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	439.62	19.82	165	4503	59900	63424454
Diabetic ketoacidosis	264.05	19.82	86	4582	20419	63463935
Blood glucose increased	169.19	19.82	94	4574	83662	63400692
Hyperglycaemia	149.12	19.82	69	4599	41798	63442556
Diabetes mellitus inadequate control	101	19.82	39	4629	15087	63469267
Wrong product administered	92.25	19.82	29	4639	6112	63478242
Acute kidney injury	82.57	19.82	99	4569	263316	63221038
Sopor	62.04	19.82	31	4637	22133	63462221
Glycosylated haemoglobin increased	55.46	19.82	24	4644	12374	63471980
Blood glucose abnormal	47.90	19.82	19	4649	7873	63476481
Hypoglycaemic coma	46.46	19.82	14	4654	2561	63481793
Hyperkalaemia	42.97	19.82	34	4634	54169	63430185
Ketoacidosis	42.97	19.82	15	4653	4363	63479991
Blood glucose decreased	40.77	19.82	23	4645	20929	63463425
Product quality issue	38.51	19.82	27	4641	35838	63448516
Product prescribing error	35.94	19.82	23	4645	26266	63458088
Blood glucose fluctuation	34.86	19.82	13	4655	4563	63479791
Anti-insulin antibody positive	34.06	19.82	6	4662	97	63484257
Dehydration	34.03	19.82	52	4616	173302	63311052
General physical health deterioration	33.48	19.82	56	4612	201346	63283008
Exposure during pregnancy	28.20	19.82	45	4623	155502	63328852
Lactic acidosis	28.17	19.82	23	4645	38264	63446090
Daydreaming	26.52	19.82	6	4662	357	63483997
Syncope	25.57	19.82	37	4631	117348	63367006
Haemorrhagic erosive gastritis	24.94	19.82	6	4662	467	63483887
Simple partial seizures	23.80	19.82	6	4662	567	63483787
Cerebrovascular accident	23.46	19.82	34	4634	107990	63376364
Thyroid cyst	23.46	19.82	6	4662	601	63483753
Monoclonal gammopathy	22.79	19.82	6	4662	673	63483681
Hypoglycaemic unconsciousness	21.99	19.82	6	4662	771	63483583
Diabetic retinal oedema	21.64	19.82	5	4663	327	63484027

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	277.14	20.51	152	6074	54488	34896217
Hyperglycaemia	189.40	20.51	106	6120	39374	34911331
Blood glucose increased	134.18	20.51	104	6122	66614	34884091
Blood glucose abnormal	124.89	20.51	45	6181	5907	34944798
Blood glucose fluctuation	117.52	20.51	39	6187	4005	34946700
Diabetes mellitus inadequate control	110.58	20.51	52	6174	13412	34937293
Wrong product administered	106.95	20.51	39	6187	5295	34945410
Intestinal haemorrhage	79.25	20.51	28	6198	3468	34947237
Glycosylated haemoglobin increased	69.75	20.51	36	6190	11324	34939381
Metabolic acidosis	62.50	20.51	56	6170	43624	34907081
Anti-insulin antibody positive	58.00	20.51	12	6214	186	34950519
Hypoglycaemic coma	57.12	20.51	20	6206	2411	34948294
Haematoma	49.36	20.51	39	6187	25566	34925139
Blood glucose decreased	43.70	20.51	28	6198	13209	34937496
Urinary incontinence	43.53	20.51	32	6194	18842	34931863
Diabetic ketoacidosis	42.56	20.51	31	6195	18001	34932704
Morganella infection	36.88	20.51	10	6216	512	34950193
Ketoacidosis	36.70	20.51	17	6209	4226	34946479
Bronchial haemorrhage	33.85	20.51	10	6216	699	34950006
Pulmonary oedema	33.83	20.51	42	6184	47487	34903218
Cognitive disorder	31.87	20.51	32	6194	28661	34922044
Contraindicated product administered	31.61	20.51	28	6198	21453	34929252
Waist circumference increased	31.44	20.51	10	6216	896	34949809
Balance disorder	30.67	20.51	37	6189	40617	34910088
Hyperhidrosis	30.45	20.51	51	6175	75641	34875064
Anti-insulin antibody increased	30.27	20.51	6	6220	74	34950631
Acute kidney injury	29.78	20.51	120	6106	304868	34645837
Mucosal haemorrhage	29.31	20.51	11	6215	1614	34949091
Diabetic bullosis	29.21	20.51	5	6221	25	34950680
Renal failure	27.31	20.51	67	6159	130490	34820215
Gastric haemorrhage	22.76	20.51	17	6209	10244	34940461
Pancreatic carcinoma	22.59	20.51	16	6210	8885	34941820
Contusion	22.51	20.51	30	6196	36334	34914371
Spontaneous haemorrhage	22.00	20.51	6	6220	314	34950391
General physical health deterioration	21.87	20.51	61	6165	128208	34822497
Electrocardiogram T wave amplitude decreased	21.27	20.51	6	6220	356	34950349

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	601.76	17.43	279	9599	101315	79633195
Hyperglycaemia	283.75	17.43	149	9729	70186	79664324
Blood glucose increased	232.68	17.43	156	9722	114819	79619691
Diabetic ketoacidosis	208.46	17.43	96	9782	34026	79700484
Diabetes mellitus inadequate control	185.83	17.43	80	9798	24184	79710326
Wrong product administered	141.34	17.43	50	9828	8962	79725548
Acute kidney injury	117.31	17.43	221	9657	519183	79215327
Blood glucose abnormal	115.60	17.43	45	9833	10521	79723989
Glycosylated haemoglobin increased	107.68	17.43	51	9827	19209	79715301
Blood glucose fluctuation	100.71	17.43	36	9842	6646	79727864
Hypoglycaemic coma	84.60	17.43	29	9849	4731	79729779
Anti-insulin antibody positive	81.31	17.43	16	9862	280	79734230
Metabolic acidosis	65.61	17.43	65	9813	82464	79652046
Sopor	62.34	17.43	43	9835	32967	79701543
General physical health deterioration	60.47	17.43	116	9762	275122	79459388
Ketoacidosis	60.43	17.43	26	9852	7828	79726682
Blood glucose decreased	56.31	17.43	37	9841	26197	79708313
Intestinal haemorrhage	55.19	17.43	23	9855	6403	79728107
Hyperkalaemia	36.60	17.43	57	9821	114341	79620169
Lactic acidosis	36.02	17.43	44	9834	70315	79664195
Haematoma	34.06	17.43	37	9841	52158	79682352
Toxicity to various agents	33.34	17.43	6	9872	421534	79312976
Morganella infection	32.86	17.43	10	9868	1117	79733393
Hyperhidrosis	32.17	17.43	63	9815	151429	79583081
Diabetic bullosis	31.94	17.43	5	9873	20	79734490
Bronchial haemorrhage	31.30	17.43	10	9868	1310	79733200
Product quality issue	31.24	17.43	29	9849	33911	79700599
Dehydration	30.32	17.43	83	9795	248104	79486406
Anti-insulin antibody increased	29.87	17.43	6	9872	117	79734393
Product prescribing error	29.64	17.43	32	9846	44781	79689729
Anaemia	29.48	17.43	121	9757	444894	79289616
Waist circumference increased	28.88	17.43	10	9868	1679	79732831
Mucosal haemorrhage	28.23	17.43	11	9867	2575	79731935
Hyperinsulinaemic hypoglycaemia	28.08	17.43	6	9872	160	79734350
Pulmonary oedema	26.87	17.43	43	9835	88211	79646299
Pancreatic carcinoma	26.36	17.43	18	9860	13559	79720951
Renal failure	26.34	17.43	69	9809	200899	79533611
Loss of consciousness	25.51	17.43	61	9817	167882	79566628
Hypoglycaemic unconsciousness	24.15	17.43	8	9870	1175	79733335
Product administration error	23.30	17.43	24	9854	31822	79702688
Thyroid cyst	22.73	17.43	6	9872	401	79734109
Systemic infection	21.52	17.43	14	9864	9738	79724772
Hydrocholecystis	21.13	17.43	6	9872	527	79733983
Gastric haemorrhage	20.27	17.43	16	9862	15034	79719476
Liquid product physical issue	20.27	17.43	7	9871	1167	79733343
Urinary incontinence	19.99	17.43	25	9853	40884	79693626
Syncope	19.92	17.43	58	9820	179391	79555119
Hypoglycaemic encephalopathy	19.85	17.43	6	9872	655	79733855
Simple partial seizures	19.48	17.43	6	9872	698	79733812
Haemorrhagic erosive gastritis	19.19	17.43	6	9872	733	79733777
Electrocardiogram T wave amplitude decreased	19.10	17.43	6	9872	744	79733766
Abdominal discomfort	18.90	17.43	4	9874	250723	79483787
Diabetic retinal oedema	18.66	17.43	5	9873	354	79734156
Spontaneous haemorrhage	18.60	17.43	6	9872	811	79733699
Hypoglycaemic seizure	18.55	17.43	6	9872	818	79733692
Diabetic foot	18.42	17.43	9	9869	3623	79730887
Inflammatory marker increased	17.97	17.43	13	9865	10727	79723783
Monoclonal gammopathy	17.95	17.43	6	9872	906	79733604
Daydreaming	17.82	17.43	6	9872	927	79733583

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
DB00030	DRUGBANK_ID
253182	RXNORM
18596	MMSL
4885	MMSL
4886	MMSL
53478	MMSL
d00262	MMSL
d04369	MMSL
d05278	MMSL
000869	NDDF
000870	NDDF
006518	NDDF
010953	NDDF
126210001	SNOMEDCT_US
411530000	SNOMEDCT_US
411532008	SNOMEDCT_US
417423002	SNOMEDCT_US
420609005	SNOMEDCT_US
96367001	SNOMEDCT_US
C0795635	UMLSCUI
5186	INN_ID
118984375	PUBCHEM_CID

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	33 sections
Apidra	HUMAN PRESCRIPTION DRUG LABEL	1	0088-2500	INJECTION, SOLUTION	100 [iU]	SUBCUTANEOUS	BLA	33 sections
Apidra SoloStar	HUMAN PRESCRIPTION DRUG LABEL	1	0088-2502	INJECTION, SOLUTION	100 [iU]	SUBCUTANEOUS	BLA	33 sections
Apidra SoloStar	HUMAN PRESCRIPTION DRUG LABEL	1	0088-2502	INJECTION, SOLUTION	100 [iU]	SUBCUTANEOUS	BLA	33 sections