Nervous System Drugs - Classes

Question 1

Cyclobenzaprine

Answer 1

Centrally acting skeletal muscle relaxant

Structurally related to TCAs, similar anticholinergic side effects

Question 2

Propofol

Answer 2

IV anesthetic

Potentiates GABAa

Question 3

Benztropine

Answer 3

Antimuscarinic: Improves tremor and rigidity but has little effect on bradykinesia in Parkinson disease

Question 4

Rocuronium

Answer 4

Non-depolarizing NM blocking drug:

Competitive antagonists (compete with ACh for receptors)

Reversal: Neostigmine, edrophonium, other AChE inhibitors (must be given with atropine to prevent muscarinic effects such as bradycardia)

Question 5

Secobarbital

Answer 5

Bariturate: Faciliate GABAa action by increasing duration of Cl channel opening, thus decreasing neuron firing

Question 6

Tacrine

Answer 6

AChE inhibitor

Alzheimer disease drug

Question 7

Dantrolene

Answer 7

Prevents release of Ca²⁺ from SR of skeletal muscle by binding to the ryanodine receptor

Uses:

Malignant hyperthermia

Neuroleptic malignant syndrome (NMS)

Question 8

Amantadine

Answer 8

Increases DA release and decreases DA reuptake

Parkinson drug

Question 9

Loperamide

Answer 9

Act as agonists at opioid receptors to modulate synaptic transmission - open K⁺ channels, close Ca²⁺ channels → decrease synaptic transmission

Inhibit release of:

1. ACh
2. NE
3. 5-HT
4. Glutamate
5. Substance P

Question 10

Butorphanol

Answer 10

k-opioid receptor agonist

mu-opioid receptor partial agonist

Produces analgesia

Question 11

Isoflurane

Answer 11

Inhaled anesthetic

Question 12

Cocaine

Answer 12

Local anesthetic

Ester (one eyed ester)

Question 13

Thiopental

Answer 13

Bariturate: Faciliate GABAa action by increasing duration of Cl channel opening, thus decreasing neuron firing

IV anesthetic (induction of anesthesia)

Question 14

Eszopiclone

Answer 14

Non-BDZ hypnotic:

Act via BZ1 subtype of the GABA receptor

Effects reversed by flumazenil

Sleep cycle less affected as compared with BDZs

Question 15

Sumatriptan

Answer 15

5-HT_1B/1D agonist:

Inhibits trigeminal nerve activation

Prevent vasoactive peptide release

Induce vasoconstriction

Question 16

Zaleplon

Answer 16

Non-BDZ hypnotic:

Act via BZ1 subtype of the GABA receptor

Effects reversed by flumazenil

Sleep cycle less affected as compared with BDZs

Question 17

Tetracaine

Answer 17

Local anesthetic

Ester (one eyed ester)

Question 18

Riluzole

Answer 18

Decreases glutamate excitotoxicity via an unclear mechanism

Treatment for ALS (modestly improves survival)

Question 19

Chlordiazepoxide

Answer 19

Benzodiazepine: Facilitate GABAa action by increasing frequency of Cl channel opening

Question 20

Desflurane

Answer 20

Inhaled anesthetic

Question 21

Tubocurarine

Answer 21

Non-depolarizing NM blocking drug:

Competitive antagonists (compete with ACh for receptors)

Reversal: Neostigmine, edrophonium, other AChE inhibitors (must be given with atropine to prevent muscarinic effects such as bradycardia)

Question 22

Rivastigmine

Answer 22

AChE inhibitor

Alzheimer disease drug

Question 23

Morphine

Answer 23

Act as agonists at opioid receptors to modulate synaptic transmission - open K⁺ channels, close Ca²⁺ channels → decrease synaptic transmission

Inhibit release of:

1. ACh
2. NE
3. 5-HT
4. Glutamate
5. Substance P

Question 24

Fentanyl

Answer 24

Opioid: Used with other CNS depressants during general anesthesia

Question 25

Zolpidem

Answer 25

**Non-BDZ hypnotic:** Act via **BZ1 subtype** of the GABA receptor Effects reversed by **flumazenil** Sleep cycle less affected as compared with BDZs

Question 26

Codeine

Answer 26

Act as **agonists at opioid receptors** to modulate synaptic transmission - open K⁺ channels, close Ca²⁺ channels → decrease synaptic transmission **Inhibit release of:** 1. ACh 2. NE 3. 5-HT 4. Glutamate 5. Substance P

Question 27

Galantamine

Answer 27

**AChE inhibitor** Alzheimer disease drug

Question 28

Methadone

Answer 28

Act as **agonists at opioid receptors** to modulate synaptic transmission - open K⁺ channels, close Ca²⁺ channels → decrease synaptic transmission **Inhibit release of:** 1. ACh 2. NE 3. 5-HT 4. Glutamate 5. Substance P

Question 29

Donepezil

Answer 29

**AChE inhibitor** Alzheimer disease drug

Question 30

Trihexyphenidyl

Answer 30

**Antimuscarinic:** Improves tremor and rigidity but has little effect on bradykinesia in Parkinson disease

Question 31

Arylcyclohexylamines: **Ketamine**

Answer 31

**IV anesthetic: PCP analog** that acts as a dissociative anesthetic Block NMDA receptors CV stimulant

Question 32

Diazepam

Answer 32

**Benzodiazepine:** Facilitate GABAa action by increasing **frequency** of Cl channel opening

Question 33

Name the **benzodiazepines** that are **metabolized outside the liver** (**no active metabolites**; better in elderly patients)

Answer 33

**O**xazepam **T**emazepam **L**orazepam **C**lonazepam

Question 34

Oxycodone

Answer 34

Act as **agonists at opioid receptors** to modulate synaptic transmission - open K⁺ channels, close Ca²⁺ channels → decrease synaptic transmission **Inhibit release of:** 1. ACh 2. NE 3. 5-HT 4. Glutamate 5. Substance P

Question 35

Entacapone

Answer 35

**COMA inhibitor:** Prevents peripheral L-DOPA degradation to **3-O-methyldopa (3-OMD)** by inhibiting COMT Parkinson drug

Question 36

Meperidine

Answer 36

Act as **agonists at opioid receptors** to modulate synaptic transmission - open K⁺ channels, close Ca²⁺ channels → decrease synaptic transmission **Inhibit release of:** 1. ACh 2. NE 3. 5-HT 4. Glutamate 5. Substance P

Question 37

Benzocaine

Answer 37

Local anesthetic Ester (one eyed ester)

Question 38

Ramelteon

Answer 38

**Melatonin receptor agonist:** Binds **MT1** and **MT2** in suprachiasmatic nucleus

Question 39

Carbidopa

Answer 39

**Peripheral DOPA decarboxylase inhibitor:** Blocks peripheral conversion of L-DOPA to dopamine by inhibiting **DOPA decarboxylase** Parkinson drug

Question 40

Rasagiline

Answer 40

**Selective MAO-B inhibitor:** Blocks **CENTRAL (post-BBB)** conversion of DA to DOPAC Parkinson drug

Question 41

Pentobarbital

Answer 41

**Bariturate:** Faciliate GABAa action by increasing **duration** of Cl channel opening, thus decreasing neuron firing

Question 42

Tramadol

Answer 42

**Very weak opioid agonist** Also **inhibits 5-HT** and **NE reuptake** (works on multiple neurotransmitters

Question 43

Midazolam

Answer 43

**Benzodiazepine:** Facilitate GABAa action by increasing frequency of Cl channel opening ## Footnote **IV anesthetic**

Question 44

Name the **short-acting benzodiazepines** Less daytime side effects Higher addictive potential

Answer 44

**A**lprazolam **T**rizolam **O**xazepam **M**idazolam

Question 45

Sevoflurane

Answer 45

Inhaled anesthetic

Question 46

Tolcapone

Answer 46

**COMT inhibitor:** Prevents peripheral **AND CENTRAL** L-DOPA degradation to **3-O-methyldopa (3-OMD)** by inhibiting **COMT** Parkinson drug

Question 47

Lidocaine

Answer 47

Local anesthetic Amide (one eyed ester)

Question 48

Pentazocine

Answer 48

**k-opioid** receptor **agonist** **mu-opioid** receptor weak antagonist/partial agonsit

Question 49

Diphenoxylate

Answer 49

Act as **agonists at opioid receptors** to modulate synaptic transmission - open K⁺ channels, close Ca²⁺ channels → decrease synaptic transmission **Inhibit release of:** 1. ACh 2. NE 3. 5-HT 4. Glutamate 5. Substance P

Question 50

Suvorexant

Answer 50

Orexin (hypocretin) receptor antagonist

Question 51

Pramipexol

Answer 51

**Dopamine agonist (non-ergot - preferred)** Parkinson drug

Question 52

Vecuronium

Answer 52

**Non-depolarizing NM blocking drug**: Competitive antagonists (compete with ACh for receptors) **Reversal:** Neostigmine, edrophonium, other AChE inhibitors (must be given with **atropine** to prevent muscarinic effects such as bradycardia)

Question 53

Ropinirole

Answer 53

**Dopamine agonist (non-ergot - preferred)** Parkinson drug

Question 54

Treatment and MOA for **malignant hyperthermia**

Answer 54

**Dantrolene:** Ryanodine receptor antagonist → decreases calcium release from SR

Question 55

Bupivacaine

Answer 55

Local anesthetic Amide (one eyed ester)

Question 56

Reserpine

Answer 56

**Vesicular monoamine transporter (VMAT) inhibitor:** Decrease DA vesicle packaging and release Huntington disease drug

Question 57

Phenobarbital

Answer 57

**Bariturate:** Faciliate GABAa action by increasing **duration** of Cl channel opening, thus decreasing neuron firing

Question 58

Enflurane

Answer 58

Inhaled anesthetic

Question 59

Dextromethorphan

Answer 59

Act as **agonists at opioid receptors** to modulate synaptic transmission - open K⁺ channels, close Ca²⁺ channels → decrease synaptic transmission **Inhibit release of:** 1. ACh 2. NE 3. 5-HT 4. Glutamate 5. Substance P

Question 60

Succinylcholine

Answer 60

**Depolarizing NM blocking drug:** **Strong ACh receptor agonist →** produces sustained depolarization and prevents muscle contraction

Question 61

Bromocriptine

Answer 61

**Dopamine agonist (ergot)** Parkinson drug

Question 62

Pancuronium

Answer 62

**Non-depolarizing NM blocking drug**: Competitive antagonists (compete with ACh for receptors) **Reversal:** Neostigmine, edrophonium, other AChE inhibitors (must be given with **atropine** to prevent muscarinic effects such as bradycardia)

Question 63

Atracurium

Answer 63

**Non-depolarizing NM blocking drug**: Competitive antagonists (compete with ACh for receptors) **Reversal:** Neostigmine, edrophonium, other AChE inhibitors (must be given with **atropine** to prevent muscarinic effects such as bradycardia)

Question 64

Methoxyflurane

Answer 64

Inhaled anesthetic

Question 65

Mepivacaine

Answer 65

Local anesthetic Amide (one eyed ester)

Question 66

Tetrabenazine

Answer 66

**Vesicular monoamine transporter (VMAT) inhibitor:** Decrease DA vesicle packaging and release Huntington disease drug

Question 67

Fentanyl

Answer 67

Act as **agonists at opioid receptors** to modulate synaptic transmission - open K⁺ channels, close Ca²⁺ channels → decrease synaptic transmission **Inhibit release of:** 1. ACh 2. NE 3. 5-HT 4. Glutamate 5. Substance P

Question 68

Mivacurium

Answer 68

**Non-depolarizing NM blocking drug**: Competitive antagonists (compete with ACh for receptors) **Reversal:** Neostigmine, edrophonium, other AChE inhibitors (must be given with **atropine** to prevent muscarinic effects such as bradycardia)

Question 69

Memantine

Answer 69

**NMDA receptor antagonist** Helps prevent excitotoxicity (mediated by Ca²⁺) Alzheimer disease drug

Question 70

Selegiline

Answer 70

**Selective MAO-B inhibitor:** Blocks conversion of DA to DOPAC Parkinson drug

Question 71

Procaine

Answer 71

**Local anesthetic:** Blocks Na⁺ channels by binding to specific receptors on inner portion of channel Ester (one eyed ester)

Question 72

Haloperidol

Answer 72

**D₂ receptor antagonist** Huntington disease drug

Question 73

Nitrous oxide (N₂O)

Answer 73

**Inhaled anesthetic** Low blood/lipid solubility Fast induction; Low potency

Question 74

Treat BDZ OD with \_\_\_. What is the mechanism?

Answer 74

**Flumazenil:** Competitive antagonist at GABAa receptor

Question 75

Baclofen

Answer 75

**Activates GABA_B receptors** at spinal cord level, inducing skeletal muscle relaxation

Question 76

Halothane

Answer 76

**Inhaled anesthetic** High lipid/blood solubility Slow induction; high potency