Peringatan Keamanan

The oral LD50 in mice and rats is 2764 mg/kg and >5300 mg/kg, respectively.L11917

Prescribing information for trimethoprim states that signs of overdose may be evident following ingestion of doses >1 gram, and may include nausea, vomiting, dizziness, headaches, mental depression, confusion, and bone marrow depression.L11893 Treatment should consist of general supportive measures and gastric lavage, if applicable. Urinary acidification may increase renal elimination of trimethoprim. Hemodialysis is only moderately effective in eliminating trimethoprim and peritoneal dialysis is of no benefit.L11893

Trimethoprim

DB00440

small molecule approved vet_approved

Deskripsi

Trimethoprim is an antifolate antibacterial agent that inhibits bacterial dihydrofolate reductase (DHFR), a critical enzyme that catalyzes the formation of tetrahydrofolic acid (THF) - in doing so, it prevents the synthesis of bacterial DNA and ultimately continued bacterial survival.L11893 Trimethoprim is often used in combination with sulfamethoxazole due to their complementary and synergistic mechanisms but may be used as a monotherapy in the treatment and/or prophylaxis of urinary tract infections.L11893,L11830 It is structurally and chemically related to pyrimethamine, another antifolate antimicrobial used in the treatment of plasmodial infections.T707

Struktur Molekul 2D

Berat 290.3177
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Trimethoprim half-life ranges from 8-10 hours, but may be prolonged in patients with renal dysfunction.[L11890]
Volume Distribusi Trimethoprim is extensively distributed into various tissues following oral administration. It distributes well into sputum, middle ear fluid, and bronchial secretions.[L11830] Trimethoprim distributes efficiently into vaginal fluids, with observed concentrations approximately 1.6-fold higher than those seen in the serum.[L11893] It may pass the placental barrier and into breast milk.[L11830] Trimethoprim is also sufficiently excreted in the feces to markedly reduce and/or eliminate trimethoprim-susceptible fecal flora.[L11893]
Klirens (Clearance) Following oral administration, the renal clearance of trimethoprim has been variably reported between 51.7 - 91.3 mL/min.[A191368]

Absorpsi

Steady-state concentrations are achieved after approximately 3 days of repeat administration.A191368 Average peak serum concentrations of approximately 1 µg/mL (Cmax) are achieved within 1 to 4 hours (Tmax) following the administration of a single 100mg dose.L11893 Trimethoprim appears to follow first-order pharmacokinetics,A191368 as a single 200mg dose results in serum concentrations approximately double that of a 100mg dose.L11893 The steady-state AUC of orally administered trimethoprim is approximately 30 mg/L·h.A191368

Metabolisme

Trimethoprim undergoes oxidative metabolism to a number of metabolites, the most abundant of which are the demethylated 3'- and 4'- metabolites, accounting for approximately 65% and 25% of the total metabolite formation, respectively.A191149 Minor products include N-oxide metabolites (<5%) and benzylic metabolites in even smaller quantities.A191149 The parent drug is considered to be the therapeutically active form.L11893 The majority of trimethoprim biotransformation appears to involve CYP2C9 and CYP3A4 enzymes, with CYP1A2 contributing to a lesser extent.A191149

Rute Eliminasi

Approximately 10-20% of an ingested trimethoprim dose is metabolized, primarily in the liver, while a large portion of the remainder is excreted unchanged in the urine.L11893 Following oral administration, 50% to 60% of trimethoprim is excreted in the urine within 24 hours, approximately 80% of which is unchanged parent drug.L11890

Interaksi Obat

1243 Data
Valsartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Valsartan.
Olmesartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Olmesartan.
Losartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Losartan.
Candesartan cilexetil The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Candesartan cilexetil.
Eprosartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Eprosartan.
Telmisartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Telmisartan.
Irbesartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Irbesartan.
Forasartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Forasartan.
Saprisartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Saprisartan.
Tasosartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Tasosartan.
Saralasin The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Saralasin.
Azilsartan medoxomil The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Azilsartan medoxomil.
Fimasartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Fimasartan.
Candesartan The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Candesartan.
Ramipril Trimethoprim may increase the hyperkalemic activities of Ramipril.
Fosinopril Trimethoprim may increase the hyperkalemic activities of Fosinopril.
Trandolapril Trimethoprim may increase the hyperkalemic activities of Trandolapril.
Benazepril Trimethoprim may increase the hyperkalemic activities of Benazepril.
Enalapril Trimethoprim may increase the hyperkalemic activities of Enalapril.
Moexipril Trimethoprim may increase the hyperkalemic activities of Moexipril.
Lisinopril Trimethoprim may increase the hyperkalemic activities of Lisinopril.
Perindopril Trimethoprim may increase the hyperkalemic activities of Perindopril.
Quinapril Trimethoprim may increase the hyperkalemic activities of Quinapril.
Omapatrilat Trimethoprim may increase the hyperkalemic activities of Omapatrilat.
Rescinnamine Trimethoprim may increase the hyperkalemic activities of Rescinnamine.
Captopril Trimethoprim may increase the hyperkalemic activities of Captopril.
Cilazapril Trimethoprim may increase the hyperkalemic activities of Cilazapril.
Spirapril Trimethoprim may increase the hyperkalemic activities of Spirapril.
Temocapril Trimethoprim may increase the hyperkalemic activities of Temocapril.
Enalaprilat Trimethoprim may increase the hyperkalemic activities of Enalaprilat.
Imidapril Trimethoprim may increase the hyperkalemic activities of Imidapril.
Zofenopril Trimethoprim may increase the hyperkalemic activities of Zofenopril.
Delapril Trimethoprim may increase the hyperkalemic activities of Delapril.
Benazeprilat Trimethoprim may increase the hyperkalemic activities of Benazeprilat.
Fosinoprilat Trimethoprim may increase the hyperkalemic activities of Fosinoprilat.
Ramiprilat Trimethoprim may increase the hyperkalemic activities of Ramiprilat.
Trandolaprilat Trimethoprim may increase the hyperkalemic activities of Trandolaprilat.
Moexiprilat Trimethoprim may increase the hyperkalemic activities of Moexiprilat.
Perindoprilat Trimethoprim may increase the hyperkalemic activities of Perindoprilat.
Quinaprilat Trimethoprim may increase the hyperkalemic activities of Quinaprilat.
Cilazaprilat Trimethoprim may increase the hyperkalemic activities of Cilazaprilat.
Dofetilide Trimethoprim may decrease the excretion rate of Dofetilide which could result in a higher serum level.
Dapsone The serum concentration of Dapsone can be increased when it is combined with Trimethoprim.
Metformin The serum concentration of Metformin can be increased when it is combined with Trimethoprim.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Trimethoprim.
Metildigoxin The serum concentration of Metildigoxin can be increased when it is combined with Trimethoprim.
Acetyldigoxin The serum concentration of Acetyldigoxin can be increased when it is combined with Trimethoprim.
Azathioprine Trimethoprim may increase the myelosuppressive activities of Azathioprine.
Phenytoin The serum concentration of Trimethoprim can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Trimethoprim can be decreased when it is combined with Fosphenytoin.
Mercaptopurine Trimethoprim may increase the myelosuppressive activities of Mercaptopurine.
Methotrexate The risk or severity of adverse effects can be increased when Trimethoprim is combined with Methotrexate.
Pralatrexate Trimethoprim may decrease the excretion rate of Pralatrexate which could result in a higher serum level.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Trimethoprim.
Varenicline The serum concentration of Varenicline can be increased when it is combined with Trimethoprim.
Folic acid Folic acid may decrease the excretion rate of Trimethoprim which could result in a higher serum level.
Fluvoxamine The metabolism of Trimethoprim can be decreased when combined with Fluvoxamine.
Nabilone The metabolism of Nabilone can be decreased when combined with Trimethoprim.
Felbamate The metabolism of Trimethoprim can be decreased when combined with Felbamate.
Sulfinpyrazone The metabolism of Trimethoprim can be decreased when combined with Sulfinpyrazone.
Iproniazid The metabolism of Trimethoprim can be decreased when combined with Iproniazid.
Medical Cannabis The metabolism of Trimethoprim can be decreased when combined with Medical Cannabis.
Troglitazone The metabolism of Trimethoprim can be decreased when combined with Troglitazone.
Mifepristone The metabolism of Trimethoprim can be decreased when combined with Mifepristone.
Fluoxetine The metabolism of Trimethoprim can be decreased when combined with Fluoxetine.
Imatinib The metabolism of Trimethoprim can be decreased when combined with Imatinib.
Valproic acid The metabolism of Trimethoprim can be decreased when combined with Valproic acid.
Fluconazole The metabolism of Trimethoprim can be decreased when combined with Fluconazole.
Floxuridine The metabolism of Trimethoprim can be decreased when combined with Floxuridine.
Nicardipine The metabolism of Trimethoprim can be decreased when combined with Nicardipine.
Miconazole The metabolism of Trimethoprim can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Trimethoprim can be decreased when combined with Gemfibrozil.
Sulfaphenazole The metabolism of Trimethoprim can be decreased when combined with Sulfaphenazole.
Ketorolac The metabolism of Ketorolac can be decreased when combined with Trimethoprim.
Dexibuprofen The metabolism of Dexibuprofen can be decreased when combined with Trimethoprim.
Amitriptyline The metabolism of Amitriptyline can be decreased when combined with Trimethoprim.
Diltiazem The metabolism of Trimethoprim can be decreased when combined with Diltiazem.
Zidovudine The metabolism of Zidovudine can be decreased when combined with Trimethoprim.
Estradiol The metabolism of Estradiol can be decreased when combined with Trimethoprim.
Ethinylestradiol The metabolism of Ethinylestradiol can be decreased when combined with Trimethoprim.
Ibuprofen The metabolism of Ibuprofen can be decreased when combined with Trimethoprim.
Apixaban The metabolism of Apixaban can be decreased when combined with Trimethoprim.
Pitavastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Trimethoprim is combined with Pitavastatin.
Estradiol acetate The metabolism of Estradiol acetate can be decreased when combined with Trimethoprim.
Estradiol benzoate The metabolism of Estradiol benzoate can be decreased when combined with Trimethoprim.
Estradiol cypionate The metabolism of Estradiol cypionate can be decreased when combined with Trimethoprim.
Estradiol dienanthate The metabolism of Estradiol dienanthate can be decreased when combined with Trimethoprim.
Estradiol valerate The metabolism of Estradiol valerate can be decreased when combined with Trimethoprim.
Verapamil The metabolism of Trimethoprim can be decreased when combined with Verapamil.
Trimethadione The metabolism of Trimethadione can be decreased when combined with Trimethoprim.
Rosiglitazone The metabolism of Rosiglitazone can be decreased when combined with Trimethoprim.
Celecoxib The metabolism of Celecoxib can be decreased when combined with Trimethoprim.
Mephenytoin The metabolism of Mephenytoin can be decreased when combined with Trimethoprim.
Piroxicam The metabolism of Piroxicam can be decreased when combined with Trimethoprim.
Diclofenac The metabolism of Diclofenac can be decreased when combined with Trimethoprim.
Paramethadione The metabolism of Paramethadione can be decreased when combined with Trimethoprim.
Naproxen The metabolism of Naproxen can be decreased when combined with Trimethoprim.
Propofol The metabolism of Propofol can be decreased when combined with Trimethoprim.
Terbinafine The metabolism of Terbinafine can be decreased when combined with Trimethoprim.
Buprenorphine The metabolism of Buprenorphine can be decreased when combined with Trimethoprim.

Target Protein

Dihydrofolate reductase DHFR
Dihydrofolate reductase folA

Referensi & Sumber

Synthesis reference: Yasushi Takagishi, Kiichiro Ohsuga, Sadao Ohama, "Suppository containing sulfamethoxazole/trimethoprim complex and process for preparing the same." U.S. Patent US4461765, issued December, 1975.
Artikel (PubMed)
  • PMID: 8195839
    Brumfitt W, Hamilton-Miller JM: Reassessment of the rationale for the combinations of sulphonamides with diaminopyrimidines. J Chemother. 1993 Dec;5(6):465-9.
  • PMID: 8071675
    Brumfitt W, Hamilton-Miller JM: Limitations of and indications for the use of co-trimoxazole. J Chemother. 1994 Feb;6(1):3-11.
  • PMID: 16150859
    Bean DC, Livermore DM, Papa I, Hall LM: Resistance among Escherichia coli to sulphonamides and other antimicrobials now little used in man. J Antimicrob Chemother. 2005 Nov;56(5):962-4. Epub 2005 Sep 8.
  • PMID: 12239226
    Felmingham D, Reinert RR, Hirakata Y, Rodloff A: Increasing prevalence of antimicrobial resistance among isolates of Streptococcus pneumoniae from the PROTEKT surveillance study, and compatative in vitro activity of the ketolide, telithromycin. J Antimicrob Chemother. 2002 Sep;50 Suppl S1:25-37.
  • PMID: 12103291
    Johnson JR, Manges AR, O'Bryan TT, Riley LW: A disseminated multidrug-resistant clonal group of uropathogenic Escherichia coli in pyelonephritis. Lancet. 2002 Jun 29;359(9325):2249-51.
  • PMID: 26138612
    Goldman JL, Leeder JS, Van Haandel L, Pearce RE: In Vitro Hepatic Oxidative Biotransformation of Trimethoprim. Drug Metab Dispos. 2015 Sep;43(9):1372-80. doi: 10.1124/dmd.115.065193. Epub 2015 Jul 2.
  • PMID: 30528339
    Kito T, Ito S, Mizuno T, Maeda K, Kusuhara H: Investigation of non-linear Mate1-mediated efflux of trimethoprim in the mouse kidney as the mechanism underlying drug-drug interactions between trimethoprim and organic cations in the kidney. Drug Metab Pharmacokinet. 2019 Feb;34(1):87-94. doi: 10.1016/j.dmpk.2018.08.005. Epub 2018 Sep 20.
  • PMID: 26702643
    Misaka S, Knop J, Singer K, Hoier E, Keiser M, Muller F, Glaeser H, Konig J, Fromm MF: The Nonmetabolized beta-Blocker Nadolol Is a Substrate of OCT1, OCT2, MATE1, MATE2-K, and P-Glycoprotein, but Not of OATP1B1 and OATP1B3. Mol Pharm. 2016 Feb 1;13(2):512-9. doi: 10.1021/acs.molpharmaceut.5b00733. Epub 2016 Jan 19.
Menampilkan 8 dari 10 artikel.
Textbook
  • ISBN: 9780702080609
    Antibacterial Agents That Interfere With Folate Synthesis. (2020). In Rang and Dale's Pharmacology (9th ed.). Edinburgh: Elsevier.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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