Lantus

Lantus is an antidiabetic insulin drug.

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Indications Lantus

Indicated for the treatment of insulin-dependent diabetes in children aged 6 years and over, as well as adults.

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Release form

It is produced as an injection solution contained in 3 ml cartridges. There are 5 cartridges inside 1 blister. There is 1 blister plate inside a separate package.

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Pharmacodynamics

The active component of the drug is insulin glargine (an artificial analogue of human insulin), which has poor solubility in a neutral environment. In a medicinal solution, this substance completely dissolves, being in an acidic environment, but after subcutaneous administration, the acid is neutralized with the formation of microprecipitates, and from them the insulin glargine component begins to be gradually released (in small portions). This allows achieving smooth AUC values of the substance in the plasma (sharp peaks and declines are not observed). Also, due to the formation of microprecipitates, the drug acquires prolonged properties.

The affinity of the active substance of the drug to insulin conductors is similar to the analogous properties of the human analogue. Synthesis with the IGF-1 conductor of insulin glargine exceeds the human indicators by 5-8 times, but at the same time the indicators of its decay products are slightly lower than those of the human analogue.

The overall level of medicinal insulin concentration (active substance together with breakdown products) observed in individuals with type 1 diabetes mellitus is much lower than the values suitable for half-maximal synthesis with IGF-1 conductors, and at the same time for further activation of the mitogenic-proliferative effect process that occurs under the influence of this receptor.

In a normal state, internal IGF-1 is capable of triggering mitogenic-proliferative action, but the medicinal doses of insulin used during insulin therapy are much lower than the values required to trigger this process (indirectly through IGF-1).

The main function of the substance insulin (also insulin glargine) is the normalization of carbohydrate metabolism (the process of glucose metabolism). At the same time, the drug reduces plasma glucose levels (increasing the need of peripheral tissues (muscles and fat deposits) for this substance), and at the same time suppresses the process of formation of this element inside the liver. In addition, insulin suppresses proteolysis, as well as lipolysis inside adipocytes, simultaneously launching the process of binding to proteins.

During clinical pharmacological tests, it was found that insulin glargine together with its human analogue in the same dosages are equivalent after intravenous injections.

As with other insulins, the properties and duration of the effect of insulin glargine are influenced by the level of physical activity and other factors.

Slow absorption of the solution when administered subcutaneously makes it possible to perform the treatment procedure once a day. However, it should be taken into account that the effect of insulin has significant individual variability in terms of time intervals.

During the testing, no significant differences were found in the dynamics of the development of proliferative retinopathy in the case of using NPH insulin, as well as insulin glargine.

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Pharmacokinetics

The absorption of the active substance is very slow, so after subcutaneous administration the drug does not have a peak concentration (compared to NPH insulin). After a single daily injection of the drug, the equilibrium value is observed on the 2nd-4th day of the treatment course. In the case of intravenous administration, the half-life of insulin glargine was equal to the half-life of the human analogue.

The metabolism of the active component occurs with the formation of 2 active derivatives (M1 and M2). The effect of subcutaneous administration is associated mostly with the exposure of the M1 element, but insulin glargine with M2 was not detected in many test participants.

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Dosing and administration

The drug solution is administered subcutaneously, but the intravenous method is prohibited, since even in normal doses it can provoke the occurrence of severe hypoglycemia. The prolonged properties of the drug are provided by injection into the subcutaneous fat layer.

During treatment, it is necessary to adhere to a certain regimen, as well as correctly perform the procedure for administering the drug.

There are no clinically significant differences when injecting the drug into the deltoid, abdomen or thigh area. However, while remaining within the most suitable areas for injection, the injection site should be changed during each new procedure.

The medicine must not be diluted or mixed with other drugs.

Dosage sizes:

Lantus contains insulin, which has a prolonged effect. It must be administered once a day, and the procedure must always be carried out at the same time. The regimen is selected for each person individually - dose sizes, procedure time, etc. It is allowed to use the drug in the combined treatment of type 2 diabetes (together with hypoglycemic drugs).

It should be taken into account that the ED values of Lantus are different from the ED values of other insulin products.

In elderly people, due to progressive kidney dysfunction, the body's need for insulin may be constantly reduced. Therefore, if a person has kidney dysfunction, there may be a reduced (compared to patients with healthy kidney function) need for this substance.

In case of impaired liver function, the need for insulin may also decrease (since the metabolism of this substance slows down, and a decrease in gluconeogenesis is also observed).

When switching to Lantus from other types of insulin medications:

In the case of using insulins with a long or medium duration of action, after the transition it may be necessary to adjust the background insulin dose, and at the same time change the concomitant treatment. To reduce the likelihood of hypoglycemia at night, as well as in the morning, people changing the background insulin regimen (transition from 2-time injections (use of NPH insulin) to single ones (administration of Lantus)), need to reduce its dosage by 20-30% during the first weeks of treatment. At the same time, it is necessary to slightly increase the dosage of insulin taken with food. After 2-3 weeks, the dose sizes are adjusted taking into account the patient's characteristics.

People who have antibodies to human insulin may have an altered response to the substance when using the drug. This may require dosage adjustments.

The dosage should also be changed in the event of changes in lifestyle, weight, and other factors that can affect the properties of insulin.

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Use Lantus during pregnancy

Clinical trials of Lantus use in pregnant women have not been conducted. Information obtained during post-marketing studies (approximately 300-1000 reported cases) showed that the active ingredient does not have a negative effect on fetal development and pregnancy. Animal tests also did not reveal any toxic effects on the fetus. Based on this, it can be concluded that the drug does not interfere with the reproductive system.

If necessary, the doctor may prescribe a solution for treating the pregnant woman. But it is necessary to closely monitor plasma glucose values and the general condition of the woman. In the 1st trimester, the need for insulin may decrease, but in the 2nd and 3rd, on the contrary, it may increase. Then, immediately after childbirth, there is a sharp decrease in this need with the risk of further hypoglycemia.

During lactation, it is allowed to use the medicine, but it is necessary to carefully monitor the dosage of the substance. After penetrating the digestive tract, the active ingredient is broken down into amino acids, so it is not capable of harming a breastfed baby. There is no information about insulin glargine getting into breast milk.

Contraindications

Among the contraindications:

• the presence of intolerance to the active substance or additional elements that are present in the composition of the drug;
• the patient has hypoglycemia;
• It is prohibited to prescribe to children under 6 years of age;
• should not be chosen as a drug for the treatment of diabetic ketoacidosis.

Caution is required when used by individuals with a high risk of health complications during hypoglycemic episodes. This includes patients with diabetic retinopathy, as well as cerebral or coronary vasoconstriction.

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Side effects Lantus

As a result of using the drug, hypoglycemia most often develops (in situations where insulin is administered in quantities that exceed a person's needs). In addition, insulin glargine can cause the following side effects:

• nervous system organs: weakening of vision, development of retinopathy or dysgeusia;
• subcutaneous tissue with skin: development of lipodystrophy or lipohypertrophy;
• metabolic disorders: development of hypoglycemia;
• allergic symptoms: the appearance of swelling or hyperemia at the injection site, the development of urticaria, angioedema, anaphylaxis or bronchospasm;
• Others: accumulation of sodium in the body, development of myalgia.

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Overdose

If the solution is administered in large quantities, severe and prolonged hypoglycemia may develop, the progression of which may become life-threatening.

If overdose episodes are mild, carbohydrate intake helps. If hypoglycemia occurs regularly, lifestyle adjustments are required, along with the size of the drug dose.

In the case of severe forms of hypoglycemia (including episodes accompanied by various neurological disorders, seizures and comatose states), it is necessary to administer glucagon intramuscularly or subcutaneously or to administer glucose (concentrated solution) intravenously. Since Lantus has a prolonged effect, even if the patient's health improves, it is necessary to continue giving the patient carbohydrates for a long time and monitor his/her well-being.

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Interactions with other drugs

In case of combination with drugs that affect glucose metabolism processes, it may be necessary to adjust the dose of Lantus.

Increased hypoglycemic properties of the drug are observed when combined with fluoxetine, propoxyphene, salicylates, fibrates, as well as pentoxifylline, sulfonamides and disopyramide. In addition, similar effects are exerted by MAO and ACE inhibitors, as well as hypoglycemic drugs for oral administration.

Weakening of the hypoglycemic properties of the drug is caused by corticosteroids, glucagon, isoniazid with danazol and somatropin. In addition, also progestins with estrogens, clozapine, diazoxide and olanzapine. Along with this, diuretic drugs, phenothiazine derivatives, sympathomimetics, protease inhibitors and thyroid hormones.

Lithium drugs, clonidine, as well as β-blockers with ethanol can both enhance and weaken the effect of the drug.

The combination with pentamidine can provoke hypoglycemia, which subsequently transforms into hyperglycemia.

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Storage conditions

Lantus must be kept at a temperature of 2-8 ^o C. The solution must not be frozen. After opening the cartridge, the medicine must be stored at a temperature of 15-25 ^o C.

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Shelf life

Lantus is suitable for use for 3 years from the date of release of the solution. But after opening the cartridge with the medicine, it is allowed to use it for no more than 1 month.