CNS Depressants + More

Question 1

CNS Depressants Properties

Answer 1

-Dose-dependent increase
-Raise seizure threshold
-Psychomotor impairment
-Drowsy/confusion/amnesia
-Additive, synergistic effects
-Tolerance (cross)
-Physical dependence
-Substance abuse disorder

Question 2

Benzodiazepines

Answer 2

PAMs and LAMs

MOA: increase aff GABAa receptors

AE:
-Drowsy
-Confusion
-Amnesia
-Psychomotor impair
-Substance use disorder (tol/wd)

Question 3

BDZs that skip Phase 1

Answer 3

-Oxazepam
-Temazepam
-Lorazepam

FOR PTS
-Drugs that inhibit CYP
-Elderly
-Liver disease

Question 4

BDZ Treatment

Answer 4

-Selection based on pharmacokinetics
-Duration: shortest time possible, >1 month = taper dose down
-Age and hepatic function of pt

Question 5

Flumazenil

Answer 5

MOA: BZD comp antagonist

USE:
-Antidote for BDZ overdose
-Anesthesiology to reverse BDZ

Question 6

Zolpidem, Zaleplon, Eszopiclone

Answer 6

Z compounds

MOA: increase aff to GABAa

USE: insomnia only

AE: fewer than BDZ (same but less occurrence)

Can be long-term (ZOL/ESZO)

Question 7

Ramelteon

Answer 7

MOA: melatonin receptor agonist (MT1/2)

USE: insomnia (sleep onset)

Less efficacious - ONLY approved sedative hypnotic drug that is not scheduled substance

Question 8

Suvorexant

Answer 8

MOA: Orexin antagonist (OX1/2)

USE: insomnia

AE: suv is the SIS
-Sedation
-Impaired driving
-Substance use disorder

Question 9

Barbiturates: Pentobarbital

Answer 9

MOA: increase aff GABAa

USE: insomnia/seizure

-Supplanted by BDZs

Tolerance, physical dependence, addition potential, low therapeutic index, CYP induction, long half life

Question 10

Diphenhydramine,
Doxylamine (first-generation)

Answer 10

MOA: H1 receptor antagonist

USE: insomnia

AE:
-Sedation
-Anticholinergic

Question 11

Psychostimulants

Answer 11

– Drugs that produce temporary improvements in mental and/or physical function
* Increase arousal, attention, wakefulness
* Increase mood (maygeuphoria)
* Increase motor performance
* Increase respiration
* Decrease appetite

Abuse
-Euphoria, academic benefit, weight loss

Question 12

Amphetamine

Answer 12

MOA: displaces stored catecholamines

USE: ADHD, sleepiness/narcolepsy

AE: CABIG
-NE (Increase BP, CA, insomnia)
-DA (Growth inhibition)
-5HT (Anorexia)

Question 13

Methylphenidate

Answer 13

MOA: blocks NET/DAT, increase DA/NE

USE: ADHD, sleepiness/narcolepsy

AE: like amphetamine

Question 14

Modafinil, Armodafinil

Answer 14

MOA: blocks NET/DAT, increase DA/NE

USE: excessive sleepiness (narc, etc)

AE: less than others