Dopamine- Metcalf

identify this structure

tyrosine

identify this structure

l dopa

identify this structure

dopamine

What enzyme metabolizes dopamine in path A? path b?

MAO

COMT

Identify the following structure

DA quinone

Identify the following environmental neurotoxicant

paraquat

Identify the following environmental neurotoxicant

rotenone

Identify the following toxic metabolite

MPP+

What type of bond is indicated by the red circle?

amide/ peptide bond

How many chiral centers does bromocriptine have?

6

Why is cabergoline not recommended for treating Parkinson's disease?

It's active at 5HT-2B receptors, which causes vascular heart disease especially with larger doses

Identify the following dopamine agonist (D2)

(S)-pramipexole

Identify the following dopamine agonist (D2)

ropinirol

Identify the following dopamine agonist that is available as a transdermal patch (D1/2/3)

rotigotine

Identify the following structure (AAD inhibitor)

S(-)-Carbidopa

What vitamin should not be taken with carbidopa/levodopa?

Vitamin B6 (pyridoxine) is a co-factor for AAD and can decrease CD's effectiveness

What MAOI's are contraindicated in combination with L-dopa?

Phenelzine and tranylcypromine due to risk of hypertensive crisis and delirium

Identify the following functional group

Propargyl group

what is the reversible MAO-B inhibitor

safinamide

what is the reversible COMT inhibitor

(E)-entacapone

Identify the following glutamate antagonist

amantadine

List substituents for position 2 in order of potency

SO2N(CH3)2 > CF3 > COCH3 >Cl

What substitution on position 10 position of typical antipsychotics is the most potent?

Piperazine, which also has increased risk of developing EPS

What substitution on position 10 position of typical antipsychotics is the least potent?

Aliphatic, which also has the highest amount of sedation and hypotension

Which configuration of thiothixene is more potent?

A, which is in the cis configuration and closer to the #2 position

How are phenothiazines metabolized?

N-dealkylation, S-oxidation to sulfone, and oxidation of aromatic ring which can undergo phase II metabolism

What must be present on a phenothiazine to be made into a prodrug?

A free hydroxyl so it can converted to an ester and add a long fatty acid chain to increase DOA, metabolized by esterase into active form

What is unique about diphenylbutyl butyrophenones?

Do not have ketones, increased duration of action

Which diphenylbutyl butyrophenone also treats Tourette syndrome?

pimozide

Identify the following structure

haloperidol metabolite

Why does haloperidol decanoate have a long duration of action?

a. The ester form is a long duration drug

b. The ester form is a prodrug serving as a depot of haloperidol

c. The ester form slowly releases the active drug as it is hydrolyzed

b. The ester form is a prodrug serving as a depot of haloperidol

What is an azepine?

a. Nitrogen containing heterocycle

b. Heterocycle containing two nitrogens

c. 7-membered nitrogen containing heterocycle

d. 7-membered heterocycle containing two nitrogens

c. 7-membered nitrogen containing heterocycle

Identify the following atypical antipsychotic

olanzapine

Identify the following atypical antipsychotic

Loxapine

Identify the following atypical antipsychotic that is also useful in treating depression

Amoxapine (Nor-loxapine)

Identify the following atypical antipsychotic

quetiapine

Identify the following atypical antipsychotic

Asenapine

Identify the following benzisoxazole

risperidone

Identify the following benzisoxazole

paliperidone

what is the only prodrug we talked about

haloperidol

1st generation antipsychotics

typical, block DA, high EPS risk, positive symptoms

2nd generation antipsychotics

atypical, other than or in addition to DA blockade, serotonin blocking, low EPS, positive and negative symptoms

5HT2B

antitarget cardiotoxic and produces vavulopathy

5HT2A

antagonism inhibits DA release, autoreceptor, decreases EPS