Second generation drugs

At therapeutic doses, the first- and second-generation antihistamines are equilibrium-competitive inhibitors of Hi-receptor-mediated responses. Certain second-generation drugs are noncompetitive inhibitors at high concentrations. Both first- and second-generation compounds have negligible abilities to block the H2-, H3-, or H4-receptors. The therapeutic effectiveness of these... 

All quinolones interact with multivalent cations, forming chelation complexes resulting in reduced absorption. Major offenders are antacids vitamins containing calcium and iron can also be problematic. All fluoroquinolones interact with warfarin, didanosine (ddi), and phenytoin, resulting in decreased absorption or metabolism. Ciprofloxacin and other second-generation drugs interact with theophylline by decreasing its clearance, which leads to theophylline toxicity. 

Clozapine Generaiiy considered the prototype for other second-generation drugs but is... 

The second-generation drugs are aiso readiiy absorbed. Quetiapine and ziprasidone have short eiimination haif-iives (<10 hours) but the others have half-lives in the region of 20-30 hours. Active metaboiites generaiiy do not contribute significantly to the action of these drugs. 

Cephalexin Oral, first-generation drug, used for treating skin and soft tissue infections and urinary tract infections Cefuroxime Oral and intravenous, second generation drug, improved activity versus Pneumococcus and Haemophilus influenzae... 

Cefotetan, cefoxitin Intravenous, second-generation drugs, activity versus Bacteroides fragilis allows for use in abdominal/pelvic infections... 

In fact, the very recent 195Pt NMR results of Bancroft et al. (41) indicate that, in agreement with Miller and House (36c), most likely [cis-Pt(NH3)2Cl(H20)]+ is the predominant species that reacts with biomolecules (at least with DNA). Other Pt amine compounds that are antitumor active have different kinetics of the hydrolysis reactions, and usually react much slower. The second-generation drug CBDCA (Fig. 2) is known to hydrolyze (in a 1 mAf solution) with a half-life at 37°C of a few days (41a) (compared to only 1 hour for cis-Pt). 

The minor perturbation of the DNA structure caused by cis-platin may well not be detected in a cell which has a deficiency in the repair mechanism, whereas a normal cell might have a more selective repair mechanism. Whether this is the mechanism of action of the platinum anticancer drugs still has to be established, but it is the first model which satisfactorily accounts for all the known chemical and structural restraints. In addition, it suggests further modeling experiments with the more effective second generation drugs. 

In the past, tricyclic drugs such as amitriptyline and nortriptyline were the most commonly used antidepressants and were the standard against which other antidepressants were measured.30 The use of tricyclic drugs as the initial treatment of depression has diminished somewhat in favor of some of the newer second-generation drugs, which may have more favorable side-effect profiles. Tricyclic agents, nonetheless, remain an important component in the management of depressive disorders, especially in more severe forms of depression that fail to respond to other antidepressants.6,53... 

The term antihistamine, without a modifying adjective, refers to the classic Hi receptor blockers. These compounds do not influence the formation or release of histamine, but rather they competitively block the receptor-mediated response of a target tissue. [Note This contrasts with the action of cromolyn (see p. 220), which inhibits the release of histamine from mast cells and is useful in the treatment of asthma.] The H receptor blockers can be divided into first- and second generation drugs.(Figure 40.5). The first generation drugs are still widely used because they are effective and inexpensive. 

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