Advanced Pharm Test 2

Front 1

List 3 dopaminergic agents:

Back 1

Levodopa
Carbidopa/Levodopa
Amantadine

Front 2

mechanism of action of levodopa:

Back 2

• Biosynthetic precursor of dopamine
• Increases the concentration of dopamine in the brain.

Front 3

Levodopa is metabolized in the peripheral tissue by two enzymes

Back 3

• Decarboxilase
• COMT

Front 4

why is Carbidopa used in combination with Levodopa?

Back 4

o Carbidopa inhibits the conversion of levodopa in peripheral tissues through inhibition of decarboxalase
o Increases the amount of lebodopa that enters the brain
o Decreased GI and CV adverse effects because less levodopa in the peripheral tissue.

Front 5

What are the mechanism of action and adverse effects of Amantadine?
What type of drug is amantadine?

Back 5

Amantadine is a Dopaminergic agent used in the treatment of Parkinsons.
o Mechanism of action:
• Increases the release of dopamine from neurons in the brain.
• Inhibits the reuptake of dopamine by neurons
o Significant adverse effects:
• Confusion, hallucinations, insomnia, nightmares, peripheral edema.

Front 6

What type of drug is Selegaline?
What are its mechanism of action and adverse effects?

Back 6

- MOA-B inhibitor, used in the treatment of Parkinsons.
o Mechanism of action:
• Irreversibly inhibits MAO-B which degrades dopamine.
• Neuroprotective (blocks formation of free radicals released with dopamine degradations that contribute to neuronal degeneration).
o Significant adverse effects:
• Nausea, dizziness, orthostatic hypotension, hallucination, insomnia.

Front 7

What type of drugs are Tolcapone and Entacapone? What are their mechanisms of action and significant adverse effects?

Back 7

- COMT Inhibitor
o Mechanism of action:
• Inhibits peripheral metabolism of levodopa through inhibition of COMT.
o Used to enhance the effectiveness of levodopa.
o Significant adverse effects:
• Hepatotoxicity (not in Entacapone)
• Orthostatic hypotension
• Diarrhea
• Hallucinations

Front 8

List 4 dopamine receptor agonists:

Back 8

- Bromocriptine (Parlodel)
- Pramipexole (Mirapex)
- Ropinirole (Requip)
- Apomorphine (Apokyn)

Front 9

What are the mechanisms of action and adverse effects of Dopamine Receptor Agonists?

Back 9

o Mechanism of action:
• Directly activate the dopamine receptors (D2) in the brain
• Significatn Adverse effects:
• Nausea, hypotension, sedation and hallucinations.

Front 10

What are the advantages of Dopamine receptor agonists over Levodopa (Dopaminergic agent) ?

Back 10

• Direct action on receptor (no conversion of dopamine means less free radicals released)
• Longer half-life (not dosed as often)
• Given with OR without food (no absorption delay).

Front 11

List two Acetylcholine Receptor Antagonists:

Back 11

Benztropine
Trihexyphenidyl

Front 12

What are the mechanisms of action and adverse effects of Acetylcholine Receptor antagonists?

Back 12

o Mechanism of action:
• Help reduce tremor more than other manifestations of the disease
• May also inhibit the uptake of dopamine in the neutron of the brain
o Significant adverse effects:
• Sedation, depression, confusion
• Dry mouth, blurred vision, constipations, urinary retention.

Front 13

List two types of drugs that are used to treat Alzheimer's Disease?

Back 13

Cholinesterase inhibitors
NMDA receptor antagonists

Front 14

How do Cholinesterase inhibitors work to treat Alzheimer's Disease?

Back 14

- selectively inhibit cholinesterase in the CNS and increase acetylcholine levels in the cerebral cortex.
these agents may slow deterioration of cognitive function, but they do NOT affect the underlying neurodegenerative process.

Front 15

List 3 Cholinesterase Inhibitors and what these drugs are used for:

Back 15

- Donepezil (Aricept)
- Rivastigmine (Exelon)
- Galantamine (Razadyne)

- used for the treatment of Alzeimers disease.

Front 16

List significant adverse effects and drug interactions of Chilnesterase inhibitors used in the treatment of Alzheimers Disease:

Back 16

- Significant adverse effects: Bradycardia, Diarrhea, nausea, vomiting, Hepatotoxicity (tacrine, rivastigmine), gastrointestinal bleeding.
- drug interactions: anticholinergic drugs will inhibit the effects.

Front 17

What type of drug is Memantine and what is it used for? What are its MOA and adverse effects?

Back 17

A NMDA receptor antagonist, used in the treatment of Alzheimers disease.
- Noncompetitive antagonist at the NMDA receptor, attenuates the excitotoxic effects of glutamate.
- adverse effects: constipation, insomnia, headache, over excitation.