Peringatan Keamanan

Oral LD50 in rat is 8900 mg/kg MSDS. Neurological adverse reactions, including convulsions, may occur with the attainment of high CSF levels of beta-lactams. Neutropenia can occur if high doses are administered consistently for over 2 weeks.

Benzylpenicillin

DB01053

small molecule approved vet_approved

Deskripsi

Benzylpenicillin (Penicillin G) is narrow spectrum antibiotic used to treat infections caused by susceptible bacteria. It is a natural penicillin antibiotic that is administered intravenously or intramuscularly due to poor oral absorption. Penicillin G may also be used in some cases as prophylaxis against susceptible organisms.

Natural penicillins are considered the drugs of choice for several infections caused by susceptible gram positive aerobic organisms, such as *Streptococcus pneumoniae*, groups A, B, C and G streptococci, nonenterococcal group D streptococci, viridans group streptococci, and non-penicillinase producing staphylococcus. Aminoglycosides may be added for synergy against group B streptococcus (*S. agalactiae*), *S. viridans*, and *Enterococcus faecalis*. The natural penicillins may also be used as first or second line agents against susceptible gram positive aerobic bacilli such as *Bacillus anthracis*, *Corynebacterium diphtheriae*, and *Erysipelothrix rhusiopathiae*. Natural penicillins have limited activity against gram negative organisms; however, they may be used in some cases to treat infections caused by *Neisseria meningitidis* and *Pasteurella*. They are not generally used to treat anaerobic infections. Resistance patterns, susceptibility and treatment guidelines vary across regions.

Struktur Molekul 2D

Berat 334.39
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In adults with normal renal function is reportedly 0.4–0.9 hours
Volume Distribusi 0.53–0.67 L/kg in adults with normal renal function
Klirens (Clearance) 560ml/min in healthy humans

Absorpsi

Rapidly absorbed following both intramuscular and subcutaneous injection. Initial blood levels following parenteral administration are high but transient. Oral absorption in fasting, healthy humans is only about 15-30% as it is very susceptible to acid-catalyzed hydrolysis.

Metabolisme

About 16-30% of an intramuscular dose is metabolized to penicilloic acid, an inactive metabolite. Small amounts of 6-aminopenicillanic acid have been recovered in the urine of patients on penicillin G. A small percentage of the drug appears to be hydroxylated into one or more active metabolites, which are also excreted via urine.

Rute Eliminasi

Penicillin G is eliminated by the kidneys. Nonrenal clearance includes hepatic metabolism and, to a lesser extent, biliary excretion.

Interaksi Obat

503 Data
Methotrexate The excretion of Methotrexate can be decreased when combined with Benzylpenicillin.
Probenecid The excretion of Benzylpenicillin can be decreased when combined with Probenecid.
Doxycycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Doxycycline.
Lymecycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Lymecycline.
Clomocycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Clomocycline.
Tigecycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Tigecycline.
Oxytetracycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Oxytetracycline.
Demeclocycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Demeclocycline.
Tetracycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Tetracycline.
Metacycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Metacycline.
Minocycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Minocycline.
Rolitetracycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Rolitetracycline.
Sarecycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Sarecycline.
Eravacycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Eravacycline.
Omadacycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Omadacycline.
Penimepicycline The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Penimepicycline.
Aspartame The excretion of Benzylpenicillin can be decreased when combined with Aspartame.
Pravastatin The excretion of Benzylpenicillin can be decreased when combined with Pravastatin.
Pantoprazole The excretion of Benzylpenicillin can be decreased when combined with Pantoprazole.
Cefotiam The excretion of Benzylpenicillin can be decreased when combined with Cefotiam.
Liothyronine The excretion of Benzylpenicillin can be decreased when combined with Liothyronine.
Conjugated estrogens The excretion of Benzylpenicillin can be decreased when combined with Conjugated estrogens.
Indomethacin The excretion of Benzylpenicillin can be decreased when combined with Indomethacin.
Aminohippuric acid The excretion of Benzylpenicillin can be decreased when combined with Aminohippuric acid.
Lansoprazole The excretion of Benzylpenicillin can be decreased when combined with Lansoprazole.
Cefalotin The excretion of Benzylpenicillin can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Benzylpenicillin can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Benzylpenicillin can be decreased when combined with Cefotaxime.
Zidovudine The excretion of Benzylpenicillin can be decreased when combined with Zidovudine.
Cimetidine The excretion of Benzylpenicillin can be decreased when combined with Cimetidine.
Guanidine The excretion of Benzylpenicillin can be decreased when combined with Guanidine.
Piroxicam The excretion of Benzylpenicillin can be decreased when combined with Piroxicam.
Cephalexin The excretion of Benzylpenicillin can be decreased when combined with Cephalexin.
Enalapril The excretion of Benzylpenicillin can be decreased when combined with Enalapril.
Diclofenac The excretion of Benzylpenicillin can be decreased when combined with Diclofenac.
Leucovorin The excretion of Benzylpenicillin can be decreased when combined with Leucovorin.
Esomeprazole The excretion of Benzylpenicillin can be decreased when combined with Esomeprazole.
Acyclovir The excretion of Benzylpenicillin can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Benzylpenicillin can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Benzylpenicillin can be decreased when combined with Cefaclor.
Quinidine The excretion of Benzylpenicillin can be decreased when combined with Quinidine.
Dinoprostone The excretion of Benzylpenicillin can be decreased when combined with Dinoprostone.
Famotidine The excretion of Benzylpenicillin can be decreased when combined with Famotidine.
Salicylic acid The excretion of Benzylpenicillin can be decreased when combined with Salicylic acid.
Acetylsalicylic acid The excretion of Benzylpenicillin can be decreased when combined with Acetylsalicylic acid.
Ganciclovir The excretion of Benzylpenicillin can be decreased when combined with Ganciclovir.
Ketoprofen The excretion of Benzylpenicillin can be decreased when combined with Ketoprofen.
Ibuprofen The excretion of Benzylpenicillin can be decreased when combined with Ibuprofen.
Novobiocin The excretion of Benzylpenicillin can be decreased when combined with Novobiocin.
Succinic acid The excretion of Succinic acid can be decreased when combined with Benzylpenicillin.
Citrulline The excretion of Citrulline can be decreased when combined with Benzylpenicillin.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Benzylpenicillin.
Tenofovir disoproxil The excretion of Tenofovir disoproxil can be decreased when combined with Benzylpenicillin.
Piperacillin The excretion of Piperacillin can be decreased when combined with Benzylpenicillin.
Trifluridine The excretion of Trifluridine can be decreased when combined with Benzylpenicillin.
Allopurinol The excretion of Allopurinol can be decreased when combined with Benzylpenicillin.
Cefdinir The excretion of Cefdinir can be decreased when combined with Benzylpenicillin.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Benzylpenicillin.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Benzylpenicillin.
Fluorescein The excretion of Fluorescein can be decreased when combined with Benzylpenicillin.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Benzylpenicillin.
Ranitidine The excretion of Ranitidine can be decreased when combined with Benzylpenicillin.
Quinapril The excretion of Quinapril can be decreased when combined with Benzylpenicillin.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Benzylpenicillin.
Captopril The excretion of Captopril can be decreased when combined with Benzylpenicillin.
Sitagliptin The excretion of Sitagliptin can be decreased when combined with Benzylpenicillin.
Cefazolin The excretion of Cefazolin can be decreased when combined with Benzylpenicillin.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Benzylpenicillin.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Benzylpenicillin.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Benzylpenicillin.
Tazobactam The excretion of Tazobactam can be decreased when combined with Benzylpenicillin.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Benzylpenicillin.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Benzylpenicillin.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Benzylpenicillin.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Benzylpenicillin.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Benzylpenicillin.
Doripenem The excretion of Doripenem can be decreased when combined with Benzylpenicillin.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Benzylpenicillin.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Benzylpenicillin.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Benzylpenicillin.
Avibactam The excretion of Avibactam can be decreased when combined with Benzylpenicillin.
Eluxadoline The excretion of Eluxadoline can be decreased when combined with Benzylpenicillin.
Silibinin The excretion of Silibinin can be decreased when combined with Benzylpenicillin.
Tenofovir alafenamide The excretion of Tenofovir alafenamide can be decreased when combined with Benzylpenicillin.
Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Benzylpenicillin.
Relebactam The excretion of Relebactam can be decreased when combined with Benzylpenicillin.
Tenofovir The excretion of Tenofovir can be decreased when combined with Benzylpenicillin.
Melatonin The excretion of Benzylpenicillin can be decreased when combined with Melatonin.
Ouabain The excretion of Benzylpenicillin can be decreased when combined with Ouabain.
Cefadroxil The excretion of Benzylpenicillin can be decreased when combined with Cefadroxil.
Ceftriaxone The excretion of Benzylpenicillin can be decreased when combined with Ceftriaxone.
Cefamandole The excretion of Benzylpenicillin can be decreased when combined with Cefamandole.
Cefoperazone The excretion of Benzylpenicillin can be decreased when combined with Cefoperazone.
Liotrix The excretion of Benzylpenicillin can be decreased when combined with Liotrix.
Cilastatin The excretion of Benzylpenicillin can be decreased when combined with Cilastatin.
trans-2-hydroxycinnamic acid The excretion of Benzylpenicillin can be decreased when combined with trans-2-hydroxycinnamic acid.
Topiroxostat The excretion of Benzylpenicillin can be decreased when combined with Topiroxostat.
Benzoic acid The excretion of Benzylpenicillin can be decreased when combined with Benzoic acid.
Caprylic acid The excretion of Benzylpenicillin can be decreased when combined with Caprylic acid.
Ataluren The excretion of Benzylpenicillin can be decreased when combined with Ataluren.

Target Protein

Peptidoglycan synthase FtsI ftsI
Penicillin-binding protein 1A mrcA
Penicillin-binding protein 1B mrcB
Penicillin-binding protein 1C pbpC
Penicillin-binding protein 3 pbp3
Organic anion transporter 3 SLC22A8
Solute carrier family 15 member 1 SLC15A1
Solute carrier family 15 member 2 SLC15A2

Referensi & Sumber

Synthesis reference: Gunter Schumacher, Peter Buckel, "Plasmids for the increased production of penicillin G amidase." U.S. Patent US5053335, issued May, 1984.
Artikel (PubMed)
  • PMID: 16695494
    Eagle H, Newman E, Musselman AD, Robinson M, Birmingham M: THE RENAL CLEARANCE OF PENICILLINS F, G, K, AND X IN RABBITS AND MAN. J Clin Invest. 1947 Sep;26(5):903-18.

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