NovoRapid
Active material: insulin aspart
When ATH: A10AB05
CCF: An analogue of human insulin short acting
ICD-10 codes (testimony): E10, E11
When CSF: 15.01.01.01
Manufacturer: NOVO NORDISK A/S (Denmark)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
Solution for p / and / in the introduction clear, colorless.
| 1 ml | |
| insulin aspart | 100 U * |
Excipients: glycerol, phenol, cresol, zinc chloride, disodium phosphate dihydrate, sodium chloride, Sodium hydroxide, hydrochloric acid, water d / and.
* 1 ED matches 35 g anhydrous insulin aspart.
3 ml – pen with multidose dispenser (5) – packs cardboard.
Pharmacological action
Hypoglycemic agents, human insulin analog short-acting, produced by recombinant DNA biotechnology using the strain Saccharomyces cerevisiae, wherein the amino acid proline at position B28 is substituted with aspartic acid.
It interacts with a specific receptor cytoplasmic outer cell membrane to form insulin-receptor complex, stimulating intracellular processes, incl. Several key enzymes (geksokinaza, pyruvate, glikogensintetaza). The decrease in blood glucose due to an increase of intracellular transport, increasing assimilation tissue, stimulation of lipogenesis, glikogenogeneza, reducing the rate of hepatic glucose production.
Substitution of amino acid proline at position B28 with aspartic acid in the formulation NovoRapid® FlexPen® It reduces the tendency of the molecules to form hexamer, which is observed in conventional insulin solution. Therefore NovoRapid® FlexPen® much more quickly absorbed from the subcutaneous fat and begins to act more quickly, than soluble human insulin. NovoRapid® FlexPen® strongly reduces the blood glucose level in the first 4 h postprandial, than soluble human insulin.
The duration of drug action NovoRapid® FlexPen® after s / to the introduction of shorter, than soluble human insulin.
After p / to the introduction of effect of the drug begins within 10-20 minutes after administration. The maximum effect is observed after 1-3 hours after injection. The duration of action of the drug is 3-5 no.
In clinical studies in patients with diabetes mellitus type 1 It is shown to reduce the risk of nocturnal hypoglycemia when administered insulin aspart compared with soluble human insulin. The risk of daytime hypoglycaemia was not significantly increased.
Insulin aspart is equipotent to soluble human insulin on a molar basis of indicators.
In clinical studies involving Adult patients with diabetes mellitus type 1 shows, that the introduction of the drug NovoRapid® FlexPen® there is a lower postprandial blood glucose levels compared to soluble human insulin.
In applying the drug NovoRapid® FlexPen® in Children and Adolescents shows similar results prolonged glucose control compared to soluble human insulin. A clinical trial with soluble human insulin before a meal and insulin aspart postprandial, It was conducted in children aged from 2 to 6 years (26 patients); and pharmacokinetic / pharmacodynamic study with single dose administration was conducted in children 6-12 and teenagers 13-17 years. The pharmacodynamic profile of insulin aspart in children were similar to those in adults.
Clinical studies of comparative safety and efficacy of insulin aspart and human insulin in the treatment of pregnant women with diabetes mellitus type 1 (322 examined: 157 – received insulin aspart, 165 – received human insulin) did not reveal any adverse effects of insulin aspart on pregnancy or the health of the fetus / newborn. Additional clinical trials of women with gestational diabetes, treated with insulin aspart (14 patients) and human insulin (13 patients) indicate comparability security profiles along with significantly improved control of blood glucose after meals when treated with insulin aspart.
Pharmacokinetics
Absorption
After s / c insulin aspart Tmax in plasma on average 2 half, than after administration of soluble human insulin. Cmax in plasma is on average 492 ± 256 pmol / l and is achieved through the 40 min after the s / c administration at a dose 0.15 IU / kg of body weight in patients with diabetes mellitus type 1. Insulin concentrations returned to baseline after 4-6 hours after injection. The absorption rate is slightly lower in patients with diabetes mellitus type 2, that results in a lower Cmax (352± 240 pmol / l) and later Tmax (60 m). Interindividual variability in Tmax significantly lower when insulin aspart compared to soluble human insulin, whereas the said variation in the value of Cmax insulin aspart More.
Pharmacokinetics in special clinical situations
Pharmacokinetic studies have not been conducted in elderly patients and in patients with impaired renal or hepatic function.
In children 6-12 years and adolescents 13-17 years with diabetes mellitus type 1 absorption of insulin aspart is fast in both age groups, Tmax, similar to that of adults. However, there are differences in the magnitude of Cmax in two age groups, underscoring the importance of individual choice dosing regimen of the drug.
Testimony
- Diabetes.
Dosage regimen
NovoRapid® FlexPen® for p / and / in the introduction. NovoRapid® FlexPen® It has more rapid onset and shorter duration of action, than soluble human insulin. Due to the faster onset of action NovoRapid® FlexPen® should be administered, usually, immediately before meal (if necessary, can be administered shortly after a meal).
Dose determined by the physician based on the individual blood glucose. NovoRapid® FlexPen® It is generally used in combination with insulin preparations expectancy or long-acting, are administered at least 1 time / day.
Typically, the total daily insulin requirements ranging from 0.5-1 U / kg body weight. With the drug before a meal, insulin requirements may be provided by NovoRapid drug® FlexPen® on 50-70%, There remains a need for insulin provided acting insulin.
Temperature of insulin must correspond to room.
NovoRapid® FlexPen® injected s / c to the anterior abdominal wall, hips, shoulder or buttocks. Injection sites within the same part of the body need to be changed regularly.
As with any other insulin products the duration of action NovoRapid® FlexPen® dose dependent, insertion site, the intensity of the blood flow, temperature and level of physical activity.
P / to introduction into the anterior abdominal wall provides a more rapid absorption compared with administration to other locations. Nonetheless, faster onset of action compared to soluble human insulin is maintained regardless of the site of the injection site.
If necessary, NovoRapid® FlexPen® It may be introduced into / in, but only by skilled health personnel.
For / in the infusion systems are used with the drug NovoRapid® FlexPen® 100 U / ml with a concentration of 0.05 IU / ml to 1 IU / ml insulin aspart in 0.9% sodium chloride solution; 5% or 10% dextrose, contains 40 mmol / l potassium chloride, with the use of polypropylene bags for infusion. These solutions are stable at room temperature for 24 no. During infusion of insulin necessary to constantly monitor the blood glucose level.
NovoRapid® FlexPen® It can also be used for long p / insulin infusion (CSII) in insulin pumps, developed for infusion of insulin. CSII should be made in the abdominal wall. Infusion site should be changed periodically.
If you use an insulin infusion pump NovoRapid® FlexPen® should not be confused with other types of insulin.
Patients, using CSII, You must be fully trained to use the pump, suitable tank and a pump tubing. Infusion Set (and the catheter tube) should be changed in accordance with the user manual, attached to the infusion set.
Patients, poluchaющie NovoRapid® FlexPen® using CSII, You must be available in case of additional insulin infusion system failure.
NovoRapid® FlexPen® It is a pre-filled syringe with the dispenser knob. Pen FleksPen® designed for use with injection systems for insulin needles companies with short cap NovoFayn. Packing needles marked with the symbol “S”. Pen FleksPen® It provides an opportunity to introduce by 1 to 60 ED drug up 1 ED. You must follow the exact instructions manual on the use, supplied with the device.
Pen FleksPen® intended for personal use only and can not be refilled.
Side effect
Side effects, related to the effect on carbohydrate metabolism: gipoglikemiâ (desudation, pale skin, nervousness or tremor, anxiety, unusual tiredness or weakness, disorientation, impaired concentration, dizziness, pronounced hunger, temporary blurred vision, headache, nausea, tachycardia). Severe hypoglycemia may lead to unconsciousness and / or convulsions, temporary or permanent impairment of brain function and death.
Determining the frequency of side effects: sometimes (>1/1000, <1/100), rarely (>1/10 000, <1/1000); rarely ( <1/10 000), including individual cases.
Allergic reactions: sometimes – hives, skin rash; rarely – anaphylactic reactions. Generalized allergic reaction may include skin rash, itchy skin, increased sweating, disorders of the gastrointestinal tract, angioedema, difficulty breathing, taxikardiju, decrease in blood pressure.
Local reactions: Local allergic reaction (redness, puffiness, itching at the injection site), usually temporary and passing as further treatment; sometimes – lipodystrophy.
Other: at the beginning of therapy rarely – swelling, sometimes – violation of refraction. These side effects usually are temporary.
Adverse Reactions, observed in patients, poluchaющih NovoRapid® FlexPen®, are dose dependent and are mainly due to the pharmacological effect of insulin.
Contraindications
- Gipoglikemiâ;
- Hypersensitivity to insulin aspart, and other ingredients.
Do not use the drug NovoRapid® FlexPen® children under the age of 2 years, tk. clinical trials in this age group have not been conducted.
Pregnancy and lactation
NovoRapid® (insulin aspart) It can be administered during pregnancy. In two randomized, controlled clinical study (322+27 surveyed pregnant) It did not reveal any adverse effect of insulin aspart on pregnancy or the health of the fetus / newborn when compared to human insulin.
During a possible pregnancy and throughout its life it is necessary to control the level of glucose in the blood and maintain a careful monitoring of the patients with diabetes (type 1, type 2 or gestatsionnыy diabetes). The need for insulin, usually, decreases in I trimester, and gradually increased in the II and III trimester of pregnancy. Shortly after birth, insulin requirements quickly return to the level, that was before pregnancy.
During the period of lactation (breast-feeding) NovoRapid® FlexPen® It can be used without restrictions. Insulin nursing mother presents no risk to the baby. However, it may be necessary to correct dose.
Cautions
Lack of dose or discontinuation of treatment, particularly diabetes Type 1, may lead to hyperglycemia or diabetic ketoacidosis. Usually, hyperglycemia symptoms appear gradually, for several hours or days. Symptoms of hyperglycemia include nausea, vomiting, drowsiness, redness and dryness of the skin, dry mouth, an increase in urine output, thirst and loss of appetite, and the odor of acetone in exhaled air. Without proper treatment of hyperglycemia can lead to death. After compensation of carbohydrate metabolism, such as intensified insulin therapy, patients can change their typical symptoms of hypoglycemia-precursors, what patients should be informed.
In patients with diabetes mellitus with optimal metabolic control late complications of diabetes develop later and slowly progresses. In this connection, it is recommended to carry out actions, to optimize metabolic control, including monitoring of blood glucose levels.
The consequence of the pharmacodynamic characteristics of the short-acting insulin analogues is that, that the development of hypoglycemia when used starts earlier, than with soluble human insulin.
NovoRapid® FlexPen® It should be used in direct connection with a meal. Note speed of onset of effect of the drug in the treatment of patients, with concomitant diseases or taking drugs, slowing down the absorption of food. In the presence of comorbidities, especially infectious nature, insulin requirements, usually, increases. Violation of renal or hepatic function may lead to a decrease in insulin requirements.
When transferring a patient to other types of insulin-harbingers of early symptoms of hypoglycaemia may change or become less pronounced, compared with those using previous type of insulin.
Transfer the patient to a new type of insulin or insulin product of another manufacturer must be carried out under strict medical supervision. If you change the concentration, type, manufacturer and type (human insulin, Insulin of animal origin, human insulin analog) insulin and / or method of manufacture may require a change in dose. Patients, perehodящim treatment preparatom NovoRapid® FlexPen®, You may need to increase the frequency of injection or changing dose compared to the dose previously used insulin. If necessary, dose adjustment, it can be made already at the first administration of the preparation or during the first weeks or months of treatment.
Besides, change in dose may be necessary when changing the diet and increased physical activity. Physical exercise, performed immediately after a meal, may increase the risk of hypoglycemia. Skipping meals or unplanned exercise can lead to hypoglycaemia.
A significant improvement in the compensation of carbohydrate metabolism may lead to a state of acute painful neuropathy, which is generally reversible.
Long-term improved glycemic control decreases the risk of progression of diabetic retinopathy. However, intensification of insulin therapy with abrupt improvement in glycemic control may be associated with temporary worsening of diabetic retinopathy.
NovoRapid® FlexPen® It contains cresol, which in rare cases may cause allergic reactions.
Effects on ability to drive vehicles and management mechanisms
The patient's ability to concentrate and the reaction rate can be violated at the time of hypoglycemia and hyperglycemia, that may constitute a danger in situations, When these abilities are especially needed (eg, when driving or operating machines and mechanisms). Patients should be advised to take measures to prevent the development of hyperglycemia and hypoglycemia while driving and operating machinery. This is especially important for patients with absence or reduction in symptoms, precursors of developing hypoglycemia or frequent episodes of hypoglycemia sufferers. In these cases, you should consider the appropriateness of performing such work.
Overdose
Symptoms: gipoglikemiâ.
Treatment: mild hypoglycemia patient can correct yourself, taking into glucose, sugar or carbohydrate-rich foods (Patients should always carry sugar, confection, biscuits or sugary fruit juice). In severe cases,, loss of consciousness patient, I / O is introduced 40% Dextrose (Glucose); / m or s / c – glucagon (0.5-1 mg). After regaining consciousness of the patient is recommended to take food, rich in carbohydrates, to prevent recurrence of hypoglycemia.
Drug Interactions
Hypoglycemic effect of insulin increase the oral hypoglycemic drugs, MAO inhibitors, ACE inhibitors, carbonic anhydrase inhibitors, non-selective beta-blockers, bromocriptine, Octreotide, sulfonamides, anabolic steroid, tetracikliny, clofibrate, ketoconazole, meʙendazol, pyridoxine, theophylline, cyclophosphamide, fenfluramin, lithium preparations, preparations, containing ethanol.
Hypoglycemic effect of insulin impaired oral contraceptives, GCS, thyroid hormones, thiazide diuretics, Heparin, tricyclic antidepressants, sympathomimetic, danazol, klonidin, Calcium channel blockers, diazoksid, morphine, phenytoin, nicotine.
Under the influence of reserpine and possibly as a weakening of salicylates, and strengthening of the drug.
Pharmaceutical incompatibility
Drugs, containing thiol or sulfite, adding insulin cause its destruction.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored at 2 ° to 8 ° C (in a refrigerator), but not next to freezer compartment; Do not freeze. To protect from light store NovoRapid® FlexPen® with the protective cap. Shelf life – 30 Months.
After the first use of NovoRapid® FlexPen® should not be stored in the refrigerator. Store at temperatures above 30 ° C. 4 weeks from the beginning of Use.
