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M4 Pharm B3 > 2 - Sedative Hypnotics > Flashcards

2 - Sedative Hypnotics Flashcards

1
Q

Sedatives: Defined (3) and what level of CNS depression (1)

A

Decreases activity

Moderates excitement

Calms the recipient

Lowest level of CNS depression

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2
Q

Hypnotics Defined And Used for What?

A

Produces drowsiness and facilitates the onset and maintenance of a state of sleep that resembles natural sleep and form which the recipient can be aroused easily

Used for insomnia, for high doses

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3
Q

Classification of Sedative-Hypnotics: Long Acting Barbiturates (1) and Barbiturates in general bind between what 2 subunits?

A

Phenobartbital

Bind between alpha 1 and beta 2

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4
Q

Classification of Sedative-Hypnotics: Short Acting Barbiturates (2)

A

Pentobarbital

Secobarbital

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5
Q

Classification of Sedative-Hypnotics: Ultra Short Acting Barbiturates and are type of soluble? (3)

A

Thiopentone (Pentothal) –> lethal injection/truth serum

Methohexitone

Lipid-soluble, enter brain within seconds of IV administration

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6
Q

Classification of Sedative-Hypnotics: Benzodiazepines (BZDS) (10) and also bind between what 2 subunits?

A
  1. Diazepam (Valium)
  2. Chlordiazepoxide (Librium)
  3. Clonazepam
  4. Oxazepam
  5. Lorazepam (Ativan)
  6. Triazolam
  7. Flunitrazepam (Rohypnol, “Roofies”, anterograde amnesia)
  8. Nitrazepam (also a date rape drug)
  9. Alprazolam (Xanax, short acting)
  10. Midazolam (shortest acting, used in aneasthesia)

Bind between interface of alpha1 and gamma2

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7
Q

Classification of Sedative-Hypnotics: Newer Hypnotics (3) and effect on REM upon discontinuation

A

Zolpidem

Eszopiclone

Zaleplon

Don’t increase REM sleep duration upon discontinuation (less effect on sleep pattens)

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8
Q

Barbiturates: MOA (Pathway and 2 Facts)

A

Act on GABA-A (ionotropic) receptor Cl channel complex —>

Prolong DURATION of GABA-mediated chloride channel OPENINGS –>

Membrane hyperpolarization – inhibition

Also have inhibitory effects on glutamate receptors

High doses: GABA mimetic action

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9
Q

Benzodiazepines (BZDs) MOA Pathway

A

Act on GABA-A receptor Cl channel complex –>

Increased FREQUENCY of GABA-mediated chloride channel openings cause chloride influx –>

Membrane Hyperpolarization (membrane inhibition)

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10
Q

Zolpidem and Zaleplon MOA

A

Bind to GABA-A receptor isoforms that contain Alpha-1 subunits

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11
Q

Pharmacokinetics: Barbiturates

A

Activity of hepatic microsomal drug (CYP) –> metabolizing enzymes may be increased, so interfere with other drugs

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12
Q

Pharmacokinetics: Benzodiazepines - Phases 1 and 2 (2) and Exception (1)

A

Phase 1: undergo metabolism in liver

Phase 2: conjugation reaction outside of liver

Major route of metabolism for oxazepam and lorazepam –> conjugation (skip phase 1 and go directly to phase 2)

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13
Q

Sedative-Hypnotics Actions on CNS (2)

A

CNS: Dose dependent effects

Sedation (anxiolysis) –> sleep (hypnosis) –> anaesthesia –> coma

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14
Q

Sedative-Hypnotics Actions on CNS: Pentobarbital example, and curve for barbiturates and benzos

A

Low doses causes sedation (50-100 mg)

Hypnosis (100-200 mg)

Anesthesia (300-400 mg)

High doses can cause death (>600 mg)

Barbiturates: Curve is steep –> coma and death

Benzos –> Eventually flat, may not cause coma and death, so may be safer

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15
Q

Sedative-Hypnotics: Smaller Doses Effects (6)

A
  1. Reduction in anxiety
  2. Drowsiness
  3. Impaired motor coordination
  4. Impaired learning and memory
  5. Euphoria, impaired judgment, and loss of self-control (paradoxical reaction, due to LOSS of inhibition; dysinhibition of previously suppressed behavior)
  6. Anterograde amnesia (hangover movie)
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16
Q

Sedative-Hypnotics: Effects on Sleep Patterns (5)

A

1. Decreases latency of sleep onset

    1. Duration of stage 2 increased*
      - Sleep duration
  1. REM sleep is decreased
  2. Duration of stage 3 and 4 NREM slow-wave sleep is decreased
  3. On discontinuation
    • Rebound increase in REM sleep
    • Worsening insomnia irritability, dizziness, mood upset
17
Q

Sedative-Hypnotics: Anaesthesia in High Doses (3)

A
  1. Depress the CNS - general anaesthesia
  2. Thiopental, methohexital (ultra short acting) - inducing anaesthesia only
  3. Diazepam, lorazepam, and midazolam i.v anaesthesia, along with other agents to maintain anaesthesia
18
Q

Sedative-Hypnotics: Anticonvulsants (Benzos and Barbiturates) - MOA

A

Inhibit the development and spread of epileptiform electrical activity

19
Q

Sedative-Hypnotics: Anticonvulsants (Benzos and Barbiturates) - Drugs (4)

A

Clonezepam

Nitrazepam

IV Diazepam (1st line status epilepticus)

Phenobarbital (3rd line for status epilepticus)

20
Q

Sedative-Hypnotics: Skeletal Muscle Relaxation (Benzos only) (2)

A

Inhibitory effects polysynaptic reflexes and internuncial transmission and at high doses

May also depress transmission at the skeletal NMJ

21
Q

Sedative-Hypnotics: Effect on Respiratory System in High Doses (Barbiturates)

A

Lead to respiratory depression

22
Q

Sedative-Hypnotics: Effect on CVS in High Doses

A

Lead to fall in blood pressure

23
Q

Sedative-Hypnotics: Tolerance (1) and with Barbiturates and Benzos

A

Repeated use = a decrease in responsiveness

Barbiturates: induce their own metabolism so become less effective over time

Benzos: Receptors become desensitized, so need to increase the dose (may lead to addiction)

24
Q

Sedative-Hypnotics: Psychological Dependance

A

Compulsive use of the drug to relieve anxiety

25
Q

Sedative-Hypnotics: Physiologic Dependance

A

Altered physiologic state that requires continuous drug administration to prevent an abstinence or withdrawal syndrome (CNS excitation –> anxiety, insomnia, convulsions)

26
Q

Sedative-Hypnotics: Clinical Uses - Insomnia (3)

A

Barbiturates NOT preferred due to addiction risk and other side effects

Short acting BZDs: Flurazepam, Triazolam, Alprazolam

BEST: Zolpidem and Zaleplon –> less cognitive impairment, no rebound insomnia

27
Q

Sedative-Hypnotics: Clinical Uses - Anxiety (3 Drugs)

A

Alprazolam, Lorezepam, and Clonezepam –> more efficacy

28
Q

Sedative-Hypnotics: Clinical Uses - Epilepsy

A
  1. Phenobarbitone - Generalized tonic clonic seizures and status epilepticus (3rd line)
  2. BZDs- Diazepam-Status epilepticus (1st line), tetanus, febrile convulsions
29
Q

Sedative-Hypnotics: Induction of GA (2 Drugs)

A

Thiopentone, Midazolam

30
Q

Sedative-Hypnotics: Other Uses - Endoscopy and Bronchoscopy (2 Drugs)

A

Diazepam

Midazolam

31
Q

Sedative-Hypnotics: Other Uses - Premedication prior to?

A

Anesthesia to remove anxiety for surgery

32
Q

Sedative-Hypnotics: Other Uses - During Withdrawal from Physiologic Dependence on Ethanol (2 Drugs)

A

Long Acting Benzos: Diazepam and Chlordiazepoxide

33
Q

Sedative-Hypnotics: Other Uses - Delirium Tremens (Severe Alcohol Withdrawal) (1 Benzo drug)

A

Lorazepam –> preferred due to avoidance of metabolism in liver

34
Q

Sedative-Hypnotics: Other Uses - Central Muscle Relaxants (1)

A

Diazepam for spastic conditions (cerebral palsy)

35
Q

Sedative-Hypnotics: Adverse Effects (7)

A
  1. Psychomotor dysfunction:
  2. Hangover – Barbs and BZDs metabolites which have long half life
  3. Dependence
  4. Overdosage (Acute barbiturate poisoning)
    * 5. Porphyria – barbiturates (activates ALA synthase)* –> CONTRAINDICATED
  5. Can exacerbate breathing problems –COPD, OSA
  6. Drug interactions with barbiturates (OCP and Warfarin)
36
Q

Sedative-Hypnotics: Treatment of Barbiturate Poisoning (5)

A
  1. Gastric lavage
  2. Oxygen, supportive measures
    * 3. Forced alkaline diuresis: i.v sodium bicarbonate/NAHCO3*
  3. Hemodialysis
  4. No specific antidote
37
Q

Sedative-Hypnotics: Benzodiazepines Overdosage (Facts and Treatment, 3)

A

Is not as fatal as barbiturates

Specific antidote

Treatment: Flumazenil (BZD antagonist)

M4 Pharm B3 (9 decks)

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