insulin aspart

インスリンアスパルト

WordNet

1. hormone secreted by the isles of Langerhans in the pancreas; regulates storage of glycogen in the liver and accelerates oxidation of sugar in cells

PrepTutorEJDIC

1. インシュリン(膵臓(すいぞう)ホルモンで糖尿病治療剤)

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/02/08 06:05:52」(JST)

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Insulin Aspart

Clinical data
AHFS/Drugs.com	monograph
MedlinePlus	a605013
Pregnancy category	US: C (Risk not ruled out)
Legal status	US: ℞-only
Routes of administration	Subcutaneous
Identifiers
CAS Number	116094-23-6 N
ATC code	A10AB05
PubChem	CID 16132418
DrugBank	DB01306 Y
ChemSpider	none
UNII	D933668QVX N
KEGG	D04475 Y
ChEMBL	CHEMBL1201496 N
Chemical data
Formula	C256H381N65O79S6
Molar mass	5825.8 g/mol
NY (what is this?)  (verify)

Insulin aspart is a fast-acting insulin analog marketed by Novo Nordisk as NovoLog/NovoRapid. It is a manufactured form of human insulin; where a single amino acid has been exchanged. This change helps the fast-acting insulin analog be absorbed quickly into the bloodstream. As a result, it starts working in minutes, which allows one to take insulin and eat right away. Fast-acting insulin analogs are considered to act similarly to the way insulin is released in people without diabetes mellitus.

Novolog allows for a flexible dosing schedule, which allows patients to adjust their insulin according to any changes in their eating habits.

The safety and efficacy of insulin aspart (NovoLog/NovoRapid) in real-life clinical practice was evaluated in the A1chieve study.

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 analog 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 analog, 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.

Chemical properties

The components of insulin aspart are as follows:

• Metal ion – zinc (19.6 μg/mL)
• Buffer – disodium hydrogen phosphate dihydrate (1.25 mg/mL)
• Preservatives – m-cresol (1.72 mg/mL) and phenol (1.50 mg/mL)
• Isotonicity agents – glycerin (16 mg/mL) and sodium chloride (0.58 mg/mL).

The pH 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 kept refrigerated at all times. The manufacturer claims it can last 28 days without refrigeration, as long as it is kept below 86 °F / 30 °C. Above these temperatures, the potency of the insulin quickly degrades, rendering it less effective.

Usage

Insulin aspart can be used in CSII pumps 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 in reservoirs of insulin pumps and infusion sets should be changed every 48 hours to avoid insulin degradation and loss of preservative. 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 μg/mL)
• Buffer – dibasic sodium phosphate (1.25 mg/mL)
• Preservatives – m-cresol (1.72 mg/mL) and phenol (1.50 mg/mL)
• Isotonicity agents – 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 3-mL 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.

Efficacy

There is a lack of compelling evidence to conclude superiority of insulin aspart over human insulin with regard to efficacy leading some to question the shifting of patients from human insulin to this modern insulin.

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 hypoglycemia. 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.

External links

• NovoLog Prescribing Information (PDF)
• A1chieve Resource Centre (supported by Novo Nordisk)

References

UpToDate Contents

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• 1. 2型糖尿病におけるインスリン療法 insulin therapy in type 2 diabetes mellitus
• 2. 糖尿病におけるインスリン療法の一般原則 general principles of insulin therapy in diabetes mellitus
• 3. 成人の1型糖尿病における血糖値マネージメント management of blood glucose in adults with type 1 diabetes mellitus
• 4. 糖尿病症例解説6：インスリン治療を施行中の64歳女性におけるコントロール不良の糖尿病 interactive diabetes case 6 uncontrolled diabetes in a 64 year old woman treated with insulin
• 5. Cases illustrating problems with insulin therapy for diabetes mellitus

English Journal

• Improved health status with insulin degludec compared with insulin glargine in people with Type 1 diabetes.

• Home PD, Meneghini L, Wendisch U, Ratner RE, Johansen T, Christensen TE, Jendle J, Roberts AP, Birkeland KI.SourceInstitute of Cellular Medicine-Diabetes, Newcastle University, Newcastle upon Tyne, UK Miller School of Medicine, University of Miami, Miami, FL, USA Gemeinschaftspraxis für Innere Medizin und Diabetologie, Hamburg, Germany MedStar Health Research Institute, Hyattsville, MD, USA Novo Nordisk A/S, Søborg, Denmark Endocrine and Diabetes Centre, Karlstad Hospital, Faculty of Health Sciences, Örebro University, Örebro, Sweden Endocrine and Metabolic Unit, Royal Adelaide Hospital, Adelaide, SA, Australia Faculty of Medicine, University of Oslo, Department of Endocrinology, Oslo University Hospital, Oslo, Norway.
• Diabetic medicine : a journal of the British Diabetic Association.Diabet Med.2011 Dec 12. doi: 10.1111/j.1464-5491.2011.03547.x. [Epub ahead of print]
• Aims:  The efficacy and safety of insulin degludec (degludec), a new-generation ultra-long-acting basal insulin, was compared with insulin glargine (glargine) in people with Type 1 diabetes mellitus in a 16-week, open-label, randomizsed trial. Health status, an important aspect of effective diab
• PMID 22150786

• Doping control analysis of selected peptide hormones using LC-MS(/MS).

• Thevis M, Thomas A, Schänzer W.SourceInstitute of Biochemistry-Center for Preventive Doping Research, German Sport University Cologne, Am Sportpark Müngersdorf 6, 50933 Cologne, Germany. m.thevis@biochem.dshs-koeln.de
• Forensic science international.Forensic Sci Int.2011 Dec 10;213(1-3):35-41. Epub 2011 Jul 12.
• With the constantly increasing sensitivity and robustness of liquid chromatography-mass spectrometry-based instruments combined with enhanced reproducibility as well as mass accuracy and resolution, LC-MS(/MS) has become an integral part of sports drug testing programs particularly concerning the de
• PMID 21752560

Japanese Journal

• Attainment of glycaemic goals by step-up therapy with biphasic insulin aspart-70/30 in Japanese type 2 diabetic patients

• HOSOI Yasuhiro,OHTANI Ken-Ichi,SHIMIZU Hiroyuki,KASHIMA Kouji,SATO Noriyuki,AKIYAMA Hitoshi,MORI Masatomo
• Endocrine journal 58(2), 131-135, 2011-02-01
• NAID 10029587731

• NICE Study

• 西村 治男
• 内分泌・糖尿病・代謝内科 30(6), 604-610, 2010-06
• NAID 40017666415

Related Links

• Insulin Aspart (rDNA Origin) Injection: MedlinePlus Drug ...

Insulin aspart must be injected shortly before or after a meal. If you remember your dose before or shortly after your meal, inject the missed dose right away. If some time has passed since your meal, follow the ...

• Insulin aspart medical facts from Drugs.com

Physician reviewed insulin aspart patient information - includes insulin aspart description, dosage and directions. ... Insulin aspart dosing information Usual Adult Dose for Diabetes Type 1: Individualize dose based on metabolic needs ...

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insulin aspart

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ノボラピッド

• 超速効型インスリンアナログ

超速効型インスリンと中間型インスリンの混合製剤

• ノボラピッド注

• 超速効型インスリン：100%

• ノボラピッド30ミックス注

• 溶解インスリンアスパルト　：　プロタミン結晶性インスリンアスパルト　＝　３　：　７

添付文書

• ノボラピッド注 フレックスペン／*ノボラピッド注 イノレット

http://www.info.pmda.go.jp/go/pack/2492415G1031_1_03/2492415G1031_1_03?view=body

• ノボラピッド30ミックス注　フレックスペン

http://www.info.pmda.go.jp/go/pack/2492415G2020_1_11/2492415G2020_1_11?view=body