Apomorphine

Apomorphine drug was approved for the treatment of erectile dysfunction (erectile dysfunction) in 2001. This drug is sold in Europe under two brand names:

  1. Uprima
  2. Taluvian.

The developer, producer and owner of the European authorization for Apomorphine is the company Abbott. One of the Abbott’s partners that supplies Apomorphine drug for the erectile dysfunction treatment in Spain is Esteve Company.

Abbott and Esteve supplied to the European market sublingual tablets:

  • Apomorphine 2mg.
  • Apomorphine 3mg.

In 2001, besides Apomorphine tablets, Sildenafil tablets were the only ones for the erectile dysfunction treatment available for sale in Europe (Viagra).

Despite the attractive competitive conditions in the market of medicines for the treatment of erectile dysfunction, Abbott failed to achieve successful commercialization of Apomorphine.

Low levels of Apomorphine retail sales were due to the fact that this drug did not work for more than 2 hours, and was not effective in the treatment of severe erectile dysfunction.

Apomorphine mechanism of action is based on the stimulation of the central nervous system (CNS) areas that regulate the erection mechanism.

  • The advantage of such action mechanism lies in the fact that Apomorphine can restore the ability to achieve an erection only in response to sexual fantasies and/or visual sexual stimuli.
  • The drawback of such action mechanism lies in the fact that Apomorphine has virtually no effect on the physiological reasons for the lack of erection, and is not very effective in the treatment of mixed erectile dysfunction form.

The European Medicines Agency has approved two Apomorphine doses for the treatment of erectile dysfunction: 2mg and 3mg. Such doses provide a successful treatment of erectile dysfunction only in half of men, who suffer from erectile problems.

Post-marketing studies have demonstrated that many men needed higher Apomorphine doses of 5 mg or 6 mg to achieve a firm erection.

Apomorphine doses above 3 mg caused nausea and other side effects. Therefore, one single 3mg Apomorphine tablet is considered a maximum single dose of this medication.

In addition to serious drawbacks, Apomorphine did have several advantages that, however, failed to make it the best drug for the erectile dysfunction treatment.

The first advantage is the rapid onset of action. Apomorphine sublingual tablets start working no more than 20 minutes after the intake.The second advantage lies in the fact that Apomorphine tablet can be taken every 8 hours up to three times a day.

Since 2005, Apomorphine is not used to treat erectile dysfunction, yet it is still sold in pharmacies. Today, you can find in the retail sale Apomorphine injection solution, which is used for the symptomatic treatment of Parkinson’s disease.

Effect of Apomorphine injection on male sexual function was not been studied. Therefore, you should not use the injectable form of the drug for the treatment of erectile dysfunction.

Apomorphine indications

Apomorphine: drug therapy in Parkinson’s disease.

Today, Apomorphine is a drug of choice for patients with progressing parkinsonism. For effective treatment of this degenerative disease, Apomorphine is used in Australia as solution for injections:

  • 10mg/1mL
  • 20 mg/2 mL
  • 50 mg/5 mL
  • 100 mg/20 mL.

Apomorphine has a direct effect on dopaminergic structures of the brain stimulating synthesis of dopamine hormone. Subcutaneous administration of Apomorphine helps to improve impulse transmission between neurons.

This leads to gradual relief of Parkinson’s disease symptoms, such as:

  • Speech disorders
  • Limb tremor
  • Slowness of movements
  • Severe muscle stiffness.

Due to this mechanism of Apomorphine action, regular use of this drug helps patients with Parkinson’s disease to restore or maintain ability to coordinate their movements.

Syringe pens with Apomorphine solution are prescribed for treatment of parkinsonism in patients who fail to control its symptoms by means of oral medications.

In Australia, use of Apomorphine for treatment of Parkinson’s disease was approved in 1996. At Australian pharmacies, Apomorphine solution is sold under the brand names:

  • Movapo
  • Apomine.

Apomorphine for erectile dysfunction

Buy Apomorphine for erectile dysfunction treatment.

Men, who have contraindications to erectile dysfunction inhibitors (Sildenafil, Tadalafil and Vardenafil), can use Apomorphine to treat erectile dysfunction.

Although Apomorphine is less effective for solving potency problems than erectile dysfunction inhibitors, the main advantage of the drug is safety related to its smallest profile of side effects.

Apomorphine 2mg and 3 mg sublingual tablets for treatment of erectile dysfunction have become available in Europe at the beginning of this century, when were approved the following drugs:

  • Ixense
  • Uprima
  • Taluvian.

Ixense was sold in Sweden, Austria, Germany, France and Italy. Residents of Ireland, the UK, Spain, France, Sweden and Norway could use Uprima to solve sexual problems. Taluvian was sold only in Spain.

Despite a broad geographic coverage of the market, Apomorphine-containing drugs for erectile dysfunction had no a commercial success. On May 13, 2004, the drug was withdrawn from sale at the owner request of the trademark Taluvian, Abbott S.p.A. (Italy) company. On August 23 of the same year, Takeda – holder of registration certificate for Ixense took the same decision like Abbott.

On May 28, 2006, a 5-year-old trade agreement for Uprima sale was expired in European countries. The global pharmaceutical company Abbott took a decision not to renew the marketing authorization because of low sales of the drug.

Currently Apomorphine is no longer used to treat erectile dysfunction. To date, the drug is used only for fighting Parkinson’s disease.

Apomorphine for treatment of Parkinson’s disease

Apomorphine: a drug that is prescribed for patients with Parkinson’s disease

Injectable solution Apomorphine is not always used for treatment of Parkinson’s disease symptoms. Since the mid-1900s, the initial indications for Apomorphine use were:

  • muscle spasms
  • depressive state
  • drug dependence.

Antiparkinsonian effect of the drug was first demonstrated by Dr. R.S. Schwab. Since 1951, indications for Apomorphine use are movement disorders caused by Parkinson’s disease.

This drug should be used only for reduction of spontaneous locomotor activity. Such frequent symptoms of Parkinson’s disease as sleep disorders or excessive sweating are not indications for Apomorphine use.

Injectable solution was not always the only dosage form of Apomorphine. From 2001 to 2006, sublingual tablets Uprima, Taluvian and Ixense were sold in many European countries. Each tablet contained 2mg or 3mg of Apomorphine. An indication for Uprima, Taluvian and Ixense use is erectile dysfunction.

Apomorphine contraindications

Restrictions on the use of Apomorphine.

To decrease spontaneous motor activity in people with Parkinson’s disease, Apomorphine can be taken only in the absence of contraindications. Not all patients can take the medicine. Contraindications to the use of Apomorphine are:

  • Up to 18 years of age
  • Difficulty breathing
  • Severe hepatic insufficiency
  • Hypersensitivity to the active component.

Pharmacokinetic researches of drugs based on Apomorphine were not conducted in patients younger than 18 years. Therefore, Apomorphine is contraindicated in patients of childhood and adolescence age.

Breath holding during sleep is a common disorder in patients with Parkinson’s disease.
Apomorphine is contraindicated in people with difficulty breathing, because the drug may cause complex and ambiguous respiratory side effects:

  • increase in respiratory rate
  • reduction of pulmonary ventilation
  • decrease in tidal volume.

Intake of Apomorphine is sometimes associated with increased activity of liver enzymes. This drug may cause hepatotoxicity symptoms in patients with moderate to severe liver function disorders.

Apomorphine is prescribed in combination therapy with other drugs to treat Parkinson’s disease, such as Levodopa. However, Apomorphine is contraindicated if intake of Levodopa is accompanied with such symptoms as severe dyskinesia or dystonia.

Apomorphine side effects

How to avoid adverse reactions of Apomorphine.

In non-compliance with the recommended dosing regimen, Apomorphine may cause some side effects.

Patients who take high doses of this drug to improve the penile rigidity may experience such undesirable effects as:

  • sweating
  • dizziness.

Frequency and intensity of these Apomorphine side effects directly depend on a dose and duration of using this drug. Adverse reactions of Apomorphine are mild and transient, and quickly disappear after reducing the dose.

Oral administration of Apomorphine tablets for a long time may cause an overabundance of dopamine in the body. A sharp increase of this hormone concentration is associated with prolonged use of Apomorphine, can cause orthostatic hypotension.

The results of several clinical studies have confirmed that in prolonged use, Apomorphine sublingual tablets may also cause such adverse reactions as:

  • Vomiting (in approximately 7% of men)
  • Nausea (in more than 6% of patients)
  • Drowsiness (in less than 10% of men with erectile dysfunction).

A risk of bradycardia or fainting significantly increases in elderly men who take Apomorphine tablet to restore potency.

Apomorphine may cause adverse reactions extremely rarely when following the recommendations on the use of this drug. High safety profile is the most significant advantage of Apomorphine over other drugs for treatment of erectile dysfunction.