Cottonpol tablets are an effective emergency contraceptive for men. They mainly inhibit the formation and activity of sperm. The main effect is in the spermatogenic epithelial cells of the male testicles. They are more sensitive in sperm cells and spermatocytes, which can cause abnormal sperm death and eventually even azoospermia. In clinical medicine, after men take them for 4 months, they will have very low sperm count and even dead sperm, thus achieving the actual effect of contraception. However, once the medication is stopped, the testicles will still produce sperm, and the sperm will transform into perfect sperm again, and the man will regain his fertility. Therefore, taking cotton phenol tablets orally is not a very good sterilization solution, and it is best to consider vasectomy. 1. Pharmacology Gossypol acetic acid has an inhibitory effect on steroid hormone protein kinases in the uterus, ovaries, uterine wall and myometrium, thereby significantly softening the uterine wall and myometrium and reducing menstrual volume. High concentrations of gossypol can interact with enzymes or functional proteins related to cell growth, causing cell necrosis, but it is not easy to induce malignant hyperplasia of somatic cells. Gossypol acetic acid inhibits the co-transport system of the thick ascending limb of the kidney's functional loop of Henle (Na--K--Cl-), reducing the decomposition and metabolism of potassium ions, calcium ions and sulfates, leading to renal potassium excretion. 2. Toxicology In 11 normal subjects who took standard doses of gossypol for 30-48 months, gossypol had no significant effect on the number of nucleolar tissue regions or the distribution of proximal centromeres in somatic cells. Gossypol did not induce chromosomal aberrations at clinically relevant doses or concentrations. Thirty women took gossypol for 6 months to treat endometriosis. There was no significant difference in the single exchange of sister chromosomes in reticulocytes before and after taking the medicine or compared with the control experiment. The experiment showed that the squamous epithelial cells and glandular cells of the rat uterine wall were damaged to varying degrees, but it had no toxic effects on the rat's internal organs, and the ultrastructural changes caused by the damaged cells of the rat uterine wall were mostly reversible. Cottonpol also had little effect on the production of uterine ovaries and the value of metabolic progesterone. Ten rats at 7 days of gestation (2 days after fertilization) were injected intrauterine with glacial acetic acid gossypol to completely prevent early pregnancy. The rats were able to give birth to offspring again, some of which prevented the birth rate after early pregnancy, and their grandchildren showed no significant differences in the chromosomal aberration rate of bone marrow cells and the micronucleus rate of fetal liver when compared with the control experiment. Pharmacokinetics of Gossypol Acetate Tablets When rats were orally administered 740KBq (20μCi)/7.5mg/rat of 14C-gossypol aqueous solution, it was observed that the time for half of the radioactive substances to disappear from the animals' bodies was 60 hours. After 9 days, the amount of radioactive substances excreted from the animals' bodies was 97.24% of the dose taken in, indicating that gossypol is slowly excreted from the body and may accumulate in the body if the drug is continuously administered. When rats were orally administered 1250g of cottonpol suspension, the largest distribution in the body was in the liver, followed by the spleen, lungs, kidneys, heart, blood and body fat. No detection was found in the brain, indicating the existence of a blood-brain barrier. It is mainly excreted from the body in the form of excrement. |
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