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These agents antagonise inhibit catecholamine uptake in smooth muscle cells of peripheral vasculature, resulting in vasodilation and blood pressure lowering. Examples include
Generic name | Common brand names | Usual dose range (mg/day) | Daily frequency |
Prazosin | Minipress | 2 – 20 | 2 or 3 |
Doxazosin | Cardura | 1 – 16 | 1 |
Terazosin | Hytrin | 1 – 20 | 1 or 2 |
Some noted possible side effects of α-adrenoreceptor blockers
Central α2-agonists lower blood pressure primarily by stimulating α2-adrenergic receptors in the brain, which reduces sympathetic outflow from the vasomotor centre and increases vagal tone. Stimulation of presynaptic α2-receptors peripherally may contribute to reduced sympathetic tone. Consequently, there may be decreases in heart rate, cardiac output, total peripheral resistance, plasma renin activity, and baroreceptor reflexes. Examples of central α2-agonists include
Generic name | Common brand names | Usual dose range (mg/day) | Daily frequency |
Methyldopa | Aldomet | 250 – 1,000 | 2 |
Clonidine HCl | Catapres | 0.1 – 0.8 | 2 |
Clonidine patch | Catapres-TTS | 0.1 – 0.3 | 1 weekly |
Guanfacine | Tenex | 0.5 – 2 | 1 |
Some noted possible side effects of central α2-agonists
These drugs cause direct arteriolar smooth muscle relaxation. They decrease total peripheral resistance and thus correct the hemodynamic abnormality that is responsible for the elevated blood pressure in primary hypertension. In addition, because they act directly on vascular smooth muscle, the vasodilators are effective in lowering blood pressure, regardless of the aetiology of the hypertension.
Generic name | Common brand names | Usual dose range (mg/day) | Daily frequency |
Minoxidil | Loniten | 10 – 40 | 1 or 2 |
Hydralazine | Apresoline | 20 – 100 | 2 to 4 |
Some noted possible side effects of direct vasodilators
Similar to ACEIs or ARBs, direct renin inhibitors target the rate-limiting step in the RAAS. Aliskiren, approved in 2007, is the only direct renin inhibitor. It is contraindicated in pregnancy due to known teratogenic effects.
Generic name | Common brand names | Usual dose range (mg/day) | Daily frequency |
Aliskiren | Tekturna | 150 – 300 | 1 |
Some noted possible side effects of direct renin inhibitors
Aldosterone exerts its effects at the nephron through mineralocorticoid receptors, which translocate to the nucleus upon aldosterone binding and exert genomic effects leading to increased sodium reabsorption. Potent blockade of the aldosterone receptor inhibits sodium and water retention and inhibits vasoconstriction. These agents are also considered potassium-sparing diuretics.
Generic name | Common brand names | Usual dose range (mg/day) | Daily frequency |
Eplerenone | Inspra | 50 – 100 | 1 or 2 |
Spironolactone | Aldactone | 25 – 50 | 1 or 2 |
Spironolactone/hydrochlorothiazide | Aldactazide | 25 – 50/25 – 50 | 1 |
Some noted possible side effects of aldosterone receptor antagonists
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