Pharmacology VIII

Question 1

Name four strategic drug approaches used to treat Parkinson’s disease.

Answer 1

Dopamine agonists, increase dopamine levels, prevent dopamine breakdown, curb excess cholinergic activity (p.455)

Question 2

Name three dopamine agonist drugs.

Answer 2

Bromocriptine, pramipexole, ropinirole (p.455)

Question 3

What is the mechanism of action of Amantadine and what conditions is it used to treat?

Answer 3

Increases dopamine in treatment of Parkinson’s disease; also used as an antiviral against influenze A and rubella (p.455)

Question 4

What toxicity is associated with amantadine use?

Answer 4

Ataxia (p.455)

Question 5

What is the mechanism of action of L-dopa/carbidopa and what is it used to treat?

Answer 5

Treatment of Parkinson’s; Crosses BBB and converts to dopamine in the CNS by dopa decarboxylase (p.455, 456)

Question 6

What drugs prevent dopamine breakdown?

Answer 6

Selegine (selective Mao type B inhibitor), entacapone, tolcapone (p.455)

Question 7

What type of drugs are entacapone and tolcapone?

Answer 7

COMT inhibitors that prevent L-dopa degradation thereby increasing dopamine activity (p.455)

Question 8

What is the mechanism of action of Benztropine and what is it used to treat?

Answer 8

Antimuscarinic drug that improves tremor and rigidity associated with Parkinsons. It has little effect on bradykinesia however (p.455)

Question 9

Why is carbidopa given with L-dopa?

Answer 9

Carbidopa is a peripheral decarboxylase inhibitor given with L-dopa to increase bioavailability of L-dopa in the brain and to limit peripheral side effects (p.456)

Question 10

What toxicites are associated with L-dopa (levodopa) use?

Answer 10

Arrhythmias from increased formation of peripheral catecholamines; long term use can lead to dyskinesia following administration and akinesia between doses (p.456)

Question 11

What is the mechanism of action of Selegine?

Answer 11

Selective inhibition of MAO-B to preferentially metabolize dopamine over NE and 5-HT; increases dopamine availability (p.456)

Question 12

What is Selegine used for in the treatment of Parkinson’s?

Answer 12

As an adjunctive treatment to L-dopa (toxicity: may enhance L-dopa effects) (p.456)

Question 13

Name four drugs used in the treatment of Alzheimer’s disease.

Answer 13

Memantine, Donepezil, galantamine, rivastigmine (p.456)

Question 14

What is the mechanism of action of Memantine?

Answer 14

NMDA receptor antagonist that helps prevent excitotoxicity (mediated by Ca2+) (p.456)

Question 15

What toxicities are associated with use od Memantine?

Answer 15

Dizziness, confusion, hallucinations (p.456)

Question 16

What is the mechanism of action of donepezil, galantamine, and rivastigmine?

Answer 16

Acetylcholinesterase inhibitors (p.456)

Question 17

What toxicities are associated with use of donepezil, galantamine, and rivastigmine?

Answer 17

Nausea, dizziness, insomnia (p.456)

Question 18

What neurotransmitter changes are associated with Huntington’s disease?

Answer 18

Decreased GABA and Ach, increased dopamine (p.456)

Question 19

Name three drugs used to treat Huntington’s disease?

Answer 19

Tetrabenazine, reserpine, Haloperidol (p.456)

Question 20

What is the mechanism of action in Tetrabenzine and reserpine in treatment of Huntington’s?

Answer 20

Inhibit VMAT; limit dopamine vesicle packaging and release (p.456)

Question 21

What is the mechanism of action of haloperidol in treatment of Huntington’s?

Answer 21

Dopamine receptor antagonist (p.456)

Question 22

What is the mechanism of action of Sumatriptan?

Answer 22

5-HT(1b/1d) agonist that inhibits trigeminal nerve activation and prevents vasoactive peptide release; induces vasoconstriction (p.456)

Question 23

What is the half life of sumatriptan?

Answer 23

Less than 2 hours (p.456)

Question 24

What is sumatriptan used to treat?

Answer 24

Acute migraine, cluster headache attacks (p.456)

Question 25

What toxicities are associated with use of sumatriptan?

Answer 25

Coronary vasospasm, mild tingling (p.456)

Question 26

What condition makes use of sumatriptan contraindicated?

Answer 26

CAD or Prinzmetal’s angina (p.456)