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Some fundamental points concerning the clinical aspects of desensitization
Abstract:
Continued exposure of target cells to a hormonal agonist frequently leads to a blunted response to that agonist. This process has been termed desensitization, refractoriness, tolerance or tachyphylaxis. The receptor involved in case of beta-sympathomimetics is the beta-adrenergic receptor. When the clinical aspects of beta-adrenergic receptor desensitization are considered, a number of points need serious attention: 1) the route of administration of the drug and the concentration of the drug reached at the receptor site; 2) other factors which may cause reduced responsiveness of the beta-adrenergic receptor besides beta-sympathomimetics and interfere with this process; 3) the different cell-types which are studied and thought to be representative for processes taking place at lung tissue level; 4) the in vivo parameter(s) chosen to describe desensitization; 5) the difference between normal and asthmatic subjects; 6) the mechanism behind desensitization. The paper concerns a review of these points. Since the clinical findings with respect to the induction of desensitization by beta-sympathomimetics are rather controversial, the therapeutic advice should be: use it with caution.
Insights
Beta-adrenergic receptor desensitization can blunt drug response. This review examines factors influencing desensitization, including drug administration and cell type, advising cautious use of beta-sympathomimetics.
Area of Science:
- Pharmacology
- Cellular Biology
- Respiratory Medicine
Background:
- Hormonal agonists can cause target cells to become less responsive over time, a process known as desensitization.
- Beta-adrenergic receptors are key mediators in the response to beta-sympathomimetic drugs.
- Understanding beta-adrenergic receptor desensitization is crucial for effective therapeutic strategies, particularly in respiratory conditions.
Purpose of the Study:
- To review critical factors influencing beta-adrenergic receptor desensitization.
- To analyze the clinical implications and controversies surrounding beta-sympathomimetic drug use.
- To provide a comprehensive overview of desensitization mechanisms and their impact.
Main Methods:
- Literature review focusing on beta-adrenergic receptor desensitization.
- Analysis of factors such as drug administration route, concentration, and interfering agents.
- Examination of different cell types and in vivo parameters used in desensitization studies.
- Comparison of desensitization in normal versus asthmatic subjects.
Main Results:
- Beta-adrenergic receptor desensitization is a complex process influenced by multiple factors.
- Clinical findings regarding beta-sympathomimetic-induced desensitization are often contradictory.
- Variations in cell types and experimental parameters contribute to the controversy.
Conclusions:
- The clinical use of beta-sympathomimetics requires careful consideration due to potential desensitization.
- Further research is needed to clarify the mechanisms and clinical relevance of beta-adrenergic receptor desensitization.
- Therapeutic recommendations emphasize cautious application of these drugs.