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Antidementia Drugs

Drug Nomenclature

Synonyms: Aniracetam; Ro-13-5057
USAN: Aniracetam
INN: Aniracetam [rINN (en)]
INN: Aniracetam [rINN (es)]
INN: Aniracétam [rINN (fr)]
INN: Aniracetamum [rINN (la)]
INN: Анирацетам [rINN (ru)]
Chemical name: 1-(4-Methoxybenzoyl)-2-pyrrolidinone
Molecular formula: C12H13NO3 =219.2
CAS: 72432-10-1
ATC code: N06BX11

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Aniracetam is a nootropic drug that has been tried in senile dementia. It is given orally in usual doses of 1.5 g daily.

Proprietary Preparations

Argentina: Aniran; Conectol ; Pergamid;

Greece: Memodrin; Referan;

Italy: Ampamet; Draganon .

Drug Nomenclature

Synonyms: Bifemelano; MCI-2016 (bifemelane hydrochloride)
INN: Bifemelane [rINN (en)]
INN: Bifemelano [rINN (es)]
INN: Bifémélane [rINN (fr)]
INN: Bifemelanum [rINN (la)]
INN: Бифемелан [rINN (ru)]
Chemical name: N-Methyl-4-[(α-phenyl-o-tolyl)oxy]butylamine
Molecular formula: C18H23NO =269.4
CAS: 90293-01-9 (bifemelane); 62232-46-6 (bifemelane hydrochloride)
ATC code: N06AX08

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Bifemelane is a nootropic that has been given orally in a usual dose of 150 mg of the hydrochloride daily in divided doses for the treatment of cerebrovascular disorders including some forms of dementia.

Proprietary Preparations

Argentina: Alemelano ; Cordinal; Neurocine; Neurolea.

Drug Nomenclature

Synonyms: l-αGlycerylphosphorylcholine; Alfoscerato de colina; Choline Alphoscerate; Choline Glycerophosphate; Colina, alfoscerato de
INN: Choline Alfoscerate [rINN (en)]
INN: Alfoscerato de colina [rINN (es)]
INN: Choline, Alfoscérate de [rINN (fr)]
INN: Cholini Alfosceras [rINN (la)]
INN: Холина Альфосцерат [rINN (ru)]
Chemical name: Choline hydroxide, (R)-2,3-dihydroxypropyl hydrogen phosphate, inner salt
Molecular formula: C8H20NO6P =257.2
CAS: 28319-77-9
ATC code: N07AX02
Antidementia-Drugs

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Choline alfoscerate is a precursor of acetylcholine and has been tried in the treatment of Alzheimer’s disease and other dementias (below). The usual oral dose is 0.8 to 1.2 g daily in divided doses; doses of 1 g daily have been given by intramuscular or slow intravenous injection.

Dementia. Treatment with precursors of acetylcholine is not generally thought to be of benefit in dementia. However, in an analysis of 8 controlled clinical studies the use of choline alfoscerate in patients with dementia of the Alzheimer’s type, vascular dementia, or acute cerebrovascular disease was claimed to be of some benefit. Results of a further 3 uncontrolled studies in the same review suggested that it might favour functional recovery in patients with cerebral stroke.

Proprietary Preparations

Argentina: Gliatilin ;

Czech Republic: Gliatilin ;

Greece: Gliatilin;

Italy: Brezal; Delecit; Gliatilin;

Poland: Gliatilin;

Russia: Cerepro; Gliatilin.

Drug Nomenclature

Synonyms: Dihidroergocristina, mesilato de; Dihidroergokristino mesilatas; Dihidroergokrisztin-mezilát; Dihydroergocristine Mesylate; Dihydroergocristine Methanesulphonate; Dihydroergocristini Mesilas; Dihydroergokristiinimesilaatti; Dihydroergokristin-mesylát; Dihydroergokristinmesilat
BAN: Dihydroergocristine Mesilate [BANM]
Chemical name: (6aR,9R,10aR)-N-[(2R,5S,10aS,10bS)-5-Benzyl-10b-hydroxy-2-isopropyl-3,6-dioxooctahydro-8H-[1,3]oxazolo[3,2-a]pyrrolo[2,1-c]pyrazin-2-yl]-7-methyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxamide methanesulphonate
Molecular formula: C35H41N5O5,CH4O3S =707.8
CAS: 17479-19-5 (dihydroergocristine); 24730-10-7 (dihydroergocristine mesilate)
ATC code: C04AE04

 

European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Dihydroergocristine Mesilate). A white or almost white, fine crystalline powder. Slightly soluble in water; soluble in methyl alcohol. A 0.5% solution in water has a pH of 4.0 to 5.0. Protect from light.

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Dihydroergocristine mesilate is a component of codergocrine mesilate (above) and has similar actions. In some countries it has been given orally in doses of 3 to 6 mg daily in divided doses in the symptomatic treatment of mental deterioration associated with cerebrovascular insufficiency and in peripheral vascular disease. It has also been given by intramuscular or intravenous injection.

Preparations

Proprietary Preparations

Austria: Nehydrin;

Brazil: Iskemil; Iskevert ;

Greece: Agiobita; Alfacrist; Beytina; Cristil; Diertina; Ergobel; Ergocrist; Ergofil; Fenitina; Guadal; Memotil; Mentidose ; Normocedon; Thriolan; Tonergon;

Italy: Defluina ; Diertina Difluid ;

Portugal: Diertina;

Spain: Diertine; Ergodavur

Multi-ingredient

Argentina: Cervilane; Cinacris; Micerfin;

Austria: Brinerdin; Defluina;

Brazil: Isketam; Norogil; Vertizine D;

Chile: Cervilane;

Czech Republic: Anavenol; Crystepin; Ersilan; Neocrystepin; Trimecryton ;

France: Iskedyl;

Italy: Brinerdina;

Mexico: Cervilan;

Poland: Anavenol; Normatens; Venacorn;

Portugal: Brinerdine ; Cervilane ;

Russia: Anavenol; Crystepin;

South Africa: Brinerdin;

Spain: Brinerdina Clinadil; Diemil;

Switzerland: Brinerdine;

Thailand: Bedin; Brinerdin; Hyperdine.

Drug Nomenclature

Synonyms: Dihidroergocriptina, mesilato de; Dihydroergocryptine Mesylate; Dihydroergocryptine Methanesulphonate; Dihydroergokryptine Mesylate
Molecular formula: C32H43N5O5,CH4O3S =673.8
CAS: 25447-66-9 (dihydroergocryptine, α-isomer); 19467-62-0 (dihydroergocryptine, β-isomer); 14271-05-7 (dihydroergocryptine mesilate, α-isomer); 65914-79-6 (dihydroergocryptine mesilate, β-isomer)
ATC code: N04BC03

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Dihydroergocryptine mesilate is a component of codergocrine mesilate and has similar actions. It has been given orally in doses of up to 20 mg daily for migraine, and in maintenance doses of up to 60 to 120 mg daily for parkinsonism. It has also been used for age-related dementia and to inhibit lactation. In some countries it has been given with caffeine for cerebrovascular and peripheral vascular disorders.

Preparations

Proprietary Preparations

Czech Republic: Almirid;

Germany; Almirid; Cripar;

Greece: Daverium;

Italy: Daverium;

Mexico: Diamin;

Poland: Almirid;

Portugal: Striatal;

Russia: Vasobral;

Switzerland: Cripar

Multi-ingredient

France: Vasobral;

Hong Kong; Vasobral;

Italy: Vasobral.

Drug Nomenclature

Synonyms: Idazoxano, hidrocloruro de; RX-781094
BAN: Idazoxan Hydrochloride [BANM]
INN: Idazoxan Hydrochloride [pINNM (en)]
INN: Hidrocloruro de idazoxano [rINNM (es)]
INN: Idazoxan, Chlorhydrate d’ [rINNM (fr)]
INN: Idazoxani Hydrochloridum [rINNM (la)]
INN: Идазоксана Гидрохлорид [rINNM (ru)]
Chemical name: 2-(2,3-Dihydro-1,4-benzodioxin-2-yl)-2-imidazoline hydrochloride
Molecular formula: C11H12N2O2HCl =240.7
CAS: 79944-58-4 (idazoxan); 79944-56-2 (idazoxan hydrochloride)

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Idazoxan hydrochloride is an alpha2-adrenoceptor antagonist that has been investigated in neurological disorders including depression, dementia, and parkinsonism.

Drug Nomenclature

Synonyms: CV-2619; Idebenona
INN: Idebenone [rINN (en)]
INN: Idebenona [rINN (es)]
INN: Idébénone [rINN (fr)]
INN: Idebenonum [rINN (la)]
INN: Идебенон [rINN (ru)]
Chemical name: 2-(10-Hydroxydecyl)-5,6-dimethoxy-3-methyl-p-benzoquinone
Molecular formula: C19H30O5 =338.4
CAS: 58186-27-9
ATC code: N06BX13

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Idebenone has been used in the treatment of mental impairment associated with cerebrovascular disorders. A dose of 90 mg daily has been given orally in 2 divided doses after food. Idebenone has also been tried in Alzheimer’s disease. It has also been investigated for the management of various clinical manifestations of Friedreich’s ataxia and is used orally in a dose of 5 mg/kg daily in 3 divided doses for cardiomyopathy in this disease.

Idebenone is also available as a 1 % cream for the cosmetic treatment of wrinkles.

Dementia. Idebenone was found to be safe and effective in patients with mild to moderate Alzheimer’s disease when followed for up to 2 years. In a further study, its safety and efficacy were comparable to tacrine. However, another study found no clinically significant slowing of cognitive decline in patients with Alzheimer’s disease treated with idebenone.

Friedreich’s ataxia. Preliminary studies of idebenone in the treatment of Friedreich’s ataxia.

Preparations

Proprietary Preparations

Argentina: Esanic; Geniceral; Idesole; Nemocebral; Pavertrin; Sicoplus; Ulcourona ;

Italy: Daruma ; Mnesis;

Mexico: Lucebanol;

Portugal: Amizal; Cerestabon; Idecortex;

Russia: Noben;

Switzerland: Mnesis;

United States of America (US and USA): Prevage.

Multi-ingredient

Argentina: Idesole Plus; Nemocebral Plus.

Drug Nomenclature

Synonyms: DM-9384; DZL-221; Nefiracetam
INN: Nefiracetam [rINN (en)]
INN: Nefiracetam [rINN (es)]
INN: Néfiracétam [rINN (fr)]
INN: Nefiracetamum [rINN (la)]
INN: Нефирацетам [rINN (ru)]
Chemical name: 2-Oxo-1-pyrrolidineaceto-2´,6´-xylidide
Molecular formula: C14H18N2O2 =246.3
CAS: 77191-36-7

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Nefiracetam acts on the CNS and has been described as a nootropic. It has been investigated in some cerebrovascular disorders and for the treatment of Alzheimer’s disease.

Drug Nomenclature

Synonyms: Nizofenona; Y-9179
INN: Nizofenone [rINN (en)]
INN: Nizofenona [rINN (es)]
INN: Nizofénone [rINN (fr)]
INN: Nizofenonum [rINN (la)]
INN: Низофенон [rINN (ru)]
Chemical name: 2´-Chloro-2-[2-[(diethylamino)methyl]imidazol-1-yl]-5-nitrobenzophenone
Molecular formula: C21H21ClN4O3 =412.9
CAS: 54533-85-6
ATC code: N06BX10

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Nizofenone has been investigated as a nootropic and cerebral vasodilator. It has been used parenterally as the fumarate.

Drug Nomenclature

Synonyms: CGP-21690E; CT-848; ISF-2522; Oksirasetaami; Oxiracetam; Oxiracetamum; Oxracetam
BAN: Oxiracetam
INN: Oxiracetam [rINN (en)]
INN: Oxiracetam [rINN (es)]
INN: Oxiracétam [rINN (fr)]
INN: Oxiracetamum [rINN (la)]
INN: Оксирацетам [rINN (ru)]
Chemical name: 4-Hydroxy-2-oxo-1-pyrrolidineacetamide
Molecular formula: C6H10N2O3 =158.2
CAS: 62613-82-5
ATC code: N06BX07

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Oxiracetam has been used as a nootropic in organic brain syndromes and senile dementia.

Dementia. Clinical benefit has been reported in patients with dementia given oxiracetam, but in the USA it was withdrawn from phase II clinical studies in patients with Alzheimer’s disease due to lack of efficacy.

Drug Nomenclature

Synonyms: BRN-5030440; Carphedon; Karfedon
Chemical name: 2-Oxo-4-phenyl-1-pyrrolidineacetamide
Molecular formula: C12H14N2O2 =218.3
CAS: 77472-70-9

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4-Phenylpiracetam is a nootropic and has been used in the management of various cerebrovascular disorders. It has also been abused in sport.

Proprietary Preparations

Russia: Phenotropil.

Drug Nomenclature

Synonyms: Posatirelina; RGH-2202
INN: Posatirelin [rINN (en)]
INN: Posatirelina [rINN (es)]
INN: Posatiréline [rINN (fr)]
INN: Posatirelinum [rINN (la)]
INN: Позатирелин [rINN (ru)]
Chemical name: (2S)-N[(1S)-1-[[(2S)-2-Carbamoyl-1-pyrrolidinyl]carbonyl]-3-methylbutyl]-6-oxopipecolamide
Molecular formula: C17H28N4O4 =352.4
CAS: 78664-73-0

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Posatirelin is an analogue of protirelin. It is claimed to have beneficial effects on CNS function, and has been investigated in the management of dementia of various causes.

Drug Nomenclature

Synonyms: Amacetam Sulphate; CI-879; Pramiracetam Sulphate; Pramiracetam, sulfato de
USAN: Pramiracetam Sulfate
INN: Pramiracetam Sulfate [rINNM (en)]
INN: Sulfato de pramiracetam [rINNM (es)]
INN: Pramiracétam, Sulfate de [rINNM (fr)]
INN: Pramiracetami Sulfas [rINNM (la)]
INN: Прамирацетама Сульфат [rINNM (ru)]
Chemical name: N-[2-(Diisopropylamino)ethyl]-2-oxo-1-pyrrolidineacetamide sulphate
Molecular formula: C14H27N3O2,H2SO4 =367.5
CAS: 68497-62-1 (pramiracetam); 72869-16-0 (pramiracetam sulfate)
ATC code: N06BX16

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Pramiracetam sulfate has been used in age-related memory impairment and senile dementia. It has also been tried, without much success, as an adjunct to ECT in severe depression.

Proprietary Preparations

Italy: Neupramir.

Drug Nomenclature

Synonyms: Piritinol, hidrocloruro de; Pyrithioxine Hydrochloride
BAN: Pyritinol Hydrochloride [BANM]
INN: Pyritinol Hydrochloride [rINNM (en)]
INN: Hidrocloruro de piritinol [rINNM (es)]
INN: Pyritinol, Chlorhydrate de [rINNM (fr)]
INN: Pyritinoli Hydrochloridum [rINNM (la)]
INN: Пиритинола Гидрохлорид [rINNM (ru)]
Chemical name: 5,5-Dihydroxy-6,6-dimethyl-3,3-dithiodimethylenebis(4-pyridylmethanol) dihydochloride monohydrate
Molecular formula: C16H20N2O4S2,2HCl,H2O =459.4
CAS: 1098-97-1 (pyritinol); 10049-83-9 (anhydrous pyritinol hydrochloride)
ATC code: N06BX02

Pharmacopoeias. In China and Poland

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Pyritinol hydrochloride has been described as a nootropic that promotes the uptake of glucose by the brain. It has been used in the treatment of various cerebrovascular and mental function disorders. It has been given in a usual oral dose of 600 mg daily in 3 divided doses. Pyritinol hydrochloride has also been given as an alternative to penicillamine in rheumatoid arthritis. It is also an ingredient of various preparations promoted as tonics.

Preparations

Proprietary Preparations

Argentina: Epocan ;

Austria: Encephabol;

Chile: Encefabol;

Czech Republic: Encephabol; Enerbol;

Germany: Ardeyceryl P; Encephabol;

Hong Kong: Encephabol

Hungary: Enerbol ;

India: Encephabol;

Indonesia: Encepan; Encephabol; Enerbol;

Malaysia: Encephabol ; Fyritil;

Mexico: Bonifen ; Encephabol;

Philippines: Encephabol;

Portugal: Bonifen ; Cerbon;

Russia: Encephabol; Enerbol;

South Africa: Encephabol;

Singapore: Encephabol ;

Thailand: Encephabol; Memonol; Fyritil;

Venezuela: Aeon; Boniten; Bonitrop; Fitina; Garan.

Multi-ingredient

Argentina: Gabimex Plus;

Spain: Retulgin; Viadetres.

Drug Nomenclature

Synonyms: R-58735; Sabeluzol
BAN: Sabeluzole
USAN: Sabeluzole
INN: Sabeluzole [rINN (en)]
INN: Sabeluzol [rINN (es)]
INN: Sabéluzole [rINN (fr)]
INN: Sabeluzolum [rINN (la)]
INN: Сабелузол [rINN (ru)]
Chemical name: (±)-4-(2-Benzothiazolylmethylamino)-α[(4-fluorophenoxy)methyl]-1-piperidineethanol
Molecular formula: C22H26FN3O2S =415.5
CAS: 104153-38-0; 104383-17-7;

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Sabeluzole is a benzothiazole derivative with anticonvulsant and antihypoxic properties. It has been investigated in the treatment of Alzheimer’s disease and of sleep apnoea.

Drug Nomenclature

Synonyms: LY-246708; NNC-11-0232; Xanomelina
USAN: Xanomeline
INN: Xanomeline [rINN (en)]
INN: Xanomelina [rINN (es)]
INN: Xanoméline [rINN (fr)]
INN: Xanomelinum [rINN (la)]
INN: Ксаномелин [rINN (ru)]
Chemical name: 3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridine
Molecular formula: C14H23N3OS =281.4
CAS: 131986-45-3

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Xanomeline is a selective muscarinic M: agonist. Xanomeline tartrate has been studied in the management of Alzheimer’s disease but drugs of this type have not generally produced benefit.

 

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