Remeron is Mirtazipine. It is a noradrenergic and specific seratonergic antidepressant.
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Mirtazapine has a tetracyclic chemical structure and belongs to the piperazino-azepine group of compounds. It is designated 1,2,3,4,10,14b-hexahydro-2-methylpyrazino [2,1-a] pyrido [2,3-c] benzazepine and has the empirical formula of C17H19N3. Its molecular weight is 265.36.
The mechanism of action is unknown. Mirtazapine acts as an antagonist at central presynaptic a2 adrenergic inhibitory autoreceptors. Mirtazapine is a potent antagonist of 5-HT2 and 5-HT3 receptors. Mirtazapine has no significant affinity for the 5-HT1A and 5-HT1B receptors. Mirtazapine is a potent antagonist of histamine (H1) receptors, a property that may explain its prominent sedative effects. Mirtazapine is a moderate peripheral a1 adrenergic antagonist, a property that may explain the occasional orthostatic hypotension reported in association with its use.
It is rapidly and completely absorbed following oral administration and has a half-life of about 20–40 hours. Peak plasma concentrations are reached within about 2hours following an oral dose. The presence of food in the stomach has a minimal effect on both the rate and extent of absorption and does not require a dosage adjustment.
Mirtazapine is extensively metabolized after oral administration. Major pathways of biotransformation are demethylation and hydroxylation followed by glucuronide conjugation. In vitro data from human liver microsomes indicate that cytochrome 2D6 and 1A2 are involved in the formation of the 8-hydroxy metabolite of mirtazapine, whereas cytochrome 3A is considered to be responsible for the formation of the N-desmethyl and N-oxide metabolite. Mirtazapine has an absolute bioavailability of about 50%. It is eliminated predominantly via urine (75%) with 15% in feces. Several unconjugated metabolites possess pharmacological activity but are present in the plasma at very low levels. The (–) enantiomer hasanelimination half-life that is approximately twice as long as the (+) enantiomer and therefore achieves plasma levels that are about three times as high as that of the (+) enantiomer.
Plasma levels are linearly related to dose over a dose range of 15–80 mg. The mean elimination half-life of mirtazapine after oral administration ranges from approximately 20–40 hours across age and gender subgroups, with females of all ages exhibiting significantly longer elimination half-lives than males (mean half-life of 37 hours for females vs. 26 hours for males). Steady state plasma levels of mirtazapine are attained within 5 days, with about 50% accumulation (accumulation ratio = 1.5).
Mirtazapine is approximately 85% bound to plasma proteins over a concentration range of 0.01 to 10 mg/m.
Females of all ages exhibiting significantly longer elimination half-lives than males.
The most commonly observed adverse events are: Somnolence, increased appetite, weight gain, and dizziness.
Other adverse effects: Flu-Like Symptoms, dry mouth, constipation, peripheral oedema, myalgia, tremor, confusion, shortness of breath and urinary frequency.
Impairment of motor skills with mirtazipine is additive with benzodiazepines and alcohol.