Linda's 30

Active material: Ethinylestradiol, Gestodene
When ATH: G03AA10
CCF: Monophasic oral contraceptive
ICD-10 codes (testimony): Z30.0
When CSF: 15.11.04.01
Manufacturer: GEDEON RICHTER Ltd. (Hungary)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills, coated yellow color, round, lenticular, both sides unprinted; to break white or almost white with yellow trim.

Excipients: sodium calcium edetate, magnesium stearate, colloidal silicon dioxide, povidone, corn starch, lactose monohydrate.

The composition of the shell: quinoline yellow dye (D C Yellow №10) (E104), povidone, Titanium dioxide, macrogol 6000, talc, calcium carbonate, sucrose.

21 PC. – blisters (1) – packs cardboard.
21 PC. – blisters (3) – packs cardboard.

Pharmacological action

Monophasic oral contraceptive. It inhibits secretion of pituitary gonadotropins. The contraceptive effect of the drug is associated with several mechanisms. Estrogen component of the drug is ethinyl estradiol – synthetic analogue follicular hormone estradiol, involved with the corpus luteum hormone in the regulation of the menstrual cycle. Progestogens component is gestodene – a derivative of 19-nortestosterone, superior strength and selectivity of action is not only a natural hormone progesterone luteum, but other synthetic progestins (eg, levonorgestrel). Due to the high activity of gestodene used in low dosages, in which it does not exhibit androgenic properties and has practically no effect on the lipid and carbohydrate exchanges.

Along with said central and peripheral mechanisms, preventing the maturation of the ability to fertilize the egg, the contraceptive effect is due to a decrease in endometrial receptivity to the blastocyst, as well as an increase in the viscosity of mucus, located in the cervix, which makes it relatively impenetrable to sperm. In addition to the contraceptive effect of the drug when taken regularly and has a therapeutic effect, normalizing menstrual cycle and contributing to the prevention of a number of gynecological diseases, incl. the nature of the tumor.

Pharmacokinetics

Gestodene

Absorption

Once inside quickly and completely absorbed from the gastrointestinal tract. After a single use C_max observed after 1 h and is 2-4 ng / ml. Bioavailability – about 99%.

Distribution

Gestodene binds to albumin and globulin, sex hormone binding (SHBG). 1-2% It stored in the free form in plasma, 50-75% specifically binds with SHBG. Increased SHBG in the blood, called ethinylestradiol, It affects the level of gestodene: increasing fraction, associated with SHBG, and declining fraction, bound to albumin. Average V_d – 0.7-1.4 l / kg. Pharmacokinetics of gestodene is dependent on the level of SHBG. The concentration of SHBG in plasma under the action of estradiol increases 3 times. With daily administration of gestodene concentration in blood plasma increases in 3-4 times in the second half of the cycle reaches a state of saturation.

Metabolism and excretion

Gestodene biotransformed in the liver. The average plasma clearance is 0.8-1.0 ml / min / kg. Gestodene level in serum decreased dwuhfazno. T_1/2 in the β-phase – 12-20 no. Gestodene is displayed only in the form of metabolites, 60% – urine, 40% – with feces. T_1/2 metabolites – about 1 d.

Ethinylestradiol

Absorption

After oral ethinyl estradiol is absorbed rapidly and almost completely. Average C_max of serum is reached after 1-2 hours after administration and was 30-80 pg / ml. The absolute bioavailability of presistemna conjugation and primary metabolism – about 60%.

Distribution

Fully (about 98.5%), but nonspecifically bound to albumin and SHBG level induces an increase in blood serum. Average V_d – 5-18 l / kg.

C_ss set to 3-4 day dosing, and she 20% higher, than after a single dose.

Metabolism

Treated aromatic hydroxylation with the formation of hydroxylated and methylated metabolites, are present in the form of free metabolites or in the form of conjugates (sulfates and glucuronides). Metabolic clearance from the plasma is about 5-13 ml.

Deduction

The concentration in the serum is reduced dwuhfazno. T_1/2 in the β-phase – about 16-24 no. Ethinylestradiol released only in the form of metabolites, in relation to 2:3 urine and bile. T_1/2 metabolites – about 1 d.

Testimony

- Contraception.

Dosage regimen

Assign 1 tab. / day for 21 day, as much as possible at one and the same time of day. After taking the last pill of the box makes the 7-day break, during the withdrawal bleeding which occurs. On the next day after a 7-day interval (ie. through 4 weeks after the first tablet, on the same day of the week) resume taking the drug.

Receiving the first tablet of the drug Lindinet 30 should start from the 1st to the 5th day of the menstrual cycle.

At switching to the drug Lindinet 30 from another combined oral contraceptive first pill Lindinet 30 to be taken after the last pill from the pack of other oral hormonal contraceptive, the first day of withdrawal bleeding.

At the transition to the reception Lindinet 30 with drugs, containing only progestin (“minipill”, injection, Implant), when receiving “minipill” the drug Lindinet 30 You can start on any day of the cycle, go with the use of the implant on the drug Lindinet 30 It can be the day after implant removal, with injections – on the eve of the last injection. In these cases, the first 7 days should apply additional methods of contraception.

After an abortion in the I trimester of pregnancy you can start taking the drug Lindinet 30 immediately after surgery. In this case there is no need for additional contraceptive.

After childbirth or after abortion in the II trimester of pregnancy the drug can be started at 21-28 day. In these cases, the first 7 days necessary to apply additional methods of contraception. At a later beginning of the drug in the first 7 extra days should be used, a barrier method of contraception. When, when the sexual contact occurred before birth, before receiving the drug should exclude pregnancy or postpone the start of the reception until the first menstruation.

At Skipping taking the pill missed tablet must be taken as soon as possible. If the interval tablet-up less 12 no, the contraceptive effect of the drug is not reduced, and in this case there is no need to use an additional method of contraception. The remaining tablets should be taken at the usual time. If the interval is reached more 12 no, the contraceptive effect of the drug can be reduced. In such cases, should not make up the missed dose, the drug continues as normal, however, in subsequent 7 days necessary to use an additional method of contraception. If the packaging remains less 7 tab., the drug of the next pack should be started without a break. In this case, withdrawal bleeding does not occur until completion of the drug from the second packing, but may appear spotting or breakthrough bleeding.

If withdrawal bleeding does not occur after the ingestion of the second package, before the continuation of the drug should exclude pregnancy.

If during the 3-4 hours after taking the drug begins vomiting and / or diarrhea, may reduce the contraceptive effect. In such cases it is necessary to act in accordance with the instructions of missed tablets. If the patient does not want to deviate from the normal mode of contraception, missed pills should be taken from a new package.

To accelerating the onset of menstruation should reduce the break in taking the drug. The shorter the break, the more likely the occurrence of breakthrough bleeding or spotting while taking tablets from the next package (Such cases delayed menstruation).

To delay the onset of menstruation the drug must be continued from the new packaging without the 7-day break. Menstruation can be delayed so long, as required, until the end of reception the last tablet from the second package. At a delay menstruation can occur breakthrough bleeding or spotting. Regular use of the drug Lindinet 30 It can be restored after the usual 7 day break.

Side effect

Side effects, requiring discontinuation of the drug

Cardio-vascular system: arterial hypertension; rarely – arterial and venous thromboembolism (v.t.ch. myocardial infarction, stroke, deep vein thrombosis of the lower limbs, pulmonary embolism); rarely – arterial or venous thromboembolism liver, mesenteric, kidney, retinal arteries and veins.

From the senses: hearing loss, due to otosclerosis.

Other: hemolytic uremic syndrome, porphyria; rarely – Reactive worsening of systemic lupus erythematosus; rarely – Huntington Sidenhema (passing after drug withdrawal).

Other side effects are more common, but less severe. Desirability of the continuation of the drug is solved individually after consultation with the doctor, based on the benefit / risk ratio.

On the part of the reproductive system: acyclic bleeding / spotting from the vagina, amenorrhea after discontinuation of the drug, change in the state of vaginal mucus, the development of inflammation of the vagina, candidiasis, voltage, pain, breast enlargement, galactorrhea.

From the digestive system: epigastric pain, nausea, vomiting, Crohn's disease, yazvennыy colitis, emergence or worsening jaundice and / or pruritus, associated with cholestasis, cholelithiasis, hepatitis, liver adenoma.

Dermatological reactions: uzlovataya эritema, erythema, rash, chloasma, increased hair loss.

CNS: headache, migraine, mood lability, depression.

From the senses: hearing loss, increased sensitivity of the cornea (while wearing contact lenses).

Metabolism: fluid retention, change (increase) body weight, reduced tolerance to carbohydrates, giperglikemiâ, increase in TG.

Other: allergic reactions.

Contraindications

- The presence of severe and / or multiple risk factors for venous or arterial thrombosis (incl. complicated valvular lesions, Atrial fibrillation, cerebrovascular disease, or coronary artery, hypertension severe or moderate with BP ≥ 160/100 mmHg.);

- An indication of the presence or a history of thrombosis precursors (incl. tranzitornaya ishemicheskaya attack, angina);

- Migraine with focal neurological symptoms, incl. history;

- Venoznыy or arteryalnыy thrombosis / tromboэmbolyya (incl. myocardial infarction, stroke, deep vein thrombosis shin, pulmonary embolism) in the present or past;

- The presence of venous thromboembolism;

- Surgery with prolonged immobilization;

- Diabetes (with angiopathy);

- Pancreatitis (incl. history), accompanied by severe hypertriglyceridemia;

- Dyslipidaemia;

- Severe liver disease, cholestatic jaundice (incl. Pregnancy), hepatitis, incl. history (to the normalization of functional and laboratory parameters and within 3 months after the normalization of their);

- Jaundice while taking corticosteroids;

- Gallstone disease now or in history;

- Gilbert's syndrome, Dubin-Johnson syndrome, Rotor syndrome;

- Liver tumors (incl. history);

- Severe itching, otosclerosis or progression during a previous pregnancy or GCS;

- Hormone-dependent malignancies genitals and mammary glands (incl. for suspected them);

- Vaginal bleeding of unknown etiology;

- Smoking age 35 years (more 15 cigarettes per day);

- Pregnancy or suspected it;

- Lactation;

- Hypersensitivity to the drug.

FROM caution should be prescribed for conditions, increase the risk of venous or arterial thrombosis / embolism: older than 35 years, smoking, a genetic predisposition to thrombosis (thrombosis, myocardial infarction or cerebrovascular accident at a young age in any of the next of kin), hemolytic uremic syndrome, hereditary angioedema, liver disease, disease, for the first time created or aggravated during pregnancy or previous use of the background of sex hormones (incl. porphyria, Herpes pregnant, chorea / disease Sydenham /, Huntington Sidenhema, chloasma), obesity (body mass index 30 kg / m²), dyslipoproteinemia, arterial hypertension, migraine, epilepsy, valvular heart disease, fibrillyatsiya predserdiya, prolonged immobilization, major surgery, surgery of the lower limbs, severe injury, varicose veins and superficial thrombophlebitis, postpartum (not lactating women /21 the day after the birth /; lactating women after the lactation period), the presence of severe depression, (incl. history), changes in biochemical parameters (Activated protein C resistance, hyperhomocysteinemia, antithrombin III deficiency, deficiency of protein C or S, antiphospholipid antibodies, incl. antibodies to cardiolipin, volchanochnyi anticoagulant), diabetes, not complicated by vascular disorders, SLE, Crohn's disease, yazvennыy colitis, drepanocytemia, hypertriglyceridemia (incl. family history), acute and chronic liver disease.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

The small amounts of the components of the drug are excreted in breast milk.

When used in lactation may decrease the milk.

Cautions

Before the start of the drug necessary to carry out general medical (a detailed family and personal history, measurement of blood pressure, laboratory research) and gynecological examination (incl. breast examination, pelvic, cytological analysis of cervical smears). A similar survey in the period of the drug is carried out on a regular basis, every 6 Months.

The drug is a reliable contraceptive: Pearl Index (It measures the number of pregnancies, occurring during the use of contraceptive methods in 100 for women 1 year) when properly used is about 0.05. Because, that the contraceptive effect of the drug from the beginning of the reception fully manifested to 14 Day, in the first 2 week dosing, it is recommended to use an additional non-hormonal methods of contraception.

In each case, before prescribing hormonal contraceptives alone are estimated benefits and possible negative effects of their reception. This issue should be discussed with the patient, that after receiving the necessary information to take a final decision on preference hormone or any other method of contraception.

The health status of women should be carefully monitored. If during treatment appears or worsens any of the following conditions / diseases, you need to stop taking the drug and go to another, non-hormonal methods of contraception:

- Diseases of hemostasis;

- Conditions / diseases, predisposing to the development of cardiovascular, renal failure;

- Epilepsy;

- Migraine;

- The risk of estrogen-dependent tumors or estrogen-dependent gynecological diseases;

- Diabetes, not complicated by vascular disorders;

- Severe depression (if depression is associated with impaired metabolism of tryptophan, the purpose of correction can be applied vitamin B₆);

- Sickle cell anemia, tk. in some cases (eg, infection, gipoksiya) estrogensoderzhaschie drugs in this pathology can provoke thromboembolic events;

- Occurrence of abnormalities in laboratory tests evaluating liver function.

Thromboembolic disease

Epidemiological studies have shown, that there is a link between the use of oral hormonal contraceptives and an increased risk of arterial and venous thromboembolic disease (incl. myocardial infarction, stroke, deep vein thrombosis of the lower limbs, pulmonary embolism). We prove an increased risk of venous thromboembolic disease, but it is considerably less, than during pregnancy (60 accidents 100 thousand pregnancies). When using oral contraceptive agents is very rare, arterial or venous thromboembolism liver, mesenteric, renal vessels or vessels of the retina.

The risk of arterial or venous thromboembolic disease increases:

- With age;

- When smoked (heavy smoking and age over 35 years refer to the risk factors);

- If there is a family history of thromboembolic disease (eg, parents, brother or sister). If you suspect a genetic predisposition, is necessary before using the product to consult with a specialist;

- Obesity (body mass index 30 kg / m²);

- When dyslipoproteinemia;

- In hypertension;

- In diseases of the heart valves, complicated with hemodynamic compromise;

- Atrial fibrillation;

- For patients with diabetes, complicated vascular lesions;

- During prolonged immobilization, after the big surgery, after surgery on the lower extremities, after serious injury.

In these cases, it assumed temporary cessation of the drug (not later than, than 4 weeks before surgery, A resume – not earlier, than 2 weeks after remobilization).

In women after giving birth increases the risk of venous thromboembolic disease.

It should be taken into account, that diabetes, systemic lupus erythematosus, hemolytic uremic syndrome, Crohn's disease, nespetsificheskiy yazvennыy colitis, drepanocytemia, increase the risk of venous thromboembolic disease.

It should be taken into account, that resistance to activated protein C, hyperhomocysteinemia, deficiency of protein C and S, antithrombin III deficiency, the presence of antiphospholipid antibodies, increase the risk of arterial or venous thromboembolic disease.

In assessing the benefit / risk ratio of the drug should be considered, that the targeted treatment of this condition reduces the risk of thromboembolism. The symptoms of thromboembolism are:

- Sudden pain in the chest, that radiates to the left arm;

- Sudden shortness of breath;

- Any unusually severe headache, continuing a long time, or first appears, especially when combined with the sudden total or partial loss of vision or diplopia, afaziej, dizziness, collapse, focal epilepsy, weakness or numbness in half of the body expressed, movement disorders, strong one-sided pain in the calf muscles, acute abdomen.

Neoplastic Diseases

Some studies have reported an increase in the frequency of cervical cancer in women, which for a long time took hormonal contraceptives, but research results are contradictory. In the development of cervical cancer play a significant role sexual behavior, infection with the human papilloma virus, and other factors.

Metaanaliz 54 Epidemiological studies have shown, that there is a relative increase in the danger of breast cancer among women, taking oral hormonal contraceptives, however, a higher detection rate of breast cancer could be associated with a regular medical examinations. Breast cancer is rare in women younger than 40 years, regardless of Togo, they take hormonal contraceptives or not, and increases with age. Pills can be regarded as one of the many risk factors. Nonetheless, the woman should be advised of the possible risk of breast cancer, based on the assessment of benefit-risk ratio (protection against ovarian cancer and endometrial).

There are a few reports on the development of benign or malignant liver tumors in women, taking long-term hormonal contraceptives. It should be borne in mind in the differential-diagnostic evaluation of abdominal pain, that may be associated with an increase in liver size or intraperitoneal bleeding.

Chloasma

Chloasma can develop in women, having a history of the disease during pregnancy. Those women, in which there is a risk of occurrence chloasma, it is necessary to avoid exposure to sunlight or ultraviolet radiation while taking Lindinet 30.

Effectiveness

Efficacy may be reduced in the following cases: Missed pills, vomiting and diarrhea, the simultaneous use of other drugs, reduce the effectiveness of birth control pills.

If the patient is simultaneously taking other drugs, which may reduce the effectiveness of birth control pills, should use additional methods of contraception.

Efficacy may be reduced, If after several months of use appear irregular, spotting or breakthrough bleeding, In such cases it is advisable to continue taking pills until their closure in the following packaging. If at the end of the second cycle menstrualnopodobnoe bleeding begins or acyclic bleeding does not stop, stop taking the tablets and to resume it only after excluding pregnancy.

Changes in laboratory parameters

Under the influence of oral contraceptive pills – due to the estrogen component – It may change the levels of certain laboratory parameters (functional parameters of the liver, kidney, adrenal, Thyroid, hemostasis, lipoprotein and transport proteins).

Additional Information

After acute viral hepatitis drug should be taken after normalization of liver function (no earlier than 6 Months).

When diarrhea or intestinal disorders, vomiting contraceptive effect may be reduced. Without stopping taking the drug, you must use an additional non-hormonal methods of contraception.

Women who smoke have an increased risk of cardiovascular disease with serious consequences (myocardial infarction, stroke). The risk depends on the age (especially in older women 35 years) and the number of cigarettes smoked.

It should warn the woman, that the drug does not protect against HIV infection (AIDS) and other diseases, sexually transmitted.

Effects on ability to drive vehicles and management mechanisms

Studies on the effect of the drug Lindinet 30 the ability, necessary for driving and industrial machinery, not performed.

Overdose

Not described severe symptoms after taking the drug at high doses.

Symptoms: nausea, vomiting, vaginal bleeding (young girls).

Treatment: appoint symptomatically, No specific antidote.

Drug Interactions

Contraceptive activity Lindinet 30 decreases while taking ampicillin, tetracycline, rifampicin, ʙarʙituratami, primidone, karʙamazepinom, phenylbutazone, phenytoin, griseofulvin, topiramatom, felʙamatom, oxcarbazepine. Contraceptive effect of oral contraceptives reduced by the use of combinations of data, frequent breakthrough bleeding and menstrual disorders. During the reception Lindinet 30 with the above drugs, as well as for 7 days after the completion of their admission should be applied in addition hormonal (condom, spermicidal gels) methods of contraception. When using rifampicin additional methods of contraception should be used for 4 weeks after the completion of its reception.

In an application with Lindinet 30 any drug, increases the motility of the gastrointestinal tract, It reduces the absorption of active substances and their level in the blood plasma.

Ethinyl sulfation occurs in the intestinal wall. Preparations, are also subjected to sulphation in the gut wall (incl. vitamin C), competitively inhibit the sulfation of ethinyl estradiol and thereby increase the bioavailability of ethinyl estradiol.

Inductors of microsomal liver enzymes decrease ethinyl estradiol levels in the blood plasma (rifamiiцin, barbiturates, phenylbutazone, phenytoin, griseofulvin, topiramate, gidantoin, felʙamat, rifabutin, oskarʙazepin). Inhibitors of liver enzymes (itraconazole, fluconazole) ethinyl estradiol increases the level of blood plasma.

Some antibiotics (ampicillin, tetracycline), preventing intrahepatic circulation of estrogens, reduce the level of ethinyl estradiol in the plasma.

Ethinylestradiol by inhibiting liver enzymes or acceleration conjugation (primarily glyukuronirovaniya) It may affect the metabolism of other drugs (incl. cyclosporine, theophylline); concentrations of these drugs in the blood plasma can rise or descend.

In an application Lindinet 30 with drugs St. John's wort (incl. infusion) reduced concentration of active substances in the blood, that can lead to breakthrough bleeding, pregnancy. The reason for this is the effect of St. John's wort induces liver enzymes, which continues even 2 weeks after the completion of receiving St. John's wort. Do not assign this combination of drugs.

Ritonavir AUC snizhaet of эtinilэstradiola 41%. In this regard, during use of ritonavir to be applied hormonal contraceptive with a higher content of ethinyl estradiol or additionally apply hormonal contraceptives.

You may need correction mode when used hypoglycemic agents, tk. Oral contraceptives can reduce carbohydrate tolerance, increase the need for insulin or oral antidiabetic agent.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 30 ° C. Shelf life – 3 year.