Premium
Measurement of activity of 5‐HT antagonists following oral administration in man: a comparison of methysergide and BW501.
Author(s) -
O'Grady J,
Peringer E,
John G
Publication year - 1979
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1979.tb00921.x
Subject(s) - methysergide , pharmacology , drug , crossover study , medicine , oral administration , dosing , serotonin , chemistry , receptor , alternative medicine , pathology , placebo
1 Oral doses of BW501 and methysergide administered to healthy volunteers inhibited the ex vivo platelet aggregation response to 5‐ hydroxytryptamine (5‐HT). 2 Two volunteers received 100 mg BW501 and two received 10 mg BW501 and aggregation response was measured immediately pre drug and at 1,3 and 24 h post drug. After 100 mg BW501 the response to 5‐HT was completely inhibited at all times studied, after 10 BW501 a response too small to measure was apparent at 24 h only. 3 In two randomised crossover studies subjects received either 2 mg BW501 (nine subjects), 2 mg methysergide (six subjects) or no drug (nine subjects) and aggregation response to 5‐HT was measured immediately pre drug and at 1, 2, 3, 5, 7, 24 h post drug. 4 Methysergide (2 mg) produced complete inhibition of aggregation for 24 h after dosing; following 2 mg BW501 the aggregation response was significantly lower than on the control occasion at 1 (P less than 0.01), 2 (P less than 0.01) and 3 (P less than 0.05) h post drug. The response was inhibited by rr%, 31% and 16% at these times respectively. 5 It is suggested that this technique provides a suitable method for demonstration of activity of 5‐HT antagonists after oral dosing in man.