Drug information of Triamterene


Drug group:

Triamterene (2,4,7-triamino-6-phenylpteridine) is a potassium-sparing diuretic that is used in the management of hypertension.

Mechanism of effect

Triamterene inhibits the epithelial sodium channels (ENaC) located on the lumenal side in the late distal convoluted tubule and collecting tubule, which are transmembrane channels that normally promotes sodium uptake and potassium secretion. In the late distal tubule to the collecting duct, sodium ions are actively reabsorbed via ENaC on the lumnial membrane and are extruded out of the cell into the peritubular medium by a sodium-potassium exchange pump, the Na-K-ATPase, with water following passively. Triamterene exerts a diuretic effect on the distal renal tubule to inhibit the reabsorption of sodium ions in exchange for potassium and hydrogen ions and its natriuretic activity is limited by the amount of sodium reaching its site of action. Its action is antagonistic to that of adrenal mineralocorticoids, such as aldosterone, but it is not an inhibitor or antagonist of aldosterone. Triamterene maintains or increases the sodium excretionm, thereby increasing the excretion of water, and reduces the excess loss of potassium, hydrogen and chloride ions by inhibiting the distal tubular exchange mechanism. Due to its diuretic effect, triamterene rapidly and reversibly reduces the lumen-negative transepithelial potential difference by almost complete abolition of Na+ conductance without altering K+ conductance. This reduces the driving force for potassium movement into the tubular lumen and thus decreases potassium excretion. Triamterene is similar in action to amiloride but, unlike amiloride, increases the urinary excretion of magnesium.


As triamterene tends to conserve potassium more strongly than promoting Na+ excretion, it can cause an increase in serum potassium, which may result in hyperkalemia potentially associated with cardiac irregularities. In healthy volunteers administered with oral triamterene, there was an increase in the renal clearnace of sodium and magnesium, and a decrease in the clearance of uric acid and creatinine due to its effect of reducing glomerular filtration renal plasma flow. Triamterene does not affect calcium excretion.


Half-Life: 1.5-2.5 hr

Duration: 7-9 hr

Onset: Initial effect: 2-4 hr; Max effect: diuresis: several days, HTN: 2-3 months

Peak Plasma Time: 1.5-3 hr

Bioavailability: 30-70%

Protein Bound: 55-67%

Metabolism: Liver

Metabolites: hydroxytriamterene sulfate (active)

Excretion: urine 21%

Dialyzable: Yes (hemodialysis)

Drug indications

edema , Hypertension




100-300 mg/day PO qDay or divided q12hr


100-300 mg/day PO qDay or divided q12hr


Hypertension (Off-label)

Safety & efficacy not established

1-2 mg/kg/day PO divided q12hr 

Maximum dose: 3-4 mg/kg/day PO divided q12hr up to 300 mg/day

Drug contraindications

renal failure , Anuria , Hypersensitivity


Acid-base imbalance, electrolyte abnormalities, hyperuricemia or gout, liver dz, renal impairment, renal stones


Interferes with fluorescent assay of quinidine

Not recommended for pregnancy-induced HTN

Use during pregnancy may increase risk of cardiovascular defects and oral cleft in child

Points of recommendation

Take triamterene exactly as it was prescribed for you. Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Take this medicine after eating a meal.

Taking a diuretic can make you urinate more often, which could disrupt your sleep if this happens at night. If you take triamterene only once per day, take it in the morning to reduce the chance of night-time urination.

While using this medicine, you may need frequent blood tests. Your kidney function may also need to be checked.

Your heart function may need to be checked using an electrocardiogram or ECG (also called an EKG).

This medicine can cause unusual results with certain medical tests. Tell any doctor who treats you that you are using triamterene.

If you need surgery, tell the surgeon ahead of time that you are using triamterene.

Store at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

This medicine may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Drinking alcohol with this medicine can cause side effects.

Do not use salt substitutes or low-sodium milk products that contain potassium. These products could cause your potassium levels to get too high while you are taking triamterene.

Pregnancy level

Group c - Not adequate studies in pregnant women

Related drugs

Amiloride , Spironolactone , eplerenone

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