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99 Cards in this Set
- Front
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Benzodiazepines
MOA |
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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Barbiturates
MOA |
Bind to beta subunit of GABA(a) complex; GABAmimetic activity at high doses, Prolong GABA activity by increase duration of Cl- channel opening; ; 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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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, Desflurane, Sevoflurane, Eflurane, Isoflurane
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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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Name the 4 stages of anesthesia?
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1 analgesia
2 disinhibition 3 surgical anesthesia 4 medullary depression |
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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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Intravenous anesthetic drugs
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Midazolam, thiopental, propofol, fentanyl, ketamine
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Midazolam
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IV benzodiazepine used for preoperative sedation and commonly in anesthesia protocols (e.g.,
conscious sedation) affording anterograde amnesia. Depresses respiratory function but reversed by the BZ receptor antagonist flumazenil |
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Thiopental
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Highly lipid-soluble, rapid-onset, and short-acting barbiturate used mainly for induction.
Depresses respiratory and cardiac function but does not increase cerebral blood flow. Rapid recovery associated with redistribution from CNS to peripheral tissues, but liver metabolism required for elimination. |
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Propofol
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Very rapid onset and recovery, plus antiemetic effects, used for both induction and maintenance;
especially useful in outpatient surgery. |
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Fentanyl
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One of several related opioid analgesics used in anesthesia. Potent analgesic, with shorter durations
of action than most opioids; oral and patch formulations are also used. Chest wall rigidity with IV use. Neurolept anesthesia = combination of fentanyl, droperidol, and nitrous oxide. |
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Ketamine
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Rapid-onset and short-duration agent that causes "dissociative anesthesia" with amnesia, catatonia,
and analgesia. Only anesthetic that causes CV stin~ulation!E mergence reactions (vivid dreams, hallucinations) partly offset by benzodiazepines. |
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KETAMINE does not produce its effect via facilitation of GABA receptors, but possibly via its antagonism of the action via what neurotransmitter at what receptor?
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Excitatory neurotransmitter GLUTAMATE on the NMDA receptor.
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How is the production of anesthesia and recovery of anesthesia of PROPOFOL in comparison with barbiturates (thiopental)?
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Its anesthetic effect is faster and it recovers faster.
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What are the ester local anesthetics?
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Procaine, cocaine, benzocaine. Metabolized by plasma and tissue 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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Neostigmine
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AChE inhibitor reverses non-depolarizing muscle relaxants
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Opiod analgesic drugs
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Morphine, meperidine, methadone, codeine, fetanyl, heroin
Fentanyl, Hydromorphone, Meperidine, Morphine, Methadone Oxymorphone, Codeine, Hydrocodone, Buprenorphine, Nalbuphine, Naloxone, Naltrexone, Nalmefene, Codeine, Dextromethorphan, Tramadol |
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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
Analgesia Sedation Respiratory Depression Cardiovascular GI Tract Decreased peristalsis 4 constipation (or clinical use in diarrheal states, e.g., loperamide and diphenoxylate). Smooth Muscle Increased tone of biliary, bladder, and ureter with possible spasms Pupils Miosis Cough Suppression Antitussive action-independent of analgesia (e.g., dextromethorphan) and at subanalgesic doses with codeine. Nausea and Emesis |
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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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Naloxone
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Antidote for opiods
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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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