Usage
- Medical Conditions: This combination drug is primarily prescribed for contraception (preventing pregnancy). It’s also used to treat menstrual disorders such as dysmenorrhea (painful menstruation), premenstrual syndrome (PMS), menorrhagia (heavy menstrual bleeding), and irregular menstrual cycles. It can also improve iron deficiency anemia associated with menstruation.
- Pharmacological Classification: This is a combination product containing a hormonal contraceptive (estrogen and progestin) and an iron supplement. Specifically, it’s classified as a combined oral contraceptive (COC) and a hematinic.
- Mechanism of Action: Primarily prevents pregnancy by inhibiting ovulation (the release of an egg from the ovary). It also thickens cervical mucus, making it harder for sperm to enter the uterus and reach the egg, and alters the uterine lining, making implantation of a fertilized egg less likely. The ferrous fumarate component replenishes iron lost during menstruation.
Alternate Names
- While the generic name is Ethinyl Estradiol + Ferrous Fumarate + Levonorgestrel, specific formulations may have various names depending on the manufacturer and region.
- Brand Names: Trust Pill, Ashlyna (for Levonorgestrel + Ethinylestradiol component only), several more exist and vary by region.
How It Works
- Pharmacodynamics: Ethinyl estradiol and levonorgestrel suppress the hypothalamic-pituitary-ovarian axis, leading to decreased secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This prevents follicular development and ovulation. The progestin component also thickens cervical mucus and induces endometrial atrophy. Ferrous fumarate provides supplemental iron, which is incorporated into hemoglobin.
- Pharmacokinetics:
- Absorption: Ethinyl estradiol and levonorgestrel are rapidly absorbed from the gastrointestinal tract. Levonorgestrel has nearly 100% bioavailability, while ethinyl estradiol’s bioavailability is lower (around 40-45%) due to first-pass metabolism. Ferrous fumarate absorption can be affected by various dietary factors.
- Metabolism: Levonorgestrel is metabolized in the liver to sulfate and glucuronide conjugates. Ethinyl estradiol is metabolized by hepatic CYP3A4.
- Elimination: Metabolites of both hormones are primarily excreted in urine and feces. Iron is eliminated through shedding of intestinal mucosal cells, bile, and urine.
- Mode of Action: Ethinyl estradiol and levonorgestrel bind to estrogen and progesterone receptors, respectively, modulating gene expression and downstream effects. These hormonal actions suppress the release of gonadotropin-releasing hormone (GnRH), ultimately inhibiting ovulation.
- Receptor Binding/Enzyme Inhibition: These hormones exert their effects through interactions with steroid hormone receptors.
- Elimination Pathways: Primarily hepatic metabolism and renal/biliary excretion.
Dosage
Standard Dosage
Adults:
- One tablet daily, starting on the first day of menstruation or any day during the first five days. If starting later in the cycle, backup contraception is advised for the initial 7 days.
- Follow the specific instructions on the blister pack.
- Twenty-one active pills (containing hormones) are typically followed by seven inactive pills (containing iron or placebo) to maintain a 28-day cycle.
Children:
- Not typically prescribed for premenarchal girls. Use in adolescents should consider individual developmental stage and risk factors.
Special Cases:
- Elderly Patients: Not generally recommended for postmenopausal women.
- Patients with Renal Impairment: Caution is advised. Dose adjustments may be necessary depending on the degree of impairment.
- Patients with Hepatic Dysfunction: Contraindicated in severe liver disease. Caution in mild to moderate hepatic impairment, with careful monitoring.
- Patients with Comorbid Conditions: Use with caution in patients with diabetes, cardiovascular disease, hypertension, hyperlipidemia, history of thromboembolic events, or certain types of cancer.
Clinical Use Cases
This combination drug is not indicated for use in intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dose adjustments are based on individual patient factors, such as renal/hepatic function and concomitant medications. Drug interactions can influence the dosage of both ethinyl estradiol and levonorgestrel.
Side Effects
Common Side Effects:
- Nausea, vomiting
- Breast tenderness
- Headache
- Breakthrough bleeding or spotting
- Mood changes
- Weight changes
- Fluid retention
Rare but Serious Side Effects:
- Blood clots (deep vein thrombosis, pulmonary embolism, stroke, heart attack)
- Liver problems (jaundice, liver tumors)
- High blood pressure
- Gallbladder disease
- Vision changes
Long-Term Effects:
- Increased risk of certain cancers (breast, cervical, liver) with long-term use, though the absolute risk remains relatively low.
- Increased risk of cardiovascular complications in certain individuals, especially smokers and those with underlying risk factors.
Adverse Drug Reactions (ADR):
- Angioedema
- Hypersensitivity reactions
Contraindications
- Pregnancy
- Breastfeeding (unless child is > 6 months old and progestin only pills are not suitable)
- History of thromboembolic disorders, stroke, or heart attack
- Severe liver disease
- Undiagnosed vaginal bleeding
- Breast cancer or other estrogen/progestin-sensitive cancers
- Uncontrolled hypertension
- Smokers over age 35
- Diabetes with vascular complications
Drug Interactions
- Certain antibiotics (e.g., rifampin, tetracyclines) may reduce the effectiveness of COCs.
- Anticonvulsants (e.g., phenytoin, carbamazepine) can decrease hormonal contraceptive effectiveness.
- Antifungal medications (e.g., ketoconazole, itraconazole) may increase hormone levels.
- HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors can interact with COCs.
- St. John’s Wort may reduce effectiveness.
- Grapefruit juice can increase hormone levels.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: X (Contraindicated)
- Fetal Risks: COCs are contraindicated during pregnancy.
- Breastfeeding: Ethinyl estradiol and levonorgestrel can be excreted in breast milk. Not generally recommended during breastfeeding, especially in the first 6 months postpartum. Progestin-only pills or other contraceptive methods may be preferred during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Inhibits ovulation, thickens cervical mucus, alters endometrium. Provides supplemental iron.
- Side Effects: Nausea, breast tenderness, headache, breakthrough bleeding, mood changes, blood clots (rare but serious).
- Contraindications: Pregnancy, breastfeeding, thromboembolic disorders, severe liver disease, breast cancer, uncontrolled hypertension, smoking over 35.
- Drug Interactions: Certain antibiotics, anticonvulsants, antifungals, HIV medications, St. John’s Wort, grapefruit juice.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy. Not recommended during breastfeeding, especially in the first 6 months.
- Dosage: One tablet daily, starting on the first day of the menses or as prescribed. 21 active pills followed by 7 inactive pills.
- Monitoring Parameters: Blood pressure, liver function tests, signs of thromboembolism.
Popular Combinations
This product already combines three components. Co-prescribing with other medications should be done cautiously, considering potential drug interactions.
Precautions
- General Precautions: Screen for contraindications and risk factors before prescribing. Monitor blood pressure and assess for signs and symptoms of complications.
- Specific Populations: See contraindications and pregnancy/breastfeeding sections.
- Lifestyle Considerations: Smoking significantly increases the risk of serious cardiovascular events. Alcohol should be consumed in moderation.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ethinyl Estradiol + Ferrous Fumarate + Levonorgestrel?
A: One tablet daily, starting on the first day of menstruation or within the first five days. 21 hormone-containing pills followed by 7 iron-containing (or placebo) pills, according to the package instructions.
Q2: Can this pill be used as emergency contraception?
A: No, this specific formulation is designed for daily use and is not intended for emergency contraception. Dedicated emergency contraceptive pills containing levonorgestrel alone or ulipristal acetate are available.
Q3: What should a patient do if she misses a pill?
A: Refer to the package insert for specific instructions based on how many pills were missed and when in the cycle they were missed. Generally, taking the missed pill as soon as possible and continuing with the regular schedule is recommended. Backup contraception may be advised.
Q4: Can this pill cause weight gain?
A: Weight changes are a possible side effect, but significant weight gain is uncommon. Counsel patients about lifestyle factors that can influence weight.
Q5: Does this medication protect against sexually transmitted infections (STIs)?
A: No, this pill does not protect against STIs. Barrier methods like condoms are necessary for STI prevention.
Q6: Can this pill impact fertility after discontinuation?
A: Fertility typically returns soon after discontinuation, though it may take a few months for some women to resume their normal menstrual cycle.
Q7: Are there any dietary restrictions while taking this medication?
A: No specific dietary restrictions are typically necessary, but some medications and supplements can interact with COCs. Grapefruit juice should be avoided.
A: Severe abdominal pain, chest pain, shortness of breath, severe headache, leg pain or swelling, vision changes, or speech disturbances should be evaluated immediately, as they could indicate a serious complication like a blood clot.
A: Patients should consult their doctor if they experience any unusual or bothersome side effects, miss multiple pills, or have any health concerns while taking this medication.
