Determination of the optimal dose of the antihypertensive drug cicletanine hydrochloride in man.
The optimal antihypertensive dose of cicletanine (BN 1270) was investigated in 3 short-term and 3 long-term therapeutic trials using doses of 12.5 to 200 mg. There was a dose-response effect such that in double-blind studies of 1 month's duration, 50 mg/d was the minimum effective dose in mild to moderate hypertensive patients, while a higher dose, 200 mg/d, was more effective in patients with severe hypertension. Despite a quicker reduction in blood pressure by 100 mg cicletanine compared with 50 mg, a similar antihypertensive effect resulted after 3 months' treatment. In patients with mild to moderate hypertension the average decrease in blood pressure over this period was 43.7/38.0 mmHg. A daily dose of 50 mg, which may be increased, particularly at the beginning of treatment, is therefore the optimal recommended dose for these patients. Furthermore, the similar efficacy of the 50 mg and 100 mg doses was confirmed in the long-term trial in the elderly. In all studies, at all doses, cicletanine had a gradual antihypertensive effect, avoiding the risks associated with a sudden fall in blood pressure. The different rates of effect of the 50 mg and 100 mg doses are thought to be due to different mechanisms of action: since 50 mg has no natriuretic effect and 100 mg has a slight natriuretic effect, which is even more pronounced at higher doses.
Guinot
P
P
Ipsen International Ltd., London, U.K.
Jewitt-Harris
J
J
Tarrade
T
T
D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D004232:Diuretics / Q000008:administration & dosage* / Q000627:therapeutic use; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D008297:Male; D008875:Middle Aged; D011725:Pyridines; D011897:Random Allocation; D012964:Sodium / Q000652:urine; D013997:Time Factors
D000959:Antihypertensive Agents; D004232:Diuretics; D011725:Pyridines; D012964:Sodium; C038068:cicletanine