From Diabetes in Pets
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Glulisine)
Insulin hexamers (as produced by the body or injected) must break down into dimers and monomers to be absorbed
[1].
is a brand name for insulin
glulisine, a fast-acting human
analog[2] manufactured by
Aventis. It is a
soluble insulin and can be used
intravenously for diabetic emergencies such as
DKA. Apidra has been found to be equipotent (equally potent) to
R/
neutral R-DNA/GE/GM insulin when administered intravenously.
Given subcutaneously in normal injection form, Apidra has a more rapid onset and shorter duration than R human insulin[3].
[edit] Technical details
The alterations to the human insulin molecule that produces insulin Glulisine are all to the B insulin chain; position B-#3, which is normally amino acid asparagine is replaced with lysine and the lysine amino acid which is normally found at position B-#29 is replaced by glutamic acid[4]. Making substitutions at these positions on the B insulin chain, inhibits hexamer formation[5].
Since insulin in hexamer form must break down into dimers and monomers to become active, inhibiting the molecule's natural tendency to form hexamers by self-association, means better, faster absorption, more rapid onset, peak and shorter duration. Apidra[6] may be diluted for all uses except in insulin pumps. It may be mixed in the same syringe with NPH/isophane insulin only.
http://products.sanofi-aventis.us/apidra/images/apidra_chem.gif
Alterations to human insulin producing insulin glulisine (Apidra).
There is no clinical data regarding same syringe mixing of Apidra and any other insulin preparations in humans, but testing conducted in dogs indicates a slower onset when mixed with NPH/isophane insulin. Used on its own, Apidra displayed an earlier onset with them[7]. Antibody formation in the dog was noted.
Dr. Nelson of University of California-Davis said in his lecture at the Ohio State Endocrinology Symposium in 2006 that if the short-acting analog insulins have any role in feline and canine diabetes, it is not yet determined[8].
[edit] Insulin amino acid sequences
| Amino Acid Sequence of Insulin Preparations[9]
|
| Amino Acid Substitutions
|
|
|
A-Chain Position
|
B-Chain Position
|
Source
Species
| A-8
| A-10
| A-21
| B-28
| B-29
| B-30
| B-31
B-32
|
| Beef
| Ala
| Val
| Asn
| Pro
| Lys
| Ala
| N/A
|
| Pork
| Thr
| Ilc
| Asn
| Pro
| Lys
| Ala
| N/A
|
| Human
| Thr
| Ilc
| Asn
| Pro
| Lys
| Thr
| N/A
|
| Aspart
| Thr
| Ilc
| Asn
| Aspartic Acid
| Lys
| Thr
| N/A
|
| Lispro
| Thr
| Ilc
| Asn
| Lys
| Pro
| Thr
| N/A
|
| Glulisine
| Thr
| Ilc
| Asn
| Pro
| Glu
| Thr
| N/A
|
| Lantus (glargine)
| Thr
| Ilc
| Gly
| Pro
| Lys
| Thr
| Arg
|
| Levemir(detemir)
| Thr
| Ilc
| Asn
| Pro
| Lys
| N/A
| Myristic Acid
|
|
Ala=Alanine Val=Valine Asn=Asparagine Pro-Proline Lys=Lysine Thr=Threonine Ilc=Isoleucine Glu-Glutamine Gly=Glycine
|
[edit] Insulin pharmacokinetics
|
<center>Pharmacokinetics of Insulin Preparations[10]
|
|
Insulin Preparations
|
Onset (hr)
|
Peak (hr)
|
Duration (hr)
|
|
Lispro
|
0.25 to 0.5
|
0.5 to 1.5
|
2 to 5
|
|
Aspart
|
0.17 to 0.33
|
1 to 3
|
3 to 5
|
|
50/50
|
0.5 to 1
|
2 to 12
|
24
|
These are human activity profiles.
[edit] References
- ↑ Insulin Dependent Diabetes-Dr. Ragnar Hanas-1999 (Page 5)
- ↑ Apidra-Insulin Glulisine Remedyfind.com
- ↑ Rxlist.com-Patient Information-Apidra
- ↑ Prescribing Information-Sanofi-Aventis--Apidra
- ↑ EMEA Scientific Discussion-Insulin Glulisine-Apidra-Page 1
- ↑ Aventis: Apidra Information
- ↑ EMEA Scientific Discussion--Apidra-Insulin Glulisine-Pages 9-12
- ↑ Selecting an Insulin for Treating Diabetes Mellitus in Dogs & Cats-Page 39
- ↑ Pharmacy Times-Guide to Insulin Preparations
- ↑ Pharmacy Times-Guide to Insulin Preparations
- ↑ Endotext.com-Insulin Pharmacology
- ↑ Endotext.com-Insulin Pharmacology
- ↑ NetDoctor-UK Hypurin Protamine Zinc
