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  • Title: Concentration-dependent blood pressure effects of guanfacine.
    Author: Frisk-Holmberg M, Wibell L.
    Journal: Clin Pharmacol Ther; 1986 Feb; 39(2):169-72. PubMed ID: 2867846.
    Abstract:
    Central alpha 2-adrenoceptor stimulation decreases blood pressure, whereas stimulation of postjunctional peripheral adrenoceptors induces a pressor response. The net blood pressure response during multiple dosing is the sum of these effects and is dependent on drug kinetics, receptor affinity, and receptor occupancy. Guanfacine (2 to 6 mg/day), a selective alpha 2-adrenoceptor agonist, decreased blood pressure in patients with hypertension. At a dose greater than 6 mg/day the antihypertensive response deteriorated. Steady-state kinetics were linear but there was a tendency for a decrease in clearance after the highest dose. These results have practical implications for the therapeutic handling of the drug: Low doses for maximal therapeutic effect and longer dosage intervals at high-dosage schedules are indicated.
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