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Amoxapine
drug data and news
Amoxapine 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 | Amoxapine | ||
| Brand Names/Synonyms | Amoxapine; Amoxepine; Ascendin; Asendin; Asendis; CL-67.772; Demolox; Moxadil | ||
| Indication | For the relief of symptoms of depression in patients with neurotic or reactive depressive disorders as well as endogenous and psychotic depressions. It is indicated for depression accompanied by anxiety or agitation. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Amoxapine is a tricyclic antidepressant. It was thought that tricylic antidepressants work by inhibiting the re-uptake of the neurotransmitters norepinephrine and serotonin by nerve cells. However, this response occurs immediately, yet mood does not lift for around two weeks. It is now thought that changes occur in receptor sensitivity in the cerebral cortex and hippocampus. The hippocampus is part of the limbic system, a part of the brain involved in emotions. Presynaptic receptors are affected: a1 and b1 receptors are sensitized, a2 receptors are desensitised (leading to increased noradrenaline production). Tricyclics are also known as effective analgesics for different types of pain, especially neuropathic or neuralgic pain. A precise mechanism for their analgesic action is unknown, but it is thought that they modulate anti-pain opioid systems in the CNS via an indirect serotonergic route. They are also effective in migraine prophylaxis, but not in abortion of acute migraine attack. The mechanism of their anti-migraine action is also thought to be serotonergic. | ||
| Mechanism Of Action | Amoxapine acts by decreasing the reuptake of norepinephrine and serotonin (5-HT). | ||
| Amoxapine News (When available) |
Trimipramine for Refractory Panic Attacks Mar 2, 2006 Health Tip: Drugs to Avoid While Breast-Feeding Feb 16, 2006 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Antidepressants; Norepinephrine-Reuptake Inhibitors; ATC:N06AA17 | ||
| Absorption | Not Available | ||
| Interactions | Interactions for Amoxapine: Paralytic ileus may occur in patients taking tricyclic antidepressants in combination with anticholinergic drugs. Amoxapine may enhance the response to alcohol and the effects of barbiturates and other CNS depressants. Serum levels of several tricyclic antidepressants have been reported to be significantly increased when cimetidine is administered concurrently Although such an interaction has not been reported to date with amoxapine, specific interaction studies have not been done, and the possibility should be considered. Drugs Metabolized by P450 2D6 The biochemical activity of the drug metabolizing isozyme cytochrome P450 2D6 (dehrisoquin hydroxylase) is reduced in a subset of the caucasian population (about 7 to 10% of caucasians are so called of reduced P450 2D6 isozyme activity among p.o. metabolizers); reliable estimates of the prevalence Asian, African and other populatlons are not yet available when given usual doses. Poor metabolizers have higher than expected plasma concentrations tricyclic antidepressants (TCAs) when given usual doses. Depending on the fraction of drug metabolized by P450 2D6, the increase in plasma concentration may be small, or quite large (8 fold increase in plasma AUC of the TCA). In addition certain drugs inhibit the activity of this isozyme and make normal metabolizers resemble p.o. metabolizers. An individual who is stable on a given dose of TCA may become abruptly toxic when given one of these inhibiting drugs as concomitant therapy. The drugs that inhibit cytochrome P450 2D6 include some that are not metabolized by the enzymes quinidine, cimetidine, and many that are substrates for P450 2D6 (many other antidepressants, phenothiazines, and the Type 1C antiarrhythmics propafenone and flecainide). While all the selective serotonin reuptake inhibitors (SSRls), e.g. fluoxetine, sertraline, and paroxetine inhibit P450 2D6, they may vary in the extent of inhibition. The extent to which SSRI-TCA interactions may pose clinical problems will depend on the degree of inhibition and the pharmacokmetics of the SSRI involved. Nevertheless, caution is indicated in the co-administration of TCA's with any of the SSRI's and also in switching from one class to the other of particular importance. Sufficient time must elapse before initiating TCA treatment in a patient being withdrawn from fluoxetine given. The long half-life of the parent and active metabolite (at least 5 weeks may be necessary). Concomitant use of tricyclic antidepressants with drugs that can inhibit cytochrome P450 2D6 may require lower doses than usually prescribed for either the tricyclic antidepressant or the other drug. Furthermore, whenever one of these other drugs is withdrawn from co-therapy, an increased dose of tricyclic antidepressant may be required. It is desirable to monitor TCA plasma levels whenever a TCA is going to be co-administered with another drug known to be an inhibitor of P450 2D6. Therapeutic Interactions Concurrent administration with electroshock therapy may increase the hazards associated with such therapy. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | Not Available | ||
| Chemical Formula | C17H16ClN3O | ||
| Molecular Weight | 313.781 g/mol | ||
| Smiles String | C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl | ||
| Melting Point | 175.5 °C | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | 3.38 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Not Available | ||
| Half Life | 8 hours | ||
| Protein Binding [%] | >90% binding-plasma protein | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Amoxapine.html http://www.rxlist.com/cgi/generic/amoxapine.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00142 | ||
| CAS Registry Number | 14028-44-5 | ||
| KEGG Compound ID | C06826 | ||
| PubChem ID | 9044 | ||
| PharmGKB ID | PA448405 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 527106 |
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