Autonomic Drugs Flashcards by Kristen Bertrand

Class of edrophonium

Ache i - short acting (reversible)

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Class of pilocarpine

Muscarinic agonist

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Class of bethanechol

Muscarinic agonist

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Class of neostigmine

Ache i - intermediate acting (reversible)

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Class of pyridostigmine, physostigmine, donepezil

Ache i (reversible)
Used for Alzheimers
Intermediate acting

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class of echothiophate

Irreversible Ache i

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What are organophosphate insecticides

Ache i - non therapeutic

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Acetylcholinesterase inhibitors

MOA and uses

Increase ach, amplifies effects at cholinergic synapses, effects at nicotinic and muscarinic

Used to reverse NDMR blockade, MG, glaucoma, ileus, urinary retention, Alzheimer’s disease

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What toxicity is expected with AChE i’s?

Increased ach, so increase PSNS, so bradycardia, increased salivation, increase muscle tone/hyperexcitability, Bronchoconstriction
CNS - excitation (possible convulsion) followed by depression (unconsciousness)

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Ache i is not used to Reverse depolarizing blockade of succs, why?

Because sux is an agonist

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Ache i drug effects

Increased secretions, increased GI motility, Bronchoconstriction, bradycardia, hypotension, miosis, large dose = depolarizing block, MG - improves transmission, NDMR reversal

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what do we use edrophonium for?

Diagnosis of MG (to increase Ach, and increase transmission) - too short acting for therapeutic use

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What do we use physostigmine for?

Treatment of glaucoma to decrease intraocular pressure by increasing PSNS and decreasing pressure

Works postganglionic PSNS

Cross BBB

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What do we use pyridostigmine for?

Myasthenia Gravis to increase transmission at NMJ

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Cholinergic crisis S&S

D - diarrhea, diaphoresis
U - urination
M - miosis
B - bradycardia

B - bronchoconstriction
E - excitation of skeletal muscle and CNS
L - lacrimation
S - salivation
S - sweating

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What do you give as an antidote for cholinergic toxicity

Atropine = muscarinic blocker

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What are the muscarinic agonist drugs?

Acetylcholine, carbachol, methacholine, bethanechol Muscarine, pilocarpine, oxotremorine, cevimeline

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Muscarinic agonist drug effects

“Parasympathetomimetic”
CV = decrease HR, CO, and arterial blood pressure, vasodilation
GI = increased motility
Bladder = contracts
Lungs = bronchoconstriction
Increased secretions
Eye = miosis, accommodation for near vision, decreased intraocular pressure

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How do muscarinic agonists cause vasodilation in vsmc

They bind to M3 receptors on endothelial cells which secrete NO and cause vasodilation

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Where are the nicotinic acetylcholine receptors

NMJ, ganglia, CNS

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NicotinicN receptors do what?

Stimulation of post-ganglionic neuronal activity and CNS stimulation

= increased autonomic outflow

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NicotinicM receptors do what

Activation of skeletal muscle endplates leading to contraction

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What is the class of atropine

Muscarinic antagonist

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What is the class of glycopyrrolate

Muscarinic antagonist

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What is the class of scopolomine

Muscarinic antagonist

What is the class of hexamethonium

NicotinicN ganglionic blocker

What is the class of atracurium, cisatricurium, vecuronium, roc, and panc

NicotinicM blocker

Atropine uses

Crosses BBB, useful for bradycardia and as an adjunct to blockade reversal

Scopolamine uses

Cross BBB +++ | Used for motion sickness

Glycopyrrolate uses

Does not cross BBB Blockade reversal adjunct to help wiht muscarinic activities of neostigmine (aka prevents bradycardia) Short acting

Concerns with antimuscarinics

Hyperthermia, glaucoma, GU obstruction, prostatic hypertrophy, CV, GI ileus - further decreases motility

Medication classes with anticholinergic activities

Antihistamines, antispasmodics, antiparkinsonian, skeletal muscle relaxants, antipsychotics, antidepressants, antimuscarinics for urinary incontinence

NicotinicM antagonist effect

NDMRs

NicotinicN antagonist effects

Blocks ganglionic outflow

What is the class of norepinephrine?

Direct acting Nonselective Mixed alpha/beta agonist Alpha 1 and Beta 1 (little beta2)

What is the class of phenylephrine

Direct acting selective alpha1 agonist

What is the class of dexmeditominide

Direct acting alpha 2 agonist

What is the class of epinephrine

Direct acting mixed alpha/beta agonist, nonselective

What is the class of isoproterenol

Direct acting non-selective beta agonist

What is the class of dobutamine

Direct acting beta 1 agonist

What ist he class of albuterol

Direct acting beta 2 agonist

What is the class of ephedrine?

Indirect acting adrenergic agonist via NT release - can also act on receptors “Mixed” acting

How does cocaine work

NE Reuptake inhibition

What is the class of tranylcypromine and selegiline

MAOi which stops breakdown of NE and dopamine ``` Tranylcypromine = nonselective Selegiline = selective for MAO-b (dopamine) ```

What is the class of prazosin

Selective alpha 1 antagonist

What is the class of metoprolol and atenolol

Selective beta 1 antagonist

What is the class of clonidine

Selective alpha 2 agonist

What do amphetamines do

Displaces/releases stored catecholamine NT (NT releaser) | Inhibits catecholamine Reuptake

How does tyramine work

NT releaser of catecholamines | Found in food, not a drug - this is the food-drug interactions of MAOis

Dopamine receptor affinity

Low dose = dopa Med dose = beta High dose = alpha

What does alpha 1 do?

Vasoconstriction (skin and splanchnic) Mydriasis Smooth muscle contracts (except GI) GI/GU sphincter contract

What does alpha 2 do

Decrease NE release presynaptically CNS inhibit SNS outflow Platelet aggregation Pancreas = decrease insulin

What does beta 1 do?

Increase heart rate and contractility Renin release Trophic effect = hypertrophy

What does beta 2 do

``` Bronchodilator Vasodilation (skeletal muscle beds) Relaxes smooth muscle mostly Skeletal muscle contracts = tremor Relax GI/GU Relax uterine smooth muscle Glycogenolysis ```

What class is phenoxybenxamine

Nonselective alpha blocker

What class is phentolamine

Non selective alpha blocker

what class is prazosin

Alpha 1 blocker

What class is yohimbine

Alpha 2 blocker

What class is propanolol

Nonselective beta blocker

What class for metoprolol and esmolol

Beta 1 specific blocker

Why wouldn’t you use selective beta 2 blockers

Risk for bronchoconstriction

What type of innervation to the adrenal medulla, sweat glands, and blood vessels

SNS innervation only

What is the dominant tone in cardiac, bronchial smooth muscle, GI tract, salivary glands?

PSNS

What is the basal tone for sweat glands, arterioles, veins

SNS

What does botulinum toxin do

Blocks release of Ach from presynaptic terminal

What is acetylcholine synthesized from

Choline and acetyl-coA

Name the M receptors and where they are

``` M1,4,5 = CNS m2 = heart M3 = smooth muscle, glands, endothelium, eye (circular) ```

Norepinephrine synthesis

Tyrosine - dopa - dopamine - norepinephrine

What does methylphenidate do

Stops Reuptake of norepinephrine (like cocaine)

Alpha one and camp

Increases camp = smooth muscle contraction

Alpha 2 and camp

Decreases camp - decreased NE release

Betas and camp

Adenyl Cyclase = increased camp = increased kinase = activation to do the things it needs to do

Sympathetic action on the heart

B1 - increase chronotropy and inotropy

Parasympathetic action on the heart

M2 - decrease heart rate and inotropy

SNS and PSNS actions on the lungs

Beta 2 - bronchodilation | M3,2 - bronchoconstriction

SNS action on kidney

B1 - increase RASS

SNS action on liver

b2 - increase gluconeogenesis

SNS action on VSMC

Apha1 - constriction (skin and splanchnic) | Beta2 - dilation (sk muscle)

SNS and PSNS action on GI walls

B2 - relax | M3 - contract

What are the SNS and PSNS actions on GI sphincters

Alpha 1 - contract | M3 - relax

What are the PSNS actions on GI secretions

M3 - increased secretions

What are the SNS and PSNS effects on urinary bladder wall

Beta2 - relax | M3 - contracts

SNS and PSNS effects on urinary bladder sphincter

Alpha1 - contract | M3 - relax

SNS and PSNS effects on uterine smooth muscle

``` B2 = relax M = contract ```

SNS and PSNS on reproductive

Alpha 1 - ejaculate | M3 - erection

SNS effect on adrenal medulla

NicotinicN - epi/norepinephrine release

SNS and PSNS effect on eye

Alpha 1 - contract radial (SNS) - mydriasis | M3,2 - contract circular (PSNS) - miosis

SNS effect on pilomotor smooth muscle

Contract alpha 1

SNS effect on sweat glands - thermoregulatory

M - increased sweat

SNS effect on sweat glands - aprocrine (stress)

Alpha 1 - sweat

SNS effect on fat cells

B3 - lipolysis

Autonomic Drugs Flashcards

(91 cards)