Peringatan Keamanan

Acute oral LD50 of triamterene in rats is 400 mg/kg and 285-380 mg/kg in mice.L6166,MSDS There has been a case of reversible acute renal failure following ingestion of 50 combination pills containing 50 mg triamterene and 25 mg hydrochlorothiazide. Symptoms of overdose, such as nausea, vomiting, gastrointestinal disturbances, weakness, and hypotension, are related to electrolyte imbalances, such as hyperkalemia. As there is no specific antidote, emesis and gastric lavage should be use to induce immediate evacuation of the stomach and careful evaluation of the electrolyte pattern and fluid balance should be made. Dialysis may be somewhat effective in case of an overdosage.L6166

In a carciongenicity study in male and female mice administered with triamterene at the highst dosage level, there was an increased incidence of hepatocellular neoplasia, primarily adenomas. However, this was not a dose-dependent phenomenon and there was no statistically significant difference from control incidence at any dose level. In bacterial assays, there was no demonstrated mutagenic potential of triamterene. In in vitro assay using Chinese hamster ovary (CHO) cells with or without metabolic activation, there were no chromosomal aberrations. Studies evaluating the effects of triamterene on reproductive system or fertility have not been conducted. It is advised that the use of triamterene is avoided during pregnancy. As triamterene has been detected in human breast milk, triamterene should be used when nursing is ceased.L6166

Triamterene

DB00384

small molecule approved

Deskripsi

Triamterene (2,4,7-triamino-6-phenylpteridine) is a potassium-sparing diuretic that is used in the management of hypertension. It works by promoting the excretion of sodium ions and water while decreasing the potassium excretion in the distal part of the nephron in the kidneys by working on the lumenal side.A177985 Since it acts on the distal nephron where only a small fraction of sodium ion reabsorption occurs, triamterene is reported to have limited diuretic efficacy.T28 Due to its effects on increased serum potassium levels, triamterene is associated with a risk of producing hyperkalemia. Triamterene is a weak antagonist of folic acid, and a photosensitizing drug.L6163

Triamterene was approved by the Food and Drug Administration in the U.S. in 1964.L6163 Currently, triamterene is used in the treatment of edema associated with various conditions as monotherapy and is approved for use with other diuretics to enhance diuretic and potassium-sparing effects.L6166 It is also found in a combination product with hydrochlorothiazide that is used for the management of hypertension or treatment of edema in patients who develop hypokalemia on hydrochlorothiazide alone.

Struktur Molekul 2D

Berat 253.2626
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 the drug in plasma ranges from 1.5 to 2 hours.[L6193] In a pharmacokinetic study involving healthy volunteers, the terminal half-lives for triamterene and 4?-hydroxytriamterene sulfate were 255 ± 42 and 188 ± 70 minutes, respectively, after intravenous infusion of the parent drug.[A577,L6163]
Volume Distribusi In a pharmacolinetic study involving healthy volunteers receiving triamterene intravenously, the volumes of distribution of the central compartment of triamterene and its hydroxylated ester metabolite were 1.49 L/kg and 0.11 L/kg, respectively.[A577] Triamterene was found to cross the placental barrier and appear in the cord blood of animals.[L6166]
Klirens (Clearance) The total plasma clearance was 4.5 l/min and renal plasma clearance was 0.22 l/kg following intravenous administration of triamterene in healthy volunteers.[A577]

Absorpsi

Triamterene is shown to be rapidly absorbed in the gastrointestinal tract L6166,T28 Its onset of action achiveved within 2 to 4 hours after oral ingestion L6166 and its duration of action is 12-16 hours.T28 It is reported that the diuretic effect of triamterene may not be observed for several days after administration.L6166 In a pharmacokinetic study, the oral bioavailability of triamterene was determined to be 52%.A178012 Following administration of a single oral dose to fasted healthy male volunteers, the mean AUC of triamterene was about 148.7 ng*hr/mL L6169 and the mean peak plasma concentrations (Cmax) were 46.4 ng/mL reached at 1.1 hour after administration.L6169 In a limited study, administration of triamterene in combination with hydrochlorothiazide resulted in an increased bioavailability of triamterene by about 67% and a delay of up to 2 hours in the absorption of the drug.L6169 It is advised that triamterene is administered after meals; in a limited study, combination use of triamterene and hydrochlorothiazide with the consumption of a high-fat meal resulted in an increase in the mean bioavailability and peak serum concentrations of triamterene and its active sulfate metabolite, as well as a delay of up to 2 hours in the absorption of the active constituents.L6169

Metabolisme

Triamterene undergoes phase I metabolism involving hydroxylation, via CYP1A2 activity, to form 4'-hydroxytriamterene. 4'-Hydroxytriamterene is further transformed in phase II metabolism mediated by cytosolic sulfotransferases to form the major metabolite, 4?-hydroxytriamterene sulfate, which retains a diuretic activity. A39120,L6163 Both the plasma and urine levels of this metabolite greatly exceed triamterene levels L6166 while the renal clearance of the sulfate conjugate was les than that of triamterene; this low renal clearance of the sulfate conjugate as compared with triamterene may be explained by the low unbound fraction of the metabolite in plasma.A178057

Rute Eliminasi

Triamterene and its metabolites are excreted by the kidney by filtration and tubular secretion.L6193 Upon oral ingestion, somewhat less than 50% of the oral dose reaches the urine.L6166 About 20% of an oral dose appears unchanged in the urine, 70% as the sulphate ester of hydroxytriamterene and 10% as free hydroxytriamterene and triamterene glucuronide.L6193

Interaksi Makanan

1 Data
  • 1. Avoid potassium-containing products. The risk of hyperkalemia can be increased with the intake of potassium supplementation or potassium-rich foods.

Interaksi Obat

1359 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Triamterene is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Triamterene is combined with Levodopa.
Risperidone Triamterene may increase the hypotensive activities of Risperidone.
Deferasirox The serum concentration of Triamterene can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Triamterene can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Triamterene can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Triamterene can be decreased when it is combined with Teriflunomide.
Dofetilide The serum concentration of Dofetilide can be increased when it is combined with Triamterene.
Indomethacin Indomethacin may increase the nephrotoxic activities of Triamterene.
Foscarnet The risk or severity of nephrotoxicity can be increased when Triamterene is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Triamterene.
Tenofovir disoproxil Triamterene may increase the nephrotoxic activities of Tenofovir disoproxil.
Tenofovir alafenamide Triamterene may increase the nephrotoxic activities of Tenofovir alafenamide.
Tenofovir Triamterene may increase the nephrotoxic activities of Tenofovir.
Abiraterone The serum concentration of Triamterene can be increased when it is combined with Abiraterone.
Aripiprazole Aripiprazole may increase the hypotensive activities of Triamterene.
Aripiprazole lauroxil Aripiprazole lauroxil may increase the hypotensive activities of Triamterene.
Nicorandil Nicorandil may increase the hypotensive activities of Triamterene.
Cyproterone acetate The metabolism of Triamterene can be increased when combined with Cyproterone acetate.
Acetyldigitoxin Triamterene may decrease the excretion rate of Acetyldigitoxin which could result in a higher serum level.
Deslanoside Triamterene may decrease the excretion rate of Deslanoside which could result in a higher serum level.
Ouabain Triamterene may decrease the excretion rate of Ouabain which could result in a higher serum level.
Digitoxin Triamterene may decrease the excretion rate of Digitoxin which could result in a higher serum level.
Oleandrin Triamterene may decrease the excretion rate of Oleandrin which could result in a higher serum level.
Cymarin Triamterene may decrease the excretion rate of Cymarin which could result in a higher serum level.
Proscillaridin Triamterene may decrease the excretion rate of Proscillaridin which could result in a higher serum level.
Metildigoxin Triamterene may decrease the excretion rate of Metildigoxin which could result in a higher serum level.
Lanatoside C Triamterene may decrease the excretion rate of Lanatoside C which could result in a higher serum level.
Gitoformate Triamterene may decrease the excretion rate of Gitoformate which could result in a higher serum level.
Acetyldigoxin Triamterene may decrease the excretion rate of Acetyldigoxin which could result in a higher serum level.
Peruvoside Triamterene may decrease the excretion rate of Peruvoside which could result in a higher serum level.
Digoxin Triamterene may decrease the excretion rate of Digoxin which could result in a higher serum level.
Cyclosporine The risk or severity of hyperkalemia can be increased when Triamterene is combined with Cyclosporine.
Icosapent The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Icosapent is combined with Triamterene.
Mesalazine The risk or severity of nephrotoxicity can be increased when Mesalazine is combined with Triamterene.
Nabumetone The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Nabumetone is combined with Triamterene.
Ketorolac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Ketorolac is combined with Triamterene.
Tenoxicam The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Tenoxicam is combined with Triamterene.
Celecoxib The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Celecoxib is combined with Triamterene.
Tolmetin The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Tolmetin is combined with Triamterene.
Piroxicam The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Piroxicam is combined with Triamterene.
Fenoprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Fenoprofen is combined with Triamterene.
Valdecoxib The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Valdecoxib is combined with Triamterene.
Diclofenac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Diclofenac is combined with Triamterene.
Sulindac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Sulindac is combined with Triamterene.
Flurbiprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Flurbiprofen is combined with Triamterene.
Etodolac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Etodolac is combined with Triamterene.
Mefenamic acid The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Mefenamic acid is combined with Triamterene.
Naproxen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Naproxen is combined with Triamterene.
Sulfasalazine The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Sulfasalazine is combined with Triamterene.
Phenylbutazone The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Phenylbutazone is combined with Triamterene.
Carprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Carprofen is combined with Triamterene.
Diflunisal The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Diflunisal is combined with Triamterene.
Salicylic acid The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Salicylic acid is combined with Triamterene.
Meclofenamic acid The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Meclofenamic acid is combined with Triamterene.
Oxaprozin The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Oxaprozin is combined with Triamterene.
Ketoprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Ketoprofen is combined with Triamterene.
Balsalazide The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Balsalazide is combined with Triamterene.
Ibuprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Ibuprofen is combined with Triamterene.
Olsalazine The risk or severity of nephrotoxicity can be increased when Triamterene is combined with Olsalazine.
Lumiracoxib The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Lumiracoxib is combined with Triamterene.
Magnesium salicylate The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Magnesium salicylate is combined with Triamterene.
Salsalate The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Salsalate is combined with Triamterene.
Choline magnesium trisalicylate The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Choline magnesium trisalicylate is combined with Triamterene.
Antrafenine The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Antrafenine is combined with Triamterene.
Aminophenazone The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aminophenazone is combined with Triamterene.
Antipyrine The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Antipyrine is combined with Triamterene.
Tiaprofenic acid The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Tiaprofenic acid is combined with Triamterene.
Etoricoxib The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Etoricoxib is combined with Triamterene.
Taxifolin The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Taxifolin is combined with Triamterene.
Oxyphenbutazone The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Oxyphenbutazone is combined with Triamterene.
Licofelone The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Licofelone is combined with Triamterene.
Nimesulide The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Nimesulide is combined with Triamterene.
Benoxaprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Benoxaprofen is combined with Triamterene.
Metamizole The risk or severity of nephrotoxicity can be increased when Triamterene is combined with Metamizole.
Zomepirac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Zomepirac is combined with Triamterene.
Cimicoxib The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Cimicoxib is combined with Triamterene.
Lornoxicam The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Lornoxicam is combined with Triamterene.
Aceclofenac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aceclofenac is combined with Triamterene.
Zaltoprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Zaltoprofen is combined with Triamterene.
Azapropazone The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Azapropazone is combined with Triamterene.
Parecoxib The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Parecoxib is combined with Triamterene.
Salicylamide The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Salicylamide is combined with Triamterene.
Kebuzone The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Kebuzone is combined with Triamterene.
Isoxicam The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Isoxicam is combined with Triamterene.
Indoprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Indoprofen is combined with Triamterene.
Ibuproxam The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Ibuproxam is combined with Triamterene.
Floctafenine The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Floctafenine is combined with Triamterene.
Fenbufen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Fenbufen is combined with Triamterene.
Etofenamate The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Etofenamate is combined with Triamterene.
Epirizole The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Epirizole is combined with Triamterene.
Benzydamine The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Benzydamine is combined with Triamterene.
Dexibuprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Dexibuprofen is combined with Triamterene.
Dexketoprofen The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Dexketoprofen is combined with Triamterene.
Droxicam The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Droxicam is combined with Triamterene.
Tolfenamic acid The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Tolfenamic acid is combined with Triamterene.
Firocoxib The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Firocoxib is combined with Triamterene.
Clonixin The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Clonixin is combined with Triamterene.
Morniflumate The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Morniflumate is combined with Triamterene.
Propacetamol The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Propacetamol is combined with Triamterene.

Target Protein

Amiloride-sensitive sodium channel subunit gamma SCNN1G
Amiloride-sensitive sodium channel subunit alpha SCNN1A
Amiloride-sensitive sodium channel subunit beta SCNN1B
Amiloride-sensitive sodium channel subunit delta SCNN1D

Referensi & Sumber

Synthesis reference: Frederic J. Nugent, John K. C. Yen, "Process for preparing the combination products of triamterene and hydrochlorothiazide." U.S. Patent US4804540, issued July, 1987.
Artikel (PubMed)
  • PMID: 6628507
    Gilfrich HJ, Kremer G, Mohrke W, Mutschler E, Volger KD: Pharmacokinetics of triamterene after i.v. administration to man: determination of bioavailability. Eur J Clin Pharmacol. 1983;25(2):237-41.
  • PMID: 13863613
    BABA WI, TUDHOPE GR, WILSON GM: Triamterene, a new diuretic drug. I. Studies in normal men and in adrenalectomized rats. Br Med J. 1962 Sep 22;2(5307):756-60. doi: 10.1136/bmj.2.5307.756.
  • PMID: 130243
    Knauf H, Wais U, Lubcke R, Albiez G: On the mechanism of action of triamterene: effects on transport of Na+, K+, and H+/HCO3- -ions. Eur J Clin Invest. 1976 Jan 30;6(1):43-50.
  • PMID: 6831748
    Mutschler E, Gilfrich HJ, Knauf H, Mohrke W, Volger KD: Pharmacokinetics of triamterene. Clin Exp Hypertens A. 1983;5(2):249-69.
  • PMID: 4552822
    Walker BR, Hoppe RC, Alexander F: Effect of triamterene on the renal clearance of calcium, magnesium, phosphate, and uric acid in man. Clin Pharmacol Ther. 1972 Mar-Apr;13(2):245-50.
  • PMID: 133688
    Knauf H, Wais U, Albiez G, Lubcke R: Inhibition of the exchange of Na+ for K+ and and H+ by triamterene (in epithelia)(author's transl). Arzneimittelforschung. 1976 Apr;26(4):484-6.
  • PMID: 26194642
    Tu W, Decker BS, He Z, Erdel BL, Eckert GJ, Hellman RN, Murray MD, Oates JA, Pratt JH: Triamterene Enhances the Blood Pressure Lowering Effect of Hydrochlorothiazide in Patients with Hypertension. J Gen Intern Med. 2016 Jan;31(1):30-6. doi: 10.1007/s11606-015-3469-1.
  • PMID: 2455308
    Horisberger JD, Giebisch G: Potassium-sparing diuretics. Ren Physiol. 1987;10(3-4):198-220.
Menampilkan 8 dari 10 artikel.
Textbook
  • ISBN: 978-0-7020-3471-8
    28. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 352-353, 356). Edinburgh: Elsevier/Churchill Livingstone.

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