Diagnosis: Proven benefits of insulin Levemir®. Levemir - official* instructions for use Insulin Levemir short or extended
Insulin detemir
Composition and release form of the drug
Solution for subcutaneous administration transparent, colorless.
Excipients: glycerol - 16 mg, phenol - 1.8 mg, metacresol - 2.06 mg, zinc acetate - 65.4 mcg, sodium hydrogen phosphate dihydrate - 0.89 mg, - 1.17 mg, hydrochloric acid or sodium hydroxide - q.s., water d/i - up to 1 ml.
3 ml (300 units) - glass cartridges (1) - multi-dose disposable syringe pens for multiple injections (5) - cardboard packs.
* 1 unit contains 142 mcg of salt-free insulin detemir, which corresponds to 1 unit. human insulin (IU).
pharmachologic effect
Long-acting insulin, a soluble analogue of human insulin. Produced by recombinant DNA biotechnology using the Saccharomyces cerevisiae strain.
The prolonged effect is due to the pronounced self-association of insulin detemir molecules at the injection site and the binding of drug molecules to the side chain. Insulin detemir, compared to insulin isophane, reaches peripheral target tissues more slowly. These combined mechanisms of delayed distribution provide a more reproducible absorption and action profile of insulin detemir compared to insulin isophane.
Interacts with a specific receptor on the outer cytoplasmic membrane of cells and forms an insulin-receptor complex that stimulates intracellular processes, incl. synthesis of a number of key enzymes (hexokinase, pyruvate kinase, glycogen synthetase).
At doses of 0.2-0.4 U/kg 50%, the maximum effect occurs in the range from 3-4 hours to 14 hours after administration. The duration of action is up to 24 hours depending on the dose.
After subcutaneous administration, a pharmacodynamic response is observed, proportional to the administered dose (maximum effect, duration of action, overall effect).
The nocturnal glucose control profile is flatter and more even with insulin detemir compared with insulin isophane, which is reflected in a lower risk of developing nocturnal hypoglycemia.
Pharmacokinetics
Terminal T1/2 after subcutaneous injection is determined by the degree of absorption from the subcutaneous tissue and is 5-7 hours, depending on the dose.
Indications
Diabetes.
Contraindications
Increased individual sensitivity to insulin detemir.
Dosage
Inject s/c into the thigh, anterior abdominal wall or shoulder. It is necessary to change injection sites within the anatomical region to prevent the development of lipodystrophy. Insulin will act faster if it is injected into the anterior abdominal wall.
Administer 1 or 2 times a day based on the patient’s needs. For patients requiring twice daily dosing for optimal glycemic control, the evening dose may be administered either with the evening meal, at bedtime, or 12 hours after the morning dose.
In elderly patients, as well as with impaired liver and kidney function, blood glucose levels should be more carefully monitored and the insulin dose adjusted.
Dose adjustment may also be necessary if the patient increases physical activity, changes his usual diet, or has a concomitant illness.
When switching from intermediate-acting insulins and long-acting insulins to insulin detemir, adjustment of the dose and time of administration may be required. Careful monitoring of blood glucose levels is recommended during transfer and in the first weeks of treatment with insulin detemir. Adjustment of concomitant hypoglycemic therapy (dose and timing of administration of short-acting insulin preparations or dose of oral hypoglycemic drugs) may be required.
Side effects
Adverse reactions associated with the effect on carbohydrate metabolism: often - hypoglycemia, the symptoms of which usually develop suddenly and may include pale skin, cold sweat, increased fatigue, nervousness, tremors, anxiety, unusual fatigue or weakness, disorientation, difficulty concentrating, drowsiness, severe hunger, blurred vision , headache, nausea, palpitations. Severe hypoglycemia can lead to loss of consciousness and/or convulsions, temporary or irreversible impairment of brain function, and even death.
Adverse reactions at injection sites: often - local hypersensitivity reactions (redness, swelling and itching at the injection site), as a rule, are temporary, i.e. disappear with continued treatment; rarely - lipodystrophy (as a result of non-compliance with the rule of changing the injection site within the same area).
Allergic reactions: rarely - urticaria, skin rash, as well as generalized reactions - skin itching, increased sweating, gastrointestinal disorders, angioedema, difficulty breathing, tachycardia, decreased blood pressure.
From the side of the organ of vision: rarely - refractive error (usually temporary and observed at the beginning of insulin treatment), diabetic retinopathy (long-term improvement in glycemic control reduces the risk of progression of diabetic retinopathy; however, intensification of insulin therapy with a sharp improvement in the control of carbohydrate metabolism can lead to a temporary worsening of diabetic retinopathy).
From the nervous system: in some cases - peripheral neuropathy, which is usually reversible.
Others: rarely - swelling.
Drug interactions
The hypoglycemic effect of insulin is enhanced by oral hypoglycemic drugs, MAO inhibitors, ACE inhibitors, carbonic anhydrase inhibitors, non-selective, bromocriptine, sulfonamides, anabolic steroids, tetracyclines, clofibrate, ketoconazole, mebendazole, pyridoxine, theophylline, cyclophosphamide, fenfluramine, lithium preparations, drugs containing ethanol. The hypoglycemic effect of insulin is weakened by oral contraceptives, corticosteroids, thyroid hormones, thiazide diuretics, tricyclic antidepressants, sympathomimetics, danazol, clonidine, slow calcium channel blockers, diazoxide, morphine, phenytoin, nicotine.
Under the influence of reserpine and salicylates, it is possible to both weaken and enhance the effect of insulin detemir.
/lanreotide can either increase or decrease the body's need for insulin.
Beta blockers may mask symptoms of hypoglycemia and delay recovery from hypoglycemia.
Ethanol can enhance and prolong the hypoglycemic effect of insulin.
Pharmaceutical interactions
Some drugs, such as those containing thiol or sulfite, when added to insulin detemir, can cause the destruction of insulin detemir.
special instructions
It is believed that intensive therapy with insulin detemir does not lead to weight gain.
The lower risk of nocturnal hypoglycemia compared to other insulins allows for more intensive dose selection in order to achieve the target blood glucose level.
Insulin detemir provides better glycemic control (based on fasting glucose measurements) compared with isophane insulin. Insufficient dosage of the drug or discontinuation of treatment, especially in type 1 diabetes mellitus, can lead to the development of hyperglycemia or diabetic ketoacidosis. Typically, the first symptoms of hyperglycemia appear gradually, over several hours or days. These symptoms include thirst, frequent urination, nausea, vomiting, drowsiness, redness and dryness of the skin, dry mouth, loss of appetite, and the smell of acetone in the exhaled air. In type 1 diabetes without appropriate treatment, hyperglycemia leads to the development of diabetic ketoacidosis and can be fatal.
Hypoglycemia can occur if the insulin dose is too high in relation to insulin needs.
Skipping meals or unplanned intense physical activity can lead to hypoglycemia.
After compensation of carbohydrate metabolism, for example, with intensified insulin therapy, patients may experience changes in their typical symptoms that are precursors of hypoglycemia, of which patients should be informed. The usual warning symptoms may disappear with prolonged diabetes mellitus.
Concomitant diseases, especially infectious ones and those accompanied by fever, usually increase the body's need for insulin.
Transferring a patient to a new type or insulin preparation from another manufacturer should occur under strict medical supervision. If the concentration, manufacturer, type, type (animal, human, analogues of human insulin) and/or method of its production (genetically engineered or animal-derived insulin) change, dose adjustment may be required.
Insulin detemir should not be administered intravenously as this may lead to severe hypoglycemia.
Mixing insulin deremir with a rapid-acting insulin analogue, such as insulin aspart, results in an action profile with a reduced and delayed maximum effect compared to administering them separately.
Impact on the ability to drive vehicles and operate machinery
Patients' ability to concentrate and react quickly may be impaired during hypoglycemia and hyperglycemia, which can be dangerous in situations where these abilities are especially needed (for example, when driving a car or working with machinery). Patients should be advised to take measures to prevent the development of hypoglycemia and hyperglycemia when driving a car and working with machinery. This is especially important for patients with no or decreased severity of symptoms that are warning signs of developing hypoglycemia or who suffer from frequent episodes of hypoglycemia. In these cases, the feasibility of performing such work should be considered.
Pregnancy and lactation
Currently, there are no data on the clinical use of insulin detemir during pregnancy and lactation.
During the period of possible onset and throughout the entire period of pregnancy, it is necessary to carefully monitor the condition of patients with diabetes mellitus and monitor the level of glucose in the blood plasma. The need for insulin, as a rule, decreases in the first trimester and gradually increases in the second and third trimesters of pregnancy. Shortly after birth, insulin requirements quickly return to pre-pregnancy levels.
During breastfeeding, it may be necessary to adjust the dose of the drug and diet.
IN experimental studies In animals, no differences have been established between the embryotoxic and teratogenic effects of insulin detemir and human insulin.
In elderly patients, blood glucose levels should be monitored more carefully and insulin dosage adjustments should be made.
About Levemir Flexpen for diabetes
Today, specialists have developed a significant number of different types of insulin: starting with short-acting and ending, respectively, with long-acting ones. They all have their advantages, but you should remember that not every variety can be used for a specific type of diabetes. What can be said about insulin, which is known as Levemir Flexpen?
About the drug
So, this medication is a long-acting insulin. Its significant advantage over other varieties lies precisely in the fact that it is an analogue of human insulin used in. This, of course, should be considered a positive characteristic, due to the fact that many diabetics, when thinking about which insulin to choose, prefer to purchase human analogues.
This is explained by them:
- effective impact;
- ease of assimilation;
- quickly addictive and does not cause addiction.
Thus, Levemir Flexpen belongs to the group of long-acting insulins, which, in turn, are human analogues.
About the release form and composition
The presented insulin is produced as a special solution, which is used for penetration under the skin. It is colorless and transparent.
What is the composition and release form of Levemir Flexpen?
The main component in this case is a substance called “insulin detemir”. This is a very active substance, just one ml of which contains 100 units. In turn, only one unit of this indicator is 142 mcg of salt-free insulin detemir. This is in direct correspondence with one unit of human insulin (IU).
The excipients are the following components, namely glycerol, phenol, metacresol, zinc acetate, sodium chloride and much more. All this is direct evidence that Levemir Flexpen will be truly effective for any type of diabetes. Thus, its use is completely justified and desirable in any case. This is explained by the significant demand for the described component.
However, what are the rules and regulations for its storage? After all, they must be followed in order for insulin to be as effective as possible.
About storage conditions and periods
At the same time, despite the fact that it should be kept in the refrigerator, it is optimal to store it away from the freezer.
Thus, Levemir Flexpen should under no circumstances be frozen. Its permissible storage period is 30 months.
For additional protection from any light sources, the pen syringe must be stored with a special cap, which must always be worn.
After initial use, it should not be kept in the refrigerator. It is advisable to store the insulin pen used or used as a spare syringe with the provided insulin at a temperature of no more than 30 degrees for up to six weeks.
About using Levemir Flexpen
This insulin, of course, must be kept out of the reach of children of any age. This will be the key to the safety of their health, as well as the entire environment, for example, plants. If we talk about transportation, then it would be best to transport Levemir Flexpen in special boxes, which can be purchased at any pharmacy or, for example, in a specialized store.
About dosage and use
It must be remembered that the insulin presented and its dosage should be selected solely on an individual basis. Moreover, this should be done by a specialist, who is based on criteria such as:
- patient's age group;
- severity of the disease and burden with other ailments;
- use of any other medications;
- the needs of the diabetic himself.
All this is very much in the process of properly organizing the treatment course. If the drug Levemir Flexpen is used as part of a basal or bolus regimen, it is recommended to prescribe it either once or twice a day. In this case, they proceed exclusively from the needs of the patient.
Those diabetics who need to use the drug twice a day for rational control of glycemic levels may well take an evening dosage either during dinner or just before going to bed. Dosage adjustments may be necessary if the patient's physical activity level changes, his or her usual diet changes, or if there is any concomitant illness.
How to administer Levemir Flexpen?
This medicinal insulin can be used not only as monotherapy, but also in combination with so-called bolus insulin. In addition, it can be used in active combination with oral hypoglycemic agents, as well as as an additional measure to existing treatment with liraglutide.
It is very important to remember that Levemir Flexpen is used only for subcutaneous administration. It should not be injected into any fibers because this may cause severe hypoglycemia. It is also recommended, if possible, intramuscular administration of the drug. In addition, it is not designed to be used in special insulin pumps.
- into the thigh itself;
- anterior abdominal wall;
- in the shoulder area;
- deltoid or gluteal plane.
As with the use of other medications, in this case insulin, the duration of its effect is directly dependent on the dosage, area of application, degree of forced blood flow, temperature indicators and the ratio in terms of physical activity.
Therefore, Levemir Flexpen should only be used in accordance with strict guidelines. But what is its drug interaction with other medications?
About drug interactions
About interactions with other medications
The effect of hypoglycemic insulin is enhanced by oral medications, as well as specific MAO and ACE inhibitors. This is also affected by similar carbonic anhydrases and ketoconazole.
Certain medications, for example those that contain thiol or sulfite groups, when introduced into insulin, are quite capable of provoking destabilization of insulin detemir.
Also, Levemir Flexpen does not need to be added to infusion solutions. This can cause significant harm to the health of a diabetic, and also affect many functions of the body: gastrointestinal tract, brain, liver and much more. What can be said about the side effects that occur while taking the drug described?
About side effects
The side effects that are observed in those patients who use this insulin are considered to be mainly dosage dependent and due to the pharmacological effects of insulin. The most common side effect should be considered hypoglycemia, which occurs during the administration of too large a dosage of the drug. We are talking exclusively about a person’s need for the amount of insulin.
Local and allergic reactions to Levemir Flexpen are also possible, which manifest themselves in skin itching, rash, and a significant increase in sweat production. Dysfunctions of the organs of vision are also likely. We are talking about destabilization of refraction and the formation of retinopathy. And, if the first phenomenon is only temporary, then in the second case the diabetic may face a fairly long-term manifestation.
Are there any side effects?
There is also likely some deterioration that occurs on the part of the human nervous system. We are talking about peripheral neuropathy, which, however, is also exclusively reversible. Thus, taking into account all the information presented, we can confidently say that this long-term insulin should be taken:
- solely on medical advice;
- with strict adherence to dosage.
In this case, side effects will be minimized. Next, we should talk about contraindications that do not even allow the use of Levemir Flexpen.
About contraindications
A contraindication to the use of medicinal insulin should be considered an individual high degree of sensitivity to the main component - insulin detemir or all the others that are included in the list of components of the drug.
It is not advisable to use insulin when treating children under two years of age. This is explained by the fact that clinical studies have not been carried out in children under two years of age.
In case of pregnancy (at all stages), as well as during the lactation period, maximum caution must be observed.
If using Levemir Flexpen is still recommended, then this, of course, should be done, but in small dosages, using caution. This is explained by the fact that its use should not in any way affect all the functions of a pregnant and then lactating woman.
Thus, there are quite serious contraindications to the use of this drug that must be observed. This is what will help not only significantly alleviate a person’s health condition with diabetes, but also achieve significant and long-term results as a result of treatment. All this can be achieved only by using insulin and taking care of your own health.
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Comments:
The instructions for use describe the features of the drug Levemir in sufficient detail and contain information about possible side effects, permissible dosage and methods of administration. The drug is intended for the treatment of diabetes mellitus. Levemir is one of the few drugs that is prescribed to both adults and children over 6 years of age.
Features of the medicine
Levemir FlexPen - injection solution. The medicine is prescribed to patients with diabetes of any type. Levemir is a basal type insulin that has a prolonged action. Regular use of this medication in most cases does not lead to weight gain. The developed insulin analog significantly reduces the risk of developing hypoglycemia attacks at night.
The drug must be taken daily, at the same time. If the patient is about to go on a long trip, which involves a change in time zone, the patient must consult with the attending physician to calculate a new time for taking the medication.
If there is a need to stop taking Levemir, reducing the dose or abruptly stopping the drug is strictly prohibited, since in this case a severe hypoglycemic attack may develop, especially in type 1 diabetes.
Hypoglycemia occurs if insulin enters the blood in insufficient or excessive quantities. In the presence of kidney dysfunction, especially severe renal failure, liver dysfunction or endocrine system dysfunction, dosage adjustments and constant measurement of glucose in the body are required.
In what cases is a hypoglycemic drug prescribed?
Levemir FlexPen is prescribed for the treatment of all types of diabetes. The dosage is calculated depending on the characteristics of the patient’s body. The solution is administered once a day (in some cases, double administration is necessary) with constant monitoring of blood sugar concentration.
The injection is placed in the thigh, shoulder area or the anterior wall of the peritoneum. To prevent the occurrence of allergic reactions on the skin, the area of application of the product must be constantly alternated. Insulin acts most quickly when the drug is injected into the abdominal wall.
Constant monitoring of blood sugar during the administration of Levemir should be carried out by elderly patients in the presence of complications or unstable glucose levels; the dosage can be adjusted by a doctor.
If the patient plays sports or does not adhere to a special therapeutic diet, the dose should be calculated individually. With extreme caution, the drug should be administered to persons with kidney, liver, dysfunction of the heart muscle and circulatory system.
Excessive amounts of insulin often cause problems in the functioning of internal organs. The dosage for each patient should be different, since an incorrectly selected dose can cause complications. An attack of hypoglycemia (as a reaction to an overdose) can develop gradually. With a mild symptomatic overdose, the patient can stop it on his own; to do this, it is enough to eat foods enriched with carbohydrates or sugar. A patient with diabetes should always have various sweets, candies and cookies with them. Severe attacks of hypoglycemia require immediate hospitalization of the patient in a hospital. The attack is controlled by the administration of glucose.
Possible complications from taking the drug
If you take a large dose, or due to intolerance to certain components of the drug, Levemir Flexpen can cause the following side effects:
- metabolic disorder;
- dysfunction of the central nervous system;
- allergic skin reactions at the injection site;
- visual impairment.
Insulin has side effects in some patients who are dependent on regular administration of the drug. Hypoglycemia, as one of the manifestations of complications from taking the drug, is provoked by the administration of too large a dose of Levemir. Disorders of carbohydrate metabolism are expressed in cold sweat, pale skin, severe fatigue of the body, and tremors.
Often in patients, the use of Levemir leads to disruption of the nervous system, developing an anxious feeling, gagging, and increased heart rate. Frequent, severe headaches may occur, vision is impaired, and there is a constant feeling of hunger.
Severe attacks of hypoglycemia, which are often repeated when taking Levemir and are not stopped in time, can lead to irreversible consequences in the body, especially in the brain, which often causes death. Typically, severe hypoglycemia is associated with malnutrition.
Allergic skin reactions (itching, redness, hives) may occur at the injection site. Some patients may have problems with the respiratory system. Shortness of breath, decreased blood pressure, and rapid heartbeat may occur. In extremely rare cases, which amount to no more than 0.5%, the patient experiences soft tissue swelling.
Who is prohibited from taking the drug?
Before administering Levemir Penfill solution, the instructions for use must be carefully studied, since there are a number of contraindications for which the use of the medicine is strictly prohibited. Levemir should not be administered to children under 6 years of age, as clinical trials have not been conducted on patients in this age group.
It is strictly forbidden to use the medicine by persons who have individual allergic reactions to individual components of the drug. The effect of the drug on the body of a pregnant woman and the fetus has not been studied, so the use of Levemir is not recommended. In exceptional cases, the drug is prescribed to pregnant women: when the benefits of taking it outweigh the possible risk of complications. Pregnant women need to constantly monitor their blood sugar levels while taking Levemir and carefully follow the dosage prescribed by their doctor.
The use of the drug during lactation requires careful adherence to the dosage, which is prescribed individually by the attending physician. Patients with heart and kidney failure can take Levemir, carefully observing the dosage and constantly monitoring sugar levels.
Abruptly stopping medication is strictly prohibited. If it is necessary to change the drug, the insulin concentration should be gradually reduced.
Rules for administering Levemir
The box with the medicinal injection includes a special syringe that has a dispenser. Before administering the drug, you must take a disposable needle, remove it from the protective film and carefully insert it into the syringe.
Before injection, you need to remove the air from the syringe by pressing the plunger until a few drops of the substance emerge from the needle. After the injection, the needle must be disposed of. To disinfect, the syringe can be wiped with cotton wool soaked in medical alcohol.
Levemir should be stored at 2–8˚C. This temperature is maintained in the refrigerator, but not near the freezer. Shelf life - no more than 30 months. The medicine should be administered only intramuscularly; when administering the drug into a vein, a severe attack of hypoglycemia may develop.
Levemir can be used both as an independent medicine for the treatment of diabetes mellitus and in complex therapy. The greatest effectiveness of the product is achieved by a proper diet and avoidance of alcoholic beverages. Levemir can have a depressant effect on the central nervous system, so when using it you need to be especially careful when driving a car or working with complex machinery, as attention is dulled and the reaction slows down.
Certain types of adverse reactions
The use of Levemir for the treatment of diabetes rarely leads to adverse allergic reactions. As a rule, this is due to the use of a medication in complex treatment with other medications.
Generalized hypersensitivity to the administration of the drug may appear at the injection site (rash, itching, urticaria, slight swelling and hardening of the skin). Symptoms such as hypotension, tachycardia, difficulty breathing appear extremely rarely and are temporary, but they must be stopped immediately, as they pose a threat to human health and life.
Hypoglycemia occurs in most cases due to poor diet, consumption of alcoholic beverages, or incorrect dosage of medication. The attack is manifested by a sudden deterioration in the general condition, the patient becomes covered in sticky sweat, becomes too nervous, and has tremor of the limbs.
If the dosage of the drug is insufficient or the solution is frequently missed, the patient may develop hyperglycemia (dangerously high concentration of sugar in the blood). The symptomatic picture of hyperglycemia develops progressively. Signs of hyperglycemia: extreme thirst, increased urge to urinate, increased fatigue, drowsiness, decreased appetite.
With hyperglycemia, a person constantly smells acetone. In patients with type 1 diabetes mellitus, hyperglycemia can cause the development of ketoacidosis, and in some cases, cause death.
Levemir in complex therapy
Severe forms of diabetes mellitus require an integrated approach to treatment, necessitating the need to take multiple medications. The simultaneous use of Levemir and drugs of the beta-blocker group can lead to changes in the clinical picture, attacks of hypoglycemia and inhibit the recovery of the patient’s body after stopping a severe attack.
Most drugs weaken or significantly increase the effectiveness of insulin. The hypoglycemic effect may be reduced while taking hormonal contraceptives, antidepressants, and drugs that block calcium channels. The effect of the drug is enhanced by simultaneous use of tetracyclines, inhibitors and other drugs of the hypoglycemic group.
Levemir should not be taken with medications that contain sulfite and thiol groups, as they have a destructive effect on insulin. Levemir is not intended as an additive to infusion-type solutions. If necessary, take it with other drugs, the doctor adjusts the dosage of all drugs. This medicine is prescribed exclusively by a doctor, based on medical history, diagnostics, and individual characteristics of the patient.
Thank you for your feedback
Comments
Megan92 () 2 weeks ago
Has anyone managed to completely cure diabetes? They say it is impossible to completely cure...
Daria () 2 weeks ago
I also thought it was impossible, but after reading this article, I had long since forgotten about this “incurable” disease.
Megan92 () 13 days ago
Daria () 12 days ago
Megan92, that’s what I wrote in my first comment) I’ll duplicate it just in case - link to article.
Sonya 10 days ago
Isn't this a scam? Why do they sell on the Internet?
Yulek26 (Tver) 10 days ago
Sonya, what country do you live in? They sell it on the Internet because stores and pharmacies charge outrageous markups. In addition, payment is only after receipt, that is, they first looked, checked and only then paid. And now they sell everything on the Internet - from clothes to TVs and furniture.
Editor's response 10 days ago
Sonya, hello. This drug for the treatment of diabetes mellitus is indeed not sold through the pharmacy chain in order to avoid inflated prices. Currently you can only order from official website. Be healthy!
Increased glucose in diabetes mellitus is always a consequence of insulin deficiency. That is why for more than 10 years, modern classifications of the disease have not included the terms “insulin-dependent” and “non-insulin-dependent” diabetes mellitus. Despite the emergence of more and more new classes of drugs for the treatment of diabetes mellitus, insulin therapy continues to occupy its important place in the treatment of type 2 diabetes and still remains the basis for the treatment of type 1 diabetes.
BASAL INSULIN SECRETION
All “classical” approaches to insulin therapy are based on replacing the deficiency of basal secretion of this hormone with long-acting drugs and both to reduce glucose and to absorb carbohydrates eaten with food with faster-acting insulins.
The role of the basal section of insulin cannot be overestimated. It ensures optimal glycemic levels in the intervals between meals and during sleep. On average, insulin secretion at this time is approximately 1 unit per hour, and during prolonged fasting or physical exercise 0.5 units per hour. It accounts for approximately half of the body's need for insulin per day.
Basal insulin secretion is subject to daily fluctuations, the greatest need for insulin is observed in the early morning hours, the lowest in the afternoon and at the beginning of the night. In both type 1 and type 2 diabetes, long-acting insulin preparations are used to compensate for the effects of “basal” insulin secretion. Until the beginning of this decade, these were the so-called intermediate-acting insulins. The main representatives of this class were the so-called neutral protamine Hagedorn (NPH) insulins.
Protamine protein with alkaline properties was added to the insulin preparation, which slows down the resorption of insulin from subcutaneous tissue. When this protein was combined with insulin in isophane (equilibrium) concentrations, the duration of action of insulin extended to 14-16 hours. NPH insulins have gained enormous popularity among endocrinologists and patients with diabetes, as they make it possible to optimize disease therapy and improve glycemia at night and in the morning without additional injections every 3-4 hours.
However, NPH drugs had several problem areas:
- high biovariability, which prevented the rapid selection of an individual daily dose that replaces the “basal” secretion of insulin;
- uneven insulin activity during the period of action of the drug, which required additional meals at night and during the day;
- since the insulin preparation consisted of a complex of proteins, it was necessary to stir the drug correctly and evenly, which was often not done by patients and significantly increased the biovariability of insulin.
All these essential points made it possible to only relatively model the basal secretion of insulin in patients with diabetes. The requirement to optimize existing approaches to therapy remained on the agenda.
ANALOG BREAKTHROUGH
This became possible with the discovery of the structure of DNA and the introduction of recombinant technologies in 1977. Scientists now have the ability to determine individual amino acid sequences in proteins, modify them, and evaluate the biological effects of the resulting products.
A fundamentally new direction has emerged in pharmacology - the synthesis of new molecules with improved properties of previously studied substances and drugs. Thus, by the mid-90s of the last century, insulin analogues were included in the drug therapy of diabetes mellitus.
The emergence of insulin analogues has significantly improved the quality of life of patients with diabetes and reduced the main obstacles to insulin prescription, such as:
- in the “pre-analog” period of diabetes treatment, an increase in the dose of short-acting insulin shifted the peak activity of the drug and required correction of the insulin/carbohydrate proportion; when using fast-acting analogues, this proportion is more stable;
- absorption of short-acting insulin from the injection site lagged significantly behind that of fast-acting analogues, which required administering the drug 30-40 minutes before meals; the introduction of analogues made it possible to give an injection in 5-10 minutes;
- the high risk of hypoglycemia, especially at night, when taking NPH insulins was significantly reduced when prescribing “basal” analogues.
Thus, the advent of insulin analogs into clinical practice allowed doctors and patients to prescribe insulin therapy in a timely manner, correctly titrate drug doses, and have less fear of hypoglycemia and other adverse reactions. Among the insulins that came into the new millennium, insulin detemir (Levemir) occupies a special place.
WHAT LEVEMIR CAN DO
The genetically engineered insulin analogue Levemir® is the reference drug of a new direction - insulin analogues in the treatment of diabetes. This drug is slowly absorbed from the injection depot and has a long period of activity due to self-association in the subcutaneous fat depot and binding to human albumin. Circulating in the bloodstream, the drug periodically evenly dissociates with albumin and exerts its insulin-like effect.
At a dose of insulin Levemir® 0.4 U/kg body weight or more, a single administration of the drug per day is justified; the duration of action of the drug is 18-20 hours. If the daily dose should be higher, a two-fold administration regimen is recommended; The duration of action of the drug in this case covers 24 hours.
Insulin Levemir® has found wide use in the Russian Federation over the past 3 years. Among its advantages, it should be noted that there is a significantly greater intra-individual predictability of action in patients than that of “classical” NPH insulins. This is due to the following factors:
- dissolved state of detemir at all stages - from its dosage form to binding to the insulin receptor;
- buffering effect of binding to serum albumin.
These properties of the drug ultimately lead to better control of blood sugar levels compared to NPH insulin - when titrating the drug to achieve similar glycemic goals. During treatment with insulin Levemir®, with better or similar control of glucose reduction, fewer hypoglycemic conditions are observed (especially at night). Based on my own experience and the experience of my colleagues, I can say that treatment with insulin Levemir® is consistently accompanied in patients with diabetes types 1 and 2 by less dynamics of body weight gain (and in some studies even weight loss was obtained). And in obese patients, a decrease in body weight is observed.
In an 18-week study conducted at the ERC to study the effectiveness of insulin Levemir® in patients with type 1 diabetes in combination with insulin aspart (NovoRapid), a decrease in glycated hemoglobin was obtained twice as much as in the group of NPH insulin and genetically engineered human insulin. At the same time, the number of hypoglycemia was 21% less in the Levemir® insulin group. As in many similar studies abroad, no weight gain was noted in the first group.
In type 2 diabetes, Levemir® has also shown its high clinical effectiveness, opening up promising opportunities for patients to start and intensify insulin therapy. According to numerous studies, administration of insulin Levemir® once a day is optimal for most patients with type 2 diabetes.
Initial data were obtained that a single use of this drug for a year in patients who had not previously used insulin was as effective as the use of insulin glargine (Lantus).
At the same time, it was found that when using the drug Levemir® in type 2 diabetes, a less pronounced increase in body weight is observed. Moreover, achieving on average the same plasma glucose parameters, insulin therapy with Levemir® was marked by a lower frequency of hypoglycemia in patients compared to Lantus - 5.8 and 6.2, respectively.
Similar data were obtained in another large study - PREDICTIVE™ 303, involving more than 5 thousand patients. According to his data, in patients with type 2 diabetes who were switched from NPH-insulin or insulin glargine to Levemir®, a significant decrease in body weight was noted over 26 weeks (more than 0.6 kg in 3 months) against the background of improved glycemia and a decrease in frequency of hypoglycemic episodes.
Based on the data obtained, it should be recognized that:
- for most patients with type 2 diabetes, the use of Levemir® insulin once a day is optimal;
- on Levemir® insulin, the decrease in glycemia is not accompanied by an increase in body weight compared to NPH insulin or glargine;
- low risk of hypoglycemia episodes with Levemir® insulin compared with NPH insulin when glycemia is normalized in patients with type 2 diabetes.
IMPROVING QUALITY OF LIFE…
The doctor determines the dose of Levemir® insulin individually in each specific case. The drug should be administered 1 or 2 times a day, as mentioned above, based on the patient’s needs. Moreover, a clinical study of the drug made it possible to prescribe Levemir insulin not only in adults, but also in children, starting from the age of 6.
Those patients with diabetes who require twice-daily dosing for optimal blood glucose control may administer the evening dose either with the evening meal, at bedtime, or 12 hours after the morning dose.
Levemir® is injected subcutaneously into the thigh, anterior abdominal wall or shoulder. Patients should not forget to change injection sites within the anatomical area.
It is optimal to use a Levemir® Flexpen® pen pre-filled with insulin. The convenience and accuracy of these syringe pens ensures easy administration of the drug, helps prevent errors in insulin administration, generally guaranteeing better glycemic indicators in patients with diabetes.
1 ml of the drug contains 100 units of Levemir® insulin, the syringe pen is filled with 3 ml of the drug, the package contains 5 Flex-Pen devices. There is no doubt that the new technology for administering the drug - an individual, ready-to-use syringe pen Levemir® Flexpen® improves the quality of life of patients with diabetes while maintaining the biological effects inherent to the drug.
Extensive experience in using the drug Levemir® in the Russian Federation in recent years allows us to classify this drug as a standard for basal insulins, and the high safety of the drug in the absence of weight gain allows its wider use in complex groups of patients, in particular, in senile and elderly people.
Candidate of Medical Sciences, Associate Professor of the Department
endocrinology MMA
them. I. M. Sechenova Alexey Zilov
The original article can be found on the official website of the newspaper DiaNews
Treatment of diabetes mellitus is carried out in the form of replacement therapy. Since your own insulin cannot help the absorption of glucose from the blood, its artificial analogue is introduced. For type 1 diabetes, this is the only way to maintain the health of patients.
Currently, the indications for treatment with insulin drugs have expanded, since with their help it is possible to achieve a decrease in sugar levels in severe type 2 diabetes, with concomitant diseases, pregnancy and surgical interventions.
Insulin therapy should be similar to the natural production and release of insulin from the pancreas. For this purpose, not only short-acting insulins are used, but also medium-acting ones, as well as long-acting insulin.
Rules for insulin therapy
With normal insulin secretion, it is constantly present in the blood in the form of a basal (background) level. It is designed to reduce the effect of glucagon, which is also produced continuously by alpha cells. Background secretion is small - approximately 0.5 or 1 unit every hour.
Long-acting medications are used to ensure that such basal insulin levels are maintained in diabetic patients. These include insulin Levemir, Lantus, Protafan, Tresiba and others. Long-acting insulin is administered once or twice a day. When administered twice, the interval is 12 hours.
The dose of the drug is selected individually, since the need for insulin may be higher at night, then the evening dose is increased; if there is a need for a better reduction in the daytime, then the larger dose is transferred to the morning hours. The total dose of the administered drug depends on weight, diet, and physical activity.
In addition to background secretion, the production of insulin for food intake is reproduced. When blood glucose levels rise, active synthesis and secretion of insulin begins in order to absorb carbohydrates. Normally, 12 g of carbohydrates require 1-2 units of insulin.
Short-acting (Actrapid) and ultra-short-acting (Novorapid) drugs are used as a substitute for “food” insulin, which reduces hyperglycemia after meals. Such insulins are administered 3-4 times a day before each main meal.
Short-acting insulin requires a snack after 2 hours for the peak period of action. That is, with a 3-time administration, you need to have a snack 3 more times. Ultrashort preparations do not require such an intermediate meal. Their peak action allows the carbohydrates supplied with the main meal to be absorbed, after which their effect ceases.
The main insulin administration regimens include:
- Traditional - first the insulin dose is calculated, and then the food, carbohydrates in it, and physical activity are adjusted to it. The day is completely scheduled hour by hour. Nothing about it can be changed (amount of food, type of food, time of intake).
- Intensified - insulin adapts to the daily routine and gives freedom to schedule insulin administration and food intake.
With an intensive insulin therapy regimen, both background - long-acting insulin once or twice a day - and short (ultra-short) insulin before each meal are used.
Levemir FlexPen - properties and application features
Sugar level
Levemir FlexPen insulin (an analogue of human insulin) contains the active ingredient detemir. The drug was produced using genetic engineering, which makes it possible to prescribe it to patients with an allergy to insulin of animal origin.
1 ml of Levemir insulin contains 100 units, the solution is placed in a syringe pen that contains 3 ml, that is, 300 units. The package contains 5 plastic disposable pens. The price of Levemir FlekPen is slightly higher than for drugs produced in cartridges or vials.
Instructions for use of Levemir indicate that this insulin can be used by patients with type 1 and type 2 diabetes mellitus, and also that it is good for replacement therapy for diabetes in pregnant women.
Studies have been conducted on the effect of the drug on the degree of weight gain in patients. When administered once a day after 20 weeks, the weight of patients increased by 700 g, and the comparison group that received insulin isophane (Protafan, Insulim) the corresponding increase was 1600 g.
All insulins are divided into groups according to their duration of action:
- With an ultra-short hypoglycemic effect - onset of action in 10-15 minutes. Aspart, Lizpro, Khmumulin R.
- Short-acting - onset after 30 minutes, peak after 2 hours, total time - 4-6 hours. Aktrapid, Farmasulin N.
- Average duration of action - after 1.5 hours it begins to lower blood sugar, reaches a peak after 4-11 hours, the effect lasts from 12 to 18 hours. Insuman rapid, Protafan, Vozulim.
- Combined action - activity appears within 30 minutes, peak concentrations from 2 to 8 hours from the moment of administration, lasts 20 hours. Mixtard, Novomix, Farmasulin 30/70.
- Prolonged action begins after 4-6 hours, peak - 10-18 hours, total duration of action up to 24 hours. This group includes Levemir, Protamine.
- Ultra-long insulin works for 36-42 hours - Tresiba insulin.
Levemir is a long-acting insulin with a flat profile. The action profile of the drug is less variable compared to isophane insulin or glargine. The prolonged action of Levemir is due to the fact that its molecules form complexes at the injection site and also bind to albumin. Therefore, this insulin reaches target tissues more slowly.
Isophane insulin was chosen as an example for comparison, and it was proven that Levemir has a more uniform flow into the blood, which ensures consistency of action throughout the day. The mechanism of the lowering effect on glucose levels is associated with the formation of the insulin-receptor complex on the cell membrane.
Levemir has the following effect on metabolic processes:
- Accelerates the synthesis of enzymes inside the cell, including those for the formation of glycogen - glycogen synthetase.
- Activates the movement of glucose into the cell.
- Accelerates tissue absorption of glucose molecules from circulating blood.
- Stimulates the formation of fat and glycogen.
- Inhibits the synthesis of glucose in the liver.
Due to insufficient data on the safety of Levemir, it is not recommended for children under 2 years of age. When used in pregnant women, there were no negative effects on the course of pregnancy, the health of the newborn, or the appearance of malformations.
There is no data on the effect on infants during breastfeeding, but since it belongs to a group of proteins that are easily destroyed in the digestive tract and absorbed through the intestines, it can be assumed that it does not penetrate into breast milk.
How to use Levemir FlexPen?
The advantage of Levemir is that it does not have a pronounced peak of action. Therefore, when administered, there is no risk of excessively low blood sugar levels. It has been established that the risk of hypoglycemia during the day occurs less often by 70%, and night attacks by 47%. The studies were carried out on patients for 2 years.
Despite the fact that Levemir acts within 24 hours, it is recommended to administer it twice to lower and maintain stable blood sugar levels. If insulin is used in combination with short-acting insulins, it is administered in the morning and evening (or before bedtime) with a 12-hour interval.
For the treatment of type 2 diabetes, Levemir can be administered once and at the same time tablets with a glucose-lowering effect can be taken. The initial dose for such patients is 0.1-0.2 units per 1 kg of body weight. Dosages for each patient are selected individually, based on the level of glycemia.
Levemir is administered under the skin of the anterior thigh, shoulder or abdomen. The injection site must be changed each time. To administer the drug you must:
- Use the dose selector to select the required number of units.
- Insert the needle into a fold of skin.
- Click the “Start” button.
- Wait 6 – 8 seconds
- Remove the needle.
Dose adjustment may be necessary in elderly patients with decreased renal or hepatic function, concomitant infections, changes in dietary intake, or increased physical activity. If the patient is transferred to Levemir from other insulins, then a new dose selection and regular glycemic monitoring are necessary.
Long-acting insulins, which include Levemir, are not administered intravenously due to the risk of severe forms of hypoglycemia. When administered intramuscularly, the onset of action of Levemir appears earlier than with subcutaneous injection.
The drug is not intended for use in insulin pumps.
Adverse reactions when using Levemir FlexPen
Side effects in patients using Levemir FlexPen are mainly dose-dependent and develop due to the pharmacological action of insulin. Hypoglycemia occurs most often among them. It is usually associated with incorrect selection of the dose of the drug or insufficient nutrition.
So Levemir’s price is lower than that of similar drugs. If a low concentration of glucose in the blood nevertheless occurs, this is accompanied by dizziness, an increased feeling of hunger, and unusual weakness. An increase in symptoms may manifest itself in impaired consciousness and the development of hypoglycemic coma.
Local reactions occur in the injection area and are temporary. More often there is redness and swelling, itching of the skin. If the rules for administering the drug are not followed and frequent injections are made in the same place, lipodystrophy may develop.
General reactions to the use of Levemir occur less frequently and are a manifestation of individual hypersensitivity. These include:
- Swelling in the first days of drug administration.
- Hives, skin rashes.
- Gastrointestinal disorders.
- Difficulty breathing.
- Widespread itching of the skin.
- Angioedema.
If the dose is lower than the insulin requirement, an increase in blood sugar levels can lead to the development of diabetic ketoacidosis.
Symptoms increase gradually over several hours or days: thirst, nausea, increased urine output, drowsiness, redness of the skin and the smell of acetone from the mouth.
Combined use of Levemir with other drugs
Medicines that enhance the lowering properties of Levemir on blood sugar include antidiabetic tablets, Tetracycline, Ketoconazole, Pyridoxine, Clofibrate, Cyclophosphamide.
The hypoglycemic effect is enhanced by the joint administration of certain antihypertensive drugs, anabolic steroids, and medications that contain ethyl alcohol. May also cause uncontrolled, long-term, increased blood sugar levels.
Corticosteroids, oral contraceptives, medications containing heparin, antidepressants, diuretics, especially thiazide diuretics, morphine, nicotine, clonidine, growth hormone, calcium blockers can weaken the effect of Levemir.
If reserpine or salicylates, as well as octreotide are used together with Levemir, they have multidirectional effects and can weaken or enhance the pharmacological properties of Levemir.
The video in this article provides an overview of Levemir FlexPen insulin.
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