Hormonal Contraceptives

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HORMONAL CONTRACEPTIVES : 

HORMONAL CONTRACEPTIVES These are the hormonal preparations used for reversible suppression of fertility. Oral contraceptives Parenteral: I/M Injections & S/C implants. Transdermal Patch Intrauterine devices with progestin.

ORAL CONTRACEPTIVES: 

ORAL CONTRACEPTIVES Oral contraceptives are used worldwide for a convenient, affordable & reliable means of contraception. Types: 1. Combination contraceptive pills--- contain both an Estrogen & a Progestin.99.9% efficacious. 2. Progestin only contraceptives. 3. Emergency contraception.

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Contraceptive Preparations Combination Tablets/Pills : Contain both Estrogen & Progestin. Commonly used Estrogens : Ehinyl estradiol / Mestranol Commonly used Progestins : Norethindrone / L- Norgestrel Norgestimate : Recent – less androgenic Combination tablets are available in packs of 21 or 28 pills. 21tablets contain the hormones & 7 are placebo. 3 subtypes ; depending upon the amount of hormones in different tablets. Monophasic . Biphasic. Triphasic .

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Combination contraceptive pills: a. Monophasic pills : Same/ constant amount of Estrogen & Progestin in each pill in one packet: Levlite Estrogen (mg) Progestin (mg) Ethinyl estradiol 0.02 L-Norgestrel 0.1 Nordette, Portia Ethinyl estradiol 0.03 L-Norgestrel 0.15 Ovral-28 Ethinyl estradiol 0.05 D, L-Norgestrel 0.5 Ovcon 50 Ethinyl estradiol 0.05 Norethindrone 1.0 Norinyl 1 +, Ortho-Novum 1/35 Norinyl 1/50, Ortho-Novum 1/50 Ethinyl estradiol 0.035 Mestranol 0.05 Norethindrone 1.0

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b. Biphasic pills : Two different Combinations of Estrogen & Progestin in one packet: Estrogen (mg) Progestin (mg) Ortho-novum 10/11 , Necon 10/11. Day 1 – 10 Ethinyl estradiol 0.035 Norethindrone 0.5 Day 11 - 21 Ethinyl estradiol 0.035 Norethindrone 1.0

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c. Triphasic Tablets: Contain a constant dose of Estrogen with increasing doses of Progestin given over 3 successive 7 days period . Attempt to mimic the natural female cycle. Triphasil , Trivora Days 1 – 6 Days 7 – 11 Days 12 - 21 Estrogen (mg) Progestin (mg) Ethinyl estradiol 0.03 Ethinyl estradiol 0.04 Ethinyl estradiol 0.03 L-Norgestrel 0.05 L-Norgestrel 0.075 L-Norgestrel 0.125 Orthonovum 7/7/7 , Necon 7/7/7 Days 1 – 7 Days 8 – 14 Days 15 - 21 Ethinyl estradiol 0.035 Ethinyl estradiol 0.035 Ethinyl estradiol 0.035 Norethindrone 0.5 Norethindrone 0.75 Norethindrone 1.0 Orthro-Tri-Cyclen Days 1 – 7 Days 8 – 14 Days 15 - 21 Ethinyl estradiol 0.035 Ethinyl estradiol 0.035 Ethinyl estradiol 0.035 Norgestimate 0.18 Norgestimate 0.215 Norgestimate 0.25

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M.O.A of combination pills: Main Mechanism :- Inhibition of ovulation—99.9% . The combination of Estrogen & Progestin given for 3 weeks acts by preventing ovulation; through selective inhibition of release of FSH & LH from pituitary via - ve feedback Estrogen & Progestin exert hypothalamic & pituitary effects as follows: Progestin diminishes the GnRH pulses & also decreases responsiveness of pituitary to GnRH . Estrogen suppresses FSH release from pituitary during the follicular phase of the cycle---- lack of follicular development. Progestin may also inhibit the estrogen induced LH surge at mid -cycle Ovulation does not occur, so conception can not take place.

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Contributory mechanisms : The combination pills also produce following effects: 1. Thickness of cervical mucus. 2. ↓ motility and secretion of fallopian tubes. 3. Alterations in uterine endometrium These changes reduce the likelihood of transport of sperms, conception and implantation . During the 4 th week of placebo; withdrawal of progestin stimulates menstrual bleeding .

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Clinical Uses 1. Contraception . Combination pills are very effective, failure rate 0.5-1% Endometriosis. Intractable dysmenorrhea . Drug – Interactions: Broad spectrum antimicrobials--  EHC --- bioavailability ---  efficacy. Enzyme Inducers: Carbamazepine , Rifampin & Phenytion ----  Metabolism of estrogens & progestins ---  efficacy of oral contraceptives. 3. Oral contraceptives  Metabolism of corticosteroids and diazepam.

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Non-contraceptive Beneficial Effects:  Risk of : Ovarian cysts Cancer of ovary & endometrium . Lower incidence of : Ectopic pregnancy ,Iron deficiency anemia , Pelvic inflammatory disease. Rheumatoid arthritis. Relief of : Irregular cycles. Premenstrual symptoms , Dysmenorrhoea Endometriosis, Hirsutism & Acne.

Adverse effects of combination pills: : 

Adverse effects of combination pills: Since contraceptives are used in otherwise healthy & young females ; the adverse effects are of significant importance. Adverse effects : Are related to dose & the type of hormone . They may be Mild, Moderate or Severe. Severe A/E require cessation of therapy .

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A. Severe Adverse Effects: Require cessation of therapy 1. Vascular Effects:- Most common in smokers & above 35yrs , may affect any age . Venous Thromboembolic disease: Three times greater risk of Superficial or Deep Vein Thrombosis & Pulmonary embolism(3 in 1000). Risk is related to estrogen content. Risk is more in presence of pre-disposing factors----stasis altered clotting factors, injury, genetic factors. Risk is not related to age, parity, mild obesity. Oral contracptives produce  venous blood flow. Endothelial proliferation in arteries & veins. Increase in factors VII, VIII, IX & X.  anti thrombin III.

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Hypertension: New cases worsening of hypertension. 5-10 % Both estrogen & progestin are responsible. Blood pressure normalizes in 3-6 months after stopping the drug. c. Myocardial Infarction: Slightly higher risk of Myocardial infarction. Incidence more in : Obese women Have a H/O pre- eclampsia or hypertension. Have hyperliproteinemia Smokers have much higher risk(135 casesin100,000) than non-smokers(4 cases in100,000)than ) Risk is not increased in past users.

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Acceleration of artherogenesis is due to: ↓ glucose tolerance.  HDL,  LDL (Progestin HDL in proportion to their androgenic activity) ↑ platelet aggregation. Antithrombin III Facilitation of coronary spasm

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d. Cerebrovascular disease: Oral contraceptives ↑ risk of thromboembolic or hemorrhagic stroke in women at all ages. Risk is increased in current & not in past users. More risk in women over 35 yrs specially in smokers.

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2. Depression: Significant depression in 6%--- stop therapy. 3. GIT. Disorders: Many cases of cholestatic Jaundice (specially with H/O Jaundice in pregnancy, genetic pre-disposition). Cholangitis , cholecystitis , gall stones. Ischemic bowel disease secondary to thrombosis of mesenteric arteries . Rare-- incidence of Hepatic adenomas--- rupture-- bleeding 4. Cancer: A small  in risk of Breast Cancer in younger females.  risk of cervical cancer (controversial) may be due to infection with human papilloma virus. ( Risk of Ovarian cysts Cancer of ovary & endometrium ) 5. Others: Alopecia, Skin disorders like Erythema multiforme Erythema nodosum .

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B.Moderate Adverse Effects: May r equire discontinuation of therapy 1. Break through bleeding. 25 % 2. Changes in serum lipids : Progestin HDL,  LDL , Estrogens:  HDL,  LDL. 3. Weight gain, specially with nortestosterone derivatives. 4.  Skin Pigmentation & Hirsutism ; with androgenic progestin. 5. Acne :  with androgenic progestin, improvement with estrogenic prep. 6. Ureteral Dilation &  bacteriuria like pregnancy . 6. Vaginal infections more common & difficult to treat. 7.  Amenorrhea. In some patients for yrs

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C. Mild Adverse Effects: Nausea , breast tenderness, breakthrough bleeding & edema are related to estrogen content. 2. Changes in Serum Proteins:  TBG ,  CBG (Affects estimation of hormones)  Fibrinogen so  ESR. 3. Headache: Often mild and transient Worsening of Migraine / onset of migraine may be associated with cerebrovascular accidents. 4. Failure of withdrawal bleeding: Change the preparation or method of contraception.

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Contraindications: a) Absolute b) Relative Absolute Contraindications: Thrombophlebitis &   Thromboembolism. Cardiovascular & Cerebrovascular disorders Recent or past H/O Vaginal bleeding of unknown cause. Suspected breast /other estrogen dependent neoplasm. Relative contraindications: Liver disease. Asthma Diabetes Mellitus Hypertension. Optic neuritis, Reterobulbar Neuritis Convulsive disorders Chronic heart failure Adolescents prior to epiphysial closure

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Contraception with Progestin Alone MOA of Progestin only contraceptives: Progestin does not always inhibit ovulation; only 60-80 %. Progestin produces following effects: 1. Thickness of cervical mucus. 2. ↓ motility and secretion of fallopian tubes. 3. Alterations in uterine endometrium These changes reduce the likelihood of transport of sperms, conception and implantation . .

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Contraception with Progestin Alone 1. Progestin pill (mini pill): Norethindrone ( Micronor ) Or Norgesterol ( Ovrette ) A/E: The most common A/E is Episodes of irregular, unpredictable spotting & breakthrough bleeding Incidence decreases with time ,amenorrhea common after use for one year.

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2. Injection: Depot Medroxyprogesterone Acetate--- I/ M 150 mg every 3 months A/E. Less reliable. Menstrual disturbances are common. Headache Acne from androgenic progestin. Decrease in HDL & increase in HDL levels Decrease in bone density---- risk of osteoprosis . Mood changes Weight gain

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3. Progestin implant : S/C implantation --- 6 tubes, each of 36 mg L- Norgesterol ( norplant system). Contraception for 3 yrs. A/E: Unpredictable spotting & bleeding. More common during the first year. Implant Useful in: Pts. With hepatic disease. Hypertension. Psychosis. Prior thromboembolism.

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4. Transdermal patch : containing Ethinyl estradiol & progestin norelgastromin . Patch applied for 3 weeks ,4 th week is patch free & withdrawal bleeding occurs. 5. Progestin intrauterine device: A Levonorgesterel - releasing intrauterine system offers a highly effective method of long term contraception—5yrs Suitable for women With at least one child. No H/O PID No H/o ectopic pregnancy A/E: Local irritation, infection, pain at site of insertion , Rarely expulsion of insert. Headache ,mood changes ,wt gain & acne occur in a few patients,

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Schedules of Post – coital contraceptives or (Morning after contraception): - Conjugated estrogens: 10 mg 3 times daily for 5 days Ethinyl estradiol : 2.5 mg twice daily for 5 days Diethylstillbestrol : 50 mg daily for 5 days L- Norgestrel : 0.75 mg twice daily for 1 day Norgestrel 0.5 mg, with ethinly estradiol , 0.05 mg ( Ovral ) Two tablets immediately and two at 12 hours) Mifepristone : 600 mg once on day one with misoprostol 400 μ g once on day three. MOA ofPost – coital pills : - Unclear mechanism. Probable effect on tubal transport

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Chemical contraception in men: No effective oral contraception available Gossypol: Extensive trial in China Cottonseed derivative Destroys elements of the semineferous epithelium but does not alter the endocrine function of the testes. Intravaginal spermicide contraceptives used by females, kill the sperms & prevent conception.