Parlodel (bromocriptine mesylate)*
Validus Pharmaceuticals
Approved for PD, but rarely used. Other indications: hyperprolactinemic states, acromegaly |
Strengths: 2.5-mg tablet; 5-mg capsule Initial dose in PD: one-half of 2.5-mg tablet (1.25 mg) BID with meals Dosage may be increased every 14 to 28 days by 2.5 mg/day with meals Safety has not been demonstrated in dosages exceeding 100 mg/day
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Hepatic metabolism; CYP3A4 substrate Excretion: 82% in feces; 6% in urine 90% to 96% bound to serum albumin Half-life: 5–15 hours
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Pulmonary: pleural thickening (fibrosis) after long-term treatment GI: nausea, vomiting, abdominal discomfort CNS: abnormal involuntary movements, ataxia, hallucinations, confusion, “on-off” phenomenon, dizziness, syncope, drowsiness, insomnia, depression Other: visual disturbance, hypotension, shortness of breath, constipation, vertigo, asthenia
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Pulmonary function Blood pressure Daytime alertness Weight Heart rate
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Requip, Requip XL (ropinirole)*
GlaxoSmithKline
Approved for PD and restless legs syndrome (IR) or for idiopathic PD (XL) |
IR strengths: 0.25-mg, 0.5-mg, 1-mg, 2-mg, 3-mg, 4-mg, 5-mg tablets XL strengths: 2-mg, 4-mg, 8-mg, 12-mg tablets IR starting dose: 0.25 mg TID; titrate weekly to maximum of 24 mg/day XL starting dose: 2 mg QD for 1–2 weeks; titrate weekly to maximum of 24 mg/day
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Hepatic metabolism; CYP1A2 substrate (inactive metabolites) Excretion: > 88% of radiolabeled dose in urine (IR); < 10% in urine as unchanged drug (XL) Half-life: about 6 hours (IR/XL)
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GI: nausea, vomiting, dyspepsia, abdominal pain, constipation CNS: dizziness, somnolence, headache, syncope, confusion, hallucinations, impulse control disorders, sleep attacks Other: fatigue, asthenia, dependent/leg edema, viral infection, pain, increased sweating, orthostatic symptoms, pharyngitis, abnormal vision, UTIs
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Blood pressure Daytime alertness Weight Heart rate
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Mirapex, Mirapex ER (pramipexole)*
Boehringer Ingelheim
Approved for PD and restless legs syndrome (IR) or for PD (ER).
Overnight switch from IR to ER successful in 80% of patients |
IR strengths: 0.125-mg, 0.25-mg, 0.5-mg, 0.75-mg, 1-mg, 1.5-mg tablets ER strengths: 0.375-mg, 0.75-mg, 1.5-mg, 2.25-mg, 3.0-mg, 3.75-mg, 4.5-mg tablets IR starting dose: 0.125 mg TID; titrate weekly to 0.25–1.5 mg TID; BID dosing not approved ER starting dose: 0.375 mg QD; titrate weekly to maximum of 4.5 mg QD
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Negligible metabolism (< 10%) Excretion: 90% in urine as unchanged drug (via renal tubules) Half-life: about 8 hours in young, healthy subjects; about 12 hours in elderly subjects (IR) Dose adjustment required in renal impairment
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GI: nausea, abdominal pain/discomfort, constipation CNS: dizziness, somnolence, headache, hallucinations, impulse control disorders, sleep attacks Other: dyskinesia, orthostatic hypotension, xerostomia, peripheral edema, muscle spasms
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Blood pressure Daytime alertness Weight Heart rate
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Neupro (rotigotine)
UCB, Inc. Transdermal patch; indicated for PD and restless legs syndrome |
Strengths: 1 mg/24 hours, 2 mg/24 hours, 3 mg/24 hours, 4 mg/24 hours, 6 mg/24 hours, 8 mg/24 hours Initial dose: 2 mg/24 hours (early PD) or 4 mg/24 hours (advanced PD); may be increased at weekly intervals to maximum of 6 mg/24 hours or 8 mg/24 hours, respectively Apply QD to healthy skin; do not use same site more than once every 2 weeks
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Extensive metabolism Excretion: 71% in urine (inactive conjugates); about 23% in feces Initial half-life: 3 hours Terminal half-life: 5 to 7 hours after patch removal
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GI: nausea, vomiting CNS: somnolence, dizziness Other: application-site reactions, dyskinesia, anorexia, hyperhidrosis, visual disturbance, peripheral edema Avoid in patients with sulfa allergy Remove patch prior to MRI (burn risk): patch contains aluminum
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Blood pressure Daytime alertness Weight Heart rate Skin reactions
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Apokyn (apomorphine)
US MedWorlds
Subcutaneous injection into abdominal wall, upper arm, or upper leg (rotate sites); indicated for hypo mobility, “off” episodes associated with PD |
Strength: 30 mg/3 mL (10 mg/mL) glass cartridge Initial dose: 0.2 mL (2 mg) under medical supervision; can be titrated to maximum dose of 0.6 mL Reduce starting dose in patients with renal impairment Treatment with concomitant antiemetic (e.g., trimethobenzamide) is recommended, starting 3 days before first Apokyn dose and continuing for at least first 2 months of therapy
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GI: nausea, vomiting CNS: drowsiness, somnolence, dizziness, postural hypotension, hallucinations, confusion Other: dyskinesia, rhinorrhea, edema/ swelling of extremities Avoid use with serotonin blockers (may cause profound hypotension)
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