Drugs

Question 1

Tacrine

Answer 1

Alzheimer’s
Cholinesterase Inhibitor
Hepatotoxic
Increases soluble APP

Question 2

Aricept

Answer 2

Alzheimer’s
Cholinesterase Inhibitor
Fewer side-effects than tacrine

Question 3

Memantine

Answer 3

Alzheimer’s

NMDA antagonist.

Question 4

Carbidopa

Answer 4

Parkinson’s
Dopa decarboxylase inhibitor.
Prevents break down of L-Dopa

Question 5

Bromocriptine

Answer 5

Parkinson’s
D2 agonist
Decreases cAMP levels

Question 6

Benztropine

Answer 6

Parkinson’s
Cholinergic antagonist
Reduces tremor and rigidity but NOT akinesia

Question 7

Phencyclidine

Answer 7

Schizophrenia
PCP/Angel dust
Best model of psychosis
Non-competitive NMDA receptor antagonist, decreases NMDA action as it binds IN the channel. 
"Open channel blocker"

Question 8

Neuroleptics

Answer 8

Schizophrenia

Increases glutamate release

Question 9

Cycloserine

Answer 9

Schizophrenia
Glycine site agonist on NMDA receptor
With neuroleptic: reduces negative symptoms

Question 10

Chlorpromazine

Answer 10

Schizophrenia
Typical drug
Best for positive symptoms
Tricyclic
DA antagonist for D2 and D4
Shows extrapyramidal side effects such as Dyskinesias and Parkinson’s symptoms
Side effect: Anti-muscarinic (dries secretions)

Question 11

Haloperidol

Answer 11

Schizophrenia
Typical drug
DA antagonist for D2 and D4 receptors
D2 up-regulated in cortex AND striatum
Shows extrapyramidal side effects such as Dyskinesias and Parkinson's symptoms

Question 12

Clozapine

Answer 12

Schizophrenia
Atypical drug
10 fold greater affinity for D4 receptors than D2 (dec. cAMP)
Reduces negative symptoms
No extrapyramidal symptoms as low D2 affinity
Up-regulates D2 in cortex
Side effect: Decreases macrophages

Question 13

Risperidone

Answer 13

Schizophrenia

DA and Serotonin antagonist

Question 14

Diazepam

Answer 14

Anxiety + Epilepsy (status epilepticus)
Benzodiazepine
GABAa agonist
Incr frequency of Cl- channel opening
Incr GABAergic inhibition in brain
Decreases anxiety/seizures/muscle tone
Increases sedation/sleep

Question 15

Midazolam

Answer 15

Anxiety (BZ)
Decreases anxiety
Pre-med used before surgery

Question 16

Flumazenil

Answer 16

Anxiety
Benzodiazepine antagonist (increases anxiety)
used to treat BZ overdose
Blocks effect of inverse agonists (B-carbolines)

Question 17

Beta-carbolines (FG7142)

Answer 17

Anxiety
Inverse agonist to BZ receptors
Increases anxiety

Question 18

Buspirone

Answer 18

Anxiety
Acts on Dorsal raphe nucleus, hippocampus, amygdala
Serotonin partial agonist
Binds to DA receptors too
Selective anxiolytic
Does NOT bind to GABAa/BZ receptors
May act on the 5-HT autoreceptors, decr. 5-HT from raphe nucleus, thus decr. anxiety

Question 19

Prozac

Answer 19

Anxiety: inhibits serotonin re-uptake, incr. synaptic levels

Question 20

Reserpine

Answer 20

Depression (monoamine theory)

Depletes monoamines -> Depression

Question 21

Amphetamine

Answer 21

Depression (MA theory)
Increases MA available, blocking reuptake
Increases mood

Question 22

Amitriptyline & Imipramine

Answer 22

Depression
Tricyclic - first generation drug
Blocks NA and 5-HT reuptake
Anti-muscarinic actions (dries secretions)

Question 23

Phenelzine

Answer 23

Depression
MAO inhibitor - first generation drug
Increases monoamine levels
Toxic, so less widely used

Question 24

Moclobemide

Answer 24

Depression
REVERSIBLE MAOa selective inhibitor - 2nd generation
Increase in NA and 5-HT
Doesn’t target dopamine

Question 25

Fluoxetine (prozac) | Paroxetine (aropax)

Answer 25

Depression SSRIs (Selective serotonin re-uptake inhibitors) Potent Better tolerated than tricyclic antidepressants

Question 26

Lithium carbonate

Answer 26

``` Depression Most effective treatment for BIPOLAR depression No effect on unipolar depression Stabilises manic and depressive phases Increases grey matter volume Stimulates neurogenesis ```

Question 27

Carbamazepine

Answer 27

Depression (BIPOLAR): Particularly for rapid cyclers ``` Epilepsy: Not absence Half life - 30-50 hours anticholinergic decrease in repetitive firing neurons ```

Question 28

Phenobarbitone

Answer 28

Epilepsy barbituate Increases Cl- channel opening of GABAa ( incr. inhibition) Used mainly for tonic/clonic seizures Half life = 50-140 hours Increases lipid solubility (getting through membranes) Tolerance issues

Question 29

Phenytoin

Answer 29

Epilepsy Antiepileptic lacking sedative effects (good thing) Partial and tonic/clonic seizures (not absence) Stabilises inactive form of Na channel (decreases repetitive firing)

Question 30

Sodium valproate

Answer 30

Depression (BIPOLAR): Particularly for rapid cyclers Epilepsy: short chain fatty acid half life = 15 hours some hepatotoxicity For absence epilepsy (inhibits T-type Ca currents) Blocks GABA transaminase (increases GABA in brain)

Question 31

Felbamate

Answer 31

Epilepsy NEW complex partial seizures MAY block NMDA receptors

Question 32

Gabapentin

Answer 32

Epilepsy NEW partial and tonic/clonic MOA unclear

Question 33

Lamotrigine

Answer 33

Epilepsy NEW partial and tonic/clonic MOA: reduces glutamate release

Question 34

Vigabatrin

Answer 34

Epilepsy NEW good for childhood epilepsy