Gestodene use and interaction

Gestodene purposes: as anti-progesterone drug
Pharmacology and Applications: To date, the strongest effect of progesterone and a minimum dose contraceptives. Its progestin norethindrone activity of L-A 2 times, no androgen and estrogen activity, there are anti-estrogen effect. Rapidly and completely absorbed orally, after 1 to 2 hours peak blood concentration, bioavailability 100 percent, eliminating t1/28 hours. Composite sheet consisting of clinical and ethinyl estradiol or three photos as short-acting oral contraceptives. Due to its contraceptive effect is reliable, cycle control, and on the favorable impact on lipid metabolism can improve hdl, so for the most ideal kind of oral contraceptives.

Interactions:
1, can be elevated plasma concentration of the drug Gestodene: eg atorvastatin, vitamin C and other drug metabolizing enzyme preparations such as fluconazole. Triacetyl oleandomycin used simultaneously with combined oral contraceptives may increase the incidence of intrahepatic cholestasis of risk.
2, can Gestodene contraceptive effect lowering drugs; antimicrobial agents, especially broad-spectrum antibiotics, drug metabolizing enzyme inducers such as rifampicin, phenobarbital, phenytoin, etc., should be avoided while taking.
3, Gestodene affect the efficacy of other drugs, it has weakened the role of anti-hypertensive drugs, anticoagulants and hypoglycemic agents; make enhanced efficacy of tricyclic antidepressants.
4, if used simultaneously with other drugs may occur drug interactions, please consult your physician or pharmacist.



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Mifepristone contraceptive efficacy

Mifepristone for the new anti-progesterone, no progesterone, estrogen, androgen and anti-estrogenic activity, with the progesterone receptor and glucocorticoid receptor binding, endometrial progesterone receptor affinity 5 times stronger than progesterone, pregnant animals for each period of pregnancy are abortion effect, can be used as non-surgical anti-pregnancy drugs. In the effective dose had no significant effect on cortisol levels. Because the drug can lead to insufficient uterine activity, anti-pregnancy when used alone incomplete abortion rate is higher, but it can increase the sensitivity of uterine prostaglandins.
Mifepristone also has a role in softening and dilatation of the cervix, it is clinically except for the anti-pregnancy, pregnancy ended after reminders, fetal death, abortion, but also for gynecological surgical procedures, such as the IUD placement and removal, take the inner membrane specimen, cervical dysplasia and cervical dilation and laser separation dilatation and curettage, The oral bioavailability of 70%. Plasma protein binding rate of 98% after 1.5 hours peak blood concentration, the role for 12 hours, eliminating the t1 / 2. Of 18 hours. Generally begin 30 hours after oral administration of vaginal bleeding, continued from 1 to 16 days. Endometrial progesterone receptor affinity five times stronger than progesterone, pregnant animals for each period of pregnancy are abortion effect, can be used as non-surgical anti-pregnancy drugs. IPPF medication is divided into two kinds of birth control pills and anti-pregnancy drug. Taking different doses of mifepristone may achieve different effects, under normal circumstances, each taking 10-25 mg of mifepristone for emergency contraception; taking 150 mg can be terminated within 49 days of pregnancy. Diagnosis of intrauterine pregnancy to the FDA. Menopause generally should not exceed 49 days, pregnancy shorter the better.


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Clinical application of Stanozolone

Stanozolone is a white crystalline powder, odorless. Almost insoluble in water, soluble in ethanol, chloroform, slightly soluble in acetone. Closed to avoid light preservation. Assimilation of this product is protein and male activity is weak, the differentiationindex of about 120. Clinical for the treatment of various relates tovascular diseases, such as Behr Chet syndrome (Behcet syn-drome), vascular phenomenon in hereditary angioedema,Raynaud's syndrome, superficial thrombophlebitis, venous ulcer.Can also be used for chronic bone wasting disease, osteoporosis,and growth hormone treatment in Turner syndrome (Turn-erssyndrome). Adverse reactions with nandrolone phenylpropionate.

Clinical application:

Female patient androgen or anabolic hormone, can cause malephenomenon, such as hirsutism, long beard, voice and tonedown, acne, generally in the withdrawal symptoms gradually subsided. Long-term application of this kind of hormones in malepatients, drug may be converted in the body to estrogen, and mayinhibit the secretion of gonadotropin and cause atrophy of testisand spermatogenesis suppression; due to the inhibition of endogenous testosterone, can lead to impotence; children's long-term application of androgen, can seriously affect the growth and development, such as accelerated epiphyseal closure effect instopping drug after still can last several months; application ofanabolic hormone, can lead to obesity. 17 effect of α - methyl testosterone on liver damage was more serious, the main interference intrahepatic bile capillary excretion function, make the cholestasis in the liver lobule central capillary bile duct damage caused by stasis of liver cells, bile, clinical manifestations of cholestatic hepatitis. Long-term use of androgens, may occur in liver cancer, prostate cancer and renal cell carcinoma. In addition, because of the sodium and water retention effect, can cause edema. Kidney disease and heart failure patients with prostate cancer are disabled, pregnant women

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New indications that the American Oxandrolone

The American College of chest physicians meeting two ofoxandrolone (oxandrolone) report aroused great concern from people, oxandrolone is anabolic steroid drugs for oral administration, increased body weight and restore muscle functionin metabolic diseases for. In acute burn patients requiring mechanical ventilation treatment (burn area accounts for 22 of the total area of the body: 27%) were randomized, placebo controlled trial of oxandrolone. Test the patient to take two times a dayoxandrolone, each 10mg, for 21 to 28 days. Results compared with the placebo group, visceral protein storage test groups wereincreased significantly, and have not found adverse reactions andabnormal liver function serious. The researchers think that need to be studied deeply to determine higher doses of oxandrolonewhether can accelerate recovery of critical burn patientanabolism. Oxandrolone also has the auxiliary treatment of chronic obstructive pulmonary disease (COPD) and unintendedweight loss (IML) potential. In a multicenter, double-blind trial, with both COPD and IML patients were randomized to receive placebo or oxandrolone treatment, daily 10 or 20mg, for 4 months. The preliminary results show that oxandrolone can improve the nutritional status of patients, increased patient body weight andlean body weight, its effect is dose related. It has good toleranceto the drug, but in some cases caused elevated liver enzyme levels, therefore discontinued therapy for these patients.


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Prasterone Enanthate Profile

[Chinese name]: Pula DHEA enanthate
[Chinese alias]: Dehydroepiandrosterone enanthate; DHEA enanthate
[English name]: Prasterone Enanthate
[English Name]: 3b-Hydroxyandrost-5-en-17-one heptanoate
[CAS Number] :23983 -43-9
[Properties]: White crystalline powder
[Specification: 99%, pharmaceutical grade
[Packing]: 5kg / listen
[Molecular Formula]: C26H40O3
[Molecular Weight]: 400.59
[Use]: Pharmaceutical intermediates and APIs



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Exemestane of Toxicology

Toxicology：
With Exemestane single dose toxicity: mice single oral dosages up to 3200mg/kg (according to body surface area, approximately 640 times the recommended clinical dose) when the death occurred. Single dose in rats and dogs, respectively 5000mg/kg and 3000mg/kg (according to body surface area, were approximately 2000 times the recommended clinical dose and 4,000 times), the animals appear dead. Mice and dogs single dose 400mg/kg respectively and 3000mg/kg (according to body surface area, were approximately 80 times the recommended clinical dose and 4,000 times), the animals convulsions.
Clinical studies, a single healthy person this product dosages up to 800mg/kg and advanced breast cancer at doses up to 600mg administered continuously at 12 weeks, have shown good tolerability.
Reproductive toxicity: 14 days before mating to gestation 15-20 days, rats were given the product, administered 21 days of lactation continues, the dose of 4mg/kg / day (according to body surface area, equivalent to the human clinical recommended dose is 1.5 fold) occurs when the placenta weight increase; doses greater than or equal to 20mg/kg / day occurs when pregnancy prolongation, abnormal or difficult childbirth, and also observed increased fetal absorption, reducing the number of live births, fetal weight reduction, delayed ossification . Gestation period of organogenesis in rats administered doses less than or equal to 810mg/kg (according to body surface area, approximately 320 times the recommended clinical dose) when no obvious teratogenic effects. Rabbits organogenesis dose 90mg/kg / day (according to body surface area, which is about the recommended human clinical dose used 70 times) occurs when the placenta weight reduction; dose of 270mg/kg / day, a miscarriage, the absorption fetal growth and fetal rabbit weight loss; doses less than or equal to 270mg/kg / day (according to body surface area, approximately 210 times the recommended clinical dose), the rabbit malformation rate has not increased. There is no effect of this product on pregnant women in clinical research data, if the pregnancy using this service, you should tell the patient the product potentially harmful to the fetus and potential risk of miscarriage.
63 days prior to mating and during caged together, male rats administered 500mg/kg / day (according to body surface area, approximately 200 times the clinically recommended amount), the administration can not mate with the female fertility in rats is reduced. This product is a dose of 20mg/kg / day (according to body surface area, the equivalent of one 8 times the recommended clinical dose) when female rats fertility parameters (such as ovarian function, mating behavior, conception rate) had no effect, but makes The average litter size decreased. In addition, the general toxicity studies, according to body surface area, human clinical dose of 3-20 times the recommended dose, mice, rats and dogs have varying degrees of ovarian changes, including hyperplasia, increased the number of ovarian cysts and reduce the number of corpus luteum.
Rats were orally administered radiolabeled 14C-exemestane 1mg/kg, found it through the placenta, 15 minutes after administration appears in breast milk with radioactivity exemestane, the dose, a single to 24 hours after treatment, the product and its metabolites in the maternal and fetal blood concentration considerably. Jhihben whether the product is not through human milk secretion. Because many drugs can be secreted in milk, therefore breast-feeding women should be careful.
Genetic Toxicity: Ames test and in V79 Chinese hamster lung cell test showed no mutagenic effect. In vitro without metabolic activation in the case of human lymphocytes exhibit mutagenic effects, but mouse micronucleus test were negative. This product does not increase the rat hepatocyte unscheduled DNA synthesis procedures.
Carcinogenicity: No carcinogenic effects of this product research data.



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The Testosterone Undecanoate Products

Principle introduced Testosterone Undecanoate
Method name: testosterone undecanoate API - Determination of testosterone undecanoate - spectrophotometry
Application: This method of spectrophotometric determination of testosterone undecanoate drug substance testosterone undecanoate content.
This method is suitable for testosterone undecanoate API.
Principle of the method: the test sample for the test solution add ethanol made, set the UV-visible spectrophotometer at 240nm wavelength absorbance, calculate its content.
Adverse reactions:
In androgen therapy has been found following adverse reactions: prepubertal boys: precocious puberty, increased frequency of erections, penis enlargement and early closure of the epiphyseal bone. Man: priapism and other signs of excessive sexual stimulation, long-term high-dose use may cause decreased sperm, ejaculate volume decreased. All patients: older men urination problems; Shuinazhuliu.
Note:
1 serious adverse reactions, they should immediately stop treatment until the symptoms disappear, and then re-start from a lower dose.
2 Patients who have heart failure (including asymptomatic), renal failure, prostatic hypertrophy, hypertension, epilepsy or trigeminal neuralgia (or have a history of these diseases) caution, should be closely observed, because androgens may cause water and sodium retention.
3 prepubertal boys should be used with caution in order to avoid early epiphyseal closure or precocious puberty.
4 There is a tendency to edema kidney disease, heart disease patients with caution.



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