Methyldopa in Hypertension Clinical and Pharmacological Studies

Dollery, C. T.; Harington, M.

doi:10.1016/s0140-6736(62)91781-6

Cited by 128 publications

(32 citation statements)

References 5 publications

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“…The peak effect is delayed and occurs 6-9 h after the dose; the effect then declines with a half-life of approximately 10 h and only a small effect remains by 24-26 h. This time course is similar (0) to that found in earlier studies where the antihypertensive effect was measured after a single oral dose (Dollery & Harrington, 1962;Gillespie et al, 1962). The time course of antihypertensive effect does not correlate with the rapid serum half-life of methyldopa (1-2 h); however, it may correlate with a second phase serum half-life of methyldopa and/or metabolites (Stenbeak et al, 1977).…”

Section: Discussionsupporting

confidence: 80%

“…(2) Single oral doses of methyldopa produced antihypertensive effects which were still noticeable 24 h later (Dollery & Harrington, 1962;Jain etal., 1973). (3) In a doubleblind (Wright et al, 1976) and open (Pipkin et al, 1980) The patients were prescribed a total daily dose of methyldopa which was the nearest multiple of 500 mg to the dosage of methyldopa which they were previously receiving.…”

Section: Introductionmentioning

confidence: 99%

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Duration of effect of single daily dose methyldopa therapy.

Jm¹,

Orozco-Gonzalez²,

Polak³

et al. 1982

Brit J Clinical Pharma

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1 Methyldopa has a short plasma half‐life, but longer duration of antihypertensive effect. A single bedtime dose of methyldopa has been recommended to improve compliance and decrease side effects. 2 This double‐blind crossover study was designed to determine the duration of antihypertensive effect of methyldopa by comparing hourly supine and standing blood pressures, throughout the day during placebo, single morning dose, and single evening dose methyldopa therapy in 10 patients. The major side effects, drowsiness and dry mouth were assessed by visual analogue scale. Exercise blood pressures were measured 6, 12, 18 and 24 h after the dose. 3 The antihypertensive effect of methyldopa peaked after 6‐9 h and declined thereafter with a half‐life of approximately 10 h. Little antihypertensive effect remained 24‐26 h after the dose. The time course of the reduction in blood pressure during exercise and of the major side effects paralleled the antihypertensive effects. 4 The results suggest that the duration of antihypertensive effect of methyldopa is long enough to permit twice daily dosing, but that single daily dosing cannot be recommended for most patients. The study illustrates the importance of knowing the time of the last methyldopa dose when assessing blood pressure measurements in patients taking the drug.

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Section: Discussionsupporting

confidence: 80%

Section: Introductionmentioning

confidence: 99%

Duration of effect of single daily dose methyldopa therapy.

Jm¹,

Orozco-Gonzalez²,

Polak³

et al. 1982

Brit J Clinical Pharma

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“…The urinary metabolites of orally administered 2-14C-labeled a-methyldopa were measured in 20 hypertensive patients before and after treatment with a-methyldopa in a dose of 3.0 g daily for 3 months. There was considerable variation in the absorption, biotransformation and excretion of a-methyldopa after an oral dose, but differences in clinical response to a-methyldopa could not be attributed to this.…”

Section: Discussionmentioning

confidence: 99%

Combined Clinical and Metabolic Study of the Effects of Alpha-Methyldopa on Hypertensive Patients

Prescott¹,

Buhs²,

Beattie³

et al. 1966

Circulation

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“…The effect of a-methyldopa on heart rate in the rat is less well documented. A decrease in heart rate has been reported after a-methyldopa administration in man and in anesthetized dogs (Dollery and Harington, 1962;Antonaccio et al, 1974). In the anesthetized rat, however, a short lasting increase * Present address: Department of Pharmacology, University of Toronto, Medical Sciences Building, Toronto 181, Canada.…”

Section: Introductionmentioning

confidence: 99%

Central inhibitory effect of α-methyldopa on blood pressure, heart rate and body temperature of renal hypertensive rats

Nijkamp

Ezer

Jong

1975

European Journal of Pharmacology

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Central inhibitory effect of a-methyldopa on blood pressure, heart rate and body temperature of renal hypertensive rats, European J. Pharmacol. 31 (1975) 243--249.The central inhibitory effect of ~-methyldopa on blood pressure, heart rate and body temperature was studied in conscious renal hypertensive rats. Systemic administration of a-methyldopa decreased mean arterial blood pressure and body temperature and caused a short lasting increase in heart rate followed by a long lasting decrease. Inhibition of central decarboxylase activity prevented the decrease in blood pressure, heart rate and body temperature but not the initial increase in heart rate. Inhibition of peripheral decarboxylase activity blocked the increase in heart rate and partially reduced the decrease in heart rate and body temperature but did not affect the decrease in blood pressure. ~-Methyldopa also decreased blood pressure at an ambient temperature of 30 ° C, but the decrease of body temperature was absent and the heart rate remained elevated for 7 hr. Similar results were obtained in normotensive rats. The decrease in heart rate was correlated with the decrease in body temperature in normotensive and renal hypertensive rats.These findings suggest that in the renal hypertensive rat the decrease in blood pressure and in body temperature depends on a central action of a-methyldopa metabolites.

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Methyldopa in Hypertension Clinical and Pharmacological Studies

Cited by 128 publications

References 5 publications

Duration of effect of single daily dose methyldopa therapy.

Duration of effect of single daily dose methyldopa therapy.

Combined Clinical and Metabolic Study of the Effects of Alpha-Methyldopa on Hypertensive Patients

Central inhibitory effect of α-methyldopa on blood pressure, heart rate and body temperature of renal hypertensive rats

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