Peringatan Keamanan

LD50 information

The oral LD50 of metronidazole in rats is 5000 mg/kg L7432

Overdose information

Adverse effects that may be exaggerated with an overdose include peripheral neuropathy, central nervous system toxicity, seizures, disulfiram-like effect (if combined with alcohol) dark urine, a metallic taste in the mouth, nausea, epigastric discomfort, and vertigo, in addition to neutropenia.A181054,L7432 There is no specific antidote for metronidazole overdose. Symptomatic and supportive treatment should be employed in addition to the administration of activated charcoal to remove the unabsorbed drug from the gastrointestinal tract. In addition to the above measures, contact the local poison control center for updated information on the management of a metronidazole overdose.L7432

Metronidazole

DB00916

small molecule approved

Deskripsi

Metronidazole is a commonly used antibiotic, belonging to the nitroimidazole class of antibiotics.L3754 It is frequently used to treat gastrointestinal infections as well as trichomoniasis and giardiasis, and amebiasis which are parasitic infections.A181036,A181039 Metronidazole has been used as an antibiotic for several decadesL7429, with added antiparasitic properties that set it apart from many other antibacterial drugs, allowing it to treat a wide variety of infections. It is available in capsule form, tablet form, and topical form, and suppository preparations for the treatment of various infections.

Struktur Molekul 2D

Berat 171.154
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of metronidazole is 7.3 ± 1.0 after a single 500mg IV dose in healthy subjects.[L7432] Another resource indicates that the elimination half-life for metronidazole ranges from 6 to 10 hours.[A181045]
Volume Distribusi Metronidazole is widely distributed throughout the body[A181039] and various body fluids. They include the bile, saliva, breastmilk, cerebrospinal fluid, and the placenta.[L7432] Steady-state volume distribution of metronidazole in adults ranges from 0.51 to 1.1 L/kg. It attains 60 to 100% of plasma concentrations in various tissues, such as the central nervous system, however, is not measured in high concentrations in the placental tissue.[A181045]
Klirens (Clearance) Dose adjustments may be required in patients with hepatic impairment, as clearance is impaired in these patients.[L7432] The clearance of metronidazole in the kidneys is estimated at 10 mL/min/1.73 m2.[L3754] The total clearance from serum is about 2.1 to 6.4 L/h/kg.[A181045]

Absorpsi

After the intravenous infusion of a 1.5g dose, peak concentration was reached within 1 hour and was peak level of 30-40 mg/L.L7432 When a multiple-dose regimen of 500mg three times a day administered intravenously, steady-state concentrations were achieved within about 3 days and peak concentration was measured at 26 mg/L.L7432 When administered orally in the tablet form, metronidazole is absorbed entirely absorbed, showing a bioavailability of greater than 90%.A181045 One resource indicates that Cmax after a single oral dose of 500mg metronidazole ranges from 8 to 13 mg/L, with a Tmax of 25 minutes to 4 hours. The AUC following a single 500mg oral dose of metronidazole was 122 ± 10.3 mg/L
• h.A181045 A note on the absorption of topical preparations Insignificant percutaneous absorption of metronidazole occurs after the application of 1% metronidazole cream topically. Healthy volunteers applied one 100 mg dose of 14C-labelled metronidazole 2% cream to unbroken skin. After 12 hours, metronidazole was not detected in the plasma. Approximately 0.1% to 1% of the administered metronidazole was measured in the urine and feces.L7432

Metabolisme

Metronidazole undergoes hepatic metabolism via hydroxylation, oxidation, and glucuronidation. The metabolism of metronidazole yields 5 metabolites. The hydroxy metabolite, 1-(2-hydroxy-ethyl)-2-hydroxy methyl-5-nitroimidazole, is considered the major active metabolite.A181045,A181144 Unchanged metronidazole is found in the plasma along with small amounts of its 2- hydroxymethyl metabolite. Several metabolites of metronidazole are found in the urine. They are primarily a product of side-chain oxidation in addition to glucuronide conjugation. Only 20% of the dose found in the urine is accounted for by unchanged metronidazole.L7432 The two main oxidative metabolites of metronidazole are hydroxy and acetic acid metabolites.A181042,A181051

Rute Eliminasi

Metronidazole and metabolites are 60 to 80% eliminated in the urine, and 6-15% excreted in the feces.A181045,L3754

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Unpleasant symptoms such as nausea, vomiting, and abdominal distress may occur with alcohol.
  • 2. Take with or without food. The extended release formulation should, however, be taken without food.

Interaksi Obat

978 Data
Eliglustat The metabolism of Eliglustat can be decreased when combined with Metronidazole.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Metronidazole.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Metronidazole.
Colchicine The metabolism of Colchicine can be decreased when combined with Metronidazole.
Fentanyl The metabolism of Metronidazole can be decreased when combined with Fentanyl.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Metronidazole.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Metronidazole.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Metronidazole.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Metronidazole.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Metronidazole.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Metronidazole.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Metronidazole.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Metronidazole.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Metronidazole.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Metronidazole.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Metronidazole.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Metronidazole.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Metronidazole.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Metronidazole.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Metronidazole.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Metronidazole.
Desogestrel The metabolism of Metronidazole can be increased when combined with Desogestrel.
Zidovudine The metabolism of Metronidazole can be increased when combined with Zidovudine.
Lamotrigine The metabolism of Metronidazole can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Metronidazole can be increased when combined with Efavirenz.
Primidone The metabolism of Metronidazole can be increased when combined with Primidone.
Ethinylestradiol The metabolism of Metronidazole can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Metronidazole can be increased when combined with Testosterone propionate.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Metronidazole.
Busulfan The serum concentration of Busulfan can be increased when it is combined with Metronidazole.
Capecitabine The serum concentration of the active metabolites of Capecitabine can be increased when Capecitabine is used in combination with Metronidazole.
Carbocisteine The risk or severity of adverse effects can be increased when Metronidazole is combined with Carbocisteine.
Mebendazole The risk or severity of adverse effects can be increased when Mebendazole is combined with Metronidazole.
Phenytoin The serum concentration of Metronidazole can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Metronidazole can be decreased when it is combined with Fosphenytoin.
Ritonavir The risk or severity of adverse effects can be increased when Ritonavir is combined with Metronidazole.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Metronidazole.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be decreased when it is combined with Metronidazole.
Mycophenolic acid The serum concentration of Mycophenolic acid can be decreased when it is combined with Metronidazole.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Metronidazole.
Fluorouracil The serum concentration of Fluorouracil can be increased when it is combined with Metronidazole.
Flucytosine The serum concentration of Flucytosine can be increased when it is combined with Metronidazole.
5-fluorouridine The serum concentration of 5-fluorouridine can be increased when it is combined with Metronidazole.
Uracil The serum concentration of Uracil can be increased when it is combined with Metronidazole.
Tegafur The serum concentration of Tegafur can be increased when it is combined with Metronidazole.
Doxifluridine The serum concentration of Doxifluridine can be increased when it is combined with Metronidazole.
Disulfiram The risk or severity of psychotic reaction can be increased when Disulfiram is combined with Metronidazole.
Ethanol The risk or severity of adverse effects can be increased when Metronidazole is combined with Ethanol.
Tipranavir The risk or severity of adverse effects can be increased when Metronidazole is combined with Tipranavir.
Leuprolide The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Goserelin.
Azithromycin The metabolism of Azithromycin can be decreased when combined with Metronidazole.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Moxifloxacin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Sulfisoxazole.
Methadone The metabolism of Methadone can be decreased when combined with Metronidazole.
Sulpiride The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Sulpiride.
Nimodipine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Nimodipine.
Promazine The metabolism of Promazine can be decreased when combined with Metronidazole.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Prochlorperazine.
Droperidol The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Droperidol.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Metronidazole.
Perflutren The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Perflutren.
Cinnarizine The metabolism of Metronidazole can be decreased when combined with Cinnarizine.
Atropine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Atropine.
Adenosine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Adenosine.
Pentamidine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Pentamidine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Cinoxacin.
Granisetron The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Granisetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Desloratadine.
Telithromycin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Telithromycin.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Dimenhydrinate.
Primaquine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Primaquine.
Papaverine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Papaverine.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Chlorpheniramine.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Ofloxacin.
Propafenone The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Propafenone.
Flecainide The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Flecainide.
Mibefradil The metabolism of Metronidazole can be decreased when combined with Mibefradil.
Probucol The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Terlipressin.
Prenylamine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Prenylamine.
Fluspirilene The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Fluspirilene.
Lofexidine The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Lofexidine.
Azimilide The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Azimilide.
Pracinostat The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Telavancin.

Target Protein

Oxygen-insensitive NADPH nitroreductase rdxA
Anaerobic bacterial DNA
Protozoal DNA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 16398774
    Shennan A, Crawshaw S, Briley A, Hawken J, Seed P, Jones G, Poston L: A randomised controlled trial of metronidazole for the prevention of preterm birth in women positive for cervicovaginal fetal fibronectin: the PREMET Study. BJOG. 2006 Jan;113(1):65-74.
  • PMID: 10676835
    Williams CS, Woodcock KR: Do ethanol and metronidazole interact to produce a disulfiram-like reaction? Ann Pharmacother. 2000 Feb;34(2):255-7.
  • PMID: 12022894
    Visapaa JP, Tillonen JS, Kaihovaara PS, Salaspuro MP: Lack of disulfiram-like reaction with metronidazole and ethanol. Ann Pharmacother. 2002 Jun;36(6):971-4.
  • PMID: 29077920
    Dingsdag SA, Hunter N: Metronidazole: an update on metabolism, structure-cytotoxicity and resistance mechanisms. J Antimicrob Chemother. 2018 Feb 1;73(2):265-279. doi: 10.1093/jac/dkx351.
  • PMID: 30657582
    Hernandez Ceruelos A, Romero-Quezada LC, Ruvalcaba Ledezma JC, Lopez Contreras L: Therapeutic uses of metronidazole and its side effects: an update. Eur Rev Med Pharmacol Sci. 2019 Jan;23(1):397-401. doi: 10.26355/eurrev20190116788.
  • PMID: 15561831
    Sprandel KA, Schriever CA, Pendland SL, Quinn JP, Gotfried MH, Hackett S, Graham MB, Danziger LH, Rodvold KA: Pharmacokinetics and pharmacodynamics of intravenous levofloxacin at 750 milligrams and various doses of metronidazole in healthy adult subjects. Antimicrob Agents Chemother. 2004 Dec;48(12):4597-605. doi: 10.1128/AAC.48.12.4597-4605.2004.
  • PMID: 10384859
    Lamp KC, Freeman CD, Klutman NE, Lacy MK: Pharmacokinetics and pharmacodynamics of the nitroimidazole antimicrobials. Clin Pharmacokinet. 1999 May;36(5):353-73. doi: 10.2165/00003088-199936050-00004.
  • PMID: 26065445
    Morales-Leon F, von Plessing-Rossel C, Villa-Zapata L, Fernandez-Rocca P, Sanhueza-Sanhueza C, Bello-Toledo H, Mella-Montecinos S: Pharmacokinetics/pharmacodinamic (PK/PD) evaluation of a short course of oral administration of metronidazole for the management of infections caused by Bacteroides fragilis. Rev Chilena Infectol. 2015 Apr;32(2):135-41. doi: 10.4067/S0716-10182015000300001.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 526 • International brands: 28
Produk
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    Capsule • 500 mg • Oral • Canada • Generic • Approved
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  • Auro-metronidazole
    Capsule • 500 mg • Oral • Canada • Generic • Approved
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Sekuens Gen/Protein (FASTA)

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