Cyclo-Progynova Bayer drugs treated estrogen deficiency syndrome (1 blister x 21 tablets)

Pharmacokological

estrogen in Cyclo - Progynova is Estradiol Valerate, a precursor of 17 - Beta - Estradiol naturally in the human body. The structure of Norgestrel is a Progestogen complex. With the ingredients and mode of regular use of Cyclo - Progynova include using estrogen a one -phase for 11 days and combining estrogen - progestogen for 10 days, followed by 7 days of stopping the medication, if used regularly, there will be normal menstrual cycles in the case of the uterus intact.

Ovulation is usually not inhibited during the use of cyclo - progynova and the production of endogenous hormones is seriously affected. This preparation can be used for young women to create and regulate menstruation as well as treat abnormal uterine bleeding during menopause.

During menopause, the decline and loss of estradiol production process of the ovaries can lead to changes in body temperature, hark accompanied by insomnia and sweating, atrophy of the urinary organs with vaginal dryness syndrome. Pain during intercourse and uncontrolled urination.

Not characteristic but often mentioned similar to symptoms during menopause are signs of angina, tachycardia, irritability, neurasthenia, reduced capacity and concentration, forgetting, decreased sexual ability, muscle aches.

Hormone replacement therapy (HRT) will reduce the above -mentioned syndrome due to the lack of estradiol for women during menopause. Hormone replacement therapy with equilibrium dose of estrogen in cyclo - progynova reduces the risk of osteoporosis and slows bone loss during premenopause.

When stopping treatment with this therapy, the mass of the bone is equivalent to the early stages of the postmenopausal period. There is no evidence that hormonal replacement therapy retains the mass of bones as in the premenopausal stage. Hormone replacement therapy has a positive effect on the skin and skin thickness ingredients while slowing down the skin's wrinkle process.

pharmacokinetics

estradiol valeate

absorption

Estradiol Valerate is absorbed quickly and completely. This steroid ester is separated into estradiol and valeric acid during the first absorption and liver absorption process. At the same time, the amount of estradiol under many metabolic processes later, for example into estrogen, estriol and estrone sulfate. Only about 3% of Estradiol becomes a form of bioavailability after drinking. Food does not affect the bioavailability of Estradiol.

Distribution

The maximum concentration of estradiol in plasma is 30pg/ml, achieved within 4 - 9 hours after drinking. 24 hours after drinking, estradiol concentration drops to 15pg/ml. Estradiol is connected to albumin and globulin associated with sex hormones (SHBG). However, the cohesion ratio of Estradiol's SHBG is lower than the ratio of cohesion to the SHBG of Levonorgestrel.

Metabolism

After the exile estradiol is separated the ester, the drug is metabolized through the biological transformation path of endogenous estradiol. Estradiol is metabolized in the liver, but it is also metabolized in other organs other than the liver such as the intestines, kidneys, musculoskeletal systems and other target organs.

These processes are involved in the formation of Estron, Estriol, Catecholestrogen and Sulfate and the glucuronide links of the small components of estrogenic or nonestrogenic.

Elimination

The total serum clearance of estradiol after taking a single dose by vein, very different from 10 - 30ml/minute/kg. A certain amount of Estradiol's metabolites is exported into bile fluid and participates in the circulatory round of the liver - intestines.

The metabolism of estradiol in the final stage is mainly excreted into sulfate form and glucuronide in the urine.

Norgestrel

absorption

Norgestrel is absorbed quickly and completely after drinking. The active ingredient of Norgestrel is Levonogestrel, a substance with an active activity equivalent to about half of the dose of Norgestrel.

Distribution

The maximum concentration of levonorgestrel in serum 7 - 8ng/ml and achieved within 1 - 1.5 hours after taking a single dose of Cyclo - Progynova. The concentration of levonogestrel will then be reduced to 2 stages with the average selling time within 27 hours and the minimum concentration reached about 1ng/mL within 24 hours after taking the drug.

levonogestrel is connected to albumin and SHBG in plasma. Only about 1 - 1.5% of the total amount of levonogestrel in plasma is not associated with protein. The relationship between free drug ratio, associated with albumin and cohesion with SHBG depends heavily on the concentration of SHBG in plasma.

After cohesion to protein, the part that is connected to SHBG increases while the drug parts associated with albumin and the drug in the form of freelance decrease. At the end of the time when using estrogen alone when using Cyclo - Progynova, the concentration of SHBG reaches the highest concentration in the serum and later will decrease to the lowest concentration at the end of the period of combined drug use.

Accordingly, the amount of freely Lenovogestrel is at 1% at the start of the beginning and reaches 1.5% at the end of the period of combining drug use. The amount of Lenovogestrel achieved at the two times mentioned above is 70 and 65%.

Metabolism

Norgestrel is completely metabolized. Levonogestrel's biodegrad process follows steroid's metabolism. Pharmacological characteristics of metabolites are not known.

Elimination

The total serum clearance is 1ml/min/kg. With an average selling time of about 1 day, approximately an equivalent amount of metabolites of Norgestrel is eliminated into urine and in bile fluid.

Caution when using

cyclo - progynova is not used for birth control purposes. When taking the drug, the contraceptive should be applied by non -hormonal methods (exception: do not use the method of cyclic calculation and body temperature monitoring). If the possibility of pregnancy can occur, immediately stop taking the drug until this ability to remove this ability.

venous thrombosis

Hormone replacement therapy (HRT) may be associated with an increase in the risk of developing venous embolism due to thrombosis (VTE), for example, deep veins or pulmonary embolism. Careful consideration between the risk and benefits of drug use and advise patients on the risk of hormone use instead of women with risk factors.In general, risk factors for venous thrombosis can be recognized including personal history, family history (venous thrombosis in people with direct blood relations at a young age may be due to genetic trends) and serious obesity. The risk of venous thrombosis increases with age. The risk of venous thrombosis can temporarily increase when prolonged immobility, postoperative surgery or program surgery, or major injury.

depends on the nature of each case and the time of immobility, it is necessary to consider temporarily stop using HRT. It is necessary to consider the ability to increase the risk of thrombosis in women with many risk factors or have a severe risk factor. This will be much more serious, not simply the sum of risk factors. Do not apply hormone replacement therapy (HRT) for cases of superior risks.

arterial thrombosis

Two major clinical trials have been conducted in combination with conjugated Equine estrogen (CEE) with Medroxy Progestogen Acetate (MPA), hormones used in hormone therapy instead of the risk of coronary artery disease (CHD) that can increase slightly in the first year of use.

Clinical trials with CEE simply show the ability to reduce the rate of CHD in women aged 50 - 59 and absolutely no benefits for the total number of experiments. In these two clinical trials with this hormone, the risk of stroke increased from 30% to 40%.

Diseases of gallbladder

estrogen is thought to increase the risk of gallstones. Some women are likely to suffer from gallbladder diseases during the use of estrogen therapy.

Innovation

Clinical experiments with cee -containing preparations show that it is very little likely to increase the risk of dementia if starting to use this hormone in women over 65 years old. This risk may be reduced if the treatment is started in the early stages of menopause.

tumors

Breast cancer

Clinical observation and clinical research studies have recorded the risk of diagnosed breast cancer increased with women who have used hormone replacement therapy for several years. This finding may be due to early diagnosis, or due to the development of available tumors, or by both. The risk is relatively increasing over time of treatment and may be lower or not increased if treatment with products contains only estrogen.

It is also observed that the risk of breast cancer increases similarly in some cases such as the natural menopause that takes place slowly, drinking alcohol or obesity. This increase is lost in a few years after stopping the use of hormone replacement therapy. The replacement hormone therapy increases the density of X -ray images. In some cases, this may affect the detection of breast cancer from X -ray images.

Ovarian cancer

less common than breast cancer.

Endometrial cancer

liver

In a rare number of cases that have been benign in the liver and more rare is the malignant tumor of the liver after using hormones containing hormones that are similar to drugs used in hormone replacement therapy. In some cases, severe hemorrhage may occur in the abdominal threat of patients' lives. It is advisable to think about the possibility of liver tumors by distinguished diagnosis in the case of symptoms of upper abdominal pain, large liver or signs of bleeding in the abdominal cavity.

The relationship between HRT and clinical hypertension use has not been determined. The mild hypertension in women who use HRT has also been reported. Often rarely have clinical manifestations. However, if in some cases the signs of clinical hypertension lasts continuously during HRT use, may need to stop using the drug.

The liver dysfunctions are not serious, including hyperbilirubin in the blood such as Dubin syndrome - Johnson or rotor syndrome, need to closely monitor and check the liver function periodically. In case of signs of liver failure, HRT should be stopped.

For women with triglycerides an increase in moderate levels that need special monitoring. The use of HRT for these women can increase the triglyceride index, which can cause acute pancreatitis.

Although using HRT can affect insulin resistance in peripherals and glucose tolerance, generally no need to adjust the dose of diabetes treatment drugs during HRT use. However, women with diabetes should be carefully monitored during HRT use.

Some certain cases may appear signs of stimulating estrogenic system during HRT use such as abnormal uterine bleeding. Abnormal or persistent vaginal bleeding during treatment may be a sign to assess endometrial condition.

If the abnormal menstrual treatment is not effective, it is necessary to apply appropriate diagnosis to eliminate diseases of other organs.

Uterine fibroids may increase the size due to the effect of estrogen. If this sign appears, HRT should be stopped.

If endometriosis reappears during treatment, HRT should be stopped.

Need to monitor strict medical (including periodic concentration test) in patients with tumors with prolactin secretion.

The tanning phenomenon is often very rare, common in patients with a history of tanning during pregnancy. Women who tend to be tanning should avoid direct contact with sunlight or ultraviolet rays during HRT use.

The following signs have also been reported as possible or worse when using HRT. However, that does not show that there is a clear related to the use of HRT, these women need to be closely monitored during the use of HRT: epilepsy, benign diseases in the breast, bronchial asthma, migraine, porphyrinuria, osteoporosis, systemic lupus system, mild dance.

In women with genetic angiography, external estrogen can produce or increase angioedema symptoms.

The ability to drive and operate machinery

There has been no research on the ability to drive and operate machinery. No effect has been observed on the ability to drive and operate machinery during the use of the drug. However, the drug causes headaches, depression, dizziness, visual disorders. Therefore, it is necessary to be cautious when driving a train and operating machinery.

Pregnancy

Do not use hormone replacement therapy for pregnant and lactating women. If pregnant during the use of cyclo - progynova, should stop treatment immediately.

Breastfeeding period

Wide -scale epidemic research on the use of hormones steroids shows no increased risk for children born in women who use hormones before pregnancy and no monster manifestation for mothers who use hormones during the first time of pregnancy.

Small amount of sex hormones are exported into breast milk.

Drug interaction

The effect of other drugs on cyclo - Progynova

Interactions that can occur with drugs include microscopic enzymes that can lead to increased clearance of sex hormones and can lead to changes in uterine bleeding or reducing treatment effect.

Medications that increase the clearance of sex hormones (effectively reduced by enzyme induction)

Phenytoin, barbiturates, primidone, carbamazepine, rifampicin and can also oxacarbazepine, topiramate, felbamate, griseofulvin and products containing herbal grass St. John. Enzyme touch may also have been observed after a few days of treatment. Maximum enzyme induction is observed all after 2-3 weeks. After stopping the above -mentioned drugs, enzyme induction can be maintained for about 4 weeks.

Drugs with different effects on the clearance of sex hormones

When used in combination with sex hormones, many protein hydrolytic enzyme inhibitors (HIV/HIV/HIV/HCV and inhibitors still turn young - nucleoside can reduce or increase the plasma concentration of estrogen or progestin. These changes may be clinically related in some cases.

Medications that reduce the clearance of sex hormones (enzyme inhibitors)

Average and powerful CYP3A4 inhibitors such as Azole antifungal (fluconazole, iTraconazole, ketoconazole, voriconazole), verapamil, macrolide (Clarithromycin, erythromycin), Diltiazem and grapefruit juice can increase plasma concentrations of estrogen or ProGestin two.

The active ingredients undergo a conjugated reaction (eg Paracetamol) may increase Estradiol's biodiversity by inhibiting the competition of the combined system during absorption.

Interaction with alcohol

Using alcohol during treatment with hormone replacement therapy can lead to increased estradiol level.

Other types of interactions

Subclinical test results, using sexual steroids can affect certain subclinical test results, including biochemical indicators of the liver, thyroid, adrenal glands and kidney function, the content of proteins (transportation) in plasma, for example, globulin associated with corticosteroids and lipid/ lipoprotein, the number of caroo metabolic indicators and bleeding. These changes are often maintained within the usual range.