Triamterene is a potassium-conserving (antikaliuretic) diuretic with relatively weak natriuretic properties. It exerts its diuretic effect on the distal renal tubule to inhibit the reabsorption of sodium in exchange for potassium and hydrogen. With this action, triamterene increases sodium excretion and reduces the excessive loss of potassium and hydrogen associated with hydrochlorothiazide. Triamterene is not a competitive antagonist of the mineralocorticoids and its potassium-conserving effect is observed in patients with Addison's disease, i.e., without aldosterone. Triamterene's onset and duration of activity is similar to hydrochlorothiazide. No predictable antihypertensive effect has been demonstrated with triamterene.

Triamterene is rapidly absorbed following oral administration. Peak plasma levels are achieved within one hour after dosing. Triamterene is primarily metabolized to the sulfate conjugate of hydroxytriamterene. Both the plasma and urine levels of this metabolite greatly exceed triamterene levels.

The amount of triamterene added to 50 mg of hydrochlorothiazide in triamterene and hydrochlorothiazide tablets, 75 mg/50 mg was determined from steady-state dose-response evaluations in which various doses of liquid preparations of triamterene were administered to hypertensive persons who developed hypokalemia with hydrochlorothiazide (50 mg given once daily). Single daily doses of 75 mg triamterene resulted in greater increases in serum potassium than lower doses (25 mg and 50 mg), while doses greater than 75 mg of triamterene resulted in no additional elevations in serum potassium levels. The amount of triamterene added to the 25 mg of hydrochlorothiazide in triamterene and hydrochlorothiazide tablets, 37.5 mg/25 mg was also determined from steady-state dose-response evaluations in which various doses of liquid preparations of triamterene were administered to hypertensive persons who developed hypokalemia with hydrochlorothiazide (25 mg given once daily). Single daily doses of 37.5 mg triamterene resulted in greater increases in serum potassium than a lower dose (25 mg), while doses greater than 37.5 mg of triamterene, i.e., 75 mg and 100 mg, resulted in no additional elevations in serum potassium levels. The dose-response relationship of triamterene was also evaluated in patients rendered hypokalemic by hydrochlorothiazide given 25 mg twice daily. Triamterene given twice daily increased serum potassium levels in a dose related fashion. However, the combination of triamterene and hydrochlorothiazide given twice daily also appeared to produce an increased frequency of elevation in serum BUN and creatinine levels. The largest increases in serum potassium, BUN and creatinine in this study were observed with 50 mg of triamterene given twice daily, the largest dose tested. Ordinarily, triamterene does not entirely compensate for the kaliuretic effect of hydrochlorothiazide and some patients may remain hypokalemic while receiving triamterene and hydrochlorothiazide. In some individuals, however, it may induce hyperkalemia (see WARNINGS).

The triamterene and hydrochlorothiazide components of triamterene and hydrochlorothiazide tablets are well absorbed and are bioequivalent to liquid preparations of the individual components administered orally. Food does not influence the absorption of triamterene or hydrochlorothiazide from triamterene and hydrochlorothiazide tablets. The hydrochlorothiazide component of triamterene and hydrochlorothiazide tablets is bioequivalent to single entity hydrochlorothiazide tablet formulations.