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
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Related Studies
| Definition (MSH) | A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. |
| Definition (CSP) | derivative of morphine that is a dopamine D2 agonist; a powerful emetic useful in acute poisoning; has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D001058 |
| SnomedCT | 387375001, 67939000 |
| English | Apomorphine, 4H-Dibenzo(de,g)quinoline-10,11-diol, 5,6,6a,7-tetrahydro-6-methyl-, (R)-, Apomorphine [Chemical/Ingredient], APOMORPHINE, Apomorphine (product), Apomorphine (substance), apomorphine |
| Swedish | Apomorfin |
| Czech | apomorfin |
| Finnish | Apomorfiini |
| Russian | APOMORFIN, АПОМОРФИН |
| Polish | Apomorfina |
| Japanese | アポモルフィン, アパフィナム, 塩酸アポモルヒネ, アポモルヒネ |
| Spanish | apomorfina (producto), apomorfina (sustancia), apomorfina, Apomorfina |
| French | Apomorphine |
| German | Apomorphin |
| Italian | Apomorfina |
| Portuguese | Apomorfina |
Ontology: Uprima (C1657321)
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| English | Uprima |
