Neuro - sedatives Flashcards

1
Q

Barbiturates

A

Phenobarbital; Pentobarbital; Thiopental; Secobarbital

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2
Q

MOA of barbiturates

A

Facilitate GABA-A action by increasing duration of chloride channel opening; thus decreasing neuron firing; Contraindicated in porphyria; Used as a sedative for anxiety; seizures; insomnia; and induction of anesthesia (thiopental)

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3
Q

Side effects of barbiturates

A

Respiratory and cardiovascular depression (can be fatal); CNS depression (can be exacerbated by EtOH use); Dependence; Drug interactions (induces cytochrome P-450); Overdose treatment is supportive (assist respiration and maintain BP)

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4
Q

Benzodiazepines

A

Diazepam; Lorazepam; Triazolam Temazepam Oxazepam Midazolam Chlordiazepoxide Alprazolam

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5
Q

MOA of benzodiazepines

A

Facilitate GABA-A action by increasing frequency of chloride channel opening; Decrease REM sleep; Most have long half lives and active metabolites; Exceptions - triazolam; oxazepam; and midazolam are short acting - higher addictive potential; Used in anxiety; spasticity; status elipticus (lorazepam and diazepam); detoxification (especially alcohol withdrawal-DTs); night terrors; sleepwalking; general anesthetic (amnesia; muscle relaxation); hypnotic (insomnia)

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6
Q

Side effects of benzodiazepines

A

Dependence; Additive CNS depression effects with alcohol; Less risk of respiratory depression and coma than with barbiturates; Treat overdose with flumazenil (competitive antagonist at GABA benzodiazepine receptor)

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7
Q

ZolpidemZaleplonEszopiclone

A

Nonbenzodiazepine hypnoticsAct via the BZ1 subtype of the GABA receptorEffects reversed by flumazenilUsed to treat insomnia

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8
Q

Side effects of zolpidem; zaleplon; and eszopiclone

A

Ataxia; headaches; confusionShort duration because of rapid metabolism by liver enzymesUnlike older sedative-hypnotics; cause only modest day-after psychomotor depression and few amnestic effectsDecreased dependence risk than benzodiazepines

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9
Q

Inhaled anesthetics

A

HalothaneEnfluraneIsofluraneSevofluraneMethoxyflurane**Nitrous Oxide

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10
Q

Effects of inhaled anesthetics

A

Myocardial depressionRespiratory depressionNausea/emesisIncreased cerebral blood flow**Decreased cerebral metabolic demand

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11
Q

Side effects of halothane

A

Hepatotoxicity

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12
Q

Side effects of methoxyflurane

A

Nephrotoxicity

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13
Q

Side effects of enflurane

A

Proconvulsant

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14
Q

Side effects of nitrous oxide

A

Expansion of trapped gas in a body cavity

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15
Q

Malignant Hyperthermia

A

Rare; life-threatening hereditary condition in which inhaled anesthetics (except nitrous oxide) and succinylcholine induce fever and severe muscle contractions Treatment is dantrolene.

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16
Q

Nitrous Oxide

A

Inhaled anesthetic Low blood solubility; Low lipid solubility; Low blood solubility provides rapid induction and recovery time; Low lipid solubility means it has low potency

17
Q

Halothane

A

Inhaled anesthetic; High blood solubility; High lipid solubility; High lipid solubility means it is highly potent; High blood solubility means there is slow induction and recovery

18
Q

Thiopental

A

Intravenous Anesthetic - Barbiturate; High potency; high lipid solubility; rapid entry into brain; Used for induction of anesthesia and short surgical procedures; Effect terminated by rapid redistribution into tissue and fat; Decreases cerebral blood flow

19
Q

Midazolam

A

Intravenous Anesthetic - Benzodiazepine; Most common drug used for endoscopy; Used adjunctively with gaseous anesthetics and narcotics; May cause severe postoperative respiratory depression; decrease in BP; and anterograde amnesia; Treat overdose with flumazenil

20
Q

Ketamine

A

Intravenous Anesthetic - Arylcyclohexylamines; PCP analog that acts as dissociative anesthetic; Blocks NMDA receptors; Cardiovascular stimulant; Causes disorientation; hallucination; and bad dreams; Increases cerebral blood flow

21
Q

Morphine and fentanyl

A

Opiods used with other CNS depressants during general anesthesia

22
Q

Propofol

A

Intravenous anesthetic; Used for sedation in the ICU; rapid anesthesia induction; and short procedures.; Less postoperative nausea than thiopental; Potentiates GABA-A

23
Q

Esters - local anesthetics

A

Procaine; Cocaine; Tetracaine

24
Q

Amides - local anesthetics

A

Lidocaine; Mepivacaine; Bupivacaine

25
Q

MOA of local anesthetics

A

Block sodium channels by binding to specific receptors on the inner portion of the channel;Preferentially bind to activated sodium channels; so most effective in rapidly firing neurons;Tertiary amine local anesthetics penetrate membrane in uncharged form; then bind to ion channels as charged form

26
Q

Side effects of local anesthetics

A

CNS excitation; Severe cardiovascular toxicity (bupivacaine); Hypertension; Hypotension; Arrhythmias (cocaine)

27
Q

Succinylcholine

A

Depolarizing Neuromuscular Blocking Drug; Strong ACh receptor agonist - produces sustained depolarization and prevents muscle contraction; Reversal of blockade: Phase I (prolonged depolarization) - no antidote - block potentiated by cholinesterase inhibitors. Phase II (repolarized but blocked; ACh receptors are available; but desensitized) - antidote consists of cholinesterase inhibitors

28
Q

Side effects of succinylcholine

A

*Complications include: Hypercalcemia + Hyperkalemia; Malignant Hypertension

29
Q

Nondepolarizing neuromuscular blockers

A

Tubocurarine; atracurium; mivacurium; pancuronium; vecuronium; rocuronium; Competitive antagonists - compete for ACh for receptors; Reversal of blockade - neostigmine; edrophonium; and other cholinesterase inhibitors

30
Q

Neostigmine

A

Cholinesterase Inhibitor; Used to reverse neuromuscular blockade with nondepolarizing blockers; Must be given with atropine to prevent muscarinic effects such as bradycardia

31
Q

Dantrolene

A

Prevents the release of calcium from the sarcoplasmic reticulum of skeletal muscle; Used to treat malignant hyperthermia and neuroleptic malignant syndrome (a toxicity of antipsychotic drugs)