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Parkinsons

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alex0624's version from 2016-07-16 19:56

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drugs that induce parkisonismHaloperidol and MPTP
D2 receptor antagonist that can lead to parkisonismHaloperidol
Is a chemical which destructs the dopaminergic neurons leading to irreversible parkisoninsmMPTP
DA release from Substantia nigra is reduced. Direct pathway is affected thereby release of gabaergic neurons fom globus palidus medial will occur and inhibition of thalmous output will not occur leading to a hypokinetic condition known asParkisons disease
_______inmediate precursor of dopamineLevodopa
Levodopa is converted to dopamine byDOPA-decarboxilase
DOPA-decarboxylase also known asAromatic L-amino acid decarboxylase
dopa preparation containing carbidopa and levodopaSinemet
Side effects: Ameliorates the signs of parkinsonism, Particularly bradykinesia(recall neuro video), Not a cure to the disease, As disease progresses, the response to drug decreasesEffects of L-DOPA
Anorexia, nausea, vomiting, tachycardia, ventricular extrasystoles and atrial fibrillation. Dyskinesia in patiens using levodopa therapy for long periods(chorea, ballism)ADR of levodopa when given alone
Choreoathetosis of face and distal extremities seen inLevodopa treatment(side effects)
Fluctuations in clinical response to levodopa occur with increasing freq as treatment continues. Two types:Wearing-off reactions and on-off phenomenon
fluctuations relate to the timing of levodopa intake are refered to asWearing-off reactions
fluctuations in clinical state are unrelated to the timing of doseson-off phenomenon
enhance the extracerebral metabolism of levodopa and may therefore prevent its therapeutic effect Pirydoxine(vit B6)
Contraindicated in psychotic patients (exacerbate the mental disturbance)Levodopa
contraindicated in patients with angle-closure glaucoma, but those with chronic open-angle glaucoma may be given levodopa if IOP is well controlledLevodopa
precursor of skin melanin and may activate malignant melanomaL-DOPA
acts as a partial agonist at D2 receptors in the brainBromocryptine
acts as an agonist at D2 receptorsPergolide
often these drugs are given along with L-dopa and they prolong the effectiveness of L-dopaBromocryptine, Pergolide, Pramipexole, Ropinirole, rotigotine
agonist at D3 receptors, now considered first line drugs, less ADRPramipexole
also used for hyperprolactinemia & acromegalyBromocriptine
MAO- B -inhibitorsSelegiline, rasagiline
COMT-inhibitorsEntacapone, tolcapone
Drugs inhibiting the enzymatic degradation of DAMAO-B inhibitors and COMT inhibitors
the isoform that metabolizes dopamine in preference to NE and 5-HTMAO-B inhibitor
MAO B, drug interaction with ______ causes agitation, delirium and death, extreme caution with TCA and SSRI for serotonine syndrome.Meperidine
COnverts Levodopa to 3-0 methyldopa(3-0-MD)COMT
COMT with both central and peripheral effectsTolcapone
COMT with only peripheral effectsEntacapone
COMT causing hepatic damageTolcapone(preferred is entacapone)
Antiviral drug that enhances dopaminergic neurotansmissionAmantadine
Proposed MOA: increased synthesis, release and inhibition of dopamine reuptakeAmatadine(less efficacious than Levodopa)
its benefits may be short-lived, often disappearing after only a few weeks of treatment.Amantadine
ADR:restlessness, depression, irritability, insomnia, agitation, excitement, hallucinations, and confusionAmantadine
anticholinergic drugsBenztropine, biperiden, procyclidine & trihexyphenidyl
Improve tremor and rigidity Anticholinergic drugs
IMPORTANT--> reverse extrapyramidal side effects of antipsychoticsAnticholinergic drugs
Used in drug induced parkisonismAnticholinergic drugs
ADR(DUMBELLS)Dry mouth, urinary retention, sedation, delirium, confusion, hallucinations, constipationBenzotropine, biperidine, ...
DOC for tremorsPropranolol – b-blocker; Also used: topiramate (anti-epileptics)
DOC for Huntingtons choreaTetrabenazine, reserpine – depletes cerebral dopamine; Haloperidol
DOC Tourette’s SyndromeHaloperidol (blocks central D2 R); Also carbamazepine, clonazepam and clonidine (a2 agonist)
DOC Wilson’s DiseaseIron gets accumulated --> Leads to hepatic and neurological damage,Treated with chelator – penicillamine
DOC Restless legs syndromeDA agonist – ropinirole or pramipexole
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