ME01865B - Upotreba agomelatina za dobijanje ljekova namijenjenih za tretman generalizovanog anksioznog poremećaja - Google Patents
Upotreba agomelatina za dobijanje ljekova namijenjenih za tretman generalizovanog anksioznog poremećajaInfo
- Publication number
- ME01865B ME01865B MEP-2010-497A MEP49710A ME01865B ME 01865 B ME01865 B ME 01865B ME P49710 A MEP49710 A ME P49710A ME 01865 B ME01865 B ME 01865B
- Authority
- ME
- Montenegro
- Prior art keywords
- agomelatine
- anxiety disorder
- treatment
- generalized anxiety
- pharmaceutically acceptable
- Prior art date
Links
- YJYPHIXNFHFHND-UHFFFAOYSA-N agomelatine Chemical compound C1=CC=C(CCNC(C)=O)C2=CC(OC)=CC=C21 YJYPHIXNFHFHND-UHFFFAOYSA-N 0.000 title claims description 27
- 229960002629 agomelatine Drugs 0.000 title claims description 24
- 208000011688 Generalised anxiety disease Diseases 0.000 title claims description 13
- 229940079593 drug Drugs 0.000 title claims description 3
- 239000003814 drug Substances 0.000 title claims description 3
- 238000011282 treatment Methods 0.000 claims description 22
- 208000029364 generalized anxiety disease Diseases 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 8
- 239000002253 acid Substances 0.000 claims description 5
- 150000004677 hydrates Chemical class 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000007170 pathology Effects 0.000 description 8
- 239000000902 placebo Substances 0.000 description 5
- 229940068196 placebo Drugs 0.000 description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 208000011580 syndromic disease Diseases 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- 208000019901 Anxiety disease Diseases 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
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- 230000000144 pharmacologic effect Effects 0.000 description 2
- 229940001470 psychoactive drug Drugs 0.000 description 2
- 239000004089 psychotropic agent Substances 0.000 description 2
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- 230000009291 secondary effect Effects 0.000 description 2
- AHOUBRCZNHFOSL-YOEHRIQHSA-N (+)-Casbol Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-YOEHRIQHSA-N 0.000 description 1
- 102000006902 5-HT2C Serotonin Receptor Human genes 0.000 description 1
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 description 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
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- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
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- 241000416162 Astragalus gummifer Species 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 208000020401 Depressive disease Diseases 0.000 description 1
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- 108010010803 Gelatin Proteins 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 101150013372 Htr2c gene Proteins 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 208000019022 Mood disease Diseases 0.000 description 1
- PMDCZENCAXMSOU-UHFFFAOYSA-N N-ethylacetamide Chemical compound CCNC(C)=O PMDCZENCAXMSOU-UHFFFAOYSA-N 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 208000029808 Psychomotor disease Diseases 0.000 description 1
- 206010039897 Sedation Diseases 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- 239000002250 absorbent Substances 0.000 description 1
- 230000002745 absorbent Effects 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000008272 agar Substances 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- VREFGVBLTWBCJP-UHFFFAOYSA-N alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 235000010210 aluminium Nutrition 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000002249 anxiolytic agent Substances 0.000 description 1
- 230000000949 anxiolytic effect Effects 0.000 description 1
- 229940005530 anxiolytics Drugs 0.000 description 1
- 229940049706 benzodiazepine Drugs 0.000 description 1
- 150000001557 benzodiazepines Chemical class 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 159000000007 calcium salts Chemical class 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000010877 cognitive disease Diseases 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 210000002249 digestive system Anatomy 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 229960004341 escitalopram Drugs 0.000 description 1
- WSEQXVZVJXJVFP-FQEVSTJZSA-N escitalopram Chemical compound C1([C@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 WSEQXVZVJXJVFP-FQEVSTJZSA-N 0.000 description 1
- PPRRDFIXUUSXRA-UHFFFAOYSA-N flibanserin Chemical compound FC(F)(F)C1=CC=CC(N2CCN(CCN3C(NC4=CC=CC=C43)=O)CC2)=C1 PPRRDFIXUUSXRA-UHFFFAOYSA-N 0.000 description 1
- 229960002053 flibanserin Drugs 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- -1 glosses Substances 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 206010022437 insomnia Diseases 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000000391 magnesium silicate Substances 0.000 description 1
- 235000019792 magnesium silicate Nutrition 0.000 description 1
- 229910052919 magnesium silicate Inorganic materials 0.000 description 1
- ZADYMNAVLSWLEQ-UHFFFAOYSA-N magnesium;oxygen(2-);silicon(4+) Chemical compound [O-2].[O-2].[O-2].[Mg+2].[Si+4] ZADYMNAVLSWLEQ-UHFFFAOYSA-N 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 229940126601 medicinal product Drugs 0.000 description 1
- 230000001193 melatoninergic effect Effects 0.000 description 1
- 230000003340 mental effect Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 229940127285 new chemical entity Drugs 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 229960002296 paroxetine Drugs 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 208000012672 seasonal affective disease Diseases 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000006190 sub-lingual tablet Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 229960004688 venlafaxine Drugs 0.000 description 1
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/04—Nitro compounds
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
Opis
Ovaj pronalazak se odnosi na korišćenje agomelatina ili N-[2-(7-metoksi-1-naftil)etil]acetamida, formule (I):
kao i njegovih hidrata, kristalnih oblika i adicionih soli sa jednom farmaceutski prihvatljivom kiselinom ili bazom, za dobijanje lekova namenjenih lečenju generalizovanog anksioznog poremećaja ili TAG.
Agomelatin ili N-[2-(7-metoksi-1-naftil)etil]acetamid ispoljava dvostruku karakteristiku, da je sa jedne strane agonist na receptorima melatoninergičnog sistema i, da je, sa druge strane, antagonist 5-HT2c receptora. Ove osobine mu daju aktivnost u centralnom nervnom sistemu, a naročito za tretman: depresije major, sezonskih depresija, poremećaja spavanja, kardiovaskularnih patologija, patologija digestivnog sistema, nesanice i umora kao rezultata promene vremenske zone, poremećaja apetita i gojaznosti.
Agomelatin, njegova proizvodnja i korišćenje u terapiji, opisani su u evropskim patentima EP 0 447 285 i EP 1 564 202.
Zahtevalac je sada otkrio da agomelatin ili N-[2-(7-metoksi-1-naftil) etiljacetamid, kao i njegovi hidrati, kristalni oblici i adicione soli sa jednom farmaceutski prihvatljivom kiselinom ili bazom, poseduje korisna svojstva koja mu omogućavaju da se koristi u tretmanu generalizovanog anksioznog poremećaja.
Opisan uticajnim strahom a bez predmeta, generalizovani anksiozni poremećaj odgovara kriterijumima koji su potpuno definisani i sastavni su deo jednog naučno opisanog entiteta posebne celine (300.02 - DSM IV - Manuel Diagnostique et Statistique des Troubles Mentaux, 4eme edition, American Psychiatric Association). Ova hronična patologija ima za posledicu brojne pridružene poremećaje, a pre svega kognitivnu disfunkciju, preciznije razmišljanje i mentalna predstavljanja, promene rasuđivanja, mišljenja i prema tome uspeha ali, kao posledicu ima isto tako i
psihomotorne poremećaje koji su izvori smetenosti, smanjenjenih kapaciteta reakcija, osećanja ništavila (VVittchen HU et al., Arch. Gen. Psychiatry, 1994, 51 (5), 355-364).
Specifičnost ovog poremećaja je s druge strane prepoznata od strane evropskih i američkih autoriteta u zadravstvu i izdate su “preporuke” za razvoj molekula koji će specifično preuzeti ovu indikaciju (Committee for Proprietary Medicinal Produst (CPMP) /EVVP/4284/02/ London - 20. januar 2005. - Preporuke za klinička istraživanja tretmana medicinskim proizvodima indikovanim za generalizovani anksiozni poremećaj).
Nedavne epidemiološke studije su pokazale da je prevalenca ove patologije otprilike 5 do 6% u opštoj populaciji sa jednim trendom, koji može dostići 10% za žene preko 40 godina starosti. Zbog toga je pojava ove patologije važna u zdravstvenom i ekonomskom smislu.
U ovom trenutku ne postoji zaista zadovoljavajući i priznati tretman za generalizovani anksiozni poremećaj. Dugo su benzodiazepini, a u nekim zemljama su i ostali, bili tretman prvog izbora. Poslednja tehnika, VV02006/096434 opisuje korišćenje flibanserina udruženog sa jednim ili više anksiolitika za tretman anksioznih poremećaja. Jednako je objavljena, u W02005/002562, asocijacija koja sadrži inhibitor koji je selektivan prema serotoninskim receptorima i agomelatin, a za tretman depresije, anksioznih poremećaja i drugih afektivnih poremećaja.
Nedavno je potvrđeno primenjivanje molekula, kao što su venlafaksin, paroksetin ili escitalopram. U međuvremenu, ove različite terapeutske kategorije su bile izvor brojnih sekundarnih dejstava, pre svega, sedacije, farmako-zavisnosti, interakcije sa alkoholom i kardiovaskularnih smetnji i/ili seksualnih, koje nisu zanemarljive...
Sem toga, u većini slučajeva, zaustavljanje ovih tretmana ima izraženu pojavu sindroma diskontinuiteta, kog pacijenti teško prihvataju.
Dakle, stavljanje na raspolaganje novih tretmana za ovu patologiju je neophodnost kako ističu “preporuke" CPMP.
Agomelatin, novi hemijski entitet sa novim farmakološkim svojstvima, u toku kontrolisanih kliničkih ispitivanja u odnosu na placebo, ispoljio je efikasnost u epizodi depresije major.
Zahtevalac sada otkriva da se agomelatin, na ime svojih farmakoloških svojstava može koristiti kod generalizovanog anksioznog poremećaja.
Jedno kliničko ispitivanje, izvedeno u odnosu na placebo, na pacijentima koji su patili od generalizovanog anksioznog poremećaja, dopustilo je da se na značajan način dokaže da za ovu patologiju, agomelatin čini potpuno prilagođen tretman.
Sem toga, zapažene su i druge aktivnosti tokom tretmana
generalizovanog anksiozonog poremećaja, agomelatin ispoljava jedan dobar profil prihvatljivosti od strane pacijenata : posebno, agomelatin je lišen sekundarnih efekata povezanih sa klasičnim psihotropicima. Od ovih efekata, sindroma diskontinuiteta na završetku tretmana sa klasičnim psihotropicima sa agomelatinom nema i to ga čini tretmanom izbora za ovu patologiju.
Pronalazak se dakle odnosi na korišćenje agomelatina, kao i njegovih hidrata, kristalnih oblika i adicionih soli sa jednom farmaceutski prihvatljivom kiselinom ili bazom, za dobijanje farmaceutskih smeša namenjenih tečenju generalizovanog anksioznog poremećaja.
Posebno se pronalazak odnosi na korišćenje agomelatina dobijenog u kristalnom obliku II, opisanom u zahtevu patenta EP 1 564 202, za dobijanje farmaceutskih smeša namenjenih lečenju generalizovanog anksioznog poremećaja.
Farmaceutske smeše se mogu predstaviti u obliku formi prikladnih za primenjivanje oralnim putem, parenteralnim, transkutanim, nazalnim, rektalnim, perlingvalnim i, pre svega, u obliku injektabilnih preparata, tableta, sublingvalnih tableta, gloseta, želatinskih kapsula, kapsula, tableta, supozitorija, kremova, masti, kožnih gelova i td...
Sem agomelatina, farmaceutske smeše koje su u skladu sa pronalaskom sadrže jednu ili više podloga ili vehikuluma, odabranih od: diluenata, lubrikanasa, sredstava za vezivanje, sredstava za raspadljivost, absorbanata, boja, zaslađivača i td...
U smislu primera i bez cilja ograničavanja, mogu se navesti:
• kao diluenti : laktoza, dekstroza, saharoza, manitol, sorbitol, celuloza, glicerin,
• kao lubrikansi : silika, talk, stearinska kiselina i njene soli magnezijuma i kalcijuma, polietilen glikol,
• kao sredstva za vezivanje : aluminijum i magnezijum silikat, škrob, želatin, tragakanta, metilceluloza, natrijum karboksimetilceluloza i polivinilpirolidon,
• kao sredstva za raspadljivost: agar, alginska kiselina i njena natrijumova so, smeše efervescenata.
Doziranje koje se koristi varira prema polu, starosti i težini pacijenta, puta primene, prirode bolesti i eventualno pridruženih tretmana i kreće se između 1 mg i 50 mg agomelatina u toku 24 sata.
Poželjno, dnevna doza agomelatina će biti 25 mg na dan, sa mogućnošću povećanja na 50 mg dnevno.
Farmaceutska smeša :
Formula za izradu 1000 tableta doza od 25 mg :
Kliničko ispitivanje :
Jedno kliničko ispitivanje u odnosu na placebo, izvedeno je na 121 pacijentu. Ovih 121 pacijent nasumično su podeljeni u dve jednake grupe, koje su primale ili agomelatin u dozi od 25 mg dnevno ili placebo.
Posle dve nedelje tretmana i u slučaju nedovoljnog odgovora, doza je naslepo dvostruko povećana na 50 mg za pacijente na agomelatinu putem sistema IVRS (Interactive Voice Response System). Pacijenti su tretirani dve nedelje.
Efikasnost je procenjena pomoću instrumenata ispitivanja preporučenih od zdravstvenih službi, pre svih, Hamiltonovom skalom straha (Hamilton M., J. Neurol. Neurosurg. Psychiat., 1959, 23, 56-62), ili Sheehanovom skalom funkcionalnog odraza (International Clinical Psychopharmacology, 1996, 11, 89-95). Istovremeno se ispitivao i profil prihvatljivosti.
Dobijeni rezultati pokazuju da je razlika u ukupnom skoru Hamiltonove skale, glavnog kriterijuma ispitivanja, između grupe na tretmanu sa agomelatinom i grupe na placebu bila -3,28 (p=0,040), što odgovara klinički i statistički značajnoj razlici.
Isto tako, ispitivanje je pokazalo jedan dobar profil prihvatljivosti proizvoda od strane pacijenata, kao i odsustvo sindroma diskontinuiteta po završetku tretmana.
Claims (4)
1. Upotreba agomelatina ili N-[2-(7-metoksi-1-naftil)etil]acetamida ili jednog od njegovih hidrata, kristalnih oblika i adicionih soli sa jednom farmaceutski prihvatljivom kiselinom ili bazom, kao jedinog aktivnog principa za dobijanje leka namenjeng tretmanu generalizovanog anksioznog poremećaja.
2. Upotreba, kao u patentnom zahtevu 1, naznačena time što se agomelatin dobija u kristalnom obliku II.
3. Farmaceutska smeša, koja sadrži kao jedini aktivan princip, agomelatin ili jedan od njegovih hidrata, kristalnih oblika i adicionih soli sa jednom farmaceutski prihvatljivom kiselinom ili bazom, sam ili u kombinaciji sa jednom ili više farmaceutski prihvatljivih podloga za upotrebu u tretmanu generalizovanog anksioznog poremećaja.
4. Farmaceutska smeša, kao u patentnom zahtevu 3, naznačena time što se agomelatin dobija u kristalnom obliku II.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0603083A FR2899472B1 (fr) | 2006-04-07 | 2006-04-07 | Utilisation de l'agomelatine pour l'obtention de medicaments destines au traitement du trouble anxiete generalisee |
| EP07290420A EP1842535B1 (fr) | 2006-04-07 | 2007-04-06 | Utilisation de l'agomélatine pour l'obtention de médicaments destinés au traitement du Trouble Anxiété Généralisée |
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| ME01865B true ME01865B (me) | 2011-04-30 |
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| Application Number | Title | Priority Date | Filing Date |
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| MEP-2010-497A ME01865B (me) | 2006-04-07 | 2007-04-06 | Upotreba agomelatina za dobijanje ljekova namijenjenih za tretman generalizovanog anksioznog poremećaja |
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| CN101481321B (zh) * | 2009-02-27 | 2012-04-18 | 上海医药工业研究院 | 阿戈美拉汀卤化氢复合物及其制备方法 |
| CN101585779B (zh) * | 2009-03-10 | 2014-04-02 | 上海医药工业研究院 | 阿戈美拉汀的晶型vi及其制备方法和应用 |
| FR2956031B1 (fr) * | 2010-02-11 | 2012-03-02 | Servier Lab | Utilisation de l'agomelatine pour l'obtention de medicaments destines au traitement du trouble obsessionnel compulsif (toc) |
| CN102190594A (zh) * | 2010-03-17 | 2011-09-21 | 上海医药工业研究院 | 阿戈美拉汀氯化氢水合物及其制备方法 |
| CN102190595A (zh) * | 2010-03-17 | 2011-09-21 | 上海医药工业研究院 | 阿戈美拉汀溴化氢水合物及其制备方法 |
| PH12012000132B1 (en) * | 2011-06-09 | 2014-10-20 | Servier Lab | New co-crystals of agomelatine, a process for their preparation and pharmaceutical compositions containing them |
| FR2978916B1 (fr) * | 2011-08-10 | 2013-07-26 | Servier Lab | Composition pharmaceutique solide pour administration buccale d'agomelatine |
| EP2810647A1 (en) | 2013-06-06 | 2014-12-10 | Zentiva, a.s. | Pharmaceutical formulations comprising agomelatine in the form of agomelatine co-crystal with an organic acid |
| HUE036989T2 (hu) | 2013-06-06 | 2018-08-28 | Zentiva Ks | Agomelatin készítmény, amely agomelatint ko-kristály formájában tartalmaz |
| IT201900002913A1 (it) | 2019-03-01 | 2020-09-01 | Nicola Pescosolido | Composto utile per il trattamento del glaucoma |
| CN110867197A (zh) * | 2019-10-23 | 2020-03-06 | 吴杰 | 语音交互过程中实时打断语音机器人的方法及设备 |
| CN116785225A (zh) * | 2022-03-15 | 2023-09-22 | 湖南慧泽生物医药科技有限公司 | 阿戈美拉汀鼻部制剂 |
| CN118021721A (zh) * | 2024-01-19 | 2024-05-14 | 沈阳药科大学 | 一种脑靶向阿戈美拉汀鼻喷胶束的制备方法与应用 |
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| FR2658818B1 (fr) * | 1990-02-27 | 1993-12-31 | Adir Cie | Nouveaux derives a structure naphtalenique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| US5737438A (en) * | 1994-03-07 | 1998-04-07 | International Business Machine Corp. | Image processing |
| DE19532842C1 (de) * | 1995-09-05 | 1996-12-19 | Ibm | Bildaufnahmesystem |
| AR047553A1 (es) * | 2003-07-04 | 2006-01-25 | Lundbeck & Co As H | La combinacion de un inhibidor de reabsorcion de serotonina y agomelatina |
| WO2005063297A2 (en) * | 2003-12-24 | 2005-07-14 | Sepracor Inc. | Melatonin combination therapy for improving sleep quality |
| FR2866335B1 (fr) * | 2004-02-13 | 2006-05-26 | Servier Lab | Nouveau procede de synthese de l'agomelatine |
| CA2599937A1 (en) * | 2005-03-04 | 2006-09-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions for the treatment and/or prevention of anxiety disorders |
| US7635721B2 (en) * | 2005-08-03 | 2009-12-22 | Les Laboratoires Servier | Crystalline form III of agomelatine, a process for its preparation and pharmaceutical compositions containing it |
| US7358395B2 (en) * | 2005-08-03 | 2008-04-15 | Les Laboratories Servier | Crystalline form V of agomelatine, a process for its preparation and pharmaceutical compositions containing it |
| TW200735878A (en) * | 2005-11-18 | 2007-10-01 | Astrazeneca Ab | Pharmaceutical compositions |
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- 2006-04-07 FR FR0603083A patent/FR2899472B1/fr active Active
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2007
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- 2007-03-26 AP AP2007003953A patent/AP2488A/xx active
- 2007-03-28 CR CR9019A patent/CR9019A/es not_active Application Discontinuation
- 2007-03-28 TN TNP2007000118A patent/TNSN07118A1/fr unknown
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- 2007-03-29 NI NI200700084A patent/NI200700084A/es unknown
- 2007-04-03 MA MA29798A patent/MA28987B1/fr unknown
- 2007-04-03 CO CO07033655A patent/CO5840252A1/es not_active Application Discontinuation
- 2007-04-03 NO NO20071774A patent/NO20071774L/no not_active Application Discontinuation
- 2007-04-04 MX MX2007004100A patent/MX2007004100A/es active IP Right Grant
- 2007-04-04 AR ARP070101420A patent/AR060349A1/es unknown
- 2007-04-04 TW TW096112141A patent/TWI374736B/zh active
- 2007-04-04 US US11/732,762 patent/US7960438B2/en active Active
- 2007-04-05 SG SG200702552-1A patent/SG136881A1/en unknown
- 2007-04-05 JO JOP/2007/0119A patent/JO3440B1/ar active
- 2007-04-05 MY MYPI20070536A patent/MY143269A/en unknown
- 2007-04-05 GE GEAP20079966A patent/GEP20094743B/en unknown
- 2007-04-05 AU AU2007201527A patent/AU2007201527B2/en active Active
- 2007-04-05 BR BRPI0701601-8A patent/BRPI0701601A/pt not_active Application Discontinuation
- 2007-04-05 NZ NZ554347A patent/NZ554347A/en unknown
- 2007-04-05 ZA ZA200702865A patent/ZA200702865B/xx unknown
- 2007-04-06 PL PL07290420T patent/PL1842535T3/pl unknown
- 2007-04-06 EP EP07290420A patent/EP1842535B1/fr not_active Revoked
- 2007-04-06 CN CN2007100910721A patent/CN101049290B/zh active Active
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- 2007-04-06 DK DK07290420.4T patent/DK1842535T3/da active
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- 2007-04-06 WO PCT/FR2007/000586 patent/WO2007116136A1/fr not_active Ceased
- 2007-04-06 JP JP2009503617A patent/JP4880031B2/ja active Active
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- 2007-04-06 DE DE602007008494T patent/DE602007008494D1/de active Active
- 2007-04-06 SI SI200730345T patent/SI1842535T1/sl unknown
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