Mypill

Approved Indications:

• Oral contraception (birth control): Prevention of pregnancy in women of reproductive age. This is the primary FDA-approved indication.
• Regulation of menstrual cycles: For treatment of irregular or anovulatory cycles.
• Treatment of dysmenorrhea: Alleviation of painful menstruation.
• Management of acne vulgaris (in females ≥14 years): When topical treatments are ineffective and contraception is desired.
• Polycystic Ovary Syndrome (PCOS): To manage symptoms such as hirsutism, acne, and cycle irregularities.
• Premenstrual syndrome (PMS) / Premenstrual dysphoric disorder (PMDD): Hormonal regulation to reduce mood and physical symptoms.
• Functional ovarian cysts: Reducing the formation of benign ovarian cysts.

Clinically Accepted Off-Label Uses:

• Endometriosis: Symptom control through hormonal suppression.
• Heavy menstrual bleeding (menorrhagia): To reduce blood loss.
• Perimenopausal hormonal regulation: In younger women needing contraception and cycle control.

Standard Adult Dosing:

• One tablet daily, orally, at the same time each day, for 21 consecutive days, followed by 7 days of placebo or tablet-free interval (28-day cycle).
• Some formulations may be extended-cycle (e.g., 84 active tablets + 7 placebo).

Initiation Instructions:

• Day 1 start: First tablet on the first day of menstruation — no backup needed.
• Sunday start: First tablet on the Sunday after menstruation begins — backup contraception required for 7 days.
• Quick start: Begin any day — backup needed for 7 days.

Missed Dose Protocol:

• 1 missed pill: Take as soon as remembered, then continue as normal.
• 2 or more missed pills: Follow package-specific instructions and use backup contraception.

Pediatric Use (post-menarche):

• Approved for females ≥14 years for contraception and acne management.
• Use only after menarche and with appropriate counseling.

Geriatric Use:

• Not indicated post-menopause.

Renal/Hepatic Impairment:

• Hepatic impairment: Contraindicated in severe liver dysfunction.
• Renal impairment: Use with caution; no standard dose adjustment, but monitor closely.

Route of Administration:

• Oral only (tablet form)

Desogestrel, a third-generation progestin, and Ethinyl Estradiol, a synthetic estrogen, work synergistically to inhibit ovulation by suppressing gonadotropin (FSH and LH) secretion from the pituitary gland. This prevents the mid-cycle LH surge necessary for follicular maturation and ovulation. Additionally, they induce endometrial thinning, making the uterine lining less suitable for implantation, and thicken cervical mucus, creating a barrier to sperm penetration. These combined effects result in highly effective contraception and hormonal cycle regulation.

Absorption:

• Ethinyl Estradiol: Rapidly absorbed; peak levels in 1–2 hours.
• Desogestrel: Prodrug converted to active etonogestrel; peak levels in 1.5–2 hours.

Bioavailability:

• Ethinyl Estradiol: ~40–45% due to first-pass hepatic metabolism.
• Desogestrel: ~75–85%

Distribution:

• Both drugs bind to plasma proteins; ethinyl estradiol binds to albumin, while etonogestrel binds to SHBG and albumin.

Metabolism:

• Ethinyl Estradiol: Extensively metabolized in the liver via CYP3A4, sulfation, and glucuronidation.
• Desogestrel: Metabolized to etonogestrel, mainly via CYP3A4.

Half-life:

• Ethinyl Estradiol: ~24 hours
• Etonogestrel (from desogestrel): ~30 hours

Elimination:

• Primarily hepatic metabolism with excretion via urine and feces.

Pregnancy:

• Category X (contraindicated): Not to be used during pregnancy.
• No contraceptive benefit during pregnancy; may pose risk of hormonal exposure.

Lactation:

• Not recommended in breastfeeding mothers during the first 6 weeks postpartum due to potential reduction in milk production.
• Desogestrel may be excreted in breast milk in small amounts; clinical significance is minimal, but caution is advised.

• Primary Class: Combined Oral Contraceptive (COC)
• Subclass: Estrogen-Progestin Combination (3rd-generation progestin)

• Known hypersensitivity to ethinyl estradiol, desogestrel, or excipients
• Pregnancy
• Active or history of thromboembolic disorders (e.g., DVT, PE)
• History of cerebrovascular accident or coronary artery disease
• Estrogen-dependent tumors (e.g., breast cancer, endometrial cancer)
• Undiagnosed abnormal vaginal bleeding
• Severe liver disease or hepatic tumors
• Migraine with aura
• Smokers ≥35 years of age
• Known thrombophilia (e.g., Factor V Leiden)

• Thromboembolic Risk: Increased risk of venous and arterial thromboembolism, particularly in smokers and women over 35.
• Hypertension: May elevate blood pressure; monitor regularly.
• Liver function: Discontinue if jaundice or liver enzyme elevation occurs.
• Depression: Monitor for mood changes or worsening of pre-existing depression.
• Migraine: New-onset or worsening migraine may warrant discontinuation.
• Breast cancer: Long-term use may be associated with a slightly increased risk.
• Diabetes: May affect glucose tolerance.
• Visual disturbances: Discontinue immediately if sudden vision loss or proptosis occurs.

Common:

• Nausea, vomiting
• Headache
• Breast tenderness
• Spotting or breakthrough bleeding
• Weight gain or fluid retention
• Mood changes
• Decreased libido

Less Common:

• Acne
• Bloating
• Melasma or skin pigmentation
• Vaginal discharge or irritation

Serious:

• Deep vein thrombosis (DVT)
• Pulmonary embolism (PE)
• Myocardial infarction
• Stroke
• Liver dysfunction or hepatic adenomas
• Gallbladder disease
• Anaphylaxis (rare)

Enzyme-Inducing Drugs (↓ efficacy):

• CYP3A4 inducers: Rifampin, phenytoin, carbamazepine, phenobarbital, St. John’s Wort
• May require backup contraception during and after use.

Enzyme-Inhibiting Drugs (↑ estrogen levels):

• CYP3A4 inhibitors: Ketoconazole, clarithromycin, itraconazole — may increase risk of estrogen-related side effects.

Other Interactions:

• Antibiotics: Controversial, but rifampin is confirmed to reduce COC efficacy.
• Antiretrovirals: May alter hormone levels (e.g., efavirenz, ritonavir).
• Lamotrigine: Estrogens may reduce lamotrigine levels, risking seizure breakthrough.

Alcohol Interaction:

• No direct interaction, but excess alcohol can impair adherence.

• FDA & EMA: Continue to emphasize thromboembolic risks with third-generation progestins like desogestrel; patient selection and risk screening are vital.
• Updated guidelines recommend caution in women with migraine with aura or history of thromboembolic events.
• Newer formulations with lower doses of ethinyl estradiol (20 mcg) are now preferred for reduced side effect burden while maintaining efficacy.

• Temperature: Store at 20°C to 25°C (68°F to 77°F)
• Allowable range: 15°C to 30°C
• Humidity: Store in a dry place
• Light: Protect from direct sunlight
• Container: Keep in original blister packaging until use
• Handling: Keep out of reach of children; do not use if the tablet is discolored or damaged