Hormonal Contraceptives

2 A. Hormonal Contraceptives 1.Combined Oral Contraceptive Pills (COCPs) – Contain both estrogen and progesterone 2.Progestin only preparations – Progestin-only pills (“mini-pill”) – Progestin implants/depot (Levonorgestrel, medroxyprogesterone) – Progestin containing Intrauterine device 3.Emergency contraception – Postcoital contraception

1. Combined Oral Contraceptive Pills (COCPs) Mechanism of action: 1.Estrogen and progesterone causes feedback inhibition of FSH and LH secretion from the pituitary gland to inhibit ovulation. (main mechanism) 2.Progestins thicken the cervical mucous and prevent the entry of sperm. 3. Effects on uterine tubes and endometrium decrease the likelihood of fertilization and implantation 3 Feedback inhibition ↓ LH surge No Ovulation

4 Adverse effects: – Nausea, vomiting, mastalgia, Breakthrough bleeding – Migraine headache – Wt. gain – Acne and Hirsutism (19-nortestosterone derivatives) – Chloasma (skin pigmentation) – Thromboembolism – Ischemic heart disease – Hypertension – Increase TAG – Cholecystitis and gall stones. – Hepatotoxicity

5 Contraindications: Absolute contraindications 1.Thromboembolic, coronary, cerebrovascular disease. Greater risk for : – Women > 35 years of age – Heavy smokers – Obese 2.Active liver disease 3.Suspected or overt malignancy of genitals/breast 4.Undiagnosed vaginal bleeding

6 Relative contraindications: – Hypertension – Migraine – Diabetes mellitus – Uterine leiomyoma – Mental illness – Gall bladder disease Drug Interactions: 1.Enzyme inducers (Phenytoin, barbiturates, carbamazapine, Rifampin) cause contraceptive failure 2.Antibiotics (Tetracyclines, ampicillin, etc.) cause contraceptive failure by suppressing intestinal microflora

7 2. Progestin-only preparations Progestin-only pill (“Mini-pill”) –norethindrone or levonorgestrel Progestin implants/depot –Levonorgestrel: subcutaneous implant, 5 years –Medroxyprogesterone acetate (DMPA): IM, every 3 months. Progestin containing Intrauterine devices –Progestasert contains progesterone & mirena contains levonorgestrel

8 Uses: Progestin-only preparations are suitable for women when estrogens are contraindicated : – Smokers – Age > 35 years – H/O cardiovascular disease – Migraine – Liver impairment

9 Disadvantages of progestins: – Frequent spotting – Irregular and unpredictable menstrual cycles – Failure rate is higher as compared to combined COCPs – Unfavorable effect on lipid profile

10 Emergency contraception Postcoital or “morning after” contraception 1.Combined oral contraceptive pills: 2 pills within 72 hours of unprotected sexual intercourse and 2 exactly 12 hours later. 2.Progestin-only pills (Levonorgestrel): one tablet within 72 hours of unprotected sexual intercourse followed by second dose exactly 12 hrs later. 3.Ulipristal: a selective progesterone receptor modulator; taken within 120 hrs of unprotected sexual intercourse

11 Menopausal hormone therapy (HRT) Used to treat estrogen deficiency symptoms: – Hot flashes, chills, night sweats, mood swings, insomnia, headache, palpitation – Vaginal and urethral atrophy – Osteoporosis (others drugs are preferred) Lowest effective dose of estrogen for the shortest duration to relieve estrogen deficiency symptoms in postmenopausal period.

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