Lindynette 21-63 tablets 20-30mg - Contraception

Structure and Composition:

Film-coated tablets. 1 tablet contains:

ethinyl estradiol 20 or 30 mcg

gestodene 75 mcg

Excipients: sodium edetate calcium stearate, magnesium colloidal anhydrous silica, corn starch, povidone, lactose monohydrate - in the tablet core. D + C Yellow N 10 CI 47005, E104, povidone, titanium dioxide, C.I. 7791, E171 Macrogol 6000 Talc Calcium carbonate Sucrose - in the shell

in blisters 21 pcs. in box 1 or 3 pieces.

Description pharmaceutical form:

Round, biconvex tablets, film-coated, light yellow, kink white or nearly white with light yellow trim, both sides without inscription.

Characteristic:

Monophasic combined progestogen-estrogen contraceptive product.

Pharmacokinetics:

gestodene

It absorbed from the gastrointestinal tract (about 99% bioavailability) Quickly and almost 100%. After 1 h after a single administration of a concentration of 4.2 ng / ml. Bound to albumin and globulin, sex hormone binding (SHBG). 1-2% is in the form of the free steroid, 50-75% specifically binds with SHBG. Increased SHBG levels in the blood caused by ethinylestradiol, gestodene affects the level: increasing the fraction associated with the reduced SHBG fraction and associated with albumin. The average volume of distribution of gestodene 0.7-1.4 l / kg. Treated biotransformation is similar to other steroids. Average clearance values: 0.8-1.0 ml / min / kg. Serum levels decreased dwuhfazno. . In the final phase of T1 / 2 - 12-20 hours Provided only in the form of metabolites: 60% - in the urine and 40% - in the feces. T1 / 2 metabolites about 1 day.

Ethinylestradiol

Quickly and almost completely absorbed from the gastrointestinal tract. The mean Cmax value in the blood serum - 30-80 pg / ml, achieved after 1-2 h after administration. Bioavailability of presistemna primary metabolism and conjugation of about 60%. Completely, but nonspecifically bound to albumin (about 98.5%) and induces an increase in serum levels of SHBG. The average volume of distribution - 5-18 L / kg. Basically subjected aromatic hydroxylation to form hydroxylated and methylated metabolites that are present in free form or in the form of metabolites conjugates (glucuronides and sulfates). Metabolic clearance from the blood plasma of about 5-13 ml / min / kg. serum concentration of reduced bi-phase. . T1 / 2 of the second phase - about 16-24 hours Ethinylestradiol allocated only in the form of metabolites in the urine and bile in a ratio of 2: 3. T1 / 2 metabolites - about 1 day. Stable concentration (20% higher than after a single dose) is set to the 3-4 day.

Description of the pharmacological actions:

It inhibits secretion of pituitary hormones gonadotropin inhibits the maturation of follicles and inhibiting ovulation. It increases the viscosity of cervical mucus, which hinders the penetration of sperm into the uterus.

Clinical Pharmacology:

Oral contraceptives, in addition to preventing pregnancy, have a positive effect on the menstrual cycle (when it is violated): monthly cycle becomes regular, reduced blood loss during menstruation and the incidence of iron deficiency anemia, reduced the frequency of dysmenorrhea, the emergence of functional ovarian cysts, ectopic pregnancy, the appearance fibroadenomas and fibrokist in the mammary glands, pelvic inflammatory disease and endometrial cancer education improves skin with acne.

Testomony:

Contraception.

Contraindications:

• Hypersensitivity to the drug
• diseases accompanied by severe hepatic impairment
• liver tumors (including history)
• thrombosis and thromboembolism (including history)
• myocardial infarction (including history)
• heart failure, cerebrovascular disease (including history)
• state prior thrombosis (including transient ischemic attack, angina)
• coagulopathy
• drepanocytemia
• estrogen dependent tumors, including tumors of breast or endometrial (including history)
• diabetes complicated by microangiopathy
• uterine bleeding of unknown etiology
• idiopathic jaundice and itching during a previous pregnancy
• a history of herpes
• otosclerosis with deterioration during previous pregnancy
• pregnancy.

Carefully:

• mammary cancer
• chorea of ??pregnant women (previous appointment may worsen during pregnancy chorea)
• diabetes
• epilepsy
• gallbladder disease, especially cholelithiasis (including history)
• liver failure
• arterial hypertension
• immobilization
• major surgery
• cholestatic jaundice (including pregnancy in history)
• depression (including history)
• migraine.

Application of pregnancy and breastfeeding:

The drug is contraindicated in pregnancy. If necessary, the appointment during lactation should decide the issue of termination of breastfeeding (active ingredients of the drug are excreted in breast milk in small quantities).

Side effect:

Since the cardiovascular system: rarely - thromboembolism, venous thrombosis (including retinal vessels), increased blood pressure.

From the digestive system: sometimes - nausea, vomiting, hepatitis, hepatocellular adenoma.

On the part of the reproductive system: rarely - intermenstrual spotting, changes in vaginal secretion, changes in libido.

From endocrine system: sometimes - a feeling of tension in the breasts, change in body weight.

CNS: emotional lability, depression, dizziness, headaches, migraine, weakness, fatigue.

Other: possible abdominal pain, chloasma, discomfort while wearing contact lenses, fluid retention and sodium in the body, allergic reactions, impaired glucose tolerance.

Changes in laboratory parameters: under the influence of oral contraceptives, some laboratory parameters (liver function indexes, renal, adrenal, thyroid, blood clotting parameters and fibrinolytic factors, levels of lipoproteins and transport proteins) may vary, but in the normal range.

Drug Interactions:

Rifampicin (increase clearance) as well as barbiturates, carbamazepine, phenylbutazone, phenytoin, griseofulvin, topiramate, felbamate, oxcarbazepine may lead to breakthrough uterine bleeding or reducing the contraceptive effect.

Contraceptive reliability is reduced when taking ampicillin, tetracycline (mechanism of action has not been elucidated). During concomitant with the above drugs, and for 7 days after completion of the course they receive, it is necessary to use other non-hormonal (condoms, spermicidal gels) contraceptive methods. When using rifampicin additional methods of contraception must be used within 4 weeks after completion of its reception. Any drug that increases the motility of the gastrointestinal tract, lowers blood levels of the drug.

Drugs (such as ascorbic acid), are subjected to sulphation in the intestinal wall, competitively inhibit sulfation of ethinyl estradiol and enhance its bioavailability. Inhibitors of hepatic enzymes (e.g., itraconazole, fluconazole), increase the concentration of ethinyl estradiol in the blood plasma.

Ethinylestradiol liver by inhibiting or accelerating the conjugation enzymes (primarily glyukuronirovaniya) may affect the metabolism of other drugs, increasing or reducing their concentration in the blood (for example cyclosporin, theophylline).

Use of Hypericum preparations (including tea) reduces the concentration of drug in the blood which may lead to breakthrough bleeding, pregnancy (the reason is Hypericum inducing action on liver enzymes, which continues for 2 weeks after the completion of reception of hypericum). Ritonavir reduces the AUC of ethinyl estradiol by 41%. Therefore, during use of ritonavir should be used with higher drug doses of ethinyl estradiol (Lindinet 30) or to apply hormonal contraceptives.

Dosage and administration:

The inside is not liquid, squeezed enough water, regardless of meals.

Take 1 tablet per day (preferably at the same time of the day) for 21 days followed by a 7-day rest period during which there menstrualnopodobnoe bleeding due to discontinuation. After a 7-day interval, regardless of the bleeding has ended or has just begun, the drug continues from the next pack. This sets the rhythm easily reproducible: 3 weeks - pills, 1 week - a break. The drug of the start of each new pack in the same day of the week.

The first method of preparation: reception Lindinet drug should be started from the first day of the menstrual cycle. Shall start receiving 2-5 days of the menstrual cycle, but in this case it is recommended to use additional methods of contraception.

Go to the drug from another oral contraceptive. When changing from contraceptive containing 20 .mu.g of ethinylestradiol transition occurs normally after 7-day interval. When switching from tablets containing 30 mg etinilestadiola, it is recommended to exclude the 7-day interval, and then take in the usual way.

Going on with the drug formulations containing only a progestogen ( "mini-pill", injections, implants): with the "mini-pill" you can go to the reception Lindinet drug in any day of the cycle. With the implant can go to the drug Lindinet the day after the removal of the implant with the solution for injection - the day before the injection. In these cases, in the first 7 days necessary to apply additional methods of contraception.

The drug Lindinet after the abortion I trimester of pregnancy: after an abortion as soon as possible to start taking the drug, in this case there is no need to use an additional method of contraception.

The drug Lindinet after delivery or abortion in the II trimester of pregnancy: the reception of the drug can be started 21-28 days after delivery, provided that the woman is not breastfeeding, or abortion in the II trimester of pregnancy. In these cases, in the first 7 days necessary to apply additional methods of contraception. If, after childbirth or abortion already had sexual intercourse, pregnancy should be ruled, or wait until the first menstrual period before taking the drug.

Pass to the pill: if a pill is missed - missed tablet to take as soon as possible. If the interval was less than 12 hours, the effectiveness of the drug decreases and in this case there is no need to use an additional method of contraception. The remaining tablets taken at the usual time. If the interval was more than 12 hours, the effectiveness of the drug can be reduced. In this case, the woman should take the missed (s) tablet (s), and the next tablet - taking in the normal mode, while in the next 7 days is necessary to use additional methods of contraception. If less than 7 Table left in the pack., The drug of the next pack is started without interruption. In this case, there is no menstrualnopodobnoe bleeding due to discontinuation of the drug until the completion of the reception of the second package of the drug, but may appear spotting or breakthrough bleeding. If there is no menstrualnopodobnoe bleeding due to discontinuation of the drug after completion of the reception of the second pack, then pregnancy should be excluded before continuing treatment.

Measures taken by vomiting and diarrhea, if within 3-4 hours after taking the drug begins vomiting and / or diarrhea may reduce the contraceptive effect. In this case, it is necessary to act in accordance with paragraph "Skipping to the pill." If the patient does not want to change the receive mode, the missed tablet should be taken from a new package.

Changing the date of the onset of menstruation: it is possible to accelerate the start of menstruation by reducing the interruption of taking the drug. The shorter the break in taking the drug, the more likely that there will not menstrualnopodobnoe bleeding or spotting and breakthrough bleeding will occur during treatment of the next pack. To delay menstruation taking this medication should be continued from the new packaging without the 7-day break. Menstruation can be delayed as long as necessary: ??to the end taking the last pill in the second package. When you delay menstruation can occur breakthrough bleeding or spotting. Regular intake Lindinet drug can be restored after the usual 7-day break.

Overdose:

Severe symptoms after administration of large doses of the contraceptive is not described.

Symptoms include nausea, vomiting, and in young girls - a slight vaginal bleeding.

Treatment: symptomatic. No specific antidote.

Precautionary measures:

Diseases of the circulatory system. Oral contraceptives increase the risk of myocardial infarction. The risk of myocardial infarction and thromboembolic complications of various localization increases in smoking women who have other risk factors (eg, hypertension, hypercholesterolemia, obesity, diabetes, family history of VPP, age over 35-40 years old). This should be considered for women over 35 years old and a lot of smokers. In women at an older age and taking the drug for a long time there was an increase in blood pressure. Increased blood pressure often seen with the use of drugs with large doses of hormones.

It is necessary to consult with a specialist before using the product, if the woman observed: congenital predisposition to thromboembolic disease, obesity (body mass index above 30 kg / m2), violation of metabolism of fats (dislipoproteinemia), hypertension, diseases of the heart valves, atrial fibrillation, in cases prolonged immobilization, major surgery, surgery on the legs, severe injury (due to the fact that the risk of thromboembolic disease is increasing in the postoperative period, you must stop taking the drug for 4 weeks before the planned operation and resume the reception after 2 weeks after the activation of the patient).

The drug should be discontinued immediately if symptoms of thromboembolism: chest pain, which may radiate to the left arm, an unusually severe pain in the legs, swelling of the legs, sharp stabbing pain when breathing or coughing, coughing up blood.

Tumors. Some studies have noted a higher incidence of cervical cancer among women who took a long time oral contraceptives (however, a causal relationship with the administration of the drug has not been proven). The likelihood of developing cervical cancer depends on the sexual behavior and other factors (human papilloma virus). Studies have not proven a causal link between breast cancer and taking drugs: in women taking oral contraceptives, the disease is detected in an earlier stage than women who were not taking these drugs. There were isolated reports of the development of hepatic benign tumor in women receiving long-term hormonal contraceptives, with the development of intra-abdominal bleeding.

Other pathological conditions. The drug should be discontinued in case of occurrence of loss of vision (total or partial), proptosis, diplopia, or upon detection of edema of the papilla of the optic nerve or retinal vascular disorders. According to studies, the relative risk of developing gallstones increases with age among women taking oral contraceptives or drugs containing estrogen. Recent studies have revealed that the risk of gallstone disease is less than when using drugs with a low dose of hormones. When migraines, worsening of migraine or when constant or repeated unusually severe headache, the drug should be discontinued. Admission Lindinet the drug must be stopped immediately when a generalized itching or when an epileptic seizure.

Effect on lipid and carbohydrate metabolism. Women taking oral contraceptives may experience reduced tolerance to carbohydrates. Some women have increased blood triglyceride was found in the application of oral contraceptive. In women with hereditary hyperlipidemic taking medication with estrogen, a sharp increase in plasma triglyceride was found, which could lead to the development of pancreatitis. When using oral contraceptives, especially during the first 3 months, may appear irregular (spotting or breakthrough) bleeding. If the bleeding is noted for a long time or there were formed after regular cycles, the cause is usually non-hormonal, and it is necessary to hold the appropriate pelvic examination to rule out pregnancy or malignancy. If non-hormonal cause can be eliminated, and intermenstrual bleeding continues for more than 4 months, should go to the reception of another drug. In some cases, menstrualnopodobnoe bleeding in connection with the discontinuation of the drug for a 7-day interval is not shown. Before the absence of bleeding was broken dosing regimen, or if there is no bleeding after taking the second pack, to continue taking this medication should be deleted pregnancy. should gather detailed family and personal medical history and carry out general medical and gynecological examination before the beginning of the use of contraceptive pills. These studies are repeated every 6 months. On physical examination, measure blood pressure, conducted studies of breast, abdominal palpation, conduct gynecological examination with cytology and laboratory studies indicated (liver function indexes, renal, adrenal, thyroid, indicators of blood coagulation and fibrinolytic factors, levels of lipoproteins and transport proteins). The woman should be warned that the drug does not protect it from infections, sexually transmitted diseases, particularly AIDS. When acute or chronic disturbances of liver function should stop taking the drug to restore the values ??of hepatic enzymes. If abnormal liver function may be disturbed metabolism of steroid hormones. Those women who appear depressed when taking contraceptives, it is advisable to repeal the drug and temporarily switch to another contraceptive method to clarify the connection between the development of depression and drug intake. It is necessary to closely monitor the presence of a history of depression, and the resumption of depression should complete the course receive an oral contraceptive. When the use of oral contraceptives folic acid concentration in the blood can be reduced. It has clinical significance only in the case of pregnancy in a short period of time after completion of receiving the oral contraceptive.

When diarrhea is enhanced intestinal motility and reduces the absorption of the drug.

Special instructions:

Studies to identify the possible impact of the drug on driving ability or the ability to drive is not carried dangerous machinery.