| Hint | Answer |
| Butyrophenones class | |
| Entacapone class | |
| Interactions: Vitamin B6 enhances the extracerebral metabolism of L-dopa. MAOI w/ L-dopa can --> HTNive crisis if given within 2 weeks of each other. | |
| SE: Mental Disturbances: confusion, hallucinations, delusions, other psychiatric reactions. | |
| SE: Ergoline-induced toxicity effects unlikely. Postural hypotension, fatigue, somnolence, peripheral edema, nausea, constipation, dyskinesias, & confusion. | |
| MOA: Dopamine precursor able to cross the BBB where it is decarboxylated by dopa decarboxylase to form dopamine. | |
| Group P-kinetics: Advantages: No enzymatic conversion required, crosses BBB w/o competing for amino acid transporter. No potentially toxic metabolites | |
| Selegiline class | |
| Apomorphine class | |
| MOA: Not completely known. Inhib effects on glutamate-R, NMDA antag, Inactivation of voltage gated Na+ channels. Interferes w/ intracellular events post excitatory AA-R activation | |
| SE: Insomnia when taken late in the day | |
| Risperidone class | |
| MOA: D2 receptor agonist (partial D1 agonist) | |
| MOA: Preferential affinity for D3 family of receptors | |
| SE: Asthenia, dizziness, GI disorders, & elevation of liver enzymes. | |
| SE: GI: anorexia, n/v, constipation, dyspepsia, peptic ulcers, symptoms of reflux esophagitis. CV: postural hypotension & cardiac arrhythmias. Dyskinesias. | |
| SE: Increased L-dopa toxicity (dyskinesias, nausea, & confusion), diarrhea, abd pain, orthostatic hypotension, sleep disturbances, & orange urine. | |
| Use: alleviation of chorea if refractory to atypical | |
| Clonazepam class | |
| Use: prolong ALS survival by months | |
| SE: Nausea (pretreat w/ anti-emetic - trimethobenzamide or domiperidone), dyskinesias, drowsiness, sweating, hypotension | |
| Use: Gold standard in Parkinson's dz - most efficacious treatment | |
| Carbamazepine class | |
| Biperiden class | |
| SE: HA, nasal congestion, increased arousal, pulmonary infiltrates, ergoline-induced s/s, erythromelagia, vasospasm, & pleural or retroperitoneal fibroses. | |
| P-kinetics: Readily absorbed from intestines (depends on rate of gastric emptying and pH -- delayed by food). Some other AAs can compete for transport across the BBB. | |
| Use: Temporary relief of off-period akinesia in Parkinsons. Also used to tx ED. | |
| Haloperidol class | |
| MOA: Increases dopamine release & reduces dopamine reuptake into dopaminergic nerve terminals of substantia nigra neurons. Unknown MOA. | |
| P-kinetics: Response can decline over time or stop completely. Start at small dose & escalate as effects diminish. Wearing off rxs. Toxicity concern is supersensitivity develpmnt - | |
| P-kinetics: Similar to Pramipexole | |
| P-kinetics: Start with a small dose | |
| | Hint | Answer |
| Use: Enhance & prolong the effects of L-dopa; reduce response fluctuations; lowers necessary dose of L-dopa. ?Antioxidant properties? | |
| SE: Other: dry mouth, blurred vision, mydriasis, urinary retention, n/v, constipation, tachycardia, increased IOP. | |
| Contraindications: psychotic pts, angle closure glaucoma (Increased IOP), active peptic ulcers, hx of melanoma (melanin precursor) | |
| Reserpine class | |
| Tolcapone class | |
| Fluphenzaine class | |
| Use: Most effective drug in tx of Tourette's | |
| P-kinetics: Only helpful for Huntington's dz chorea at very high doses | |
| SE: May interfere with uptake - Rx metabolizes L-dopa into 3-methyldopa which competes for active transport across the BBB. | |
| Amantadine class | |
| Carbidopa class | |
| Ropinirole class | |
| Use: Huntington's dz pts w/ psychosis or disruptive behavior. Also helpful w/ chorea | |
| P-kinetics: Start at low dose & gradually increase | |
| MOA: Pure D2 receptor agonist | |
| Interactions: Should not be taken w/ meperidine, TCAs, serotonin reuptake inhibitors, or in combo w/ nonspecific MAOIs | |
| P-kinetics: SQ. Rapid onset ~ 10 min. Duration 2 hrs | |
| MOA: Central (brain) anti-cholinergic | |
| Carbidopa + levidopa (1:10 or 1:4) | |
| Use: Similar to Bromocriptine, but more effective. May benefit pts not receiving L-dopa. Aids pt w/ response fluctuations to L-dopa | |
| SE: Dyskinesias: chorea, ballismus, athetosis, dystonia, myoclonus, tics, tremors. Behavioral effects: anxiety/ agitation, insomnia/ somnolence, confusion/ delusions/ hallucination | |
| Procyclidine class | |
| Contraindications: Prostatic hyperplasia, obstructive GI dz, & angle-closure glaucoma | |
| P-kinetics: Note: Antidepressant MAOIs are either nonspecific or inhibit MAO-A more specifically (5-HT & NE) | |
| Benzotropine class | |
| SE: CV: Increased HR, PVCs, A fib (rare), postural hypotension, HTN (usually in the presence of non-specific MAOI or with large doses). | |
| Use: Reduced response to fluctuations w/ L-dopa. Decreased L-dopa clearance. Decreased dopa decarboxylase --> compensatory increase in COMT. | |
| Tetrabenxine class | |
| Riluzole class | |
| Use: Increases amount of L-dopa able to cross the BBB. Combo with L-dopa allows for L-dopa dose reduction up to 85%. | |
| Phenothiazine class | |
| P-kinetics: Well absorbed orally. T1/2 ~ 12 hrs. Hepatic metabolism (cytochrome P450, CYP1A2) -- caution in pts w/ hepatic insufficiency. | |
| | Hint | Answer |
| Olanzapine class | |
| Use: Monotherapy for mild Parkinsonism or combo tx for advanced pts. Reduces L-dopa dose & smooths response fluctuations. Putative neuroprotective effects (scavenges free radicals) | |
| Use: alleviation of chorea | |
| Bromocriptine class | |
| Use: Can be used as 1st line tx for Parkinson's dz - often in combo w/ Sinemet. Commonly used to tx hyperprolactinemia. | |
| MOA: Somewhat selective MAO-B inhibitors. Retard the breakdown of dopamine | |
| P-kinetics: Variable absorption from GI, peak plasma levels 1-2 hrs post PO dose. Excreted in bile & feces. Build up dose slowly over 2-3 mo to avoid adverse effects | |
| P-kinetics: Rapid PO absorption, excreted unchanged in urine, gradually increase dose | |
| TCA class | |
| SE: CNS: drowsiness, mental slowness, inattention, restless, confusion, agitation, delusions, hallucinations, & mood changes. | |
| P-kinetics: Given PO. Loses effectiveness over time. | |
| Contraindications: psychotic illness, MI hx, PVD, peptic ulcers | |
| Orphenadrine class | |
| Quetiapine class | |
| Use: May improve tremor & rigidity in Parkinsons. Little effect on bradykinesia. | |
| SE: If adverse effects become too severe withdraw gradually. break for 3-21 days, and reinstate gradually | |
| SE: GI (L-dopa alone): anorexia, n/v (avoid anti-emetics like phenothiazines d/t their extrapyramidal effects -- dopamine antagonist; carbidopa reduces these effects. | |
| Pramipexole class | |
| P-kinetics: Only 1-3% enters the brain across BBB unaltered. Peak plasma levels 1-2 hrs post PO dose. Plasma t1/2 = 1-2 hrs (pts vary -- dosing 3-4x/day). | |
| Rasagiline class | |
| Pergolide class | |
| MOA: D1 and D2 receptor agonist | |
| Use: depression associated with Huntington's disease | |
| MOA: Prevents the metabolism of L-dopa --> 3-O-methyldopa (3OMD) by Catechol-0-methyltransferase | |
| Use: Similar to Pramipexole | |
| Trihexyphenidyl class | |
| Levodopa class | |
| MOA: Inhibits the L-dopa --> dopamine conversion by dopa decarboxylase in the periphery (does not cross BBB). | |
| SE: May be hepatotoxic - (needs signed pt consent & liver monitoring Q 2 wks x 1 yr) | |
| Clonidine class | |
| P-kinetics: 2/3 appears in urine as metabolites within 8 hrs (homovanillic acid - HVA and dihydrocyphenylacetic acid - DOPAC). Best response is in the first few yrs of tx. | |
| SSRI class | |
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