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CNS Pharmacology > Anxiolytics & Sedative Hyponotics > Flashcards

Anxiolytics & Sedative Hyponotics Flashcards

1
Q

Mention drugs with sedative-hypnotic side effects

A

Antidepressants
Antipsychotics
Antihistamines
BBs

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2
Q

Classify GABA receptors with actions

A

GABA-A: mediate postsynaptic neuronal inhibition
GABA-B: metabotropic (Gi-protein linked), presynaptic neuronal inhibition by inhibiting Ca++ influx & postsynaptic by K+ outflux hyperpolarization.

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3
Q

GABA binding site is at……..

A

interface between alpha & beta sub

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4
Q

BZD binding site is on…..

A

Gamma subunit or an area on alpha subunit regulated by gamma

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5
Q

Alpha1 subunit mediates…….while alpha2 mediates……

A

Sedation/hypnosis
Anxiolytic & muscle relaxant actions

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6
Q

Barbiturates increase…….of opening of Cl- channels while BZD increase THE…..

A

Duration
Frequency

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7
Q

Describe mechanism of action of zolpidem

A

Binds to BZD1 receptor subtype with alpha1 subunit related to sedation & hypnosis, facilitation of GABA inhibitory effect

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8
Q

GR: Barbiturates are largely replaced by BZD

A
  1. Narrow therapeutic index (dose-dependent action leading eventually to coma & death)
  2. No specific antidote
  3. More drug dependence
  4. Enzyme induction occurs with barbiturates but not BZD
  5. Acute porphyria
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9
Q

GR: Barbiturates have more powerful CNS depressant action

A

They have GABA-mimetic action and can block AMPA-R of gluatamte in high conc or even directly block Na channel

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10
Q

Mention the untrashort acting barbiturate & its dosage form

A

Thiopental
IV anesthetic

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11
Q

Classify BZDs according to duration of action

A

Long, diazepam, clonazepam
Intermediate, alprazolam, lorazepam
Ultrashort acting, midazolam

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12
Q

The BZD with no active metabolites & can be given IM is…..

A

Lorazepam

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13
Q

Describe BZDs metabolism

A

Oxidation by CYP3A4 then glucoronidation or some are conjugated directly by gluco.

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14
Q

GR: The clinical duration of long-acting BZD does not correlate with their actual half life times

A

Because they form active metabolites with long hakf lifes also due to receptor dissocaition in CNS & subsequent redistribution to fatty tissues & other areas

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15
Q

Enumerate effect of BZD on sleep patterns

A
  1. Dec sleep latency
  2. Inc Stage 2 sleep
  3. Dec REM sleep& so dec memory consolidation
    4.dec stage 3& 4 NREM
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16
Q

Mention drugs metabolised directly by conjugation

A

Lorazepam
Oxazepam
Temazepam

17
Q

List pharmacological actions of BZDs

A

Anxiolytic/euphoric
Sedative/hypnotic
Anesthetic
Anticonvulsant
Skeletal muscle relaxant
Alcohol withdrawal (diazepam, long acting)

18
Q

Mention uses of BZDs as:
1. Anxiolytics
2. Sedative

A
  1. Anxiety & Panic disorders (Potentiate GABA in limbic system)
  2. Insomia, nightmares & night terrors (potentiate GABA in brainstem reticular formation)
19
Q

Mention uses of BZDs as:
1. Anesthetic
2. Anticonvulsant
3. Skeletal muscle relaxant

A
  1. Conscious sedation, pre-anesthesia, balanced anesthesia (midazolam)
  2. Epilepsy & status epilepticus (s.e.:diazepam)
  3. Muscle spasticity (in inflammation, trauma, cerebral palsy, MS)
20
Q

Mention adverse effects of BDZs

A
  1. Ataxia
  2. Anterograde amnesia
  3. Abuse
  4. Additive CNS depression
  5. Abnormal response (paradoxical excitement)
  6. Dowsiness, confusion, dec cognitive function, hangover
  7. Withdrawal of hypnotics, rebound insomnia & inc in REM sleep with nightmares
21
Q

Describe symptoms of BZD toxicity

A

Prolonged sleep
Respiratory & cardiovascular depression (rare except if given IV rapidly or with other CNS depressants

22
Q

Mention therapeutic uses of Flumazenil

A

Antidote to BZDs & zolpidem
Termination of their effect in anesthesia

23
Q

Mention adverse effects of flumazenil

A

Agitation
Withdrawal syndrome or convulsions in BZD dependent patients

24
Q

Mechanism of action of Zolpidem

A

Non-BZDs acting on BDZ1 receptor subtype involved in hypnosis

25
Q

Enumerate advantages of Zolpidem over BZDs

A
  1. Rapid onset
  2. Less hangover
  3. Less cognitive impairment
  4. Less tolerance & dependence with less rebound insomnia
  5. Less suppression of REM sleep
26
Q

…..is similar to zolpidem but with fewer effects on cognition & psychomotor function & rapid elimination

A

Zaleplon

27
Q

Mention adverse effects of eszopiclone

A

Anxiety, dry mouth, headache, peipheral edema, somnolence, unpleasant taste

28
Q

MT agonist is……, acts as…..
Mention its adverse effects

A

Ramelteon
Hypnotic
Dizziness, somnolence, fatigue

29
Q

Mention use of buspirone, its advantages & disadvatages

A

U, selective anxiolytic, chronic anxietry, generalized anxiety disorder
A, No amnesia or dec cognitive function or additive CNS depression with alcohol or other sedatives
No ataxia nor abuse
D, delayed onset, does not treat insomnia

30
Q

Agents uses to decrease sleep latency are…..while agents used for early morning awakening are……

A

Midazolam, lorazepam
Diazepam

31
Q

Chronic insomnia is usually treated with……

A

Antidepressant

32
Q

GR: BZD is added ti initial depression therapy

A

To calm the patient until antidepressant becomes effective

33
Q

…….is preferred in liver cirrhosis

A

Lorazepam

34
Q

GR: Dose of BZD should be reduced in elderly

A

To avoid accumulation (red liver metabolis) & prevent falls due to confusion/ataxia

CNS Pharmacology (11 decks)

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