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LEUCOVORIN CALCIUM INJECTION Faulding Citrovorum Factor Folic Acid Derivative Action And Clinical Pharmacology: Leucovorin is a reduced form of folic acid, which is readily converted to other reduced folic acid derivatives (e.g., tetra-hydrofolate). Because it does not require reduction by dihydrofolate reductase as does folic acid, leucovorin is not affected by blockages of this enzyme by folic acid antagonists (dihydrofolate reductase inhibitors). This allows purine and thymidine synthesis, and thus…

LEUSTATIN® Janssen-Ortho Cladribine Antineoplastic – Chemotherapeutic Agent Warning: Cladribine should be administered under the supervision of a qualified physician experienced in the use of antineoplastic therapy. Suppression of bone marrow function should be anticipated. This is usually reversible and appears to be dose-dependent. Significant and prolonged lymphopenia has been noted. Serious neurological toxicity (including irreversible paraparesis and quadriparesis) has been reported in patients who received cladribine injection by continuous infusion…

LEVAQUIN® Janssen-Ortho Levofloxacin Antibacterial Action And Clinical Pharmacology: Levofloxacin is a synthetic broad spectrum antibacterial agent for oral and i.v. administration. Levofloxacin is the l-isomer of the racemate, ofloxacin, a quinolone antibacterial agent. The antibacterial activity of ofloxacin resides primarily in the l-isomer. The mechanism of action of levofloxacin and other quinolone antibacterials involves inhibition of DNA gyrase (bacterial topoisomerase II), an enzyme required for DNA replication, transcription, repair and…

LECTOPAM® Roche Bromazepam Anxiolytic – Sedative Action And Clinical Pharmacology: Bromazepam is a benzodiazepine with anxiolytic and sedative properties which are of value in the symptomatic relief of pathological anxiety in psychoneurotic patients. The absolute bioavailability of unchanged, orally administered bromazepam is 60%, and peak blood levels are achieved within 2 hours after administration. On average, 70% of bromazepam is bound to plasma proteins. Bromazepam is metabolized in the liver,…

LEDERLE LEUCOVORIN® CALCIUM Wyeth-Ayerst Citrovorum Factor Folic Acid Derivative Action And Clinical Pharmacology: Lederle Leucovorin Calcium (calcium folinate), the calcium salt of folinic acid (citrovorum factor), is a mixture of the diastereoisomers of the 5-formyl derivative of tetrahydrofolic acid. The biologically active compound of the mixture is the (-)-L-isomer. It is a metabolite of folic acid and an essential coenzyme for nucleic acid synthesis. Leucovorin is a reduced form of…

exoLERITINE® Injection LERITINE® Tablets Frosst Anileridine Phosphate Anileridine HCl Opioid Analgesic Action And Clinical Pharmacology: Anileridine, a synthetic opioid, is a strong analgesic. The chief pharmacologic action is exerted on the CNS. The analgesic effects usually are prompt in onset either orally or parenterally (approximately within 15 minutes). Duration of action is about 2 or 3 hours. Respiratory depression, when it occurs, is of shorter duration than that seen with…

LESCOL® Novartis Pharmaceuticals Fluvastatin Sodium Lipid Metabolism Regulator Action And Clinical Pharmacology: Fluvastatin is a fully synthetic HMG-CoA reductase inhibitor and is hydrophilic. Fluvastatin is a racemate of two erythro enantiomers of which one exerts the pharmacological activity. Fluvastatin is a competitive inhibitor of HMG-CoA reductase, which is responsible for the conversion of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, a precursor of sterols, including cholesterol. The inhibition of cholesterol biosynthesis reduces…

LANVIS® Glaxo Wellcome Thioguanine Antileukemic Agent Action And Clinical Pharmacology: Thioguanine is a close relative of mercaptopurine and like the latter is an antimetabolite which blocks purine metabolism. It causes depletion of human bone marrow producing neutropenia, reticulopenia, anemia, thrombocytopenia, and prolongation of clotting time. The protracted but reversible aplasia of bone marrow closely resembles the effects of ionizing radiations. In man, thioguanine is extensively converted to 2-amino-6-methyl-mercaptopurine which is…

LARIAM® Roche Mefloquine HCl Antimalarial Agent Action And Clinical Pharmacology: Mefloquine acts on the asexual intraerythrocytic forms of the human malaria parasites: P. falciparum, P. vivax, P. malariae and P. ovale. Mefloquine is also effective against malaria parasites resistant to other antimalarials such as chloroquine, proguanil, pyrimethamine and pyrimethamine-sulfonamide combinations. Resistance to P. falciparum to mefloquine has been reported, mainly in parts of South-East Asia. Cross-resistance between mefloquine and halofantrine…

LASIX® SPECIAL Hoechst Marion Roussel Furosemide Diuretic Action And Clinical Pharmacology: Animal experiments using stop-flow and micropuncture techniques have demonstrated that furosemide inhibits sodium reabsorption in the ascending limb of Henle’s loop as well as in both proximal and distal tubules. The action of furosemide on the distal tubule is independent of any inhibitory effect on carbonic anhydrase or aldosterone. The diuretic effect of furosemide is exerted even when glomerular…