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Pronunciation |
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(ES
troe jenz & meth il tes TOS te
rone) |
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U.S. Brand
Names |
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Estratest®; Estratest® H.S.;
Premarin® With
Methyltestosterone |
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Generic
Available |
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No |
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Synonyms |
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Conjugated Estrogen and Methyltestosterone; Esterified Estrogen and
Methyltestosterone |
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Pharmacological Index |
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Estrogen Derivative |
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Use |
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Atrophic vaginitis; hypogonadism; primary ovarian failure; vasomotor symptoms
of menopause; prostatic carcinoma; osteoporosis
prophylactic |
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Pregnancy Risk
Factor |
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X |
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Contraindications |
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Conjugated estrogens: Known or suspected cancer of the breast, except in
appropriately selected patients being treated for metastatic disease; known or
suspected estrogen-dependent neoplasia; known or suspected pregnancy;
undiagnosed abnormal genital bleeding; active thrombophlebitis or thromboembolic
disorders; past history of thrombophlebitis, thrombosis, or thromboembolic
disorders associated with previous estrogen use (except when used in the
treatment of breast or prostatic malignancy); acute liver disease; chronic
impaired liver function; neuro-ophthalmologic vascular disease
Testosterone: Contraindicated in patients hypersensitive to this agent, in
males with breast carcinoma, during pregnancy (or in women who may become
pregnant) and lactation, in the presence of extensive cardiac, hepatic, or renal
disease, and with known or suspected carcinoma of the prostate gland in males
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Adverse
Reactions |
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1% to 10%:
Central nervous system: Depression, headache
Dermatologic: Chloasma, melasma
Endocrine & metabolic: Breast tenderness, change in menstrual flow,
hypercalcemia
Gastrointestinal: Nausea, vomiting
Hepatic: Cholestatic jaundice |
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Mechanism of
Action |
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Conjugated estrogens: Combination of the sodium salts of the sulfate esters
of estrogenic substances, representing the average composition of material
obtained from pregnant mare's urine. The primary preparation utilized is
Premarin®; however, other generic products are available.
Premarin® contains 50% to 65% estrone sodium sulfate, 20%
to 35% equilin sodium sulfate, and 17 alpha-dihydroequilin, together with
smaller amounts of 17 alpha-estradiol, equilenin, and 17 alpha-dihydroequilenin,
all as salts of the sulfate ester. Estrogens are important for developing
secondary sex characteristics. Estrogens promote growth in development of the
vagina, uterus, fallopian tubes, and enlargement of the breast. Eventually, they
stimulate and limit linear skeletal growth. Estrogens have widespread effects on
metabolism such as transporting proteins and electrolyte balance.
Testosterone: It has been reported that androgens increase protein anabolism
and decrease protein catabolism; however, nitrogen balance is only improved when
androgen therapy is accompanied by adequate caloric and protein intake.
Testosterone and related androgens cause retention of phosphorous, potassium,
sodium, and nitrogen, and decrease renal excretion of calcium. Production of red
blood cells secondary to erythropoietic factor stimulation has been reported
with androgen administration. |
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Pharmacodynamics/Kinetics |
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Conjugated estrogens:
Absorption: Readily absorbed from GI tract
Testosterone:
Duration of therapeutic effect: Depends upon route of administration and
which testosterone ester used; slow absorption extends duration of activity;
I.M. administration usually lasts for 2-4 weeks
Absorption: I.M.: Absorbed slowly allowing for dosing intervals of 2-4 weeks
Half-life: I.M.: ~8 days |
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Usual Dosage |
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Adults: Female: Oral: Lowest dose that will control symptoms should be
chosen, normally given 3 weeks on and 1 week off |
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Dietary
Considerations |
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Should be administered with food at same time each day |
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Mental Health: Effects
on Mental Status |
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May cause depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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Barbiturates and carbamazepine may decrease the effects of estrogens;
estrogens may affect metabolism of benzodiazepines; monitor for clinical
effect |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Women should inform their physicians if signs or symptoms of any of the
following occur: thromboembolic or thrombotic disorders including sudden severe
headache or vomiting, disturbance of vision or speech, loss of vision, numbness
or weakness in an extremity, sharp or crushing chest pain, calf pain, shortness
of breath, severe abdominal pain or mass, mental depression or unusual bleeding;
women should discontinue taking the medication if they suspect they are pregnant
or become pregnant. |
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Nursing
Implications |
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Women should inform their physicians if signs or symptoms of any of the
following occur: thromboembolic or thrombotic disorders including sudden severe
headache or vomiting, disturbance of vision or speech, loss of vision, numbness
or weakness in an extremity, sharp or crushing chest pain, calf pain, shortness
of breath, severe abdominal pain or mass, mental depression or unusual bleeding;
women should discontinue taking the medication if they suspect they are pregnant
or become pregnant. |
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Dosage Forms |
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Tablet:
Estratest® H.S., Menogen H.S.®:
Esterified estrogen 0.625 mg and methyltestosterone 1.25 mg
Premarin® With Methyltestosterone: Conjugated estrogen
0.625 mg and methyltestosterone 5 mg; conjugated estrogen 1.25 mg and
methyltestosterone 10 mg |
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