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41 Cards in this Set

  • Front
  • Back
Symptoms of excess parasymp. activity?
DUMBBELSS:

Diarrhea, Urination, Miosis, Bronchospasm, Brady, Excitation of Skeletal m. and CNS, Lacrimation, Sweating, Salivation
What drugs are used for Alzheimers?
Donepezil, Galantamine, Rivastigmine
Pathology of Myasthenia gravis? How treated?
Myasthenia gravis = Ab's to Acetylcholine receptor = pt presents with Diplopia and Ptosis = drooping eye that worsens throughout day, can also have Thymic Hyperplasia, Atrophy or tumor --> can lead to Myasthenic Crisis = progressing weakness in respiratory muscles

Dx = Tensilon test

Tx = Acetylcholinesterases (Pyridostigmine, Neostigmine), Corticosteroids, Thymectomy = remove thymus, Plasmapharesis = will remove the Abs to the Ach receptor
What drug regenerates Ach after organophosphate poisoning?
Pralidoxime = 2-PAM
What is the antidote for organophosphate poisoning?
Atropine
Which anticholinesterases are used in the treatment of Alzheimer's disease?
Donepezil, Galantamine, Rivastigmine
T/F: Nicotinic Ach receptors are ligand gated Na+/K+ channels and Muscarinic Ach receptors are G-protein-coupled receptors that act through second messenger subtypes M1, M2, M3, M4, M5
True
List the Direct Ach Agonists (=Cholinergic Agonists) that mimic Ach
Bethanechol (post-op and neurogenic ileus and urinary retention), Carbachol (galucoma, pupillary contraction, releif of intraocular pressure), Pilocarpine (stimulator of sweat, tears, salica), Methacholine (challenge test to Dx asthma)
What are the Indirect Agonists of Ach (=target Anti-cholinesterase which normally works to break down Ach)
Neostigmine (post-op and neurogenic ileus and urinary retention, myasthenia gravis, reverses neuromuscular junction blockade), Pyridostigmine (Myasthenia gravis doesn't penetrate CNS, Edrophonium (Dx Myasthenia gravis), Physostigmine (Glaucoma and atropne over-dose), Ecothiophate (glaucoma), Donepazil (Alzheimer's)
Organophosphates such as Parathion used by farmers and gardeners does what? Tx?
Irreversibly inhibit AchE = we get Inc Ach = DUMBBELSS symptoms

Tx = Atropine and then Pralidoxine regenerates the AchE
Most common Neuro-muscular junction disorder?
Myasthenia Gravis

= Abs to post-synaptic Ach receptor causes ptosis, diplopia, general weakness
What are the Muscarinic Blockers?
Atropine, Homatropine, Tropicamide, Benztropine, Scopolamine, Ipratropium, Oxybutynin, Glycopyrrolate, Methscopolamine, Pirenzepine, Propantheline
Use for Atropine?
Mydriasis and Clycloplegia
Use of Benztropine?
Parkinsons

"Park my Benz"
Use of Scopolamine
Motion sickness
What are the symptoms of inhibiting parasympathetic activity?
"Dry Everywhere"

Ileus, urinary retention, hyper-pyrexia (=hot), dry mouth, Flushing of skin, blind tachy, dilation of eye, delirium
Physostigmine, Echothiophate, Donepezil, Neostigmine, Edrophonium, Rivastigmine, Pyridostigmine

These are all are?
Anti-AchE = anti-acetylcholinesterase = Inc. Ach b/c they inhibit the thing that breaks Ach down
Pilocarpine, Bethanechol, Carbachol are all?
Cholinergic Agonists = Inc Ach
Oxybutynin, Atropine, Darifenacin, Ipratropium, Tropicamide, Benztropine, Scopolamine, Tolterodine, Trospium, Homatropine are all?
M-Blockers = Block Ach binding
Which of the M-Agonists are used to improve FEV1 in a pt with asthma?
Ipratropium
A 30 year old schizophrenic now has urinary retention due to his neuropleptic - what do you treat him with?
Bethanechol
What drugs can dilate pupils?
Sympathetic Agonist OR Anti-cholinergic like an M-blocker
What drugs can be used in treatment of urge incontinence?
M Blockers:

Oxybutynin, Tolteradine, Darifenacin, Solfenacin, Trospium
List the steps in Ach Synthesis and neurotransmission
Choline enters with the help of Na+ --> (Hemicholnium inhibits this process) --> Acetyl CoA and choline acetyltransferase are made into Ach, then packaged into vessicles --> Ca2+ needed for release

Black widow spider toxin causes release, while Botulinum toxin inhibits release and causes flaccid paralysis
What inhibits the making of Ach by disabling it from being packaged into vessicles?
Vesamicol
List the steps involved in NE synth and neurotransmission
Tyrosine enters cell with the help of Na+ --> Tyrosine turned into DOPA by Tyrosine Hydroxylase (inhibited by Metyrosine) --> DOPA turned into Dopamine by Dopadecarboxylase --> Dopamine pachaged into vessicle (inhibited by Reserpine) --> Ca2+ needed to release vessicle into synapse
What things promote NE release? Inhibit? Inhibit NE RE-UPTAKE?
Promote NE release: Amphetamines, Ephedrine, Tyrosine, Angiotensin II

Inhibit NE release: Guanethidine, Bretylium, Alpha 2 and M2 ie if parasympathetic activity is going on, we don't want NE to be released = we want to inhibit Symps

Inhibit re-uptake: Coccaine, TCA's
What are two molecules that metabolize NE once it gets into the synapse (note, these are similar to Acetylcholiesterase which degrades Ach in synapse)
COMT (methylates NE) and MAO (Monoamine Oxidase Oxidizes NE)

* Both make NE Unusable
Vit B 6 and Vit C are needed in which steps of the making of NE from Tyrosine?
Vit B6 needed in step from Dihydroxyphenylalanine to Dopamine

Vit C needed in step from Dopamine to NE
What G proteins are coupled to the various receptors?
Inhibitory G proteins = "MAD2"

Gi = M2, A2, D2

"qt's HAV 1 m&m"

Gq = H1, A1, V1, M1, M3

*Everything else is Gs
Outline the path after a Gq receptor is stimulated
Gq = Activates Phospholipase C --> Cleaves Lipids to PIP2 --> DAG or IP3... IP3 increases Ca2+ in cell while DAG leads to protein kinase C
Outline the path after Gs or Gi stiulates or inhibits Aneylyl cyclase
Gs or Gi stimulate (path preoceeds) or inhibit (path stops) Adenylyl cyclase --> ATP --> cAMP --> Protein kinase A
What regulates prolactin secretion from pituitary?
Dopamine from hypothalamus = INHIBITS prolactin secretion

Prolactin inhibits its own secretion by increasing Dopamine synthesis
Effect of Epinephrine, NE, Isoproterenol, Dopamine, Dobutamine, Phenylephrine on alpha 1, 2, beta 1, 2, and D1 receptors?
Epinephrine does alpha 1, alpha 2, and beta 1 >> Beta 2 (Anaphylaxis, glaucoma, asthma, hypotension)

NE does alpha 1 and alpha 2 >> beta 1 (Hypotension but dec renal perfusion, inc BP, dec. HR due to reflex brady)

Isoproterenol does beta 1 and beta 2 (AV Block, vasodilation causes reflex tachy)

Dopamine does alpha 1, alpha 2, beta 1 >> beta 2 and Dopamine receptors at low doses (High dose = vasoconstriction, low dose = augments renal blood flow...uses = chock, heart failure)

Dubutamine does Beta 1 (heart failure, cardiac stress testing,

Phenylephrine does alpha 1 (pupillary dilation, vasoconstriction, nasal decongestion)
Albuterol, Metaproterenol, and Salmeterol are are all used for what?
ASTHMA

Metaproterenol and Albuterol for Acute asthma

Salmeterol for long-term tx

(All work on Beta 2's)
What do we use to reduce premature uterine contraction?
Terbutaline or Ritodrine

(works on Beta 2's to dec. contractions)
Most common first line agent for pts in septic shock? Cardiogenic shock?
Septic chock = NE

Cardiogenic shock = Dobutamine
What is Epi's affect on BP if administered after an alpha blocker is given?
alpha blocker will block alphas so that Epi only works on the Beta 2's on blood vessels meaning we vasodilate
Common side effects of beta blockers?
Exacerbate asthma, raise blood glu, mask symptoms of hypoglycemia, bradycardia, AV Block, CHF, Impotence, Erectile Dysfunction,
Be careful giving be blockers to pts with what conditions?
Asthmatics, Diabetics, CHF
What are the various clinical applications of Beta Blockers?
HTN, Angina pectoralis, MI, SVT, CHF