ANS Pharmacology - Drugs
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- How do you keep Dave Rosenthal entertained for hours?
- How do you keep Dave Rosenthal entertained for hours?
- Phenytoin
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Antiepileptic
Blocks Na, Ca channels - Halothane
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General Anesthetic
Increases GABA action - Lidocaine
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Local Anesthetic & Antiarrythmic
Blocks Na, K channels - a-bungarotoxin
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Blocks Nicotinic ACh receptors
(direct antagonist) - Hemicholinium
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Presynaptic Choline block
Blocks choline uptake --> dec MEPP size - Tetrodotoxin (TTX)
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From pufferfish
Blocks Na conduction change
--> no AP - a-latrotoxin
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From black widow spider
Massive secretion of ALL ACh at once --> depletion of ACh - BoTox
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Botulism Toxin A
Cleaves SNAP25, reducing affinity for Ca - Tubocurarine
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Non-depolarizing competitive inhibitor of ACh receptors
Side effects: Histamine, ganglion block (DEC BP) -
_Curium
_Curonium -
Nondepolarizing AChR blockers
(Competitive inhibition) - Pancuronium
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Steroid nondepolarizing AChR blocker (long action)
-More potent
-Blocks vagal tone (Tachycardia) - Vecuronium
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Int. duration nondepolarizing blocker
No hist or CV effect
Liver elimination - Atracurium
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Int duration
Elim in plasma
Some histamine (may cause hives)
Steroisomers may cause seizure - Cisatracurium
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Nondepolariznig AChR blocker (int action)
Single Steroisomer of Atracurium
(fewer seizures) - Rocuronium
- Rapid onset, int duration non-dep AChR blocker
- Nicotine
- Depolarizing AChR blocker
- (no question)
- -
- Dantrolene
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Blocks release of Ca from S.R. Ryanodine channels
Treat Malignant hyperthermia in succinylcholine - Succinylcholine
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Depolarizing ACh blocker - esp for intubation.
May cause brady or tachycardia
May cause mal. hyperthermia
NO LONG TERM USE - Neostigmine
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Acetylcholinesterase inhibitor
Treat M.G., reverses Pancuronium - Edrophonium
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Short lived anticholinesterase
Use to test for M.G. - Atropine
- Competitive blocker of Muscarinic Receptors
- Acetylcholine (as a drug)
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Primary effect is to stimulate P.S.
--> slowed HR (via G protein)
--> Vasodilation (non-inervated muscarinic receptors) - Methacholine
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Muscarinic ACh analog
Slowly hydrolyzed by AChE
Used in bronchial asthma challenge - Carbachol
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Nonspecific (Musc&Nic) ACh analog
Also a post depol blocker
No degradation by cholinesterase - Bethanacol
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Muscarinic ACh analog
Res. to hydrolysis
Treatment of low bowel tone (adynamic ileus), urinary retention - Pilocarpine
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Muscarinic ACh analog
No breakdown
Treat Glaucoma via pupillary constriction, contraction of ciliary muscle - Physostigmine
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Reversible cholinesterase inhibitor (esp. for muscarinic receptors) crosses blood brain barrier
For glaucoma, and as antidote irrev AchR inhibitors - Pyridostigmine
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Slow release neostigmine
Acetylcholinesterase inhibitor - DFP
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Irreversible ChE inhibitor
Oily & well absorbed through skin - Tabin
- Irreversible ChE inhibitor
- Sarin
- Irreversible ChE inhibitor
- Parathion
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Irreversible ChE inhibitor
Agricultural Insecticide - Malathion
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Irreversible ChE inhibitor
Agricultural insecticide
Less harmful to humans - VX
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Irreversible ChE inhibitor
Very deadly nerve gas - Antilirium
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Salycate salt of Physostigmine
Acetylcholinesterase inhib - Homatropine
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Short lived Atropine
(muscarinic blocker) - Scopolamine
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Muscarinic Antagonist
Like atropine, but more CNS
Esp for anti-emetic, sedation, amnesia, twilight sleep - 3 Drugs for urinary incontinence
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Tolteridine
Oxybutin
Solifanacin
(All musc. blockers) - 3 preferred ocular muscarinic blockers
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Tropilamide
Cyclopentalate
Homatropine - 2 muscarinic blockers in parkinsons
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Benztropine
Trihexyphenidyl - 2 muscarinic blockers for bronchiolar dilation
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Ipratropium
Tiotropium - 2 muscarinic blockers for GI spasm
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Lomotil (atropine + opioid (dihenoxylate)
Glycopyrolate - 4 ganglionic blockers
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Hexamethonium
Trimethaphan
Mecamylamine
Tubocurarine - Uptake 1 inhibitors
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Tricyclic Antidepressants
Cocaine
Ritalin - Phenylephrine
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a1 receptor agonist
For: Mydriasis
Eye vasoconstriction
Nasal Decongestant - Imadolazine derivatives
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a1 agonists
Not broken down by MAO or COMT
Effect a2 at high doses - Midodrine
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a1 agonist
Used for BP (esp postural) - Methoxamine
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a1 agonist w/ sustained effects
Doesn't affect cardiac receptors. - clonidine
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central a2 agonist (high dose stimulates peripheral - vasoconstriction)
Decrease BP, Decrease NE
S.E. -- sedation, sex dysfunction
O.D. activates a2 receptors --> vasoconstriction - Guanfacine / Guanabez
- a2 agonists
- a-methyl dopa
- Metabolized into a-methyl NE that is then released as an a2 agonist
- Dobutamine
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B1 agonist
Used to increase CO in cardiogenic shock (primary) (Increase contract w/o increasing hr) - Albuterol
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Prototype B2 agonist
- Bronchiloar and uterine relaxation(prevent premature labor) - Terbutaline
- Parenteral B2 agonist - Approved for asthma, used for premature labor.
- Ritodrine
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B2 agonist approved for preventing premature labor.
Causes increased HR, etc in both mother and baby. - Ephedrine/Pseudoephedrine
- Indirectly activates NE release. Also a B2 agonist.
- Dopamine
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B1, and dopamine agonist
Use to increase CO in cardiogenic shock (secondary). Causes oliguria, small inc in vasoconstriction - phenoxybenzamine
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a1, a2 blocker (more a1)
Effect depends on level of symp. tone
Treat pheo, sex dys, prophylactic in surgery - Phentolamine
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a1,a2 blocker.
Use in pheo, sex dysfunction, tyramin hypertensive crisis. - Prazosin (_azosin)
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a1 receptor blocker
- Decrease BP
- Decrease urine block (in erethra, prostate, bladder neck) - Terazosin
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a1 blocker.
Treat BPH - Tamsulosin (flomax)
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Block a1A receptors (in prostate/bladder)
NOT a1B (in blood vessels) - Alfuzosin
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a1A antagonist
Pee. - Yohimbine
- Selective a2 antagonist - Causes tachycardia, aphrodisiac
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Sildenafil (Viagra)
_denafil (others) -
Phosphodiesterase 5 inhibitors.
Contraindicated w/ nitrates or nonspecific a1 blockers. - Propranolol
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Non selective b blocker.
Antiarrythmic, antianginal, antihypertensive, pheochromocytoma, stage fright, migraine.
CONTRA: Diabetics/asthmatics - Timolol
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Nonselective B blocker
Treat open angle glaucoma via decreased secretion of aqueous humor.
Also treats migraines. - Metoprolol
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Specific B1 blocker
No bronchiolar effects
Cardiac arrhytmia, hypertension, angina - Betaxolol
- Specific B1 blocker for Glaucoma (in place of timolol)
- Butoxamine
- B2 receptor blocker
- Labetalol
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a1 & b1 blocker
Treat hypertensive crisis
Pheochromocytoma - Tyramine
- Indirect sympathomemitic
- Amphetamines
- Indirect acting sympathomimetics
- Ephedrine
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Mixed sympathomimetic.
Indirect actions
EPI actions (esp B2) - Phentermine
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(works like ephedrine)
Phen in Fen-Phen
Beta stimulation blocks feeding. - Theophyline
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Blocks a phosphodiesterase (increasing beta 2) - Helps in bronchodilation.
Synergistic w/ psuedoephedrine - Levefed
- Norepinephrine. Used for severe hypotension (i.e. in the ICU)