Prograf, 0.5 mg capsules 50 pcs

Prograf is an immunosuppressant of the macrolide group.

At the molecular level the effects of tacrolimus are mediated by binding to the cytosolic protein (FKBP12) which is responsible for intracellular accumulation of the drug.

The FKBP12-tacrolimus complex binds specifically and competitively to calcineurin and inhibits it, resulting in calcium-dependent inhibition of T-cell signal transduction pathways, thus preventing transcription of a discrete group of lymphokine genes.

Tacrolimus is a highly active immunosuppressive drug: suppresses the formation of cytotoxic lymphocytes, which are mainly responsible for transplant rejection, reduces T-cell activation, T-helper-dependent B-cell proliferation, and lymphokine formation (such as interleukins-2, -3 and γ-interferon) and interleukin-2 receptor expression.

Indications

Prevention and treatment of hepatic, renal and cardiac allograft rejection, including those resistant to standard immunosuppressive therapy regimens.

Active ingredient

Composition

1 capsule contains tacrolimus 0.5 mg

How to take, the dosage

It is recommended that the daily oral dose be divided into two doses (e.g., in the morning and in the evening). The capsules should be taken immediately after taking them out of the blister pack. The capsules should be swallowed with liquids (preferably water).

To achieve maximum absorption, the capsules should be taken on an empty stomach (on an empty stomach) or at least 1 hour or 2-3 hours after a meal.

No detectable effect of food on absorption of the drug in patients with a kidney transplant has been noted.

Interaction

Tacrolimus is incompatible with polyvinyl chloride (PVC).

If the contents of the capsules are to be inserted through a nasogastric tube, the latter must not contain PVC.

Contraindications

Known hypersensitivity to tacrolimus or other macrolides.

Known hypersensitivity to polyoxyethylated hydrogenated castor oil (HCO-60) or structurally related components.

Side effects

Many of the adverse drug reactions stated below are reversible and/or reduced with dosage reduction. The incidence of adverse drug reactions is lower with oral administration than with intravenous administration. The reactions are listed below in descending order of frequency of occurrence:

Very common – ≥1/10; common – ≥1/100,

Cardiovascular: very often – hypertension; often – hypotension, tachycardia, cardiac arrhythmia and conduction disturbances, thromboembolic and ischemic manifestations, angina pectoris, vascular disease; infrequently – abnormal ECG parameters, infarction, heart failure, shock, myocardial hypertrophy, cardiac arrest.

Gastrointestinal and liver diseases: very common – diarrhea, nausea and/or vomiting; common – GI dysfunction (such as dyspepsia), abnormal liver enzyme levels, abdominal pain, constipation, changes in body weight and appetite, inflammation and ulcers in GI, jaundice, biliary tract and gallbladder disease; infrequent – ascites, bowel obstruction (ileus), liver tissue lesions, pancreatitis; rare – liver failure.

Blood and lymphatic system: frequently – anemia, leukopenia, thrombocytopenia, hemorrhage, leukocytosis, coagulation disorders; infrequently – insufficiency of hematopoietic system, including pancytopenia, thrombotic microangiopathy.

Kidney: very common – renal dysfunction (e.g., increased serum creatinine level); common – renal tissue damage, renal failure; infrequent – proteinuria.

Metabolism and electrolytes: very common – hyperglycemia, hyperkalemia, diabetes mellitus; common – hypomagnesemia, hyperlipidemia, hypophosphatemia, hypokalemia, hyperuricemia, hypocalcemia, acidosis, hyponatremia, hypovolemia, dehydration; infrequent – hypoproteinuria, hyperphosphatemia, increased amylase levels, hypoglycemia.

Muscular and skeletal system: frequently – seizures; infrequently – myasthenia gravis, joint diseases.

Nervous system/sensory system: very common – tremor, headache, insomnia; common – sensory disturbances (e.g. paresthesia), visual disturbances, confusion, depression, dizziness, agitation, neuropathy, seizures, discoordination, psychosis, anxiety, nervousness, sleep disturbances, impaired consciousness, emotional lability, hallucinations, hearing disturbances, thinking disorders, encephalopathy; infrequent – hypertension, eye disease, amnesia, cataracts, speech impairment, paralysis, coma, deafness; very rare – blindness.

Respiratory system: often – respiratory dysfunction (e.g., shortness of breath), pleural effusion; infrequently – atelectasia, bronchospasm.

The skin: often – itching, alopecia, rash, sweating, acne, photosensitivity; infrequent – hirsutism; rare – Lyell’s syndrome; very rare – Stevens-Johnson syndrome.

Mixed manifestations: very often – localized pain (e.g., arthralgia); often – fever, peripheral edema, asthenia, urinary disorders; infrequently – disorders of genitalia in women, including edema.

New diseases: patients receiving immunosuppressive therapy are in the group of increased risk of malignant tumors. Both benign and malignant tumors, including Epstein-Barr virus (EBV)-associated lymphoproliferative diseases and skin cancer, have been reported with tacrolimus use.

Hypersensitivity reactions: allergic and anaphylactic reactions.

Infections: in patients receiving tacrolimus, as well as during treatment with other immunosuppressive drugs, the risk of developing infectious diseases (viral, bacterial, fungal, protozoal) is increased. The course of previously diagnosed infectious diseases may worsen.

Overdose

Clinical experience with overdose treatment is limited.

There have been several cases of accidental overdose of the drug with the following symptoms: tremor, headache, nausea, vomiting, infections, urticaria, lethargy, increased blood urea nitrogen levels, increased serum creatinine concentration, and increased alanine aminotransferase levels.

Pregnancy use

The results of preclinical and human studies show that the drug may pass through the placenta.

Since the safety of Prograf in pregnant women is not well established, the drug should not be prescribed unless the possible benefit of treatment justifies the potential risk to the fetus.

The results of preclinical and human studies show that tacrolimus is excreted with breast milk.

Since adverse effects on newborns cannot be ruled out, women taking Prograf should not breastfeed.

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