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Transcript
Drugs affecting reproductive system Drugs related to female hormones Estrogens Antiestrogens Progesterone and progestogens Antiprogestogens Female contraception drugs Drug related to male hormones Androgens Antiandrogens Anabolic steroids Male contraception drugs Estrogens 1. Pharmacological effects (1) Development of the female genital tract and of the female secondary sex characeteristics. (2) Maintenance of both proliferative and secretory phases of the uterine endometrium (4) Development of the breast and lactescence (5) Other actions: decreasing postmenopausal disturbances in sleep inhibiting the reabsorption of bone increasing aldosterone and causing water and Na+ retention decreasing LDL and increasing HDL levels in plasma increasing factor II, VII, IX, X and coagulation 2. Clinical uses (1) Postmenopausal syndrome(绝经期综合征): Postmenpausal hormone replacement therapy (HRT): prevention of osteoporosis; - Fractures of the spine, wrist, and hips decrease by 50-70% and spinal bone density increases by ~5% in women treated with estrogen within 3 years of the onset of menopause and for 5–10 years thereafter. treat vasomotor & CNS symptoms - hot flushes, vaginal dryness, urinary stress incontinence, chilly sensations, dizziness, fatigue, irritability, and sweating. prevention of cardiovascular disease -lowers LDL ,TG; raises HDL levels -endothelial vasodilatation properties , anti-inflammatory (2) Primary hypogonadism (卵巢功能不全): replacement vaginal atrophy, hypoestrogenism (3) Menstrual disorders amenorrhea , dysmenorrhea, and oligomenorrhea; severe dysfunctional uterine bleeding (4) Contraception (5) Others: suppress lactation after child birth advanced breast cancer (postmenopausal) and prostatic cancer -hormone-sensitive or hormone-receptor-positive cancers -hormone therapy, or anti-estrogen therapy (not to be confused with hormone replacement therapy) acne neuroprotection 3. Adverse effects (1) Oral administration: nausea,vomiting, diarrhea (2) Cardiovascular effects: risk of venous thromboembolisis plasma triglycerides hypertension, edema (3) Others: gallbladder disease risk of breast and endometrial carcinoma Clomifene 氯米芬 (克罗米酚) (1) Effects: Partial agonist/antagonist for estrogen receptor (2) Uses: anovulatory infertility (无排卵性不孕) menstrual disorders advance breast cancer functional amenorrhea (功能性闭经) amenorrhea galactorrhea syndrome (闭经溢乳综合征) (3) Adverse effects: Multiple ovulation with multiple pregnancy (多胎) ovary tumefaction (卵巢肿大) ovarian carcinoma following multiple exposure. Progestogens 1. Pharmacological effects (1) Converting the uterine epithelium from the proliferative to the secretory phase (2) Inhibiting LH secretion and ovulation (3) Development of galactophore (乳管) (4) Thermoregulation: increasing body temperature (5) Metabolism: antagonizing aldosterone, inducing hepatic drug-metabolizing enzyme 2. Clinical uses (1)Menstrual disorders secondary amenorrhage, exacerbated uterine bleeding, dysmenorrhea (痛经) and premenstrual syndrome, etc. artificially induce progestogen withdrawal bleeding. - Norethindrone acetate -medroxyprogesterone acetate (2) Cancers megestrol acetate solid malignancy, especially gastric and pancreatic cancer, improve appetite and reduce wasting. used in combination with dexamethasone. effects take several weeks to become apparent, but are relatively long-lived compared to those of corticosteroids. the only drugs to increase lean body mass. (3) Others endometriosis (子宫内膜异位症), hormone replacement therapy (HRT), premature pregnancy (流 产), etc. 3. Adverse effects GI reactions edema virilization (男性化) acne hirsulism (多毛) weight gain etc. Mifepristone 米非司酮 Clinical uses 1.Medical termination of intrauterine pregnancies of up to 49 days gestation 3. termination of pregnancies between 13 and 24 weeks gestation softening and dilatation of the cervix prior to mechanical cervical dilatation for pregnancy termination in combination with gemeprost 4.Labor induction in fetal death in utero. 5. emergency contraceptive used in smaller doses (10 mg) taken after sex but before ovulation→prevent ovulation and so prevent pregnancy. C. Contraceptive drugs For female: (1) Inhibition of ovulation (2) Prevention of fertilization (3) Inhibition of implantation (4) Use of spermicides in the vagina For male: (1) Direct inhibition of spermatomatogenesis (2) Indirect inhibition of spermatomatogenesis Steroid contraceptives for female Estrogens + progestogens 1. Pharmacological effects (1) Inhibition of ovulation (2) Inhibition of implantation (3) Increase in viscidity of cervical mucus(宫颈黏液) (4) Others: interfering uterus or oviducal motility 2. Clinical uses (1) Oral: short-acting contraceptives long-acting contraceptives postcoital (事后,探亲) contraceptives (2) long-acting injections (3) Slow-releasing preparations (4) Multiphasic preparations 3. Adverse effects (1) GI reactions (2) Menstrual disorders: breakthrough bleeding, amenorrhea (3) Increased coagulation: venous thromboembolism (4) Others: edema, depression, weight gain, acne, hirsutism, etc. 4. Drug interactions: Hepatic enzyme inducers attenuate the effect of contraceptive drugs Contraceptives for male Gossypol 棉酚 This compound destroys elements of the seminiferous epithelium (生精上皮) but does not alter the endocrine function of the testis. GI and hepatic reactions, hypopotassaemia, etc. Stimulatants of uterus Oxytocin 缩宫素(催产素) Pituitrin 垂体后叶素 Ergot alkaloid 麦角生物碱 Prostaglandins 前列腺素类 Relaxants of uterus Ritodrine 利托君 Terbutaline 特布他林 Salbuterol 沙丁胺醇 Magnesiun sulfate 硫酸镁 Oxytocin 缩宫素(催产素) Pharmacological effects Uterine contraction important for cervical dilation before birth and causes contractions during the second and third stages of labor. assist the uterus in clotting the placental attachment point postpartum- during the first few weeks of lactation. However, in knockout mice lacking the oxytocin receptor, reproductive behavior and parturition are normal. Clinical uses Small doses (2-5 U): rhythmic contraction; induction of labor Large doses (5-10 U): tonic contraction; postpartum hemorrhage relatively safe when used at recommended doses, and side effects are uncommon Cautions in induction of labor Ergot alkaloid 麦角生物碱 Pharmacological effects 1.Uterine smooth muscle stimulation Selectively and determined by the functional state of the uterus 2.Vessel-contracting effect Directly contract artery and venous vessels Damage vascular endothelial cells at high dose Lead to dry gangrene of the extremities after long term use 3.α-receptor blocking effect Reverse the BP-elevating effect of NA Used in uterus bleeding postpartum hemorrhage(产后出血) migraine(偏头痛) Adverse effects GI disturbances: diarrhea, nausea, and vomiting prolonged vasospasm Contraindications obstructive vascular; pregnancy Prostaglandins 前列腺素类 dinoprostone(地诺前列酮,PGE2) dinoprost(地诺前列素, ) sulprostone(硫前列酮) carboprost (卡前列素) Used in Abortion(流产): combined with mifepristone Facilitation of labor Adverse effects GI disturbances: nausea, vomiting and abdominal pain Contraindications bronchial asthma; glaucoma