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Basal Ganglia Drugs
Drugs for movement disorders
Question | Answer |
---|---|
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 |