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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
barbiturates: withdrawal
- CAN BE SEVERE - restlessness, anxiety, weakness, orthostatic hypotension, hyperactive reflexes, seizures
26
barbiturates: overdose/toxicity
- major problem - LOW MARGIN OF SAFETY - NO "CEILING EFFECT" - effects SUPRA-ADDITIVE, esp w/ alcohol - overdose = coma, resp depression, decr BP
27
barbiturates: how to treat overdose/toxicity?
- treatment supportive - stimulants incr mortatlity rate - may be cleared w/ diuresis, alkalization of urine
28
benzodiazepines: gen info
- most commonly used group anxiolytics & sedatives - CNS DEPRESSION - decrease in anxiety, followed by drowsiness - HYPNOSIS w/ high doses
29
benzodiazepines: pharmacokinetics
- 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
benzodiazepines: metabolism
- metabolized by CYP3A4 in LIVER | - converted to active metabolites
31
Which benzos have a LONG duration of action?
- 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
Which benzos have INTERMEDIATE duration of action?
- ALPRAZOLAM (t1/2 < 6 hrs) - converted to short acting metabolites OXAZEPAM/LORAZEPAM (t1/2 6-24 hrs) - converted to inactive metabolites
33
Which benzos have SHORT duration of action?
- MIDAZOLAM (t1/2 < 2 hr) - for pre-anesthesia
34
Benzodiazepines: moa
- bind to GABA(a) receptor - EFFECT DEPENDENT ON GABA - increases affinity of receptor to GABA, prolonging action - CEILING EFFECT
35
Benzodiazepines: uses (anxiety)
- use lowest effective dose for shortest possible duration w/ fewest side effects - DOC BASED ON DURATION OF ACTION
36
For which anxiety disorders are benzos NOT used? | KNOW THESE!!!
- OCD (SSRIs) - agoraphobia/panic disorders (SSRIs) - PTSD (antidepressants) - anxiety in kids/teens (antidepressants)
37
Benzodiazepines: uses (insomnia)
- FLURAZEPAM & TEMAZEPAM = hypnotics - minor depression REM sleep, may cause "HANGOVER" effect - SHORTER ACTING DRUGS (good for person who has trouble just falling asleep)
38
Benzodiazepines: uses (epilepsy/seizures)
- DIAZEPAM & LORAZEPAM for STATUS EPILEPTICUS
39
Benzodiazepines: uses (sedation, amnesia, anesthesia)
- MIDAZOLAM - used in anesthesia for short procedures (given IV) - ANTEROGRADE AMNESIA
40
Benzodiazepines: uses (muscle relaxant)
- DIAZEPAM for acute muscle spasm and pain from injury
41
Benzodiazepines: uses (withdrawal from alcohol and barbiturates)
- CHLORDIAZEPOXIDE, DIAZEPAM, LORAZEPAM (long acting benzos) used for more tapered withdrawal - can prevent/treat seizures from withdrawal
42
Benzodiazepines: side effects
- 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
Benzodiazepines: tolerance/dependence
- common, but pts don't increase dosage - HIGH ABUSE POTENTIAL - withdrawal --> anxiety, insomnia
44
Benzodiazepines: contraindications
- NOT DURING PREGNANCY UNLESS ABSOLUTELY NEC (CAT D) - SLEEP APNEA - ELDERLY
45
Benzodiazepines: withdrawal
- ABRUPT DISCONTINUATION can cause rebound insomnia, anxiety | - should be TAPERED SLOWLY following chronic use
46
Benzodiazepines: overdose
- BZs pretty safe - overdose = usu long sleep 24-48 hrs - fatalities w/ respiratory problems, children, when combined w/ alcohol
47
Flumazenil: gen info
- 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
Flumanezil: adverse effects
- triggers withdrawal, seizures in pts who are physically dependent
49
Flumanezil: contraindications
- NOT FOR PTS w/ HX OF SEIZURES
50
"Z" drugs: gen info/uses
- Zolpidem, Zaleplon, Eszopiclone - bind to BZ1, increase GABA mediated inhibition - strong/rapid sedative effects - NO ANXIOLYTIC, ANTICONVULSANT, MUSCLE RELAXANT PROPERTIES - USED FOR INSOMNIA
51
"Z" drugs: pharmacokinetics
- orally absorbed - peak levels 30-60 min - metabolized in liver, excreted by kidney (half life can be longer in hepatic dz)
52
Which "Z" drug has a longer half life?
Eszopiclone
53
"Z" drugs: side effects
- 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
Ramelteon: gen info
- MELATONIN ANALOGUE - RESETS SLEEP-WAKE CYCLE - PROMOTES SLEEPINESS w/out GABA EFFECT
55
Ramelteon: pharmacokinetics
- orally absorbed, extensive first pass metabolism - metabolized by CYP450s in liver - ADDITIVE SEDATION w/ ALCOHOL AND OTHER SEDATIVE HYPNOTICS
56
Ramelteon: side effects
- FEW! | - DROWSINESS, DIZZINESS, NAUSEA
57
Benadryl: gen info
- ANTIHISTAMINE w/ sedative properties - USEFUL FOR OCCASIONAL INSOMNIA - good for ppl addicted to benzos or alcohol
58
Chloral Hydrate: gen info
- converted to TRICHLOROETHANOL - causes sedation - ACTS LIKE BARBITURATES ON GABA(a) RECEPTOR - LOW MARGIN SAFETY (high doses induce respiratory and vasomotor depression)
59
Chloral Hydrate: side effects
- gastric irritation, nausea, emesis - allergic responses - cardiac arrythmias - long term use LIVER DAMAGE & FATAL INTOXICATION
60
Chloral Hydrate: uses
- CHEAP! - kids during dental procedures - nursing homes, care institutions
61
Buspirone: gen info
- 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
Buspirone: uses
- 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
Buspirone: pharmacokinetics
- orally absorbed, sig first pass metabolism | - metabolized in LIVER (CYP3A4)
64
Buspirone: side effects
- fairly safe | - light-headedness, restlessness, HA, drowsiness, N/V

KG - pharmacology 3 (11 decks)

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