Katzung Pharmacology Chapter 2

Regulatory proteins
Best-characterized and most receptors, mediate endogenous chemical signals

Targeted for inhibition

Transport proteins
Na+/K+ ATPase receptor for cardiovascular digitalis glycosides

Structural proteins
Tubulin, receptor for colchicine (anti-inflammatory)

Direct proportion
Relation between drug concentration and drug effect

Inverse proportion
Relation between dose and response increment

Direct proportion
Relation between drug concentration and receptor bound drug

Receptor-bound drug max
Total concentration of receptor sites

Spare receptors
Maximal biologic response is observed at a concentration of agonist that does not result in occupancy of available receptors

Degree of spareness
Total number of receptors vs. number needed to elicit maximum biological response

Competitive antagonist
Progressively inhibit the agonist response but reversible

Irreversible antagonist
Formation of covalent bonds where receptor is no longer available

Allosteric modulators
Antagonists that function noncompetitively and bind on site separate from the agonist binding site

Chemical antagonist
Drug that ionically binds to another drug making it unavailable

Physiologic antagonist
Between endogenous regulatory pathways

Glucocorticoid hormone
Lead to increased blood sugar

Regulates blood sugar

Full agonist
Produce maximun response

Partial agonist
Produce lower response and may act as antagonist to full agonists

Concentration or dose of a drug required to produce 50% maximal effect

Affinity and efficiency
Potency depends on these

Maximal efficacy
Degree at which drug is able to produce its effect

Clinical effectiveness
This depends on maximal efficacy rather than potency

Quantal dose effect
Dose of drug required to produce a specified effect

Median effect dose
Dose at which 50% of individuals exhibit specified quantal effect

Median toxic dose
Dose required to produce toxic effect in 50% of animals

Therapeutic index
Relation between desired effect and undesired effect

Therapeutic index
Ratio of TD50 and ED50

Individual respond differently to same drug at different times during treatment

Increased effect of drug on individual compared to most people

Diminished effect of drug on individual compared to most people

Decreased responsiveness due to continued drug administration

Rapid decrease in response after drug administration

Drug availability
Patient differ in drug distribution

Drug that increases or decreases blood pressure

Compensatory mechanisms
These may make patient respond and oppose the beneficial effects of the drug

Therapeutic effects of a drug

Adverse effects or side effects of a drug

systemic dose relationship has two components: Dose – Plasma concentration relationship -Determined by pharmacokinetics parameters of drug (half life, clearance, volume of distribution) Plasma Concentration – Response relationship -Can be studied using in vitro studies How to Determine a Dose- …

EC50 the drug concentration giving 50% maximal effect (not binding affinity – the magnitude of a drug effect is not proportional to the proportion of receptors occupied by that drug) a drug with a lower EC50 is more potent (half …

What does it mean that DR interactions are concentration dependent? It means that as the concentration of the drug increases the % of receptors bound increases What does it mean the DR interactions are saturable? At a certain concentration 100% …

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1. A drug, given as a 100-mg single dose, results in a peak plasma concentration of 20 μg/mL. The apparent volume of distribution is (assume a rapid distribution and negligible elimination prior to measuring the peak plasma level): A. 0.5 …

agonist a drug that activates a receptor by binding to that receptor antagonist a drug that binds to the receptor without activating the receptor WE WILL WRITE A CUSTOM ESSAY SAMPLE ON ANY TOPIC SPECIFICALLY FOR YOU FOR ONLY $13.90/PAGE …

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