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Block 4 Drugs

Acetylsalicylate use alleviate mild, non-visceral pain
Acetylsalicylate class NSAID
Acetylsalicylate MOA irreversible COX inhibitor
Acetylsalicylate probs binds albumin, when saturated can enter CNS
NSAID MOA inhibit COX, decrease PG synth
NSAID site of action PNS
Acetominophen site of action CNS
Ibuprofen class NSAID
Ibuprofen MOA reversible COX inhibitor
NSAID uses anti-inflammatory, anti-pyretic
Sulindac MOA metabolized to sulfide- NSAID
Sulindac class NSAID
Ketorolac class NSAID
NSAID probs GI, renal, CHF, bleeding
COX II inhibitors more selective for COXII, otherwise not many benefits
How does toxicity vary in NSAIDs toxicity parallels half-life with chronic use
Acetominophen class non-opioid analgesic
Acetominophen toxicity due to glutathione depletion
3 opioid branches POMC, proenkephalin, prodynorphin
Enkephalins endogenous opiods, reguate pain perception
Enkephalins endogenous opioid, regulates pain pereception
B-endorphin endogenous opiod, regulates stress
Dynorphin endogenous opioid, regulates pain perception
B-endorphin source POMC
Enkephalins source unmyelinated C-fibers
Which opioid receptors are targeted by drugs? mu and kappa
Opioid MOA inhibit adenylate cyclase, decrease cAMP
Opioid cellular effects hyperpolarization, NT release inhibition, disinhibition
Morphine effectiveness better for C-fiber pain than A-delta
Morphine side effect respiratory depression
Why is morphine not anticonvulsant? Excreted by glucuronidation- buildup causes seizures
Why not give morphine with asthma? high association with histamine release
When does mydriasis occur with morphine OD? Once asphyxia occurs
Why does morphine cause resp depression? medullary respiratory center becomes less sensitive to CO2
What morphine effects induce tolerance? resp. depression, euphoria, analgesia
CV morphine side effect orthostatic hypertension, less sensitive baroreceptor reflex
What morphine effects do not induce tolerance? GI effects- constipation, reflux
Acute opioid toxicity pinpoint pupils, resp depression, coma
When is a low dose of naloxone needed to reverse opioid OD? in a chronic abuser
acute withdrawal rxn (opioids) copious release of body fluids
Why choose oral opioid admin? prolonged analgesia, less toxicity, tighter control, increased mobility
Why is codeine not always effective polymorphism- some don't have P450 req to convert
Hydromorphone Dilaudid
Meperidine Demerol
Hydromorphone class opioid receptor agonist
Naloxone opioid receptor antagonist
Meperidine class opioid receptor agonist
Fentanyl street name China white
Fentanyl class opiod receptor agonist
Fentanyl use pre- post- and during surgery
Hydromorphone plus very potent, no metabolites
Meperidine minus euphoric- pts request it
Meperidine plus fewer GI effects, used in OB
diphenoxylate, loperamide Lomotil, Imodium- GI affecting opioids
Fentanyl plus quick onset, no histamine release, no hemodynamic instability
Methadone use oral analgesic
Methadone plus less sedation than morphine
Methadone class opioid receptor agonist
Why hydrocodone over codeine? more effective, less GI prob, no polymorphism concern
Propoxyphene Darvon
Propoxyphene use weak analgesic, antitussive
Propoxyphene class opioid receptor agonist
Pentazocine Talwin
Pentazocine class mixed opioid agonist/antagonist
mixed opioid ag/antag probs resp depression, dysphoria, induce withdrawal
Naltrexone class opioid receptor antagonist
Hydromorphone is chosen over which drug? meperidine
norepinephrine class sympathomimetic
epinephrine class sympathomimetic
dopamine class sympathomimetic
isoproterenol class sympathomimetic
dobutamine class sympathomimetic
phenylephrine class sympathomimetic
methoxamine class sympathomimetic
clonidine class sympathomimetic
dexmedetomidine class sympathomimetic
terbutaline class sympathomimetic
albuterol class sympathomimetic
ephedrine class sympathomimetic
cocaine class indirect sympathomimetic
imipramine class indirect sympathomimetic
amphetamine class indirect sympathomimetic
tyramine class indirect sympathomimetic
prazosin class a-adrenergic blocker
terazosin class a-adrenergic blocker
doxazosin class a-adrenergic blocker
phenoxybenzamine class a-adrenergic blocker
phentolamine class a-adrenergic blocker
tamsulosin class a-adrenergic blocker
yohimbine class a-adrenergic blocker
Rauwolscine class a-adrenergic blocker
atipamezole class a-adrenergic blocker
propranolol class B-adrenergic blocker
metoprolol class B-adrenergic blocker
atenolol class B-adrenergic blocker
butoxamine class B-adrenergic blocker
Reserpine class adrenergic blocker
guanethedine class adrenergic neuron blocker
sympathomimetic effect inc. HR, inc. BP, bronchodilation
phenylephrine use nasal decongestant
apraclonidine, brimonidine use tx. glaucoma
methylphenidate use (Ritalin) ADD
dextroamphetamine use tx. narcolepsy
phentiramine/fenfluramine use weight loss (phen/fen)
TCA MOA serotonin/norepi reuptake inhibitors
desipramine class TCA
amitriptyline class TCA
sertraline class TCA
TCA side effects heart, dry mouth, constipation, urinary retention
MAOI MOA inhibit dopamine breakdown by MAO
phenylzine class MAO-A inhibitor
phenylzine use tx. depression
selegiline class MAO-B inhibitor
selegiline use tx. Parkinson's Disease
MAOI side effects acture hypertension, chronic hypotension
Botox clostridium botulinum
Botox MOA blocks Ca2+ mediate ACh release
hemicholinium MOA blocks choline reuptake
Tubocurarine, pancuronium class neuromuscular blockers
tubocurarine, pancuronium MOA competitive nicotinic receptor antagonists
tubocurarine, pancuronium effect flaccid paralysis
decamethonium, succinylcholine class neuromuscular blockers
decamethonium, succinylcholine MOA nicotinic receptor agonists, AChE resistant
decamethonium, succinylcholine effect muscle paralysis
why does deamethonium last longer than succ? not hydrolyzed by AChE
Botox class Ganglionic blocker
hemicholinium class Ganglionic blocker
edrophonium (Tensilon) class short acting AChE inhibitor
Neostigmine class medium acting AChE inhibitor
Neostigmine use tx. Myasthenia Gravis
Edrophonium (Tensilon) use diagnosis of Myasthenia Gravis
Pyridostigmine class medium acting AChE inhibitor
Pyridostigmine use reversal of competitive neuromuscular blockade
Physostigmine class medium acting AChE inhibitor
Physostigmine use tx. anticholinergic OD, glaucoma
Organophosphates, war chemicals irreversible, toxic AChE inhibitors
AChE I side effects parasympathetic activation
Bethanechol class cholinomimetic (muscarinic receptor agonist)
Bethanechol use tx. post-op, post-partum urinary retention
pilocarpine class cholinomimetic (muscarinic receptor agonist)
pilocarpine use tx. glaucoma
atropine class anticholinergic (muscarinic receptor antag)
atropine use pupillary dilation
scopolamine class anticholinergic (muscarinic receptor antagonist)
scopolamine use motion sickness, post-op nausea
ipratropium class anticholinergic (muscarinic receptor antagonist)
ipratropium use tx. bronchospasm
tolterodine class anticholinergic (muscarinic antagonist)
tolterodine use tx. overactive bladder
PCP, ketamine NMDA antagonists- anesthetics
gabapentin use tx. neuropathic pain
pregabalin class Ca channel blocker
pregabalin use tx. neuropathic pain
cocaine MOA inhibits catecholamine reuptake
benzodiazepine MOA GABAa agonist
ambien (zolpidem) MOA GABAa agonist
Baclofen MOA GABAb agonist
Selegiline class MAO-B inhibitor
Bromocriptine direct dopamine receptor agonist
Amantadine blocks reuptake and enhances release of dopamine
trihexyphenidyl and benztropine anti-cholinergics for PD
anticholinergic toxicity signs tachycardia, urinary retention
Sinemet Carbidopa/Levodopa
Created by: glavik