Steroid contraceptive

Vaginal Rings. Vaginal epithelium is readily permeable to contraceptive steroids. Since the vascular drainage of the vagina bypasses the Hver, this route of adrninistration potentially permits utilisation of dmgs that have low oral activity. 

A. T. Gregoire and R. P. Blye, eds.. Contraceptive Steroids Pharmacology and Safety, Plenum Press, New York, 1986. 

E. Michal, ed.. Safety Requirements for Contraceptive Steroids, Cambridge University Press, Cambridge, 1980. 

Implantable controlled release dmg deUvery systems, including Norplant and other contraceptive steroids ia siUcone-based devices, have been reviewed (91,92). 

J. A. Edgren, in Pharmacology of the Contraceptive Steroids, ed. J. W. Goldzieher, Raven Press,... 

Contraceptive, steroid, 1083 Cope rearrangement, 1193-1194 suprafacial geometry of, 1194 Copolymer, 1210-1212 block. 1212 graft. 1212 table of. 1211... 

Controlled release fiber systems based on aliphatic polyesters were investigated by Dunn and Lewis (51-54). The feasibility of hollow fibers spun from poly (L-lactide) and containing the contraceptive steroid levonorgestrel has been demonstrated (55). 

A. G., and Perkins, B. H., Biodegradable fibers for the controlled release of tetracycline in treatment of peridontal disease, Proc. Int. Symp. Control. Rel. Bioact. Mater., 14, 289, 1987. Dunn, R. L., Lewis, D. H., and Beck, L. R., Fibrous polymer for the delivery of contraceptive steroids to the female reproductive tract, in Controlled Release of Pesticides and Pharmaceuticals (D. H. Lewis, ed.). Plenum Press, New York, 1981, pp. 125-146. 

J. B., Polylactic acid as a biodegradable carrier for contraceptive steroids. Contraception, 8, 227, 1973. 

Lewis, D. H. and Tice, T. R., Polymeric considerations in the design of microencapsulated contraceptive steroids, in Long-Acting Contraceptive DeUvery Systems (G. I. Zatuchni, ed.). Harper and Row, Philadelphia, 1983, pp. 77-95. 

Heller, J., Penhale, D. W. H., Fritzinger, B. K., Rose, J. E., and Helwing, R. F., Controlled release of contraceptive steroids from biodegradable poly(ortho esters), Contracept. Deliv. Syst., 4, 43-53, 1983. 

J. E., Synthesis and release of contraceptive steroids from bio-erodible poly(ortho esters), in Polymers in Medicine (E. Chielini and P. Giusti, eds.). Plenum Publishing, New York, 1983, pp. 169-178. 

Sustained- and controlled-release devices for drug delivery in the vaginal and uterine areas are most often for the delivery of contraceptive steroid hormones. The advantages in administration by this route—prolonged release, minimal systemic side effects, and an increase in bioavailability—allow for less total drug than with an oral dose. First-pass metabolism that inactivates many steroid hormones can be avoided [183,184],... 

This system is the only osmotic system developed commercially at this time that is suitable for the oral administration of insoluble drugs to humans. It has been utilized in the development of several other drugs including isradipine, doxazosin, diltiazem, contraceptive steroids, glipizide, and verapamil [48-53], The system has also been utilized to codeliver the free bases of compounds normally administered as water-soluble salts such as pseudoephedrine and bromo-pheniramine [54], The latter system includes both a loading dose and a controlled release dose and is intended for applications in the over-the-counter market. 

Urinary D-glucaric acid levels have been shown to be a sensitive indicator of microsomal enzyme induction in workers exposed to chlordecone (Guzelian 1985). However, other substances such as barbiturates, phenytoin, chlorbutanol, aminopyrine, phenylbutazone, and contraceptive steroids as well as other organochlorinated pesticides also cause microsomal enzyme induction and cause changes in urinary D-glucaric acid (Morgan and Roan 1974). 

A. Hussain, S. Hirai, and R. Bawarshi. Nasal absorption of natural contraceptive steroids in rats-progesterone absorption. J Pharm Sci 70 466 167 (1981). 

Since the development of the oral contraceptive steroids in the 1960s, various steroids and procedures have been used. Synthetic steroids are now used since their half-hves in the body are longer than the natural steroids. Combined oestrogen-progesterone contraception involves taking one piU each day which contains a synthetic progestogen plus an oestrogen. The pill is taken for 21 dyas, with a break for... 

Abernethy DR, Greenblatt DJ, Ochs HR, et al Lorazepam and oxazepam kinetics in women on low-dose oral contraceptives. Clin Pharmacol Ther 33 628-632, 1983 Abernethy DR, Greenblatt DJ, Shader Rl Imipramine disposition in users of oral contraceptive steroids. Clin Pharmacol Ther 35 792-797, 1984 Abou-Saleh MT Lithium and bipolar illness, in Long-Term Treatment of Depression. Edited by Montgomery SA, Rouillon F. Chichester, England, Wiley, 1992, pp 113-138... 

Patwardhan RV, Mitchell MC, Johnson RF, et al Differential effects of oral contraceptive steroids on the metabolism of benzodiazepines. Hepatology 3(2) 248-253, 1983... 

ALESSE 28 (levonorgestrel and ethinyl estradiol tablets) Wyeth April 2004 labeling Precautions. Drug Interactions Herbal products containing St. John s wort H. perforatum) may induce hepatic enzymes (CYP) and P-gp transporter and may reduce the effectiveness of contraceptive steroids. This may also result in breakthrough bleeding ... 

Frequently, the constant release of a drug from pharmaceutical dosage forms enables one to obtain a suitable pharmacological and therapeutic response. However, for therapy of certain pathologies, i.e. some heart and rheumatic diseases, or in the utilization of some drags such as contraceptive steroids and antibiotics, it would be more useful to obtain different plasma levels of the active principle at different times related to painful symptoms or circadian rhythms, etc. In these cases the desired therapeutic results can usually be obtained with frequent administration of conventional dosage forms which lead to a prompt absorption of the active principle. This kind of drag treatment is often compromised by a lack of full compliance by the patient. Until now there have been few systems that allow the release of the active principle in successive pulses at precise and well-controlled time periods [11,12]. 

Both benign and malignant liver tumors may arise from exposure to hepatotoxins and can be derived from various cell types. Thus, adenomas have been associated with the use of contraceptive steroids and exposure to aflatoxin Bi, and dimethylnitrosamine can produce hepatocellular carcinomas, whereas vinyl chloride causes hemangiosarcomas derived from the vasculature (see chap. 7). 

Interactions in which other drugs influence the effects of contraceptive steroids... 

Antacids apparently do not affect the systemic availability of oral contraceptives, but since magnesium-containing antacids can cause diarrhea, they might reduce absorption of contraceptive steroids. 

There are sporadic, but well documented, reports of women using oral contraceptive steroids who became pregnant while taking a variety of antibiotics (337). However, there is much interindividual variation, which... 

Oral contraceptives reduce the clearance of imipramine, probably by reducing hepatic oxidation, and thus increase its half-life. Hydroxylation of amitriptyline is inhibited by contraceptive steroids. The clinical significance is uncertain, but there is at least anecdotal evidence of an increase in antidepressant adverse effects (360). Caution should be exercised when tricyclic antidepressants are used long term in women taking oral contraceptives. 

Beller FK. Cardiovascular system coagulation, thrombosis, and contraceptive steroids is there a link In Goldzieher JW, Fotherby K, editors. Pharmacology of the Contraceptive Steroids. New York Raven Press, 1994 309. 

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