Drugs Block 4 Flashcards
Natalizumab
MS drug that blocks cell adhesion molecules (blocks alpha 4 Beta 1) thus preventing diapediesis of T cells and macrophages across BBB
Reduces number of new MS lesions.
Nimodipine
MOA: Calcium Channel Blocker
Preferentially effects CNS.
Dialates small vessels to increase collateral circulation and preserve cerebral perfusion (prunuske) Prevents vasospasm (First Aid) Used to treat Sub Arachnoid Hemorrhage
Tissue Plasminogen Activator (TPA)
Converts plasminogen to plasmin to break down clots.
Must use within 3 (old) -4.5 (young) hrs. Can use later w/ IR guided TPA.
Contraindications: HEMORRHAGE, BP>185/110, MI, Stroke, or Head Injury in past 3 mo, Anti-coagulation therapy.
Levodopa (L-DOPA)*
MOA: Immediate precursor converted into Dopamine via AAAD throughout the body.Dependent on intact presynaptic neuron.
Decreases akinesia, rigidity, and tremor. Better when used early.
Pharmakinetics: short plama half-life, absorbed erratically from GI. Amino acids can compete for transport. Peaks and troughs.
Transported in CNS via amino acid transporters.
Given with carbidopa (blocks action in body but not CNS)
Adverse Effects: Peak dose dyskinesia, Diphasic dyskinesia, off period dystonia, schizophrenia (limbic activation), nausea, vomiting, anorexia (chemoreceptor triggerzone just outside BBB.
Entacapone*
COMT Inhibitor
Decreased peripheral metabolism of L-DOPA by COMT. Leading to smoother response and prolonged “on” time.
Used as adjunctive with L-DOPA to reduce L-DOPA dose.
Selegiline*
MAOi
Inhibits MAO-B primarily metabolizes dopamine.
Effective early treatment or used in conjunction with L-DOPA. Smooths “on-off” fluctuations, reduce wearing off phenomenon.
Pramipexole*
D3 receptor agonist (D2 family). Can be used alone or with Sinemet. Can help with “on-off” fluctuations with L-DOPA.
Also used to treat RLS.
Adverse effects: response fluctuations, dyskinesia (less than L-DOPA)
Ropinirole
D2 receptor agonist. Can be used alone or with Sinemet. Can help with “on-off” fluctuations with L-DOPA.
Also used to treat RLS.
Adverse effects: response fluctuations, dyskinesia (less than L-DOPA)
Sinemet
L-DOPA and Carbidopa. Standard of Care for PD.
Carbidopa
Inhibits AAAD peripherally (doesn’t cross BBB). Inhibits L-DOPA peripheral side effects. Reduce L-DOPA dose by 75%.
Co administered with L-DOPA.
Trihexylphenidyl*
Muscarinic antagoinst.
ACh is used as a neurotransmitter by a small but important subgroup of striatal interneurons. Unkown mechanism, but believed that with DA loss DA/ACh balance is off leading to excess ACh production.
Side effects: sedation, mental confusion, constipation, urinary retention.
Amantadine (Symmetrel)*
Antiviral drug that can be used in conjunction with levodopa. Unclear mechanism of help.
Tissue transplantation
Human fetal adrenal medullary tissue into caudate nucleus to treat PD.
Can cause runaway hyperkinesia
Electrical Stimulation
Stimulate Thalamus to increase motor activity.
Pallidotomy
Electric cutting out of Globus Pallidus
Alleviates akinesia, rigidity, and drug induced dyskinesia
