The clinical pharmacology, pharmacokinetics and metabolism of sumatriptan.
Clinical pharmacology studies were undertaken in young healthy volunteers, in a small number of elderly subjects and in migraine subjects during and between attacks. Absorption after subcutaneous and oral administration was rapid. Bioavailability was nearly 100% after subcutaneous administration and averaged 14% after oral administration. Elimination was predominantly by metabolism to a non-active indoleacetic acid analogue. The plasma half-lives of sumatriptan and the metabolite were about 2 h. Pharmacokinetic and pharmacodynamic variables were similar in all groups studied and were not altered by the presence of food, alcohol, dihydroergotamine or prophylactic migraine treatments. Sumatriptan produced a number of minor adverse events, but had no clinically significant effect on routine haematological or biochemical investigations using the intravenous, subcutaneous or oral routes. Transient rises in blood pressure were observed which were no greater than those that would be anticipated during moderate exercise. The physician-administered subcutaneous injection resulted in transient stinging at the site of injection in many subjects; administration using the auto-injector was better tolerated.
Fowler
P A
PA
Glaxo Group Research Ltd, Greenford, Middlesex, UK.
Lacey
L F
LF
Thomas
M
M
Keene
O N
ON
Tanner
R J
RJ
Baber
N S
NS
D000368:Aged; D000369:Aged, 80 and over; D001682:Biological Availability; D004334:Drug Administration Schedule; D004347:Drug Interactions; D005260:Female; D006207:Half-Life; D006801:Humans; D007211:Indoles / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D008297:Male; D008881:Migraine Disorders / Q000188:drug therapy*; D012016:Reference Values; D019966:Substance-Related Disorders / Q000209:etiology; D013449:Sulfonamides / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D018170:Sumatriptan; D014662:Vasoconstrictor Agents / Q000493:pharmacokinetics / Q000494:pharmacology*
D007211:Indoles; D013449:Sulfonamides; D014662:Vasoconstrictor Agents; D018170:Sumatriptan