Velcade

Velcade has an antitumor effect.

Indications of the velcade

It is used to eliminate multiple myeloma, and in addition to lymphoma of mantle cell origin (in persons who have already been treated).

[1]

Release form

The drug is produced in the form of a powder, from which a medicinal solution is made, introduced into / in or by a / c method. Contained in vials with a capacity of 3.5 mg.

[2]

Pharmacodynamics

The active element of Velcade, bortezomib, is a substance that reversibly retards the chymotrypsin-like activity of the 26S proteasome located inside specific mammalian cells. The above proteasome is the largest protein complex that has the ability to break down proteins that are conjugated to the ubiquitin substance. It should be noted that ubiquitin-proteasome form of transportation is extremely important in the regulation of intracellular levels of individual proteins, because it supports the process of homeostasis within cells.

The suppression of the function of the proteasome leads to the prevention of selective proteolysis processes, which also affect a variety of cellular responses. If the mechanism of maintaining homeostasis processes has been violated, the cell may die. Often, bortezomib causes inhibition of tumor growth (for example, in multiple myeloma).

[3], [4], [5], [6]

Pharmacokinetics

After performing the procedure, SCI or IV injection during the treatment course, the plasma parameters of the drug are significantly increased.

Bortezomib is distributed mainly inside tissues of the peripheral type. Protein synthesis is approximately 83%.

During the metabolism of the drug, two degradation products are formed, which then undergo the hydroxylation process, as a result of which other decomposition products are formed.

[7], [8], [9], [10], [11],

Dosing and administration

The drug is used solely for injections of SC or an IV method. When the substance is administered by other methods, a lethal outcome can be observed.

It must be remembered that a person who has the required experience and knowledge should prepare the solution, and then introduce it. With the introduction of IV injections, a concentration of 1 mg should be used, and with a SC injection a concentration of 2.5 mg is required.

Calculate the drug concentration should be extremely carefully, because it affects not only the process of therapy, but also the life of the patient.

When carrying out monotherapy, the drug is injected n / k or in / in the method (jet infusion, lasting 3-5 seconds).

The size of the therapeutic dose is 1.3 mg. Enter it should be twice a week, in the period of 14 days. Often, the treatment scheme looks like this - the injection is administered on the 1st, 4th, and then the 8th and 11th days, after which you need to take a break of 10 days. Intervals between injection procedures should be at least 72 hours.

The effectiveness of the drug will be possible to evaluate after passing the 3rd, and also the 5th course of therapy. After receiving a full-fledged clinical reaction, it is necessary to supplement the therapy with two more treatment cycles.

Long-term treatment (more than 8 cycles) can be performed in accordance with the standard treatment scheme or in the form of supporting procedures (13-day intervals must be observed).

The complex treatment is performed with the use of jet iv injection (duration is 3-5 seconds) in conjunction with melphalan, as well as prednisone, used orally. Often in this case, a scheme consisting of 9 cycles is assigned, and lasts for 1.5 months. During the first 4 cycles, the substance is administered twice a week (on the 1st, 4th, 8th and 11th days, and in addition on the 22nd, 25th, 29th, and 32 th days). Throughout the same cycles, 5-9, the medication is used once a week - on the 1st, 8th, and 22nd and 29th days.

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

Changing the size of portions or a treatment regimen can only be done by a doctor.

[18]

Use of the velcade during pregnancy

It is forbidden to prescribe Velcade during pregnancy.

Contraindications

The main contraindications of drugs:

• the presence of hypersensitivity to the elements of the drug;
• lesions affecting the pericardium;
• the period of breastfeeding;
• pulmonary diseases of an acute type (having an infiltrative diffuse character);
• appointment to children.

It is required to use the medicine with care during therapy in people with different functional renal / hepatic disorders, epilepsy or seizures, dehydration, diabetic polyneuropathy, constipation and so on.

[12], [13], [14]

Side effects of the velcade

The use of medication can cause negative symptoms affecting any system and organs - SSS, hematopoietic, respiratory, digestive functions, NS, visual and auditory organs, and so on.

Often, there are side effects such as neutron-, leuko-, thrombocyto- or lymphopenia, cardiogenic shock, anemia, angina pectoris, 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, we can expect the development of diarrhea, abdominal pain, vomiting, constipation, impaired appetite, nausea, dyspeptic manifestations, stomatitis or bloating. Also sometimes there are headaches, paresthesia, dizziness, polyneuropathy develops, depression and sensation of confusion. It can be observed vertigo, a disorder in the work of the kidneys, a weakening of visual clarity, dysuria, rashes and so on.

[15], [16], [17]

Overdose

When intoxication, when the size of the permissible dose was doubled, the victims developed thrombocytopenia and acute decrease in blood pressure, resulting in death.

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

[19], [20], [21]

Interactions with other drugs

The use of Velcade with drugs that moderately or moderately slow the activity of isoenzymes of the hemoprotein (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 forbidden to use the CYP3A4 element (such as phenytoin, carbamazepine or phenobarbital) and ordinary St. John's wort, in combination with powerful inducers, because this can reduce the effectiveness of the medication.

The use of melphalan-prednisone together with the complex can increase the level of bortezomib, although it does not have any pharmacological significance.

At times in people with diabetes, who use antidiabetic drugs for ingestion, the combination with Velcade causes the development of hyper- or hypoglycemia.

Caution is required when the drug is combined with antiviral medications, amiodarone, isoniazid, and in addition nitrofurantoin or statins.

[22], [23]

Storage conditions

Velcade must be kept in a place closed from sunlight and access to small children, with standard temperature for medicines.

[24], [25]

Shelf life

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

[26], [27]

Reviews

Velcade often receives feedback, which describes its rather high efficiency. It is often reported that therapy with its use could stop the development of a rather serious pathology - myeloma.

There are also comments that indicate a lack of monoclonal protein inside the bone marrow and blood (during the evaluation of the patient's condition after the completion of the 5th cycle of treatment). But at this stage, the change in the therapy regimen and dosage dosage size is of decisive importance - that is, the competent approach of the treating doctor is required. This is due to the fact that there is evidence that a decrease in portion caused the return of values observed before the start of therapy.

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

Summarizing, 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 give up therapy. If there is any doubt as to the competence of the specialist treating you, it is recommended that you seek out another doctor.