Pharmacology VIII Flashcards
Name four strategic drug approaches used to treat Parkinson’s disease.
Dopamine agonists, increase dopamine levels, prevent dopamine breakdown, curb excess cholinergic activity (p.455)
Name three dopamine agonist drugs.
Bromocriptine, pramipexole, ropinirole (p.455)
What is the mechanism of action of Amantadine and what conditions is it used to treat?
Increases dopamine in treatment of Parkinson’s disease; also used as an antiviral against influenze A and rubella (p.455)
What toxicity is associated with amantadine use?
Ataxia (p.455)
What is the mechanism of action of L-dopa/carbidopa and what is it used to treat?
Treatment of Parkinson’s; Crosses BBB and converts to dopamine in the CNS by dopa decarboxylase (p.455, 456)
What drugs prevent dopamine breakdown?
Selegine (selective Mao type B inhibitor), entacapone, tolcapone (p.455)
What type of drugs are entacapone and tolcapone?
COMT inhibitors that prevent L-dopa degradation thereby increasing dopamine activity (p.455)
What is the mechanism of action of Benztropine and what is it used to treat?
Antimuscarinic drug that improves tremor and rigidity associated with Parkinsons. It has little effect on bradykinesia however (p.455)
Why is carbidopa given with L-dopa?
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)
What toxicites are associated with L-dopa (levodopa) use?
Arrhythmias from increased formation of peripheral catecholamines; long term use can lead to dyskinesia following administration and akinesia between doses (p.456)
What is the mechanism of action of Selegine?
Selective inhibition of MAO-B to preferentially metabolize dopamine over NE and 5-HT; increases dopamine availability (p.456)
What is Selegine used for in the treatment of Parkinson’s?
As an adjunctive treatment to L-dopa (toxicity: may enhance L-dopa effects) (p.456)
Name four drugs used in the treatment of Alzheimer’s disease.
Memantine, Donepezil, galantamine, rivastigmine (p.456)
What is the mechanism of action of Memantine?
NMDA receptor antagonist that helps prevent excitotoxicity (mediated by Ca2+) (p.456)
What toxicities are associated with use od Memantine?
Dizziness, confusion, hallucinations (p.456)
What is the mechanism of action of donepezil, galantamine, and rivastigmine?
Acetylcholinesterase inhibitors (p.456)
What toxicities are associated with use of donepezil, galantamine, and rivastigmine?
Nausea, dizziness, insomnia (p.456)
What neurotransmitter changes are associated with Huntington’s disease?
Decreased GABA and Ach, increased dopamine (p.456)
Name three drugs used to treat Huntington’s disease?
Tetrabenazine, reserpine, Haloperidol (p.456)
What is the mechanism of action in Tetrabenzine and reserpine in treatment of Huntington’s?
Inhibit VMAT; limit dopamine vesicle packaging and release (p.456)
What is the mechanism of action of haloperidol in treatment of Huntington’s?
Dopamine receptor antagonist (p.456)
What is the mechanism of action of Sumatriptan?
5-HT(1b/1d) agonist that inhibits trigeminal nerve activation and prevents vasoactive peptide release; induces vasoconstriction (p.456)
What is the half life of sumatriptan?
Less than 2 hours (p.456)
What is sumatriptan used to treat?
Acute migraine, cluster headache attacks (p.456)
What toxicities are associated with use of sumatriptan?
Coronary vasospasm, mild tingling (p.456)
What condition makes use of sumatriptan contraindicated?
CAD or Prinzmetal’s angina (p.456)
