Investigation of Oral Contraceptives

Investigation of Oral Contraceptives Oral Contraceptives Made by LAB GROUP: C2 Lab Instructors: A.L/ Ahmed Refaat Spring 2015 Oral Contraception: Contraception can be defined as the method of prevention of pregnancy also referred to as Birth Control medication. Mainly contraceptives are composed of hormones thus, referred to as hormonal contraceptives they consist of synthetic sex hormones female based hormones such as estrogen or progestin. Their mechanism of action is to block the process of ovulation hence, preventing pregnancy. Methods of contraception: There are a lot of contraception methods theyre mainly divided into physical-mechanical or chemical methods. Physical-mechanical methods include: Caps: it is a thin soft silicone prevents sperm penetration by covering the cervix. Male and female condoms Contraceptive Implants: flexible and small forty mm long tube. A trained professional usually inserts the implant; it stops the release of eggs from the ovary. Diaphragms: placed inside the vagina before intercourse, it covers the cervix as well. IUD: T-shaped intrauterine device placed inside the womb by a specialized professional; it terminates sperms and eggs in the fallopian tube or womb. IUS: plastic T-shaped intrauterine system placed inside the womb by a physician, it releases progestogen (steroid) that thickens the mucus in the cervix making it impossible for a sperm to penetrate it. Vaginal ring: a plastic soft and ring shaped placed inside the vagina, releases as well progestogen with the same effects as the IUS. Natural family planning Chemical methods include: Combined pills Contraceptive patches Progestogen pill Contraceptive injection There are permanent methods of contraception such as: Vasectomy in males Sterilization or sealing of the fallopian tube in females Classification of drugs is mainly based on the type of chemical or active ingredient. Oral contraceptives are classified into 3 categories: Combination (estrogen/progestin) oral contraceptives Progestin only based oral contraceptives Effects of different oral contraceptives Oral contraceptive Drugs: Ortho Micronor (Norethindrone): Drug class: It is a First generation Progestin. It is less androgenic than second generation progestin such as levonorgestrel. Mechanism of action: Ortho Micronor is a progestin-only contraceptive oral pill. It is designed for the prevention of pregnancy by suppressing ovulation in nearly half of the users, thickening the cervical mucus to prevent sperm penetration, and the reduction of LH midcycle tops FSH, it slows the motility of the ovum altering the endometrium and the fallopian tubes. Pharmacological action: Progestin oral contraceptives are used for the prevention of pregnancy. Pharmacokinetics: Serum progesterone levels peak after oral administration in about two hours, then through distribution and rapid elimination. In 24 hours after drug intake, serum levels are close to the base line, which makes the efficiency depends on rigid adherence to the dosage. There are wide variations between individual users in serum levels. The results of the progestin administration lower the levels of serum progesterone balance and a shorter half-life of the concomitant administration with estrogens. Contraindications: Carcinoma of the breast suspected pregnancy Hypersensitivity to any component of this product liver disease Drug interactions: Thyroxine concentrations inevitably decrease eventually, because there is a decrease in main binding thyroid globulin The efficacy of pills that are progestin based only is reduced by the (HEID) or hepatic enzyme-inducing drugs for example carbamazepine, anticonvulsants phenytoin, and the antituberculosis drug rifampin and barbiturates. Side-effects: Vomiting, Nausea, bloating, Vaginal bleeding, headache Plan B (levonorgestrel): Drug class: Second Generation progestin. Used worldwide and FDA approves as plan B. It has high androgenic effects. Pharmacokinetics: No particular examination of irrefutably for the bioavailability of plan B (levonorgestrel) in people has been directed. Be that as it may, writing demonstrates that levonorgestrel is quickly and totally assimilated after oral organization (bioavailability around 100%) and is not subject to first pass digestion system. After a solitary measurements of Arrangement plan B (levonorgestrel) (0.75 mg) regulated to 16 ladies under fasting conditions, greatest serum centralizations of levonorgestrel are 14.1  ± 7.7 ng/mL (mean  ± SD) at a normal of 1.6  ± 0.7 hours. Pharmacological action: Plan B is proposed to avert pregnancy after known or suspected prophylactic disappointment or unprotected intercourse. Mechanism of action: Crisis contraceptives are not successful if the lady is now pregnant. Plan B (levonorgestrel) is accepted to go about as a crisis prophylactic essentially by avoiding ovulation or preparation (by modifying tubal transport of sperm and/or ova). Whats more, it may hinder implantation (by modifying the endometrium). It is not successful once the methodology of implantation has started. Side effects: Nausea Headache Breast tenderness Fatigue Vomiting Abdominal pain Diarrhea Contraindications: It is not prescribed for utilization in the accompanying conditions: Known or suspected pregnancy Hypersensitivity to any segment of the drug Drug interactions: Hypothetically, the adequacy of low-measurement progestin-just pills is diminished by hepatic catalyst instigating medications, for example, the anticonvulsants carbamazepine, phenytoin, anti- tuberculosis and barbiturates. Yasmin (drospirenone/ethinyl estradiol): Drug class: Third generation oral contraceptive. It is mostly disliked due to dangerous side effects. Pharmacokinetics: Irrefutably the bioavailability of DRSP from a solitary element tablet is around 76%. Unquestionably the bioavailability of EE is pretty nearly 40% as a consequence of presystemic conjugation and first-pass digestion system. Indisputably the bioavailability of Yasmin, which is a mix tablet of EE and DRSP, it has not been assessed. Serum convergances of DRSP and EE arrived at top levels inside 1-2 hours after organization of Yasmin. Pharmacodynamics: Pharmacodynamic studies were not conducted specifically with Yasmin. Therapeutic use: Yasmin is demonstrated for utilization by ladies to avert pregnancy. Mechanism of action: COCs bring down the risk of getting to be pregnant basically by smothering ovulation. Other conceivable components may incorporate cervical bodily fluid changes that restrain sperm entrance and endometrial changes that decrease the probability of implantation. Side effects: Irregular uterus bleeding Headache Nausea Liver disease Breast tenderness Contraindications: Dont endorse Yasmin to ladies who are known to have the accompanying: Renal impedance Adrenal deficiency Hypertension Have breast cancer Have coronary vein illness Have thrombogenicvalvular or thrombogenic mood illnesses of the heart (for instance, subacute bacterial endocarditis with valvular malady, or atrial fibrillation) Have Diabetes mellitus Drug interactions: Substances reducing the viability of COCs: Medications or home grown items that incite certain chemicals, including cytochrome P450 3A4 (CYP3A4), may diminish the adequacy of COCs or build achievement dying. Effects of Joined Oral Contraceptives on Different Medications COCs containing EE may hinder the digestion system of different mixes. Potential to Build Serum Potassium Focus: There is a potential for an increment in serum potassium fixation in ladies bringing Yasmin with different medications. Mircette (desogestrel/ethinyl estradiol and ethinyl estradiol): Second generation Mechanism of action: The mechanism of action of it works over four directions: suppression of the gonadotropins alteration changes in the mucus which make it hard and difficult to the sperm to entire the uterus The endometrial changes that reduce the likelihood of the implantation process inhibition of ovulation from happening Pharmacokinetics: The substance desogestrel is completely and fast absorbed then converted to the active form which is etonogestrel after taking the oral route of administration the bioavailability was measured and found approximately 100%; by taking serum levels of etonogestrel . Therapeutic uses: It is used to prevent the pregnancy. Side effects: Vomiting Gastrointestinal symptoms (such as abdominal cramps and bloating) Nausea problems in menstruation process Breast changes:, enlargement, tenderness , and secretion Contraindications: Past problems concerning deep vein Thrombophlebitis  or thromboembolic disorders If there is any predication for breast carcinoma or current one Drug interactions: Increase in factors ix ,vii,viii,x and prothrombin levels this will cause increase in nor adrenline induced platelets aggregation Increase in other binding proteins in serum levels Increase in the levels of thyroid binding globulin References: Contraceptives. (2015, February 17) Drugs.com Available at:  http://www.drugs.com/drug-class/contraceptives.html (Accessed: 5 March 2015) Contraception. Division Of Reproductive Health. (2015, February 24) CDC Available at: http://www.cdc.gov/reproductivehealth/unintendedpregnancy/contraception.htm  (Accessed: 5 March 2015) Types Of Oral Contraceptives. (2010, December 12) OralContraceptives.com Available at: http://www.oralcontraceptives.com/about_types.asp (Accessed: 5 March 2015) Contraception Guide. (2015, February 2) nhs.uk Available at: http://www.nhs.uk/Conditions/contraception-guide/Pages/contraception.aspx  (Accessed: 5 March 2015) Plan B. (2007, May 24) rxlist.com (Drug index) Available at:  http://www.rxlist.com/plan-b-drug.htm  (Accessed: 5 March 2015) Yasmin. (2012, April 23) rxlist.com (Drug index) Available at:  http://www.rxlist.com/yasmin-drug.htm  (Accessed: 5 March 2015) Ortho Micronor. (2008, July 24) rxlist.com (Drug index) Available at: http://www.rxlist.com/ortho-micronor-drug.htm  (Accessed: 12 March 2015) Mircette. (2012, July 27) rxlist.com (Drug index) Available at:  http://www.rxlist.com/mircette-drug.htm (Accessed: 12 March 2015)