Insulin aspart
Encyclopedia
A fast acting insulin analog
(marketed by Novo Nordisk
as "NovoLog/NovoRapid") is a man-made form of human insulin. A single amino acid
has been slightly changed in its molecular structure. This change helps the fast-acting insulin analog absorb quickly into the bloodstream. As a result, it starts working in minutes, which allows you to take insulin and eat right away. Fast-acting insulin analogs are considered to act similar to the way insulin is released in people without diabetes mellitus
.
Novolog allows for a flexible dosing schedule, which allows the patient to adjust their insulin according to any changes in their eating habits.
It was created through recombinant DNA
technology so that the amino acid, B28, which is normally proline
, is substituted with an aspartic acid
residue. This analogue has increased charge repulsion, which prevents the formation of hexamers, to create a faster acting insulin. The sequence was inserted into the yeast
genome, and the yeast expressed the insulin analogue, which was then harvested from a bioreactor
.
According to JDRF, insulin aspart was approved for marketing in the United States by the Food and Drug Administration
in June 2000.
The pH
of insulin aspart is 7.2-7.6.
Novolog (vial) should be stored in the refrigerator between 2°C and 8°C (36°F and 46°F), until it is first used. Novolog should never be used if it has been frozen. NovoLog® FlexPen®, vials and cartridges that are being used can be kept at room temperature—below 30°C (86°F)—for up to 28 days. Novolog should not be stored in areas of extreme moisture or where there may be extreme temperatures, like a freezer or car.
and Flexpen, Novopen delivery devices for subcutaneous injection
. Additionally, it can be used with an injection port
such as the I-port.
Novolog® is used for the treatment of patients with diabetes mellitus to control hyperglycemia. Novolog® has a more rapid onset, and a shorter duration of activity than normal human insulin. Therefore, Novolog® given by injection should normally be used in a regimen with long-acting or intermediate insulin. Novolog® can also be used with external insulin pumps. The insulin should be changed in the reservoir of the insulin pump at least every 6 days, and the infusion sets should be changed at least every 3 days. The following insulin pumps have been used in Novolog® clinical or in vitro studies conducted by Novo Nordisk: Medtronic Paradigm® 512 and 712, Minimed 508, Disetronic® D-TRON® and H-TRON®.
The components of NovoLog Mix 70/30 are as follows:
The pH is 7.2-7.44.
NovoLog Mix is marketed to be used with the Novo Nordisk FlexPen. The onset of action is less than 30 minutes, the peak action is reached in 1–4 hours, and the duration is less than 24 hours.
NovoLog® is available in different forms. There are 10-mL vials, 3-mL PenFill® cartridges, and 3mL NovoLog® FlexPens®. The NovoLog® FlexPen® is a way to take NovoLog® via a prefilled, disposable insulin pen delivery system. The NovoLog® FlexPen® can be used for up to 28 days without being refrigerated once it has been used. The large, clear dosing window allows for accurate dose setting and adjustment. NovoLog® is also supplied in 3-mL PenFill® cartridges and can be used in the NovoPen® 3 insulin delivery system.
. The most common side effect is hypoglycemia. Long-term use of insulin, including Novolog®, can cause lipodystrophy
at the site of repeated injections or infusion. To reduce the risk of lipodystrophy, rotate the injection sites within the same region. Weight gain can also occur with the use of Novolog® and it has been attributed to anabolic effects of insulin and a decrease in glucosuria. Use of Novolog® has also been associated with sodium retention and edema
.
Insulin analog
An insulin analog is an altered form of insulin, different from any occurring in nature, but still available to the human body for performing the same action as human insulin in terms of glycemic control...
(marketed by Novo Nordisk
Novo Nordisk
Novo Nordisk manufactures and markets pharmaceutical products and services. Created in 1989 through a merger of two Danish companies dating back to the 1920s, it has become one of the world's leading companies in diabetes care, where Novo Nordisk pursues research into pulmonary delivery systems;...
as "NovoLog/NovoRapid") is a man-made form of human insulin. A single amino acid
Amino acid
Amino acids are molecules containing an amine group, a carboxylic acid group and a side-chain that varies between different amino acids. The key elements of an amino acid are carbon, hydrogen, oxygen, and nitrogen...
has been slightly changed in its molecular structure. This change helps the fast-acting insulin analog absorb quickly into the bloodstream. As a result, it starts working in minutes, which allows you to take insulin and eat right away. Fast-acting insulin analogs are considered to act similar to the way insulin is released in people without diabetes mellitus
Diabetes mellitus
Diabetes mellitus, often simply referred to as diabetes, is a group of metabolic diseases in which a person has high blood sugar, either because the body does not produce enough insulin, or because cells do not respond to the insulin that is produced...
.
Novolog allows for a flexible dosing schedule, which allows the patient to adjust their insulin according to any changes in their eating habits.
It was created through recombinant DNA
Recombinant DNA
Recombinant DNA molecules are DNA sequences that result from the use of laboratory methods to bring together genetic material from multiple sources, creating sequences that would not otherwise be found in biological organisms...
technology so that the amino acid, B28, which is normally proline
Proline
Proline is an α-amino acid, one of the twenty DNA-encoded amino acids. Its codons are CCU, CCC, CCA, and CCG. It is not an essential amino acid, which means that the human body can synthesize it. It is unique among the 20 protein-forming amino acids in that the α-amino group is secondary...
, is substituted with an aspartic acid
Aspartic acid
Aspartic acid is an α-amino acid with the chemical formula HOOCCHCH2COOH. The carboxylate anion, salt, or ester of aspartic acid is known as aspartate. The L-isomer of aspartate is one of the 20 proteinogenic amino acids, i.e., the building blocks of proteins...
residue. This analogue has increased charge repulsion, which prevents the formation of hexamers, to create a faster acting insulin. The sequence was inserted into the yeast
Yeast
Yeasts are eukaryotic micro-organisms classified in the kingdom Fungi, with 1,500 species currently described estimated to be only 1% of all fungal species. Most reproduce asexually by mitosis, and many do so by an asymmetric division process called budding...
genome, and the yeast expressed the insulin analogue, which was then harvested from a bioreactor
Bioreactor
A bioreactor may refer to any manufactured or engineered device or system that supports a biologically active environment. In one case, a bioreactor is a vessel in which a chemical process is carried out which involves organisms or biochemically active substances derived from such organisms. This...
.
According to JDRF, insulin aspart was approved for marketing in the United States by the Food and Drug Administration
Food and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...
in June 2000.
Chemical properties
The components of insulin aspart are as follows:- Metal ion – zincZincZinc , or spelter , is a metallic chemical element; it has the symbol Zn and atomic number 30. It is the first element in group 12 of the periodic table. Zinc is, in some respects, chemically similar to magnesium, because its ion is of similar size and its only common oxidation state is +2...
(19.6 ug/mL) - Buffer – disodium hydrogen phosphate dihydrate (1.25 mg/mL)
- Preservative – m-cresol (1.72 mg/mL) and phenolPhenolPhenol, also known as carbolic acid, phenic acid, is an organic compound with the chemical formula C6H5OH. It is a white crystalline solid. The molecule consists of a phenyl , bonded to a hydroxyl group. It is produced on a large scale as a precursor to many materials and useful compounds...
(1.50 mg/mL) - Isotonicity agent – glycerin (16 mg/mL) and sodium chlorideSodium chlorideSodium chloride, also known as salt, common salt, table salt or halite, is an inorganic compound with the formula NaCl. Sodium chloride is the salt most responsible for the salinity of the ocean and of the extracellular fluid of many multicellular organisms...
(0.58 mg/mL).
The pH
PH
In chemistry, pH is a measure of the acidity or basicity of an aqueous solution. Pure water is said to be neutral, with a pH close to 7.0 at . Solutions with a pH less than 7 are said to be acidic and solutions with a pH greater than 7 are basic or alkaline...
of insulin aspart is 7.2-7.6.
Action time
The onset of action is approximately 15 minutes, the peak action is reached in 45–90 minutes, and the duration is 3–5 hours. However, as with all insulin, these numbers are based on averages, and vary between individuals due to blood flow, injection site, temperature and exercise.Temperature
It has been debated whether or not insulin aspart (or NovoLog/NovoRapid) should be refrigerated. Recent studies have shown that there is no difference, however insulin should not be stored in intense heat for a long period of time. This causes the hormone to reach a pre- boiling state, and separate. This can change the potency of the insulin, and it would no longer be as effective.Novolog (vial) should be stored in the refrigerator between 2°C and 8°C (36°F and 46°F), until it is first used. Novolog should never be used if it has been frozen. NovoLog® FlexPen®, vials and cartridges that are being used can be kept at room temperature—below 30°C (86°F)—for up to 28 days. Novolog should not be stored in areas of extreme moisture or where there may be extreme temperatures, like a freezer or car.
Usage
Insulin aspart can be used in CSII pumpsInsulin pump
The insulin pump is a medical device used for the administration of insulin in the treatment of diabetes mellitus, also known as continuous subcutaneous insulin infusion therapy.The device includes:...
and Flexpen, Novopen delivery devices for subcutaneous injection
Subcutaneous injection
A subcutaneous injection is administered as a bolus into the subcutis, the layer of skin directly below the dermis and epidermis, collectively referred to as the...
. Additionally, it can be used with an injection port
Injection port
An injection port is a medical device used for the administration of insulin or other physician approved medicine into the subcutaneous tissue...
such as the I-port.
Novolog® is used for the treatment of patients with diabetes mellitus to control hyperglycemia. Novolog® has a more rapid onset, and a shorter duration of activity than normal human insulin. Therefore, Novolog® given by injection should normally be used in a regimen with long-acting or intermediate insulin. Novolog® can also be used with external insulin pumps. The insulin should be changed in the reservoir of the insulin pump at least every 6 days, and the infusion sets should be changed at least every 3 days. The following insulin pumps have been used in Novolog® clinical or in vitro studies conducted by Novo Nordisk: Medtronic Paradigm® 512 and 712, Minimed 508, Disetronic® D-TRON® and H-TRON®.
Variations on Insulin Aspart
NovoLog Mix 70/30 is a product marketed by Novo Nordisk which contains 30% insulin aspart and 70% insulin aspart protamine. The insulin aspart protamine portion is a crystalline form of insulin aspart, which delays the action of the insulin, giving it a prolonged absorption profile after injection. The combination of the fast-acting form and the long-acting form allows the patient to receive fewer injections over the course of the day.The components of NovoLog Mix 70/30 are as follows:
- Metal ion – zinc (19.6 ug/mL)
- Buffer – dibasic sodium phosphate (1.25 mg/mL)
- Preservative – m-cresol (1.72 mg/mL) and phenol (1.50 mg/mL)
- Isotonicity agent – sodium chloride (0.58 mg/mL) and mannitol (36.4 mg/mL)
- Modifying protein – protamine (0.33 mg/mL)
The pH is 7.2-7.44.
NovoLog Mix is marketed to be used with the Novo Nordisk FlexPen. The onset of action is less than 30 minutes, the peak action is reached in 1–4 hours, and the duration is less than 24 hours.
NovoLog® is available in different forms. There are 10-mL vials, 3-mL PenFill® cartridges, and 3mL NovoLog® FlexPens®. The NovoLog® FlexPen® is a way to take NovoLog® via a prefilled, disposable insulin pen delivery system. The NovoLog® FlexPen® can be used for up to 28 days without being refrigerated once it has been used. The large, clear dosing window allows for accurate dose setting and adjustment. NovoLog® is also supplied in 3-mL PenFill® cartridges and can be used in the NovoPen® 3 insulin delivery system.
Side effects
The safety of Novolog in patients with diabetes has been evaluated in several clinical studies. Novolog was compared with regular human insulin, and there was no difference in the frequency of adverse effects between the two treatments. The side effects that are commonly associated with insulin therapy include: allergic reactions, injection site irritation, rashes, and hypoglycemiaHypoglycemia
Hypoglycemia or hypoglycæmia is the medical term for a state produced by a lower than normal level of blood glucose. The term literally means "under-sweet blood"...
. The most common side effect is hypoglycemia. Long-term use of insulin, including Novolog®, can cause lipodystrophy
Lipodystrophy
Lipodystrophy is a medical condition characterized by abnormal or degenerative conditions of the body's adipose tissue. A more specific term, lipoatrophy is used when describing the loss of fat from one area...
at the site of repeated injections or infusion. To reduce the risk of lipodystrophy, rotate the injection sites within the same region. Weight gain can also occur with the use of Novolog® and it has been attributed to anabolic effects of insulin and a decrease in glucosuria. Use of Novolog® has also been associated with sodium retention and edema
Edema
Edema or oedema ; both words from the Greek , oídēma "swelling"), formerly known as dropsy or hydropsy, is an abnormal accumulation of fluid beneath the skin or in one or more cavities of the body that produces swelling...
.