Drug Name

Meloset (Melatonin)

Pharmacological action

A synthetic analog of the pineal body hormone (epiphysis) melatonin.

It has adaptogenic, sedative, hypnotic effect.

Normalizes circadian rhythms. Increases the concentration of GABA and serotonin in the midbrain and hypothalamus, changes the activity of pyridoxal kinase, which is involved in the synthesis of GABA, dopamine and serotonin. GABA is known to be an inhibitory mediator in the CNS, and reduced serotonergic activity may be important in the pathogenesis of depressive states and disorders.

It regulates the sleep-wake cycle, daily changes of locomotor activity and body temperature, has a positive effect on the intellectual and mental functions of the brain, and on the emotional-personal sphere. Contributes to the organization of the biological rhythm and normalization of night sleep. Improves sleep quality, reduces the frequency of attacks of headaches, dizziness, improves mood. Speeds up falling asleep, reduces the frequency of night awakenings, improves feelings after waking up in the morning, does not cause a feeling of lethargy, discomfort and fatigue upon awakening. Makes dreams more vivid and emotionally rich.

Adapts the body to rapid change of time zones, reduces stress reactions, regulates neuroendocrine functions.

It has immunostimulatory and antioxidant properties.

The main physiological effect of melatonin is to inhibit the secretion of gonadotropins. In addition, the secretion of other adenohypophysis hormones - corticotropin, TSH, and STH - is reduced, but to a lesser extent.

Melatonin secretion is subordinated to the circadian rhythm, which, in turn, determines the rhythmicity of gonadotropic effects and sexual function. Melatonin synthesis and secretion are light-dependent - excess light inhibits its formation, while decreased light increases synthesis and secretion of the hormone. In humans, the night hours account for 70% of daily melatonin production.

Pharmacokinetics

After oral administration, it is quickly and completely absorbed from the gastrointestinal tract. It penetrates easily through the histohaematic barriers (including the HEB). T1/2 is short.

Contraindications to use

Hypersensitivity to melatonin; severe renal impairment (CKD <30 ml/min), autoimmune diseases (no clinical data available), liver failure, pregnancy, breastfeeding, age under 18 years (effectiveness and safety not established).

Caution: renal failure (CKR >30 ml/min), old age.

Administration during pregnancy and lactation

It is contraindicated for use during pregnancy and lactation (breast-feeding).

It is not recommended to use for women who want to get pregnant because of some contraceptive effects of melatonin.

Administration in patients with liver dysfunction

It is contraindicated in patients with hepatic insufficiency.

Usage in patients with kidney dysfunction

It is contraindicated in patients with severe renal impairment (CKD < 30 ml/min). Caution should be exercised when using in patients with renal insufficiency (CKD > 30 ml/min).

Administration in children

Administration in children and adolescents under 18 years old is contraindicated (efficacy and safety have not been established).

Administration in elderly patients

Caution should be exercised when using in elderly patients.

Indications for the active ingredient Melatonin

In sleep disorders including those caused by a sleep-wake rhythm disorder, such as desynchronosis (rapid change of time zones).

Dosing regimen

Individual. It is taken orally in dose 1.5-3 mg 1 time per day 30-40 min before sleep.

Maximal daily dose is 6 mg.