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Look Up > Drugs > Estrogens and Methyltestosterone
Estrogens and Methyltestosterone
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Adverse Reactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms

Pronunciation
(ES troe jenz & meth il tes TOS te rone)

U.S. Brand Names
Estratest®; Estratest® H.S.; Premarin® With Methyltestosterone

Generic Available

No


Synonyms
Conjugated Estrogen and Methyltestosterone; Esterified Estrogen and Methyltestosterone

Pharmacological Index

Estrogen Derivative


Use

Atrophic vaginitis; hypogonadism; primary ovarian failure; vasomotor symptoms of menopause; prostatic carcinoma; osteoporosis prophylactic


Pregnancy Risk Factor

X


Contraindications

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


Adverse Reactions

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


Mechanism of Action

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.


Pharmacodynamics/Kinetics

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


Usual Dosage

Adults: Female: Oral: Lowest dose that will control symptoms should be chosen, normally given 3 weeks on and 1 week off


Dietary Considerations

Should be administered with food at same time each day


Mental Health: Effects on Mental Status

May cause depression


Mental Health: Effects on Psychiatric Treatment

Barbiturates and carbamazepine may decrease the effects of estrogens; estrogens may affect metabolism of benzodiazepines; monitor for clinical effect


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

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.


Nursing Implications

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.


Dosage Forms

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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