Guanadrel is rapidly absorbed, leading to maximal levels in plasma at 1—2 hours. Because gua-nadrel must be transported into and accumulate in adrenergic neurons, the maximum effect on blood pressure is not seen until 4—5 hours. Although the ¡3 phase of its elimination has a t/2 of ~5—10 hours, this almost certainly does not reflect the longer t/2 of drug stored at its site of action in the secretory vesicles of adrenergic neurons. The t122 of the pharmacological effect of guanadrel is determined by the drug's persistence in this neuronal pool and is probably at least 10 hours. Guanadrel is administered in a regimen of twice-daily doses.
Guanadrel is cleared by both renal and nonrenal disposition. Its elimination is impaired in patients with renal insufficiency; total-body clearance is reduced by four- to fivefold in patients with severe renal dysfunction.
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