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Velcade instructions for use

Farm group: Velcade refers to a group of drugs for the treatment of tumors.

The form of release of the drug, its composition and packaging

Velcade comes in the form of a lyophilized powder, which is used to prepare a solution for intravenous and subcutaneous injections.

The powder is in a glass vial with a volume of 10 ml, packed in a blister and enclosed in a cardboard box.

1 bottle of the drug contains bortezomib 3.5 mg and 35 mg mannitol as excipients.

Mechanism of action

Bortezomib is a substance that reversibly inhibits the production of 26S-proteasomes in all mammalian cells. The 26S proteasome is a complex of protein nature, which affects the proteins associated with ubiquintin. This mechanism is involved in maintaining the constancy of the intracellular environment. Inhibition of the proteasome, through a series of cascade reactions leads to disruption of homeostasis and subsequently cell death.

When tested in vivo, the drug slowed cell growth in simulated tumors, including multiple myeloma.

Pharmacokinetics

Intravenous administration of bortezomib is carried out in doses of 1 mg / m2 and 1.3 mg / m2. The maximum concentration in the blood is 57 and 112 ng / ml, respectively. With repeated injections, these figures increase, and fluctuates between 67-106 and 89-120 ng / ml.

After administration, the drug is intensively distributed in all tissues, binding to plasma proteins is approximately 83%.

In the metabolism of the active substance isoenzymes play a direct role CYP3A4, CYP2C19 and CYP1A2. At the same time, the metabolites formed do not exhibit the pharmacological action characteristic of bortezomib.

Ways of removing the drug in humans have not been studied. The elimination half-life at repeated injections is more than at the primary one, and varies between 40-193 hours.

The effect on the pharmacokinetics of Velcade's age, race, and gender has not been studied.

In the treatment of cancer patients with concomitant disorders of the liver, the need to adjust the dose depends on the severity of organ dysfunction. In case of mild disorders of the liver there is no need to change the dose of Velcade. For moderate to severe disorders, it is worth reducing the dosage and carefully controlling the process of therapy.

The pharmacokinetic characteristics of Velcade administered in various doses and in different ways do not change with impaired renal function, regardless of the severity of the organ dysfunction.

When is appointed?

The drug Velcade is prescribed for:

  • multiple myeloma
  • mantle cell lymphoma, provided that the patient has already received at least 1 line of treatment.

When and to whom it is not recommended

Velcade is contraindicated in the case of:

  • individual intolerance to bortezomib, boron and / or mannitol
  • pregnancy and lactation
  • childhood
  • pericardial diseases
  • lung damage

Extreme care should be exercised when using Velcade with:

  • moderate and severe liver dysfunction
  • severe kidney dysfunction
  • convulsive syndrome, epilepsy
  • penchant for fainting
  • neuropathy of diabetic origin
  • dehydration caused by vomiting or diarrhea
  • constipation
  • risk of heart failure.

Dosing

The drug Velcade is intended only for intravenous and subcutaneous injections. It is unacceptable to introduce intertekalno, since they were recorded lethal outcomes.

For intravenous administration, a solution with a concentration of 1 mg / ml is prepared, for subcutaneous 2.5 mg / ml.

The concentration should be calculated very carefully, as it is different for different routes of administration.

Intravenous administration is carried out in 3-5 seconds or subcutaneously. The starting dose is 1.3 mg / m 2 with a frequency of 2 times a week. Therapy is carried out for 2 weeks (4 injections), then a 10-day break is observed. Be sure to comply with the 72-hour break between injections.

It is worth evaluating the clinical outcome of therapy only after 3 or 5 courses of treatment. If a full therapeutic result has been achieved, it is worthwhile to spend another 2 courses to consolidate it.

If therapy did not produce sufficient results, specialists may be prescribed Velcade's combination treatment with dexamethasone in high dosages. With each injection, 40 mg of dexamethasone is taken orally, dividing this amount into two doses. The first half is taken orally on the day of Velcade's injection, and the second the next day.

All concomitant changes in the patient's condition during the period of taking the drug should be carefully monitored and accompanied by changes in the dosage and frequency of treatment.

Mode of application

Velcade refers to drugs for the treatment of tumors, so it must be handled with great care. Preparation of the solution for injection requires compliance with the rules of sterility. It is necessary to avoid contact of the solution with the skin, for this it is necessary to use gloves and other protective elements of clothing. Do not mix Velcade with other drugs with the exception of saline (sodium chloride 0.9%).

For intravenous administration, 3.5 ml of a physiological solution per 1 bottle of Velcade is taken as a solvent. Thus, a concentration of the prepared solution of 1 mg / ml is obtained. Required to control the quality of the resulting liquid - it should be colorless and transparent, without any mechanical impurities. If there is any deviation from the indicated norms, the solution cannot be used for injections. Introduction is performed intravenously through the catheter for 3-5 seconds, then the catheter is washed with saline.

For subcutaneous administration, 1.4 ml of physiological saline is taken as a solvent and a prepared preparation with a concentration of 2.5 mg / ml is obtained. Quality control is the same - colorless, transparent and free of mechanical impurities. Any deviation is the reason for the disposal of the solution, since it can not be used for injection. The injection site is the skin of the thigh or abdomen (right or left). Enter the drug subcutaneously. Each subsequent injection should be carried out in a new place with a minimum distance from the previous injection site - 2.5 cm. It is impossible to carry out an injection into irritated, damaged places, with hematomas, as well as where it is difficult to insert the needle. If a local reaction to the drug occurs, you can proceed to the introduction of a solution of a lower concentration — 1 mg / ml, or to administer the drug intravenously.


Symptoms of overdose and their treatment.

Signs of an overdose of the drug is a sharp drop in blood pressure, a decrease in the number of platelets in the blood with a fatal outcome. These symptoms are observed with an increase in dose of 2 times.

Therapy of an overdose condition consists in careful monitoring of vital signs, organ function, blood pressure level (use of intravenous infusions, vasoconstrictor administration), and body temperature. Specific antidote to the drug is not installed.

Interaction Velcade with other drugs.

Bortezomib is a weak inhibitor of isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYPZA4. Accordingly, you must be careful when taking other medicines that can affect the activity of these substances. Since ketoconazole, the inhibitory isoenzyme CYP3A4 affects the pharmacokinetics of bortezomib, therefore, the joint reception of these drugs should be carried out under the attention of doctors. The same applies to taking together Velcade and ritonavir.

The effectiveness of therapy with Velcade decreases when it is taken during treatment with rifampicin, carbamazepine, phenobarbital, phenytoin - strong inducers of the CYP3A4 isoenzyme. But dexamethasone exhibits less pronounced inducing abilities for this substance, and therefore has no significant effect on the effectiveness of bortezomib.

Combined treatment with Velcade with melfan and prednisone is acceptable, since the change in pharmacokinetic characteristics is negligible.

When taking oral hypoglycemic agents, it is possible to change their activity with the development of both an increase and a decrease in blood sugar below normal.

Gently used in conjunction with drugs against pressure, antiviral drugs, statins.

Features of use of Velcade during pregnancy and lactation

The use of Velcade in the period of childbearing and breastfeeding is strictly prohibited.

Side effects

From the side of blood-forming organs: violation of laboratory parameters in the direction of reducing the number of cells - platelets, leukocytes, lymphocytes, neutrophils and others

From the side of the heart and blood vessels: heart attack, cardiac arrest, heart failure, rhythm disturbance, edema of the lung tissue, fall and increase in blood pressure, slowing of the heart rhythm, hemorrhage in the brain membrane, stroke, inflammation of the vascular wall, embolism of peripheral and central vessels.

On the part of the respiratory system: violation of respiratory rhythm, shortness of breath. Cough, rhinitis, pain in the chest, in the nasal sinuses, respiratory failure, hemorrhage in the alveoli.

On the part of the digestive tract: dyspeptic symptoms, loss of appetite, bloating, stomatitis, sore throat, inflammation of the gastric mucosa. Inflammation of the pancreas, increased salivation, discoloration and surface of the tongue, colitis.

On the part of the liver: inflammation, hemorrhage, increased levels of bilirubin in the blood, organ failure.

From the side of the central nervous system: neuropathy, convulsions , loss of consciousness, gustatory disturbances, speech disorder, tremor, memory and attention disorders.

On the part of the psyche: confused consciousness, alternation of arousal and depression, depression, sleep disturbance, irritability.

On the part of the kidneys and other urinary organs: impaired urination, insufficiency of kidney function, urinary incontinence, blood and protein in the urine, changes in the amount of urine, pain in the lumbar region.

On the ear: impaired hearing, ringing in the ears, deafness in both ears.

On the part of the eyes: impaired visual function, inflammation of the conjunctiva, dry mucous membranes, hemorrhages, blindness, herpes eyes.

Immunity: an allergic reaction - angioedema , hypersensitivity to the ingredients of the drug.

Metabolism: dehydration, impaired level of potassium, sodium, calcium, magnesium, phosphorus and uric acid in the blood, exhaustion, vitamin B12 deficiency.

From the skin: rash, swelling, itching, urticaria , psoriasis , nodules under the skin, skin pigmentation, baldness, increased sweating, especially at night, bruising and hematoma.

On the part of the musculoskeletal system: pain in the muscles and joints, cramps, spasms, twitching, impaired mobility of the joints and their swelling.

On the part of the reproductive system: erectile dysfunction, pain in the testicles.

How and where to store?

Velcade is stored in its original packaging for 3 years from the date of issue, at a temperature of up to 30 ° C. Keep out of the reach of children.

The prepared solution for injection can be stored in a vial or syringe for up to 8 hours in a room with natural light, at a temperature not higher than 25 ° C.

Pharmacy sales terms

The drug belongs to the list of prescription drugs.

Velcade price

Velcade lyophilisate for injection of 3 mg - 55000-60000 rub.

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