Drugs to treat inflamation

Nonselective COX Inhibitors:Diclofenac Diclofenac is a phenylacetic acid derivative that is relatively nonselective as a COX inhibitor.Gastrointestinal ulceration may occur less frequently than with some other NSAIDs. A preparation combining diclofenac and misoprostol decreases upper gastrointestinal ulceration but may result in diarrhea. Another combination of diclofenac and omeprazole was also effective with respect to the prevention of recurrent bleeding, but renal adverse effects were common in high-risk patients. Diclofenac, 150 mg/d, appears to impair renal blood flow and glomerular filtration rate. Elevation of serum aminotransferases occurs more commonly with this drug than with other NSAIDs.A 0.1% ophthalmic preparation is recommended for prevention of postoperative ophthalmic...

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Posted in: Anti inflamatory drugs

Drugs to treat inflamation

COX-2 Selective Inhibitors: COX-2 selective inhibitors, or coxibs, were developed in an attempt to inhibit prostaglandin synthesis by the COX-2 isozyme induced at sites of inflammation without affecting the action of the constitutively active "housekeeping" COX-1 isozyme found in the gastrointestinal tract, kidneys, and platelets. Coxibs selectively bind to and block the active site of the COX-2 enzyme much more effectively than that of COX-1. COX-2 inhibitors have analgesic, antipyretic, and anti-inflammatory effects similar to those of nonselective NSAIDs but with an approximate halving of gastrointestinal adverse effects. Likewise, COX-2 inhibitors at usual doses have been shown to have no impact on platelet aggregation, which is mediated by thromboxane produced by the COX-1 isozyme....

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Antihypertensive Agents

Introduction: Hypertension is the most common cardiovascular disease. In a survey carried out in 2000, hypertension was found in 28% of American adults. The prevalence varies with age, race, education, and many other variables. According to some studies, 60–80% of both men and women will develop hypertension by age 80. Sustained arterial hypertension damages blood vessels in kidney, heart, and brain and leads to an increased incidence of renal failure, coronary disease, heart failure, and stroke. Effective pharmacologic lowering of blood pressure has been shown to prevent damage to blood vessels and to substantially reduce morbidity and mortality rates. Unfortunately, several surveys indicate that only one third to one half of Americans...

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Posted in: Cardio vascular drugs

Salicylates

Aspirin: Aspirin's long use and availability without prescription diminishes its glamour compared with that of the newer NSAIDs. Aspirin is now rarely used as an anti-inflammatory medication and will be reviewed only in terms of its anti platelets effect (ie, doses of 81–325 mg once daily). Pharmacokinetics:Salicylic acid is a simple organic acid with a pKa of 3.0. Aspirin (acetylsalicylic acid; ASA) has a pKa of 3.5. The salicylates are rapidly absorbed from the stomach and upper small intestine yielding a peak plasma salicylate level within 1–2 hours. Aspirin is absorbed as such and is rapidly hydrolyzed (serum half-life 15 minutes) to acetic acid and salicylate by esterases in tissue and blood. Salicylate is nonlinearly bound to albumin. Alkalinization of the urine increases the...

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Nonsteroidal Anti-Inflammatory Drugs

Introduction: Salicylates and other similar agents used to treat rheumatic disease share the capacity to suppress the signs and symptoms of inflammation. These drugs also exert antipyretic and analgesic effects, but it is their anti-inflammatory properties that make them most useful in the management of disorders in which pain is related to the intensity of the inflammatory process.Since aspirin, the original NSAID, has a number of adverse effects, many other NSAIDs have been developed in attempts to improve upon aspirin's efficacy and decrease its toxicity. Chemistry & Pharmacokinetics The NSAIDs are grouped in several chemical classes. This chemical diversity yields a broad range of pharmacokinetic characteristics. Although there are many differences in the kinetics of NSAIDs,...

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Anatomy of the Autonomic Nervous System

Anatomy of ANS The ANS lends itself to division on anatomic grounds into two major portions: the sympathetic (thoracolumbar) division the parasympathetic (craniosacral) division Both divisions originate in nuclei within the CNS and give rise to preganglionic efferent fibers that exit from the brain stem or spinal cord and terminate in motor ganglia. The sympathetic preganglionic fibers leave the CNS through the thoracic and lumbar spinal nerves. The parasympathetic preganglionic fibers leave the CNS through the cranial nerves (especially the third, seventh, ninth, and tenth) and the third and fourth sacral spinal roots. Most sympathetic preganglionic fibers are short and terminate in ganglia located in the paravertebral chains...

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Therapeutic Strategies

Therapeutic Strategies The treatment of patients with inflammation involves two primary goals: first, the relief of symptoms and the maintenance of function, which are usually the major continuing complaints of the patient second, the slowing or arrest of the tissue-damaging process.  Reduction of inflammation with nonsteroidal anti-inflammatory drugs (NSAIDs) often results in relief of pain for significant periods. Furthermore, most of the nonopioid analgesics (aspirin, etc) have anti-inflammatory effects, so they are appropriate for the treatment of both acute and chronic inflammatory conditions. The glucocorticoids also have powerful anti-inflammatory effects and when first introduced were considered to be the ultimate answer to the treatment of inflammatory arthritis....

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The Immune Response

What is immune response? The immune response occurs when immunologically competent cells are activated in response to foreign organisms or antigenic substances liberated during the acute or chronic inflammatory response. The outcome of the immune response for the host may be beneficial, as when it causes invading organisms to be phagocytosed or neutralized. On the other hand, the outcome may be deleterious if it leads to chronic inflammation without resolution of the underlying injurious process. Chronic inflammation involves the release of a number of mediators that are not prominent in the acute response. One of the most important conditions involving these mediators is rheumatoid arthritis, in which chronic inflammation results in pain and destruction of bone and cartilage that...

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