Tretinoin | Vesanoid capsules 10 mg, 100 pcs.
Special Price
$240.56
Regular Price
$255.00
In stock
SKU
BID886939
Latin name
VESANOID
VESANOID
Latin name
VESANOID
Release form
Capsules.
Packing
100 pcs.
Pharmacological action
Antitumor drug. Systemic retinoid, inducer of cell differentiation. Tretinoin (a completely trans-retinoic acid) is a natural retinol metabolite belonging to the class of retinoids, which includes natural and synthetic analogues. In vitro studies have shown that trans-retinoic acid induces differentiation and inhibits the proliferation of transformed hematopoietic cells, including with myeloid leukemia in humans. The mechanism of action in acute promyelocytic leukemia may consist in a change in the binding of trans retinoic acid to nuclear retinoic acid receptors, and the β receptor of retinoic acid also changes due to fusion with the PML protein.
Pharmacokinetics
Absorption
Tretinoin (a fully trans retinoic acid) is an endogenous metabolite of vitamin A, normally present in plasma. After oral administration, it is well absorbed. Cmax in blood plasma is reached after 3 hours. Absorption varies greatly both in different patients and in the same patient.
Distribution of
Plasma protein binding is high. After reaching a peak, the plasma concentration decreases. After a single dose of the drug in a dose of 40 mg, the plasma concentration returns to the endogenous level after 7-12 hours. With multiple doses, the drug does not accumulate, the drug does not stay in the tissues.
Metabolism
Tretinoin (a completely trans-retinoic acid) isomerizes to 13-cis-retinoic acid and oxidizes to 4-hydroxymetabolites.
With repeated administration, the plasma concentration of the drug may decrease significantly, possibly due to the induction of the cytochrome P450 enzyme system, which increases clearance and decreases the bioavailability of the drug after oral administration.
The main route of elimination (60%) is the elimination by the kidneys in the form of metabolites formed during oxidation and glucuronidation. They have a longer T1 / 2 than trans retinoic acid and can accumulate in small amounts. The average T1 / 2 is 0.7 hours.
Pharmacokinetics in special cases
The pharmacokinetics and the need for dose adjustment in patients with impaired renal or hepatic function have not been studied.
Indications
Induction of remission in acute promyelocytic leukemia (AMPL classification according to FAB - AML-M3). The drug can be prescribed both to previously untreated patients and patients with relapses or refractory to standard chemotherapy (daunomycin and cytosine arabinoside or their analogues).
Contraindications
Hypersensitivity to the drug
pregnancy
lactation (breastfeeding)
concomitant use of tetracyclines, mini-drinks with progesterone and vitamin A.
Use during pregnancy and lactation
All of the following measures should be considered in relation to the severity of the disease and the urgency of therapy.
Tretinoin has a teratogenic effect. Therefore, the drug is contraindicated in women who are already pregnant. If pregnancy occurs during the period when a woman takes tretinoin, regardless of the dose and duration of treatment, there is a very high risk of having a baby with developmental defects. Treatment is prescribed to patients of childbearing age only if each of the following conditions is met:
the patient is informed by doctors about the risk of pregnancy during and within 1 month after treatment with
tretinoin, the patient wishes to use mandatory contraceptive measures. It is imperative that every patient of childbearing age receiving tretinoin used effective contraceptive measures during the treatment process and within 1 month after completion of
treatment during treatment, pregnancy tests should be performed at least 1 time per month.
If, despite these precautions, pregnancy occurs during treatment with tretinoin or within 1 month after drug discontinuation, the risk of having a baby with developmental defects is very high, especially if the drug was prescribed in the first trimester of pregnancy.
If Vesanoid therapy is started, breast-feeding should be discontinued.
Composition
1 capsule contains:
Active substances: tretinoin (fully trans-retinoic acid) 10 mg.
Excipients: beeswax yellow, soybeans oil, soybeans, hydrogenated oil, soybeans, partially hydrogenated oil.
Composition of the capsule shell: glycerol 85%, gelatin, Karion 83 (hydrolyzed potato starch, mannitol, sorbitol), titanium dioxide (E171), yellow iron dye (E172), red iron dye (E172).
Dosage and administration
The drug is administered orally at a daily dose of 45 mg / m2 of body surface in 2 divided doses (for adults, approximately 8 capsules). For children, the same dose is recommended, unless severe toxic phenomena occur (in particular, the dose must be reduced if the child has unbearable headaches).
Treatment should be continued for 30 to 90 days until complete remission is achieved. After this, you should immediately switch to the standard consolidation chemotherapy regimen, for example, three courses of daunomycin and cytosine arabinoside with an interval of 5-6 weeks.
If remission occurs with monotherapy with Vesanoid, you do not need to change its dose when chemotherapy is attached.
Due to the lack of sufficient information regarding patients with renal and / or liver failure, it is necessary to reduce the dose to 25 mg / m2 in this category of patients.
Side effects of
Symptoms of hypervitaminosis A, which occur when using all other retinoids, have often been observed with the drug at the recommended doses.
Dermatological reactions: dry skin, erythema, rash, itching, increased sweating, alopecia, cheilitis, dry mucous membranes of the oral cavity, nose, conjunctiva and other mucous membranes, with or without signs of inflammation - formation of ulcers on the mucous membrane of the genital organs, Sweet syndrome erythema nodosum.
From the side of the central nervous system and peripheral nervous system: headache, intracranial hypertension (mainly in children), fever, chills, dizziness, confusion, anxiety, agitation, depression, paresthesia, insomnia, weakness.
On the part of the sensory organs: impaired vision and hearing.
From the musculoskeletal system: bone pain, chest pain rarely - myositis.
From the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, decreased appetite, pancreatitis, increased transaminase activity (ALT, AST).
Metabolism: increased triglycer concentrationserides, cholesterol, creatinine in the blood serum in some cases - hypercalcemia.
From the respiratory system: pleural effusion, shortness of breath, respiratory failure, bronchospasm.
From the cardiovascular system: rhythm disturbances, hot flashes, edema in some cases - thrombosis.
From the hemopoietic system: rarely - thrombocytosis, severe basophilia with clinically manifested hyperhistaminemia or without it, mainly in patients with a rare variant of acute promyelocytic leukemia with basophilic differentiation.
The decision to interrupt or continue therapy should be based on an assessment of the ratio of treatment benefits to the severity of side effects.
Retinoic Acid Syndrome in Acute Promyelocytic Leukemia
In clinical trials, hyperleukocytosis (75% of patients) was often observed. In many patients with acute promyelocytic leukemia (up to 25%), retinoic acid syndrome (IBS) occurs during treatment with tretinoin, which is characterized by fever, shortness of breath, acute respiratory distress syndrome, the occurrence of pulmonary infiltrates, arterial hypotension, pleural and pericardial effusion, edema, an increase body weight, liver, kidney and multiple organ failure. IBS is often accompanied by hyperleukocytosis. Without treatment, this syndrome can be fatal.
Information on the use of tretinoin in children is limited. There are reports of an increase in toxic effects in children receiving tretinoin, in particular, intracranial hypertension.
overdose
Symptoms: No acute overdose has been reported to date. Apparently, accidental overdose of tretinoin will be manifested by the reversible symptoms characteristic of hypervitaminosis A. The dose recommended for patients with acute promyelocytic leukemia is 1/4 of the dose most tolerated in patients with solid tumors and is less than the maximum tolerable for children .
Treatment: There is no specific treatment for overdose, but it is important that the patient is placed in the hematology unit.
Storage conditions
Vials should be stored tightly closed, in a dark place at a temperature of no higher than 30 РC. Blisters should be stored in a place protected from light and moisture, at a temperature not exceeding 25 РC.
The drug should be stored out of the reach of children.
Expiration
3 years.
Deystvuyuschee substances
Tretinoin
Pharmacy leave
Po
dosage form
Dosage form
capsules
VESANOID
Release form
Capsules.
Packing
100 pcs.
Pharmacological action
Antitumor drug. Systemic retinoid, inducer of cell differentiation. Tretinoin (a completely trans-retinoic acid) is a natural retinol metabolite belonging to the class of retinoids, which includes natural and synthetic analogues. In vitro studies have shown that trans-retinoic acid induces differentiation and inhibits the proliferation of transformed hematopoietic cells, including with myeloid leukemia in humans. The mechanism of action in acute promyelocytic leukemia may consist in a change in the binding of trans retinoic acid to nuclear retinoic acid receptors, and the β receptor of retinoic acid also changes due to fusion with the PML protein.
Pharmacokinetics
Absorption
Tretinoin (a fully trans retinoic acid) is an endogenous metabolite of vitamin A, normally present in plasma. After oral administration, it is well absorbed. Cmax in blood plasma is reached after 3 hours. Absorption varies greatly both in different patients and in the same patient.
Distribution of
Plasma protein binding is high. After reaching a peak, the plasma concentration decreases. After a single dose of the drug in a dose of 40 mg, the plasma concentration returns to the endogenous level after 7-12 hours. With multiple doses, the drug does not accumulate, the drug does not stay in the tissues.
Metabolism
Tretinoin (a completely trans-retinoic acid) isomerizes to 13-cis-retinoic acid and oxidizes to 4-hydroxymetabolites.
With repeated administration, the plasma concentration of the drug may decrease significantly, possibly due to the induction of the cytochrome P450 enzyme system, which increases clearance and decreases the bioavailability of the drug after oral administration.
The main route of elimination (60%) is the elimination by the kidneys in the form of metabolites formed during oxidation and glucuronidation. They have a longer T1 / 2 than trans retinoic acid and can accumulate in small amounts. The average T1 / 2 is 0.7 hours.
Pharmacokinetics in special cases
The pharmacokinetics and the need for dose adjustment in patients with impaired renal or hepatic function have not been studied.
Indications
Induction of remission in acute promyelocytic leukemia (AMPL classification according to FAB - AML-M3). The drug can be prescribed both to previously untreated patients and patients with relapses or refractory to standard chemotherapy (daunomycin and cytosine arabinoside or their analogues).
Contraindications
Hypersensitivity to the drug
pregnancy
lactation (breastfeeding)
concomitant use of tetracyclines, mini-drinks with progesterone and vitamin A.
Use during pregnancy and lactation
All of the following measures should be considered in relation to the severity of the disease and the urgency of therapy.
Tretinoin has a teratogenic effect. Therefore, the drug is contraindicated in women who are already pregnant. If pregnancy occurs during the period when a woman takes tretinoin, regardless of the dose and duration of treatment, there is a very high risk of having a baby with developmental defects. Treatment is prescribed to patients of childbearing age only if each of the following conditions is met:
the patient is informed by doctors about the risk of pregnancy during and within 1 month after treatment with
tretinoin, the patient wishes to use mandatory contraceptive measures. It is imperative that every patient of childbearing age receiving tretinoin used effective contraceptive measures during the treatment process and within 1 month after completion of
treatment during treatment, pregnancy tests should be performed at least 1 time per month.
If, despite these precautions, pregnancy occurs during treatment with tretinoin or within 1 month after drug discontinuation, the risk of having a baby with developmental defects is very high, especially if the drug was prescribed in the first trimester of pregnancy.
If Vesanoid therapy is started, breast-feeding should be discontinued.
Composition
1 capsule contains:
Active substances: tretinoin (fully trans-retinoic acid) 10 mg.
Excipients: beeswax yellow, soybeans oil, soybeans, hydrogenated oil, soybeans, partially hydrogenated oil.
Composition of the capsule shell: glycerol 85%, gelatin, Karion 83 (hydrolyzed potato starch, mannitol, sorbitol), titanium dioxide (E171), yellow iron dye (E172), red iron dye (E172).
Dosage and administration
The drug is administered orally at a daily dose of 45 mg / m2 of body surface in 2 divided doses (for adults, approximately 8 capsules). For children, the same dose is recommended, unless severe toxic phenomena occur (in particular, the dose must be reduced if the child has unbearable headaches).
Treatment should be continued for 30 to 90 days until complete remission is achieved. After this, you should immediately switch to the standard consolidation chemotherapy regimen, for example, three courses of daunomycin and cytosine arabinoside with an interval of 5-6 weeks.
If remission occurs with monotherapy with Vesanoid, you do not need to change its dose when chemotherapy is attached.
Due to the lack of sufficient information regarding patients with renal and / or liver failure, it is necessary to reduce the dose to 25 mg / m2 in this category of patients.
Side effects of
Symptoms of hypervitaminosis A, which occur when using all other retinoids, have often been observed with the drug at the recommended doses.
Dermatological reactions: dry skin, erythema, rash, itching, increased sweating, alopecia, cheilitis, dry mucous membranes of the oral cavity, nose, conjunctiva and other mucous membranes, with or without signs of inflammation - formation of ulcers on the mucous membrane of the genital organs, Sweet syndrome erythema nodosum.
From the side of the central nervous system and peripheral nervous system: headache, intracranial hypertension (mainly in children), fever, chills, dizziness, confusion, anxiety, agitation, depression, paresthesia, insomnia, weakness.
On the part of the sensory organs: impaired vision and hearing.
From the musculoskeletal system: bone pain, chest pain rarely - myositis.
From the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, decreased appetite, pancreatitis, increased transaminase activity (ALT, AST).
Metabolism: increased triglycer concentrationserides, cholesterol, creatinine in the blood serum in some cases - hypercalcemia.
From the respiratory system: pleural effusion, shortness of breath, respiratory failure, bronchospasm.
From the cardiovascular system: rhythm disturbances, hot flashes, edema in some cases - thrombosis.
From the hemopoietic system: rarely - thrombocytosis, severe basophilia with clinically manifested hyperhistaminemia or without it, mainly in patients with a rare variant of acute promyelocytic leukemia with basophilic differentiation.
The decision to interrupt or continue therapy should be based on an assessment of the ratio of treatment benefits to the severity of side effects.
Retinoic Acid Syndrome in Acute Promyelocytic Leukemia
In clinical trials, hyperleukocytosis (75% of patients) was often observed. In many patients with acute promyelocytic leukemia (up to 25%), retinoic acid syndrome (IBS) occurs during treatment with tretinoin, which is characterized by fever, shortness of breath, acute respiratory distress syndrome, the occurrence of pulmonary infiltrates, arterial hypotension, pleural and pericardial effusion, edema, an increase body weight, liver, kidney and multiple organ failure. IBS is often accompanied by hyperleukocytosis. Without treatment, this syndrome can be fatal.
Information on the use of tretinoin in children is limited. There are reports of an increase in toxic effects in children receiving tretinoin, in particular, intracranial hypertension.
overdose
Symptoms: No acute overdose has been reported to date. Apparently, accidental overdose of tretinoin will be manifested by the reversible symptoms characteristic of hypervitaminosis A. The dose recommended for patients with acute promyelocytic leukemia is 1/4 of the dose most tolerated in patients with solid tumors and is less than the maximum tolerable for children .
Treatment: There is no specific treatment for overdose, but it is important that the patient is placed in the hematology unit.
Storage conditions
Vials should be stored tightly closed, in a dark place at a temperature of no higher than 30 РC. Blisters should be stored in a place protected from light and moisture, at a temperature not exceeding 25 РC.
The drug should be stored out of the reach of children.
Expiration
3 years.
Deystvuyuschee substances
Tretinoin
Pharmacy leave
Po
dosage form
Dosage form
capsules
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