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Mirtazapine
drug data and news
Mirtazapine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Mirtazapine | ||
| Brand Names/Synonyms | CHEMBANK1791; Mepirzepine; Mirtazapina [Inn-Spanish]; Mirtazapine; Mirtazapine [Usan:Ban:Inn]; Mirtazapinum [Inn-Latin]; Mirtazepine; ORG 3770; Olsalazine; Org-3770; Remeron; Remeron Soltab; Soltabt | ||
| Indication | For the treatment of major depressive disorder | ||
| Sponsored links | Description | Not Available | |
| 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 receptors and contributing to the anxiolytic effects of mirtazapine. Mirtazapine also acts as a weak antagonist at 5-HT1 receptors and as a potent antagonist at 5-HT2 (particularly subtypes 2A and 2C) and 5-HT3 receptors. Blockade of these receptors may explain the lower incidence of adverse effects such as anxiety, insomnia, and nausea. Mirtazapine also exhibits significant antagonism at H1-receptors, resulting in sedation. Mirtazapine has no effects on the reuptake of either NE or 5-HT and has only minimal activity at dopaminergic and muscarinic receptors. | ||
| Mirtazapine News (When available) |
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| Dosage Forms | TABLET; TABLET (ORALLY DISINTEGRATING) | ||
| Drug_Category | Adrenergic alpha-Antagonists; Antidepressive Agents, Tricyclic; Histamine H1 Antagonists; ATC:N06AX11 | ||
| Absorption | Rapid and complete, but, due to first-pass metabolism, absolute bioavailability is 50%. | ||
| Interactions |
-->Interactions for Mirtazapine: As with other drugs, the potential for interaction by a variety of mechanisms (e.g., pharmacodynamic, pharmacokinetic inhibition or enhancement, etc.) is a possibility. Drugs Affecting Hepatic Metabolism The metabolism and pharmacokinetics of REMERONSolTabÒ (mirtazapine) Orally Disintegrating Tablets may be affected by the induction or inhibition of drug-metab-olizing enzymes. Drugs that are Metabolized by and/or Inhibit Cytochrome P450 Enzymes Many drugs are metabolized by and/or inhibit various cytochrome P450 enzymes, e.g., 2D6, 1A2, 3A4, etc. In vitro studies have shown that mirtazapine is a substrate for several of these enzymes, including 2D6, 1A2, and 3A4. While in vitro studies have shown that mirtazapine is not a potent inhibitor of any of these enzymes, an indication that mirtazapine is not likely to have a clinically significant inhibitory effect on the metabolism of other drugs that are substrates for these cytochrome P450 enzymes, the concomitant use of REMERONSolTabÒ with most other drugs metabolized by these enzymes has not been formally studied. Consequently, it is not possible to make any definitive statements about the risks of coadministration of REMERONSolTab® with such drugs. Alcohol Concomitant administration of alcohol (equivalent to 60 g) had a minimal effect on plasma levels of mirtazapine (15 mg) in 6 healthy male subjects. However, the impairment of cognitive and motor skills produced by REMERONÒ were shown to be additive with those produced by alcohol. Accordingly, patients should be advised to avoid alcohol while taking REMERONSolTabÒ . Diazepam Concomitant administration of diazepam (15 mg) had a minimal effect on plasma levels of mirtazapine (15 mg) in 12 healthy subjects. However, the impairment of motor skills produced by REMERONÒ has been shown to be additive with those caused by diazepam. Accordingly, patients should be advised to avoid diazepam and other similar drugs while taking REMERONSolTabÒ . | ||
| Toxicity | disorientation, drowsiness, impaired memory, and tachycardia. LD50=mg/kg(orally in rat) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1,2,3,4,10,14b-hexahydro-2-methylpyrazino[2,1-a]pyrido[2,3-c][2]benzazepine | ||
| Chemical Formula | C17H19N3 | ||
| Molecular Weight | 265.353 g/mol | ||
| Smiles String | CN1CCN2C(C1)C3=CC=CC=C3CC4=C2N=CC=C4 | ||
| Melting Point | 114-116°C | ||
| Water Solubility | Not Available | ||
| State | Solid (white to creamy white crystalline powder) | ||
| LogP/Hphobicity | 2.369 | ||
| Isoelectric Point | Not Available | ||
| 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 3A is responsible for the formation of the N-desmethyl and N-oxide metabolites. Several metabolites possess pharmacological activity, but plasma levels are very low. | ||
| Half Life | 20-40 hours | ||
| Protein Binding [%] | 85% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Mirtazapine.html http://www.rxlist.com/cgi/generic/mirtaz.htm http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/rem1371.shtml | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00685 | ||
| CAS Registry Number | 61337-67-5 | ||
| KEGG Compound ID | C07570 | ||
| PubChem ID | SID:183976 | ||
| PharmGKB ID | PA450522 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2256126 |
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