Movement Disorder Drugs Flashcards
What is the drug class of Levodopa/Carbidopa?
Dopamine precursor and decarboxylase inhibitor
What is the mechanism of action of Levodopa/Carbidopa?
Levodopa is converted to dopamine in the brain, while carbidopa inhibits the peripheral breakdown of levodopa, increasing its availability to the brain.
What are the drug targets of Levodopa/Carbidopa?
Dopamine receptors in the brain
What is the expected time for effect of Levodopa/Carbidopa?
30 minutes to 2 hours
What is the pharmacodynamics of Levodopa/Carbidopa?
Increases dopamine levels in the brain to improve motor function in Parkinson’s disease.
What are the pharmacokinetics of Levodopa/Carbidopa?
Rapidly absorbed from the small intestine, widely distributed in the body, crosses the blood-brain barrier, primarily excreted in urine, and metabolized in the liver and peripheral tissues.
What are the dosage ranges for Levodopa/Carbidopa?
Varies based on individual response and disease severity
What are the key features of Levodopa/Carbidopa?
May cause dyskinesia, nausea, and orthostatic hypotension
What is the drug class of Pimavanserin?
Atypical antipsychotic
What is the mechanism of action of Pimavanserin?
Selective serotonin inverse agonist and antagonist at 5-HT2A receptors
What are the drug targets of Pimavanserin?
5-HT2A receptors
What is the expected time for effect of Pimavanserin?
Several weeks
What is the pharmacodynamics of Pimavanserin?
Modulates serotonin activity to reduce psychosis in Parkinson’s disease
What are the pharmacokinetics of Pimavanserin?
Well absorbed orally, widely distributed, high protein binding, primarily excreted in feces, and metabolized by CYP3A4 and CYP3A5.
What are the dosage ranges for Pimavanserin?
Typically 34 mg once daily
What are the key features of Pimavanserin?
Black box warning for increased mortality in elderly patients with dementia-related psychosis
What is the drug class of Pramipexole?
Dopamine agonist
What is the mechanism of action of Pramipexole?
Stimulates dopamine receptors in the brain
What are the drug targets of Pramipexole?
Dopamine D2 and D3 receptors
What is the expected time for effect of Pramipexole?
1 to 3 hours
What is the pharmacodynamics of Pramipexole?
Mimics dopamine to improve motor function in Parkinson’s disease
What are the pharmacokinetics of Pramipexole?
Well absorbed orally, widely distributed, low protein binding, primarily excreted unchanged in urine, and minimal hepatic metabolism.
What are the dosage ranges for Pramipexole?
Varies based on individual response and disease severity
What are the key features of Pramipexole?
May cause sleep attacks, hallucinations, and compulsive behaviors
What is the drug class of Selegiline?
MAO-B inhibitor
What is the mechanism of action of Selegiline?
Inhibits monoamine oxidase B, increasing dopamine levels in the brain
What are the drug targets of Selegiline?
Monoamine oxidase B enzyme
What is the expected time for effect of Selegiline?
Several weeks
What is the pharmacodynamics of Selegiline?
Increases dopamine levels to improve motor function in Parkinson’s disease
What are the pharmacokinetics of Selegiline?
Well absorbed orally, widely distributed, crosses the blood-brain barrier, primarily excreted in urine, and metabolized in the liver to active metabolites.
What are the dosage ranges for Selegiline?
Typically 5 to 10 mg daily
What are the key features of Selegiline?
May cause insomnia, nausea, and hypertensive crisis with high tyramine intake
What is the drug class of Tolcapone?
COMT inhibitor
What is the mechanism of action of Tolcapone?
Inhibits catechol-O-methyltransferase, increasing levodopa levels in the brain
What are the drug targets of Tolcapone?
Catechol-O-methyltransferase enzyme
What is the expected time for effect of Tolcapone?
1 to 2 hours
What is the pharmacodynamics of Tolcapone?
Increases levodopa levels to improve motor function in Parkinson’s disease
What are the pharmacokinetics of Tolcapone?
Well absorbed orally, widely distributed, crosses the blood-brain barrier, primarily excreted in urine, and metabolized in the liver.
What are the dosage ranges for Tolcapone?
Typically 100 to 200 mg three times daily
What are the key features of Tolcapone?
Black box warning for hepatotoxicity, requires liver function monitoring
What is the drug class of Apomorphine?
Dopamine agonist
What is the mechanism of action of Apomorphine?
Stimulates dopamine receptors in the brain
What are the drug targets of Apomorphine?
Dopamine D2 receptors
What is the expected time for effect of Apomorphine?
10 to 20 minutes
What is the pharmacodynamics of Apomorphine?
Mimics dopamine to improve motor function in Parkinson’s disease
What are the pharmacokinetics of Apomorphine?
Rapidly absorbed subcutaneously, widely distributed, crosses the blood-brain barrier, primarily excreted in urine, and metabolized in the liver.
What are the dosage ranges for Apomorphine?
Varies based on individual response and disease severity
What are the key features of Apomorphine?
May cause nausea, vomiting, and orthostatic hypotension
What is the drug class of Baclofen?
Muscle relaxant
What is the mechanism of action of Baclofen?
Activates GABA-B receptors, inhibiting neurotransmitter release
What are the drug targets of Baclofen?
GABA-B receptors
What is the expected time for effect of Baclofen?
1 to 2 hours
What is the pharmacodynamics of Baclofen?
Reduces muscle spasticity
What are the pharmacokinetics of Baclofen?
Well absorbed orally, widely distributed, crosses the blood-brain barrier, primarily excreted unchanged in urine, and minimal hepatic metabolism.
What are the dosage ranges for Baclofen?
Typically 5 to 20 mg three times daily
What are the key features of Baclofen?
May cause drowsiness, dizziness, and withdrawal symptoms with abrupt discontinuation
What is the drug class of Tetrabenazine?
VMAT2 inhibitor
What is the mechanism of action of Tetrabenazine?
Inhibits vesicular monoamine transporter 2, reducing dopamine release
What are the drug targets of Tetrabenazine?
Vesicular monoamine transporter 2
What is the expected time for effect of Tetrabenazine?
Several weeks
What is the pharmacodynamics of Tetrabenazine?
Reduces chorea in Huntington’s disease
What are the pharmacokinetics of Tetrabenazine?
Well absorbed orally, widely distributed, crosses the blood-brain barrier, primarily excreted in urine, and metabolized in the liver to active metabolites.
What are the dosage ranges for Tetrabenazine?
Typically 12.5 to 50 mg daily
What are the key features of Tetrabenazine?
Black box warning for depression and suicidal thoughts
What is the drug class of Haloperidol?
Typical antipsychotic
What is the mechanism of action of Haloperidol?
Blocks dopamine D2 receptors in the brain
What are the drug targets of Haloperidol?
Dopamine D2 receptors
What is the expected time for effect of Haloperidol?
Several days to weeks
What is the pharmacodynamics of Haloperidol?
Reduces psychosis and agitation
What are the pharmacokinetics of Haloperidol?
Well absorbed orally, widely distributed, high protein binding, primarily excreted in urine, and metabolized in the liver.
What are the dosage ranges for Haloperidol?
Typically 0.5 to 20 mg daily
What are the key features of Haloperidol?
May cause extrapyramidal symptoms, tardive dyskinesia, and neuroleptic malignant syndrome
What is the drug class of Riluzole?
Glutamate inhibitor
What is the mechanism of action of Riluzole?
Inhibits glutamate release and blocks sodium channels
What are the drug targets of Riluzole?
Glutamate receptors and sodium channels
What is the expected time for effect of Riluzole?
Several weeks
What is the pharmacodynamics of Riluzole?
Slows progression of amyotrophic lateral sclerosis (ALS)
What are the pharmacokinetics of Riluzole?
Well absorbed orally, widely distributed, crosses the blood-brain barrier, primarily excreted in urine, and metabolized in the liver.
What are the dosage ranges for Riluzole?
Typically 50 mg twice daily
What are the key features of Riluzole?
May cause liver toxicity, requires liver function monitoring
What is the drug class of Tacrine?
Acetylcholinesterase inhibitor
What is the mechanism of action of Tacrine?
Inhibits acetylcholinesterase, increasing acetylcholine levels in the brain
What are the drug targets of Tacrine?
Acetylcholinesterase enzyme
What is the expected time for effect of Tacrine?
Several weeks
What is the pharmacodynamics of Tacrine?
Improves cognitive function in Alzheimer’s disease
What are the pharmacokinetics of Tacrine?
Well absorbed orally, widely distributed, crosses the blood-brain barrier, primarily excreted in urine, and metabolized in the liver.
What are the dosage ranges for Tacrine?
Typically 10 to 40 mg four times daily
What are the key features of Tacrine?
May cause liver toxicity, requires liver function monitoring
What is the drug class of Memantine?
NMDA receptor antagonist
What is the mechanism of action of Memantine?
Blocks NMDA receptors, reducing excitotoxicity
What are the drug targets of Memantine?
NMDA receptors
What is the expected time for effect of Memantine?
Several weeks
What is the pharmacodynamics of Memantine?
Improves cognitive function in Alzheimer’s disease
What are the pharmacokinetics of Memantine?
Well absorbed orally, widely distributed, crosses the blood-brain barrier, primarily excreted unchanged in urine, and minimal hepatic metabolism.
What are the dosage ranges for Memantine?
Typically 5 to 20 mg daily
What are the key features of Memantine?
May cause dizziness, headache, and confusion