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CEFOTAN® Wyeth-Ayerst Cefotetan Disodium Antibiotic Action And Clinical Pharmacology: Cefotetan disodium is a semisynthetic, beta-lactamase resistant, cephalosporin (cephamycin) antibiotic. In vitro studies indicate that the bactericidal action of cefotetan results from an interference of bacterial cell wall synthesis by inhibiting the cross-linking of peptidoglycan. Studies with 4-labeled cefotetan have shown that on reaching the target penicillin-binding proteins (PBPs) in the inner membrane, the radiolabeled antibiotic binds principally to PBP 3…

CAVERJECT™ Pharmacia & Upjohn Alprostadil Prostaglandin Action And Clinical Pharmacology: Alprostadil is a prostaglandin with various pharmacological actions that include vasodilatation and inhibition of platelet aggregation, inhibition of gastric secretion, stimulation of intestinal smooth muscle and stimulation of uterine smooth muscle. Alprostadil, when given to impotent men by intracavernous injection, induces erections within 5 to 20 minutes after administration. The duration of erection is dose-dependent. The mechanism of penile erection…

CECLOR® Lilly Cefaclor Antibiotic Action And Clinical Pharmacology: Like other b-lactam antibiotics, cefaclor owes its antibacterial activity to its ability to bind to and inhibit the action of certain bacterial cell wall synthetic enzymes, the penicillin-binding proteins. Cefaclor is well absorbed after oral administration to fed and fasted subjects. Following doses of 250 mg, 500 mg and 1 g to fasted subjects, average peak serum levels of approximately 7, 13…

CEDOCARD® SR Pharmascience Isosorbide Dinitrate Antianginal Agent Action And Clinical Pharmacology: The principal action of isosorbide dinitrate is that of all nitrates, the relaxation of vascular smooth muscle. The efficacy of nitrates in alleviating pain in angina pectoris is probably due primarily to reduction in myocardial oxygen demand rather than an increase in myocardial oxygen supply. This effect is thought to be brought about predominantly by a peripheral action. Although…

CARDURA-1™ CARDURA-2™ CARDURA-4™ Astra Doxazosin Mesylate Antihypertensive Agent – Symptomatic Treatment of Benign Prostatic Hyperplasia (BPH) Action And Clinical Pharmacology: The mechanism of action of doxazosin is selective blockade of alpha1 subtype of post-synaptic, post-junctional alpha-adrenergic receptors. Pharmacodynamics: Hypertension: Administration of doxazosin results in a reduction in systemic vascular resistance. In patients with hypertension there is little change in cardiac output. Maximum reductions in blood pressure usually occur 2 to…

CARNITOR® Sigma-Tau Levocarnitine Carnitine Replenisher Action And Clinical Pharmacology: Levocarnitine is a naturally occurring substance required in mammalian energy metabolism. It has been shown to facilitate long-chain fatty acid entry into cellular mitochondria, therefore delivering substrate for oxidation and subsequent energy production. Fatty acids are utilized as an energy substrate in all tissues except the brain. In skeletal and cardiac muscle they serve as major fuel. Primary systemic carnitine deficiency…

CASODEX® Zeneca Bicalutamide Nonsteroidal Antiandrogen Action And Clinical Pharmacology: Bicalutamide is a nonsteroidal antiandrogen, devoid of other endocrine activity. Bicalutamide competitively inhibits the action of androgens by binding to cytosol androgen receptors in target tissue. This inhibition results in regression of prostatic tumors. Bicalutamide is a racemate and the (R)-enantiomer is primarily responsible for the antiandrogenic activity of bicalutamide. Pharmacokinetics : The absorption, distribution, metabolism and excretion of bicalutamide has…

CATAPRES® Boehringer Ingelheim Clonidine HCl Antihypertensive Action And Clinical Pharmacology: Clonidine is an a-adrenergic agonist which also has some a-adrenergic antagonist effects. The antihypertensive effect of clonidine is thought to be due to central a2-adrenergic stimulation, which results in a decreased sympathetic outflow to the heart, kidneys, and peripheral vasculature and thus decreased peripheral vascular resistance, decreased systolic and diastolic blood pressure and decreased heart rate. Renal blood flow and…

CARDIOQUIN® Purdue Frederick Quinidine Polygalacturonate Antiarrhythmic Agent Action And Clinical Pharmacology: Quinidine depresses excitability, conduction velocity and contractility of most cardiac tissues by a direct action on cardiac cells. Indirectly, cardiac tissues will also be affected by the anticholinergic and a-adrenoceptor blocking properties of quinidine. According to Vaughan Williams antiarrhythmic drug classification, quinidine is a Class IA agent. Thus, quinidine reduces the maximal rate of phase 0 depolarization, prolongs repolarization…

CARDIZEM® CARDIZEM® SR CARDIZEM® CD Hoechst Marion Roussel Diltiazem HCl Antianginal Antihypertensive – Antianginal Action And Clinical Pharmacology: Diltiazem is a calcium ion influx inhibitor (calcium entry blocker or calcium ion antagonist). The therapeutic effect of this group of drugs is believed to be related to their specific cellular action of selectively inhibiting transmembrane influx of calcium ions into cardiac muscle and vascular smooth muscle. The contractile processes of these…