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Antiparkinson Drugs (Dopamine Agonists (These are the direct agonists of…
Antiparkinson Drugs
Dopamine Agonists
These are the direct agonists of striatal DA receptors. They can be Non-Ergot derived (first line) or Ergot derived
Non-Ergot derived are the selective D2/3 agonist such as APOMORPHINE, PRAMIPEXOLE, ROPINIROLE and ROTIGOTINE
Ergot derived are the D1 and D2 agonists such as BROMOCRIPTINE, PERGOLIDE and CABERGOLINE
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Amorphine is used to control the 'off' effect with L-dopa but it is a powerful emetic but there is a risk of cardiac dysrhythmias
Dopamine Agonist Withdrawal Syndrome where there is tampered dose reduction and the level of depression should be observed.
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COMT Inhibitors
Inhibits the breakdown of levodopa by inhibiting catechol-O-methyltransferase, the enzyme responsible for the breakdown of Dopamine
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It reduces off time, it reduced the levodopa dose and improves motor impairment and disability
Administered with other anti-Parkinson's drugs such as levodopa, cardiopa and entacapone
S.E: Severe diarrhea, hepatic toxicity, CV risk with Stalevo, urine discolouration with Entacapone
Levodopa
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Given with decarboxylase inhibitor such as Carbidopa as L-Dopa is metabolised in the peripheral tissues so it is unable to enter the BBB. The use of an inhibitor will increase the levels of levodopa in the brain and decrease peripheral bioavailability. Breakdown in peripheral tissues causes symptoms such as nausea.
S.E: Nausea, vomiting, motor complication, psychological effects such as confusion, L-dopa dyskinesia, Impulse Control Disorder and Dopamine Deregulation Syndrome(dysfunction of the reward system and could start craving for dopamine)
Motor complications include dyskinesia, freezing of gait, end of dose wearing off, loss of smooth muscle control
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Anti-cholinergic
Muscarinic nerve terminal exerts an inhibitory effect on the dopamine nerve terminals and suppression compensates for the lack of dopamine
Examples include ORPHENADRINE, PROCYCLIDINE and TRIHEXPHENIDYL
Dry mouth, constipation, impaired vision and urinary retention
AMANTADINE is an anti-viral, which alters dopamine release, blocks NMDA receptors and its anti-cholinergic properties. It reduced L-dopa induced dyskinesia in advanced disease