DRM SCIENCE LECTURE 2 CONTRACEPTIVES AND IUDs

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Dr. RAGHU PRASADA M S MBBS,MD ASSISTANT PROFESSOR DEPT. OF PHARMACOLOGY SSIMS & RC. :

Dr. RAGHU PRASADA M S MBBS,MD ASSISTANT PROFESSOR DEPT. OF PHARMACOLOGY SSIMS & RC. CONTRACEPTIVES AND INTRA UTERINE DEVICES

ORAL CONTRACEPTIVES:

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.

Mechanism of OCPs:

Mechanism of OCPs 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 so that they cannot effectively move eggs toward the uterus

Mechanism of OCPs:

Mechanism of OCPs

Available Dosage forms:

Available Dosage forms Birth control(contraceptive ) medications contain hormones (estrogen and progesterone or progesterone alone ). 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

Menstrual hormones:

Menstrual hormones

OCPs:

OCPs Estrogens- Ethinyl estradiol-30 micro grams Mestranol-50 micro grams Progesterones Norethindrone - 1mg Norethindrone acetate Norgestimate Desogestrel 150 micro grams Norgestrel -0.5mg Levonorgestrel 150 micro grams

Hormone-Containing Contraceptives:

Hormone-Containing Contraceptives Combination contraceptives, that is, contraceptive medications containing both estrogen and progesterone, are the most effective means for contraception with the exception of surgical sterilization. Several types of combination birth control pills exist, including monophasic pills, biphasic pills, triphasic pills, and 91-day-cycle pills.

Post-coital- morning after pill:

Post-coital- morning after pill Two tablets of progestin levonorgestrol containing 1500mg Or single 1500mcg tablet taken as soon as possible after unprotected intercourse (up to 72 hours after) Preferably within 12 hours, no later than 72 hours Ethinyl estradiol 50 micro gram+ levonorgestrol 250 micro gram. Two such tablets are to be taken with in 72 hrs of unprotected sex Ulipristal (SPRM-Selective Progesterone Receptor Modulator) single dose 30mg effective with in 120hrs/5days

Centchroman -SAHELI:

Centchroman -SAHELI Non steroidal estrogen receptor antagonist- serm Centchroman - 30mg twice in a week for first 3month and once in a week subsequently as long as the contraception is preferred Reversible in 6 months It is potent competitive antagonist at peripheral estrogen receptors and supresses proliferative stage of endometrium It accelerates ovum transport, without affecting ovulation No risk of teratogenesis C/I- hepatic dysfunction, polycystic ovarian disease, cervical hyperplasia, tuberculosis, renal disease

Injectable Contraceptives:

Injectable Contraceptives Depot medroxy progesterone acetate ( Depot-Provera ) -DMPA The first injection is given within 5 days following the onset of menstruation. After that, an injection is needed every 11-13 weeks.   Side effects: Since progesterone is the only hormonal ingredient, estrogen-related side effects are avoided . A side effect unique to this method of birth control is that most women eventually stop having their periods. Depo-Provera may last in the body for several months in women who have used it on a long-term basis and can actually delay the return to fertility after stopping the drug . Other side effects include weight gain and depression.

Topical Contraceptive Patch:

Topical Contraceptive Patch Norelgestromin / ethinyl estradiol The topical patch may be applied to clean, on the shoulders, upper arms, buttocks or abdomen. The patch may be less effective in women weighing more than 198 pounds (90 kg). Use: A new patch is applied on the same day of the week, each week for 3 weeks in a row. The first patch is applied either on the first day of the menstrual period or on the Sunday following menses . On the fourth week, no patch is applied. This 4-week period is considered 1 cycle. Another 4-week cycle is started by applying a new patch following the 7-day patch-free period.

Side effects:

Side effects Side effects are similar to other birth control agents containing both estrogen and progesterone. Effects include menstrual irregularities, weight gain, and mood changes. Other specific side effects include a skin reaction at the site of application and problems with contact use

Progesterone-Only Pills:

Progesterone-Only Pills Norethindrone Progesterone-only pills (POPs), also known as mini-pills. Less than 1% of users of oral contraceptives use them as their only method of birth control. Those who use them include women who are breast feeding and women who cannot take estrogen . Use : POPs are ingested once daily, every day. POPs may be started on any day, and there are no pill-free days or different-colored pills to track. Since progesterone is the only hormonal ingredient, estrogen-related side effects are avoided. However , since POPs do not include estrogen, they have a higher failure rate. Users must take this pill at the same time daily for greatest effectiveness.

Contra indications:

Contra indications Women with the following conditions should not use estrogen-containing birth control medications: to any component of the product History of blood clotting disorders History of stroke or heart attack heart valve disease with complications Severe hypertension Poorly controlled diabetes Recent major surgery with prolonged bed rest Breast cancer, Liver cancer (or liver disease) Uterine cancer or other known or suspected estrogen-dependent cancers jaundice during pregnancy or jaundice with prior hormonal contraceptive use  

Drug Interactions:

Drug Interactions The effectiveness of oral contraceptives, Progesterone Only Pill and post coital pill will be reduced by interaction with drugs that are enzyme inducers Drugs that may cause this effect include: many antibiotics (e.g., cephalosporins , chloramphenicol, macrolides, penicillins , tetracyclines, sulfas), aprepitant , bexarotene , Broad spectrum antibiotics may reduce effectiveness of OCPs by altering the bacterial flora of the bowel

Side effects:

Side effects Nausea, breast tenderness, fluid retention , weight gain, acne, breakthrough bleeding , missed periods, headaches, depression, change in vision, other mood changes, and lower sexual desire . Additionally, the following more serious side effects may occur: thromboembolism (blood clots ) Breast cancer, cervical cancer Benign liver tumors Diabetes

Precautions :

Precautions Smoking cigarettes while using this medication increases your chance of having heart problems. Do not smoke while using this medication. The risk of heart problems increases with age (especially in women greater than 35 years of age) and with frequent smoking (15 cigarettes per day or greater) May experience vaginal bleeding.

Non contraceptive uses:

Non contraceptive uses Menstrual Bleeding Disorders Dysmenorrhea Symptoms of Androgenisation (Seborrhea, Acne, Hirsutism, Alopecia) Premenstrual Syndrome (PMS) and Premenstrual Disphoric Disorder ( PMDD ) Ovarian Cysts Endometriosis/ Adenomyosis Pelvic Inflammatory Disease (PID) Multiple Sclerosis Menstrual Migraine Endometrial Hyperplasia Benign Breast Disease Prevention of Ovarian Cancer Endometrial Cancer Colon Cancer

Slide20:

IUD’s are medicated or non-medicated devices which exerts it’s contraceptive action in the uterine cavity continuously for a prolonged period of time without requiring patients motivation. An IUD prevents sperm from meeting an egg. An IUD may stop a fertilized egg from growing inside the uterus. INTRA UTERINE DEVICES-IUDs

Slide21:

1 . Non-medicated IUD’s : Contraceptive action by producing sterile inflammatory response in Endometrium. These are available in ring shaped IUD’s made up of s.s and plastic fabricated form polyethylene, polypropylene. 2. Medicated IUD’s: - Copper IUD’s - Progesterone releasing IUD’s INTRA UTERINE DEVICES-IUDs

IUDs:

IUDs Most common: T-shaped, copper bands on plastic stem/arms Inserted in uterus through vagina and cervical opening Strings: assure IUD is in place; facilitate removal Most common copper IUD: TCu-380A Less common: hormonal IUDs

Copper T IUD:

Copper T IUD Primary mechanism is prevention of fertilization Reduce motility and viability of sperm Approved for 10 years of use but can be removed any time Prevents fertilization by: Impairing the viability of the sperm I nterfering with sperm movement

Copper T IUD:

Copper T IUD Copper is known to be cytotoxic in high concentration it enhances the spermatocidal and spermato depressive action of an IUD. The copper concentration in endometrial epithelium and superficial stromata inhibits the binding of steroids of their receptors. Cupric ion inhibits the binding of 17- β - estradiol to human endometrial cytosol. Cupric ions shows only little effect on sperm motility. Copper wire was also “Blastocystocidal”.

Slide26:

A copper bearing IUD was reported to produce significant effects like: Increased alkaline phosphate activity in uterine fluids and endometrium tissue. No change of acid phosphate activity in uterine fluid but its concentration in endometrium tissue increases. Copper T IUD

Copper IUDs: Advantages:

Copper IUDs: Advantages Highly effective and very safe Does not interfere with intercourse Easy to use Long lasting Easily reversible Quick return to fertility No systemic effects Complications are rare

Ring and Patch for Continuous/Extended Use:

Ring and Patch for Continuous/Extended Use The contraceptive ring can be left in for 4 weeks and replaced immediately with another ring. The patch can be used for more than 3 consecutive weeks. (“apply new patch each week x 9 weeks…”)

:

T-shaped piece of plastic that releases Small amounts of levonorgestrel each day Primary mechanisms: inhibits sperm movement , progestin thins the endometrial lining , thickens cervical mucus Typically does not prevent ovulation ( low systemic levels of progesterone ) Approved for 5 years of use: remove any time, immediate return to fertility Levonorgestrel IUD

Copper IUDs-Disadvantages:

Copper IUDs-Disadvantages Side effects, including cramping and increased or prolonged bleeding Rare complications include perforation and pelvic inflammatory disease Method failure can lead to ectopic pregnancy (extremely rare) Insertion and removal require trained provider No STI/HIV protection Side effects are most common during the first 3 months.

IUDs – Pelvic Inflammatory Disease (PID):

IUDs – Pelvic Inflammatory Disease (PID) Risk of PID in IUD users: Low overall risk of PID attributable to IUD is 0.15% to 0.30% Higher during first 20 days after insertion Due mostly to presence of gonorrhea or chlamydia at time of insertion Similar to risk of PID in women with gonorrhea and chlamydia who are not using IUD

IUDs – Reducing the Risk of PID:

IUDs – Reducing the Risk of PID Do not insert IUD if: at high individual risk of STIs, or clinical symptoms and signs of an STI are present Follow infection prevention procedures during insertion Recommend follow-up visit at 3 to 6 weeks to check for infection Return immediately if any symptoms of PID develop Source: WHO, 2004; updated 2008.

IUD Myths:

IUD Myths IUDs: Are not abortificients Do not cause infertility Do not cause discomfort for the male partner Do not travel to distant parts of the body Are not too large for small women

IUDs for women:

IUDs for women

Slide35:

Very effective with nothing to remember for up to 7 years. “Are you looking for a method that is easy to use effectively?” Side-effects : see page IM3. For STI/HIV/AIDS protection, also use condoms. Norplant Implants 6 small plastic tubes placed under skin of upper arm Heavy women may need them removed after 4 or 5 years (see page IM4). Another set of capsules can be inserted if client wants to continue using implants. Can get pregnant soon after capsules are taken out. Very effective Last up to 7 years, depending on your weight Very safe Usually change monthly bleeding No protection against STIs or HIV/AIDS Implants Implants are not harmful for health. They do not bother her or affect strength. For breastfeeding women, they do not affect the quality of breastmilk. Check for concerns, rumours: “What have you heard about implants?” Explain common myths. Capsules do not break inside the body. They are bendable. (Also see Appendix 10.) About Norplant implants: Contain progestogen but not estrogen hormones. Work mainly by thickening the cervical mucus and by stopping ovulation (see Appendices 4 & 5) . Soft capsules that are just visible under the skin. Do not leave noticeable scar if inserted and removed correctly. Inserted and removed by trained personnel in simple surgical procedure.

Single-rod contraceptive implant:

Single-rod contraceptive implant One 4cm x 2mm rod Contains progestin and no estrogen Suppresses ovulation and thickens cervical mucus Highly effective for 3 years Not user dependent and only 1 visit Very discreet and rapidly reversible Can be used during lactation

Slide37:

Effectiveness of methods Oral contraceptives Percentage of women pregnant in first year of use Rate during typical use Rate during perfect use Female condom Female sterilization Implants DMPA Spermicides Standard Days Method Male condom IUD (TCu-380A) 0 10 15 20 25 5 30

Spermicides :

Sperm-killing substances inserted deep in the vagina, near the cervix, before sex. − Nonoxynol-9 is most widely used. − Others include benzalkonium chloride, chlorhexidine , menfegol , octoxynol-9, and sodium docusate. Available in foaming tablets, melting or foaming suppositories, cans of pressurized foam, melting film, jelly, and cream. − Jellies, creams, and foam from cans can be used alone, with a diaphragm, or with condoms. − Films, suppositories, foaming tablets, or foaming suppositories can be used alone or with condoms. Work by causing the membrane of sperm cells to break, killing them or slowing their movement. This keeps sperm from meeting an egg. Spermicides

Spermicides :

Spermicides Do not reduce vaginal secretions or make women bleed during sex. Do not cause cervical cancer or birth defects. Do not protect against STIs. Do not change men’s or women’s sex drive or reduce sexual pleasure for most men. Do not stop women’s monthly bleeding

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