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