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PD: drugs
Parkinson's Disease drugs
| Question | Answer |
|---|---|
| Etiology of Parkinson's Disease | Destruction of dopaminergic neurons in the substantia nigra |
| What is the Substantia Nigra? | located in the midbrain. controls reward/addiction/movement |
| Inhibitory/Excitatory? (1) Dopamine | Inhibit |
| Inhibitory/Excitatory> (2) GABA | Inhibit |
| Inhibitory/excitatory? ACh | excitatory |
| "Can't SEE, can't PEE, can't SPIT, can't SHIT" | Anticholinergic Drugs |
| What do anticholinergic drugs do? | they block muscarinic receptors |
| what do muscarinic receptors do? | inhibit metabolism which increases drug availability |
| non-motor symptoms of Parkinson's Disease | depression, dementia, psychosis (usually dt drug) |
| How much Levodopa reaches the brain? Why? | only 2% because it is metabolized in the periphery by decarboxylase |
| Levodopa is administered via what route? | Oral |
| how does food interact with Levodopa? | it delays absorption. It does NOT inhibit absorption, just delays it |
| High protein foods interact with Levodopa by what? | decrease therapeutic effects |
| where is Levodopa absorbed? | in the small intestine |
| what are the adverse effects of Levodopa? | dark sweat/urine n/v dyskinesias postural hypotension dysrhythmias psychosis |
| Levodopa drug interactions | 1st generation antipsychotics MAO inhibitor Anticholinergic drugs Pyridoxine (Vit. B6) |
| 1st generation antipsychotics interaction with Levodopa | blocks receptors for dopamine in stratum |
| how does MAO inhibitors interact with levodopa? | inhibits breakdown of NE/dopamine/ leading to increased amount of these which leads to activation of alpha1 --> HTN CRISIS! |
| Anticholinergic drugs interacting with Levodopa | enhances response to Levodopa |
| Pyridoxine (Vitamin B6) interacts with Levodopa | stimulates decarboxylase activating |
| why administer Levodopa/Carbidopa? | carbidopa inhibits decarbocxylation which will increase amount of levodopa that reaches the brain. |
| /Can carbidopa cross the BBB? | NO |
| what are the therapeutic effects of carbidopa? | none on its own. |
| advantages of Levodopa/Carbidopa | decreased levodopa dose decreased cardio side effects decreased n/v pt CAN take B6 |
| Disadvantages to Levodopa/Carbidopa | abnormal movements and psychiatric disturbances sooner and more intense. |
| Dopamine Agonists PRO | no conversion needed decreased drug failure decreased disabling dyskinesis |
| CONs of dopamine agonists | more serious side effects: Hallucinations, daytime sleepiness, postural hypotension |
| Categories of dopamine agonists. and tell me about them. | Ergot vs Nonergot Nonergot = highly selective to dopamine receptors |
| Premipexole [Mirapex] Adverse Effects | when used alone: n/v, dizziness, INSOMNIA, DAYTIME SOMNOLENCE, constipation, weakness, hallucinations Combined: Orthostatic hypotension, Dyskinesias SLEEP ATTACKS! COMPULSIVE SELF-REWARDING BEHAVIORS |
| Drug interaction with Premipexole [Mirapex] | Cimetidine: drugs used for peptic ulcers decrease renal excretion which increases plasma level |
| Ropinirole [Requip]: adverse Effects | Same as Mirapex |
| Ropinirole [Requip]: drug interactions | SAME as Mirapex |
| MAO-B inhibitors: what does it do? | can decrease wearing off effects when combined with Levodopa |
| Which PD drug may delay neurodegeneration | Selegiline |
| What does selegiline do? | causes selective irreversable inhibition of MAO-B |
| discuss metabolism of Selegiline | metabolized by liver: 2 metabolites = harmful because they are CNS stimulant -> agination/insomnia |
| what kind of drug is Selegiline | Dopamine Agonist |
| what kind of drug is Premipexole? | dopamine agonist |
| how long does it take for levodopa to see therapeutic effects? | 6 months |
| should you take Requip with food? | yes |