Treatment of acromegalic patients in whom the response to surgical treatment and / or radiotherapy was insufficient and in whom adequate treatment with somatostatin analogues did not normalize IGF-1 levels or did not tolerate such therapy.
Composition:
1 vial contains 10 mg or 15 mg of pegvisomant.
Action:
An analog of human growth hormone modified to act as a growth hormone receptor antagonist. It is highly selective for the GH receptor and does not cross-react with other cytokine receptors, including the prolactin receptor. Inhibition of growth hormone by pegvisomant leads to a decrease in insulin-like growth factor-1 (IGF-1) in the blood and other hormone-stimulating proteins such as: free IGF-1, acid-sensitive IGF-1 subunit (ALS) ) and insulin-like growth factor-3 binding protein (IGFBP-3). After subcutaneous administration, the pegvisoma is slowly absorbed, reaching Cmax after 33-77 h from the application. Bioavailability after administrations.c.. is 57%. Medium T0,5 pegvisomant is 74-172 h. The pharmacokinetics of pegvisomant are similar in healthy volunteers and in patients with acromegaly, however, it has been observed that patients with higher body weight have a higher clearance of pegvisomant and may require higher doses of the drug.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients.
Precautions:
The safety and efficacy of the preparation in children and in patients with impaired renal or hepatic function have not been established. Treatment with pegvisomant does not reduce the growth hormone secreting tumor size - all patients with pituitary tumor should remain under strict control during treatment to observe any tumor growth. Patients with co-morbid diabetes should be monitored as the dose of insulin or oral hypoglycaemic agents may need to be reduced during treatment. Patients with acromegaly should be advised that as a result of treatment with pegvisomant, fertility may potentially increase - it is recommended to use adequate contraception during treatment with the preparation. The drug should be discontinued if symptoms of liver dysfunction persist during treatment.
Pregnancy and lactation:
Do not use in pregnancy, except for absolute necessity. Do not use during breast-feeding.
Side effects:
Common: headache, dizziness, drowsiness, tremor, diarrhea, constipation, nausea, vomiting, abdominal fullness, indigestion, bloating, sweating, pruritus, rash, joint pain, muscle pain, peripheral edema, hypercholesterolemia, weight gain , hyperglycemia, feeling of hunger, hypertension, flu-like syndrome, fatigue, hematoma and bleeding at the injection site, local reactions at the injection site (including hypersensitivity reaction at the injection site), tissue hypertrophy at the injection site (eg lipohypertrophy), abnormal test results liver function (eg increased transaminase activity), unusual dreams, sleep disorders. Uncommon: thrombocytopenia, leukopenia, leukocytosis, bleeding tendency, hypoaesthesia, dysphoria, migraine, narcolepsy, visual disturbances, eye pain, Meniere's disease, shortness of breath, dry mouth, anal hemorrhagia, hypersecretion of the salivary glands, disorders on the part of the teeth, hematuria, proteinuria, polyuria, renal dysfunction, facial edema, dry skin, bruising, night sweats, arthritis, hypertriglyceridaemia, hypoglycaemia, lower limb edema, fever, weakness, altered well-being, healing disorders, peripheral edema , irritability, apathy, confusion, increased libido, panic attacks, short-term loss of memory. In 16.9% of patients receiving the preparation, the appearance of low titers of antibodies against growth hormone was observed; the clinical significance of the appearance of these antibodies has not been established.
Dosage:
Subcutaneously. Initially (under the supervision of a doctor) a loading dose of 80 mg should be given.Then 10 mg of the reconstituted solution in 1 ml of solvent (water for injections) once a day. Doses should be adjusted based on blood IGF-1 concentration, determining IGF-1 concentrations every 4-6 weeks and dose should be increased accordingly by 5 mg / day to maintain IGF-1 concentrations within the appropriate age range and achieve optimal therapeutic response . The maximum dose is 30 mg / day. Change the injection site every day to prevent lipohypertrophy.
(C)
