Hormones and Endocrine Drugs

Norethisterone, a derivative of 19 demethyltestosterone, is an oral progesterone. Its progesterone activity is 4 times higher than that of progesterone, and its estrogen and androgen activities are weak. It can inhibit the secretion of hypothalamic luteinizing releasing hormone (LHRH). By stimulating the anterior pituitary, it can reduce the sensitivity of the body to LHRH, so as to block the release of gonadotropin and inhibit ovulation. After oral administration of this product for 0.5 ~ 4 hours, the blood concentration can reach the peak, and the half-life is 5 ~ 14 hours. Most of the metabolites are discharged from the body through the kidney.

Epalrestat is a carboxylic acid derivative and a noncompetitive and reversible aldose reductase inhibitor used for the treatment of diabetic neuropathy, which is one of the most common long-term complications in patients with diabetes mellitus. It reduces the accumulation of intracellular sorbitol which is believed to be the cause of diabetic neuropathy, retinopathy and nephropathy It is well tolerated, with the most commonly reported adverse effects being gastrointestinal issues such as nausea and vomiting, as well as increases in certain liver enzymes. Chemically, epalrestat is unusual in that it is a drug that contains a rhodanine group. Aldose reductase is the key enzyme in the polyol pathway whose enhanced activity is the basis of diabetic neuropathy. Aldose reductase inhibitors (ARI) target this enzyme. Out of the many ARIs developed, ranirestat and fidarestat are in the trial stage. Others have been discarded due to unacceptable adverse effects or weak efficacy. Epalrestat is the only ARI commercially available. It is easily absorbed into the neural tissue and inhibits the enzyme with minimum side effects.

The treatment of 2 adults with diabetes mellitus who had failed to achieve adequate glycemic control with the combination of etamline and glycemic control improved glycemic control.

Eplerenone, a new selective aldosterone receptor antagonist, was approved by the State Food and Drug Administration for clinical application in 2002. It has a stronger antagonistic effect on aldosterone than spironolactone, and has a very low affinity for androgen and progesterone receptors. It has a definite curative effect on the treatment of high blood pressure, heart failure and myocardial infarction with less adverse reactions and good tolerance, It is a good substitute for spironolactone. For severe hypertension which can not be controlled by combination of antihypertensive drugs, eplerenone can significantly reduce blood pressure, especially systolic blood pressure. It is closely related to angiotensin converting enzyme inhibitor (ACEI) and β Receptor blockers can improve the quality of life and reduce mortality in patients with severe heart failure and myocardial infarction.

Medicinal efficacy: improving and controlling blood sugar is the latest treatment for type II diabetes.