Melperon

Melperone is an active substance for the treatment of schizophrenia and its accompanying symptoms, such as sleep disorders, restlessness, agitation, anxiety disorders or confusion (delirium) in dementia. Melperone is a sedative, i.e. an anxiolytic and calming agent from the group of low-potency neuroleptics (butyrophenones).

It is structurally very similar to haloperidol. Melperone also has a mood-enhancing and, in high doses, sleep-promoting effect. A major advantage of melperone over other low-potency neuroleptics is that it has very little effect on the cardiovascular system and therefore cardiovascular-related side effects are kept to a minimum.

Compared to benzodiazepines, melperone lacks the muscle relaxant effect, which leads to a reduction in falls in older people. It is therefore often used in older people.

Melperone is a dopamine antagonist, which means that it inhibits the effect of dopamine. It does this by binding to the D2 receptors and blocking them. The inhibition of dopamine results in a calming, anxiety-relieving effect (sedative effect).

Melperone is metabolized by the liver and has a bioavailability - i.e. the percentage of the active substance available in the blood - of 50-70%. It is excreted in the urine. The half-life, i.e. the time the body needs to excrete half of the active ingredient, is 3-4 hours after ingestion. When injected into the muscle (intramuscularly), the half-life is approx. 6 hours. The maximum plasma concentration (Cmax), i.e. the maximum concentration of the active substance in the blood plasma (liquid cell-free portion of the blood), is reached 1-3 hours after oral administration (swallowed in tablet form).

Always take Melperon exactly as described in the package leaflet or as advised by your doctor.

The usual recommended dose for confusion and restlessness is 25-75 mg per day and can be increased to 200-300 mg per day.

For withdrawal symptoms in alcoholics, it is usually started at 150-400 mg daily and then reduced to 75-150 mg daily.

For psychosis, the dose is started at 50-100 mg per day and increased until the optimum effect is achieved.

In general, the maximum dose is 300 mg per day. Exceptions are withdrawal symptoms in alcoholics.

The duration of treatment should be as short as possible. However, the effect can only occur after two or three weeks.

Melperon should be taken after meals and before going to bed with some liquid.

The following side effects may occur:

Gastrointestinal tract:

• Dry mouth

Nervous system:

• Drowsiness
• Lack of movement
• stiffness
• trembling
• rigidity
• dizziness
• headaches
• Lack of tension in muscles and blood vessels (dystonia)
• Inability to sit still (akathisia)

Liver and gall bladder:

• Elevated liver values
• congestion of bile
• jaundice

Vascular system:

• drop in blood pressure when standing up or sitting down (orthostatic hypotension)
• increased heart rate (tachycardia)

Blood and lymphatic system:

• Impaired formation of red and white blood cells

Other side effects:

• Cardiac arrest
• malignant neuroleptic syndrome
• cardiac arrhythmia
• Stevens-Johnson syndrome
• Sudden death
• Tardive dyskinesia (movement disorder in the face, throat, neck and extremities)
• Increased risk of thrombosis
• Leg vein thrombosis
• pulmonary embolism

An overdose of melperone can lead to severe cardiac arrhythmia.

Interactions may occur if the following medicines are taken at the same time:

Melperon should not be taken with coffee, tea or milk, as the effect may be reduced.

The simultaneous intake of Melperon with alcohol should be avoided at all costs!

Melperon must NOT be taken in the following cases

• in case of allergy to Melperon
• in case of severe liver or kidney dysfunction
• in the case of a pheochromocytoma
• in case of poisoning with substances that impair brain function (e.g. alcohol)
• in cases of circulatory collapse
• in comatose states
• in the case of previous suffering from malignant neuroleptic syndrome
• in disorders of blood formation

Melperon is not approved under the age of 12 and is not recommended under the age of 18.

Pregnancy

During pregnancy, Melperon should only be taken after careful consideration of the risk-benefit profile and under medical supervision.

The Pharmacovigilance and Advisory Center for Embryonal Toxicology at Charité-Universitätsmedizin (www.embryotox.de) recommends this:

In the 1st trimester of pregnancy, there is no evidence of an increased risk of malformation of the unborn child. However, there is very little experience on this.

In the 2nd & 3rd trimester of pregnancy, the data situation is insufficient and it is therefore not advisable to take it.

If taken in the 2nd & 3rd trimester of pregnancy, it is possible thatthe newborn baby may experience adjustment disorders (tremors, weakness, breathing problems, etc.) after birth.

If Melperon is taken during pregnancy, the unborn child should be closely monitored by means of ultrasound examinations. The birth should be carried out in a hospital with a neonatology unit.

Analternative to melperone during pregnancy is promethazine. Diphenhydramine and amitriptyline can be taken for sleep disorders.

Breastfeeding

Melperon should NOT be taken while breastfeeding, as it is not known how much of the active ingredient passes into breast milk. If Melperon is nevertheless taken while breastfeeding, breastfeeding should be discontinued .

The Pharmacovigilance and Advisory Center for Embryonal Toxicology at Charité University Medicine (www.embryotox.de) recommends

Low-dose therapy with good observation of the child is acceptable with reservations. If symptoms of sedation occur in the infant (e.g. restlessness, difficulty drinking, gastrointestinal symptoms, etc.), a pediatrician shouldbe consulted IMMEDIATELY .