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29 Cards in this Set
- Front
- Back
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What are the names of the three drugs used to treat ALS? What are their mechanisms of action? |
ANTISPASMODIC/MUSCLE RELAXANTS: 1. Baclofen: GABAB agonist 2. Tizanidine: alpha 2 adrenergic agonist
REDUCES EXCITOTOXICITY (can prolong patient survival and decrease progression, but NOT reverse damage): 3. Riluzole: blocks voltage gated Na channels; inhibits presynaptic release of glutamate; blocks NMDA and kainate receptors |
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In treatment of Parkinson: Best results of levodopa are in the first few years of treatment. Unfortunately, the effects diminish 3-4 years after therapy begins. Why does this occur? |
-loss of dopaminergic nigrostriatal nerve terminals -reduction in dose due to adverse effects -tolerance |
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What is the problem with administration of levodopa? How is this problem minimized? |
90 % of levodopa taken b.o.p. is destroyed in the gut due to peripheral metabolism (although, it is well absorbed by GI tract, if not destroyed and taken on an empty stomach) Give carbidopa -Carbidopa inhibits DOPA carboxylase which converts levodopa to dopamine = more levodopa will cross BBB before being converted to dopamine _____________ levodopa alone: brain gets 1- 3% levodopa levodopa/carbidopa: brain gets 10% levodopa |
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What are the adverse effects of levodopa? |
nausea vomiting loss of appetite |
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With administration of levodopa, what is the "on-off phenomenon"? |
alternating periods of mobility and immobility --may be due to fluctuating levels of dopamine in the basal ganglia or chronic stimulation of dopamine receptors --smaller doses at more frequent intervals can help |
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What is a drug interaction associated with levodopa? |
antipsychotic drugs -- this is because antipsychotics block dopamine receptors, while levodopa will be converted to dopa in order to bind to D2 receptor |
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Name the three drug classes of enzyme inhibitors involved in treatment of Parkinsons. What is their enzymatic function? |
1. carbidopa: inhibits DOPA carboxylase 2. MAO-B (monoamine oxidase): metabolizes dopamine 3. COMT (catechol-o-methyltransferase): metabolizes dopamine both peripherally and centrally |
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What drugs fall under the class of MAO-B? |
Selegiline Rasagiline (more potent and effective) |
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What are the adverse effects of drugs in the class of MAO-B? |
similar to levodopa = nausea, vomiting, loss of appetite |
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What drugs fall under the class of COMT? |
"capone"
Tolcapone Entacapone |
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What are the adverse effects of drugs in the class of COMT? |
similar to levodopa NOTE: tolcapone can increase liver enzymes, which may lead to hepatic failure |
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With Parkinson, another treatment option is Dopamine receptor agonists. These drugs have less incidence of movement disorders and motor disturbances as levodopa BUT what do they produce a greater incidence of? |
psychiatric symptoms |
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What drugs fall in the class of dopamine receptor agonists? |
1. Bromocriptine mesylate (not used as much today because of the adverse effects and decreased effectiveness compared to newer drugs) 2. Pramipexole 3. Ropinirole 4. Apomorphine |
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What adverse effects are involved with Pramipexole and Ropinirole? |
similar adverse effects to levodopa linked to impulse control disorders: excessive gambling, binge eating, shopping, etc |
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When is apopmorphine used?
List adverse effects of apomorphine. |
used when patients are experience off periods during the on-off phenomenon.
nausea, chest pain |
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Describe MOA of Amantadine in the tx of parkinson's disease. At what point in treatment is it used? |
antiviral agent that increases synthesis and release of dopamine as well as inhibits reuptake of dopamine
EARLY -- not effective in advance stages when stored pools of dopamine are low |
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What is the adverse effect of Amantadine? |
livedo reticularis = skin finding consisting of a mottled reticulated vascular pattern that appears as a lace-like purplish discoloration of the skin
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What is the purpose of Anticholinergic in the treatment of Parkinson's? |
help reduce the symptoms of tremor and muscle rigidity (not bradykinesia) |
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List the anticholinergic drugs involved in tx of parkinson. |
trihexyphenidyl benztropine |
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Treatment protocol for Parkinson's--drugs for: Early stage Mild/Moderate stage Advance stage |
Early stage: Anticholingerics or amatandine to control tremors and rigidity Rasagiline may also be used
Mild/Moderate stage: levodopa/carbidopa may add COMT and MAO-B inhibitors
Advance stage: frequent administration of levodopa/carbidopa if not already, may add COMT and MAO-B inhibitors additional Dopa agonists if needed |
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What is the NT imbalance with Huntington's dz? |
GABA and ACh synthesis is reduced, but note that enhancement of either does not help alleviate chorea
overactivity of dopaminergic nigrostriatal pathways, but drugs that impair dopaminergic transmission CAN alleviate chorea |
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Which drugs are used in the treatment of Huntington's disease to decrease dopaminergic transmission? |
reserpine haloperidol (butyrophenones) perphenazine (perphenazines) |
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What is the pharmacotherapy (if needed) for Tourette's ? _____ Which drug is first choice for treatment of Tourette's? What do you use if the patient is intolerant or refractory to the drug of choice?
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antipsychotics ___________
haloperidol - first choice
Pimozide - used if patient is refractory or intolerant to haloperidol |
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What is first line treatment for Alzheimer disease?
What are the adverse effects of this drug class? |
Acetylcholinesterase inhibitors -- most beneficial EARLY in Alzheimer dz.
results in excess parasympathetic activity (vomiting, nausea, diarrhea, bradycardia) |
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List the Acetylcholinesterase inhibitors: When are they used? |
ALL STAGES: Donepezil --- GI upset
Mild to moderate stages: Galantamine Rivastigmine |
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Reducing excitotoxicity of neurons is thought to be beneficial in treatment of Alzheimer disease. What is the drug used for this form of treatment? |
Memantine NMDA receptor antagonist |
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List the stimulants that treat ADHD along with their MOA. |
1. d-amphetamine -- 5HT reuptake inhibitor 2. amphetamine 3. lisdexamfetamine
4. methylphenidate -- dopa and NORE reuptake inhibitor |
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Which drug is first line for tx of ADHD? |
methylphenidate -- less euphoric effects and abuse potential |
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What non-stimulant treats ADHD? What is the black box warning with this drug |
atomoxetine -- selective NORE reuptake inhibitor
suicide ideation |
