WordNet

a complex consisting of an organic base in association with hydrogen chloride
a tricyclic antidepressant drug that activates the psychomotor system

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/07/20 10:49:21」(JST)

wiki en

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.^[2]

Medical uses

It is primarily used for the treatment of depression.^[2] It may also be useful to treat symptoms of attention deficit hyperactivity disorder.^[3] Evidence of benefit is only in the short term and with concerns of side effects its overall usefulness is not clear.^[4] Desipramine at very low doses is also used to help reduce the pain associated with functional dyspepsia.^[5]

It has also been tried, albeit with little evidence of efficacy, in the treatment of cocaine dependence.^[6] Evidence for usefulness in neuropathic pain is also poor.^[7]

Adverse effects

Desipramine tends to be less sedating than other TCAs and tends to produce fewer anticholinergic effects like dry mouth, urinary retention, blurred vision, memory impairment and constipation.^[8]

Genotoxicity

Desipramine has been shown to be genotoxic in fruit flies;^[9] and it is associated with an increased risk of breast cancer in women.^{[medical citation needed]}

Overdose

Desipramine is particularly toxic in cases of overdose, compared to other antidepressants.^[10] Any overdose or suspected overdose of desipramine is considered to be a medical emergency and can result in death without prompt medical intervention.

References

^ ^a ^b ^c Sallee, FR; Pollock, BG (May 1990). "Clinical pharmacokinetics of imipramine and desipramine.". Clinical Pharmacokinetics 18 (5): 346–64. doi:10.2165/00003088-199018050-00002. PMID 2185906.
^ ^a ^b Brunton, L; Chabner, B; Knollman, B (2010). Goodman and Gilman's The Pharmacological Basis of Therapeutics (12th ed.). New York: McGraw-Hill Professional. ISBN 978-0-07-162442-8.
^ Ghanizadeh, A (July 2013). "A systematic review of the efficacy and safety of desipramine for treating ADHD.". Current Drug Safety 8 (3): 169–74. doi:10.2174/15748863113089990029. PMID 23914752.
^ Otasowie, J; Castells, X; Ehimare, UP; Smith, CH (Sep 19, 2014). "Tricyclic antidepressants for attention deficit hyperactivity disorder (ADHD) in children and adolescents.". The Cochrane database of systematic reviews 9: CD006997. doi:10.1002/14651858.CD006997.pub2. PMID 25238582.
^ http://www.uptodate.com/contents/upset-stomach-functional-dyspepsia-in-adults-beyond-the-basics
^ Pani, PP; Trogu, E; Vecchi, S; Amato, L (December 2011). "Antidepressants for cocaine dependence and problematic cocaine use.". The Cochrane Database of Systematic Reviews (12): CD002950. doi:10.1002/14651858.CD002950.pub3. PMID 22161371.
^ Hearn, L; Moore, RA; Derry, S; Wiffen, PJ; Phillips, T (Sep 23, 2014). "Desipramine for neuropathic pain in adults.". The Cochrane database of systematic reviews 9: CD011003. doi:10.1002/14651858.CD011003.pub2. PMID 25246131.
^ "Desipramine Hydrochloride" Check |url= value (help). Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. 13 December 2013. Retrieved 17 July 2014.
^ van Schaik, N; Graf, U (May 1991). "Genotoxicity evaluation of five tricyclic antidepressants in the wing somatic mutation and recombination test in Drosophila melanogaster.". Mutation Research 260 (1): 99–104. doi:10.1016/0165-1218(91)90085-Z. PMID 1902910.
^ White, N; Litovitz, T; Clancy, C (December 2008). "Suicidal antidepressant overdoses: a comparative analysis by antidepressant type.". Journal of Medical Toxicology 4 (4): 238–50. doi:10.1007/BF03161207. PMC 3550116. PMID 19031375.

External links

Desipramine - medlineplus.org

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. Pharmacotherapy for stimulant use disorder in adults
2. 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
3. 成人における過敏性腸症候群の治療 treatment of irritable bowel syndrome in adults
4. 小児および思春期における注意欠陥多動性障害治療薬の薬理学 pharmacology of drugs used to treat attention deficit hyperactivity disorder in children and adolescents
5. 癌疼痛のマネージメント：鎮痛補助剤（鎮痛剤） cancer pain management adjuvant analgesics coanalgesics

English Journal

Effects of proarrhythmic drugs on relaxation time and beating pattern in rat engineered heart tissue.

Eder A1, Hansen A, Uebeler J, Schulze T, Neuber C, Schaaf S, Yuan L, Christ T, Vos MA, Eschenhagen T.
Basic research in cardiology.Basic Res Cardiol.2014 Nov;109(6):436. doi: 10.1007/s00395-014-0436-7. Epub 2014 Sep 11.
The assessment of proarrhythmic risks of drugs remains challenging. To evaluate the suitability of rat engineered heart tissue (EHT) for detecting proarrhythmic effects. We monitored drug effects on spontaneous contractile activity and, in selected cases, on action potentials (sharp microelectrode)
PMID 25209140

Pharmacological evidence that 5-HT1A/1B/1D, α2-adrenoceptors and D2-like receptors mediate ergotamine-induced inhibition of the vasopressor sympathetic outflow in pithed rats.

Villamil-Hernández MT1, Alcántara-Vázquez O1, Sánchez-López A1, Gutiérrez-Lara EJ1, Centurión D2.
European journal of pharmacology.Eur J Pharmacol.2014 Oct 5;740:512-21. doi: 10.1016/j.ejphar.2014.06.036. Epub 2014 Jun 27.
The sympathetic nervous system that innervates the peripheral circulation is regulated by several mechanisms/receptors. It has been reported that prejunctional 5-HT1A, 5-HT1B, 5-HT1D, D2-like receptors and α2-adrenoceptors mediate the inhibition of the vasopressor sympathetic outflow in pithed rats
PMID 24975101

Enduring deficits in brain reward function after chronic social defeat in rats: susceptibility, resilience, and antidepressant response.

Der-Avakian A1, Mazei-Robison MS2, Kesby JP1, Nestler EJ3, Markou A4.
Biological psychiatry.Biol Psychiatry.2014 Oct 1;76(7):542-9. doi: 10.1016/j.biopsych.2014.01.013. Epub 2014 Jan 31.
BACKGROUND: Anhedonia, or diminished interest or pleasure in rewarding activities, characterizes depression and reflects deficits in brain reward circuitries. Social stress induces anhedonia and increases risk of depression, although the effect of social stress on brain reward function is incomplete
PMID 24576687

Japanese Journal

The Effects of T-588, a Novel Cognitive Enhancer, on Noradrenaline Uptake and Release in Rat Cerebral Cortical Slices

MAEKAWA Mutsuko,MURAYAMA Toshihiko,ONO Satoshi,NARITA Hirokazu,NOMURA Yasuyuki
The Japanese journal of pharmacology 77(2), 155-160, 1998-06-01
… Previously, we reported that (R)-(-)-1-(benzo[b]thiophen-5-yl)-2-[2-(N, N-diethylamino)-ethoxy]ethanol hydrochloride (T-588), a novel cognitive enhancer, stimulated noradrenaline (NA) release from rat cerebral cortical slices. … In this study, we investigated the effects of T-588 on NA uptake and release, compared to the effects of desipramine, a blocker of the NA carrier on the plasma membrane. … Both T-588 and desipramine caused dose-dependent inhibition of [3H]NA uptake into the slices. …
NAID 10008193015

Profiles of the Antinociceptive Effect of R - 84760, a Selective κ - Opioid Receptor Agonist, in the Formalin Test in Mice

FUJIBAYASHI Kenji,IIZUKA Yoshio
The Japanese journal of pharmacology 68(1), 57-63, 1995-05-01
… The antinociceptive effect of a selective κ-opioid receptor agonist R-84760, (3<I>R</I>)-3-(1-pyrrolidinylmethyl)-4-[(1<I>S</I>)-5, 6-dichloro-1-indancarbonyl]-tetrahydro-1, 4-thiazine hydrochloride, in the second phase of the formalin test, a model of tonic pain, was examined in mice. … Intrathecally administered phentolamine, an α-adrenoceptor antagonist, attenuated and desipramine, a noradrenaline reuptake inhibitor, augmented the antinociceptive effect of R-84760. …
NAID 10005710564

Related Pictures

★リンクテーブル★

リンク元	「デシプラミン」「norpramin」「pertofrane」
関連記事	「hydrochloride」

「デシプラミン」

Desipramine
Systematic (IUPAC) name
	3-(10,11-Dihydro-5H-dibenzo[b,f]azepin-5-yl)-N-methylpropan-1-amine
Clinical data
Trade names	Norpramin
AHFS/Drugs.com	Monograph
MedlinePlus	a682387
Pregnancy; category	US: C (Risk not ruled out); ;
Routes of; administration	Oral
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Bioavailability	73-92%
Metabolism	Hepatic (CYP2D6)
Biological half-life	21-125 hours
Excretion	Urine (70%)
Identifiers
CAS Number	50-47-5
ATC code	N06AA01 (WHO)
PubChem	CID 2995
IUPHAR/BPS	2399
DrugBank	DB01151
ChemSpider	2888
UNII	TG537D343B
KEGG	D07791
ChEBI	CHEBI:47781
ChEMBL	CHEMBL72
Chemical data
Formula	C18H22N2
Molar mass	266.381 g/mol
	SMILES c1cc3c(cc1)CCc2c(cccc2)N3CCCNC ;
	InChI InChI=1S/C18H22N2/c1-19-13-6-14-20-17-9-4-2-7-15(17)11-12-16-8-3-5-10-18(16)20/h2-5,7-10,19H,6,11-14H2,1H3 ; Key:HCYAFALTSJYZDH-UHFFFAOYSA-N ;
(verify)

　　[★]

英: desipramine
化: 塩酸デシプラミン desipramine hydrochloride
同: デスメチルイミプラミン desmethylimipramine
商: Norpramin, Pertofrane
関: 抗うつ薬

「norpramin」

　　[★]

同: desipramine hydrochloride

「pertofrane」

　　[★]

同: desipramine hydrochloride

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[clinp-1] Sallee, FR; Pollock, BG (May 1990). "Clinical pharmacokinetics of imipramine and desipramine.". Clinical Pharmacokinetics 18 (5): 346–64. doi:10.2165/00003088-199018050-00002. PMID 2185906.

[GG-2] Brunton, L; Chabner, B; Knollman, B (2010). Goodman and Gilman's The Pharmacological Basis of Therapeutics (12th ed.). New York: McGraw-Hill Professional. ISBN 978-0-07-162442-8.

[3] Ghanizadeh, A (July 2013). "A systematic review of the efficacy and safety of desipramine for treating ADHD.". Current Drug Safety 8 (3): 169–74. doi:10.2174/15748863113089990029. PMID 23914752.

[4] Otasowie, J; Castells, X; Ehimare, UP; Smith, CH (Sep 19, 2014). "Tricyclic antidepressants for attention deficit hyperactivity disorder (ADHD) in children and adolescents.". The Cochrane database of systematic reviews 9: CD006997. doi:10.1002/14651858.CD006997.pub2. PMID 25238582.

[5] ttp://www.uptodate.com/contents/upset-stomach-functional-dyspepsia-in-adults-beyond-the-basics

[6] Pani, PP; Trogu, E; Vecchi, S; Amato, L (December 2011). "Antidepressants for cocaine dependence and problematic cocaine use.". The Cochrane Database of Systematic Reviews (12): CD002950. doi:10.1002/14651858.CD002950.pub3. PMID 22161371.

[7] Hearn, L; Moore, RA; Derry, S; Wiffen, PJ; Phillips, T (Sep 23, 2014). "Desipramine for neuropathic pain in adults.". The Cochrane database of systematic reviews 9: CD011003. doi:10.1002/14651858.CD011003.pub2. PMID 25246131.

[MD-8] "Desipramine Hydrochloride" Check |url= value (help). Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. 13 December 2013. Retrieved 17 July 2014.

[9] van Schaik, N; Graf, U (May 1991). "Genotoxicity evaluation of five tricyclic antidepressants in the wing somatic mutation and recombination test in Drosophila melanogaster.". Mutation Research 260 (1): 99–104. doi:10.1016/0165-1218(91)90085-Z. PMID 1902910.

[10] White, N; Litovitz, T; Clancy, C (December 2008). "Suicidal antidepressant overdoses: a comparative analysis by antidepressant type.". Journal of Medical Toxicology 4 (4): 238–50. doi:10.1007/BF03161207. PMC 3550116. PMID 19031375.

v t e Sigma receptor modulators

Agonists	3-MeO-PCE 3-MeO-PCP 3-PPP 4-MeO-PCP 4-IBP 4-PPBP Afobazole Alazocine Amantadine Amitriptyline Arketamine BD-1008 BD1031 BD1052 Berberine Buprenorphine Captodiame Citalopram Clorgiline Cocaine Cutamesine Cyclazocine DHEA DHEA-S Desipramine Dextrallorphan Dextromethorphan Dextrorphan Dimemorfan DMT Donepezil DTG Escitalopram Fluoxetine Fluvoxamine Heroin Ibogaine Igmesine Imipramine JO-1784 Ketamine L-687,384 Lamotrigine Lu 28-179 MDMA Memantine Metaphit Methamphetamine Methoxetamine Methylphenidate Morphine Naluzotan Noscapine OPC-14523 Opipramol PB-28 PD-144,415 Pentazocine Pentoxyverine Phencyclidine PRE-084 Pregnenolone Pregnenolone sulfate Quetiapine RTI-55 SA-4503 Siramesine Tapentadol Tenocyclidine Tramadol UMB23 UMB82 Venlafaxine

Antagonists	AC927 AHD1 AZ66 BD1008 BD1047 BD1060 BD1063 BD1067 BMY-14802 CM156 E-5842 Haloperidol Lamotrigine LR132 LR172 MIN-101 MS-377 Naloxone Naltrexone NE-100 Panamesine PD-144418 Progesterone Quingestrone Rimcazole S1RA (E-52862) Sertraline SM-21 SR-31742A UMB100 UMB101 UMB103 UMB116 YZ-011 YZ-069 YZ-185

Unknown / unsorted	4C-T-2 5-MeO-DiPT 18-MC β-Endopsychosin Chlorpromazine Clemastine Clocapramine Cloperastine D-Deprenyl DiPT DPT Gevotroline Nepinalone Selegiline TMA; Allosteric modulators: SKF-83959

v t e Tricyclics

Classes	Acridine Anthracene Dibenzazepine Dibenzocycloheptene Dibenzodiazepine Dibenzothiazepine Dibenzothiepin Dibenzoxazepine Dibenzoxepin Phenothiazine Pyridazinobenzoxazine Pyridinobenzodiazepine Thioxanthene

Antidepressants (TCAs and TeCAs)	7-OH-Amoxapine Amezepine Amineptine Amitriptyline Amitriptylinoxide Amoxapine Aptazapine Azepindole Azipramine Batelapine Butriptyline Cianopramine Ciclazindol Ciclopramine Cidoxepin Clomipramine Cotriptyline Cyanodothiepin Demexiptiline Depramine/Balipramine Desipramine Dibenzepin Dimetacrine Dosulepin/Dothiepin Doxepin Enprazepine Esmirtazapine Fantridone Fluotracen Hepzidine Homopipramol Imipramine Imipraminoxide Intriptyline Iprindole Ketipramine Litracen Lofepramine Losindole Loxapine Maprotiline Mariptiline Mazindol Melitracen Metapramine Mezepine Mianserin Mirtazapine Monometacrine Naranol Nitroxazepine Nortriptyline Noxiptiline Octriptyline Opipramol Oxaprotiline Pipofezine Pirandamine Propizepine Protriptyline Quinupramine Setiptiline/Teciptiline Spiroxepin Tandamine Tampramine Tianeptine Tienopramine Trimipramine

Antihistamines	Azatadine Clobenzepam Cyproheptadine Dacemazine Deptropine Desloratadine Epinastine Etymemazine Fenethazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Ketotifen Latrepirdine Loratadine Mebhydrolin Mequitazine Methdilazine Olopatadine Oxomemazine Phenindamine Pimethixene Promethazine Propiomazine Rupatadine Thiazinamium

Antipsychotics	Acetophenazine Alimemazine Amoxapine Asenapine Butaclamol Butaperazine Carfenazine (carphenazine) Carpipramine Chlorpromazine Chlorprothixene Ciclindole Citatepine Clocapramine Clomacran Clorotepine Clotiapine Clozapine Cyanothepin Doclothepin Docloxythepin Erizepine Flucindole Flumezapine Fluotracen Flupentixol Fluphenazine Gevotroline Homopipramol Isofloxythepin Levomepromazine/Methotrimeprazine Loxapine Maroxepin Meperathiepin Mesoridazine Metiapine Metitepine Metoxepin Mosapramine Naranol Octomethothepin Olanzapine Oxyclothepin Oxyprothepin Pentiapine Peradithiepin Perathiepin Perazine Perphenazine Periciazine Pinoxepin Piperacetazine Pipotiazine Piquindone Prochlorperazine Promazine Prothipendyl Quetiapine Savoxepin/Cipazoxapine Sulforidazine Tenilapine Thiethylperazine Thiopropazate Thioridazine Thiothixene Tilozepine Traboxopine Trifluoperazine Triflupromazine Trifluthepin Zotepine Zuclopenthixol

Anticonvulsants	Carbamazepine Dizocilpine Eslicarbazepine Eslicarbazepine acetate Etazepine Licarbazepine Oxcarbazepine Oxitriptyline Rispenzepine

Others	Adosopine Aminopromazine Atiprosin Beloxepin Carvedilol Cidoxepin Cyclobenzaprine Damotepine Darenzepine Elanzepine Methylene blue Monatepil Nuvenzepine Oxetorone Perlapine P7C3 Pinadoline Pirenzepine Pirolate Pitrazepin Pizotifen Profenamine Serazapine Siltenzepine Telenzepine Tipindole Tropatepine Zolenzepine

匿名

検索

案内

案内

desipramine hydrochloride