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BBDA Spring (Exam 6) > Sedatives and SMR's > Flashcards

Sedatives and SMR's Flashcards

1
Q

Sedative Hypnotics

A

Alcohol

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2
Q

Benzos

A

Xanax, Klonopin, Valium, Ativan, temazepam

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3
Q

Barbiturates

A

phenobarbital, secobarbital

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4
Q

Newer hypnotics

A

zolpidem, zaleplon, eszopiclone

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5
Q

Melatonin receptor agonist

A

Ramelteon (Rozerem)

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6
Q

5-HT agonist

A

buspirone

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7
Q

Centrally acting spasmolytics

A

baclofen, flexeril, soma, metaxalone, methocarbamol, tizanidine

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8
Q

Direct acting muscle relaxant

A

Dantrolene

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9
Q

Sedative hypnotics

A

reduce anxiety and cause drowsiness (sedatives or anxiolytics exert a calming effect) (hypnotics produce drowsiness), may be referred to as CNS depressants, most act via action on GABA receptors in the CNS

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10
Q

GABA

A

major inhibitory transmitters, GABAa and GABAb, responsible for sedation, amnesia, anesthesia, anticonvulsant, antianxiety and muscle relaxation

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11
Q

Drugs that affect GABA

A

Ethanol
Benzos
Barbiturates
Non-BZ sedative hypnotics

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12
Q

Alcohol ADE

A

sedation, euphoria, slowed reaction time, coma, emesis, respiratory depression

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13
Q

Ethanol MOA

A

enhances GABA @ GABAa, inhibits ability of glutamate, depression of contractility of heart, vasodilation in periphery, treatment for essential tremor

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14
Q

Metabolism of Ethanol

A

Ethanol to acetaldehyde via ADH and then to Acetic acid via ALDH

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15
Q

Ethanol ADE

A

hepatitis, cirrhosis, damage to intestines and esophagus, can lead to physical dependence and abuse, increased cardiomyopathy

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16
Q

Treatment of ethanol dependence

A

Disulfiram, Naltrexone, Acamprosate (for acute withdrawal - chlordiazepoxide and clorazepate)

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17
Q

Benzos

A

phase 1 oxidation, phase 2 conjugation,
Short acting- Xanax/Triazolam
Intermediate- clonazepam/ativan
Long acting- Valim/Fluzazepam

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18
Q

Non-BZ hypnotics

A

bind GABAa receptors in different sites than BZ’s, rapidly absorbed, short half-lives,

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19
Q

Flumazenil

A

overdose management of BZ’s, lunesta, ambien, sonata

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20
Q

Anesthesia

A

BZ’s are used IV in combo with other agents

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21
Q

Anticonvulsant

A

Phenobarb, Klonopin, Valium, Ativan

22
Q

Tolerance

A

the need for higher doses to produce response

23
Q

Physical dependence

A

withdrawal symptoms elicited upon d/c

24
Q

Addiction

A

use despite harm, psychological craving and display of addictive behaviors

25
Clinical uses of sedative hypnotics
anxiety, insomnia, sedation and amnesia during procedures, tx of epilepsy and seizures, component of anesthesia, for alcohol and sedative hypnotic withdrawal states, muscle relaxation
26
Rozerem
ramelteon, no effects on GABA, reduces sleep latency, could decrease testosterone and increase prolactin
27
Buspar
buspirone, reduces anxiety w/out sedation, acts via 5-HT and NE, nor for acute anxiety
28
Hydroxyzine
Atarax (anthihistamine)
29
Trazodone
Desyrel
30
Neuromuscular Blocking Agents
Non-depolarizing=pancuronium | Depolarizing=succinylcholine
31
Centrally-acting relaxants
BZ's, baclofen, flexeril, soma, methocarbamol
32
Non-depolarizing blockers
antagonize ACh by blocking ACh binding at nicotinic receptors, prevents deplarization and propagation of the action potential, vercuronium etc.
33
Depolarizing Blockers
too much depolarizing agonsits also stop the propagation of the action potential, persistent depolarization makes the muscle fiber resistant to ACh, ex succinylcholine
34
Depolarizing Blockers
too much depolarizing agonsits also stop the propagation of the action potential, persistent depolarization makes the muscle fiber resistant to ACh, ex succinylcholine
35
Botox
blocks ACh at motor endplate, results in paralysis
36
Clinical use of neuromuscular blocking drugs
relaxation for surgery, intubation, control of ventilation, tx of convulsions
37
Spasticity
exaggerated muscle stretch reflex, occurs when supra spinal control is lost b/c of damage to spinal cord/brain (causes: CVA, CP, MS)
38
Spasticity Triad
Painful mass muscle spasms, rigid posturing of limbs, increased reflexes
39
Muscle Spasms
increased tension in skeletal muscle following strain, pt is unable to relax, tonic contraction of muscle
40
SMR ADE
drowsiness, dizziness, ataxia (w/out control during voluntary mvmt), fatigue and muscle weakness
41
Agents for Spasticity
baclofen (Lioresal) dantrolene (Dantrium) tizanidine (Zanaflex)
42
Spasticity MOA
decrease reflex activity in spinal cord and inhibit motor neuron activity,
43
Baclofen MOA
activates pre and post synaptic GABAb receptors, results in hyperpolarization and Ca influx, can be intrathecal
44
Dantrolene
directly inhibits skeletal muscle contraction, ONLY one to exert its effects DIRECTLY on the skeletal muscle cell, impairs Ca release from SR, enhances relaxation, used to treat malignant hyperthermia
45
Tizanidine
agonist at central alpha-2 receptors, much less blood pressure lowering ability
46
Agents for muscle spasms
Soma, chlorzoxazone, Flexeril, Skelaxin, Robaxin, Norflex, Zanaflex
47
Muscle spasms meds MOA
blocks inter-neuronal activity of the descending reticular formation
48
Soma Toxicity
metabolized via liver into meprobamate which is a sedative hypnotic, causes tremors, hallucinations, and anxiety
49
Flexeril
structurally related to TCA
50
Summary:
include BZ, barbiturates, non-BZ gabaergic agents, used for sleep, anxiety, convulsions or muscle relaxants, BZ differ in half life and active metabolites, non-BZs used for sleep, SMR include neuromuscular blokcers, centrally acting agents and dantrolene (directly on skeletal muscle), all used for spasticity or muscle spasms

BBDA Spring (Exam 6) (5 decks)

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