Therapeutic uses

Methadone is used as an analgesic for the relief of moderate to severe pain. It is effective in conditions in which the analgesic effect of morphine is desirable, and it exerts a satisfactory antitussive action. 

In adults, a dose of 2.5 to 10 mg is satisfactory for the relief of most forms of pain. This is administered orally every 3 to 4 h. For suppression of nonproductive cough, 1.25 to 2.5 mg orally every 3 h is usually satisfactory. Where oral administration is undesirable, the drug may be administered subcutaneously, but the oral route is almost as effective as its hypodermic injection. It may also be administered intramuscularly, but should not be injected intravenously. 

Dextromoramide tartrate (Pallium ), which is related chemically to methadone, is as effective when administered orally in doses of 5 to 10 mg as when injected. 

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Many antibiotics are unsuitable for therapeutic use, frequently because of their general toxicity or as a result of other drawbacks such as instability, inadequate solubility or malabsorption. 

Radon is still produced for therapeutic use by a few hospitals by pumping it from a radium source and sealing it in minute tubes, called seeds or needles, for application to patient. This... 

The compound shown is diethylstilbestrol (DES) it has a number of therapeutic uses in estrogen replacement therapy DES is not a steroid but can adopt a shape that allows it to mimic estrogens such as estradiol (p 1100) and bind to the same receptor sites Construct molecular models of DES and estradiol that illustrate this similanty in molecular size shape and location of polar groups... 

Description of Method. Fluoxetine, whose structure is shown in Figure 12.31a, is another name for the antidepressant drug Prozac. The determination of fluoxetine and its metabolite norfluoxetine. Figure 12.31 b, in serum is an important part of monitoring its therapeutic use. The analysis is complicated by the complex matrix of serum samples. A solid-phase extraction followed by an HPLC analysis using a fluorescence detector provides the necessary selectivity and detection limits. 

Other furan compounds, best derived from furfural, are of interest although commercial volumes are considerably less than those of furfural, furfuryl alcohol, furan, or tetrahydrofurfuryl alcohol. Some of these compounds are stiU in developmental stages. Apphcations include solvents, resin intermediates, synthetic mbber modifiers, therapeutic uses, as well as general chemical intermediates. 

AHopregnanolone and similar A-ring-reduced pregnanes potentiate GABA effects at these receptors. These steroids mimic the effects of the benzodiazepines, changing chloride ion conductance and producing sedative and hypnotic behavioral effects (276,277). Neuroactive steroids can be therapeutically useful as anticonvulsants, anxiolytics, or anesthetics (qv) (see also Hypnotics, sedatives, anticonvulsants, and anxiolytics). 

Noncontraceptive Uses of Progestins. Progestins have other therapeutic uses aside from contraception. Hormone-dependent tumors and cysts involving reproductive tissues respond to progestins. Megestrol acetate and MPA are the two most commonly used progestins to treat breast cancer... 

The two synthetic steroidal estrogens which have attained the greatest degree of therapeutic use are ethinyl estradiol [57-63-6] (EE) (5) and its 3-methyl ether, mestranol [72-33-3]((5). In contrast to the naturally occurring estrone derivatives, these acetylenic analogues are orally active and are the main estrogenic components of combination oral contraceptives (see Contraceptives) and certain estrogen replacement products. 

Galen, a physician whose views outUved him by about a thousand years, died about 200 AD. He beUeved that mercurials were toxic, and did not use any mercury compound therapeutically. However, as a result of Arabian influence, the therapeutic uses of mercury were slowly recognized by Western Europe. In the thirteenth century mercury ointments were prescribed for treating chronic diseases of the skin. Mercury and its compounds, such as mercurous chloride, mercuric oxide, mercuric chloride, and mercuric sulfide, were used widely from the fifteenth to the nineteenth centuries, and to some extent in the twentieth century. During the first half of the twentieth century, the primary therapeutic uses of mercury included bactericidal preparations, such as mercuric chloride, mercuric oxycyanide, and mercuric oxide and diuretics, such as aryl HgX (Novasural) and mercurated ahyl derivatives (14). 

Initially, it was beheved that the abiUty of xanthines phosphodiesterase (PDF) led to bronchodilation (Fig. 2). One significant flaw in this proposal is that the concentration of theophylline needed to significantly inhibit PDE in vitro is higher than the therapeutically useful semm values (72). It is possible that concentration of theophylline in airways smooth muscle occurs, but there is no support for this idea from tissue distribution studies. Furthermore, other potent PDE inhibitors such as dipyridamole [58-32-2] are not bronchodilators (73). EinaHy, although clinical studies have shown that neither po nor continuous iv theophylline has a direct effect on circulating cycHc AMP levels (74,75), one study has shown that iv theophylline significant potentiates the increase in cycHc AMP levels induced by isoproterenol (74). 

Knowledge of the mechanism of action and investigations on the physico-chemical characteristics of the therapeutically used dalbaheptides has stimulated the transformation of natural antibiotics into new derivatives using both chemical and biosynthetic modification. 

For therapeutic use, riboflavin is produced by chemical synthesis, whereas concentrates for poultry and Hvestock feeds are manufactured by fermentation using microorganisms such as Jishbyagossypii and remothecium ashbyii which have the capacity to synthesi2e large quantities of riboflavin. 

One approach to combating antibiotic resistance caused by P-lactamase is to inhibit the enzyme (see Enzyme inhibition). Effective combinations of enzyme inhibitors with P-lactam antibiotics such as penicillins or cephalosporins, result in a synergistic response, lowering the minimal inhibitory concentration (MIC) by a factor of four or more for each component. However, inhibition of P-lactamases alone is not sufficient. Pharmacokinetics, stability, ability to penetrate bacteria, cost, and other factors are also important in determining whether an inhibitor is suitable for therapeutic use. Almost any class of P-lactam is capable of producing P-lactamase inhibitors. Several reviews have been pubUshed on P-lactamase inhibitors, detection, and properties (8—15). 

Although tyrothricia is too toxic for parenteral therapy, it was formerly sold in the United States as oral lo2enges. Modem tyrothricin formulations are composed of 70—80% tyrocidines and 30—20% linear gramicidins. Tyrocidines are not as active as linear gramicidins and are too toxic for any therapeutic use by themselves. The bactericidal linear gramicidins are used in the United States solely as an ophthalmic solution in combination with polymyxin B sulfate and neomycin sulfate. The linear gramicidin is used in this aqueous product as a substitute for bacitracin, which lacks stabiUty under such conditions. 

It is essential to maintain high, maximal velocities of enzymatic activity for the attainment of optimal therapeutic efficacy. As a general rule, only enzymes whose MichaeHs-Menten constants He between 1—100 ]lM are effective as dmgs (16) because most substrates for therapeutically useful enzymes are present ia body fluids and cells at suhmillimolar concentrations. 

The thermo- and chemolabilc genuine valepotriates arc not present in the usual therapeutically used formulations (infusion, extract, fluid extract, tincture),... 

Although the information is important, especially for the manufacturer of phytophar-maceuticals, it should also interest the pharmacist and doctor which indications, contraindications, side effects, interactions, dosages, manner of use, and effects are, as it were, officially recognized in some cases, where the evidence is insufficient, the Commission E came to the conclusion not to advocate therapeutic use - this, of course, in no way prohibits their use, but the pharmacist in his discussions with his clients will be hesitant in recommending or will inform them of the fact. Since the information regarding the constituents of the drugs in this book is mostly more detailed than in the monographs of the Commission F, as a rule this has been omitted here. 

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