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Lantus
Lantus is an antidiabetic insulin drug.
Pharmacodynamics
The active component of the drug is insulin glargine (an artificial analog of human insulin), which has a weak solubility within the neutral medium. In the drug solution, this substance completely dissolves, staying in an acidic environment, but after the introduction under the skin, the acid is neutralized with the formation of micro-precipitates, and then the insulin glargine component (small portions) is gradually released from them. This makes it possible to achieve a smooth AUC of the substance inside the plasma (sharp peaks along with recessions are not observed). Also, due to the formation of microprecipitates, the drug acquires extended properties.
The affinity of the active substance LS to insulin conductors is similar to that of the human analogue. Synthesis with the IGF-1 conductor of insulin glargin exceeds human indices by 5-8 times, but at the same time its decay products are slightly lower than the human analogue.
The total level of drug concentration of insulin (the active ingredient together with the decay products) observed in individuals with type 1 diabetes mellitus is much lower than the values suitable for semi-maximal synthesis with IGF-1 conductors, and at the same time for further activation of the mitogenic-proliferative process influence that arises under the influence of this receptor.
Internal IGF-1, under normal conditions, is capable of triggering a mitogenic-proliferative effect, but insulin dosages used during insulin therapy are much lower than the indices 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 (increasing the need for peripheral tissues (muscles and fat deposits) in this substance), and at the same time it suppresses the process of forming this element inside the liver. In addition, insulin suppresses proteolysis, as well as lipolysis inside adipocytes, while at the same time launching the binding process with proteins.
When conducting clinical and pharmacological tests, it was found that insulin glargine, together with its human analog at the same dosages, is equivalent after IV injections.
In accordance with other insulins, the properties and duration of the insulin glargine effect is affected by the level of physical activity, as well as other factors.
Slow absorption of the solution with n / k introduction makes it possible to conduct the treatment procedure once per day. But it must be borne in mind that, relative to time intervals, the effect of insulin has a marked individual variability.
During the tests, there were no significant differences in the dynamics of proliferative retinopathy in the case of NPH insulin, as well as insulin glargine.
Pharmacokinetics
Absorption of the active substance is very slow, so after the sc administration, the drug has no peak concentration (compared with NPH insulin). After the injection of the medication, the equilibrium value is observed on the 2-4th day of the treatment course once a day. In the case of intravenous administration, the half-life of insulin glargine was equal to the half-life of the human analogue.
Metabolism of the active component occurs with the formation of 2 active derivatives (M1, as well as M2). The effect of SC administration is mainly associated with the exposure of the element M1, but insulin glargine with M2 was not detected in many participants of the test.
Use of the lantus during pregnancy
Clinical tests for the use of Lantus were not carried out by pregnant women. Information that was obtained during postmarketing studies (approximately 300-1000 described cases) showed that the active ingredient does not have a negative effect on fetal development and pregnancy. Animal tests also showed no toxic effects on the fetus. Proceeding from this, it can be concluded that the medicine does not disrupt the reproductive system.
If there is a need, the doctor can prescribe a solution to treat a pregnant woman. But you need to carefully monitor the plasma glucose values and the general condition of the woman. At the first trimester, the need for insulin may decrease, but on the second and third it may, on the contrary, increase. Further, immediately after birth, there is a sharp decrease in this need with the risk of further occurrence of hypoglycemia.
During lactation it is allowed to use the medicine, but you need to carefully monitor the dosage of the substance. After penetrating the digestive tract, the active ingredient is split into amino acids, so it can not harm the breast baby that the mother is breast-feeding. Information on the ingestion of insulin glargine into the mother's milk - no.
Contraindications
Among the contraindications:
- the presence of intolerance with respect to the active substance or additional elements that are present in the medicinal product;
- the patient has hypoglycemia;
- it is forbidden to appoint children under the age of 6;
- Do not choose as a remedy for the elimination of the diabetic form of ketoacidosis.
Care should be taken when using high-risk patients complications of health during episodes of hypoglycemia. This includes patients with a diabetic form of retinopathy, and in addition a narrowing of the vessels of the cerebral or coronary type.
Side effects of the lantus
As a result of the use of drugs, hypoglycemia most often develops (in situations where insulin is administered in quantities that exceed human need). In addition, insulin glargine can cause the following side effects:
- organs of the National Assembly: impaired vision, development of retinopathy or dysgeusia;
- subcutaneous tissue with skin: development of lipodystrophy or lipogypertrophy;
- disorders of metabolic processes: development of hypoglycemia;
- allergic symptoms: the appearance on the site of injection of swelling or hyperemia, the development of urticaria, angioedema, anaphylaxis or spasm of the bronchi;
- Other: accumulation in the body of sodium, development of myalgia.
Dosing and administration
The administration of the drug solution is carried out by the method, but the method of in / in use is forbidden, since it even in usual dosages can provoke the appearance of hypoglycemia in severe form. Prolonged properties of drugs provide exactly the injection in the subcutaneous fat layer.
During treatment, it is necessary to follow a certain regimen, and also to correctly perform the procedure of drug administration.
There are no clinically significant differences in the case of drug administration to the deltoid muscle, abdomen or thigh region. However, while remaining within the most suitable areas for the introduction, it is necessary to change the injection site during each new procedure.
The medicine can not be diluted or mixed with other drugs.
Dosage dimensions:
In Lantus contains insulin, which has a prolonged effect. It is required to enter it once a day, and the procedure should always be carried out at the same time. The regime is selected for each separately - the size of the doses, the time of the procedure, etc. It is allowed to use the medicine in combination treatment of type 2 diabetes mellitus (together with hypoglycemic drugs).
It should be taken into account that the ED of Lantus is different from the indices of ED of other insulin products.
In elderly people, due to a progressive disorder in the work of the kidneys, the body's need for insulin can be constantly reduced. Therefore, in the case of a person with disorders of kidney function, there may be a reduced (in comparison with patients with healthy renal function) the need for this substance.
In case of impaired hepatic function, the need to receive insulin may also decrease (as the metabolism of this substance slows down, and gluconeogenesis is reduced).
When implementing the transition to Lantus from other types of insulin medicines:
In case of using insulin having a high or medium extent of exposure, after the transition, it may be necessary to correct the size of the dose of the background insulin, and with it the change in the concomitant treatment. To reduce the likelihood of hypoglycemia in the night, and also in the morning, people who change the mode of taking background insulin (switching from 2-time injections (application of NPH insulin) to disposable (Lantus administration)), it is necessary to reduce its dosage during 20-30% 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 characteristics of the patient.
In humans, which have antibodies to human insulin, during the use of the medicine, the body can give a modified reaction to this substance. Due to such a violation, dosage adjustment may be required.
Dosage should be changed in case of a change in lifestyle, weight, and other factors that can affect the properties of insulin.
Overdose
In the case of administering the solution in large quantities, it is possible to develop severe and prolonged hypoglycemia, the progression of which can become life-threatening.
If episodes of overdose are poorly expressed, the intake of carbohydrates helps. If hypoglycemia appears regularly, a person's lifestyle needs to be corrected, and with it the dose of the drug.
With the development of severe forms of hypoglycemia (amongst such episodes, accompanied by various neurological disorders, seizures and coma), it is necessary to inject glucagon into / m or s / c or to inject iv glucose (concentrated solution). Since Lantus has a prolonged effect, even in the case of improving health, it takes a long time to continue to give the patient carbohydrates and monitor his state of health.
Interactions with other drugs
In the case of combination with drugs that affect the processes of glucose metabolism, you may need to adjust the size of the dose of Lantus.
Strengthening hypoglycemic properties of drugs is observed when combined with fluoxetine, propoxyphene, salicylates, fibrates, as well as pentoxifylline, sulfonamides and disopyramide. In addition, such an action has inhibitors of MAO and ACE, as well as hypoglycemic drugs for oral administration.
Weakening hypoglycemic properties of the drug cause corticosteroids, glucagon, isoniazid with danazol and somatropin. In addition, there are also progestins with estrogens, clozapine, diazoxide and olanzapine. Along with this, diuretics, phenothiazine derivatives, sympathomimetics, protease inhibitors and thyroid hormones.
Lithium drugs, clonidine, as well as β-blockers with ethanol are able to both enhance and weaken the effect of the drug.
The combination with pentamidine can provoke hypoglycemia, which later becomes hyperglycemia.