Apomorphin
Apomorphin Uses, Dosage, Side Effects, Food Interaction and all others data.
Apomorphin is a non-ergoline dopamine D2 agonist indicated to treat hypomobility associated with Parkinson's. It was first synthesized in 1845 and first used in Parkinson's disease in 1884. Apomorphin has also been investigated as an emetic, a sedative, a treatment for alcoholism, and a treatment of other movement disorders.
Apomorphin was granted FDA approval on 20 April 2004.
Apomorphin is a dopaminergic agonist that may stimulate regions of the brain involved in motor control. It has a short duration of action and a wide therapeutic index as large overdoses are necessary for significant toxicity. Patients should be counselled regarding the risk of nausea, vomiting, daytime somnolence, hypotension, oral mucosal irritation, falls, hallucinations, psychotic-like behaviour, impulsive behaviour, withdrawal hyperpyrexia, and prolongation of the QT interval.p
| Trade Name | Apomorphin |
| Availability | Prescription only |
| Generic | Apomorphine |
| Apomorphine Other Names | Apomorfina, Apomorphin, Apomorphine |
| Related Drugs | Neupro, Azilect, Duopa, Apokyn, Xadago, Ongentys, Gocovri, Rytary, Sinemet, Sinemet CR |
| Type | |
| Formula | C17H17NO2 |
| Weight | Average: 267.3224 Monoisotopic: 267.125928793 |
| Protein binding | Apomorphine is expected to be 99.9% bound to human serum albumin, as no unbound apomorphine is detected. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Apomorphin is a morphine derivative D2 dopamine agonist used to treat hypomobile "off" episodes of advanced Parkinson's disease.
Apomorphin is indicated to treat acute, intermittent treatment of hypomobility, off episodes associated with advanced Parkinson's disease.
Apomorphin is also used to associated treatment for these conditions: Mobility decreased
How Apomorphin works
Apomorphin is a non-ergoline dopamine agonist with high binding affinity to dopamine D2, D3, and D5 receptors. Stimulation of D2 receptors in the caudate-putamen, a region of the brain responsible for locomotor control, may be responsible for apomorphine's action. However, the means by which the cellular effects of apomorphine treat hypomobility of Parkinson's remain unknown.
Toxicity
Patients experiencing an overdose of apomorphine may present with nausea, hypotension, and loss of consciousness. Treat patients with symptomatic and supportive measures.
The intraperitoneal LD50 in mice is 145µg/kg.
Food Interaction
- Avoid alcohol. Ingesting alcohol may potentiate hypotension caused by apomorphine.
Apomorphin Alcohol interaction
[Moderate] GENERALLY AVOID:
Alcohol and apomorphine may have additive hypotensive and sedative effects.
Coadministration of 0.6 or 0.3 g/kg of ethanol with apomorphine in healthy subjects resulted in greater decreases in blood pressure compared to apomorphine alone.
The mean largest decrease (the mean of each subject's largest drop in blood pressure measured within 6 hours after apomorphine administration) in standing systolic and diastolic blood pressure was 6.7 and 8.4 mmHg, respectively, with apomorphine alone.
When coadministered with 0.6 g/kg of ethanol (equivalent to approximately 3 standardized alcohol-containing beverages), the mean largest decrease in standing systolic and diastolic blood pressure was 11.3 and 12.6 mmHg, respectively (standing systolic and diastolic blood pressure decreased by as much as 61 and 51 mmHg, respectively, in this group).
When coadministered with 0.3 g/kg of ethanol, the mean largest decrease in standing systolic and diastolic blood pressure was 8.4 and 7.1 mmHg, respectively.
Patients should be advised to avoid consumption of alcohol during apomorphine treatment.
Apomorphin Drug Interaction
Moderate: zolpidem, zolpidem, metoprolol, metoprolol, morphine, morphine, rotigotine, rotigotine, quetiapine, quetiapineUnknown: charcoal, charcoal, rasagiline, rasagiline, sodium iodide, sodium iodide, acetaminophen, acetaminophen, cholecalciferol, cholecalciferol
Apomorphin Disease Interaction
Volume of Distribution
The apparent volume of distribution of subcutaneous apomorphine is 123-404L with an average of 218L. The apparent volume of distribution of sublingual apomorphine is 3630L.
Elimination Route
Apomorphin has a plasma Tmax of 10-20 minutes and a cerebrospinal fluid Tmax. The Cmax and AUC of apomorphine vary significantly between patients, with 5- to 10-fold differences being reported.
Half Life
The terminal elimination half life of a 15mg sublingual dose of apomorphine is 1.7h, while the terminal elimination half life of an intravenous dose is 50 minutes.
Clearance
The clearance of a 15mg sublingual dose of apomorphine is 1440L/h, while the clearance of an intravenous dose is 223L/h.
Elimination Route
Data regarding apomorphine's route of elimination is not readily available. A study in rats has shown apomorphine is predominantly eliminated in the urine.
Innovators Monograph
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