Apomorphine

The similarity of the Apomorphine with the body's own messenger substance dopamine, it is one of the most effective dopamine imitators available to medicine and pharmacy today. Formerly used primarily as an emetic, today apomorphine has a wider range of effects in different areas of indication.

What is apomorphine?

The active ingredient is most frequently and most importantly used in the treatment of Parkinson's disease in the late phase, as a continuous infusion or subcutaneous injection.

Apomorphine belongs (eponymous) to the aporphine aklaloids. The morphine derivative is obtained by heating morphine with concentrated hydrochloric acid. Its structure is closely related to that of human dopamine. The rather water-resistant crystals of the salt apomorphine hydrochloride can appear in different colors, white, slightly yellowish-brownish or gray-green.

It turns green when exposed to light. Although it is a dopamine agonist, the morphine derivative itself does not have an opioid effect. The triggering effect is more like that of the body's own messenger substance dopamine. The nausea-inducing apomorphine was previously mainly used for poisoning. From 2001 onwards, it was used in the form of a lozenge, which acted on the oral mucosa under the tongue, in the treatment of male erectile dysfunction.

Apomorphine has occasionally been used as an adjunct to drug withdrawal. The active ingredient is most frequently and most importantly used in the treatment of Parkinson's disease in the late phase, as a continuous infusion or subcutaneous injection. Apomorphine is also used in homeopathy.

Pharmacological effect

In contrast to libido-strengthening preparations, the pro-erectile effect of apomorphine is more centrally mechanical. Via the dopamine connection in the hypothalamus, the active ingredient relaxes the muscles in the erectile tissue of the penis over several neuronal levels. The improved blood supply promotes erectile function.

Since the active ingredient is absorbed very well by the cells, administration as a tablet under the tongue is most successful. Here it shows the desired success through the rapid absorption in the mucous membrane within 20 minutes. Apomorphine does not create an obsessive-compulsive disorder, leaves the sex drive unchanged and does not have a negative impact on the psyche.

Apomorphine is particularly suitable for the treatment of Parkinson's patients in the late phase. The symptoms of this disease are due to a lack of dopamine. The reason for this is the loss or destruction of dopamine-producing nerve cells in the central nervous system. The normal sequence of movements is severely disturbed, tremors (tremors), akinesia (movement disorders) and rigidity (strong muscle tension, muscle rigidity) are the consequences.

Medical application & use

Because of its property as a dopamine receptor agonist, apomorphine is well suited for reducing the motor symptoms of Parkinson's disease when taking levodopa. Its effect lies in the brain, where it mimics the mode of action of the body's own messenger substance. However, due to the severe side effects, it is not considered a primary drug.

The nausea-inducing effect also sets in right here when certain dopamine receptors in the central nervous system are stimulated. To empty the patient's stomach, the active ingredient domperidone is given two days before the start of treatment.

As an emetic, apomorphine has meanwhile been replaced by far more tolerable means, as there is a risk of cardiovascular disorders or respiratory paralysis, especially in children. Apomorphine attracted negative attention when taking illegal drugs in the drug scene.

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Risks & side effects

The side effects that occur may depend on the form of administration (syringe, tablet, infusion, ointment) and the frequency of use. The common combination of apomorphine with levodopa makes it difficult to identify the cause of the drug side effects that have actually occurred.

In addition to the increased tendency to nausea and nausea, hypotension (drop in blood pressure when getting up from a lying position), uncontrollable, voluntary movements, confusion or drowsiness, hallucinations, digestive disorders and breathing disorders often occurred. Infections, mouth ulcers, taste disorders occur, as well as inflammation of the nasal or throat mucous membrane.

Less often the increased formation of white blood cells and psychoses. Obsessive-compulsive behavioral problems may require a change in treatment. There are interactions with clozapine (agent for the treatment of mental and nervous symptoms) and neuroleptics taken at the same time. Apomorphine can increase the effects of antihypertensive drugs and alcohol.

It is not recommended to pregnant and breastfeeding women, as well as children and adolescents, people with weak liver and kidney functions, with a pre-existing tendency to nausea, with hypotension, cardiovascular or lung diseases. Elderly and debilitated people should only be prescribed apomorphine after a careful benefit / risk assessment.