insulin glulisine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	5057	207748-29-6

Description:

Molecule	Description
Synonyms: insulin glulisine insulin glulisine (genetical recombination) HMR 1964 apidra glulisine apidra insulin glulisine recombinant insulin glulisine [rDNA origin] insulin glulisine (rDNA origin)	Insulin glulisine [rDNA origin] is a rapid-acting human insulin analog used to lower blood glucose. Insulin glulisine is produced by recombinant DNA technology utilizing a non-pathogenic laboratory strain of Escherichia coli (K12). Insulin glulisine differs from human insulin in that the amino acid asparagine at position B3 is replaced by lysine and the lysine in position B29 is replaced by glutamic acid. Molecular weight: 5822.64 Formula: C258H384N64O78S6 CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: 2293.28 ALOGS: ROTB: None

Molecule

Description

Synonyms:

insulin glulisine
insulin glulisine (genetical recombination)
HMR 1964
apidra
glulisine apidra
insulin glulisine recombinant
insulin glulisine [rDNA origin]
insulin glulisine (rDNA origin)

Insulin glulisine [rDNA origin] is a rapid-acting human insulin analog used to lower blood glucose. Insulin glulisine is produced by recombinant DNA technology utilizing a non-pathogenic laboratory strain of Escherichia coli (K12). Insulin glulisine differs from human insulin in that the amino acid asparagine at position B3 is replaced by lysine and the lysine in position B29 is replaced by glutamic acid.

Molecular weight: 5822.64
Formula: C258H384N64O78S6
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA: 2293.28
ALOGS:
ROTB: None

Drug dosage:

Dose	Unit	Route
40	U	P

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Sept. 27, 2004	EMA
April 16, 2004	FDA	SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypoglycaemia	421.37	20.62	158	3834	53423	50547709
Diabetic ketoacidosis	217.19	20.62	73	3919	17799	50583333
Blood glucose increased	130.73	20.62	77	3915	71247	50529885
Hyperglycaemia	101.78	20.62	52	3940	36353	50564779
Diabetes mellitus inadequate control	92.89	20.62	36	3956	13109	50588023
Wrong product administered	81.60	20.62	26	3966	5334	50595798
Sopor	60.21	20.62	30	3962	19849	50581283
Glycosylated haemoglobin increased	50.82	20.62	22	3970	10584	50590548
Acute kidney injury	44.82	20.62	71	3921	227987	50373145
Hyperkalaemia	42.29	20.62	33	3959	48056	50553076
Product quality issue	40.48	20.62	27	3965	30831	50570301
Blood glucose abnormal	39.19	20.62	16	3976	6656	50594476
Hypoglycaemic coma	38.33	20.62	12	3980	2321	50598811
Ketoacidosis	32.30	20.62	12	3980	3883	50597249
Blood glucose decreased	28.98	20.62	18	3974	18193	50582939
Blood glucose fluctuation	28.01	20.62	11	3981	4135	50596997
Dehydration	27.88	20.62	46	3946	152403	50448729
Anti-insulin antibody positive	27.69	20.62	5	3987	87	50601045
Haemorrhagic erosive gastritis	27.61	20.62	6	3986	276	50600856
Daydreaming	26.80	20.62	6	3986	317	50600815
Exposure during pregnancy	25.54	20.62	39	3953	120976	50480156
Syncope	24.33	20.62	35	3957	102967	50498165
Simple partial seizures	23.66	20.62	6	3986	541	50600591
Thyroid cyst	23.38	20.62	6	3986	567	50600565
Lactic acidosis	23.24	20.62	20	3972	33335	50567797
Monoclonal gammopathy	22.98	20.62	6	3986	607	50600525
Hypoglycaemic unconsciousness	22.01	20.62	6	3986	716	50600416
Diabetic retinal oedema	21.38	20.62	5	3987	321	50600811

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypoglycaemia	274.20	19.77	143	4933	48203	29521248
Blood glucose increased	121.83	19.77	92	4984	58892	29510559
Wrong product administered	110.70	19.77	38	5038	4493	29564958
Blood glucose abnormal	106.42	19.77	38	5038	5045	29564406
Diabetes mellitus inadequate control	101.76	19.77	47	5029	12087	29557364
Hyperglycaemia	94.96	19.77	64	5012	34223	29535228
Blood glucose fluctuation	87.21	19.77	30	5046	3567	29565884
Intestinal haemorrhage	68.16	19.77	24	5052	3055	29566396
Hypoglycaemic coma	56.18	19.77	19	5057	2144	29567307
Anti-insulin antibody positive	52.74	19.77	11	5065	185	29569266
Diabetic ketoacidosis	46.83	19.77	31	5045	16042	29553409
Haematoma	40.84	19.77	33	5043	23179	29546272
Blood glucose decreased	39.39	19.77	25	5051	12044	29557407
Urinary incontinence	39.08	19.77	28	5048	16453	29552998
Morganella infection	38.27	19.77	10	5066	461	29568990
Ketoacidosis	36.54	19.77	16	5060	3623	29565828
Bronchial haemorrhage	34.59	19.77	10	5066	673	29568778
Glycosylated haemoglobin increased	34.49	19.77	21	5055	9405	29560046
Acute kidney injury	33.88	19.77	111	4965	265156	29304295
Waist circumference increased	33.64	19.77	10	5066	742	29568709
Anti-insulin antibody increased	30.73	19.77	6	5070	71	29569380
Mucosal haemorrhage	30.42	19.77	11	5065	1510	29567941
Cognitive disorder	30.34	19.77	28	5048	23471	29545980
Diabetic bullosis	30.11	19.77	5	5071	21	29569430
Contraindicated product administered	28.03	19.77	24	5052	18242	29551209
Hyperhidrosis	26.50	19.77	43	5033	64497	29504954
Renal failure	26.47	19.77	61	5015	118538	29450913
Balance disorder	23.53	19.77	30	5046	36140	29533311
Device operational issue	21.54	19.77	5	5071	140	29569311
Spinal pain	20.83	19.77	12	5064	4852	29564599
Sopor	20.19	19.77	16	5060	10918	29558533
Diabetic foot	19.86	19.77	9	5067	2207	29567244
General physical health deterioration	19.81	19.77	50	5026	102807	29466644

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypoglycaemia	583.15	18.39	264	7845	89628	64400995
Blood glucose increased	194.16	18.39	132	7977	97941	64392682
Diabetic ketoacidosis	181.26	18.39	84	8025	29761	64460862
Diabetes mellitus inadequate control	171.21	18.39	73	8036	21248	64469375
Hyperglycaemia	139.77	18.39	90	8019	60878	64429745
Wrong product administered	136.46	18.39	47	8062	7673	64482950
Acute kidney injury	90.81	18.39	184	7925	449056	64041567
Blood glucose abnormal	86.64	18.39	35	8074	8878	64481745
Blood glucose fluctuation	77.84	18.39	29	8080	5926	64484697
Hypoglycaemic coma	75.44	18.39	26	8083	4248	64486375
Anti-insulin antibody positive	69.50	18.39	14	8095	273	64490350
Glycosylated haemoglobin increased	67.02	18.39	35	8074	15984	64474639
Sopor	63.52	18.39	42	8067	29619	64461004
Ketoacidosis	50.14	18.39	22	8087	6841	64483782
Intestinal haemorrhage	44.62	18.39	19	8090	5495	64485128
General physical health deterioration	43.80	18.39	86	8023	204339	64286284
Blood glucose decreased	42.97	18.39	30	8079	23093	64467530
Product quality issue	34.13	18.39	29	8080	29770	64460853
Hyperkalaemia	34.05	18.39	52	8057	101077	64389546
Morganella infection	33.84	18.39	10	8099	996	64489627
Bronchial haemorrhage	31.92	18.39	10	8099	1212	64489411
Diabetic bullosis	31.87	18.39	5	8104	20	64490603
Waist circumference increased	30.79	18.39	10	8099	1361	64489262
Anti-insulin antibody increased	29.88	18.39	6	8103	115	64490508
Toxicity to various agents	29.74	18.39	5	8104	363508	64127115
Hyperhidrosis	29.73	18.39	55	8054	124865	64365758
Mucosal haemorrhage	29.41	18.39	11	8098	2270	64488353
Dehydration	28.32	18.39	75	8034	216688	64273935
Haematoma	25.08	18.39	30	8079	46220	64444403
Hypoglycaemic unconsciousness	24.46	18.39	8	8101	1113	64489510
Lactic acidosis	24.17	18.39	34	8075	61376	64429247
Product administration error	23.96	18.39	23	8086	27620	64463003
Renal failure	23.86	18.39	63	8046	181625	64308998
Thyroid cyst	22.85	18.39	6	8103	387	64490236
Haemorrhagic erosive gastritis	21.68	18.39	6	8103	472	64490151
Syncope	20.02	18.39	54	8055	157581	64333042
Diabetic foot	19.92	18.39	9	8100	2996	64487627
Simple partial seizures	19.67	18.39	6	8103	665	64489958
Monoclonal gammopathy	19.04	18.39	6	8103	741	64489882
Loss of consciousness	19.02	18.39	51	8058	148314	64342309
Hypoglycaemic seizure	18.88	18.39	6	8103	762	64489861
Diabetic retinal oedema	18.75	18.39	5	8104	342	64490281
Accidental overdose	18.57	18.39	22	8087	33535	64457088
Daydreaming	18.56	18.39	6	8103	804	64489819

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A10AB06	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES INSULINS AND ANALOGUES Insulins and analogues for injection, fast-acting
FDA CS	M0011417	Insulin
FDA Chemical/Ingredient	N0000004931	Insulin
FDA EPC	N0000175453	Insulin Analog
MeSH PA	D007004	Hypoglycemic Agents
CHEBI has role	CHEBI:35526	antidiabetic
FDA EPC	N0000175944	Insulin

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Diabetes mellitus	indication	73211009	DOID:9351

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Insulin receptor	Kinase	P06213	INSR_HUMAN	AGONIST				DRUG LABEL	DRUG LABEL

External reference:

ID	Source
7XIY785AZD	UNII
D04540	KEGG_DRUG
4021469	VUID
N0000179777	NUI
4017559	VANDF
4017569	VANDF
4019786	VANDF
4021469	VANDF
C1313386	UMLSCUI
CHEBI:5931	CHEBI
CHEMBL1201613	ChEMBL_ID
16136701	PUBCHEM_CID
DB01309	DRUGBANK_ID
8044	INN_ID
C479079	MESH_SUPPLEMENTAL_RECORD_UI
118984375	PUBCHEM_CID
DB00030	DRUGBANK_ID
253182	RXNORM
18596	MMSL
4885	MMSL
4886	MMSL
53478	MMSL
d00262	MMSL
d04369	MMSL
d05278	MMSL
126210001	SNOMEDCT_US
411530000	SNOMEDCT_US
411532008	SNOMEDCT_US
417423002	SNOMEDCT_US
420609005	SNOMEDCT_US
96367001	SNOMEDCT_US
C0795635	UMLSCUI
5186	INN_ID
000869	NDDF
000870	NDDF
006518	NDDF
010953	NDDF

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Apidra	HUMAN PRESCRIPTION DRUG LABEL	1	0088-2500	INJECTION, SOLUTION	100 [iU]	SUBCUTANEOUS	BLA	31 sections
Apidra SoloStar	HUMAN PRESCRIPTION DRUG LABEL	1	0088-2502	INJECTION, SOLUTION	100 [iU]	SUBCUTANEOUS	BLA	31 sections