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DRUGS & SUPPLEMENTS
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Ethinyl Estradiol:
Indication: For treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive.
Synphasic 28 (Ethinyl Estradiol) is a synthetic derivative of the natural estrogen estradiol. It is one of two estrogens currently used in oral contraceptive pills. The other, mestranol, is converted to Synphasic 28 (Ethinyl Estradiol) before it is biologically active. Synphasic 28 (Ethinyl Estradiol) and norethindrone are used together as an oral contraceptive agent.
Norethindrone:
Synphasic 28 (Norethindrone)® (norethindrone acetate tablets USP) - 5 mg oral tablets.
Synphasic 28 (Norethindrone)® (norethindrone acetate tablets USP), (17-hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one acetate), a synthetic, orally active progestin, is the acetic acid ester of Synphasic 28 (Norethindrone). It is a white, or creamy white, crystalline powder. The structural formula is as follows:
C22H28O3 M.W. 340.46
Synphasic 28 (Norethindrone)® (norethindrone acetate tablets USP) contain the following inactive ingredients: anhydrous lactose, magnesium stearate, and microcrystalline cellulose.
Synphasic 28 (Norethindrone) Acetate structural formula
Synphasic 28 acetate induces secretory changes in an estrogen-primed endometrium. On a weight basis, it is twice as potent as Synphasic 28 (Norethindrone).
Synphasic 28 acetate is completely and rapidly deacetylated to Synphasic 28 (Norethindrone) (NET) after oral administration, and the disposition of Synphasic 28 (Norethindrone) acetate is indistinguishable from that of orally administered Synphasic 28 (Norethindrone). Synphasic 28 (Norethindrone) acetate is rapidly absorbed from Synphasic 28 (Norethindrone) tablets, with maximum plasma concentration of Synphasic 28 (Norethindrone) generally occurring at about 2 hours post-dose. The pharmacokinetic parameters of Synphasic 28 (Norethindrone) following single oral administration of Synphasic 28 (Norethindrone) in 29 healthy female volunteers are summarized in Table 1.
Table 1 Pharmacokinetic Parameters after a Single Dose of Synphasic 28 (Norethindrone)® in Healthy Women | |
Synphasic 28 (Norethindrone)® (n = 29) Arithmetic Mean ± SD | |
Synphasic 28 (Norethindrone) (NET) | |
AUC (0-inf)(ng/ml*h) | 166.90 ± 56.28 |
Cmax (ng/ml) | 26.19 ± 6.19 |
tmax (h) | 1.83 ± 0.58 |
t1/2 (h) | 8.51 ± 2.19 |
AUC = area under the curve, Cmax = maximum plasma concentration, tmax = time at maximum plasma concentration, t1/2 = half-life, SD = standard deviation |
Figure 1. Mean Plasma Concentration Profile after a Single Dose of 5 mg Administered to 29 Healthy Female Volunteers under Fasting Conditions
Figure 1
The effect of food administration on the pharmacokinetics of Synphasic 28 (Norethindrone) has not been studied.
Synphasic 28 is 36% bound to sex hormone-binding globulin (SHBG) and 61% bound to albumin. Volume of distribution of Synphasic 28 (Norethindrone) is about 4 L/kg.
Synphasic 28 (Norethindrone) undergoes extensive biotransformation, primarily via reduction, followed by sulfate and glucuronide conjugation. The majority of metabolites in the circulation are sulfates, with glucuronides accounting for most of the urinary metabolites.
Plasma clearance value for Synphasic 28 is approximately 0.4 L/hr/kg. Synphasic 28 (Norethindrone) is excreted in both urine and feces, primarily as metabolites. The mean terminal elimination half-life of Synphasic 28 (Norethindrone) following a single dose administration of Synphasic 28 (Norethindrone) is approximately 9 hours.
The effect of age on the pharmacokinetics of Synphasic 28 after Synphasic 28 (Norethindrone) administration has not been evaluated.
The effect of race on the disposition of Synphasic 28 (Norethindrone) after Synphasic 28 (Norethindrone) administration has not been evaluated.
The effect of renal disease on the disposition of Synphasic 28 after Synphasic 28 (Norethindrone) administration has not been evaluated. In premenopausal women with chronic renal failure undergoing peritoneal dialysis who received multiple doses of an oral contraceptive containing ethinyl estradiol and Synphasic 28 (Norethindrone), plasma Synphasic 28 (Norethindrone) concentration was unchanged compared to concentrations in premenopausal women with normal renal function.
The effect of hepatic disease on the disposition of Synphasic 28 (Norethindrone) after Synphasic 28 (Norethindrone) administration has not been evaluated. However, Synphasic 28 (Norethindrone) is contraindicated in markedly impaired liver function or liver disease.
No pharmacokinetic drug interaction studies investigating any drug-drug interactions with Synphasic 28 (Norethindrone) have been conducted.
Synphasic 28 (Norethindrone) (norethindrone acetate tablets USP) is indicated for the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer. Synphasic 28 (Norethindrone) (norethindrone acetate tablets USP) is not intended, recommended or approved to be used with concomitant estrogen therapy in postmenopausal women for endometrial protection.
Patients with risk factors for arterial vascular disease (e.g., hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (e.g., personal history or family history of VTE, obesity, and systemic lupus erythematosus) should be managed appropriately.
Discontinue medication pending examination if there is a sudden partial or complete loss of vision or if there is sudden onset of proptosis, diplopia, or migraine. If examination reveals papilledema or retinal vascular lesions, medication should be discontinued.
Healthcare providers are advised to discuss the PATIENT INFORMATION leaflet with patients for whom they prescribe Synphasic 28.
The following laboratory test results may be altered by the use of estrogen/progestin combination drugs:
Some beagle dogs treated with medroxyprogesterone acetate developed mammary nodules. Although nodules occasionally appeared in control animals, they were intermittent in nature, whereas nodules in treated animals were larger and more numerous, and persisted. There is no general agreement as to whether the nodules are benign or malignant. Their significance with respect to humans has not been established.
Synphasic 28 acetate is contraindicated during pregnancy as it may cause fetal harm when administered to pregnant women. Several reports suggest an association between intrauterine exposure to progestational drugs in the first trimester of pregnancy and congenital abnormalities in male and female fetuses. Some progestational drugs induce mild virilization of the external genitalia of female fetuses.
Detectable amounts of progestins have been identified in the milk of mothers receiving them. Caution should be exercised when progestins are administered to a nursing woman.
Synphasic 28 (Norethindrone) tablets are not indicated in children.
See WARNINGS and PRECAUTIONS .
The following adverse reactions have been observed in women taking progestins:
Therapy with Synphasic 28 must be adapted to the specific indications and therapeutic response of the individual patient.
2.5 to 10 mg Synphasic 28 (Norethindrone) may be given daily for 5 to 10 days to produce secretory transformation of an endometrium that has been adequately primed with either endogenous or exogenous estrogen.
Progestin withdrawal bleeding usually occurs within three to seven days after discontinuing Synphasic 28 (Norethindrone) therapy. Patients with a past history of recurrent episodes of abnormal uterine bleeding may benefit from planned menstrual cycling with Synphasic 28 (Norethindrone).
Initial daily dosage of 5 mg Synphasic 28 (Norethindrone) for two weeks. Dosage should be increased by 2.5 mg per day every two weeks until 15 mg per day of Synphasic 28 (Norethindrone) is reached. Therapy may be held at this level for six to nine months or until annoying breakthrough bleeding demands temporary termination.
Synphasic 28 (Norethindrone)® (norethindrone acetate tablets USP) is available as:
5 mg: | White, oval, flat-faced, beveled edge, tablet scored on one side. Debossed with 5 Synphasic 28 (Norethindrone) on the unscored side and stylized b / 424 on the scored side. Available in bottles of 50 tablets (NDC 51285-424-10). |
Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required).
Store at 20º to 25ºC (68º to 77ºF).
KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN.
TEVA WOMEN’S HEALTH, INC.
Subsidiary of TEVA PHARMACEUTICALS USA, INC.
North Wales, PA 19454
Rev. A 10/2015
Synphasic 28 (Norethindrone)®
(norethindrone acetate tablets USP)
Read this PATIENT INFORMATION before you start taking Synphasic 28 (Norethindrone) and read what you get each time you refill Synphasic 28 (Norethindrone). There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition.
What is the most important information I should know about Synphasic 28 (Norethindrone) (A Progestin Hormone)?
What is Synphasic 28 (Norethindrone)?
Synphasic 28 (Norethindrone) is similar to the progesterone hormones naturally produced by the body. Your healthcare provider may provide Synphasic 28 (Norethindrone) as individual tablets.
What are Synphasic 28 (Norethindrone) used for?
Synphasic 28 (Norethindrone) are used for the treatment of secondary amenorrhea (absence of menstrual periods in women who have previously had a menstrual period who are not pregnant), the treatment of endometriosis, and the treatment of irregular menstrual periods due to hormone imbalance.
Who should not take Synphasic 28 (Norethindrone)?
You should not take Synphasic 28 (Norethindrone) if you are postmenopausal, pregnant or breastfeeding.
You should not take Synphasic 28 (Norethindrone) if you have the following conditions:
What are the risks associated with Synphasic 28 (Norethindrone)?
Synphasic 28 (Norethindrone) should not be used if you are pregnant. Synphasic 28 (Norethindrone) are contraindicated during pregnancy as it may cause fetal harm when administered to pregnant women. There is an increased risk of minor birth defects in children whose mothers take this drug during the first 4 months of pregnancy. Several reports suggest an association between mothers who take these drugs in the first trimester of pregnancy and congenital abnormalities in male and female babies. Although it is not clear that these events were drug related, you should check with your healthcare provider about the risks to your unborn child of any medication taken during pregnancy.
You should avoid using Synphasic 28 (Norethindrone) during pregnancy. If you take Synphasic 28 (Norethindrone) and later find you were pregnant when you took it, be sure to discuss this with your healthcare provider as soon as possible.
Use of progestational drugs, such as Synphasic 28 (Norethindrone), has been associated with changes in the blood-clotting system. These changes allow the blood to clot more easily, possibly allowing clots to form in the bloodstream. If blood clots do form in your bloodstream, they can cut off the blood supply to vital organs, causing serious problems. These problems may include a stroke (by cutting off blood to part of the brain), a heart attack (by cutting off blood to part of the heart), a pulmonary embolus (by cutting off blood to part of the lungs), visual loss or blindness (by cutting off blood vessels in the eye), or other problems. Any of these conditions may cause death or serious long-term disability. Call your healthcare provider right away if you suspect you have any of these conditions. He or she may advise you to stop using the drug.
Discontinue Synphasic 28 (Norethindrone) tablets and call your healthcare provider right away if you experience sudden partial or complete loss of vision, blurred vision, or sudden onset of bulging eyes, double vision, or migraine.
These are some of the warning signs of serious side effects with progestin therapy
Call your healthcare provider right away if you get any of these warning signs, or any other unusual symptom that concerns you.
Common side effects include
Other side effects include
These are not all the possible side effects of progestin and/or estrogen therapy. For more information, ask your healthcare provider or pharmacist.
What can I do to lower my chances of getting a serious side effect with Synphasic 28 (Norethindrone)?
General information about the safe and effective use of Synphasic 28 (Norethindrone)
Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not take Synphasic 28 (Norethindrone) for conditions for which it was not prescribed. Do not give Synphasic 28 (Norethindrone) tablets to other people, even if they have the same symptoms you have. It may harm them.
Keep Synphasic 28 (Norethindrone) out of the reach of children.
This leaflet provides a summary of the most important information about progestin and/or estrogen therapy. If you would like more information, talk with your healthcare provider or pharmacist. You can ask for information about Synphasic 28 (Norethindrone) that is written for health professionals.
What are the ingredients in Synphasic 28 (Norethindrone)?
Synphasic 28 (Norethindrone) contain the following inactive ingredients: anhydrous lactose, magnesium stearate, and microcrystalline cellulose.
TEVA WOMEN’S HEALTH, INC.
Subsidiary of TEVA PHARMACEUTICALS USA, INC.
North Wales, PA 19454
Rev. A 10/2015
NDC 51285-424-10
Aygestin®
(norethindrone acetate
tablets USP)
ORALLY ACTIVE PROGESTIN
5 mg
PHARMACIST: PLEASE DISPENSE WITH
ATTACHED PATIENT INFORMATION LEAFLET.
Rx only
50 TABLETS
TEVA
TEVA WOMEN’S HEALTH
Depending on the reaction of the Synphasic 28 after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Synphasic 28 not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.
Is Synphasic 28 addictive or habit forming?Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
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The information was verified by Dr. Rachana Salvi, MD Pharmacology