Introduction to Neuropharmacology

Question 1

Lidocaine

Answer 1

PRESYNAPTIC DRUG

Modifies Na+ VG channels - blocks the pore, which prevents Na+ entry

Used as a local anaesthic

Question 2

Carbamazepine

Answer 2

PRESYNAPTIC DRUG

Modify Na+ VG channels - stabilizes the inactivation gate

Used as an anti-epileptic drug

Question 3

Lamotrigine

Answer 3

PRESYNAPTIC DRUG

Inhibits Ca2+ VG channels - blocks the pore

Used as an anti-epileptic drug (for absence seizures)

Question 4

Botox

Answer 4

PRESYNAPTIC DRUG

Toxin from Clostridium bacteria
Enters axon terminal & degrades protein involved in PM docking (SNARE complex)

Only acts on cholinergic neurons

Used for cosmetic purposes & hyperactive muscles (stroke victims)

Question 5

Amphetamines

Answer 5

PRESYNAPTIC DRUG/SYNAPTIC DRUG

Increase NT release (excess)

• Excess SNS activation (sim. effects to NA)
• Reverses the direction of uptake transporters (pumps out NTs out into the cleft)

Question 6

SSRIs

Answer 6

SYNAPTIC DRUG

Selective Serotonin Reuptake Inhibitors

Blocks uptake transporters (dopamine, serotonin, NA, A…)

Treatment for depression (inc. dopamine levels in the cleft)

Question 7

MAOi

Answer 7

PRESYNAPTIC DRUG
Monoamines = Dopamine, Serotonin, NA
Breakdown NTs inside axon terminal (MAO)
2 types (A & B) - metabolize diff NTs

MAOi - increase accumulation of monoamines in axon terminal
More NT = released by vesicles
More NT = in cleft

Question 8

Donepezil

Answer 8

SYNAPTIC DRUG

Blocks Achase - Increases Ach levels in the cleft

Used in dementia

• Disease = d/t low cholinergic signaling
• Inc. in Ach = Dec. dementia SYMPTOMS

Question 9

Buspirone

Answer 9

Agonist for 5HT1 receptors

Treats anxiety

Question 10

Atypical Antipsychotics

Answer 10

Antagonist for 5HT2 receptors

Treats schizophrenia & bipolar

Question 11

Pramipexole

Answer 11

Agonist for D2 receptors

Treats Parkinson’s Disease

Question 12

Typical Antipsychotics

Answer 12

Antagonist for D2 receptors
Treats schizophrenia & bipolar
Too much dopamine = hallucinations (happens when PD patients take too high of a dose of Pramipexole/dopamine)

Question 13

Ach - 
NA - 
Serotonin - 
Dopamine - 
Glutamate - 
GABA -

Answer 13

Ach - Alzheimer’s, dementia, some movement
NA - anxiety, depression
Serotonin - depression, anxiety, schizophrenia
Dopamine - PD, schizophrenia, some movement disorders
Glutamate - epilepsy, AD, schizophrenia
GABA - anxiety, epilepsy

Question 14

Memantine

Answer 14

NMDA Antagonist

Treats dementia, ALS, PD

Question 15

GABAa Receptor

Answer 15

Cl- ion channel

Question 16

GABAb Receptor

Answer 16

GPCR

Question 17

Benzodiazepines

Answer 17

MODULATOR - NOT AGONIST

• Still requires GABA binding for GABAa channel activity
• Just increases GABA affinity
• Increases the f of channel opening

Treats anxiety & epilepsy

Question 18

Barbiturates

Answer 18

MODULATOR - NOT AGONIST

• Still requires GABA binding for GABAa channel activity
• Just increases GABA affinity
• Increases the length of channel opening (DANGEROUS)
• Causes greater degree of hyperpolarization
• Inc. resp. distress/depression
• Also affects metabolizing enzymes (CYP)

Treats anxiety & epilepsy