ANS- RECEPTORS AND MEDS Flashcards
cholinergic agonists- direct vs indirect (names)
direct- bind and activate cholinergic receptors
- choline ester
- plant alkaloids
indirect- inc synaptic conc of ACh
- cholinesterase inhibitors
remember cholinersterase is what breaks down ACh in synaptic cleft
direct cholinertic agonist
choline esters
what receptors
- ACh
- Carbachol
- bethanechol
- methacholine
ACh & Carbachol- activate nicotinic and muscarinic
- lack of specificity for musc= wide range of effects on many organs
Bethanechol & Methacholine- activate ONLY muscarinic
direct cholinergic agonists
choline esters
- bethanechol
- receptor
- therapeutic effects and uses
receptor- muscarinic
effect- stimulate bladder/inc intestinal motility w out significant efects on HR/BP
use- tx of urinary retention post op/post partum
make pt pee
lack of nicotinic activity = more action of gi and bladder
direct cholinergic agonists
choline esters
- carbachol
- receptor
- therapeutic effects and uses
receptor- muscarinic + nicotinic
effect- miosis during optho surgery
use- chronic open angle glaucoma
eat carbs, u get fat, u DILATE
direct cholinergic agonists
plant alkaloids
- muscarine and nicotine
- use
muscarine- no current medical use
nicotine- smoking cessation
direct cholinergic agonists
plant alkaloids
- pilocarpine
- receptor
- therapeutic effects and uses
pilocarpine= isoptocarpine, ocusert, salagen
receptor- high affinity for muscarinic
use- tx for glaucoma
effect- stim contraction cliary muscle fibers, inc aqueous humor outlow, dec ocular pressure
direct cholinergic agonists
plant alkaloids
- cevimeline (exovac)
- use
tx for dry mouth assoc with sjogren’s syndrome
sjorgens- immune ds characterized by dry eyes and mouth (xerostonia)
indirect cholinergic agonists
Cholinesterase inhibitors
- MOA
MOA- inhibit breakdown of ACh at ALL cholinergic synapses (INHIBIT THE ENZYME/ACE)—> INC ACh concentration
- reversible vs irreversible
indirect cholinergic agonists
Cholinesterase inhibitors: REVERSIBLE agents
- donepezil (aricept)
tx for alzheimers ds
indirect cholinergic agonists
Cholinesterase inhibitors: REVERSIBLE agents
- edrophonium (enlon)
- duration and use
- short duration
use- dx of mysathenia gravis
indirect cholinergic agonists
Cholinesterase inhibitors: REVERSIBLE agents
- neostigmine (prostigmin)
- use
use- tx of mysathenia gravis, antidote for skeletal muscle relaxants
indirect cholinergic agonists
Cholinesterase inhibitors: REVERSIBLE agents
- physostigmine (eserine)
- use
use- tx overdose of drugs with anticholinergic effects (ex: atropine, TCAs)
indirect cholinergic agonists
Cholinesterase inhibitors: REVERSIBLE agents
- pyridostigmine (mestinon)
- use
use- tx of mysathetnia gravis
indirect cholinergic agonists
Cholinesterase inhibitors: IRREVERSIBLE agents
- ecothiophate (phospholine)
- duration and use
use- tx of chronic refractory glaucoma
duration up to one week
indirect cholinergic agonists
Cholinesterase inhibitors: IRREVERSIBLE agents
- pesticides (parathion and malathion)
- soman
pesticides- controls pests/insecticide
soman- chemical warfare agent
organophosphate poisoning
- what is it
- effects
- tx
- causes augmented cholinergic neurotransmission at central and peripheral synapses (by inhibiting ACE enzyme)
- All effects of muscarinic activation
- cholinergic activation in CNS (seizures, resp depression, coma)
- excessive activation of nicotinic receptors (neuromusc blockade and muscle paralyis)
(SLUDGE, spasm, bronchoconstrict, dec HR and CO)
organophosphate poisoning Tx
- symptomatic
- decontamination
- antidotes (atropine and pralidoxime to generate cholinesterase)
pralidoxime = 2-PAM
cblonergic antagonists
nicotinic receptor antagonists
- ganglionic blockers
- neuromuscular blockers: curium
- depolarizing neuromuscular blocker- succinylcholine
cholinergic antagonists
muscarinic receptor antagonists
- BellaDonna Alkaloids
- Synthetic/semi synthetic
alkaloids- atropine, scopolamine, hyoscyamine
synthetic/semi- ipratropium, tolterodine, oxybtynin, propantheline, dicyclomine, benztropine
cholinergic antagonists
muscarinic receptor antagonists (BellaDonna Alkaloids
and Synthetic)
EFFECTS and THERAPEUTIC USES
- general, ocular, and cardiac
general- relax smooth musc, inc HR/CO, inhbit exocrine gland secretion
ocular- mydriasis, dry eyes
- use: mydriatic to faciliate eyes exam (atropine, scopolamine)
cardiac- inc HR and AV conduction
- use: sinus brady and AV block (atropine)
cholinergic antagonists
muscarinic receptor antagonists (BellaDonna Alkaloids
and Synthetic)
EFFECTS and THERAPEUTIC USES
- resp, GI and urinary tract
resp- bronchodilate
- uses: COPD, emphysema, bronchitis
- ipratropium/atrovent, tiotropium/spiriva
GI/Urinary- relax gi muscle, dec intestinal motility, inhbit gastric acid secretion and urinary retention
- uses: tx intestinal spams/pain (hysosamine, donnatal, dicyclomine)
- tx dysuria and urinary incontinence (oxybutynin, tolterodine, darifenacin, solifenacin)
cholinergic antagonists
muscarinic receptor antagonists (BellaDonna Alkaloids
and Synthetic)
EFFECTS and THERAPEUTIC USES
- CNS
tx for motion sickness (scopolamine patch)
tx for parkinsons ds- reduce tremor (benztropine and trihexyphenidyl)
side effects- sedation, confusion, altered mental status
nicotinic receptor antagonists
- ganglionic blockers
- neuromuscualr blocking agents
ganglionic- limited due to AE
- trimethaphan (used rarely for HTN emergency)
neuromusc- depol and nondepolarizing agents
nicotinic receptor antagonists
neuromuscular blocking agents
- non depol
- depol
causes, effects, use, reversible?, duration
NONDEPOLARIZING (curariforms)
- atracurium pancuronium, vecuronium, rocuronium
- comptetitive antag of ACh at nicotinic musc receptors
causes- muscle relax and paralysis
effects reversed by- cholinesterease inhibitors
use- surgery, itubation, ventilators
DEPOLARIZING
- succinylcholine
- causes- persistent depol
- use- surgery, RSI kits
- effect NOT reversed by cholinesterase inhibit, not antidote if overdose
- SHORT DURATION
adrenergic agonists
direct acting agonists
- catecholamines (epi, NE, isoproterenol, dopamine, dobutamine)
- non catech (albuterol, clonidine, phenylephrine)
adrenergic agonists
indirect agonists
amphetamine, cocaine, tyramine
adrenergic agonists
mixed direct/indirect agonists
psuedoephedrine
direct adrenergic agonists
catecholamines
- preferred route
- effects
- rapidly metab by MAO and COMT enzymes in gut, liver, other tissues
- must give PARENTERALLY
- effect depend on affinity/specificity for type od adrenergic receptor
direct adrenergic ago- catecholamines
epinephrine
- MOA
- effects
- binds to all adrenergic receptors
- vasoconstrict, INC BP (a1)
- cardiac stim (b1)
- bronchodilate, skeletal musc vasodilate (b2)
- use- anaphylactic shock and cardiac arrest
direct adrenergic ago- catecholamines
norepinephrine
- use
- effects
use- hypotension and shock
- vasoconstrict and INC BP (a1)
- cardiac stim (b1)
direct adrenergic ago- catecholamines
isoproterenol (isoprel)
effects
use
- cardiac stim (b1), bronchodilate (b2)
use- tx asthma, AV block and bradycardia
direct adrenergic ago- catecholamines
dopamine (precursor to epi, NE)
effects
use
- renal vasodilate (D1)
- cardiac stim (b1)
- INC BP (a1)
use- tx cardiogenic shock, septic shock, HF, adjunct to fluid administration in hypovolemic shock
direct adrenergic ago- catecholamines
dobutamine
affinity for which receptors
use
highest affinity b1, less on a1
use- tx cardiogenic shock, cardiac arrest, HF
direct adrenergic ago- NON catecholamines
phenylephrine (neosynephrine)
- effect
- use
- vasoconstrict, INC BP, mydriasis (a1)
- use- nasal and ocular decongestant, maintenance BP during surgery
direct adrenergic ago- NON catecholamines
albuterol (proventil)
- use
- effects
- bronchodilate (b2)
- tx asthma
direct adrenergic ago- NON catecholamines
clonidine (catapres)
- MOA
- effects
- use
MOA- inhibit NE release from nerve terminal of postgang neuron (feedback inhibition, a2)
effect- CNS/sedation
use- tx for chronic HTN
