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

Definitions

• the present invention relates to a composition for relieving pruritis.
• pruritis Itching or pruritis is a common dermatologi ⁇ symptom. ⁇ p ne causes of pruritis are complex and poorly understood. The best understood mechanism of itching is the release of histamine in the skin leading to urticarial wheals-and intense itching. Such itching has traditionally been relieved by antihistamines. While antihistamine therapy is often effective, the sedation and drowsiness produced by antihistaminic agents limits their effectiveness.
• Naloxone is a narcotic antagonist which is not known to cause physical or psychological dependence and which exhibits essentially no pharmacological activity in non-addicts. Naloxone is normally given by injection to addicts to assist them in narcotic with ⁇ drawal and"sometimes is administered to post operative patients for partial reversal of narcotic depression following the use of narcotics during surgery. It has been found surprisingly that topical " applications of Naloxone are useful in alleviating severe itching in various conditions.
• the present invention provides a method for relieving severe itching in patients in need of such treatment, said method comprising topically administer ⁇ ing a therapeutically effective amount of Naloxone or a pharmaceutically acceptable salt thereof or Naltrex- one to a patient in need of such treatment.
• Naloxone hydrochloride is commercially avail- able from Endo Laboratories, Inc., a subsidiary of the DuPont Company, 1000 Stewart Avenue, Garden City, New York 11530.
• the preparation of Naloxone is disclosed in U.S. Patent No. 3,254,088.
• pharmaceutically acceptable salts refers to the physiologically acceptable acid addition salts of Naloxone such as the hydrochloride, hydrobromide, hydroiodide, acetate, valerate, oleate, etc.
• Liquid dosage forms for topical administra- tion includes acceptable emulsions, solutions and sus ⁇ pensions containing volatile diluents commonly used in the art, such as alcohol, glycol and the like. Besides such diluents, topically applied compositions may also include wetting agents, emulsifying and suspending agents.
• & JREA the form of a pharmaceutically acceptable salt such as the hydrochloride and pharmaceutically acceptable chemical derivatives thereof such as Naltrexone which is the n-methyl cyclopropyl derivative are incorporated into solutions, lotions, creams, and ointments for topical application in concentrations of from 0.01 to about 5 percent by weight. These topical products are applied to the skin 1 to 8 times daily. The relief experienced by those receiving the topical application was prompt although temporary.
• Naloxone hydrochloride 1 percent by weight Naloxone hydrochloride was incorporated into a solution composed of 70 percent by volume ethyl alcohol and 30 percent by volume propylene glycol and applied 6 times daily to 2 mosquito bites of less than 24 hours duration on an 11 year-old male. This child noted relief from his itching within 10 minutes of each application and the relief lasted 2-4 hours.
• Eucerin (R.T.M) cream is a synthetic lanolin containing cream produced by Beiersdorf, Inc. of South Norwalk, Conneticut 06854. This was the first topical product the patient used that provided him with any significant relief from his itching.
• Naloxone hydrochloride 5% by weight Naloxone hydrochloride was in ⁇ corporated into an ointment and applied 4 times daily for two days to a small eczematous patch on the left hand of a 38 hear-old male. Itching was dramatically reduced by each application of the test ointment.

Landscapes

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

Priority Applications (5)

Applications Claiming Priority (1)

Publications (1)

Family

ID=22168155

Family Applications (1)

Country Status (5)

Cited By (8)

Families Citing this family (3)

Citations (2)

• 1982
  • 1982-08-25 EP EP19820902866 patent/EP0116538A4/en not_active Withdrawn
  • 1982-08-25 WO PCT/US1982/001152 patent/WO1984000889A1/en not_active Application Discontinuation
  • 1982-08-25 AU AU89522/82A patent/AU8952282A/en not_active Abandoned
  • 1982-08-25 JP JP50294282A patent/JPS59501712A/ja active Pending
• 1984
  • 1984-04-25 DK DK206584A patent/DK206584A/da not_active Application Discontinuation

Patent Citations (2)

Non-Patent Citations (2)

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