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Parkinson's Drugs
USMLE Step 1
Drug | MOA & ADRs |
---|---|
Pharmacological approach to Parkinson's | 1) antiACh, 2) COMT -, 3) Dopaminergic agents, 4) MAOI |
Levodopa aka L-dopa MOA | metabolic precursor to DA, restore DA levels in the substantia nigra, taken up by fxing neurons thus used early in the disease-no longer useful in 3rd-5th yr of tx, rapid absorbed w/o food from the small intestine, can permeate the CNS unlike DA |
Carbidopa | MOA:- aromatic-L-amino-acid decarboxylase stops biosyn of L-dopa 2 DA,combined w/ L-dopa,no BBB penetration,good 2 increase amt of L-dopa in periphery;ADRs:n/v,bld dyscrasia,dyskinesia,mydriasis,brown urine & saliva,psychic disturbances,tachy & hypoTN |
Ropinirole | MOA:DA receptor agonist,direct + DA receptors,used exclusively as adjunct w/ levodopa is reserved for later disease when levodopa wearing off,approved for use as tx of restless leg syndrome;ADRs:confusion,dizziness,fatigue |
Rotigotine | MOA:DA receptor agonist,direct + DA receptors,only as transdermal patch,used as monotx in early disease or adjunct in later disease;ADRs:nausea,dizziness & sometimes incapacitating somnolence |
Bromocriptine | MOA:direct DA agonist,vasoconstrictive action,used w/ L-dopa,not as commonly used;ADRs:nausea, hallucinations,confusion,delirium,orthostatic hypoTN,serious cardiovascular problems,& worsening of preexistent ulcers |
Amantadine | MOA: antiviral that enhances DA presence(synthesis, release & reuptake) from surviving neurons, not as commonly used as once was prior; ADRs: restlessness, hallucinations, confusion, increased doses cause acute toxic psychosis |
Deprenyl aka Selegiline | MOA: MAOI, more specifically MAO-B which is selective for DA destruction, allows for increase in DA levels; ADRs: at high levels, it starts to inhibit the breakdown of other catecholamines, causing severe HPTN |
Benztropine | MOA: Anti-ACh, more specific anti-muscarinic used as adjuncts to tx, when decrease levels of ACh then DA effects are enhanced ;ADRs: contra in glaucoma, BPH & pyloric stenosis, visual problems, mood changes & possible hallucinations |
Proyclidine | MOA: Anti-ACh, more specific anti-muscarinic used as adjuncts to tx, when decrease levels of ACh then DA effects are enhanced ;ADRs: contra in glaucoma, BPH & pyloric stenosis, visual problems, mood changes & possible hallucinations |
Trihexyphenidyl | MOA: Anti-ACh, more specific anti-muscarinic used as adjuncts to tx, when decrease levels of ACh then DA effects are enhanced ;ADRs: contra in glaucoma, BPH & pyloric stenosis, visual problems, mood changes & possible hallucinations |
Biperiden | MOA: Anti-ACh, more specific anti-muscarinic used as adjuncts to tx, when decrease levels of ACh then DA effects are enhanced ;ADRs: contra in glaucoma, BPH & pyloric stenosis, visual problems, mood changes & possible hallucinations |
Levodopa aka L-dopa ADRs | increases IOP in glaucoma, arrhythmias in heart pts, contraindicated w/ antipsychotic drugs, Vit B6 increases peripheral breakdown, MAOIs w/ levodopa can cause HPTN crisis due to increased catecholamine production |
Antipsychotics, e.g. phenothiazine & haloperidol | MOA: block DA receptors; ADRs: strongly contraindicated in Parkinson's |