Apokyn

Apokyn (apomorphine hydrochloride) is a prescription injection for Parkinson's disease to manage "off" episodes in people with advanced PD. Apokyn works by acting on dopamine receptors in the brain to restore motor control quickly, typically within 10 to 20 minutes of injection. It is intended to rescue patients from acute off episodes when oral medications are not working. It is used alongside other PD medications, not as a replacement for oral levodopa.

Apokyn works by stimulating D1 and D2 dopamine receptors in the area of the brain responsible for coordinating movement. Apokyn mimics the action of dopamine by activating these receptors, which restores motor function even when oral levodopa is not effective.

Apokyn injection can begin working in as few as 10 minutes because it is injected subcutaneously (under the skin), which reaches the bloodstream and the brain much faster than oral medications.

Apokyn (apomorphine) is a non-selective dopamine agonist.

Apokyn injection significantly improved movement and motor symptoms compared to placebo at 20 minutes after injection. This was demonstrated across three clinical trials in patients with advanced Parkinson's disease.

Study 1: Most Patients Responded Within 20 Minutes Apokyn achieved a therapeutic response in 18 out of 20 patients (90%) at approximately 20 minutes. None of the 9 patients who received a placebo achieved a response. All patients in this study of 29 people experienced at least two hours of off time daily despite optimised oral therapy.

Study 2: Consistent Results in Established Users A single dose of Apokyn produced significantly greater improvement in movement symptoms at 20 minutes compared to placebo. This was demonstrated in a second study of 17 patients who had already been using Apokyn for at least 3 months.

Study 3: Usual Dose Works Best Apokyn significantly improved movement symptoms compared to placebo at 20 minutes in a third study of 62 patients. Increasing the dose by 2 mg above the usual prescribed amount offered little additional benefit and was associated with more side effects, supporting the use of the lowest effective dose.

Talk to your healthcare provider about all risks before starting Apokyn. The following warnings are based on the FDA prescribing information.

Subcutaneous injection only Apokyn must only be injected under the skin. Injecting into a vein can cause serious blood clots and pulmonary embolism.

Drowsiness and falling asleep Apokyn caused drowsiness in 35% of patients in clinical studies. Some patients fell asleep suddenly without warning during everyday activities such as eating, talking, or driving. Do not drive or operate heavy machinery until you know how Apokyn affects you.

Low blood pressure and fainting Apokyn can lower blood pressure, particularly when standing up from sitting or lying down. In clinical trials, 11% of patients experienced low blood pressure or fainting. Get up slowly and avoid alcohol, as it worsens this effect.

Falls 30% of patients in clinical trials had events that could be considered falls, with 5% experiencing serious falls. Low blood pressure and changes in mobility may both contribute.

Hallucinations and psychotic-like behavior Hallucinations were reported in patients taking Apokyn during clinical trials. These can include seeing or hearing things that are not real, confusion, and paranoid thinking. Contact your healthcare provider if you or a family member notices any of these changes.

Uncontrolled movements (dyskinesia) Apokyn may cause or worsen uncontrolled, involuntary movements. This was reported in 24% of patients in clinical studies.

Low red blood cell count (hemolytic anemia) Apokyn can cause a reduction in red blood cells at any point during treatment. Severe anemia, angina, and dyspnea have occurred with hemolytic anemia.

Impulse control problems Some patients taking Apokyn have reported sudden strong urges to gamble, increased sexual urges, or uncontrolled spending. Tell your healthcare provider if you or those around you notice any unusual urges or behaviours.

Heart events In clinical studies, some patients experienced coronary events, including angina, heart attack, or cardiac arrest. Seek emergency care immediately if you experience chest pain or shortness of breath.

Heart rhythm changes (QTc prolongation) Apokyn can affect heart rhythm in a way that may increase the risk of a serious irregular heartbeat. This risk increases with doses above 6 mg, which is why higher doses are not recommended. Tell your healthcare provider right away if you experience palpitations or fainting. The risks and benefits of treatment should be considered prior to initiating treatment with Apokyn in patients with risk factors for prolonged QTc.

Stopping Apokyn suddenly Do not stop taking Apokyn suddenly without speaking to your healthcare provider. Rapid withdrawal has been associated with a serious condition involving high fever, muscle rigidity, and confusion.

Allergic reactions Apokyn contains sodium metabisulfite, a sulfite that can cause severe allergic reactions including anaphylaxis, particularly in people with asthma or known sulfite sensitivity.

Prolonged painful erection (priapism) Apokyn may cause prolonged painful erections in some men. In clinical studies this was reported in 3 of 361 men. If an erection lasts more than 4 hours, seek emergency medical care immediately.

Fibrotic complications Cases of tissue scarring affecting the lungs, pelvis, and heart valves have been reported with some dopamine agonist medications. Whether Apokyn carries this risk is currently unknown.

Retinal pathology Retinal changes were observed in animal studies but have not been established as clinically significant in humans. Discuss any vision concerns with your healthcare provider.

Many drugs can interact and cause dangerous effects. Some drugs should not be used together with Apokyn. Your doctor may change your treatment plan if you also use:

• alosetron;
• dolasetron;
• granisetron;
• ondansetron (Zofran); or
• palonosetron.

To make sure Apokyn is safe for you, tell your doctor if you have ever had:

• asthma or a sulfite allergy;
• low blood pressure or dizzy spells;
• narcolepsy, falling asleep during the daytime;
• heart problems, long QT syndrome;
• a stroke;
• liver or kidney disease;
• mental illness or psychosis; or
• if you drink alcohol.

Tell your doctor if you are pregnant or breastfeeding.

Do not take this medicine if:

• You take medicines called 5-HT3 antagonists (ondansetron, granisetron, dolasetron, palonosetron, alosetron), these medicines are contraindicated.
• You have a known hypersensitivity to apomorphine or any Apokyn excipient, including sodium metabisulfite (sulfite allergy).

Common Apokyn side effects

Common Apokyn side effects may include:

• dizziness, drowsiness;
• nausea, vomiting;
• pain or swelling in your nose, mouth, or throat;
• numbness, tingling, burning pain;
• swelling in your hands or feet;
• confusion, hallucinations;
• yawning;
• runny nose; or
• uncontrolled muscle movements.

Serious side effects

Get emergency medical help if you have signs of an allergic reaction to Apokyn: hives, itching, difficulty breathing, swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• a light-headed feeling, like you might pass out;
• extreme drowsiness, falling asleep suddenly, even after feeling alert;
• confusion, hallucinations, unusual thoughts or behavior;
• twitching or uncontrollable movements of your eyes, lips, tongue, face, arms, or legs;
• fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness (like you might pass out);
• ongoing nausea or vomiting (even after taking anti-nausea medicine);
• new or worsening cough, fever, pain when you breathe, feeling short of breath while lying down;
• penis erection that is painful or lasts 4 hours or longer;
• worsening of your Parkinson symptoms;
• pale or yellowed skin, dark colored urine, fever, confusion or weakness; or
• severe nervous system reaction - very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, feeling like you might pass out.

Serious side effects may be more likely in older adults.

You may have increased sexual urges, unusual urges to gamble, or other intense urges while using this medicine. Talk with your doctor if this occurs.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In advanced Parkinson's disease (PD), patients may experience "off" episodes, which are when symptoms like stiffness, slowness, and tremors return before the next scheduled medication dose.

Off episodes significantly affect quality of life, often making it difficult for patients to perform basic daily activities such as walking, speaking, or dressing.

Usual Adult Dose of Apokyn for Parkinson's Disease:

Dose initiation should be supervised by a healthcare provider: Antiemetic premedication should be initiated prior to therapy due to high incidence of nausea and vomitingInitial dose: 2 mg (0.2 mL) subcutaneously during an "off" episodeFirst dose: Obtain pulse, supine and standing blood pressure pre-dose, 20, 40, and 60 minutes post-dose; if significant hypotension is present 60 minutes post-dose, recheck after 60 minutes; if significant hypotension occurs in response to initial dose, patients should not be considered good candidates for treatmentTitration: If initial dose is tolerated, but response is insufficient, may increase in 2 mg increments up to 6 mg (under medical supervision) or in increments of 1 mg every few days up to 3 mg (outpatient) for subsequent "off" episodes; allow at least 2 hours between doses; assess response until an effective and tolerable dose is achievedMaintenance dose: 2 to 6 mg subcutaneously during an "off" episode; doses should be separated by at least 2 hours; average dosing frequency in clinical trials was 3 times per dayMaximum single dose: 6 mg (0.6 mL)Maximum dosing frequency: 5 times per dayMaximum daily dose: 20 mg (2 mL) per day

Administration: Inject subcutaneously in the stomach area (at least 2 inches from the naval), upper arm, or upper thigh. Rotate the injection site with each injection.

Use the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not use two doses at one time.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Some people using Apokyn have fallen asleep during normal daytime activities such as working, talking, eating, or driving. Avoid driving or operating machinery until you know how this medicine will affect you. Dizziness or severe drowsiness can cause falls or other accidents.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.

Do not drink alcohol. It can further lower your blood pressure and may increase certain side effects of apomorphine.

Tell your healthcare provider about all medications, supplements, and herbal products you take. Important interactions include:

This list is not complete and many other drugs may interact with apomorphine. Not all possible drug interactions are listed here.