Apomorphine

What is Apomorphine?

• Apomorphine (Apokyn;Kynmobi), is a non-ergoline dopamine agonist.

Apomorphine

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What are the uses of this medicine?

• Apomorphine (Apokyn;Kynmobi) is a prescription medicine used to treat acute, intermittent episodes of poor mobility called "off" episodes (end-of-dose wearing "off" or unpredictable "on-off" episodes) in people with advanced Parkinson's disease (PD).

How does this medicine work?

• The hydrochloride salt form of apomorphine, a derivative of morphine and non-ergoline dopamine agonist with high selectivity for dopamine D2, D3, D4 and D5 receptors.
• Apomorphine hydrochloride acts by stimulating dopamine receptors in the nigrostriatal system, hypothalamus, limbic system, pituitary gland, and blood vessels.
• This enhances motor function, suppresses prolactin release, and causes vasodilation and behavioral effects.
• Apomorphine hydrochloride is used in the treatment of Parkinson's disease and erectile dysfunction.
• In addition, apomorphine hydrochloride acts on the chemoreceptor trigger zone and is used as a central emetic in the treatment of drug overdose.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• taking certain medicines to treat nausea called 5HT 3 antagonists including, ondansetron, granisetron, dolasetron, palonosetron, and alosetron.
• allergic to apomorphine hydrochloride or to any of the ingredient.
• Apokyn and Kynmobi, also contains a sulfite called sodium metabisulfite. Sulfites can cause severe, life-threatening allergic reactions in some people. An allergy to sulfites is not the same as an allergy to sulfa. People with asthma are more likely to be allergic to sulfites. Call your healthcare provider if you have hives, itching, rash, swelling of the eyes, tongue, lips, chest pain, trouble breathing or swallowing.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• If you take nitroglycerin under your tongue while using Apomorphine, your blood pressure may decrease and cause dizziness.
• After taking nitroglycerin, you should lie down and try to continue lying down for at least 45 minutes.
• You should avoid standing for 45 minutes after taking nitroglycerin.

Is this medicine FDA approved?

• Apomorphine was approved for use in the United States in 2004, but had been used in Europe for more than a decade.

How should this medicine be used?

Recommended dosage: Apokyn:

• The starting dose of Apokyn is 0.1 mL (1mg) to 0.2 mL (2 mg); give the first dose under medical supervision; titrate the dose to effect and tolerance; the maximum recommended dose is 0.6 mL (6 mg).
• Treatment with trimethobenzamide is recommended, starting 3 days prior to the first dose of Apokyn.
• Treatment with trimethobenzamide should only be continued as long as necessary to control nausea and vomiting, and generally no longer than two months.

Kynmobi:

• Trimethobenzamide may be considered for nausea and/or vomiting, if needed.
• The dose range for Kynmobi is 10 mg to 30 mg per dose, administered sublingually, as needed.

Administration: Apokyn:

• Use Apokyn exactly as your healthcare provider tells you to use it.
• Your healthcare provider will tell you how much Apokyn to use and teach you the right way to use it.
• Your healthcare provider may change your dose if needed.
• Do not change your dose of Apokyn or use it more often than prescribed unless your healthcare provider has told you to.
• Do not give another dose of Apokyn sooner than 2 hours after the last dose.
• Your healthcare provider will prescribe Apokyn that comes in prefilled glass cartridges, for single-patient-use, that are used with a special pen injector.
• Your Apokyn pen is dosed in milliliters (mL), not milligrams (mg). Make sure your prescription tells you how many milliliters (mL) to use.
• Inject Apokyn under your skin (subcutaneously). Do not inject Apokyn into a vein.
• Keep a record of how much Apokyn you have used each time you inject or your care partner gives you an injection.
• Use a new needle with each injection. Never reuse a needle.
• Apokyn is a clear and colorless liquid. Do not use Apokyn if it appears cloudy, colored, or to contain particles, and call your pharmacist.
• Your healthcare provider may prescribe another medicine called an antiemetic to take while you are using Apokyn. Antiemetic medicines help to decrease the symptoms of nausea and vomiting that can happen with Apokyn.

Kynmobi:

• Take Kynmobi exactly as your healthcare provider tells you to take it.
• Your healthcare provider will tell you how much Kynmobi to take and teach you the right way to take it.
• Your healthcare provider may change your dose if needed.
• Do not change your dose of Kynmobi or take it more often than prescribed unless your healthcare provider has told you to.
• Do not take more than 1 dose of Kynmobi to treat an “OFF” episode.
• Do not take another dose of Kynmobi sooner than 2 hours after the last dose.
• Do not take Kynmobi more than 5 times a day.
• Do not cut, chew, or swallow Kynmobi.
• Your healthcare provider may prescribe another medicine for nausea called trimethobenzamide, an antiemetic, to take while you are taking Kynmobi. Antiemetic medicines help to decrease the symptoms of nausea and vomiting that can happen when you take Kynmobi.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Kynmobi sublingual film: 10 mg, 15 mg, 20 mg, 25 mg, and 30 mg of apomorphine hydrochloride
• Apokyn injection: 30 mg/3 mL (10 mg/mL) apomorphine hydrochloride.

This medicine is available in fallowing brand namesː

• Apokyn;Kynmobi

What side effects can this medication cause?

The most common side effects of this medicine include:

• yawning
• runny nose
• confusion
• swelling of your hands, arms, legs, and feet
• nausea
• sleepiness
• dizziness
• mouth swelling, pain, or sores

Less common,but serious side effects may include:

• nausea and vomiting
• sleepiness or falling asleep during the day
• allergic reactions
• dizziness
• mouth (oral) irritation
• strong (intense) urges
• high fever and confusion
• blood clots
• falls
• hallucinations or psychotic-like behavior
• dyskinesias
• hemolytic anemia
• intense urges
• heart problems
• QT prolongation
• injection site problems
• fever and confusion
• fibrotic complications
• priaprism
• swelling of ankles/legs

What special precautions should I follow?

• Following intravenous administration of Apokyn, serious adverse reactions including thrombus formation and pulmonary embolism due to intravenous crystallization of apomorphine have occurred. Consequently, Apokyn should not be administered intravenously.
• Nausea and vomiting, which may be severe, can happen with Apomorphine. Treatment with the antiemetic trimethobenzamide may be considered to pretreat or treat nausea and/or vomiting.
• Patients treated with dopaminergic medications, including apomorphine, have reported falling asleep while engaged in activities of daily living, including the operation of motor vehicles, which sometimes has resulted in accidents. Patients may not perceive warning signs, such as excessive drowsiness, or they may report feeling alert immediately prior to the event.
• Do not drive a car, operate machinery, or do anything that might put you at risk of getting hurt until you know how this medication affects you.
• Oral soft tissue swelling (lips, tongue, gingiva, and mouth) was reported with apomorphine. It is not known whether these events are related to apomorphine, sodium metabisulfite.
• Apokyn and Kynmobi contains sodium metabisulfite, a sulfite that may cause allergic-type reactions, including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in non-asthmatic people.
• Apomorphine may cause syncope, hypotension, or orthostatic hypotension. Do not change your body position too fast. Get up slowly from sitting or lying.
• Do not drink alcohol while you are taking Apomorphine . It can increase your chance of developing serious side effects.
• Some people who took medications such as apomorphine developed gambling problems or other intense urges or behaviors that were compulsive or unusual for them, such as increased sexual urges or behaviors. There is not enough information to tell whether the people developed these problems because they took the medication or for other reasons. Call your doctor if you have an urge to gamble that is difficult to control, you have intense urges, or you are unable to control your behavior. Tell your family members about this risk so that they can call the doctor even if you do not realize that your gambling or any other intense urges or unusual behaviors have become a problem.
• You should know that you may suddenly fall asleep during your regular daily activities while you are using apomorphine sublingual. You may not feel drowsy before you fall asleep. If you suddenly fall asleep while you are doing an everyday activity such as eating, talking, or watching television, call your doctor. Do not drive a car or operate machinery until you talk to your doctor.
• You should know that if you use nitroglycerin under your tongue while using apomorphine sublingual, your blood pressure may decrease and cause dizziness. After using apomorphine sublingual, you should lie down before and/or after using nitroglycerin.
• The use of apomorphine has been limited, but it has not been associated with serum enzyme elevations during treatment nor has it been implicated in cases of acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• Nausea
• loss of consciousness

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• There are no adequate data on the developmental risk associated with use of Apomorphine in pregnant women.

Can this medicine be used in children?

• The safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Kynmobi: Active ingredient:

• apomorphine hydrochloride

Inactive ingredients:

• disodium EDTA dihydrate, FD&C Blue #1, glycerol, glyceryl monostearate, hydroxyethyl cellulose, hydroxypropyl cellulose, maltodextrin, (-)-menthol, pyridoxine hydrochloride, sodium hydroxide, sodium metabisulfite, sucralose, and white ink.

Apokyn:

• Active ingredient: apomorphine hydrochloride, USP

• Inactive ingredients:' sodium metabisulfite, NF, benzyl alcohol, NF, water for injection, USP. It may also contain sodium hydroxide, NF and/or hydrochloric acid, NF.

Who manufactures and distributes this medicine?

Kynmobi: Manufactured for:

• Sunovion Pharmaceuticals Inc.
• Marlborough, Massachusetts; USA

Apokyn: Distributed by:

• MDD US Operations, LLC, as subsidiary of Supernus Pharmaceuticals
• Rockville, MD

What should I know about storage and disposal of this medication?

Kynmobi:

• Store Kynmobi at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep Kynmobi in the foil pouch until you are ready to take it.

Apokyn:

• Store Apokyn at room temperature, 68°F to 77°F (20°C to 25°C).
• Safely throw away medicine that is out of date or no longer needed.

• Dailymed label info on Apomorphine
• FDA Apomorphine

Apomorphine Resources
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