Category Archives: Products

Efesir

March 18, 2024Productsclarity-admin

Efesir

(Deferasirox)

Composition:

Each dispersible tablet contains Deferasirox 250 mg and 500 mg.

ATC Code

V03AC03 — Deferasirox

Structure

Description

Deferasirox is an iron chelator and the first oral medication FDA approved for chronic iron overload in patients receiving long term blood transfusions.

Introduction

For the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years of age and older.

Indication

Associated Conditions

Pharmacodynamics

Deferasirox is an orally active chelator that is selective for iron (as Fe3+). It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Although deferasirox has very low affinity for zinc and copper there are variable decreases in the serum concentration of these trace metals after the administration of deferasirox. The clinical significance of these decreases is uncertain.

Mechanism of Action

Two molecules of deferasirox are capable of binding to 1 atom of iron. Deferasirox works in treating iron toxicity by binding trivalent (ferric) iron (for which it has a strong affinity), forming a stable complex which is eliminated via the kidneys.

Product Information

Gemcitabel

March 18, 2024Productsclarity-admin

Gemcitabel

(Gemcitabine)

Composition:

Each 10 ml vial contains gemcitabine (as gemcitabine hydrochloride) 200 mg and 1000 mg.

ATC Code

L01BC05 — Gemcitabine

Structure

Description

Gemcitabine is a nucleoside analog used as chemotherapy. As with fluorouracil and other analogues of pyrimidines, the drug replaces one of the building blocks of nucleic acids, in this case cytidine, during DNA replication. The process arrests tumor growth, as new nucleosides cannot be attached to the “faulty” nucleoside, resulting in apoptosis (cellular “suicide”).

Gemcitabine is used in various carcinomas: non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. It is being investigated for use in oesophageal cancer, and is used experimentally in lymphomas and various other tumor types.

Indication

Associated Conditions

Advanced Ovarian Cancer
Carcinoma Breast Stage IV
Locally Advanced Biliary Tract Cancer
Locally Advanced Non-Small Cell Lung Cancer
Locally Advanced Pancreatic Adenocarcinoma
Metastatic Biliary Tract Cancer
Metastatic Bladder Cancer
Non-small Cell Lung Cancer (NSCLC), Stage IV
Advanced Bladder cancer
Stage 4 Pancreatic adenocarcinoma

Pharmacodynamics

Gemcitabine is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine – which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the “S” phase (or DNA synthesis phase of the cell cycle), stopping normal development and division. Gemcitabine blocks an enzyme which converts the cytosine nucleotide into the deoxy derivative. In addition, DNA synthesis is further inhibited because Gemcitabine blocks the incorporation of the thymidine nucleotide into the DNA strand. It demonstrates dose-dependent synergistic activity with cisplatin in vitro. In vivo, gemcitabine showed activity in combination with cisplatin against the LX-1 and CALU-6 human lung xenografts, but minimal activity was seen with the NCI-H460 or NCI-H520 xenografts. Gemcitabine was synergistic with cisplatin in the Lewis lung murine xenograft. Sequential exposure to gemcitabine 4 hours before cisplatin produced the greatest interaction.

Mechanism of Action

Gemcitabine inhibits thymidylate synthetase, leading to inhibition of DNA synthesis and cell death. Gemcitabine is a prodrug so activity occurs as a result of intracellular conversion to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate by deoxycitidine kinase. Gemcitabine diphosphate also inhibits ribonucleotide reductase, the enzyme responsible for catalyzing synthesis of deoxynucleoside triphosphates required for DNA synthesis. Finally, Gemcitabine triphosphate (diflurorodeoxycytidine triphosphate) competes with endogenous deoxynucleoside triphosphates for incorporation into DNA.

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HDX

March 18, 2024Productsclarity-admin

HDX

(Hydroxyurea)

Composition:

Each capsule contains Hydroxyurea 500mg

ATC Code

L01XX05 – Hydroxycarbamide

Description

An antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase.

Indication

Associated Conditions

Essential Thrombocythemia (ET)
Head and Neck Carcinoma
Hypereosinophilic Syndromes
Melanoma
Meningiomas
Ovarian Cancer Metastatic
Polycythemia Vera (PV)
Sickle Cell Anemia
Chronic, refractory Myeloid Leukemia
Inoperable Ovarian cancer

Pharmacodynamics

Hydroxyurea has dose-dependent synergistic activity with cisplatin in vitro. In vivo Hydroxyurea showed activity in combination with cisplatin against the LX-1 and CALU-6 human lung xenografts, but minimal activity was seen with the NCI-H460 or NCI-H520 xenografts. Hydroxyurea was synergistic with cisplatin in the Lewis lung murine xenograft. Sequential exposure to Hydroxyurea 4 hours before cisplatin produced the greatest interaction.

Mechanism of Action

Hydroxyurea is converted to a free radical nitroxide (NO) in vivo, and transported by diffusion into cells where it quenches the tyrosyl free radical at the active site of the M2 protein sub unit of ribonucleotide reductase, inactivating the enzyme. The entire replicase complex, including ribonucleotide reductase, is inactivated and DNA synthesis is selectively inhibited, producing cell death in S phase and synchronization of the fraction of cells that survive. Repair of DNA damaged by chemicals or irradiation is also inhibited by hydroxyurea, offering potential synergy between hydroxyurea and radiation or alkylating agents. Hydroxyurea also increases the level of fetal hemoglobin, leading to a reduction in the incidence of vasoocclusive crises in sickle cell anemia. Levels of fetal hemoglobin increase in response to activation of soluble guanylyl cyclase (sGC) by hydroxyurea-derived NO.

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Metast

March 18, 2024Productsclarity-admin

Metast

(Zoledronic acid)

Composition:

Each vial contains zoledronic acid (as zoledronic acid monohydrate) – 4 mg.

ATC Code

M05BA08 — Zoledronic acid

Structure

Description

Zoledronic acid is a bisphosphonate and used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases.
An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture.

Indication

Associated Conditions

Pharmacodynamics

Zoledronate is a bisphosphonic acid which is an inhibitor of osteoclastic bone resorption. Zoledronate is used to prevent osteoporosis and skeletal fractures, particularly in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia, particularly hypercalcemia of malignancy. It can also be helpful for treating pain from bone metastases.

Mechanism of Action

The action of zoledronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Zoledronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates such as zoledronate appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.

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For References

Methobel

March 18, 2024Productsclarity-admin

Methobel

(Methotrexate)

Composition:

Each ampoule/vial contains methotrexate (as methotrexate sodium) 50 mg

ATC Code

L01BA01 — Methotrexate

Structure

Description

Methotrexate is a folate derivative that inhibits several enzymes responsible for nucleotide synthesis. This inhibition leads to suppression of inflammation as well as prevention of cell division. Because of these effects, methotrexate is often used to treat inflammation caused by arthritis or to control cell division in neoplastic diseases such as breast cancer and non-Hodgkin’s lymphoma.

Due to the toxic effects of methotrexate, it is indicated for treatment of some forms of arthritis and severe psoriasis only if first line treatment has failed or patients are intolerant of those treatments.

Indication

Methotrexate oral solution is indicated for pediatric acute lymphoblastic leukemia and pediatric polyarticular juvenile idiopathic arthritis.4 Methotrexate injections for subcutaneous use are indicated for severe active rheumatoid arthritis, polyarticular juvenile idiopathic arthritis and severe, recalcitrant, disabling psoriasis.
Other formulations are indicated to treat gestational choriocarcinoma, chorioadenoma destruens, hydatiform mole, breast cancer, epidermoid cancer of the head and neck, advanced mycosis fungoides, lung cancer, and advanced non-Hodgkin’s lymphoma.7 It is also used in the maintenance of acute lymphocytic leukemia.7 Methotrexate is also given before treatment with leucovorin to prolong relapse-free survival following surgical removal of a tumour in non-metastatic osteosarcoma.

Associated Conditions

Acute Lymphocytic Leukemia (ALL)
Acute Promyelocytic Leukemia (APL)
Breast Cancer
Cancer, Bladder
Central Nervous System Lymphoma
Choriocarcinoma
Crohn’s Disease (CD)
Dermatomyositis
Disseminated Sclerosis
Extrauterine Pregnancy
Graft Versus Host Disease (GVHD)
Head and Neck Carcinoma
Hydatidiform Mole
Lung Cancer Small Cell Lung Cancer (SCLC)
Meningeal leukemia
Polymyositis
Sarcoma, Osteogenic
Soft Tissue Sarcoma (STS)
Squamous Cell Carcinoma of Lung
Systemic Lupus Erythematosus (SLE)
Uveitis
Active Pauciarticular juvenile rheumatoid arthritis
Advanced Alibert-Bazin syndrome
Advanced non-Hodgkin lymphoma
Nonleukemic meningeal cancer
Refractory Takayasu arteritis
Severe Psoriasis
Severe, active Rheumatoid arthritis

Pharmacodynamics

Methotrexate inhibits enzymes responsible for nucleotide synthesis which prevents cell division and leads to anti-inflammatory actions. It has a long duration of action and is generally given to patients once weekly. Methotrexate has a narrow therapeutic index.

Mechanism of Action

Methotrexate enters tissues and is converted to a methotrexate polyglutamate by folylpolyglutamate.
Methotrexate’s mechanism of action is due to its inhibition of enzymes responsible for nucleotide synthesis including dihydrofolate reductase, thymidylate synthase, aminoimidazole caboxamide ribonucleotide transformylase (AICART), and amido phosphoribosyltransferase. Inhibtion of nucleotide synthesis prevents cell division.
In rheumatoid arthritis, methotrexate polyglutamates inhibit AICART more than methotrexate. This inhibition leads to accumulation of AICART ribonucleotide, which inhibits adenosine deaminase, leading to an accumulation of adenosine triphosphate and adenosine in the extracellular space, stimulating adenosine receptors, leading to anti-inflammatory action.

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Oncofos

March 18, 2024Productsclarity-admin

Oncofos

(Cyclophosphamide)

Composition:

Each vial contains Cyclophosphamide eq. to Anhydrous Cyclophosphamide 500mg

ATC Code

L01AA01 — Cyclophosphamide

Structure

Description

Precursor of an alkylating nitrogen mustard antineoplastic and immunosuppressive agent that must be activated in the liver to form the active aldophosphamide. It has been used in the treatment of lymphoma and leukemia. Its side effect, alopecia, has been used for defleecing sheep. Cyclophosphamide may also cause sterility, birth defects, mutations, and cancer.

Indication

Associated Conditions

Acute Lymphoblastic Leukaemias (ALL)
Acute Myelocytic Leukemia
Adenocarcinoma of the Ovaries
Autoimmune Hemolytic Anemia
Breast Cancer
Burkitt’s Lymphoma
Chronic Lymphocytic Leukaemia (CLL)
Chronic Myeloid Leukemia (CML)
Disseminated Neuroblastoma
Ewing’s Sarcoma (ES)
Granulomatosis With Polyangiitis
Juvenile Idiopathic Arthritis (JIA)
Lung Cancers
Lymphoma, Hodgkins
Minimal Change Nephrotic Syndrome (MCNS)
Multiple Myeloma (MM)
Myasthenia Gravis
Nephritis, Lupus
Non-Hodgkin’s Lymphoma (NHL)
Ovarian germ cell tumour
Pheochromocytomas
Retinoblastoma
Rhabdomyosarcomas
Uveitis
Waldenström’s Macroglobulinemia (WM)
Advanced Alibert-Bazin syndrome
Histiocytic lymphoma
Metastatic gestational trophoblastic tumor
Mixed-cell type lymphoma
Recurrent Pericarditis
Refractory Small cell lung cancer
Refractory immune thrombocytopenia
Relapsed Wilm’s tumor

Pharmacodynamics

Cyclophosphamide is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands – directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result – disruption of DNA function and cell death.

Mechanism of Action

Alkylating agents work by three different mechanisms:

1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA,

2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations.

Oxabel

March 15, 2024Productsclarity-admin

Oxabel

(Oxaliplatin)

Composition:

Each vial contains oxaliplatin (50 mg or 100 mg)

ATC Code

L01XA03 — Oxaliplatin

Structure

Description

Oxaliplatin is a platinum-based chemotherapy drug in the same family as cisplatin and carboplatin. It is typically administered in combination with fluorouracil and leucovorin in a combination known as Folfox for the treatment of colorectal cancer. Compared to cisplatin the two amine groups are replaced by cyclohexyldiamine for improved antitumour activity. The chlorine ligands are replaced by the oxalato bidentate derived from oxalic acid in order to improve water solubility.

Indication

Associated Conditions

Advanced Colorectal Cancer
Advanced Ovarian Cancer
Advanced Pancreatic Cancer
Chronic Lymphocytic Leukemia (CLL) – Refractory
Colon Cancer Stage III
Esophageal Cancers
Malignant Neoplasm of Stomach
Advanced biliary adenocarcinoma
Refractory Neuroendocrine Tumour
Refractory Non-Hodgkin’s lymphoma
Refractory Testicular cancer

Pharmacodynamics

Oxaliplatin selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of Oxaliplatin-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed.

Mechanism of Action

Oxaliplatin undergoes nonenzymatic conversion to active derivatives via displacement of the labile oxalate ligand. Several transient reactive species are formed, including monoaquo and diaquo DACH platinum, which covalently bind with macromolecules. After activation, oxaliplatin binds preferentially to the guanine and cytosine moieties of DNA, leading to cross-linking of DNA, thus inhibiting DNA synthesis and transcription. Cytotoxicity is cell-cycle nonspecific.

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Repitant

March 15, 2024Productsclarity-admin

Repitant

(Aprepitant)

Composition:

each capsule contains aprepitant – 125mg and 80mg.

ATC Code

A04AD12 — Aprepitant

Structure

Description

Aprepitant, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).

Indication

Pharmacodynamics

Mechanism of Action

Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis.

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Riprone

March 15, 2024Productsclarity-admin

Riprone

(Deferapirone)

Composition:

Each film coated tablet contains Deferiprone 500mg

ATC Code

V03AC02 — Deferiprone

Structure

Description

Deferiprone is an oral iron chelator used as a second line agent in thalassemia syndromes when iron overload from blood transfusions occurs. Thalassemias are a type of hereditary anaemia due a defect in the production of hemoglobin. As a result, erythropoiesis, the production of new red blood cells, is impaired.

Indication

Associated Conditions

Mechanism of Action

Deferiprone is an iron chelator that binds to ferric ions (iron III) and forms a 3:1 (deferiprone:iron) stable complex and is then eliminated in the urine. Deferiprone is more selective for iron in which other metals such as zinc, copper, and aluminum have a lower affinity for deferiprone.

Product Information

Decarb

March 15, 2024Productsclarity-admin

Decarb

(Decarbazine)

Composition:

Each vial contains Decarbazine 200 mg

ATC Code

L01AX04 — Dacarbazine

Structure

Description

Bicalutamide is an oral non-steroidal anti-androgen for prostate cancer. It is comprised of a racemic mixture that is a 50:50 composition of the (R)-bicalutamide and (S)-bicalutamide enantionmers. Bicalutamide binds to the androgen receptor.

Indication

Associated Conditions

Pharmacodynamics

Bicalutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Bicalutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Bicalutamide blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue. Prostate cancer is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen monotherapy has not consistently been shown to be equivalent to castration.

Mechanism of Action

Bicalutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue.