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pharmacology > Anxiolytics & Hypnotics > Flashcards

Anxiolytics & Hypnotics Flashcards

1
Q

What are anxiolytics?

A

drugs that decrease anxiety + stress

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2
Q

What are hypnotics?

A

A drug that induces sleep in insomnia

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3
Q

What is insomnia?

A

difficulty in initiation & maintenance of sleep

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4
Q

What is hypersomnia

A

excessive sleep or sleepiness

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5
Q

What does tolerance of a drug mean?

A

↓ drug effect requiring ↑ of dosage → same
effect

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6
Q

What is physical & physiological dependence?

A

stopping of a drug →
unpleasant symptoms

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7
Q

Classification of anxiolytics & hypnotics

A

1- barbiturates
2- benzodiazepines
3- 5-HT blockers
4- Miscellaneous

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8
Q

classification of benzodiazepines

A

1- hypnotics -> Flurazepam
2- anxiolytic -> Diazepam
3- anticonvulsant -> Clonazepam
4- anesthesia -> Midazolam
5- muscle relaxant -> Diazepam

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9
Q

what is an allosteric site example?

A

BZs don’t bind to GABA receptors themselves but they bind to one next to it to potentiate GABA receptors

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10
Q

mode of action of BZs

A

BZ binds to specific sites on the cell membrane adjacent to GABA receptors -> GABA receptors contain primary agonist binding site (GABA) & multiple allosteric sites -> conformational change in receptor -> cl- channel opens -> increase cl- conductance -> hyperpolarization -> CNS depression

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11
Q

BZs receptor ligands

A

Agonists: e.g. BZs & zolpidem → anxiolytic effect.
Antagonists: e.g. flumazenil→ block anxiolytic effect.
Inverse agonists: e.g. picrotoxin & β-carbolines -> anxiety & seizures (opposite of BZs, toxic CNS stimulant)

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12
Q

BZ Long-acting BZs 1-3 days

A

diazepam

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13
Q

BZ intermediate-acting 10-20 hrs

A

lorazepam

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14
Q

BZ short-acting 3-8 hrs

A

oxazepam

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15
Q

which BZ drug is most likely to be abused? what is its duration of action?

A

oxazepam

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16
Q

Metabolism & Excretion of BZs

A

liver microsomal enzymes
as glucuronides

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17
Q

Effects of BZ

A

1- Drowsiness, confusion -> extreme CNS depression
2- anterograde memory confusion -> useful in anesthesia
3- ataxia & respiratory depression -> extreme doses

18
Q

Overcoming toxicity of BZs

A

flumazenil IV

19
Q

Withdrawal symptoms of BZ

A

confusion, sweating, anxiety, agitation,
palpitation, restlessness, insomnia & tension
induced by short-acting derivatives >
long-acting ones (related to elimination t½)

20
Q

Interactions of BZ

A

Toxicity of alcohol & other CNS depressants.
Patients with hepatic dysfunction or hypersensitivity to BZs.
Enzyme inducers & inhibitors. (affects other drugs dosage)

21
Q

Action of Barbiturates

A

increase the opening duration of GABA receptors -> increase GABA transmission
decrease activation of glutamate receptors

21
Q

Pharma actions of barbiturates

A

sedation -> hypnosis -> anesthesia -> respiratory depression -> death

22
Q

therapeutic uses of barbiturates

A

anesthesia -> thiopental
anticonvulsant -> phenobarbital

23
Q

Barbiturates Long-acting 1-2 days

A

phenobarbital

24
Q

barbiturates short-acting 3-8 hours

A

secobarbital

25
Q

Barbiturates ultra short-acting 20 min

A

thiopental

26
Q

barbiturates metabolism + excretion

A

liver microsomal enzymes & in urine

27
Q

barbiturates side effects

A
  1. Drowsiness & impaired concentration.
  2. Drug hangovers.
  3. Respiratory & circulatory depression.
  4. Enzyme induction.
  5. Addiction
28
Q

barbiturates withdrawal

A

1- anxiety, tremors, weakness
2- seizures
3- nausea, vomiting
4- cardiac arrest, death

29
Q

Barbiturate management of toxicity

A

1- artificial respiratory
2- gastric lavage
3- hemodialysis
4- alkalinization of urine (changing ph of urine so it isn’t reabsorbed)

30
Q

barbiturates contraindications

A

1- hepatic or renal disease
2- drug interactions due to enzyme induction
3- allergic reactions

31
Q

barbiturates side effects

A

induces cytochrome p450s -> acute porphyria

32
Q

atypical drugs

A

1- drugs that act through BZ receptors
2- drugs that act through melatonin receptors
3- drugs that act through serotonin receptors
4- drugs that act through orexin receptors

33
Q

drugs that act through BZ receptors

A

ZOLPIDEM ZALEPLON
- increase in chloride channel flow
- bz1 receptor agonist
- less effect on cognition
- used in insomnia
- less likely to be abused

34
Q

drugs that act through melatonin receptors

A

RAMELTEON
- used in insomnia
- less likely to be abused

35
Q

drugs that act through orexin receptors

A

SUVOREXANT
-orexin receptor antagonist
-hypnotic properties
-HME interaction

36
Q

5-HT Receptor Antagonists (serotonin antagonist)

A

Buspirone
-selective anxiolytic
-no effect on GABA
-5-ht partial agonist
-GAD
- non-sedative
-safe in pregnancy + elderly
-slow onset

37
Q

Miscellaneous drugs classification

A

Chloral hydrate
hydroxine
b blockers
alcohol

38
Q

Chloral hydrate (miscellaneous drugs)

A

GIT Distress -> not used anymore

39
Q

hydroxine (miscellaneous drugs)

A

antihistaminic (main job) but crosses brain barrier so it has anxiolytic effects
useful in abuse history

40
Q

B blockers (miscellaneous drugs)

A

decrease tremors associated with anxiety e.g stage fright -> not safe tho

41
Q

Alcohol (miscellaneous drugs)

A

toxicity outweighs sedation
toxic effects: nausea, vomiting, drug abuse, liver cirrhosis
potentiates CNS depressants
DISULFIRAM to quit
Mechanism -> decrease aldehyde dehydrogenase -> increase acetyladehyde level -> flushing, hyperventilation, tachycardia, nausea

pharmacology (4 decks)

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