Levemir

Levemir is an antidiabetic drug that is an analog of human insulin, and has a prolonged effect.

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Indications of the lewemere

It is used for basal treatment in people with diabetes mellitus. The medication can be prescribed for the treatment of diabetes in addition to adults, as well as children aged 2 years.

Release form

The drug is released in the form of a parenteral drug solution, in special syringe pens with a volume of 3 ml. Inside the box - 1 or 5 of these syringes.

Pharmacodynamics

Levemir is a soluble form of basal human insulin. It has a powerful prolonged effect and is used for basal treatment of people diagnosed with type 1 diabetes mellitus.

The drug has a noticeable predictability of the severity and nature of the effect (if you compare it with insulin glargine, as well as NPH-insulin). Its long therapeutic effect is associated with a significant interconnection of the insulin detemir element structures, and in addition with the synthesis of the active element of the drug with albumin (binding occurs with the participation of side chains of fatty acids).

However, the prolonged effect of the drug is provided by the ability of insulin detemir significantly more slowly (if we compare these indicators with NPH-insulin) to be distributed inside the target tissues. A comprehensive mechanism for prolonging exposure helps to provide a well-predicted mechanism of drug effect.

The antidiabetic effect of the drug is due to the improvement in the ability of target tissues to absorb glucose (after the synthesis of insulin with specific endings of muscle, and in addition fatty tissue), and in addition, a decrease in the ability of the liver to release glucose.

The drug lasts for a maximum of 24 hours (the exact duration depends on the size of the applied dosage), so that one-time or two-time application of the solution can be prescribed. On average, 2-3 drug injections are necessary to achieve the required glycemic control with a two-time administration.

During the tests, the use of drugs in a dose of 0.2-0.4 U / kg caused the development of 50% of the highest impact on the 3-4th hour after the injection (the whole action lasted a maximum of 14 hours).

The solution has linear parameters of influence - the total and peak effects, as well as the duration of the action of the drug, are proportional to the size of the dosages.

Long-term use of the drug during clinical tests showed a small (in comparison with the indices when NPH-insulin was administered) basal variation of the level of glucose inside the serum.

However, during prolonged clinical tests, we found weaker changes in weight in people who received Leuemir (compared to those who used other forms of insulin).

In people with Type 2 diabetes who used insulin in addition to treatment with oral antidiabetics, there was a decrease in the incidence of nighttime hypoglycemia after Levemir.

In some groups treated with long-term use of insulin detemir, the appearance of antibodies was noted, but this effect did not affect the therapeutic effectiveness of glycemic control.

Pharmacokinetics

Peak values of the active element of the drug are noted inside the serum after 6-8 hours after the SC injection. In the case of administration of the solution twice per day, a suitable glycemic control is noted after the application of a 2-3 injection. Different groups of patients have a significantly smaller individual difference in the rate of absorption of the active component (compared with the use of other basic insulin drugs).

The absolute bioavailability of the drug is approximately 60% (after the administration of the solution).

The main part of the used portion of the medicine circulates inside the vascular bed - this fact shows an index of the distribution volume, which is about 0.1 l / kg.

Tests in vivo, as well as in vitro, did not find a clinically significant interaction between insulin detemir in combination with fatty acids or other preparations synthesized with the protein.

The metabolic processes of Levemir's active substance are similar to those that are performed with endogenous insulin. All derivatives of the drug have no drug activity.

The exponent of the final half-life after the administration of drugs depends on the values of the rate of absorption inside the subcutaneous layer and, taking into account the number, reaches an interval of 5-7 hours.

The solution has linear pharmacokinetic parameters.

Dosing and administration

The medication is administered subcutaneously through a special syringe pen. The drug helps the development of prolonged antidiabetic effect (maximum 24 hours), so that it can be used as a basal form of insulin, administered once or twice a day. It is possible to use the drug for monotherapy either in combination with a bolus form of insulin, liraglutide or antidiabetic oral drugs.

The size of a portion of the drug is determined individually, a small daily variability of basal glucose values within the serum allows you to select the exact dosage of insulin for glycemic control as accurately as possible.

The size of the average recommended initial portion of medicines for people who take oral antidiabetics is 10 units or 0.1-0.2 units / kg once a day. It is necessary to monitor the glucose values inside the serum at the initial stage of treatment, in order to correctly choose the size of the portion.

If the glucose values after an independent measurement of them on an empty stomach in the morning are equal to more than 10 mmol / l, the dose of the drug is increased by 8 units, and if these values are in the range 9.1-10, and also 8.1-9 and 6.1 -8, you need to increase the portions by 6, 4 or 2 units, respectively. At glucose values measured under the conditions described above, 3.1-4 mmol / l are equal, the size of the insulin detemir should be reduced by 2 units, and at a value of less than 3.1 mmol / l - reduced by 4 units.

The frequency of injection is prescribed by the doctor, taking into account the auxiliary treatment and the need for the patient's body to receive insulin.

People who are required to administer insulin twice a day are advised to have a 2nd procedure before the evening meal or before bedtime.

It must be taken into account that the correction of exercise and nutrition, and in addition severe stress or the development of concomitant pathology may cause the need to change the dosage of the drug.

Use Levemir in some categories of patients.

It should be remembered that with changes in the liver / kidneys, dosage adjustment may be necessary (as the patient's need for insulin changes). It is necessary to closely monitor the condition of people in this group and change the portion size if there is a deterioration in glycemic control.

During the tests, the safety and therapeutic effectiveness of drug use in patients aged 2 years was noted. Children needing insulin therapy need careful monitoring of serum glucose values. It is necessary to carefully select the sizes of insulin doses for children.

Scheme of transition to Levemir from other insulin forms.

People who previously used insulin, having long or moderate duration of exposure, should carefully select the dosage during the transition to Leu-mire. When it is carried out, very careful monitoring of the level of glucose inside the serum is necessary.

Conducting combined treatment of diabetes requires a review of the regimen of use and dosage of all medications used during the transition to a different type of insulin.

Scheme of administration of drug solution.

Injection is necessary only by subcutaneous method. Intravenous injections and intramuscular injections are prohibited. With / in the introduction of insulin, hypoglycemia can develop in a pronounced form (up to a fatal outcome).

You can not prescribe a drug injection with insulin pumps that have a continuous function of administration, the drug can be administered only through a syringe pen.

With n / k injections, you should choose a place in the area of the front femoral surface, on the shoulder or in the anterior part of the peritoneum. All injections are recommended to be performed in different areas of the body (even within one small site), otherwise it can provoke the development of lipodystrophy.

The duration of exposure and the degree of manifestation of the antidiabetic effect of drugs can vary with the speed of circulation, temperature, the size of the dose of the drug, the site of injection, as well as physical activity (in connection with the metabolic rate and absorption of the active element of the drug).

Injections should be performed at the same time of day, the most convenient for the patient.

The syringe is used in combination with disposable needles (NovoTvist or NovoFine), having a length of 8 mm. The syringe is able to administer insulin within 1 to 60 units, also having a step of 1 unit.

Scheme of using a syringe-pen when injecting.

The syringe pen is intended exclusively for the administration of insulin injections to Leuwemir.

Scheme of injection:

• Before the introduction, it is necessary to check the insulin type;
• remove the protective cap from the syringe;
• remove the packing label from the needle for a single dose, and then tightly attach it to the syringe;
• remove the outer cap from the needle (you need to save it before the end of the injection procedure);
• remove the inner protective cap from the needle, and immediately dispose of it;
• set the portion size, after which you can start the injection. To set the dosage, you need to use a special selector;
• Insert the needle into the chosen place, and then press the button on the syringe;
• it is required to hold the button clamped, without taking out the needle for at least 6 seconds (to enter the whole portion);
• get a needle and remove it from the syringe, using an external protective cap for this;
• close the syringe with a protective cap.

For each injection, you need to install a new needle. If the needle has been damaged or bent before the procedure, you should recycle it and use a new one. To prevent accidental pricking with a needle, it is forbidden to re-put an inner protective cap on it after removing it.

Before starting the medication, you need to check your insulin current. This is done as follows:

• it is necessary to put a mark of 2 units on the selector;
• While holding the syringe in the upright position, with the needle up, you should tap it gently in the area where the cartridge is located;
• Still holding the syringe in a vertical position, you need to press the button. As a result, the metering selector should return to the 0 mark, and a drop of medicine should appear at the tip of the needle;
• if after aforementioned manipulations a drop of solution does not occur, it is necessary to replace the needle and repeat the procedure described above;
• it is forbidden to repeat this manipulation more than 6 times - if there is no result after such a number of attempts, it can be concluded that the syringe is defective, and therefore it is no longer possible to use it.

The portion set on the selector is allowed to be changed both in the direction of decrease and upwards, for this purpose, scrolling the selector in the required direction. During the installation of the dosing, it is necessary to carefully check that the start button is not pressed (because this can cause the leakage of insulin).

It is necessary to remember that on the syringe selector you can not set a dosage that exceeds the amount of drugs left inside the cartridge. You can not also use the insulin residue scale to select the portion.

It is necessary to remove the needle from the syringe after each procedure, because if left in place, it can cause the drug to leak.

During the implementation of injection procedures, general aseptic rules are required.

It must also be remembered that the syringe is intended only for individual use.

Cleaning and subsequent storage of the syringe pen.

It is not recommended to use the syringe if it fell or was deformed (because this could cause leakage of the drug).

The outer part of the used syringe must be cleaned with cotton, which is pre-wetted in ethanol. Do not hold the syringe under running water, completely immerse it in alcohol or lubricate it with different means.

Re-fill the syringe - it is forbidden.

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Use of the lewemere during pregnancy

Pregnant women who use insulin detemir should closely monitor the glucose values inside the serum. When pregnancy changes the body's need for insulin, in accordance with which and need to adjust the portion of the medicine. At the 1st trimester, there is a decrease in the need for insulin, but on the 2 nd and 3 rd - significantly increases. After delivery, a rapid return of indicators of this need to the level observed before pregnancy.

Levemir does not adversely affect the course of pregnancy, as well as the healthy development of the fetus, and during the tests there was no increase in the probability of the appearance of pathologies in the fetus.

Tests conducted on animals did not demonstrate the toxic effect of drugs on reproductive activity.

There is no information regarding the penetration of the drug into the mother's milk. The likelihood of the effect of its active component on infants who are breastfed is not too great, because as inside the GI tract the element splits, acquiring the shape of amino acids.

Lactation may require a more careful selection of the size of the portion of insulin, as well as the diet regime.

Contraindications

Contraindicated use of drugs in the presence of the patient's hypersensitivity against insulin detemir or auxiliary medicinal elements.

Side effects of the lewemere

Most of the negative signs revealed during the testing of the solution were the result of the antidiabetic effect of insulin or the consequence of the effect of the underlying disease.

Often when applying the drug in patients developed hypoglycemia.

In the process of using a syringe for subcutaneous injection, local reactions can develop - for example, the appearance of tissue edema, itching, skin hyperemia, as well as bruising at the site of injection. In addition, generalized signs of hypersensitivity can occur on the skin, including itching, hives and rashes.

Local symptoms often disappear on their own without requiring special therapy. These manifestations are most pronounced at the initial stage of drug use, the intensity gradually decreases during the course of therapy.

At the initial stage of insulin therapy, treating people can develop refractory disorders, and in addition tissue swelling, which disappear themselves during the treatment.

With the development of a significant positive dynamics in the control of glycemia in people with diabetes, painful neuropathy can develop in the acute stage (it is curable and arises because of strong changes in serum glucose values).

At the first stage of treatment, along with a significant improvement in the effectiveness of glycemic control, patients may experience transient negative dynamics of the course of the diabetic form of retinopathy (in this case, prolonged and effective glycemic control reduces the risk of development and progression of this pathology).

In total, during post-marketing and clinical testing, the following side-effects were noted in patients (this includes reactions that were only observed singly):

• immune lesions: rashes, allergic symptoms, urticaria and manifestations of anaphylaxis;
• disorders of metabolic processes: development of hypoglycemia;
• disorders in the work of the central nervous system: the emergence of polyneuropathy;
• manifestations of the senses: a diabetic form of retinopathy, as well as temporary refractory disorders;
• lesions affecting the subcutaneous layer and skin: development of lipodystrophy (the risk of this disease increases with regular repeated injections of drugs in the same area of the skin without changing the site of administration);
• local signs: temporary swelling, itching and hyperemia.

The single use of the drug led to the appearance of symptoms of anaphylaxis (among such cases and potentially fatal). If a patient develops signs of anaphylaxis or Quincke's edema during treatment, he should immediately seek emergency medical attention.

The hypoglycemia that occurs during the use of Levemir is usually caused by improper selection of a portion of insulin, and besides this, a change in diet or exercise. In addition, the risk of hypoglycemia increases with the presence of the patient's infections, against which hyperthermia occurs.

Hypoglycemia in a severe degree can lead to the development of seizures, loss of consciousness, and then to the ongoing and permanent head injuries and death. Among the first signs of pathology: a feeling of weakness, drowsiness and thirst, loss of orientation, development of tremors, tachycardias, headaches, nausea and visual disorders, and besides pale skin, hunger and cold sweat. It must be remembered that the early symptoms of the disease can diminish their intensity with long-term treatment with insulin, and in combination with other drugs and people with diabetes for a long time.

Overdose

In our time, it has not been possible to fully formulate the specific concept of insulin intoxication. If too high portions of Levemir are administered, the patient may develop hypoglycemia.

If a mild form of impairment is noted, the patient should use fast carbohydrates (for example, a glucose tablet or a small piece of sugar). People with diabetes should always have something sweet with them.

With the development of hypoglycemia in severe form, when the patient loses consciousness, it is necessary to administer glucagon (in / m or s / c method in a dose of 0.5-1 mg). In the absence of improvements from the use of glucagon after 10-15 minutes, you should perform an infusion of glucose solution.

After returning to the patient consciousness, it is required to let him take carbohydrates inside to prevent the development of relapse.

Interactions with other drugs

During combined use of drugs and other medicines, it is necessary to take into account the effect of different drugs on the body's need for insulin, and also the level of glucose tolerance.

Antidiabetic drugs for ingestion, non-selective β-adrenoreceptor antagonists, MAOI, ACE inhibitors, salicylates, and in addition, steroidal anabolics and sulfonamides can reduce the need of the body for patients to receive insulin.

SCS, oral contraception, thiazide diuretics, sympathomimetics, growth hormones, thyroid hormones and danazol on the contrary - increase the need for insulin.

Combination with levemir antagonists of β-adrenergic receptors can lead to masking of symptoms of hypoglycemia.

The need for insulin production can vary with the use of octreotide or lanreotide.

Ethanol in combination with the drug is able to potentiate the duration and severity of the antidiabetic effect of insulin detemir.

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Storage conditions

The syringe-pen used by the patient must be kept in a place closed from children's access at standard temperature marks. If the syringe is not being used, it should be kept at a temperature of 2-8 grades ^of C.

At the standard temperature, the syringe of the preparation can be stored for a maximum of 1.5 months.

Freeze the solution Levemir is prohibited. The syringe should be kept in a dark place, closed from sunlight.

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Shelf life

Levemir can be used for 2.5 years since the release of the drug.

Application for children

Children under the age of 2 years are not allowed to be appointed Levemir.

Analogues

Analogues of drugs are such means: Insulin Lente GPP, Insulong SPP, Actrafan NM, and in addition Insulin Minilente SPP, Iletin II Lente and Insulin Superlente SPP. The list also includes Limifomiosot, Yanuvia, Humulin ultralente, as well as Multisorb, Lymphomyosot, Bagomet, Metamin and Apidra. In addition, Glukobay, Glamaz and Leveemir Penfill.

Reviews

Levemir gets good feedback from people with diabetes. Among the pluses, patients note high efficiency, lack of addiction to the drug, as well as weight gain, and also the possibility of using the drug during pregnancy.

Of the minuses, however, the majority highlights the high cost of the medication. Some also complain of the inconvenience of using medical cartridges.