CS277525B6 - Mixture against migraine - Google Patents

Mixture against migraine Download PDF

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CS277525B6
CS277525B6 CS906641A CS664190A CS277525B6 CS 277525 B6 CS277525 B6 CS 277525B6 CS 906641 A CS906641 A CS 906641A CS 664190 A CS664190 A CS 664190A CS 277525 B6 CS277525 B6 CS 277525B6
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Czechoslovakia
Prior art keywords
migraine
mixture
phenobarbital
caffeine
seizure
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CS906641A
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Czech (cs)
Slovak (sk)
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CS664190A3 (en
Inventor
Pavel Rndr Rac
Jozef Rndr Baluch
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Pavel Rndr Rac
Jozef Rndr Baluch
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Priority to CS906641A priority Critical patent/CS277525B6/en
Publication of CS664190A3 publication Critical patent/CS664190A3/en
Publication of CS277525B6 publication Critical patent/CS277525B6/en

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Abstract

Riešenie sa týká antimigrenóznej zmesi proti migrenóznym bolestiam hlavy všetkých typov, ktoré obsahuje 150 až 400 mg paracetamolu, 150 až 350 mg acidum acetylosalicylicum v pufrovanej formě, 0,6 až 2,0 mg ergotaminium tartaricum, 50 až 150 mg coffeinum, 5 až 20 mg codeinum dihydrogenphosphoricum a 15 až 30 mg fenobarbitalum. Riešenie je možné využiť v medicíně v odbore neurológie.The solution relates to an antimigraine mixture for migraine headaches of all types, which contains 150 to 400 mg of paracetamol, 150 to 350 mg of acetylsalicylic acid in buffered form, 0.6 to 2.0 mg of ergotamine tartaricum, 50 to 150 mg of caffeine, 5 to 20 mg of codeine dihydrogenphosphoricum and 15 to 30 mg of phenobarbital. The solution can be used in medicine in the field of neurology.

Description

1 CS 277525 B61 CS 277525 B6

Vynález sa týká antimigrenóznej zmesi, ktorá účinkuje ajv stave plné rozvinutého migrenózneho záchvatu.The invention relates to an anti-migraine composition which also acts in a state of full developed migraine attack.

Podlá róznych světových statistik 5 až 10 % populácie (hlav-ně ženy vo veku 17 až 55 rokov) trpí migrenóznymi bolesisami hlavyrózneho typu. Pacienti sú liečení ambulantně alebo sú hospitali-zovaní . .Serious world statistics of 5 to 10% of the population (mainly women aged 17 to 55) suffer from migraine headaches. Patients are treated on an outpatient basis or are hospitalized. .

Pri liečbe akútneho migrenózneho stavu (pacient by mal byťpodlá mienky váčšiny lekárov hospitalizovaný) sa podávájúz jednozložkových liečiv napr. Cornutamín (ergotamínium tartari-cum), Dihydergot (dihydroergotamín metánsulfonát), Protazín(prometázínium chlorid), Diazepam (chlórdiazepoxid), Papaverín(papaverínium hydrochlorid), Indren (indometacín); z viaczložko-vých napr. Ergofein (ergotamínium tartaricum + coffeinum),Bellaspon (ergotamínium tartaricum + radobelín + fenobarbital),Spasmoveralgin (aminofenazonum + brómizoval + fenobarbital +papaverínium hydrochlorid + codeínum dyhydrogénfosforicum + efed-rínium hydrochlorid + metobromid), Sedolor (fenacetínum + amino-fenazonum + coffeinum), Migrenin (phenazum cum acidum citricum).In the treatment of an acute migraine condition (the patient should be hospitalized for all physicians), single-component drugs such as Cornutamine (ergotaminium tartari-cum), Dihydergot (dihydroergotamine methanesulfonate), Protazine (promethniinium chloride), Diazepam (chlordiazepoxide), Papaverine (papaverine hydrochloride) ), Indren (indomethacin); from multi-component eg Ergophein (ergotaminium tartaricum + coffeinum), Bellaspon (ergotaminium tartaricum + radobelin + phenobarbital), Spasmoveralgin (aminophenazone + brominated + phenobarbital + papaverine hydrochloride + codein dyhydrogenphosphoricum + ephedin-rinium hydrochloride + metobromide), Sedolor (phenacetin + amino-phenazone + caffeine), Migrenine (phenazum cum acid citricum).

Na prevenciu záchvatov sa používajú napr. Clavigrenin (dihy-droergotamínium mesylicum), Secatoxín (dihydroergotoxín), Lysenyl(lysuridium hydrogénmaleinicum), Cornutamin, Divascol (tolazoli-nium chlorid), Sandomigran (pizotifenum).For example, Clavigrenin (dihydroergotaminium mesylicum), Secatoxin (dihydroergotoxin), Lysenyl (lysuridium hydrogen maleate), Cornutamin, Divascol (tolazolium chloride), Sandomigran (pizotifenum) are used to prevent seizures.

Nevýhodou prípravkov používaných pri akútnom záchvate je ichslabá účinnosť a nespolahlivosť, ktoré vedú k zvyšovaniu dávoka tým aj nežiadúcich účinkov (srdce, cievy, zažívací trakt, CNS).Přípravky používané ako prevencia v dlhodobých kúrách (niekolkotýždňov až mesiacov) frekvenciu a intenzitu záchvatov podstatnéneznižujú. Dlhodobým podáváním napr. Sandomigranu sa prejavujejeho sedatívny účinok, zvýšená chuť do jedla, prírastok nahmotnosti, parestézia, zažívacie ťažkosti, po niekolkonásobnomopakovaní kúry znížený až nulový efekt, v dósledku čoho pacientiorientujú svoju liečbu na tlmenie akútnych stavov vysokými dávka-mi analgetík, niekolkonásobne přesahujúcimi terapeutické dávky(5 až 12 tabliet jednorázovo).A disadvantage of the preparations used in acute seizures is their poor efficacy and unreliability, leading to an increase in the dose of the adverse effects (heart, vessels, digestive tract, CNS). The preparations used to prevent long-term cures (several weeks to months) do not significantly reduce the frequency and intensity of seizures. Prolonged administration of e.g. doses (5-12 tablets once).

Napriek velkým vědeckým pokrokom nie je v súčasnej doběproblém liečenia migrény (podobné ako iných vasogénnych ochorení)vyriešený.Despite great scientific advances, the current problem of treating migraine (similar to other vasogenic diseases) is not resolved.

Viacročným sledováním účinkov niektorých doteraz používanýchpreparátov ako aj nových liečiv sa podařilo pripraviť antimigre-nóznu zmes podlá vynálezu, ktorá odstraňuje váčšinu nevýhod dote-raz používaných liečiv proti migréně. Podstata vynálezu spočíváv tom, že antimigrenózna zmes obsahuje v jednotlivéj dávke 150 až400 mg paracetamolu, 150 až 350 mg acidum acetylosalicylicumv pufrovanej formě, 0,6 až 2,0 mg ergotamínium tartaricum, 50 až150 mg coffeinum, 5 až 20 mg codeínum dihydrogénphosphorciuma 15 až 30 mg fenobarbitolu, čo je svojím zložením zmes šetrná,ale prekvapujúco velmi účinná, s účinkom takej intenzity, akádoteraz nebola popísaná. Táto antimigrenózna zmes podlá vynálezu pri poměrně nízkých množstvách jednotlivých liečivých látok zabezpečuje požadované CS 277525 B6 2 účinky nielen pri migrenóznom stave v ešte nerozvinutom stádiu,ale aj v stave plné rozvinutého záchvatu aj tam, kde doterajšialiečba neholá úspěšná.By monitoring the effects of some of the hitherto used preparations as well as new medicaments, it has been possible to prepare an anti-migraine composition according to the invention which eliminates most of the disadvantages of the currently used migraine drugs. SUMMARY OF THE INVENTION The anti-migraine composition comprises 150 to 400 mg of paracetamol, 150 to 350 mg of acetylsalicylic acid in buffered form, 0.6 to 2.0 mg of ergotaminium tartaric, 50 to 150 mg of caffeine, 5 to 20 mg of codeine dihydrogenphosphoric acid 15 to 15 mg. 30 mg phenobarbitol, which by its composition is gentle, but surprisingly very effective, with the effect of such intensity as has not been described. This anti-migraine composition of the present invention, at relatively low levels of the individual drug substance, provides the desired CS 277525 B6 effects not only in the migraine state in the still underdeveloped state, but also in a fully developed seizure state, even where treatment has not been successful.

Pri podáni v ešte nerozvinutom štádiu aury účinok nastupujeo 10 až 25 minút (podlá obsahu žalúdka) a je definitívny, t.j.záchvat sa nerozvinie. Pri podaní v štádiu plné rozvinutéhomigrénozneho záchvatu účinok nastupuje do 20 až 30 minúta v případe neúplnej eliminácie (podlá typu záchvatu) je možné po1 až 2 hodinách podat druhů dávku, ktorá definitivně záchvatutlmí. Potřeba podania třetej dávky na definitívnu elimináciuzáchvatu sa vyskytuje ojedinele. Podáváním tejto zmesi sa inter-valy medzi jednotlivými záchvatmi dokonca predlžujú a znižuje saich početnost na polovicu. Podáváním antimigrenóznej zmesi podlávynálezu len pri akútnych stavoch t.zn. 1 až 2 dávky pri záchvate(teda nie preventivné, dlhodobo) sa znižuje riziko prekročeniajednotlivých a denných dávok ako aj riziko nežiadúcich účinkov.Spolupráca medzi lekárom a pacientom sa výrazné zlepšuje, nakolkopo mnohých, doteraz neúspěšných dlhodobých kúrách nachádza výcho-disko zo svojho stavu.When administered in an undeveloped aura, the effect occurs 10 to 25 minutes (depending on the gastric content) and is definitive, i.e., the seizure does not develop. When administered at the stage of full-blown seizure, the effect occurs within 20 to 30 minutes in the event of incomplete elimination (depending on the seizure type), one to two hours can be given a dose that is definitely binge. The need for a third dose for definitive elimination of seizure is rare. By administering this mixture, they are even prolonged between each seizure and halved. By administering an anti-migraine blend of subfamilies only in acute conditions, e.g. 1 to 2 bouts of seizure (ie not preventive, long-term) reduce the risk of exceeding individual and daily doses, as well as the risk of adverse effects. Co-operation between the doctor and the patient is greatly improved, as many of the previously unsuccessful long-term treatments are the starting point of their condition.

Uvedené příklady ilustrujú ale neobmedzujú predmet vynálezu.Příklad 1These examples illustrate but do not limit the invention

Migrénozna zmes (1) paracetamolum 250 mg acidum acetylosalicylicum 350 mg ergotaminiumtartaricum 1,5 mg coffeinum 50,0 mg codeinum dihydrogenphosphoricum 10,0 mg fenobarbitalum 15,0 mg bola připravená zmiešaním jednotlivých zložiek do formy prášku.Migraine mixture (1) paracetamol 250 mg acetylsalicylic acid 350 mg ergotaminium tartaric 1.5 mg caffeine 50.0 mg codein dihydrogenphosphoricum 10.0 mg phenobarbital 15.0 mg was prepared by mixing the individual ingredients into a powder.

Rovnakým spósobom bola připravená antimigrenózna zmes (2)zmiešaním paracetamolum 350,0 mg acidum acetylosalicylicum 200,0 mg ergotaminium tartaricum 0,8 mg coffeinum 150,0 mg codeinum dihydrogenphosphoricum 15,0 mg fenobarbitalum 25,0 mg a finalizovaním do formy tablety.In the same way, an anti-migraine mixture (2) was prepared by mixing paracetamol 350.0 mg acetylsalicylic acid 200.0 mg ergotaminium tartaricum 0.8 mg caffeine 150.0 mg codeinum dihydrogenphosphoric 15.0 mg phenobarbital 25.0 mg and finalizing into tablet form.

Antimigrenózne zmesi (1,2) podlá vynálezu boli s nasledujú-cim výsledkom: testovaná látka 1. pacient 2. pacient 3. pacient 4. pacient Sandomigran - - - - zmes (1) +- Φ +++ ++ zmes (2) Φ ++ Φ ΦThe anti-migraine compositions (1, 2) of the invention were as follows: test substance 1st patient 2nd patient 3rd patient 4th patient Sandomigran - - - - mixture (1) + - Φ +++ ++ mixture (2 ) Φ ++ Φ Φ

Claims (1)

PATENTOVÉ NÁROKYPATENT CLAIMS Antimigrenózna zmes, vyznačujúca sa tým, že v jednotlivéj dávke obsahuj e .An antimigraine mixture, characterized in that it contains e. 150 až 400 mg paracetamolu,150 to 400 mg of paracetamol, 150 až 350 mg acidum acetylosalicylicum v pufrovanej forme,150 to 350 mg of acetylsalicylic acid in buffered form, 0,6 až 2,0 mg ergotamínium tartaricum,0.6 to 2.0 mg ergotamine tartaric acid, 50 až 150 mg coffeinum,50 to 150 mg of caffeine, 5 až 20 mg codeinum dihydrogenphosphoricum a5 to 20 mg codeinum dihydrogenphosphoricum a 15 až 30 mg fenobarbitalum.15 to 30 mg of phenobarbital.
CS906641A 1990-12-27 1990-12-27 Mixture against migraine CS277525B6 (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5972916A (en) * 1997-07-14 1999-10-26 Bristol-Myers Squibb Company Compositions containing the nonprescription combination of acetaminophen, aspirin and caffeine to alleviate the pain and symptoms of migraine
US7332183B2 (en) 2002-12-26 2008-02-19 Pozen Inc. Multilayer dosage forms containing NSAIDs and triptans
US8022095B2 (en) 1996-08-16 2011-09-20 Pozen, Inc. Methods of treating headaches using 5-HT agonists in combination with long-acting NSAIDs

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8022095B2 (en) 1996-08-16 2011-09-20 Pozen, Inc. Methods of treating headaches using 5-HT agonists in combination with long-acting NSAIDs
US5972916A (en) * 1997-07-14 1999-10-26 Bristol-Myers Squibb Company Compositions containing the nonprescription combination of acetaminophen, aspirin and caffeine to alleviate the pain and symptoms of migraine
US7332183B2 (en) 2002-12-26 2008-02-19 Pozen Inc. Multilayer dosage forms containing NSAIDs and triptans

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