Pharm

Apomorphine

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Apomorphine, Apokyn, Uprima, Kynmobi, Zydis

  • See Also
  1. Dopamine Agonist
  2. Parkinsonism
  3. Erectile Dysfunction
  • Indications
  1. Parkinsonism
    1. Hypomobility episodes (rescue)
  2. Erectile Dysfunction
    1. Effective in 55 to 60% of men (contrast 32% in Placebo)
  • Precautions
  1. Never use IV (high risk of cardiovascular complications)
  • Mechanism
  1. Central acting, Non-ergot Dopamine Agonist
  • Pharmacokinetics
  1. Sublingual (Uprima)
    1. Onset: 10 minutes
    2. Duration: 30 minutes
  • Dosing
  • Parkinsonism - Acute hypomobility ("Off" Episode or severe "freezing" episode)
  1. Preparations
    1. Administered by Apokyn injector pen (10 mg/ml)
    2. Apomorphine Sublingual Film (Kynmobi) is also available
      1. However, intolerable due to oropharyngeal adverse effects in a third of patients
  2. First test dose (observed by clinician): 0.2 ml SQ
    1. Reduce starting dose to 0.1 ml in mild to moderate renal disease
    2. May try higher test dose if ineffective
    3. Monitor for Orthostatic Hypotension
  3. If test dose effective and tolerated
    1. May increase by 0.1 ml/dose every few days as needed
    2. Rotate injection sites
    3. Monitor for Orthostatic Hypotension
  4. Typical frequency: three times daily as needed for Acute hypomobility ("Off" Episode)
  5. Maximum: 0.6 ml/dose (or 2 ml/day)
  6. Duration: Avoid use longer than 2 months
  7. Pretreat dose with Antiemetic (Nausea and Vomiting is very common)
    1. Start Antiemetic three days prior to initiating Apomorphine
    2. Do NOT combine with 5-HT3 Antagonists (e.g. Ondansetron) due to risk of Hypotension, Syncope
    3. Trimethobenzamide (Tigan) 300 mg orally three times daily
  1. Uprima 2 to 6 mg SL prn
  1. Adverse effects seen in 58% of men on 6 mg
  2. Nausea (39%) and Vomiting (10%)
    1. Due to Dopaminergic stimulation at the ChemoreceptorTrigger Zone (CMZ) in Medulla
  3. Dizziness (20%)
  4. Somnolence (11%)
  5. Sweaty (18%)
  6. Hypotension (4%)
  7. Syncope (2%)
  • Resources
  1. Apomorphine (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3235535d-9ef9-4657-8b2a-176a807d091c
  • References
  1. (2021) Med Lett Drugs Ther 63(1618): 25-32
  2. Hamilton (2020) Tarascon Pocket Pharmacopoeia