Estradiol Valerate

Estradiol Valerate tablet is indicated in Hormone Replacement Therapy (HRT) for estrogen deficiency symptoms in peri- and postmenopausal women. It is used for the prevention of osteoporosis in postmenopausal women at high risk of future fracture.

Estradiol enters target cells freely and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA.

• Peri- and postmenopausal estrogen deficiency symptoms: Used for treatment of hot flushes, night sweats and mood changes.
• Osteoporosis prevention: Used for prevention of bone loss and fractures in postmenopausal women.

Drugs for menopausal symptoms: Hormone replacement therapy, Female Sex hormones

Estrogen

Estradiol enters target cells freely and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell.

Estradiol is an estrogen that helps relieve menopause symptoms and prevents bone loss.

Adult Dose:

• Estrogen-only therapy: 1 mg tablet daily (progestogen should be added if uterus is intact).
• Control of menopausal symptoms: Lowest effective dose for shortest duration should be used.
• Initiation: Start with 1 mg; if necessary, 2 mg should be used.

Swallow the tablet whole, do not chew. May be taken with or without food. Take at the same time each day. Continuous treatment: next pack follows immediately without a break.

If you forget to take a tablet at the usual time, take it within the following 12 hours. If more than 12 hours late, do not take the forgotten tablet and take the remaining tablets at the usual time.

Common Side Effects:

• Breast cancer (more common with HRT use)
• Endometrial hyperplasia or cancer
• Ovarian cancer
• Venous thromboembolism
• Heart disease
• Stroke
• Breast pain, tenderness or enlargement
• Headache, migraine
• Dizziness
• Nausea
• Abdominal pain
• Muscle cramps
• Fluid retention
• Weight changes

Precautions:

• HRT should only be initiated for symptoms that adversely affect quality of life.
• Annual risk-benefit assessment should be undertaken.
• Complete personal and family medical history should be taken before initiation.
• Physical (including pelvic and breast) examination should be done.
• Periodic check-ups recommended during treatment.
• Any changes in breasts should be reported to doctor.

Contraindications:

• Known, past or suspected breast cancer
• Known or suspected estrogen-dependent malignant tumours
• Undiagnosed genital bleeding
• Untreated endometrial hyperplasia
• Previous idiopathic or current venous thromboembolism
• Active or recent arterial thromboembolic disease
• Acute liver disease or history of liver disease
• Porphyria
• Hypersensitivity

Drug Interactions:

• Hepatic enzyme-inducing drugs (anticonvulsants, antimicrobials): May increase clearance of sex hormones and reduce clinical efficacy.
• Antibiotics (penicillins, tetracycline): Rarely may reduce estradiol levels.
• Paracetamol: May increase bioavailability of estradiol.
• Oral antidiabetics or insulin: Requirement may change due to effect on glucose tolerance.

Food Interactions: May be taken with or without food. Caution with alcohol.

Use in Pregnancy: Not indicated during pregnancy. If pregnancy occurs, treatment should be withdrawn.

Use in Lactation: Not indicated during breastfeeding.

Pediatric Use: Not recommended for children.

Geriatric Use: No specific dosage adjustment is necessary for elderly patients.

Renal Impairment: Use with caution in patients with kidney disease.

Hepatic Impairment: Contraindicated in severe liver disease.

Overdose: Overdose may cause nausea, vomiting and withdrawal bleeding. No specific antidotes; symptomatic treatment.

Storage: Store below 30 degree C in a dry place. Keep away from light. Keep out of reach of children.

Estradiol Valerate