WO2001043730A2 - The treatment of convulsive states - Google Patents
The treatment of convulsive states Download PDFInfo
- Publication number
- WO2001043730A2 WO2001043730A2 PCT/GB2000/004838 GB0004838W WO0143730A2 WO 2001043730 A2 WO2001043730 A2 WO 2001043730A2 GB 0004838 W GB0004838 W GB 0004838W WO 0143730 A2 WO0143730 A2 WO 0143730A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- mph
- found
- therapy
- treatment
- enantiomer
- 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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4458—Non condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
Definitions
- This invention relates to the treatment of epilepsy and other convulsive states, bipolar disorder and narcolepsy.
- Epili ® sodium valproate
- liver dysfunction including hepatic failure which has resulted in death, and has been found to interact with other drugs such as monoamine oxidase inhibitors.
- Drowsiness and sedation are among the side-effects on the CNS that have been noted for Epanutin ®
- Ther. 24:152-158 (1987) indicates that the pharmacological action of d, 1-MPH in the treatment of attention-deficit hyperactivity disorder (ADHD) is the property of the d-enantiomer (d-MPH), as no action on the part of the 1-enantiomer (1-MPH) has been detected; see also Srinivas et al , Clin. Pharm. Ther. 52:561-8 (1992). It has also been found that, following oral dosing, the 1-enantiomer is metabolised preferentially, such that plasma levels of the d-enantiomer are generally found to be higher than those of the 1-enantiomer (Aoyama et al , Eur . J. Clin. Pharm.
- WO-A-99/30694 discloses the topical application of d, 1-MPH, using substantially zero order kinetics.
- An example of a topical composition comprises the drug in an adhesive base.
- a topical composition comprises 1-MPH and a suitable carrier.
- the 1-enantiomer possesses pharmacological activity broadly similar to that of the d-enantiomer and the racemate .
- the two enantiomers and the racemate induced similar stimulant effects in the
- Irwin Observation Test including mainly excitation with signs of hypersensitivity to external stimulation, stereotypies with fore-paw treading, myd ⁇ asis and hyperthermia .
- the 1-enantiomer was found to possess anticonvulsant activity m an animal model, the Pentylenetetrazole (PTZ) Seizure Test, a property which was not shown by the d-enantiomer .
- PTZ Pentylenetetrazole
- Topical application of drugs provides many advantages over conventional oral administration. Advantages include convenience, uninterrupted therapy, improved patient compliance, ease of discontinuation, elimination of presystemic metabolism, a high degree of control over blood concentration of the drug and improved overall therapy.
- the 1-MPH may be administered by the same means as is known for d, 2-MPH, e.g. as described m O-A-99/30694. In this way, substantially zero order kinetics, for delivery to the skin or mucosa, over a period of at least 10 hours, may be achieved.
- the 1-MPH may also be administered by any other conventional topical application method at any anatomical site. Conventional dosing parameters may be adopted, i.e. those which are known to or adapted to the practice of those skilled m the art.
- Known topical formulations comprise emulsions, suspensions, solutions, creams, ointments and many other, with or without a vehicle such as a subcutaneous implant, suppository, patch or applicator.
- a vehicle such as a subcutaneous implant, suppository, patch or applicator.
- the most appropriate formulation and its delivery will be apparent to, or can readily be determined by, one skilled m the art.
- the appropriate dosage can be determined, having regards to conventional factors such as the condition of the patient, the severity of the illness, the number and type of applications, etc.
- a typical dosage might comprise 10 to 200 mg 2-MPH, to be applied 1-2 times per day.
- the 2-MPH will usually be used m substantially single enantiomer form, e.g. m at least 90%, preferably at least 95%, and most preferably at least 98% ee, with respect to d-MPH.
- Methods for preparing the active component used m this invention are known.
- Hyperthermia and mydriasis were evaluated by comparison of the mean scores obtained in treated and control animals.
- Tables 2a and 2b shows the effects of 2-MPH, Ro 15- 4513 (positive control, proconvulsant ) and Diazepam (positive control, anticonvulsant) in the PTZ test, using 10 rats per group.
- Table 2b reports results observed during 60 minutes. In these Tables:
- Table 3 shows the results of the barbital-interaction sleep induction test, again using 10 rats per group, for 1- MPH and also d-MPH, d, 1-MPH and caffeine.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Hydrogenated Pyridines (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
Claims
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU21999/01A AU2199901A (en) | 1999-12-17 | 2000-12-15 | The treatment of convulsive states |
US10/148,535 US7384959B2 (en) | 1999-12-17 | 2000-12-15 | Treatment of convulsive states |
EP00985589A EP1239858B1 (en) | 1999-12-17 | 2000-12-15 | Pharmaceutical for the treatment of convulsive states |
AT00985589T ATE252903T1 (en) | 1999-12-17 | 2000-12-15 | MEDICINAL PRODUCTS FOR THE TREATMENT OF CONVULSIVE CONDITIONS |
DE60006284T DE60006284T2 (en) | 1999-12-17 | 2000-12-15 | MEDICINAL PRODUCTS FOR TREATING CONVULSIVE STATES |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB9929981.0A GB9929981D0 (en) | 1999-12-17 | 1999-12-17 | The treatment of convulsive states |
GB9929981.0 | 1999-12-17 | ||
GB0019061.1 | 2000-08-03 | ||
GB0019061A GB0019061D0 (en) | 2000-08-03 | 2000-08-03 | The treatment of convulsive states |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2001043730A2 true WO2001043730A2 (en) | 2001-06-21 |
WO2001043730A3 WO2001043730A3 (en) | 2002-06-13 |
Family
ID=26244786
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/GB2000/004838 WO2001043730A2 (en) | 1999-12-17 | 2000-12-15 | The treatment of convulsive states |
Country Status (7)
Country | Link |
---|---|
US (1) | US7384959B2 (en) |
EP (1) | EP1239858B1 (en) |
AT (1) | ATE252903T1 (en) |
AU (1) | AU2199901A (en) |
DE (1) | DE60006284T2 (en) |
ES (1) | ES2210025T3 (en) |
WO (1) | WO2001043730A2 (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002017919A2 (en) * | 2000-08-28 | 2002-03-07 | Sention, Inc. | Use of threo-methylphenidate compounds to enhance memory |
US7115631B2 (en) | 1995-12-04 | 2006-10-03 | Celgene Corporation | Methods for treatment of cognitive and menopausal disorders with D-threo methylphenidate |
WO2014203696A1 (en) * | 2013-06-20 | 2014-12-24 | 国立大学法人 岡山大学 | Anti-epileptic drug |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20110200663A1 (en) * | 2010-02-12 | 2011-08-18 | Nitto Denko Corporation | Methylphenidate patch preparation |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1997027176A1 (en) * | 1996-01-22 | 1997-07-31 | Medeva Europe Limited | Optical resolution of methylphenidate by 0,0'-bisaroyl tartaric acids |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6210705B1 (en) * | 1997-12-15 | 2001-04-03 | Noven Pharmaceuticals, Nc. | Compositions and methods for treatment of attention deficit disorder and attention deficit/hyperactivity disorder with methylphenidate |
-
2000
- 2000-12-15 AU AU21999/01A patent/AU2199901A/en not_active Abandoned
- 2000-12-15 ES ES00985589T patent/ES2210025T3/en not_active Expired - Lifetime
- 2000-12-15 AT AT00985589T patent/ATE252903T1/en not_active IP Right Cessation
- 2000-12-15 WO PCT/GB2000/004838 patent/WO2001043730A2/en active IP Right Grant
- 2000-12-15 US US10/148,535 patent/US7384959B2/en not_active Expired - Fee Related
- 2000-12-15 EP EP00985589A patent/EP1239858B1/en not_active Expired - Lifetime
- 2000-12-15 DE DE60006284T patent/DE60006284T2/en not_active Expired - Fee Related
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1997027176A1 (en) * | 1996-01-22 | 1997-07-31 | Medeva Europe Limited | Optical resolution of methylphenidate by 0,0'-bisaroyl tartaric acids |
Non-Patent Citations (3)
Title |
---|
AOYAMA T ET AL: "NONLINEAR KINETICS OF THREO-METHYLPHENIDATE ENANTIOMERS IN A PATIENT WITH NARCOLEPSY AND IN HEALTHY VOLUNTEERS" EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, SPRINGER VERLAG, DE, vol. 44, no. 1, 1993, pages 79-84, XP000602466 ISSN: 0031-6970 * |
DING Y-S ET AL: "CHIRAL DRUGS: COMPARISON OF THE PHARMACOKINETICS OF 11CD-THREO AND I-THREO-METHYLPHENIDATE IN THE HUMAN AND BABOON BRAIN" PSYCHOPHARMACOLOGY, SPRINGER VERLAG, BERLIN, DE, vol. 131, 1997, pages 71-78, XP000964662 ISSN: 0033-3158 * |
ECKERMAN D A ET AL: "ENANTIOSELECTIVE BEHAVIORAL EFFECTS OF THREO-METHYLPHENIDATE IN RATS" PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, ELSEVIER, US, vol. 40, no. 4, 1991, pages 875-880, XP000602558 ISSN: 0091-3057 * |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7115631B2 (en) | 1995-12-04 | 2006-10-03 | Celgene Corporation | Methods for treatment of cognitive and menopausal disorders with D-threo methylphenidate |
WO2002017919A2 (en) * | 2000-08-28 | 2002-03-07 | Sention, Inc. | Use of threo-methylphenidate compounds to enhance memory |
WO2002017919A3 (en) * | 2000-08-28 | 2003-02-27 | Sention Inc | Use of threo-methylphenidate compounds to enhance memory |
WO2014203696A1 (en) * | 2013-06-20 | 2014-12-24 | 国立大学法人 岡山大学 | Anti-epileptic drug |
JPWO2014203696A1 (en) * | 2013-06-20 | 2017-02-23 | 国立大学法人 岡山大学 | Antiepileptic drugs |
Also Published As
Publication number | Publication date |
---|---|
EP1239858B1 (en) | 2003-10-29 |
US7384959B2 (en) | 2008-06-10 |
US20030162810A1 (en) | 2003-08-28 |
DE60006284T2 (en) | 2004-07-29 |
ES2210025T3 (en) | 2004-07-01 |
DE60006284D1 (en) | 2003-12-04 |
ATE252903T1 (en) | 2003-11-15 |
EP1239858A2 (en) | 2002-09-18 |
AU2199901A (en) | 2001-06-25 |
WO2001043730A3 (en) | 2002-06-13 |
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