Description

Simple

A medication that reduces swelling of the body caused by fluid buildup, and lowers blood pressure.

Clinical

A potassium-sparing diuretic used in the treatment of edema and in the management of hypertension.

Overview

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.[2] 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.[11] 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.[12]

Triamterene was approved by the Food and Drug Administration in the U.S. in 1964.[12] Currently, triamterene is used i... Read more

Pharmacology

Indication

Triamterene is indicated for the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and the nephrotic syndrome; also in steroid-induced edema, idiopathic edema, and edema due to secondary hyperaldosteronism.[ Read more

Pharmacodynamic

Triamterene, a relatively weak, potassium-sparing diuretic and antihypertensive, is used in the management of hypertension and edema. It primarily works on the distal nephron in the kidneys; it acts from the late distal tubule to the collecting duct to inhibit Na+ reabsorption and decreasing K+ excr... Read more

Mechanism of action

Triamterene inhibits the epithelial sodium channels (ENaC) located on the lumenal side in the late distal convoluted tubule and collecting tubule [ Read more

Absorption

Triamterene is shown to be rapidly absorbed in the gastrointestinal tract [15, Read more

Protein binding

67% bound to proteins. [15]

Volume of distribution

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.[ Read more

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.[ Read more

Half life

The half-life of the drug in plasma ranges from 1.5 to 2 hours.[14] In a pharmacokinetic study involving healthy volunteers, the terminal half-lives for tri... Read more

Route of elimination

Triamterene and its metabolites are excreted by the kidney by filtration and tubular secretion.[14] Upon oral ingestion, somewhat less than 50% of the oral... Read more

Toxicity

Acute oral LD50 of triamterene in rats is 400 mg/kg and 285-380 mg/kg in mice.[15,MSDS] There has been a case of reversible acute renal failure following ingestion of 50 combination pills containing... Read more

Adverse Effects

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

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

Interactions

Type in a drug name to check for interaction with Triamterene
Type a drug name in the box above to get started
  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Triamterene.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Triamterene.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Triamterene.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Triamterene.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Triamterene.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Triamterene.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Triamterene.
Abacavir
Triamterene may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Triamterene can be increased when combined with Abatacept.
Abiraterone
The serum concentration of Triamterene can be increased when it is combined with Abiraterone.
Acarbose
Triamterene may decrease the excretion rate of Acarbose which could result in a higher serum level.
Acebutolol
The risk or severity of hyperkalemia can be increased when Triamterene is combined with Acebutolol.
Aceclofenac
The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aceclofenac is combined with Triamterene.
Acefylline
The metabolism of Acefylline can be decreased when combined with Triamterene.
Acemetacin
The therapeutic efficacy of Triamterene can be decreased when used in combination with Acemetacin.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Triamterene.
Acetaminophen
The metabolism of Triamterene can be decreased when combined with Acetaminophen.
Acetyldigitoxin
Triamterene may decrease the excretion rate of Acetyldigitoxin 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.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Triamterene which could result in a higher serum level.
15 References
  1. 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. 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. 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. 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. 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. 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. 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. 8 . Horisberger JD, Giebisch G: Potassium-sparing diuretics. Ren Physiol. 1987;10(3-4):198-220.PubMed: 2455308
  9. 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. 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. 11 . 28. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 352-353, 356). Edinburgh: Elsevier/Churchill Livingstone.
  12. 12 . Triamterene - International Agency for Research on Cancer (IARC) Monographs Link
  13. 13 . DYAZIDE (hydrochlorothiazide and triamterene) - FDA Label Link
  14. 14 . PRO-TRIAZIDE (Triamterene 50 mg and Hydrochlorothiazide 25 mg) - Product Monograph Link
  15. 15 . DailyMed - DYRENIUM- triamterene capsule Link