[Tibolone].

La tibolone.

Publisher: Elsevier Masson Country of Publication: France NLM ID: 8302490 Publication Model: Print Cited Medium: Print ISSN: 0755-4982 (Print) Linking ISSN: 07554982 NLM ISO Abbreviation: Presse Med Subsets: MEDLINE

Publication: <2012- > : Paris : Elsevier Masson
Original Publication: Paris ; New York : Masson, [c1983-

Estrogen Replacement Therapy*; Estradiol/*analogs & derivatives ; Estradiol/*therapeutic use ; Estrogen Receptor Modulators/*therapeutic use ; Norethindrone/*analogs & derivatives ; Norpregnenes/*therapeutic use ; Osteoporosis, Postmenopausal/*prevention & control; Adult ; Aged ; Animals ; Blood Coagulation ; Breast/drug effects ; Cardiovascular Diseases/prevention & control ; Controlled Clinical Trials as Topic ; Double-Blind Method ; Endometrium/drug effects ; Estradiol/administration & dosage ; Estradiol/adverse effects ; Estradiol/pharmacology ; Estrogen Receptor Modulators/administration & dosage ; Estrogen Receptor Modulators/adverse effects ; Estrogen Receptor Modulators/pharmacology ; Estrogens, Conjugated (USP)/administration & dosage ; Estrogens, Conjugated (USP)/adverse effects ; Estrogens, Conjugated (USP)/pharmacology ; Estrogens, Conjugated (USP)/therapeutic use ; Female ; Follow-Up Studies ; Humans ; Hysterectomy ; Lipid Metabolism ; Lipids/blood ; Medrogestone/administration & dosage ; Medrogestone/adverse effects ; Medrogestone/pharmacology ; Medrogestone/therapeutic use ; Menopause ; Middle Aged ; Norethindrone/administration & dosage ; Norethindrone/pharmacology ; Norethindrone/therapeutic use ; Norethindrone Acetate ; Norpregnenes/administration & dosage ; Norpregnenes/adverse effects ; Norpregnenes/pharmacology ; Ovariectomy ; Placebos ; Postmenopause ; Progesterone Congeners/administration & dosage ; Progesterone Congeners/adverse effects ; Progesterone Congeners/pharmacology ; Progesterone Congeners/therapeutic use ; Prospective Studies ; Rabbits ; Rats ; Risk Factors ; Surveys and Questionnaires ; Time Factors

INDIRECT MECHANISM OF ACTION: Tibolone (OD 14) is the precursor of its active principles that are its metabolites: 3 alpha and 3 beta hydroxylated derivatives. In vivo, the latter behave like estrogens. Certain tissues (liver, endometrium) may metabolize the 3 beta ol derivative into the delta 4 isomer with progestagenic and androgenic activity. The metabolism of the product in other tissues such as the breast and brain is unknown.
Activity: At the dose of 2.5 mg/day, the product expresses an estrogen activity equivalent to that observed with classical doses of estrogens in the brain, genito-urinary tract, vascular endothelium and bone. In the brain and muscle, it also has a slightly androgenic effect and in the breast an antiestrogenic effect. ON METABOLIC LEVEL: The product acts like a minor androgen (lowering triglycerides and HDL cholesterol without interfering in the cholesterol cell flow) and it stimulates fibrinolysis. ON CLINICAL LEVEL: Tibolone treats the symptoms of estrogen privation and protects against bone loss, without inducing bleeding or mastodynia. There is a lack of large epidemiological studies on prevention of fracture risks, cardiovascular effects and breast. Tolerance in the population studied was excellent (healthy population). However, tolerance remains to be assessed in particular sub-groups (populations at risk of certains pathologies).

29

0 (Estrogen Receptor Modulators)
0 (Estrogens, Conjugated (USP))
0 (Lipids)
0 (Norpregnenes)
0 (Placebos)
0 (Progesterone Congeners)
077DN93G5B (Medrogestone)
4TI98Z838E (Estradiol)
9S44LIC7OJ (Norethindrone Acetate)
FF9X0205V2 (tibolone)
T18F433X4S (Norethindrone)

Date Created: 20021003 Date Completed: 20021011 Latest Revision: 20220330

20250114

12355994