Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C221H366N72O67S • xC2H4O2 where x averages 7.4 acetate counter ions per peptide molecule.
Phân tử khối
5135.9 Daltons (base free)
Điểm đẳng điện tích
10.54
Dược Lực Học :
Tesamorelin stimulates growth hormone secretion, and subsequently increases IGF-1 and IGFBP-3 levels.
Cơ Chế Tác Dụng :
Tesamorelin is a stabilized synthetic peptide analogue of the hypothalamic peptide, Growth Hormone Releasing Hormone (GHRH) indicated for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. Lipodystrophy is a metabolic condition characterized by insulin resistance, fat redistribution, and hyperlipidemia associated with antiretroviral therapy for HIV infection.
By acting on the pituitary cells in the brain, tesamorelin stimulates production and release of the endogenous hormone (hGRF). Tesamorelin therapy predisposes the patient to glucose intolerance and can also increase the risk of type 2 diabetes, so the drug is contraindicated in pregnancy.
Dược Động Học :
▧ Absorption :
The absolute bioavailability was determined to be less than 4% in healthy adult subjects following a 2 mg subcutaneous dose.
▧ Volume of Distribution :
9.4±3.1 L/kg in healthy subjects.
10.5±6.1 L/kg in HIV-infected patients.
▧ Metabolism :
No formal metabolism studies have been performed in humans.
▧ Half Life :
26 and 38 minutes in healthy subjects and HIV-infected patients, respectively.
Độc Tính :
Diarrhea, congestive heart failure, peripheral neuropathy, and loss of
mobility were the four serious adverse events reported during
the clinical studies
Chỉ Định :
Tesamorelin acetate is a synthetic analogue of human hypothalamic Growth Hormone Releasing Factor (hGRF) indicated to induce and maintain a reduction of excess abdominal fat in HIV-infected patients with lipodystrophy.
Liều Lượng & Cách Dùng :
Injection, powder, lyophilized, for solution - Subcutaneous - 2 mg
Tài Liệu Tham Khảo Thêm
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