Fluvoxamine

Fluvoxamine is an active ingredient for the treatment of depression and obsessive-compulsive disorder. It is an antidepressant from the group of SSRIs, the selective serotonin reuptake inhibitors. However, fluvoxamine can also be used to treat borderline syndrome, anxiety disorders, panic attacks and post-traumatic stress disorder (PTSD). Fluvoxamine is usually found in medicines as fluvoxamine maleate. It is a white, odorless and crystalline (crystal-forming) powder. It is only slightly soluble in water.

Fluvoxamine very specifically (selectively) inhibits the reuptake of serotonin. However, it hardly inhibits the reuptake of noradrenaline and dopamine at all. In depression, it is assumed (based on current knowledge) that there is a lack of monoamines, i.e. chemical molecules that only have one amino group (NH group), in the synaptic cleft, i.e. the transition from one synapse to the next. These monoamines also include noradrenaline and serotonin. Depression is therefore caused by a lack of noradrenaline and serotonin, among other things. Antidepressants are said to increase the amount of monoamines in the synaptic cleft. Fluvoxamine inhibits the serotonin transporter (SERT), which transports the monoamine serotonin out of the synaptic cleft. The inhibition of SERT increases the serotonin concentration.

Due to the high binding strength (affinity) to the gamma receptor - which is a special feature of fluvoxamine - it is often used to treat delusional or anxiety-induced depression.

Fluvoxamine is mainly broken down by the liver. The bioavailability - i.e. the percentage of the active ingredient available in the blood - is 53%. The half-life, i.e. the time the body needs to excrete half of the active ingredient, is approx. 15 hours.

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

The usual recommended dose for adults is 50 mg daily. The dosage can be increased by the doctor in 50 mg increments over a period of days until the desired therapeutic effect is achieved. The maximum dose is 300 mg daily.

Fluvoxamine can increase the risk of suicide in children and young adults up to the age of 24. Therefore, fluvoxamine should only be used under the age of 18 for the treatment of obsessive-compulsive disorder.

The recommended dose in children is 25 mg daily and can also be increased in 25 mg increments over a period of days. The maximum dose for children between 11 and 17 years of age is 300 mg daily. For children aged 8 to 10 years, the maximum dose is 200 mg per day .

If the daily dose is more than 100 mg, the dose should be divided into two doses per day. If the doses cannot be divided equally, the larger amount should be taken before bedtime.

Fluvoxamine can increase the risk of suicide in children and young adults up to the age of 24. Therefore, fluvoxamine should only be used under the age of 18 to treat obsessive-compulsive disorder.

The following side effects may occur:

Frequent:

• States of agitation
• Anxiety
• Constipation or diarrhea
• sleep disturbances
• Dizziness (vertigo)
• dry mouth
• rapid heartbeat (tachycardia)
• listlessness
• malaise
• headaches
• indigestion
• loss of appetite
• nervousness
• Stomach ache
• sweating
• trembling
• Muscle weakness (asthenia)
• vomiting

Occasionally:

• Allergic skin reactions
• Confusion
• Delayed ejaculation
• Dizziness when sitting up or standing up (orthostatic syncope)
• hallucinations
• coordination disorders
• Muscle or joint pain
• Aggression

Rarely:

• Seizures
• Liver problems
• Abnormal mood elevation (mania)
• Sensitivity to light
• Unexpected milk secretion from the mammary gland

Frequency unknown:

• Restlessness (akathisia)
• Inability to have an orgasm (anorgasmia)
• menstrual disorders
• Heavy vaginal bleeding shortly after birth
• Bladder emptying disorders
• Sensory disorders such as tingling or numbness
• Glaucoma
• pupil dilation
• Increased prolactin levels
• changes in weight
• Increased risk of suicide

Side effects, especially in children and adolescents:

• unnaturally increased cheerfulness and activity (hypomania)
• states of agitation
• convulsions
• sleep disorders
• Lack of energy (asthenia)
• Hyperactivity (hyperkinesia)
• Feeling sleepy (drowsiness)
• Digestive disorders

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

• St. John's wort preparations
• Medication for the treatment of depressive disorders:
  • Benzodiazepines
  • Tricyclic antidepressants
  • Neuroleptics or antipsychotics
  • lithium
  • tryptophan
  • Monoamine oxidase inhibitors (MAO inhibitors) such as moclobemide
  • pimozide
  • Selective serotonin reuptake inhibitors (SSRIs) such as citalopram
• Acetylsalicylic acid (aspirin)
• Ciclosporin
• methadone
• mexiletine
• Phenytoin or carbamazepine
• propranolol
• ropinirole
• triptans
• terfenadine
• sildenafil
• theophylline
• Opioid preparations such as buprenorphine and tramadol
• Clopidogrel, warfarin and nicoumalone

Fluvoxamine in combination with caffeine can trigger symptoms similar to those of a caffeine overdose (e.g. tremors, palpitations, etc.).

Fluvoxamine in combination with alcohol can make you very tired and increases the risk of falling.

Fluvoxamine must NOT be taken in the following cases

• if you are allergic to fluvoxamine
• if you are taking monoamine oxidase inhibitors (MAO inhibitors) at the same time
• if you are taking tizanidine or pimozide at the same time

Fluvoxamine should only be used under the age of 18 for the treatment of obsessive compulsive disorder.

Fluvoxamine is NOT approved for use under the age of 8.

Fluvoxamine can lead to a decrease in sperm quality. This can therefore lead to impaired fertility. However, this has so far only been observed in animal experiments.

Pregnancy

During pregnancy, fluvoxamine should only be taken if absolutely necessary. This will be decided by your doctor.

In the first trimester of pregnancy, no clear indications of an increased malformation rate have been shown when taking fluvoxamine or other SSRIs(sertraline, citalopram, paroxetine and fluoxetine). Unfortunately, however, this cannot be ruled out. A few publications have discussed a slightly increased risk of cardiac malformations.

It is worth mentioning the high level of experience not only with fluvoxamine, but also with other SSRIs (> 10,000 case reports).

Fluvoxamine use in the 2nd & 3rd trimester of pregnancy can lead to postpartum adjustment disorders and numerous side effects. These include hyperexcitability, tremors, drinking disorders and shortness of breath. These normally subside after one month after birth at the latest. In a few cases, persistent pulmonary hypertension has been observed in newborns. However, this has not yet been confirmed.

If fluvoxamine was taken during pregnancy, the birth should take place in a neonatal clinic.

Fluvoxamine intake should not be stopped abruptly during pregnancy.

Alternatively, sertraline and citalopram can be taken, but only when treatment is restarted.

Breastfeeding

Fluvoxamine can be taken during breastfeeding . However, the risk-benefit profile should still be weighed up. It is therefore essential that you talk to your doctor. The level of experience is very low.

Fluvoxamine passes into breast milk, but symptoms in breastfed children have not yet been described. Although fluvoxamine is the drug of choice for breastfeeding, it should only be used with great caution. If you notice symptoms in your infant, please consult a pediatrician IMMEDIATELY .

Fluvoxamine has been developed by the pharmaceutical company Solvay since it was tested in clinical trials in 1983 and has been in use ever since. It was tested on around 35,000 patients and introduced in Switzerland in 1984, in the USA in 1994 and in Japan in 1999. In 1995, over 10 million patients had already been successfully treated with fluvoxamine.