Clinical Pharmacology Details


Estradiol


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Indications & Dose:

INDICATIONS AND USES:


Symptoms associated with menopause (vasomotor symptoms, atrophic vaginitis, kraurosis vulvae), breast cancer, prostatic cancer, atrophic vaginitis, hypogonadism, castration, primary ovarian failure, prevention of osteoporosis


DOSAGE


Adult


• Menopause/hypogonadismlcastration/ovarian failure/osteoporosis prevention: PO 1-2 mg qd 3wk on, 1 wk off or 5 days on, 2 days off; 1M 1-5 mg q3-4wk (cypionate); 10-20 mg q4wk ( valerate);


TRANSDERM 0.025-0.1 mg worn continuously, change once (Climara, EzIII) or twice (Estraderm, Vivelle, CombiPatch) per week; VAG RING insert ring into vagina, change rings q3mo


• Prostatic cancer: 1M 30 mg ql-2 wk (valerate); PO 1-2 mg tid (oral estradiol)


• Breast cancer: PO 10 mg tid for 3 mo or longer


• Atrophic vaginitis: Vag cre 2-4 g (marked on applicator) qd for 1-2 wk, then 1 g 1-3 times/wk

Contraindications:

Breast cancer (except in selected patients being treated for metastatic disease), active thromboembolic disorders, known or suspected estrogendependent neoplasia, undiagnosed abnormal genital bleeding 

Side Effects:

CNS: Depression, migraine headache, emotional lability
CV: Arterial thromboembolism, pulmonary embolism, eVA,. MI, hypertension, venous thrombosis, edema
EENT: Contact lens intolerance, retinal thrombosis
Gl: Nausea and vomiting, gallbladder disease bloating, benign hepatic tumors, mesenteric thrombosis
GU: Breakthrough bleeding, spotting, amenorrhea, change in cervical secretions, breast enlargement, breast tenderness, testicular atrophy, endometrial cancer
METAB: Hyperglycemia, hypertrigIyceridemia, hypercalcemia
SKIN: Melasma 

Cautions:

Precautions:

Hypertension, gallbladder disease, CHF, diabetes mellitus, depression, migraine headache, seizure disorders, hepatic disease, family history of breast or endometrial cancer, history of thromboembolic disorders, uterine fibroids, hypertriglyceridemia, hypercalcemia 

Interaction:

Drugs


P450 inducers (e.g., rifampin, barbiturates): Decreased estrogen levels


Corticosteroids: Increased steroid effect


Phenytoin: Loss of seizure control, decreased estrogen levels


Warfarin: Theoretical increased risk thromboembolism 


SPECIAL CONSIDERATIONS


• Progestins recommended in nonhysterectomized women. Estring may have minimal systemic absorption

Warnings:

Adverse Effects:

Lactations:

Pregnancy category X; may reduce quantity and quality of breast milk 

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

Patient And Carer Advice: