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Parkinson's Disease - Medications
amantadine (Symmetrel ®)
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Use Prophylaxis and treatment of influenza A viral infection; treatment of parkinsonism; treatment of drug-induced extrapyramidal symptoms Mechanism of Action As an antiviral, blocks the uncoating of influenza A virus preventing penetration of virus into host; antiparkinsonian activity may be due to its blocking the reuptake of dopamine into presynaptic neurons or by increasing dopamine release from presynaptic fibers Dosing: Adults: ------------------------------ Drug-induced extrapyramidal symptoms: 100 mg twice daily; may increase to 300-400 mg/day, if needed Parkinson's disease or Creutzfeldt-Jakob disease (unlabeled use): 100 mg twice daily as sole therapy; may increase to 400 mg/day if needed with close monitoring; initial dose: 100 mg/day if with other serious illness or with high doses of other anti-Parkinson drugs Influenza A viral infection: 100 mg twice daily; initiate within 24-48 hours after onset of symptoms; discontinue as soon as possible based on clinical response (generally within 3-5 days or within 24-48 hours after symptoms disappear). Influenza A prophylaxis: 100 mg twice daily Note: Continue treatment throughout the peak influenza activity in the community or throughout the entire influenza season in patients who cannot be vaccinated. Development of immunity following vaccination takes ~2 weeks; amantadine therapy should be considered for high-risk patients from the time of vaccination until immunity has developed ------------------------------ Elderly: Adjust dose based on renal function; some patients tolerate the drug better when it is given in 2 divided daily doses (to avoid adverse neurologic reactions). ------------------------------ Dosing interval in renal impairment: Clcr 30-50 mL/minute: Administer 200 mg on day 1, then 100 mg/day Clcr 15-29 mL/minute: Administer 200 mg on day 1, then 100 mg on alternate days Clcr<15 mL/minute: Administer 200 mg every 7 days Hemodialysis: Administer 200 mg every 7 days Peritoneal dialysis: No supplemental dose is needed Continuous arterio-venous or venous-venous hemofiltration: No supplemental dose is needed Supplied: Capsule, as hydrochloride: 100 mg Syrup, as hydrochloride (Symmetrel®): 50 mg/5 mL (480 mL) Tablet, as hydrochloride (Symmetrel®): 100 mg |
benztropine (Cogentin ®)
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Anticholinergic. Use Adjunctive treatment of Parkinson's disease; treatment of drug-induced extrapyramidal symptoms (except tardive dyskinesia) Mechanism of Action Possesses both anticholinergic and antihistaminic effects. In vitro anticholinergic activity approximates that of atropine; in vivo it is only about half as active as atropine. Animal data suggest its antihistaminic activity and duration of action approach that of pyrilamine maleate. May also inhibit the reuptake and storage of dopamine and thereby, prolong the action of dopamine. --------------------------- Dosing: Adults: 1-4 mg/dose 1-2 times/day Acute dystonia: Adults: I.M., I.V.: 1-2 mg Parkinsonism: Oral: Adults: 0.5-6 mg/day in 1-2 divided doses; if one dose is greater, administer at bedtime; titrate dose in 0.5 mg increments at 5- to 6-day intervals Elderly: Initial: 0.5 mg once or twice daily; increase by 0.5 mg as needed at 5-6 days; maximum: 4 mg/day --------------------------- Supplied: Injection, solution, as mesylate (Cogentin®): 1 mg/mL (2 mL) Tablet, as mesylate: 0.5 mg, 1 mg, 2 mg |
bromocriptine (Parlodel ®)
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Dopamine agonist. Use Amenorrhea with or without galactorrhea; infertility or hypogonadism; prolactin-secreting adenomas; acromegaly; Parkinson's disease Mechanism of Action Semisynthetic ergot alkaloid derivative and a dopamine receptor agonist which activates postsynaptic dopamine receptors in the tuberoinfundibular and nigrostriatal pathways Dosing: Adults: (May be taken with food to decrease GI distress.) Parkinsonism: 1.25 mg 2 times/day, increased by 2.5 mg/day in 2- to 4-week intervals (usual dose range is 30-90 mg/day in 3 divided doses), though elderly patients can usually be managed on lower doses Neuroleptic malignant syndrome: 2.5-5 mg 3 times/day Hyperprolactinemia: 2.5 mg 2-3 times/day Acromegaly: Initial: 1.25-2.5 mg increasing as necessary every 3-7 days; usual dose: 20-30 mg/day Prolactin-secreting adenomas: Initial: 1.25-2.5 mg/day; may be increased as tolerated every 2-7 days until optimal response (range: 2.5-15 mg/day) --------------------------- Monitoring: Monitor blood pressure closely as well as hepatic, hematopoietic, and cardiovascular function --------------------------- Supplied: Capsule, as mesylate: 5 mg Tablet, as mesylate: 2.5 mg |
entacapone (Comtan ®)
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Use Adjunct to levodopa/carbidopa therapy in patients with idiopathic Parkinson's disease who experience "wearing-off" symptoms at the end of a dosing interval Mechanism of Action Entacapone is a reversible and selective inhibitor of catechol-O-methyltransferase (COMT). When entacapone is taken with levodopa, the pharmacokinetics are altered, resulting in more sustained levodopa serum levels compared to levodopa taken alone. The resulting levels of levodopa provide for increased concentrations available for absorption across the blood-brain barrier, thereby providing for increased CNS levels of dopamine, the active metabolite of levodopa. --------------------------- Dosing: Oral: Adults: 200 mg with each dose of levodopa/carbidopa, up to a maximum of 8 times/day (maximum daily dose: 1600 mg/day). To optimize therapy, the dosage of levodopa may need reduced or the dosing interval may need extended. Patients taking levodopa >/= 800mg/day or who had moderate-to-severe dyskinesias prior to therapy required an average decrease of 25% in the daily levodopa dose. Dosage adjustment in hepatic impairment: Treat with caution and monitor carefully; AUC and Cmax can be possibly doubled --------------------------- Administration Always administer in association with levodopa/carbidopa; can be combined with both the immediate and sustained release formulations of levodopa/carbidopa. Can be taken with or without food. Should not be abruptly withdrawn from patient's therapy due to significant worsening of symptoms. --------------------------- Supplied: Tablet: 200 mg |
pergolide (Permax ®)
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Use Adjunctive treatment to levodopa/carbidopa in the management of Parkinson's disease Mechanism of Action Pergolide is a semisynthetic ergot alkaloid similar to bromocriptine but stated to be more potent (10-1000 times) and longer-acting; it is a centrally-active dopamine agonist stimulating both D1 and D2 receptors. Pergolide is believed to exert its therapeutic effect by directly stimulating postsynaptic dopamine receptors in the nigrostriatal system. Dosing: When adding pergolide to levodopa/carbidopa, the dose of the latter can usually and should be decreased. Patients no longer responsive to bromocriptine may benefit by being switched to pergolide. Adults: Parkinson's disease: Start with 0.05 mg/day for 2 days, then increase dosage by 0.1 or 0.15 mg/day every 3 days over next 12 days, increase dose by 0.25 mg/day every 3 days until optimal therapeutic dose is achieved, up to 5 mg/day maximum; usual dosage range: 2-3 mg/day in 3 divided doses --------------------------- Monitoring: Blood pressure (both sitting/supine and standing), symptoms of parkinsonism, dyskinesias, mental status --------------------------- Supplied: Tablet: 0.05 mg, 0.25 mg, 1 mg |
pramipexole (Mirapex ®)
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Dopamine receptor agonist (D3>>D2). Use Treatment of the signs and symptoms of idiopathic Parkinson's disease Mechanism of Action Pramipexole is a nonergot dopamine agonist with specificity for the D2 subfamily dopamine receptor, and has also been shown to bind to D3 and D4 receptors. By binding to these receptors, it is thought that pramipexole can stimulate dopamine activity on the nerves of the striatum and substantia nigra. --------------------------- Dosing: (May be taken with food to decrease nausea.) Adults: Oral: Initial: 0.375 mg/day given in 3 divided doses, increase gradually by 0.125 mg/dose every 5-7 days; range: 1.5-4.5 mg/day --------------------------- Dosage adjustment in renal impairment: Clcr 35-59 mL/minute: Initial: 0.125 mg twice daily (maximum dose: 1.5 mg twice daily) Clcr 15-34 mL/minute: Initial: 0.125 mg once daily (maximum dose: 1.5 mg once daily) Clcr<15 mL/minute (or hemodialysis patients): Not adequately studied --------------------------- Administration Doses should be titrated gradually in all patients to avoid the onset of intolerable side effects. The dosage should be increased to achieve a maximum therapeutic effect, balanced against the side effects of dyskinesia, hallucinations, somnolence, and dry mouth. --------------------------- Monitoring Monitor for improvement in symptoms of Parkinson's disease (eg, mentation, behavior, daily living activities, motor examinations), blood pressure, body weight changes, and heart rate --------------------------- Supplied: Tablet, as dihydrochloride monohydrate: 0.125 mg, 0.25 mg, 0.5 mg, 1 mg, 1.5 mg |
ropinirole (Requip ®)
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Dopamine-2 (D2)-receptor agonist. Use Treatment of idiopathic Parkinson's disease; in patients with early Parkinson's disease who were not receiving concomitant levodopa therapy as well as in patients with advanced disease on concomitant levodopa Mechanism of Action Ropinirole has a high relative in vitro specificity and full intrinsic activity at the D2 and D3 dopamine receptor subtypes, binding with higher affinity to D3 than to D2 or D4 receptor subtypes; relevance of D3 receptor binding in Parkinson's disease is unknown. Ropinirole has moderate in vitro affinity for opioid receptors. Ropinirole and its metabolites have negligible in vitro affinity for dopamine D1, 5-HT1, 5-HT2, benzodiazepine, GABA, muscarinic, alpha1-, alpha2-, and beta-adrenoreceptors. Although precise mechanism of action of ropinirole is unknown, it is believed to be due to stimulation of postsynaptic dopamine D2-type receptors within the caudate-putamen in the brain. Ropinirole caused decreases in systolic and diastolic blood pressure at doses >0.25 mg. The mechanism of ropinirole-induced postural hypotension is believed to be due to D2-mediated blunting of the noradrenergic response to standing and subsequent decrease in peripheral vascular resistance. --------------------------- Dosing: Adults: Oral: The dosage should be increased to achieve a maximum therapeutic effect, balanced against the principal side effects of nausea, dizziness, somnolence and dyskinesia Recommended starting dose is 0.25 mg 3 times/day; based on individual patient response, the dosage should be titrated with weekly increments as described below: Week 1: 0.25 mg 3 times/day; total daily dose: 0.75 mg Week 2: 0.5 mg 3 times/day; total daily dose: 1.5 mg Week 3: 0.75 mg 3 times/day; total daily dose: 2.25 mg Week 4: 1 mg 3 times/day; total daily dose: 3 mg After week 4, if necessary, daily dosage may be increased by 1.5 mg per day on a weekly basis up to a dose of 9 mg/day, and then by up to 3 mg/day weekly to a total of 24 mg/day Removal by hemodialysis is unlikely. --------------------------- Supplied: Tablet, as hydrochloride: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg, 5 mg |
selegiline (Eldepryl ®)
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Monoamine oxidase (MAO) inhibitor that is specific for the MAO-B isozyme.
Use Adjunct in the management of parkinsonian patients in which levodopa/carbidopa therapy is deteriorating Mechanism of Action Potent monoamine oxidase (MAO) type-B inhibitor; MAO type B plays a major role in the metabolism of dopamine; selegiline may also increase dopaminergic activity by interfering with dopamine reuptake at the synapse -------------------------- Dosing: Adults: Parkinson's disease: 5 mg twice daily with breakfast and lunch or 10 mg in the morning Elderly: Parkinson's disease: Initial: 5 mg in the morning, may increase to a total of 10 mg/day -------------------------- Supplied: Capsule, as hydrochloride (Eldepryl®): 5 mg Tablet, as hydrochloride: 5 mg |
Sinemet ® (carbidopa/levodopa):
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Use Idiopathic Parkinson's disease; postencephalitic parkinsonism; symptomatic parkinsonism Mechanism of Action Parkinson's symptoms are due to a lack of striatal dopamine; levodopa circulates in the plasma to the blood-brain-barrier (BBB), where it crosses, to be converted by striatal enzymes to dopamine; carbidopa inhibits the peripheral plasma breakdown of levodopa by inhibiting its decarboxylation, and thereby increases available levodopa at the BBB ------------------------- Dosing: Oral: Adults: Parkinson's disease: Immediate release tablet: Initial: Carbidopa 25 mg/levodopa 100 mg 3 times/day Dosage adjustment: Alternate tablet strengths may be substituted according to individual carbidopa/levodopa requirements. Increase by 1 tablet every other day as necessary, except when using the carbidopa 25 mg/levodopa 250 mg tablets where increases should be made using 1 /2-1 tablet every 1-2 days. Use of more than 1 dosage strength or dosing 4 times/day may be required (maximum: 8 tablets of any strength/day or 200 mg of carbidopa and 2000 mg of levodopa) Sustained release tablet: Initial: Carbidopa 50 mg/levodopa 200 mg 2 times/day, at intervals not <6 hours Dosage adjustment: May adjust every 3 days; intervals should be between 4-8 hours during the waking day (maximum: 8 tablets/day) Restless leg syndrome (unlabeled use): Carbidopa 25 mg/levodopa 100 mg given 30-60 minutes before bedtime; may repeat dose once Elderly: Initial: Carbidopa 25 mg/levodopa 100 mg twice daily, increase as necessary ------------------------- Administration Space doses evenly over the waking hours. Give with meals to decrease GI upset. Sustained release product should not be crushed. Orally-disintegrating tablets do not require water; the tablet should disintegrate on the tongue's surface before swallowing. ------------------------- Supplied: Tablet immediate release (Sinemet®): 10/100: Carbidopa 10 mg and levodopa 100 mg 25/100: Carbidopa 25 mg and levodopa 100 mg 25/250: Carbidopa 25 mg and levodopa 250 mg Tablet, immediate release, orally-disintegrating (Parcopa™): 10/100: Carbidopa 10 mg and levodopa 100 mg 25/100: Carbidopa 25 mg and levodopa 100 mg 25/250: Carbidopa 25 mg and levodopa 250 mg Tablet, sustained release (Sinemet® CR): Carbidopa 25 mg and levodopa 100 mg Carbidopa 50 mg and levodopa 200 mg |
tolcapone (Tasmar ®)
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First of new class of COMT inhibitors. Increases the elimination
half-life of levodopa. Maximum: 600 mg/day. Use Adjunct to levodopa and carbidopa for the treatment of signs and symptoms of idiopathic Parkinson's disease Mechanism of Action Tolcapone is a selective and reversible inhibitor of catechol-o-methyltransferase (COMT) Dosage Adults: Oral: Initial: 100-200 mg 3 times/day; levodopa therapy may need to be decreased upon initiation of tolcapone Supplied: Tablet: 100 mg, 200 mg |
trihexyphenidyl (Artane ®)
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Anticholinergic. Use Adjunctive treatment of Parkinson's disease; treatment of drug-induced extrapyramidal symptoms Mechanism of Action Exerts a direct inhibitory effect on the parasympathetic nervous system. It also has a relaxing effect on smooth musculature; exerted both directly on the muscle itself and indirectly through parasympathetic nervous system (inhibitory effect) Dosing: Adults: Oral: Initial: 1-2 mg/day, increase by 2 mg increments at intervals of 3-5 days; usual dose: 5-15 mg/day in 3-4 divided doses Supplied: Elixir, as hydrochloride: 2 mg/5 mL (480 mL) Tablet, as hydrochloride: 2 mg, 5 mg |
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