Various Oral Contraceptives and related Drugs

Various Oral contraceptives and related drugs

1. Contraceptive Word Contraceptive = Contra st (Against) + Con ception (Pregnancy) Broadly categorized into four main types: 1. Barrier Methods 2. Hormonal Methods 3. IUDs 4. Sterilization i. Condoms (Male & Female) i. Oral i. Copper i. Female (Tubal Ligation) ii. Diaphragms ii. Injectable i. Hormonal ii. Male (Vasectomy) iii. Cervical Caps iii. Implants iv. Patches

2. A. Oral Contraceptives These Can be – i. COPs (Combined Oral Pills) POPs (Progesterone Only Pills) PCPs (Post Coital Pills) 1. Combined Oral Pills : - Progestin combined with Estrogen Doses are reduced or increased to increase Efficacy and decrease safety, hence available as Monophasic – Fixed Dose during Cycle Biphasic – two Variations in Dose during Cycle Triphasic – three Variations in Doses during Cycle

3. 1. Combined Oral Pills : Estrogen in form of EthinylEstradiol 30mcg & Progesterone in form of Norgestrel 300mcg, Also Available in Transdermal patches (Once weekly for 3 weeks f/b 1 week gap) The amount in pill is 2-3 times higher than usual to attain max efficiency One tablet daily for 21 days started on D5 of Menstruation with 7 days gap for beginning of next cycle, thus to maintain cycle it is replaced with FS 60mg Phasic Pills consist of Low Progestin increased further with Fixed range of E2 (30- 50mg), mimicking normal hormonal pattern, hence given to above 35y females with no withdrawal or breakthrough bleeding from monophasic, though efficacy is same If missed a pill, take 2 on next day & If missed 2 pills, Abort the cycle and start new cycle on D5 of Next Menstruation If pregnant, Congenital anomalies S/e – Contraindicated in CVS Dis/Obese, Breakthrough Bleedings (Increase E2 Dose), Breast Ca., Headache, Nausea, Vomiting, Rebound Increased Fertility or Multiple pregnancies

4. A. Oral Contraceptives These Can be – i. COPs (Combined Oral Pills) POPs (Progesterone Only Pills) PCPs (Post Coital Pills) Progestin Only Pills : - Progestin (19-NorTestesterone) Where E2 Contraindicated Daily 250mcg without any gap MOA – Menstruation Irregularities, Ovulation stopped, Cervical Mucous thickened S/e – Osteoporosis (D/t Low Estrogen), Menopause Symptoms (Hot flushes, Dry Vagina, Reduced libido) Post Coital Pills: - Weight Gain, Headache, Nausea & Vomiting is less compared to COPs Levo- Norgestrel – 1.5mg within 3 days (2- 3 times effective than Yuzpe method) Yuzpe Method: - levo- Norgestrel 1mg + E2 0.2mg within a Day Ulipristal (SPRM): - 30mg within 5 days Mifepristone 600mg within 3 days Failure rate: 2- 4% Chances of Multiple/Tubal Pregnancies

5. B. Mechanism of Action GnRH Inhibition by Negative Feedback (decrease FSH & LH) Suppression Of Ovulation (Anti-Ovulatory) Direct Action on Genital Tract (Thick Cervical Mucous) Prevent Implantation (Ou of Phase Uterus – Hyperproliferative or Hypersecretory or Atrophic) Dislodging implanted Blastocyst (P) C. Adverse Effects + Contraindications Weight Gain, Acne, Increased Body Hair (d/t androgenic action of P) Chloasma Diabetes precipitates Mental Disturbances, Mood Swings Thrombosis & Embolism (More with smoking) Rise in BP – D/t Plasma Angiotensin & Renin, Increased Aldosterone Gallstones – E Increases Bile Strokes/MI – Increase in blood clotting factors (coagulability is enhanced). Decreased antithrombin III. Decreased plasminogen activator in endothelium. Increased platelet aggregation.

6. D. Contraceptives Failures / Interactions Enzyme Inducers – Phenytoin, phenobarbitone, carbamazepine, rifampicin Antibiotics – Suppress Intestinal Microflora (Deconjugation of E excreted in bile fails)

7. i. E. MALE CONTRACEPTION Inhibit Spermatogenesis Hormonal pills Practically difficult because Complete inhibition without affecting other tissues is impossible as 15- 200 million sperms per ejaculation and even one viable sperm is enough Cycle is of 64 days, hence long- acting drug is needed Gn Suppression leads to Loss of Libido and testosterone Non- hormonal (Gossypol): - From cotton seeds, used in China MOA – Suppress spermatogenesis and motility S/e – No Loss of Libido as non-hormonal, HypoK + - Muscular weakness, Edema , Breathlessness, Neuritis Hence, Discontinued.

8. Natural nthetlc ESTROGENS A nd RELATED DRUGS

9. PROGESTERONE DERIVATIVES Medroxyprogesterone acetate Megestrol acetate Dydrogesterone Hydroxyprogesterone caproate Newer compound Nomegestrol acetate

10. 19-NORTESTOSTERONE DERIVATIVES Estranes Norethindrone (Norethisterone) Lynestrenol (Ethinylestrenol) Allylestrenol Gonanes Levonorgestrel Desogestrel Norgestimate :Gestodene