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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1989-2-17
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pubmed:abstractText |
The pharmacokinetics and bioavailability of ergoloid mesylates following single administrations of various dose levels (3-9 mg), dosage forms (oral swallow and sublingual tablets, solution) and under different dosing conditions (fasted, with meal) were studied in young healthy volunteers. Male and female subjects showed a similar rate and extent of bioavailable ergoloid after drug treatment. The absorption of ergoloid using either the tablet dosage forms or the drug administered as a solution was rapid, with peak levels of about 60-80 pg ml-1 mg-1 dose achieved after 0.6 to 1.3 h. The elimination half-life for ergoloid in plasma was 2-5 h. Administration of drug with food had no effect on the extent of absorption (AUC) but lowered the absorption rate. This resulted in a reduction of (by 25 per cent) and delay in (by 1 h) achieving peak levels (Cmax). Increasing the ergoloid dose caused a proportional increase in the AUC, but a smaller than proportional increase for Cmax. The tablet formulations provided similar AUCs as the solution; the objective of the sublingual tablet formulation to provide improved bioavailability over the swallow tablet via circumvention of first-pass metabolism was therefore not realized. Transient decreases in blood pressure after ergoloid treatment paralleled the plasma level profiles. Higher ergoloid levels were paired with the larger pressure decreases.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:issn |
0142-2782
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
9
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
349-61
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:3207855-Administration, Oral,
pubmed-meshheading:3207855-Administration, Sublingual,
pubmed-meshheading:3207855-Adolescent,
pubmed-meshheading:3207855-Adult,
pubmed-meshheading:3207855-Biological Availability,
pubmed-meshheading:3207855-Blood Pressure,
pubmed-meshheading:3207855-Ergot Alkaloids,
pubmed-meshheading:3207855-Female,
pubmed-meshheading:3207855-Food,
pubmed-meshheading:3207855-Humans,
pubmed-meshheading:3207855-Male,
pubmed-meshheading:3207855-Middle Aged,
pubmed-meshheading:3207855-Posture,
pubmed-meshheading:3207855-Radioimmunoassay
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pubmed:articleTitle |
Pharmacokinetics and bioavailability of ergoloid mesylates.
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pubmed:affiliation |
Drug Safety and Metabolism Division, Sandoz Research Institute, East Hanover, New Jersey 07936.
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pubmed:publicationType |
Journal Article,
Clinical Trial,
Controlled Clinical Trial
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