Neuro Drugs 2 - Sedatives and Hypnotics

Question 1

Adverse effects: Barbiturates

Phenobarbital

Pentobarbital

Thiopental

Secobarbital

Answer 1

1. Respiratory and CV depression (can be fatal)
2. CNS depression (exacerbated by EtOH)
3. Dependence
4. P-450 inducer
5. OD treatment: Supportive

Question 2

Clinical use: Barbiturates

Phenobarbital

Pentobarbital

Thiopental

Secobarbital

Answer 2

1. Sedative for anxiety, seizures, insomnia
2. Induction of anesthesia (Thiopental)

Question 3

Short-acting BDZs [4]

Answer 3

1. Alprazolam
2. Triazolam
3. Oxazepam
4. Midazolam

Higher addictive potential

Less daytime side effects

Question 4

BDZs with no active metabolites [4]

Answer 4

1. Oxazepam
2. Temazepam
3. Lorazepam
4. Clonazepam

Question 5

Clinical use: BDZs

Answer 5

1. Anxiety
2. Spasticity
3. Status epilepticus (Lorazepam, Diazepam)
4. Eclampsia
5. Detoxicification (EtOH withdrawal - DTs)
6. Night terrors
7. Sleepwalking
8. General anesthetic (amnesia, muscle relaxation)
9. Hyponotic (insomnia)

Question 6

Do not use BDZs with [4]

Answer 6

1. EtOH
2. Barbs
3. Neuroleptics
4. 1st generation anti-histamines

Question 7

Adverse effects: BDZs

Answer 7

1. Dependence
2. Additive CNS depression effects with EtOH
3. Less risk of respiratory depression/coma than barbiturates
4. Treat OD: Flumazenil (competitive antagonist at GABA receptor)
   
   • Can precipitate seizures by causing acute BDZ withdrawal

Question 8

Mechanism: Non-BDZ hypnotics

Zolpidem

Zaleplon

Eszopiclone

Answer 8

Act via the BZ1 subtype of the GABA receptor

Effects reversed by Flumazenil

Sleep cycle less affected as compared with BDZ hypnotics

Question 9

Clinical use: Non-BDZ hypnotics

Zolpidem

Zaleplon

Eszopiclone

Answer 9

Insomnia

Question 10

Adverse effects: Non-BDZ hypnotics

Zolpidem

Zaleplon

Eszopiclone

Answer 10

1. Ataxia, headache, confusion
2. Short duration - rapid metabolism by liver
3. Only modest day-after psychomotor depression and few amnestic effects
4. Decreased dependence risk than BDZs

Question 11

Mechanism: Suvorexant

Answer 11

Orexin (hypocretin) receptor antagonist

Question 12

Clinical use: Suvorexant

Answer 12

Insomnia

Question 13

Adverse effects: Suvorexant

Answer 13

1. CNS depression
2. Headache
3. Dizziness
4. Abnormal dreams
5. Upper respiratory tract infection
6. C/I: Narcolepsy, strong CYP3A4 inhibitors
7. Not recommended in patients with liver disease
8. No or low physical dependence

Question 14

Mechanism: Ramelteon

Answer 14

Melatonin receptor agonist

Binds MT1 and MT2 in suprachiasmatic nucleus

Question 15

Clinical use: Ramelteon

Answer 15

Insomnia

(best for elderly)

Question 16

Adverse effects: Ramelteon

Answer 16

1. Dizziness
2. Nausea
3. Fatigue
4. Headache
5. No dependence (not controlled substance)

Question 17

Mechanism: Triptans

Sumatriptan

Answer 17

5-HT_1B/1D agonists

Inhibit trigeminal nerve activation

Prevent vasoactive peptide release

Induce vasoconstriction

Question 18

Clinical use: Triptans

Sumatriptan

Answer 18

1. Acute migraine
2. Cluster headache attacks

Question 19

Adverse effects: Triptans

Sumatriptan

Answer 19

1. Coronary vasospasm
   
   • C/I in CAD, Prinzmetal angina
2. Mild paresthesia
3. Serotonin syndrome
   (in combination with other 5-HT agonists)