Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1291
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Delestrogen (Injection)
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Care should be taken to inject deeply into the upper,
outer quadrant of the gluteal muscle following the usual precautions
for intramuscular administration. By virtue of the low viscosity of
the vehicles, the various preparations of DELESTROGEN (estradiol valerate
injection, USP) may be administered with a small gauge needle. Since
the 40 mg potency provides a high concentration in a small volume,
particular care should be observed to administer the full dose. DELESTROGEN should be visually inspected for particulate
matter and color prior to administration; the solution is clear, colorless
to pale yellow. Storage at low temperatures may result in the separation
of some crystalline material which redissolves readily on warming. Note: A dry needle and syringe should be used. Use of
a wet needle or syringe may cause the solution to become cloudy; however,
this does not affect the potency of the material. Treated patients with an intact uterus should be
monitored closely for signs of endometrial cancer, and appropriate
diagnostic measures should be taken to rule out malignancy in the
event of persistent or recurring abnormal vaginal bleeding. See PRECAUTIONS A.1
concerning addition of a progestin.
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DELESTROGEN (estradiol valerate
injection, USP) contains estradiol valerate, a long-acting estrogen
in sterile oil solutions for intramuscular use. These solutions are
clear, colorless to pale yellow. Formulations (per mL): 10 mg estradiol
valerate in a vehicle containing 5 mg chlorobutanol (chloral derivative/preservative)
and sesame oil; 20 mg estradiol valerate in a vehicle containing 224
mg benzyl benzoate, 20 mg benzyl alcohol (preservative), and castor
oil; 40 mg estradiol valerate in a vehicle containing 447 mg benzyl
benzoate, 20 mg benzyl alcohol, and castor oil. Estradiol valerate is designated chemically as estra-1,3,5(10)-triene-3,
17-diol(17��)-, 17-pentanoate. Graphic formula:
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Estrogen drug products act by regulating the transcription
of a limited number of genes. Estrogens diffuse through cell membranes,
distribute themselves throughout the cell, and bind to and activate
the nuclear estrogen receptor, a DNA-binding protein which is found
in estrogen-responsive tissues. The activated estrogen receptor binds
to specific DNA sequences, or hormone-response elements, which enhance
the transcription of adjacent genes and in turn lead to the observed
effects. Estrogen receptors have been identified in tissues of the
reproductive tract, breast, pituitary, hypothalamus, liver, and bone
of women. Estrogens are important in the development
and maintenance of the female reproductive system and secondary sex
characteristics. By a direct action, they cause growth and development
of the uterus, fallopian tubes, and vagina. With other hormones, such
as pituitary hormones and progesterone, they cause enlargement of
the breasts through promotion of ductal growth, stromal development,
and the accretion of fat. Estrogens are intricately involved with
other hormones, especially progesterone, in the processes of the ovulatory
menstrual cycle and pregnancy, and affect the release of pituitary
gonadotropins. They also contribute to the shaping of the skeleton,
maintenance of tone and elasticity of urogenital structures, changes
in the epiphyses of the long bones that allow for the pubertal growth
spurt and its termination, and pigmentation of the nipples and genitals. Estrogens occur naturally in several forms. The primary
source of estrogen in normally cycling adult women is the ovarian
follicle, which secretes 70 to 500 micrograms of estradiol daily,
depending on the phase of the menstrual cycle. This is converted primarily
to estrone, which circulates in roughly equal proportion to estradiol,
and to small amounts of estriol. After menopause, most endogenous
estrogen is produced by conversion of androstenedione, secreted by
the adrenal cortex, to estrone by peripheral tissues. Thus, estrone���especially
in its sulfate ester form���is the most abundant circulating
estrogen in postmenopausal women. Although circulating estrogens exist
in a dynamic equilibrium of metabolic interconversions, estradiol
is the principal intracellular human estrogen and is substantially
more potent than estrone or estriol at the receptor. Estrogens used in therapy are well absorbed through the skin, mucous
membranes, and gastrointestinal tract. When applied for a local action,
absorption is usually sufficient to cause systemic effects. When conjugated
with aryl and alkyl groups for parenteral administration, the rate
of absorption of oily preparations is slowed with a prolonged duration
of action, such that a single intramuscular injection of estradiol
valerate or estradiol cypionate is absorbed over several weeks. Administered estrogens and their esters are handled within
the body essentially the same as the endogenous hormones. Metabolic
conversion of estrogens occurs primarily in the liver (first pass
effect), but also at local target tissue sites. Complex metabolic
processes result in a dynamic equilibrium of circulating conjugated
and unconjugated estrogenic forms which are continually interconverted,
especially between estrone and estradiol and between esterified and
non-esterified forms. Although naturally-occurring estrogens circulate
in the blood largely bound to sex hormone- binding globulin and albumin,
only unbound estrogens enter target tissue cells. A significant proportion
of the circulating estrogen exists as sulfate conjugates, especially
estrone sulfate, which serves as a circulating reservoir for the formation
of more active estrogenic species. A certain proportion of the estrogen
is excreted into the bile and then reabsorbed from the intestine.
During this enterohepatic recirculation, estrogens are desulfated
and resulfated and undergo degradation through conversion to less
active estrogens (estriol and other estrogens), oxidation to nonestrogenic
substances (catecholestrogens, which interact with catecholamine metabolism,
especially in the central nervous system), and conjugation with glucuronic
acids (which are then rapidly excreted in the urine). When given orally, naturally-occurring estrogens and their esters
are extensively metabolized (first pass effect) and circulate primarily
as estrone sulfate, with smaller amounts of other conjugated and unconjugated
estrogenic species. This results in limited oral potency. By contrast,
synthetic estrogens, such as ethinyl estradiol and the nonsteroidal
estrogens, are degraded very slowly in the liver and other tissues,
which results in their high intrinsic potency. Estrogen drug products
administered by non-oral routes are not subject to first-pass metabolism,
but also undergo significant hepatic uptake, metabolism, and enterohepatic
recycling.
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Estrogens should not be used in individuals with
any of the following conditions:
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DELESTROGEN (estradiol valerate
injection, USP) Multiple Dose Vials 10 mg/mL (5
mL): NDC 61570-180-01 20 mg/mL (5 mL): NDC
61570-181-01 40 mg/mL (5 mL): NDC 61570-182-01
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WARNINGS
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A. General:<br/>B. Information for the Patient.: See text of Patient Package Insert.<br/>C. Laboratory Tests.: Estrogen administration should generally be guided
by clinical response at the smallest dose, rather than laboratory
monitoring, for relief of symptoms for those indications in which
symptoms are observable.<br/>D. Drug/Laboratory Test Interactions.:<br/>E. Carcinogenesis, Mutagenesis, and Impairment of Fertility.: Long term continuous administration of natural and
synthetic estrogens in certain animal species increases the frequency
of carcinomas of the breast, uterus, cervix, vagina, testis, and liver.
See CONTRAINDICATIONS and WARNINGS.<br/>F. Pregnancy Category X.: Estrogens should not be used during pregnancy. See CONTRAINDICATIONS and Boxed WARNINGS.<br/>G. Nursing Mothers.: As a general principle, the administration of any
drug to nursing mothers should be done only when clearly necessary
since many drugs are excreted in human milk. In addition, estrogen
administration to nursing mothers has been shown to decrease the quantity
and quality of the milk.<br/>H. Pediatric Use.: Safety and effectiveness in pediatric patients have
not been established. Large and repeated doses of estrogen over an
extended period of time may accelerate epiphyseal closure. Therefore,
periodic monitoring of bone maturation and effects on epiphyseal centers
is recommended in patients in whom bone growth is not complete.
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Serious ill effects have not been reported following
acute ingestion of large doses of estrogen-containing oral contraceptives
by young children. Overdosage of estrogen may cause nausea and vomiting,
and withdrawal bleeding may occur in females.
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estradiol valerate
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Delestrogen (Injection)
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The following additional adverse reactions have
been reported with estrogen therapy (see WARNINGS regarding induction of neoplasia, adverse effects
on the fetus, increased incidence of gallbladder disease, cardiovascular
disease, elevated blood pressure, and hypercalcemia).
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DELESTROGEN (estradiol valerate injection, USP)
is indicated in the:
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Delestrogen
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