Saxenda injection 6mg ml 3ml
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Active ingredients
Lyraglutide
Release form
Solution
Composition
1 ml contains: Active ingredient: liraglutide 6 mg (3 ml of solution are contained in one pre-filled syringe, which corresponds to 18 mg of liraglutide); Excipients: sodium hydrogen phosphate dihydrate 1.42 mg, phenol 5.5 mg, propylene glycol 14 , 0 mg; hydrochloric acid / sodium hydroxide (for pH adjustment), water for injection up to 1 ml.
Pharmacological effect
Mechanism of actionLiraglutide is an analogue of human glucagon-like peptide-1 (GLP-1), produced by recombinant DNA biotechnology using Saccharomyces cerevisiae strain, having 97% homology with human GLP-1, which binds and activates GLP-1 receptors in humans. The GLP-1 receptor serves as a target for native GLP-1, an endogenous hormone incretin, which stimulates glucose-dependent insulin secretion in pancreatic beta cells. Unlike native GLP-1, the pharmacokinetic and pharmacodynamic profiles of liraglutide allow it to be administered to patients 1 time per day. The long-acting profile of liraglutide in s / c injection is provided by three mechanisms: self-association, which results in slow absorption of the drug, binding to albumin and more high level of enzymatic stability with respect to dipeptidyl peptidase-4 (DPP-4) and the enzyme neutral endopeptidase (NEP), due to which a long-term T1 / 2 drug from plasma is provided. The action of liraglutide is due to the interaction with specific GLP-1 receptors, as a result of which the concentration of cAMP increases. Under the action of liraglutide, glucose-dependent stimulation of insulin secretion and improvement of pancreatic beta-cell function occurs. At the same time, liraglutide suppresses the excessively high glucose-dependent secretion of glucagon. Thus, with an increase in blood glucose concentration, insulin secretion is stimulated and glucagon secretion is suppressed. On the other hand, during hypoglycemia, liraglutide decreases insulin secretion, but does not inhibit glucagon secretion. The mechanism of reducing blood glucose levels also includes a slight delay in gastric emptying.Liraglutide reduces body weight and reduces body fat with the help of mechanisms that cause a decrease in hunger and reduced energy consumption. Studies on experimental animal models with pre-diabetes have shown that liraglutide slows down the development of diabetes. In vitro diagnostics have shown that liraglutide is a powerful factor in the specific stimulation of the proliferation of beta cells in the pancreas and prevents the formation of cytokines and free fatty acids, inducing death of beta cells (apoptosis). In vivo, liraglutide increases insulin biosynthesis and increases the mass of beta cells in experimental animal models with diabetes mellitus. When the glucose concentration is normalized, liraglutide stops increasing the mass of the beta cells of the pancreas.
Pharmacokinetics
Absorption Liraglutide suction after s / c injection occurs slowly, the time to reach Cmax in plasma - 8-12 hours after a dose of the drug. Cmax of liraglutide in plasma after s / c injection in a single dose of 0.6 mg is 9.4 nmol / l. With the introduction of liraglutide at a dose of 1.8 mg, the average Css in plasma (AUC0-24) reaches approximately 34 nmol / l. The exposure of liraglutid increases in proportion to the dose administered. After the introduction of liraglutide in a single dose, the intrapopulation coefficient of variation of AUC is 11%. The absolute bioavailability of liraglutide after s / c infusion is approximately 55%. Distribution The apparent Vd of liraglutide in tissues after s / c infusion is 11-17 liters. The average Vd of liraglutide after i / v administration is 0.07 l / kg. Lyraglutide is largely bound to plasma proteins (more than 98%). Metabolism For 24 hours after administration of a single dose of a radiolabeled [3H] -lraglutide to healthy volunteers, the main component of plasma remained unchanged liraglutide. Two plasma metabolites were detected (≤9% and ≤5% of the total radioactivity level in the blood plasma). Lyraglutide is metabolized endogenously like large proteins, without the involvement of any specific organ as a route of excretion. ExcretionAfter administration of a dose of [3H] -lraglutide, unchanged liraglutide was not detected in the urine or feces. Only an insignificant part of the administered radioactivity in the form of metabolites associated with liraglutide (6% and 5%, respectively) was excreted by the kidneys or through the intestines. Radioactive substances are excreted by the kidneys or through the intestines, mainly within the first 6-8 days after a dose, and are three metabolites.The average clearance from the body after s / c administration of liraglutide in a single dose is approximately 1.2 l / h with an elimination T1 / 2 of approximately 13 hours. Pharmacokinetics in special groups of patients Data from pharmacokinetic studies in the group of healthy volunteers and analysis of the pharmacokinetic data obtained in the patient population (from 18 to 80 years) indicate that age does not have a clinically significant effect on the pharmacokinetic properties of liraglutide. Population pharmacokinetic analysis of data obtained during the study of the effect of liraglutide in female and male patients, and pharmacokinetic studies in a group of healthy volunteers indicate that sex does not have a clinically significant effect on the pharmacokinetic properties of liraglutide. Population pharmacokinetic analysis of data obtained in a study of liraglutide in subjects of white, black, Asian and Latino racial groups suggest that ethnicity has no clinically significant effect on pharmacokinetics Genetic properties of liraglutide. Population pharmacokinetic analysis of the data suggests that BMI does not have a clinically significant effect on the pharmacokinetic properties of liraglutide. The pharmacokinetic properties of liraglutide were investigated in a clinical study of a single dose of the drug in subjects with varying degrees of hepatic failure. The study included patients with mild hepatic insufficiency (5-6 points on the Child-Pugh scale) and severe hepatic insufficiency (more than 9 points on the Child-Pugh scale). Exposure of liraglutide in the group of patients with impaired liver function was not higher than that in the group of healthy volunteers, which indicates that hepatic impairment does not have a clinically significant effect on liraglutide pharmacokinetics. The pharmacokinetics of liraglutide were studied in patients with varying degrees of renal insufficiency in a one-time study doses. This study included patients with varying degrees of renal failure: from mild (CK 50-80 ml / min) to severe (CK less than 30 ml / min) and patients with end-stage renal failure who need hemodialysis.Renal failure did not have a clinically significant effect on the pharmacokinetics of liraglutide. The study of the drug in children has not been carried out. Pre-clinical safety studies The results of preclinical toxicological studies with the introduction of repeated doses of the drug, including genotoxicity, showed that the use of liraglutide does not pose a threat to human health. The thyroid C-cell tumors of rats and mice were identified during two years of studies of the carcinogenicity of the drug in rodents and were not fatal. Non-toxic dose (NOAEL) in rats has not been established. The appearance of such tumors in monkeys treated with liraglutide for 20 months was not observed. The results obtained in rodent studies are related to the fact that rodents are particularly sensitive to the GLP-1 receptor-mediated non-genotoxic specific mechanism. The significance of the data obtained for humans is low, but cannot be completely excluded. No other neoplasms related to the therapy were reported. The animal studies showed no direct adverse effect of the drug on fertility, but there was a slight increase in the frequency of early embryonic death in the treatment with the highest dose of the drug. The administration of the drug to rats in the middle of the gestation period caused their mother to lose weight and the growth of the embryo with an effect on the ribs that was not fully studied, and in the group of rabbits - deviations in the skeletal structure. The growth of newborns in the group of rats during drug therapy decreased, and this decrease persisted steadily in the period after the end of breastfeeding in the group of models receiving high doses of liraglutide. It is not known what caused such a decrease in the growth of newborn rats - a decrease in their consumption of mother's milk due to the direct effect of GLP-1 or insufficient production of breast milk by the mothers of rats due to a decrease in their calorie intake.
Indications
Saxend is shown as a supplement to a low-calorie diet and increased physical activity for long-term use in order to correct body weight in adult patients with a BMI: - ≥30 kg / m2 (obesity) or- ≥ 27 kg / m2 to less than 30 kg / m ( overweight) with at least one associated with overweight associated disease, such as impaired glucose tolerance, type 2 diabetes, arterial hypertension,dyslipidemia or obstructive sleep apnea.
Contraindications
- hypersensitivity to liraglutide or any of the auxiliary components of the drug; - medullary thyroid cancer in history, including familial; - multiple endocrine neoplasia type 2; - severe depression, suicidal thoughts or behavior, including anamnesis. Application is contraindicated in the following groups of patients and in the following conditions / diseases due to the lack of data on efficacy and safety: - severe renal dysfunction; - severe liver dysfunction; - children under 18 years of age; - pregnancy and breastfeeding periods; - heart failure III-IV functional class (in accordance with the classification of NYHA (New York Heart Association)); - simultaneous use of other drugs for the correction of body weight; - simultaneous use nenie insulin; - secondary obesity amid endocrinological diseases or eating disorders, or treatment with drugs that may lead to an increase of the drug weight tela.Opyt Saksenda in patients with inflammatory bowel diseases and diabetic gastric paresis limited. The use of liraglutide in these patients is not recommended because it is associated with transient adverse reactions from the gastrointestinal tract, including nausea, vomiting and diarrhea.
Precautionary measures
Due to limited experience, it is recommended to use with caution in patients with heart failure I-II functional class (in accordance with the NYHA classification), impaired renal function of moderate severity, aged 75 years and older.
Use during pregnancy and lactation
Cannot be used during pregnancy, insulin treatment is recommended instead. If the patient is preparing for pregnancy, or the pregnancy has already begun, treatment with Victoza should be stopped immediately. It is not known whether liraglutide is excreted in breast milk of women. Animal studies have shown that the penetration of liraglutide and metabolites of a close structural bond into breast milk is low.The experience of using the drug Victoza in nursing women is absent; use of the drug during breastfeeding is contraindicated.
Dosage and administration
Saxend preparation is intended only for subcutaneous administration. It can not be administered intravenously or intramuscularly. The Saxend preparation is administered once a day at any time, regardless of the meal. It should be injected into the abdomen, thigh, or shoulder area. Place and time of injection can be changed without dose adjustment. However, it is advisable to give injections at about the same time of day after choosing the most convenient time. Doses: The initial dose is 0.6 mg per day. The dose is increased to 3 mg per day, adding 0.6 mg at intervals of at least one week to improve gastrointestinal tolerance. If, with an increase in dose, the new dose is poorly tolerated by the patient for 2 weeks in a row, consideration should be given to discontinuing therapy. The use of the drug in a daily dose of more than 3 mg is not recommended. Patients with type 2 diabetes. The Saxend drug should not be used in combination with other EPP-EB receptor agonists when starting therapy with Saxend. development of hypoglycemia.
Side effects
Immune system disordersAnaphylactic reactions - Rarely Metabolic and Nutritional DisordersHypoglycemia - Often Dehydration - InfrequentlyMental DisordersInsomiousness - OftenNervous System DisordersHegirthfulness - OftenDisturbations of the HeartTachycardia - Infrequently, gastric disturbances - Heartbrokenness - Heartbeat, Heartbeat, Heartbeat, Heartbeat, Heartbrokenness - Frequently, , dyspepsia, gastritis, gastroesophageal reflux, upper abdominal pain, flatulence, belching, abdominal distension - Often Pancreatitis - Not astoNarusheniya of the liver and biliary puteyHolelitiaz - ChastoHoletsistit - NechastoNarusheniya of the skin and subcutaneous tkaneyKrapivnitsa - NechastoNarusheniya the kidneys and urinary puteyOstraya renal failure, renal function - RedkoObschie disorders and in place vvedeniyaReaktsii at the injection site, asthenia, fatigue - ChastoNedomoganie - Infrequently
Overdose
Symptoms: during clinical studies and the post-marketing period, cases of using the drug were reported in doses up to 40 times the average recommended dose (72 mg), which was accompanied by the development of severe nausea and vomiting. No cases of severe hypoglycemia were noted. All patients recovered completely without complications. Treatment: in case of an overdose of the drug Viktoz, appropriate symptomatic therapy is recommended.
Interaction with other drugs
Evaluation of drug interactions in vitro Liraglutide showed a very low capacity for drug pharmacokinetic interaction due to metabolism in the cytochrome P450 system, as well as binding to plasma proteins. Evaluation of drug interaction in vivo A slight delay in gastric emptying when using liraglutide may affect the absorption of concurrent oral dos drugs . Studies of drug interactions have not shown any clinically significant delay in the absorption of these drugs. Several patients treated with the drug had at least one episode of acute diarrhea. Diarrhea can affect the absorption of oral medications, which are used simultaneously with the drug. Paracetamol The single use of paracetamol in a dose of 1000 mg against the background of liraglutide does not cause a change in systemic exposure. Cmax of paracetamol in plasma decreased by 31%, and the average time to reach Cmax in plasma increased by 15 minutes. At the same time taking liraglutid and paracetamol dose adjustment of the latter is not required. Atorvastatin 40 mg at the dose of liraglutide does not cause a change in systemic exposure. Thus, while taking the drug Victoza dose adjustment of atorvastatin is not required. Cmax of atorvastatin in plasma decreased by 38%, and the average time to reach Cmax in plasma against the background of liraglutide increased from 1 to 3 h. Griseofulvin. One-time use of 500 mg at the dose of liraglutide does not cause a change in systemic exposure. Cmax of griseofulvin increased by 37%, while the average value of the time to reach Cmax in plasma did not change.Dose adjustment of griseofulvin and other drugs with low solubility and high permeability is not required. Digoxin A simultaneous single dose of digoxin at a dose of 1 mg and liraglutide showed a 16% decrease in the AUC of digoxin; Cmax of digoxin decreased by 31%. The mean time to reach Cmax of digoxin in plasma increased from 1 to 1.5 hours. Based on the results, the dose adjustment of digoxin against liraglutide is not required. C max of lisinopril decreased by 27%. The mean time to reach Cmax of lisinopril in plasma against the background of liraglutide intake increased from 6 to 8 hours. Oral contraceptives Cmax of ethinyl estradiol and levonorgestrel after their single use during treatment with liraglutide decreased by 12% and 13%, respectively. The use of both drugs together with liraglutid was accompanied by an increase in the time it took for the Cmax to reach these drugs by 1.5 hours. Liraglutide does not have a clinically significant effect on the systemic exposure of ethinyl estradiol and levonorgestrel in the body. Thus, the expected contraceptive effect of both drugs does not change during therapy with liraglutide. Warfarin and other coumarin derivatives No interaction studies were conducted. At the beginning of drug treatment in patients receiving warfarin or other coumarin derivatives, it is recommended to monitor the MNO more frequently. Patients with type 2 diabetes. Pharmaceutical incompatibility Substances added to the drug can cause degradation of liraglutide. The drug Victoza can not be mixed with other drugs, including with infusion solutions.
special instructions
Patients should be warned that they should take precautions to avoid the development of hypoglycemia while driving and working with machinery.