Ethylestrenol

SRP: The most favorable course of action is to use an alternative chemical product with less inherent propensity for occupational exposure or environmental contamination. Recycle any unused portion of the material for its approved use or return it to the manufacturer or supplier. Ultimate disposal of the chemical must consider: the material's impact on air quality; potential migration in soil or water; effects on animal, aquatic, and plant life; and conformance with environmental and public health regulations.

Catatoxic steroid ethylestrenol protected female rats against acute cocaine-HCl toxicity. Hepatic enzyme induction may produce protective catatoxic activity of many steroids, irrespective of their classical hormone properties

Anticoagulant effects of coumarin- or indandione-derivative or anti-inflammatory analgesics, nonsteroidal or salicylates, in therapeutic doses may be increased during concurrent use with anabolic steroids, especially 17-alpha-alkylated compounds, because of decreased procoagulant factor concentration caused by alteration of procoagulant factor synthesis or catabolism and increased receptor affinity for the anticoagulant; anticoagulant dosage adjustment based on prothrombin time determinations may be required during and following concurrent use with anabolic steroids. /Anabolic Steroids/

Concurrent use of antidiabetic agents, sulfonylurea or insulin with anabolic steroids may decrease blood glucose concentration; diabetic patients should be closely monitored for signs of hypoglycemia ... /Anabolic Steroids/

Concurrent use of corticosteroids, glucocorticoid, especially with significant mineralocorticoid activity, prolonged therapeutic corticotropin or sodium-containing medications or foods with anabolic steroids may increase the possibility of edema; in addition, concurrent use of glucocorticoids or corticotropin with anabolic steroids may promote development of severe acne. /Anabolic Steroids/

For more Interactions (Complete) data for ETHYLESTRENOL (7 total), please visit the HSDB record page.

TERRESTRIAL FATE: Based on a classification scheme(1), an estimated Koc value of 29,000(SRC), determined from a structure estimation method(2), indicates that ethylestrenol is expected to be immobile in soil(SRC). Volatilization of ethylestrenol from moist soil surfaces is expected to be an important fate process(SRC) given an estimated Henry's Law constant of 2.3X10-5 atm-cu m/mole(SRC), using a fragment constant estimation method(3). However, volatilization from moist soil surfaces is expected to be attenuated by adsorption to the soil. Ethylestrenol is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 6.9X10-7 mm Hg(SRC), determined from a fragment constant method(4). Biodegradation data were not available(SRC, 2005).

AQUATIC FATE: Based on a classification scheme(1), an estimated Koc value of 29,000(SRC), determined from a structure estimation method(2), indicates that ethylestrenol is expected to adsorb to suspended solids and sediment(SRC). Volatilization from water surfaces is expected(3) based upon an estimated Henry's Law constant of 2.3X10-5 atm-cu m/mole(SRC), developed using a fragment constant estimation method(4). Estimated volatilization half-lives for a model river and model lake are 70 and 630 hours, respectively(3). However, volatilization from water surfaces is expected to be attenuated by adsorption to suspended solids and sediment in the water column. The estimated volatilization half-life from a model pond is 8.5 years if adsorption is considered(5). According to a classification scheme(6), an estimated BCF of 3,600(SRC), from an estimated log Kow of 5.5(7) and a regression-derived equation(8), suggests the potential for bioconcentration in aquatic organisms is very high(SRC). Biodegradation data were not available(SRC, 2005).

ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), ethylestrenol, which has an estimated vapor pressure of 6.9X10-7 mm Hg at 25 °C(SRC), determined from a fragment constant method(2), will exist in both the vapor and particulate phases in the ambient atmosphere. Vapor-phase ethylestranol is degraded in the atmosphere by reaction with photochemically-produced hydroxyl radicals(SRC); the half-life for this reaction in air is estimated to be 3.3 hours(SRC), calculated from its rate constant of 1.2X10-10 cu cm/molecule-sec at 25 °C(SRC) that was derived using a structure estimation method(3). The rate constant for the vapor-phase reaction of ethylestranol with ozone has been estimated as 4.3X10-16 cu cm/molecule-sec at 25 °C(SRC) that was derived using a structure estimation method(3). This corresponds to an atmospheric half-life of about 38 minutes at an atmospheric concentration of 7X10+11 ozone molecules per cu cm(4). Particulate-phase ethylestrenol may be removed from the air by wet and dry deposition(SRC). Ethylestrenol does not contain chromophores that absorb at wavelengths >290 nm and therefore is not expected to be susceptible to direct photolysis by sunlight(SRC).

Using a structure estimation method based on molecular connectivity indices(1), the Koc of ethylestrenol can be estimated to be 29,000(SRC). According to a classification scheme(2), this estimated Koc value suggests that ethylestranol is expected to be immobile in soil.

/CASE REPORTS/ Forty-nine patients with decreased fibrinolytic activity in the vessel walls or a decreased release mechanism, or both, were treated with ethylestrenol for three to 17 months. Forty-five of the patients had had recurrent, phlebographically verified, deep venous thrombosis (DVT) and four had arterial thrombosis. Ethyloestrenol 8 mg/day was given to 31 patients and 4 mg/day was given to 12. The remaining six patients had been treated with a combination of phenformin and ethylestrenol. The phenformin was withdrawn but they were kept on ethylestrenol 8 mg/day. Another 15 patients with a normal fibrinolytic system--four with recurrent DVT and 11 with severe arteriosclerosis--were given ethylestrenol 8 mg/day. The spontaneous fibrinolytic activity, local fibrinolytic activity during standardized venous occlusion of the arms, and fibrinolytic activity of the vessel walls increased significantly after treatment with ethylestrenol 8 mg/day for three months. No further increase occurred after three months, and ethyloestrenol 4 mg/day had no effect. No values rose significantly in the patients with a normal fibrinolytic system. One patient suffered a recurrence within three months of treatment, before the fibrinolytic system became normal. In one patient the fibrinolytic defect reappeared after 10 months in spite of continued treatment. Two of the three women of fertile age developed irregular cycles and intermenstrual bleeding, which disappeared when the treatment was withdrawn. No other side effects were observed.

An estimated BCF of 3,600 was calculated for ethylestrenol(SRC), using an estimated log Kow of 5.5(1) and a regression-derived equation(2). According to a classification scheme(3), this BCF suggests the potential for bioconcentration in aquatic organisms is very high(SRC), provided the compound is not metabolized by the organism(SRC).

The Henry's Law constant for ethylestrenol is estimated as 2.3X10-5 atm-cu m/mole(SRC) using a fragment constant estimation method(1). This Henry's Law constant indicates that ethylestrenol is expected to volatilize from water and moist soil surfaces(2). Based on this Henry's Law constant, the volatilization half-life from a model river (1 m deep, flowing 1 m/sec, wind velocity of 3 m/sec)(2) is estimated as 70 hours(SRC). The volatilization half-life from a model lake (1 m deep, flowing 0.05 m/sec, wind velocity of 0.5 m/sec)(2) is estimated as 26 days(SRC). However, volatilization from water surfaces is expected to be attenuated by adsorption to suspended solids and sediment in the water column. The estimated volatilization half-life from a model pond is 8.5 years when adsorption is considered(3). Ethylestrenol is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 6.9X10-7 mm Hg(SRC), determined from a fragment constant method(4).

/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ The effects of structurally related 19-nortestosterone derivatives on the gonads of 104 male rats were studied. Ethylestrenol, ethynylestrenol, and allylestrenol were orally administered in doses of .25, .5, 1.0, and 5.0 mg/day for 15 days. The weights of the testis, seminal vesicle, and ventral prostrate were determined, and the testis were studied histologically. The 5 mg dose of allylestrenol and ethynylestrenol were the only estrenols that produced significant changes in testicular weight (p less than .01). All the accessory sex organs showed inhibited growth with estrenol treatment. Extensive testicular damage was caused by both ethynylestrenol and ethylestrenol, whereas only a 5 mg dosage of allylestrenol produced histological alteration of the testis. Generally, ethylestrenol and ethynylestrenol caused a relatively stronger inhibiting effect in the accessory sex organs than allylestrenol did.

Anabolic steroids should be used with caution in children and adolescents and only by specialists who are aware of their effects on bone maturation because of possible premature epiphyseal closure, precocious sexual development in males, and virilization in females. The epiphyseal maturation may be accelerated more rapidly than linear growth in children, and the effect may continue for 6 months after the medication has been discontinued. /Anabolic Steroids/

Anabolic steroids are not recommended for use during pregnancy, since studies in animals have shown that anabolic steroids cause masculinization of the fetus. Risk-benefit must be carefully considered. /Anabolic steroids/

Anabolic steroids may decrease blood glucose concentrations; diabetic patients should be closely monitored for signs of hypoglycemia and dosage of hypoglycemic agent adjusted as necessary. /Anabolic steroids/

The rate constant for the vapor-phase reaction of ethylestrenol with photochemically-produced hydroxyl radicals has been estimated as 1.2X10-10 cu cm/molecule-sec at 25 °C(SRC) using a structure estimation method(1). This corresponds to an atmospheric half-life of about 3.3 hours at an atmospheric concentration of 5X10+5 hydroxyl radicals per cu cm(1). The rate constant for the vapor-phase reaction of ethylestrenol with ozone has been estimated as 4.3X10-16 cu cm/molecule-sec at 25 °C(SRC) that was derived using a structure estimation method(1). This corresponds to an atmospheric half-life of about 38 minutes at an atmospheric concentration of 7X10+11 ozone molecules per cu cm(2). Ethylestrenol is not expected to undergo hydrolysis in the environment due to the lack of hydrolyzable functional groups(3). Ethylestrenol does not contain chromophores that absorb at wavelengths >290 nm and therefore is not expected to be susceptible to direct photolysis by sunlight(SRC).

Occupational exposure to ethylestrenol may occur through dermal contact with this compound at workplaces where ethylestrenol is produced or used(SRC). Exposure to the drug among the general population may be limited to those administered ethylestrenol, an anabolic steroid(SRC). Intentional human exposure may have occurred from ethylstranol use as a possible performance enhancement drug in athletes(1).

Ethylestrenol's production and use as an anabolic steroid and possible use as a performance enhancement drug in athletes may result in its release to the environment through various waste streams. If released to air, an estimated vapor pressure of 6.9X10-7 mm Hg at 25 °C indicates ethylestrenol will exist in both the vapor and particulate phases in the atmosphere. Vapor-phase ethylestrenol will be degraded in the atmosphere by reaction with photochemically-produced hydroxyl radicals; the half-life for this reaction in air is estimated to be 3.3 hours. Particulate-phase ethylestrenol will be removed from the atmosphere by wet and dry deposition. Ethylestrenol does not contain chromophores that absorb at wavelengths >290 nm and therefore is not expected to be susceptible to direct photolysis by sunlight. If released to soil, ethylestrenol is expected to have no mobility based upon an estimated Koc of 29,000. Volatilization from moist soil surfaces is be expected to be an important fate process based upon an estimated Henry's Law constant of 2.3X10-5 atm-cu m/mole. However, adsorption to soil is expected to attenuate volatilization. Ethylestrenol is not expected volatilize from dry soil surfaces based upon its vapor pressure. Biodegradation data were not available. If released into water, ethylestrenol is expected to adsorb to suspended solids and sediment based upon the estimated Koc. Volatilization from water surfaces is expected to be an important fate process based upon this compound's estimated Henry's Law constant. Estimated volatilization half-lives for a model river and model lake are 70 and 630 hours, respectively. However, volatilization from water surfaces is expected to be attenuated by adsorption to suspended solids and sediment in the water column. The estimated volatilization half-life from a model pond is 8.5 years if adsorption is considered. An estimated BCF of 3,600 suggests the potential for bioconcentration in aquatic organisms is very high. Hydrolysis is not expected to be an important environmental fate process since this compound lacks functional groups that hydrolyze under environmental conditions. Occupational exposure to ethylestrenol may occur through dermal contact with this compound at workplaces where ethylestrenol is produced or used. Exposure to the drug among the general population may be limited to those administered ethylestrenol, an anabolic steroid. Intentional human exposure may have occurred from possible ethylstrenol use as a performance enhancement drug in athletes. (SRC)

Schedules of controlled substances are established by section 202 of the Controlled Substances Act (21 U.S.C. 812). Schedule III shall consist of the drugs and other substances, by whatever official name, common or usual name, chemical name, or brand name designated, listed in this section. Unless specifically excepted or unless listed in another schedule, any material, compound, mixture, or preparation containing any quantity of the following substances, including its salts, isomers, and salts of isomers whenever the existence of such salts of isomers is possible within the specific chemical designation. DEA Code #: 4000; Drug class: anabolic steroids.

The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed discontinued drug products, incl ethylestrenol.