Pharmacological properties monophasic combined contraceptive drug with anti-androgen activity. Blocks androgen receptors, inhibits the secretion of pituitary gonadotropins. The mechanism of action is due to its constituent steroidal antiandrogen buildings – andriol for sale acetate and oral estrogen – ethinyl estradiol. andriol for sale has the ability to competitively bind to the receptors of the natural male sex hormones – androgens (testosterone, dehydroepiandrosterone, androstenedione, and others.), Produced in small quantities in the body of women, mainly in the adrenal glands, ovaries and skin. By blocking the androgen receptors in target organs, reduces androgenization phenomenon in women (due to violations of the processes mediated by the hormone-receptor complex on the main level of intracellular mechanisms). Along with antiandrogenic properties, it possesses progestational activity simulating properties luteum hormone. andriol for sale, possessing progestin activity, inhibits the secretion of pituitary gonadotropins and inhibits ovulation, which accounts for its contraceptive effect. Ethinyl estradiol enhances the central and peripheral effect of andriol for sale ovulation, retains a high viscosity of the cervical mucus, which hinders the penetration of sperm into the uterus and helps to ensure a reliable contraceptive effect.
The pharmacokinetics of andriol for sale acetate : completely absorbed after oral administration. After receiving 1 tablet 35 Bellona maximum serum concentration of 15 ng / ml and is created through 1.6 hours. Almost entirely bound to plasma albumin. During the course of treatment is observed drug accumulation, his serum concentration is increased from 15 ng / ml on the first day of treatment, up to 21 ng / ml at the end of the first cycle and 24 ng / ml at the end of the third treatment cycle. The area under the curve of concentration vs. time is increased by 2.2 times (the end of the first cycle) and 2.4 times (end of the third cycle).The equilibrium concentrations are approximately 16 days after initiation of treatment. The bioavailability is 88% of the administered dose. The half-life of plasma dvufazny period, the first phase – 0.8 hours, the second phase – 2.3 days. The total clearance is 3.6 ml / min / kg. Metabolized in the liver by a variety of reactions, including hydroxylation and conjugation. . The main metabolite – 15-hydroxy-andriol for sale Part of the administered dose excreted unchanged in the bile;the main way of elimination – kidneys as metabolites. Half-life of the kidneys and the bile is 1.9 days. Ethinylestradiol : after ingestion rapidly and completely absorbed. After receiving 1 tablet 35 Bellona maximum serum concentration of 80 pg / ml, and is created through 1.7 hours. Plasma half-life biphasic, the first phase of -1-2 hours, the second phase -. 20 hours, apparent volume of distribution of 5 l / kg, the plasma clearance – 5 ml / min / kg. Almost completely bound to plasma proteins. During the suction and the first passage through the liver is metabolized, resulting in reduced bioavailability. Equilibrium concentration generated 3-4 days after initiation of treatment. Displayed as metabolites through the intestine and kidney (4:6 ratio), the half-life is about 1 day.
- Contraception in women with androgenization events
- The treatment of androgen-dependent diseases / conditions in women ( “vulgar” acne (acne papulopustulosa, acne nodulocystica); seborrhea, androgenetic alopecia, hirsutism).
- Pregnancy and lactation.
- Thrombosis (venous and arterial) and thromboembolism currently or history (including deep vein thrombosis, pulmonary embolism), coronary heart disease, stroke.
- Conditions prior thrombosis (including transient ischemic attack, angina pectoris) now or in history.
- Complicated valvular lesion (pulmonary hypertension, atrial fibrillation, subacute bacterial endocarditis).
- Uncontrolled hypertension (systolic blood pressure above 160 mm Hg. Or diastolic blood pressure greater than 100 mm Hg).
- Major surgery with prolonged immobilization.
- Diabetes mellitus with vascular complications.
- Multiple or severe venous or arterial thrombosis risk factors, including diseases of the brain or blood vessels of the coronary arteries, hypertension, elderly age.
- Liver failure and severe liver disease (liver function tests before normalization); active viral hepatitis, cirrhosis of the liver in the art. decompensation; idiopathic jaundice or pruritus during pregnancy of the former; congenital hyperbilirubinemia (Gilbert syndrome, Dubin-Johnson and Rotor); liver tumors (benign or malignant), or at the moment in history.
- Migraine with focal neurological symptoms in the present or in history.
- Smoke over the age of 35 years.
- Pancreatitis with severe hypertriglyceridemia now or in history.
- Identified hormone cancers (including breast and endometrial cancer), or are suspected.
- Bleeding from the vagina of unknown origin.
- Sickle cell disease, otosclerosis with deterioration during pregnancy, herpes during pregnancy in history.
- Hypersensitivity to any component of the drug.
should carefully weigh the potential risks and expected benefits of the use of combined oral contraceptives in each individual case in the presence of the following diseases / conditions and risk factors:
Risk factors for thrombosis and thromboembolism: smoking; obesity; dislipoproteinemia, hypertension; migraine; valvular disease; prolonged immobilization, major surgery, major trauma; . genetic predisposition to thrombosis (thrombosis, coagulation disorders, myocardial infarction or cerebrovascular accident at a young age in any of the next of kin)
Conditions that may occur peripheral circulatory disorders: diabetes mellitus (or predisposition, eg unexplained glycosuria) ; systemic lupus erythematosus; tetany, renal failure, hemolytic uremic syndrome;Crohn’s disease and ulcerative colitis; varicose veins, phlebitis of superficial veins.
Hypertriglyceridemia, liver disease, breast cancer, family history, or benign tumor of the breast in a personal history of diagnosed depression in the personal history of uterine fibroids, gallstone disease, intolerance to contact lenses.
Diseases for the first time created or aggravated during pregnancy, or on the background of the previous use of sex hormones (eg, jaundice and / or pruritus related to cholestasis, cholelithiasis, porphyria, Sydenham’s chorea, chloasma).
Application of pregnancy and breastfeeding period
The drug is contraindicated during pregnancy and lactation.
Dosing and Administration
Bellona 35 are inside of 1 tablet per day, with liquid squeezed small amount of liquid. The reception should be made every day in the same selected hour, preferably after breakfast or dinner.
Reception Bellona 35 start in the 1st day of the menstrual cycle ( ie the first day of menstrual bleeding ), using a tablet corresponding day of the week of the calendar packaging.
The daily intake of the drug was carried out using a tablet of the calendar packaging sequentially in the direction of arrows printed on the foil until all the pills are taken. After receiving all of the tablets 21 calendar packaging is a break in the reception duration of drug 7 days, during which bleeding occurs menstrualnopodobnoe.
After 28 days from the start of treatment (21 days and 7 days reception interval), i.e. on the same day of the week, as in the beginning of the course, continue taking the drug from the next pack. In the transition from 21-day combined oral contraceptive intake Bellona 35 should begin the day after the last previous drug pills, but in any case no later than the next day after the usual 7 day break in reception.Further, according to the scheme described above. The use of additional contraception is needed. In the transition from 28-day combined oral contraceptive intake Bellona 35 should begin the day after the last active pill. Further, according to the scheme described above. The use of additional contraception is needed. When switching from contraceptives containing only progestin ( “mini-pill”) Bellona 35 should start to apply without interruption. Further, according to the scheme described above. The use of additional contraception is needed. If you are using injectables contraceptives Bellona 35 begin to take on the day when the next injection should be done. When changing from an implant – on the day of its removal. In all cases, you must use an additional barrier method of contraception (condom) during the first 7 days of taking the pills. After the abortion I trimester of pregnancy a woman can begin taking the drug immediately. In this case, the woman does not need any additional contraceptive methods. After delivery or abortion in the II trimester of pregnancy, the drug should start at 21-28 minutes per day. If the reception is started later, you must use an additional barrier method of contraception (condom) during the first 7 days of taking the pills. If a woman has been sexually active in the period between the birth or abortion and the beginning of the reception Bellona 35, you must first rule out pregnancy or the need to wait for the first menstrual period. missed tablet the woman should take as soon as possible, the next tablet is taken at the usual time. At delay of less than 12 hours, contraceptive reliability is not reduced. If the delay in receiving the tablets accounted for more than 12 hours, contraceptive reliability can be reduced. It should be borne in mind that a pill should never be interrupted for more than 7 days, 7 days, and that continuous administration of tablets required to achieve adequate suppression of the hypothalamic-pituitary ovarian system. Therefore, if the delay in taking the pill was more than 12 hours (range since taking the last pill more than 36 hours) during the first and second weeks of taking the drug, the woman should take the last missed tablet as soon as possible, as soon as you remember (even if this means taking two tablets at the same time). Next tablet is taken at the usual time. Additionally, you should use a barrier method (condom) for the next 7 days. If the delay in taking the pill was more than 12 hours(range since taking the last pill more than 36 hours) during the third week of taking the drug, the woman should take the missed pill as possible rather, as soon as you remember (even if this means taking two tablets at the same time). Next tablet is taken at the usual time. Furthermore, a pill from a new package to be started as soon as the current package, i.e. no 7 day break. Additionally, you should use a barrier method (condom) for the next 7 days. It is likely that the woman will not be withdrawal bleeding until the end of the second pack, but she may experience spotting or breakthrough uterine bleeding in the days of taking the pills. If you forget to receive 3 or more pills should consult your doctor. If a woman has been vomiting or diarrhea within 3 to 4 hours after administration Bellona 35, absorption of the active substances may be incomplete. In this case, you need to focus on the recommendations by skipping pills. If a woman does not want to change the normal dose, it must take, if necessary, an additional tablet (or more tablets) from a new package. In order to delay the onset of menstruation , the woman should continue taking pills from a new package Bellona 35 immediately after taken all tablets from the previous one, without a break in the reception. Tablets of this new packaging may be taken for as long as the woman wants (as long as the packaging is not finished). Against the background of the drug from the second package, women may experience spotting or breakthrough uterine bleeding. Reactivate reception Bellona 35 of the new packaging should be after the usual 7-day break. In order tomove the first day of menstruation to another day of the week , a woman should shorten the next tablet-free interval for as many days, as much as she wants. The shorter the interval, the higher the risk that she will not have withdrawal bleeding will continue to spotting and breakthrough bleeding while taking second pack (just as when she wanted to delay the onset of menses). In the treatment of hyperandrogenic states the duration of reception determined by the severity of the disease. After the disappearance of the symptoms it is recommended to take 35 Bellona at least another 3-4 months. In case of relapse after a few weeks or months after completion of therapy can be carried out re-Bellona 35.
All women taking combined oral contraceptives are at increased risk of thrombosis and thromboembolism, some increase in the risk of occurrence and worsening of other diseases (see. Section “Precautions”). When you receive a combined oral contraceptives may experience irregular (acyclic) vaginal bleeding (spotting or breakthrough bleeding), especially during the first months of treatment.
Most – more than 1/100 and less than 1/10, rarely – more and less than 1/1000 1/100, rarely – more than 1/10000 and less than 1/1000,
Common: nausea, abdominal pain, weight gain, headache, depression, mood changes, breast pain, breast tenderness
not often vomiting, diarrhea , fluid retention, headache, decreased libido, skin rash, hives, breast hypertrophy.
rare: intermenstrual bleeding, oligomenorrhea, increased libido, weight loss, deterioration tolerability of contact lenses, allergic reactions, erythema nodosum, erythema multiforme; long-term use – chloasma.
Overdosing Symptoms : nausea, vomiting, bleeding, to remove the drug. Treatment – symptomatic. No specific antidote.
The interaction with other drugs
Effect on hepatic metabolism: use of drugs that induce hepatic microsomal enzymes which may lead to increased clearance of sex hormones, which in turn can lead to breakthrough bleeding or decreased contraceptive reliability. Such drugs include phenytoin, barbiturates, primidone, carbamazepine, rifampicin, rifabutin, also possible – oxcarbazepine, topiramate, felbamate, griseofulvin preparations containing St. John’s wort.
HIV protease (such as ritonavir) and non-nucleoside reverse transcriptase inhibitors (e.g., NVP), and combinations thereof are also potentially affect hepatic metabolism.
during reception drugs affecting microsomal enzymes and for 28 days after their removal should additionally use a barrier method of contraception.
Effect on enterohepatic circulation: some antibiotics (e.g. penicillin and tetracycline) can reduce circulating estrogen kishechnopechenochnuyu, thereby reducing the concentration of ethinyl estradiol.
during reception antibiotics (such as penicillins and tetracyclines) and for 7 days after their removal should additionally use a barrier method of contraception. If the period of use of barrier protection method ends later than pills in the package, it is necessary to move the next package Bellona 35 without the usual tablet-free interval.
Oral combined contraceptives may affect the metabolism of other drugs, which leads to an increase (e.g., cyclosporin) or decrease ( eg, lamotrigine), their concentration in the plasma and tissues.
It may require correction dosing regimen hypoglycemic agents.
If any of the conditions, diseases, and the risk factors listed below are currently available, you should carefully weigh the potential risks and expected benefits of the use of combined oral contraceptives in each individual case and discussed with the woman before she decides start taking the drug. In the event of aggravation, the gain or the first manifestation of any of these conditions, diseases or risk factors, the woman should consult with your doctor, who can decide whether to cancel the drug. Diseases of the cardiovascular system are available to increase the frequency of data of venous and arterial thrombosis and thromboembolism (such as deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke) when taking combined oral contraceptives. These diseases are rare. The risk of venous thromboembolism is greatest in the first year of receiving such drugs. The risk of thrombosis (venous and / or arterial) and thromboembolism is increased:
- with age;
- smokers (with the number of cigarettes or increasing age the risk further increases, especially in women over 35 years old);
in the presence of:
- family history (ie venous or arterial thromboembolism ever in close relatives or parents at a relatively young age). In the case of hereditary predisposition, the woman should be assessed and the appropriate specialist to resolve the question of the possibility of using combined oral contraceptives;
- obesity (body mass index over 30 kg / m 2 );
- diseases of the heart valves;
- atrial fibrillation;
- prolonged immobilization, major surgery, any surgery to the legs, or major trauma. In these situations, it is desirable to discontinue the use of combined oral contraceptive (in case the intended operation of at least four weeks prior to it) and not to resume reception within two weeks after the immobilization.
The question of the possible role of varicose veins and superficial thrombophlebitis in venous thromboembolism remains controversial.
It is necessary to take into account the increased risk of thromboembolism during the postpartum period. Peripheral circulatory disorders also may occur in diabetes mellitus, systemic lupus erythematosus, tetany, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn’s disease or ulcerative colitis) and sickle cell disease.
The increase in the frequency and severity of migraine during use of combined oral contraceptives ( which may be preceded by a cerebrovascular accident) may be a reason for immediate discontinuation of these drugs. Tumors An important risk factor for cervical cancer is HPV persistence. The results of some epidemiological studies suggest a further increase of the risk of long-term use of combined oral contraceptives (CCP), however, this assertion remains controversial, as finally established, as far as the results of studies into account associated risk factors, such as screening for cervical status and sexual behavior including a rare use of barrier methods of contraception. The relationship between the intake of PDAs and breast cancer has not been proven. There is a slightly increased relative risk of developing breast cancer diagnosed in women taking the CPC now. The increased risk disappears gradually within 10 years after discontinuation of these drugs. The observed increase in risk may be the result of careful observation and an earlier diagnosis of breast cancer in women who use PDAs cancer. Women who had ever used a PDA, revealed earlier stages of breast cancer and clinically it is less pronounced than in women, never let them apply. In individual cases, the background of the CCP observed the development of benign and extremely rare – malignant liver tumors which in some cases led to life-threatening intra-abdominal haemorrhage. In case of severe pain in the abdomen, liver enlargement or signs of intra-abdominal bleeding differentsionnoy diagnosis should take into account the possibility of a tumor of the liver in patients taking the CPC. Other conditions Women with hypertriglyceridemia (or the presence of the state in family history) may increase the risk of pancreatitis while taking combined oral contraceptives. in spite of the fact that a small increase in blood pressure has been described in many women receiving combined oral contraceptives, clinically significant elevations have been rare.However, if while taking combined oral contraceptives develops persistent, clinically significant increase in blood pressure, should be discontinued these drugs and begin treatment of hypertension.Acceptance of combined oral contraceptives may be continued if using antihypertensive treatment achieved normal blood pressure values. The following conditions have been reported to develop or worsen both during pregnancy and while taking combined oral contraceptives, but their relationship with the intake of combined oral contraceptives do not proved: jaundice and / or pruritus related to cholestasis; the formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; chorea; herpes gestationis; hearing loss associated with otosclerosis. Cases of Crohn’s disease and ulcerative colitis during treatment with combined oral contraceptives have also been described. In women with hereditary forms of angioedema exogenous estrogens may induce or worsen symptoms of angioedema.Acute or chronic disturbances of liver function may require the cancellation of combined oral contraceptives as long as liver function tests have not returned to normal. Recurrent cholestatic jaundice, which develops for the first time during pregnancy or previous use of sex hormones, requires discontinuation of combined oral contraceptives. Although combined oral contraceptives may have an effect on insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetics using low-dose COCs (<0.05 mg ethinylestradiol). However, women with diabetes should be carefully observed while taking combined oral contraceptives. Sometimes it can develop chloasma, especially in women with a history of chloasma during pregnancy. Women with a tendency to chloasma while taking combined oral contraceptives should avoid prolonged exposure to sunlight and ultraviolet radiation. Treatment (contraception) should be immediately discontinued if pregnancy occurs, the development of migraine headaches (if they were not before), the appearance of early signs of phlebitis or phlebothrombosis (unusual pain or swelling of veins), with the appearance of jaundice, visual disturbances, cerebrovascular disorders, stabbing pain of unknown etiology when breathing or coughing, pain and tightness in the chest, with the increase in blood pressure. The reception also stopped 3 months before planned pregnancy, 6 weeks before the planned surgery and during prolonged immobilization. If diarrhea and vomiting contraceptive effect is reduced, therefore, not stopping taking the drug, it is necessary to use additional non-hormonal contraceptive methods. Laboratory tests using combined oral contraceptives can affect the results of certain lab tests, including liver function tests, kidney, thyroid gland, adrenal glands, the level of traffic proteins in plasma, carbohydrate metabolism, coagulation and fibrinolysis parameters. It is necessary to warn the laboratory personnel on oral contraceptives. To change the results of skin allergy tests, reduction in the concentration of LH and FSH. Due to the fact that the contraceptive effect is fully manifested to the 14th day from the beginning of the reception, in the first 2 weeks is recommended to further apply hormonal (barrier) methods of contraception. The drug has no effect on the course of puberty, during the formation of the normal menstrual cycle. Appointment after childbirth is not recommended before the first normal menstruation after childbirth. In the case of acyclic bleeding during the first 3 weeks of hormonal contraception – perhaps a continuation of the drug – usually bleeding stopped on their own. In the absence of bleeding during the 7-day interval between administration of the drug, the pills should be stopped prior to removal of pregnancy. The influence of the menstrual cycle on the intake of combined oral contraceptives may experience irregular (acyclic) bleeding / vaginal bleeding (spotting or breakthrough bleeding ), especially during the first months of use. Therefore, the evaluation of any irregular bleeding should be done after the adjustment period of approximately three cycles. If the irregular bleeding recur or occur after previous regular cycles, you should conduct a thorough examination to exclude malignancy or pregnancy. Some women during the tablet-free interval may not develop withdrawal bleeding. If combined oral contraceptives are taken according to the recommendations, it is unlikely that the woman is pregnant. However, the irregular use of combined oral contraceptives and the absence of two consecutive withdrawal bleeding, the drug can not be extended to exclude pregnancy. Medical check-ups Before you start or resumption of the use of Bellona 35 women drug should conduct a thorough medical, including measurement of blood pressure, heart rate cuts, body mass index, and gynecological examination, including a study of mammary glands and cytological examination of scrapings from cervical (Pap test), exclude pregnancy. The amount of additional research and the frequency of check-ups is determined individually. Typically, control examinations should be carried out at least 2 times a year. It is necessary to warn the woman that drugs such as Bellona 35 do not protect against HIV infection (AIDS) and other sexually transmitted diseases through! buy anabolic steroids online bruce lee’s workout anabolic steroids online uk