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QuickView for Mirtazapine (compound)

Name: mirtazapine
PubChem Compound ID: 3085218
Molecular formula: C17H19N3
Molecular weight: 265.353 g/mol
Tocris-2018; 61337-87-9; NCGC00025346-01; (S)-1,2,3,4,10,14b-Hexahydro-2-methylpyrazino(2,1-a)pyrido(2,3-c)(2)benzazepine; EINECS 262-714-0
Name: mirtazapine
Name (isomeric): DB00370
Drug Type: small molecule
Mirtazapinum [INN-Latin]; Mepirzepine; Mirtazepine; Mirtazapina [INN-Spanish]; Mirtazapine [Usan:Ban:Inn]
Brand: Axit, Mirtabene, Remergon, Mirtazon, Promyrtil, Norset, Rexer, Remergil, Mirtaz, Remeron Soltab, Zispin, Remeron, Avanza
Category: Histamine H1 Antagonists, Adrenergic alpha-Antagonists, Antidepressive Agents, Tricyclic
CAS number: 61337-67-5
Indication: For the treatment of major depressive disorder.
Pharmacology: Mirtazapine, an antidepressant of the piperazinoazepine class, is a tetracyclic compound with an anxiolytic effect. Mirtazapine has fewer ADRs than tricyclic antidepressants and is better tolerated. Selective blockade of specific serotonin receptors by mirtazapine likey minimizes side effects typical of other antidepressants.
Mechanism of Action:
Mirtazapine acts as an antagonist at central pre-synaptic alpha(2)-receptors, inhibiting negative feedback to the presynaptic nerve and causing an increase in NE release. Blockade of heteroreceptors, alpha(2)-receptors contained in serotenergic neurons, enhances the release of 5-HT, increasing the interactions between 5-HT and 5-HT1 rece...
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Absorption: Rapid and complete, but, due to first-pass metabolism, absolute bioavailability is 50%.
Protein binding: 85%
Biotransformation: Mirtazapine is extensively metabolized by demethylation and hydroxylation followed by glucuronide conjugation. Cytochrome P450 2D6 and cytochrome P450 1A2 are involved in formation of the 8-hydroxy metabolite of mirtazapine, and cytochrome P450 3A4 is responsible for the formation of the N-desmethyl and N-oxide metabolites. Several metabolites possess pharmacological activity, but plasma levels are very low.
Route of elimination: This drug is known to be substantially excreted by the kidney (75%).
Half Life: 20-40 hours
Toxicity: Symptoms of overdose include disorientation, drowsiness, impaired memory, and tachycardia. LD50 is 600-720mg/kg (oral, mice) and 320-490mg/kg (oral, rat) [PMID: 10333982]
Affected organisms: Humans and other mammals
Food interaction:
Take without regard to meals. Avoid alcohol.
Drug interaction:
ClonidinePossible hypertensive crisis
PhenelzinePossible severe adverse reaction with this combination
TramadolIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
FluvoxamineFluvoxamine may increase the therapeutic and adverse effects of mirtazapine.
ZolmitriptanUse of two serotonin modulators, such as zolmitriptan and mirtazapine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
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