Graphic representation of pharmacology: Development of an alternative model
| Autor: | Saklad, Stephen R. |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
receptor binding Pimavanserin Pharmacology haloperidol chemistry.chemical_compound 0302 clinical medicine pimavanserin Pharmacology (medical) General Pharmacology Toxicology and Pharmaceutics Receptor Updates in Drug Therapy chlorpromazine Original Research clozapine graphic comparison fluphenazine serotonin Dissociation constant iloperidone Neuropsychology and Physiological Psychology dopamine paliperidone Agonist medicine.drug_class cariprazine olanzapine ziprasidone molindone Partial agonist norepinephrine 03 medical and health sciences aripiprazole medicine Inverse agonist Binding site Ion channel brexpiprazole risperidone model psychotropics quetiapine perphenazine histamine lurasidone antipsychotics loxapine 030104 developmental biology asenapine chemistry functional activity Neurology (clinical) pharmacology 030217 neurology & neurosurgery |
| Zdroj: | The Mental Health Clinician |
| ISSN: | 2168-9709 |
| DOI: | 10.9740/mhc.2017.09.201 |
| Popis: | Introduction:Providing clinicians with an easy to grasp and understandable representation of pharmacology is important to allow optimal clinical decisions to be made. Two of the most clinically relevant dimensions are receptor binding affinity and functional activity. The binding affinity for an agonist is described by the dissociation constant (KA), and an antagonist by the inhibition constant (Ki). Functionally, medications can act as superagonists, agonists, partial agonists, antagonists, partial inverse agonists, or inverse agonists at several receptor sites, transporters, or ion channels. Comprehending the differences between agents is complicated by the number and types of binding sites.Methods:Binding and functional data are obtained from primary literature, product labels, human cloned receptor binding, and other sources. Binding affinities are converted into ratios relative to the putative primary receptor for that category of agent. Antipsychotic binding is referenced to dopamine type 2 long (D2L) receptor binding. Binding affinity ratios (BARs) generate a 6-spoked diagram, with D2L as the hub. The most avidly bound sites are the spokes, and the disk diameter represents the BAR. Where functional data are available, they are shown as a pie chart shading the binding site's disk.Results:Binding and function diagrams are shown for the antipsychotics where binding data are available and are compared to previous methods of pharmacologic comparisons of antipsychotics.Discussion:Use of graphic models of psychotropic pharmacology improves clinician comprehension and may serve as an aid to improve rational therapeutics and patient outcomes. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|