Pharmacology Flashcards

1
Q

Effects of parasympathetic stimulation - Cardiac

A

Decreased heart rate and AV conduction rate

Decreased contractility

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2
Q

Effects of parasympathetic stimulation* - Vascular

A

Vasodilation

*Vessels do not receive parasympathetic innervation; muscarinic ACh channels may be activated by ACh agonists

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3
Q

Effects of parasympathetic stimulation - Respiratory

A

Bronchoconstriction

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4
Q

Effects of parasympathetic stimulation - GI

A

Increased secretory and motor activity; relaxation of sphincters

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5
Q

Efffects of parasympathetic stimulation - GU

A

Relaxation of sphincters

Promotion of voiding (urination, defecation)

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6
Q

Effects of alpha 1 sympathetic stimulation - vasculature

A

Vasoconstriction of cutaneous and splanchnic vasculature - diverts blood from these areas

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7
Q

Effects of alpha 1 sympathetic stimulation - GU

A

Contraction of uretal sphincters, bladder and prostate; promotes continence
Ejaculation

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8
Q

Effects of Beta 1 sympathetic stimulation - Heart

A

Increased heart rate (positive chronotropy)
Increased conduction velocity at AV node
Increased contractility (positive inotropy)

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9
Q

Effects of B1 sympathetic stimulation - Kidney

A

Increased renin release causing elevation of BP

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10
Q

Effects of B2 sympathetic stimulation - Vasculature

A

Vasodilation of skeletal muscle vessels - shunts blood toward skeletal muscle

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11
Q

Effects of B2 sympathetic stimulation - Respiratory

A

Bronchodilation

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12
Q

Effects of B2 sympathetic stimulation - Eye

A

Increased aqueous humor production causing increased intraocular pressure

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13
Q

Effects of B2 sympathetic stimulation - GU

A

Uterine smooth muscle relaxation

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14
Q

Bethanechol - Mechanism

A

Parasympathetic agonist; synthetic analog of ACh

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15
Q

Atropine - Mechanism

A

Reversible, competitive inhibitor of ACh at muscarinic receptors

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16
Q

Edrophonium - Mechanism & Pharmacokinetics

A

Reversible, short acting inhibitor of acetylcholine esterase; indirect muscarinic agonist

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17
Q

Neostigmine - Mechanism & Pharmacokinetics

A

Reversible, intermediate to long acting inhibitor of acetylcholine esterase; indirect muscarinic agonist

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18
Q

Prazosin - Mechanism

A

Selective A1 antagonist

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19
Q

Propanolol - Mechanism

A

Nonselective B1 and B2 antagonist

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20
Q

Metoprolol / Atenolol - Mechanism

A

Selective B1 antagonist

21
Q

Pilocarpine - Mechanism, Pharmacokinetics, Uses

A

Direct parasympathetic agonist; enters CNS

22
Q

Bethanechol - Mechanism & Pharmacokinetics

A

Direct parasympathetic agonist; does not enter CNS

23
Q

Therapeutic uses of parasympathetic agonists (direct/indirect) - ANS

A

Glaucoma - pilocarpine (topical)

Urinary retention / paralytic ileus (bethanechol, neostigmine)

Xerostomia (pilocarpine)

24
Q

Therapeutic uses of parasympathetic agonists (direct/indirect) - NMJ

A

Myasthenia gravis - edrophonium, neostigmine

25
Therapeutic uses of parasympathetic agonists (direct/indirect) - CNS
``` Treatment of antimuscarinic drug intoxication (AChE inhibitors) Smoking cessation (nicotine) Alzheimer's disease (AChE inhibitors) ```
26
Parasympathetic Agonists - Muscarinic receptor adverse effects (direct/indirect)
SLUDGE = salivation, lacrimation, urination, diarrhea, GI upset, emesis + Crampy abdominal pain, bronchial constriction, hypotension / shock
27
Parasympathetic Agonists - Nicotinic receptor adverse effects
Convulsions, hypertension, arrhythmias Effects mediated by nicotinic ganglia and NMJ receptors
28
Parasympathetic agonists - antidotes to OD
Atropine - blocks excessive muscarinic receptor stimulation Pralidoxime - hydrolyzes the AChE/organophosphate complex, regenerating the inactivated cholinesterase
29
Alpha latrotoxin
i.e. Black widow spider venom Forms pores in the axon terminal membrane, allowing excessive Ca2+ influx; causes explosive release of ACh leading to depolarization blockade
30
Effects of nicotine - Peripheral
Activate both PNS and SNS via stimulation of ganglionic nicotinic receptors At therapeutic doses (smoking), acts as an agonist - causes increased BP, HR, vasoconstriction via Epi released from adrenal gland Increased GI motility via ganglionic stimulation of parasympathetic system
31
Lidocaine
Blocks voltage-sensitive Na channels in the pre-synaptic axon terminal; blocks pre-synaptic action potentials
32
How does Mg2+ (sulfate) affect nerve transmission at the NMJ?
Calcium antagonist; diminishes muscle contraction Mg2+ blocks the voltage-sensitive Ca2+ channel, diminishing ACh release from the nerve terminal; this effect mimics the myesthenic syndrome
33
Depolarization Blockade
Prolonged binding of an ACh agonist at the post-synaptic nicotinic receptor causes an EPP that excites a muscle action potential via activation of VSSCs; however, prolonged depolarization prohibits repolarization of the cell and so VSSCs remain in their inactive state and cannot initiate subsequent action potentials
34
Mechanism of organophosphate nerve gasses
Permanent acetylcholinesterase inhibitors; massive flood of ACh causes depolarization blockade of the post-synaptic muscle, causing flaccid paralysis
35
Dantrolene sodium
Competitive inhibitor of the RyR Ca2+ release channel; used in the treatment of malignant hyperthermia
36
Nondepolarizing (competitive) NMJ blocking agents - 3 examples
Curare Atracurium Rocuronium Side effects: Histamine release (vasodilation), effects on muscarinic receptors (tachycardia)
37
Mechanism and effects of succinylcholine
Muscarinic agonist that is not recognized by AChE, allowing prolonged action at the receptor Initial stimulation of nicotinic receptors at NMJ associated with muscle fasciculations; prolonged depolarization prohibits repolarization of the muscle cell membrane, blocking EC coupling and leading to flaccid paralysis
38
Succinylcholine - Side effects
Muscle pain Hyperkalemia Increased IOP
39
Pralidoxime
Nerve gas poisoning antidote; cleaves the bond between AChE and the organophosphate inhibitor molecule, regenerating functional AChE enzyme
40
Therapeutic uses of NMJ blockers
Surgical paralysis during general anesthesia Management of ventilator patients Attenuate peripheral convulsions associated with ECT
41
Curare poisoning - how do you treat it?
Death caused by flaccid paralysis of respiratory muscles Edrophonium and neostigmine (AChEIs) can reverse poisoning by increasing synaptic ACh to out-compete the antagonist
42
Doxazosin
alpha-1 antagonist
43
Labetaolol/Carvedilol
alpha-1, Beta-1, Beta-2 antagonist
44
How does sympathetic stimulation affect vessels in the skin vs. skeletal muscle?
alpha-1 activation causes vasoconstriction of superficial vessels beta-2 activation causes vasodilation of skeletal muscle vasculature
45
Phenylephrine
alpha-1 agonist
46
Dobutamine
B1 agonist
47
Isoproterenol
B1 and B2 agonist
48
Clonidine
alpha 2 agonist