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Biomedical subjects

T G Kantor

Publications and source records attributed to T G Kantor.

At least 19 recordsLinked to original sources

Current nonsteroidal anti-inflammatory drug applications for rheumatic diseases.

This article reviews recent knowledge of the pharmacology of non-steroidal anti-inflammatory drugs (NSAIDs). Changes in use and perception of safety considerations are discussed. Additionally, the concept that all NSAIDs are both anti-inflammatory and analgesic is introduced, discussing the mechanism for each effect. A glimpse into the future of NSAIDs is presented, including different formulations and the concept of enantiomers and their possible role in future developments.

Aged

The pharmacological control of musculoskeletal pain.

The modern therapy of the pain of inflammatory rheumatic disease and osteoarthritis is based on several advances in molecular biology, which are reviewed in this paper. Inhibition of the ubiquitous enzyme cyclooxygenase by the nonsteroidal anti-inflammatory drugs including the salicylates prevents the production of endoperoxides, which are pro-inflammatory, and prostaglandins E2 and I2, which sensitize peripheral pain receptors. In addition, a fundamental understanding of neural tracts that inhibit the pain signal has introduced the concept of giving low dose tricyclic antidepressants for chronic pain to block the re-uptake of serotonin from the neural cleft of synapses. This amplifies the effect of serotonin and catecholamines, which are neurotransmitters for these inhibitory tracts.

Animals

Current modalities in arthritic diseases.

Little progress has been made in identifying the etiologies of the major rheumatologic diseases, which substantially limits our ability to identify truly disease-modifying treatments. Despite this constraint, major advances in the suppression of the signs and symptoms of these diseases have been made. Second-line drugs such as methotrexate have gained wide acceptance among rheumatologists and may supplant gold as the major therapy for rapidly advancing rheumatoid arthritis. The nonsteroidal anti-inflammatory drugs (NSAIDs), however, remain the first line of treatment for arthritic conditions. In recent years, much has been learned about how the NSAIDs suppress the inflammation and pain of arthritis. Even here, however, several inconsistencies exist with our current understanding. New findings in neurobiology may shed light on some of these puzzling features. Although the number of NSAIDs currently available seems a bit overwhelming, rationale exists for their continued development. Many patients do not have a response to some or all of these agents, with noncompliance because of gastrointestinal intolerance being among the probable causes. New compounds that offer improved safety in this regard are greatly needed.

Acetaminophen

Management of cancer pain with oral controlled-release morphine sulfate.

Morphine sulfate Contin (MSC) is an investigational matrix delivery system for oral morphine sulfate that allows for prolonged blood levels of morphine. Twenty-six patients with inadequately controlled cancer-related pain were examined in an open but controlled study using MSC. Initially, all patients were converted from the prestudy analgesic regimen to an equianalgesic amount of immediate-release morphine sulfate (IRMS) on a q4h dose schedule that was in turn titrated to the level of adequate pain relief. Patients then were switched to MSC q8h and eventually to q12h, starting at doses representing the same total daily amount of morphine that was in the final IRMS dose. Of the 18 patients who completed the study, all achieved satisfactory levels of analgesia on MSC, seven at q8h and 11 at q12h dosing intervals. All patients reported better analgesia while taking MSC compared with their previous regimen. Side effects associated with MSC included sedation and constipation but not nausea or respiratory difficulty. Significant drug tolerance did not develop during a mean follow-up period of four weeks (range, 1-18 weeks). MSC is an effective oral opioid analgesic that allows an increased dose interval without increased side effects or decreased potency. It can improve the quality of life of cancer patients by allowing them to be maintained without frequent dosing or parenteral medication.

Administration, Oral

Use of diclofenac in analgesia.

The inhibition of prostaglandin synthesis by nonsteroidal anti-inflammatory drugs can alleviate the pain and inflammation associated with a variety of disorders. Nonsteroidal anti-inflammatory drugs have a role, therefore, in the treatment of nonrheumatic conditions as well as in the treatment of rheumatic diseases, an area in which these agents have been used and studied more extensively. In clinical conditions marked by acute or chronic pain and inflammation, such as oral surgery, dysmenorrhea, low back pain, renal colic, and biliary colic, as well as in post-traumatic and postoperative conditions, diclofenac sodium, a nonsteroidal anti-inflammatory drug with potent prostaglandin synthetase inhibition, has been shown to be an effective analgesic agent. In the current studies, diclofenac was given orally or by intramuscular injection in doses ranging from 50 to 75 mg daily, or up to 150 mg per day for longer-term use. When compared with placebo, diclofenac provided consistently superior relief of symptoms. Comparisons with other nonsteroidal anti-inflammatory drugs or with opioids, such as pentazocine or Spasmofen, demonstrate that symptom relief with diclofenac was either comparable to or better than that obtained with these agents.

Analgesia

Oral nalbuphine in postpartum pain.

One hundred twenty-one patients with postpartum pain caused by uterine cramp or episiotomy pain were the subjects of a randomized, double-blind, single-dose study of oral nalbuphine (N), 15 mg (N = 39); codeine (C), 60 mg (N = 42); and placebo (N = 40) for analgesia. Observations were made over 6 hr. There were significant differences for sum of pain intensity differences and total pain relief between the active drugs and placebo but not between N and C. Time to onset of analgesia favored N (mean = 0.65 min) over C (mean = 0.74 min), but the analgetic effect of N diminished more rapidly at this dose. Results were the same for both uterine cramp and episiotomy pain. Adverse effects were of the narcotic type and of the same incidence for the two active drugs. Two new parameters for determining analgetic effect are introduced: number of dropouts per dose and number of subjects with zero analgetic effect.

Administration, Oral

Adverse effects of commonly ordered oral narcotics.

Approximately equianalgesic oral doses of codeine, an oxycodone compound resembling Percodan, and pentazocine were compared for adverse effects in a double-blind, randomized study of four doses of each drug given over two days to 247 postsurgical patients with pain. Placebo and parenteral morphine were also treated as negative and positive controls, respectively. Approximately 50 patients each received one of the five drugs. Codeine, pentazocine, and morphine had the same incidence of adverse effects (22 to 28 per cent). One capsule of oxycodone compound was the analgesic equivalent of 12.5 mg morphine with an adverse effect incidence of 4 per cent (placebo 8 per cent). Smoking made no difference in analgesic effect or adverse effects. Analgesics given in the evening intervening between the two days may have affected the analgesic performance of placebo.

Administration, Oral

A study of hospitalized surgical patients on methadone maintenance.

It is possible that admission to hospital of methadone maintenance clients requiring treatment for pain with narcotics may result in an increase in methadone maintenance dose and affect subsequent rehabilitation of the client. The hospital admission itself may modify the subsequent outcome of the client. Fifty clients of a Methadone Maintenance Therapy Program were retrospectively evaluated. Twenty-five had been admitted to the Surgical Service of Bellevue Hospital, New York City, for a variety of conditions and for periods ranging from 2 to 43 days; twenty-five were not admitted to the Hospital. Irrespective of whether or not large amounts of narcotic analgesics had been added to the maintenance methadone, patients were discharged on the same amounts of maintenance methadone as on admission and had eventual courses and outcomes similar to the control group when followed for a mean period of 20 months.

Adult

Ibuprofen.

Ibuprofen was introduced in England in 1967 and in the United States in 1974 as an anti-inflammatory drug in humans. It has weak but definite anti-inflammatory properties similar to those of aspirin, milligram for milligram, but with considerably less adverse effect on the stomach. Ibuprofen is chemically related to fenoprofen and naproxen, but lack of effect for any one in this chemical class of propionic-acid derivatives does not necessarily mean lack of effect for any other in an individual patient. The drug has analgesic properties, probably related to its anti-inflammatory effect. It inhibits prostaglandin synthesis and has no effect on the adrenopituitary axis, making it a nonsteroidal agent. Ibuprofen has been shown to be effective in rheumatoid arthritis and osteoarthritis and is probably effective in ankylosing spondylitis, gout, and Bartter's syndrome.

Analgesics