Dosing and uses of Apokyn, Uprima (apomorphine)
Adult dosage forms and strengths
injection solution
- 10mg/mL
Parkinson Disease
Indicated for the acute, intermittent treatment of hypomobility, off episodes (end-of-dose wearing-off and unpredictable on-off episodes) associated with advanced Parkinson's disease
Initial: 2 mg (0.2 mL) SC
If no response, titrate every few days by 1-mg doses up to 6 mg SC q8hr; administration for up to 5 times daily reported
No more than 6 mg during hypomobility episodes 3-5 times/day
Vegetative State (Orphan)
Treatment of patients in a vegetative state or minimally conscious state for up to 12 months following a severe traumatic brain injury
Orphan indication sponsor
- NeuroHealing Pharmaceuticals, Inc; 50 Undine Road; Newton, MA 02135
Renal Impairment
Reduce test dose and starting dose to 1 mg (0.1 mL)
Hepatic Impairment
Mild to moderate impairment: Use caution
Severe impairment: Safety and efficacy not established
Other Information
Antiemetics recommended with or just prior to treatment, and continue as long as needed (BUT not 5-HT3 antagonists as noted below)
Pediatric dosage forms and strengths
Not indicated
Geriatric dosage forms and strengths
Parkinson disease
Indicated for the acute, intermittent treatment of hypomobility, off episodes (end-of-dose wearing-off and unpredictable on-off episodes) associated with advanced Parkinson's disease
Initial: 2 mg (0.2 mL) SC
If no response, titrate every few days by 1-mg doses up to 6 mg SC q8hr; administration for up to 5 times daily reported
No more than 6 mg during hypomobility episodes 3-5 times/day
Apokyn, Uprima (apomorphine) adverse (side) effects
>10%
Dizziness or postural hypotension (20%)
Dyskinesia (35%)
Injection site reaction (26%)
Nausea or vomiting (30%)
Somnolence (35%)
Yawning (40%)
1-10%
Anxiety
Arthralgia
Back pain
CHF
Confusion (10%)
Depression
Edema (10%)
Hallucinations (10%)
Headache
Injection site pain
Insomnia
Limb pain
Rhinorrhea (10%)
UTI
Warnings
Contraindications
Hypersensitivity to apomorphine
Sulfite/sulfur allergies (contains sulfite)
Do not use 5-HT3 antagonist antiemetics (eg, granisetron, dolasetron) - risk of profound hypotension and loss of consciousness
Cautions
Monitor for hypotension
Hallucinations or confusion may occur
New or worsening mental status and behavioral changes may occur; some severe, including psychosis; avoid with pre-existing major psychotic disorder
Pregnancy and lactation
Pregnancy category: C
Lactation: It is not known whether apomorphine is excreted in milk. Because of the potential for serious adverse reactions in nursing infants from apomorphine, a decision should be made as to whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Apokyn, Uprima (apomorphine)
Mechanism of action
Morphine derivative; nonergoline dopamine agonist of D2-type receptors within the caudate putamen in the brain
Pharmacokinetics
Peak Plasma Time:10-60 min
Half-life, elimination: 30-60 min
Vd: 218 L
Metabolism: Sulfation, oxidation, glucuronidation, N-demethylation, and cetechol-O methyltransferase
Excretion: Urine (93%); feces (16%)
