Norgestrel [For breastfeeding mother]

Approved Indications:

• Contraception:
• Prevention of pregnancy in women of reproductive age
• Especially suitable for lactating women who wish to avoid estrogen-containing contraceptives

Clinically Accepted Off-label Uses:

• Dysfunctional Uterine Bleeding (DUB):
  As a short-term measure in certain cases
• Endometrial Protection in HRT:
  Used with estrogen in postmenopausal women (less common than norethisterone or medroxyprogesterone)

Adults (Contraception):

• Standard Dose for Breastfeeding Women:
  0.075 mg orally once daily at the same time every day
• Begin 6 weeks postpartum if exclusively breastfeeding
• If not breastfeeding or partially breastfeeding, begin within 3 weeks postpartum
• No pill-free interval; taken continuously without interruption

Missed Dose:

• If taken >3 hours late, use backup contraception (e.g., condoms) for 48 hours

Elderly:

• Not indicated for postmenopausal women

Pediatrics/Adolescents:

• Approved for use in adolescents who have reached menarche

Renal/Hepatic Impairment:

• Contraindicated in severe hepatic dysfunction
• Use with caution in mild impairment

Administration:

• Oral route, with or without food
• Must be taken at exact same time daily to maintain contraceptive efficacy

Norgestrel is a synthetic progestin belonging to the gonane class. It exerts its contraceptive effect primarily by thickening cervical mucus, which impedes sperm penetration. It also induces endometrial atrophy, rendering the uterus less suitable for implantation. In some women, Norgestrel inhibits ovulation, though this is not the primary mechanism of action in progestin-only pills. Its high progestational activity ensures effective contraception without the need for estrogen, making it ideal for use during lactation when estrogen use is discouraged.

• Absorption:
  Rapidly absorbed after oral administration
• Bioavailability:
  Approximately 65–75%
• Peak Plasma Time:
  Within 1–2 hours
• Distribution:
  High plasma protein binding (mainly to albumin and sex hormone-binding globulin)
• Metabolism:
  Hepatic metabolism via reduction and conjugation; minimal CYP450 involvement
• Half-life:
  Approximately 13 hours
• Elimination:
  Excreted primarily in urine as metabolites

• Pregnancy:
  Category X – Contraindicated in known or suspected pregnancy
• Lactation:
  Safe during breastfeeding
• Minimal excretion into breast milk
• Clinical studies show no adverse effects on breastfed infants' growth or development
• Does not reduce milk production, unlike estrogen-containing pills
• Recommended by WHO and ACOG as a preferred contraceptive during lactation

• Primary Class: Hormonal Contraceptive
• Subclass: Progestin-only pill (POP) – First-generation synthetic progestin
• Chemical Class: Gonane derivative

• Known hypersensitivity to Norgestrel or any tablet component
• Known or suspected pregnancy
• Active or past thromboembolic disease (e.g., DVT, PE)
• Known or suspected breast carcinoma or progestin-sensitive tumors
• Undiagnosed abnormal genital bleeding
• Severe hepatic impairment or liver tumors
• History of jaundice during previous hormonal contraceptive use

• Thromboembolism:
  Although lower than estrogen-containing contraceptives, still a risk in predisposed women
• Ectopic Pregnancy:
  Slightly increased risk; consider in case of abdominal pain or amenorrhea
• Menstrual Irregularity:
  May cause spotting, amenorrhea, or irregular cycles—typically improves with time
• Liver Disease:
  Monitor liver function; discontinue if jaundice or hepatic dysfunction occurs
• Breast Cancer:
  Avoid in women with active or history of breast cancer
• Monitoring:
  Regular gynecologic evaluations are advised, especially during long-term use

Common (≥1%):

• Menstrual/Reproductive:
• Irregular bleeding
• Amenorrhea
• Breast tenderness
• Central Nervous System:
• Headache
• Mood changes
• Dizziness
• Gastrointestinal:
• Nausea
• Bloating

Less Common/Serious:

• Acne or oily skin
• Weight gain
• Libido changes
• Depression (monitor mental health)
• Ectopic pregnancy (rare)

Onset & Severity:

• Side effects typically mild to moderate and appear within the first few cycles
• Most resolve with continued use

• Enzyme Inducers (CYP3A4):
• Rifampin, carbamazepine, phenytoin – may decrease contraceptive efficacy
• Antibiotics (e.g., ampicillin, tetracyclines):
• Limited evidence of reduced efficacy; backup contraception may be advisable
• Herbal Interactions:
• St. John’s Wort – reduces effectiveness by inducing metabolism
• Other Hormonal Agents:
• Use caution if combined with estrogen or other progestins
• Alcohol:
• No known direct interaction

• WHO and CDC Guidelines (2023–2024):
• Continue to recommend progestin-only pills (like Norgestrel) as first-line postpartum contraceptives
• ACOG Practice Bulletin:
• Confirms no adverse effect on infant growth or milk production
• Recent Studies:
• Show increased user satisfaction due to fewer estrogen-related side effects
• Long-term data confirm low risk of thromboembolism and cancer in breastfeeding users

• Temperature Range:
  Store below 25°C (77°F)
• Humidity:
  Store in a dry, moisture-free environment
• Light Protection:
  Keep in original packaging away from direct sunlight
• Handling:
  No special precautions needed; store out of reach of children
• Shelf Life:
  Usually 3–5 years; refer to product label