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Triamterene

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Triamterene

Triamterene
Systematic (IUPAC) name
6-phenylpteridine-2,4,7-triamine
Clinical data
Trade names Dyrenium, Dyazide, Maxzide
AHFS/Drugs.com
MedlinePlus
Pregnancy cat.
Legal status
Routes oral
Pharmacokinetic data
Bioavailability 30-70%
Protein binding 67%
Metabolism conjugated to hydroxytriamterene
Half-life 1-2 hours, active metabolite 3 hours
Excretion renal <50%, 21% unchanged
Identifiers
CAS number  YesY
ATC code C03
PubChem
IUPHAR ligand
DrugBank
ChemSpider  YesY
UNII  YesY
KEGG  N
ChEMBL  YesY
Chemical data
Formula C12H11N7 
Mol. mass 253.263 g/mol
 N   

Triamterene (trade name Dyrenium) is a potassium-sparing diuretic used in combination with thiazide diuretics for the treatment of hypertension and edema. In combination with hydrochlorothiazide, it is marketed under the names Maxzide and Dyazide.

Contents

  • Mechanism of action 1
  • Side effects 2
  • Caution with certain disease states 3
  • With hydrochlorothiazide 4
  • Use in Ménière's disease 5
  • References 6
  • External links 7

Mechanism of action

Triamterene directly blocks the epithelial sodium channel[1] (ENaC) on the lumen side of the kidney collecting tubule. Other diuretics cause a decrease in the sodium concentration of the forming urine due to the entry of sodium into the cell via the ENaC, and the concomitant exit of potassium from the principal cell into the forming urine. Blocking ENaC prevents this from happening. Amiloride works in the same way. Sodium channel blockers directly inhibit the entry of sodium into the sodium channels.

Side effects

Common side effects may include a depletion of sodium, folic acid and calcium, nausea, vomiting, diarrhea, headache, dizziness, fatigue, and dry mouth. Serious side effects may include heart palpitations, tingling/numbness, fever, chills, sore throat, rash, and back pain. Triamterene can also cause kidney stones through direct crystallization or by seeding calcium oxalate stones. Triamterene is best avoided in patients with chronic kidney disease due to the possibility of hyperkalemia. People using this drug should use salt substitute cautiously.[2]

Triamterene may impart a blue fluorescent color to the urine.

Caution with certain disease states

Diabetes: Use with caution in patients with prediabetes or diabetes mellitus as there may be a change in glucose control.

Hepatic impairment: Use with caution in patients with severe hepatic dysfunction; in cirrhosis, avoid electrolyte and acid/base imbalances that might lead to hepatic encephalopathy.

Kidney stones: Use with caution in patients with kidney stones.

Use should be avoided if the creatinine clearance is less than 10 ml/minute.

With hydrochlorothiazide

Triamterene is commonly prepared in combination with hydrochlorothiazide for treatment of hypertension (high blood pressure) and edema (water retention). This combination is in a class of medications called diuretics or 'water pills', and causes the kidneys to get rid of the body's unneeded water and sodium through the urine.[3] Dyazide is marketed by GlaxoSmithKline and Maxzide is marketed by Mylan.

Use in Ménière's disease

While there is a lack of randomized controlled trials evaluating the use of triamterene in the treatment of Ménière's disease, the typical treatment is 37.5 mg of triamterene with 25 mg of hydrochlorothiazide 1–2 capsules daily.[4][5] This recommendation was given a Strength of Recommendation Taxonomy (SORT) grade of C.

References

  1. ^ Busch AE; Suessbrich H; Kunzelmann K; et al. (September 1996). "Blockade of epithelial Na+ channels by triamterenes - underlying mechanisms and molecular basis". Pflugers Arch. 432 (5): 760–6.  
  2. ^ LoSalt Advisory Statement (PDF)
  3. ^ "Triamterene and Hydrochlorothiazide". MedlinePlus. U.S. National Library of Medicine. National Institutes of Health. September 1, 2008.
  4. ^ Swartz R; Longwell P (March 2005). "Treatment of vertigo".  
  5. ^ Sloane PD; Coeytaux RR; Beck RS; Dallara J (May 2001). "Dizziness: state of the science".  

External links

  • Dyazide Prescribing Information GlaxoSmithKline
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