Block 4 Drugs
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| Acetylsalicylate use | alleviate mild, non-visceral pain
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| Acetylsalicylate class | NSAID
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| Acetylsalicylate MOA | irreversible COX inhibitor
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| Acetylsalicylate probs | binds albumin, when saturated can enter CNS
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| NSAID MOA | inhibit COX, decrease PG synth
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| NSAID site of action | PNS
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| Acetominophen site of action | CNS
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| Ibuprofen class | NSAID
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| Ibuprofen MOA | reversible COX inhibitor
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| NSAID uses | anti-inflammatory, anti-pyretic
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| Sulindac MOA | metabolized to sulfide- NSAID
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| Sulindac class | NSAID
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| Ketorolac class | NSAID
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| NSAID probs | GI, renal, CHF, bleeding
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| COX II inhibitors | more selective for COXII, otherwise not many benefits
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| How does toxicity vary in NSAIDs | toxicity parallels half-life with chronic use
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| Acetominophen class | non-opioid analgesic
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| Acetominophen toxicity | due to glutathione depletion
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| 3 opioid branches | POMC, proenkephalin, prodynorphin
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| Enkephalins | endogenous opiods, reguate pain perception
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| Enkephalins | endogenous opioid, regulates pain pereception
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| B-endorphin | endogenous opiod, regulates stress
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| Dynorphin | endogenous opioid, regulates pain perception
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| B-endorphin source | POMC
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| Enkephalins source | unmyelinated C-fibers
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| Which opioid receptors are targeted by drugs? | mu and kappa
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| Opioid MOA | inhibit adenylate cyclase, decrease cAMP
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| Opioid cellular effects | hyperpolarization, NT release inhibition, disinhibition
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| Morphine effectiveness | better for C-fiber pain than A-delta
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| Morphine side effect | respiratory depression
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| Why is morphine not anticonvulsant? | Excreted by glucuronidation- buildup causes seizures
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| Why not give morphine with asthma? | high association with histamine release
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| When does mydriasis occur with morphine OD? | Once asphyxia occurs
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| Why does morphine cause resp depression? | medullary respiratory center becomes less sensitive to CO2
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| What morphine effects induce tolerance? | resp. depression, euphoria, analgesia
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| CV morphine side effect | orthostatic hypertension, less sensitive baroreceptor reflex
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| What morphine effects do not induce tolerance? | GI effects- constipation, reflux
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| Acute opioid toxicity | pinpoint pupils, resp depression, coma
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| When is a low dose of naloxone needed to reverse opioid OD? | in a chronic abuser
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| acute withdrawal rxn (opioids) | copious release of body fluids
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| Why choose oral opioid admin? | prolonged analgesia, less toxicity, tighter control, increased mobility
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| Why is codeine not always effective | polymorphism- some don't have P450 req to convert
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| Hydromorphone | Dilaudid
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| Meperidine | Demerol
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| Hydromorphone class | opioid receptor agonist
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| Naloxone | opioid receptor antagonist
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| Meperidine class | opioid receptor agonist
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| Fentanyl street name | China white
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| Fentanyl class | opiod receptor agonist
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| Fentanyl use | pre- post- and during surgery
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| Hydromorphone plus | very potent, no metabolites
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| Meperidine minus | euphoric- pts request it
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| Meperidine plus | fewer GI effects, used in OB
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| diphenoxylate, loperamide | Lomotil, Imodium- GI affecting opioids
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| Fentanyl plus | quick onset, no histamine release, no hemodynamic instability
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| Methadone use | oral analgesic
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| Methadone plus | less sedation than morphine
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| Methadone class | opioid receptor agonist
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| Why hydrocodone over codeine? | more effective, less GI prob, no polymorphism concern
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| Propoxyphene | Darvon
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| Propoxyphene use | weak analgesic, antitussive
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| Propoxyphene class | opioid receptor agonist
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| Pentazocine | Talwin
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| Pentazocine class | mixed opioid agonist/antagonist
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| mixed opioid ag/antag probs | resp depression, dysphoria, induce withdrawal
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| Naltrexone class | opioid receptor antagonist
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| Hydromorphone is chosen over which drug? | meperidine
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| norepinephrine class | sympathomimetic
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| epinephrine class | sympathomimetic
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| dopamine class | sympathomimetic
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| isoproterenol class | sympathomimetic
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| dobutamine class | sympathomimetic
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| phenylephrine class | sympathomimetic
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| methoxamine class | sympathomimetic
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| clonidine class | sympathomimetic
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| dexmedetomidine class | sympathomimetic
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| terbutaline class | sympathomimetic
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| albuterol class | sympathomimetic
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| ephedrine class | sympathomimetic
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| cocaine class | indirect sympathomimetic
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| imipramine class | indirect sympathomimetic
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| amphetamine class | indirect sympathomimetic
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| tyramine class | indirect sympathomimetic
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| prazosin class | a-adrenergic blocker
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| terazosin class | a-adrenergic blocker
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| doxazosin class | a-adrenergic blocker
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| phenoxybenzamine class | a-adrenergic blocker
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| phentolamine class | a-adrenergic blocker
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| tamsulosin class | a-adrenergic blocker
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| yohimbine class | a-adrenergic blocker
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| Rauwolscine class | a-adrenergic blocker
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| atipamezole class | a-adrenergic blocker
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| propranolol class | B-adrenergic blocker
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| metoprolol class | B-adrenergic blocker
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| atenolol class | B-adrenergic blocker
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| butoxamine class | B-adrenergic blocker
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| Reserpine class | adrenergic blocker
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| guanethedine class | adrenergic neuron blocker
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| sympathomimetic effect | inc. HR, inc. BP, bronchodilation
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| phenylephrine use | nasal decongestant
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| apraclonidine, brimonidine use | tx. glaucoma
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| methylphenidate use | (Ritalin) ADD
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| dextroamphetamine use | tx. narcolepsy
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| phentiramine/fenfluramine use | weight loss (phen/fen)
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| TCA MOA | serotonin/norepi reuptake inhibitors
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| desipramine class | TCA
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| amitriptyline class | TCA
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| sertraline class | TCA
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| TCA side effects | heart, dry mouth, constipation, urinary retention
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| MAOI MOA | inhibit dopamine breakdown by MAO
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| phenylzine class | MAO-A inhibitor
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| phenylzine use | tx. depression
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| selegiline class | MAO-B inhibitor
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| selegiline use | tx. Parkinson's Disease
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| MAOI side effects | acture hypertension, chronic hypotension
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| Botox | clostridium botulinum
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| Botox MOA | blocks Ca2+ mediate ACh release
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| hemicholinium MOA | blocks choline reuptake
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| Tubocurarine, pancuronium class | neuromuscular blockers
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| tubocurarine, pancuronium MOA | competitive nicotinic receptor antagonists
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| tubocurarine, pancuronium effect | flaccid paralysis
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| decamethonium, succinylcholine class | neuromuscular blockers
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| decamethonium, succinylcholine MOA | nicotinic receptor agonists, AChE resistant
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| decamethonium, succinylcholine effect | muscle paralysis
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| why does deamethonium last longer than succ? | not hydrolyzed by AChE
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| Botox class | Ganglionic blocker
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| hemicholinium class | Ganglionic blocker
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| edrophonium (Tensilon) class | short acting AChE inhibitor
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| Neostigmine class | medium acting AChE inhibitor
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| Neostigmine use | tx. Myasthenia Gravis
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| Edrophonium (Tensilon) use | diagnosis of Myasthenia Gravis
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| Pyridostigmine class | medium acting AChE inhibitor
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| Pyridostigmine use | reversal of competitive neuromuscular blockade
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| Physostigmine class | medium acting AChE inhibitor
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| Physostigmine use | tx. anticholinergic OD, glaucoma
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| Organophosphates, war chemicals | irreversible, toxic AChE inhibitors
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| AChE I side effects | parasympathetic activation
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| Bethanechol class | cholinomimetic (muscarinic receptor agonist)
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| Bethanechol use | tx. post-op, post-partum urinary retention
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| pilocarpine class | cholinomimetic (muscarinic receptor agonist)
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| pilocarpine use | tx. glaucoma
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| atropine class | anticholinergic (muscarinic receptor antag)
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| atropine use | pupillary dilation
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| scopolamine class | anticholinergic (muscarinic receptor antagonist)
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| scopolamine use | motion sickness, post-op nausea
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| ipratropium class | anticholinergic (muscarinic receptor antagonist)
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| ipratropium use | tx. bronchospasm
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| tolterodine class | anticholinergic (muscarinic antagonist)
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| tolterodine use | tx. overactive bladder
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| PCP, ketamine | NMDA antagonists- anesthetics
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| gabapentin use | tx. neuropathic pain
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| pregabalin class | Ca channel blocker
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| pregabalin use | tx. neuropathic pain
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| cocaine MOA | inhibits catecholamine reuptake
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| benzodiazepine MOA | GABAa agonist
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| ambien (zolpidem) MOA | GABAa agonist
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| Baclofen MOA | GABAb agonist
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| Selegiline class | MAO-B inhibitor
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| Bromocriptine | direct dopamine receptor agonist
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| Amantadine | blocks reuptake and enhances release of dopamine
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| trihexyphenidyl and benztropine | anti-cholinergics for PD
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| anticholinergic toxicity signs | tachycardia, urinary retention
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| Sinemet | Carbidopa/Levodopa
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