Loteprednol (as the ester loteprednol etabonate) is a corticosteroid used to treat inflammations of the eye. It is marketed by Bausch and Lomb as Lotemax. It is a topical corticoid anti-inflammatory. It is used in ophthalmic solution for the treatment of steroid responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, and selected infective conjunctivitis’s. Lotemax is less effective than prednisolone acetate 1% in two 28-day controlled clinical studies in acute anterior uveitis, where 72% of patients treated with Lotemax experienced resolution of anterior chamber cells, compared to 87% of patients treated with prednisolone acetate 1%. Lotemax is also indicated for the treatment of post-operative inflammation following ocular surgery. Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation. There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Corticosteroids are capable of producing a rise in intraocular pressure (IOP). Loteprednol etabonate is structurally similar to other corticosteroids. However, the number 20 position ketone group is absent. It is highly lipid soluble, which enhances its penetration into cells. Loteprednol etabonate is synthesized through structural modifications of prednisolone-related compounds so that it will undergo a predictable transformation to an inactive metabolite. Based upon in vivo and in vitro preclinical metabolism studies, loteprednol etabonate undergoes extensive metabolism to inactive carboxylic acid metabolites. Lotemax possesses some adverse reactions associated with ophthalmic steroids include elevated intraocular pressure, which may be associated with optic nerve damage, visual acuity and field defects, posterior subcapsular cataract formation, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera.

Promestriene (3-propyl ethyl, 17B-methyl estradiol) is a synthetic estrogen analog, which is used in topical estrogen therapy. Promestriene’s potential for treating vaginal atrophy symptoms associated with aromatase inhibitor treatment would be precluded if its minimal absorption leads to estrogen-like effects on cell proliferation and estrogen-responsive gene expression. The concern with absorbed vaginal estrogens or estrogen analogs is that they activate occult sites of residual breast cancer or negate the tumor suppressive effects of aromatase inhibitor adjuvant therapy. Promestriene has been studied in phase IV of the clinical trial on improvement of hormonal cytology, local and systemic climacteric complaints, as well as its endometrial security in patients with vaginitis atrophic pelvic; organ prolapse and endometrial hyperplasia. It has been also studied in phase III of the clinical trial in the post-operative patients with hypospadias. In addition, promestriene was in phase IV of the clinical trial to study its treatment of patients with vaginosis, bacterial, but that studied was terminated.

Deprodone is a steroid that was approved in Japan for the treatment of inflammatory skin disorders. The drug is marketed under the name Eclar and contains 0.3% of the prodrug, deprodone propionate.

Etiroxate is a synthetic thyroxine derivative. It was used for the treatment of patients with hyperlipoproteinaemia. There were only slight side effects, such as gastric and autonomic nervous system symptoms. No statistically significant increase in anginal symptoms was found, even in patients with known coronary insufficiency. No negative effects on hepatic and renal function or the peripheral blood count were observed. Etiroxate caused a significant reduction in serum cholesterol, LDL-cholesterol, and serum apolipoprotein B. There was a significant decrease in HDL-cholesterol. Etiroxate might be used for the treatment and prevention of atherosclerotic disease.

Flumedroxone is a progestative agent. It is a pregnane derivative substituted at C-6 by a trifluoromethyl group. It was tested whether flumedroxone had prophylactic value in migraine. No benefit was found in males, or in females with no history of menstrual exacerbation of migraine. In women whose migraine was worse around the time of menstruation flumedroxone resulted in statistically fewer headaches of less severity. With the dose used in this trial side-effects were frequent, the commonest being polymenorrhagia, which occurred in half the women of reproductive age.

Anagestone acetate is a progestin medication, used in the 1960s in combination with the estrogen mestranol as a combined birth control pill. Toxicological study of chronic administration in dogs and monkeys showed the increased risk of developing malignant tumors in the mammary glands and a dose-dependent, nonprogressive decrease in hemoglobin and hematocrits. The drug was voluntarily withdrawn from the market in 1969.

Amcinafide is triamcinolone acetophenide exerting antiinflammatory and antiallergic properties.

Moxestrol (11β-methoxy-17-ethynyl-estradiol) is estrogen receptor agonist. It is used in the studies of estrogen receptor activity and distribution. Moxestrol is rapidly metabolized by the liver. Hydroxylation was the main transformation pathway. Moxestrol yielded metabolites hydroxylated (or methoxylated) at C-2, C-15 and C-16, but not at C-6, and also gave rise to D-homo derivatives. It was considered as a potentially effective drug in the treatment of postmenopausal disturbances.

Epiestriol (INN) (brand names Actriol, Arcagynil, Klimadoral), or epioestriol (BAN), also known as 16β-epiestriol or simply 16-epiestriol as well as 16β-hydroxy-17β-estradiol, is an endogenous, steroidal, weak estrogen, and the 16-epimer of estriol (which is 16α-hydroxy-17β-estradiol). Epiestriol is (or has previously been) used clinically in the treatment of acne. In addition to its estrogenic actions, epiestriol has been found to possess significant anti-inflammatory properties without glycogenic activity or immunosuppressive effects, an interesting finding that is in contrast to conventional anti-inflammatory steroids like hydrocortisone (aglucocorticoid).

Chloroprednisone is a glucocorticoid. The acetated ester prodrug was used as topical anti-inflammatory agent.