cns depressants and muscle relaxants Flashcards

1
Q

sedatives

A
  • drugs that have inhibitory effect on the CNS to the degree where they reduce nervousness, excitability and irritability
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2
Q

hypnotics

A
  • cause sleep
  • more potent than sedatives
  • sedative can become a hypnotic if dose is large enough
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3
Q

CNS depressants

A
  • large doses= cause sleep
  • small doses= calm CNS without causing sleep
  • 3 groups= barbiturates, benzodiazepines, miscellaneous drugs
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4
Q

sleep

A
  • cyclic and repetitive
  • response to stimuli is reduced
    -REM and non REM
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5
Q

benzodiazepines

A
  • favourable adverse effects profiles, efficacy and safety
  • classified as sedative-hypnotic or anxiolytic (relieves anxiety)
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6
Q

benzodiazepines (sedative hypnotic) long acting, intermediate and short

A
  • long acting= diazepam (valium)
  • intermediate acting= lorazepam (ativan)
  • short acting= midazolam hcl
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7
Q

benzodiazepine MOA

A
  • depresses CNS
  • affect hypothalamic, thalamic and limbic system of brain
  • GABA receptors
  • dont suppress REM as much as barbituates
  • dont increase metabolism of other drugs
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8
Q

benzodiazepine drug effects

A
  • calms CNS
  • controls agitation and anxiety
  • reduces sensory stimulation inducing sleep
  • induces skeletal muscle relaxation
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9
Q

benzodiazepine indications

A
  • sedation
    -sleep induction
  • muscle relaxation
  • anxiety relief
  • anxiety related depression
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10
Q

benzodiazepine uses

A

-treatment of acute seizures
- treatment of alc withdrawal
- short term therapy for insomnia

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11
Q

benzodiazepine adverse effects

A
  • headaches
  • drowsiness
  • ataxia
  • paradoxical nervousness
  • dizziness
  • cognitive impairment
  • vertigo
  • lethargy
  • fall hazard in older adults
  • hangover effect of daytime sleepiness
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12
Q

benzodiazepine contraindications

A

pregnancy and glaucoma

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13
Q

benzodiazepine toxicity and overdose

A

somnolence, confusion, coma, diminished reflexes
- rarely results in hypotension and resp depression unless taken with other CNS depressants (alc)
- treatment symptomatic and supportive

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14
Q

antidote for benzodiazepine toxicity

A

flumazenil

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15
Q

benzodiazepine interactions

A
  • azole antifungals, verapamil, diltiazem, protease inhib, macrolide antibiotics, grapefruit juice
  • CNS depressants
  • kava and valerian
  • food drug interactions with grapefruit
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16
Q

diazepam (valium)

A
  • first available benzo
  • treatment of anxiety
  • long acting
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17
Q

midazolam

A
  • short acting
  • used pre-op and for procedural sedation
  • causes amnesia and anxiolysis
  • IV admin in adults
  • liquid oral dosage is available for children
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18
Q

lorazepam (ativan)

A
  • intermediate acting benzo
  • used to treat anxiety
  • max dose 4mg/day
  • induces sleep within 30-60min
  • long onset so take 1hr before bed
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19
Q

nonbenzodiazepine (zopiclone)

A
  • imovane, rhovane
  • short acting benzodiazepinelike drug
  • very short half life
  • short term treatment of insomnia (7-10 days)
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20
Q

kava indications and adverse effects

A
  • relieve anxiety, stress and restlessness
  • causes temporary jaundice, scaly skin and visual disturbances
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21
Q

kava interactions

A
  • interactions with alc, barbituates and psychoactive drugs
22
Q

kava contraindications

A
  • liver disease, alcoholism, parkinsons
23
Q

dont operate heavy machinery with

A

kava and valerian

24
Q

valerian

A
  • relieve anxiety, restlessness and sleep disorders
25
valerian adverse effects
- CNS depression, heaptotoxicity, nausea, vomiting, anorexia, headache, restlessness and insomnia
26
valerian interactions
- CNS depressants, MAOIs, phenytoin, warfarin, alcohol
27
valerian contraindications
- cardiac and liver disease
28
barbituates
- introduced in 1903, were the standard drug for insomnia and sedation - low therapeutic index (easy to become toxic) -contraindicated in pregnancy
29
barbituates MOA
- acts on brainstem (reticular formation) - potentiates action of GABA, nerve impulses traveling in the cerebral cortex are inhibited
30
barbituates indications
- sedatives - anticonvulsants - anaesthesia for surgical procedures
31
barbiturates adverse effects: cardiovascular
vasodilation, hypotension
32
barbiturates adverse effects: CNS
drowsiness, lethargy, vertigo
33
barbiturates adverse effects: resp
resp depress and cough
34
barbiturates adverse effects: GI
nausea, vomiting, diarrhea, constipation
35
barbiturates adverse effects: hematological
agranulocytosis and thrombocytopenia
36
barbiturates adverse effects other
hypersensitivity. stevens-johnson syndrome, paradoxical excitement in children, confusion in older adults
37
barbiturate overdose
resp depression and resp arrest CNS depression can be therapeutic for: - anaesthesia induction - uncontrollable seizures -phenobarbital coma
38
treatment of barbiturate overdose
- symptomatic and supportive - maintain adequate airway - assisted ventilation or o2 therapy - fluids - alkalization -activated charcoal
39
barbiturates additive effects
- alc, antihistamines, benzodiazepines, opioids, tranquilizers
40
barbiturates inhibited metabolism
- MAOIs prolong the effects of barbiturates
41
barbiturates increased metabolism
- reduces anticoagulant response leading to possible clot formation
42
barbiturate example
phenobarbital
43
phenobarbital
- prototypical barbiturate - long acting - for prevention of generalized tonic clonic seizures and fever induced convulsions as well as treatment of hyperbilirubinemia in neonates - rarely used -adverse effect: anemia - taper dose to prevent seizures and hallucinations
44
OTC hypnotics
- doxylamine succinate (unisom-2) - dyphenhydramine hcl (sleep-eze) - acetaminohpen/diphenhydramine (extra strength Tylenol nighttime)
45
muscle relaxants
- relieve pain from muscle spasms - central acting (CNS) -similar to other CNS depressants - direct acting (on skeletal muscle, closely resemble GABA)
46
muscle relaxant indications
- relief of painful musculoskeletal conditions - management of MS and cerebral palsy - works best with physical therapy
47
muscle relaxant adverse effects
- euphoria, lightheadedness, dizziness, drowsiness, fatigue, confusion, muscle weakness
48
common muscle relaxants
-baclofen injectable (lioresal - cyclobenzaprine hcl PO (novocycloprine)
49
when to administer hypnotics
30-60 mins before bed for max effectiveness
50
benzodiazepine hangover effect
REM interference and tiredness the next day in older adults
51
rebound insomnia
may occur after a 3-4 week regimen has been discontinued