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  • Title: [Progress in the area of drug development. 15].
    Author: Henkler G, Klotzbach M, Koch H, Müller W, Richter J.
    Journal: Pharmazie; 1982 Nov; 37(11):753-65. PubMed ID: 6131442.
    Abstract:
    Progress in new drug developments is discussed in relation to newly registered drugs and drugs in the animal and/or clinical research stage. Of central nervous system drugs new neuroleptics, antidepressants, tranquilizers, psychotropics, antiparkinson and anticonvulsant agents are discussed in terms of chemical structure, pharmacokinetics and toxicity. Likewise for anti-infective drugs such as antibiotics, antifungal, and antiparasitic agents. New synthetic antiinflammatory glucocorticoids are being developed and tested for toxicity and clinical effect. Estrogen and gestagen research continues but few new substances with more effective action than currently-used compounds have been found. Initial clinical testing of Tibolon shows it to prevent postmenopausal osteolysis and hot flashes. ST-1435 is still being tested as an implantable contraceptive. It causes amenorrhea and reduces plasma estradiol and progesterone. No progress is seen in research on nonhormonal substances with contraceptive action, except for prostaglandins although no new derivatives with high tissue selectivity for uterine smooth muscle, nor early applicable abortifacients, have been found. Metenprost is being studied as a self-administered abortifacient: in one study 98% of completed abortions were seen with 30-40% adverse effects (nausea, vomiting, fever). DL204-IT and L-11,204 are triazoloisoindole and triazoloisoquinolone derivatives which have been tested in various dosages and dosage forms on animals in various pregnancy stages. Optimum contraceptive action occurs in the early blastocyst stage. The plant extracts Zoapatanol and Montanol show dose-dependent inhibition of implantation in animal studies but the contraceptive action mechanism is not known. Oxendolone shows an unmistakable antiandrogenic effect. Action mechanism is assumed to be inhibition of the 5 alpha-reduction of testosterone. It has a long plasma half-life in rats (3.6 days). It has been clinically tested in Japan (weekly intramuscular injection of 200-400 mg) in prostatic hypertrophy. Longterm studies are not yet available.
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