
Chloroquine The therapeutic efficacy of Pyrantel can be increased when used in combination with Chloroquine.
Demeclocycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Demeclocycline.
Mecamylamine The therapeutic efficacy of Pyrantel can be increased when used in combination with Mecamylamine.
Tobramycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Tobramycin.
Tetracycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Tetracycline.
Gentamicin The therapeutic efficacy of Pyrantel can be increased when used in combination with Gentamicin.
Etacrynic acid The therapeutic efficacy of Pyrantel can be increased when used in combination with Etacrynic acid.
Metacycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Metacycline.
Netilmicin The therapeutic efficacy of Pyrantel can be increased when used in combination with Netilmicin.
Neomycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Neomycin.
Streptomycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Streptomycin.
Colistimethate The therapeutic efficacy of Pyrantel can be increased when used in combination with Colistimethate.
Kanamycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Kanamycin.
Rolitetracycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Rolitetracycline.
Magnesium oxide The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium oxide.
Magnesium cation The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium cation.
Paromomycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Paromomycin.
Lincomycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Lincomycin.
Ribostamycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Ribostamycin.
Geneticin The therapeutic efficacy of Pyrantel can be increased when used in combination with Geneticin.
Apramycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Apramycin.
Gentamicin C1a The therapeutic efficacy of Pyrantel can be increased when used in combination with Gentamicin C1a.
Neamine The therapeutic efficacy of Pyrantel can be increased when used in combination with Neamine.
Arbekacin The therapeutic efficacy of Pyrantel can be increased when used in combination with Arbekacin.
Viomycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Viomycin.
Puromycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Puromycin.
Magnesium hydroxide The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium hydroxide.
Magnesium trisilicate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium trisilicate.
Magnesium chloride The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium chloride.
Magnesium acetate tetrahydrate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium acetate tetrahydrate.
Magnesium carbonate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium carbonate.
Magnesium citrate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium citrate.
Magnesium glycinate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium glycinate.
Magnesium Aluminum Silicate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium Aluminum Silicate.
Dihydrostreptomycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Dihydrostreptomycin.
Hygromycin B The therapeutic efficacy of Pyrantel can be increased when used in combination with Hygromycin B.
Sisomicin The therapeutic efficacy of Pyrantel can be increased when used in combination with Sisomicin.
Magnesium silicate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium silicate.
Penimepicycline The therapeutic efficacy of Pyrantel can be increased when used in combination with Penimepicycline.
Magnesium aspartate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium aspartate.
Isepamicin The therapeutic efficacy of Pyrantel can be increased when used in combination with Isepamicin.
Magnesium gluconate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium gluconate.
Magnesium orotate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium orotate.
Magnesium phosphate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium phosphate.
Magnesium acetate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium acetate.
Dantrolene The therapeutic efficacy of Pyrantel can be increased when used in combination with Dantrolene.
Vancomycin The therapeutic efficacy of Pyrantel can be increased when used in combination with Vancomycin.
Quinidine The therapeutic efficacy of Pyrantel can be increased when used in combination with Quinidine.
Procainamide The therapeutic efficacy of Pyrantel can be increased when used in combination with Procainamide.
Plazomicin The therapeutic efficacy of Pyrantel can be increased when used in combination with Plazomicin.
Magnesium stearate The therapeutic efficacy of Pyrantel can be increased when used in combination with Magnesium stearate.
Colistin The therapeutic efficacy of Pyrantel can be increased when used in combination with Colistin.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Pyrantel.
Ethanol Pyrantel may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Pyrantel may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Pyrantel.
Fluvoxamine The risk or severity of adverse effects can be increased when Pyrantel is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Pyrantel is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Pyrantel is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Pyrantel is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Pyrantel is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Pyrantel is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Pyrantel is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Pyrantel is combined with Nefazodone.

Target Protein

G-protein coupled receptor 35 GPR35
Muscarinic acetylcholine receptor M1 CHRM1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 5417856
    Aubry ML, Cowell P, Davey MJ, Shevde S: Aspects of the pharmacology of a new anthelmintic: pyrantel. Br J Pharmacol. 1970 Feb;38(2):332-44.
  • PMID: 11489460
    Rayes D, De Rosa MJ, Spitzmaul G, Bouzat C: The anthelmintic pyrantel acts as a low efficacious agonist and an open-channel blocker of mammalian acetylcholine receptors. Neuropharmacology. 2001 Aug;41(2):238-45.
  • PMID: 25015542
    Gokbulut C, Aksit D, Smaldone G, Mariani U, Veneziano V: Plasma pharmacokinetics, faecal excretion and efficacy of pyrantel pamoate paste and granule formulations following per os administration in donkeys naturally infected with intestinal strongylidae. Vet Parasitol. 2014 Sep 15;205(1-2):186-92. doi: 10.1016/j.vetpar.2014.06.026. Epub 2014 Jun 26.
  • PMID: 7993990
    Fasanmade AA, Akanni AO, Olaniyi AA, Fasanmade AA, Tayo F: Bioequivalence of pyrantel pamoate dosage forms in healthy human subjects. Biopharm Drug Dispos. 1994 Aug;15(6):527-34.
  • PMID: 9024887
    Bjorn H, Hennessy DR, Friis C: The kinetic disposition of pyrantel citrate and pamoate and their efficacy against pyrantel-resistant Oesophagostomum dentatum in pigs. Int J Parasitol. 1996 Dec;26(12):1375-80.
  • PMID: 12920490
    Li XQ, Bjorkman A, Andersson TB, Gustafsson LL, Masimirembwa CM: Identification of human cytochrome P(450)s that metabolise anti-parasitic drugs and predictions of in vivo drug hepatic clearance from in vitro data. Eur J Clin Pharmacol. 2003 Sep;59(5-6):429-42. Epub 2003 Aug 12.

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