CRNA Pharmacology Study Guide
4 Types of receptors CORRECT ANSWER -G-protein coupled receptor: adrenergic, serotonin, dopamine, acetylcholine, dopamine,histamine, opiates
-Ligand Gated Ion Channel: Acetylcholine (nicotinic) NMDA, GABA competitive/noncompetitive /allosteric (NAM, PAM (benzos), allosteric modulator)
-Tyrosine Kinase Receptor: Dimers, Jac/stat, example is insulin
-Steroid Hormone receptors: steroids are transported in blood by corticosteroid binding protein to CYTOSOL. Activated by Estrogen, progesterone, glucocorticoids and regulate DNA transcription.
Selectivity CORRECT ANSWER Drugs will interact with different receptors to different degrees. The HIGHEST degree of selectivity resides in a drug that interacts with ONLY ONE sub-type.
Kinetic Analysis of Drug-Receptor Interactions:***** CORRECT ANSWER Kd of a drug is the concentration of drug that occupies 50% of receptor
Kd= equilibrium dissociation constant, binding affinity of drug to receptor. KEY for understanding drug receptor interactions
If a drug has a high affinity for receptor, low Kd
Determines SELECTIVITY for drug to specific receptors
Drug Ki ratios (same as Kd) CORRECT ANSWER higher the B2/B1 selectivity ratio above one, the more selective it will be for B2
under a value of 1, the drug will favor B1 Agonist receptor Interactions CORRECT ANSWER Binding of an agonist in a tissue can lead to a myriad of effects due to MULTIPLE receptor subtypes in tissues with opposing/additive/ independent effects.
Concentration Response Curve CORRECT ANSWER Response on Y axis, concentrationof drug on x axis.
EC 50: Effective concentration, 50% response
EC 50 is concentration of drug which produces the half maximal response; or POTENCY.
POTENCY refers to amount of drug DOSE ***** CORRECT ANSWER ED 50 measures drug potency at half maximal response
Smaller the ED50, the higher the potency
Leftward means the drug is more potent
Rightward: lower potency
Graded dose response curve: test on a SINGLE TEST SUBJECT
Maximal level of RESPONSE: EFFICACY***** CORRECT ANSWER maximal level of response achievable (highest ceiling)
Drugs can have the same potency, but efficacy can be different
Up and down: higher and lower efficacy!
Partial agonist will have a lower efficacy, but still creates a response
******A partial agonist will behave as a competitive antagonist to the full agonist (endogenous ligand)
Competitive antagonist ***** CORRECT ANSWER ex. Beta blockers Bind in reversible manner to agonist, shifts to the right, agonist becomes LESS potent (in terms of dose response curve)
**Competitive antagonist decreases agonist potency
This is the MOA of the antagonist, and the amount of agonist can be increased to overcome the effect.
HOWEVER, In a PERSON , the agonist response (efficacy) will be less.
Phenoxybenzamine CORRECT ANSWER an irreversible -adrenoceptor antagonist, is used to control the hypertension caused by catecholamines released from pheochromocytoma, a tumor of the adrenal medulla
Noncompetitive antagonist CORRECT ANSWER Irreversible binding to active site: Orthosteric site*
Same effect as a drug that binds and inhibits ALLOSTERICALLY:
In both cases, efficacy is lower.
Potency remains the same.
Graded dose-response curve CORRECT ANSWER shows relationship between drug dose and response between drugs, showing potency and efficacy
Curve determined for one individual/ situation!
Cumulative quantal LDR curve***** . CORRECT ANSWER All or none, did the drug work or not.
Axis: % of cumulative responders vs dose
Curve determined as an effect on a patient population!
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