CA2019797A1 - Method and composition for treating nasal disorders and headaches - Google Patents
Method and composition for treating nasal disorders and headachesInfo
- Publication number
- CA2019797A1 CA2019797A1 CA 2019797 CA2019797A CA2019797A1 CA 2019797 A1 CA2019797 A1 CA 2019797A1 CA 2019797 CA2019797 CA 2019797 CA 2019797 A CA2019797 A CA 2019797A CA 2019797 A1 CA2019797 A1 CA 2019797A1
- Authority
- CA
- Canada
- Prior art keywords
- solution
- composition
- suspension
- effective amount
- therapeutically effective
- 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.)
- Abandoned
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 13
- 206010019233 Headaches Diseases 0.000 title claims abstract description 9
- 231100000869 headache Toxicity 0.000 title claims abstract description 9
- 208000026344 Nasal disease Diseases 0.000 title claims 2
- 208000030880 Nose disease Diseases 0.000 title claims 2
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 claims abstract description 48
- 229960002504 capsaicin Drugs 0.000 claims abstract description 24
- 235000017663 capsaicin Nutrition 0.000 claims abstract description 24
- 230000000699 topical effect Effects 0.000 claims abstract description 11
- 239000000739 antihistaminic agent Substances 0.000 claims abstract description 7
- 239000003589 local anesthetic agent Substances 0.000 claims abstract description 7
- 150000003431 steroids Chemical class 0.000 claims abstract description 7
- 208000024891 symptom Diseases 0.000 claims abstract description 7
- 239000000725 suspension Substances 0.000 claims abstract 13
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims abstract 6
- 230000001387 anti-histamine Effects 0.000 claims abstract 6
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 claims description 7
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 claims description 6
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 5
- 229960004194 lidocaine Drugs 0.000 claims description 5
- 229960005274 benzocaine Drugs 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 229960004311 betamethasone valerate Drugs 0.000 claims description 3
- SNHRLVCMMWUAJD-SUYDQAKGSA-N betamethasone valerate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O SNHRLVCMMWUAJD-SUYDQAKGSA-N 0.000 claims description 3
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical group C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 claims description 3
- 229960000520 diphenhydramine Drugs 0.000 claims description 3
- ODQWQRRAPPTVAG-GZTJUZNOSA-N doxepin Chemical group C1OC2=CC=CC=C2C(=C/CCN(C)C)/C2=CC=CC=C21 ODQWQRRAPPTVAG-GZTJUZNOSA-N 0.000 claims description 3
- 229960005426 doxepin Drugs 0.000 claims description 3
- 230000000172 allergic effect Effects 0.000 claims description 2
- 208000010668 atopic eczema Diseases 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 229960000890 hydrocortisone Drugs 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 230000007815 allergy Effects 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 description 8
- 210000001331 nose Anatomy 0.000 description 5
- 206010041232 sneezing Diseases 0.000 description 5
- 239000006196 drop Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 235000002566 Capsicum Nutrition 0.000 description 3
- 241000722363 Piper Species 0.000 description 3
- 206010039085 Rhinitis allergic Diseases 0.000 description 3
- 201000010105 allergic rhinitis Diseases 0.000 description 3
- 229940100662 nasal drops Drugs 0.000 description 3
- 229940100656 nasal solution Drugs 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
- 206010052437 Nasal discomfort Diseases 0.000 description 2
- 239000006002 Pepper Substances 0.000 description 2
- 235000016761 Piper aduncum Nutrition 0.000 description 2
- 235000017804 Piper guineense Nutrition 0.000 description 2
- 235000008184 Piper nigrum Nutrition 0.000 description 2
- 229960000631 hydrocortisone valerate Drugs 0.000 description 2
- 210000002850 nasal mucosa Anatomy 0.000 description 2
- 208000001319 vasomotor rhinitis Diseases 0.000 description 2
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 244000036975 Ambrosia artemisiifolia Species 0.000 description 1
- 235000003129 Ambrosia artemisiifolia var elatior Nutrition 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- 208000000059 Dyspnea Diseases 0.000 description 1
- 206010013975 Dyspnoeas Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 206010028735 Nasal congestion Diseases 0.000 description 1
- 241000758706 Piperaceae Species 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 206010051496 Rhinalgia Diseases 0.000 description 1
- 241000208292 Solanaceae Species 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- KRMDCWKBEZIMAB-UHFFFAOYSA-N amitriptyline Chemical compound C1CC2=CC=CC=C2C(=CCCN(C)C)C2=CC=CC=C21 KRMDCWKBEZIMAB-UHFFFAOYSA-N 0.000 description 1
- 229960000836 amitriptyline Drugs 0.000 description 1
- 230000003444 anaesthetic effect Effects 0.000 description 1
- 229940035674 anesthetics Drugs 0.000 description 1
- 235000003484 annual ragweed Nutrition 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 235000006263 bur ragweed Nutrition 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 235000003488 common ragweed Nutrition 0.000 description 1
- 208000027744 congestion Diseases 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- 230000003292 diminished effect Effects 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 239000003193 general anesthetic agent Substances 0.000 description 1
- 229960001340 histamine Drugs 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 235000009736 ragweed Nutrition 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 230000001932 seasonal effect Effects 0.000 description 1
- 208000018316 severe headache Diseases 0.000 description 1
- 208000013220 shortness of breath Diseases 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
Abstract of the Disclosure Compositions and methods for treating the symptoms of certain allergy-related conditions using capsaicin in solution or suspension combined with a selected local anesthetic, topical steroid or antihistamine. The same methods and compositions may be used to treat headaches.
Description
2~7~
MET~IOD AND COMPO~;ITIO~ FOR T~EATING
NASAL D ISORDERS Al\~D ~lEADACElES
Backqround of the Invention Capsaicin is a chemical isolated from the fruits of plants of the nightshade family, principally the pepper plant. It requires processing of about 10,000 pounds of peppers to extract a yield of 1 pound of capsaicin. Capsaicin has in recent years been used topically on the skin to treat psoriasis and to relieve certain types of superficial pain.
Ground pepper, containing capsaicin, has long been utilized by magicians and tricksters as "sneezing powder". It affects the nose and airway passages of the respitory system by causing intense irritation, producing vigorous sneezing and coughing and, if exposure is extreme, shortness of breath. Additionally, direct exposure of pepper to the mucosa of the nose may result in intense local pain, and not uncommonly, severe headache.
It has been discovered that capsaicin, when applied repeatedly locally to the nasal mucosa or directed to the respiratory passages can produce quite contrary and surprising effects.
In particular, it has been found that capsaicin has beneficial effects in treating the symptoms of vasomotor rhinitis, commonly encountered throughout the year, and allergic rhinitis encounterea during the ragweed and mold season. It was noticed that a person suffering from these conditions, while working with capsaicin powder, inhaled relatively large amounts of the powder over a several day period, causing intense burning pain and sneezing. This was followed several hours later by an intense .~ ~ 201~P~7 headache involving the tempero-frontal areas. On the second day of exposure to the powder, the foregoing symptoms were similar, but less intense. After four days of exposure, the subject no longer experienced the intense nasal pain, sneezing, or headache, but noticed that congestion fro~ vasomotor rhinitis was no longer apparent. Indeed for the next few days, the subject experienced substantially less of his usual seasonal nasal discomfort.
On the basis of these results, solutions of capsaicin were prepared for introduction into the nose to treat allergic and other inflammatory disorders of the nose as well as to prevent or treat headaches. In introducing such drops into the nasal passages of several test subjects it was discovered that the capsaicin drops could produce intense almost unbearable pain in the naive patient. Several types of other agents were then incorporated into the foemulation along with the capsaicin to relieve this adverse reaction to the capsaicin nose drops. In the course of trying to reduce this aaverse capsaicin effect, the topical anesthetics lidocaine (Entry 5310, p. 786, herck Index, Tenth Edition 1983~ and benzocaine (ethyl aminobenzoate, Entry 3710, p. 546, herck Index, Tenth Edition 1983~ , the topical steroids hydrocortisone and betamethasone valerate and the histamine blockers diphenhydramine, doxepin and amitriptyline were used.
. .
It was discovere~ that the topical anesthetics lidocaine and benzocaine, in concentrations of from about 0.5~ to about 20%
were most effective in preventing the intense burning pain of the nasal mucosa induced by capsaicin. ~opical steriods and anihistamines appeared to reduce the burning effects of capsaicin, but to a lesser degree than the anesthetics.
Detailed Description of the Invention In the practice of this invention nose drops are prepared by introducing capsaicin into a pharmaceutically acceptable carrier in concentrations from about 0.001~ to about 1.0% by weight, and the resulting composition is used to treat or prevent inflammations of the nose (such as from allergic rhinitis~ as well as to treat or prevent severe recurring headaches. Because these drops may produce initial pain of an unbearable type, in the preferred practice of this invention, from about 0.5% to about 20%
by weight of a topical anesthetic such as lidocaine or ben~ocaine are included in the preparation to reduce the intial discomfort that the capsaicin drops may produce. Corticosteroids, such as hydrocortisone or betamethasone valerate or antihistamines such as doxepin or diphenhydramine may also be incorporated into the nasal drops to reduce the symptoms of discomfort produced, with the corticosteriods being present in concentrations of about 0.05%
to about 5.0%.
Use of this- invention is illustrated by the following examples.
EXA~PLE 1 A 44 year old male with allergic rhinitis and accompanying headaches was treated with a nasal solution containing 0.025~
capsaicin. The nasal solution was instilled four times daily. On the first 2 days introduction of the nasal solutions produced burning pain and sneezing. ~owever, after 3 days these effects diminished and after 7 days of continued capsaicin application to the nasal passages, the patient no longer experienced episodes of nasal congestion, snee~ing, or hea~aches.
The 44 year old patient described in Example 1 was treated with a nasal solution containing 0.025% capsaicin and 10~
lidocaine. This solution produced similar relief of the patient's symptoms as in Example 1 above, with only mild nasal discomfort during the first few days of capsaicin application.
While the foregoing has presentea certain specific embodiments of the invention, it is to be understood that such have been made by way of example only and are not intended to limit the scope of the invention as herein described and claimed.
It is expected that others will perceive variations which, while differing from the foregoing, do not depart from the spirit and scope of the invention.
MET~IOD AND COMPO~;ITIO~ FOR T~EATING
NASAL D ISORDERS Al\~D ~lEADACElES
Backqround of the Invention Capsaicin is a chemical isolated from the fruits of plants of the nightshade family, principally the pepper plant. It requires processing of about 10,000 pounds of peppers to extract a yield of 1 pound of capsaicin. Capsaicin has in recent years been used topically on the skin to treat psoriasis and to relieve certain types of superficial pain.
Ground pepper, containing capsaicin, has long been utilized by magicians and tricksters as "sneezing powder". It affects the nose and airway passages of the respitory system by causing intense irritation, producing vigorous sneezing and coughing and, if exposure is extreme, shortness of breath. Additionally, direct exposure of pepper to the mucosa of the nose may result in intense local pain, and not uncommonly, severe headache.
It has been discovered that capsaicin, when applied repeatedly locally to the nasal mucosa or directed to the respiratory passages can produce quite contrary and surprising effects.
In particular, it has been found that capsaicin has beneficial effects in treating the symptoms of vasomotor rhinitis, commonly encountered throughout the year, and allergic rhinitis encounterea during the ragweed and mold season. It was noticed that a person suffering from these conditions, while working with capsaicin powder, inhaled relatively large amounts of the powder over a several day period, causing intense burning pain and sneezing. This was followed several hours later by an intense .~ ~ 201~P~7 headache involving the tempero-frontal areas. On the second day of exposure to the powder, the foregoing symptoms were similar, but less intense. After four days of exposure, the subject no longer experienced the intense nasal pain, sneezing, or headache, but noticed that congestion fro~ vasomotor rhinitis was no longer apparent. Indeed for the next few days, the subject experienced substantially less of his usual seasonal nasal discomfort.
On the basis of these results, solutions of capsaicin were prepared for introduction into the nose to treat allergic and other inflammatory disorders of the nose as well as to prevent or treat headaches. In introducing such drops into the nasal passages of several test subjects it was discovered that the capsaicin drops could produce intense almost unbearable pain in the naive patient. Several types of other agents were then incorporated into the foemulation along with the capsaicin to relieve this adverse reaction to the capsaicin nose drops. In the course of trying to reduce this aaverse capsaicin effect, the topical anesthetics lidocaine (Entry 5310, p. 786, herck Index, Tenth Edition 1983~ and benzocaine (ethyl aminobenzoate, Entry 3710, p. 546, herck Index, Tenth Edition 1983~ , the topical steroids hydrocortisone and betamethasone valerate and the histamine blockers diphenhydramine, doxepin and amitriptyline were used.
. .
It was discovere~ that the topical anesthetics lidocaine and benzocaine, in concentrations of from about 0.5~ to about 20%
were most effective in preventing the intense burning pain of the nasal mucosa induced by capsaicin. ~opical steriods and anihistamines appeared to reduce the burning effects of capsaicin, but to a lesser degree than the anesthetics.
Detailed Description of the Invention In the practice of this invention nose drops are prepared by introducing capsaicin into a pharmaceutically acceptable carrier in concentrations from about 0.001~ to about 1.0% by weight, and the resulting composition is used to treat or prevent inflammations of the nose (such as from allergic rhinitis~ as well as to treat or prevent severe recurring headaches. Because these drops may produce initial pain of an unbearable type, in the preferred practice of this invention, from about 0.5% to about 20%
by weight of a topical anesthetic such as lidocaine or ben~ocaine are included in the preparation to reduce the intial discomfort that the capsaicin drops may produce. Corticosteroids, such as hydrocortisone or betamethasone valerate or antihistamines such as doxepin or diphenhydramine may also be incorporated into the nasal drops to reduce the symptoms of discomfort produced, with the corticosteriods being present in concentrations of about 0.05%
to about 5.0%.
Use of this- invention is illustrated by the following examples.
EXA~PLE 1 A 44 year old male with allergic rhinitis and accompanying headaches was treated with a nasal solution containing 0.025~
capsaicin. The nasal solution was instilled four times daily. On the first 2 days introduction of the nasal solutions produced burning pain and sneezing. ~owever, after 3 days these effects diminished and after 7 days of continued capsaicin application to the nasal passages, the patient no longer experienced episodes of nasal congestion, snee~ing, or hea~aches.
The 44 year old patient described in Example 1 was treated with a nasal solution containing 0.025% capsaicin and 10~
lidocaine. This solution produced similar relief of the patient's symptoms as in Example 1 above, with only mild nasal discomfort during the first few days of capsaicin application.
While the foregoing has presentea certain specific embodiments of the invention, it is to be understood that such have been made by way of example only and are not intended to limit the scope of the invention as herein described and claimed.
It is expected that others will perceive variations which, while differing from the foregoing, do not depart from the spirit and scope of the invention.
Claims (17)
1. A composition for treating the symptoms or nasal disorders and headaches, said composition comprising:
a solution or suspension formulated from a pharmaceutically acceptable carrier for instillation into the nose, said solution or suspension containing capsaicin in concentrations from about .001% to about 1% by weight.
a solution or suspension formulated from a pharmaceutically acceptable carrier for instillation into the nose, said solution or suspension containing capsaicin in concentrations from about .001% to about 1% by weight.
2. The compositon of Claim 1, including a pharmaceutically acceptable local anesthetic in concentrations from about 0.5% to about 20% by weight.
3. The composition of Claim 2 wherein said local anesthetic is selected from the group comprising lidocaine or benzocaine.
4. The composition of Claim 1 including a topical steroid.
5. The composition of Claim 4, wherein said topical steroid is hydrocortisone in concentrations from about 1.0% to about 5.0% by weight.
6. The composition of Claim 4 wherein said topical steroid is betamethasone valerate in concentrations from about 0.05 to about 0.2% by weight.
7. The composition Claim 1 including a topical antihistamine.
8. The composition of Claim 7 wherein said topical antihistamine is doxepin in concentrations from about 1.0%
to about 5.0% by weight.
to about 5.0% by weight.
9. The composition of Claim 7 wherein said topical antihistamine is diphenhydramine in concentrations of from about 5.0% to about 10.0% by weight.
10. A method of preventing or treating the symptoms of allergic and other inflammatory disorders of the nose, said method comprising the steps of:
(a) preparing a solution or suspension containing a therapeutically effective amount of capsaicin combined with a pharmaceutically acceptable carrier; and (b) instilling said solution or suspension into the nasal passages.
(a) preparing a solution or suspension containing a therapeutically effective amount of capsaicin combined with a pharmaceutically acceptable carrier; and (b) instilling said solution or suspension into the nasal passages.
11. The method of Claim 10 including the step of adding a therapeutically effective amount of a local anesthetic to said solution or suspension prior to carrying out step (b).
12. The method of Claim 10 including the step of adding a therapeutically effective amount of a topical steroid to said solution or suspension prior to carrying out step (b).
13. The method of Claim 10 including the step of adding a therapeutically effective amount of an antihistamine to said solution or suspension prior to carrying out step (b).
14. A method of preventing or treating headaches, said method comprising the steps of:
(a) preparing a solution or suspension of a therapeutically effective amount of capsaicin combined with a pharmaceutically acceptable carrier; and (b) instilling said solution or suspension into the nasal passages.
(a) preparing a solution or suspension of a therapeutically effective amount of capsaicin combined with a pharmaceutically acceptable carrier; and (b) instilling said solution or suspension into the nasal passages.
15. The method of Claim 14 including the step of adding a therapeutically effective amount of a local anesthetic to said solution or suspension prior to carrying out step (b).
16. The method of Claim Claim 14 including the step of adding a therapeutically effective amount of a topical steroid to said solution or suspension prior to carrying out step (b).
17. The method of Claim 14 including the step of adding a therapeutically effective amount of an antihistamine to said solution or suspension prior to carrying out step (b).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA 2019797 CA2019797A1 (en) | 1990-06-26 | 1990-06-26 | Method and composition for treating nasal disorders and headaches |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA 2019797 CA2019797A1 (en) | 1990-06-26 | 1990-06-26 | Method and composition for treating nasal disorders and headaches |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2019797A1 true CA2019797A1 (en) | 1991-12-26 |
Family
ID=4145331
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA 2019797 Abandoned CA2019797A1 (en) | 1990-06-26 | 1990-06-26 | Method and composition for treating nasal disorders and headaches |
Country Status (1)
| Country | Link |
|---|---|
| CA (1) | CA2019797A1 (en) |
-
1990
- 1990-06-26 CA CA 2019797 patent/CA2019797A1/en not_active Abandoned
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Dead |