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Active Ingredient: Methotrexate.

Active Ingredient: Methotrexate 2.5 mg

Release form, composition and packaging
Coated tablets 1 tab.

Methotrexate is used for treating certain types of cancer, severe psoriasis, or rheumatoid arthritis in certain patients.

Pharmachologic effect
An antitumor agent from the group of antimetabolites – folic acid antagonists. Acts in the S-phase of mitosis. The mechanism of action is associated with the inhibition of the synthesis of purine nucleotides and thymidylate as a result of irreversible binding to dihydrofolate reductase, which prevents the restoration of dihydrofolate to active tetrahydrofolate. More active against rapidly growing cells. It has some immunosuppressive effect.

To a small extent penetrates the BBB (depending on the dose used). With intrathecal administration, a significant amount enters the systemic circulation. Binding to plasma proteins (mainly with albumin) of plasma is about 50%. Biotransformed in the liver. It is excreted by the kidneys (unchanged) and with bile (less than 10%). T1 / 2 depends on the dose used and has significant individual differences. With repeated administration, it accumulates in the tissues in the form of metabolites.

Acute lymphocytic leukemia, trophoblastic disease, skin cancer, cervical and vulvar cancer, esophageal cancer, squamous cell carcinoma of the head and neck, cancer of the renal pelvis and ureter, osteogenic and soft-cell sarcoma, Ewing’s sarcoma, lung cancer, breast cancer, germ cell tumors of the testis and testicles , liver cancer, kidney cancer, retinoblastoma, medulloblastoma, penile cancer, lymphogranulomatosis.

Severe forms of psoriasis (in case of failure of standard therapy).

Severe form of rheumatoid arthritis (in case of failure of standard therapy).

Dosage regimen
It is taken orally, administered iv, intramuscularly, intramuscularly. Installed individually, depending on the indications and stage of the disease, the state of the hematopoietic system, anti-tumor therapy regimen.
Side effect
From the digestive system: possible ulcerative stomatitis, anorexia, gingivitis, pharyngitis, nausea; rarely – diarrhea, melena, enteritis, pancreatitis; in some cases (with prolonged daily use) – liver necrosis, cirrhosis, fatty atrophy, periportal liver fibrosis.

From the hemopoietic system: leukopenia, anemia, thrombocytopenia.

From the side of the central nervous system: feeling tired, dizziness; rarely – headache, aphasia, drowsiness, cramps.

From the reproductive system: disorders of oogenesis and spermatogenesis, oligospermia, menstrual irregularities, decreased libido, impotence.

From the urinary system: hematuria, cystitis, severe renal dysfunction.

Allergic reactions: chills, decreased resistance to infection; rarely – urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome.

Dermatological reactions: skin rash, photosensitivity, pigmentation disorders, telangiectasia, acne, furunculosis.

Severe impaired liver and / or kidney function, leukopenia, thrombocytopenia, pregnancy. Methotrexate should not be used in immunodeficiency conditions.

Pregnancy and lactation
Methotrexate is contraindicated in pregnancy. If necessary, use during lactation should stop breastfeeding.

Women of childbearing age should use reliable methods of contraception while using methotrexate.

In experimental studies, the embryotoxic and teratogenic effects of methotrexate have been established.

Use for impaired liver function
Contraindicated in severely impaired liver function.
Use for impaired renal function
Contraindicated in severe renal impairment.
special instructions
Methotrexate should not be used for ascites, pleural effusion, gastric ulcer and duodenal ulcer, ulcerative colitis, gout or nephropathy (including a history).

It is not recommended for use in patients with chickenpox (including recently transferred or after contact with patients), herpes zoster, and other acute infectious diseases.

Before starting therapy and against the background of the treatment, the picture of peripheral blood, liver and kidney function, chest x-ray should be monitored.

In the treatment of rheumatoid arthritis or psoriasis, a comprehensive blood count should be done at least 1 time per month, and laboratory tests of liver or kidney function at least 1 time in 1-2 months.

When used for psoriasis, the local treatment of the disease should not be interrupted. In case of an overdose, the use of calcium folinate is recommended (but not later than 4 hours later).

When conducting combination antitumor therapy, special care should be taken while using methotrexate in high doses with drugs that have a nephrotoxic effect (for example, with cisplatin).

It is not recommended to vaccinate patients and their families.

Methotrexate (even at low doses) with acetylsalicylic acid should be combined with caution.

In experimental studies, the carcinogenic and mutagenic effects of methotrexate have been established.

Drug interaction
With simultaneous use with vitamin preparations containing folic acid or its derivatives, a decrease in the effectiveness of methotrexate is possible.

The simultaneous use of NSAIDs in high doses can lead to an increase in the concentration of methotrexate in plasma and to an increase in its T1 / 2, as well as to an increase in the concentration of methotrexate not associated with plasma albumin, which in turn enhances the toxic effects of methotrexate (primarily on the gastrointestinal tract and system hematopoiesis).

With the simultaneous use of methotrexate with penicillins (even at low doses), its toxic effects may increase.

With simultaneous use with sulfonamides, especially with co-trimoxazole, there is a risk of increased myelodepressive effect.

When nitrous oxide is used in patients receiving methotrexate, severe unpredictable myelodepression and stomatitis may develop.

With the simultaneous use of valproic acid with methotrexate, a decrease in its concentration in blood plasma is possible.

Colestyramine binds methotrexate, reduces its enterohepatic recirculation, which leads to a decrease in its concentration in blood plasma.

With simultaneous use with mercaptopurine, it is possible to increase its bioavailability due to metabolic disorders during the “first passage” through the liver.

Neomycin and paromomycin reduce the absorption of methotrexate from the gastrointestinal tract.

In patients receiving omeprazole, an increase in the concentration of methotrexate in blood plasma is possible.

With simultaneous use with probenecid, a 3-4-fold increase in the concentration of methotrexate in blood plasma is possible due to a decrease in its renal excretion.

With the simultaneous use of methotrexate with retinoids, an increased risk of hepatotoxic action is possible.

Salicylates potentiate the effect of methotrexate due to a decrease in its renal excretion.

After a course of treatment with tetracycline, methotrexate, used even in low doses, can have a toxic effect.

With the sequential administration of methotrexate and fluorouracil, a synergy of action is possible; fluorouracil introduced before methotrexate may reduce its toxicity.

Cisplatin has a nephrotoxic effect and therefore can reduce the renal excretion of methotrexate, which leads to an increase in its toxicity.

Possible increased toxicity with cyclosporine in patients receiving methotrexate.

A description of the active substances of the drug is provided. The scientific information provided is generalized and cannot be used to decide on the possibility of using a particular drug.

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Active Ingredient: Cabergoline.

Analogs of Cabgolin:Dostinex.

Chemical name
1 – [(6-Allylergolin-8beta-yl) carbonyl] -1- [3- (dimethylamino) propyl] -3-ethylurea.

Chemical properties
This substance is a fairly common dopaminomimetic, a derivative of ergot alkaloids. The tool is synthesized in the form of a white fine powder, which is highly soluble in ethanol, N, N-dimethylformamide and chloroform. The chemical compound is slightly soluble in 0.1 n hydrochloric acid, n-hexane. The product does not dissolve in water.

In medicine, drugs based on Cabergoline are used to treat hyperprolactinemia, and the substance is also used by athletes.

Cabergoline in bodybuilding
The medicine is used to reduce prolactin levels and eliminate unwanted side effects from taking progestin anabolics – trenbolone and nandrolone. During the treatment, athletes monitor the level of prolactin and continue taking the medicine, depending on the results of the tests. It is believed that the substance eliminates fluid retention in the tissues and accelerates the growth of lean muscle mass.

Pharmachologic effect

Pharmacodynamics and pharmacokinetics
Cabergoline is a long acting dopamine receptor antagonist. The drug acts mainly on D2-dopamine receptors, to a lesser extent – on D1-dopamine, serotonin, alpha2- and alpha1-adrenergic receptors.

Laboratory data show that the drug has a direct effect on the synthesis of prolactin by lactotrophs in rats, lactotrophs are located in the pituitary gland. Plasma prolactin levels are significantly reduced, especially in reserpine individuals.

The hypoprolactinemic effect of the drug was carefully studied in two independent, randomized, double trials involving a placebo-controlled and comparative group. The effect of the substance was studied on women suffering from hyperprolactinemia. The test results improved, and the normal menstrual cycle was restored in about 77% of women who took the drug 2 times in 7 days at a dosage of 0.5 mg. In 73% of the subjects, galactorrhea disappeared.

Pharmacokinetic parameters are directly proportional to the dosage of the drug. Eating does not affect the processes of assimilation, metabolism and excretion. After penetration into the digestive tract, the maximum concentration of a substance in the blood plasma was observed after 2-3 hours. With systematic administration of the drug, its equilibrium concentration is several times higher than the concentration with a single dose.

It is not completely known what bioavailability Cabergoline has, but it is unambiguously exposed to the effect of “first passage” through the liver tissue. The degree of binding of the agent to plasma proteins ranges from 40 to 42%, depending on the dose taken. The medicine and its metabolites are quickly and well distributed in tissues and organs, the highest concentration was found in the pituitary gland.

The substance is metabolized by hydrolysis reactions involving urea residues or an acylurea bond in the liver tissues. Cytochrome P450 takes part to a small extent in the biotransformation of the drug. The half-life of the drug is about 65 hours. The substance and its metabolites are completely eliminated from the body within 20 days, mainly through the intestines and urine.

Mild to moderate renal failure and mild to moderate hepatic failure do not require dosage adjustment. With serious violations in the liver, an increase in the concentration of the drug in the blood plasma and AUC is observed. For elderly patients, the drug can be prescribed in the same dosages as for young ones, however, special care must be taken, taking into account all the concomitant diseases and the state of the body as a whole.

The effect of taking the drug is observed after 3 hours, after taking the tablets, reaching its maximum within 48 hours. The duration of the drug is 14 days. Cabergoline does not affect the secretion of other hormones of the anterior pituitary gland or cortisol level. The substance does not have mutagenic activity, slightly reduces fertility.

Indications for use
The tool is prescribed:

  • for the treatment of idiopathic hyperprolactinemia;
    – with macro- and microadenoma of the pituitary gland;
    – patients with amenorrhea, anovulation, oligomenorrhea and
  • – galactorrhea according to indications;
    – to suppress or prevent lactation after childbirth;
    -as part of complex therapy or as a monotherapy for Parkinson’s disease.

  • Contraindications
    The medicine should not be taken:
  • in the presence of hypersensitivity reactions to the active component or – – derivatives of ergoalkaloids;
    – during lactation;
    – patients with uncontrolled hypertension;
    – pregnant women
    – with fibrotic changes in the heart muscle or respiratory system, which – caused disturbances in the functioning of the organs.

  • Caution is recommended to observe:

– with low blood pressure;
– if parallel therapy with dopamine receptor antagonists, antihypertensive – drugs;
– with eclampsia or preeclampsia;
– persons suffering from liver disease;
– with psychosis, including a history of;
– to children.

Side effects
Adverse reactions due to treatment with this substance are quite rare, and in mild or moderate severity.

During clinical trials, the following adverse reactions have been identified.

Most often occur: constipation, headache and dizziness, nausea, pericarditis, peripheral edema, pericardial effusion.

Often develop:

hallucinations, confusion, depression;
indigestion, gastritis, angina pectoris, vomiting;
heart palpitations, flushing and redness of the face;
a decrease in the level of hemoglobin, red blood cells or hematocrit in the blood;
shortness of breath, increased sexual activity, asthenia, pain in the chest and lower back;
weakness, drowsiness (sudden falling asleep in people with Parkinson’s disease).

Less commonly observed:

hyperkinesia, psychotic disorders, fainting, delirium;
malfunctioning of the liver, dyskinesia of the gallbladder and biliary tract, spasm of the vessels of the fingers and toes;
respiratory failure, nosebleeds;
allergic rashes, alopecia, increased levels of creatine kinase in the blood, cramps of the fingers and muscles on the calves;
pulmonary fibrosis, hemionopsia, erythromelalgia, pleurisy, edema (rarely).

Cabergoline, instructions for use (Method and dosage)

In order to prevent lactation in the postpartum period, the medicine is taken once, on the first day after birth, at a dosage of 1 mg. To stop the existing lactation, 250 μg of the drug is used, every 12 hours, 4 times. The duration of treatment, therefore, is 2 days.

The treatment of hyperprolactinemia is carried out in accordance with the recommendations of the attending physician.

As a rule, the initial dosage is 500 mcg per week at a time or distributed over 2 applications. If necessary, the dosage can be increased by 0.5 mg per week, for a month. If the likelihood of developing unwanted adverse reactions is increased, then treatment can begin with 250 mg per week.

The standard therapeutic dose is 1 to 2 mg in 7 days. The maximum amount of a drug that can be prescribed per week is 4.5 mg.

Patients with Parkinson’s disease during monotherapy are prescribed from 500 μg to 3 mg of the substance, 1 time per day. The duration of treatment is determined by the doctor.

In case of an overdose, the victim has nasal congestion, hallucinations, increased side effects, and fainting. As a treatment, supportive and symptomatic therapy is used.

It is better to avoid co-administration of this substance and ergot alkaloids (their derivatives).

The drug is not recommended to be combined with macrolide antibiotics, they increase its bioavailability, more often and more side effects are manifested.

The drug cannot be combined with dopamine receptor antagonists (phenothiazines, thioxanthene, butyrophenone, metoclopramide), this leads to a decrease in the effectiveness of the drug.

Cabergoline is better not to use along with medicines that lower blood pressure.

Storage conditions
Tablets are stored in the original packaging in a cool place.

Shelf life
2 years.

Special instructions
Extra care must be taken in the treatment of patients with cardiovascular diseases, gastric and duodenal ulcers, Raynaud’s syndrome, gastrointestinal bleeding, severe liver diseases (dosage must be adjusted).

The first few days of drug therapy, it is recommended to control the patient’s blood pressure. The drug may cause it to decrease. Also, once a month you need to determine the level of prolactin in the blood. After discontinuation of the drug, prolactin levels can remain at a normal level from 2 weeks to several months.

Before starting treatment, the patient must undergo an examination to identify possible pathologies of the heart valves, liver or kidneys. It is also recommended to do an ECG about 1 time per six months or once a year, in accordance with the doctor’s recommendations. If valve regurgitation worsens, the valve wall thickens, and the lumen narrows, the drug must be replaced.

If during the course of therapy with the agent new clinical symptoms of the respiratory system have appeared, an X-ray of the lungs must be taken. If a patient develops pleural effusion or fibrosis (accompanied by shortness of breath, cough, chest pain and rapid breathing), blood ESR levels increase, additional studies are also needed.

Before starting treatment, it is necessary to accurately determine the cause of the development of hyperprolactinemia in order to exclude the presence of a pituitary tumor.

If you are taking drugs based on Cabergoline, then you can not drive a car and perform potentially dangerous activities, it should be remembered that drugs can lower blood pressure.

For children
This substance, as a rule, is not used in pediatric practice.
With antibiotics
The medicine cannot be combined with erythromycin and some macrolide antibiotics.

During pregnancy and lactation
During pregnancy, the drug is used with extreme caution. Pregnant women can start or continue treatment with the drug only after consulting a specialist.

The drug and its metabolites were found in the milk of experimental rats; it is not known whether the substance is excreted in milk in women. Since the drug can have a negative effect on the infant, it is recommended to stop breastfeeding or replace the medicine.

With antibiotics
The medicine cannot be combined with erythromycin and some macrolide antibiotics.

During pregnancy and lactation
During pregnancy, the drug is used with extreme caution. Pregnant women can start or continue treatment with the drug only after consulting a specialist.

The drug and its metabolites were found in the milk of experimental rats; it is not known whether the substance is excreted in milk in women. Since the drug can have a negative effect on the infant, it is recommended to stop breastfeeding or replace the medicine.

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