Pharmacology of ANS Flashcards
cholinergic receptors
*receive Ach as neurotransmitter
*nicotinic and muscarinic receptors
adrenergic receptors
*receive norepinephrine as neurotransmitter
*alpha (1 + 2) and beta (1, 2, 3) receptors
cholinomimetics
drugs that mimic or augment the action of acetylcholine (parasympathetic agonists)
muscarinic receptors are found on
*organs innervated by PARASYMPATHETIC nerves
*PLUS sweat glands (innervated by ACh sympathetic nerves)
*CNS
M2 receptor - location
HEART, nerves, smooth muscle
M3 receptor - location
GLANDS, smooth muscle, endothelium
direct-acting cholinomimetics: MOA
bind and activate muscarinic and/or nicotinic receptors
indirect-acting cholinomimetics - MOA
*inhibits acetylcholinesterase
*result: amplification of endogenous ACh (keeps for ACh around at the receptor)
*note: affect both nicotinic and muscarinic receptors
important direct-acting cholinomimetics to know
1) bethanechol
2) pilocarpine
3) carbachol
4) muscarine-containing mushrooms
bethanechol
*muscarinic agonist (direct-acting cholinomimetic; results in parasympathetic responses)
pilocarpine
*muscarinic agonist, penetrates CNS
(direct-acting cholinomimetic; results in parasympathetic responses)
carbachol
*muscarinic AND nicotinic agonist (direct-acting cholinomimetic; results in parasympathetic responses)
*mostly used as eye drops for GLAUCOMA
important indirect-acting cholinomimetics to know
1) edrophonium (we don’t use this anymore)
2) neostigmine
3) pyridostigmine
4) physostigmine - crosses BBB
*also, organophosphates (parathion, sarin)
neostigmine
*indirect acting cholinomimetic (acetylcholinesterase inhibitor)
*quaternary: poor CNS penetration
pyridostigmine
*indirect acting cholinomimetic (acetylcholinesterase inhibitor)
*quaternary: poor CNS penetration
physostigmine
*indirect acting cholinomimetic
(acetylcholinesterase inhibitor)
*tertiary: better CNS penetration - crosses the blood-brain barrier
main difference in effect of indirect-acting cholinomimetics (compared to direct-acting)
act like direct-acting agents, EXCEPT FOR THE VASCULATURE EFFECTS
what cholinomimetic do we use to treat dry mouth
pilocarpine (direct-acting cholinomimetic)
ACh toxicity (organophosphate poisoning) - SLUDGE
Salivation
Lacrimation
Urination
Defecation
GI symptoms
Emesis
(also, constricted pupil, slow heart rate, and bronchospasm)
ACh toxicity (organophosphate poisoning) - DUMBBELSS
Diarrhea
Urination
Miosis
Bronchoconstriction
Bradycardia
Emesis
Lacrimation
Salivation
Sweating
carbamates
*pesticide; reversible AChE inhibitors
what do you treat carbamate toxicity with
atropine (antimuscarinic) alone
what do you treat organophosphate poisoning with
atropine + pralidoxime
anticholinergics
*acetylcholine receptor-blocking drugs
*antimuscarinics are a subtype
*atropine is the protype
antimuscarinic drug actions
loss of parasympathetic activities: sedation, mydriasis, cycloplegia (can’t accommodate), dry “sandy” eyes, tachycardia, bronchodilation, decreased respiratory secretions, dry mouth, decreased GI secretions + motility, relaxes smooth muscles of ureters and bladder, slows voiding, suppresses thermoregulatory sweating
important antimuscarinic drugs to know
1) atropine
2) scopolamine
3) ipratropium
4) glycopyrrolate
5) oxybutynin
what antimuscarinic drug is used for asthma and COPD
inhaled ipratropium
what antimuscarinic drug is used for bradycardia
atropine
what antimuscarinic drug is used for motion sickness
scopolamine
what antimuscarinic drug is used for overactive bladder/spasms
oxybutynin (inhibits detrusor contraction, leading to urinary retention)
what antimuscarinic drug is used to decrease secretions
glycopyyrolate
what antimuscarinic drug is used to counteract muscarinic effects when neostigmine is given to reverse muscle relaxants
glycopyyrolate
symptoms of excess cholinergic blockade (too much antimuscarinic effects) - “mnemonic”
mad as a hatter
blind as a bat
dry as a bone
hot as a pistol
red as a beet
full as a flask
symptoms of excess cholinergic blockade (too much antimuscarinic effects) - symptoms
*CNS delirium & irritability (mad as a hatter)
*mydriasis & blurry vision (blind as a bat)
*loss of sweating, dry mouth, decreased tear production (dry as a bone)
*loss of sweating and temperature control (hot as a pistol)
*vasodilation in response to increased temp (red as a beet)
*urinary retention (full as a flask)
what drug is used to treat anticholinergic toxicity
physostigmine (a direct-acting cholinomimetic that crosses the BBB)
sympathomimetics
drugs that mimic or augment sympathetic responses
direct-acting sympathomimetics - MOA
norepinephrine (neurotransmitter) ; epinephrine (hormone)
indirect-acting sympathomimetics - MOA
1) displace stored catecholamines from nerve ending
2) decrease clearance of NE (inhibit reuptake or prevent metabolism)
epinephrine
*direct acting sympathomimetic (agonist)
*both alpha and beta
norepinephrine
*direct acting sympathomimetic (agonist)
*alpha-1, alpha-2 > beta-2
phenylephrine
*direct acting sympathomimetic (agonist)
*alpha-1 agonist
midodrine
*direct acting sympathomimetic (agonist)
*alpha-1 (oral drug to tx orthostatic hypertension)
clonidine
*direct acting sympathomimetic (agonist)
*alpha-2 agonist
isoproterenol
*direct acting sympathomimetic (agonist)
*beta-1, beta-2 agonist
dobutamine
*direct acting sympathomimetic (agonist)
*mostly beta-1 agonist
albuterol
*direct acting sympathomimetic (agonist)
*beta-2 agonist
terbutaline
*direct acting sympathomimetic (agonist)
*beta-2 agonist
important direct-acting sympathomimetics to know
1) epinephrine
2) norepinephrine
3) phenylephrine
4) midodrine
5) clonidine
6) isoproterenol
7) dobutamine
8) albuterol
9) terbutaline
pulse pressure
systolic pressure - diastolic pressure
uses of epinephrine
*ANAPHYLAXIS
*local vasoconstrictor
*cardia arrests
note - epi is an alpha and beta receptor agonist
uses of norepinephrine
BP support (IV) (increases BP)
note - NE is an alpha 1, alpha 2, and beta 1 agonist
uses of phenylephrine
BP support
mydriatic
decongestant
note - phenylephrine is an alpha 1 agonist
uses of isoproterenol
increase cardiac output
note - isoproteronol is a beta 1 and beta 2 agonist
uses of dobutamine
increase cardiac output
cardiac stress tests
note - dobutamine is a beta-1 agonist
uses of dopamine
support BP and cardiac output
NOTE: effects are related to dose
uses of albuterol
asthma & COPD
note - albuterol is a beta 2 agonist
uses of terbutaline
asthma & COPD
reduce premature uterine contractions
note - terbutaline is a beta 2 agonist
uses of clonidine
hypertension (decreases central sympathetic outflow)
withdrawal symptoms
note - clonidine is an alpha-2 agonist
important indirect-acting sympathomimetics
1) ephedrine
2) amphetamine
3) cocaine
ephedrine
*indirect acting sympathomimetic
*causes the release of stored catecholamines
use of ephedrine
hypotension with anesthesia
*ephedrine is an indirect-acting sympathomimetic (promotes release of stored catecholamines)
use of pseudoephedrine
nasal decongestant
make meth
phentolamine
*reversible alpha blocker
*blocks alpha 1 and alpha 2
prazosin
*reversible alpha blocker
*blocks alpha 1
*used for BPH (benign prostatic hypertrophy)
phenoxybenzamine
*irreversible alpha blocker
*blocks alpha 1 more than alpha 2
*used for pheochromocytoma
important alpha blockers to know
1) phentolamine
2) prazosin
3) phenoxybenzamine
effects of beta blockers
*decrease HR, contractility, and conductance
*block beta 2 vasodilation (lower blood pressure)
*increased airway resistance, especially in asthma
*reduce intraocular pressure
*inhibit lipolysis
*decrease renin release
beta blockers to know
1) propranolol
2) metoprolol
3) labetalol
propranalol
*beta blocker
*non-selective (blocks beta-1 and beta-2)
metoprolol
*beta blocker
*selectively blocks beta-1
labetalol
*beta blocker
*blocks alpha-1 in addition to beta-1 and beta-2