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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/03/11 19:17:35」(JST)
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| Systematic (IUPAC) name | |
|---|---|
| N-(4-chlorobenzoylmethyl)-3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-N-methylpropan-1-amine | |
| Clinical data | |
| AHFS/Drugs.com | International Drug Names |
| Pregnancy cat. | ? |
| Legal status | ℞ Prescription only |
| Routes | Oral |
| Pharmacokinetic data | |
| Half-life | 4-6 hours (lofepramine - prodrug); 21-23 hours (desipramine - active metabolite) |
| Identifiers | |
| CAS number | 23047-25-8 N |
| ATC code | N06AA07 |
| PubChem | CID 3947 |
| ChemSpider | 3810 Y |
| UNII | OCA4JT7PAW Y |
| KEGG | D08140 Y |
| ChEBI | CHEBI:47782 Y |
| ChEMBL | CHEMBL87708 Y |
| Chemical data | |
| Formula | C26H27ClN2O |
| Mol. mass | 418.958 g/mol |
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| N (what is this?) (verify) |
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Lofepramine (Gamanil, Tymelyt, Lomont) is a third Generation[1] tricyclic antidepressant which was introduced in 1983 for the treatment of depressive disorders.[2] It is partially converted to its active metabolite desipramine in vivo.[2] However, it is unlikely this property plays a substantial role in its overall effects as lofepramine exhibits lower toxicity and anticholinergic side effects relative to desipramine while retaining equivalent antidepressant efficacy.[2]
Contents
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Indications
In the United Kingdom, lofepramine is licensed for the treatment of depression.
Description: An antidepressant administered orally (as tablets). It has fewer sedative properties than many of the products used to treat depressive illnesses and is suited to patients whose symptoms tend towards withdrawal and apathy, rather than restlessness and agitation.
It is commonly prescribed for major depressive disorder, anxiety, insomnia, neuropathic/chronic pain, and treatment resistant depression.[3]
Side effects
Delusions, headache, nightmares, facial oedema, general feeling of being unwell, bleeding from skin, excitement/anxiety, nausea, inflammation of mucous membranes, loss of taste, parasthesia, skin rash, psychiatric problems such as self-harm, drowsiness, dry mouth, pins and needles, heartbeat irregularities, sweating, low blood pressure, constipation, blurred vision palpatations, dizziness and urinary retention. Can cause confusion in elderly patients or behavioural disturbance in the young. May produce weight gain or cause changes in the levels of blood sugar. Some patients report muscular discomfort, particularly in the shoulders. However, lofepramine is less sedating than, for instance, amitriptyline, and is safer in overdose than older tricyclics.
Warnings
To be used with caution for epileptic patients or those with glaucoma or psychosis. Lofepramine should not be given to people who have suffered liver failure or heart disease. Not advisable for use in pregnant women.
Availability
In the United Kingdom, lofepramine is marketed (as the hydrochloride salt) in the form of 70 mg tablets and 5ml oral suspension as the generic Lomont.[4]
See also
- Tricyclic antidepressant
References
- ^ http://www.safcglobal.com/safc-pharma/en-us/home/small-molecule-api/services-overview/generic-products/lofepramine-hydrochloride.html
- ^ a b c Leonard BE (October 1987). "A comparison of the pharmacological properties of the novel tricyclic antidepressant lofepramine with its major metabolite, desipramine: a review". International Clinical Psychopharmacology 2 (4): 281–97. PMID 2891742.
- ^ Essential Psychopharmacology: The Prescriber's Guide, ISBN 0-521-68350-5, http://books.google.com/books?id=-ppHkXw5zwMC, p.263
- ^ Lomont , SPC from the eMC
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UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
- 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
English Journal
- UV-photodegradation of desipramine: Impact of concentration, pH and temperature on formation of products including their biodegradability and toxicity.
- Khaleel ND1, Mahmoud WM1, Olsson O2, Kümmerer K3.
- The Science of the total environment.Sci Total Environ.2016 Oct 1;566-567:826-40. doi: 10.1016/j.scitotenv.2016.05.095. Epub 2016 May 30.
- Desipramine (DMI) is a widely used tricyclic antidepressant, and it is the major metabolite of imipramine (IMI) and lofepramine (LMI); IMI and LMI are two of the most commonly used tricyclic antidepressants. If DMI enters the aquatic environment, it can be transformed by the environmental bacteria o
- PMID 27254290
- Antidepressant use and risk of cardiovascular outcomes in people aged 20 to 64: cohort study using primary care database.
- Coupland C1, Hill T1, Morriss R2, Moore M3, Arthur A4, Hippisley-Cox J1.
- BMJ (Clinical research ed.).BMJ.2016 Mar 22;352:i1350. doi: 10.1136/bmj.i1350.
- OBJECTIVE: To assess associations between different antidepressant treatments and rates of three cardiovascular outcomes (myocardial infarction, stroke or transient ischaemic attack, and arrhythmia) in people with depression.DESIGN: Cohort study.SETTING: UK general practices contributing to the QRes
- PMID 27005565
- Antidepressant use and risk of epilepsy and seizures in people aged 20 to 64 years: cohort study using a primary care database.
- Hill T1, Coupland C2, Morriss R3, Arthur A4, Moore M5, Hippisley-Cox J6.
- BMC psychiatry.BMC Psychiatry.2015 Dec 17;15:315. doi: 10.1186/s12888-015-0701-9.
- BACKGROUND: Epilepsy is a serious condition which can profoundly affect an individual's life. While there is some evidence to suggest an association between antidepressant use and epilepsy and seizures it is conflicting and not conclusive. Antidepressant prescribing is rising in the UK so it is impo
- PMID 26678837
Japanese Journal
- 難治性めまいとうつ傾向
- Equilibrium research 58(4), 317-322, 1999-08-01
- NAID 10008712867
- Simultaneous determination of lofepramine and desipramine by a high-performance liquid chromatographic method used for therapeutic drug monitoring
- Journal of chromatography. B, Biomedical applications 665(2), 355-361, 1995-03-24
- NAID 10024545523
- うつ状態に対するLofepramine(DB-2182)の使用経験
- 臨牀と研究 54(4), p1282-1286, 1977-04
- NAID 40003783406
Related Links
- Lofepramines like Lomont are an antidepressant. How and when to take Lofepramine (Lomont) including side effects. ... Before taking lofepramine Some medicines are not suitable for people with certain conditions, and sometimes a ...
- Buy Lofepramine (CAS 23047-25-8), a serotonin and noradrenalin re-uptake inhibitor, from Santa Cruz. Molecular Formula: C26H27ClN2O, MW: 418.97 ... アプリケーション： A serotonin and noradrenalin re-uptake inhibitor CAS 番号：
Related Pictures
★リンクテーブル★
| リンク元 | 「ロフェプラミン」 |
| 拡張検索 | 「lofepramine hydrochloride」 |
「ロフェプラミン」
- 三環系抗うつ薬;モノアミン再取り込み阻害