Clinical pharmacokinetics of moxonidine

The pharmacokinetic profile of moxonidine was determined in healthy volunteer and patient populations. Moxonidine is rapidly and almost completely absorbed from the gastrointestinal tract. The drug is not subject to first-pass metabolism; its absolute bioavailability is 88%. Only 7.2% is bound to plasma proteins. Moxonidine is predominantly eliminated as unchanged drug via the renal route with a plasma half-life of approximately 2 h. Concurrent food intake does not influence the systemic availability of moxonidine, nor does drug accumulation occur after repeated administration. The systemic availability is increased in renal impairment, necessitating dose adjustment in patients with reduced renal function. Aging does not affect the pharmacokinetics to a clinically relevant extent. Moxonidine can be coadministered with drugs such as digoxin, hydrochlorothiazide, and glibenclamide without risk of pharmacokinetic interactions.