Investigation of Oral Contraceptives

Investigation of Oral ContraceptivesOral ContraceptivesMade byLAB GROUP C2Lab Instructors A.L/ Ahmed RefaatSpring 2015Oral ContraceptionContraception 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 lie in of synthetic sex hormones female based hormones such as estrogen or progestin. Their mechanism of achievement is to block the process of ovulation hence, preventing pregnancy.Methods of contraceptionThere are a lot of contraception methods theyre mainly divided into physical-mechanical or chemical methods. Physical-mechanical methods includeCaps it is a thin soft silicone prevents sperm penetration by covering the cervix.Male and female condomsContraceptive Im intendts flexible and small forty mm long tube. A trained professional usually inserts the implant it bread the release of eggs from the ovary.Diaphragms placed inside the va gina before intercourse, it covers the cervix as well.IUD T- influence 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 planningChemical methods includeCombined pillsContraceptive patches progestin pillContraceptive injectionThere are permanent methods of contraception such asVasectomy in malesSterilization or sealing of the fallopian tube in femalesClassification of drugs is mainly based on the type of chemical or active ingredient. Oral contraceptives are classified into 3 categoriesCombination (estrogen/progestin) oral examination contraceptivesprogestoge n only based oral contraceptivesEffects of different oral contraceptivesOral contraceptive DrugsOrtho Micronor (Norethindrone)Drug classIt is a First generation Progestin. It is less androgenic than second generation progestin such as levonorgestrel.Mechanism of actionOrtho 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 round tops FSH, it slows the motility of the ovum altering the endometrium and the fallopian tubes.Pharmacological actionProgestin oral contraceptives are used for the prevention of pregnancy.PharmacokineticsSerum progesterone levels peak after oral administration in about two hours, thence 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 trammel to the dosag e. 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.ContraindicationsCarcinoma of the breast venture pregnancyHypersensitivity to any component of this productliver diseaseDrug interactions Thyroxine concentrations inevitably decrease eventually, because on that point is a decrease in main binding thyroid globulinThe 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 vomitive, Nausea, bloating, Vaginal bleeding, headachePlan B (levonorgestrel)Drug class Second Generation progestin. Used worldwide and FDA approves as plan B. It has high androgenic effects.PharmacokineticsNo particular examination of irrefutably for the bioavail ability 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) correct 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 actionCrisis contraceptives are not thriving 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 o nce the methodology of implantation has started.Side effectsNausea chafe converge tendernessFatigueVomitingAbdominal painDiarrheaContraindicationsIt is not prescribed for utilization in the accompanying conditionsKnown or suspected pregnancyHypersensitivity to any segment of the drugDrug interactionsHypothetically, 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.PharmacokineticsIrrefutably the bioavailability of DRSP from a solitary element tablet is around 76%. Unquestionably the bioavailability of EE is passably 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 n ot been assessed. Serum convergances of DRSP and EE arrived at top levels inside 1-2 hours after organization of Yasmin.PharmacodynamicsPharmacodynamic studies were not conducted specifically with Yasmin.Therapeutic useYasmin is demonstrated for utilization by ladies to avert pregnancy.Mechanism of actionCOCs bring exhaust the risk of getting to be pregnant basically by smothering ovulation. Other conceivable components may incorporate cervical bodily fluid changes that tighten sperm entrance and endometrial changes that decrease the probability of implantation.Side effectsIrregular uterus bleedingHeadacheNauseaLiver diseaseBreast tendernessContraindicationsDont endorse Yasmin to ladies who are known to have the accompanyingRenal impedanceAdrenal deficiencyHypertension grant breast cancerHave coronary vein illnessHave thrombogenicvalvular or thrombogenic mood illnesses of the heart (for instance, subacute bacterial endocarditis with valvular malady, or atrial fibrillation)Have Dia betes mellitusDrug interactionsSubstances trim down 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 addition in serum potassium fixation in ladies bringing Yasmin with different medications.Mircette (desogestrel/ethinyl estradiol and ethinyl estradiol) Second generation Mechanism of actionThe mechanism of action of it whole works over four directionssuppression of the gonadotropinsalteration changes in the mucus which make it hard and difficult to the sperm to entire the uterusThe endometrial changes that reduce the likeliness of the implantation processinhibition of ovulation from happeningPharmacokineticsThe 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 usesIt is used to prevent the pregnancy.Side effectsVomitingGastrointestinal symptoms (such as abdominal cramps and bloating)Nauseaproblems in menstruation processBreast changes, enlargement, tenderness , and secretionContraindicationsPast problems concerning deep vein Thrombophlebitisor thromboembolic disordersIf thither is any predication for breast carcinoma or current oneDrug interactionsIncrease in factors ix ,vii,viii,x and prothrombin levels this will cause increase in nor adrenline induced platelets aggregationIncrease in other binding proteins in serum levelsIncrease in the levels of thyroid binding globulinReferencesContraceptives. (2015, February 17) Drugs.com for sale athttp//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 athttp//www.rxlist.com/plan-b-drug.htm(Accessed 5 March 2015)Yasmin. (2012, April 23) rxlist.com (Drug index) Available athttp//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 athttp//www.rxlist.com/mircette-drug.htm (Accessed 12 March 20 15)