Generic Name

Estradiol Valerate and Dienogest

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Classification

FDA Approved Indications

• Contraception
• Treatment of symptoms of estrogen deficiency (e.g., vasomotor symptoms, vaginal atrophy)

Mechanism of Action

Estradiol Valerate is an estrogen that stimulates estrogen receptors, promoting secondary sexual characteristics and reproductive tissue development. Dienogest is a progestin that acts on progesterone receptors, stabilizing the endometrial lining and suppressing ovulation when combined, providing contraceptive effects.

Dosage and Administration

Adult: Typically, one tablet daily for 21 days followed by a 7-day hormone-free interval; specific dosing depends on the formulation.

Pediatric: Not indicated for use in individuals under 18 years.

Geriatric: Not specifically indicated; use with caution as estrogen therapy carries increased risks in older women.

Renal Impairment: Use with caution; no specific dose adjustment established.

Hepatic Impairment: Contraindicated in women with hepatic disease or tumor.

Pharmacokinetics

Absorption: Well absorbed orally.

Distribution: Extensively bound to plasma proteins, primarily albumin and sex hormone-binding globulin.

Metabolism: Metabolized in the liver via conjugation and oxidation.

Excretion: Primarily in urine and feces; metabolites excreted in urine.

Half Life: Estradiol: approximately 13-20 hours; Dienogest: approximately 9-16 hours.

Contraindications

• History of thromboembolic Disorders
• Estrogen-dependent tumors (e.g., breast cancer)
• Liver disease
• Pregnancy

Precautions

• Monitor blood pressure, liver function, and clotting factors regularly. Use with caution in women over 35 who smoke.

Adverse Reactions - Common

• Nausea (Common)
• Breast tenderness (Common)
• Headache (Common)

Adverse Reactions - Serious

• VTE (Venous Thromboembolism) (Serious, rare but higher in estrogen-containing therapies)
• Hypertension (Serious, monitor blood pressure)
• Liver dysfunction (Serious)

Drug-Drug Interactions

• Anticoagulants (may alter INR), Anticonvulsants (can decrease effectiveness), Antibiotics (may reduce contraceptive efficacy)

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Patient/Family Teaching

• Take medication at the same time daily.
• Report warning signs of thromboembolic events (pain, swelling of limb, chest pain).
• Use additional contraceptive methods if advised.
• Avoid smoking and discuss risks with healthcare provider.

Special Considerations

Black Box Warnings:

• Increased risk of thrombotic events, stroke, and myocardial infarction, especially in women over 35 who smoke.

Genetic Factors: Genetic predisposition may influence thrombotic risk.

Lab Test Interference: May alter parameters such as thyroid binding globulin and clotting factors.

Overdose Management

Signs/Symptoms: Nausea, vomiting, abdominal distress, vaginal bleeding.

Treatment: Supportive care, symptomatic treatment, and discontinuation of medication.

Storage and Handling

Storage: Store at room temperature, 20-25°C (68-77°F).

Stability: Stable until expiration date on the package.