Mirtazapine

Chemical Properties

White Solid

Uses

Mirtazapine (Remeron, Avanza) is a potent tetracyclic antidepressant. Mirtazapine (Remeron, Avanza) used primarily in the treatment of depression. It is also sometimes used as a hypnotic, antiemetic, and appetite stimulant, and for the treatment of anxiet

Uses

Mirtazapine is an α2-Adrenergic blocker; analogue of Mianserin. Antidepressant.

Definition

ChEBI: Mirtazapine is a benzazepine and a tetracyclic antidepressant. It has a role as an alpha-adrenergic antagonist, a serotonergic antagonist, a histamine antagonist, an anxiolytic drug, a H1-receptor antagonist and a oneirogen.

brand name

Remeron (Organon).

General Description

Mirtazapine is a tetracyclic antidepressant marketed under the trade names Remeron^?, Avanza, or Zispin for treatment of depression.?This Certified Spiking Solution^? is suitable for LC/MS or GC/MS applications in forensic analysis, clinical toxicology, or urine drug testing.

Biological Activity

Antidepressant agent; potent 5-HT 2 , 5-HT 3 and histamine H 1 receptor antagonist and moderately potent α 2 -adrenoceptor antagonist (pK i values are 8.05, ~ 8.1, 9.3 and 6.95 respectively). Enhances noradrenalin (NA) release in rat brain via inhibition of α 2 -adrenergic autoreceptors and displays only weak affinity for monoamine transporters (pK i values are 5.6, < 5 and < 5.1 for inhibition of NA, dopamine and 5-HT uptake respectively). Increases hippocampal NA and 5-HT levels in rats following systemic administration in vivo .

Biochem/physiol Actions

Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA). Mirtazapine agonizes selective adrenergic and serotonergic receptors so that both NE release and 5-HT1A mediated serotonergic signaling are increased.

Clinical Use

Antidepressant

Veterinary Drugs and Treatments

Currently, the only FDA approved indication for mirtazapine is depression in humans. Reported veterinary uses include treatment of chemotherapy-induced nausea and vomiting (CINV); anorexia associated with renal failure (azotemia), congestive heart failure, gastro-intestinal disorders, liver disease, or neoplasia. Other uses suggested include stress induced diseases; insomnia; post-pyometra symptoms; and post-operative inappetance. Studies have shown that mirtazapine also alleviated sleep apnea in rats and humans.
There are case reports published in human literature of mirtazapine use as treatment for non-mechanical vomiting after gastric bypass, CINV, obsessive-compulsive disorder, nocioception and chronic pain, migraine headache prophylaxis, anti-psychotic induced akathisia, idiopathic nausea and vomiting, serotonin syndrome induced nausea, anorexia, irritable bowel syndrome, resistant hyperemesis gravidarum, and for the treatment of negative symptoms of schizophrenia. Studies in rats have also shown that mirtazapine significantly improves memory.

Drug interactions

Potentially hazardous interactions with other drugs
Alcohol: increased sedative effect.
Antidepressants: possibly increased risk of serotonergic effects with fluoxetine, fluvoxamine or venlafaxine; CNS excitation and hypertension with MAOI and moclobemide - avoid.
Antimalarials: avoid with artemether and lumefantrine and piperaquine with artenimol.
Methylthioninium: risk of CNS toxicity - avoid if possible.

Metabolism

Extensively metabolised in the liver via CYP2D6, CYP1A2, and CYP3A4. The major biotransformation pathways are demethylation and oxidation followed by glucuronide conjugation. The N-desmethyl metabolite is pharmacologically active. Elimination is via urine and faeces (15%).

storage

Store at RT