Capecitabine pills 500mg №120

Active substance

Capecitabine

Composition

1 tab. - capecitabine 500 mg

Excipients: lactose - 91.11 mg, microcrystalline cellulose - 91.11 mg, croscarmellose sodium - 32.8 mg, hypromellose - 2.02 mg, Magnesium stearate - 10.93 mg.

Shell composition: film coating - 6.56 mg (hypromellose - 38.46%, talc - 30.77%, titanium dioxide (E171) - 29.41%, iron dye red oxide (E172) - 0.68%, iron dye yellow oxide (E172) - 0.68%).

pharmachologic effect

Antitumor agent, antimetabolite

Indications

Mammary cancer

- Combination therapy with docetaxel of locally advanced or metastatic breast cancer with the ineffectiveness of Chemotherapy, including the preparation of the anthracycline;

- monotherapy of locally advanced or metastatic breast cancer resistant to chemotherapy with taxanes or anthracycline drugs or in the presence of contraindications to them.

Colorectal cancer

- Adjuvant treatment of colon cancer stage III after surgical treatment;

- Therapy of metastatic colorectal cancer.

Stomach cancer

- The first-line treatment for advanced gastric cancer.

Contraindications

- Hypersensitivity to capecitabine or any other components of the drug;

- hypersensitivity to Fluorouracil or in cases of unexpected or severe adverse reactions to the treatment with a history of fluoropyrimidine derivatives;

- the established deficiency of DPD (dihydropyrimidine dehydrogenase), as well as for other fluoropyrimidines;

- simultaneous reception of sarivudin or its structural analogs of brivudin type;

- severe liver failure;

- severe renal failure (creatinine clearance below 30 ml / min);

- severe leukopenia;

- the initial content of neutrophils <1,5x109 / l and / or platelet <100x109 / l;

- if there are contraindications to one of the drugs of combination therapy, it should not be used;

- pregnancy and lactation period;

- children's age (efficacy and safety of use have not been established).

With ischemic heart disease, anemia and angina in history, moderate renal failure or liver failure, hypo-or hypercalcemia, diseases of the central and peripheral nervous system, diabetes mellitus and disorders of water and electrolyte balance, over the age of 60 years, simultaneous use with oral coumarin anticoagulants, hereditary lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Side effects

The incidence of adverse reactions is set out according to WHO recommendations: very often (> 10%), often (> 1% and <10%), infrequently (> 0.1% and <1%), rarely (> 0.01% and < 0.1%), very rarely (<0.01%).

The most frequent side effects associated with taking capecitabine were disorders of the gastrointestinal tract (GIT) (diarrhea, nausea, vomiting, abdominal pain, stomatitis), palm-plantar syndrome, increased fatigue, asthenia, anorexia, cardiotoxicity, renal growth failure in patients with impaired renal function in history, as well as thrombosis / embolism.

Side effects reported in patients taking monotherapy

Infectious and parasitic diseases: often - herpes viral infection, nasopharyngitis, infection of the lower respiratory tract; infrequently - sepsis, urinary tract infection, cellulitis, tonsillitis, pharyngitis, oral mucosa candidiasis, influenza, gastroenteritis, fungal infections, infections, abscess of the tooth.

Benign, malignant and unspecified neoplasms: infrequently - lipoma.

Disorders of the blood and lymphatic system: often - neutropenia; infrequently - febrile neutropenia, granulocytopenia, thrombocytopenia, leukopenia, hemolytic anemia, an increase in the international normalized ratio, lengthening of the prothrombin time.

Immune system disorders: infrequently - hypersensitivity. Metabolic and nutritional disorders: very often - anorexia; often - dehydration, weight loss; infrequently - diabetes, hypokalemia, indigestion, hypertriglyceridemia.

Psychiatric disorders: infrequently - panic attacks, depressed mood, decreased libido.

Nervous system disorders: often - headache, dizziness (other than vertigo), lethargy, paresthesia, dysgeusia (taste perversion): not often - aphasia, memory disorder, syncope, imbalance, loss of sensitivity, peripheral neuropathy.

Violations on the part of the organ of vision: often - increased tearing, conjunctivitis; infrequently - decreased visual acuity, diplopia.

Disturbances of the organ of hearing and labyrinth disorders: infrequently - vertigo, pain in the ears.

Heart disorders: infrequently - angina, including unstable, arrhythmia, sinus tachycardia, palpitations.

Vascular disorders: often - thrombophlebitis; infrequently - deep vein thrombosis, increased blood pressure, petechiae, lowering blood pressure, "hot flashes", cooling the distal extremities.

Disorders of the respiratory system, organs of the chest and mediastinum: often - nosebleeds, rhinorrhea; infrequently - pneumothorax, hemoptysis, bronchial asthma, shortness of breath on exertion.

Violations of the gastrointestinal tract: very often - diarrhea, vomiting, nausea, stomatitis (including ulcerative), abdominal pain; often - constipation, epigastric pain, dyspepsia; infrequently, intestinal obstruction, ascites, enteritis, dysphagia, abdominal pain, abdominal discomfort, gusgroesfagialnaya reflux disease, blood in the stool.

Disorders of the liver and biliary tract: often - a change in liver function tests; infrequently - jaundice.

Violations of the skin and subcutaneous tissues: very often - palmar and plantar syndrome (paresthesia, edema, hyperemia, peeling of the skin, blistering), dermatitis; often - hyperpigmentation of the skin, macular rash, rash, alopecia, erythema, dry skin; infrequently - blister, skin ulcers, urticaria, palmar erythema, swelling of the face, purpura. In less than 2% of patients in 7 completed clinical studies (N = 949), skin cracks were reported, at least supposedly related to capecitabine therapy.

Disorders of the musculoskeletal and connective tissues: often - pain in the limbs, back pain; infrequently - swollen joints, bone pain, facial pain, stiffness, muscle weakness.

Disorders of the kidneys and urinary tract: infrequently - hydronephrosis, urinary incontinence, hematuria, nocturia, increased creatinine in the blood plasma.

Disorders of the genital organs and breast: infrequently - vaginal bleeding.

General disorders and disorders at the injection site: very often - fatigue, drowsiness; often - peripheral edema, malaise, chest pain, fever, weakness, asthenia; Infrequently - swelling, chills, flu for a similar syndrome, trembling, fever.

Effect on laboratory and instrumental studies: often - hyperbilirubinemia.

The following adverse reactions are manifestations of toxicity, known for therapy with fluoropyrimidines; At least an indirect association between the development of such reactions and the use of capecitabine was reported in less than 5% of patients who participated in 7 completed clinical studies (N = 949):

disorders of the gastrointestinal tract: dry mouth, flatulence, adverse reactions associated with inflammation / ulceration of the mucous membranes, such as esophagitis, gastritis, duodenitis, colitis, Gastrointestinal bleeding;

disorders of the cardiovascular system: edema of the lower extremities, cardialgia, including angina pectoris, cardiomyopathy, myocardial ischemia, myocardial infarction, heart failure, sudden death, tachycardia, supraventricular arrhythmias, including atrial fibrillation, ventricular extrasystoles;

nervous system disorders: taste disturbance, insomnia, confusion, encephalopathy, cerebellar symptoms (ataxia, dysarthria, imbalance and coordination);

mental disorders: depression;

infectious and parasitic diseases: infectious complications associated with myelosuppression, weakening of the immune system and / or mucositis, such as local and fatal systemic infections (bacterial, viral or fungal etiology) and sepsis;

disorders of the blood and lymphatic system: anemia, myelosuppression / pancytopenia;

disorders of the skin and subcutaneous tissues: itching, focal peeling of the skin, skin hyperpigmentation, changes in the nails, photosensitivity reactions, radiation dermatitis;

disorders of the organ of vision: eye irritation;

disorders of the respiratory system, organs of the chest and mediastinum: shortness of breath, cough;

disorders of the musculoskeletal and connective tissues: arthralgia, myalgia, back pain;

common disorders and disorders at the injection site: chest pain (non-cardiac etiology), pain in the extremities.

Capecitabine use in combination therapy

The safety profile did not differ when prescribed for various indications and with different combinations, however, the adverse reactions listed in monotherapy can be observed with greater frequency when capecitabine is used in combination therapy.

Below are the adverse reactions that were observed in addition to those with monotherapy:

Infectious and parasitic diseases: often - candidiasis of the oral mucosa, herpes zoster, urinary tract infections, upper respiratory tract infections, rhinitis, influenza, infection, oral herpes;

Disorders of the blood and lymphatic system: very often - neutropenia, anemia, thrombocytopenia, leukopenia, febrile neutropenia; often - myelosuppression;

Immune system disorders: often - hypersensitivity;

Metabolism and nutrition disorders: very often - weight loss, loss of appetite; often - hypokalemia, hyponatremia, hypomagnesemia, hypocalcemia, hyperglycemia;

Mental disorders: often - sleep disorders, anxiety;

Nervous system disorders: very often - paresthesia, dysgeusia, headache, peripheral neuropathy, peripheral sensory neuropathy, dysesthesia; often - neurotoxicity, tremor, neuralgia, hypesthesia;

Violations of the organ of vision: very often - lacrimation; often - visual disturbances, dry eyes, pain in the eyes, blurred vision;

Disorders of the organ of hearing and labyrinth disorders: often - tinnitus, hearing loss;

Heart disorders: often - atrial fibrillation;

Vascular disorders: very often - thrombosis / embolism, high blood pressure (BP), lower extremity edema; often - hyperemia, lowering blood pressure, hypertensive crisis, "hot flashes", phlebitis;

Disturbances of the respiratory system, chest and mediastinal organs: very often - pharyngeal dysesthesia, sore throat; often - nosebleeds, dysphonia, rhinorrhea, hiccups, sore throat and larynx;

Violations of the gastrointestinal tract: very often - constipation, dyspepsia; often - bleeding from the upper gastrointestinal tract, oral ulcers, gastritis, abdominal distension, gastroesophageal reflux disease, pain in the oral cavity, dysphagia, rectal bleeding, abdominal pain, dysesthesia, paresthesia and hypoesthesia in the mouth, abdominal discomfort;

Disorders of the liver and biliary tract: often - impaired liver function;

Violations of the skin and subcutaneous tissues: very often - alopecia, changing nails; often - hyperhidrosis, erythematous rash, urticaria, night sweats;

Disorders of the musculoskeletal and connective tissues: very often - myalgia, arthralgia, pain in the limbs; often - pain in the jaw, muscle spasms, trismus, muscle weakness;

Disorders of the kidneys and urinary tract: often - hematuria, proteinuria, decreased creatinine clearance, dysuria;

General disorders and disorders at the injection site: very often - weakness, lethargy, hypersensitivity to high and low temperatures; often - fever, pain, inflammation of the mucous membrane, chills, chest pain, flu-like syndrome, contusion.

Both in clinical studies and outside of them, cases of liver failure and cholestatic hepatitis were recorded. The causal relationship with taking capecitabine has not been established.

With capecitabine therapy in combination with other chemotherapy drugs, often (but less than 5% of patients) reported cases of hypersensitivity reactions (2%) and ischemia / myocardial infarction (3%).