Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effect of high thoracic epidural anaesthesia with intermittent epidural bolus injections of bupivacaine (2.5 or 5 mg ml-1) was studied in 28 patients with unstable angina pectoris. The majority of the patients had a history of previous acute myocardial infarction(s) and/or angina pectoris and severe coronary artery disease. All patients were treated with nitroglycerin infusion for greater than 24 h and were included in the study if they had chest pain, not caused by acute myocardial infarction, at bed rest or recurrent anginal pain at rest greater than 2 days after infarction. 4.4 +/- 0.3 ml of bupivacaine induced a blockade of the upper seven sympathetic segments (Th1-7) for 98 +/- 9 min. Heart rate decreased significantly from 70 +/- 3 to 64 +/- 3 beats min-1 while blood pressure was unaffected by thoracic epidural anaesthesia. In 27 patients (96%) the anaesthesia induced complete analgesia. Nitroglycerin infusion was discontinued definitely within 3 h in 26 patients (93%) and pain was thereafter controlled by means of thoracic epidural anaesthesia as the sole treatment in 23 patients (82%) and as the major treatment in 25 patients (89%). Twenty-one patients (75%) were fully mobilized and stabilized. Treatment with thoracic epidural anaesthesia lasted for 6.0 +/- 1.1 days. The number of daily epidural injections decreased significantly with time from 2.7 +/- 0.3 the first day to 0.9 +/- 0.3 the fourth day (P less than 0.01, n = 19). Two patients developed acute myocardial infarction during the anaesthesia treatment period, and one of these patients died.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Thoracic epidural anaesthesia in patients with unstable angina pectoris. 275 7

The effects on the sphincter of Oddi of intravenous administration of dipyrone, 2.5 g; tramadol, 50 mg; indomethacin, 75 mg; N-butylscopolamine, 20 mg; and nitroglycerin, 1 mg, in comparison to physiological saline were assessed in a single-blind study in 36 patients hospitalized with upper abdominal pain. Basal sphincter pressure and sphincter motility were measured for a 5-min period after treatment by endoscopic manometry. Nitroglycerin and dipyrone both caused a significant fall in basal sphincter pressure, while N-butylscopolamine and nitroglycerin produced a significant decrease in contraction frequency. Therefore, dipyrone, in contrast to tramadol and indomethacin, exhibits spasmolytic activity in addition to analgesia in biliary pain.
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PMID:Influence of spasmolytic analgesics on motility of sphincter of Oddi. 879

Nitroglycerin is administered intravenously in acute obstetric emergencies to relax the uterus. However, complications (eg, hypotension, acute uterine bleeding) are frequent, which prompted a search for alternative routes of administration. We hypothesized that the sublingual administration of nitroglycerin would reduce uterine tone and contractility with few complications. Intrauterine pressure was measured in 12 women who were actively laboring (>4 cm dilatation, regular contractions) with epidural analgesia and who were alert and responsive throughout the study. In a double-blind fashion, subjects were randomized to receive either placebo or sublingual nitroglycerin (3 doses, 800 microg each) 10 minutes apart. The obstetric anesthesiologist continuously monitored maternal blood pressure and fetal heart rate. Cervical dilatation was assessed at the beginning and the end of the protocol. The area under the intrauterine pressure curve (integral) was used to estimate uterine contractility. Intrauterine pressure was analyzed before the randomization code was broken. Nitroglycerin did not alter the intrauterine pressure integral after the first dose (placebo, 3147 mm Hg x s [95% CI, 2206-4088] vs nitroglycerin, 4146 mm Hg x s [95% CI, 2451-5841]; P =.22), second dose (placebo, 3123 mm Hg x s [95% CI, 2447-3799] vs nitroglycerin, 3611 mm Hg x s [95% CI, 2723-4499]; P =.28), or third dose (placebo, 3303 mm Hg x s [95% CI, 2616-3990] vs nitroglycerin, 3810 mm Hg x s [95% CI, 2306-5314]; P =.45). Cervical dilation, basal uterine tone, duration and frequency of uterine contractions, or fetal heart rhythm remained unaffected. Maternal mean arterial pressure decreased significantly after nitroglycerin was administered. All women were delivered vaginally without intervention. Three doses of sublingual nitroglycerin (800 microg per dose) reduce neither uterine activity nor tone, despite lowering maternal blood pressure. If a clinical option, sublingual nitroglycerin will require a higher dose, which would place mother and fetus at risk for complication.
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PMID:Effects of sublingual nitroglycerin on human uterine contractility during the active phase of labor. 1211 17

Oral mucosal drug delivery is an alternative method of systemic drug delivery that offers several advantages over both injectable and enteral methods. Because the oral mucosa is highly vascularised, drugs that are absorbed through the oral mucosa directly enter the systemic circulation, bypassing the gastrointestinal tract and first-pass metabolism in the liver. For some drugs, this results in rapid onset of action via a more comfortable and convenient delivery route than the intravenous route. Not all drugs, however, can be administered through the oral mucosa because of the characteristics of the oral mucosa and the physicochemical properties of the drug. Several cardiovascular drugs administered transmucosally have been studied extensively. Nitroglycerin is one of the most common drugs delivered through the oral mucosa. Research on other cardiovascular drugs, such as captopril, verapamil and propafenone, has proven promising. Oral transmucosal delivery of analgesics has received considerable attention. Oral transmucosal fentanyl is designed to deliver rapid analgesia for breakthrough pain, providing patients with a noninvasive, easy to use and nonintimidating option. For analgesics that are used to treat mild to moderate pain, rapid onset has relatively little benefit and oral mucosal delivery is a poor option. Oral mucosal delivery of sedatives such as midazolam, triazolam and etomidate has shown favourable results with clinical advantages over other routes of administration. Oral mucosal delivery of the antinausea drugs scopolamine and prochlorperazine has received some attention, as has oral mucosal delivery of drugs for erectile dysfunction. Oral transmucosal formulations of testosterone and estrogen have been developed. In clinical studies, sublingual testosterone has been shown to result in increases in lean muscle mass and muscle strength, improvement in positive mood parameters, and increases in genital responsiveness in women. Short-term administration of estrogen to menopausal women with cardiovascular disease has been shown to produce coronary and peripheral vasodilation, reduction of vascular resistance and improvement in endothelial function. Studies of sublingual administration of estrogen are needed to clarify the most beneficial regimen. Although many drugs have been evaluated for oral transmucosal delivery, few are commercially available. The clinical need for oral transmucosal delivery of a drug must be high enough to offset the high costs associated with developing this type of product. Drugs considered for oral transmucosal delivery are limited to existing products, and until there is a change in the selection and development process for new drugs, candidates for oral transmucosal delivery will be limited.
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PMID:Oral mucosal drug delivery: clinical pharmacokinetics and therapeutic applications. 1212 58

Nitric oxide (NO) plays an important role in initiation and maintenance of pain, and NO precursor nitroglycerin is able to activate spinal and brain structures involved in nociception. It is also known that acute and chronic stress induce biochemical changes affecting both pain threshold and behaviour, and that the biological pattern of depression can be mimicked in the laboratory using chronic unavoidable stress paradigms (learned helplessness). We, therefore, evaluated the effects of acute and chronic immobilization stress on pain response to nitroglycerin administration in the rat. Pain perception was expressed as the latency of response to a tail-flick test (hot stimulus). Measures were made 1, 2 and 4 h following nitroglycerin (10 mg/kg i.p.) or vehicle. Nitroglycerin caused hyperalgesia after 2 and 4 h (p < 0.05 versus baseline). Acute stress (90 min) induced a clear analgesic state (p < 0.01 versus non-stressed control animals), and nitroglycerin injection was unable to reverse stress-induced analgesia in this setting. By contrast, exposition to chronic immobilization stress (7 days) caused a significant increase in pain response (p < 0.05); in this case, hyperalgesia was shown to be further enhanced by nitroglycerin administration (p < 0.05 versus vehicle). These findings support the view that a condition of chronic stress used in the laboratory to reproduce the biological features of depression can enhance hyperalgesia induced by nitroglycerin administration. These observations may be relevant to pain disorders, and particularly to migraine, since nitroglycerin is able to induce spontaneous-like pain attacks in humans, and an unfavourable migraine outcome (transformation into a chronic daily headache) is associated with chronic stress and comorbid depression.
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PMID:Effects of acute and chronic restraint stress on nitroglycerin-induced hyperalgesia in rats. 1593 4