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Apomorphine Hydrochloride Injection - Dosage, Indications, Adverse Effects, and Administration

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Apomorphine hydrochloride injections are indicated for a patient suffering from Parkinson’s disease. Read the article below to learn more about it.

Medically reviewed by

Dr. Kaushal Bhavsar

Published At March 2, 2023
Reviewed AtMarch 2, 2023

Overview

Apomorphine hydrochloride injection is commonly indicated to be administered in the skin or subcutaneously and is an "on-demand therapy for 'OFF' episodes of Parkinson's disease in people. Apomorphine is a Dopamine D2 agonist used to treat advanced stages of Parkinson's disease. It was first synthesized in 1845 and used in 1884 for Parkinson's disease. Apomorphine has also been discovered as an emetic, a sedative, a treatment for alcoholism, and a treatment for other movement disorders. Apomorphine got its FDA (Food and Drug Administration) approval on 20 April 2004.

Dosage

The dose of this medicine is indicated differently for different patients. Follow the orders or the directions given by the healthcare provider. If the dose is different, only change it if the doctor tells you to do so. The amount of medicine the patient takes depends on the strength of the medicine. It also depends on the dosage decided by the doctor. The Apomorphine Hydrochloride comes in solution for subcutaneous injection or pen in 10 milligrams per milliliter (30mg/3mL pen injector).

For Injection Dosage

Adults - The first dose is 0.1 milliliters (mL) or 1 milligram (mg) to 0.2 mL (2 mg), which is injected under the skin. The doctors may adjust the dose as required. However, the dose is not higher than 0.6 mL (6 mg) injected under the skin or subcutaneously per day.

Premedication

  • There is a high chance of experiencing nausea and vomiting with treatment. It is indicated to have an antiemetic (e.g., Trimethobenzamide 300 mg thrice a day) 3 days before the initial Apomorphine dose.

  • Apomorphine, along with Trimethobenzamide, should only be continued as long as it is necessary to control nausea and vomiting, and mostly no longer than two months after initiation of treatment.

  • Trimethobenzamide can increase the risk of somnolence, dizziness, and falls.

  • It is contraindicated with 5HT3 antagonist antiemetics such as Ondansetron, Granisetron, Dolasetron, and Palonosetron, which can result in profound hypotension and loss of consciousness when administered along with Apomorphine Hydrochloride.

For Patients

What Is Advanced Parkinson’s Disease?

Advanced Parkinson's disease is a late or last stage of Parkinson's disease that is noted by limited mobility. Certain medications are used to control Parkinson's in the early stages, but these medications lose their ability to work effectively, and symptoms worsen. So then the doctors classify this caution as advanced Parkinson's disease.

Advanced Parkinson's disease usually occurs after ten years of living affected with Parkinson's. Patients with advanced Parkison’s disease require a wheelchair or other assisting devices to move. They also feel at higher risk of falling, having cognitive problems, and dementia.

What Are the Stages of Parkinson’s?

Parkinson's disease can be divided into four stages.

Early or Diagnosis Stage - When a person is experiencing symptoms for the first time, is diagnosed, and comes to terms with this.

Maintenance Stage - When symptoms are controlled by the prescribed medication.

Advanced Stage - Generally known as the 'complex phase.'

Palliative Stage - Providing relief from the condition's symptoms, stress, and pain.

What Are the Symptoms of Advanced Parkinson’s Disease?

Advanced Parkinson's Disease Symptoms -

Parkinson's disease mainly occurs in adults or older people and is described by tremors in the hands, arms, legs, and face, slow movement, poor balance, and lack of coordination. Parkinson's disease symptoms are mild to moderate and less limiting to daily life. These include:

  • Tremors or shaking.

  • Changes in posture, walking, and facial expression.

  • Difficulty walking, talking, eating, or dressing.

  • Falling.

  • Needing a walker or wheelchair to move.

  • Needing help with daily activities.

  • Having stiffness in the legs makes it difficult to stand or walk.

  • Becoming bedridden.

  • Requiring regular nursing care.

  • Experiencing hallucinations and delusions.

Why Are Apomorphine Injections Medication Prescribed?

Apomorphine injection is indicated to treat off episodes such as times of difficulty moving, walking, and speaking. Apomorphine injections are mostly indicated in advanced Parkinson's disease (Parkinson's disease, a disorder that affects the nervous system that leads to difficulties with movement, muscle control, and balancing) when affected patients are not responding to the other medications for their condition. Apomorphine injection belongs to the class of dopamine agonist medications. Apomorphine works by acting in place of dopamine, a natural chemical synthesized in the brain that is required to control movement.

What Side Effects Can This Medication Cause?

Apomorphine injection may cause side effects.

  • Weakness.

  • Nausea.

  • Bruising.

  • Vomiting.

  • Constipation.

  • Headache.

  • Redness.

  • Yawning.

  • Runny nose.

  • Arm, leg, or back pain.

  • Pain or difficulty in urination.

  • Soreness.

  • Diarrhea.

  • Pain.

  • Swelling.

  • Itching in the place where the patient injects Apomorphine.

Some Serious Side Effects.

  • Rash.

  • Hives.

  • Itching.

  • Falling.

  • Swelling on the face.

  • Swollen eyes.

  • Swollen throat.

  • Difficulty breathing.

  • Difficulty in swallowing.

  • Fainting.

  • Rapid heartbeat.

  • Bruising.

  • Chest pain.

  • Sudden uncontrollable movements.

  • Swelling of the hands, feet, ankles, or lower legs.

  • Aggressive behavior.

  • Agitation.

  • Disorganized thoughts.

  • Depression.

  • Fever.

  • Hallucinations.

  • Confusion.

  • Painful erection.

  • Tiredness.

  • Shortness of breath.

How Should Apomorphine Hydrochloride Injection Be Administered?

Apomorphine comes as a liquid solution to inject subcutaneously or beneath the skin. Apomorphine hydrochloride is injected when it is needed. While injecting, following the directions carefully and asking your doctor or pharmacist to explain the complete procedure are very important. Use Apomorphine injection exactly as directed. Avoid using it more or less, or use it more often than prescribed.

  • Avoid the use of the second dose of apomorphine injection for the treatment of the same "off" episode. Instead, it is recommended to wait at least 2 hours between doses.

  • The healthcare provider will indicate another medication called Trimethobenzamide to take at the beginning of the Apomorphine treatment. Trimethobenzamide will help decrease the chance of developing nausea and vomiting while the patient is using an Apomorphine injection. The health care professional will probably ask the patient to start taking Trimethobenzamide a few days before they initiate the administration of Apomorphine injection and to continue taking it for two months. The patient should be aware that taking Trimethobenzamide along with an Apomorphine injection may increase the risk of drowsiness, dizziness, and falls. However, do not stop taking Trimethobenzamide without consulting a healthcare professional.

  • The doctor will start the patient's treatment with a small dose of Apomorphine injection and eventually higher the dose accordingly. It is very important to make the patient aware of the consequences of the dosage and when they need to stop taking the injection. If the patient misses the dose, they should consult the doctor about what to do if they are not using Apomorphine injection for longer than one week. The doctor will probably ask the patient to restart the administration of the Apomorphine hydrochloride with a low dose and increase the dose accordingly.

  • Apomorphine solution generally comes in a glass cartridge with an injector pen. Sometimes the needles are provided with the pen, and additional required needles are sold separately in the authorized pharmacies. Ask the doctor or pharmacist about the type of needle requirements. It is always recommended to use a new, sterile needle for each injection.

  • It is advisable to receive the first dose of Apomorphine injection in the hospital so that the doctor can monitor the patient's condition closely. After that, the doctor may ask the patient to inject Apomorphine themself and have a friend or relative perform the injections. The patient should read all the written instructions that come with it before injecting it for the first time. Then, ask the doctor or pharmacist to demonstrate the procedure for injecting the medication.

  • The patient should be able to read the numbers on the injector pen suggesting the dose of the medicine. The doctor should explain the way to read the milligrams of medicine required for the patient, but the pen is marked with milliliters.

  • The Apomorphine injector pen is only for one patient to use. Therefore, do not share the pen with anyone.

  • Be careful not to get Apomorphine injections on the skin or in the eyes. If Apomorphine injection does get on the skin or in the eyes, immediately wash the skin or flush the eyes with cold water.

  • It is recommended to inject the Apomorphine in the areas of the stomach, upper arm, or upper leg areas. Avoid injecting the pen into a vein or on sore skin, red, scarred, infected, bruised, or abnormal. Instead, use a different spot for injection every time, choosing from among the spots the patients have been told to use. Keep a record of the injection's purchasing date and the spot of each injection. Do not use the same spot again and again in a row.

  • The patient should always look at the Apomorphine solution before injecting it. It is important to make them aware of the color and consistency of the medicine. It is recommended that it should be colorless, clear, and free of particles. Avoid using or discarding the Apomorphine injections if they change color to cloudy or green, may contain some tiny particles, or have an expiration date.

  • Practice keeping a record of the Apomorphine injection dose used each time the patient receives an injection so they will know when to replace the medication cartridge.

  • The patient can clean their Apomorphine injector pen with a damp cloth as needed. Never use strong disinfectants or wash the pen under running water.

The Important Point To Remember -

  • Never reuse needles.

  • Avoid the needle getting touched at any surface except the area on the body where it will inject the medicine. Also, avoid carrying the injector pen with the attached needle.

  • Ask the doctor or pharmacist how to discard the used needles, and they may ask the patient to get a puncture-resistant container for discarding the needles and, most importantly, keep it out of reach of children.

For Doctors

Indications

Apomorphine injections are indicated to treat hypomobility and off episodes associated with advanced Parkinson's disease.

How to Administer the Apomorphine Hydrochloride Injections?

For subcutaneous (SC) administration of Apomorphine hydrochloride, it is important to take a test.

Test dose

Start the dosing when patients are in an "off" state.

  • The Initial indicated dose should be 2 mg for testing the patient's response and closely monitoring the blood pressure and pulse rate; in both standing and supine, blood pressure and pulse should be checked at 20 minutes, 40 minutes, and 60 minutes postcode.

  • If the patient develops clinically significant orthostatic hypotension after 60 minutes in response to this test dose should not be considered a candidate for treatment.

  • If the patient is able to tolerate the 2 mg dose and responds normally, the starting dose should be 2 mg, used on an as-needed basis to treat recurring "off" episodes.

  • If required, the dose can be increased to 1 mg every few days for the patient.

If the patient can tolerate a 2 mg test dose and the dose does not respond.

  • The next dose of 4 mg should be administered under a healthcare professional's supervision at least 2 hours after the initial test dose.

  • If the 4 mg test dose is tolerated and the patient responds, the initial maintenance dose should be 3 mg used on an as-needed.

  • If required, the dose can be increased to 1 mg every few days on a patient’s response.

If the patient is not able to tolerate a 4 mg test dose.

  • If a 4-mg test dose is not tolerated, a 3-mg test dose may be administered during a separate "off" period under the supervision of experienced healthcare professionals. At least 2 hr after the previous dose.

  • If a 3-mg test dose is tolerated, the initial maintenance dose should be 2 mg used on an as-needed basis to treat existing "off" episodes.

  • If needed, and the 2-mg dose is tolerated, the dose can be increased to 3 mg after some days.

What Are the Ingredients in Apomorphine?

Active Ingredient: Apomorphine hydrochloride.

Inactive Ingredients: Sodium metabisulfite, benzyl alcohol, water for injection. It may also contain sodium hydroxide and hydrochloric acid.

Storage

Subcutaneous Apomorphine hydrochloride injection requires a storage temperature of 25°C (77°F).

Pharmacology

Pharmacodynamics

Apomorphine is a dopamine agonist that can stimulate brain areas involved in motor control. It has a short duration of action and a wide therapeutic index, and overdosing on the drug can lead to significant toxicity. Patients should be guided about the side effects regarding nausea, vomiting, low blood pressure, oral mucosal inflammation or irritation, falls, hallucinations, daytime somnolence, psychotic-like behavior, impulsive or hyperactive behavior, and withdrawal hyperpyrexia.

Given the incidence of nausea and vomiting in patients taking Apomorphine, treatment with Trimethobenzamide may be recommended prior to or during therapy. Antiemetic pretreatment may be started three days prior to beginning therapy with Apomorphine - it is highly recommended that it should only be continued as long as it is required no longer than two months.

Mechanism of Action

Apomorphine is a dopamine agonist, which is a non-ergoline and has a high binding affinity to dopamine and its D2, D3, and D5 receptors. Stimulating D2 receptors in the caudate-putamen, an area of the brain responsible for movement or locomotor control, can be responsible for Apomorphine's action. However, the actual reason by which the cellular effects of apomorphine treat hypomobility of Parkinson's remains unknown.

Absorption: Apomorphine has a plasma Tmax of 10 to 20 minutes. The AUC and Cmax of Apomorphine vary between patients, with 5 to 10 minutes.

The Volume of Distribution: The volume of distribution of subcutaneous Apomorphine is 123 to 404 liters, with an average of 218 Liters.

Protein Binding: Apomorphine binds 99.9 percent of human serum albumin.

Route of Elimination: No enough studies regarding Apomorphine's route of elimination are readily available. It is stated that Apomorphine can be eliminated through urine at around 93 percent and feces at 16 percent.

Half-life: The terminal elimination half-life of subcutaneous injection of Apomorphine is 40 minutes.

Clearance: The clearance of a subcutaneous injection of Apomorphine is 223 liters per hour.

Toxicity: Patients who overdose on Apomorphine may experience nausea, hypotension, and loss of consciousness. It is recommended to treat patients with symptomatic and supportive measures.

What Are the Adverse Effects of Apomorphine Hydrochloride?

Apomorphine Hydrochloride may cause serious side effects, including

  • Hives.

  • Breathing difficulties.

  • Swelling of your face, lips, tongue, or throat.

  • Nausea.

  • Vomiting.

  • Twitching.

  • Uncontrollable movements of your eyes, tongue, face, lips, arms, or legs.

  • Chest pain.

  • Fast or slow heartbeats.

  • Shortness of breath.

  • Lightheadedness.

  • Daytime sleepiness.

  • Drowsiness.

  • Confusion.

  • Hallucinations.

  • Unusual thoughts or behavior.

  • Cough.

  • Fever.

  • Pain while breathing.

  • Shortness of breath while lying down.

  • Pain in your stomach, back, or legs.

  • Swelling in your lower legs.

  • Painful penis erection.

  • Increased sexual urges.

  • Unusual urges to gamble and other intense urges.

  • Swelling.

  • Confusion.

  • Yawning and sleepiness.

  • Runny nose.

  • Itching.

  • Bruising.

Drug Interactions

Drug interactions refer to the reaction in the body when one or more drugs are administered at the same time. These drugs can interact with each other and may result in serious medical conditions. Therefore it is important to avoid using the following drugs along with Apomorphine Hydrochloride. However, certain medicines should not be used together; sometimes, two different drugs may be used together even if they result in an interaction.

Administrating Apomorphine hydrochloride medicine with any of the following medicines is not recommended. Therefore, doctors need to advise a drug along with Apomorphine Hydrochloride that should not react and lead to adverse effects.

The following drugs are completely contraindicated along with Apomorphine hydrochloride injections.

  • Alosetron.

  • Cisapride.

  • Dolasetron.

  • Dronedarone.

  • Granisetron.

  • Netupitant/Palonosetron.

  • Ondansetron.

  • Palonosetron.

  • Thioridazine.

The Following drug reacts with Apomorphine hydrochloride and results in serious conditions.

  • Adagrasib.

  • Amiodarone.

  • Amisulpride.

  • Anagrelide.

  • Aripiprazole.

  • Arsenic Trioxide.

  • Artemether.

  • Artemether/Lumefantrine.

  • Asenapine.

  • Asenapine Transdermal.

  • Buprenorphine.

  • Buprenorphine Buccal.

  • Buprenorphine subdermal implant.

  • Buprenorphine transdermal.

  • Buprenorphine, long-acting injection.

  • Calcium/Magnesium/Potassium/Sodium Oxybate.

  • Ceritinib.

  • Chlorpromazine.

  • Clarithromycin.

  • Clozapine.

  • Disopyramide.

  • Dofetilide.

  • Droperidol.

  • Encorafenib.

  • Entrectinib.

  • Eribulin.

  • Fedratinib.

  • Fexinidazole.

  • Fluphenazine.

  • Foscarnet.

  • Glasdegib.

  • Granisetron.

  • Haloperidol.

  • Hydroxychloroquine Sulfate.

  • Ibutilide.

  • Iloperidone.

  • Inotuzumab.

  • Isoflurane.

  • Ivosidenib.

  • Lefamulin.

  • levofloxacin.

  • lofexidine.

  • lopinavir.

  • loxapine.

  • loxapine inhaled.

  • Macimorelin.

  • Maprotiline.

  • Mefloquine.

  • Methadone.

  • Metoclopramide intranasal.

  • Midostaurin.

  • Mirtazapine.

  • Moxifloxacin.

  • Nilotinib.

  • Octreotide.

  • Ofloxacin.

  • Olanzapine.

  • Olopatadine intranasal.

  • Oxaliplatin.

  • Paliperidone.

  • Panobinostat.

  • Pazopanib.

  • Pentamidine.

  • Perphenazine.

  • Pimavanserin.

  • Pimozide.

  • Pitolisant.

  • Ponesimod.

  • Procainamide.

  • Prochlorperazine.

  • Promethazine.

  • Propafenone.

  • Protriptyline.

  • Quetiapine.

  • Quinidine.

  • Ribociclib.

  • Risperidone.

  • Saquinavir.

  • Selinexor.

  • Sevoflurane.

  • Siponimod.

  • Sodium oxybate.

  • Sotalol.

  • Tetrabenazine.

  • Thioridazine.

  • Thiothixene.

  • Toremifene.

  • Trazodone.

  • Trifluoperazine.

  • Umeclidinium Bromide/Vilanterol inhaled.

  • Vandetanib.

  • Vemurafenib.

  • Vilanterol/fluticasone furoate inhaled.

  • Ziprasidone.

The following drug may react with Apomorphine hydrochloride and requires close monitoring.

  • Albuterol.

  • Alfentanil.

  • Alfuzosin.

  • Alprazolam.

  • Amifostine.

  • Amitriptyline.

  • Amobarbital.

  • Amoxapine.

  • Arformoterol.

  • Aripiprazole.

  • Atomoxetine.

  • Azelastine.

  • Azithromycin.

  • Baclofen.

  • Bedaquiline.

  • Belladonna and Opium.

  • Benazepril.

  • Bromocriptine.

  • Brompheniramine.

  • Buprenorphine.

  • Buprenorphine buccal.

  • Butabarbital.

  • Butalbital.

  • Butorphanol.

  • Cabergoline.

  • Captopril.

  • Carbinoxamine.

  • Carisoprodol.

  • Cenobamate.

  • Chloral Hydrate.

  • Chlordiazepoxide.

  • Chloroquine.

  • Chlorpheniramine.

  • Chlorpromazine.

  • Chlorzoxazone.

  • Citalopram.

  • Clemastine.

  • Clobazam.

  • Clomipramine.

  • Clonazepam.

  • Clorazepate.

  • Clozapine.

  • Codeine.

  • Crizotinib.

  • Cyclizine.

  • Cyclobenzaprine.

  • Cyproheptadine.

  • Dantrolene.

  • Daridorexant.

  • Dasatinib.

  • Degarelix.

  • Desflurane.

  • Desipramine.

  • Deutetrabenazine.

  • Dexchlorpheniramine.

  • Dexmedetomidine.

  • Diazepam.

  • Difelikefalin.

  • Difenoxin hc.

  • Dimenhydrinate.

  • Diphenhydramine.

  • Diphenoxylate HCl.

  • Donepezil.

  • Doxepin.

  • Doxylamine.

  • Droperidol.

  • Efavirenz.

  • Eliglustat.

  • Erythromycin base.

  • Erythromycin ethyl succinate.

  • Erythromycin lactobionate.

  • Erythromycin stearate.

  • Escitalopram.

  • Estazolam.

  • Ethanol.

  • Etomidate.

  • Ezogabine.

  • Fingolimod.

  • Fluconazole.

  • Fluoxetine.

  • Fluphenazine.

  • Flurazepam.

  • Formoterol.

  • Fostemsavir.

  • Gemifloxacin.

  • Gemtuzumab.

  • Gilteritinib.

  • Goserelin.

  • Haloperidol.

  • Histrelin.

  • Hydromorphone.

  • Hydroxyzine.

  • Iloperidone.

  • Imipramine.

  • Indacaterol, inhaled.

  • Indapamide.

  • Isradipine.

  • Itraconazole.

  • Ketamine.

  • Ketoconazole.

  • Ketotifen, ophthalmic.

  • Lapatinib.

  • Lenvatinib.

  • Leuprolide.

  • Levalbuterol.

  • Levodopa.

  • Levoketoconazole.

  • Levorphanol.

  • Lithium.

  • Loperamide.

  • Lorazepam.

  • Loxapine.

  • Loxapine inhaled.

  • Lurasidone.

  • Maprotiline.

  • Maraviroc.

  • Marijuana.

  • Melatonin.

  • Meperidine.

  • Meprobamate.

  • Metaxalone.

  • Methadone.

  • Methocarbamol.

  • Methyldopa.

  • Methylphenidate.

  • Metoclopramide.

  • Midazolam.

  • Midazolam intranasal.

  • Mifepristone.

  • Mirtazapine.

  • Morphine.

  • Motherwort.

  • Nabilone.

  • Nalbuphine.

  • Nortriptyline.

  • Olanzapine.

  • Olodaterol inhaled.

  • Opium tincture.

  • Orphenadrine.

  • Osilodrostat.

  • Osimertinib.

  • Oxazepam.

  • Oxycodone.

  • Oxymorphone.

  • Ozanimod.

  • Paliperidone.

  • Papaverine.

  • Pasireotide.

  • Pentazocine.

  • Pentobarbital.

  • Perphenazine.

  • Phenobarbital.

  • Phenylephrine PO.

  • Pramipexole.

  • Primaquine.

  • Primidone.

  • Prochlorperazine.

  • Promethazine.

  • Propofol.

  • Protriptyline.

  • Quazepam.

  • Quetiapine.

  • Quinine.

  • Ramelteon.

  • Ranolazine.

  • Rilpivirine.

  • Risperidone.

  • Romidepsin.

  • Ropinirole.

  • Scullcap.

  • Secobarbital.

  • Selpercatinib.

  • Sertraline.

  • Sevoflurane.

  • Shepherd's purse.

  • Solifenacin.

  • Solriamfetol.

  • Sorafenib.

  • Stiripentol.

  • Sufentanil.

  • Sunitinib.

  • Tacrolimus.

  • Tapentadol.

  • Telavancin.

  • Temazepam.

  • Thiothixene.

  • Topiramate.

  • Tramadol.

  • Trazodone.

  • Triazolam.

  • Triclabendazole.

  • Trifluoperazine.

  • Trimipramine.

  • Triptorelin.

  • Valentine.

  • Vardenafil.

  • Voclosporin.

  • Voriconazole.

  • Vorinostat.

  • Ziconotide.

The following drug reacts with Apomorphine Hydrochloride and results in minor interactions.

  • Acetazolamide.

  • Anastrozole.

  • Ceritinib.

  • Cyclophosphamide.

  • Eucalyptus.

  • Flecainide.

  • Larotrectinib.

  • Ruxolitinib Topical.

  • Sage.

  • Trimethobenzamide.

Other Interactions

Certain medicines are not recommended to be used while eating or certain items. Since it can interact and lead to problems, using alcohol or tobacco with certain medicines may also cause interactions.

If the following drug is used together, the doctor may regulate the dose or give special instructions about using food, alcohol, or tobacco.

  • Ethanol.

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Dr. Kaushal Bhavsar
Dr. Kaushal Bhavsar

Pulmonology (Asthma Doctors)

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