drugs

Apomorphine: What is it? What is it for? Side Effects and Contraindications of I.Randi

Generality

Apomorphine is an active ingredient capable of exerting a powerful dopaminergic action .

Apomorphine - Chemical Structure

Thanks to this particular action, apomorphine is used in the field of drug therapy against Parkinson's disease, to counteract movement disorders, when traditional therapies (with levodopa) are not effective or sufficient.

Until recently, apomorphine-based medicines were available on the market that could be administered sublingually with indications for the treatment of erectile dysfunction. However, to date (January 2019), apomorphine is only available in medicines to be administered parenterally (infusion or subcutaneous injection) with indications for the treatment of serious movement difficulties caused by Parkinson's disease.

Depending on the case, apomorphine-containing medicines to be administered intravenously are classified as H-band drugs (hospital drugs that can be hesitated in a pharmacy upon presentation of a non-repeatable limitative prescription - drugs sold to the public on prescription from hospitals or specialists) as Class A drugs (reimbursable by the National Health System).

Examples of Medicinal Specialties Containing Apomorphine

  • ApofinĀ®

Therapeutic indications

When is the use of apomorphine indicated?

The use of apomorphine is indicated in patients with Parkinson's disease for the treatment of serious movement difficulties that occur several times during the day and that do not respond to treatment with levodopa or other dopamine agonists.

To tell the truth, apomorphine is available both in cartridges ready for use by subcutaneous injection and in the form of a solution to be administered by subcutaneous infusion .

Apomorphine in cartridges by subcutaneous injection is normally used "as needed" in the treatment of movement difficulties mentioned above; while the solution for subcutaneous infusion is used when the patient responds only partially to the administration of apomorphine as needed, or in the case in which it is necessary to give injections as needed in an excessively frequent way to be able to control movement disorders.

Did you know that ...

Apomorphine is also included in the composition of veterinary drugs used for the induction of emesis (vomiting) in dogs.

Warnings

Warnings and Precautions for the use of Apomorphine

Usually, before starting apomorphine treatment, the doctor submits the patient to an electrocardiogram (ECG) and will investigate the presence of any other diseases or disorders.

Furthermore, in conjunction with apomorphine treatment, it is not unusual for the doctor to prescribe the concomitant use of an antiemetic drug in order to counteract the action favoring the vomiting of which apomorphine is endowed.

However, before starting apomorphine treatment, you should tell your doctor if:

  • You are suffering from renal, pulmonary, cardiac and / or vascular diseases;
  • He suffered orthostatic hypotension;
  • One has suffered or has a family history of long QT syndrome;
  • You suffer from pathologies of the glands that produce hormones;
  • You frequently suffer from nausea and / or vomiting;
  • It is debilitated.

However, as a precautionary measure, before taking apomorphine, it is advisable to inform the physician of your health conditions, informing him of the possible presence of disorders or diseases of any kind, even if not indicated in the above list.

On the other hand, during treatment with apomorphine, you must inform your doctor if they appear:

  • Cardiac symptoms (for example, palpitations, fainting, etc.);
  • Diarrhea;
  • Impulse control disorders (development of desires, impulses or unusual behaviors, inability to resist the temptation to do certain activities or behave in a certain way. Such disorders may include, for example, excessive eating, gambling addiction, excessive sexual desire, etc.);
  • If it is necessary to start other drug treatments.

Please note

Apomorphine treatment can cause side effects that can affect the ability to drive and / or use machinery (for example, drowsiness, mental confusion, etc.); therefore, these activities should be avoided.

Pharmacological Interactions

Interactions of Apomorphine with Other Drugs

Before starting apomorphine therapy it is absolutely necessary to inform your doctor:

  • If you are taking other medicines to treat Parkinson's disease, as the effect of apomorphine may increase and / or unusual side effects may appear;
  • If you are taking drugs that can act centrally (for example, antipsychotics, neuroleptics, anti-emetic drugs, etc.);
  • Drugs that have effects on the heart rhythm (for example, antiarrhythmics, antidepressants, antibiotics, etc.).

However, before starting apomorphine treatment, you need to tell your doctor if you are taking, or have recently taken, any drugs or products of any kind, including non-prescription medicines (SOPs), over-the-counter (OTC) drugs, herbal and herbal products and homeopathic products.

Side effects

Side Effects Caused by Apomorphine Intake

Like any other drug, atorvastatin can also cause side effects, although not every patient experiences them or gets them in the same way. In fact, each person reacts subjectively to the administration of the drug manifesting side effects that are different in type and intensity, or not manifesting them at all.

However, below are some of the major side effects that can occur during apomorphine treatment.

Psychiatric disorders

Apomorphine intake could lead to hallucinations, confusion and impulse control disorders, such as:

  • Excessive increase in libido;
  • Pathological addiction to gambling;
  • Compulsive Shopping;
  • Bulimia and other eating disorders;
  • Etc.

Nervous system disorders

Drowsiness, dyskinesias and syncope may occur during apomorphine treatment.

Gastrointestinal disorders

Administration of apomorphine may cause nausea and vomiting. To avoid these side effects, the doctor usually prescribes treatment with anti-emetic drugs for the patient.

Other side effects

Other side effects that could occur during apomorphine treatment consist of:

  • Allergic reactions, even serious, in sensitive individuals;
  • Reactions at the injection / infusion site (for example, pain, inflammation, formation of subcutaneous nodules, localized necrosis, etc.);
  • Orthostatic hypotension;
  • eosinophilia;
  • Autoimmune hemolytic anemia;
  • Positivity to the Coombs test.

Overdose

In the event of apomorphine overdose, severe symptoms may occur, including respiratory depression (requires the administration of naloxone intravenously) and bradycardia (requires the administration of atropine).

Moreover, in the case of overdose or individual hypersensitivity to apomorphine, the administration of sulpiride intramuscularly at a dose variable according to the symptomatology manifested by the patient should be taken into consideration. For this reason, in the case of an overdose of apomorphine - established or presumed to be - it is necessary to go immediately to the nearest emergency room, taking care to bring along the packaging of the medicine taken.

Action mechanism

How does Apomorphine work?

Apomorphine is an active ingredient with a marked dopaminergic activity . In detail, it is a powerful agonist of dopamine receptors type 1 and 2 (D1 and D2). Thanks to this action, apomorphine is able to activate the aforementioned receptors giving rise to a biological response similar to that induced by the endogenous neurotransmitter (dopamine, in fact). All this results in an improvement in movement disorders that characterize Parkinson's disease.

Method of use and Posology

How to take Apomorphine

For the treatment of severe movement disorders, apomorphine can be taken by subcutaneous injection "as needed" or by subcutaneous infusion.

Generally, the doctor also prescribes the use of an antiemetic drug, domperidone, in order to avoid the onset of vomiting (in fact, apomorphine has emetic activity).

Apomorphine by subcutaneous infusion

Subcutaneous infusion (performed at the level of the abdomen) should only be carried out by specialized healthcare personnel using a programmable mini-pump. Generally, the usual starting dose is 1 mg of apomorphine per hour. This dose can then be increased depending on the response of each patient to the treatment.

Apomorphine by subcutaneous injection

Apomorphine in the form of cartridges ready for use by subcutaneous injection, on the other hand, can also be used by the patient himself or by those who take care of him, provided that all the indications provided by the doctor and the instructions in the leaflet of the medicine are followed. that you must use. These cartridges must be inserted in a special device equipped with a needle which, by pressing a dispenser button, automatically injects. The initial dose usually administered (also in this case at abdominal level) is 1 mg of apomorphine. Later, the doctor can gradually increase this dose until the desired effect is achieved.

Generally, the dose of apomorphine administered by subcutaneous injection as needed is between 3 mg and 30 mg a day, to be taken in divided doses throughout the day.

In any case, the exact dosage of apomorphine will be established by the doctor on a case-by-case basis, in a strictly individual manner for each patient. Therefore, it is absolutely necessary to follow the instructions and instructions provided by it.

Pregnancy and breastfeeding

Can apomorphine be taken in pregnancy and during breastfeeding?

Because of the negative effects that could occur, the use of apomorphine in pregnant women and breast-feeding mothers is contraindicated .

Contraindications

When Apomorphine should not be used

The use of apomorphine is contraindicated in all the following cases:

  • Known hypersensitivity to apomorphine itself and / or to one or more of the excipients contained in the medicinal product to be used;
  • In patients who have experienced severe dyskinesias or hypotonia after levodopa treatment;
  • In the presence of respiratory depression and / or depression of the central nervous system;
  • In patients with liver failure;
  • In patients with mental disorders such as acute and chronic psychosis, visual hallucinations and mental confusion;
  • In the presence of dementia;
  • In pregnancy and during breastfeeding.

Please note

For more in-depth information on indications, warnings and precautions, interactions, side effects, use during pregnancy and during lactation and contraindications of the different types of apomorphine-based medicines, it is advisable to consult your doctor and read carefully the package insert for the medicinal product to be used.