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KG - pharmacology 3 > KG - Pharm 3, Exam 1, Sedative-Hypnotics & Antianxiolytics > Flashcards

KG - Pharm 3, Exam 1, Sedative-Hypnotics & Antianxiolytics Flashcards

1
Q

primary use of sedative-hypnotics & anxiolytics?

A
  • encourage CALMNESS (anxiolytic effect) & produce SLEEP (sedative-hypnotic effect)
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2
Q

define: sedation

A
  • reduced alertness
  • decreased motor activity
  • relaxation
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3
Q

define: hypnosis

A
  • state of drowsiness

- leads to sleep

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4
Q

describe: anxiety disorder

A
  • pervasive feeling of tension/apprehension

- symptoms = palpitations, tremor, perspiration, GI effects, dizziness, HA

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5
Q

describe: ADAPTIVE anxiety

A
  • appropriate run to danger (fear, arousal)

- increased sympathetic activity

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6
Q

describe: MALADAPTIVE anxiety

A
  • chronic, psychological stress

- organ dysfunction (GI, cardiac), physical symptoms

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7
Q

describe: acute anxiety (what drug class to treat?)

A
  • short term, self-limiting

- BENZOS

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8
Q

describe: generalized anxiety disorder (what drug class to treat?)

A
  • chronic anxiety

- BENZOS, BUSPIRONE

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9
Q

describe: panic disorder (what drug class to treat?)

A
  • episodic
  • severe attacks
  • SSRIs
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10
Q

describe: phobias (what drug class to treat?)

A
  • fear of things/circumstances

- SSRIs

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11
Q

describe: OCD (what drug class to treat?)

A
  • recurrent, obsessive, behaviors

- SSRIs

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12
Q

describe: PTSD (what drug class to treat?)

A
  • anxiety after stressful event

- ANTIDEPRESSANTS

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13
Q

describe: insomnia

A
  • difficulty falling asleep, early/freq waking, unrefreshing sleep
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14
Q

define: SHORT-TERM/TRANSIENT insomnia

A
  • occurs w/ situational stress

- treated with SEDATIVE-HYPNOTICS

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15
Q

define: LONG-TERM insomnia

A
  • may be related to underlying psychiatric dz, chronic alcohol/drug abuse
  • treated w/ behavioral therapy & lifestyle changes
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16
Q

what is the “ideal” sedative-hypnotic?

A
  • cause to fall asleep quickly
  • stay asleep as long as you want
  • wear off early in a.m.
  • no “hang over” effect
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17
Q

sedative hypnotics: moa?

A
  • GABA
  • CNS DEPRESSANT
  • major inhibitory neurotransmitter
  • widely distributed in CNS
  • relieves anxiety, promotes sedation
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18
Q

How do GABA receptors work?

A
  • Cl- channels
  • activation of GABA receptor allows Cl- to enter cell, hyper polarizing membrane
  • activation GABA(a) receptor causes depression of electrical activity, DECREASES ANXIETY & PROMOTES SLEEP
  • some drugs work independently of GABA
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19
Q

Barbiturates: gen info

A
  • binds to GABA receptor, stimulates Cl- influx
  • produces inhibition INDEPENDENT OF GABA
  • CNS DEPRESSION effect (hypnosis)
  • CAUSES EUPHORIA
  • drug of abuse
  • schedule II or III
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20
Q

barbiturates - THIOPENTAL: uses

A
  • short acting

- INDUCTION OF ANESTHESIA

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21
Q

barbiturates - PHENOBARBITAL: uses

A
  • long acting

- ANTICONVULSANTS

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22
Q

barbiturates: pharmacokinetics

A
  • ORAL, crosses BBB
  • metabolized by LIVER
  • INDUCE CYP450s w/ chronic use - alters metabolism of other drugs (esp alcohol, hormones, other barbiturates)
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23
Q

barbiturates: side effects

A
  • CNS DEPRESSION = drowsiness, mood distortion, impaired judgment & motor skills
  • can last 10-22 hrs
  • PARADOXICAL EXCITEMENT (esp in elderly)
  • vertigo, N/V, diarrhea, allergic rxns
  • may depress vasomotor/respiratory centers in medulla
  • SEVERE PSYCHOLOGICAL & PHYSIOLOGICAL DEPENDENCE
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24
Q

barbiturates: contraindications

A
  • ENHANCE PORPHYRIN SYNTHESIS (don’t use w/ porphyria)
  • PULM INSUFFICIENCY
  • SUPRA-ADDITIVE EFFECTS - when combined w/ other CNS depressants (2+2=7)
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25
Q

barbiturates: withdrawal

A
  • CAN BE SEVERE - restlessness, anxiety, weakness, orthostatic hypotension, hyperactive reflexes, seizures
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26
Q

barbiturates: overdose/toxicity

A
  • major problem
  • LOW MARGIN OF SAFETY
  • NO “CEILING EFFECT”
  • effects SUPRA-ADDITIVE, esp w/ alcohol
  • overdose = coma, resp depression, decr BP
27
Q

barbiturates: how to treat overdose/toxicity?

A
  • treatment supportive
  • stimulants incr mortatlity rate
  • may be cleared w/ diuresis, alkalization of urine
28
Q

benzodiazepines: gen info

A
  • most commonly used group anxiolytics & sedatives
  • CNS DEPRESSION
  • decrease in anxiety, followed by drowsiness
  • HYPNOSIS w/ high doses
29
Q

benzodiazepines: pharmacokinetics

A
  • PHARMACOKINETICS & DURATION OF ACTION VERY IMP IN DRUG OF CHOICE (drugs have very different half-lives & metabolites)
  • absorbed orally (IV emergency, pre-anesthesia)
  • not for elderly (don’t metabolize quickly)
30
Q

benzodiazepines: metabolism

A
  • metabolized by CYP3A4 in LIVER

- converted to active metabolites

31
Q

Which benzos have a LONG duration of action?

A
  • DIAZEPAM (t1/2 43 hrs) –> desmethyldiazepam (t1/2 24 hrs) –> oxazepan (t1/2 8 hrs) for total half life of 75 HOURS!!!
  • FLURAZEPAM (t1/2 74 hrs) converted to long acting metabolites
32
Q

Which benzos have INTERMEDIATE duration of action?

A
  • ALPRAZOLAM (t1/2 < 6 hrs) - converted to short acting metabolites

OXAZEPAM/LORAZEPAM (t1/2 6-24 hrs) - converted to inactive metabolites

33
Q

Which benzos have SHORT duration of action?

A
  • MIDAZOLAM (t1/2 < 2 hr) - for pre-anesthesia
34
Q

Benzodiazepines: moa

A
  • bind to GABA(a) receptor
  • EFFECT DEPENDENT ON GABA
  • increases affinity of receptor to GABA, prolonging action
  • CEILING EFFECT
35
Q

Benzodiazepines: uses (anxiety)

A
  • use lowest effective dose for shortest possible duration w/ fewest side effects
  • DOC BASED ON DURATION OF ACTION
36
Q

For which anxiety disorders are benzos NOT used?

KNOW THESE!!!

A
  • OCD (SSRIs)
  • agoraphobia/panic disorders (SSRIs)
  • PTSD (antidepressants)
  • anxiety in kids/teens (antidepressants)
37
Q

Benzodiazepines: uses (insomnia)

A
  • FLURAZEPAM & TEMAZEPAM = hypnotics
  • minor depression REM sleep, may cause “HANGOVER” effect
  • SHORTER ACTING DRUGS (good for person who has trouble just falling asleep)
38
Q

Benzodiazepines: uses (epilepsy/seizures)

A
  • DIAZEPAM & LORAZEPAM for STATUS EPILEPTICUS
39
Q

Benzodiazepines: uses (sedation, amnesia, anesthesia)

A
  • MIDAZOLAM - used in anesthesia for short procedures (given IV)
  • ANTEROGRADE AMNESIA
40
Q

Benzodiazepines: uses (muscle relaxant)

A
  • DIAZEPAM for acute muscle spasm and pain from injury
41
Q

Benzodiazepines: uses (withdrawal from alcohol and barbiturates)

A
  • CHLORDIAZEPOXIDE, DIAZEPAM, LORAZEPAM (long acting benzos) used for more tapered withdrawal
  • can prevent/treat seizures from withdrawal
42
Q

Benzodiazepines: side effects

A
  • CNS DEPRESSION (dizziness, drowsiness, sedation, impaired motor coordination, confusion, mem loss)
  • effects common first few weeks before tolerance
  • blurred vision/hallucinations (not common)
  • PARADOXICAL EXCITEMENT (due to DIS-INHIBITION OF SUPPRESSED BEHAVIOR), more common in elderly
  • SUPRA-ADDITIVE effects (+ effect w/ alcohol)
  • SLEEP RELATED BEHAVIORS (sleep eating, driving, walking, etc)
43
Q

Benzodiazepines: tolerance/dependence

A
  • common, but pts don’t increase dosage
  • HIGH ABUSE POTENTIAL
  • withdrawal –> anxiety, insomnia
44
Q

Benzodiazepines: contraindications

A
  • NOT DURING PREGNANCY UNLESS ABSOLUTELY NEC (CAT D)
  • SLEEP APNEA
  • ELDERLY
45
Q

Benzodiazepines: withdrawal

A
  • ABRUPT DISCONTINUATION can cause rebound insomnia, anxiety

- should be TAPERED SLOWLY following chronic use

46
Q

Benzodiazepines: overdose

A
  • BZs pretty safe
  • overdose = usu long sleep 24-48 hrs
  • fatalities w/ respiratory problems, children, when combined w/ alcohol
47
Q

Flumazenil: gen info

A
  • BENZODIAZEPINE ANTAGONIST
  • competes with benzos for GABA receptor, used to REVERSE effects of benzos (ie: reverse effect of MIDAZOLAM that causes resp depression)
  • reverses effects of Z-DRUGS
  • duration of action = 30 min
48
Q

Flumanezil: adverse effects

A
  • triggers withdrawal, seizures in pts who are physically dependent
49
Q

Flumanezil: contraindications

A
  • NOT FOR PTS w/ HX OF SEIZURES
50
Q

“Z” drugs: gen info/uses

A
  • Zolpidem, Zaleplon, Eszopiclone
  • bind to BZ1, increase GABA mediated inhibition
  • strong/rapid sedative effects
  • NO ANXIOLYTIC, ANTICONVULSANT, MUSCLE RELAXANT PROPERTIES
  • USED FOR INSOMNIA
51
Q

“Z” drugs: pharmacokinetics

A
  • orally absorbed
  • peak levels 30-60 min
  • metabolized in liver, excreted by kidney (half life can be longer in hepatic dz)
52
Q

Which “Z” drug has a longer half life?

A

Eszopiclone

53
Q

“Z” drugs: side effects

A
  • VERY HIGH MARGIN OF SAFETY
  • GI (diarrhea, nausea)
  • CNS (drowsiness, dizziness)
  • SLEEP-RELATED BEHAVIORS
  • amnesia with higher doses
  • w/ ELDERLY –> confusion, memory loss, psychosis
  • increase depressant effects of other drugs
  • low incidence tolerance, dependence
  • REBOUND INSOMNIA w/ rapid discontinuation
  • WITHDRAWAL SYMPTOMS w/ abrupt cessation after long term use eszopiclone
54
Q

Ramelteon: gen info

A
  • MELATONIN ANALOGUE
  • RESETS SLEEP-WAKE CYCLE
  • PROMOTES SLEEPINESS w/out GABA EFFECT
55
Q

Ramelteon: pharmacokinetics

A
  • orally absorbed, extensive first pass metabolism
  • metabolized by CYP450s in liver
  • ADDITIVE SEDATION w/ ALCOHOL AND OTHER SEDATIVE HYPNOTICS
56
Q

Ramelteon: side effects

A
  • FEW!

- DROWSINESS, DIZZINESS, NAUSEA

57
Q

Benadryl: gen info

A
  • ANTIHISTAMINE w/ sedative properties
  • USEFUL FOR OCCASIONAL INSOMNIA
  • good for ppl addicted to benzos or alcohol
58
Q

Chloral Hydrate: gen info

A
  • converted to TRICHLOROETHANOL - causes sedation
  • ACTS LIKE BARBITURATES ON GABA(a) RECEPTOR
  • LOW MARGIN SAFETY (high doses induce respiratory and vasomotor depression)
59
Q

Chloral Hydrate: side effects

A
  • gastric irritation, nausea, emesis
  • allergic responses
  • cardiac arrythmias
  • long term use LIVER DAMAGE & FATAL INTOXICATION
60
Q

Chloral Hydrate: uses

A
  • CHEAP!
  • kids during dental procedures
  • nursing homes, care institutions
61
Q

Buspirone: gen info

A
  • RELIEVES ANXIETY WITHOUT PRODUCES SEDATION
  • PARTIAL AGONIST AT POSTSYNAPTIC SEROTONIN RECEPTOR (inhibition cell signaling)
  • FULL AGONIST FOR PRESYNAPTIC SEROTONIN RECEPTOR (decreased release serotonin)
  • anxiolytic effect takes 2 wks to develop
  • NO MUSCLE RELAXANT/ANTICONVULSANT PROPERTIES
  • DOES NOT POTENTIATE CNS DEPRESSION w/ ALCOHOL OR BENZOS
62
Q

Buspirone: uses

A
  • anxiety, anxiety w/ depression
  • ADHD, pts w/ autism & anxiety
  • premenstrual syndrome
  • VERY LOW ADDICTION POTENTIAL - good for recovering addicts
  • not good for severe disorders
63
Q

Buspirone: pharmacokinetics

A
  • orally absorbed, sig first pass metabolism

- metabolized in LIVER (CYP3A4)

64
Q

Buspirone: side effects

A
  • fairly safe

- light-headedness, restlessness, HA, drowsiness, N/V

KG - pharmacology 3 (11 decks)

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