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karennnb
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parasymp control of eye
M3: lacrimation, miosis dec IOP
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symp control of eye
a1: mydriasis, dec IOP / b: inc IOP
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parasymp control of heart
M3: slows
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symp control of heart
B1: inc HR and force
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parasymp control of lung
M3: bronchostriction
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symp control of lung
B2: bronchodilation
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parasymp control of GI
M3: SLUD
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symp control of GI
a1: bladder constrictions (holding your pee) so a1 antagonists good for BPH
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symp control of blood vessels
a1: HTN
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symp control of kidney
b1: inc renin, inc BP, D1 DA activation
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a methyl groups on ACh
Nicotinic selective
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b methyl groups on ACh
muscarinic selective
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direct parasympathomimetics indications
glaucoma, miosis
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direct parasympathomimetics contraindications
asthma COPD
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direct parasympathomimetics SE
SLUD, confusion
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Varenicline
special direct parasympathomimetic bc it acts on NICOTINIC receptors
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use atropine for overdose of these indirect parasympathomimetics
stigmines, memantine
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scopolamine
parasympatholytic for sea sickness
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what to use as anti-GI spasms
quaternary amines (stays in gut, cant reach brain)
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parasympatholytic SE
sedation, dry mouth, blurry eyes, coma, death, tachycardia (block M2 in heart)
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ganglionic blocker structure
n= 5 or 6
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neuromuscular blocker structure
n = 7 or greater
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ganglionic nicotinic blocker indication
controlled surgical hypotension
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neuromuscular nicotinic blockers
succinylcholine, Curiums, caution DEATH by resp paralysis
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NET and DAT
uptake 1; presynaptic
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uptake 2
cationic; postsynaptic
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VMA
from MAO and COMT; too much in urine = pheochromacytoma
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a1 receptors
vessels; inc BP, dec aq humor, mydriasis
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a2 receptors
brain; presynaptic; dec BP and HR
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b1 receptors
heart, kidney, inc HR and force and BP (renin)
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b2 receptors
lungs, inc bronchodilation, inc aq humor
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psychostimulant indications
ADHD, narcolepsy
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droperidol
typical antispychotic for antiemesis
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typical antipsychotics
D2 so EPS that may progress to TARDIVE DYS (permanent)
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atypical antipsychotics
5HT2A, less EPS and TD but weight gain and diabetes; treat negative sx better
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MAOIs
irreversible; cheese syndrome (inc tyramine = inc BP, HR)
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miosis
circular muscle, M3
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mydriasis
radial muscle, a1
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varenicline
nicotinic; direct parasympathomimetic; smoking cessation
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zolines
partial a1 agonists; TACHY; eye drops and nose sprays
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phenylephrine
full a1 agonist; decongestant and glaucoma
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zosin indications
HTN, BPH but causes reflex tachy
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Phentolamine
A1 and a2 antagonist
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Phenoxybenzamine
Irreversible a antagonist for pheochromacytoma
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Clonidine
A2 agonist; HTN; alcohol withdrawal
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Guanbenz
A2 agonist; HTN; alcohol withdrawal
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Tizanidine
A2 agonist; HTN; alcohol withdrawal; muscle relaxer
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Methyldopa
A2 agonist; HTN; alcohol withdrawal
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A2 agonist SE
Causes WITHDRAWAL themselves
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Yohimbine
Indole alkaloid; a2antagonist; inc BP and HR
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Isoproterenol
Nonselective b agonist; asthma COPD, inc HR and BP
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Metaproterenol
B2 agonist
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Dobutamine
Mixed A1 b1; POSITIVE IONOTROPIC; no HR change; for cardiac failure
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Propranolol
Nonselective b blocker
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SE of all b antagonist
Bradycardia, bronchostriction, WITHDRAWAL (can be used for glaucoma)
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Pindolol
B1 b2 ; partial agonist
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Cardeolol
B1 b2 ; partial agonist
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Esmolol
B1 agonist; short ester that�s CLEAVED. IV infusion to stop heart fast
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Labetalol
Mixed a1 b; no HR effect; selectively treats BP
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Carvedilol
Mixed a1 b; no HR effect; selective treats Bp
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Reserpine
Indol alkaloid; blocks vesicular storage of DA, NE, 5ht; sympatholytic (dec BP and HR)
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Reserpine SE
PD-like sx and depression
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Cocaine
DAT/NET blocker; psychostimulant
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Methylphenidate
DAT/NET blocker; psychostimulant
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Modafinil
DAT/NET blocker; psychostimulant
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Sibutramine
DAT/NET blocker; psychostimulant
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Atomoxetine
NET selective; adhd ; psychostimulant
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Psychostimulants
ADHD; narc; inc DA�abuse
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Apomorphine
D1 d2 agonist; parkinsons
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Bromocriptine
Ergolide; d2 agonist; PD
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Pergolide
Ergolide; d2 agonist; PD
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Ropirinole
D2 agonist, PD
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Pramipexole
D2 agonist; PD
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Dihydrexidine
D1; Nichols
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Selegiline
Mao b inhib , may slow progression;neuroprotection
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Rasalgine
Mao b inhib; may slow progression; neuroprotective
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Psychadelics
5ht2a agonists; tachy, tolerance, but no abuse because no DA inc
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Psilocibine
Tryptamine psychedelic
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Mescaline
Phenethylamine psychedelic
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Mdma
5ht release (serotonin syn, deaths from dehydration and hyperthermia), da releaser (abuse)
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Haloperidol
Typical antipsychotic; d2, EPS
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Chlorpromazine
Typical antipsychotic; d2, EPS
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Thiothixene
Typical antipsychotic; d2, EPS
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Droperidol
Typical antipsychotic; d2, EPS; ANTIEMESIS
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Typical antispsychotics
D2, eps, tardive dysk
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Clozapine
Atypical antipsychotic
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Olanzapine
Atypical antipsychotic; clozapine bioisostere
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Quetiapine
Atypical antipsychotic
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Risperadone
Atypical antipsychotic
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Aripiprazole
Atypical antipsychotic; partial d2 agonist; 5ht1a (anxiety); LOTS OF USES
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Atypicals
5ht2a, less EPS and tardive but wt gain, diabetes. Treat negative sx better
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Phenalzine
MAOI antidepressant; cheese syndrome
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Selegiline
Maoi antidepressant; cheese syndrome
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Triamcypramine
Maoi antidepressant; cheese syndrome
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Moclebomide
Maoi antidepressant; reversible so no cheese syn
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Cheese syndrome
Inc tyramine;; inc BP and HR; from IRREVERSIBLE MAOIs
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Desipramine
TCA secondary
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Amitryptiline
Tca tertiary (secondary is nortriptyline)
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Nortryptiline
Secondary TCa
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SSRIs
SERT blockers with no antimusc SE but causes ANXIETY, SEXUAL DYSFCT, insomnia, tremors (xetines)
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TCA SE
Antimuscarinic, TACHY, antiSLUD
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Venlafaxine
NET SERT (dual)
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Desvenlafaxine
NET SERT dual
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Dual inhibitors
NET SERT (no antimuscarinic SE) ; net blockade can be used for neuropathic pain
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Reboxetine
NET selective antidepressant
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Atomoxetine
NET selective antidepressant
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Bupropion
DAT antidepressant; smoking cessation; gad
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Trazodone, nefazodone, mirtazapine, maprotiline
Depression
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Lithium
Dec IP turnover, small therapeutic index (toxic); mania
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Mania/bipolar other txs
Anticonvulsants; antidepressant + antipsychotic; one drug with both
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Antidepressant for mania
Fluoxetine
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Antipsychotic for mania
Olanzapine
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Antidepressant + antipsychotic for mania
Aripiprazole; partial
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Caffeine
Adenosine antagonist
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Fomepizole
ADH inhib; inc etOH; ethylene glycol and metOH poisoning
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Disulfuram
Inc acetyl aldehyde ; bad etOH effects
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MEOS
1st order; cyp2e1, on at higher conc
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EtOH moa
Enhance cl influx (gabaA)and blocks glu recep (NMDA)
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etOH withdrawal tx
bzds, pheny, naltrexone, ondansetron, disulfuram, acamprosate, baclofen, Chantix
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ondansetron for etOH withdrawal
blocks NV via 5ht3
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acamprosate for etOH withdrawal
glu blocker
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baclofen for etoh withdrawal
GABAb; heterodimer
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BZDs
Sedative hypnotics; GABAa PAM (inc GABA affinity, channel opening and cl influx)
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Bbts
Sedative hypnotic; GABA A pam, PLUS channel stays open longer; small TI
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Z hypnotics
A1 selective and controls sleeps
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Midalozam
Short acting bzd
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Z drugs
Zolpidem, zaleplone, esszopicline (long term)
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flumazenil
bzd antagonist, neutrol allosteric modulator, used for BZD or z hypnotic overdose
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GHD
gabaA PAM, gabaB agonist, no antidote, used for daytime sleepiness (GBL = prodrug)
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ramelteon
melatonin agonist; MT1 and 2; modulate circadian rhythm; no dependence, abuse; used for JET LAG
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anxiolytic for panic
BZDs only!!
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Buspirone
5ht1a partial presynaptic ; anxiolytic
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Other anxiolytics
Ssris, tcas, snris, propranolol (can penetrate brain;for acute)
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Phenytoin
Na channel ; prolongs inactivation; autoinducer; nonlinear- titrate
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Phenytoin se
Hirsutism, gingival hyperplasia
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Fosphenytoin
Prodrug; phosphatases
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Cbz
Anticonvulsant; na channel block; bipolar; neuralgia; autoinducer of 3a4
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Phenobarb
gabaA; autoinducer
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valproate;
na, ca block, inc gaba, ABSENCE; inhibits pheny and cbz metabolism (c/i)
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ethosuximide
ca selective; absence
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diazepam/any bzd for anticonvulsants
status epilepticus; quick
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gabapentin; pregabalin
inc gaba; adjucnts
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felbamate; topiramate
block glu; antipsychotic; nmda and ampa
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diazepam spasmolydic
gaba a, spinal cord only
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baclofen spasmolytic
gaba b; spinal cord only
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tizanidine spasmolytic
a2 agonist; spinal cord only
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cyclobenzaprine
brain; not good for neuralgias; spasmolytic
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carisoprodol
brain, not good for neuralgias; spasmolytic
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dantrolene
muscle ; spasmolytic; dec ca from sr; antidote for malig hypertherm
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propofol
iv anesthetic; gaba a; etoh like; antiemetic
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etomidate
gaba a iv anesthetic
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midazolam, thiopental
adjunct anes; pre-op; amnesia
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balanced anesthesia
anesthetic, analgesia (NSAID opiate) , antiemetic (propofol)/droperdiol, amnesia (midazolam, thiopental)
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local anes
na blockers; work best unionized; caines; vasoconstriction at site
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