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Clomipramine
drug data and news
Clomipramine 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 | Clomipramine | ||
| Brand Names/Synonyms | Anafranil; Anafranil Base; Chlorimipramine; Clomipramina [Inn-Spanish]; Clomipramine; Clomipramine Hcl; Clomipraminum [Inn-Latin]; Hydiphen; Monochlorimipramine | ||
| Indication | For the treatment of obsessions and compulsions in patients with Obsessive-Compulsive Disorder (OCD), depression, phobic and obsessional states | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Clomipramine 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 | Clomipramine acts by decreasing the reuptake of norepinephrine and serotonin (5-HT). | ||
| Clomipramine News (When available) |
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| Dosage Forms | TABLET | ||
| Drug_Category | Antidepressants; Norepinephrine-Reuptake Inhibitors; Serotonin Uptake Inhibitors; ATC:N06AA04 | ||
| Absorption | Not Available | ||
| Interactions |
Interactions for Clomipramine: The risks of using Anafranil in combination with other drugs have not been systematically evaluated. Given the primary CNS effects of Anafranil, caution is advised in using it concomitantly with other CNS-active drugs. Anafranil should not be used with MAO inhibitors. Close supervision and careful adjustment of dosage are required when Anafranil is administered with anticholinergic or sympathomimetic drugs. Several tricyclic antidepressants have been reported to block the pharmacologic effects of guanethidine, clonidine, or similar agents, and such an effect may be anticipated with CMI because of its structural similarity to other tricyclic antidepressants. The plasma concentration of CMI has been reported to be increased by the concomitant administration of haloperidol; plasma levels of several closely related tricyclic antidepressants have been reported to be increased by the concomitant administration of methylphenidate or hepatic enzyme inhibitors (e.g., cimetidine, fluoxetine) and decreased by the concomitant administration of hepatic enzyme inducers (e.g., barbiturates, phenytoin), and such an effect may be anticipated with CMI as well. Administration of CMI has been reported to increase the plasma levels of phenobarbital, if given concomitantly. 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 aucasian 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 lasma 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 TCAmay 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., fluoxetine, sertraline, paroxetine, and fluvoxamine, inhibit P450 2D6, they may vary in the extent of inhibition. Fluvoxamine has also been shown to inhibit P450 1A2, an isoform also involved in TCAmetabolism. The extent to which SSRI-TCAinteractions 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 TCAtreatment 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 agents in the tricyclic antidepressant class (which includes Anafranil) with drugs that can inhibit cytochrome P450 2D6 may require lower doses than usually prescribed for either the tricyclic antidepressant agent or the other drug. Furthermore, whenever one of these drugs is withdrawn from co-therapy, an increased dose of tricyclic antidepressant agent may be required. It is desirable to monitor TCAplasma levels whenever an agent of the tricyclic antidepressant class including Anafranil is going to be co-administered with another drug known to be an inhibitor of P450 2D6 (and/or P450 1A2). Because Anafranil is highly bound to serum protein, the administration of Anafranil to patients taking other drugs that are highly bound to protein (e.g., warfarin, digoxin) may cause an increase in plasma concentrations of these drugs, potentially resulting in adverse effects. Conversely, adverse effects may result from displacement of protein-bound Anafranil by other highly bound drugs. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | Not Available | ||
| Chemical Formula | C19H23ClN2 | ||
| Molecular Weight | 314.852 g/mol | ||
| Smiles String | CN(C)CCCN1C2=CC=CC=C2CCC3=C1C=C(C=C3)Cl | ||
| Melting Point | 189.5 °C | ||
| Water Solubility | 0.294 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 4.803 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Clomipramine is extensively biotransformed to DMI via CYP2D6 and other metabolites and their glucuronide conjugates | ||
| Half Life | 19-37 hours | ||
| Protein Binding [%] | 97% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Clomipramine.html http://www.rxlist.com/cgi/generic/clomipr.htm http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ana1020.shtml http://www.pharmgkb.org/views/index.jsp?objId= | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00253 | ||
| CAS Registry Number | 303-49-1 | ||
| KEGG Compound ID | C06918 | ||
| PubChem ID | SID:9135 | ||
| PharmGKB ID | PA449048 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2244818 |
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