Usage
- Desogestrel + Ethinyl Estradiol is prescribed for the prevention of pregnancy. It is a combined oral contraceptive (COC) containing a synthetic progestogen (desogestrel) and a synthetic estrogen (ethinyl estradiol).
- Pharmacological Classification: Combined Oral Contraceptive (COC), Hormone.
- Mechanism of Action: Desogestrel + Ethinyl Estradiol primarily prevents pregnancy by inhibiting ovulation. Secondary mechanisms include thickening the cervical mucus, which hinders sperm penetration, and altering the uterine lining (endometrium), making implantation less likely.
Alternate Names
- While “Desogestrel + Ethinyl Estradiol” represents the generic name, specific formulations may have various names depending on the manufacturer and dosage regimen (monophasic, biphasic, triphasic).
- Brand Names: Numerous brand names exist, including Apri, Desogen, Ortho-Cept, Velivet, Kariva, Mircette, Cyclessa, and others.
How It Works
- Pharmacodynamics: Desogestrel and Ethinyl Estradiol work synergistically to provide contraception. Ethinyl estradiol suppresses the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland, preventing ovulation. Desogestrel inhibits LH surges and thickens cervical mucus.
- Pharmacokinetics: Both components are rapidly absorbed after oral administration. Ethinyl estradiol undergoes hepatic metabolism, while desogestrel is metabolized to etonogestrel (the active metabolite). Both are primarily eliminated in the urine and feces.
- Mode of Action: Ethinyl estradiol binds to estrogen receptors, leading to negative feedback on the hypothalamic-pituitary axis, thus suppressing FSH and LH release. Desogestrel binds to progesterone receptors, further contributing to the suppression of LH and modifying cervical mucus.
- Elimination Pathways: Both drugs are metabolized in the liver and excreted through renal and hepatic pathways.
Dosage
Standard Dosage
Adults:
- Dosage regimens vary depending on the specific product (monophasic, biphasic, or triphasic). Typically, one tablet is taken daily for 21 days, followed by 7 days of inert or placebo tablets. Some formulations offer 28-day packs with active and inactive pills. The specific dose of desogestrel and ethinyl estradiol varies with the product.
- The common monophasic dose is Desogestrel 0.15 mg/Ethinyl Estradiol 0.03 mg.
- Administration is via the oral route, preferably at the same time each day.
Children:
- Not recommended for use before menarche. Postpubertal adolescents may use COCs, following the adult dosing guidelines.
Special Cases:
- Elderly Patients: COCs are generally not recommended for women over 35 who smoke due to the increased cardiovascular risks.
- Patients with Renal Impairment: Caution should be exercised in patients with renal impairment.
- Patients with Hepatic Dysfunction: COCs are contraindicated in women with active liver disease or tumors.
- Patients with Comorbid Conditions: Careful assessment is needed for women with conditions such as diabetes, hypertension, or hyperlipidemia.
Clinical Use Cases
Desogestrel + Ethinyl Estradiol is specifically indicated for contraception and not typically used in the context of intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dosage adjustments might be necessary for patients with specific conditions (e.g., hepatic impairment), but this is infrequent with COCs.
Side Effects
Common Side Effects:
- Nausea, breast tenderness, headache, breakthrough bleeding, weight changes, mood changes.
Rare but Serious Side Effects:
- Blood clots (deep vein thrombosis, pulmonary embolism), stroke, heart attack, liver tumors, high blood pressure.
Long-Term Effects:
- While generally safe for long-term use, continued monitoring for cardiovascular and liver-related complications is necessary.
Adverse Drug Reactions (ADR):
- Severe allergic reactions (rare), jaundice.
Contraindications
- Pregnancy, history of thromboembolic disorders, liver disease or tumors, undiagnosed abnormal vaginal bleeding, breast cancer, estrogen-dependent neoplasia, hypersensitivity to components.
Drug Interactions
- Certain medications (e.g., anticonvulsants, some antibiotics) may decrease the effectiveness of COCs.
- Enzyme inducers (e.g., rifampin) can reduce COC efficacy.
- St. John’s wort can also reduce the efficacy of birth control pills.
- It is crucial to discuss all concomitant medications with a physician.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: X (Contraindicated).
- COCs are contraindicated during pregnancy.
- Breastfeeding: COCs can reduce milk production. Although small amounts of hormones are excreted in breast milk, significant adverse effects on infants are rare. Non-hormonal or progestin-only contraceptives are preferred during breastfeeding, especially in the first few weeks postpartum.
Drug Profile Summary
- Mechanism of Action: Inhibits ovulation, thickens cervical mucus, alters endometrium.
- Side Effects: Nausea, breast tenderness, headache, breakthrough bleeding, serious but rare cardiovascular events.
- Contraindications: Pregnancy, history of thrombosis, liver disease, breast cancer.
- Drug Interactions: Certain medications can reduce effectiveness.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy; may reduce milk production during breastfeeding.
- Dosage: Varies based on product; typically one tablet daily for 21 days, followed by 7 days of placebo/inert tablets.
- Monitoring Parameters: Blood pressure, liver function tests.
Popular Combinations
Desogestrel + Ethinyl Estradiol is itself a combination product. Other medications may be co-prescribed to manage side effects (e.g., analgesics for headaches).
Precautions
- General Precautions: Evaluate for cardiovascular risk factors, history of liver disease, and breast cancer.
- Specific Populations: COCs should not be used in pregnant women. Caution is advised in breastfeeding mothers.
- Lifestyle Considerations: Smoking significantly increases cardiovascular risks, especially in women over 35.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Desogestrel + Ethinyl Estradiol?
A: Dosage varies based on the specific product (monophasic, biphasic, or triphasic). Consult the specific product’s prescribing information for detailed instructions, including dosage, timing, and the schedule of active versus inactive tablets. The most common dosage is one tablet containing 0.15 mg desogestrel and 0.03 mg ethinyl estradiol taken daily for 21 days, followed by a 7-day break or 7 days of placebo pills.
Q2: What should a patient do if she misses a dose?
A: Instructions for missed doses depend on the specific product and when in the cycle the dose was missed. Generally, taking the missed pill as soon as possible is recommended. If multiple pills are missed, additional contraceptive methods may be needed. Refer to the specific product’s patient information leaflet for detailed guidance.
Q3: Can Desogestrel + Ethinyl Estradiol be used while breastfeeding?
A: COCs can decrease milk production. While not absolutely contraindicated, non-hormonal or progestin-only methods are generally preferred, particularly in the first weeks postpartum.
Q4: What are the major contraindications for Desogestrel + Ethinyl Estradiol?
A: Major contraindications include pregnancy, a history of thromboembolic events, liver disease, breast cancer, or estrogen-dependent tumors.
Q5: What are the most common side effects patients should be aware of?
A: Common side effects include nausea, breast tenderness, headaches, breakthrough bleeding, and mood changes.
Q6: Are there any drug interactions I should be concerned about?
A: Some medications, including certain antibiotics, anticonvulsants, and St. John’s Wort can reduce the effectiveness of COCs. A thorough medication review is essential.
Q7: What monitoring is recommended for patients on this medication?
A: Regular blood pressure checks and monitoring for signs of liver dysfunction are important.
Q8: How does smoking affect the risks associated with this medication?
A: Smoking significantly increases the risk of cardiovascular events, particularly in women over 35. COCs are generally not recommended for women in this demographic who smoke.
Q9: Can Desogestrel + Ethinyl Estradiol help with acne or other hormonal issues?
A: Some COCs may have a beneficial effect on acne, but the primary indication for Desogestrel + Ethinyl Estradiol is contraception. Other treatments are available specifically for managing acne and hormonal imbalances.
