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Oral & Other Forms of Contraception

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Oral & Other Forms of Contraception Oral & other forms of contraception Objectives: Perceive the different contraceptive utilities available. Classify them according to their site and mechanism of action. Justify the existing hormonal contraceptives present. Compare between the types of oral contraceptives pills with respect to mechanism of action, formulations, indications, adverse effects, contraindications and possible interactions. Hint on characteristics & efficacies of other hormonal modalities. Done by: Editing file Ahmad Alkhiary, Abdulaziz Alhammad, Raghda Alqassim, Khalid Aburas, Atheer Alnashwan Revised by: Raghda Alqassim, Qusay Ajlan Drug’s name | Doctors’ notes | Important | Extra Mind Map Oral Contraceptive Pills Combined pills Mini pills (pop) Morning-after (coc) pills Contain both hormones or Contain Contain only a Each one alone estrogen & progestin (high dose) progestin (97% effective) OR (100% effective) Mifepristone + Misoprostol Estrogens + Norgestimate, Desogestrel and Drospirenone Systemic androgenic NO systemic androgenic effect: effect Norethindrone, Norgestimate, Drospirenone Levonorgestrel and and Desogestrel Medroxyprogesterone Nice introduction ^^ 4:20 min Definition Conception Contraception Fusion of the sperm & ovum to produce preventing the fusion between the a new organism. sperm and ovum to occur. Contraception can be achieved by interfering with : Normal process of Implantation Preventing sperm from ovulation fertilizing the ovum HORMONAL IUD (Copper T) THERAPY : يسمى لولب، طريقته إن النحاس يقتل الحيوانات المنوية - Oral Interruption by a Killing the sperm : Contraceptive barrier : pills (OCP) - Contraceptive • Condoms Spermicidal: • Cervical caps ( يجلس لمدة أطول) Patches - Vaginal rings Pic • Jells (Diaphragms) - Injectable • Foams • Thin films - IUD (intra- uterine devise) (with hormone) Pic Quick physiological revision 5 min 13 min Oral Contraceptive Pills Oral Contraceptive Pills According to composition & intent of use; OC are divided into three types Combined pills Mini pills (pop) Morning-after (coc) pills Contain Contain only a Contain both hormones or Each one alone (high dose) estrogen & progestin progestin OR (100% effective) (97% effective) Mifepristone + Misoprostol فعاليته أقل من الكومبايند بشوي من اسمهم )كومبايند( يعني مكونة من Induce abortion إستروجين وبروجستن Combined Pills (COC) Progestins Estrogen 1. Norethindrone Ethinyl estradiol or 2. Levonorgestrel (Norgestrel) mestranol [a “prodrug” 3. Medroxyprogesterone acetate converted to ethynyl estradiol] Not used anymore because it has systemic androgenic effects: Currently concentration acne, hirsutism, weight gain (weight used is very low to gain in all types of oral contraceptives) minimize estrogen hazards 1. Norgestimate MCQ: 2. Desogestrel Which of the following is devoid from systemic androgenic effect? اﻹجابة هي واحد من الثﻻثة Drospirenone .3 Currently used because it has no systemic androgenic effects ﻷن أكيد مافيش ستّة حتبقى عايزة يطلع لها أكني وشعر Combined Pills (COC) 1. Inhibit Ovulation by Suppressing The Release Of Gonadotrophins (FSH & LH) no action on the ovary ovulation is prevented. (the main and most في الحمل يزيد عندها اﻹستروجين والبروجستيرون بينما FSH & LH يق ّلون عشان (important mechanism ما يصير فيه ovulation )بسبب ve feedback I- .. هنا نفس الحالة 2. Inhibit IMPLANTATION by causing abnormal contraction of the fallopian of action of tubes & uterine musculature ovum will be expelled rather than implanted. 3. Increase viscosity of the cervical mucus making it so viscous no Mech. تذكروا في الluteal phase تتغير ال viscosity of cervical mucus )تحت تأثير البروجستيرون .sperm pass غالبًا( ﻷن وقت الليوتيال فيس مو مناسب للسبيرم يدخل ويسوي فرتليزيشن! هنا نفس الميكانزم صارت. 4. Abnormal transport time through the fallopian tubes . ❖ Monthly Pills: ❖ Seasonal Pills: o Pills are better taken at the same o Are known as Continuous / Extended cycle Cover 91 days الهدف هو المحافظة على تركيز ثابت في الدم .time of day schedule. cover 3 months, each 3 months o For 21 days: starting on day 5 / she will have 1 period she will have ending at day 26. (26-5=21dys) 4periods\year instead of 12 p\year. o This is followed by a 7 day pill free o Taken continuously for 84 days , and then a break for 7 days. period (7 days without pills) o Has very low doses of both يعني تبدأ المرأة تاخذها أثناء الدورة الشهرية حقتها )اليوم الخامس(، ضروري تبدأ estrogens and progestins قبل ما تخلص دورتها ﻷن مفعول الدواء ما راح يطلع إﻻ بعد ٧ أيام، تستمر تاخذها لمدة ٢١ يوم، بعدين توقف لمدة ٧ أيام.. في هذي ال٧ أيام، راح Benefit: It lessens menstrual periods ❖ تنزل عليها الدورة ثانية.. وبعدها تأخذ الدواء وهكذا كل شهر ❖ To improve compliance: we use to 4 times a year useful in those a formulation of 28 pills. who have pre - menstrual or menstrual disorders, and in o The first 21 pills are of perimenopausal women with multiphasic formulation vasomotor symptoms on pill free days يعني هي تنظم الدورة، ﻷن المرأة الmedicated) pre & peri-menopausal) تصير الدورة متخبصة عندها وكل شوي تجي وتضايقها Methods of administration of Methods o Followed by the last 7 placebo Useful in those who have pain from endometriosis and can prevent pills (dummy pills) (so in this case there is no break , but the last 7 pills have no effect) migrains during period. Disadvantages: Higher incidence of ❖ في هذا النوع بيصير أخذ الحبوب شهريًا بدون أي أيام بريك زي اللي قبل، واحد breakthrough bleeding & spotting من اﻷهداف إنه يصير أخذ الحبّة بموعد ثابت ومنظم طوال الشهر، وتصير الوحدة ما تضيّع متى أخذتها وتلخبط موعد أخذ اﻷدوية. التفاصيل هذي التفاصيل عن راح أسألكم عن .Helpful video during early use ما قالت الدكتورة قالت ما Currently, the formulation of monthly pills are improved to mimic the natural on going changes in hormonal profile. ❖ Accordingly we have now the phase formulations: كلهم ثابتين (Monophasic (a fixed amount of estrogen & progestin .1 2. Biphasic (2 doses) (a fixed amount of estrogen, while the amount of اﻹستروجين ثابت، البروجستيرون متغير (progestin increases stepwise in the second half of the cycle 3. Triphasic (3 doses) (amount of estrogen; fixed or variable & amount of اﻹستروجين ثابت أو متغير ، البروجستيرون متغير .(progestin increases stepwise in 3 phases Phase Formulation Phase هنا لما نستخدم اﻹستروجين، نستخدمه على شكل Ethinyl estradiol ولما نستخدم البروجستيرون، nd rd نستخدم وحدة من الformulas المذكورة في السﻻيد السابق (and 3 mimics the real cycle 2) Combined Pills (COC) (cont.) الجدول بس لتوضيح المفهوم حق المونو والباي والترايفيزك، :All you have to know from the tables ❖ ﻻ تضيعون وقتكم عليه the Biphasic and Triphasic tablets have a stepwise increase in the ✓ + نﻻحظ إن اﻷستروجين غالبًا قليل عشان نقللل أعراضه (concentration of Progestin (twice in Biphasic , and 3 times in Triphasic الجانبية Estrogen Related Progestin Related: 1. Nausea and breast tenderness. 1. Nausea, vomiting & headache 2. Headache . 2. Slightly higher failure rate. ”الكلف” ويطلع أثناء الحمل ويسمى Fatigue, depression of mood .3 “كلف الحمل” )البقع السوداء( Skin Pigmentation .3 4. Impaired glucose tolerance 4. Menstrual irregularities (hyperglycemia) 5. Weight gain ADRs 5. incidence of breast, vaginal & Progestin causes weight gain, why use it with obese عشان كذا يفضل إنه يؤخذ مع women? Estrogen causes increased risk of developing البروجستن عشان يقلل الكانسر إفكت .cervical cancer 6. Cardiovascular: (major concern) cancer in obese women up to 2-4 times a. Thromboembolism 6. Hirsutism . b. Hypertension 7. Masculinization (Norethindrone) 7. frequency of gall bladder disease 8. Ectopic pregnancy. ❖ Contraindications of Estrogen containing pills: 1. Thrombophlebitis / thromboembolic disorders (Estrogens enhance the coagulability of blood) 2. CHF or other causes of edema 3. Vaginal bleeding of undiagnosed etiology (fear of neoplasm) 4. Known or suspected pregnancy (it may cause miscarriage) 5. Known or suspected breast cancer, or estrogen-dependent neoplasms 6. Impaired hepatic functions C.I 7. Dyslipidemia*, diabetes, hypertension, migraine. (* bc of increase triglyceride by estrogen, Estrogens decrease hepatic oxidation of adipose tissue lipid to ketones and increase synthesis of triglycerides.) You use Mini pills (which contain only progestin) with 4 types of females: ✓ Lactating mothers (nursing women) ✓ Obese ✓ Smokers. ✓ Females > 35 years. Combined Pills (COC) (cont.) Impairing absorption: Antibiotics that interfere with normal GI flora absorption its bioavailability Medications that cause e.g.: Ampicillin contraceptive failure CYT P450 Inducers: Microsomal Enzyme Inducers catabolism of oral contraceptive its action interactions e.g.: Phenytoin, Phenobarbitone, Rifampin COC) CYT P450 Inhibitors: Medications that COC Microsomal Enzyme inhibitors metabolism of oral contraceptive toxicity toxicity e.g.: Acetaminophen, Erythromycin Medications that are Clearance in their toxicity (e.g. warfarin toxicity) altered in clearance () e.g.: Warfarin, Cyclosporine, Combined pills ( by COC Theophylline Mini pills (POP) Contain only a progestin (97% effective) Norethindrone, Levonorgestrel & Norgestimate, Drospirenone & Drug Medroxyprogesterone Desogestrel o The main effect is increasing cervical mucus, so no sperm penetration and MOA therefore, no fertilization. o Contraceptives containing only a progestin should be taken every day, the same time, all year round. P.K o I.M injections e.g. medroxyprogesterone acetate 150 mg every 3 months. هذي للناس اللي ممكن ينسون أو ما يلتزمون بالجرعة يوميًا بنفس الوقت، ياخذون الIM inection كل ٣ شهور أريح لهم o Alternative when estrogen is contraindicated (during breast feeding, نفس اللي
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