JPS59501712A - Method for treating itch and composition therefor - Google Patents

Method for treating itch and composition therefor

Info

Publication number
JPS59501712A
JPS59501712A JP57502942A JP50294282A JPS59501712A JP S59501712 A JPS59501712 A JP S59501712A JP 57502942 A JP57502942 A JP 57502942A JP 50294282 A JP50294282 A JP 50294282A JP S59501712 A JPS59501712 A JP S59501712A
Authority
JP
Japan
Prior art keywords
naloxone
pharmaceutically acceptable
acceptable salt
naltrexone
salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP57502942A
Other languages
Japanese (ja)
Inventor
バ−ンステイン・ジヨエル・イ−
Original Assignee
バ−ンステイン,ジヨエル イ−.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by バ−ンステイン,ジヨエル イ−. filed Critical バ−ンステイン,ジヨエル イ−.
Publication of JPS59501712A publication Critical patent/JPS59501712A/en
Pending legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)

Abstract

(57)【要約】本公報は電子出願前の出願データであるため要約のデータは記録されません。 (57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

【発明の詳細な説明】 痛痒症を治療する方法およびそのための組成物本発明は、痛痒症(prurit is ) を幅減するための組成物に関する。[Detailed description of the invention] Methods of treating pruritus and compositions therefor The present invention provides methods for treating pruritus and compositions therefor. The present invention relates to a composition for significantly reducing is).

かゆみ(itching )または痛痒は、普通の皮膚科学的症状である。痛痒 症の原因は初雑であり、そして少ししか理解されていない。かゆみの最高に理解 されている機構は、じんま疹の丘疹(urticarial wheals ) および強いかゆみに導く度胸におけるヒスタミンの放出である。。そのようなか ゆみは、伝統的に抗ヒスタミン剤により軽減されてきた。抗ヒスタミン療法はし ばしば有効であるけれども、抗ヒスタミン剤により導かれる鎮静および眠む気は 、それらの有効性を制限する。Itching or itching is a common dermatological symptom. Itching The causes of the disease are primitive and poorly understood. Best understanding of itching The proposed mechanism is urticarial papules. and the release of histamine in the gut leading to intense itching. . Is that so? Itching has traditionally been relieved with antihistamines. antihistamine therapy chopsticks Although often effective, the sedation and drowsiness induced by antihistamines , limiting their effectiveness.

しかしながら、多植のかゆみは、抗ヒスタミン剤によっては容易には軽減されな い。たとえば、ホジキン氏病、きのこ状フンゲス(皮屑悪性)および重篤な黄桓 のような状態は、抗ヒスタミン剤により軽減されない強いかゆみを導く。従って 、そのような治療に応答する蚊刺傷のような原因に基くかゆみの抗ヒスタミン治 療に対する代替でありうるばかりでなくまた、中枢神経系に対する全身性効果に 基く方法に関係する本発明者の先行米国特許第4,181.726号中に開示さ れた如きものを除き、従来治療することが実際上不可能であった痛痒症の難治性 事例における軽減を更に提供する、重篤なかゆみを軽減するための改善された治 療が要望されている。本発明は、中枢神経系に対する全身効果と無関係のそのよ うな組成物および方法を提供的依存性を生じることが知られておらず、また非耽 溺者に対し基本的に薬理学的活性を発揮しない麻薬拮抗剤である。ナロキソンは 、耽病者に対し麻薬離脱において彼等を助けるために通常注射により投与され、 またあるときには手術の間の麻薬の使用に引続く麻薬性抑うつの部分的逆転のた めに術後患者に投与される。However, itching is not easily relieved by antihistamines. stomach. For example, Hodgkin's disease, fungal fungus and severe fungus This condition leads to severe itching that is not relieved by antihistamines. Therefore , antihistamine treatment of itch based on causes such as mosquito bites that respond to such treatment. Not only can it be an alternative to therapy, but it also has systemic effects on the central nervous system. As disclosed in my prior U.S. Pat. No. 4,181.726 related to the underlying method, Intractable pruritus, which was practically impossible to treat with the exception of cases such as Improved treatments to relieve severe itching, providing further relief in cases Treatment is required. The present invention addresses such We provide such compositions and methods that are not known to cause dependence and are non-indulgent. It is a narcotic antagonist that basically shows no pharmacological activity in drowning victims. Naloxone is , usually administered by injection to addicts to help them with drug withdrawal; and sometimes for partial reversal of narcotic depression following narcotic use during surgery. It is administered to patients postoperatively.

ナロキソンの局所投与は種々の状節における重篤なかゆみの理解において有用で あることが、篤くべきことには見出された。Topical administration of naloxone may be helpful in understanding severe itching in various lesions. Something serious has been discovered.

本発明は、そのような治療の必要な患者における重篤なかゆみを@滅するための 方法を提供し、該方法はそのような治療の必要な患者に対し、ナロキソンまたは その医薬的に受容しつる塩、ある′いはナルトレキフン(Na1trexone  ) の治療的有効量を局所投与することからなる。The present invention provides a method for eliminating severe itching in patients in need of such treatment. Provided are methods for administering naloxone or Its pharmaceutically acceptable salts, or Naltrexone .)).

ナロキソン塩酸塩は、デュポン・カンパニー(DuPont Company  ) の従属会社であるエンド・ラボラトリーズ・インコーホレーテッド(End o Laboratories 。Naloxone hydrochloride is manufactured by DuPont Company. ) is a subsidiary of End Laboratories, Inc. (End o Laboratories.

工nc、)、スチュアート・アベニュー(Stewart Avenue)、ガ ーデン・シティ(Garden C1ty) 、ニューヨーク(Newyork ) 11560から商業的に入手しうる。ナロキソンの製造は、米国特許第3. 254,083号中に開示されている。nc,), Stewart Avenue, Ga. - Garden C1ty, New York ) 11560 commercially available. The production of naloxone is described in U.S. Patent No. 3. No. 254,083.

ここに使用される医薬的に受容される塩なる語は、ば塩酸塩、臭化水素酸塩、ヨ ウ化水素醸塩、アセテート、バレレート、オレエート等を示ス。As used herein, the term pharmaceutically acceptable salts includes hydrochloride, hydrobromide, iodine. Indicates hydrogen uride salt, acetate, valerate, oleate, etc.

局所投与用の液体投薬形は、この技術分野におし1て普通に使用される揮発性希 釈剤、たとえばアルコール、グリコール等を含有する受容しうる乳液、溶液およ び懸濁液を包含する。そのような希釈剤の他に、局所適用組成物はまた、湿潤剤 、乳化剤および懸濁化剤を包含しうる。Liquid dosage forms for topical administration are made from volatile diluted materials commonly used in the art. Acceptable emulsions, solutions and solutions containing diluents such as alcohols, glycols etc. and suspensions. In addition to such diluents, topically applied compositions may also contain humectants. , emulsifying agents and suspending agents.

本発明の実施において、医薬的に受容しうる塩たとえは塩酸塩およびその医薬的 に受容しうる化学的誘導体たとえばn−メチルシクログロピル銹導体であるナル トレキフンの形におけるナロキソンは、局所投与用の溶成、ローション、クリー ムおよび軟膏中に、それら局所製品は、1日1から8回まで度胸に適用される。In the practice of this invention, pharmaceutically acceptable salts include the hydrochloride salt and its pharmaceutically acceptable salts. Chemical derivatives acceptable to Naloxone in the form of Trekifun is available as a solution, lotion, and cream for topical administration. In creams and ointments, these topical products are applied to the chest from one to eight times a day.

局所適用された者により経験される軽減は、1時的であるけれども急速である。The relief experienced by those applying topically is temporary but rapid.

例1 ナロキソン塩酸壇1重量%を、エチルアルコール70容量%およびプロピレング リコール60容量%力)ら構成される溶液中に合体させ、そして11才の男子に 対し24時間以内の2つの蚊刺傷に1日5回適用した。この子供は、各適用の1 0分以内に彼の力Sゆみ力)らの軽減を認め、軽減は2〜4時間持続した。Example 1 1% by weight of naloxone hydrochloride, 70% by volume of ethyl alcohol and propylene. 60% by volume) and an 11-year-old boy. It was applied five times a day to two mosquito bites within 24 hours. This child has 1 of each application. He noticed a reduction in his strength within 0 minutes, and the relief lasted for 2 to 4 hours.

例2 ナロキソン塩酸塩0.0 5%をオイセリン( R.T.M )クリームに合体 させ、そしてきのこ状フンゲスに起因する難治性かゆみを有する60才の男子の 身体に1日4回適用した。オイセリン( R,T.M )クリームは、/クイエ ルスドルフ、インコニホレーテツト( Beiersdorf。Example 2 Combine naloxone hydrochloride 0.05% into Eucerin (R.T.M.) cream A 60-year-old man with intractable itching caused by fungus fungus. Applied to the body 4 times a day. Eucerin (R, T.M) cream / Kuie Beiersdorf, Inc.

■nc.)サウス・ノルウオーク( South Norwa’lk )、コネ チカット( COnnetiCut ) 0 6 8 5 4 により製造され た合成ラノリン含有クリームである。これは、使用した患者に彼のかゆみからの 何らかの顕著な軽減を提供した最初の局所製品であった。■nc. ) South Norwak, Kone Manufactured by CONnetiCut 0.6.8.5.4 It is a cream containing synthetic lanolin. It was used to give patients relief from his itching. It was the first topical product to provide any significant relief.

例ろ 主にペトロラタムから構成され、そしてナロキ゛ノン塩酸塩肌01重量%を含有 する軟膏を、きのこ状フンゲスを有する60才の男子の身体に1日4回適用した 。Just like that Mainly composed of petrolatum and contains 0.1% by weight of naquinone hydrochloride The ointment was applied four times a day to the body of a 60-year-old man with fungus fungi. .

例2におけるナロキサンのより高濃度と同しはとではないけれども、かゆみは減 少した。Although not the same as the higher concentration of naloxane in Example 2, the itching is reduced. It was a little.

例4 ナロキソン塩酸塩肌1重量%を亜鉛シェークローションに合体させ、そして6オ の女子の蚊刺隔に、夏に5回の間隔で1ケ月間適用した。この適用は、かゆみか らの顕著な軽減を提供した。Example 4 Naloxone hydrochloride skin 1% by weight was combined with zinc shake lotion and 6 oz. It was applied five times in the summer for one month to the mosquito bite intervals of girls. This application may cause itching or provided significant relief.

例5 ナロキソン塩酸塩5重量%を軟膏に合体させ、そして38才の男子の左手上の小 湿疹性斑点に1日4回2日間適用した。かゆみは試鹸軟肯の各適用により皮層科 学的に減少した。Example 5 Naloxone hydrochloride 5% by weight was combined into an ointment, and the small area on the left hand of a 38-year-old male was Applied to eczematous spots 4 times a day for 2 days. Itching can be treated by applying soap to the skin. scientifically decreased.

手続補正書(自発) 昭和59年5879日 特許庁長官殿 2、発明の名称 3、補正をする者 事件との関係 特許出願人 4、代理人 5、補正命令の日付 昭和 年 月 日 66補正により増加する発明の数 8、補正の内容 別紙のとおりProcedural amendment (voluntary) 5879, 1982 Commissioner of the Patent Office 2. Name of the invention 3. Person who makes corrections Relationship to the incident: Patent applicant 4. Agent 5. Date of amendment order Showa year, month, day Number of inventions increased by 66 amendment 8. Contents of amendment as attached

Claims (1)

【特許請求の範囲】 1 そのような治療の必要な患者における重篤な痛痒を軽減する方法において、 ナロキソンまたはその医薬的に受容しうる塩、あるいはナルトレキソンの治療的 有効量をそのような治療の必要な唐音に局所投与することからなる方法。 2 該ナロキソンまたはその医薬的に受容しうる塩、あるいはナルトレキソンが 、溶液、ローション、クリームまたは軟膏中に、約0.01重量%から約5重量 %までの範囲内において存在する、請求の範囲第1項の方法。 ろ 該ナロキソンまたはその医薬的に受容しうる塩、あるいはナルトレキソンか 、そのような治療の必要な患者に、1日当り1から8回まで周期的に投与される 、請求の範囲第1項の方法。 4 ナロキソンの該医薬的に受容しうる塩が、生理学的に受容しうる酸付加塩で ある、請求の範囲第1項の方法。 5 ナロキソンの該医薬的に受容しうる塩がナロキソン塩酸塩である、請求の範 囲第1項の方法。 6 溶液、ローション、クリームまたは軟膏中のナロキソンまたはその医薬的に 受容しうる塩、あるいはナルトレキソンの治療的有効量からなる、組成物07  ナロキソンまたはその医薬的に受容しうる塩、あるいはナルトレキソンが、溶液 、ローション、クリームまたは軟膏中に、約0.01重量%から約5重量%まで の範囲内において存在する、請求の範囲第6項の方法。 8 ナロキソンの医薬的に受容しうる塙が、生理学的に受容しうる酸付加塩であ る、請求の範囲第6項の組成物。 9 酸塩かナロキソン塩酸塩である、請求の範囲第8項の方法。 浄書(内容に変更なし)[Claims] 1. A method for alleviating severe itching in a patient requiring such treatment, naloxone or a pharmaceutically acceptable salt thereof, or therapeutic naltrexone A method comprising administering an effective amount locally to the area in need of such treatment. 2. The naloxone or a pharmaceutically acceptable salt thereof, or naltrexone is , from about 0.01% to about 5% by weight in a solution, lotion, cream or ointment. %. The naloxone or its pharmaceutically acceptable salt, or naltrexone , administered periodically from 1 to 8 times per day to a patient in need of such treatment. , the method of claim 1. 4. The pharmaceutically acceptable salt of naloxone is a physiologically acceptable acid addition salt. The method of claim 1. 5 Claims in which the pharmaceutically acceptable salt of naloxone is naloxone hydrochloride The method described in box 1. 6. Naloxone or its pharmaceutical form in solution, lotion, cream or ointment Composition 07 consisting of an acceptable salt or a therapeutically effective amount of naltrexone Naloxone or its pharmaceutically acceptable salt, or naltrexone, is , in lotions, creams or ointments, from about 0.01% to about 5% by weight. 7. The method of claim 6, lying within the scope of. 8 The pharmaceutically acceptable form of naloxone is a physiologically acceptable acid addition salt. 7. The composition of claim 6. 9. The method of claim 8, wherein the acid salt is naloxone hydrochloride. Engraving (no changes to the content)
JP57502942A 1982-08-25 1982-08-25 Method for treating itch and composition therefor Pending JPS59501712A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1982/001152 WO1984000889A1 (en) 1982-08-25 1982-08-25 Method of treating pruritis and composition therefor

Publications (1)

Publication Number Publication Date
JPS59501712A true JPS59501712A (en) 1984-10-11

Family

ID=22168155

Family Applications (1)

Application Number Title Priority Date Filing Date
JP57502942A Pending JPS59501712A (en) 1982-08-25 1982-08-25 Method for treating itch and composition therefor

Country Status (5)

Country Link
EP (1) EP0116538A4 (en)
JP (1) JPS59501712A (en)
AU (1) AU8952282A (en)
DK (1) DK206584A (en)
WO (1) WO1984000889A1 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009534334A (en) * 2006-04-21 2009-09-24 ディーエスエム アイピー アセッツ ビー.ブイ. Use of opioid receptor antagonists
JP4882744B2 (en) * 2004-03-30 2012-02-22 東レ株式会社 Antidiarrheal

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU201675B (en) * 1983-08-26 1990-12-28 Ivan Balkanyi Process for producing oral pharmaceutical compositions with unappetizing effect
US4626539A (en) * 1984-08-10 1986-12-02 E. I. Dupont De Nemours And Company Trandermal delivery of opioids
US5096715A (en) * 1989-11-20 1992-03-17 Alko Ltd. Method and means for treating alcoholism by extinguishing the alcohol-drinking response using a transdermally administered opiate antagonist
GB9725114D0 (en) * 1997-11-28 1998-01-28 Pfizer Ltd Treatment of pruritus
US20090093509A1 (en) * 2007-10-08 2009-04-09 Tahir Nazir Methods and Compositions for the Treatment of Pruritus
US20140179727A1 (en) 2012-12-14 2014-06-26 Trevi Therapeutics, Inc. Methods for treating pruritus
US8637538B1 (en) 2012-12-14 2014-01-28 Trevi Therapeutics, Inc. Methods for treatment of pruritis
US8987289B2 (en) 2012-12-14 2015-03-24 Trevi Therapeutics, Inc. Methods for treating pruritus
IL318587A (en) 2018-07-23 2025-03-01 Trevi Therapeutics Inc Treatment of chronic cough, breathlessness and dyspnea
CA3166928A1 (en) 2020-01-10 2021-07-15 Trevi Therapeutics, Inc. Methods of administering nalbuphine

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773955A (en) * 1970-08-03 1973-11-20 Bristol Myers Co Analgetic compositions
US4181726A (en) * 1978-11-16 1980-01-01 Bernstein Joel E Method of alleviating pruritis

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4882744B2 (en) * 2004-03-30 2012-02-22 東レ株式会社 Antidiarrheal
JP2009534334A (en) * 2006-04-21 2009-09-24 ディーエスエム アイピー アセッツ ビー.ブイ. Use of opioid receptor antagonists

Also Published As

Publication number Publication date
EP0116538A4 (en) 1985-04-25
WO1984000889A1 (en) 1984-03-15
EP0116538A1 (en) 1984-08-29
AU8952282A (en) 1984-03-29
DK206584D0 (en) 1984-04-25
DK206584A (en) 1984-04-25

Similar Documents

Publication Publication Date Title
JP2728284B2 (en) Hemorrhoids and other therapeutic compositions
US6433003B1 (en) Method for treating hyperhidrosis in mammals
US6524623B1 (en) Therapeutic compositions and methods of use thereof
Hay et al. Tioconazole nail solution—an open study of its efficacy in onychomycosis
DE69017596T2 (en) Use of an opiate antagonist for the production of a medicament to be administered transdermally and a device for transdermal administration.
EP2481747A1 (en) Methods of treating cutaneous flushing using selective alpha-2-adrenergic receptor agonists
JP2002536321A (en) Pharmaceutical composition
DE3023588C2 (en) Use clonidine or its hydrochloride with phentermine to quit smoking
JP2000512996A (en) Preventive and therapeutic measures for skin sensitization and irritation
US4209505A (en) Pilocarpine mouthwash for dry mouth relief
US4369190A (en) Analgesic composition and use thereof to ameliorate intractable pain
JPH01501627A (en) Composition for treating psoriasis
US20120114743A1 (en) Transdermal ricinoleic acid compositions
Schutz et al. Local anaesthetic properties of ambroxol hydrochloride lozenges in view of sore throat
Gupta et al. Intermittent short duration therapy with fluconazole is effective for tinea capitis
US4395420A (en) Method and composition for treating pruritis
Diehl Topical antifungal agents: An update.
EP0116538A1 (en) Method of treating pruritis and composition therefor
US20060205699A1 (en) Topical treatment for psoriasis
JPH01246221A (en) Phenol-containing antitussive agent
US5331012A (en) Topical pharmaceutical preparation for fever blisters and other viral infections and method of use
EP1318801B1 (en) Topical analgesic compositions containing aliphatic polyamines and methods of using same
JPH05194219A (en) Fungicidal agent for topical application
Tigerstedt et al. Comparison of the analgesic dose‐effect relationships of nefopam and oxycodone in postoperative pain
JP2008531640A (en) Antifungal composition comprising sertaconazole and hydrocortisone and / or antibacterial quinolone compound