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Pharmacokinetic and pharmacodynamic studies of oral clonidine in normotensive subjects (1982)

Anavekar, S. N. ; Jarrott, B. ; Toscano, M. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 1-5

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ISSN: 1432-1041

Keywords: clonidine ; noradrenaline ; pharmacokinetics ; arterial blood pressure ; plasma concentration

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetics of clonidine and its relation to blood pressure response and side effects were studied after single oral doses of 75 µg, 150 µg and 250 µg in normotensive subjects. Following oral administration, the drug was absorbed rapidly after an initial lag time of 19–22 min and peak levels were reached between 2.4 and 2.9 h. Sampling over 48 h was necessary for accurate estimation of pharmacokinetic parameters. Post-peak plasma concentration declined in a monoexponential manner and the half-life of the elimination phase ranged from 9.0 to 15.1 h. Maximum plasma concentration (Cmax) and area under curve (AUC) increased proportionally with increasing doses. Clonidine produced significant reductions in the pulse rate and a dose dependent decrease in blood pressure. Clonidine (150 µg) also produced significant reductions in plasma catecholamine levels.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01061368

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The relationship of plasma levels of pindolol in hypertensive patients to effects on blood pressure, plasma renin and plasma noradrenaline levels (1975)

Anavekar, S. N. ; Louis, W. J. ; Morgan, T. O. ; [et al.]

Oxford, UK : Blackwell Publishing Ltd

Clinical and experimental pharmacology and physiology 2 (1975), S. 0

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ISSN: 1440-1681

Source: Blackwell Publishing Journal Backfiles 1879-2005

Topics: Medicine

Notes: 〈list xml:id="l1" style="custom"〉1Fifteen, previously untreated, hypertensive patients were given 20 mg of pindolol, orally. The systolic and diastolic blood pressures fell significantly in 1 h; the effect was maximal 4 h after pindolol, and persisted for at least 8 h.2After oral administration of 20 mg of pindolol, its concentration in the plasma reached a peak in 2–3 h. At the end of 8 h, pindolol was not detectable in the plasma.3There was a significant relationship between the peak concentration of pindolol in plasma and the maximal change in blood pressure in fifteen previously untreated hypertensive patients. In a separate study of ninety-nine hypertensive outpatients taking 15–80 mg of pindolol daily, the blood pressure responses corresponded generally to the concentration of pindolol in plasma 2–3 h after the morning dose.4There were no significant changes in plasma renin activity, plasma renin concentration or plasma noradrenaline concentration in the previously untreated patients taking 20 mg of pindolol. There was no relationship between initial plasma renin or noradrenaline levels and blood pressure responses to pindolol. Nor was there any significant relationship between the changes in plasma renin or noradrenaline levels and the changes in blood pressure.