Today's drug is Yasmin. Yasmin is the trade name.
It has 21 yellow tablets each containing two female hormones, a synthetic estrogen called ethinyl
estradiol 0.03mg and a progestin called drospirenone 3mg, and 7 inert white tablets.
What is Yasmin indicated for?
INDICATIONS :
- Yasmin is a combined oral contraceptive, commonly known as a 'birth control pill' or 'the Pill'.
- It is used to prevent pregnancy.
How does Yasmin work?
MECHANISMS OF ACTION :
- It lowers the risk of becoming pregnant primarily by suppressing ovulation.
- Other possible mechanisms may include :
- Cervical mucus changes that inhibit sperm penetration
- Endometrial changes that reduce the likelihood of implantation.
How is acamprosate being used?
ROUTE OF ADMINISTRATION :
- It is taken orally as tablets.
- Take one tablet by mouth at the same time every day. The failure rate may increase when pills are missed or taken incorrectly.
- To achieve maximum contraceptive effectiveness, Yasmin must be taken as directed, in the order directed on the blister pack. Single missed pills should be taken as soon as remembered.
- Instruct the patient to begin taking Yasmin either on the first day of her menstrual period (Day 1 Start) or on the first Sunday after the onset of her menstrual period (Sunday Start).
- During the first cycle of Yasmin use, instruct the patient to take one yellow Yasmin daily, beginning on Day 1 of her menstrual cycle. (The first day of menstruation is Day 1.) She should take one yellow Yasmin daily for 21 consecutive days, followed by one white tablet daily on Days 22 through 28.
- Yasmin should be taken in the order directed on the package at the same time each day, preferably after the evening meal or at bedtime with some liquid, as needed.
- Yasmin can be taken without regard to meals.
- If Yasmin is first taken later than the first day of the menstrual cycle, Yasmin should not be considered effective as a contraceptive until after the first 7 consecutive days of product administration. Instruct the patient to use a non-hormonal contraceptive as back-up during the first 7 days. The possibility of ovulation and conception prior to initiation of medication should be considered.
- During the first cycle of Yasmin use, instruct the patient to take one yellow Yasmin daily, beginning on the first Sunday after the onset of her menstrual period. She should take one yellow Yasmin daily for 21 consecutive days, followed by one white tablet daily on Days 22 through 28.
- Yasmin should be taken in the order directed on the package at the same time each day, preferably after the evening meal or at bedtime with some liquid, as needed. Yasmin can be taken without regard to meals.
- Yasmin should not be considered effective as a contraceptive until after the first 7 consecutive days of product administration. Instruct the patient to use a non-hormonal contraceptive as back-up during the first 7 days. The possibility of ovulation and conception prior to initiation of medication should be considered.
- The patient should begin her next and all subsequent 28-day regimens of Yasmin on the same day of the week that she began her first regimen, following the same schedule. She should begin taking her yellow tablets on the next day after ingestion of the last white tablet, regardless of whether or not a menstrual period has occurred or is still in progress. Anytime a subsequent cycle of Yasmin is started later than the day following administration of the last white tablet, the patient should use another method of contraception until she has taken a yellow Yasmin daily for seven consecutive days.
- When switching from another birth control pill, Yasmin should be started on the same day that a new pack of the previous oral contraceptive would have been started.
- When switching from a transdermal patch or vaginal ring, Yasmin should be started when the next application would have been due. When switching from an injection, Yasmin should be started when the next dose would have been due. When switching from an intrauterine contraceptive or an implant, Yasmin should be started on the day of removal.
- Withdrawal bleeding usually occurs within 3 days following the last yellow tablet. If spotting or breakthrough bleeding occurs while taking Yasmin, instruct the patient to continue taking Yasmin by the regimen described above. Counsel her that this type of bleeding is usually transient and without significance; however, advise her that if the bleeding is persistent or prolonged, she should consult her healthcare provider.
- Although the occurrence of pregnancy is low if Yasmin is taken according to directions, if withdrawal bleeding does not occur, consider the possibility of pregnancy. If the patient has not adhered to the prescribed dosing schedule (missed one or more active tablets or started taking them on a day later than she should have), consider the possibility of pregnancy at the time of the first missed period and take appropriate diagnostic measures. If the patient has adhered to the prescribed regimen and misses two consecutive periods, rule out pregnancy. Discontinue Yasmin if pregnancy is confirmed.
- The risk of pregnancy increases with each active yellow tablet missed. For additional patient instructions regarding missed pills, see the "WHAT TO DO IF YOU MISS PILLS" section in the FDA-Approved Patient Labeling. If breakthrough bleeding occurs following missed tablets, it will usually be transient and of no consequence. If the patient misses one or more white tablets, she should still be protected against pregnancy provided she begins taking a new cycle of yellow tablets on the proper day.
- For postpartum women who do not breastfeed or after a second trimester abortion, start Yasmin no earlier than 4 weeks postpartum due to the increased risk of thromboembolism. If the patient starts Yasmin postpartum and has not yet had a period, evaluate for possible pregnancy, and instruct her to use an additional method of contraception until she has taken Yasmin for 7 consecutive days.
- In case of severe vomiting or diarrhea, absorption may not be complete and additional contraceptive measures should be taken. If vomiting occurs within 3-4 hours after tablet-taking, this can be regarded as a missed tablet.
WHAT TO DO IF YOU MISS PILLS
If you miss 1 yellow pill of your pack:
- Take it as soon as you remember. Take the next pill at your regular time. This means you may take two pills in one day.
- You do not need to use a back-up birth control method if you have sex.
If you miss 2 yellow pills in a row in Week 1 or Week 2 of your pack:
- Take two pills on the day you remember and two pills the next day.
- Then take one pill a day until you finish the pack.
- You could become pregnant if you have sex in the 7 days after you restart your pills. You must use another birth control method (such as a condom and spermicide) as a back-up for those 7 days.
If you miss 2 yellow pills in a row in Week 3 or Week 4 of your pack:
1. If you are a Day 1 Starter:
- Throw out the rest of the pill pack and start a new pack that same day.
2. If you area Sunday Starter:
- Keep taking one pill every day until Sunday. On Sunday, throw out the rest of the pack and start a new pack of pills that same day.
3. You could become pregnant if you have sex in the 7 days after you restart your pills. You must use another birth control method (such as a condom and spermicide) as a back-up for those 7 days.
4. You may not have your period this month but this is expected. However, if you miss your period two months in a row, call your healthcare provider because you might be pregnant.
If you miss 3 or more yellow pills in a row during any week:
1. If you are a Day 1 Starter:
- Throw out the rest of the pill pack and start a new pack that same day.
2. If you are a Sunday Starter:
- Keep taking 1 pill every day until Sunday. On Sunday, throw out the rest of the pack and start a new pack of pills that same day.
3. You could become pregnant if you have sex in the 7 days after you restart your pills. You must use another birth control method (such as condoms and spermicides) as a back-up for those 7 days.
4. You may not have your period this month but this is expected. However, if you miss your period two months in a row, call your healthcare provider because you might be pregnant.
- Throw away the pills you missed. Keep taking one pill each day until the pack is empty. You do not need a back-up method.
Finally, if you are still not sure what to do about the pills you have missed:
- Use a back-up method (such as condoms and spermicides) anytime you have sex.
- Contact your healthcare provider and continue taking one active yellow pill each day until otherwise directed.
Is there any contraindication?
CONTRAINDICATIONS :
Do not prescribe Yasmin to women who are known to have the following:
- Renal impairment
- Adrenal insufficiency
- A high risk of arterial or venous thrombotic diseases. Examples include women who are known to:
- Smoke, if over age 35
- Have deep vein thrombosis or pulmonary embolism, now or in the past
- Have cerebrovascular disease
- Have coronary artery disease
- Have thrombogenic valvular or thrombogenic rhythm diseases of the heart (for example, subacute bacterial endocarditis with valvular disease, or atrial fibrillation)
- Have inherited or acquired hypercoagulopathies
- Have uncontrolled hypertension
- Have diabetes mellitus with vascular disease
- Have headaches with focal neurological symptoms or have migraine headaches with or without aura if over age 35
- Undiagnosed abnormal uterine bleeding
- Breast cancer or other estrogen- or progestin-sensitive cancer, now or in the past
- Liver tumor (benign or malignant) or liver disease
- Pregnancy, because there is no reason to use COCs (Combined oral contraceptive)
Are there any possible side effects?
SIDE EFFECTS :
The most common side effects:
- Spotting or bleeding between menstrual periods
- Nausea
- Breast tenderness
- Headache
These side effects are usually mild and usually disappear with time.
Less common side effects:
- Acne
- Less sexual desire
- Bloating or fluid retention
- Blotchy darkening of the skin, especially on the face
- High blood sugar, especially in women who already have diabetes
- High fat (cholesterol; triglyceride) levels in the blood
- Depression
- Problems tolerating contact lenses
- Weight changes
What precautions are necessary?
PRECAUTIONS :
(i) Thromboembolic Disorders and Other Vascular Problems
- Stop Yasmin if an arterial or venous thrombotic (VTE) event occurs.
- Based on presently available information on Yasmin, DRSP-containing COCs may be associated with a higher risk of venous thromboembolism (VTE) than COCs containing the progestin levonorgestrel or some other progestins. Epidemiologic studies that compared the risk of VTE reported that the risk ranged from no increase to a three-fold increase. Before initiating use of Yasmin in a new COC user or a woman who is switching from a contraceptive that does not contain DRSP, consider the risks and benefits of a DRSP-containing COC in light of her risk of a VTE. Known risk factors for VTE include smoking, obesity, and family history of VTE, in addition to other factors that contraindicate use of COCs.
- If feasible, stop Yasmin at least 4 weeks before and through 2 weeks after major surgery or other surgeries known to have an elevated risk of thromboembolism.
- Start Yasmin no earlier than 4 weeks after delivery, in women who are not breastfeeding. The risk of postpartum thromboembolism decreases after the third postpartum week, whereas the risk of ovulation increases after the third postpartum week.
- Use of COCs also increases the risk of arterial thromboses such as strokes and myocardial infarctions, especially in women with other risk factors for these events.
- COCs have been shown to increase both the relative and attributable risks of cerebrovascular events (thrombotic and hemorrhagic strokes), although, in general, the risk is greatest among older (>35 years of age), hypertensive women who also smoke. COCs also increase the risk for stroke in women with other underlying risk factors.
- Oral contraceptives must be used with caution in women with cardiovascular disease risk factors.
- Stop Yasmin if there is unexplained loss of vision, proptosis, diplopia, papilledema, or retinal vascular lesions. Evaluate for retinal vein thrombosis immediately.
(ii) Hyperkalemia
- Yasmin contains 3 mg of the progestin DRSP, which has antimineralocorticoid activity, including the potential for hyperkalemia in high-risk patients, comparable to a 25 mg dose of spironolactone.
- Yasmin should not be used in patients with conditions that predispose to hyperkalemia (that is, renal impairment, hepatic impairment, and adrenal insufficiency).
- Women receiving daily, long-term treatment for chronic conditions or diseases with medications that may increase serum potassium concentration should have their serum potassium concentration checked during the first treatment cycle.
- Medications that may increase serum potassium concentration include ACE inhibitors, angiotensin-II receptor antagonists, potassium-sparing diuretics, potassium supplementation, heparin, aldosterone antagonists, and NSAIDs.
(iii) Carcinoma of the Breasts and Reproductive Organs
- Women who currently have or have had breast cancer should not use Yasmin because breast cancer is a hormonally-sensitive tumor.
- There is substantial evidence that COCs do not increase the incidence of breast cancer. Although some past studies have suggested that COCs might increase the incidence of breast cancer, more recent studies have not confirmed such findings.
- Some studies suggest that COCs are associated with an increase in the risk of cervical cancer or intraepithelial neoplasia. However, there is controversy about the extent to which these findings may be due to differences in sexual behavior and other factors.
(iv) Liver Disease
- Discontinue Yasmin if jaundice develops. Steroid hormones may be poorly metabolized in patients with impaired liver function. Acute or chronic disturbances of liver function may necessitate the discontinuation of COC use until markers of liver function return to normal and COC causation has been excluded.
- Hepatic adenomas are associated with COC use. An estimate of the attributable risk is 3.3 cases/100,000 COC users. Rupture of hepatic adenomas may cause death through intra-abdominal hemorrhage.
- Studies have shown an increased risk of developing hepatocellular carcinoma in long-term (> 8 years) COC users. However, the attributable risk of liver cancers in COC users is less than one case per million users.
- Oral contraceptive-related cholestasis may occur in women with a history of pregnancy-related cholestasis. Women with a history of COC-related cholestasis may have the condition recur with subsequent COC use.
(v) High Blood Pressure
- For women with well-controlled hypertension, monitor blood pressure and stop Yasmin if blood pressure rises significantly. Women with uncontrolled hypertension or hypertension with vascular disease should not use COCs.
- An increase in blood pressure has been reported in women taking COCs, and this increase is more likely in older women and with extended duration of use. The incidence of hypertension increases with increasing concentration of progestin.
(vi) Gallbladder Disease
- Studies suggest a small increased relative risk of developing gallbladder disease among COC users.
(vii) Carbohydrate and Lipid Metabolic Effects
- Carefully monitor prediabetic and diabetic women who are taking Yasmin. COCs may decrease glucose tolerance in a dose-related fashion.
- Consider alternative contraception for women with uncontrolled dyslipidemia. A small proportion of women will have adverse lipid changes while on COCs.
- Women with hypertriglyceridemia, or a family history thereof, may be at an increased risk of pancreatitis when using COCs.
(viii) Headache
- If a woman taking Yasmin develops new headaches that are recurrent, persistent, or severe, evaluate the cause and discontinue Yasmin if indicated.
- An increase in frequency or severity of migraine during COC use (which may be prodromal of a cerebrovascular event) may be a reason for immediate discontinuation of the COC.
(ix) Bleeding Irregularities
- Unscheduled (breakthrough or intracyclic) bleeding and spotting sometimes occur in patients on COCs, especially during the first three months of use. If bleeding persists or occurs after previously regular cycles, check for causes such as pregnancy or malignancy. If pathology and pregnancy are excluded, bleeding irregularities may resolve over time or with a change to a different COC.
- Data from ten contraceptive efficacy clinical trials (N=2,467) show that the percent of women who took Yasmin and experienced unscheduled bleeding decreased over time from 12% at cycle 2 to 6% (cycle 13). A total of 24 subjects out of 2,837 in the Yasmin trials (<1%) discontinued due to bleeding complaints. These are described as metrorrhagia, vaginal hemorrhage, menorrhagia, abnormal withdrawal bleeding, and menometrorrhagia.
- The average duration of scheduled bleeding episodes in the majority of subjects (86%-88%) was 4-7 days. Women who use Yasmin may experience absence of withdrawal bleeding, even if they are not pregnant. Based on subject diaries from contraceptive efficacy trials, during cycles 2-13,1-11% of women per cycle experienced no withdrawal bleeding. Some women may encounter post-pill amenorrhea or oligomenorrhea, especially when such a condition was pre-existent.
- If withdrawal bleeding does not occur, consider the possibility of pregnancy. If the patient has not adhered to the prescribed dosing schedule (missed one or more active tablets or started taking them on a day later than she should have), consider the possibility of pregnancy at the time of the first missed period and take appropriate diagnostic measures. If the patient has adhered to the prescribed regimen and misses two consecutive periods, rule out pregnancy.
(x) COC Use Before or During Early Pregnancy
- Extensive epidemiological studies have revealed no increased risk of birth defects in women who have used oral contraceptives prior to pregnancy. Studies also do not suggest a teratogenic effect when COCs are taken inadvertently during early pregnancy, particularly in so far as cardiac anomalies and limb-reduction defects are concerned.
- The administration of oral contraceptives to induce withdrawal bleeding should not be used as a test for pregnancy.
(xi) Depression
- Women with a history of depression should be carefully observed and Yasmin discontinued if depression recurs to a serious degree.
(xii) Interference with Laboratory Tests
- The use of COCs may change the results of some laboratory tests, such as coagulation factors, lipids, glucose tolerance, and binding proteins. Women on thyroid hormone replacement therapy may need increased doses of thyroid hormone because serum concentrations of thyroid-binding globulin increase with use of COCs.
- DRSP causes an increase in plasma renin activity and plasma aldosterone induced by its mild antimineralocorticoid activity.
(xiii) Monitoring
- A woman who is taking COCs should have a yearly visit with her healthcare provider for a blood pressure check and for other indicated healthcare.
(xiiii) Other Conditions
- In women with hereditary angioedema, exogenous estrogens may induce or exacerbate symptoms of angioedema. Chloasma may occasionally occur, especially in women with a history of chloasma gravidarum. Women with a tendency to chloasma should avoid exposure to the sun or ultraviolet radiation while taking COCs.
DRUG INTERACTIONS :
(i) Substances diminishing the efficacy ofCOCs
- Drugs or herbal products that induce certain enzymes, including cytochrome P450 3A4 (CYP3A4), may decrease the effectiveness of COCs or increase breakthrough bleeding.
- Some drugs or herbal products that may decrease the effectiveness of hormonal contraceptives include phenytoin, barbiturates, carbamazepine, bosentan, felbamate, griseofulvin, oxcarbazepine, rifampicin, topiramate and products containing St. John's wort.
- Interactions between oral contraceptives and other drugs may lead to breakthrough bleeding and/or contraceptive failure.
- Counsel women to use an alternative method of contraception or a back-up method when enzyme inducers are used with COCs, and to continue back-up contraception for 28 days after discontinuing the enzyme inducer to ensure contraceptive reliability.
(ii) Substances increasing the plasma concentrations of COCs
- Co-administration of atorvastatin and certain COCs containing EE increase AUC values for EE by approximately 20%.
- Ascorbic acid and acetaminophen may increase plasma EE concentrations, possibly by inhibition of conjugation.
- CYP3A4 inhibitors such as itraconazole or ketoconazole may increase plasma hormone concentrations.
(iii) Human immunodeficiency virus (HIV)/Hepatitis C virus (HCV) protease inhibitors and non-nucleoside reverse transcriptase inhibitors
- Significant changes (increase or decrease) in the plasma concentrations of estrogen and progestin have been noted in some cases of co-administration with HIV/HCV protease inhibitors or with non-nucleoside reverse transcriptase inhibitors.
Antibiotics:
- There have been reports of pregnancy while taking hormonal contraceptives and antibiotics, but clinical pharmacokinetic studies have not shown consistent effects of antibiotics on plasma concentrations of synthetic steroids.
Effect on DRSP
- The main metabolites of DRSP in human plasma are generated without involvement of the CYP system. Inhibitors of this enzyme system are therefore unlikely to influence the metabolism of DRSP.
Effects of Combined Oral Contraceptives on Other Drugs
- COCs containing EE may inhibit the metabolism of other compounds. COCs have been shown to significantly decrease plasma concentrations of lamotrigine, likely due to induction of lamotrigine glucuronidation. This may reduce seizure control; therefore, dosage adjustments of lamotrigine may be necessary. Consult the labeling of the concurrently-used drug to obtain further information about interactions with COCs or the potential for enzyme alterations.
- In vitro and clinical studies did not indicate an inhibitory potential of DRSP towards human CYP enzymes at clinically relevant concentrations.
- Women on thyroid hormone replacement therapy may need increased doses of thyroid hormone because serum concentration of thyroid-binding globulin increases with use of COCs.
Potential to Increase Serum Potassium Concentration
- There is a potential for an increase in serum potassium concentration in women taking Yasmin with other drugs that may increase serum potassium concentration.
Interference with Laboratory Tests
- The use of contraceptive steroids may influence the results of certain laboratory tests, such as coagulation factors, lipids, glucose tolerance, and binding proteins. DRSP causes an increase in plasma renin activity and plasma aldosterone induced by its mild antimineralocorticoid activity.
Pregnancy and breastfeeding:
- There is little or no increased risk of birth defects in women who inadvertently use COCs during early pregnancy. Epidemiologic studies and meta-analyses have not found an increased risk of genital or non-genital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to low dose COCs prior to conception or during early pregnancy.
- The administration of COCs to induce withdrawal bleeding should not be used as a test for pregnancy. COCs should not be used during pregnancy to treat threatened or habitual abortion.
- Women who do not breastfeed may start COCs no earlier than four weeks postpartum.
- When possible, advise the nursing mother to use other forms of contraception until she has weaned her child. Estrogen-containing COCs can reduce milk production in breastfeeding mothers. This is less likely to occur once breastfeeding is well-established; however, it can occur at any time in some women. Small amounts of oral contraceptive steroids and/or metabolites are present in breast milk.
- After oral administration of Yasmin, about 0.02% of the DRSP dose was excreted into the breast milk of postpartum women within 24 hours. This results in a maximal daily dose of about 0.003 mg DRSP in an infant.
References :
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