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blocks negative feedback receptors enhances NE release by blocking inhibitory presynaptic alpha2-adrenoceptors |
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weight gain block of central 5HT2 receptors stimulate appetite and weight gain |
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stimulation of 5HT3 receptors by serotonin suppresses appetite and cause nausea/vomiting s/e usually dissipates after several wks |
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Some Patients Can Feel Fine Eventually Sertraline Paroxetine Citalopram Fluoxetine Fluvoxamine Escitalopram |
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SNRI lower doses - blocks 5HT uptake higher doses - blocks 5HT/NE uptake |
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which antidepressant is dose dependent? |
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venlafaxine low doses - 5HT hight doses - NE |
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desipramine (NE) imipramine(NE/5HT) clomipramine(5HT/NE) |
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MAOI irreversible inhibitor of monoamine oxidase |
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antidepressant alpha 2 adronoceptor agonist |
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block muscarinic receptors -> dry mouth, urinary retention, blurred vision, constipation, memory impairment, sexual dysfunction; H1 histaminergic -> sedation, weight gain; alpha1 adrenergic -> orthostatic hypotension, sexual dysfunction; CV - AV block in pts w/ cardiac dz; arrhythmias in OD CNS - tremors, mania in bipolar pts, lower seizure threshold, death in OD |
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hepatic toxicity (phenelzine) CNS: tremors, insomnia, agitation CV: orthostatic hypotension "cheese reaction" - ingestion of sympathomimetic amines (tyramine) normally metabolized by MAO in GI, but since MAO is inhibited, releases more NE which raises BP |
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s/e of n/v, sex dysfxn, asthenia |
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SSRIs (sertraline, paroxetine, citaloopram, fluoxetine, fluvoxamine, escitalopram) venlafaxine(SNRI) |
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list classes of antianxiety drugs |
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Definition
benzodiaepines clomipramine SSRIs buspirone z drugs flumazenil ramelteon |
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Definition
bind at BZ receptor site on GABA-A (between alpha and gamma subunits) increase probability of channel opening so chloride enters producing hyperpolarization and inhibitory effects |
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pharmacological effects of BZs |
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Definition
1. sedative-hypnotic 2. anti-anxiety 3. anti-convulsant 4. muscle relaxant 5. anterograde amnesia |
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Definition
zolpidem zaleplon eszopiclone |
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MOA of Z drugs zolpidem, zaleplon, eszopiclone |
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Definition
BZ receptor agonist, but have different structure |
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difference between Z drugs (zolpidem, zaleplon, eszopiclone) and benzodiazepams |
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Definition
z drugs have less abuse potential, little effect on sleep stages, no alcolhol potentiation do NOT exert anti-anxiety, anticonvulsant, or skeletal muscle relaxant effects |
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Definition
melatonin receptor agonist no abuse potential |
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DOC for anxiety in older patients why |
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Definition
oxazepam metabolized via glucuronidation, which isn't decreased w/ age (oxidation is) |
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sx of withdrawal from BZs |
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Definition
flu like muscle cramps, abdominal discomfort, diarrhea, rarely seizures |
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BZ antagonist use for BZ OD, but has short t1/2 |
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partial agonist at 5HT1A receptor coupled to K channels hyperpolarizes neurons via enhancement of K conductance |
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anti-anxiety no drug dependence or withdrawal takes 4-8 wks to be effective partial agonist at 5HT receptors coupled to K channels |
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clomipramine (TCA) SSRIs (fluoxetine, fluvoxamine, paroxetine, sertraline) MUST inhibit serotonin reuptake |
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TCA used to tx OCD potent SRI |
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BZs SSRIs (fluoxetine, paroxetine, sertraline, fluvoxamine) venlafaxine (dose dependent SNRI) buspirone (5HT/K channel) |
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SSRIs(fluoxetine, paroxetine, sertraline, fluvoxamine) BZs(alprazolam, clonazepam) TCAs(clomipramine) |
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Definition
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Definition
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typical antipsychotic drugs |
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Definition
chlorpromazine (low potency) haloperidol (high potency) |
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Term
atypical antipsychotic drugs |
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Definition
clozapine (D2/5HT2 antagonist) risperidone (D2/5HT2 antagonist) olanzepine (D2/5HT2 antagonist) quetiapine aripiprazol (D2 partial agonist/5HT2 antagonist) ziprasidone |
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Term
which antipsychotics decrease positive symptoms and improve negative symptoms? |
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Definition
atypical (clozapine, risperidone, olanzepine, quetiapin, aripiprazole, ziprasidone) |
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Term
how are benzodiazepams and buspirone similar? |
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Definition
hyperpolarize cells and suppress neuronal firing BZs - increases chloride conductance buspirone - increses potassium conductance |
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where is site of action of atypicals - improve cognitive dysfunction and negative sx? |
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Definition
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where is the dopamine problem in schizophrenic brains? |
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Definition
excessive DA activity in limbic system -> postive psychotic sx reduced DA activity in prefrontal cortex -> negative sx and cognitive defects |
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Term
what are the 4 DA pathways in the CNS |
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Definition
1. nigrostriatal pathway (midbrain->basal ganglia) -> motor fxn 2. mesolimbic projections (midbrain->limbic system) -> arousal, motivation, reward 3. mesocortical projections(midbrain->frontal cortex) -> cognition, motivation 4. tuberoinfundibular pathway (hypothalamus->pituitary gland) -> inhibit prolactin secretion |
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Definition
atypical antipsychotic partial agonist at D2 receptors - acts as agonist when little DA is being released, but acts as antagonist when excessive DA is being released |
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chronic tx w/ typical antipsychotics (chlorpromazine, haloperidol) decreases dopaminergic cell firing in which pathways? |
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Definition
nigrostriatal (midbrain->basal ganglia; motor fxn) mesocortical(midbrain-> frontal ctx; cognition, motivation) |
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chronic tx w/ atypical antipsychotics (clozapine) decreases dopaminergic cell firing in which pathways? |
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Definition
only mesolimbic (arousal, motivation, reward) |
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Term
which dopaminergic pathway to we want to decrease activity of in schizophrenia? |
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Definition
limbic system - overactivity -> positive psychotic sx |
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why dont we want to decrease DA activity in the frontal cortex, basal ganglia, or hypothalamus? |
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Definition
frontal cortex - negative sx and cognitive defects basal ganglia - EPS hypothalamus - prolactin secretion |
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Term
s/e of typical antipsychotics (chlorpromazine, haloperidol) |
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Definition
antiadrenergic: sedation, orthostatic hypotension anticholinergic: dry mouth, blurred vision, urinary retention, sinus tachycardia, constipation antihistimine: sedation, weight gain general: photosensitivity, jaundice, arrhythmias, agranulocytosis endocrine: gynecomastia, galactorrhea, amenorrhea, weight gain EPS: dystonia, pseudoparkinsonism, akathisia, tarditive dyskinesias |
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s/e of low potency (chlorpromazine)vs high potency (haloperidol) typical antipsychotics |
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Definition
low: more anticholinergic, more sedative, more orthostatic hypotension high: more likely to produce EPS |
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Definition
antiadrenergic, cholinergic, histamine less EPS, no TD weight gain neuroleptic malignant syndrome |
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Term
which antipsychotics are not anticholinergic? |
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Definition
risperidone and quetiapine |
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Term
which antipsychotic is very antihistaminic? |
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Definition
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what is a serious s/e of clozapine? |
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Definition
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Term
prolactin s/e are seen in which drugs? |
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Definition
typicals (chlorpromazine and haloperidol) atypicals - risperidone (NOT clozapin, olanzapine, or quetiapine) |
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Term
which antipsychotics cause weight gain? |
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Definition
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Term
what are 3 tx choices for bipolar? |
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Definition
valproate (mania) + lamotrigine (depression
atypical antipsychotics (mania) + lamotrigine (depression)
aripiperazole (mania and depression) |
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Term
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Definition
anticonvulsant used to tx mania in bipolar |
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anticonvulsant used to tx mania in bipolar induces liver enzymes -> drug-drug interactions |
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Definition
atypical antipsychotic used to tx schizophrenia or mania and depression in bipolar |
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Definition
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Definition
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tx for absence seizures if pt can't tolerate ethosuximide? |
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Definition
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benzodiazepines are use to treat what types of seizures? |
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Definition
all generalized seizures except tonic-clonic |
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Term
which drugs have the broadest spectrum of anti-seizure activity? |
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Definition
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Definition
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brief loss of awareness, sometimes w/ eye-blinking or lip-smacking, but w/o loss of consciousness or body tone, almost always in young chilcren |
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Definition
absence (petit mal) seizure tx w/ ethosuximide |
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Term
DOC for generalized tonic-clonic seizures |
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Definition
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Term
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Definition
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DOC for trigeminal neuralgia |
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Definition
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Term
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Definition
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tx of status epilepticus if lorazepam or diazepam doesn't work |
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Definition
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Term
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Definition
prolong state of Na channel activation -> reduce frequency at which neurons may generate repetitive action potentials |
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Term
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Definition
prolong state of Na channel activation |
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Term
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Definition
prolong state of Na channel inactivation |
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Term
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Definition
prolong state of Na channel inactivation |
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Term
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Definition
prolong state of Na channel inactivation |
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Term
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Definition
prolong state of Na channel inactivation |
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Term
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Definition
blocks glutamate (excitatory) receptor acts as Kainate receptor antagonist |
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Term
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Definition
reduce low threshold calcium (T)currents |
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Term
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Definition
enhance GABA mediated increases in Cl conductance |
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Term
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Definition
increase frequency of GABA channel opening |
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Term
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Definition
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Term
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Definition
hirsutism, gingival hyperplasia, osteomalacia, megaloblastic anemia |
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Term
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Definition
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Definition
bone marrow depression, aplastic anemia, agranulocytosis, hyponatremia |
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Term
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Definition
osteomalacia, megaloblastic anemia, hemorrhage in newborn, prophyria, CNS depression if combined w/ alcohol |
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Term
benztropine tx for: MOA: effect: |
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Definition
parkinsons muscarinic cholinergic antagonist balance DA/ACh ssytems by reducing cholinergic dominance |
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Term
diphenhydramine tx: MOA: effect: |
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Definition
parkinsons antihistimine central muscarinic blockade |
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Definition
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Term
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Definition
carbidopa is peripheral DOPA decarboxylase inhibitor |
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Term
bromocriptine tx: MOA: effect: |
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Definition
parkinsons dopamine agonist stimulates D2 receptors directly |
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Term
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Definition
parkinsons dopamine agonist |
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Term
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Definition
monoamine oxidase B inhibitors elevate DA levels, possible neuroprotective action |
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Term
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Definition
parkinsons catechol-o-methyltransferase inhibitor anjunct to levodopa/carbidopa therapy; blocks peripheral conversion of L-dopa to O-methyl dopa |
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Term
how does carbidopa alter metabolism of L-dopa? |
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Definition
carbidopa is a DOPA decarboxylase inhibitor that doesn't cross the BBB and blocks peripheral conversion of L-dopa to DA -> decrease s/e, increase amt of dopa going to brain |
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Term
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Definition
release catecholamines from intraneuronal stores block catecholamine reuptake prolong action of catecholamines at the synapse |
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Term
sx of actue amphetamine toxicity |
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Definition
marked CNS stimulation paranoid psychosis hypertensive crisis, tachycardia, arrhythmias hyperthermia convulsions, coma |
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Term
sx of chronic toxicity of amphetamines |
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Definition
psychological and physiological dependence amphetamine psychosis - hallucinations, delusions of persecution, feeling of omnipotence |
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Term
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Definition
amphetamine dextroamphetamine methylphenidate |
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Term
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Definition
ritalin tx of ADHD release NE and DA from neurons and block reuptake |
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Term
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Definition
tx of narcolepsy (NOT for ADD) releases DA, NE, and 5HT in different areas of the brain |
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Term
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Definition
modafanil release DA, NE, 5HT in different areas of the brain |
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Term
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Definition
caffeine theophylline (aminophylline) |
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Term
sites of action of aspirin and ibuprofin |
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Definition
central and peripheral prostaglandin synthesis |
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Term
site of action of acetaminophen |
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Definition
central prostaglandin synthase |
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Term
nite of action of local anesthetics (lidocaine) |
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Definition
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Term
site of action of genral anesthetics (sevoflurane, desflurane) |
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Definition
K, Ca, Na channels, GABA-A receptore-Cl channel system |
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Term
site of action of injectable anesthetics (propofol, etomidate, thiopental) |
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Definition
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Term
site of action of ketamine |
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Definition
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Term
site of action of methadone |
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Definition
opiate receptors and NMDA receptors |
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Term
site of action of tramadol |
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Definition
opiate receptors and 5HT and NE reuptake |
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Term
renal excretion of aspirin is dependent on ? |
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Definition
pH more salicylate is excreted in alkaline urine |
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Term
MOA of salicylates (aspirin) and propionic acid (ibuprofin) |
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Definition
inhibit prostaglandin synthase cox I and II at central and peripherla sites |
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Term
what's the difference between COX I and II? |
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Definition
cox II: inducible, responsible for inflammatory response cox I: constitutive, beneficial in gastric mucosa and kidney |
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Term
what does aspirin do that ibuprofen doesnt? |
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Definition
decrease platelet aggregation -> protect against stroke and MI irreversibly inhibits cox II in platelets and blocks synthesis of thromboxane A2 |
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Term
what are the s/e of aspirin and ibuprofin |
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Definition
both - reduction in renal blood flow and edema aspirin - Rey's syndrome, prolonged bleeding, gastric irritation ibuprofen - birth defects |
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Term
what causes drug interactions with aspirin/ibuprofen |
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Definition
highly bound to plasma proteins so displace anticoagulants, phenytoin, etc |
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Term
how is acetaminophen different from aspirin and ibuprofen? |
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Definition
acetaminophen doesn't have anti-inflammatory properties |
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Term
toxicity of acetaminophen |
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Definition
hepatic glutathione depletion -> hepatic necrosis |
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Term
long-term abuse of acetaminophen can lead to |
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Definition
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Term
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Definition
inhibit cox I and II mediated prostaglandin synthesis |
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Term
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Definition
short term management of severe pain analgesic much more than antipyretic or anti-inflammatory |
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Term
areas of the CNS involving pain signal transmission |
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Definition
dorsal horn of spinal cord periaqueductal gray rostral ventral medulla thalamic nuclei |
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Term
what type of receptors do opiates bind to? |
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Definition
GTP dependent Protein Coupled Receptors |
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Term
what are pre- and post- synaptic actions of opiate agonists? |
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Definition
pre: decrease voltage gated Ca influx and reduce excitatory neurotransmitter release post: increase K conductance via activation of receptor operated K currents leading to hyperpolarization and reduction in responsiveness of postsynaptic neuron |
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Term
how do opiates cause analgesia |
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Definition
inhibit nociceptive reflexes at spinal and supraspinal sites acting at mu receptors dont feel pain, dont care about pain |
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Term
how do narcotic analgesics cause respiratory depression |
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Definition
decreased sensitivity of CNS respiratory center chemoreceptors to CO2 direct effects to decrease respiratory rhythmic cycle |
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Term
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Definition
morphine fentanyl methadone |
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Term
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Definition
"Partially Blocks Bummer Narcotics" pentazocine butorphanol buprenorphine nalbuphine |
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Term
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Definition
naloxone naltrexone nalmefene |
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Term
mechanism for tolerance of opiates |
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Definition
nitric oxide mediated reduction in glutamate (NMDA) reeptor ion channel function w/ increased drug use |
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Term
why are narcotic analgesics contraindicated in head injury? |
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Definition
respiratory depression -> increased CO2 -> increased cerebral blood floow -> increased intracranial pressure |
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Term
what is the only opiate that doesn't cause pinpoint pupils? |
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Definition
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Term
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Definition
partial opiate agonist use to decrease opiate craving in addicts |
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Term
2 types of local anesthetics |
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Definition
esters - procaine amides - lidocaine |
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Term
esters (procain) metabolized by |
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Definition
plasma cholinesterase -> kidney |
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Term
amides (lidocaine) metabolized by |
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Definition
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Term
amides (lidocaine) metabolized by |
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Definition
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Term
amides (lidocaine) metabolized by |
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Definition
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Term
amides (lidocaine) metabolized by |
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Definition
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Term
esters (procain) metabolized by |
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Definition
plasma cholinesterase -> kidney |
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Term
how does pH affect local anesthetics? |
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Definition
uncharged (lipophilic) base penetrates across the nerve sheath water soluble (charged) form binds to active site |
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Term
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Definition
bind to and block voltage gated Na channels thereby blocking Na conductance and the ability of nerve fibers to initiate and conduct action potentials |
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Term
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Definition
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Term
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Definition
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Term
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Definition
midozolam - benzodiazepine - antianxiety propofol - anesthetic etomidate - anesthetic ketamine - dissociative anesthetic |
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Term
what does the blood-gas partition coefficent tell you about inhalational anesthetics? |
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Definition
determines how rapidly the solubility equilibrium is reached between the concentrations in the alveolus vs the blood higher blood-gas coefficient means slower onset/offset |
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Term
what does the oil-gas partition coefficient tell you about inhalational anesthetics? |
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Definition
solubility of agent in the brain - relates to lipid solubility - MAC - correlates with potency lower oil-gas coefficient means lower MAC and lower potency |
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Term
what effect does inhalational anesthitic have on the CNS? |
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Definition
irregularly descending depression of the CNS 1) ascending reticular activating system and spinal cord 2) medullary area |
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Term
what effect do inhalational anesthetics have on cerebral blood flow? |
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Definition
small increase in cerebral blood flow due to decreased cerebral vascular resistance |
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Term
what effect does sevoflurane have on the CV system? |
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Definition
decreases contractility and cardiac output (desflurane and isoflurane produce minimal cardiac depression) |
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Term
how do inhalational anesthetics affect vascular smooth muscle? |
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Definition
all inhalational anesthetics decrease vascular smooth muscle tone -> decrease BP |
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Term
what effect does desflurane have on BP? |
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Definition
can increase BP via sympathetic activation when rapid increases in concentration occur |
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Term
what affect to inhalational anesthetics have on the respiratory system? |
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Definition
direct depression of respiratory center decrease in sensitivity of medullary respiratory center to CO2 decrease in tidal volume increase in PaCO2 (can be countered w/ assisted mechanical ventillation) |
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Term
what do inhalational anesthetics do to the neuromuscular system? |
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Definition
increase GABA -> reduce signal strenght in spinal polysynaptic interneurons -> skeletal muscle relaxation |
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Term
adverse affects of desflurane |
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Definition
CV: rapid increase -> activate sympathetic NS -> increase HR and BP Resp: arryway irritation (so pretreat w/ narcotics) Toxicity: formation of CO |
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Term
adverse effects of sevoflurane |
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Definition
toxicity: CO formation, nephrotoxic compound A formation in rats |
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|
Term
why cant nitrous oxide be used as an inhalational anesthetic? |
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Definition
MAC = 105% (so you wouldn't have room for O2) |
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Term
what are benzodiazepines (midazolam) used for in IV general anesthetics? |
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Definition
reduce anxiety, sedation NOT analgesic |
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Term
why do you have to use regional anesthesia, nitrous oxide, or narcoticx along with propofol? |
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Definition
it's NOT analgesic (supraspinal effect but not spinal) |
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Term
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Definition
increase inhibitory synaptic transmission via facilitation of GABA-a receptor ion channel function -> CNS depression |
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Term
what are propofol's affects on respiration and CV and GI? |
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Definition
depression of respiration depression of CV system ] reduced systemic vascular resistance -> hypotension anti-emetic |
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Term
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Definition
inhalational anesthetic NOT analgesic (use w/ N2O or narcotic) moa: GABA s/e: myoclonus, adrenocortical supression, n/v |
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Term
what drug produces a cataleptic trance like state in which the pt may appear awake? |
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Definition
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Term
what drug produces a cataleptic trance like state in which the pt may appear awake? |
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Definition
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Term
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Definition
inhalational anesthetic NOT analgesic (use w/ N2O or narcotic) moa: GABA s/e: myoclonus, adrenocortical supression, n/v |
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Term
what drug produces a cataleptic trance like state in which the pt may appear awake? |
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Definition
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Term
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Definition
non-competitive antagonist of NMDA glutamate receptor reduce synaptic Ca channel conduction -> decreased excitatory synaptic transmission |
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Term
drug combo used for conscious sedation |
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Definition
iv opiate (fentanyl) + anti-anxiety agent (midalzolam) |
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Term
rate limiting factor of alcohol metabolism |
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Definition
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|
Term
blood alcohol concentration depends on: |
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Definition
quantity and rate of consumption speed of absorption body weight and percentage total body water rate of metabolism |
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Term
neurotransmitter effects of aclohol at lower concentrations |
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Definition
increased neuronal signaling (stimulatory) decreases GABA (disinhibition) increases DA in nucleus accumbens (pleasure) |
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Term
neurotransmitter effects of alcohol at higher concentrations |
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Definition
decreased neuronal signaling (depressant) enhances inhibitory signaling inhibits glutamate effects at NMDA receptor |
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Term
effects of alcohol on CV and resp acute vs chronic |
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Definition
acute: small doses - cutaneous vasodilation; toxic doses - myocardial depression, central vasomotor and respiratory depression chronic: hypertension, irreversible cardiomyopathy |
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Term
changes in neurotransmitter sstems due to physical dependence on alcohol |
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Definition
downregulation of inhibitory GABA receptors upregulation of excitatory glutamate (NMDA receptors) increased central norepinephrine activity |
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Term
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Definition
alpha 2 adrenergic agonist used to decrease alcohol withdrawal symptoms |
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Term
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Definition
long acting narcotic antagonist help reduce craving for alcohol |
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Term
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Definition
used as aversive deterrent to alcohol ingestion inhibit hepatic aldehyde dehydrogenase can lead to aldehyde syndrome |
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Term
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Definition
NMDA receptor antagonist used to decrease relapse rate in alcoholics |
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Term
what causes cutaneous vasodilation, throbbing headache, respiratory difficulties, nausea, copius vomiting, sweating, chest pain, blurred vision, hypotension, orthostatic syncope, confusion after drinking alcohol |
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Definition
alcohol + disulfiram or metronidazol -> aldehyde syndrome |
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Term
pt comes in w/ headache, vertigo, vomiting, dyspnea, blurred vision 8-36 hrs after ingesting something. he also has profound alterations in respiration and metabolic acidosis. what did he ingest, what are you worried about, and what do you do? |
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Definition
methanol (wood alcohol, windshield washer) formic acid produces destructive inflammation of retinal ganglion cells and can produce bilateral blindness correct acidosis, administer ethanol to block metabolism of methanol |
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Term
pt comes in with CNS depression, metabolic acidosis, and renal failure after ingesting something. what was it, and what do you do? |
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Definition
ethylene glycol (antifreeze) administer ethanol to compete for alcohol dehydrogenase and block oxalic acid formation |
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Term
pt comes in drunk w/ gastritis, pain, and vomiting, stays intoxicated for a long time, then goes into coma. what did he drink? how do you test for it? |
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Definition
isopropyl alcohol (rubbing alcohol) look for ketoacidosis and kenones in urine |
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Term
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Definition
|
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Term
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Definition
cisatracurium, vecuronium, succinylcholine |
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Term
spinal inerneuron blocker |
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Definition
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|
Term
blocks skeletal muscle contractile process |
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Definition
|
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Term
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Definition
cleaves presynaptic proteins involved in exocytosis of synaptic vesicles containing ACh |
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|
Term
competitive NMJ blocking agents |
|
Definition
cisatracurium, vecuronium |
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Term
how can you reverse a nerve block produced by cisatracurium or vecuronium? |
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Definition
acetylcholinesterase inhibitors increase synaptic ACh |
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Term
non-competitive (depolarizing) NMJ blocker |
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Definition
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Term
what are the phases of a NMJ block by succinylcholine? |
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Definition
Phase I: sustained depolarization; increased ACh intensifies blockade Phase II: competitive blockade; at this point, increased ACh can reverse the blockade |
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Term
effect of NMJ blocking agents on pts w/ myasthenia gravis: vecuronium vs succinylcholine |
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Definition
vecuronium (competitive) - more sensitive succinylcholine (noncompetitive) - resistant |
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Term
contraindication to using succinycholine? |
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Definition
burn injuries or severe CNS trauma -> hyperkalemia |
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Term
centraling acting muscle relaxants |
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Definition
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Term
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Definition
centrally acting muscle relaxant GABA-B agonist reduces release of glutamate from spinal neuonal circuits ust to tx flexor spasms and rigidity due to MS and spinal cord injury |
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Term
peripheral acting muscle relaxant moa |
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Definition
dantrolene inhibits ryanodine receptor Ca channel function in sarcoplasmic reticulum thereby inhibiting the release of Ca during excitation contraction coupling |
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Term
prophylaxis for anesthetic induced malignant hyperthermia |
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Definition
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