Megace (Megestrol, Megace) tablets 160 mg No. 30 - Instructions

Megace (Megestrol, Megace) tablets 160 mg No. 30 - Instructions

Compound

The active component of the drug is megestrol acetate in the amount of 160 mg per tablet.
Other Ingredients: Microcrystalline cellulose, lactose monohydrate, sodium starch glycolate, povidone, magnesium stearate, colloidal anhydrous silica.

Release form

The medicine is available in tablets, 30 pieces per package.

pharmachologic effect

Megestrol is a synthetic steroid, a derivative of chlormadinone. It has progestogenic and antigonadotropic properties, but it does not exhibit androgenic and estrogenic effects. Inhibits ovulation. Megestrol acetate has been used in the treatment of hormone-dependent breast and endometrial cancer. Megestrol reduces or suppresses the stimulating effect of estrogen on receptors, and also has a direct cytotoxic effect on cancer cells. It increases body weight by stimulating appetite and stimulating the growth of fat and muscle tissue.

Pharmacokinetics

Megestrol is well absorbed after oral administration. However, its absorption from the gastrointestinal tract depends on intestinal motility, commensal flora, patient weight, diet, concomitant administration and use of other drugs.

Megestrol can accumulate in adipose tissue.

The liver is primarily responsible for metabolism, producing active metabolites. Megestrol acetate is active at androgen and glucocorticoid receptors, while its metabolites are active at progesterone receptors.

The average half-life is 34.2 hours. The substance is excreted by the kidneys by approximately 66% and by feces by approximately 20%. The portion of the drug that is not excreted through the kidneys or into the gastrointestinal tract is either eliminated through the respiratory system or accumulates in adipose tissue.

Indications for use

Megace is used to treat anorexia and weight loss caused by cancer or AIDS. The drug is also used to treat breast and endometrial cancer.

Contraindications

The medicine is contraindicated in patients with hypersensitivity to the active substance, as well as in patients during pregnancy and breastfeeding.

Side effects

The most common negative effects: diarrhea, nausea, vomiting, erectile dysfunction, weakness, rash.

Drug interactions

Megace should not be used with thalidomide (an immune-suppressing drug) and dofetilide.

You should avoid drinking alcohol while using the drug.

Application and dosage

For the treatment of breast cancer, the dose is 160 mg per day. Anorexia or weight loss - 400-800 mg per day.

The dosage should be carefully selected taking into account possible disorders of the cardiovascular system, liver and kidneys. Comorbidities should also be taken into account. In the case of tumor diseases, the dosage is selected individually by the attending physician.

Overdose

In case of drug poisoning, negative symptoms may increase. Therapy is carried out in accordance with the symptoms that arise.

special instructions

Patients with diabetes may experience an increased need for insulin when taking the drug.

Particular caution should also be exercised in patients with thrombophlebitis.

Using the drug and stopping the drug may slightly suppress adrenal function. If the drug is discontinued abruptly, patients should be monitored for symptoms such as hypotension, dizziness, nausea, and vomiting.

Use during pregnancy and breastfeeding

Due to the risk of harm to the fetus, the use of the drug during pregnancy is strictly contraindicated.

The safety of using Megaice during breastfeeding has not yet been established.

Impact on the ability to drive vehicles and operate machinery

No special precautions are required.

Terms of sale

As prescribed by a doctor.

Storage conditions

At room temperature, in a place out of reach of children.

Kahexan (Megestrol acetate) suspension! 40 mg/ml (9.6 g/pack) bottle 240 ml - Instructions

Dosage form

Oral suspension, 240 ml bottle.

Compound

1 ml of suspension contains 40 mg of megestrol acetate (Megestroli acetas).

Excipients with known effect: sucrose, macrogol 1500, polysorbate 80, xanthan gum, anhydrous citric acid, sodium citrate, orange liquid flavor, sodium benzoate, purified water.

Contains small amounts of ethanol.

pharmachologic effect

Pharmacodynamics

Megestrol acetate is a synthetic steroid with progestational activity and ovulation suppression, which has been used for many years as an anticancer agent in the treatment of breast and endometrial cancer.

The mechanism of the antitumor effect of megestrol acetate in breast cancer and the mechanism of action in anorexia and cachexia have not been fully studied and may involve inhibition of gonadotropin production by the pituitary gland.

Weight gain after treatment with megestrol acetate is associated with improved appetite, increased fat tissue and muscle mass, which is used to treat anorexia or weight loss due to cancer or AIDS.

Pharmacokinetics

Estimation of serum megestrol acetate concentration depends on the method used. Serum concentrations depend on intestinal and hepatic inactivation of the drug, which may be influenced by: gastrointestinal motility, intestinal bacteria, concomitant use of antibiotics, body weight, diet and liver function. There were no clinically significant differences in the bioavailability of products containing megestrol acetate.

Only 5-8% of the administered dose of megestrol acetate is metabolized. The major route of drug elimination in humans is urinary excretion of approximately 66% and fecal excretion of approximately 20% of the administered dose. Secretion in the respiratory tract and deposition in adipose tissue may be affected by that part of the drug that is not excreted in urine or feces. With the simultaneous administration of zidovudine and rifabutin, the pharmacokinetic parameters of megestrol acetate (oral suspension) do not change.

Indications for use

Cahexan oral suspension is indicated for the treatment of anorexia or weight loss due to cancer or acquired immunodeficiency syndrome (AIDS).

Contraindications

• Hypersensitivity to the active substance or any of the excipients.
• Pregnancy and breastfeeding.
• Thromboembolism.

Directions for use and doses

Adults: 10-20 ml (400-800 mg) orally once daily.

It is recommended that use of Cachexan oral suspension be continued for at least two months.

Elderly patients: There is insufficient data from clinical trials of megestrol acetate in patients aged 65 years and older to determine whether it works differently than in younger patients. Based on clinical experience, no differences in its effects have been observed in older and younger patients. Careful dose titration is recommended in the elderly. Because liver, kidney, or heart problems are more common, as well as comorbidities and the use of other medications, treatment is usually started at doses at the lower end of the dosage range.

Megestrol acetate is primarily excreted by the kidneys. Therefore, the risk of its toxic effects may be higher in patients with renal impairment. Because elderly patients are more likely to experience deterioration in renal function, caution should be exercised when determining dosage. Monitoring renal function may also be helpful.

Children and teenagers

The safety and effectiveness of Cachexan oral suspension in children and adolescents has not yet been established.

Mode of application

The suspension should be mixed thoroughly before use.

Special warnings and precautions for use

Cahexan Oral Suspension should not be used during pregnancy or breastfeeding. Progestogens are used from the first trimester of pregnancy to treat recurrent or threatened miscarriages. There is insufficient evidence for the effectiveness of this procedure, and there is a potential risk of fetal harm associated with the use of progestogens in the first four months of pregnancy.

The use of progestogens in women with damaged fetuses can delay spontaneous miscarriage, which is associated with the antispasmodic effect of these drugs on the uterus.

Reports have been published suggesting an association between prenatal exposure to progestogens in the first trimester of pregnancy and urogenital abnormalities in male and female fetuses. The risk of hypospadias of 5 to 8 per 1000 boys in the general population may double after exposure to these drugs. There are insufficient data to assess the risk associated with exposure to fetal progestogens in women, but some of these drugs may cause mild virilization of the external genitalia.

Fertility and reproduction studies in rats using high doses of megestrol acetate have shown a reversible feminizing effect on male fetuses.

Women of childbearing potential should be advised not to become pregnant while taking the medicine. If Cachexan Oral Suspension is used during the first four months of pregnancy, or if a woman becomes pregnant while taking the medication, she should be informed of the potential risk to the fetus.

If abrupt discontinuation occurs, monitor the patient closely, particularly for symptoms such as hypotension, nausea, vomiting, dizziness, and weakness.

Cahexan oral suspension should be used with caution in patients with thrombophlebitis.

It is unknown to what extent the results from canine studies of megestrol acetate-associated cancers may be relevant to humans. However, when assessing the ratio of side effects, this should be taken into account when prescribing Cachexan. Therefore, breast examinations should be performed during examinations during treatment.

Patients with diabetes may have an increased need for insulin.

Cachexane suspension contains a small amount of ethanol (alcohol), less than 100 mg per 20 ml suspension.

Cachexane suspension contains sucrose. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase deficiency should not take Cahexan.

Children and teenagers

The safety and effectiveness of Cachexan in children and adolescents have not yet been established.

Interaction with other drugs and other forms of interaction

There are no known confirmed interactions of megestrol acetate with other concomitant medications.

Effect on fertility, pregnancy and lactation

Pregnancy

Cachexan should not be used during pregnancy. Numerous reports suggest the possibility of potentially harmful effects of drugs in this group on the fetus when used in the first four months of pregnancy. Patients should be advised to use effective methods to avoid becoming pregnant while using Cachexan.

Breast-feeding

It is forbidden to breastfeed while using Kahexan suspension.

Effect on the ability to drive and use machines

The effect of megestrol acetate on the ability to drive and use a vehicle is not known.

Side effect

Benign neoplasms, malignant formations (including cysts and polyps): rapid increase in tumor mass.

Endocrine disorders: adrenal insufficiency, Cushing's syndrome.

Metabolic and nutritional disorders: diabetes mellitus, impaired glucose tolerance, hyperglycemia, increased appetite.

Mental disorders: mood swings.

Nervous system disorders: carpal tunnel syndrome, lethargy.

Cardiac disorders: circulatory failure.

Vascular disorders: thrombophlebitis, pulmonary embolism*, hypertension, hot flashes.

Respiratory disorders: shortness of breath.

Gastrointestinal disorders: nausea, vomiting, diarrhea, flatulence, constipation.

Diseases of the skin and subcutaneous tissue: rash, alopecia.

Renal and urinary disorders: pollakiuria.

Reproductive system and breast diseases: uterine bleeding, impotence.

General disorders: weakness, pain, swelling.

Diagnostic tests: weight gain

* Pulmonary embolism (sometimes fatal).

In clinical trials of megestrol acetate in patients with acquired immunodeficiency syndrome, there was no statistically significant difference between the group of patients receiving placebo and those receiving at least one adverse reaction.

The possibility of adrenal insufficiency should be considered in all patients treated with or discontinued long-term therapy with megestrol acetate.

Overdose

Studies of the effects of high doses of Cahexan suspension (1600 mg per day for 6 months or more) did not reveal acute signs of toxicity.

If necessary, symptomatic treatment is carried out.

Storage conditions

At room temperature, out of the reach of children.

Best before date

3 years.

Shelf life after first opening the container is 6 months.

Vacation category

On prescription.

MEGESTROL-VISTA

Compound:

Active substance:

megestrol acetate;

1 tablet contains megestrol acetate 160 mg

Cellulose

microcrystalline 101; lactose monohydrate, povidone K30; sodium starch (type A); silicon dioxide colloidal magnesium stearate.

Dosage form.

Pills.

Basic physical and chemical properties:

tablets are white or almost white, oval and biconvex with a break line on one side and without engraving on the other side.

Pharmacological group.

Antitumor agent, progestogen. ATX code L02A B01.

Pharmacological properties.

Pharmacological.

Like other progesterone drugs, the mechanism of action of megestrol acetate on malignant tumors is complex and not fully understood. Its progesterone effect is somewhat more active than that of medroxyprogesterone acetate, norethidrone acetate and noretinodrel, somewhat weaker compared to chlormadinone acetate and significantly inferior to norgestrel.

The following manifestations of the drug's action occur.

- megestrol acetate binds to cytoplasmic progesterone receptors. After the transfer of progesterone receptor complexes from megestrol acetate to the cell nucleus, RNA synthesis stops, which, in turn, causes inhibition of protein synthesis. This reduces the number of cytoplasmic estrogen receptors, meaning estrogen cannot reach the target molecule and cause DNA damage in the cell nucleus. So, estrogen is not able to cause a DNA-dependent effect on metabolism and cell growth under such conditions.

— Direct, estrogen-independent effect aimed at stopping cell growth.

- High affinity of megestrol acetate for progesterone receptors and significant ability to bind to androgen and glucocorticoid receptors.

- megestrol acetate reduces the release of follicle-stimulating hormone in the pituitary gland and, as a result, slows down the synthesis of estrogen in the ovaries relative to the synthesis of androgen in the testes.

- Megestrol acetate counteracts the stimulatory effects of estrogen on the growth of hormone receptor positive cell lines.

- megestrol acetate reduces the secretion of luteinizing hormone (LH) in the pituitary gland.

— According to animal studies, megestrol acetate reduces the secretion of prolactin in the pituitary gland.

- According to animal studies, megestrol acetate reduces the secretion of ACTH (ACTH) in the pituitary gland.

Pharmacokinetics.

Megestrol acetate is almost completely absorbed. After oral administration of 1 dose of megestrol acetate, the maximum concentration in the blood plasma is achieved within 2-3 hours. The plasma concentration level depends on the dose, but is not directly proportional to it.

The half-life is 15-20 hours.

At steady state, achieved on the 3rd day of taking the drug, the peak plasma concentration is 90%.

Megestrol acetate is metabolized in the liver. According to the results of urine analysis, which was collected over 7 days, megestrol acetate is excreted from the body in urine by 56-78%, and in feces over the same period - by 8-30%.

Clinical characteristics.

Indications.

- Palliative therapy for recurrent, metastatic or inoperable advanced breast cancer, progressing after treatment with aromatase inhibitors;

- palliative therapy for recurrent, well-differentiated (G1 / G2), receptor-positive malignant endometrial tumor.

Contraindications.

- hypersensitivity reactions to megestrol acetate or one of the excipients;

- During pregnancy and breastfeeding

- severe liver failure

- thromboembolism and thromboembolic complications.

Interaction with other drugs and other types of interactions.

Simultaneous administration of megestrol acetate with barbiturates and rifampicin leads to an increase in their metabolism.

Simultaneous use of megestrol acetate with such drugs against epilepsy as barbexaclon, carbamazepine, phenytoin, primidone leads to an increase in their metabolism.

The simultaneous use of megestrol acetate with broad-spectrum antibiotics, in particular ampicillin or tetracycline, disrupts the intestinal microflora, and, as a consequence, leads to low concentrations of the drug in the blood plasma and a deterioration in the effectiveness of megestrol acetate.

Concomitant use of megestrol acetate with hypoglycemic drugs causes changes in the level of glucose tolerance.

Pharmacokinetic studies in patients with HIV did not provide data that would support a clinically important effect of megestrol acetate on zidovudine plasma concentrations.

Features of application.

The drug should be taken under the supervision of an oncologist. During therapy, it is advisable to stay in a special institution. The drug may have a negative effect on adrenal function, which should be taken into account when monitoring the health status of patients.

The drug should be prescribed with caution:

- patients with thrombophlebitis, liver damage, pulmonary embolism;

- patients who have previously been treated for thrombophlebitis;

- patients with impaired renal function

- patients with impaired adrenal function;

- women of reproductive age.

Warning

Thrombophlebitis, liver damage, pulmonary embolism

In patients previously treated for thrombophlebitis or currently diagnosed with thrombophlebitis, severe liver failure or pulmonary embolism, treatment with megestrol acetate should be administered with caution, with the dose adjusted accordingly. In general, a dose of 160 mg of megestrol acetate is not recommended for patients who have previously suffered from thrombophlebitis.

Impaired adrenal function

Although the glucocorticoid effect of megestrol acetate has not been fully studied, according to the results of laboratory tests, the drug suppresses the pituitary-adrenal system.

During the clinical use of megestrol acetate, cases of newly diagnosed diabetes, exacerbation of previously diagnosed diabetes (the patient had to increase the insulin dose), Cushing's syndrome and, rarely, adrenal dysfunction have been reported among patients. Therefore, in case of long-term treatment with megestrol acetate, its interruption, or the appearance of symptoms or manifestations of decreased adrenal function, in particular low blood pressure, nausea, vomiting, dizziness or weakness, attention should be paid to suppressing the pituitary-adrenal axis. Such patients should undergo ongoing testing to monitor adrenal function and, if necessary, take rapid-acting glucocorticoids.

Women of reproductive age

During therapy with megestrol acetate, women of reproductive age should use effective methods of contraception. Patients with previously diagnosed and treated thrombophlebitis should be treated with extreme caution. The use of megestrol acetate during the first 4 months of pregnancy is associated with abnormal development of the fetal genital organs. Women who become pregnant while being treated with megestrol acetate should be informed of the possible negative effects on the fetus.

Long-term therapy with megestrol acetate

The results of a study on dogs that were administered megestrol acetate for 7 years indicate an increase in the incidence of benign and malignant tumors in the tissues of the mammary glands. Similar studies in rats and monkeys show no evidence of an increase in tumor formation.

Although the high incidence of tumors reported in animal studies is unlikely to apply to clinical use of the drug, these data should be taken into account when assessing the benefit/risk ratio.

Lactose

The medicinal product contains lactose and should not be taken by patients with rare hereditary galactose intolerance, lactose intolerance or impaired absorption of glucose or galactose.

Use during pregnancy or breastfeeding.

Pregnancy

During treatment, women of reproductive age should use effective contraception. Taking megestrol acetate is contraindicated during pregnancy or breastfeeding.

Several reports have suggested an association between intrauterine exposure to progestogens during the first trimester of pregnancy and abnormal development of the female or male genital organs of the fetus. Under the influence of progestogen drugs, the risk of hypospadias in male fetuses (5-8 cases per 1000) approximately doubles. Currently, there is insufficient data on the risks associated with exposure of female fetuses to such drugs to quantify them. However, some drugs cause virilization of the external female genitalia. If a patient takes megestrol acetate during the first 4 months of pregnancy or becomes pregnant during drug therapy, she should be informed of the potential risks to the fetus.

Women of reproductive age are advised to avoid pregnancy during treatment.

Lactation

Breastfeeding should be discontinued while taking megestrol acetate.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

The ability to influence reaction speed when driving vehicles or operating other mechanisms has not been studied.

Method of administration and dose.

Mammary cancer

Megestrol-Vista is prescribed 1 tablet 1 time per day, which is 160 mg of megestrol acetate. The duration of treatment is at least 2 months.

Endometrial cancer

Depending on the course of the disease, Megestrol-Vista should be prescribed ½-2 tablets once a day, which is 80-320 mg of megestrol acetate.

Elderly patients, kidney and/or liver disorders

Dose adjustment may be necessary in elderly patients, among whom the incidence of decreased liver function, kidney function and cardiovascular disorders is higher, as well as against the background of the development of concomitant diseases or therapy with other drugs. As a rule, at the beginning of treatment in elderly patients, the drug should be prescribed at a lower dose than recommended.

As is known, megestrol acetate is mainly excreted by the kidneys, so patients with impaired renal function are at risk due to the likelihood of developing toxic reactions. Megestrol acetate should be administered with caution to patients with impaired liver and/or kidney function. Doses are adjusted in accordance with the characteristics of the disease, taking into account changes in blood test parameters.

The tablets should be taken after meals with a glass of water.

To achieve the proper antitumor effect, megestrol acetate should be taken for 2 months.

Taking into account the data on documented cases of disappearance or reduction of tumors, treatment should be continued even after the completion of the process of regression of the initial existing tumors, until further progression of malignant neoplasms is observed.

If tumors progress rapidly, megestrol acetate therapy can be discontinued.

Children.

There are no data on the safety and effectiveness of megestrol acetate in children.

Overdose.

There is no acute toxic effect when taking megestrol acetate at a dose of 1600 mg for 6 months or more. During the post-registration period, cases of overdose of megestrol acetate were reported, which were accompanied by diarrhea, nausea, abdominal pain, shortness of breath, unsteady gait, cough, apathy, and chest pain. There are no drugs that have the ability to eliminate or weaken the specific effects caused by taking megestrol acetate. Treatment for overdose is aimed at eliminating symptoms.

Adverse reactions.

Adverse reactions are classified by frequency of occurrence: very often (≥ 1 in 10), often (≥ 1 in 100 to

The most common side effect of megestrol acetate is weight gain. It occurs in 81-88% of patients. Weight gain is associated with increased appetite. At the same time, the percentage of body fat and body weight increases, and water is not retained.

Glucose intolerance, hyperglycemia, cases of newly diagnosed diabetes, exacerbations of previously diagnosed diabetes, Cushing's syndrome caused by disruption of the pituitary-adrenal axis have been reported. After interruption of megestrol acetate therapy, isolated cases of temporary dysfunction of the adrenal glands were recorded. The results of laboratory studies indicate a slight suppression of adrenal function due to the action of megestrol acetate, similar to the effect of glucocorticoids.

The possibility of adrenal damage should be considered in patients during long-term treatment with megestrol acetate or after discontinuation of its use. In this case, it may be necessary to prescribe glucocorticoid drugs in appropriate doses as part of replacement therapy.

During therapy with megestrol acetate, cases of impotence have been reported among patients with HIV.

Information about suspected adverse reactions

It is important to report suspected adverse reactions when using the drug during the post-marketing period. Thanks to such information, it is possible to evaluate the benefit-risk ratio of the drug on an ongoing basis.

Best before date.

3 years.

Storage conditions.

Store in original packaging at a temperature not exceeding 25 °C. Keep out of the reach of children.

Package.

10 tablets in a blister, 3 or 10 blisters in a cardboard box.

Vacation category.

On prescription.

Manufacturer.

European Pharma Hub Ltd.

The location of the manufacturer and the address of the place of its activities.

7000/9 hrsz., Gortsev Ivan duck 5., composition 15 and 16., Gyale, 2360, Hungary.