Note: Descriptions are shown in the official language in which they were submitted.
3~
The present invention relates to a composition
for relieving pruritis.
Itching or pruritis is a common dermatologic
symptom. The causes of pruritis are complex and poorly
5 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
10 produced by antihistaminic agents limits their ef~ectiveness.
Many kinds of itching are not however easily re-
lieved by antihistamines. For example, conditions such
as Hodgkinls Disease, mycosis fungoides (cutaneous malig~
nacy) and severe jaundice produce intense itching unrelieved
15 by antihistamines. Therefore, there is a need for improved
treatment to relieve severe itching which can not only be
an alternative to antihlstaminic treatment of itching due
to such causes as mos~uitoe bites which responds to such
treatm~nt, but which further provides relief in intractable
20 cases of pruritis which heretofore have been virtually im-
possible to treat except as disclosed in U. S. Patent No.
4,181,~26 which relates to a method based on the systemic
effects on the central nervous system.
The object of the present invention is to provide
25 ~or treating pruritis which acts independent of systemic
effects on the central nervous system.
.
. ..
-- 2
The presen-t invention provides a composi-tion
for re]ieveing pruritls comprising a therapeutically ef-
fective amount of Naloxone*or a pharmaceutically acceptable
salt thereof of Naltrexone*in a solution, lotion, cream
5 or ointment.
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
10 to addicts to assist them in narcotic withdrawal and some-
times is administered to post operative patients for partial
reversal of narcotic depression following the use of nar-
cotics during surgery.
It has been ~ound surprisingly that topical ap-
15 plications of Naloxone are useful in alleviating sevexeitching in various conditions.
Naloxone hydrochloride is commercially available
from Endo Laboratories, Inc., a subsidiary of the DuPont
Company, 1000 Stewart Avenue, Garden City, New York 11530.
20 The preparation of Naloxone is disclosed in U. S. Patent
~o. 3,254,088.
The term pharmaceutically acceptable salts, as
- used herein, re~ers to the physiologically acceptable acid
addition salts of Naloxone such as the hydrochloride,
25 hydrobxomide! hydroiodide, ace-tate, valerate, oleate, etc.
Liquid dosage forms for topical administration
includes acceptable emulsions, solutions and suspensions
containiny volatile diluents commonly used in the art,
such as alcohol, glycol and the liXe. Besides such
30 diluents, topically applied compositions may also include
wetting agents, emulsifying and suspending agents.
In the practice o~ this invention Naloxone ln
*Trade ~lark
' .,~
-the form of a pharmaceutically acceptable sal-t such as
the hydrochloride and pharmaceutically acceptable chem-
ical derivatives thereo~ 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.
EXAMPLE l
1 percent by weight Naloxone hydrochloride
was incorporated into a solution eomposed of 70 percent
by volume ethyl aleohol and 30 percent by volume propylene
glyeol 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 lO minutes
of eaeh applieation and the relief lasted ~-4 hours.
EXAMPLE 2
~o A 0.05% by weight Naloxone hydroehloride was
incorporated into Eucerin (R.T.M.) eream and applied 4
times daily to the body of a 60 year-old male with in-
tractable itehing due to mycosis fungoides. Eueerin
(R.T.M.) cream is a synthetie lanolin containing cream
produced by Beiersdorf, Inc. of South Norwalk, Conneetieut
06854. This was the first topical product the patient
used that provided him with any signifieant relief from
his itching.
EXAMPLE 3
An ointment composed chiefly of petrolatum
and containing 0.01% by weight Naloxone hydrochloride
was applied 4 times daily to the body of a 60 year-old
male with mycosis fungoides. Itching was diminished,
although not as much as with the higher eoncentration of
Naloxone in Example 2.
. 4 _
EXAMPI,E 4
0.1% by we:ight Naloxone hydrochloride was
incorporated into a zinc shake lotion and applied to
the mosquitoe bites of a 6 year-old girl durlng a
5 one month five interval in the summer. This lotion
provided excellent relief from the itching.
EXAMPLE 5
5~ by weight Maloxone hydrochloride was incor-
porated into an ointment and applied 4 times daily for
10 two days to a small ec2ematous patch on the left hand
of a 38 year-old male. Itching was dramatically re-
duced by each application of the -test ointmentO
