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Primolut-N (Norethisterone)
Primolut-N is a progestogen-only medication containing norethisterone (5 mg), a synthetic progestin widely used for gynecological conditions. It is prescribed for menstrual disorders, endometriosis, and hormonal imbalances. This article explores its pharmacology, clinical applications, and safety profile, referencing authoritative sources such as the BNF, Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.
Norethisterone, a first-generation progestin, exerts its effects through:
- Endometrial Transformation: Converts proliferative endometrium into secretory tissue, stabilizing the lining and preventing irregular bleeding (Lippincott).
- Pituitary Suppression: Inhibits the release of gonadotropins (FSH and LH), preventing ovulation at higher doses (Lange).
- Anti-Estrogenic Effects: Counteracts estrogen-induced endometrial hyperplasia, reducing the risk of abnormal growth.
Norethisterone also has mild androgenic and glucocorticoid activity, which may contribute to some side effects.
- Menstrual Disorders:
- Dysfunctional Uterine Bleeding (DUB): Controls heavy or irregular bleeding.
- Amenorrhea: Induces withdrawal bleeding in secondary amenorrhea.
- Endometriosis: Reduces pain and inflammation by suppressing endometrial tissue growth (BNF).
- Premenstrual Syndrome (PMS): Alleviates physical and emotional symptoms.
- Contraception: Used in combination with estrogen for hormonal contraception.
- Hormone Replacement Therapy (HRT): Combined with estrogen to prevent endometrial hyperplasia in postmenopausal women (Lippincott).
- Dysfunctional Uterine Bleeding: 5 mg twice daily for 10 days to stop bleeding, followed by 5 mg daily from day 19 to 26 of the cycle to regulate menstruation (BNF).
- Endometriosis: 5 mg three times daily for 6–9 months.
- Amenorrhea: 5 mg twice daily for 5–7 days to induce withdrawal bleeding.
- PMS: 5 mg twice daily from day 19 to 26 of the cycle.
- Common: Nausea, headache, breast tenderness, weight gain, and mood changes.
- Serious:
- Thromboembolism: Rare but possible, particularly in high-risk patients (Lange).
- Hepatic Effects: Rare hepatotoxicity or benign liver tumors.
- Androgenic Effects: Acne, hirsutism, or hair loss due to mild androgenic activity (Lippincott).
- Absolute Contraindications: History of thromboembolic disorders, severe liver disease, or undiagnosed vaginal bleeding (BNF).
- Relative Precautions: Diabetes, hypertension, or history of depression.
- Monitoring: Regular blood pressure checks and liver function tests in long-term users.
- Reduced Efficacy: Enzyme-inducing drugs (e.g., rifampicin, carbamazepine, St. John’s Wort) accelerate metabolism of norethisterone, reducing its effectiveness (BNF).
- Anticoagulants: May reduce the efficacy of warfarin; monitor INR closely.
- Other Hormonal Therapies: Avoid concurrent use with other progestins or estrogens unless prescribed as part of HRT (Lippincott).
- Active Ingredient: Norethisterone (5 mg).
Brands: Marketed as Primolut-N; generics may be labeled as norethisterone.
