Medicine > All about Azalpho (Azacitidine lyophilized) injection
Name of Medicine:- Azalpho
Chemical Formula:- C8H12N4O5
Active Ingredient:- Azacitidine
Description:- Azalpho is indicated for the treatment of Blood cancer. It is available in the form of an injection with a strength of 100mg.
Azalpho comprises Azacitidine lyophilized as an active ingredient; this injection is prescribed for the treatment of Blood Cancer and it works by blocking the activity of an enzyme and stops the multiplication of cancer cells. Azalpho (Azacitidine) injection is available in the strength of 100mg.
Azalpho (Azacitidine) injection is indicated for the treatment of a specific type of blood cancer known as MDS (Myelodysplastic Syndrome). This injection works by blocking the activity of an enzyme and restricts the division and multiplication of cancer cells in the body. Azalpho is an anticancer medication and it exhibits the growth of cancer cells by interfering with the DNA and RNA of the cancer cell.
Azacitidine applies its antineoplastic effects by causing hypomethylation of DNA and direct cytotoxicity on abnormal hematopoietic cells in the bone marrow. The concentration of azacitidine required for maximum inhibition of DNA methylation in vitro does not cause major suppression of DNA synthesis. Hypomethylation may reinstate normal function to genes that are critical for differentiation and proliferation. Azacitidine causes the cytotoxic effects of the death of rapidly dividing cells, including cancer cells that are no longer responsive to normal growth control mechanisms. non-proliferating cells are remarkably insensitive to azacitidine. Upon uptake into cells, azacitidine is phosphorylated to the 5-azacytidine monophosphate by uridine-cytidine kinase, then to diphosphate by pyrimidine monophosphate kinases and triphosphate by diphosphate kinases. 5-Azacitidine triphosphate is incorporated into RNA, leading to the disruption of nuclear and cytoplasmic RNA metabolism and inhibition of protein synthesis. 5-aza-deoxycytidine is a reduced form of 5-Azacytidine diphosphate by ribonucleotide reductase. The resultant metabolite is phosphorylated to the 5-azadeoxycitidine triphosphate by nucleoside diphosphate kinases. 5-azadeoxycitidine triphosphate is then incorporated into DNA, leading to inhibition of DNA synthesis. The most toxic during the S-phase of the cell cycle is azacitidine.
Azacitidine (5-azacytidine) is a chemical analog of the cytosine nucleoside used in DNA and RNA. Azacitidine tends to induce antineoplastic activity by inhibiting DNA methyltransferase at lower doses and cytotoxicity by incorporation into RNA and DNA at higher doses. Covalent binding to DNA methyltransferase leads to hypomethylation of DNA that hinders DNA synthesis. As this compound is a ribonucleoside, it works to incorporate into RNA to a greater extent than into DNA. The incorporation into RNA results in the disassembly of polyribosomes, defective methylation and acceptor function of transfer RNA, and inhibition of the production of protein, resulting in cell death.
A clinical study of azacitidine incubation in human liver fractions demonstrated that this compound may be metabolized by the liver. The potential of azacitidine to inhibit cytochrome P450 (CYP) enzymes is unknown.
After IV administration of radioactive azacitidine to about five cancer patients, the mean urinary excretion was approximately 85% of the radioactive dose. Fecal excretion was about <1% of the total administered radioactivity over 3 days. The average excretion of radioactivity in urine after SC administration of 14C-azacitidine was nearly 50%.
The efficacy and safety of Azacitidine, a cytosine nucleoside analog, has been shown in two large phase III trials in patients suffering from myelodysplastic syndromes (MDS), majorly in higher-risk patients. In the Cancer and Leukemia Group B (CALGB) study (lower-and higher-risk MDS patients; n = 191) azacitidine significantly prolonged median time-to-progression to acute myeloid leukemia or death (21 vs 13 months for supportive care; p = 0.007). The AZA-001 trial (Intermediate-2-and High-risk MDS patients; n = 358) showed azacitidine significantly prolonged median overall survival compared with conventional care regimens (24.5 vs 15.0 months; p = 0.0001). These results represent Azacitidine as a reference first-line treatment in patients suffering from Intermediate-2-and High-risk MDS who are not immediate candidates for allogeneic stem cell transplantation.
When azacitidine is combined with other medications it causes various and different interactions with other medications. During the drug interaction study, when Azalpho is inhibited with other medications, some activities are observed in the absorption of azacitidine and the reported reactions are -
Severe risk of Anemia, Neutropenia, and Thrombocytopenia can be increased
Azacitidine may decrease or increase the excretion rate and it could result in a higher or lower serum level.
Risk of severe bleeding.
CYP2C8 and CYP3A4 are responsible for Azacitidine. In the absence of systematic clinical drug interaction trials, when using Azalpho (Azacitidine) with known CYP2C8 and CYP3A4 substrates or inhibitors, caution should be exercised.
Grapefruit is an agent that is responsible for the inhibition of CYP3A4 metabolism. It may increase the serum levels of Azacitidine.
Hepatic dysfunction:- Patients during treatment with Azacitidine can experience liver failure and hepatic reactions like - hepatitis and increased liver enzymes. Close monitoring of liver function is required.
Anemia:- Patients with preexisting conditions should be monitored closely and carefully. Complete and absolute monitoring of blood cell counts frequently for response and/or toxicity, at a minimum, before each dosing cycle.
Antineoplastic Agents: is an effective treatment of malignant, or cancerous, disease. These drugs come in various forms like liquid that are easily injected and oral pills such as capsules and tablets.
Myelosuppressive Agents: These agents work by stopping or slowing the growth of blood-forming cells in the bone marrow. Myelosuppressive agents are responsible for the destruction of some normal cells and cancer cells in the body.
Immunosuppressive Agents: These medicines are used for the treatment of autoimmune diseases. Immunosuppressive agents are also used to prevent organ rejection that may cause immunodeficiency with malignancy and severe infections.
Recommended dosage:- The recommended dose of Azalpho (Azacitidine) injection for the first treatment cycle, for all patients, is 75 mg/m2 intravenously, daily for 7 days. Premedicate patients for nausea and vomiting. It is necessary to obtain complete blood counts, liver function, and serum creatinine before the first dose. The dose may be increased to 100 mg/m2 if no satisfactory effect is seen after 2 treatment cycles and if no effects other than nausea and vomiting have occurred. It is recommended that patients be treated for a minimum of 4 to 6 cycles. Hence, a complete or partial response may require additional treatment cycles. Discontinuation of treatment with Azalpho is not required as long as it is beneficial for patients.
Dose adjustment:- If extremely severe decreases in serum bicarbonate levels to less than 20 mEq/L occur, dose alteration is required by 50% for the next course. Similarly, if unexplained elevations of BUN or serum creatinine occur, delay the next cycle until values return to normal or baseline and reduce the dose by 50% for the next course.
Overdose:- In case of an overdose of Azalpho (Azacitidine) injection, the patients may experience multiple symptoms that might cause fetal harm. Hence, it is important to contact a qualified physician in order to receive supportive care and regular monitoring as per the current medical condition.
Hematologic toxicity: Azacitidine is associated with anemia (low red blood cell count), neutropenia (low level of neutrophils), and thrombocytopenia (low platelet count).
Hemorrhage: Hemorrhage may occur in some patients administering Azalpho. This may show some symptoms like weakness, tingling, seizures, difficulty in speaking, changes in vision, difficulty using fine motor skills, and vomiting.
Edema and Fluid retention: Azalpho (Azacitidine) is associated with edema and severe fluid retention. It refers to an accumulation of fluid in the tissues of the body. Close monitoring should be done in patients for related signs and symptoms.
Hepatotoxicity: The most common effects associated with Hepatotoxicity are rash, nausea, vomiting, fatigue, loss of appetite, and jaundice. This condition (liver damage) occurs due to exposure to certain drugs. It is an uncommon but serious adverse reaction.
Heart failure: In some patients, the administration of Azalpho may lead to congestive heart failure and left ventricular dysfunction. This adverse event may be common in patients with patients already suffering from cardiac disease. The patients should be monitored for such symptoms.
Dermatologic Toxicities in some patients may occur during the course of Azalpho. These reactions include photosensitivity reaction, dermatitis, pigmentation disorder (a severe condition in which skin loses its pigment cells), dry skin, acne, nail disorder, urticaria (itchy welts due to a skin reaction), and hyperhidrosis.
Several gastrointestinal effects such as peptic ulcers, gastritis (inflammation of the stomach lining), gastroenteritis (including diarrhea, cramps, vomiting, and fever), stomach ache, and bloating may occur. Azalpho should be taken with food to minimize or treat these effects.
Azalpho treatment is associated with anemia, neutropenia, and thrombocytopenia. Close monitoring of blood cell count should be performed by your healthcare provider to check the response and toxicity, but at a minimum, before each dosing cycle. After administration of the recommended dosage for the first cycle, dosage for subsequent cycles should be reduced or delayed based on nadir counts (the lowest level that blood cell counts reach) and hematologic response.
Renal disorders starting from conditions like elevated serum creatinine to renal failure and death have occurred rarely in patients treated with intravenous azacitidine in combination with other chemotherapeutic agents for non-MDS conditions. Besides, renal tubular acidosis, defined as a fall in serum bicarbonate to <20 mEq/L in association with alkaline urine and hypokalemia (serum potassium <3 mEq/L) developed in 5 patients with CML treated with azacitidine and etoposide. If the extremely severe decrease in serum bicarbonate <20 mEq/L or elevations of BUN or serum creatinine occur, the dosage should be minimized.
Azacitidine is thought to be hepatotoxic in patients with severe pre-existing hepatic impairment, extreme caution is required in patients with liver disease. During treatment with Azalpho, patients with extensive tumor burden due to metastatic disease have rarely experienced progressive hepatic coma and death during treatment, especially in patients with baseline albumin <30 g/L. Azacitidine is not recommended in patients with advanced malignant hepatic tumors.
Thrombocytopenia, neutropenia, and anemia commonly occur; neutropenic fever has been reported. Monitor blood counts. Hematologic toxicity may require treatment interruption, dose alteration, and/or discontinuation with Azalpho (Azacitidine) injection. Consider supportive care with hematopoietic growth factors.
Azalpho (Azacitidine) may cause fetal harm when administered to a pregnant woman. This medicine is not indicated to patients who are pregnant and planning to become pregnant. Women possessing child-bearing potential are advised to start using proper contraceptive measures 28 days before the course of Azalpho.
It is unknown whether Azalpho (Azacitidine) is excreted in human milk or not. Since most other drugs are excreted in human milk, it is necessary to take precautions to avoid adverse reactions. Hence, breastfeeding should be discontinued while receiving treatment with Azalpho.
The safety and efficacy of Azalpho have not been established in patients below the age of 18. In patients, aged 65 and above, Azalpho (Azacitidine) has been used in several clinical trials. No notable differences in the efficacy and safety of this medicine have been observed.
Azalpho (Azacitidine) is available as an injection packed in a single-use vial. Store this medication at 20°C - 25°C; excursions permitted to 15°C - 30°C. Keep Azalpho Injection away from the reach of children and pets. Protect them from direct heat, light, and moisture. Proper care should be exercised while handling this drug. Women who are pregnant should not handle Azalpho Injection without protection (gloves). Know the procedure to dispose of the used and expired bottles of medicines from a pharmacist.
Name of Medicine: Paznib
Active Ingredient: Pazopanib
Say Goodbye to hard-to-swallow capsules and yes to Chewable vitamin gummies. Let these flavors of good health add more valMore Information
Vitagoli is a chewable bear-shaped gummy that comes with exclusive health benefits and flavors. It is an innovative producMore Information
Arechar Healthcare provides independent and precise information about prescription drugs with the related news and press releases. This content is displayed for informational purposes only and is not intended to be an alternative for any medical advice/prescription or treatment. Do not delay or ignore any medical treatment owing to something you’ve read or seen on this website. Also, this website offers links to other websites, enabling the viewers to directly switch to that website for detailed information or accurate references. Thus, Arechar is not responsible for the content displayed on the linked websites or the content of the links in the linked website.