Peringatan Keamanan

LD50 information

Clavulanic acid has demonstrated low oral acute toxicity in adult rodents, having an LD50 of more than 2000 mg/kg. The toxicity of clavulanic acid on pre-weaning rats was also studied. Gastrointestinal disturbance and mortality occurred, even at lower clavulanic acid doses of 125 mg/kg.L7898

Overdose information

Overdose information has been obtained for the combination of amoxicillin and clavulanic acid, as these drugs are frequently administered together in a single product.L7880,L7886 Changes in fluid and electrolyte balances and gastrointestinal symptoms may occur in the case of an overdose. Offer symptomatic treatment or gastrointestinal disturbances, while considering the importance of fluid and electrolyte balance. This drug may be removed by a session of hemodialysis. When coadministered with amoxicillin, crystalluria causing renal failure has been observed.L7886 Seizures may also occur in a case of overdose, or in a patient with renal failure.L7904

Clavulanic acid

DB00766

small molecule approved vet_approved

Deskripsi

Clavulanic acid is a beta-lactamase inhibitor that is frequently combined with Amoxicillin or Ticarcillin to fight antibiotic resistance by preventing their degradation by beta-lactamase enzymes, broadening their spectrum of susceptible bacterial infections.T665 Clavulanic acid is derived from the organism Streptomyces clavuligerus.A182228When it is combined with amoxicillin, clavulanic acid is frequently known as Augmentin, Co-Amoxiclav, or Clavulin.L7880,L7904,L7910

Struktur Molekul 2D

Berat 199.1608
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of clavulanic acid is reported to be similar to amoxicillin, and last 45-90 minutes.[A182261] A study of radiolabeled clavulanic acid administered to 4 healthy volunteers determined a half-life of 0.8 h.[A182267]
Volume Distribusi A study in 4 healthy volunteers administered a radiolabeled dose of clavulanic acid determined a volume of distribution of 12L.[A182267]Clavulanic acid is distributed to various tissues and interstitial fluid. Clinically significant concentrations have been measured in the gallbladder, abdomen, skin, fat, and muscle tissues. Bile, pus, synovial and peritoneal fluids are also found to have therapeutic concentrations of clavulanic acid.[L7886] Studies of animals have demonstrated that clavulanic crosses the placenta.[L7886]
Klirens (Clearance) The clearance of clavulanic acid in a pharmacokinetic study of 4 healthy volunteers administered a radiolabeled dose of clavulanic acid was 0.21 l/min.[A182267] Another resource indicates the average clearance of clavulanic acid is 12.20 liters/h/70 kg.[A182270] Dose adjustments may be required in patients with renal failure.[L7880]

Absorpsi

Clavulanic acid, when taken orally, is well absorbed in the gastrointestinal tract. After administration of radiolabeled clavulanic acid to four human subjects, a minimum of 73% absorption and the average absolute bioavailability was calculated at 64%.A182267 The mean Cmax in a group of 8 healthy research volunteers was 2.098 ± 0.441 micrograms/ml in a pharmacokinetic study. The same study reported a mean Tmax of 1.042 ± 0.80 hours.A182264 Tmax is reported to be 40-120 minutes according to another pharmacokinetic study.A182261

Metabolisme

Clavulanic acid is heavily metabolized to form the metabolites 2,5-dihydro-4-(2- hydroxyethyl)-5-oxo-1H-pyrrole-3-carboxylic acid and 1-amino-4-hydroxy-butan-2-one.A182267,L7886 The first metabolite was found to account for 15.6% of the dose while the second metabolite was reported to account for 8.8% of the dose in one pharmacokinetic study.A182267

Rute Eliminasi

About 40 to 65% of the clavulanic acid is excreted as unchanged drug in urine during the first 6 hours following ingestion. The metabolites of clavulanic acid are found to be excreted in the urine and feces and as carbon dioxide in expired air. Clavulanate is cleared by both renal and non-renal processes.L7886 About 17% of radiolabeled dose of clavulanic acid was found to be exhaled in expired air and 8% of a dose was found to be excreted in the feces.A182267

Interaksi Makanan

1 Data
  • 1. Take with food. Take at the beginning of a meal to reduce gastric irritation.

Interaksi Obat

56 Data
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Clavulanic acid.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Clavulanic acid.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Clavulanic acid.
Dicoumarol The risk or severity of bleeding can be increased when Clavulanic acid is combined with Dicoumarol.
Phenindione The risk or severity of bleeding can be increased when Clavulanic acid is combined with Phenindione.
Warfarin The risk or severity of bleeding can be increased when Clavulanic acid is combined with Warfarin.
Phenprocoumon The risk or severity of bleeding can be increased when Clavulanic acid is combined with Phenprocoumon.
Acenocoumarol The risk or severity of bleeding can be increased when Clavulanic acid is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Clavulanic acid is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Clavulanic acid is combined with Coumarin.
(R)-warfarin The risk or severity of bleeding can be increased when Clavulanic acid is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Clavulanic acid is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of bleeding can be increased when Clavulanic acid is combined with Fluindione.
Clorindione The risk or severity of bleeding can be increased when Clavulanic acid is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Clavulanic acid is combined with Diphenadione.
Tioclomarol The risk or severity of bleeding can be increased when Clavulanic acid is combined with Tioclomarol.
(S)-Warfarin The risk or severity of bleeding can be increased when Clavulanic acid is combined with (S)-Warfarin.
Methotrexate Methotrexate may increase the hepatotoxic activities of Clavulanic acid.
Lactulose The therapeutic efficacy of Lactulose can be decreased when used in combination with Clavulanic acid.
Vibrio cholerae CVD 103-HgR strain live antigen The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Clavulanic acid.
Estetrol The therapeutic efficacy of Estetrol can be decreased when used in combination with Clavulanic acid.
Lidocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Quinisocaine.
Cisatracurium Clavulanic acid may increase the neuromuscular blocking activities of Cisatracurium.
Ambroxol The risk or severity of methemoglobinemia can be increased when Clavulanic acid is combined with Ambroxol.
Fecal microbiota The therapeutic efficacy of Fecal microbiota can be decreased when used in combination with Clavulanic acid.

Target Protein

Bacterial beta-lactamase enzymes
Beta-lactamase blaZ

Referensi & Sumber

Synthesis reference: Dennis Edward Clark, Shaukat Hussain Malik, Paul Gerard Butterly, Clive Elton Badman, Jeffrey David Haseler, "Process for preparing potassium clavulanate in rossette form." U.S. Patent US5750685, issued April, 1978.
Artikel (PubMed)
  • PMID: 18450406
    Saudagar PS, Survase SA, Singhal RS: Clavulanic acid: a review. Biotechnol Adv. 2008 Jul-Aug;26(4):335-51. doi: 10.1016/j.biotechadv.2008.03.002. Epub 2008 Mar 26.
  • PMID: 17900874
    Geddes AM, Klugman KP, Rolinson GN: Introduction: historical perspective and development of amoxicillin/clavulanate. Int J Antimicrob Agents. 2007 Dec;30 Suppl 2:S109-12. doi: 10.1016/j.ijantimicag.2007.07.015. Epub 2007 Sep 27.
  • PMID: 7137979
    Adam D, de Visser I, Koeppe P: Pharmacokinetics of amoxicillin and clavulanic acid administered alone and in combination. Antimicrob Agents Chemother. 1982 Sep;22(3):353-7. doi: 10.1128/aac.22.3.353.
  • PMID: 6739312
    Weber DJ, Tolkoff-Rubin NE, Rubin RH: Amoxicillin and potassium clavulanate: an antibiotic combination. Mechanism of action, pharmacokinetics, antimicrobial spectrum, clinical efficacy and adverse effects. Pharmacotherapy. 1984 May-Jun;4(3):122-36.
  • PMID: 6511988
    Ferslew KE, Daigneault EA, Aten EM, Roseman JM: Pharmacokinetics and urinary excretion of clavulanic acid after oral administration of amoxicillin and potassium clavulanate. J Clin Pharmacol. 1984 Oct;24(10):452-6.
  • PMID: 3765664
    Bolton GC, Allen GD, Davies BE, Filer CW, Jeffery DJ: The disposition of clavulanic acid in man. Xenobiotica. 1986 Sep;16(9):853-63. doi: 10.3109/00498258609038967.
  • PMID: 26349821
    De Cock PA, Standing JF, Barker CI, de Jaeger A, Dhont E, Carlier M, Verstraete AG, Delanghe JR, Robays H, De Paepe P: Augmented renal clearance implies a need for increased amoxicillin-clavulanic acid dosing in critically ill children. Antimicrob Agents Chemother. 2015 Nov;59(11):7027-35. doi: 10.1128/AAC.01368-15. Epub 2015 Sep 8.
Textbook
  • Justin Evans; Micah Wittler (2019). Amoxicillin Clavulanate. Stat Pearls.

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