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Pharmacology > HNNS L18 - Sedatives And Hypnotics > Flashcards

HNNS L18 - Sedatives And Hypnotics Flashcards

1
Q

Diazepam

A 
Benzodiazepine
Both sedative and hypnotic 
Low dose for acute panic anxiety
Fast onset and offset
Long acting
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2
Q

Chlordiazepoxide

A

Benzodiazepine (sedative)
Low dose for chronic anxiety states
Long-acting

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3
Q

Alprazolam

A

Benzodiazepine (sedative)
Low dose for anxiolytic-antidepressant effect
Intermediate-acting

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4
Q

Lorazepam

A

Benzodiazepine (sedative)

Intermediate-acting

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5
Q

Clonazepam

A

Benzodiazepine (sedative)
Fast onset
Long-acting

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6
Q

Flurazepam

A

Benzodiazepine (hypnotics)
Long acting
High dose for sedative + hypnotic effects

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7
Q

Temazepam

A

Benzodiazepine (hypnotics)
Intermediate acting
High dose for sedative + hypnotic effects

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8
Q

Triazolam

A

Benzodiazepine (hypnotics)
Fast onset
Short acting
High dose for sedative + hypnotic effects

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9
Q

Flumazenil

A

Competitive antagonist of benzodiazepines (for overdose of BDZs and Zolpidem(?), IV)

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10
Q

MoA of Benzodiazepines

A

Activate GABA-A receptors by binding to BZ1 and BZ2 (between alpha and gamma subunits)
Increase frequency of Cl channel opening
Hyperpolarization
Increase inhibitory signals

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11
Q

Effects of Benzodiazepines

A

Anxiolytic
Induction of sleep
Reduce muscle tone and co-ordination
Anti-convulsant

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12
Q

Adverse effects of benzodiazepines

A
  • Drowsiness, confusion (most common)
  • Decrease in motor coordination
  • Decrease in psychomotor performances
  • Anterograde amnesia
  • Respiratory depression and death if taken with ethanol
  • Dependence
  • Tolerance
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13
Q

Flumazenil: MoA, Adverse effects

A

Competitive antagonist of BDZs at GABA-A receptor
- reversal of BDZ overdose (IV)

  • Dizziness, confusion, nausea
  • Agitation
  • Seizure
  • (Withdrawal)
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14
Q

Barbiturates: MoA

A

[1] Potentiate GABA action on Cl- entry into the neuron by prolonging the duration of Cl- channel openings

[2] Block excitatory glutamate AMPA receptors –> decreased glutamate-induced excitation

[3] Anaesthetic (high) concentrations of pentobarbital blocks high-frequency Na+ channels –> decrease neuronal activity

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15
Q

Barbiturates: adverse effects / disadvantages (X8)

A
  1. Drowsiness, decreased motor control
  2. Induction of hepatic CYP450, decrease effect of other drugs metabolized by these enzymes
  3. High degree of tolerance and dependence + very severe withdrawal symptoms
  4. High dose: respiratory depression, coma
  5. Low therapeutic index
  6. Increase in heme synthesis: contraindicated in porphyrias
  7. Sleep disturbance
  8. Used as hypnotics: suppress REM sleep more than other stages
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16
Q

Metabolism of BDZs

A

Conjugation with glucuronide

Urinary excretion

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17
Q

Midazolam

A

BDZ (short acting, half life <5 hours)

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18
Q

Long-acting BDZs

A

Chlordiazepoxide
Clonazepam*
Diazepam (Valium)*
Flurazepam

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19
Q

Intermediate-acting BDZs

A

Alprazolam
Lorazepam
Temazepam

20
Q

Short-acting BDZs

A

Midazolam

Triazolam

21
Q

Barbiturates: Metabolism

A 
Hepatic metabolism (some to active metabolites)
Induction of CYP450 (drug-drug interaction)
Increase in heme synthesis
22
Q

Thiopental

A

Ultra-short-acting barbiturate (10-20 min)

23
Q

Pentobarbital

A

Short-acting barbiturate (2-8 hr)

24
Q

Amobarbital

A

Short-acting barbiturate (2-8 hr)

25
Q

Secobarbital

A

Short-acting barbiturate (2-8 hr)

26
Q

Phenobarbital

A

Long-acting barbiturate (1-2 days)

27
Q

Ultra-short-acting barbiturates (10-20 min)

A

Thiopental

28
Q

Short-acting barbiturates (2-8 hours)

A

Pentobarbital
Amobarbital
Secobarbital

29
Q

Long-acting barbiturates (1-2 days)

A

Phenobarbital

30
Q

Buspirone (BuSpar): MoA and use

A 
Anxiolytic drug
- 5-HT1A 
- (DA2)
- (5-HT2A)
Slow onset
Used for treating general anxiety disorder (GAD) (with min sedation)
31
Q

Buspirone (BuSpar): Adverse effects / Disadvantages (X6)

A
  1. Headaches, Dizziness
  2. Nervousness
  3. Hypothermia
  4. Increase prolactin (breast enlargement; dopamine receptor)
  5. GI distress
  6. Drug-drug interaction: Metabolism by CYP3A4
    - Half-life shortened if taken with rifampin (inducer of CYP3A4)
    - Half-life lengthened if taken with erythromycin (CYP3A4 inhibitor)
32
Q

Hydroxyzine

A

1st generation anti-histamine with anti-emetic activity. Can be used as an anxiolytic.

33
Q

Antidepressants

A

[1] SSRI
[2] TCA
[3] MAOI
As an anxiolytic.

34
Q

Propranolol

A

Non-selective beta blocker (alleviate somatic manifestations of anxiety caused by marked sympathetic responses)

35
Q

Zolpidem (Z drug)

A

As a hypnotic:
Bind selectively to the BZ1 (subtype of BZ receptor family)
- Facilitate GABA-mediated neuronal inhibition

Antagonized by flumazenil
CYP450 metabolism to form inactive products (vs BDZs?)

36
Q

Zolpidem (Z drug): adverse effects (X6)

A
  1. Ataxia (loss of full control of bodily movements)
  2. Nightmares
  3. Agitation
  4. GI upset
  5. Headache
  6. Dizziness, daytime drowsiness, confusion
37
Q

Zolpidem (Z drug): vs BDZs

A 
Adv:
1. Less risk of developing tolerance and dependence with extended use
Disadv:
1. No anti-convulsant effect
2. No muscle-relaxing effect

(One is an anxiolytic, one causes agitation)

38
Q

Zaleplon (Z-drug)

A

Resemble zolpidem.
- Fewer residual effect on pseudo-motor and cognitive function
Rapid onset and short duration of action.

39
Q

Ramelteon

A

Hypnotic agent:
(1st line for insomnia, OTC)
Selective agonist of MT1 and MT2 melatonin receptors in hypothalamus

40
Q

Ramelteon: adverse effects

A
  1. Dizziness, frowsiness
  2. Fatigue
  3. Increased prolactin levels –> enlarged breasts
41
Q

Chloral hydrate

A

Effective sedative and hypnotic.
For diagnosis: check sleep pattern of patient.

Trichlorinated derivative of acetaldehyde
Converted to trichoroethanol, an active metabolite, in the body

Adverse effects:

  1. GI distress
  2. Unpleasant taste
42
Q

Diphenhydramine (Benadryl, Unisom SleepGels)

A

Antihistamine with sedating properties.

Adverse effects:

  1. Dry mouth
  2. Blurred vision
  3. Drowsiness
43
Q

Doxylamine

A

Antihistamine with sedating properties.

Adverse effects:

  1. Dry mouth
  2. Blurred vision
  3. Drowsiness
44
Q

Promethazine

A

Antihistamine with sedating properties.

Adverse effects:

  1. Dry mouth
  2. Blurred vision
  3. Drowsiness
45
Q

BDZs advantage over barbiturates (X8)

A
  1. Higher therapeutic index
  2. Not induce hepatic microsomal enzyme (CYP450), fewer drug-drug interaction
  3. Low abuse liability (less marked physical dependence and withdrawal symptoms)
  4. Lesser distortion of normal sleep (pattern, morning hangover)
  5. No hyperalgesia
  6. Not produce anaesthesia in high doses, patients can be aroused
  7. Not affect respiratory / CVS function (unless taken with ethanol)
  8. Specific antagonist (Flumazenil)

–> Can be used as daytime anxiolytics

Pharmacology (10 decks)

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