ANS & NMJ Drugs

acetylcholine, bethanechol, pilocarpine, cevimeline

list the direct cholinergic agonists

edrophonium, pyrostigmine, neostigmine, physostigmine

list the indirect (AChase inhibitors), reversible cholinergic agonists

echothiophate

list the indirect (AChase inhibitors), irreversible cholinergic agonists

atropine, scopolamine, ipratropium, tiotropium, oxybutynin, tolterodine, solifenacin, hyoscyamine, glycopyrrolate

list the direct cholinergic antagonists

epinephrine

list the direct acting adrenergic agonists on a1, a2, B1, B2

norepinephrine

list the direct acting adrenergic agonists on a1, a2, B1

isoproterenol

list the direct acting beta, nonselective adrenergic agonists (B1, B2)

albuterol, levalbuterol, salmeterol, formoterol

list the direct acting beta, selective adrenergic agonists (B2)

phenylephrine, oxymetazoline

list the direct selective adrenergic agonists (a1)

cocaine

list the indirect adrenergic agonists

pseudoephedrine

list the mixed (direct/indirect) adrenergic agonists

tamsulosin, terazosin, doxazosin, prazosin

list the selective alpha blockers (adrenergic antagonists, a1)

propanolol

list the non-selective beta blockers (adrenergic antagonists, B1, B2)

labetalol, carvedilol

list the non-selective alpha & beta blockers (adrenergic antagonists, B1, B2, a1)

metoprolol, atenolol

list the beta, cardio selective blockers (B1, adrenergic antagonists)

nicotine

list the ganglionic agonists

succinylcholine

list the NMJ agonists

onabotulinum toxin A, incobotulinumtoxin A

list the NMJ antagonists

acetylcholine

• type: direct acting cholinergic agonist

• limited clinical use (doesn’t pass through membranes easily, rapidly broken down by enzymes all over body, lacks specificity for muscarinic & nicotinic receptors)

• indication: can be injected into eye during surgery to cause miosis (binds to M2/M3 iris sphincter receptors)

bethanechol

• type: direct acting cholinergic agonist

• indication: urinary retention tx

• MOA: binds & stimulates M receptors

• adverse effects: SLUD, miosis, increased acc., retinal detachment, decreased IOP

pilocarpine/cevimeline

• type: direct acting cholinergic agonist

• indication: Sjogren’s tx

• MOA: binds & stimulates M receptors on lacrimal & salivary gland

• adverse effects: SLUD, miosis, increased acc., retinal detachment, decreased IOP

bradycardia, asthma, COPD

what are common contraindications for cholinergic agonists?

edrophonium

• type: indirect, reversible, cholinergic agonist

• indication: myasthenia gravis diagnosis

• MOA: binds & inhibits acetylcholinesterase

• adverse effects: SLUD, miosis, increased acc., retinal detachment, decreased IOP

pyridostigmine, neostigmine

• type: indirect, reversible, cholinergic agonist

• indication: long term treatment of myasthenia gravis & without crossing BBB

• MOA: binds & inhibits acetylcholinesterase

• adverse effects: SLUD, miosis, increased acc., retinal detachment, decreased IOP

physostigmine

• type: indirect, reversible, cholinergic agonist

• indication: tx of myasthenia gravis & does cross BBB

• MOA: binds to & inhibits acetylcholinesterase

• adverse effects: SLUD, miosis, increased acc., retinal detachment, decreased IOP

echothiophate

• type: indirect, irreversible, cholinergic agonist

• indication: decrease IOP in glaucoma (rare usage now)

• MOA: covalently binds & inhibits acetylcholinesterase

• adverse effects: SLUD, miosis, increased acc., retinal detachment, decreased IOP, skeletal muscle cramps/weakness with OD

atropine

• type: cholinergic antagonist

• indication: emergent cardiac issues, emergent respiratory issues

• MOA: binds & inhibits muscarinic receptors

scopolamine

• type: cholinergic antagonist

• indication: nausea, vomiting tx

• MOA: binds & inhibits muscarinic receptors

• adverse effects: dry mouth/skin/eyes, tachycardia, urinary retention, constipation, mydriasis, hallucinations, ataxia, delirium, coma

ipratropium, tiotropium

• type: cholinergic antagonist

• indication: treatment of respiratory disorders (asthma/COPD)

• MOA: binds & inhibits muscarinic receptors & do not cross BBB

• adverse effects: dry mouth & eyes, tachycardia, mydriasis

oxybutynin, tolterodine, solifenacin, hyoscyamine

• type: cholinergic antagonist

• indication: overactive bladder (IBD/GI spasms)

• MOA: binds & inhibits muscarinic receptors (can cross BBB)

• adverse effects: dry mouth/skin/eyes, tachycardia, urinary retention, constipation, mydriasis, hallucinations, ataxia, delirium, coma

glycopyrrolate

• type: cholinergic antagonist

• indication: hyperhidrosis treatment

• MOA: binds & inhibits muscarinic receptors

• adverse effects: dry mouth/skin/eyes, tachycardia, urinary retention, constipation, mydriasis, hallucinations, delirium, coma, ataxia

belladonna alkaloid

• examples include: atropine, scopolamine, hyoscyamine

• plant extracts cause pupil dilation

• can be highly toxic & cause accidental poisoning

physostigmine

what is given as an antidote for anticholinergic drug overdoses?

atropine

what is given as an antidote for indirect, reversible cholinergic agonist drug overdoses?

pralidoxime (with atropine to pass BBB)

what is given as an antidote for indirect, irreversible cholinergic agonist drug overdoses?

nicotine

• type: ganglionic agonist

• indication: smoking cessation

• MOA: bind nicotinic receptors in sympathetic & parasympathetic ganglia (so get both effects depending on situation)

epinephrine

• type: adrenergic agonist

• indication: anaphylaxis, cardiac arrest, respiratory emergency

• MOA: binds & stimulates a1, a2, B1, B2

• adverse effects: mydriasis, decreased tearing/acc./eye redness, eyelid raise, increased IOP

norepinephrine

• type: adrenergic agonist

• indications: shock, cardiac arrest

• MOA: binds & stimulates a1, a2, B1

• adverse effects: mydriasis, decreased tearing/eye redness, eyelid raise, increased IOP

isoproterenol

• type: beta agonist, non-selective

• indications: shock, cardiac arrest

• MOA: binds & stimulates B1, B2

• adverse effects: decreased acc., increased IOP

albuterol, levalbuterol, salmeterol, formoterol

• type: selective beta agonist

• indications: asthma/COPD

• MOA: binds & stimulates B2

• adverse effects: increased BP, mydriasis, decreased tearing & eye redness, eyelid raise

phenylephrine, oxymetazoline

• type: selective alpha agonist

• indications: binds & alleviates nasal decongestion in allergies & colds

• MOA: binds & stimulates a1

• adverse effects: increased BP, mydriasis, decreased tearing & eye redness, eyelid raise

cocaine

• type: indirect adrenergic agonist

• indications: severe nosebleed tx

• MOA: blocks reuptake of NE by binding to NE presynaptic transporter

• adverse effects: increased BP, mydriasis, decreased tearing & eye redness, eyelid raise, increased IOP

pseudoephedrine

• type: mixed acting adrenergic agonist

• indications: nasal decongestion in colds & allergy tx

• MOA: binds & stimulates a1, a2, B1, B2 and increases synaptic concentration of NE

• adverse effects: increased BP, tachycardia, urinary retention, mydriasis, decreased tearing/acc./eye redness, increased IOP, eyelid raise

tamsulosin, terazosin, doxazosin, prazosin

• type: alpha blockers

• indications: benign prostatic hyperplasia, HTN tx

• MOA: binds & inhibits a1

• adverse effects: IFIS/miosis during eye surgery

propanolol

• type: non-selective beta blockers

• indications: CV disease, lowers heart rate & BP

• MOA: binds & inhibits B1, B2

• adverse effects: increased acc., decreased IOP

bronchoconstriction, bradycardia

contraindications for non-selective beta blockers or non-selective alpha & beta blockers

labetalol, carvedilol

• type: non-selective beta & alpha blockers

• indications: CV disease, lowers heart rate and BP

• MOA; binds & inhibits B1, B2, a1

• adverse effects: miosis, increased acc., decreased IOP

metoprolol, atenolol

• type: cardio selective beta blockers

• indications: CV disease, lowers HR & BP

• MOA: binds & inhibits B1

• adverse effects: decreased IOP

bradycardia

contraindications for cardio-selective beta blockers

succinylcholine

• type: NMJ direct agonist

• indication: muscle relaxation/paralysis during surgery

• MOA: binds nicotinic NMJ receptors only

causes a twitch, then makes the receptor stop working & results in relaxation that can lead to paralysis

effect of succinylcholine

onabotulinumtoxin A, incobotulinumtoxin A

• type: NMJ indirect antagonist

• indication: blepharospasm, strabismus, reduce sweating/wrinkles/HA

• MOA: blocks pre-synaptic release of ACh at the NMJ

inhibits skeletal muscle contraction for a few months when injected into a muscle

what is the effect of onabotulinumtoxin A and incobotulinumtoxin A?