Rush NSG 531 Advanced Pharmacology Exam 2
Questions & Answers
Potency - ✔✔✔ - Dose of drug required to produce given effect; 50% of maximal response the drug is
capable of producing
Efficiacy - ✔✔✔ - Maximal response a drug is capable of producing
Ka - ✔✔✔ - Volume needed to get one mole of an unbound drug when 50% of target receptors are
occupied. L/mole
Kd - ✔✔✔ - Concentration of drug in the plasma when 50% of the target receptors are occupied. Mole/L
Non-competitive (irreversible) antagonist LDR curve - ✔✔✔ - Moves to the right and down
Competitive (reversible) antagonist LDR curve - ✔✔✔ - Moves to the right and parallel
Synthesis of NE - ✔✔✔ - Occurs at adrenergic neuron; Tyrosine to DOPA to dopamine to NE. Binds to
alpha and beta receptors. Degraded by COMT and MAO.
Bethanechol - ✔✔✔ - Muscarinic agonist prototype. Selective, binds to M3 receptors in the bladder and
causes bladder muscle contraction and sphincter relaxation.
Indicated for urinary retention in postop or pp pts.
AEs: salivation, lacrimation, bronchospasm, diarrhea, and bradycardia
Pilocarpine - ✔✔✔ - Muscarinic agonist for glaucoma. Causes ciliary muscle contraction.
, Atropine - ✔✔✔ - Muscarinic antagonist prototype. Nonselective competitive muscarinic antagonist.
Indicated for: bradycardia, pupil dilation (mydriasis) for eye exams, GI hypermotility
Contraindications: Glaucoma, urinary retention, tachycardia
AEs: Dry mouth, blurred vision, urinary retention, constipation, anhidrosis
Epinephrine binding affinity - ✔✔✔ - Binds to all four adrenoreceptors but has a greater affinity for beta
NE binding affinity - ✔✔✔ - Binds to alpha 1, alpha 2, and beta 1 but has greater affinity for alpha
Alpha 1 receptors - ✔✔✔ - Eyes: produce mydriasis
Blood vessels in skin, viscera, gut, kidney, brain: vasocontriction
GU: prostate contraction and ejaculation, smooth muscle contraction of internal urethral sphincter
Phenylephrine - ✔✔✔ - Alpha 1 receptor, prototypic agonist; used to induce mydriasis
Pseudoephedrine - ✔✔✔ - Alpha 1 receptor, prototypic agonist; nasal decongestant
Doxazosin (Cardura) - ✔✔✔ - Alpha 1 receptor prototypic antagonist; used to manage HTN
Tamsulosin (Flomax) - ✔✔✔ - Alpha 1 receptor prototypic antagonist; used to manage BPH
AE: orthostatic hypotension
Alpha 2 receptors - ✔✔✔ - Presynaptic nerve terminals: inhibit NT release
Blood vessels: vasoconstriction
Clonidine - ✔✔✔ - Alpha 2 receptor prototypic agonist
Antihypertensive: inhibits NE release by binding to presynaptic alpha 2 receptors, inhibits sympathetic
outflow in CNS (these are greater than vasoconstrictive effects)
Questions & Answers
Potency - ✔✔✔ - Dose of drug required to produce given effect; 50% of maximal response the drug is
capable of producing
Efficiacy - ✔✔✔ - Maximal response a drug is capable of producing
Ka - ✔✔✔ - Volume needed to get one mole of an unbound drug when 50% of target receptors are
occupied. L/mole
Kd - ✔✔✔ - Concentration of drug in the plasma when 50% of the target receptors are occupied. Mole/L
Non-competitive (irreversible) antagonist LDR curve - ✔✔✔ - Moves to the right and down
Competitive (reversible) antagonist LDR curve - ✔✔✔ - Moves to the right and parallel
Synthesis of NE - ✔✔✔ - Occurs at adrenergic neuron; Tyrosine to DOPA to dopamine to NE. Binds to
alpha and beta receptors. Degraded by COMT and MAO.
Bethanechol - ✔✔✔ - Muscarinic agonist prototype. Selective, binds to M3 receptors in the bladder and
causes bladder muscle contraction and sphincter relaxation.
Indicated for urinary retention in postop or pp pts.
AEs: salivation, lacrimation, bronchospasm, diarrhea, and bradycardia
Pilocarpine - ✔✔✔ - Muscarinic agonist for glaucoma. Causes ciliary muscle contraction.
, Atropine - ✔✔✔ - Muscarinic antagonist prototype. Nonselective competitive muscarinic antagonist.
Indicated for: bradycardia, pupil dilation (mydriasis) for eye exams, GI hypermotility
Contraindications: Glaucoma, urinary retention, tachycardia
AEs: Dry mouth, blurred vision, urinary retention, constipation, anhidrosis
Epinephrine binding affinity - ✔✔✔ - Binds to all four adrenoreceptors but has a greater affinity for beta
NE binding affinity - ✔✔✔ - Binds to alpha 1, alpha 2, and beta 1 but has greater affinity for alpha
Alpha 1 receptors - ✔✔✔ - Eyes: produce mydriasis
Blood vessels in skin, viscera, gut, kidney, brain: vasocontriction
GU: prostate contraction and ejaculation, smooth muscle contraction of internal urethral sphincter
Phenylephrine - ✔✔✔ - Alpha 1 receptor, prototypic agonist; used to induce mydriasis
Pseudoephedrine - ✔✔✔ - Alpha 1 receptor, prototypic agonist; nasal decongestant
Doxazosin (Cardura) - ✔✔✔ - Alpha 1 receptor prototypic antagonist; used to manage HTN
Tamsulosin (Flomax) - ✔✔✔ - Alpha 1 receptor prototypic antagonist; used to manage BPH
AE: orthostatic hypotension
Alpha 2 receptors - ✔✔✔ - Presynaptic nerve terminals: inhibit NT release
Blood vessels: vasoconstriction
Clonidine - ✔✔✔ - Alpha 2 receptor prototypic agonist
Antihypertensive: inhibits NE release by binding to presynaptic alpha 2 receptors, inhibits sympathetic
outflow in CNS (these are greater than vasoconstrictive effects)
