CNS pharmacology

Question 1

BZD-long acting

Answer 1

Chlorazepate
chlordiazepoxid
Diazepam
flurazepam
Quazepam

Question 2

BZD-intermediate acting

Answer 2

alprazolam
estazolam
lorazepam
temazepam
nitrazepam
clonazepam

Question 3

BZD -short acting

Answer 3

midazolam
oxazepam
triazolam

I: used as anxiolytics in short procedures like colonoscopy.

Question 4

Flumazenil

Answer 4

GABA-A receptor ATG.

antidote for BZD overdose

Question 5

alprazolam

clonazepam

Answer 5

BZDs. indicated in panic attacks. Most powerful anxiolytics out of the BZDs.
alprazolam-short acting
clonazepam

Question 6

Diazepam

Answer 6

BZD. long acting.
Indications:
central sk. muscle relaxant (sk. muscle spasms), epileptic state (also lorazepam), premedication before anesthesia, alcohol withdrawal, endoscopic procedures.

Question 7

Temazepam

Answer 7

BZD. short acting.

I: hypnotic - sleep disorders (in inability to stay asleep)

Question 8

Triazolam

Answer 8

BZD. short acting.

I: insomnia- difficulty falling asleep.

Question 9

clonazepam

Answer 9

BZD.

I: chronic tr. of absence seizures

Question 10

midazolam

Answer 10

BZD.

I: is a hypnotic. induction of general anesthesia (part of TIVA),

Question 11

Anxiolytic BZD

Answer 11

chlordiazepoxide
diazepam
clonazepam
alprazolam
oxazepam
lorazepam

Question 12

hypnotic BZDs

sleep inducing

Answer 12

midazolam
nitrazepam
flunitrazepam
triazolam
lorazepam

Question 13

BZD side effects

Answer 13

sedation, hangover effect (daytime sedation), dependence (more pronounced in short-acting BZDs), tolerance, anterograde amnesia, non-physiological sleep (increased REM), in elderly: confusion, ataxia, violence, withdrawal symptoms (anxiety, twitching muscles, high dose: seizures, hallucinations, fever, tremor)

Question 14

BZD indications

Answer 14

anxiety
insomnia
antiepileptic (epileptic state (diazepam), prevention of epileptic attacks - last choice)
sk. muscle relaxant
amnesia
predication before anesthesia
panic attacks
alcohol withdrawal

Question 15

Barbiturates - long acting

Answer 15

1-2 days

phenobarbital

Question 16

Barbiturates - short acting

Answer 16

3-8 hours
pentobarbital
secobarbital
amobarbital
cyclobarbital
amobarbital

Question 17

Barbiturates - ultra-short acting

Answer 17

20 min
thiopental
methohexital
hexobarbital

Question 18

Barbiturates, action and adverse effects

Answer 18

increase the duration of GABA A receptor opening. At high doses: directly activate GABA-A receptors.
SE: addiction, drowsiness, nausea, dizzoness, tremors, enzyme induction (CYP450), low therapeutic window, dependence and tolerance

Question 19

phenobarbital

Answer 19

barbiturate. long acting.
I: long term tr. of tonic-clonic seizures (last choice!), refractory status epilepticus
SE: strong enzyme inducer

Question 20

Thiopental (methohexital and hexobarbital). I, SE

Answer 20

Indication: IV anestetics
SE: rebound sedation (patient moves after anesthesia - drug redistributed to sk.muscle will enter circulation again)

Question 21

non-benzodiazepines anxiolytics

Answer 21

antidepressants -SSRIs, Buspirone

Question 22

anxiety disorders, treamtent

Answer 22

BZDs - immediate action. clonazepam, alprazolam, lorazepam. Short term use only (in beginning of treatment, in combo with SSRIs).
SSRIs - long term
Buspirone - 5-HT1A partial AG

Question 23

BZDs used in anxiety disorder

Answer 23

Clonazepam, alprazolam, lorazepam

Question 24

Buspirone

Answer 24

a 5-HT1A partial AG. only anxiolytic effect (no sedation, hypnotic, anticonvulsant or muscle relaxant effect). no dependence, no ethanol interaction.
Slow onset of action, not effective in panic disorders.

Question 25

Non-BZD hypnotics

Answer 25

Z-compounds: Zopiclone, Zolpidem, Zaleplone, esZopiclone.
Ramelteon
Suvorexant

Question 26

Zopiclone, Zolpidem, Zaleplone, eszopiclone

mechanism of action, indications, side effects

Answer 26

Bind to GABA-A receptors with alpha1 subunit (hypnotic), to the BZD receptor subunit.
Rapid onset of action.
I: insomnia (minor effect on physiological sleep patterns). Zolpidem, zaleplon: sleep onset. eszopiclone: sleep onset and maintenance.
SE: Zolpidum: nightmares, agitation, dizziness, amnesia etc.
Eszopiclone: anxiety, dry mouth, headache, somnolence, periph. edema. less risk of dependence and tolerance compared to BZDs.

Question 27

Ramelteon (and tasimelteon)

mech. of action, I, SE

Answer 27

melatonin 1 and 2 receptor AG. also tasimelteon.
I: insomnia.
SE: dizziness, fatigue, headache

Question 28

Suvorexant

mech of action, I, SE

Answer 28

Orexin R ATG
I: insomnia,
SE: unusual dreams, not always effective.

Question 29

drugs with sedative-hypnotic side effects

Answer 29

H1 ATGs (diphenhydramine, doxylamine)
antipsychotics and antidepressants
Alpha 2 AG (clonidine, dexmedetomidine
Opiates
antiepileptics like: pregabaline, vigabatrine, topiramate
Scopolamine