Pharmacology: Autonomics

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What is used to diagnose myasthenia gravis?: EDROPHONIUM - short acting (5-15mins) AChE inhib

+ test shows sudden brief inc musc strength
EDROPHONIUM: What does it mean when the weakness improves vs. worsens?: improves: weakness due to MG, Eaton-Lambert synd, or AChR antag

worsens: weakness due to depolarizing block (e.g. from overmedication)
EDROPHONIUM vs PYRIDOSTIGMINE?: EDROPHONIUM: dx MG

PYRIDOSTIGMINE: tx MG (longer half life)
tx for EDROPHONIUM O.D.?: ATROPINE
meds to treat myasthenia gravis?: AChE inhib: PYRIDOSTIGMINE, NEOSTIGMINE, AMBENOMIUM
CARBAMATE ESTERS?: NEOSTIGMINE, PHYSOSTIGMINE, PYRIDOSTIGMINE
mech of action of CARBAMATE ESTERS?: inhib AChE by carbamylating it (more stable bond)--.5-6hrs

also have weak cholinomimetic properties
what is used to reverse a non-depolarizing block?: AChE inhib: NEOSTIGMINE, PYRIDOSTIGMINE

(e.g. reverse surgical anesth induced by nicotinic AChR antag)
tx for anticholinergic drug poisoning, w/CNS toxicity present?: PHYSOSTIGMINE--can cross BBB
Which AChE inhib can be used to treat glaucoma?: PHYSOSTIGMINE
What drugs are used to inc GI motility and reduce urinary retention in p/o pts?: NEOSTIGMINE (AChE inhib)
BETHANCHOL (M2,M3 musc ag)
What AChE inhibitors are used to delay sx of Alzheimers?: TACRINE, DONEPEZIL, RIVASTIGMINE, GALANTAMINE
mech of organophosphate AChE inhibitors?: bind to and is hydrolyzed by AChE to form stable bond, undergoes "aging", becomes irreversible
what are the long-lasting AChE inhibitors?: DIISOPROPYL FLUOROPHOSPHATE (DFP), ECHOTHIOPHATE, MALATHION, PARATHIONa
antidote to organophosphate AChE inhibitors?: PRALIDOXIME--cholinesterase regenerator, must be give before again occurs
ATROPINE--to block musc effects of ACh to avoid fatal bradycardia
Sx of AChE inhibitor toxicity?: musc effects: bronchoconstriction, bradycardia, secretions, miosis, diarrhea, vasodil, urinary incont

nic effects: fascic, depol block of skel musc (diaphragm)

CNS effects: convulsions, resp and CV collapse
Where are nicotinic receptors found?: Nn subtype: autonomic (SNS) gang, adrenal medulla

Nm subtype: motor endplate
what are the effects of nicotinic stimulation on: adrenal medulla, cardiac, vascular, GI, carotid bodies, emetic chemoreceptors, NM endplate.: epineph release
inc hr
periph vasoconstric
inc GI motility
inc RR
nausea and vomiting
fasiculations/spasms, depol blockage (high doses)
what can cause depolarizing block?: SUCCINYLCHOLINE, NICOTINE, DECAMETHONIUM (nic recep agonists)
what are phase I and phase II of depolarizing block?: I: continuous depol
II: inactivation of voltage gated Na channels (desensitization)
clinical uses of SUCCINYLCHOLINE?: skel musc relax for surg
hypotens, bradycard, resp depres, musc weak, unresponsive to ATROPINE and NEOSTIGMINE. cause?: depolarizing blockade (NICOTINE, SUCCINYLCHOLINE, DECAMETHONIUM)
what are the major effects of beta-2 receptor stimulation?: vasodil, bronchodil, relax uterus, relax bladder wall
what are the selective beta-2 agonists?: ALBUTEROL, METAPROTERENOL, TERBUTALINE, RITODRINE, SALMETEROL
main drugs to treat bronchospasm, asthma, bronchitis, COPD?: ALBUTEROL, METAPROTERENOL, TERBUTALINE (beta-2 agonists)
what drugs are used in tx of premature labor?: RITADRINE, TERBUTALINE (selective beta-2 agonists -> relax uterine smooth musc)
what drug is selective agonist for beta-1 receptors?: DOBUTAMINE
clinical effects of DOBUTAMINE?: pos inotropy w/o inc myocard O2 demand (b/c also dec' SVR). used for short term mgmt of CHF
what drug is a non-selective beta-agonist?: ISOPROTERENOL
clinical effects/uses of ISOPROTERENOL?: inc inotropy, h.r.
relaxes bronchial, vascular SM

used to stim hr in pts w/bradycardia or heart block
what drug is used for tx of glaucoma that does not exert its effects on the cholinergic system?: TIMOLOL--non-selective beta antag; decreases aqueous humor production, given as eye drops
What are the muscarinic agonists?: METHACHOLINE, BETHANECHOL, CARBACHOL, PILOCARPINE
which one of these 4 is not like the others: METHACHOLINE, BETHANECHOL, CARBACHOL, PILOCARPINE: BETHANECHOL is BETter--used to treat p/o abdominal distension and gastric atony

others are topical for glaucoma
clinical uses of ATROPINE?: bradycardia, AChE inhib overdose, cycloplegia and mydriasis, tx for cramping and urgent bladder in mild cystitis
which muscarinic antagonist is used by inhalation for tx of bronchial asthma? why?: IPRATROPIUM, is a quaternary amine, cant cross lipid bilayers, thus acts locally
what are the classic sx of atropine overdose?: "red as a beets, blind as a bat, dry as a bone, hot as a hare, mad as a hatter"
what classes of agents could be used to treat asthma?: beta-2 agonists (ALBUTEROL, TERBUTALINE, METAPROTERENOL, SALMETEROL), muscarinic antag (IPRATROPIUM)
what are the common side effects of beta-2 agonists?: skeletal muscle tremors, tachycardia
what class is used as a nasal decongestant? examples?: alpha agonists. PHENYLEPHRINE, XYLOMETAZOLINE, OXYMETAZOLINE
tx for ADHD?: AMPHETAMINE, METHYLPHENIDATE, PEMOLINE
which bronchodilator (beta-agonist) is most likely to cause tachycardia and arrhythmias?: ISOPROTERENOL

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