5107 - Womens Health (181318).pdf

Page |1 Disease Management-II BPH-5107 Women's Health Women's Health Sex steroids, also known a...

Page |1 Disease Management-II BPH-5107 Women's Health Women's Health Sex steroids, also known as gonadocorticoids and gonadal steroids, are steroid hormones. The sex steroids include the androgens, estrogens, and progestogens (activate progesterone receptor). An androgen (from Greek andr-, mean"man") is steroid hormone that regulates the development and maintenance of male characteristics. Androgens increase in both boys and girls during puberty. Although androgens are commonly thought of only as male sex hormones, females also have them, but at lower levels: they function in libido and sexual arousal. Progesterone is the major and most important progestogen in the body. The ovaries produce the female sex hormone progesterone after ovulation. During pregnancy, the placenta also produces some. The role of progesterone is to: prepare the lining of the uterus for a fertilized egg. Estrogen, or oestrogen, is the primary female sex hormone. It is responsible for the development and regulation of the female reproductive system and secondary sex characteristics. Female reproductive system It is the story of us  Conception occurs about two weeks from the last day of your last menstrual period.  During menstrual cycle, one of your two ovaries matures an egg within follicle.  If both ovaries release eggs, you may have non-identical twins also known as fraternal twins.  The egg travel down fallopian tube, pushed by tiny hair and awaits the arrival or sperm.  About a teaspoon worth of semen enters the vagina containing roughly 300 million sperm, less than 1000,000 will pass into the cervix.  Only about 200 sperm successfully reached the eggs. Fertilization occurs when one sperm penetrates the egg, combining their genetic materials called fertilization.  Within 24 hours of fertilization, the egg now called zygote, few days later it reaches the uterus as a ball of roughly 500 cells surroundings a fluid field cavity. On day 7, ball of cells burrows into uterine wall called implantation.  By 38 weeks, the fertilization eggs has grown into an infant. Bidyut Chandra Paul Roll: 181318 Department of Pharmacy, PUST  Page |2 Disease Management-II BPH-5107 Women's Health From fertilization of implantation Oral contraceptives  Birth control pills (oral contraceptives) are prescription medications that prevent pregnancy.  Birth control (contraceptive) medications contain hormones (estrogen and progesterone, or progesterone alone).  Birth control pills may also be prescribed to reduce menstrual cramps or prevent anemia.  Some women experience various levels of side effects of birth control pills Question: How birth control medications work? Hormonal birth control medications prevent pregnancy through the following ways:  By blocking ovulation (release of an egg from the ovaries), thus preventing pregnancy  By altering mucus in the cervix, which makes it hard for sperm to travel further  By changing the endometrium (lining of the uterus) so that it cannot support a fertilized egg  By altering the fallopian tubes (the tubes through which eggs move from the ovaries to the uterus) so that they cannot effectively move eggs toward the uterus Question: How does it work? The hormones in the combined pill make your body think that it is pregnant. 1. As a result, your ovaries stop releasing eggs that might otherwise fertilize. 2. The lining of the womb will not develop enough for an egg to grow in it. 3. The fluid in the neck of the womb becomes thicker, which makes it more difficult for sperm to swim into the womb. Available dosage forms: 1. Birth control (contraceptive) medications contain hormones (estrogen and progesterone, or progesterone alone). 2. The medications are available in various forms, such as pills, injections (into a muscle), topical (skin) patches, and slow-release systems (vaginal rings, skin implants, and contraceptive-infused intrauterine devices. Bidyut Chandra Paul Roll: 181318 Department of Pharmacy, PUST  Page |3 Disease Management-II BPH-5107 Women's Health Question: How to choose the drugs? Choosing which estrogen and progesterone dose, type, and administration method is-  Highly patient specific, meaning that the choice greatly depends on factors unique to an individual.  General goals are to choose a product that provides good menstrual cycle control with the fewest adverse (side) effects and to use the lowest hormone dose possible.  After beginning birth control medications, it may be necessary to adjust the dose or to choose a different product. Drugs available: i. Estrogens  Ethinyl estradiol  Mestranol i. Progesterones  Norethynodrel  Ethynodiol diacetate  Norethindrone  Norgestrel  Norethindrone acetate  Levonorgestrel  Norgestimate  Drospirenone  Desogestrel Types of oral contraceptives pills: There are four types of OCP- 1. Combined pills 3. Progestin only pills 2. Phased pills 4. Emergency pills Combined pills Combination birth control pills are a daily medication that contains 2 hormones (estrogen and progestin) to prevent pregnancy.  Widely used  Contains Oestrogen and Progestin in a fixed dose.  Commonly used Progestins: Norethindrone, Levonorgestrel, Norgestrel  Commonly used Oestrogen: Ethinyl estradiol  Third genration progestins: Desogestrel, Gestodene, Norgestimate are LIPID friendly, Increase HDL and reduce atherogenioc risk. [This combined pill is taken for 21 consecutive days followed by 7 pill-free days, which causes a withdrawal bleed]. Phased pills Formulation: Formulations may be- 1. Monophasic (each tablet contains a fixed amount of estrogen and progestin); 2. Biphasic (each tablet contains a fixed amount of estrogen, while the amount of progestin increases in the second half of the cycle); or 3. Triphasic (the amount of estrogen may be fixed or variable, while the amount of progestin increases in 3 equal phases). Bidyut Chandra Paul Roll: 181318 Department of Pharmacy, PUST  Page |4 Disease Management-II BPH-5107 Women's Health  Oestrogen content – 20-50 mcg  If oestrogen is < 35 mcg → Low dose pills.  Progestin content – 0.15-1 mg Preparations:  Monophasic:  Ethinyl Estradiol (50) [EE] + Norethindrone(1.0) [NE] (Ovcon 50)  Biphasic:  Days 1 to 10 – EE(35) + NE(0.5) (NECON)  Days 11 to 21 – EE(35) + NE(1.0)  Triphasic:  Days 1 to 6 – EE(35) + NE(0.5)  Days 7 to 14 – EE(40) + NE(0.75) (ORTHONOVUM)  Days 15 to 21 – EE(35) + NE(1.0) Schedule: One Tab daily from the 1st day of bleeding till 21 days followed by 7 days gap. Gonadotropin-releasing hormone (GnRH) Gonadotropin-releasing hormone (GnRH) is a releasing hormone responsible for the release of follicle- stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary. GnRH is a tropic peptide hormone synthesized and released from GnRH neurons within the hypothalamus. Mode of action:  Oestrogen inhibits secretion of FSH via negative feedback on the anterior pituitary, and thus suppresses development of the ovarian follicle  Progestogen inhibits secretion of LH and thus prevents ovulation; it also makes the cervical mucus less suitable for the passage of sperm  Oestrogen and progestogen act in concert to alter the endometrium in such a way as to discourage implantation. They may also interfere with the coordinated contractions of cervix, uterus and fallopian tubes that facilitate fertilization and implantation. Common adverse effect:  Weight gain, owing to fluid retention or an anabolic effect, or both  Mild nausea, flushing, dizziness, depression or irritability  Skin changes (e.g. acne and/or an increase in pigmentation)  Amenorrhoea of variable duration on cessation of taking the pill. Potential adverse effect: 1. Cardiovascular: Although rare, the most serious adverse effect of oral contraceptives is cardiovascular disease, including thromboembolism, thrombophlebitis, hypertension, increased incidence of myocardial infarction, and cerebral and coronary thrombosis. These adverse effects are most common among women who smoke and who are older than 35 years, although they may affect women of any age. Bidyut Chandra Paul Roll: 181318 Department of Pharmacy, PUST  Page |5 Disease Management-II BPH-5107 Women's Health 2. Carcinogenicity: Oral contraceptives have been shown to decrease the incidence of endometrial and ovarian cancer. Their ability to induce other neoplasms is controversial. The production of benign tumors of the liver that may rupture and hemorrhage is rare. 3. Metabolic: Abnormal glucose tolerance (similar to the changes seen in pregnancy) is sometimes associated with oral contraceptives. Weight gain is common in women who are taking the nortestosterone derivatives. 4. Serum lipids: The combination pill causes a change in the serum lipoprotein profile: Estrogen causes an increase in HDL and a decrease in LDL (a desirable occurrence), whereas progestins may negate some of the beneficial effects of estrogen. [Note: The potent progestin norgestrel causes the greatest increase in the LDL : HDL ratio. Therefore, estrogen-dominant preparations are best for individuals with elevated serum cholesterol]. Question: Who should not use oral contraceptive pills? Women with the following conditions should not use estrogen containing birth control medications:  Allergy to any component of the product  Poorly controlled diabetes  History of blood clot disorders  Breast cancer  History of stroke or heart attack  Liver cancer (or liver disease)  Severe hypertension  Severe headaches (for example, migraines)  Diabetes that causes blood vessel problems Beneficial effect:  The combined pill markedly decreases menstrual symptoms such as irregular periods and intermenstrual bleeding.  Iron deficiency anaemia and premenstrual tension are reduced, as are benign breast disease, uterine fibroids and functional cysts of the ovaries. Progestin only pills Progestin-only birth control pills are a daily medication that contain only 1 hormone. They may be prescribed if you have side effects from other types of birth control pills  Contains very low dose of Progestin only (norethindrone or norgestrol).  Levonorgestrel 30 μg, norethisterone 350 μg, norgestrel 75 μg.  POP’s must be taken at the same time every day.  Good Candidate- Breastfeeding Woman.  May cause menstrual irregularities and ectopic pregnancy. Mode of action: MAO:  Thinning of the endometrial lining  Slowing ovum transport through ↓ed tubal motility  Thickening of the cervical mucus  Inhibition of ovulation Absolute C/I 1. Pregnancy 2. Breast cancer A/E: The most common A/E is Episodes of unpredictable spotting & breakthrough bleeding. Bidyut Chandra Paul Roll: 181318 Department of Pharmacy, PUST  Page |6 Disease Management-II BPH-5107 Women's Health Potential beneficial & unwanted effect:  Progestogen-only contraceptives offer a suitable alternative to the combined pill for some women in whom oestrogen is contraindicated, and are suitable for women whose blood pressure increases unacceptably during treatment with oestrogen.  However, their contraceptive effect is less reliable than that of the combination pill, and missing a dose may result in conception. Disturbances of menstruation (especially irregular bleeding) are common. Postcoital (Emergency) contraception Oral administration of levonorgestrel, alone (1.50 mg usually) or combined with oestrogen, is effective if taken within 72 hours of unprotected intercourse, repeated 12 hours later. 1. Yuzpe regimen: a. 2 doses of COCPs containing EE 50 µg & levonorgestrel 250µg-in 72 hrs & next after 12 hrs. b. Effective-90% 2. 2 doses of levonorgestrel 0.75mg each- 1st in 48hrs & 2nd in 12hrs. 3. Mifepristone: 600 mg once in 72 hrs. Nausea and vomiting are common. (Replacement tablets can be taken with an antiemetic such as domperidone). Recently approved in 2010, Ulipristal Acetate (SPRM) in a single oral dose of 30mg is more effective if taken in 120hrs/5days. If these measures fail, pregnancy should be terminated to avoid teratogenic deformities of fetus. Mode of action:  Either prevents or delays ovulation, prevents fertilization or prevents implantation of the fertilized egg into the uterus.  If ovulation & fertilization occurred then it prevents implantation of blastocyst.  Clinical opinion is that EHC (Emergency Hormonal contraception) is not an abortifacient. Bidyut Chandra Paul Roll: 181318 Department of Pharmacy, PUST  Page |7 Disease Management-II BPH-5107 Women's Health Common sign & symptoms i. Cystitis: Signs & symptoms often include-  A strong, persistent urge to urinate  Blood in the urine (hematuria)  A burning sensation when urinating  Passing cloudy or strong-smelling urine  Passing frequent, small amounts of urine  Pelvic discomfort  A feeling of pressure in the lower abdomen  Low-grade fever ii. Vaginal thrush: Typical symptoms of vaginal thrush include-  Itching and soreness around the entrance of the vagina (itchy labia)  Vaginal discharge – this is usually odourless and may be thick and white or thin and watery  Pain during sex, which may make you worry about having sex  A stinging sensation when peeing Sometimes the skin around the vagina can be red, swollen or cracked. Occasionally there may also be sores on the skin, although this is more often a sign of genital herpes. iii. Dysmenorrhea: Symptoms may include-  Nausea  Headaches  Vomiting  Low back pain  Diarrhea  Pain in the lower abdomen  Fatigue  Pain radiating down the legs  Weakness  Cramping in the lower abdomen  Fainting The symptoms of dysmenorrhea may look like other conditions or medical problems. iv. PMS (Premenstrual syndrome)  Headaches  Feeling upset, anxious or irritable  Breast tenderness  Tiredness or trouble sleeping  Mood swings  Spotty skin or greasy hair  Bloating or tummy pain  Changes in appetite and sex drive Document Credit, Assistant Professor Md. Kamal Hossain Ripon Department of Pharmacy (MBSTU) Bidyut Chandra Paul Roll: 181318 Department of Pharmacy, PUST