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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
Antiepileptic
Blocks Na, Ca channels
Halothane
General Anesthetic
Increases GABA action
Lidocaine
Local Anesthetic & Antiarrythmic
Blocks Na, K channels
a-bungarotoxin
Blocks Nicotinic ACh receptors
(direct antagonist)
Hemicholinium
Presynaptic Choline block

Blocks choline uptake --> dec MEPP size
Tetrodotoxin (TTX)
From pufferfish
Blocks Na conduction change
--> no AP
a-latrotoxin
From black widow spider
Massive secretion of ALL ACh at once --> depletion of ACh
BoTox
Botulism Toxin A
Cleaves SNAP25, reducing affinity for Ca
Tubocurarine
Non-depolarizing competitive inhibitor of ACh receptors
Side effects: Histamine, ganglion block (DEC BP)
_Curium

_Curonium
Nondepolarizing AChR blockers
(Competitive inhibition)
Pancuronium
Steroid nondepolarizing AChR blocker (long action)
-More potent
-Blocks vagal tone (Tachycardia)
Vecuronium
Int. duration nondepolarizing blocker
No hist or CV effect
Liver elimination
Atracurium
Int duration
Elim in plasma
Some histamine (may cause hives)
Steroisomers may cause seizure
Cisatracurium
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
Blocks release of Ca from S.R. Ryanodine channels
Treat Malignant hyperthermia in succinylcholine
Succinylcholine
Depolarizing ACh blocker - esp for intubation.
May cause brady or tachycardia
May cause mal. hyperthermia
NO LONG TERM USE
Neostigmine
Acetylcholinesterase inhibitor
Treat M.G., reverses Pancuronium
Edrophonium
Short lived anticholinesterase
Use to test for M.G.
Atropine
Competitive blocker of Muscarinic Receptors
Acetylcholine (as a drug)
Primary effect is to stimulate P.S.
--> slowed HR (via G protein)
--> Vasodilation (non-inervated muscarinic receptors)
Methacholine
Muscarinic ACh analog
Slowly hydrolyzed by AChE
Used in bronchial asthma challenge
Carbachol
Nonspecific (Musc&Nic) ACh analog
Also a post depol blocker
No degradation by cholinesterase
Bethanacol
Muscarinic ACh analog
Res. to hydrolysis
Treatment of low bowel tone (adynamic ileus), urinary retention
Pilocarpine
Muscarinic ACh analog
No breakdown
Treat Glaucoma via pupillary constriction, contraction of ciliary muscle
Physostigmine
Reversible cholinesterase inhibitor (esp. for muscarinic receptors) crosses blood brain barrier

For glaucoma, and as antidote irrev AchR inhibitors
Pyridostigmine
Slow release neostigmine
Acetylcholinesterase inhibitor
DFP
Irreversible ChE inhibitor
Oily & well absorbed through skin
Tabin
Irreversible ChE inhibitor
Sarin
Irreversible ChE inhibitor
Parathion
Irreversible ChE inhibitor
Agricultural Insecticide
Malathion
Irreversible ChE inhibitor
Agricultural insecticide
Less harmful to humans
VX
Irreversible ChE inhibitor
Very deadly nerve gas
Antilirium
Salycate salt of Physostigmine
Acetylcholinesterase inhib
Homatropine
Short lived Atropine
(muscarinic blocker)
Scopolamine
Muscarinic Antagonist
Like atropine, but more CNS
Esp for anti-emetic, sedation, amnesia, twilight sleep
3 Drugs for urinary incontinence
Tolteridine
Oxybutin
Solifanacin
(All musc. blockers)
3 preferred ocular muscarinic blockers
Tropilamide
Cyclopentalate
Homatropine
2 muscarinic blockers in parkinsons
Benztropine
Trihexyphenidyl
2 muscarinic blockers for bronchiolar dilation
Ipratropium
Tiotropium
2 muscarinic blockers for GI spasm
Lomotil (atropine + opioid (dihenoxylate)
Glycopyrolate
4 ganglionic blockers
Hexamethonium
Trimethaphan
Mecamylamine
Tubocurarine
Uptake 1 inhibitors
Tricyclic Antidepressants
Cocaine
Ritalin
Phenylephrine
a1 receptor agonist
For: Mydriasis
Eye vasoconstriction
Nasal Decongestant
Imadolazine derivatives
a1 agonists
Not broken down by MAO or COMT
Effect a2 at high doses
Midodrine
a1 agonist
Used for BP (esp postural)
Methoxamine
a1 agonist w/ sustained effects
Doesn't affect cardiac receptors.
clonidine
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
B1 agonist

Used to increase CO in cardiogenic shock (primary) (Increase contract w/o increasing hr)
Albuterol
Prototype B2 agonist
- Bronchiloar and uterine relaxation(prevent premature labor)
Terbutaline
Parenteral B2 agonist - Approved for asthma, used for premature labor.
Ritodrine
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
B1, and dopamine agonist
Use to increase CO in cardiogenic shock (secondary). Causes oliguria, small inc in vasoconstriction
phenoxybenzamine
a1, a2 blocker (more a1)
Effect depends on level of symp. tone
Treat pheo, sex dys, prophylactic in surgery
Phentolamine
a1,a2 blocker.
Use in pheo, sex dysfunction, tyramin hypertensive crisis.
Prazosin (_azosin)
a1 receptor blocker
- Decrease BP
- Decrease urine block (in erethra, prostate, bladder neck)
Terazosin
a1 blocker.
Treat BPH
Tamsulosin (flomax)
Block a1A receptors (in prostate/bladder)
NOT a1B (in blood vessels)
Alfuzosin
a1A antagonist

Pee.
Yohimbine
Selective a2 antagonist - Causes tachycardia, aphrodisiac
Sildenafil (Viagra)
_denafil (others)
Phosphodiesterase 5 inhibitors.
Contraindicated w/ nitrates or nonspecific a1 blockers.
Propranolol
Non selective b blocker.
Antiarrythmic, antianginal, antihypertensive, pheochromocytoma, stage fright, migraine.

CONTRA: Diabetics/asthmatics
Timolol
Nonselective B blocker
Treat open angle glaucoma via decreased secretion of aqueous humor.
Also treats migraines.
Metoprolol
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
a1 & b1 blocker
Treat hypertensive crisis
Pheochromocytoma
Tyramine
Indirect sympathomemitic
Amphetamines
Indirect acting sympathomimetics
Ephedrine
Mixed sympathomimetic.
Indirect actions
EPI actions (esp B2)
Phentermine
(works like ephedrine)
Phen in Fen-Phen
Beta stimulation blocks feeding.
Theophyline
Blocks a phosphodiesterase (increasing beta 2) - Helps in bronchodilation.
Synergistic w/ psuedoephedrine
Levefed
Norepinephrine. Used for severe hypotension (i.e. in the ICU)

Deck Info

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