NOVORAPID ® a drug based on insulin aspart.
THERAPEUTIC GROUP: Insulin aspart for injectable use - insulins and analogues
Indications NOVORAPID ® - Insulin aspart
NOVORAPID ® is a medicine used in the control of glucose metabolism in patients with diabetes mellitus.
Mechanism of action NOVORAPID ® - Insulin aspart
NOVORAPID ® is a hypoglycemic drug based on insulin aspart, so defined as it has an amino acid substitution (Proline with Aspartate) with respect to the normal sequence of this hormone.
This single amino acid variation significantly influences the pharmacokinetic properties of the hormone, which by reducing the normal tendency to form hexamers, is rapidly absorbed following subcutaneous administration, causing the onset of the hypoglycemic effect after about 10-20 minutes, the optimum between the first and third hours and a persistence of the effect for about 4 hours.
From the pharmacodynamic point of view, however, the mechanism of action remains unchanged, allowing insulin to interact with its specific receptor expressed by the cells of insulin sensitive tissues and increase the uptake and utilization of glucose, reducing blood concentrations.
The important anabolic effect of this hormone on the one hand (inducer of glycogen synthesis, protein synthesis and lipid synthesis) and the ability to act by inhibiting metabolic pathways useful for producing glucose, allows insulin to be the hypoglycemic hormone par excellence .
Studies carried out and clinical efficacy
1. ASPART INSULIN AND GESTATIONAL DIABETES
Womens Health (Lond Engl). 2008 Mar; 4: 119-24.
Insulin aspart in diabetic pregnancy: state of the art.
Mathiesen ER.
Important study showing how the treatment of gestational diabetes with insulin aspart can ensure good post-prandial glycemic control, reducing the frequency of hypoglycemic events and reducing the number of premature miscarriages.
2. INSULIN AND INSULIN ANALOGS
Diabetology. 2010 Aug; 53: 1743-53. Epub 2010 Apr 28.
Insulin analogues differently activate insulin receptor isoforms and post-receptor signaling.
Sciacca L, Cassarino MF, Genua M, Pandini G, Le Moli R, Squatrito S, Vigneri R.
It is known that insulin analogues differ from human insulin due to the different kinetics of action. This all-Italian study also demonstrates how these differences can also affect molecular dynamics with intracellular mechanisms activated in a different way depending on the type of insulin used. These studies could partly clarify some important variations on the different efficacy of insulin analogues.
3. ASPART INSULIN AND ANTI-INFLAMMATORY ACTION
Basic Clin Pharmacol Toxicol. 2011 Apr 23.
Effects of Mealtime Insulin Aspart and Bedtime NPH Insulin on Postprandial Inflammation and Endothelial Cell Function in Patients with Type 2 Diabetes.
Bladbjerg EM, Henriksen JE, Akram S, Gram J.
Although insulin aspart has a faster mode of action and guarantees a significant lowering of post-prandial glycaemia compared to regular insulin, the effects on the modulation of inflammatory markers and on the endothelial health of second type diabetic patients are almost identical.
Method of use and dosage
NOVORAPID ® 100 IU / ml insulin: 5 cartridges of 3 ml or pre-filled pen of 3 ml: the dosage of insulin aspart to be used in the treatment of diabetic pathology strictly depends on the physical condition of the patient and his clinical picture.
In general, the useful dosage should be included in the range from 0.5 - 1 IU / kg of body weight and the administration of NOVORAPID ® should be carried out immediately before a meal, given the particularly rapid action times.
It should be remembered that the dosage formulation and any other adjustments should be determined by your physician.
NOVORAPID ® warnings - Insulin aspart
To ensure good glycemic control, it is necessary for the diabetic patient to undergo periodic evaluation of serum glucose concentrations before and during the treatment period, and possibly to adapt the relative insulin therapy.
It is also necessary for the doctor to inform the patient of the correct method of preparation, administration and storage of the drug and of the potential risks, so as to be able to promptly recognize the signs of hypoglycemia and intervene before the hypoglycemic crisis occurs.
Insulin aspart, given its faster mode of action, may require more frequent administration than human soluble insulin.
Any dosage adjustments, changes in the drug used or discontinuation of therapy should be supervised by medical personnel.
In case of impaired renal function it may be necessary to reduce the dose of the drug used, unlike infections which may require an increase in the concentrations normally used.
The possible onset of hypoglycemia could reduce the patient's perceptive abilities, making the use of machinery and driving cars dangerous.
PREGNANCY AND BREASTFEEDING
Studies carried out on the use of insulin aspart in pregnant women have not reported any side effects on the fetus or the pregnant woman.
Consequently NOVORAPID ® could be effectively used in the treatment of gestational diabetes, by adjusting the dose used to the patient's physiopathological conditions and to the gestation period.
Interactions
Like classical insulin, insulin aspart is also capable of interacting with numerous active ingredients.
More precisely, the interaction with oral hypoglycemic agents, octreotide, anti-MAO, beta blocking agents, ACE inhibitors, salicylates, alcohol and anabolic steroids could enhance the hypoglycemic effects of the drug by reducing the need for insulin itself, while the simultaneous intake of oral contraceptives, thiazides, glucorticoids, thyroid hormones and sympathomimetics could reduce the therapeutic effect of NOVORAPID ®
Contraindications NOVORAPID ® - Insulin aspart
NOVORAPID ® contraindicated in case of hypoglycemia and hypersensitivity to human insulin or its excipients.
Undesirable Effects - Side Effects
NOVORAPID ® therapy could, like other hypoglycemic therapies, be associated with hypoglycemic conditions recognizable by classic signs such as cold sweat, skin pallor, nervousness, tremors, anxiety, tiredness, weakness, confusion, difficulty concentrating, headache, nausea , palpitations, visual disturbances and in the most serious cases loss of consciousness and death.
In addition, manifestations such as redness, itching and pain may occur at the injection site, while applying the injection to the same site for prolonged periods may be responsible for localized lipoatrophy.
Hypersensitivity reactions such as rash, dyspnoea and breathing difficulties, edema and sudden drop in blood pressure have been reported rarely.
Note
NOVORAPID ® sold only under medical prescription.
NOVORAPID ® falls within the doping class: Hormones and related substances (prohibited in and out of competition).
The information on NOVORAPID ® - Insulin aspart published on this page may be out of date or incomplete. For a correct use of this information, see the Disclaimer and useful information page.
