AND ANSWERS WITH COMPLETE SOLUTIONS VERIFIED
LATEST UPDATE 2024/2025
Drug
An exogenous chemical administered to alter biological/physiological process to cure/treat/prevent
disease/illness
Dissociation Constant (Kd)
The smaller the numerical value the greater the affinity a drug has for a given receptor/drug target
Transporters
Moves substances into a cell
Pumps
Moves substances out of a cell
Ion-Channels (and the two different types)
Selective transmembrane proteins with 2 types of gating mechanisms: Ligand-Gated OR Voltage-Gated
Intracellular Ion at resting membrane potential
K+
,Extracellular Ions at resting membrane potential
Na+/Ca++/Cl-
4 Main types of receptors
1. Ion-Channels
2. G-Protein Coupled Receptors (GPCR's)
3. Nuclear Hormone Receptor (NOT on cell surface but rather inside cell and response usually involves
DNA transcription
4. Receptor Tyrosine Kinase (Phosphorylation of Tyrosine amino acid)
GPCR's (3 types, subunits, effectors and second messengers)
Gs and Gq = Stimulatory whereas Gi = inhibitory
Alpha, Beta, Gamma subunits, Alpha dissociates after receptor activation to affect adenylyl cyclase (will
increase cAMP) or phospholipase C which is an enzyme that degrades phospholipid into DAG (activates
protein kinase C) and IP3 (open Ca++ ligand gated channel to increase Ca++ influx causing smooth
muscle contraction)
4 types of "Agonists" to form stable receptor-complex conformation
1. Full Agonist (selective exclusively for active receptor)
2. Partial Agonist (mostly selective for active receptors)
3. Neutral Agonist (Similar affinity for active/inactive receptor conformations) "Clinical Antagonist"
4. Inverse Agonist (Selective exclusively for inactive receptor) "Clinical Antagonist"
Graded Response dose response curve
Numerical value outcomes --> HR/BP/etc
,Quantal Response dose response curve
Yes/No outcomes --> Did pt fall asleep/get pregnant?
Explain dose response curve
Emax --> Max effect of a drug (where graph plateaus) (measure of efficacy/response)
ED50 --> Dose required for 50% of max response (measure of potency)
X-Axis(mg of drug) --> measure of a drugs potency (ED50) (Ex: If 2 drugs get to 100%, they are equally
effective)
Y-Axis (% response) --> measure of a drugs efficacy (Emax) (Ex: If 2 drugs have same ED50, they're
equally potent)
Additive Effect
Coadministration of two active agents will produce a response equal to the sum of each drug if given
separately
Synergistic Effect
Coadministration of two active drugs yield a greater response than if each drug was given individually
Potentiation
Coadministration of 1 active and 1 inactive drug yields an increased effect than the active drug alone
Competitive Antagonist
-A drug that competes with agonist for REVERSIBLE binding at the receptor active site.
-DOES NOT change the Emax (effectiveness of drug)
-DOES SHIFT ED50 to the RIGHT (appear less potent)
Noncompetitive Antagonist
, -IRREVERSIBLY bound to receptor
-DOES NOT change the ED50
-DOES REDUCE Emax ( appear less effectiveness)
Affinity
How well a ligand binds to a protein/receptor. Positive correlation between affinity and potency
Selectivity
How well a drug binds to its intended target. Ideally should have greater affinity for target receptor than
other receptors
Side effect
ANY effect other than the therapeutic effect regardless if it was beneficial or detrimental
Adverse effect (and 2 types)
a side effect that is harmful
1. Mechanism based: activation of the same receptor target elsewhere in the body (ex: Albuterol
stimulates Beta receptor in lung = bronchodilation, but it can also stimulate Beta receptor in heart which
increases HR)
2. Off-Target: Result of drug binding to something (receptor) other than intended target (ex: Diazoxide is
a direct vasodilator that can open K+ channels in pancreas to induce the release of insulin)
Toxic effect
Extension of pharmacological effect due to high dosing of a drug
Hypersensitivity/allergic effects
Invokes an immune response