Tìm theo
Buserelin
Các tên gọi khác (4 ) :
  • (Des-Gly10,D-Ser(tBu)6,Pro-NHEt9)-LHRH
  • D-Ser(Tbu)6EA10LHRH
  • Etilamide
  • Tiloryth
Thuốc Gốc
Biotech
CAS: 57982-77-1
ATC: L02AE01
CTHH: C62H90N16O15
Buserelin is a synthetic peptide analog of the luteinizing hormone-releasing hormone (LHRH) agonist, which stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). It is used in prostate cancer treatment.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C62H90N16O15
Dược Lực Học : The substitution of glycine in position 6 by D-serine, and that of glycinamide in position 10 by ethylamide, leads to a nonapeptide with a greatly enhanced LHRH effect. The effects of buserelin on FSH and LH release are 20 to 170 times greater than those of LHRH. Buserelin also has a longer duration of action than natural LHRH. Investigations in healthy adult males and females have demonstrated that the increase in plasma LH and FSH levels persist for at least 7 hours and that a return to basal values requires about 24 hours. Clinical inhibition of gonadotropin release, and subsequent reduction of serum testosterone or estradiol to castration level, was found when large pharmacologic doses (50-500 mcg SC/day or 300-1200 mcg IN/day) were administered for periods greater than 1 to 3 months. Chronic administration of such doses of buserelin results in sustained inhibition of gonadotropin production, suppression of ovarian and testicular steroidogenesis and, ultimately, reduced circulating levels of gonadotropin and gonadal steroids. These effects form the basis for buserelin use in patients with hormone-dependent metastatic carcinoma of the prostate gland as well as in patients with endometriosis.
Cơ Chế Tác Dụng : Buserelin is a synthetic peptide analog of the luteinizing hormone-releasing hormone (LHRH) agonist, which stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). It is used in prostate cancer treatment. Buserelin stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). Buserelin desensitizes the GnRH receptor, reducing the amount of gonadotropin. In males, this results in a reduction in the synthesis and release of testosterone. In females, estrogen secretion is inhibited. While initially, there is a rise in FSH and LH levels, chronic administration of Buserelin results in a sustained suppression of these hormones.
Dược Động Học :
▧ Absorption :
Buserelin is water soluble and readily absorbed after subcutaneous injection (70% bioavailable). However, bioavailability after oral absorption. When administered correctly via the nasal route, it may be absorbed in the nasal mucosa to achieve sufficient plasma levels.
▧ Volume of Distribution :
Buserelin circulates in serum predominantly in intact active form. Preferred accumulation is preferentially in the liver and kidneys as well as in the anterior pituitary lobe, the biological target organ.
▧ Protein binding :
15%
▧ Metabolism :
It is metabolized and subsequently inactivated by peptidase (pyroglutamyl peptidase and chymotrypsin-like endopeptidase) in the liver and kidneys as well as in the gastrointestinal tract. In the pituitary gland, it is inactivated by membrane-located enzymes.
▧ Route of Elimination :
Buserelin and its inactive metabolites are excreted via the renal and biliary routes. In man it is excreted in urine at 50% in its intact form.
▧ Half Life :
The elimination half-life is approximately 50 to 80 minutes following intravenous administration, 80 minutes after subcutaneous administration and approximately 1 to 2 hours after intranasal administration.
Độc Tính : Buserelin may induce early, transient increase in serum testosterone or estradiol which can lead in the exacerbation of signs and symptoms of metastatic prostate cancer or endometriosis. Adverse reactions reported at more than 10% occurrence include headache, loss of libido in patients with prostate cancer, hot flashes, hypermenorrhea, decreased libido in prostate cancer and endometriosis, flatulence, impotence, vaginal dryness, back pain and nasal mucosa irritation.
Chỉ Định : Buserelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction.
Tương Tác Thuốc :
  • Capromab Avoid combination because luteinizing Hormone-Releasing Hormone Analogs may diminish the diagnostic effect of Indium 111 Capromab Pendetide.
  • Mifepristone Buserelin moderately contributes to Q-Tc prolongation. Combination must be avoided because mifepristone can further enhance that effect.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Cinnagen
    Sản phẩm biệt dược : Cinnafact
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Suprefact
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06719
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01831
Wikipedia
http://en.wikipedia.org/wiki/Buserelin
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