Therapeutic classes

As a therapeutic class, hypnotics are nonselective CNS depressants that eflcit drowsiness and a natural sleep state from which the individual can be aroused. The effects of hypnotics are generally dose-dependent. 

Castiglioni S, Bagnati R, Calamari D, Fanelli R, Zuccato E (2005) A multiresidue analytical method using solid-phase extraction and high-pressure liquid chromatography tandem mass spectrometry to measure pharmaceuticals of different therapeutic classes in urban waste-waters. J Chromatogr A 1092 206-215... 

Nichols, DE. Differences between the mechanisms of action of MDMA, MBDB, and the classical hallucinogens. Identification of a new therapeutic class Entactogens. J Psychoactive Drugs 18 305-313, 1986. 

A.T. Derivatives of l-(l,3-benxodioxol-5-yl)-2-butanamine Repre sentatives of a novel therapeutic class. J Med Chem 29 2009-2015, 1986. 

Chemindex plus. This database contains 8000 pharmaceutical ingredients linked to 300,000 preparations. Chemindex plus [66] can be interrogated at the national or international level. It covers compounds available in 55 countries recording their brand name, local manufacturer, launch date, therapeutic class, and base forms. This product is commercially available from IMS HEALTH Global Services. 

Adverse effects associated with members of the chemical or therapeutic class. 

Compounds of the same therapeutic class may profoundly differ as to QT prolonging potential in addition, the assessment of the proarrhythmic risk must take into account pharmacokinetic aspects including metabolism, since a very low baseline proarrhythmic risk may become clinically important in case of drug interactions leading to higher than expected plasma levels. 

Other examples of secondary benzamides include the therapeutic class of orthopramides, which are, again, markedly resistant to hydrolysis. Thus, hydrolysis of the amide bond is a minor metabolic pathway in humans for the antiemetic drug metoclopramide (4.76) [49]. Clebopride (4.77), an anti-dopaminergic agent, was found to be hydrolyzed to a limited extent in rabbit liver homogenates and in dogs to 4-amino-5-chloro-2-methoxybenzoic acid (4.78) and to the amine 4.79 [48] [50], Attempts to detect in vivo formation of this metabolite in rats, rabbits, or humans were not successful [50],... 

Another therapeutic class to be briefly discussed is that of the lipid-lowering agents known as fibrates, e.g., clofibrate and fenofibrate (8.5). Here also, the acidic metabolite is the active form clofibrate (an ethyl ester) is rapidly hydrolyzed to clofibric acid by liver carboxylesterases and blood esterases [11], Human metabolic studies of fenofibrate (8.5), the isopropyl ester of fenofibric acid, showed incomplete absorption after oral administration, while hydrolysis of the absorbed fraction was quantitative [12], This was followed by other reactions of biotransformation, mainly glucuronidation of the carboxylic acid group. 

The therapeutic class that uniquely exemplifies lactone prodrugs are the statins, i.e., the cholesterol-lowering agents that act by inhibiting 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase (EC 1.1.1.34). This microsomal enzyme catalyzes conversion of HMG-CoA to mevalonate, an important rate-limiting step in cholesterol biosynthesis. Cholesterol synthesis occurs mainly... 

Bisphosphonates are drugs of great interest in a number of metabolic bone diseases [119]. This therapeutic class comprises bis(phosphonic acids) and, more recently, bis(phosphonic acid) esters. The former are hydrophilic and poorly bioavailable, and they are generally not metabolized. In contrast, bis(phosphonic acid) esters may be more prone to biotransformation, as exemplified with the lead compound known as U-91502 (9.51 in Fig. 9.11). 

Since the pharmacological effects of an NCE depend on its intrinsic properties, the studies should be selected and designed accordingly. General considerations in the selection and design of these studies that assess potential ADRs are to include effects associated (1) to the therapeutic class, (2) with members of a chemical class, (3) to nontarget mediated activities, and (4) to effects observed in previous non-clinical/clinical studies that warrant further investigation. 

Many compounds in the top decile of the returns distribution involve the first mover, or other early entrants, in a new therapeutic class. The family of medicines in a given... 

Therapeutic class (Major Subclasses) Number of Drugs in the Top 200 Total Sales (US billions) Prescriptions (nultions of units sold)... 

Therapeutic classes with three or more leading brand-name drugs in 2003. 

Environmental contamination by pharmaceutical compounds (PhCs) has become an issue of great concern to many countries in recent years. Hence, the European Community has recently funded several projects to quantify their presence in water bodies and wastewaters, to evaluate the removal rates of compounds from major therapeutic classes during conventional and advanced treatments and to assess the risks they pose to the environment. Notable examples of these studies are ... 

VerUcchi et al. [36] found that antibiotics, analgesics/anti-inflammatories and steroid compounds are the therapeutic classes most abundantly administered in Italian hospitals, but consistent consumption of cardiovascular compounds, tranquilizers, anti-neoplastics and anaesthetics was also detected. According to other authors in other localities [32, 41], PhCs detected in the largest amounts in hospital effluents are antibiotics, anti-epUeptics, beta-blockers, Upid regulators and... 

The range of variability of the concentrations of most prevalent compounds detected in hospital effluent, grouped according to their therapeutic class, is reported in Table 3 [8, 23, 42 7] ICMs are included in the list, even though they are more diagnostic than pharmaceutical agents, as they are denoted micropollutants and emerging contaminants. 

Table 3 Concentration ranges of the most abundant PhCs measured in hospital effluent, grouped according to their therapeutic class...

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