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101 Cards in this Set
- Front
- Back
Properties of benzodiazepines |
Bind to gamma subunit of GABA(A) complex to increase frequecy of Cl- channel opening; no GABAmimetic activity; BZ1 mediates sedation; BZ2 mediates antianxiety and impairment of cognitive functions
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Benzodiazepine drugs
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Alprazolam, diazepam, lorazepam, midazolam, temazepam, oxazepam
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Uses of alprazolam
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Anxiety, phobias, panic attacks
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Uses of diazepam
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Anxiety, preop sedation, muscle relaxation, withdrawal states
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Uses of lorazepam
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Anxiety, preop sedation, status epilepticus
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Uses of midazolam
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Preop sedation and anesthesia, anterograde amnesia
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Uses of temazepam
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Sleep disorders
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Uses of oxazepam
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Sleep disorder and anxiety
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Pharmacokinetics of benzodiazepines
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Liver metabolized to active compounds except oxazepam, temazepam, lorazepam; t1/2: diazepam > lorazepam > alprazolam > temazepam > oxazepam > midazolam
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Uses of barbiturates
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Phenobarbital for seizures; thiopental for induction of anesthesia
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Properties of barbiturates
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Prolong GABA activity; increase duration of Cl- channel opening; GABAmimetic activity at high doses; bind to beta subunit of GABA(a) complex; inhibit complex I of ETC
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Pharmacokinetics of barbiturates
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General inducers of P450; contraindicated in porphyrias
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Withdrawal signs of benzodiazepines
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Rebound insomnia, anxiety, seizures
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Withdrawal signs of barbiturates and ethanol
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Anxiety, agitation, life threatening seizures
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Drug interactions of GABAa drugs
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Life threatening respiratory depression if used with other CNS depressants (antihistaminics, opiates, beta blockers); Barbiturates induce metabolism of lipid-soluble drugs (oral contraceptives, carbamazepine, phenytoin, warfarin)
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Flumazenil
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Benzodiazepine receptor antagonist. Used as antidote for benzodiazepine overdose.
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Zolpidem
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BZ1 receptor agonist used in sleep disorders. No cognitive impairment (no BZ2 actions), overdose reversed by flumazenil, less tolerance and abuse liability
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Buspirone
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No effect on GABA, 5-HT1a partial agonist, used for generalized anxiety, nonsedative, 1-2 weeks for effects
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Effects of alcohols
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GABA mimetic activity causes CNS depression; metabolic acidosis; fetal alcohol syndrome
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Metabolism of ethylene glycol
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Ethylene glycol + alcohol DH --> glycoaldehyde + aldehyde DH --> glycolic acid --> oxalic acid
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Effects of ethylene glycol
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CNS depression, severe metabolic acidosis, nephrotoxicity
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Metabolism of methanol
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Methanol + alcohol DH --> formaldehyde + aldehyde DH --> formic acid
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Effects of methanol
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Respiratory failure, severe anion gap metabolic acidosis, ocular damage
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Treatment of alcohol overdose
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Fomepizole (alcohol DH inhibitor) and hemodialisis
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Metabolism of ethanol
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Ethanol + alcohol DH --> acetaldehyde + NADH + acetaldehyde DH --> acetic acid + NADH
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Effects of ethanol
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CNS depression, metabolic acidosis, acetaldehyde toxicity
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Acetyldehyde toxicity
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Nausea, vomit, headache, hypotension, inactivates folate, decreases availability of thiamine
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Drugs that cause disulfram-like effects
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Disulfram-like effects = acetaldehyde toxicity. Disulfram inhibits acetaldehyde DH. Metronidazole, cefamandole, cefoperazone, cefotetan, chlorpropamide
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Anticonvulsant drugs
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Phenytoin, carbamazepine, benzodiazepines, barbiturates, lamotrigine, topiramate, felbamate, ethosuximide, valproic acid
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Drugs used for partial seizures
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Valproic acid, phenytoin, carbamazepine
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Drugs used for general tonic-clonic seizures
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Valproic acid, phenytoin, carbamazepine
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Drugs used for general absence seizures
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Ethosuximide
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Drugs used for status epilepticus
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Lorazepam, diazepam, phenytoin
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Phenytoin MOA
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Inhibits fast Na channels in axons which decreases conduction and prevents seizure propagation
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Pharmacokinetics of phenytoin
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Variable absorption, nonlinear kinetics at low doses, zero-order kinetics at high doses, inducer of P450
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Phenytoin side effects
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CNS depression, gingival hyperplasia, hirsutism, osteomalacia (decreases vitamin D), megaloblastic anemia (decreases folate), aplastic anemia, teratogenic (cleft lip and palate).
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Carbamazepine MOA
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Inhibits fast Na channels in axons which decreases conduction and prevents seizure propagation
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Pharmacokinetics of carbamazepine
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Induces P450
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Carbamazepine side effects
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CNS depression, osteomalacia, megaloblastic anemia, aplastic anemia, exfoliative dermatitis, increases ADH secretion (dilutional hyponatremia), teratogenic (cleft lip and palate, spina bifida)
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Valproic acid MOA
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Inhibits fast Na channels in axons which decreases conduction and prevents seizure propagation; Inhibits GABA transaminase; Blocks presynaptic Ca+ channels
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Uses of valproic acid
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Seizures, bipolar mania, migraines
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Pharmacokinetics of valproic acid
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Inhibits P450
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Valproic acid side effects
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Hepatotoxic metabolite, thrombocytopenia, pancreatitis, alopecia, spina bifida
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Ethosuxamide MOA
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Blocks presynaptic T-type Ca+ channels in thalamic neurons
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Lamotrigine MOA
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Blocks Na+ channels and glutamate receptors. Side effect: Steven-Johnson
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Inhaled anesthetic drugs
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Nitrous oxide, halothane
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Properties of halothane
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High potency (0.8% MAC), high blood-gas ratio (2.3), sensitizes heart to catecholamines
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Side effects of halothane
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Malignant hyperthermia, hepatitis, cardiac arrhythmias
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What is MAC?
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Minimal alveolar concentration is the amount of anesthetic at which 50% of patients don't respond to surgical stimulus. Analogous to ED50, measures potency, the more lipid soluble the lower the MAC, lower in elderly
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What is the blood-gas ratio?
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Measure of the onset of recovery. The more soluble in the blood the slower the anesthesia and recovery.
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Intravenous anesthetic drugs
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Midazolam, thiopental, propofol, fentanyl, ketamine
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General anesthesia protocol
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Includes sedation and anterograde amnesia (midazolam), induction (propofol), analgesia (fentanyl), muscle relaxant for intubation (succinylcholine) and may or may not include atropine in case of CV depression due to propofol
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Naloxone
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Antidote for opiods
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Neostigmine
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AChE inhibitor reverses non-depolarizing muscle relaxants
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What are the ester local anesthetics?
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Procaine, cocaine, benzocaine. Metabolized by plasma esterases. All have only one "i"
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What are the amide local anesthetics?
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Lidocaine, bupivacaine, mepivacaine. Metabolized by liver amidases. All have two "i".
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MOA of local anesthetics
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Nonionized form crosses axonal membrane --> ionized form blocks inactivated Na+ channel --> prevent propagation of action potentials
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Side effects of local anesthetics
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Neurotoxicity, cardiovascular toxicity, allergies. Use alpha-1 agonists to prevent absorption.
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Skeletal muscle relaxants MOA
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Nicotinic antagonists (competitive, nondepolarizing); Nicotinic agonists (noncompetitive, depolarizing)
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Non-depolarizing muscle relaxant drugs
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Atracurium, mivacurium, tubocurarine
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Non-depolarizing muscle relaxant properties
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Nicotinic antagonists, reversible with AChE inhibitors, progressive paralysis, no effects on heart or CNS
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Properties of succinylcholine
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Depolarizing muscle relaxant, nicotinic agonist; Phase I: depolarization, fasciculation, flaccid paralysis; Phase II: desensitization. Caution in atypical pseudocholinesterase, hyperkalemia, malignant hyperthermia
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Malignant hyperthermia
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Succinylcholine side effect in genetically susceptible people. Muscle rigidity, hyperthermia, hypertension, acidosis, hyperkalemia. Rx.: dantrolene
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Opiod analgesic drugs
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Morphine, meperidine, methadone, codeine, fetanyl, heroin
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Contraindications of opiod analgesics
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Head injuries, pulmonary dysfunction, hepatic or renal dysfunction, adrenal or thyroid deficiencies, pregnancy
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Effects of morphine
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Analgesia, sedation, respiratory depression (decreased response to PCO2), miosis, cough supression, nausea, vomiting
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Pharmacokinetics of morphine
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Phase 2 metabolism by glucoronidation. Caution in renal dysfunction as morphine-6-glucoronide is highly active
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Opiod toxicity
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Pinpoint pupils, repiratory depression and coma. Rx. Naloxone
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Meperidine
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Opiod without miosis or spasms. Metabolized via P450 to normeperidine which can cause seizures
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Methadone
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Used for opiate withdrawal in addicts
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Codeine
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Cough suppressant, analgesia, use in combination with NSAIDs
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Symptoms of opiod withdrawal
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Yawning, lacrimation, rhinorrea, salivation, anxiety, muscle spasms and CNS-originating pain. Rx.: methadone
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Drugs used in Parkinson disease
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Levodopa, tolcapone, selegiline, bromocriptine, benztropine, amantadine
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Levodopa
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Crosses CNS barrier. Converted to dopamine in CNS and periphery, so use tolcapone, carbidopa and selegiline
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Tolcapone
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Inhibits COMT which blocks levodopa conversion to methyldopa which has no pharm actions
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Carbidopa
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Inhibits conversion of levodopa to dopamine in peripheral tissues, increasing CNS availability
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Selegiline
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MAOb selective inhibitor, adjunt to levodopa to decrease dopamine metabolism in CNS
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Bromocriptine
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Dopamine receptor agonist used in hyperprolactinemia, acromegaly
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Benztropine
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Muscarinic blocker used to decrease Ach activity in Parkinson. Decreases tremor and rigidity but not bradykinesia
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Atypical antipsychotics
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Clozapine, olanzapine, risperidone, aripiprazole
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Atypical antipsychotic MOA
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Inhibition of dopamine and 5HT2 receptors
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Side effects of antipsychotic drugs
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Extrapyramidal symptoms, akathisia, tardive dyskinesia, dysphoria, endocrine dysfunction, weight gain, hypotension, muscarinic blockade tachychardia
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Specific side effects of thioridazine
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Torsades, retinal deposits
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Typical antipsychotics
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Chlorpromazine, thioridazine, fluphenazine, haloperidol
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Specific side effects of haloperidol
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Neuroleptic malignant syndrome, tardive diskynesia
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Specific side effects of clozapine
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Agranylocytosis, seizures, salivation
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MAO inhibitor drugs
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phenelzine, tranylcypromine
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Drug interaction of MAO inhibitors
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Tyramine, TCAs, alpha-1 agonists, levodopa: increase NE --> hypertensive crisis; Serotonin syndrome with SSRI, TCA, meperidine --> sweating, rigidity, myoclonus, hyperthermia
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Tricyclic antidepressant drugs
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Amitriptyline, imipramine, clomipramine
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TCAs MOA
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Nonspecific blockade of 5HT and NE reuptake
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Side effects of TCAs
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Muscarinic blockade, alpha blockade, serotonin syndrome, hypertensive crisis
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SSRI drugs
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Fluoxetine, sertraline, paroxetine
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Side effects of SSRI
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Anxiety, agitation, bruxism, sexual dysfunction, weight loss
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Serotonin syndrome
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Sweating, rigidity, myoclonus, hyperthermia. Interaction between MAOi, TCAs, SSRIs, meperidine, dextromethorphan
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Drug-induced hypertensive crisis
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Due to interaction between MAOi, TCAs, alpha-1 agonists
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Venlafaxine
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Selective reuptake inhibitor of NE and 5HT. Can cause hypertensive crisis and serotonin syndrome
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Bupropion
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Dopamine reuptake blocker. Used in smoking cessation
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Lithium MOA
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Prevents recycling of inositol (decreases PIP2), decreases cAMP
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Lithium side effects
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Narrow therapeutic index requires monitoring, tremor, hypothyroidism (decreases TSH effects and inhibits 5'-deiodinase), nephrogenic diabetes insipidus (manage with amiloride), teratogenic
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Methylphenidate
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Reuptake inhibitor and releaser of DA and NE. Side effects: agitation, restlessness, insomnia, CV toxicity. Treats ADHD.
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Atomoxetine
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Selective NE reuptake inhibitor. Treats ADHD.
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