Ibuprofen pharmacological properties

Naproxen (Naprosyn) also has pharmacological properties and clinical uses similar to those of ibuprofen. It exhibits approximately equal selectivity for COX-1 and COX-2 and is better tolerated than certain NSAIDs, such as indomethacin. Adverse reactions related to the GI tract occur in about 14% of all patients, and severe GI bleeding has been reported. CNS complaints (headache, dizziness, drowsiness), dermatological effects (pruritus, skin eruptions, echinoses), tinnitus, edema, and dyspnea also occur. 

Davies EF, Avery GS. Ibuprofen a review of its pharmacological properties and therapeutic efficacy in rheumatic disorders. Drugs 1971 2(5) 416-46. 

Frequently one of the enantiomers does not have active pharmacologic properties. In such a case, the drug formulation should not include a chemical moiety that does not have therapeutic value once the separation technique is available and is considered to be economical. In addition to physiological activities, stereospecificity influences the physicochemical properties of drugs. Let s take as an example the enantiomer of ibuprofen compared with the race-mate. The chiral compound has higher aqueous solubility, higher density, and better flowability, but a lower intrinsic dissolution rate. ... 

All compounds of the test dataset are nonsteroidal anti-inflammatory drugs (NSAIDs) and are thus relatively similar in terms of their pharmacological properties (Fig. 18). The compounds are 1, acetylsalicylic acid 2, diclofenac 3, flufe-namic acid 4, flubiprofen 5, ibuprofen 6, indometacin 7, ketoprofen 8, meclofe-namic acid 9, mefenamic acid 10, naproxen 11, piroxicam 12, sulindac sulfide (active metabolite of sulindac) 13, tenoxicam 14, meloxicam 15, cgp 28238 16, DuP-697 17, L-745-337 18, 6-methoxy-2-naphthylacetic acid (active metabolite of nabumeton) 19, NS-389 20, SC 58125. 

Many drug compounds are racemic mixtures of stereoisomers. In most cases, one of the isomers is more pharmacologically active than the other isomer, and each isomer may exhibit different pharmacokinetic properties. Warfarin, propranolol, verapamil, and ibuprofen are aU racemic mixtures of stereoisomers. Some drug interactions inhibit or increase the elimination of only one stereoisomer. The importance of the drug interaction depends on which isomer is affected. Other drugs, such as dextromethorphan, levofloxacin, and dUtiazem, are composed of just one stereoisomer. 

Sesquiterpenes Sesquiterpenes normally contain 15 carbon atoms and can have very complex pharmacological activity. An example of a sesquiterpene, farnesene, is shown in Figure 3. Farnesene is often found in chamomile and rose and many other floral essential oils. Farnesene has significant anti-inflammatory and antiallergy properties and, thus, in the past essential oils containing farnesene were used for the same purposes that aspirin and ibuprofen are used today. 

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