Back to Search
Start Over
Comparison of vasodilatory responses to nitroglycerin and its dinitrate metabolites in human veins
- Source :
- Clinical pharmacology and therapeutics. 52(6)
- Publication Year :
- 1992
-
Abstract
- Independent of the route of nitroglycerin administration, substantial amounts of 1,2-glyceryl dinitrate (1,2-GDN) and 1,3-glyceryl dinitrate (1,3-GDN) metabolites accumulate in humans. Thus far their pharmacologic activity in comparison to nitroglycerin in humans is unknown. To compare the venodilatory potency of nitroglycerin and of 1,2-GDN and 1,3-GDN in vivo, cumulative dose-response curves were established in nine healthy volunteers by use of the dorsal hand vein compliance technique. Separated by a washout period, two of the three venodilators were infused in randomized order after preconstriction with phenylephrine. Values for maximum vasodilation were similar for all compounds: nitroglycerin, 109%; 1,2-GDN, 100%; and 1,3-GDN, 106%. The respective values for the dose rate exerting 50% of maximum vasodilation were 5.1, 43, and 60 ng/min, indicating that the dinitrates were about 10 times less potent than nitroglycerin (p < 0.001) but not significantly different from each other. The findings support the hypothesis that activity of nitroglycerin metabolites is related to the number of nitrate groups in the molecule and are in agreement with lower dinitrate potencies found in animal experiments.
- Subjects :
- Adult
Male
Metabolite
Vasodilator Agents
Vasodilation
Pharmacology
Veins
chemistry.chemical_compound
Nitroglycerin
Random Allocation
In vivo
Reference Values
medicine
Potency
Humans
Pharmacology (medical)
Phenylephrine
Dose-Response Relationship, Drug
business.industry
Hand
Dose–response relationship
chemistry
Anesthesia
Circulatory system
cardiovascular system
Regression Analysis
Female
business
circulatory and respiratory physiology
medicine.drug
Subjects
Details
- ISSN :
- 00099236
- Volume :
- 52
- Issue :
- 6
- Database :
- OpenAIRE
- Journal :
- Clinical pharmacology and therapeutics
- Accession number :
- edsair.doi.dedup.....36d48598dc941b231f085bfb2327299d