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Doxepin
drug data and news
Doxepin 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 | Doxepin | ||
| Brand Names/Synonyms | Adapin; Aponal; Curatin; Doxepin; Doxepin Hcl; Doxepin [Usan]; Doxepin, Hydrochloride; Doxepina [Inn-Spanish]; Doxepine; Doxepinum [Inn-Latin]; Novo-Doxepin; P-3693A; Quitaxon; Sinequan; Triadapin; Zonalon | ||
| Indication | For the treatment of psychoneurotic patients with depression and/or anxiety | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Doxepin, a tricyclic antidepressant of the dibenzoxepin type, is used to treat depression and anxiety and, topically, pruritus associated with eczema. Doxepin has substantial anticholinergic and sedative effects. | ||
| Mechanism Of Action | The mechanism of action of doxepin is not completely understood. It is thought that Like amitriptyline, doxepin enhances the actions of norepinephrine and serotonin by blocking their reuptake at the neuronal membrane. Doxepin may also act on histamine H1-receptors, resulting in sedative effects, and beta-adrenergic receptors. | ||
| Doxepin News (When available) |
Somaxon, Patheon enter manufacturing deal Feb 7, 2006 Health Tip: Drugs to Avoid While Breast-Feeding Feb 16, 2006 Piribo: Drug Companies Wake up to Insomniacs; Market for Sleeping ... Feb 13, 2006 Somaxon Pharmaceuticals, Inc. to Present at the 18th Annual Roth ... Feb 15, 2006 The American Journal of Psychiatry Publishes Data on Clinical ... Feb 3, 2006 Somaxon, Patheon enter manufacturing deal Feb 7, 2006 The American Journal of Psychiatry Publishes Data on Clinical ... Feb 3, 2006 Continuity of Antidepressant Treatment for Adults With Depression ... Jan 24, 2006 Brief Reports: Patterns of Psychotropic Medication Use by Race ... Jan 25, 2006 Your Health … Can’t seem to get your zzz’s? Stop suffering ... Jan 9, 2006 FAMILY DOCTOR: No cure yet for interstitial cystitis Dec 8, 2005 Drugs in Developement Nov 15, 2005 Oil of wintergreen time-honored rub for aches Nov 22, 2005 Evaluation of Reboxetine, a Noradrenergic Antidepressant, for the ... Sep 23, 2005 IPO REPORT: Innovene IPO Scrapped By BP In Favor Of $9B Sale Oct 7, 2005 Somaxon Pharmaceuticals, Inc. Files for Initial Public Offering Oct 7, 2005 Somaxon Pharmaceuticals, Inc. Initiates Second Phase III Clinical ... Sep 20, 2005 Firm settles suit over jail death Sep 25, 2005 Inmate's family gets settlement after death Sep 25, 2005 Many meds don't mix with the sun Sep 21, 2005 Evaluation of Reboxetine, a Noradrenergic Antidepressant, for the ... Sep 6, 2005 Somaxon Makes Big Entry Into Competitive Arena Aug 16, 2005 Treating Alcohol and Drug Abuse: An Evidence Based Review Jul 29, 2005 Acute Akathisia Associated With Quetiapine Use Jul 6, 2005 Alleviating the Itch-Scratch Cycle in Atopic Dermatitis Jul 6, 2005 Acute Akathisia Associated With Quetiapine Use Jul 6, 2005 Alleviating the Itch-Scratch Cycle in Atopic Dermatitis Jul 6, 2005 Need Shuteye? More Help Is on the Way Jun 29, 2005 Dysbetalipoproteinemia and Clomipramine Jun 30, 2005 Common skin conditions and treatments Jun 16, 2005 | ||
| Dosage Forms | Capsules | ||
| Drug_Category | Anti-anxiety Agents; Antipruritics; Antidepressants; Norepinephrine-Reuptake Inhibitors; Histamine Antagonists; ATC:N06AA12 | ||
| Absorption | well absorbed from the gut | ||
| Interactions |
-->Interactions for Doxepin: Drugs Metabolized by P450 2D6: The biochemical activity of the drug metabolizing isozyme cytochrome P450 2D6 (debrisoquin hydroxylase) is reduced in a subset of the Caucasian population (about 7-10% of Caucasians are so-called "poor metabolizers"); reliable estimates of the prevalence of reduced P450 2D6 isozyme activity among Asian, African and other populations are not yet available. Poor metabolizers have higher than expected plasma concentrations of 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 poor 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 enzyme (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 (SSRIs), e.g., citalopram, escitalopram, 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 pharmacokinetics of the SSRI involved. Nevertheless, caution is indicated in the co-administration of TCAs with any of the SSRIs 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. Doxepin is primarily metabolized by CYP2D6 (with CYP1A2 & CYP3A4 as minor pathways). Inhibitors or substrates of CYP2D6 (i.e., quinidine, selective serotonin reuptake inhibitors [SSRIs]) may increase the plasma concentration of doxepin when administered concomitantly. The extent of interaction depends on the variability of effect on CYP2D6. The clinical significance of this interaction with doxepin has not been systematically evaluated. MAO Inhibitors: Serious side effects and even death have been reported following the concomitant use of certain drugs with MAO inhibitors. Therefore, MAO inhibitors should be discontinued at least two weeks prior to the cautious initiation of therapy with SINEQUAN. The exact length of time may vary and is dependent upon the particular MAO inhibitor being used, the length of time it has been administered, and the dosage involved. Cimetidine: Cimetidine has been reported to produce clinically significant fluctuations in steady-state serum concentrations of various tricyclic antidepressants. Serious anticholinergic symptoms (i.e., severe dry mouth, urinary retention and blurred vision) have been associated with elevations in the serum levels of tricyclic antidepressant when cimetidine therapy is initiated. Additionally, higher than expected tricyclic antidepressant levels have been observed when they are begun in patients already taking cimetidine. In patients who have been reported to be well controlled on tricyclic antidepressants receiving concurrent cimetidine therapy, discontinuation of cimetidine has been reported to decrease established steady-state serum tricyclic antidepressant levels and compromise their therapeutic effects. Alcohol: It should be borne in mind that alcohol ingestion may increase the danger inherent in any intentional or unintentional SINEQUAN overdosage. This is especially important in patients who may use alcohol excessively. Tolazamide: A case of severe hypoglycemia has been reported in a type II diabetic patient maintained on tolazamide (1 gm/day) 11 days after the addition of doxepin (75 mg/day). | ||
| Toxicity | LD50=26 (mg/kg) (in mice, iv); LD50=16 (mg/kg) (in rats, iv); cardiac dysrhythmias, severe hypotension, convulsions, and CNS depression, including coma. Changes in the electrocardiogram, particularly in QRS axis or width, are clinically significant indicators of tricyclic antidepressant toxicity. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | Not Available | ||
| Chemical Formula | C19H21NO | ||
| Molecular Weight | 279.376 g/mol | ||
| Smiles String | CN(C)CCC=C1C2=CC=CC=C2COC3=CC=CC=C31 | ||
| Melting Point | 184-186 °C | ||
| Water Solubility | 4.9 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 4.189 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 6 - 8 hours | ||
| Protein Binding [%] | highly protein-bound | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Doxepin.html http://www.rxlist.com/cgi/generic/doxepin.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00398 | ||
| CAS Registry Number | 1668-19-5 | ||
| KEGG Compound ID | C06971 | ||
| PubChem ID | SID:158785 | ||
| PharmGKB ID | PA449409 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 1913425 |
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