Pharmacologic Side Effects

Side effects typically seen when opioids are used for PCA include sedation, pruritus, and gastrointestinal problems (nausea, vomiting). The incidence of these side effects, however, is not significantly increased during PCA versus more traditional methods of opioid administration such as intermittent intramuscular dosing.18 Respiratory depression is another common side effect of opioid use, but again, there is no increased incidence of this problem when appropriate amounts 

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The answer is c. (Hardman, pp 414-4163) Unwanted pharmacologic side effects produced by phenothiazine antipsychotic drugs (e.g., perphenazine) include Parkinson-like syndrome, akathisia, dystonias, galactorrhea, amenorrhea, and infertility. These side effects are due to the ability of these agents to block dopamine receptors. The phenothiazines also block muscarinic and a-adrenergic receptors, which are responsible for other effects. 

Used for malaria chemoprophylaxis and treatment the dihydrofolate reductase inhibitors do not cause pharmacological side-effects in the host. In the higher dose used for toxoplasmosis macrocytic anaemia and other adverse effects may occur. 

Anesthetized rats are used for testing the side effect potential of a candidate compound on intermediary metabolism in liver, muscle and adipose tissue with subsequent effects on metabolic blood parameters (e.g. glucose, lactate, free fatty acids, triglycerides) and insulin. The use of anesthetized rats represents more a principal assessment of the pharmacological side effect potential since the candidate compound must be administered intravenously or intraperitoneally (enteral/intestinal administration should be avoided due to the anesthesia-induced decrease in intestinal motility with subsequent impairment of enteral absorption), compared to the study in conscious rats in which the candidate compound can be studied after oral administration, which in most cases represents the clinical route of administration for small molecular drugs. 

Pantelis C, Hindler CG, Taylor JC. Use and abuse of khat (Catha edulis) a review of the distribution, pharmacology, side effects and a description of psychosis attributed to khat chewing. Psychol Med 1989 19(3) 657-68. 

Pharmacologic side effect Dry mouth from antihistamine Mild, not serious... 

Secondary pharmacologic side effect Candidiasis from oral antibiotics Moderate level of seriousness (but could be severe and life-threatening in immunocompromised patients)... 

In general, spontaneous case reports describe Type B reactions (rare, serious, allergic) rather than pharmacological side effects (Type A) detected in clinical trials. 

Most drugs used in human therapy possess more than one active principle and display major and/or minor actions, thus delivering one or several pharmacological side effects in addition to their main activity. 

Phase I. This involves general testing for human pharmacology in healthy volunteers, ie, safe-dose adjustment deterrnination of absorption, metabohsm, and excretion patterns and monitoring for side effects. Usually fewer than 10 test subjects ate involved. 

Po adrninistered nifedipine is almost completely absorbed. The onset of action is 20 min and peak effects occur at 1—2 h. The principal route of elimination is through hepatic metaboHsm by oxidation to hydroxycarboxyHc acid and the corresponding lactone. These metaboHtes are pharmacologically inactive. Almost 70—80% of dmg is eliminated in the urine during the first 24 h. About 15% is excreted in the feces. The elimination half-life of nifedipine is about 1—2.5 h (1,98,99). Frequency of occurrence of side effects in patients is about 17% with about 5% requiring discontinuation of therapy (1,98,99). 

Except for the addiction HabiUty of some of the narcotic antitussives, side effects for most of the centrally acting compounds are relatively few and mild at therapeutic doses. QuaUtative comparisons of both side effects and pharmacological profiles have been summarized for many of the compounds described above (97). 

The anxiolytic agent buspirone (131) is notable for the fact that it does not interact with the receptor for the benzodiazepines. This difference in biochemical pharmacology is reflected in the fact that buspirone (131) seems to be devoid of some of the characteristic benzodiazepine side effects. The spiran function is apparently not required for anxiolytic activity. Alkylation of 3,3-dimethylglutarimide with dichlorobutane in the presence of strong base yields the intermedi-... 

The separation of enantiomers is a very important topic to the pharmaceutical industry. It is well recognized that the biological activities and bioavailabilities of enantiomers often differ [1]. To further complicate matters, the pharmacokinetic profile of the racemate is often not just the sum of the profiles of the individual enantiomers. In many cases, one enantiomer has the desired pharmacological activity, whereas the other enantiomer may be responsible for undesirable side-effects. What often gets lost however is the fact that, in some cases, one enantiomer may be inert and, in many cases, both enantiomers may have therapeutic value, though not for the same disease state. It is also possible for one enantiomer to mediate the harmful effects of the other enantiomer. For instance, in the case of indacrinone, one enantiomer is a diuretic but causes uric acid retention, whereas the other enantiomer causes uric acid elimination. Thus, administration of a mixture of enantiomers, although not necessarily racemic, may have therapeutic value. 

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