Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0042109 (urticaria)
 6,569 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

This comprehensive review of transdermal delivery systems for estrogens and progestins covers skin structure and absorption of chemical agents by diffusion and partition, permeability and use of enhancers to speed absorption, choices of drugs for transdermal contraceptives, animal and clinical work with estradiol, ethinyl estradiol and levonorgestrel, use of pro-drugs and derivatives, types of transderm delivery systems, metabolism of these drugs by skin and skin flora, and cutaneous side effects, all illustrated graphically and mathematically. Drug absorption entails diffusion through the primarily and mathematically. Drug absorption entails diffusion through the primarily lipophilic stratum corneum, and the hydrophilic epidermis: transport between these layers is often the rate-limiting step. For many drugs, permeability enhancers such as dimethyl sulfoxide, ethanol and ethyl acetate are needed. Good drug candidates for transdermal application must be potent in low doses, have short half-lives, not elicit an allergic response nor be extensively metabolized in skin. The permeability of levonorgestrel has been increased by using esters, and "pro-drugs" which are compounds that increase polarity, but are degraded to the active drug by skin tissue. The estrogens are subject to a minor degree of oxidation, and no significant degradation by skin microbes. There are 3 types of transdermal systems: the membrane, matrix and drug reservoir types. The Estraderm brand system for estradiol is a membrane-moderated design with ethanol as the chemical enhancer. Skin penetration is the rate-limiting step. Levonorgestrel as been tested with ethyl acetate and ethanol as penetration enhancers in rats, rabbits, and in a Phase I trial. The development of a transderm system for a combination of estrogen and progestin is a complex problem because 2 different enhancers must be used. Most transdermal systems are mild skin irritants, but incidence of contact allergy or urticaria are rare, with no cases yet reported from use of Estraderm. Transdermal application of contraceptive steroids is expected to be available eventually.
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PMID:Transdermal delivery of contraceptives. 227 99

Fertility control by cyclic norethindrone (Norlutin), 17 alpha-ethinyl 19-nortestosterone, plus .06 mg 3-methoxy ethinyl estradiol (Ortho-Novum) was studied in 364 women over a period of 32 months for a total of 6062 cycles. No patient who followed the instructions became pregnant. 37 patients stopped the medication for various reasons. The interval between stopping medication and becoming pregnant averaged 1.6 months. 13 of these pregnancies occurred after 11-15 cycles of treatment. Children born to these mothers were normal with no virilization observed. Findings from all Papanicolaou smears and cervical biopsies were normal. The desirable effects of diminishing the menstrual flow, reducing dysmenorrhea and regulating the menstrual cycle, plus the all-important one of contraception, far outweighed minimal and infrequent undesirable side effects (in order of frequence: chloasma, hot flashes, headache, nausea, acne, abdominal pain, dizziness and urticaria). In only 4.8% of the total 6062 cycles was some complaint made.
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PMID:Long-term administration of norethindrone in fertility control. 1227 4

Autoimmune progesterone dermatitis is a rare clinical condition in which patients display hypersensitivity to endogenous progesterone. It manifests as a cyclical cutaneous eruption that flares during the luteal phase of the menstrual cycle, when progesterone levels peak, and resolves partially or completely a few days after menses. Its cutaneous manifestations are variable and include urticaria, eczematous eruptions, vesiculopustular eruptions, fixed drug eruptions, stomatitis, erythema multiforme, and anaphylaxis. Autoimmune progesterone dermatitis has been diagnosed previously with intradermal skin testing or intramuscular progesterone challenge. Treatment of progesterone hypersensitivity generally consists of ovulation inhibition with pharmaceutical agents or oophorectomy; other therapies (eg, thalidomide) have also been used with success. We report a case of cyclical erythema multiforme (EM) induced by hypersensitivity to endogenous progesterone in a patient with a history of past oral contraceptive use. After herpes simplex virus was ruled out as an etiologic factor, a diagnosis of progesterone hypersensitivity was confirmed with intradermal skin testing. Results of subsequent patch testing with various progesterone derivatives were negative. The EM outbreaks were suppressed temporarily by continuous administration of Loestrin (ethinyl estradiol plus norethindrone), which also increased the responsiveness of the outbreaks to prednisone tapers.
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PMID:The role of intradermal skin testing and patch testing in the diagnosis of autoimmune progesterone dermatitis. 1680 Feb 78