Apomorphine

2
Apomorphine
Brands

DEA Class;  Rx

Common Brand Names; Apokyn, Kynmobi

  • Antiparkinson Agents, Dopamine Agonists
Non-narcotic morphine derivative; dopamine agonist with potent emetic properties
Approved as a sublingual film for acute, intermittent ‘off’ episodes associated with Parkinson’s disease; subcutaneous injection approved in advanced Parkinson’s disease
Monitor for hypotension, orthostasis, new or worsening impulse control symptoms, and patient reports of sudden sleep onset
Concurrent treatment with an antiemetic (e.g., trimethobenzamide) is recommended; use with 5-HT3 antagonists is contraindicated

Indicated for acute, intermittent treatment of hypomobility, “off” episodes (end-of-dose wearing “off” and unpredictable “on-off” episodes) associated with advanced Parkinson disease

For use in the differential diagnosis of idiopathic parkinsonism and as a diagnostic test for dopaminergic responsiveness in parkinsonian syndromes to determine whether a patient will respond or is still responsive to levodopa therapy.

Hypersensitivity, including angioedema or anaphylaxis

Sulfite/sulfur allergies (Apokyn contains sodium metabisulfite)

Do not use 5-HT3 antagonists, including antiemetics (eg, granisetron, dolasetron, ondansetron, palonosetron) – risk of profound hypotension and loss of consciousness

SC

  • Yawning (40%)

  • Dyskinesia (35%)

  • Drowsiness or somnolence (35%)

  • Nausea or vomiting (30%)

  • Injection site reaction (26%)

  • Dizziness or postural hypotension (20%)

  • Rhinorrhea (20%)

  • Bruising (16%)

  • Chest pain/pressure/angina (15%)

SL

  • Nausea (21-28%)

  • Oral/pharyngeal soft tissue swelling (1-15%)

  • Somnolence (11-13%)

  • Oral/pharyngeal soft tissue pain and paresthesia (2-13%)

  • Dizziness (9-11%)

Subcutaneous use only; thrombus formation and pulmonary embolism have followed IV administration owing to crystallization of apomorphine

Severe nausea and vomiting occurs at recommended doses; because of this, pretreat or treat with trimethobenzamide; trimethobenzamide reduces incidence of nausea and vomiting during first 4 weeks of therapy; patients treated with trimethobenzamide experience greater incidence of somnolence, dizziness and falls; benefit of treatment with trimethobenzamide must be balanced with risk for those adverse events, and treatment with trimethobenzamide should only be continued as long as necessary to control nausea and vomiting, which should generally be no longer than 2 months

Closely monitor patients with mild and moderate hepatic impairment

Falling asleep during activities of daily living and daytime somnolence may occur

Oral mucosal irritaiton reported with SL product

Syncope and hypotension/orthostatic hypotension may occur

Falls may occur, or increase owing to underlying postural instability, possible autonomic instability, and syncope caused by low blood pressure

May cause hallucinations and psychotic-like behavior

Adequate data on the developmental risk associated with use of apomorphine are not available in pregnant women

Unknown if distributed in human breast milk

Adults

0.6 mL (6 mg) per single subcutaneous injection and 5 injections/day not to exceed 2 mL/day (20 mg)/day subcutaneously; for sublingual dosage form: 30 mg/dose SL and no more than 5 doses/day SL.

Geriatric

0.6 mL (6 mg) per single subcutaneous injection and 5 injections/day not to exceed 2 mL/day (20 mg)/day subcutaneously; for sublingual dosage form: 30 mg/dose SL and no more than 5 doses/day SL.

Adolescents

Safety and efficacy have not been established.

Children

Safety and efficacy have not been established.

Infants

Safety and efficacy have not been established.

Apomorphine hydrochloride

solution for SC injection

  • 10mg/mL (30mg/3mL pen injector) (Apokyn, generic)

SL film (Kynmobi)

  • 10mg
  • 15mg
  • 20mg
  • 25mg
  • 30mg
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