Apokyn (apomorphine HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Apomorphine hydrochloride is a nonergot-derivative dopamine receptor agonist.
Apomorphine hydrochloride is a nonergot-derivative dopamine receptor agonist that is structurally and pharmacologically related to dopamine. In in vitro studies, apomorphine hydrochloride demonstrated a higher affinity for the dopamine D4 receptor than for dopamine D2, D3, or D5 receptors. Apomorphine hydrochloride binds with moderate affinity to alpha-adrenergic (alpha1D, alpha2B, alpha2C) receptors but has little or no affinity for dopamine D1 receptors, serotonergic (5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C) receptors, beta1- or beta2-adrenergic receptors, or histamine H1 receptors.
The exact mechanism of action of apomorphine hydrochloride in the treatment of Parkinson disease has not been fully elucidated but may involve stimulation of postsynaptic dopamine D2 receptors within the caudate-putamen in the brain. Apomorphine has been shown to improve motor function in an animal model of Parkinson disease. In particular, apomorphine attenuates the motor deficits associated with neurotoxin (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine ((MPTP))-induced lesions in the ascending nigrostriatal dopaminergic pathway in primates.
Following a single subcutaneous injection, apomorphine exhibits linear pharmacokinetics over a dose range of 2-8 mg. Apomorphine is rapidly absorbed following subcutaneous administration in the abdominal wall; bioavailability following subcutaneous administration is equal to that of IV administration. Following subcutaneous injection, peak concentrations are reached within 10-60 minutes; maximum concentrations in the CSF are <10% of the maximum plasma concentrations and occur within 10-20 minutes.
Following initiation of a continuous subcutaneous infusion, steady-state concentrations are reached within approximately 2 hours. However, the time to reach 50% of infusion steady-state concentrations can be reduced by 50-75% by administering an extra dose when the continuous dose is initiated. If the extra dose is administered >=2 hours after the initiation of a continuous dose, supplemental exposure from the extra dose reaches a maximum concentration within 20-40 minutes.
Apomorphine is 89% protein-bound. The mean elimination half-life is 40 minutes. Metabolism of apomorphine occurs primarily via conjugation.
Within 30 minutes of administering a subcutaneous dose of radiolabeled apomorphine, only 8.3% of plasma radioactivity was apomorphine; 83% was apomorphine sulfate, 3.5% was apomorphine glucuronide, and 1% was nor-apomorphine glucuronide. Following a subcutaneously administered dose of radiolabeled apomorphine, 86% of the dose was recovered in the urine within 48 hours (as apomorphine sulfate, apomorphine glucuronide, and nor-apomorphine glucuronide) and 4.6% was recovered in the feces over 144 hours (as apomorphine sulfate, apomorphine glucuronide, and apomorphine). No clinically significant pharmacokinetic differences were observed based on age, gender, weight, duration of Parkinson disease, levodopa dose, or duration of therapy.
USES: This medication is used to treat the symptoms of Parkinson's disease. It can improve your ability to move during frequent "off" periods. It can decrease shakiness (tremor), stiffness, slowed movement, and unsteadiness.
This medication is thought to work by helping to restore the balance of a certain natural substance (dopamine) in the brain. Apomorphine is used to treat "off" episodes when they occur. It is not used to prevent "off" episodes.
This drug should not be used instead of your usual medications for Parkinson's disease. Keep taking all your medications as directed by your doctor.
Generic name: apomorphine HCl
Pronunciation: (A-poe-MOR-feen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Apokyn
Indications
The following indications are listed for Apokyn:
- Idiopathic Parkinsonism
Also known as: Paralysis Agitans, Primary Parkinson's Disease.
Dosing
Dosage of apomorphine hydrochloride is expressed in terms of the salt.
Dosage of apomorphine hydrochloride must be individualized according to the patient's response and tolerance.
Apomorphine hydrochloride is available for administration as an intermittent subcutaneous injection (Apokyn(R)) and a continuous subcutaneous infusion (Onapgo(R)).
Apomorphine hydrochloride should not be given IV because of the possibility of serious adverse effects (e.g., thrombosis, pulmonary embolism).
Apomorphine initiation and dose titrations should be performed under medical supervision; a caregiver or patient may administer subsequent doses following education and training if deemed appropriate by a healthcare provider.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Concomitant use with selective 5-HT3 receptor antagonists (e.g., alosetron, dolasetron, granisetron, ondansetron, palonosetron).
*Known hypersensitivity or allergic reaction to apomorphine hydrochloride or any ingredient in the formulation (e.g., sodium metabisulfite).
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects of apomorphine (Apokyn(R)) (incidence >=10% versus placebo) include yawning, drowsiness/somnolence, dyskinesias, dizziness/postural hypotension, rhinorrhea, nausea and/or vomiting, hallucination/confusion, and edema/swelling of extremities.
The most common adverse effects of apomorphine (Onapgo(R)) (incidence >=10% on apomorphine and at least twice the rate of placebo) include infusion site nodule, nausea, somnolence, infusion site erythema, dyskinesia, headache, and insomnia.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of apomorphine have not been established in pediatric patients.
There are no adequate data on the developmental risks associated with the use of apomorphine in pregnant women. In animal reproduction studies, an increased incidence of neonatal deaths and cardiovascular malformations was observed at clinically relevant doses associated with maternal toxicity.
It is not known whether apomorphine is distributed into human milk; effects of the drug on the breast-fed infant or on milk production also are not known. The known benefits of breast-feeding should be considered along with the mother's clinical need for apomorphine and any potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.
The manufacturer makes no specific dosage recommendations for geriatric patients. Cautious dosage selection is recommended, usually starting at the low end of the dosing range, due to the increased incidence of decreased hepatic, renal, or cardiac function and comorbid disease or other drug therapy in such patients.
An increased incidence of confusion, hallucinations, serious adverse events (life-threatening events or events resulting in hospitalization and/or increased disability), falls, cardiovascular events, respiratory disorders, and GI events has been observed in geriatric individuals treated with intermittent subcutaneous apomorphine relative to younger adults. Clinical studies of apomorphine administered via continuous subcutaneous infusion did not include sufficient numbers of patients >=65 years of age to determine whether they respond differently from younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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