| Attributes | Values |
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| rdf:type
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| http://linked.open...gbank/description
| - Desipramine hydrochloride is a dibenzazepine-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, desipramine does not affect mood or arousal, but may cause sedation. In depressed individuals, desipramine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Secondary amine TCAs, such as desipramine and nortriptyline, are more potent inhibitors of norepinephrine reuptake than tertiary amine TCAs, such as amitriptyline and doxepine. TCAs also down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine-H<sub>1</sub> receptors, α<sub>1</sub>-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Desipramine exerts less anticholinergic and sedative side effects compared to tertiary amine TCAs, such as amitriptyline and clomipramine. Desipramine may be used to treat depression, neuropathic pain (unlabeled use), agitation and insomnia (unlabeled use) and attention-deficit hyperactivity disorder (unlabeled use). (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...gy/drugbank/group
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| http://linked.open...drugbank/halfLife
| - 7-60+ hours; 70% eliminated renally (en)
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| http://linked.open...ugbank/indication
| - For relief of symptoms in various depressive syndromes, especially endogenous depression. It has also been used to manage chronic peripheral neuropathic pain, as a second line agent for the management of anxiety disorders (e.g. panic disorder, generalized anxiety disorder), and as a second or third line agent in the ADHD management. (en)
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Desipramine is a tricyclic antidepressant (TCA) that selectively blocks reuptake of norepinephrine (noradrenaline) from the neuronal synapse. It also inhibits serotonin reuptake, but to a lesser extent compared to tertiary amine TCAs such as imipramine. Inhibition of neurotransmitter reuptake increases stimulation of the post-synaptic neuron. Chronic use of desipramine also leads to down-regulation of beta-adrenergic receptors in the cerebral cortex and sensitization of serotonergic receptors. An overall increase in serotonergic transmission likely confers desipramine its antidepressant effects. Desipramine also possesses minor anticholinergic activity, through its affinity for muscarinic receptors. TCAs are believed to act by restoring normal levels of neurotransmitters via synaptic reuptake inhibition and by increasing serotonergic neurotransmission via serotonergic receptor sensitization in the central nervous system. (en)
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| http://linked.open...drugbank/packager
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| http://linked.open...outeOfElimination
| - Desipramine is metabolized in the liver, and approximately 70% is excreted in the urine. (en)
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| http://linked.open.../drugbank/synonym
| - Desipramine (en)
- Desipramin (en)
- Desmethylimipramine (en)
- Monodemethylimipramine (en)
- Norimipramine (en)
- 5-(gamma-Methylaminopropyl)iminodibenzyl (en)
- 5-(γ-methylaminopropyl)iminodibenzyl (en)
- DMI (en)
- Desipramina (en)
- Desipraminum (en)
- Déméthylimipramine (en)
- N-(3-methylaminopropyl)iminobibenzyl (en)
- 3-(10,11-DIHYDRO-5H-dibenzo[b,F]azepin-5-yl)-N-methylpropan-1-amine (en)
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| http://linked.open...drugbank/toxicity
| - Male mice: LD50 = 290 mg/kg, female rats: LD50 = 320 mg/kg. Antagonism of the histamine H<sub>1</sub> and α<sub>1</sub> receptors can lead to sedation and hypotension. Antimuscarinic activity confers anticholinergic side effects such as blurred vision, dry mouth, constipation and urine retention may occur. Cardiotoxicity may occur with high doses of desipramine. Cardiovascular side effects in postural hypotension, tachycardia, hypertension, ECG changes and congestive heart failure. Psychotoxic effects include impaired memory and delirium. Induction of hypomanic or manic episodes may occur in patients with a history of bipolar disorder. Withdrawal symptoms include GI disturbances (e.g. nausea, vomiting, abdominal pain, diarrhea), anxiety, insomnia, nervousness, headache and malaise. (en)
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...k/foodInteraction
| - Avoid alcohol. (en)
- Take with food to reduce irritation, limit caffeine intake. (en)
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| http://linked.open...nk/proteinBinding
| - 73-92% bound to plasma proteins (en)
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| http://linked.open...ogy/drugbank/salt
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| http://linked.open...ynthesisReference
| - Biel, J.H.and Judd, C.I.; US. Patent 3,454,554; July 8,1969; assigned to Colgate Palmolive Co. (en)
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
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| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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