Angiotensin-Related Drugs

Alpha Blockers – Central and Peripheral Acting


 

Mechanism of Action

Alpha-blockers work by blocking peripheral alpha receptors, thereby decreasing peripheral vascular resistance – causing relaxation and decreased blood pressure. They also relax the smooth muscle in the bladder neck and prostate gland, thus reducing bladder outlet obstruction.  Since many of the older men who suffer from hypertension also have prostate enlargement, taking alpha blockers can help with both problems.   Centrally acting agents actually work (in the brain) by binding to the same receptors as substances that usually cause an increase in blood pressure and thereby prevents binding of the other substances to result in lowering of blood pressure.


Contraindications to Therapy:

Side Effects

Peripheral Alpha Blockers


Drug Dosage Regimen Drug Interactions
Doxazosin
(Cardura®)
Oral:
Initial:1 mg once daily
Maintenance: 1-16 mg once daily
Verapamil – increased risk of severe lowering in blood pressure
Prazosin
(Minipress®)
Oral: Initial not to exceed 1 mg at bedtime
Maintenance: 3-20 mg daily (divided 2-3 times daily)
Verapamil – increased risk of severe lowering in blood pressure
Terazosin
(Hytrin®)
Oral:
Initial: 1 mg once daily at bedtime
Maintenance: 1-5 mg once or twice daily; Maximum: 20-40 mg/day
Verapamil – increased risk of severe lowering in blood pressure
 

 

Central Alpha Blockers (agonists)

Drug Dosage Regimen Drug Interactions

Clonidine hydrochloride
(Catapres®)

Oral:
Initial:  0.1 mg twice daily (morning and bedtime)
Maintenance: Increase in increments of 0.1 mg daily at weekly intervals; usual daily dose is 0.2-0.6 mg in divided doses; Maximum: 2.4 mg/day

Transdermal Patch:
Initial: 0.1 mg/day applied once every 7 days to upper outer arm or chest
Maintenance: increase by 0.1 mg/day every one to two weeks as needed; Maximum: 0.6 mg/day every 7 days

Beta-blockers-May cause acute decreases in blood pressure
Increased-risk of cyclosporine toxicity

Guanabenz Acetate (Wytensin®)

Oral:
Initial: 4 mg twice daily
Maintenance: may increase in increments of 4-8 mg/day at 1-2 wk intervals
Maximum: 32 mg twice daily

Ma Huang - increased blood pressure
Yohimbine-reduces effectiveness of guanabenz

Methyldopa (Aldomet®)

Oral:
Initial: 250 mg two-three times daily; may adjust dose at intervals of not less than every 2 days; Maintenance: 500-2000 mg daily in 2-4 divided doses; Maximum: 3000 mg daily
IV:
250-500 mg every 6 hr;
Maximum: 1000 mg IV every 6 hr