Triamterene


Description

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...

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Pharmacology

Indication

Triamterene is indicated for the treatment of edema associated with congestive heart failure, cirrho... Read more

Pharmacodynamic

Triamterene, a relatively weak, potassium-sparing diuretic and antihypertensive, is used in the mana... Read more

Mechanism of action

Triamterene inhibits the epithelial sodium channels (ENaC) located on the lumenal side in the late d... Read more

Absorption

Triamterene is shown to be rapidly absorbed in the gastrointestinal tract [ Read more

Protein binding

67% bound to proteins. [Label]

Volume of distribution

In a pharmacolinetic study involving healthy volunteers receiving triamterene intravenously, the vol... Read more

Clearance

The total plasma clearance was 4.5 l/min and renal plasma clearance was 0.22 l/kg following intraven... Read more

Half life

The half-life of the drug in plasma ranges from 1.5 to 2 hours.[ Read more

Route of elimination

Triamterene and its metabolites are excreted by the kidney by filtration and tubular secretion.[ Read more

Toxicity

Acute oral LD50 of triamterene in rats is 400 mg/kg and 285-380 mg/kg in mice.[Label,MSDS] There has... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Hyperkalemia US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Dry Mouth US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Dizziness US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Headache US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Renal Stones US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Serum creatinine elevation US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    BUN elevation US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Azotemia US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Hypokalemia US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Photosensitivity US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Rash US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Anaphylaxis US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Weakness US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Fatigue US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Megaloblastic anemia US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Thrombocytopenia US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Vomiting US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Diarrhea US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Nausea US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Liver enzyme abnormalities US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Acute Renal Failure US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Jaundice US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports
    Acute Interstitial Nephritis US
  • Kind: experimental
    • Percent: <0.1%
  • Varying Reports

    Contraindications

    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Anuria
        • Drugbank Id: DBCOND0001345
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Elevated serum potassium levels
        • Drugbank Id: DBCOND0096865
    • Route:
      • Oral
    • Regions: US
    • With Categories Coadmin:
        • Name: Potassium-Sparing Diuretics
        • Drugbank Id: DBCAT002702
        • Mesh Id: D062865
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Severe progressive kidney disease
        • Drugbank Id: DBCOND0107691
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Severe hepatic disease
        • Drugbank Id: DBCOND0107692
        • Modification Of:
          • Base:
            • Name: Hepatic Disease
            • Drugbank Id: DBCOND0069929
          • Severity:
            • Includes:
              • severe

    Food Interactions

      Information currently not available.

    Interactions

    Type in a drug name to check for interaction with Triamterene

    The metabolism of (R)-warfarin can be decreased when combined with Triamterene.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Triamterene.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Triamterene.
    The metabolism of 8-azaguanine can be decreased when combined with Triamterene.
    The metabolism of 8-chlorotheophylline can be decreased when combined with Triamterene.
    The metabolism of 9-Deazaguanine can be decreased when combined with Triamterene.
    The metabolism of 9-Methylguanine can be decreased when combined with Triamterene.
    Triamterene may decrease the excretion rate of Abacavir which could result in a higher serum level.
    The metabolism of Triamterene can be increased when combined with Abatacept.
    The serum concentration of Triamterene can be increased when it is combined with Abiraterone.
    Triamterene may decrease the excretion rate of Acarbose which could result in a higher serum level.
    The risk or severity of hyperkalemia can be increased when Triamterene is combined with Acebutolol.
    The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aceclofenac is combined with Triamterene.
    The metabolism of Acefylline can be decreased when combined with Triamterene.
    The therapeutic efficacy of Triamterene can be decreased when used in combination with Acemetacin.
    The metabolism of Acenocoumarol can be decreased when combined with Triamterene.
    The metabolism of Triamterene can be decreased when combined with Acetaminophen.
    Triamterene may decrease the excretion rate of Acetyldigitoxin which could result in a higher serum level.
    Triamterene may decrease the excretion rate of Acetyldigoxin which could result in a higher serum level.
    Acetylsalicylic acid may decrease the excretion rate of Triamterene which could result in a higher serum level.

    References

    • 1 . 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. [PubMed: 6628507]
    • 2 . 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. [PubMed: 13863613]
    • 3 . 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. [PubMed: 130243]
    • 4 . Mutschler E, Gilfrich HJ, Knauf H, Mohrke W, Volger KD: Pharmacokinetics of triamterene. Clin Exp Hypertens A. 1983;5(2):249-69. [PubMed: 6831748]
    • 5 . 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. [PubMed: 4552822]
    • 6 . 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. [PubMed: 133688]
    • 7 . 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. [PubMed: 26194642]
    • 8 . Horisberger JD, Giebisch G: Potassium-sparing diuretics. Ren Physiol. 1987;10(3-4):198-220. [PubMed: 2455308]
    • 9 . Hasegawa J, Lin ET, Williams RL, Sorgel F, Benet LZ: Pharmacokinetics of triamterene and its metabolite in man. J Pharmacokinet Biopharm. 1982 Oct;10(5):507-23. [PubMed: 7166735]
    • 10 . Fuhr U, Kober S, Zaigler M, Mutschler E, Spahn-Langguth H: Rate-limiting biotransformation of triamterene is mediated by CYP1A2. Int J Clin Pharmacol Ther. 2005 Jul;43(7):327-34. [PubMed: 16035375]
    • 11 . 28. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 352-353, 356). Edinburgh: Elsevier/Churchill Livingstone.
    • 12 . Triamterene - International Agency for Research on Cancer (IARC) Monographs [Link]
    • 13 . DYAZIDE (hydrochlorothiazide and triamterene) - FDA Label [Link]
    • 14 . PRO-TRIAZIDE (Triamterene 50 mg and Hydrochlorothiazide 25 mg) - Product Monograph [Link]

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