MonoNessa

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MONONESSA

Student’ name

is a combined oral contraceptive that contains two femalehormones estrogen and progestin. This drug is used to preventpregnancy through three main mechanisms. The first mechanism involvesthe prevention of ovulation during the menstrual cycle. The secondmode of action involves preventing the penetration of spermatozoainto the uterus to reach the eggs in the oviduct through thickeningof the vaginal fluid. In the third mechanism, initiatessome changes in the lining of the uterus to prevent attachment offertilized egg. This paper explores various pharmacological aspectsof .

Brand andgeneric names

is abrand name of this combined oral contraceptive. Other brand namesinclude Ortho-Cyclen, Ortho Tri-Cyclen, Orth Tri-Cyclen Lo, andSprintec. The generic name is Norgestimate-Ethinyl Estradiol (ActavisPharma Inc., 2015).

Pharmacokinetics

Pharmacokineticsis used to study how a given drug is absorbed into, distributedwithin and eliminated from the body. is administered orallyand swallowed. It is absorbed into the bloodstream through the wallsof the gastrointestinal tract. The drug is composed of norgestimateand ethinyl-estradiol. Most of the drug is absorbed in the smallintestines because it has larger surface area compared to the stomach(Jeske A. H. 2013). is actively absorbed into thecirculation. The metabolites of norgestimate and ethinyl-estradiol(EE) reach their highest plasma concentrations within a period notmore than 2 hours. The drug attains its steady-state plasmaconcentration by the seventh day of every dosing cycle.

Distribution isreferred to as the process by which drug metabolites are transportedto their target cells through the circulatory system. Thedistribution of drug metabolites is affected by various factors. Inthe case of , distribution is significantly enhanced by itsmolecular size and protein binding ability (Jeske A. H. 2013). Therate of distribution is higher when the molecular size of themetabolites is small like the case of . Norelgestromin andnorgestrel are the metabolites of norgestimate, and they bind toplasma proteins by 97%. Norelgestromin binds to albumin only.Norgestrel mainly binds to sex hormone binding globulin (SHBG) butcan also bind to plasma albumin. The binding of EE to plasma albuminresults in an increase in the plasma concentration of SHBG.Norgestimate undergoes first pass metabolism. Norelgestromin is themain metabolite of norgestimate after the metabolism in the smallintestines (Kennedy, Parker &amp Lott, 2014). Hepatic metabolismresults in active norgestrel and hydroxylated and conjugatemetabolites. EE is metabolized through hydrolytic and conjugationreactions. The conjugates of EE include glucuronate and sulfateproducts. The metabolites of norgestimate and EE are eliminated fromthe body through renal (45%) and fecal (35%) pathways. Onlymetabolized norgestimate is excreted by the renal pathway.

Pharmacodynamics

Pharmacodynamicsis described as the study of the effects of a drug and its mode ofaction in the body. Norgestimate is the synthetic form of the femalesex hormone known as progesterone. The ovary produces progesteroneafter ovulation. Therefore, it prevents subsequent ovulation andinitiates the thickening of the uterus. Fall in the level ofprogesterone in the body when implantation does not take placeinitiates another ovulation. Norgestimate mimics progesterone. When awoman in her productive age takes , norgestimate interfereswith the menstrual cycle by ensuring high concentrations of thesynthetic progesterone. In order to prevent ovulation, norgestimatebinds to progesterone and androgen receptors in the female gonad,mammary glands, hypothalamus and the pituitary glands. The bindinginterferes with the stability of the receptor membrane andinactivates specific hormone-responsive genes in the nucleus. Thisreduces the rate of secretion of the gonadotropin-releasing hormoneby the hypothalamus. Therefore, the release of luteinizing hormone(LH) is slowed down. Low concentration of LH delays maturation andrelease of an ovum.

Indications

is usedas oral contraceptives to prevent pregnancy as a method of birthcontrol in women.

Contraindications

Women with thefollowing conditions are not recommended to use due to therisks involved (Grossman et al. 2011):

  • Thromboembolic disorders

  • Displaying thromboembolic conditions

  • Current or history of cerebral vascular disease

  • Coronary heart disease

  • Persistent blood pressure of more than 160mm Hg (systolic) and more than 100 mg Hg diastolic

  • History of deep vein thromboembolic disorders

  • Diabetes with vascular involvement

  • Endometrial carcinoma and known or signs of estrogen-dependent neoplasia

  • Headaches with focal neurological symptoms

  • Women who have had major surgery involving prolonged immobilization

  • Confirmed or suspected breast carcinoma or personal history of breast cancer.

  • Abnormal genital bleeding

  • History of cholestatic jaundice or jaundice caused by using pills

  • Hepatic adenomas or carcinomas

  • Hypersensitivity to any component of

  • Confirmed or suspected pregnancy

  • Acute and chronic hepatocellular disease associated with malfunction of the liver

  • Smoking at the age of 35 and above

  • Inherited or acquired hyper-coagulopathies

Side effects

pillsmay have some side effects on the women who use it. However, theusers of the drug should seek emergency medical assistance when theyexperience any allergic reaction presented in the form of hives,breathing difficulties, and swelling of the face, lips, the tongue orthroat. Common side effects of include:

  • Nausea and vomiting

  • Breasts become tender

  • Loss of scalp hair

  • The facial skin darkens

  • May have headaches and become dizzy and nervous

  • Experience difficulties in vision when wearing contact lenses

  • Appetite or weight changes

  • Irregular monthly period

  • Vaginal spotting

  • Vaginal discharge and itching

  • Rash

Adverseeffects

There are casesthat require women to stop using and seek help from adoctor. Users should stop using when they experience any ofthe following conditions:

  • Signs of stroke such as sudden numbness or body weakness, sudden severe headache, slurred speech, and difficulties in vision and body balance

  • Blood clot in the lungs which is exhibited by signs such as chest pain, sudden cough, wheezing sound, breathing faster and coughing blood

  • Symptoms of heart attack

  • Liver problems

  • Change in the pattern or severity of migraine headaches

  • Hand, ankle or feet swelling

  • A breast lump

  • Signs of depression

Other adverseeffects of include:

  • Clotting of blood within blood vessels of the eye

  • Absence of monthly periods

  • Bleeding that is not associated with menstrual cycle

  • Gallbladder disease

  • Body weakness

  • Gallstones

  • Giant hives

  • Hepatitis

  • Increased levels of triglycerides in the blood

  • Vaginal inflammation or infection

  • Pancreatitis

  • Pain and sudden loss of vision while moving the eye

  • Yellowing of the eye or skin caused by bile flow problems

  • High blood pressure

  • Musculoskeletal disorders such as muscle spasms, pain in extremity and myalgia

  • Ovarian cyst, vulvovaginal dryness or suppressed lactation

Patientvariables

Pregnancy

isassociated with little or no risk of birth defects in women whoinadvertently use it during the early stages of pregnancy. There isno increased risk of having genital or non-genital birth problemswhen women are exposed to low dose of before conceiving orin the early stages of pregnancy. However, the drug is notrecommended for inducing withdrawal bleeding as a way of testingpregnancy or to treat threaten or habitual abortion (ActavisPharmacy, 2015).

Nursing mothers

Nursing mothersare required to use other methods of birth control until they haveweaned their children. Traces of the components of arepresent in the milk of lactating mothers and they may lead to adverseeffects such as breast enlargement and jaundice on the child. The useof in lactating mothers may result in the decrease in thequality and quantity of breast milk.

Pediatric use

is safeand effective for women in their reproductive age as well as inpostpubertal adolescents below and above the age of 16.

Geriatric use

The safety andefficacy of this drug have not been confirmed in women at the age ofover 65 years. Furthermore, it is not indicated for women in thispopulation.

Off-label uses

The combined oralcontraceptive can be used in treating some gynecologic conditions. may be used in managing irregular menstrual cycles,reducing flow, and controlling dysmenorrhea. Since this combined oralcontraceptive reduces circulating androgens, it can benefit womenwith polycystic ovarian syndrome. The use of the COC may improvepremenstrual symptoms.can also benefit older women whoexperience an ovulatory cycles that are characterized by heavybleeding. It can also help in alleviating other perimenopausalsymptoms (Lynna Y. L. &amp Joan E. 2012). Other conditions that canbe managed using include endometriosis, hirsutism, andmenorrhagia.

References

Actavis Pharma Inc. (2015), , retrieved fromhttp://medlibrary.org/lib/rx/meds/-2/on 24 August 2016

Grossman et al. (2011), Contraindications to Combined OralContraceptives Among Over-the-Counter Compared With PrescriptionUsers, Obstetrics and Gynecology, 117(3), 558.

Jeske A. H. (2013), Mosby`s Dental Drug Reference, ElsevierHealth Sciences

Kennedy, B. J., Parker, D., &amp Lott, R. S. (2014).&nbspCapstonePharmacy Review. Burlington, MA: Jones &amp Bartlett Learning.

Kimble T., Thurman A. &amp Scharwtz J. (2011), Currently availablecombined oral contraception, Expert Review of Obstetrics &ampGynecology, Volume 6, Issue 5

Lynna Y. L. &amp Joan E. (2012), Maternity Nursing Care,Cengage Learning

PubChem, NORGESTIMATE, retrieved fromhttps://pubchem.ncbi.nlm.nih.gov/compound/norgestimate#section=Topon 21 August 2016

Mononessa

  • Uncategorized

MONONESSA 1

  1. Generic Name And Brand Name(S)

Birth controlis a method used by men and women to avoid pregnancy after sexualintercourse. Various methods of birth control include the use ofcontraceptives. The use of oral contraceptives is a safe andefficient approach to preventing pregnancy. The drugs are used bymillions of women in the United States and all over the world(Goodman et al., 2011).

isa brand name for an estrogen and progesterone contraceptive commonlyemployed in the prevention of pregnancy or as a treatment for acne.The generic name of the contraceptive is Ethinylestradiol-norgestimate.The common name of the medicine represents the combination of femalehormones that prevent ovulation (Stegeman et al., 2013). Estradiolrepresents the type of estrogen contained in female sex hormonesproduced by the ovaries. On the other hand, Norgestimate is a form ofprogesterone produced by the female body to regulate menstruation andovulation (Trung &amp Jensen, 2014). The combination of the twohormones is used to treat symptoms such as hot flashes, burningvagina, dryness, and irritation that occur on the onset of menopause.The medicine causes several changes in a woman’s cervical mucus aswell as the uterine lining. Such changes make it hard for the spermto access the uterus as well as for the fertilized egg to attach tothe uterus ( (28), 2016).

2.Pharmacokinetics

contains the norgestimate (NGM) and the Ethinyl estradiol (EE)hormones that are rapidly absorbed after they are swallowed throughthe mouth. Mechanisms in the intestines metabolize the Norgestimatehormone into norgestrel (NG) and norelgestromin (NGMN) (Patel et al.,2015). The two hormones are the key active metabolites fornorgestimate. The norgestimate reaches a peak serum concentrationwithin the first two hours after the administration of mononessa. Amultiple dosing of 250 mcg of norgestimate per 35-mcg dose isconsidered two-fold for both the norelgestromin and estradiol incomparison to a single dose of administration. The absorption ofnorgestimate is proportional after the administration of 180mcg to250 mcg of norelgestromin. The estradiol hormone reaches a steadystate of concentration in the body after 7 days of continuous dosingcycle (Wahl, 2014). The two hormones achieve steady state levels ofnorgestimate and norgestrel after 21 days. Norgestrel assumes anon-steady rate of accumulation at approximately 8 times more due tothe high-affinity connections to the sex chemicals binding globulin(SHBG) that limits the hormones biological activity (Jensenet al.,2013).

3.Pharmacodynamics

The Estrogenslower the possibilities of becoming pregnant by suppressing ovulationin the female body. The hormones also use the cervical mucusmechanisms to inhibit the sperm`s penetration as well as endometricalchanges that reduce the chances of egg implantation (Goodman et al.,2011). The Estrogens interact with the protein receptors located inthe target in the female reproductive tract, hypothalamus, thepituitary and mammary glands. Afterward, the estrogens enhance thesynthesis of hepatic hormones such as the thyroid-binding globulin(TBG), sex hormone binding globulin (SHBG) to suppress the folliclestimulating hormone (FSH) produced by the anterior pituitary. Thecombinations of estrogens and progestin suppress thehypothalamic-pituitary system and hamper the secretion ofgonadotropin-releasing hormone (GnRH) (Stegeman et al., 2013).

4.Indications

isused in the deterrence of pregnancy in females who choose to use oralcontraceptives as an approach to contraception. Oral contraception isa highly effective method of pregnancy prevention. The chances ofgetting pregnant depend on how well the user follows the directionsfor taking the birth control pills. The better a person follows theinstructions, the lower the chances of getting pregnant. According toclinical studies, one in every one hundred women who use Ethinylestradiol-norgestimate may get pregnant during their first year ofuse (Trung &amp Jensen, 2014).

5.Contraindications

The use oforal contraception approaches is associated with heightened risks ofsevere infections such as myocardial infarction, stroke, hepaticneoplasia, thromboembolism and gallbladder disease. However, therisk of death is lower in healthy women without the underlying riskfactors (Patel et al., 2015). The risk of morbidity increases in thepresence of other factors such as hyperlipidemia, obesity, diabetesand hypertension. Cigarette smoking increases the chances ofcardiovascular events from the combination of various contraceptives.The risk increases with age and specifically among women aged over 35years old as well as the number of cigarettes smoked. Consequently,women above the age of 35 years should not combine withother contraceptives (- norgestimate and Ethinyl estradiol,2015).

6.Side-effects

The use ofmononessa is associated with irregular vaginal bleeding or spottingwhile taking the pills. The bleeding may vary from experiencingslight stains between the menstrual periods to intense bleedingsimilar to that experienced during normal periods. Irregular bleedingoccurs temporarily and does not serve as a sign to any seriousproblems. Users are advised to take their pills on schedule andmonitor for any prolonged bleeding (- norgestimate andEthinyl estradiol, 2015).

Second, theuse of the drug results to fluid retention or edema. The userexperiences swelling in the fingers and ankles. It also causes a risein the blood pressure. Users are advised to consult their healthprofessionals after experiencing edema. also results to thepersistent darkening of the skin or Melasma (Jensenet al., 2013).

Other sideeffects related to the administration of the drug include vomiting,nausea, diarrhea, constipation, low appetite, nervousness, headache,dizziness, muscle cramps, loss of scalp hair, vaginal infections,vertigo, pancreatitis, urinary tract and vaginal infections and skinsensitivity to the sun (Wahl, 2014)..

7.Adverse effects

The principalnegative effects of the disease include the development of bloodclots caused by the blockage of blood vessels. Blood clots aredetrimental and can result in severe disability or death. Most of theclotting occurs in the legs and results to thrombophlebitis.Additional clotting can block the vessels carrying blood to thelungs. Sometimes, the clots can occur in the blood vessels of the eyeresulting in double vision, impaired visualization or blindness(Wahl, 2014).

Second, theuse of mononessa can increase the risk of heart attacks and strokedue to the rupture of blood vessels in the brain and the blockage ofblood vessels in the heart. The occurrence of such conditions resultsin severe disability or even death. Smoking increases the possibilityof suffering strokes and heart attacks (Patel et al., 2015).

Third, theuse of the oral contraceptive increases the chance of developing thegallbladder disease due to the exposure to high doses of estrogens.It also contributes to the development of benign but dangerous tumorsin the liver. The rupture of such tumors results in fatal internalbleeding and further increases the chances of developing liver cancer(Patel et al., 2015).

Fourth, oralcontraceptives slightly increase the likelihood of developing cancerin the reproductive organs and the breasts. The risk increases withthe use of contraceptives from a younger age. Users are advised tohave regular breast examinations from a health professional. Theyshould also disclose any family history of breast cancer, thepresence of breast nodules or irregular mammogram. Women diagnosedwith breast cancer should abstain from the use of the contraceptivesince cancer involves the development of hormone-sensitive tumors(Patel et al., 2015).

8.Patient Variables

a.Geriatrics

The use ofmononessa on old women has not been studied extensively. However,women above the age of 35 years should not use the medicine. Theextended use of the drug is associated with an increase in bloodpressure among old women. Besides, aged females are prone to develophypertension due to the increase of progestin (Trung &amp Jensen,2014).

b.Pediatrics

issafe and efficient when used by women of reproductive age. It is safefor post-pubertal adolescents below the age of 16 years. However, theuse of the medicine is not recommended for females before the startof the menstrual periods (Stegeman et al., 2013).

c.Pregnancy

The key useof mononessa is to avoid pregnancy. Consequently, the usage of themedication during pregnancy has the potential to harm the unbornchild. Users are advised to inform the doctors about their pregnancystatus four weeks before prescription. Besides, users who suspectthey are pregnant are advised to take a pregnancy test to determinewhether they can use the contraceptive. After pregnancy, users areadvised to check with the doctor before refilling an old prescription(Trung &amp Jensen, 2014).

d.Lactation

The use of slows down the production of milk among breastfeedingmothers. Besides, the hormones of the drug spread to the milk and maycause harm to a nursing baby (Trung &amp Jensen, 2014).

9.Off-label uses

The drug isused to relieve pain caused by menses and other symptoms ofendometriosis. The contraceptives reduce bleeding, swelling,endometriotic lesions and inflammation. Although the drug does notcure endometriosis, it provides significant relief for a majority ofwomen. The treatment drugs for endometriosis through contraceptivesare prescribed continuously for several months. Taking a combinationof oral contraceptives reduces the incidence of period-related pain(Stegeman et al., 2013).

Reference

Goodman, N., Rhoda, F., Beth, S., Katz. I., &amp Woode, D. (2011).American Association of clinical endocrinologists medical guidelinesfor clinical practice for the diagnosis and treatment of menopause.AACE Guidelines, 17, (1).1-25 Retrieved fromhttps://www.aace.com/files/menopause.pdf

Jensen, J., Parke, S., Mellinger, U., Serran, M. &ampMabey, G.(2013).Hormone withdrawal-associated symptoms: Comparison ofoestradiolvalerate/dienogest versus ethinylestradiol/norgestimate.TheEuropean Journal of Contraception &amp Reproductive Health Care,2(1)274-283 Retrieved fromhttp://www.tandfonline.com/doi/abs/10.3109/13625187.2013.785516?journalCode=iejc20

(28) (2016).WebMD. Retrieved on 24 August 2016 fromhttp://www.webmd.com/drugs/2/drug-64714/mononessa-28-oral/details

MONONESSA-norgestimate and ethinyl estradiol, (2015).ActavisPharma,Inc. Retrievedfromhttps://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=167222

Patel, G., King, A., Dutta, S., Korb, Sarah. Wade, J., Foulds,P., &ampSumeray, M. (2015). Evaluation of the Effects of the Weak CYP3AInhibitors Atorvastatin and Ethinyl Estradiol/Norgestimate onLomitapide Pharmacokinetics in Healthy Subjects. The Journal ofClinical Pharmacology, 56(1) 47-55 Retrived fromhttp://onlinelibrary.wiley.com/doi/10.1002/jcph.581/pdf

Stegeman,B.,&nbspBastos,M.,&nbspRosendaal,,Hylckama,A., Helmerhorst, F.,&nbspStijnen,T. &ampDekkers, O. (2013).Different combinedoral contraceptives and the risk of venous thrombosis: systematicreview and network meta-analysis. The BiomedicalJournal,1(1)347-351 Retrieved fromhttp://www.bmj.com/content/347/bmj.f5298

Trung, B. N., &amp Jensen, J. T. (2014).Evaluating the efficacy andsafety of a progestin- and estrogen-releasing ethylene vinyl acetatecopolymer contraceptive vaginal ring.The European Journal ofContraception &amp Reproductive Health Care, 1423-1430.Retrieved fromhttp://www.tandfonline.com/doi/full/10.1517/14740338.2014.948842?scroll=top&ampneedAccess=true

Wahl, M., (2014). Antibiotic interference with oral contraceptives:can a dental visit make you pregnant? Ineedce. Retrieved fromhttp://www.ineedce.com/courses/2584/pdf/1404cei_wahl_web.pdf

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