Peringatan Keamanan

Procaine benzylpenicillin is associated with the pain at the injection site, blood clotting problems, and seizures. Treatment targeted against syphilis is often associated with Jarisch-Herxheimer reaction. The main unwanted effects are hypersensitivity reactions caused by the degradation products of penicillin, which combine with host protein and become antigenic. Other common adverse effects include skin rashes, fever and delayed serum sickness. Rare but fatal anaphylactic shock may occur. Oral LD50 values in mouse and rat are > 2000 mg/kg. Overdosage can cause convulsions, paralysis and even death. Emesis and gastric lavage may be of value if begun within a few hours of injection. Excessive blood concentrations can be lowered by haemodialysis L783.

Procaine benzylpenicillin

DB09320

small molecule approved vet_approved

Deskripsi

Procaine benzylpenicillin (INN), also known as procaine G penicillin, is an injectable antiobiotic. It is a poorly soluble salt form of penicillin which is a combination of naturally occuring benzylpenicillin (penicillin G) and the local anaesthetic agent procaine in equimolar amounts. Procaine benzylpenicillin is administered by deep intramuscular injection. It is slowly absorbed and hydrolyzed to benzylpenicillin. This drug is used where prolonged exposure to benzylpenicillin at a low concentration is required. This combination is aimed at reducing the pain and discomfort associated with a large intramuscular injection of penicillin. It is widely used in veterinary settings. Benzylpenicillin is active against a wide range of organisms and is the drug of first choice for many infections.

Struktur Molekul 2D

Berat 570.71
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Intramuscular injection of benzylpenicillin has a plasma half-life of 30 minutes [L783].
Volume Distribusi The drug is distributed throughout the body tissues in widely varying amounts and spinal fluid to a lesser degree. Highest levels are found in the kidneys with lesser amounts in the liver, skin, and intestines. It displays low solubility thus results in blood serum levels much lower but more prolonged than other parenteral penicillins.
Klirens (Clearance) -

Absorpsi

After intramuscular injection, it dissolves slowly at the site of injection, giving a plateau type of blood level at about 4 hours which falls slowly over a period of the next 15 to 20 hours.

Metabolisme

Procaine is rapidly hydrolyzed by plasma esterases to nontoxic metabolites.

Rute Eliminasi

The drug is rapidly and predominantly cleared via renal elimination, with 90% being through tubular secretion. Approximately 60 -90 % of a dose of parenteral penicillin G is excreted in the urine within 24 to 36 hours.

Interaksi Obat

868 Data
Methotrexate The excretion of Methotrexate can be decreased when combined with Procaine benzylpenicillin.
Probenecid The excretion of Procaine benzylpenicillin can be decreased when combined with Probenecid.
Doxycycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Doxycycline.
Lymecycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Lymecycline.
Clomocycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Clomocycline.
Tigecycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Tigecycline.
Oxytetracycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Oxytetracycline.
Demeclocycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Demeclocycline.
Tetracycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Tetracycline.
Metacycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Metacycline.
Minocycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Minocycline.
Rolitetracycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Rolitetracycline.
Sarecycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Sarecycline.
Eravacycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Eravacycline.
Omadacycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Omadacycline.
Penimepicycline The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Penimepicycline.
Dicoumarol Procaine benzylpenicillin may increase the anticoagulant activities of Dicoumarol.
Phenindione Procaine benzylpenicillin may increase the anticoagulant activities of Phenindione.
Phenprocoumon Procaine benzylpenicillin may increase the anticoagulant activities of Phenprocoumon.
Acenocoumarol Procaine benzylpenicillin may increase the anticoagulant activities of Acenocoumarol.
4-hydroxycoumarin Procaine benzylpenicillin may increase the anticoagulant activities of 4-hydroxycoumarin.
Coumarin Procaine benzylpenicillin may increase the anticoagulant activities of Coumarin.
(R)-warfarin Procaine benzylpenicillin may increase the anticoagulant activities of (R)-warfarin.
Ethyl biscoumacetate Procaine benzylpenicillin may increase the anticoagulant activities of Ethyl biscoumacetate.
Fluindione Procaine benzylpenicillin may increase the anticoagulant activities of Fluindione.
Clorindione Procaine benzylpenicillin may increase the anticoagulant activities of Clorindione.
Diphenadione Procaine benzylpenicillin may increase the anticoagulant activities of Diphenadione.
Tioclomarol Procaine benzylpenicillin may increase the anticoagulant activities of Tioclomarol.
(S)-Warfarin Procaine benzylpenicillin may increase the anticoagulant activities of (S)-Warfarin.
Diethylstilbestrol The therapeutic efficacy of Diethylstilbestrol can be decreased when used in combination with Procaine benzylpenicillin.
Desogestrel The therapeutic efficacy of Desogestrel can be decreased when used in combination with Procaine benzylpenicillin.
Levonorgestrel The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Procaine benzylpenicillin.
Progesterone The therapeutic efficacy of Progesterone can be decreased when used in combination with Procaine benzylpenicillin.
Norethisterone The therapeutic efficacy of Norethisterone can be decreased when used in combination with Procaine benzylpenicillin.
Ethynodiol diacetate The therapeutic efficacy of Ethynodiol diacetate can be decreased when used in combination with Procaine benzylpenicillin.
Mifepristone The therapeutic efficacy of Mifepristone can be decreased when used in combination with Procaine benzylpenicillin.
Norgestimate The therapeutic efficacy of Norgestimate can be decreased when used in combination with Procaine benzylpenicillin.
Ethinylestradiol The therapeutic efficacy of Ethinylestradiol can be decreased when used in combination with Procaine benzylpenicillin.
Mestranol The therapeutic efficacy of Mestranol can be decreased when used in combination with Procaine benzylpenicillin.
Octylphenoxy polyethoxyethanol The therapeutic efficacy of Octylphenoxy polyethoxyethanol can be decreased when used in combination with Procaine benzylpenicillin.
Cyproterone acetate The therapeutic efficacy of Cyproterone acetate can be decreased when used in combination with Procaine benzylpenicillin.
Trestolone The therapeutic efficacy of Trestolone can be decreased when used in combination with Procaine benzylpenicillin.
Norelgestromin The therapeutic efficacy of Norelgestromin can be decreased when used in combination with Procaine benzylpenicillin.
Gestodene The therapeutic efficacy of Gestodene can be decreased when used in combination with Procaine benzylpenicillin.
Hydroxyprogesterone caproate The therapeutic efficacy of Hydroxyprogesterone caproate can be decreased when used in combination with Procaine benzylpenicillin.
Ulipristal The therapeutic efficacy of Ulipristal can be decreased when used in combination with Procaine benzylpenicillin.
Norethynodrel The therapeutic efficacy of Norethynodrel can be decreased when used in combination with Procaine benzylpenicillin.
Norgestrel The therapeutic efficacy of Norgestrel can be decreased when used in combination with Procaine benzylpenicillin.
Cloprostenol The therapeutic efficacy of Cloprostenol can be decreased when used in combination with Procaine benzylpenicillin.
Gestrinone The therapeutic efficacy of Gestrinone can be decreased when used in combination with Procaine benzylpenicillin.
Nomegestrol The therapeutic efficacy of Nomegestrol can be decreased when used in combination with Procaine benzylpenicillin.
Lynestrenol The therapeutic efficacy of Lynestrenol can be decreased when used in combination with Procaine benzylpenicillin.
Gossypol The therapeutic efficacy of Gossypol can be decreased when used in combination with Procaine benzylpenicillin.
Ormeloxifene The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Procaine benzylpenicillin.
Chlormadinone The therapeutic efficacy of Chlormadinone can be decreased when used in combination with Procaine benzylpenicillin.
Norgestrienone The therapeutic efficacy of Norgestrienone can be decreased when used in combination with Procaine benzylpenicillin.
Quingestanol The therapeutic efficacy of Quingestanol can be decreased when used in combination with Procaine benzylpenicillin.
Demegestone The therapeutic efficacy of Demegestone can be decreased when used in combination with Procaine benzylpenicillin.
Etynodiol The therapeutic efficacy of Etynodiol can be decreased when used in combination with Procaine benzylpenicillin.
Estradiol benzoate The therapeutic efficacy of Estradiol benzoate can be decreased when used in combination with Procaine benzylpenicillin.
Nomegestrol acetate The therapeutic efficacy of Nomegestrol acetate can be decreased when used in combination with Procaine benzylpenicillin.
Norethindrone enanthate The therapeutic efficacy of Norethindrone enanthate can be decreased when used in combination with Procaine benzylpenicillin.
Framycetin The serum concentration of Framycetin can be decreased when it is combined with Procaine benzylpenicillin.
Paromomycin The serum concentration of Paromomycin can be decreased when it is combined with Procaine benzylpenicillin.
Geneticin The serum concentration of Geneticin can be decreased when it is combined with Procaine benzylpenicillin.
Apramycin The serum concentration of Apramycin can be decreased when it is combined with Procaine benzylpenicillin.
Neamine The serum concentration of Neamine can be decreased when it is combined with Procaine benzylpenicillin.
Puromycin The serum concentration of Puromycin can be decreased when it is combined with Procaine benzylpenicillin.
Dihydrostreptomycin The serum concentration of Dihydrostreptomycin can be decreased when it is combined with Procaine benzylpenicillin.
Hygromycin B The serum concentration of Hygromycin B can be decreased when it is combined with Procaine benzylpenicillin.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Procaine benzylpenicillin.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Procaine benzylpenicillin.
Acemetacin Acemetacin may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Cyclosporine Cyclosporine may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Procaine benzylpenicillin which could result in a higher serum level.

Target Protein

Penicillin-binding protein dacA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17472651
    Olsen L, Ingvast-Larsson C, Brostrom H, Larsson P, Tjalve H: Clinical signs and etiology of adverse reactions to procaine benzylpenicillin and sodium/potassium benzylpenicillin in horses. J Vet Pharmacol Ther. 2007 Jun;30(3):201-7.
  • PMID: 10895905
    Uboh CE, Soma LR, Luo Y, McNamara E, Fennell MA, May L, Teleis DC, Rudy JA, Watson AO: Pharmacokinetics of penicillin G procaine versus penicillin G potassium and procaine hydrochloride in horses. Am J Vet Res. 2000 Jul;61(7):811-5.
  • PMID: 7944023
    Papich MG, Korsrud GO, Boison JO, Yates WD, MacNeil JD, Janzen ED, McKinnon JJ, Landry DA: Disposition of penicillin G after administration of benzathine penicillin G, or a combination of benzathine penicillin G and procaine penicillin G in cattle. Am J Vet Res. 1994 Jun;55(6):825-30.
Textbook
  • ISBN: 978-0-7020-5362-7
    51. (2016). In Rang & Dale's pharmacology (8th ed., pp. 626-641). Elsevier Churchill Livingstone.

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