- a tricyclic antidepressant drug that activates the psychomotor system
|Systematic (IUPAC) name|
|Pregnancy cat.||C (US)|
|Legal status||℞-only (US)|
|Mol. mass||266.381 g/mol|
|Y (what is this?)|
Desipramine (also known as desmethylimipramine) is a tricyclic antidepressant (TCA). It inhibits the reuptake of norepinephrine and to a minor extent serotonin. It is used to treat depression, but not considered a first line treatment since the introduction of SSRI antidepressants. Desipramine is an active metabolite of imipramine. It is sold under the brand names Norpramin and Pertofrane.
Along with other tricyclics, desipramine has found use in treating neuropathic pain. The mechanism of action seems to involve the activation, through norepinephrine reuptake inhibition, of descending pathways in the spinal cord that block pain signals from ascending to the brain. Desipramine is one of the most potent and selective medications in this respect. It may also be used to treat symptoms of Attention Deficit Hyperactivity Disorder, as the underproduction of norepinephrine has been increasingly linked to symptoms associated with Attention Deficit Disorder. It may also be used to treat symptoms of cocaine withdrawal.
- 1 Cardiac arrhythmia
- 2 Genotoxicity
- 3 Overdose
- 4 See also
- 5 References
- 6 External links
On December 2, 2009, the US Food and Drug Administration (FDA) and Sanofi-Aventis are warning healthcare professionals to use caution when prescribing the antidepressant desipramine hydrochloride (Norpramin) in patients with a family history of dysrhythmias or sudden cardiac death.
"The new safety information states that extreme caution should be used when this drug is given to patients who have a family history of sudden death, cardiac dysrhythmias, and cardiac conduction disturbances," according to an alert sent today from MedWatch, the FDA's safety information and adverse event reporting program.
The FDA and the manufacturer also warn that some patients may have seizures before cardiac dysrhythmias and death. Desipramine overdose is more likely to result in death than overdose with other tricyclic antidepressants, notes a company letter sent to healthcare professionals.
The "warnings" and "overdosage" sections of the drug's labeling are being changed to reflect these potential adverse events.
Desipramine has been shown to be genotoxic in fruit flies and associated with an increased risk of breast cancer in women.
As tricyclic antidepressants have a relatively narrow therapeutic index, the likelihood of overdose (both accidental and intentional) is fairly high and should be considered carefully by the prescribing physician prior to patient use. Symptoms of overdose are similar to those of other tricyclic antidepressants, with cardiac toxicity (due to inhibition of sodium and calcium channels) generally occurring before the threshold for serotonin syndrome is reached. Due to this risk, tricyclic antidepressants are rarely selected as the first line treatment for depression. Desipramine overdose should always be considered a medical emergency. In the event of a suspected or known overdose, a poison control center (in the U.S. 1-800-222-1222), or 911 (999 in the UK) should be contacted immediately. The victim should be brought to the nearest hospital when/where phone services are not available.
- Tricyclic antidepressant
- British Journal of Cancer 2002: volume 86, pages 92-97
|This article needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (December 2007)|
- Desipramine - medicinenet.com
- Desipramine - medlineplus.org
- Desipramine - mentalhealth.com
- Desipramine - medscape.com
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- 1. 三環系抗うつ剤および四環系抗うつ剤：薬理学、投与、および副作用 tricyclic and tetracyclic drugs pharmacology administration and side effects
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- Effects of desvenlafaxine on the pharmacokinetics of desipramine in healthy adults.
- Nichols AI, Madelyn A, Chen Y, Behrle JA, Frick G, Paul J.SourceaPfizer Inc., formerly Wyeth Research, Collegeville, Pennsylvania bDepartment of Pharmaceutical Sciences, University at Buffalo, The State University of New York, Buffalo, New York, USA.
- International clinical psychopharmacology.Int Clin Psychopharmacol.2013 Mar;28(2):99-105. doi: 10.1097/YIC.0b013e32835c1f49.
- The results of two single-center, two-period, open-label trials that evaluated the effects of multiple doses of desvenlafaxine on the pharmacokinetics of desipramine, a cytochrome P450 (CYP) 2D6 enzyme substrate, are presented. Healthy individuals aged 18-45 years were administered a single oral dos
- PMID 23221858
- Active behaviours produced by antidepressants and opioids in the mouse tail suspension test.
- Berrocoso E, Ikeda K, Sora I, Uhl GR, Sánchez-Blázquez P, Mico JA.SourceNeuropsychopharmacology Research Group, Psychobiology Area, Department of Psychology, University of Cadiz, Cadiz, Spain.
- The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP).Int J Neuropsychopharmacol.2013 Feb;16(1):151-62. doi: 10.1017/S1461145711001842. Epub 2012 Jan 5.
- Most classical preclinical tests to predict antidepressant activity were initially developed to detect compounds that influenced noradrenergic and/or serotonergic activity, in accordance with the monoaminergic hypothesis of depression. However, central opioid systems are also known to influence the
- PMID 22217458
- Pharmacological Interaction With the Sigma1 (σ1)-Receptor in the Acute Behavioral Effects of Antidepressants
- Villard Vanessa,Meunier Johann,Chevallier Nathalie,Maurice Tangui
- Journal of Pharmacological Sciences 115(3), 279-292, 2011
- … The SSRI fluoxetine and sertraline, but not fluvoxamine, and the tricyclic antidepressants imipramine, desipramine, and amitriptyline were also effective. …
- NAID 130000663391
- A Novel Approach to the Prediction of Drug-Drug Interactions in Humans Based on the Serum Incubation Method
- SHIBATA Yoshihiro,TAKAHASHI Hiroyuki,CHIBA Masato,ISHII Yasuyuki
- Drug metabolism and pharmacokinetics 23(5), 328-339, 2008-10-25
- NAID 10024384558
- Desipramine (also known as desmethylimipramine) is a tricyclic antidepressant ( TCA). It inhibits the reuptake of norepinephrine and to a lesser extent serotonin. It is used to treat depression, but not considered a first line treatment since the ...
- The anticholinergic actions of desipramine are responsible for many of the commonly observed side effects of the drug. Desipramine causes ECG changes such as prolongation of the P-R interval and a decreased magnitude with an increased ...
三環系抗うつ薬 tricyclic antidepressant
- 1. (急性作用)シナプス前膜におけるノルアドレナリン、セロトニンの再取り込み↓→シナプス間隙における薬剤濃度↑
- 2. (慢性作用)(2週間後)シナプス後膜における受容体の数↓
- 非定型抗うつ薬 atypical agent