Identification

Name
Insulin Glulisine
Accession Number
DB01309
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Hormones / Insulins
Description

Insulin glulisine is a biosynthetic, rapid-acting human insulin analogue produced in a non-pathogenic laboratory strain of Escherichia coli (K12). This recombinant hormone differs from native human insulin in that the amino acid arginine at position B3 is replaced by lysine and the lysine at position B29 is replaced by glutamic acid. These structural modifications decrease hexamer formation, stabilize insulin glulisine monomers and increase the rate of absorption and onset of action compared to human insulin.

Protein chemical formula
C258H384N64O78S6
Protein average weight
5823.0 Da
Sequences
>A chain
GIVEQCCTSICSLYQLENYCN
>B chain
FVKQHLCGSHLVEALYLVCGERGFFYTPET
Download FASTA Format
Synonyms
  • Insulin Glulisine (recombinant DNA origin)
  • Insulin glulisine recombinant
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ApidraInjection, solution100 Units/mlSubcutaneousSanofi Aventis Deutschland Gmb H2004-09-27Not applicableEu
ApidraInjection, solution100 Units/mlSubcutaneousSanofi Aventis Deutschland Gmb H2004-09-27Not applicableEu
ApidraInjection, solution100 Units/mlSubcutaneousSanofi Aventis Deutschland Gmb H2004-09-27Not applicableEu
ApidraInjection, solution100 Units/mlIntravenous; SubcutaneousSanofi Aventis Deutschland Gmb H2004-09-27Not applicableEu
ApidraInjection, solution100 Units/mlSubcutaneousSanofi Aventis Deutschland Gmb H2004-09-27Not applicableEu
ApidraSolution100 unitSubcutaneousSanofi Aventis2008-09-22Not applicableCanada
ApidraInjection, solution100 Units/mlSubcutaneousSanofi Aventis Deutschland Gmb H2004-09-27Not applicableEu
ApidraInjection, solution100 Units/mlIntravenous; SubcutaneousSanofi Aventis Deutschland Gmb H2004-09-27Not applicableEu
ApidraInjection, solution100 Units/mlSubcutaneousSanofi Aventis Deutschland Gmb H2004-09-27Not applicableEu
ApidraSolution100 unitSubcutaneousSanofi AventisNot applicableNot applicableCanada
Categories
UNII
7XIY785AZD
CAS number
207748-29-6

Pharmacology

Indication

For the treatment of Type 1 and 2 diabetes mellitus. Should be used in regimens including a long-acting or basal insulin analogue unless it is used in a continuous infusion pump. May be used with oral antidiabetic agents.

Structured Indications
Pharmacodynamics

Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, a basal level of insulin is supplemented with insulin spikes following meals. Postprandial insulin spikes are responsible for the metabolic changes that occur as the body transitions from a postabsorptive to absorptive state. Insulin promotes cellular uptake of glucose, particularly in muscle and adipose tissues, promotes energy storage via glycogenesis, opposes catabolism of energy stores, increases DNA replication and protein synthesis by stimulating amino acid uptake by liver, muscle and adipose tissue, and modifies the activity of numerous enzymes involved in glycogen synthesis and glycolysis. Insulin also promotes growth and is required for the actions of growth hormone (e.g. protein synthesis, cell division, DNA synthesis). Insulin glulisine is a rapid-acting insulin analogue used to mimic postprandial insulin spikes in diabetic individuals. The onset of action of insulin glulisine is approximately 15 minutes. Its activity peaks 60 minutes following subcutaneous injection and its duration of action is 2-4 hours.

Mechanism of action

Insulin glulisine binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor autophosphorylates and phosphorylates numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. Activation of these proteins leads to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC), both of which play critical roles in metabolism and catabolism. In humans, insulin is stored in the form of hexamers; however, only insulin monomers are able to interact with IR. Substitution of the arginine at position B3 for lysine and replacement of the B29 lysine with glutamic acid decreases the propensity to form hexamers, stabilizes the hormone in monomeric form and results in a rapid rate of absorption and short duration of action.

TargetActionsOrganism
AInsulin receptor
agonist
Human
Absorption

Compared to regular human insulin, insulin glulisine is faster absorbed. When 0.15 units/kg was subcutaneously administered to type 1 diabetes patients, the pharmacokinetic parameters are as follows: Tmax = 60 minutes (range of 40 - 120 minutes); Cmax = 83 microUnits/mL (range of 40 - 131 microUnits/mL). Absolute bioavailability following subcutaneous administration is approximately 70%, regardless of site of injection.

Volume of distribution

13 L

Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

Elimination half life= 42 minutes (following subcutaneous injection)

Clearance
Not Available
Toxicity

Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Neuroglycopenic signs and symptoms of hypoglycemia include difficulty concentrating, lethargy/weakness, confusion, drowsiness, vision changes, difficulty speaking, headache, and dizziness. Mild hypoglycemia is characterized by the presence of autonomic symptoms. Moderate hypoglycemia is characterized by the presence of autonomic and neuroglycopenic symptoms. Individuals may become unconscious in severe cases of hypoglycemia.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2,4-thiazolidinedione2,4-thiazolidinedione may increase the hypoglycemic activities of Insulin Glulisine.Investigational
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Insulin Glulisine.Experimental
AcarboseAcarbose may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Insulin Glulisine.Investigational, Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Insulin Glulisine.Approved, Vet Approved
AICA ribonucleotideAICA ribonucleotide may increase the hypoglycemic activities of Insulin Glulisine.Experimental, Investigational
AlaproclateAlaproclate may increase the hypoglycemic activities of Insulin Glulisine.Experimental
AllicinAllicin may increase the hypoglycemic activities of Insulin Glulisine.Investigational
AlogliptinAlogliptin may increase the hypoglycemic activities of Insulin Glulisine.Approved
AloxiprinAloxiprin may increase the hypoglycemic activities of Insulin Glulisine.Experimental
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Insulin Glulisine.Approved
AmphetamineAmphetamine may increase the hypoglycemic activities of Insulin Glulisine.Approved, Illicit
AripiprazoleThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Asenapine.Approved
AtazanavirThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Atazanavir.Approved, Investigational
BalaglitazoneBalaglitazone may increase the hypoglycemic activities of Insulin Glulisine.Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
Bempedoic acidBempedoic acid may increase the hypoglycemic activities of Insulin Glulisine.Investigational
BendroflumethiazideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
BetamethasoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BrexpiprazoleThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Brexpiprazole.Approved
BrofaromineBrofaromine may increase the hypoglycemic activities of Insulin Glulisine.Experimental
BuforminBuformin may increase the hypoglycemic activities of Insulin Glulisine.Investigational, Withdrawn
BumetanideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Bumetanide.Approved
BuserelinThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Buserelin.Approved
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Insulin Glulisine.Approved
Carbaspirin calciumCarbaspirin calcium may increase the hypoglycemic activities of Insulin Glulisine.Experimental, Investigational
CarbutamideCarbutamide may increase the hypoglycemic activities of Insulin Glulisine.Experimental
CaroxazoneCaroxazone may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
CastanospermineCastanospermine may increase the hypoglycemic activities of Insulin Glulisine.Experimental
CeritinibThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Ceritinib.Approved
ChlorothiazideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Insulin Glulisine.Approved
ChlorthalidoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Chlorthalidone.Approved
CiglitazoneCiglitazone may increase the hypoglycemic activities of Insulin Glulisine.Experimental
CinoxacinCinoxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational, Withdrawn
CitalopramCitalopram may increase the hypoglycemic activities of Insulin Glulisine.Approved
ClozapineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Clozapine.Approved
CorticotropinThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Cortisone acetate.Approved
CyclopenthiazideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Cyclopenthiazide.Experimental
Cyproterone acetateThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Insulin Glulisine.Investigational
DarunavirThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Darunavir.Approved
DeoxyspergualinDeoxyspergualin may increase the hypoglycemic activities of Insulin Glulisine.Investigational
dersalazinedersalazine may increase the hypoglycemic activities of Insulin Glulisine.Investigational
DesogestrelThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Insulin Glulisine.Approved
DexamethasoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Diazoxide.Approved
DienogestThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Dienogest.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Insulin Glulisine.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Insulin Glulisine.Illicit
DisopyramideDisopyramide may increase the hypoglycemic activities of Insulin Glulisine.Approved
DrospirenoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Drospirenone.Approved
DulaglutideDulaglutide may increase the hypoglycemic activities of Insulin Glulisine.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Insulin Glulisine.Approved
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Insulin Glulisine.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
EpinephrineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Epinephrine.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
EstradiolThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Estrone sulfate.Approved
Etacrynic acidThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Ethinyl Estradiol.Approved
Ethynodiol diacetateThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
EverolimusThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Everolimus.Approved
ExenatideExenatide may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
FleroxacinFleroxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved
FludrocortisoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Fludrocortisone.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
FluoxetineFluoxetine may increase the hypoglycemic activities of Insulin Glulisine.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Illicit
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
FosamprenavirThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Fosamprenavir.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational, Vet Approved
FurosemideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Furosemide.Approved, Vet Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Insulin Glulisine.Investigational
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
GlibornurideGlibornuride may increase the hypoglycemic activities of Insulin Glulisine.Investigational, Withdrawn
GliclazideGliclazide may increase the hypoglycemic activities of Insulin Glulisine.Approved
GlimepirideGlimepiride may increase the hypoglycemic activities of Insulin Glulisine.Approved
GlipizideGlipizide may increase the hypoglycemic activities of Insulin Glulisine.Approved
GliquidoneGliquidone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
GLPG-0492GLPG-0492 may increase the hypoglycemic activities of Insulin Glulisine.Investigational
GlyburideGlyburide may increase the hypoglycemic activities of Insulin Glulisine.Approved
GoserelinThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Insulin Glulisine.Investigational, Withdrawn
GuacetisalGuacetisal may increase the hypoglycemic activities of Insulin Glulisine.Experimental
GusperimusGusperimus may increase the hypoglycemic activities of Insulin Glulisine.Investigational
HarmalineHarmaline may increase the hypoglycemic activities of Insulin Glulisine.Experimental
Hemoglobin crosfumarilHemoglobin crosfumaril may increase the hypoglycemic activities of Insulin Glulisine.Experimental
HistrelinThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Insulin Glulisine.Experimental
HydrochlorothiazideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Hydroflumethiazide.Approved, Investigational
Hydroxyprogesterone caproateThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IloperidoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Iloperidone.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Insulin Glulisine.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Indapamide.Approved
IndinavirThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Indinavir.Approved
Insulin AspartInsulin Aspart may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin DetemirInsulin Detemir may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanInsulin Human may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Insulin Glulisine.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Insulin Glulisine.Approved
LanreotideInsulin Glulisine may increase the hypoglycemic activities of Lanreotide.Approved
LeuprolideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Insulin Glulisine.Approved
LevonorgestrelThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LinagliptinLinagliptin may increase the hypoglycemic activities of Insulin Glulisine.Approved
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Insulin Glulisine.Approved, Nutraceutical
LiraglutideLiraglutide may increase the hypoglycemic activities of Insulin Glulisine.Approved
LopinavirThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Lopinavir.Approved
LurasidoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Lurasidone.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
MecaserminMecasermin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MesalazineMesalazine may increase the hypoglycemic activities of Insulin Glulisine.Approved
MesteroloneMesterolone may increase the hypoglycemic activities of Insulin Glulisine.Experimental
MestranolThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Mestranol.Approved
MetforminMetformin may increase the hypoglycemic activities of Insulin Glulisine.Approved
MethotrimeprazineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Methyclothiazide.Approved
Methyl salicylateMethyl salicylate may increase the hypoglycemic activities of Insulin Glulisine.Approved, Vet Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
MethylprednisoloneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Insulin Glulisine.Approved
MetolazoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Metolazone.Approved
MifepristoneMifepristone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
MiglitolMiglitol may increase the hypoglycemic activities of Insulin Glulisine.Approved
MiglustatMiglustat may increase the hypoglycemic activities of Insulin Glulisine.Approved
MilnacipranMilnacipran may increase the hypoglycemic activities of Insulin Glulisine.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Insulin Glulisine.Approved
MitiglinideMitiglinide may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
MoclobemideMoclobemide may increase the hypoglycemic activities of Insulin Glulisine.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
NandroloneNandrolone may increase the hypoglycemic activities of Insulin Glulisine.Experimental, Investigational
Nandrolone decanoateNandrolone decanoate may increase the hypoglycemic activities of Insulin Glulisine.Approved, Illicit
NateglinideNateglinide may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
NefazodoneNefazodone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Withdrawn
NelfinavirThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Insulin Glulisine.Investigational
NiacinThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
NilotinibThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Insulin Glulisine.Investigational
NorethisteroneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved
NorgestimateThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Norgestimate.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
OctreotideOctreotide may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
OlanzapineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Olanzapine.Approved, Investigational
OlsalazineOlsalazine may increase the hypoglycemic activities of Insulin Glulisine.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
Oxolinic acidOxolinic acid may increase the hypoglycemic activities of Insulin Glulisine.Experimental
OxymetholoneOxymetholone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Illicit
PaliperidoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Paliperidone.Approved
PargylinePargyline may increase the hypoglycemic activities of Insulin Glulisine.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
PasireotideInsulin Glulisine may increase the hypoglycemic activities of Pasireotide.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Insulin Glulisine.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Insulin Glulisine.Approved
PentamidinePentamidine may increase the hypoglycemic activities of Insulin Glulisine.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Insulin Glulisine.Approved
PhenforminPhenformin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational, Withdrawn
PheniprazinePheniprazine may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
PioglitazonePioglitazone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
Pipemidic acidPipemidic acid may increase the hypoglycemic activities of Insulin Glulisine.Experimental
PiperazineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Pipotiazine.Approved, Investigational
PirlindolePirlindole may increase the hypoglycemic activities of Insulin Glulisine.Approved
Piromidic acidPiromidic acid may increase the hypoglycemic activities of Insulin Glulisine.Experimental
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
PolythiazideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Polythiazide.Approved
PramlintidePramlintide may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
PrednisoloneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Prednisone.Approved, Vet Approved
ProcarbazineProcarbazine may increase the hypoglycemic activities of Insulin Glulisine.Approved
ProgesteroneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Progesterone.Approved, Vet Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Insulin Glulisine.Investigational
QuetiapineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Quinethazone.Approved
QuinineQuinine may increase the hypoglycemic activities of Insulin Glulisine.Approved
RasagilineRasagiline may increase the hypoglycemic activities of Insulin Glulisine.Approved
RepaglinideRepaglinide may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
RisperidoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Ritonavir.Approved, Investigational
RosiglitazoneRosiglitazone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
RufloxacinRufloxacin may increase the hypoglycemic activities of Insulin Glulisine.Experimental
SafrazineSafrazine may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Insulin Glulisine.Approved, Vet Approved
SaquinavirThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Saquinavir.Approved, Investigational
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Insulin Glulisine.Approved
SelegilineSelegiline may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational, Vet Approved
SertralineSertraline may increase the hypoglycemic activities of Insulin Glulisine.Approved
SirolimusThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Sirolimus.Approved, Investigational
SitafloxacinSitafloxacin may increase the hypoglycemic activities of Insulin Glulisine.Experimental, Investigational
SitagliptinSitagliptin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
SotagliflozinSotagliflozin may increase the hypoglycemic activities of Insulin Glulisine.Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
StanozololStanozolol may increase the hypoglycemic activities of Insulin Glulisine.Approved, Vet Approved
SulfadiazineSulfadiazine may increase the hypoglycemic activities of Insulin Glulisine.Approved, Vet Approved
SulfamethoxazoleSulfamethoxazole may increase the hypoglycemic activities of Insulin Glulisine.Approved
SulfisoxazoleSulfisoxazole may increase the hypoglycemic activities of Insulin Glulisine.Approved, Vet Approved
SulodexideSulodexide may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
SunitinibSunitinib may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
TacrolimusThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Tacrolimus.Approved, Investigational
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
TemsirolimusThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Temsirolimus.Approved
TestosteroneTestosterone may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
Testosterone PropionateTestosterone Propionate may increase the hypoglycemic activities of Insulin Glulisine.Approved, Vet Approved
TipranavirThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Tipranavir.Approved, Investigational
TolazamideTolazamide may increase the hypoglycemic activities of Insulin Glulisine.Approved
TolbutamideTolbutamide may increase the hypoglycemic activities of Insulin Glulisine.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Insulin Glulisine.Approved
TorasemideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Torasemide.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Insulin Glulisine.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Insulin Glulisine.Approved
TriamcinoloneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TriptorelinThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TroglitazoneTroglitazone may increase the hypoglycemic activities of Insulin Glulisine.Investigational, Withdrawn
Trolamine salicylateTrolamine salicylate may increase the hypoglycemic activities of Insulin Glulisine.Approved
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational, Withdrawn
VenlafaxineVenlafaxine may increase the hypoglycemic activities of Insulin Glulisine.Approved
VildagliptinVildagliptin may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
VogliboseVoglibose may increase the hypoglycemic activities of Insulin Glulisine.Approved, Investigational
VorinostatThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Vorinostat.Approved, Investigational
ZimelidineZimelidine may increase the hypoglycemic activities of Insulin Glulisine.Withdrawn
ZiprasidoneThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Ziprasidone.Approved
Food Interactions
Not Available

References

General References
  1. Arnolds S, Rave K, Hovelmann U, Fischer A, Sert-Langeron C, Heise T: Insulin glulisine has a faster onset of action compared with insulin aspart in healthy volunteers. Exp Clin Endocrinol Diabetes. 2010 Oct;118(9):662-4. doi: 10.1055/s-0030-1252067. Epub 2010 Apr 28. [PubMed:20429049]
  2. Becker RH: Insulin glulisine complementing basal insulins: a review of structure and activity. Diabetes Technol Ther. 2007 Feb;9(1):109-21. [PubMed:17316105]
  3. Becker RH, Frick AD: Clinical pharmacokinetics and pharmacodynamics of insulin glulisine. Clin Pharmacokinet. 2008;47(1):7-20. [PubMed:18076215]
  4. Cox SL: Insulin glulisine. Drugs Today (Barc). 2005 Jul;41(7):433-40. [PubMed:16193096]
  5. Garnock-Jones KP, Plosker GL: Insulin glulisine: a review of its use in the management of diabetes mellitus. Drugs. 2009 May 29;69(8):1035-57. doi: 10.2165/00003495-200969080-00006. [PubMed:19496630]
  6. Horvath K, Bock G, Regittnig W, Bodenlenz M, Wutte A, Plank J, Magnes C, Sinner F, Furst-Recktenwald S, Theobald K, Pieber TR: Insulin glulisine, insulin lispro and regular human insulin show comparable end-organ metabolic effects: an exploratory study. Diabetes Obes Metab. 2008 Jun;10(6):484-91. Epub 2007 Aug 30. [PubMed:17764465]
  7. Authors unspecified: Insuline glusine (Apidra): a new rapid-acting insulin. Med Lett Drugs Ther. 2006 Apr 24;48(1233):33-4. [PubMed:16625142]
  8. Robinson DM, Wellington K: Insulin glulisine. Drugs. 2006;66(6):861-9. [PubMed:16706558]
  9. Ulrich H, Snyder B, Garg SK: Combining insulins for optimal blood glucose control in type I and 2 diabetes: focus on insulin glulisine. Vasc Health Risk Manag. 2007;3(3):245-54. [PubMed:17703632]
External Links
KEGG Drug
D04540
PubChem Substance
46504450
ChEMBL
CHEMBL1201613
Therapeutic Targets Database
DAP001093
PharmGKB
PA164760859
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Insulin_glulisine
ATC Codes
A10AB06 — Insulin glulisine
AHFS Codes
  • 68:20.08 — Insulins
FDA label
Download (1.67 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceDiabetes1
1CompletedTreatmentDiabetes Mellitus (DM)1
1CompletedTreatmentDiabetes, Diabetes Mellitus Type 13
1CompletedTreatmentDiabetes / Type 2 Diabetes Mellitus1
1CompletedTreatmentType 2 Diabetes Mellitus2
1RecruitingTreatmentDown Syndrome (DS)1
1RecruitingTreatmentType1 Diabetes Mellitus1
2Active Not RecruitingTreatmentDiabetes During Pregnancy1
2CompletedTreatmentAlzheimer's Disease (AD)1
2CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
2CompletedTreatmentType 2 Diabetes Mellitus1
2RecruitingTreatmentAlzheimer's Disease (AD) / Mild Cognitive Impairment (MCI)1
3CompletedTreatmentCardiovascular Disease (CVD) / Hyperglycemias / Myocardial Infarction (MI)1
3CompletedTreatmentDiabetes Mellitus (DM)3
3CompletedTreatmentDiabetes Mellitus, Insulin-Dependent1
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 12
3CompletedTreatmentPoor Glycemic Control1
3CompletedTreatmentType 2 Diabetes Mellitus9
3CompletedTreatmentType I Diabetes1
3RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
3TerminatedTreatmentAMI1
4CompletedTreatmentDiabetes Mellitus (DM)1
4CompletedTreatmentDiabetes Mellitus (DM) / Diabetic Kidney Disease / Diabetic Nephropathies / Glucagon-Like Peptide 11
4CompletedTreatmentDiabetes, Diabetes Mellitus Type 110
4CompletedTreatmentDiabetes / Hyperglycemias1
4CompletedTreatmentHyperglycemias / Type 2 Diabetes Mellitus1
4CompletedTreatmentImpaired Renal Function / Type 2 Diabetes Mellitus1
4CompletedTreatmentInpatient Hyperglycemia / Type 2 Diabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus10
4Enrolling by InvitationTreatmentDiabetes, Diabetes Mellitus Type 1 / Lipoatrophy1
4Not Yet RecruitingTreatmentType2 Diabetes1
4RecruitingTreatmentDiabetes type11
4RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
4RecruitingTreatmentPatient With Type 2 Diabetes Treated With Insulin Using a Baseline/Bolus Strategy1
4RecruitingTreatmentType 2 Diabetes Mellitus1
4TerminatedTreatmentType 2 Diabetes Mellitus3
4Unknown StatusTreatmentDiabetes, Diabetes Mellitus Type 11
4Unknown StatusTreatmentInsulin-requiring Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentLiver Cirrhosis / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentType 2 Diabetes Mellitus1
Not AvailableCompletedSupportive CareDiabetes, Diabetes Mellitus Type 11
Not AvailableCompletedTreatmentDiabetes or With New Hyperglycemia1
Not AvailableCompletedTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus1
Not AvailableNot Yet RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableTerminatedTreatmentChronic Obstructive Pulmonary Disease (COPD) / Hyperglycemias1
Not AvailableUnknown StatusTreatmentDiabetes Mellitus (DM)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionIntravenous; Subcutaneous100 Units/ml
Injection, solutionSubcutaneous100 [iU]/mL
Injection, solutionSubcutaneous100 Units/ml
SolutionSubcutaneous100 unit
Prices
Unit descriptionCostUnit
Apidra 100 unit/ml cartridge13.3USD ml
Apidra 100 unit/ml Cartridge3.56USD cartridge
Apidra 100 unit/ml Syringe3.56USD syringe
Apidra 100 unit/ml2.67USD cartridge
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US9011391No2004-03-262024-03-26Us
US9233211No2004-03-022024-03-02Us
US8603044No2004-03-022024-03-02Us
US8512297No2004-09-152024-09-15Us
US8679069No2005-04-122025-04-12Us
US8992486No2004-06-052024-06-05Us
US8556864No2004-03-032024-03-03Us
US7918833Yes2008-03-232028-03-23Us
US6221633No1998-06-182018-06-18Us
US6960561No2003-01-252023-01-25Us
US7696162No2002-03-222022-03-22Us
US7452860No2002-03-222022-03-22Us
US9561331No2004-08-282024-08-28Us
US9623189No2004-08-192024-08-19Us
US9610409No2004-03-022024-03-02Us
US9526844No2004-03-022024-03-02Us
US9604008No2004-03-022024-03-02Us
US9533105No2004-08-172024-08-17Us
US9408979No2004-03-022024-03-02Us
US9775954No2004-03-022024-03-02Us

Properties

State
Liquid
Experimental Properties
Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Receptor signaling protein tyrosine kinase activity
Specific Function
Receptor tyrosine kinase which mediates the pleiotropic actions of insulin. Binding of insulin leads to phosphorylation of several intracellular substrates, including, insulin receptor substrates (...
Gene Name
INSR
Uniprot ID
P06213
Uniprot Name
Insulin receptor
Molecular Weight
156331.465 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Sciacca L, Cassarino MF, Genua M, Pandini G, Le Moli R, Squatrito S, Vigneri R: Insulin analogues differently activate insulin receptor isoforms and post-receptor signalling. Diabetologia. 2010 Aug;53(8):1743-53. doi: 10.1007/s00125-010-1760-6. Epub 2010 Apr 28. [PubMed:20424816]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Drug created on June 30, 2007 08:46 / Updated on November 19, 2017 20:34