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203 Cards in this Set
- Front
- Back
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Morphine mechanism of action?
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Opioid agonist. Open K+ channels, close Ca2+ channels; decreases synpatic transmission thus decreasing release of Ach, NE, 5-HT, glutamate, substance P.
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Morphine uses?
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Analgesic.
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Morphine side effects?
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Respiratory depression, miosis, CNS depression (additive with other drugs), constipation, addiction. Tolerance doesn't develop to miosis and constipation. Treat overdose with naloxone. Increases ICP, contraindicate with head trauma.
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Fentanyl mechanism of action?
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Opioid agonist. Open K+ channels, close Ca2+ channels; decreases synpatic transmission thus decreasing release of Ach, NE, 5-HT, glutamate, substance P.
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Fentanyl uses?
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Analgesic.
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Fentanyl side effects?
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Respiratory depression, miosis, CNS depression (additive with other drugs), constipation, addiction. Tolerance doesn't develop to miosis and constipation. Treat overdose with naloxone. Increases ICP, contraindicate with head trauma.
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Codeine mechanism of action?
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Opioid agonist. Open K+ channels, close Ca2+ channels; decreases synpatic transmission thus decreasing release of Ach, NE, 5-HT, glutamate, substance P.
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Codeine uses?
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Cough suppressant, analgesic.
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Codeine side effects?
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Respiratory depression, miosis, CNS depression (additive with other drugs), constipation, addiction. Tolerance doesn't develop to miosis and constipation. Treat overdose with naloxone. Increases ICP, contraindicate with head trauma.
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Heroin mechanism of action?
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Opioid agonist. Open K+ channels, close Ca2+ channels; decreases synpatic transmission thus decreasing release of Ach, NE, 5-HT, glutamate, substance P.
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Heroin uses?
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Analgesic.
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Heroin side effects?
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Respiratory depression, miosis, CNS depression (additive with other drugs), constipation, addiction. Tolerance doesn't develop to miosis and constipation. Treat overdose with naloxone. Increases ICP, contraindicate with head trauma.
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Methadone mechanism of action?
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Long lasting opioid agonist. Open K+ channels, close Ca2+ channels; decreases synpatic transmission thus decreasing release of Ach, NE, 5-HT, glutamate, substance P.
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Methadone uses?
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Maintence programs for addicts.
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Methadone side effects?
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Respiratory depression, miosis, CNS depression (additive with other drugs), constipation, addiction. Tolerance doesn't develop to miosis and constipation. Treat overdose with naloxone. Increases ICP, contraindicate with head trauma.
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Meperidine (demerol) mechanism of action?
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Opioid agonist. Open K+ channels, close Ca2+ channels; decreases synpatic transmission thus decreasing release of Ach, NE, 5-HT, glutamate, substance P.
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Meperidine (demerol) uses?
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Analgesic.
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Meperidine (demerol) side effects?
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Respiratory depression, miosis, CNS depression (additive with other drugs), constipation, addiction. Tolerance doesn't develop to miosis and constipation. Treat overdose with naloxone. Contraindicate with SSRIs and MAOIs (serotonin syndrome). Increases ICP, contraindicate with head trauma.
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Dextromethorphan mechanism of action?
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Opioid agonist. Open K+ channels, close Ca2+ channels; decreases synpatic transmission thus decreasing release of Ach, NE, 5-HT, glutamate, substance P.
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Dextromethorphan uses?
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Abused as a halucinogen. Cough suppressant.
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Dextromethorphan side effects?
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Respiratory depression, miosis, CNS depression (additive with other drugs), constipation, addiction. Tolerance doesn't develop to miosis and constipation. Treat overdose with naloxone.
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Loperamide, diphenoxylate mechanism of action?
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Opioid agonist. Open K+ channels, close Ca2+ channels; decreases synpatic transmission thus decreasing release of Ach, NE, 5-HT, glutamate, substance P.
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Loperamide, diphenoxylate uses?
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Antidiarrheal (induces constipation).
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Loperamide, diphenoxylate side effects?
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Respiratory depression, miosis, CNS depression (additive with other drugs), constipation, addiction. Tolerance doesn't develop to miosis and constipation. Treat overdose with naloxone.
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Butorphanol mechanism of action?
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Partial agonsit at opioid mu receptors; agonist at kappa receptors.
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Butorphanol uses?
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Pain.
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Butorphanol side effects?
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Less respiratory depression than full agonists; induces withdrawal if on a full opioid agonist (higher affinity, less effect).
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Tramadol mechanism of action?
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Very weak opioid agonist; inhibits serotonin and norepinephrine reuptake.
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Tramadol uses?
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Chronic pain.
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Tramadol side effects?
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Decreases seizure thresholds; similar to opioids.
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Carbamazepine mechanism of action?
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Inhibits voltage-gated sodium channel activation (doesn't block pores).
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Carbamazepine uses?
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Trigeminal neuralgia, tonic-clonic seziures.
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Carbamazepine side effects?
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Diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, induction of cytochrome P-450, SIADH, Stevens-Johnson syndrome. NTD in pregnancy.
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Ethoxumide mechanism of action?
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Inhibits thalamic T-type calcium channels.
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Ethoxumide uses?
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Absence seizures; ineffective for other types.
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Ethoxumide side effects?
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GI distress, fatigue, headache, urticaria, Steven-Johnson syndrome.
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Barbituates mechanism of action?
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GABA(A) agonist that increases DURATION of Cl- channel opening, thus decreasing neuron firing.
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Barbituates uses?
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First line antiepileptic in children and pregnant women. Rapid anesthesia induction.
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Barbituates side effects?
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Sedation, tolerance, dependence, induction of cytochrome P-450, additive respiratory depression with alcohol. Contraindicate with porphyria because of P-450 induction.
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Phenytoin mechanism of action?
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Use-dependent blockade of voltage-gated Na+ channels; increases refractory period; inhibition of glutamate release from excitatory presynaptic neuron.
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Phenytoin uses?
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Status epilepticus, tonic-colnic seizures. Class IB antiarrhythmic.
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Phenytoin side effects?
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Pseudolymphoma (generalized LAD), nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, peripheral neuroapthy, megaloblastic anemia, teratogenesis (fetal hydantoin syndrome), SLE-like syndrome, induction of cytochrome P-450. NTD in pregnancy.
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Valproic acid mechanism of action?
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Inhibits voltage-gated sodium channel activation, increases GABA concentration, inactivates T-type calcium channels.
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Valproic acid uses?
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Tonic-clonic seizures, absence seizures. Bipolar disorder.
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Valproic acid side effects?
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GI distress, rare but fatal hepatotoxicity (measure LFTs) , neural tube defects in fetus (spina bifida), tremor, weight gain. Contraindicated in pregnancy.
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Lamotrigine, felbamate mechanism of action?
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Blocks voltage-gated sodium channels and glutamate receptors.
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Lamotrigine, felbamate uses?
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All seizure types except absence.
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Lamotrigine, felbamate side effects?
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Stevens-Johnson syndrome, hepatotoxicity and aplastic anemia
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Gabapentin mechanism of action?
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GABA analog; inhibits HVA calcium channels.
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Gabapentin uses?
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All seizure types except absence.
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Gabapentin side effects?
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Sedation, ataxia.
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Toprimate mechanism of action?
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Blocks sodium channels and increases GABA action.
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Toprimate uses?
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All seizure types except absence.
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Toprimate side effects?
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Sedation, mental dulling, kidney stones, weight loss. Inhibits CYP-450.
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Benzodiazepines (-epam, -olam) mechanism of action?
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GABA(A) agonist that increases FREQUENCY of Cl- channle opening; decreases REM sleep.
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Benzodiazepines (-epam, -olam) uses?
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Terminates acute status epilepticus, eclampsia, insomnia, night terrors, sleepwalking, detoxiciation (alcohol), anxiety, spasticity.
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Benzodiazepines (-epam, -olam) side effects?
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Sedation, tolerance, dependence. Short acting agents = TOM (Triazolam, Oxazepam, Midazolam; highest addictive potential). Long acting agents = CCDF (chlordiazepoxide, chlorazepate, diazepam, flurazepam.) Long lasting agents have higher risk of daytime drowsiness and risk of falls (CI with parkinson's).
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Tiagabine mechanism of action?
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Inhibits GABA reuptake.
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Tiagabine uses?
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All seizure types except absence.
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Vigabatrin mechanism of action?
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Irreversible inhibits GABA transaminase; increases GABA levels.
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Vigabatrin uses?
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All seizure types except absence.
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Levetiracetam mechanism of action?
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Modulates GABA and glutamate release.
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Levetiracetam uses?
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All seizure types except absence.
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MgSO4 uses?
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Prevents seziures of eclampsia.
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Halothane mechanism of action?
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Myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow (decrease cerebral metabolic demand).
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Halothane side effects?
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Severe hepatic necrosis, malignant hyperthermia.
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Enflurane mechanism of action?
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Myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow (decrease cerebral metabolic demand).
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Enflurane side effects?
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Proconvulsant, malignant hypertermia.
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Isoflurane mechanism of action?
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Myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow (decrease cerebral metabolic demand).
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Isoflurane side effects?
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Malignant hyperthermia.
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Sevoflurane mechanism of action?
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Myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow (decrease cerebral metabolic demand).
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Sevoflurane side effects?
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Malignant hyperthermia.
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Methoxyflurane mechanism of action?
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Myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow (decrease cerebral metabolic demand).
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Methoxyflurane side effects?
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Nephrotoxicity, malignant hyperthermia.
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Nitrous oxide uses?
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Analgesic.
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Ketamine (arylcyclohexylamines) mechanism of action?
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NMDA antagonist; PCP analog.
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Ketamine (arylcyclohexylamines) uses?
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Dissociative anesthetic; especially useful for burn patients.
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Ketamine (arylcyclohexylamines) side effects?
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CV stimulant; disorientation, hallucination, bad dreams (in children). Increases cerebral blood flow.
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Propofol mechanism of action?
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Potentiates GABA(A).
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Propofol uses?
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For short procedures; rapid induction of anesthesia. Anti-emetetic.
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Procaine, cocaine, tetracaine mechanism of action?
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Ester anesthetic. Block voltage gated sodium channels by stabilizng inactive form; selectively targets more rapidly firing neurons.
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Procaine, cocaine, tetracaine uses?
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Only cocaine causes vasoconstriction; the rest must be administered with vasoconstrictors to enhance local action. Targets small myelinated nerves first; pain > temperature > touch > pressure (last).
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Procaine, cocaine, tetracaine side effects?
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Hypersensitivity. CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, hypotension, arrhythmia (cocaine).
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Lidocaine, mepivacaine, bupivacaine mechanism of action?
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Amide anesthetic.
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Lidocaine, mepivacaine, bupivacaine uses?
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Must be coadministered with a vasoconstrictor. Targets small myelinated nerves first; pain > temperature > touch > pressure (last).
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Lidocaine, mepivacaine, bupivacaine side effects?
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If allergic to esters, give amides. CV toxicity, HTN, CNS excitation.
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Succinylcholine mechanism of action?
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Depolarizing neuromuscular blocker (NAChR).
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Succinylcholine uses?
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Rapid intubation.
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Succinylcholine side effects?
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Hypercalcemia, hyperkalemia, malignant hyperthermia. Contraindicate acetylcholinesterase inhibitors.
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Tubocurarine mechanism of action?
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Non-depolarizing neuromuscular blocker (NAChR). Competitive NAChR antagonist.
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Tubocurarine uses?
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Muscle paralysis in surgery.
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Tubocurarine side effects?
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Reverse blockade with an acetylcholinesterase inhibitor.
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Atracurium mechanism of action?
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Non-depolarizing neuromuscular blocker (NAChR). Competitive NAChR antagonist.
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Atracurium uses?
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Muscle paralysis in surgery.
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Atracurium side effects?
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Reverse blockade with an acetylcholinesterase inhibitor.
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Mivacurium mechanism of action?
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Non-depolarizing neuromuscular blocker (NAChR). Competitive NAChR antagonist.
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Mivacurium uses?
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Muscle paralysis in surgery.
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Mivacurium side effects?
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Reverse blockade with an acetylcholinesterase inhibitor.
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Pancuronium mechanism of action?
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Non-depolarizing neuromuscular blocker (NAChR). Competitive NAChR antagonist.
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Pancuronium uses?
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Muscle paralysis in surgery.
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Pancuronium side effects?
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Reverse blockade with an acetylcholinesterase inhibitor.
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Vecuronium mechanism of action?
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Non-depolarizing neuromuscular blocker (NAChR). Competitive NAChR antagonist.
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Vecuronium uses?
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Muscle paralysis in surgery.
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Vecuronium side effects?
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Reverse blockade with an acetylcholinesterase inhibitor.
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Rocuronium mechanism of action?
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Non-depolarizing neuromuscular blocker (NAChR). Competitive NAChR antagonist.
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Rocuronium uses?
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Muscle paralysis in surgery.
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Rocuronium side effects?
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Reverse blockade with an acetylcholinesterase inhibitor.
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Dantrolene mechanism of action?
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Prevents Ca2+ release from SER by antagonizing the ryanodine receptor.
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Dantrolene uses?
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Malignant hyperthermia, neuroleptic malingant syndrome.
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Bromocriptine mechanism of action?
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Dopamine agonist.
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Bromocriptine uses?
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Parkinson's disease.
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Pergolide mechanism of action?
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Dopamine agonist.
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Pergolide uses?
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Parkinson's disease.
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Pramipexole mechanism of action?
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Dopamine agonist.
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Pramipexole uses?
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Parkinson's disease.
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Ropinirole mechanism of action?
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Dopamine D2 agonist.
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Ropinirole uses?
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Parkinson's disease, restless leg syndrome
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Amantadine mechanism of action?
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Dopamine agonist.
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Amantadine uses?
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Parkinson's disease.
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L-dopa/carbidopa mechanism of action?
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Dopamine agonist (L-DOPA); inhibits DOPA decarboxylase peripherally (carbidopa)
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L-dopa/carbidopa uses?
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Parkinson's disease.
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L-dopa/carbidopa side effects?
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Arrhythmias from peripheral conversion to dopamine. Long-term use can increase dyskinesia following administration, akinesia between doses. Carbidopa limits peripheral side effects. Contraindicate with B6 since it increases peripheral metabolism of levodopa.
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Selegiline mechanism of action?
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Selective MAO B inhibitor. Decreases dopamine metabolism.
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Selegiline uses?
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Parkinson's disease.
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Selegiline side effects?
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Enhances L-dopa toxicity.
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Entacapone mechanism of action?
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Peirpheral COMT inhibitor. Decreases dopamine metabolism.
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Entacapone uses?
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Parkinson's disease.
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Tolcapone mechanism of action?
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Peripheral and central COMT inhibitor. Decreases dopamine metabolism.
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Tolcapone uses?
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Parkinson's disease.
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Benztropine mechanism of action?
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Anticholinergic.
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Benztropine uses?
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Parkinson's disease; improves tremor and rigidity but no effect on bradykinesia.
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Memantine mechanism of action?
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NMDA receptor antagonist.
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Memantine uses?
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Alzheimer's disease; helps prevent excitoxicity mediated by calcium.
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Memantine side effects?
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Dizziness, confusion, hallucinations.
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Donepezil mechanism of action?
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Acetylcholinesterase inhibitor.
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Donepezil uses?
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Alzhiemer's disease.
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Donepezil side effects?
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Nausea, dizziness, insomnia.
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Galantamine mechanism of action?
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Acetylcholinesterase inhibitor.
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Galantamine uses?
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Alzhiemer's disease.
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Galantamine side effects?
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Nausea, dizziness, insomnia.
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Rivastigmine mechanism of action?
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Acetylcholinesterase inhibitor.
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Rivastigmine uses?
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Alzhiemer's disease.
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Rivastigmine side effects?
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Nausea, dizziness, insomnia.
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Resperine + tetrabenzine mechanism of action?
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Amine depleting; lowers dopamine levels.
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Resperine + tetrabenzine uses?
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Huntington's disease (caused by too much dopamine, too little GABA and ACh).
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Resperine + tetrabenzine side effects?
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0
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Sumatriptan mechanism of action?
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5-HT1B/1D agonist; causes vasoconstriction, inhibition of trigeminal activation and CGRP release.
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Sumatriptan uses?
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Acute migraines, cluster headache attacks.
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Sumatriptan side effects?
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Coronary vasospasm (CI in patients with coronary artery disease of Prinzmetal's angina).
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Ergotamine mechanism of action?
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5-HT1 agonist
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Ergotamine uses?
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Acute migraines.
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Ergotamine side effects?
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Rebound headaches; more severe side effecst than sumatriptan; angina, vasoconstriction (gangrene, thrombosis).
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Fomepizole mechanism of action?
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Competitive inhibitor of alcohol dehydrogenase.
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Fomepizole uses?
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Antidote for methanol or ethylene glycol poisoning.
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Ramelteon mechanism of action?
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Melatonin agonist.
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Ramelteon uses?
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Insomnia; less side effects than GABA agonists.
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Baclofen mechanism of action?
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GABA(B) agonist (K+ efflux)
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Baclofen uses?
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Muscle relaxant.
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Zolpidem mechanism of action?
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BDZ1 agonist on GABA(A) receptors.
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Zolpidem uses?
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Insomnia.
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Zolpidem side effects?
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Ataxia, headaches, confsuion. Short duration due to liver metabolism. Modest day-after psychomotor depression and few amnestic side effects. Lower dpeenence risk than benzodiazepines.
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Zaleplon mechanism of action?
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BDZ1 agonist on GABA(A) receptors.
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Zaleplon uses?
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Insomnia.
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Zaleplon side effects?
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Ataxia, headaches, confsuion. Short duration due to liver metabolism. Modest day-after psychomotor depression and few amnestic side effects. Lower dpeenence risk than benzodiazepines.
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Eszopiclone mechanism of action?
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BDZ1 agonist on GABA(A) receptors.
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Eszopiclone uses?
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Insomnia.
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Eszopiclone side effects?
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Ataxia, headaches, confsuion. Short duration due to liver metabolism. Modest day-after psychomotor depression and few amnestic side effects. Lower dpeenence risk than benzodiazepines.
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Cyclobenzaprine mechanism of action?
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Activates locus ceruleus; increases norepinephrine release and inhibits alpha-motor neurons.
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Cyclobenzaprine uses?
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Muscle relaxant.
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Cyclobenzaprine side effects?
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Contraindicate MAOIs.
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Latanoprost mechanism of action?
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PGF2-alpha. Increases outflow of aqueous humor.
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Latanoprost uses?
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Glaucoma.
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Latanoprost side effects?
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Darkens color of iris (browning).
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Acetazolamide mechanism of action?
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Carbonic anhydrase inhibitor. Decreases aqueous humor secretion due to decrease in HCO3.
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Acetazolamide uses?
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Glaucoma.
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Acetazolamide side effects?
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No pupillary or vision changes.
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Pilocarpine, carabachol mechanism of action?
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Direct cholinergic agonists. Increases outflow fo aqueous humor; contract ciliary muscle and open trabecular meshwork; use pilocarpine in emergencies; ery effect at opening canal of Schlemm.
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Pilocarpine, carabachol uses?
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Glaucoma.
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Pilocarpine, carabachol side effects?
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Miosis, cyclospasm.
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Physostigmine, echothiophate mechanism of action?
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Indirect cholinergic agonists; acetylcholinesterase inhibitor. Increases outflow fo aqueous humor; contract ciliary muscle and open trabecular meshwork.
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Physostigmine, echothiophate uses?
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Glaucoma.
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Physostigmine, echothiophate side effects?
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Miosis, cyclospasm.
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Timolol, betaxolol, carteolol mechanism of action?
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Beta-blocker; decreases aqueous humor secretion by acting on the ciliary epithelium.
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Timolol, betaxolol, carteolol uses?
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Glaucoma.
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Timolol, betaxolol, carteolol side effects?
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No pupillary or vision changes.
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Epinephrine mechanism of action?
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Alpha/beta agonist; decreases aqueous humor synthesis due to vasoconstriction.
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Epinephrine uses?
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Open-angle glaucoma.
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Epinephrine side effects?
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Mydriasis, stinging; do not use in closed-angle glaucoma.
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Brimonidine mechanism of action?
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Alpha 2-agonist; decreases aqueous humor synthesis.
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Brimonidine uses?
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Glaucoma.
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Brimonidine side effects?
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No pupillary or vision changes.
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Primidone mechanism of action?
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Precursor to phenobarbital; anticonvulsant that acts via inhibition of voltage gated sodium channels.
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Pentazocine mechanism of action?
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Partial mu agonist.
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Pentazocine uses?
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May precipitate withdrawal symptoms. Pain management with little to no abuse potential.
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Methysergide mechanism of action?
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Serotonin agonist.
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Methysergide uses?
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Used for migraine headaches
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Methysergide side effects?
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Retroperitoneal fibrosis.
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Riluzole mechanism of action?
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Blocks TTX sensitive sodium channels.
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Riluzole uses?
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ALS
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Acamprosate mechanism of action?
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NMDA antagonists; GABA agaonists
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Acamprosate uses?
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Alcoholism
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Tacrine mechanism of action?
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Acetylcholinesterase inhibitor.
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Tacrine uses?
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Alzheimer's disease.
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