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Amantidine is an antiviral used for the treatment of
Influenza A , herpes simplex and varicella zoster
has modest anti parkinsonian activity
Given orally and is well tolerated
MOA of Amantidine as an anti parkinsonian drug
acts by releasing dopamine from intact dopaminergic neurons - increases levels in the synpases
also decreases dopamine reuptake in CNS
Only a few benefits and tolerance develops with time.
ADRS of Amantidine
nightmares
insomnia
Hallucinations
Delirium
dizziness
GIT disturbances
skin discoloration
dry mouth
peripheral edema
rarely - leukopenia
DOPAMINE METABOLISM INHIBITORS
MAOb inhibitors - selegiline , rosagiline
COMT inhibitors - entacapone and tolcapone
dopamine is metabolised by MAO (mono amine oxidase) and COMT (catechol-o-methyl transferase)
Does Entacapone act centrally or peripherally
peripherally
Does Tolcapone act centrally or peripherally
both centrally and peripherally
Entacapone is useful in
end dose of motor flactuations as an adjunct to L dopa - carbidopa combinations.
use of dopamine decarboxylase inhibitors is associated with the rise in 3-o methyldopa
ADRS of entacapone
increased L DOPA associated dyskinesias , nausea and confusion
diarrhea
abdominal pain
orthostatic hypotension
sleep disturbances
orange discolouration in urine.
ADRs of tolcapone
Hepatotoxic effects - hepatotoxicity with cases of acute hepatic failure rarely reported.
SELEGELINE
MAO B inhibitor. In high doses inhibits MAO A.
ā¢ Used in conjunction with L-dopa in severe disease to reduce end of dose deterioration.
Early use may delay need for L-dopa therapy and slow down progression of disease.
DOSAGE OF SELEGINE
ā¢ Given orally.
ā¢ Dose 10MG OD in the morning, or 5mg at breakfast and 5 mg at midday.
ADRS OF SELEGELINE
ā¢ Nausea, vomiting
ā¢ Hypotension
ā¢ Confusion
ā¢ Agitation
DIs OF SELEGELINE
ā¢ Should not be taken with:
ā¢ Meperidine
ā¢ TCAs
ā¢ Serotonin reuptake inhibitors- may cause acute toxic reaction of serotonin syndrome
ā¢ Adverse effects of levodopa may be increased by selegeline.
Rasagiline
ā¢ MAO B inhibitor
ā¢ Pharmacology like selegeline, but pore potent in preventing MPTP induced Parkinsonism.
Used as a neuroprotective agent and for early treatment.
ā¢ Preps - 0.5mg, 1mg
ā¢ Dose - standard dose 0.5 mg /d
Other movement disorders
ā¢ Tremors
ā¢ Chorea
ā¢ Huntington's disease
ā¢ Ballismus
ā¢ Athetosis and dystonia
ā¢ Tics
ā¢ Drug induced dyskinesias
ā¢ Restless leg syndrome
ā¢ Wilson's disease