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Nervous System I > Pharmacology > Flashcards

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
Q

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

A 
Treatment of antimuscarinic drug intoxication (AChE inhibitors) 
Smoking cessation (nicotine) 
Alzheimer's disease (AChE inhibitors)
26
Q

Parasympathetic Agonists - Muscarinic receptor adverse effects (direct/indirect)

A

SLUDGE = salivation, lacrimation, urination, diarrhea, GI upset, emesis
+ Crampy abdominal pain, bronchial constriction, hypotension / shock

27
Q

Parasympathetic Agonists - Nicotinic receptor adverse effects

A

Convulsions, hypertension, arrhythmias

Effects mediated by nicotinic ganglia and NMJ receptors

28
Q

Parasympathetic agonists - antidotes to OD

A

Atropine - blocks excessive muscarinic receptor stimulation

Pralidoxime - hydrolyzes the AChE/organophosphate complex, regenerating the inactivated cholinesterase

29
Q

Alpha latrotoxin

A

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
Q

Effects of nicotine - Peripheral

A

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
Q

Lidocaine

A

Blocks voltage-sensitive Na channels in the pre-synaptic axon terminal; blocks pre-synaptic action potentials

32
Q

How does Mg2+ (sulfate) affect nerve transmission at the NMJ?

A

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
Q

Depolarization Blockade

A

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
Q

Mechanism of organophosphate nerve gasses

A

Permanent acetylcholinesterase inhibitors; massive flood of ACh causes depolarization blockade of the post-synaptic muscle, causing flaccid paralysis

35
Q

Dantrolene sodium

A

Competitive inhibitor of the RyR Ca2+ release channel; used in the treatment of malignant hyperthermia

36
Q

Nondepolarizing (competitive) NMJ blocking agents - 3 examples

A

Curare
Atracurium
Rocuronium

Side effects: Histamine release (vasodilation), effects on muscarinic receptors (tachycardia)

37
Q

Mechanism and effects of succinylcholine

A

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
Q

Succinylcholine - Side effects

A

Muscle pain
Hyperkalemia
Increased IOP

39
Q

Pralidoxime

A

Nerve gas poisoning antidote; cleaves the bond between AChE and the organophosphate inhibitor molecule, regenerating functional AChE enzyme

40
Q

Therapeutic uses of NMJ blockers

A

Surgical paralysis during general anesthesia
Management of ventilator patients
Attenuate peripheral convulsions associated with ECT

41
Q

Curare poisoning - how do you treat it?

A

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
Q

Doxazosin

A

alpha-1 antagonist

43
Q

Labetaolol/Carvedilol

A

alpha-1, Beta-1, Beta-2 antagonist

44
Q

How does sympathetic stimulation affect vessels in the skin vs. skeletal muscle?

A

alpha-1 activation causes vasoconstriction of superficial vessels

beta-2 activation causes vasodilation of skeletal muscle vasculature

45
Q

Phenylephrine

A

alpha-1 agonist

46
Q

Dobutamine

A

B1 agonist

47
Q

Isoproterenol

A

B1 and B2 agonist

48
Q

Clonidine

A

alpha 2 agonist

Nervous System I (10 decks)

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