Benzo

Question 1

Antischizophrenic drugs act on:

Answer 1

the dopamine pathways of the CNS

Question 2

Schizophrenia:

Answer 2

Elevated level of dopamine in the mesocortical pathway

Question 3

Specific receptor in schizophrenia:

Answer 3

D2 receptor for dopamine (is an inhibitory receptor)

Question 4

Dopaminergic receptors are (type of receptor)

Answer 4

GPCRs (which have inhibitory and excitatory pathways

Question 5

Chlorpromazine is

Answer 5

first effective neuroleptic drugs
Belong to the Phenothiazine family (block dopamine D2 receptor)
Block the symptoms of schizophrenia by occupying the dopamine site of D2 receptor (prevent activation of dopamine)

Question 6

Why Chlorpromazine had several side effect?

Answer 6

Because act as modulator but also directly on many others receptors (wide spread action) such as 5-HT, NA, cholinergic, adrenergic, histamine…

Question 7

3 main categories of antidepressant drugs?

Answer 7

1. Monoamine Oxidase Inhibitors (MAOIs)
2. Tricyclic Antidepressants (TCAs)
3. Selective Serotonin Reuptake Inhibitors (SSRIs)

Question 8

Antidepressant drugs are all doing the same thing:

Answer 8

Increasing the number of neurotransmitters in the synapse to increase the neurotransmission through the aminergic pathway.

Question 9

TCAs had many side effects because it also blocks various receptors such as:

Answer 9

Adrenergic receptor
Histamine receptor
Cholinergic muscarinic acetylcholine receptors (mAChRs)

Question 10

SSRI drugs (most commun)?

Answer 10

Fluoxetine (Prozac)

Question 11

SSRI target?

Answer 11

The reuptake of 5-HT (most focus on 5-HT3 receptors)

Question 12

5-HT3 receptor is a (type of receptor)?

Answer 12

Ligand-gated ion channel. (need 2 molecules of 5-HT to activate the receptor to open the channel for Na+)

Question 13

Benzodiazepines target:

Answer 13

GABA A receptors (Ligand-gated ion channel) (allosteric site)

Question 14

Benzodiazepine specific binding site located:

Answer 14

Jonction between the alpha and gamma subunits (require 2 GABAs bing to the receptor to activated and lead to influx of Cl-)

Question 15

Barbiturates are not safe compare to Benzodiazepine because:

Answer 15

Barbiturates increases the duration of opening but ALSO act directly on opening the channels

Question 16

Alpha 1unit related to: (effect and location)

Answer 16

Sedation/hypotonic in the cerebral cortex

Question 17

Alpha 2units related to: (effect and location)

Answer 17

Antianxiety in the hippocampus and amygdala.

Question 18

Benzodiazepine antagonist drugs:

Answer 18

Flumazenil

Question 19

Inverse agonists of benzodiazepines are:

Answer 19

Allosteric antagonists (weaken the function of GABA)
Shift GABA dose response curve to the right (Need more GABA to open channel)

Question 20

GABA B receptor:

Answer 20

Presynaptic receptors (G-coupled K channel)
Muscle relaxation (Parkinson disease)

Question 21

Drugs interaction with benzodiazepine:

Answer 21

Ketoconazole (antifungal drugs) inhibit the breakdown of benzo (accumulation in the body–>side effect)