Exenatide (Exenatidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Hypoglycemic synthetic and other agents

Included in the formulation
  • Baeta®
    solution PC 
    AstraZeneca UK Ltd     United Kingdom
  • Baeta® Long
    powder PC 
    AstraZeneca UK Ltd     United Kingdom
    • АТХ:

    A.10.B.X.04   Exenatide

    Pharmacodynamics:

    Pharmacological effects: glucose-dependent hypoglycemic; slowing the evacuation of food from the stomach; decreased appetite; reduction of glucagon effects; the severity of the effects of hyperglycemia after eating.

    The functional analogue of human incretin - glucagon-like peptide-1: an increase in glucose-dependent insulin secretion and the manifestation of other effects caused by hyperglycemia. Increased insulin secretion only in the presence of glucose. Effect on the effects of glucagon in hyperglycemia without affecting its release.

    Pharmacokinetics:

    After subcutaneous administration of exenatide in a dose of 10 mcg in patients with type 2 diabetes mellitus exenatide quickly absorbed. Maximum concentration is achieved after 2.1 hours. The volume of exenatide distribution after subcutaneous administration is 28.3 liters.

    Exenatide is mainly excreted by glomerular filtration followed by proteolytic decay. The clearance of exenatide is 9.1 l / h. Final half-life is 2.4 hours. These pharmacokinetic characteristics of exenatide are dose independent.The measured concentrations of exenatide are determined approximately 10 hours after dose administration.

    Indications:

    Type 2 diabetes mellitus is used as monotherapy in addition to diet and exercise to achieve adequate glycemic control, as an additional therapy for metformin, a sulfonylurea derivative, thiazolidinedione, a combination of metformin and a sulfonylurea derivative, or metformin and thiazoldinedione in the absence of adequate glycemic control.

    ICD-10

    IV.E10-E14.E11   Non-insulin-dependent diabetes mellitus

    Contraindications:

    Diabetes mellitus type 1 or the presence of diabetic ketoacidosis; severe renal insufficiency (creatinine clearance <30 mL / min); presence of severe diseases of the gastrointestinal tract with concomitant gastroparesis; pregnancy; lactation period (breastfeeding); children and adolescents under 18; increased sensitivity to exenatide.

    Carefully:

    In the postmarketing period, rare cases of development of acute pancreatitis in patients taking exenatide. Patients should be informed that prolonged severe abdominal pain,which can be accompanied by vomiting - a sign of pancreatitis. If there is a suspicion of developing pancreatitis, you should cancel exenatide or other potentially suspected drugs, to conduct confirmatory tests and begin appropriate treatment. If the diagnosis of pancreatitis is confirmed, the resumption of treatment with exenatide is not recommended in the future.

    During the postmarketing period, rare cases of renal impairment were noted, including increased serum creatinine, worsening of chronic renal insufficiency, acute renal failure, sometimes requiring hemodialysis. Some of these cases were observed in patients who took one or more drugs with a known effect on renal function and / or in patients who had nausea, vomiting and / or diarrhea with / without hydration, while using medications, including ACE inhibitors, NSAIDs, diuretics. Disturbance of renal function was reversible with maintenance therapy and withdrawal of drugs potentially affecting renal function, including exenatide. In preclinical and clinical studies exenatide did not show a direct nephrotoxic effect.

    Pregnancy and lactation:

    Action category for the fetus by FDA - C.

    Contraindicated in pregnancy and during breastfeeding.

    Dosing and Administration:

    Enter subcutaneously into the thigh, abdomen or forearm.

    The initial dose is 5 μg, which is administered 2 times a day at any time during the 60-minute period before the morning and evening meals. Do not administer after eating. 1 month after the start of treatment, the dose of the drug can be increased to 10 μg 2 times a day.

    When co-administered with metformin, thiazolidinedione or a combination of these drugs, the initial dose of metformin and / or thiazolidinedione can not be changed. In the case of combination with sulfonylurea derivatives, a dose reduction of the sulfonylurea derivative may be required to reduce the risk of hypoglycemia.

    Side effects:

    From the side digestive system: with monotherapy - nausea, vomiting, diarrhea, dyspepsia, decreased appetite; with combined therapy - nausea, vomiting, diarrhea, decreased appetite, dyspepsia, gastroesophageal reflux, abdominal pain, bloating, belching, constipation, flawed sensation, flatulence, acute pancreatitis. Perhaps - belching, constipation, flatulence; rarely acute pancreatitis.

    From the side CNS: with monotherapy - dizziness; with combined therapy - dizziness, headache, drowsiness. Maybe dysgeusia, drowsiness.

    From the side endocrine system: hypoglycemia is possible; with combined therapy - hypoglycemia (in combination with the sulfonylurea derivative).

    From the side metabolism: with combined therapy - hyperhidrosis, dehydration (associated with nausea, vomiting and / or diarrhea).

    From the side urinary system: with combined therapy - renal dysfunction, including acute renal failure, aggravation of chronic renal failure, increased serum creatinine content.

    Allergic reactions: with combined therapy - angioedema, anaphylactic reaction.

    Dermatological reactions: possibly - maculopapular rash, itching, hives, angioedema, alopecia.

    Local reactions: itching at the injection site, rash, redness at the injection site.

    Other: with combined therapy - trembling, weakness. Perhaps - an increase in the international normalized relationship (when combined with warfarin), in some cases accompanied by the development of bleeding).

    Overdose:

    Symptoms: severe nausea and vomiting, as well as the rapid development of hypoglycemia (with a dose of 10 times the maximum recommended).

    Treatment: Perform symptomatic therapy, including parenteral administration of glucose in the case of severe hypoglycemia.

    Interaction:

    Means taken orally - slowing the absorption of drugs due to delayed evacuation of the stomach, take at least 1 hour before the introduction of exenatide.

    Warfarin - increased risk of bleeding.

    Digoxin, lisinopril, lovastatin - an increase in plasma concentrations of these agents.

    Special instructions:

    Do not enter exenatide after eating. Do not administer intravenously or intramuscularly.

    In view of the potential immunogenicity of drugs containing proteins and peptides against the background of exenatide therapy, antibodies to the active substance may be produced. In most patients who have seen the production of such antibodies, their titer decreased as the therapy continued and remained low for 82 weeks. The presence of antibodies does not affect the frequency and types of reported side effects.

    Exenatide is able to cause a delay in the emptying of the stomach.Therefore, simultaneous use with drugs for the development of which requires rapid absorption from the digestive tract is not recommended.

    Patients should be informed that exenatide treatment may lead to a decrease in appetite and / or body weight and that, because of these effects, there is no need to change the dosage regimen.

    On the background of exenatide therapy, antibodies to the drug may appear.

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