Ovacon Gold

Approved Indications:

• Hormonal Contraception:
  Indicated for the prevention of pregnancy in women of reproductive age.
• Menstrual Regulation:
  Used to manage irregular menstrual cycles, especially in women with oligomenorrhea or amenorrhea due to hormonal imbalance.
• Dysmenorrhea:
  Effective in reducing painful menstruation by suppressing ovulation and stabilizing endometrial lining.
• Dysfunctional Uterine Bleeding (DUB):
  Helps manage abnormal uterine bleeding due to hormonal causes, particularly in adolescent girls and premenopausal women.
• Acne Vulgaris (Moderate):
  In women who also desire contraception, this combination may reduce androgen-driven acne by suppressing ovulation and androgen levels.

Clinically Accepted Off-label Uses:

• Polycystic Ovary Syndrome (PCOS):
  Used to manage hyperandrogenism, regulate cycles, and reduce risks of endometrial hyperplasia.
• Endometriosis (Symptom Control):
  May reduce endometriotic pain and lesions by maintaining a hypoestrogenic, progestin-dominant hormonal environment.

Standard Adult Dosage:

• Ethinyl Estradiol (EE) 0.05 mg + Lynestrenol 5 mg
  One tablet daily for 21 consecutive days, followed by a 7-day tablet-free interval.

Route of Administration: Oral

Administration Instructions:

• Start on Day 1 of the menstrual cycle (first day of bleeding).
• Tablet should be taken once daily at the same time, preferably with food or water.
• After 21 active pills, a 7-day break allows for withdrawal bleeding.

Missed Dose Guidance:

• <12 hours delay: Take the missed dose immediately.
• >12 hours delay or multiple missed doses: Backup contraception is recommended for 7 days.

Special Populations:

• Adolescents (post-menarche):
  Same dosage as adults; suitable for regulating cycles and managing DUB.
• Elderly:
  Not indicated post-menopause.
• Hepatic Impairment:
  Contraindicated in severe liver disease; avoid use due to first-pass metabolism.
• Renal Impairment:
  No dosage adjustment specified; use with caution and monitor clinical status.

Ethinyl Estradiol + Lynestrenol functions as a combined oral contraceptive. Ethinyl Estradiol inhibits the release of follicle-stimulating hormone (FSH), preventing follicular development, while Lynestrenol (a prodrug of norethisterone) inhibits luteinizing hormone (LH) secretion, blocking ovulation. Lynestrenol also induces a progestogenic effect on the endometrium, leading to a less receptive lining for implantation and thickens cervical mucus, impeding sperm penetration. The estrogen-progestin synergy ensures effective ovulation suppression, cycle regulation, and hormonal balance.

• Absorption:
• Ethinyl Estradiol: Rapid; bioavailability 40–50% due to hepatic first-pass metabolism.
• Lynestrenol: Well absorbed; peak plasma levels within 2–4 hours.
• Distribution:
• Ethinyl Estradiol: ~98% bound to albumin.
• Lynestrenol: Converted in vivo to norethisterone, which binds to SHBG and albumin.
• Metabolism:
• Ethinyl Estradiol: Metabolized in liver by CYP3A4; undergoes glucuronidation/sulfation.
• Lynestrenol: Hepatically metabolized to norethisterone (active form).
• Excretion:
• Half-life: EE ~13–27 hours; Lynestrenol/norethisterone ~8–22 hours.
• Eliminated via urine and feces.

• Pregnancy:
  Contraindicated. Not to be used during pregnancy due to lack of contraceptive benefit and potential hormonal effects on fetal development.
• Lactation:
  Use with caution.
• Ethinyl Estradiol may reduce milk production.
• Small amounts of both components may pass into breast milk.
• Preferable to use progestin-only pills during the first 6 weeks postpartum.

• Primary Class: Combined Oral Contraceptive (COC)
• Sub-Class: Estrogen-Progestin Combination
• Progestin Generation: Lynestrenol is a first-generation progestin (prodrug of norethisterone)

• Known hypersensitivity to Ethinyl Estradiol, Lynestrenol, or any excipients
• Confirmed or suspected pregnancy
• History of thromboembolic disorders (DVT, PE)
• Cerebrovascular accident or coronary artery disease
• Known thrombophilia (e.g., protein C/S deficiency, antiphospholipid syndrome)
• Severe liver disease or liver tumors
• Uncontrolled hypertension
• Breast cancer or hormone-dependent neoplasia
• Migraine with aura
• Smokers aged ≥35 years

• Thrombotic Risk:
  Elevated risk in smokers, older women, obese patients, and those with thrombophilia.
• Cardiovascular Risk:
  Use with caution in women with hypertension, diabetes, or lipid disorders.
• Cancer:
  Slightly increased risk of breast and cervical cancer; routine screening advised.
• Liver Function:
  Discontinue if significant hepatic enzyme elevation or jaundice occurs.
• Mood & Psychiatric Effects:
  Monitor for signs of depression or mood changes.
• Vision Changes or Severe Headache:
  May indicate thrombotic event; discontinue immediately.

Common Adverse Effects:

• Gastrointestinal: Nausea, vomiting, abdominal discomfort
• CNS: Headache, mood swings, dizziness
• Menstrual: Breakthrough bleeding, spotting, amenorrhea
• Dermatologic: Acne, chloasma, breast tenderness

Serious Side Effects:

• Cardiovascular: Thromboembolism, stroke, myocardial infarction
• Hepatic: Hepatic adenomas, cholestatic jaundice
• Ophthalmic: Retinal vascular thrombosis, visual disturbances
• Psychiatric: Depression, anxiety, irritability

Rare Side Effects:

• Pancreatitis
• Gallbladder disease
• Anaphylactic reaction

• Enzyme Inducers (↓ contraceptive efficacy):
• Rifampicin, Carbamazepine, Phenytoin, Phenobarbital, St. John's Wort
• Enzyme Inhibitors (↑ hormonal exposure):
• Ketoconazole, Itraconazole, Ritonavir
• Antibiotics:
• Rifampicin significantly reduces efficacy; most antibiotics do not unless impacting gut flora severely.
• Anticoagulants:
• Reduced efficacy of warfarin and other coumarins.
• Alcohol:
• Chronic use may impair hepatic metabolism and contraceptive reliability.

Metabolism Pathway:
Primarily CYP3A4-mediated hepatic metabolism

• No major recent changes to regulatory labeling specific to Ethinyl Estradiol + Lynestrenol.
• WHO and EMA continue to support the use of COCs, including older progestins like Lynestrenol, in low-resource settings.
• Clinical guidelines recommend:
• Risk assessment for cardiovascular disease and thrombosis before initiating therapy.
• Preference of newer progestins in women with acne or androgen excess, but Lynestrenol remains effective and well-studied.

• Temperature Range: 20°C to 25°C (68°F to 77°F)
• Permissible Excursions: 15°C to 30°C (59°F to 86°F)
• Humidity Protection: Store in a dry environment; avoid moisture exposure.
• Light Protection: Keep in original packaging to protect from light.
• Handling Instructions:
• Do not refrigerate or freeze.
• Keep out of reach of children.
• Do not use after expiration date.