CN103784451A - Drug for treating depression - Google Patents
Drug for treating depression Download PDFInfo
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- CN103784451A CN103784451A CN201210428565.0A CN201210428565A CN103784451A CN 103784451 A CN103784451 A CN 103784451A CN 201210428565 A CN201210428565 A CN 201210428565A CN 103784451 A CN103784451 A CN 103784451A
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- depression
- fluoxetine
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 8
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims description 3
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- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
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- AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 description 1
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- RONZAEMNMFQXRA-UHFFFAOYSA-N mirtazapine Chemical compound C1C2=CC=CN=C2N2CCN(C)CC2C2=CC=CC=C21 RONZAEMNMFQXRA-UHFFFAOYSA-N 0.000 description 1
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- VGKDLMBJGBXTGI-SJCJKPOMSA-N sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 description 1
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- 229960004688 venlafaxine Drugs 0.000 description 1
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 description 1
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a drug for treating depression. The drug contains an effective amount of 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-ylmethyl)piperidine-4-yl]-1H-imidazole-5-yl}pyrimidine-2-amine and an effective amount of fluoxetine, and the mass ratio of 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-ylmethyl)piperidine-4-yl]-1H-imidazole-5-yl}pyrimidine-2-amine to fluoxetine is 3:1 to 6:1. Through combined use of specific drugs, side effects during treatment of depression are greatly reduced, pain of patients is reduced, and recovery of the patients is availed.
Description
Technical field
The present invention relates to a kind of medicine, be specifically related to a kind of medicine of Cure of depression.
Background technology
Depression is a kind of common mood disorders, can be caused by a variety of causes, low as main clinical characteristics take remarkable and lasting mental state, and mental state is low unbecoming with its situation, and suicidal thought and behavior can appear in severe patient.Majority of cases has the tendency of outbreak repeatedly, and the great majority that at every turn show effect can be alleviated, and part can have residual symptoms or transfer to chronic.
Depression has at least 10% patient can occur maniac access, now should be diagnosed as two-phase obstacle.The depression that we often say in addition, refers to major depression (major depression) clinically in fact, has 16% people affected by it in certain period in all one's life in crowd.Suffer from depression except paying serious emotion and social costs, economic cost is also huge.According to World Health Organization's statistics, depression has become the large illness in the world the 4th, expects the year two thousand twenty, may become the second largest disease that is only second to coronary heart disease.
The typical performance of depression clinical symptoms comprises the reduction of three dimension activities: depressed, retardation of thinking, bulesis go down, and other patient can show as main take somatization.Specifically can show as remarkable and lasting depression pessimism, unbecoming with actual environment.The patient that degree is lighter feels depressed, and without happy sense, everything lacks interest, feels " having sense of depression at heart ", " can'ting be happy "; What degree was heavy can be pessimistic desperate, has the sense that one day seems like a year, to live is no better than to die, and patient often tells " the not meaning lives ", " feeling bad " etc. at heart.Climacteric and senile patients with depressive disorder can be with dysphoria, malaise, scorching, flushing hyperhidrosis etc. from head to foot, and child and teenager can show as irritability (as impatient, get angry for some minor matters).Typical depressive mood also has the feature of the light rhythm and pace of moving things at heavy night in morning, depressed comparatively serious in the morning, and can alleviate to some extent at dusk time.
It is blunt that patient may feed back brain response, or memory, aprosexia, and study or ability to work decline or be irresolute, and power shortage, thinks of nothing dry, and adequate Working Life was felt to be unable to cope with now in the past; Patient not only starts self evaluation and reduces, sometimes also all mistakes can be attributed to oneself, normal generation sense of uselessness, nothing are wished sense, helplessness and valueless sense, even start self-accusation from crime, when serious, can occur that delusion of sin (is entangled with and more own little faults repeatedly, think that oneself makes a really big mistake, be about to pay for), repeatedly there is passive idea or behavior.
When a lot of patients do not go on a diet can with appetite decline or hyperfunction, lose weight or (for example increase, in one month, body weight change exceedes 5%), almost have insomnia or hypersomnia every day, also have some patients to there will be hyposexuality, female patient there will be the disorder of menstruation.
The feature of Drug therapy is that onset is relatively very fast, and curative effect is more definite, is suitable for moderate, major depressive disorder patient.Antidepressants are main medicines of the various depressive disorders of current treatment, can efficient solution remove depressive mood and the anxiety of following, anxiety and somatization, effective percentage approximately 60%~80%.
The antidepressant of a current line comprises SSRI class medicine, as paroxetine, Sertraline, fluoxetine, citalopram, fluvoxamine etc., is commonly called as " Five Golden Flowers ", and the reaction of SSRI badness is less and slight, and especially the untoward reaction of anticholinergic and heart is few.That common untoward reaction has is nauseating, vomiting, anorexia, constipation, diarrhoea, xerostomia, tremble, insomnia, anxiety and sexual dysfunction etc.
SNRI class medicine, as venlafaxine, duloxetine, certainly, onset is very fast, has obvious antidepressant and angst resistance effect for SNRI curative effect.Also effective to intractable case.That common adverse reactions has is nauseating, xerostomia, perspiration, weak, anxiety, tremble, sexual impotence and defective ejaculation, when heavy dose of, some patients were blood pressure may slightly raise.
NaSSAs class (NE and specificity 5-HT energy antidepressants), as mirtazapine, there are good antidepressant, anxiety and improve sleep effect, oral absorption is fast, rapid-action, anticholinergic effect is little, has sedation, sexual function is not almost affected, and common adverse reactions is that calmness, drowsiness, dizziness, tired, appetite and body weight increase.
Amfebutamone, the weak inhibitor of norepinephrine, 5-hydroxy tryptamine, dopamine reuptake, does not have inhibitory action to monoamine oxidase, MAO, is applicable to depression and Bipolar Depression, and advantage is little on body weight and sexual function impact.Common untoward reaction has: excitement, xerostomia, insomnia, headache or migraine, feel sick, vomiting, constipation, tremble, hyperhidrosis.
For some anxieties obviously, with the patient of sleep disorder, can short-term use some Benzodiazepineses (stable class) medicine or sleeping medicine that some are novel, as zolpidem, zopiclone.For some serious symptoms, even, with the patient of psychotic symptoms, can merge antipsychotic medications.
But existing medicine is most expensive, and with larger side effect.
Summary of the invention
The object of the present invention is to provide a kind of medicine of Cure of depression, described medicine, by drug combination, in guaranteeing drug effect, significantly reduces side effect.
Technical problem of the present invention solves by following technical solution:
A kind of medicine of Cure of depression, it is characterized in that, described medicine contains effective dose: 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-base methyl) piperidin-4-yl]-1H-imidazoles-5-yl } fluoxetine of pyrimidine-2-amine and effective dose, described 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-base methyl) piperidin-4-yl]-1H-imidazoles-5-yl } pyrimidine-2-amine and fluoxetine mass ratio be 3:1 ~ 6:1.
4-{4-of the present invention (4-fluorophenyl)-1-[1-(isoxazole-3-base methyl) piperidin-4-yl]-1H-imidazoles-5-yl } pyrimidine-2-amine and fluoxetine mass ratio, preferably 3.5:1 ~ 5:1, further preferred 4:1.
4-{4-of the present invention (4-fluorophenyl)-1-[1-(isoxazole-3-base methyl) piperidin-4-yl]-1H-imidazoles-5-yl } pyrimidine-2-amine and fluoxetine, all the known medical compoundss of affiliated technical field, it can be bought and obtain from market, also can prepare voluntarily by the preparation method disclosing in prior art, the present invention no longer does further restriction with regard to its source with preparation technology.
The present invention is by the use of combining of certain drug, and the side effect while greatly reducing its Cure of depression, has reduced patient's misery, is conducive to patient's recovery.
The specific embodiment
For ease of understanding the present invention, it is as follows that the present invention enumerates embodiment.Those skilled in the art should understand, described embodiment only, for helping to understand the present invention, should not be considered as concrete restriction of the present invention.
Embodiment 1
A kind of medicine of Cure of depression, it is characterized in that, described medicine contains effective dose: 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-base methyl) piperidin-4-yl]-1H-imidazoles-5-yl } fluoxetine of pyrimidine-2-amine and effective dose, described 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-base methyl) piperidin-4-yl]-1H-imidazoles-5-yl } pyrimidine-2-amine and fluoxetine mass ratio be 4:1.
The preparation process of described medicine is the known formulations method of this area, such as blend pelletize etc.
Show by method of testing test known in the art, after patient takes above-mentioned medicament, vomiting and sleep disorder are obviously eliminated, and the side effect while proving this compound medicine to Cure of depression is eliminated obviously.
Applicant's statement, the present invention illustrates detailed process composition and engineering flow process of the present invention by above-described embodiment, but the present invention is not limited to above-mentioned detailed process composition and engineering flow process, do not mean that the present invention must rely on above-mentioned detailed process composition and engineering flow process and could implement.Person of ordinary skill in the field should understand, any improvement in the present invention, and the selections of the equivalence replacement to the each raw material of product of the present invention and the interpolation of auxiliary element, concrete mode etc., within all dropping on protection scope of the present invention and open scope.
Claims (1)
1. the medicine of a Cure of depression, it is characterized in that, described medicine contains effective dose: 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-base methyl) piperidin-4-yl]-1H-imidazoles-5-yl } fluoxetine of pyrimidine-2-amine and effective dose, described 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-base methyl) piperidin-4-yl]-1H-imidazoles-5-yl } pyrimidine-2-amine and fluoxetine mass ratio be 3:1 ~ 6:1.
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CN201210428565.0A CN103784451A (en) | 2012-10-31 | 2012-10-31 | Drug for treating depression |
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CN201210428565.0A CN103784451A (en) | 2012-10-31 | 2012-10-31 | Drug for treating depression |
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2016149756A1 (en) * | 2015-03-23 | 2016-09-29 | The University Of Melbourne | Treatment of respiratory diseases |
CN106466416A (en) * | 2015-08-20 | 2017-03-01 | 山东金诃药物研究开发有限公司 | Application in preparation medicament for treatment of depression for the compound recipe Rhizoma Gymnadeniae ball |
WO2017050297A1 (en) * | 2015-09-25 | 2017-03-30 | Sun Jet Biotechnology Inc. | Combination therapy for ev71 infection |
US12215095B2 (en) | 2018-11-07 | 2025-02-04 | The University Of Melbourne | Compounds for the treatment of respiratory diseases |
-
2012
- 2012-10-31 CN CN201210428565.0A patent/CN103784451A/en active Pending
Cited By (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2016149756A1 (en) * | 2015-03-23 | 2016-09-29 | The University Of Melbourne | Treatment of respiratory diseases |
CN107847480A (en) * | 2015-03-23 | 2018-03-27 | 墨尔本大学 | The treatment of respiratory disease |
US10722513B2 (en) | 2015-03-23 | 2020-07-28 | The University Of Melbourne | Treatment of respiratory diseases |
CN107847480B (en) * | 2015-03-23 | 2021-06-25 | 墨尔本大学 | Treatment of Respiratory Diseases |
US11564925B2 (en) | 2015-03-23 | 2023-01-31 | The University Of Melbourne | Treatment of respiratory diseases |
US11975005B2 (en) | 2015-03-23 | 2024-05-07 | Tianli Biotech Pty Ltd | Treatment of respiratory diseases |
CN106466416A (en) * | 2015-08-20 | 2017-03-01 | 山东金诃药物研究开发有限公司 | Application in preparation medicament for treatment of depression for the compound recipe Rhizoma Gymnadeniae ball |
WO2017050297A1 (en) * | 2015-09-25 | 2017-03-30 | Sun Jet Biotechnology Inc. | Combination therapy for ev71 infection |
US10548915B2 (en) | 2015-09-25 | 2020-02-04 | Sun Jet Biotechnology Inc. | Combination therapy for EV71 infection |
US12215095B2 (en) | 2018-11-07 | 2025-02-04 | The University Of Melbourne | Compounds for the treatment of respiratory diseases |
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Application publication date: 20140514 |