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MCBD > ANS Drugs > Flashcards

ANS Drugs Flashcards

1
Q

Botulinum toxin - mechanism

A

Blocks ACh release by cleaving SNARE proteins required for neurotransmitter release.

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2
Q

Botulinum toxin - Theraputic uses

A

long-term neuromuscular blockade for pts with blepharospam, strabismus, facial wrinkles, other issues related to spasm.

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3
Q

Botulinum action at target organs of parasympathetic NS

A

blocks cholinergic transmission – Tx of urinary incontinence.

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4
Q

Botulinum action at target organs of sympathetic NS

A

blocks cholinergic neurons that innervate sweat glands – blocks excessive sweating when administered in axilla.

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5
Q

Competitive blockers

A

competitive antagonists: inhibits the binding of ACh to the nAChR, blocking transmission

Prototype: tubocurarine

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6
Q

Succinylcholine mechanism

A

depolarizing blocker, partial agonist of nAChR - initially depolarizes endplate, causing muscle twitching, which interferes with nerve-evoked muscle contraction.

Persistent binding = desensitization of receptor to cholinergic agonists.

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7
Q

Succinylcholine uses

A

muscle relaxant/paralytic used during surgery/procedures

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8
Q

Succinylcholine side-effects/toxicity

A

can affect autonomic ganglia - arrhythmias, BP changes

can cause histamine release - bronchial spasm and hypotension

malignant hyperthermia

Toxic effects: overdose = cardiopulmonary failure d/t neuromuscular blockage, ganglion block, and histamine release

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9
Q

Acetylcholine - what receptors, what uses?

A

Agonist at both nicotinic and muscarinic receptors

causes meiosis (constriction of pupil) - used in extraction of cataracts

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10
Q

Methacholine - what is it, why is it different from ACh?

A

muscarinic agonist

choline ester of acetylcholine

more resistant to hydrolysis by acetylcholinesterase and plasma cholinesterase

very little nicotinic activity

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11
Q

Methacholine uses

A

diagnostic tool in its with asthma to determine airway hyperactivity - inhalation causes bronchoconstriction

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12
Q

Possible side-effects of non-subtype selective muscarinic receptors acetylcholine and methacholine?

A

hypotension - via vasodilation via mAChR on endothelial cells of vessels

bradycardia - via mAChR on heart

tachycardia - via hypotension-produced reflex increase in sympathetic tone

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13
Q

Cevimeline mechanism & use

A

M3 selective muscarinic agonist

used to treat dry mouth in pts with Sjogren’s syndrome

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14
Q

Atropine mechanism, uses, and side-effects

A

non-selective, competitive muscarinic antagonist for AChR

Blocks parasympathetic (rest and digest) stimulation at effector organs - affects many organs

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15
Q

Darifenacin

A

M3-selective antagonist that treats overactive bladder

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16
Q

AChE inhibitors

A

inhibit acetylcholinesterase (AChE), which hydrolyses ACH.

Increase lifetime of ACh and transmission of ACh signals

17
Q

Edrophonium

A

Non-covalent reversible AChE inhibitor.

competitive enzyme inhibitor.

used in cardiac arrhythmias and in the diagnosis of myasthenia gravis (induces transient increase in strength.)

eliminated by kidneys rapidly - short duration of action

18
Q

Pyridostigmine

A

covalent, slowly reversible AChE inhibitor.

Tx of Myasthenia Gravis - increases efficiency of NMJ by increasing ACh availability

19
Q

Donepezil

A

noncompetitive AChE inhibitor

improves cognition/delays progression of Alzheimers

20
Q

What are the naturally occurring catecholamines?

A

Epinephrine, norepinephrine, and dopamine

21
Q

What is the main pathway for adrenergic for stopping adrenergic transmission?

A

Reuptake of norepinephrine back into the nerve terminal, metabolism by monoamine oxidase (MAO), extraneuronal catelchol-o-methytransferase (COMT)

22
Q

Cocaine mechanism

A

Blocks the reuptake of catecholamines into the nerve terminal

23
Q

Ephedrine

A

Mixed-acting (stimulates alpha and beta receptors) sympathomimetic (causes release of norepinephrine) and is an agonist for adrenergic receptors. Used to prevent hypotension during spinal anesthesia.

24
Q

Indirect-acting sympathomometics

A

Act on the noradrenergic nerve terminal to cause release of norepinephrine – sympathetic effect.

25
Q

Methyldopa

A

False transmitter (can be released in reponse to neuron stimulation). Stored in vesicles in adrenergic terminals

26
Q

Alpha adrenergic versus beta-adrenergic responses

A

In alpha-adrenergic responses: potency EPI > NE&raquo_space; ISO (isoprotenerol)

In beta-adrenergic responses: potency ISO > EPI > NE

27
Q

Isoproterenol

A

High specificity for all 3 beta-receptors
Relaxes skeletal muscle vascular beds, decreasing blood pressure.
Also increases heartrate and cardiac output d/t decrease in peripheral resistance.

28
Q

Dopamine

A

Activates vasodilatory dopamine receptors in mesenteric and renal vessels.

29
Q

Phenylephrine

A

synthetic amine

stimulates alpha 1 adrenergic receptors & very little beta-receptor activity

increases blood pressure and peripheral resistance

decreases heart rate due to baroreceptor reflex

30
Q

Midodrine

A

alpha 1 adrenergic agonist

prodrug - metabolically converted to the active form

increases blood pressure in pts with autonomic insufficiency and hypotension

31
Q

Clonidine

A

selective alpha2 adrenergic agonist

Tx of hypertension

decreases BP by acting on a2 receptors in the CNS to decrease sympathetic outflow

32
Q

Dobutamine

A

beta1 selective adrenergic agonist

increases cardiac output in conditions such as heart failure

33
Q

Albuterol

A

Beta2 selective adrenergic agonists

bronchodilator - relaxes bronchial and other smooth muscle with little cardiac stimulation

34
Q

Metoprolol

A

Beta1-selective agonist

Inhibits cardiac effects of sympathetic activity or adrenergic drugs - fewer effects on other organs

35
Q

Propanolol

A

Non-selective beta blocker

Blocks all 3 beta receptors, decrease HR, cardiac output, BP. Can also block other beta-mediated effects

36
Q

Uses for beta blockers

A

HTN
Angina
Cardiac arrhythmias
Glaucoma

37
Q

Toxic effects of beta-blockers

A

Blockage of beta2 receptors causes bronchoconstriction in pts with respiratory system disorders
Bradycardia and hypotension – cold extremities and claudication from blocking beta2 receptors in skeletal muscle vasculature
Delay recovery from insulin-induced hypoglycemia in diabetics

38
Q

Carvedilol

A

Combined adrenergic alpha and beta blocker

HTN and CHF Tx

MCBD (45 decks)

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