Velcade

Velcade has an antitumor effect.

Indications Velcade

It is used to treat multiple myeloma, as well as mantle cell lymphoma (in people who have already undergone treatment).

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Release form

The drug is released in the form of a powder, from which a medicinal solution is prepared, administered intravenously or subcutaneously. It is contained in vials with a capacity of 3.5 mg.

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Pharmacodynamics

The active ingredient of Velcade, bortezomib, is a substance that reversibly slows down the chymotrypsin-like activity of the 26S proteasome located inside specific mammalian cells. The above-mentioned proteasome is the largest protein complex capable of breaking down proteins conjugated with the substance ubiquitin. It should be noted that the ubiquitin-proteasome form of transport is extremely important in the regulatory processes of the intracellular level of individual proteins, because it maintains the process of homeostasis inside the cells.

Inhibition of proteasome function leads to the prevention of selective proteolysis processes, which also affect many cellular reactions. If the mechanism for maintaining homeostasis processes is disrupted, the cell may die. Bortezomib often causes inhibition of tumor growth (for example, in myeloma, which is multiple).

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Pharmacokinetics

After performing the procedure of subcutaneous or intravenous injection during the course of treatment, the plasma levels of the drug increase significantly.

Bortezomib is distributed primarily into peripheral tissues. Protein synthesis is approximately 83%.

During drug metabolism, two breakdown products are formed, which then undergo a hydroxylation process, resulting in the formation of other breakdown products.

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Dosing and administration

The medicine is used exclusively for injection by subcutaneous or intravenous method. When the substance is administered by other methods, a lethal outcome may occur.

It is important to remember that the solution must be prepared and then administered by a person with the required experience and knowledge. When administering intravenous injections, a concentration of 1 mg must be used, and when administering subcutaneous injections, a concentration of 2.5 mg must be used.

It is necessary to calculate the drug concentration extremely carefully, because it affects not only the therapy process, but also the life of the patient.

When carrying out monotherapy, the drug is administered subcutaneously or intravenously (jet injection lasting 3-5 seconds).

The size of the therapeutic dose is 1.3 mg. It should be administered twice a week, over a period of 14 days. Often, the treatment regimen looks like this: an injection is administered on the 1st, 4th, and then on the 8th and 11th days, after which a break of 10 days should be taken. The intervals between injection procedures should be at least 72 hours.

The effectiveness of the drug will be assessed after the 3rd and 5th course of therapy. After receiving a full clinical response, it is necessary to supplement the therapy with 2 more treatment cycles.

Long-term treatment (more than 8 cycles) can be carried out in compliance with the standard treatment regimen or in the form of maintenance procedures (in this case, it is necessary to observe 13-day intervals).

Complex treatment is performed using intravenous jet injections (duration is 3-5 seconds) in combination with melphalan, as well as prednisone, taken orally. In this case, a scheme consisting of 9 cycles and lasting 1.5 months is often prescribed. During the first 4 cycles, the substance is administered twice a week (on the 1st, 4th, 8th and 11th days, and also on the 22nd, 25th, 29th and 32nd days). During cycles 5-9, the drug is used once a week - taken on the 1st, 8th, as well as the 22nd and 29th days.

Before starting a course of treatment, the patient should undergo a full medical examination, which also includes various laboratory tests and analyses.

Only the attending physician may change portion sizes or the treatment regimen.

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Use Velcade during pregnancy

Velcade should not be used during pregnancy.

Contraindications

Main contraindications of the drug:

• the presence of hypersensitivity to the components of the medication;
• lesions affecting the pericardium;
• breastfeeding period;
• acute pulmonary diseases (having an infiltrative diffuse nature);
• assignment to children.

The drug should be used with caution during therapy in people with various functional renal/hepatic disorders, epilepsy or seizures, dehydration, diabetic polyneuropathy, constipation, etc.

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Side effects Velcade

The use of the drug can cause negative symptoms affecting any system and organ – cardiovascular system, hematopoietic, respiratory, digestive functions, nervous system, visual and auditory organs, etc.

Frequently observed side effects include neutro-, leukopenia, thrombocytopenia, or lymphopenia, cardiogenic shock, anemia, angina, or cardiac arrest. In addition, exacerbation of CHF, myocardial infarction, ventricular hypokinesia, as well as dyspnea, pulmonary edema, rhinorrhea, cough, and nosebleeds may develop.

In addition, diarrhea, abdominal pain, vomiting, constipation, loss of appetite, nausea, dyspeptic symptoms, stomatitis or bloating may develop. Headaches, paresthesia, dizziness, polyneuropathy, depression and a feeling of confusion may also sometimes occur. Vertigo, kidney dysfunction, decreased visual acuity, dysuria, rashes, etc. may be observed.

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Overdose

In cases of intoxication, when the permissible dose was exceeded twice, the victims developed thrombocytopenia and a sharp decrease in blood pressure, resulting in death.

Because of this, in case of poisoning, it is necessary to urgently carry out all necessary measures that will support the function of vital systems, and then constantly monitor their indicators and perform symptomatic procedures.

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Interactions with other drugs

Concomitant use of Velcade with drugs that weakly or moderately inhibit the activity of heme protein isoenzymes (such as dexamethasone or ketoconazole) may slightly alter the pharmacokinetic parameters of bortezomib.

When combined with rifampicin, the values of this drug decrease.

It is prohibited to use in combination with strong inducers of the CYP3A4 element (such as phenytoin, carbamazepine or phenobarbital) and St. John's wort - because this may reduce the effectiveness of the drug.

Use with the melphalan-prednisone complex may increase bortezomib levels, although this does not have any pharmacological significance.

Occasionally, in people with diabetes mellitus using oral antidiabetic drugs, the combination with Velcade causes the development of hyper- or hypoglycemia.

Caution is required when combining the drug with antiviral drugs, amiodarone, isoniazid, and also nitrofurantoin or statins.

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Storage conditions

Velcade should be stored in a place protected from sunlight and out of reach of small children, at standard drug temperatures.

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Shelf life

Velcade can be used for 3 years from the date of manufacture of the drug.

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Reviews

Velcade often receives reviews that describe its fairly high effectiveness. It is often reported that therapy using it was able to stop the development of a rather severe pathology - myeloma.

There are also comments that indicate the absence of monoclonal protein in the bone marrow and blood (during the assessment of the patient's condition after the completion of the 5th cycle of treatment). But at this stage, the change in the treatment regimen and the size of the drug dosage is of decisive importance - that is, a competent approach by the attending physician is required. This is due to the fact that there is evidence that a reduction in the dose caused the return of the values observed before the start of therapy.

At the same time, patients often say that along with the effect of using the drug, negative symptoms appear. Often, patients complain of dyspnea, changes in blood pressure, and tremor. But usually these inconveniences have to be tolerated, because it is not always possible to find an alternative to the drug.

To sum up, we can say that the effectiveness of the drug is largely determined by the individual characteristics of the patient, as well as the actions of the doctor. But in general, under any circumstances, you should not refuse therapy. If you have doubts about the competence of the specialist treating you, it is recommended to find another doctor.