From Wikipedia, the free encyclopedia
Rapid-acting insulin analogue
Insulin glulisine
is a rapid-acting
modified
form of
medical insulin
that 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
.
[4]
It was developed by
Sanofi-Aventis
and approved for marketing by the
FDA
[5]
and the
EMA
[6]
in 2004; it is sold under the trade name
Apidra
.
[7]
When injected subcutaneously, it appears in the blood earlier than regular human insulin (RHI).
[8]
When used as a meal time insulin, the dose is to be administered within 15 minutes before or 20 minutes after starting a meal.
[9]
Intravenous injections may also be used for extreme hyperglycemia, but must be performed under the supervision of a medical professional.
[2]
The most common side effects include hypoglycaemia (low blood glucose levels).
[3]
Medical uses
[
edit
]
Insulin glulisine is
indicated
for the treatment of diabetes mellitus.
[3]
[2]
Mechanism behind the rapid bioavailability
[
edit
]
The monomer-monomer interactions are weaker in insulin glulisin compared to unmodified human insulin, and therefore, it does not as readily form dimers and
hexamers
, which are dominant in unmodified insulin. Due to their large size, insulin hexamers need to break up into dimers or monomers before they are able to enter the blood and become biologically active.
Specifically, the B3 mutation causes electrostatic repulsion in the hexamer to arginine-22 in the B chain of other insulin molecules in the same hexamer, while the B29 mutation causes fewer
hydrogen bonds
to stabilize the dimer. Furthermore, the
isoelectric point
of insulin glulisine insulin, which is shifted from 5.5 (of unmodified human insulin) to 5.1, increases the solubility at physiological pH levels.
[10]
References
[
edit
]
- ^
a
b
"Insulin glulisine Use During Pregnancy"
.
Drugs.com
. 6 April 2020
. Retrieved
21 September
2020
.
- ^
a
b
c
"Apidra- insulin glulisine injection, solution Apidra SoloStar- insulin glulisine injection, solution"
.
DailyMed
. 6 December 2019
. Retrieved
21 September
2020
.
- ^
a
b
c
"Apidra EPAR"
.
European Medicines Agency
(EMA)
. Retrieved
7 October
2020
.
- ^
"Apidra (insulin glulisine) injection, solution"
.
DailyMed
.
- ^
"Apidra FDA Approval History"
.
Drugs.com
. Retrieved
25 August
2022
.
- ^
"Apidra"
.
ema.europa.eu
. Retrieved
3 December
2023
.
- ^
Jasek W, ed. (2007).
Austria-Codex
(in German) (2007/2008 ed.). Vienna: Osterreichischer Apothekerverlag.
ISBN
978-3-85200-181-4
.
- ^
Garnock-Jones KP, Plosker GL (May 2009). "Insulin glulisine: a review of its use in the management of diabetes mellitus".
Drugs
.
69
(8): 1035?57.
doi
:
10.2165/00003495-200969080-00006
.
PMID
19496630
.
S2CID
41839395
.
- ^
"Insulin Glulisine"
.
Drugs.com
.
- ^
Gillis RB, Solomon HV, Govada L, Oldham NJ, Dinu V, Jiwani SI, Gyasi-Antwi P, Coffey F, Meal A, Morgan PS, Harding SE, Helliwell JR, Chayen NE, Adams GG (January 2021).
"Analysis of Insulin Glulisine at the Molecular Level by X-Ray Crystallography and Biophysical Techniques"
.
Scientific Reports
.
11
: 1737.
doi
:
10.1038/s41598-021-81251-2
.
PMC
7814034
.
PMID
33462295
.
External links
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]
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fast-acting
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short-acting
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long-acting
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ultra-long-acting
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inhalable
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