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41 Cards in this Set

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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