General information Defibrotide is a polydeoxyribonucleotide extracted from mammalian organ [ ]. Its antithrombotic activity is partly ascribed to enhancement of eicosanoid metabolism, in particular increased release of prostacyclin, with ensuing vasodilatation and inhibition of platelet aggregation. An additional mechanism is activation of the fibrinolytic system, primarily increased activation of tissue plasminogen in the vessel wall. The antithrombotic potential of defibrotide has been reported in patients…

General information Deferoxamine is a polyhydroxamine acid with specific affinity for iron and, less strongly, aluminium. It is a naturally occurring siderophore produced by Streptomyces pilosus. Uses Deferoxamine is used in the treatment of acute iron poisoning and in iron storage diseases, notably beta-thalassemia [ ]. The usual regimen is 40 mg/kg/day as a subcutaneous infusion over 10–12 hours, starting at an early age (3 years).…

General information Deferiprone is an alpha-ketohydroxypyridine compound with metal-chelating properties [ ]. It is absorbed within minutes after oral administration and reaches maximum blood concentrations within 1 hour. It has a half-life of 1–2 hours, and is almost completely undetectable in blood within 5–7 hours after a single dose. Deferiprone is mostly metabolized to a glucuronide conjugate that reaches maximum blood concentrations within 1.0–1.5 hours. Deferiprone,…

General information Deferasirox (ICL670), a hydroxyphenyltriazole derivative, is a tridentate selective iron chelator and an N-substituted bis-hydroxyphenyltriazole compound for oral use, available as 125, 250, and 500 mg tablets and administered in a daily dose of 20–50 mg It is rapidly absorbed (about 70%), highly bound to albumin, has a plasma half-life of 11–19 hours, and probably undergoes enterohepatic recirculation [ ]. Two molecules of deferasirox…

General information Decitabine (5-aza-2′-deoxycytidine) is structurally very similar to azacitidine [ ]. Both drugs have promising activity against acute myeloblastic leukemia and myelodysplastic syndrome. In addition, decitabine has significant activity against chronic myeloid leukemia. It is rapidly metabolized in the liver by cytidine deaminase, which explains its short half-life of 8–30 minutes. In an intravenous dose of 100 mg/m 2 over 6 hours every 12 hours…

General information Decamethonium, a depolarizing neuromuscular blocker, is little used nowadays. A dose of 3 mg provides adequate relaxation for intra-abdominal surgery for about 15 minutes, supplements being required at intervals of 10–30 minutes. It is not as rapid in onset of action as suxamethonium. It is not hydrolysed by plasma cholinesterase, but is eliminated by the kidneys [ ]. Tachyphylaxis occurs and a phase II…

General information Dasatinib (BMS-354825), a thiazole carboximide derivative, is structurally related to imatinib. It targets src kinase and imatinib-resistant bcr–abl kinase and has impressive activity in patients with chronic myeloid leukemia or Philadelphia chromosome-positive acute lymphoblastic leukemia [ , ]. Although dasatinib has been approved for these indications in a dosage of 70 mg bd, the search for the optimal dose regimen continues [ ]. Preliminary…

General information Daptomycin is a novel lipopeptide antibiotic, an inhibitor of lipoteichoic acid synthesis, with potent bactericidal activity against most clinically important Gram-positive bacteria, including resistant strains [ , ], such as meticillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci and was the first inhibitor of lipoteichoic acid synthesis. Daptomycin was initially developed in the late 1980s and early 1990s [ ] but was ultimately shelved owing to…

General information Dapsone is 4,4-diaminodiphenylsulfone (DDS, avlosulfone, disulfone) [ ]. It is a bacteriostatic antileprosy drug with a sulfonamide-like structure. The dosage should be 50–100 mg/day in adults [ ]. In children aged 3–5 years, the dosage should be reduced according to weight to, for example, 25 mg/day [ ]. Studies of patients with borderline leprosy have suggested that dapsone has mild immunosuppressive effects [ ].…

General information Dantrolene, a hydantoin derivative, is well established in clinical practice, being of greatest value for the reduction of clonus and involuntary muscle spasms [ , ]. The recommended oral doses for the treatment of spastic conditions are 75–400 mg Dantrolene [ , ] is the agent of choice for treatment of malignant hyperthermia and greatly reduces the mortality to under 10% if given in…

General information Danazol is a weak androgen and can thus exert the adverse effects of androgens, but because it inhibits LH and FSH secretion it can also elicit menopausal-like symptoms. However, from time to time it has other types of adverse effect. It has been used with some success in the management of pelvic pain associated with endometriosis [ ], heavy menstrual bleeding [ ], and…

General information Danaparoid is a low molecular heparinoid consisting of a mixture of sulfated glycosaminoglycans (heparan, dermatan, and chondroitin sulfates). It has an antithrombotic effect via antithrombin III-mediated inhibition of factor Xa and to a lesser extent through inhibition of factor IIa. The ratio of antifactor Xa to antifactor IIa is over 20. Danaparoid is as effective as heparins in inhibiting the formation of thrombi. Its…

General information Dalbavancin (BI 397) is a semi-synthetic derivative of A40926, a glycopeptide with a structure related to that of teicoplanin [ , ]. Dalbavancin is more active against Streptococcus pneumoniae than conventional glycopeptides are, and its activity against Staphylococcus aureus is also substantially better. However, it is not more active than teicoplanin against enterococci harboring the VanA phenotype of resistance to glycopeptides. Dalbavancin is also…

See also Cytotoxic and immunosuppressant drugs General information Dactinomycin (actinomycin D) is used to treat cancers in children, in particular Wilms’ tumor. It has similar adverse effects to doxorubicin. You’re Reading a Preview Become a Clinical Tree membership for Full access and enjoy Unlimited articles Become membership If you are a member. Log in here

See also Monoclonal antibodies General information Daclizumab, a humanized antibody directed against the alfa chain of the interleukin-2 receptor, has been used for initial immunosuppression in transplant patients. In a phase III trial in 275 patients who received ciclosporin, glucocorticoids, and daclizumab or placebo, there were no specific adverse effects associated with daclizumab [ ]. In particular, the cytokine-release syndrome did not occur, and there was…

See also Cytotoxic and immunosuppressant drugs General information Dacarbazine is converted to an active metabolite that is thought to be an alkylating agent. It has been used to treat metastatic melanoma and, in combination regimens, soft-tissue sarcomas and Hodgkin’s disease. Temozolomide is structurally related to dacarbazine and is thought to act via the same active metabolite. It has been used to treat malignant gliomas and malignant…

General information Dabigatran etexilate is a prodrug of dabigatran, a specific, competitive, reversible inhibitor of thrombin. Dabigatran etexilate is rapidly absorbed after oral administration and converted to dabigatran. Its half-life is about 8 hours after a single dose and 14–17 hours after multiple doses. It is cleared renally. Its pharmacology has been reviewed [ , ]. Drug studies Comparative studies You’re Reading a Preview Become a…

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See also Alkylating cytostatic agents—nitrosoureas and N -lost derivatives ; Platinum-containing cytostatic drugs General information Cytotoxic drugs generally have both anticancer and immunosuppressive properties, while immunosuppressant drugs have more specific immunosuppressive effects, although this is a somewhat arbitrary distinction. Monoclonal antibodies and corticosteroids are not included in the following list. A. Cytotoxic drugs 1. Alkylating drugs Nitrosoureas : carmustine (BCNU), lomustine (CCNU), nimustine (ACNU), streptozocin. N-lost…

See also Cytotoxic and immunosuppressant drugs General information Cytarabine is a pyrimidine nucleoside that is used to treat acute myelogenous leukemia and lymphocytic leukemias. It is activated intracellularly by deoxycytidine kinase to phosphorylated nucleotides that interfere with DNA synthesis in the S phase of the cell, and is rapidly deaminated intracellularly to the inactive metabolite uracil arabinoside. Organs and systems Respiratory Two cases of respiratory failure…