Ceiling effect (pharmacology)
In pharmacology, the ceiling effect ( saturation effect ) is the property of some active ingredients that, despite an increase in dose, there is no increase in the effects; that is, the dose-response curve reaches a maximum before the maximum effect of an active ingredient ( efficacy ) is reached. In contrast to the ceiling effect , the pharmacological ceiling effect does not depend on the upper detection limit of the measurement method, but on the dose-effect curve. Side effects that are not biochemically related to the effect underlying a ceiling effect, however, may increase further. Ceiling effects can be observed particularly with partial agonists and allosteric modulators . The ceiling effect is e.g. B. for the opioid analgesic buprenorphine , a partial agonist, described, whereas it does not occur with other opioids such as fentanyl .
The ceiling effect should not be confused with tolerance or tachyphylaxis , which only occur with regular administration.
See also
Rebound phenomenon (kickback)
literature
- Christopoulos A, Kenakin T: G protein-coupled receptor allosterism and complexing . In: Pharmacol Rev . 54, No. 2, June 2002, pp. 323-74. PMID 12037145 .
- General and special pharmacology and toxicology , 7th edition, Spektrum Verlag, 1998, ISBN 3-8274-0088-0
Individual evidence
- ^ DJ Goldstein, JH Meador-Woodruff: Opiate receptors: opioid agonist-antagonist effects . In: Pharmacotherapy . 11, No. 2, 1991, pp. 164-7. PMID 1646994 .