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65 Cards in this Set
- Front
- Back
What are the 4 other receptors that are involved with imipramine's side effects?
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1. Cardiac fast channels = arrhythmias, cardiotoxicity, wide QRS complex
2. muscarinic Ach receptors = flushing, hyperthermia, dilated pupils, ileus, urinary retention, sinus tachy, confusion, hallucination 3. alpha 1 receptors = hypotension, vasodilation 4. H1 receptors = sedation |
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mechanism of methadone, meperidine, dextromethorphan, codeine
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opioids open K+ channels, close Ca2+ channels --> hyperpolarization and inhibition, causing decrease synaptic transmission of ACh, NE, 5-HT, glutmate, substance P/
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opiod rx for diarrhea
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loperamide, diphenoxylate
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how do you treat a person who comes in ODing on a substance that causes:
-respiratory/CNS depresion -constipation -PINPOINT pupils |
Opioid toxicity treated with naloxone, naltrexone
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In chronic opioid use, what 3 things do you build tolerance to, what 2 things can you not develop tolerance to?
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Build tolerance to:
-CNS depression -Resp depression -cough Do NOT develop tolerance to: -miosis (pinpoint pupils) -constipation |
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Partial agonist at opioid mu receptor, agonist at kappa receptor
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Butrophanol
*used for pain- has less resp. depression than full mu agonists. |
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Tramadol
-mechanism -uses |
very weak opioid agonist- also inhibits serotonin and NE reuptake.
Used for chronic pain, has similar opioid side effects, also has decreased seizure threshold. |
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3 drugs that are 1st line for tonic clonic
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phenytoin, carbamazepine, valproic acid
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5 indications for carbamazepine
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1. tonic clonic seizures
2. partial (simple or complex) seizures 3. trigeminal neuralgia 4. diabetic neuropathy 5. mood stabilizer |
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5 classes of side effects for phenytoin
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1. neuro: nystagmus*, diplopia, ataxia, sedation, peripheral neuropathy*
2. cosemtic: gingival hyperplasia*, hirsutism*, acne 3. megaloblastic anemia 4. teratogen "fetal hydantoin syndrome" 5. SLE like syndrome* *also induces CYP450 |
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we all know agranulocytosis, aplastic anemia, liver toxicity are the 3 feared side effects of carbamazepine.
what are 5 other, less famous, side effects? |
1. diplopia, ataxia
2. teratogen (like phenytoin) 3. induces CYP450 (like phenytoin) 4. SIADH stevens-johnson syndrome |
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This drug blocks voltage gated Na+ channels and has the dreaded side effect of Stevens-Johnson syndrome
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Lamotrigine (used 2nd line for partial and tonic clonic)
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Mechanism and 3 uses of Gabapentin
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mechanism: designed as GABA analog, but ironically inhibits HVA Ca2+ channels.
Uses = -partial, tonic clonic. -peripheral neuropathy (post herpetic neuralgia) -bipolar disease. |
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Blocks Na+ and GABA
Causes mental dulling, kidney stones, weight loss |
Topiramate
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4 uses of barbituates (which increase duration of Cl- channel opening)
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1. anxiety
2. seizures partial or generalized - phenobarbital 3. insomnia 4. induction of anestheia - thiopental |
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3 epilepsy drugs that induce CYP450
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PCP induce (thus would make heparin subtherapeutic)
phenytoin, carbamazepine, phenobarbital (barbituates) |
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Use for patient with absence seizure AND has tonic clonic.
Inactivates Na+ channels, and increases GABA concentration. |
Valproic acid
*also 1st line for MYOclonic seizures |
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1st line for absence seizures
what are 5 main side effects? |
ethosuximide - blocks thalamic T-type Ca2+ channels
fatigue GI symptoms headache urticaria stevens johnson syndrome |
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rare side effect of valproic acid
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rare but fatal hepatotoxicity
also, tremor, weight gain *teratogen = neural tube defects in fetus |
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Inhibits GABA reuptake
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tiagabine
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irreversibly iinhibits GABA transaminase --> increased GABA
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vigabatrin
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4 short acting benzos
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triazolam
oxazepam midazolam alprazolam |
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3 intermediate acting benzos
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lorazepam
estazolam temazepam |
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4 long acting benzos
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diazepam
chloridazepoxide clorazepate flurazepam |
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4 clinical uses of benzos
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1. anxiolytic
2. sedative - night terrors, sleepwalking, insomnia 3. anticonvulsant (used acutely and for alcoholic DTs) 4. muscle relaxant - spasticity |
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OD of benzo rx
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flumazenil (competitive antagonist at GABA benzodiazepine receptor)
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Which are more likely for withdrwal, oxazepam or flurazepam?
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oxazepam = short acting (along with triazolam, midazolam, alprazolam)
short acting are more likely to cause withdrawl flurazepam = long acting along with diazepam, chlordiazepoxide, clorazepate |
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act via BZ1 receptor and treats insomnia with less addictive potential because it is rapidly metabolized and has less psychomotor depression.
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zolpidem (ambien), zaleplon, eszopiclone
*side effects = ataxia, headache, confusion |
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what determines rapid induction and recovery times in anesthetics?
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less solubility in blood = rapid induction and recovery times
*high blood solubility = high blood/gas partition coefficient = increased gas to saturate blood = slower onset of action |
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what determines potency in anesthestics?
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drugs with more lipid solubility = increased potency = 1/MAC (minimum alveolar conc.)
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inhaled anesthetic side effects = CV/resp depression, nausea/emesis, increased cerebral blood flow, rarely malignant hyperthermia
what are specific side effects for: -halothane -methoxyflurane -enflurane |
-halothane: fulminant hepatoxicity
-methoxyflurane: nephrotoxicity -enflurane: proconvulsant |
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thiopental has one weird side effect
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decreases cerebral blood flow
*high potency, rapid entry. effect terminated by redistribution in to tissue/fats. |
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anesthetic commonly used for endoscopy with inhaled anesthetics, can cause severe postoperative resp depression
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midazolam (short acting benzo)
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ketamine mechanism and side effects
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block NMDA receptors- cardiovascular stimulants.
cause disorientation, hallucination, bad dreams. increase cerebral blood flow. |
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order of nerve blockade with local anesthetics (esters-procaine, amides-lidocaine)
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small myelinated > small unmyelinated > large myelinated > large unmyelinated
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order of pain loss with local anesthestics (esters-procaine, amides-lidocaine)
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pain > temperature > touch > presure
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side effects of bupivicaine (amide local anesthetic) and cocaine (ester local anesthetic)
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bupivicaine = severe CV tox
cocaine = arrhythmias *all local anesthetics cause CNS excitation |
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reversal of succinylcholine phase 1 and phase 2
what happens when given cholinesterase inhibitors (neostigmine) |
phase 1 = prolonged depolarization, no antidote, block POTENTIATED by cholinesterase inhibitors
phase 2 = repolarized but blocked, neostigmine works. *general side effects of succinylcholine = hypercalcemia, hyperkalemia |
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neuromuscular blocking drugs that block ACh receptors
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tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium
*can reverse with neostigmine |
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Rx for neuroleptic malignant syndrome
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dantrolene
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3 parkinson's drugs that are dopamine agonists
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bromocriptine
pramipexole ropinirole |
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3 drugs that prevent dopamine breakdown
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selegiline = selectively inhibits MAO-B, which preferentially metabolizes dopamine ofver NE/5-HT
COMT inhibitors, prevent L-dopa degradation entacapone tolcapone |
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What side effects will NOT be prevented by carbidopa
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Carbidopa is administereed with L-Dopa to prevent peripheral conversion to dopamine, which can cause arrhythmias, vomiting, nausea.
However, it will NOT prevent axiety/agitation of parkinson's disease as these are CNS symptoms and carbidopa only works peripherally. |
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NMDA receptor antagonist for Alzheimers
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memantine
remember alzheimers = low ACh, high NE, high glutamate by blocking NMDA you can decrease the effect of the increased glutamate (which works on NMDA receptors) and help prevent excitotoxicity. side effects can include hallucinations |
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acetylcholinesterase inhibitors that treat alzheimers
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donepezil, galantamine, rivastigmine
side effects can include insomnia |
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two treatment options for huntingtons
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disease = high dopamine, low ACh, low GABA
1. reserpine + tetrabenazine - prevent neurotranmitter entry to presynpatic vesicles, amine depleting 2. haloperidol - dopamine receptor antagonist |
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major side effect of sumatriptan
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sumatriptan = 5HT IB/ID agonist which causes vasoconstruction, inhibition of trigeminal activationa and vasoactive peptide release.
used for acute migrane, cluster headaches. tox = coronary vasospasm - contraindicated in patients with CAD or prinzmetal's angina. |
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ADHD treatment
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methylphenidate (ritaline), dextroamphetamine
*can also be used for narcolepsy |
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Evolution of EPS side effects with typical antipsychotics:
4h 4d 4wk 4mo |
4h: acute dystonia (muscle spasm, stiffness, oculogyric crisis)
4d: akinesia (parkinsonian symptoms) 4wk: akathasia (restlesness) 4mo: tardative dyskinesia (lock smaking, tongue chewing) *occurs from upregulation or hypersensitivity of dopamine receptors and a decrease in cholinergic tone. |
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4 main symptoms of neuroleptic malignant syndrome
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hyperthermia (dopamine is involved in temp regulation)
rigidity autonomic instability/encephalopathy myoglobinuria |
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Other than EPS side effects and NMS, what are 4 other side effects (things blocked) by typical antipsychotics (haloperidol + -azines)
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1. endocrine side effects --> hyperprolactinemia
2. blocking muscarinic (dry mouth, constipation) 3. blocking alpha (hypotension) 4. blocking histamine (sedation) *also remember that typical antipsychotics are highly lipid soluble and are very slow to be removed by the body. |
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Which are the high potency and which are the low potency typical psychotics?
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High potency: haloperidol, trifluoperazine, fluphenazine *have more neurologic side effects (EPS)
Low potency: thioridazine, chloropromazine (non neuro side effects- anticholinergic, antihistamine, alpha blocker) |
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special side effects of chloropromazine and thirodazine (both low potency)
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chloropromazine - corneal deposits
thioridazine - retinal deposits |
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mechanism of olanzapine
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block 5-HT2, dopamine, alpha, H1 receptor
*used to treat pos + neg symptoms of schizophrenia. -Olanzapine is also used for OCD, anxiety, depression, mania, Tourette's *has less EPS/anticholinergic symptoms than typicals. |
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side effects of olanzapine and clozapine
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both olanzapine and clozapine cause weight gain.
clozapine also can cause agranulocytosis. |
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mood stabilizer for bipolar disorder and can treat SIADH
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lithium
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What are the 5 side effects of lithium
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Movement (tremor)
Nephrogenic diabetes inspidus- hypernatremia, polyuria, polydispia hypOthyroidism Pregnancy problems Fetal cardiac defects- ebstein abomaly (fucked up tricsupid valve), malformation of the great vessels |
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What is the mechanism of TCAs?
what are the names of 5 common TCAs |
imipramine (bed wetting), amitriptyline (very anticholinergic), nortryptiline (not so anticholinergic), desipramine, clomopramine (OCD), doxapine, amoxapine
block reuptake of NE + Serotonin |
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what are the 4 other things that TCA can accidentally block?
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1. Cardiac fast channels = arrhythmias, cardiotoxicity, wide QRS complex
2. muscarinic ACh receptor = flushing, hyperthermia, dilated pupils, ileus, urinary retention, sinus tachy, confusion, hallucination 3. alpha 1 block = hypotension 4. H1 block = sedation |
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which drug TCA has the least anticholinergic effects?
what about least sedating? |
amitriptyline has more anticholinergic side effects than nortriptyline
desipramine is the least sedating and has lower seizure threshold (desis keep you awake) |
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rescue for TCA cardiotoxicity (wide QRS from blocking Na+ fast channels)
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NaHCO3
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patient presents with hyperthermia, muscle rigidity, CV collapse, flushing, diarrhea, seizures. what is the treatment?
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serotonin syndrome - occurs when you comine MAOi + SSRI
treat with cyproheptadine (5-HT2 receptor antagonist) *differentiate from NMS because it has flushing, diarrhea, seizures |
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2 SNRIs and their main toxicity
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venlafaxine (depression + GAD), duloxetine (depression + diabetic peripheral neuropathy)
main tox: high BP |
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name the 4 SSRIs
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fluoxetine, paroxetine, sertraline, citaprolam
rx for depression, OCD, bulimia, social phobias, PTSD, panic disorder |
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4 common MAOi's
what is the mechanism |
phenezline, tranylcypromine, isocarboxazid, selegiline (selective for dopamine)
*mechanism: inhibit breakdown of NE, serotonin, dopamine |