By Bertram Katzung, Anthony Trevor
Equipped to mirror the syllabi in lots of pharmacology classes and in built-in curricula, easy & medical Pharmacology, 12e covers the real techniques scholars want to know in regards to the technological know-how of pharmacology and its software to scientific perform. number of the subject material and order of its presentation are in line with the authors’ a long time event in educating this fabric to millions of clinical, pharmacy, dental, podiatry, nursing, and different well-being technological know-how scholars.
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STAT dimers then travel to the nucleus, where they regulate transcription. relevant ion and thereby altering the electrical potential across the membrane. For example, acetylcholine causes the opening of the ion channel in the nicotinic acetylcholine receptor (nAChR), + which allows Na to flow down its concentration gradient into cells, producing a localized excitatory postsynaptic potential—a depolarization. The nAChR is one of the best characterized of all cell-surface receptors for hormones or neurotransmitters (Figure 2–9).
If C′ is twice C, for example, then [I] = Ki. For the clinician, this mathematical relation has two important therapeutic implications: 1. The degree of inhibition produced by a competitive antagonist depends on the concentration of antagonist. The competitive β-adrenoceptor antagonist propranolol provides a useful example. Patients receiving a fixed dose of this drug exhibit a wide range of plasma concentrations, owing to differences among individuals in clearance of propranolol. As a result, inhibitory effects on physiologic responses to norepinephrine and epinephrine (endogenous adrenergic receptor agonists) may vary widely, and the dose of propranolol must be adjusted accordingly.
Coupling efficiency is also determined by the biochemical events that transduce receptor occupancy into cellular response. Sometimes the biologic effect of the drug is linearly related to the number of receptors bound. This is often true for drug-regulated ion channels, eg, in which the ion current produced by the drug is directly proportional to the number of receptors (ion channels) bound. In other cases, the biologic response is a more complex function of drug binding to receptors. This is often true for receptors linked to enzymatic signal transduction cascades, eg, in which the biologic response often increases disproportionately to the number of receptors occupied by drug.
Basic & Clinical Pharmacology by Bertram Katzung, Anthony Trevor