Anxiolytics & Hypnotics

Question 1

What are anxiolytics?

Answer 1

drugs that decrease anxiety + stress

Question 2

What are hypnotics?

Answer 2

A drug that induces sleep in insomnia

Question 3

What is insomnia?

Answer 3

difficulty in initiation & maintenance of sleep

Question 4

What is hypersomnia

Answer 4

excessive sleep or sleepiness

Question 5

What does tolerance of a drug mean?

Answer 5

↓ drug effect requiring ↑ of dosage → same
effect

Question 6

What is physical & physiological dependence?

Answer 6

stopping of a drug →
unpleasant symptoms

Question 7

Classification of anxiolytics & hypnotics

Answer 7

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

Question 8

classification of benzodiazepines

Answer 8

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

Question 9

what is an allosteric site example?

Answer 9

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

Question 10

mode of action of BZs

Answer 10

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

Question 11

BZs receptor ligands

Answer 11

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)

Question 12

BZ Long-acting BZs 1-3 days

Answer 12

diazepam

Question 13

BZ intermediate-acting 10-20 hrs

Answer 13

lorazepam

Question 14

BZ short-acting 3-8 hrs

Answer 14

oxazepam

Question 15

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

Answer 15

oxazepam

Question 16

Metabolism & Excretion of BZs

Answer 16

liver microsomal enzymes
as glucuronides

Question 17

Effects of BZ

Answer 17

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

Question 18

Overcoming toxicity of BZs

Answer 18

flumazenil IV

Question 19

Withdrawal symptoms of BZ

Answer 19

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

Question 20

Interactions of BZ

Answer 20

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

Question 21

Action of Barbiturates

Answer 21

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

Question 21

Pharma actions of barbiturates

Answer 21

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

Question 22

therapeutic uses of barbiturates

Answer 22

anesthesia -> thiopental
anticonvulsant -> phenobarbital

Question 23

Barbiturates Long-acting 1-2 days

Answer 23

phenobarbital

Question 24

barbiturates short-acting 3-8 hours

Answer 24

secobarbital

Question 25

Barbiturates ultra short-acting 20 min

Answer 25

thiopental

Question 26

barbiturates metabolism + excretion

Answer 26

liver microsomal enzymes & in urine

Question 27

barbiturates side effects

Answer 27

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

Question 28

barbiturates withdrawal

Answer 28

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

Question 29

Barbiturate management of toxicity

Answer 29

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

Question 30

barbiturates contraindications

Answer 30

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

Question 31

barbiturates side effects

Answer 31

induces cytochrome p450s -> acute porphyria

Question 32

atypical drugs

Answer 32

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

Question 33

drugs that act through BZ receptors

Answer 33

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

Question 34

drugs that act through melatonin receptors

Answer 34

RAMELTEON - used in insomnia - less likely to be abused

Question 35

drugs that act through orexin receptors

Answer 35

SUVOREXANT -orexin receptor antagonist -hypnotic properties -HME interaction

Question 36

5-HT Receptor Antagonists (serotonin antagonist)

Answer 36

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

Question 37

Miscellaneous drugs classification

Answer 37

Chloral hydrate hydroxine b blockers alcohol

Question 38

Chloral hydrate (miscellaneous drugs)

Answer 38

GIT Distress -> not used anymore

Question 39

hydroxine (miscellaneous drugs)

Answer 39

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

Question 40

B blockers (miscellaneous drugs)

Answer 40

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

Question 41

Alcohol (miscellaneous drugs)

Answer 41

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