Buformin
(US Adopted Name, rINN)
Drug Nomenclature
Synonyms: Buformina; DBV; W-37
USAN: Buformin
INN: Buformin [pINN (en)]
INN: Buformina [pINN (es)]
INN: Buformine [pINN (fr)]
INN: Buforminum [pINN (la)]
INN: Буформин [pINN (ru)]
Chemical name: 1-Butylbiguanide
Molecular formula: C6H15N5 =157.2
CAS: 692-13-7 (buformin); 1190-53-0 (buformin hydrochloride)
ATC code: A10BA03
Profile
Buformin is a biguanide antidiabetic. It has been given orally in the treatment of type 2 diabetes mellitus in doses of up to 300 mg daily. Buformin is also used as the hydrochloride.
Proprietary Preparations
Czech Republic: Adebit † Silubin- †
Hungary: Adebit
Spain: Silubin †
Switzerland: Silubin †
Carbutamide
Drug Approvals
(British Approved Name, rINN)
International Nonproprietary Names (INNs) in main languages (French, Latin, Spanish):
Synonyms: BZ-55; Ca-1022; Carbutamida; Carbutamidum; Glybutamide; Karbutamid; Karbutamidi; U-6987
BAN: Carbutamide
INN: Carbutamide [rINN (en)]
INN: Carbutamida [rINN (es)]
INN: Carbutamide [rINN (fr)]
INN: Carbutamidum [rINN (la)]
INN: Карбутамид [rINN (ru)]
Chemical name: 1-Butyl-3-sulphanilylurea
Molecular formula: C11H17N3O3S =271.3
CAS: 339-43-5
ATC code: A10BB06
Profile
Carbutamide is a sulfonylurea antidiabetic. It is given orally in the treatment of type 2 diabetes mellitus in single daily doses of 0.5 to 1 g, but is more toxic than chlorpropamide.
Proprietary Preparations
France: Glucidoral
Epalrestat
(rINN)
Drug Nomenclature
Synonyms: Epalrestat; ONO-2235
INN: Epalrestat [rINN (en)]
INN: Epalrestat [rINN (es)]
INN: Épalrestat [rINN (fr)]
INN: Epalrestatum [rINN (la)]
INN: Епалрестат [rINN (ru)]
Chemical name: 5-[(Z,E)-β-Methylcinnamylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid
Molecular formula: C15H13NO3S2 =319.4
CAS: 82159-09-9
Profile
Epalrestat inhibits the enzyme aldose reductase which catalyses the conversion of glucose to sorbitol. It has been suggested that accumulation of sorbitol in certain cells, occurring only in conditions of hyperglycaemia and resulting in a hyperosmotic effect, may be involved in the pathogenesis of some diabetic complications. Aldose reductase inhibitors have no influence on blood-glucose concentrations. Epalrestat is given orally for the treatment of diabetic complications including neuropathy, in a usual dose of 50 mg three times daily before meals.
Proprietary Preparations
Japan: Kinedak
Glibornuride
Drug Approvals
(British Approved Name, US Adopted Name, rINN)
INNs in other languages (French, Latin, and Spanish):
Synonyms: Glibornurid; Glibornurida; Glibornuridi; Glibornuridum; Ro-6-4563
USAN: Glibornuride
INN: Glibornuride [rINN (en)]
INN: Glibornurida [rINN (es)]
INN: Glibornuride [rINN (fr)]
INN: Glibornuridum [rINN (la)]
INN: Глиборнурид [rINN (ru)]
Chemical name: 1-[(2S,3R)-2-Hydroxyborn-3-yl]-3-tosylurea; 1-[(2S,3R)-2-Hydroxyborn-3-yl]-3-p-tolylsulphonylurea
Molecular formula: C18H26N2O4S =366.5
CAS: 26944-48-9
ATC code: A10BB04
Read code: y00Rb
Note. The name glibornuride has frequently but erroneously been applied to glibenclamide.
Profile
Glibornuride is a sulfonylurea antidiabetic. It is given orally in the treatment of type 2 diabetes mellitus in doses of 12.5 to 75 mg daily. Daily doses of 50 mg or more are given in 2 divided doses.
Proprietary Preparations
Austria: Glutril
France: Glutril
Germany: Gluborid Glutril
Switzerland: Gluborid Glutril
Turkey: Glutril
Glisentide
Drug Nomenclature
Synonyms: Glipentide; Glisentida
INN: Glisentide [rINN (en)]
INN: Glisentida [rINN (es)]
INN: Glisentide [rINN (fr)]
INN: Glisentidum [rINN (la)]
INN: Глизентид [rINN (ru)]
Chemical name: 1-Cyclopentyl-3-[p-(2-o-anisamidoethyl)benzenesulphonyl]urea
Molecular formula: C22H27N3O5S =445.5
CAS: 32797-92-5
Profile
Glisentide is a sulfonylurea antidiabetic. It is given orally in the treatment of type 2 diabetes mellitus in doses of 2.5 to 20 mg daily.
Proprietary Preparations
Spain: Staticum
Glisolamide
Drug Nomenclature
INN: Glisolamide [rINN (en)]
INN: Glisolamida [rINN (es)]
INN: Glisolamide [rINN (fr)]
INN: Glisolamidum [rINN (la)]
INN: Глизоламид [rINN (ru)]
Chemical name: 1-Cyclohexyl-3-{p-[2-(5-methylisoxazole-3-carboxamido)ethyl]benzenesulphonyl}urea
Molecular formula: C20H26N4O5S =434.5
CAS: 24477-37-0
Profile
Glisolamide is a sulfonylurea antidiabetic. It has been given in the treatment of type 2 diabetes mellitus.
Proprietary Preparations
Italy: Diabenor
Glisoxepide
Drug Nomenclature
Synonyms: Bay-b-4231; FBB-4231; Glisoxepid; Glisoxepida; RP-22410
BAN: Glisoxepide
INN: Glisoxepide [rINN (en)]
INN: Glisoxepida [rINN (es)]
INN: Glisoxépide [rINN (fr)]
INN: Glisoxepidum [rINN (la)]
INN: Глизоксепид [rINN (ru)]
Chemical name: 1-(Perhydroazepin-1-yl)-3-{4-[2-(5-methylisoxazole-3-carboxamido)ethyl]benzenesulphonyl}urea
Molecular formula: C20H27N5O5S =449.5
CAS: 25046-79-1
ATC code: A10BB11
Profile
Glisoxepide is a sulfonylurea antidiabetic. It has been given in the treatment of type 2 diabetes mellitus.
Proprietary Preparations
Austria: Pro-Diaban
Glybuzole
Drug Nomenclature
Synonyms: AN-1324; Désaglybuzole; Glibuzol; RP-7891
INN: Glybuzole [rINN (en)]
INN: Glibuzol [rINN (es)]
INN: Glybuzole [rINN (fr)]
INN: Glybuzolum [rINN (la)]
INN: Глибузол [rINN (ru)]
Chemical name: N-(5-tert-Butyl-1,3,4-thiadiazol-2-yl)benzenesulphonamide
Molecular formula: C12H15N3O2S2 =297.4
CAS: 1492-02-0
Profile
Glybuzole is an oral antidiabetic with a structure distinct from that of the sulfonylureas, biguanides, or sulfonamidopyrimidines.
Proprietary Preparations
Japan: Gludiase
Glycyclamide
Drug Nomenclature
Synonyms: Gliciclamida; Gliciclamide; K-38; K-386; Tolcyclamide
INN: Glycyclamide [rINN (en)]
INN: Gliciclamida [rINN (es)]
INN: Glycyclamide [rINN (fr)]
INN: Glycyclamidum [rINN (la)]
INN: Глицикламид [rINN (ru)]
Chemical name: 1-Cyclohexyl-3-tosylurea; 1-Cyclohexyl-3-p-tolylsulphonylurea
Molecular formula: C14H20N2O3S =296.4
CAS: 664-95-9
Profile
Glycyclamide is a sulfonylurea antidiabetic. It is given by mouth in the treatment of type 2 diabetes mellitus.
Preparations
Proprietary Preparations
Italy: Diaborale
Mitiglinide
INN: Mitiglinide [rINN (en)]
INN: Mitiglinida [rINN (es)]
INN: Mitiglinide [rINN (fr)]
INN: Mitiglinidum [rINN (la)]
INN: Митиглинид [rINN (ru)]
Chemical name: (-)-(2S,3a,7a-cis)-αBenzylhexahydro-γ-oxo-2-isoindolinebutyric acid
Molecular formula: C19H25NO3 =315.4
CAS: 145375-43-5 (mitiglinide); 145525-41-3 (anhydrous mitiglinide calcium); 207844-01-7 (mitiglinide calcium dihydrate)
Profile
Mitiglinide is a meglitinide antidiabetic that is under investiga tion in the treatment of type 2 diabetes mellitus.
Muraglitazar
Synonyms: BMS-298585
USAN: Muraglitazar
INN: Muraglitazar [rINN (en)]
INN: Muraglitazar [rINN (es)]
INN: Muraglitazar [rINN (fr)]
INN: Muraglitazarum [rINN (la)]
INN: Мураглитазар [rINN (ru)]
Chemical name: {[(4-Methoxyphenoxy)carbonyl]{4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]benzyl}amino}acetic acid
Molecular formula: C29H28N2O7 =516.5
CAS: 331741-94-7
Profile
Muraglitazar is a dual alfa/gamma peroxisome proliferator-activated receptor (PPAR) activator. It has been investigated in the treatment of type 2 diabetes mellitus.
Adverse effects. A review of data from 5 studies suggested that muraglitazar may be associated with an increased risk of adverse cardiovascular events and heart failure.
Phenformin Hydrochloride
Synonyms: Fenformina Cloridrato; Fenformina, hidrocloruro de
INN: Hidrocloruro de fenformina [pINNM (es)]
INN: Phenformine, Chlorhydrate de [pINNM (fr)]
INN: Phenformini Hydrochloridum [pINNM (la)]
INN: Фенформина Гидрохлорид [pINNM (ru)]
Chemical name: 1-Phenethylbiguanide hydrochloride
Molecular formula: C10H15N5,HCl =241.7
ATC code: A10BA01
Pharmacopoeias. In China
Profile
Phenformin hydrochloride is a biguanide antidiabetic. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries for the treatment of type 2 diabetes mellitus.
Phenformin was implicated in the controversial reports of excess cardiovascular mortality associated with oral hypoglycaemic therapy (see under Sulfonylureas, Effects on the Cardiovascular System).
Proprietary Preparations
Greece: Informin
India: DBI
Portugal: Debeina
Multi-ingredient
Greece: Daopar †
India: Chlorformin †
Italy: Bi-Euglucon Bidiabe Gliben † Gliformin Suguan
Pimagedine
INN: Pimagedine [rINN (en)]
INN: Pimagedina [rINN (es)]
INN: Pimagédine [rINN (fr)]
INN: Pimagedinum [rINN (la)]
INN: Пимагедин [rINN (ru)]
Chemical name: Aminoguanidine
Molecular formula: CH6N4 =74.09
CAS: 79-17-4
Pimagedine Hydrochloride
Drug Approvals
(US Adopted Name, rINNM)
INNs in main languages (French, Latin, and Spanish):
Synonyms: GER-11
USAN: Pimagedine Hydrochloride
INN: Pimagedine Hydrochloride [rINNM (en)]
INN: Hidrocloruro de pimagedina [rINNM (es)]
INN: Pimagédine, Chlorhydrate de [rINNM (fr)]
INN: Pimagedini Hydrochloridum [rINNM (la)]
INN: Пимагедина Гидрохлорид [rINNM (ru)]
Chemical name: Aminoguanidine monohydrochloride
Molecular formula: CH6N4,HCl =110.5
CAS: 1937-19-5
Profile
Pimagedine reportedly inhibits the formation of glycosylated proteins (advanced glycosylation end-products) and has other actions including inhibition of aldose reductase. It has been investigated for the prevention of diabetic complications.
Ruboxistaurin
Synonyms: LY-333531; LY-341684 (ruboxistaurin mesilate)
INN: Ruboxistaurin [rINN (en)]
INN: Ruboxistaurina [rINN (es)]
INN: Ruboxistaurine [rINN (fr)]
INN: Ruboxistaurinum [rINN (la)]
INN: Рубоксистаурин [rINN (ru)]
Chemical name: (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,19H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-18,20-dione
Molecular formula: C28H28N4O3 =468.5
CAS: 169939-94-0 (ruboxistaurin); 169939-93-9 (ruboxistaurin hydrochloride); 202260-21-7 (ruboxistaurin mesilate)
Profile
Ruboxistaurin is an oral inhibitor of the p-isoform of the enzyme protein kinase C, which is thought to play a role in the development of diabetic microvascular complications. It is under investigation as an adjunct in the treatment of diabetic retinopathy.
Voglibose
Pharmacopoeias. In Japan.
Synonyms: A-71100; AO-128; Voglibosa
USAN: Voglibose
INN: Voglibose [rINN (en)]
INN: Voglibosa [rINN (es)]
INN: Voglibose [rINN (fr)]
INN: Voglibosum [rINN (la)]
INN: Воглибоза [rINN (ru)]
Chemical name: 3,4-Dideoxy-4-{[2-hydroxy-1-(hydroxymethyl)ethyl]amino}-2-C-(hydroxymethyl)-D-epi-inositol
Molecular formula: C10H21NO7 =267.3
CAS: 83480-29-9
ATC code: A10BF03
Profile
Voglibose is an alpha-glue osidase inhibitor with general properties similar to those of acarbose. It is used in the treatment of diabetes mellitus in oral doses of 200 to 300 micrograms three times daily before meals.
Hepatic encephalopathy. Vbglibose has been investigated in the management of hepatic encephalopathy.
Proprietary Preparations
Japan: Basen
Philippines: Basen
Thailand: Basen.