WO1995022324A1 - Treatment of migraine headaches and formulations - Google Patents
Treatment of migraine headaches and formulations Download PDFInfo
- Publication number
- WO1995022324A1 WO1995022324A1 PCT/US1994/001741 US9401741W WO9522324A1 WO 1995022324 A1 WO1995022324 A1 WO 1995022324A1 US 9401741 W US9401741 W US 9401741W WO 9522324 A1 WO9522324 A1 WO 9522324A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- treatment
- pharmaceutically acceptable
- migraine headaches
- compound
- formulations
- Prior art date
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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
Landscapes
- Health & Medical Sciences (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)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A method of treatment of treating migraine headaches in humans by the administration of the compound of formula (I), or a pharmaceutically acceptable acid addition salt thereof in a non-toxic, effective therapeutic amount (calculated as base) to a human in need thereof.
Description
TREATMENT OF MIGRAINE HEADACHES AND FORMULATIONS
Background of the Invention This invention is directed to a method of treatment of migraine headaches in humans by the administration to the humans of the compound of the formula I
In U.S. Patents 3,819,706 and 3,885,046 m-chloro-α-t-butylaminopropiophenone and salts thereof, in particular the hydrochloride salt, were disclosed on being antidepressants.
Bupropion hydrochloride is the generic name for m-chloro-α-t-butylaminoproxinphenone which is used under the trademark WELLBUTRIN® in the United States of America for the treatment of depressions. The neurochemical mechanism of the antidepressant effect of bupropion is not known.
I have now found that bupropion hydrochloride is effective in treating migraine headaches in humans. It is effective when administered alone or together with caffeine, e.g., with one or two cups of coffee.
The compound of formula (I) (the active ingredient) or the pharmaceutically acceptable acid addition salt thereof is preferably administered in unit dosage form to the human being treated.
A pharmaceutical composition containing a compound of formula (I), or a pharmaceutically acceptable salt thereof, may be presented in discrete units such as tablets, capsules, ampules or suppositories, each containing an effective amount of the compound or salt for treatment of migraine.
As an example, for the treatment of humans having migraines the preferred unit dosage of a compound of formula (I) as the hydrochloride salt thereof for oral administration is about 10 mg to 450 mg, preferably 50 mg to 300 mg, and the most preferred unit dosage of 100 to 200 mg optionally given in divided doses. Treatment is preferably initiated at the first (prodromal) symptom of a migraine.
The compound of formula (I) may also be administered prophylactically, e.g., at a preferred dose of 100 mg per day, especially for patients suffering frequent migraines.
A compound of formula (I) or pharmaceutically acceptable salts thereof may be presented as an oral unit preparation (for example as a cachet, tablet or capsule) containing one or more pharmaceutically
acceptable carriers which may take the form of solid diluents such as lactose, cornstarch, micronized silica gel as well as other excipients known in the art.
It should be understood that in addition to the aforementioned ingredients, the pharmaceutical composition of this invention may include one or more of additional ingredients e.g., pharmaceutically acceptable carriers such as diluents, buffers, flavouring agents, binders, surface active agents, thickeners, lubricants, preservatives, and the like. The formulations may be prepared by admixture of the ingredients, and, if necessary, shaping the resulting mass, and filling into suitable containers.
A preferred pharmaceutical formulation comprises bupropion hydrochloride (100 mg) and caffeine (200 mg) and a pharmaceutically acceptable carrier therefor.
The compound used in this invention is preferably presented for use as a pharmaceutically acceptable acid addition salt. Examples of some of the pharmaceutically acceptable salts which can be utilized are salts of the following acids: hydrochloric, sulfuric, phosphoric and toluenesulphonic.
Reference should be had to U.S. Patents 3,819,706 and 3,885,046, which are incorporated herein by reference hereto for a description of the preparation of the compound of formula (I), acid addition salts thereof, tablets, capsules, parenteral solutions and suppositories incorporating same.
Claims
1. A method of treating migraine in a human suffering from same which comprises administering to said human as effective migraine testing amount of bupropion hydrochloride.
2. A method according to claim 1 wherein an effective amount of caffeine is also administered.
3. A pharmaceutical formulation comprising an effective migraine testing amount of bupropion hydrochloride and caffeine and pharmaceutically acceptable carries therefor.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/693,158 US5753712A (en) | 1994-02-18 | 1994-02-18 | Treatment of migraine headaches and formulations |
| PCT/US1994/001741 WO1995022324A1 (en) | 1994-02-18 | 1994-02-18 | Treatment of migraine headaches and formulations |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US1994/001741 WO1995022324A1 (en) | 1994-02-18 | 1994-02-18 | Treatment of migraine headaches and formulations |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO1995022324A1 true WO1995022324A1 (en) | 1995-08-24 |
Family
ID=22242285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1994/001741 WO1995022324A1 (en) | 1994-02-18 | 1994-02-18 | Treatment of migraine headaches and formulations |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO1995022324A1 (en) |
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6110973A (en) * | 1998-01-29 | 2000-08-29 | Sepracor | Methods for treating obesity and weight gain using optically pure (-)-bupropion |
| US6280763B1 (en) | 1999-05-10 | 2001-08-28 | Pierce Management, Llc | Apparatus and method for transdermal delivery of bupropion |
| US6337328B1 (en) | 1999-03-01 | 2002-01-08 | Sepracor, Inc. | Bupropion metabolites and methods of use |
| US6342496B1 (en) | 1999-03-01 | 2002-01-29 | Sepracor Inc. | Bupropion metabolites and methods of use |
| US6458374B1 (en) | 1998-01-29 | 2002-10-01 | Sepracor, Inc. | Methods and compositions for treating chronic disorders using optically pure (+)-bupropion |
| US6734213B2 (en) | 1999-01-20 | 2004-05-11 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US6855820B2 (en) | 1999-01-20 | 2005-02-15 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US6998400B2 (en) | 1998-01-22 | 2006-02-14 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US7098206B2 (en) | 1998-01-21 | 2006-08-29 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3819706A (en) * | 1969-12-04 | 1974-06-25 | Burroughs Wellcome Co | Meta chloro substituted-alpha-butylamino-propiophenones |
| US3885046A (en) * | 1969-12-04 | 1975-05-20 | Burroughs Wellcome Co | Meta chloro or fluoro substituted alpha-T-butylaminopropionphenones in the treatment of depression |
-
1994
- 1994-02-18 WO PCT/US1994/001741 patent/WO1995022324A1/en active Application Filing
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3819706A (en) * | 1969-12-04 | 1974-06-25 | Burroughs Wellcome Co | Meta chloro substituted-alpha-butylamino-propiophenones |
| US3885046A (en) * | 1969-12-04 | 1975-05-20 | Burroughs Wellcome Co | Meta chloro or fluoro substituted alpha-T-butylaminopropionphenones in the treatment of depression |
Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7098206B2 (en) | 1998-01-21 | 2006-08-29 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US6998400B2 (en) | 1998-01-22 | 2006-02-14 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US6495605B2 (en) | 1998-01-29 | 2002-12-17 | Sepracor Inc. | Methods and compositions for aiding in smoking cessation and for treating pain and other disorders using optically pure (+)-bupropion |
| US6277887B1 (en) | 1998-01-29 | 2001-08-21 | Sepracor, Inc. | Methods for treating Parkinson's disease using optically pure (−)-bupropion |
| US6110973A (en) * | 1998-01-29 | 2000-08-29 | Sepracor | Methods for treating obesity and weight gain using optically pure (-)-bupropion |
| US6369113B2 (en) | 1998-01-29 | 2002-04-09 | Sepracor, Inc. | Method for treating depression using optically pure (−)-bupropion |
| US6451860B1 (en) | 1998-01-29 | 2002-09-17 | Sepracor, Inc. | Methods for treating depression and other disorders using optically pure (−)-bupropion |
| US6458374B1 (en) | 1998-01-29 | 2002-10-01 | Sepracor, Inc. | Methods and compositions for treating chronic disorders using optically pure (+)-bupropion |
| US6734213B2 (en) | 1999-01-20 | 2004-05-11 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US6855820B2 (en) | 1999-01-20 | 2005-02-15 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US6342496B1 (en) | 1999-03-01 | 2002-01-29 | Sepracor Inc. | Bupropion metabolites and methods of use |
| US6337328B1 (en) | 1999-03-01 | 2002-01-08 | Sepracor, Inc. | Bupropion metabolites and methods of use |
| US6280763B1 (en) | 1999-05-10 | 2001-08-28 | Pierce Management, Llc | Apparatus and method for transdermal delivery of bupropion |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US5753712A (en) | Treatment of migraine headaches and formulations | |
| US4507323A (en) | Treatment of psychosexual dysfunctions | |
| HU225534B1 (en) | Pharmaceutical compositions comprising mirtazapine and one or more selective serotonin reuptake inhibitors | |
| JPH06102622B2 (en) | Treatment of obesity | |
| US4590213A (en) | Anti-anxiety method | |
| US4435449A (en) | Treatment of minimal brain dysfunction (MBD) | |
| US4438138A (en) | Reduction of cholesterol with meta-chloro α-t-butylaminopropiophenone | |
| KR20010015918A (en) | Fluoxetine Hydrochloride for Decreasing Hot Flashes | |
| RU2003100507A (en) | PHARMACEUTICAL COMPOSITIONS | |
| WO1995022324A1 (en) | Treatment of migraine headaches and formulations | |
| EP0629400B1 (en) | Idebenone compositions for treating Alzheimer's disease | |
| EP0171227B1 (en) | Use of propiophenone compound | |
| JPH03170475A (en) | Therapeutic agent for combating depression | |
| US6413993B1 (en) | Combination preparation for treating malaria | |
| JP2588191B2 (en) | Therapeutic agent for improving neurological symptoms associated with malignant tumors and severe viral infections | |
| WO2001093850B1 (en) | Methods and compositions using sulodexide for the treatment of diabetic nephropathy | |
| Saalbach et al. | Antihypertensive efficacy, tolerance, and safety of ramipril in young vs. old patients: a retrospective study | |
| CA2183539A1 (en) | Treatment of migraine headaches and formulations | |
| IE55181B1 (en) | Treatment of minimal brain dysfunction(mbd) | |
| HUT53526A (en) | Process for production of medical compositions suitable for treatment of dislipidemia | |
| US4701467A (en) | Tolrestat as anti-hypertensive agent | |
| US4716177A (en) | Tolrestat for inhibition of weight gain | |
| CA2456721A1 (en) | Pharmaceutical composition comprising salmeterol and budesonide for the treatment of respiratory disorders | |
| JP2001089375A (en) | Composition for common cold | |
| JPH06102624B2 (en) | Anti-arrhythmic drugs of non-heart origin |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| AK | Designated states |
Kind code of ref document: A1 Designated state(s): CA US |
|
| DFPE | Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101) | ||
| WWE | Wipo information: entry into national phase |
Ref document number: 2183539 Country of ref document: CA |
|
| WWE | Wipo information: entry into national phase |
Ref document number: 08693158 Country of ref document: US |