CN109700805A - Ornidazole is as controlling application of the demodicidosis drug in clinic - Google Patents
Ornidazole is as controlling application of the demodicidosis drug in clinic Download PDFInfo
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- CN109700805A CN109700805A CN201811629806.1A CN201811629806A CN109700805A CN 109700805 A CN109700805 A CN 109700805A CN 201811629806 A CN201811629806 A CN 201811629806A CN 109700805 A CN109700805 A CN 109700805A
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Abstract
The present invention relates to a kind of Ornidazoles as controlling application of the demodicidosis drug in clinic.It is proved by clinical case, Ornidazole can be obviously improved erythema, papule, warts and tubercle symptom, and pretherapy and post-treatment demodicidosis skin lesion is significantly improved.Clinical test verifying: for Ornidazole as demodicidosis drug is controlled, compliance is good, highly-safe, and patient is easier to receive, and is suitable for promoting.
Description
Technical field
The invention belongs to field of medicaments, a kind of new application, in particular to Ornidazole for being related to Ornidazole are controlling demodicidosis
Application of the drug in clinic.
Background technique
Ornidazole is (bacteroides fragilis, bacteroides disiens, oval bacteroid, bacteroides thetaiotaomicron, general by anaerobic bacteria for treating
Logical bacteroid, clostridium, Eubacterium, peptococcus and peptostreptococcus, helicobacter pylori, bacaeroides melaninogenicus, shuttle
Bacillus, CO2, which bite, knits dimension bacterium, gum bacteroid etc.) infect caused a variety of diseases；Men and women's urogenital tract trichmonad, merchant Shi
Disease caused by flagellum insect infection (such as trichomoniasis)；Intestines, liver amoeba parasitosis (including amoebic dysentery, amoeba liver
Abscess), intestines, liver deform disease caused by insect infection；Be also used to prevent and treat operation after anaerobic infection.
Demodicidosis (Demodicosis) it is as caused by people vermiform mite, based on Head And Face pilosebaceous unit
Common parasitic insect infection disease parasitizes only two kinds of human body, i.e. demodex folliculorum and demodex brevis.Have found vermiform mite
Be found in following skin obstacle: with or not with the facial itch of erythema, without telangiectasis or flushing acneform eruptions, eyelid
Edge inflammation, seborrhea, face or scalp papulopustular fash, Perioral Dermatitis, steroid dependent dermatitis and chemotherapy cause are exempted from
Epidemic disease inhibits the skin lesion of patient or AIDS patient.
Research in recent years shows that the pathogenesis of vermiform mite specifically includes that mechanical stimulus caused by vermiform mite polypide, foreign matter are anti-
It answers, the chemical stimulation of vermiform mite secretion, excreta attracts immunocyte such as neutrophil leucocyte, NK cell, the lymph of body thin
Born of the same parents etc. participate in, and are inflamed reaction so as to cause body.
Summary of the invention
In view of above-mentioned, demodicidosis disease incidence is high, and treatment lacks specific drug, and the purpose of the present invention is to provide a kind of nitre difficult to understand
Azoles is as controlling application of the demodicidosis drug in clinic
Ornidazole main component is Ornidazole；Auxiliary material is microcrystalline cellulose, hydroxypropyl methylcellulose, carboxyrnethyl starch sodium and stearic acid
Magnesium.
Chemical structural formula are as follows:
It is calculated by dry product, contains C7H10ClN3O399.0% must not be less than.
This product is white to yellowish crystalline powder；It is odorless, bitter；It is yellow to meet photochromic gradual change.
This product is readily soluble in ethanol, slightly molten in water.
Drug is tablet；Drug is oral preparations.
The dosage of ornidazole tablets is 0.25g/ piece, and daily oral 2 times, each 0.5g, 2 weeks as a treatment course, according to patient
The state of an illness is taken 2~8 weeks.
Ornidazole is the novel nitro imidazole derivatives of the third generation, and there is good anaerobe resistant and the raw texture dye of antigen to make
With the mechanism for killing microorganism is to be reduced into amino in oxygen-free environment by the nitro in its molecule or pass through free radical
Formation, interact with microbial cell ingredient, be a kind of to be suitble to treatment Human Follicle Mite Infection so as to cause the death of microorganism
Drug.
The present invention carries out histopathological examination to demodicidosis lesions of patients, expands from the visible intradermal capillary of inspection
It opens, blood vessel hyperplasia, forms granuloma structure above sebaceous glands, which is exactly as caused by vermiform mite.
Ornidazole illustrates as the mechanism for controlling demodicidosis drug:
Vermiform mite (referring to Fig. 1) parasitizes in the hair follicle and sebaceous glands of people and mammal, and acarid stimulates surrounding into human dermis' layer
Keratinocyte hyperplasia can make the lymphocytic infiltration of vermiform mite polypide perifollicolar.The vermiform mite of proliferation destroys hair by chelicera
Capsular epithelium cell salivary gland secretion catabolic enzyme leads to Skin barrier destruction, induces the hypersensitivity of IV type, i.e. vermiform mite is thin by phagocytosis
Born of the same parents' attack, causes the granuloma (referring to fig. 2) centered on vermiform mite, face red spot, papule, tubercle is caused to be formed.Oral Austria
After nitre azoles, Ornidazole is easy to absorb through gastrointestinal tract, is distributed widely in tissue and body fluid, Ornidazole molecule is reached with blood transportation
Dermal layer of the skin affected area, the nitro in molecule, in oxygen-free environment, some is reduced into amino, and some passes through raw after oxidation
It at free radical, interacts with the DNA of vermiform mite polypide cell, makes the fracture of DNA helical structure, blocks its transcription duplication,
It is dead so as to cause vermiform mite polypide, after the anti-vermiform mite treatment of Ornidazole, inhibit monokaryon/macrophage by killing vermiform mite
The cell activation and release for reducing proinflammatory reaction cell factor, growth factor and chemokines causes to mitigate inflammatory reaction
The tubercle that inflammatory cell package vermiform mite is formed is gradually recovered back normal tissue, and whelk, tubercle gradually calm down, and inflammation is gradually
Subside, it is final to fully recover.
Advantages of the present invention:
The present invention uses Ornidazole oral tablet, for treating demodicidosis patient, take can be obviously improved after Ornidazole erythema,
The skin lesion of papule and tubercle symptom, pretherapy and post-treatment demodicidosis patient is significantly improved, and achieves gratifying clinical efficacy.It is clinical
Research confirms: Ornidazole is good to the therapeutic effect of demodicidosis, and patient compliance is high, and adverse reaction is few, and patient facial region's skin lesion disappears
It moves back, face red spot papule calms down disappearance, and pruritis is clearly better, and has no obvious new hair and recurrence skin lesion, releases the heart for patient
Reason pain.Have the function for the treatment of demodicidosis by anti-vermiform mite to further disclose Ornidazole.
Detailed description of the invention
Fig. 1 is the vermiform mite figure that microscopically observation arrives.
Fig. 2 is the demodicidosis skin lesion histopathology figure that microscopically observation arrives: the vermiform mite polypide structure of intradermal.
Fig. 3 a patient suffers from papule and multiple wellability erythema atrophicans, is covered with the tiny scales of skin that peel off thereon, and occasionally there is scabies in private prosecution face
Gargalesthesia.
Fig. 3 b patient's papule subsides, and erythema partial remission locally leaves pigmentation.
At the end of 4 course for the treatment of of Fig. 3 c, patient facial region's skin lesion is subsided, and has no Xin Fa and recurrence skin lesion.
Fig. 4 a lesions of patients shows as the erythema of Middle face, is distributed mainly on Face and cheek, nose week and mouth week.
The area of Fig. 4 b patient facial region's erythema reduces, and itch is alleviated, and after taking 2 courses for the treatment of, erythema subsides substantially.
Patient facial region's erythema disappears at Fig. 4 c 6 months, and pruritis is clearly better.Have no obvious new hair and recurrence skin lesion.
Erythematous papules companion's Fig. 5 a patient facial region itches repeatedly.
Fig. 5 b patient takes 3 courses for the treatment of, and face red spot subsides substantially, and papule is calmed down.
At Fig. 5 c patient 6 months, face red spot papule calms down disappearance, and conscious pruritis is clearly better, and has no obvious new
Hair and recurrence skin lesion,
Specific embodiment
It is difficult to understand in order to clearly demonstrate first generation nitro glyoxaline antimicrobial metronidazole and third generation nitro glyoxaline antimicrobial
The difference of nitre azoles, table 1 are that metronidazole is contrasted with Ornidazole molecular structural formula and physics, chemical property
Table 1 is that metronidazole is contrasted with Ornidazole molecular structural formula and physics, chemical property
Ornidazole and the two drugs of metronidazole belong to nitro glyoxaline antimicrobial, and wherein metronidazole is first generation nitroimidazole
Class antimicrobial, Ornidazole are the novel nitro imidazole derivatives after metronidazole.
Ornidazole has good anaerobe resistant effect and anti-trichomonal effect and adverse reaction is less.With similar drugs first
It is compared for metronidazole, antibacterial activity is strong, long half time, and clinical efficacy is definite.From 1 chemical structural formula of table it can be seen that nitre difficult to understand
Azoles and metronidazole have common main ring, and only the side chain on ring is different, in addition, its physico-chemical property different from, is demonstrated by Austria
Nitre azoles makees drug specific function and effect, in the new application for controlling demodicidosis.Although Ornidazole and both drugs of metronidazole
Anaerobe resistant mechanism is similar, that is, is selectively entered protozoon body (including trichomonad, amoeba, Giardiasis, colon pouch flagellum
Worm etc.) and anaerobic bacteria body in after, under the action of distinctive low redox potential and enzyme, oxidation-reduction process have it is stronger also
The ability of originality nitroimidazole, it is activated by flavine electron transit mediator, and receives the electronics that carrier transmits, followed by by peroxidating
The oxygen that object generates reoxidizes, and generates toxic oxidized derivatives, and further reduction obtains nitroso-derivative.Free nitroso
Root and hydroxylamine derivative, these intermediate products have a cytotoxicity, bacterial cell and the intracellular deoxynucleotide of polypide (DNA),
Ribonucleic acid (RNA), protein and other targets work, to kill bacterium and polypide.The difference of Ornidazole and metronidazole
It also resides in drug half-life, the effect of antibacterial anti-trichomonal and adverse reaction.Ornidazole is constantly improved on the basis of metronidazole,
Good anaerobe resistant effect and anti-trichomonal effect are obtained, and adverse reaction is less, long half time, clinical efficacy exact one
Kind drug.There is apparent killing effect to various common pathogenic anaerobic bacterias and trichomonad according to current clinical observation Ornidazole,
Its activity is strong compared with metronidazole, suitable with metronidazole to the curative effect of amoebic dysentery and parenteral amcbiasis, and toxic side effect is obvious
Lower than metronidazole.Lot of documents and clinical report, metronidazole is mainly absorbed by gastrointestinal tract, so bad hair should be anti-with alimentary canal
It answers common, is mainly shown as Nausea and vomiting, epigastric pain, loss of appetite and oral cavity metallic taste etc., therefore, general one after each meal.And
The adverse reaction of Ornidazole is rare compared with metronidazole and slight, occasionally have slight digestive tract reaction or occur pruitus, constipation and
Phenomena such as general malaise.These side effect symptoms can disappear quickly usually after drug withdrawal.Ornidazole is third generation nitro glyoxaline
For antibiotic compared with metronidazole, duration of efficacy is longer, and Ornidazole half-life is longer than metronidazole half-life by 1.7
Times, and patient is made to show better compliance.It can be seen that Ornidazole is than metronidazole Small side effects, times for spraying is few, patient
Compliance is good.
The present invention is further elaborated Ornidazole drug controlling demodicidosis with clinical test case:
The present invention treats people vermiform mite patient, and carries out statistical analysis to result:
The present invention chooses the 100 vermiform mite sufferers gone to a doctor between 2017-01~2018-10 in Lanzhou hospital general Dermatology Outpatient Department
Person, wherein women 72 (72.0%), male 28 (28.0%), between 20~49 years old age, the course of disease 0.08~19 year.Nitre difficult to understand
Azoles treatment gives ornidazole tablets 0.5g and takes orally 2/d, is taken 2~8 weeks according to conditions of patients.June is observed after the completion for the treatment of.Treatment
Effect judgment criteria: observation index: photo archive is carried out by the same doctor when patient per is medical, at the end of follow-up
Skin lesion improvement degree be divided into recovery from illness, it is effective, improve, be invalid.Curing is skin lesion recession >=90%, and papule, warts disappear substantially, nose
The smooth no protrusion in portion, pore become smaller；Effective to subside 60~90%(containing 60%) for skin lesion, papule, warts disappear substantially, skin of nose
It has clear improvement；Improving is that skin lesion subsides 30~60%(containing 30%), more than half recession of papule, warts, skin of nose is changed
It is kind；Subside 0~30%(containing 0%) for skin lesion in vain, papule, warts disappear less than half, and skin of nose is substantially without improvement.Recurrence:
Skin lesion has the new hair skin lesion of same symptoms again after curing；Treat total effective rate=(healing+effective)/total number of persons × 100%.(result
Referring to table 2)
2. Ornidazole of table treats patient's total effective rate
As can be seen from Table 2: Ornidazole treats 100 patients, and at 2 weeks of follow-up, total efficiently individual quantity reached 27, total effective rate
Total efficiently individual quantity reaches 63 when total efficiently individual quantity reaches 38, total effective rate 38%, 6 week when being 27%, 4 week, total effective rate
Total efficiently individual quantity reaches 83 when being 63%, 8 week, total effective rate 83%.By clinical observation, Ornidazole is to people's demodicidosis
Total effective rate is high.
After oral Ornidazole, main component Ornidazole molecule reaches dermal layer of the skin with blood transportation, passes through blood-body fluid
Exchange, Ornidazole molecule reach affected area, and the nitro in molecule, in oxygen-free environment, some is reduced into amino, and some passes through
Free radical is generated after oxidation, is interacted with the DNA of vermiform mite polypide cell, is broken DNA helical structure, is blocked it
Transcription duplication, it is dead so as to cause vermiform mite polypide.
Clinical test confirms: Ornidazole is good to the therapeutic effect of demodicidosis, patient compliance is strong, and adverse reaction is few,
Theoretically Ornidazole is supported to treat demodicidosis.
In the following, the present invention by taking typical case as an example, illustrates Ornidazole as the effect controlled in demodicidosis drug:
Typical case 1: Feng so-and-so, male, 26 years old, in April, 2018 was medical because " right face erythematous papules tubercle with itch August " are medical
When lesions of patients be distributed mainly on right side face and auricle, show as being dispersed in diameter 0.3-1cm or so tubercle, papule and multiple
Wellability erythema atrophicans, are covered with the tiny scales of skin that peel off thereon, and occasionally there are scratchiness (referring to Fig. 3 A), Lanzhou hospital general skin in private prosecution face
Section's outpatient service detects the vermiform mite positive, is diagnosed as " demodicidosis ", is treated using the present invention, when taking orally 2 course for the treatment of using Ornidazole agent,
Face red spot color is thin out, and papulonodule part is calmed down, and pruritis mitigates, after taking 3 courses for the treatment of, face red spot partial remission,
Substantially reduced, at the end of 4 courses for the treatment of, patient's tubercle, papule subside, and erythema partial remission locally leaves pigmentation (referring to figure
3B), treatment end follow-up 6 months when visible patient facial region's skin lesion subside, have no Xin Fa and recurrence skin lesion (referring to Fig. 3 C).
Typical case 2: Mr. Li, female, 48 years old, because of " face red spot is medical with itching ", skin lesion was shown as in face in September, 2017
The erythema in portion, it is all (A referring to fig. 4) to be distributed mainly on Face and cheek, nose week and mouth, the easy flush of patient's private prosecution, itch, drying and tight
Etc. subjective symptoms.Lanzhou hospital general Dermatology Outpatient Department detects the vermiform mite positive, is diagnosed as " demodicidosis ", oral using the present invention
Ornidazole agent 0.5g, 2 times a day, after taking 1 course for the treatment of, the area of face red spot reduces, and itch is alleviated, after taking 2 courses for the treatment of, erythema
Basic to subside (B referring to fig. 4), at treatment end follow-up 6 months, face red spot disappears, and pruritis is clearly better.Have no obvious
New hair and recurrence skin lesion (C referring to fig. 4).
Typical case 3: Zhang, female, 20 years old, in January, 2018, readme symptom was most opened because of " erythematous papules companion's face itches repeatedly "
Begin gradually to spread to bilateral Face and cheek (referring to Fig. 5 A) around, itch is obvious at papule, and entire face has tightly from nose Zhou Fasheng
Taut and burn feeling, face are dispersed in about 0.1-0.4cm or so papule on the basis of erythema, and invalid using product for resolving poxes, Lanzhou is total
Hospital dermatology department outpatient service detects the vermiform mite positive, is diagnosed as " demodicidosis ", rear using the oral Ornidazole agent 0.5g of the present invention, often
It 2 times, 2 courses for the treatment of are taken, face red spot gradually calms down reduction without significant change, papule, takes 3 courses for the treatment of, and face red spot disappears substantially
It moves back, papule is calmed down (referring to Fig. 5 B), and at treatment end follow-up 6 months, face red spot papule calms down disappearance, and conscious pruritis is bright
It is aobvious to improve, have no obvious new hair and recurrence skin lesion (referring to Fig. 5 C).
From clinical application, we recognize that: demodicidosis is a kind of common disease.Research shows that: demodicidosis is
The skin disease with genetic predisposition mediated by the specific immune function defect or reduction of host.Pass through mechanical stimulus, inflammation
Mediation destroys skin barrier function, and then causes the formation of the skin lesions such as erythema, papule, tubercle.Furthermore skin temperature increase,
Oiliness or combination, facial cleansing situation are poor, and the facial inducements such as thicker of making up, and cause skin microenvironment to change, stimulation
Vermiform mite is proliferated and causes the generation of demodicidosis.Ornidazole can inactivate, reduce the oxygen radical ROS generated in inflammation, reach
The effect of local anti-inflammatory, so as to preferably control the inflammatory skin lesion of demodicidosis.It is difficult to understand after metronidazole, Tinidazole
Nitre azoles (ornidazole, ONZ) is the novel nitro imidazole derivatives of the third generation, has preferable anaerobe resistant and antigen raw
Texture dye can treat a variety of diseases caused by being infected by anaerobic bacteria, merchant trichomonad, Amoeba, trichmonad etc. extensively.Especially
Demodicidosis drug is controlled in Ornidazole conduct good effect, releases mental anguish for patient.Ornidazole can be existed by its nitro
It is reduced into amino in oxygen-free environment or forms free radical, reacts with vermiform mite polypide cellular elements and causes vermiform mite dead
It dies.In order to determine that its biological safety is guaranteed, and under the premise of meeting ethics, this seminar is in the nitre difficult to understand of application in 2015
The clinical research (clinical test ChiCTR-IPR-15006451) of azoles treatment demodicidosis.The present invention is oral using Ornidazole
Tablet can be obviously improved erythema, papule and tubercle symptom after taking Ornidazole, before and after treatment for treating demodicidosis patient
The skin lesion of demodicidosis patient is significantly improved, and achieves gratifying clinical efficacy.Clinical research confirmation: Ornidazole is to vermiform mite
The therapeutic effect of disease is good, and patient compliance is high, and adverse reaction is few, can promote on a large scale.
Claims (1)
1. Ornidazole is as application of the demodicidosis drug in clinic is controlled, in clinical test, patient's medication dose is 0.25g/
Piece, daily oral 2 times, each 0.5g, 2 weeks as a treatment course.
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| CN201811629806.1A CN109700805A (en) | 2018-12-29 | 2018-12-29 | Ornidazole is as controlling application of the demodicidosis drug in clinic |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110624102A (en) * | 2019-11-08 | 2019-12-31 | 罗洋 | Clinical application of bevacizine as medicine for repairing demodex disease skin damage |
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| CN102525889A (en) * | 2012-03-19 | 2012-07-04 | 段亚东 | Ornidazole ophthalmic gel and preparation method and application thereof |
| CN102641267A (en) * | 2012-05-15 | 2012-08-22 | 段亚东 | Externally-applied skin gel as well as preparation method and application thereof |
| CN104640451A (en) * | 2012-07-04 | 2015-05-20 | 雷蒙特亚特特拉维夫大学有限公司 | Ornidazole and related compounds for use as herbicides |
| CN106551929A (en) * | 2016-11-05 | 2017-04-05 | 罗洋 | New application of the Ornidazole in treatment acne rosacea medicine |
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2018
- 2018-12-29 CN CN201811629806.1A patent/CN109700805A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102525889A (en) * | 2012-03-19 | 2012-07-04 | 段亚东 | Ornidazole ophthalmic gel and preparation method and application thereof |
| CN102641267A (en) * | 2012-05-15 | 2012-08-22 | 段亚东 | Externally-applied skin gel as well as preparation method and application thereof |
| CN104640451A (en) * | 2012-07-04 | 2015-05-20 | 雷蒙特亚特特拉维夫大学有限公司 | Ornidazole and related compounds for use as herbicides |
| CN106551929A (en) * | 2016-11-05 | 2017-04-05 | 罗洋 | New application of the Ornidazole in treatment acne rosacea medicine |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110624102A (en) * | 2019-11-08 | 2019-12-31 | 罗洋 | Clinical application of bevacizine as medicine for repairing demodex disease skin damage |
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