• Friday May 29,2020

fluvoxamine

Fluvoxamine is an antidepressant belonging to the group of selective serotonin reuptake inhibitors. In Germany, the drug was approved for the treatment of depression and obsessive-compulsive disorder, but is also often used to treat anxiety and panic disorders and in post-traumatic stress disorder. Use of the drug requires interaction with other medicines, such as monoamine oxidase (MAO) inhibitors, and significant side effects may occur.

What is fluvoxamine?

The active ingredient is used for the treatment of depression and obsessive-compulsive disorder.

Fluvoxamine is a drug with the chemical formula C15H21F3N2O2. It contains a monocyclic aromatic ring and has been approved as an antidepressant in Germany since the mid-1980s. The product belongs to the group of selective serotonin reuptake inhibitors (SSRIs). The abbreviation SSRI derives from the term "selective serotonin reuptake inhibitor".

The monocyclic structure and its particular binding ability and affinity for the σ receptors (sigma receptors) distinguish fluvoxamine from most other antidepressants that have a particular binding affinity to opioid receptors.

The drug shows, inter alia, a strong interaction with reversible and irreversible MAO inhibitors (monoamine oxidase inhibitors), which non-selectively inhibit the degradation of neurotransmitters such as serotonin, norepinephrine and dopamine and are also used as antidepressants. Fluvoxamine should therefore not be taken with MAO inhibitors. Before switching from MAO inhibitors to fluvoxamine or vice versa, fixed waiting times must be adhered to.

Pharmacological action

As a selective serotonin reuptake inhibitor, fluvoxamine affects only the reuptake or re-transport of serotonin into the vesicles of certain cells or the degradation of this neurotransmitter, so that its concentration in the synaptic cleft increases.

Due to the selective mode of action of the drug, degradation or repatriation of the other neurotransmitters from the group of monoamines such as adrenaline, dopamine, melatonin and others are not impaired. Fluvoxamine therefore leads to a unilateral increase in the concentration of serotonin in the synaptic cleft due to its prolonged residence time there.

The monoamine serotonin is as neurotransmitters in the central nervous system (CNS) attributed psychological effects. Serotonin is considered as mood-enhancing, motivating and anxiolytic. Depressive moods and depression often show a lack of serotonin. Assuming that the removal of the reduced serotonin concentration also dissipates the depressive mood, an attempt is made to remedy the relative deficiency via the addition of additional serotonin or by the prevention of rapid inactivation of the messenger substance.

Ingestion of fluvoxamine results in increased serotonin levels via the inhibition of rapid inactivation of serotonin. If the serotonin concentration exceeds a certain level, the effect of the messenger substance can almost reverse. It sets in a serotonin syndrome, which is typically characterized by symptoms such as anxiety, inner restlessness, muscle tension, tremors and muscle twitching.

For example, a serotonin syndrome can occur if the interaction of fluvoxamine with MAO inhibitors is ignored and an uncontrollably high serotonin level occurs.

Medical application & use

Ingestion of fluvoxamine, in its capacity as selective serotonin reuptake inhibitor, leads to an increase in serotonin levels in the blood and is therefore considered for the treatment of all mental illnesses associated with a decreased serotonin level. This applies first and foremost to pathological depression.

It is not yet sufficiently known whether manifest depression is the cause or consequence of serotonin deficiency. Fluvoxamine is therefore prescribed primarily for the treatment of depression.

According to original approval in the mid-1980s, the drug is also expressly intended to improve obsessive-compulsive disorder. In the course of other applications, which go well beyond the originally investigated disease spectrum, the drug is also frequently used for the treatment of anxiety disorders, panic attacks, posttraumatic stress disorder and social phobia, as well as irritable bowel syndrome. Even with diagnosed borderline syndrome, which can be classified in the border region between neurosis and overt psychosis, treatment with the SSRI fluvoxamine is quite common.

The empirical knowledge has prevailed that also anxiety disorders, which can develop, for example, to a social phobia, are accompanied by a lowered serotonin level. In order to treat the social phobia itself and thus prevent the development of a number of negative side effects, the use of fluvoxamine is considered by many doctors and also partly preferred.

Often the drug is estimated in addition to its effectiveness also because of its relatively low physiological half-life of about 15 hours. The low half-life allows a rapid switch to an alternative psychotropic drug within a few days with a detected incompatibility of the agent.

Risks & Side Effects

Fluvoxamine, like other inhibitors of selective serotonin inhibitors, is relatively insensitive, one-sided and systemic in the metabolism of monoamines. There is a one-sided increase in serotonin concentration in the nervous system without fully understanding the associated systemic effects on many relevant metabolic processes.

Despite unquestionable treatment successes to improve a range of psychopathological disorders, the use of fluvoxamine is often accompanied by adverse events that occur. Fluvoxamine may cause anxiety, drowsiness, tremors and sleep disturbances. Likewise, there is often an increase in the heart rate as well as sweating and hypersensitivity reactions of the skin.

Particularly in combination with drugs that lead to an increase in serotonin levels in other ways, can set in a serotonin syndrome, a toxic over-supply of serotonin. Serotonin syndrome is typically accompanied by dizziness, muscle rigidity, tremors, and fever, and requires immediate medical attention.

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