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Basal Ganglia Drugs

Drugs for movement disorders

QuestionAnswer
Trihexyphenidyl Antimuscarinic / Targets ACh action in basal ganglia to restore ACh-DA balance / Used in early parkinson's for tremor / Side effects, common anti parasympathetic
Benztropine Antimuscarinic / Targets ACh action in basal ganglia to restore ACh-DA balance / Used in early parkinson's for tremor / Side effects, common anti parasympathetic
Levodopa Converted to DA via the AA decarboxylase / Helps restore ACh-DA balance / Decreased effectiveness with time (less than 5 effective years) / Avoid abrupt cessation / Parkinson's
Carbidopa Peripheral inhibitor of amino acid decarboxylase (does not cross BBB) / Helps keep levadopa from being metabolized in the periphery / Decreased effectiveness with time (less than 5 effective years) / Avoid abrupt cessation / Parkinson's
Entacapone COMT Inhibitor / Acts in periphery only / Helps keep more DA in synaptic cleft / Contraindicated with MAO Inhibitors / Parkinson's
Tolcapone COMT Inhibitor / Crosses the BBB / Helps keep more DA in synaptic cleft / Contraindicated with MAO Inhibitors / Parkinson's
Selegiline Irreversible MAO-B Inhibitor / Decrease degradation of Dopamine/Levadopa / Parkinson's
Rasagiline Irreversible MAO-B Inhibitor / Decrease degradation of Dopamine/Levadopa / Parkinson's
Apomorphine Dopamine Receptor Agonist / Parkinson's’s disease “rescue therapy” / Parkinson's temporary treatment only
Pramipexole Dopamine Receptor D2&D3 Agonist / Directly stimulate the basal ganglia / Non-ergot derivative / Parkinson's and Restless leg syndrome
Ropinirole Dopamine Receptor D2 Agonist / Directly stimulate the basal ganglia / Non-ergot derivative / Parkinson's & Restless leg syndrome
Bromocriptine Dopamine Receptor D2 Agonist, Partial D1 / Directly stimulate the basal ganglia / Less favored than the non-ergot DA agonists / Parkinson's
Amantadine Antiviral / Only provides temporary relief for parkinson's
Tetrabenazine Reversible inhibitor of VMAT2 / BB: May increase risk of depression or suicidal ideation / Used in Huntington's disease to reduce chorea
Deutetrabenazine Reversible inhibitor of VMAT2 / BB: May increase risk of depression or suicidal ideation / Used in Huntington's disease to reduce chorea
Haloperidol Dopamine Receptor DA2 Antagonist / Used in Huntington's disease to reduce chorea / QT prolongation and potential for life-threatening arrhythmias /
Penicillamine Copper chelation / Used to treat Wilson's disease
Propranolol Beta Blocker / Used to treat essential tremor
Baclofen Agonist at GABAb receptors / Leads to reduction in Ca++ influx leading to less neurotransmitter release. Also opens K+ channels postsynaptically (hyperpolarization) / Used for spasticity and dystonia
Tizanidine Alpha2 agonist / Used to treat spasticity less muscle weakness than diazepam, baclofen, dantrolene.
Diazepam Long-acting benzodiazepine / Potentiates effects of GABA at GABAa receptors / Used to treat spasticity, anxiety, epilepsy, sedation.
Dantrolene NOT CENTRALLY ACTING / Binds to ryanodine receptor and blocks its opening thus decreasing the release of calcium from sarcoplasmic reticulum in the muscle fiber / Used for spasticity
Botulinum Toxin Destroys synaptic proteins involved in ACh vesicular release thus resulting in muscle weakness and paralysis
Cyclobenzaprine Structurally related to tricyclic antidepressants. / Used to treat ACUTE local muscle spasm due to local tissue trauma or muscle sprains.
Succinylcholine Atracurium Cistracurium Mivacurium Vecuronium Neuromuscular blockers
Created by: carchase