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Pharmacokinetics and Antihypertensive Effects of Low Dose Clonidine During Chronic Therapy
Author(s) -
Anavekar Sadanand N.,
Howes Laurence G.,
Jarrott Bevyn,
Syrjanen Marie,
Conway Elizabeth L.,
Louis William J.
Publication year - 1989
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1989.tb03335.x
Subject(s) - clonidine , medicine , pharmacokinetics , pharmacology , anesthesia
Using a sensitive and specific radioimmunoassay the pharmacokinetic disposition of clonidine was determined in hypertensive patients after a single dose and then after 5, 28 and 56 days of chronic dosing with 75 μg bd. Following a single dose of clonidine maximal plasma concentrations of 0.34 ± 0.06 ng/ml were achieved after 3.6 ± 1.2 hours. After 5 days of repetitive dosing the maximal concentration was significantly higher, 0.66 ± 0.06 ng/ml and remained so throughout chronic therapy ( P = 0.018). The AUC, T max and T 1/2 did not differ significantly between the acute dose and the chronic dosing pharmacokinetic studies. Clonidine also produced a significant fall in blood pressure. Supine diastolic blood pressure fell from 106 ± 5 mmHg predose to 99 ± 6 mmHg 2 hours after the first dose ( P < 0.05). The corresponding values after cyclopenthiazide alone were 108 ± 8 and 105 ± 8 mmHg ( P = 0.13). Similar falls in blood pressure were produced during chronic therapy .