Arzneimittel Forsch
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Arzneimittel Forsch · Jan 1984
Randomized Controlled Trial Comparative Study Clinical Trial Controlled Clinical TrialEffects of isosorbide dinitrate spray on central hemodynamics. Comparison with sublingual glyceryl trinitrate and isosorbide dinitrate.
Effects of isosorbide dinitrate (ISDN) spray (Iso Mack Spray) on central hemodynamics were determined in comparison to sublingual glyceryl trinitrate (nitroglycerin) and ISDN, paying particular attention to their onset and duration of action. In nine patients with uncomplicated acute myocardial infarction, ISDN spray (2 sprays, 2.5 mg) glyceryl trinitrate (TNG, 0.3 mg) and ordinary ISDN tablet (5 mg) were administered by the single-blind crossover method under hemodynamic monitoring with a Swan-Ganz catheter. Systolic pulmonary artery pressure (s-PA), systolic pressure (s-BP) and heart rate were measured every minute for 10 min, every 5 min for the subsequent 20 min and thereafter every 15 to 30 min up to 120 min. ⋯ ISDN spray had a quick onset of action (2.67 +/- 2.4 min, mean +/- SD) comparable to that of TNG (2.67 +/- 1.00 min), while ISDN spray had a long duration of action (57.4 +/- 42.1 min), which was comparable to that of sublingual ISDN (85.6 +/- 39.5 min, ns) and was significantly longer than that of TNG (11.4 +/- 6.4 min, p less than 0.05). ISDN spray (2.5 mg) showed the same hemodynamic changes as were induced by 0.3 mg TNG or 5 mg ISDN. The results of this study led us to conclude that ISDN spray is a useful agent which induces the abortion of anginal attacks by its quick onset and long duration of action.
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Pain originating in the peripheral nervous system is based on the excitation of nociceptive afferent fibers, which are contained among A-delta- and C-fibers from skin, viscera, joints and muscles. Often, this excitation originates at the peripheral fiber ending, the nociceptor. Nociceptors are excited by strong stimuli, which may eventually become destructive. ⋯ Here, the chronic pain may be sustained by a positive feedback loop via somato-sympathetic reflexes (sympathetic reflex dystrophy). Similar mechanisms of positive feedback also occur in the skeletomotor system, where chronic pain conditions can be sustained by inappropriate muscle tone. In the central nervous system much of the information from the nociceptive afferent fibers is contained in the discharges of multireceptive neurons.(ABSTRACT TRUNCATED AT 250 WORDS)
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Intravenous demand analgesia is introduced as a possible way to optimize the treatment of acute pain. Within certain limits patients are allowed to self-administer small doses of analgesics as often as they need; microprocessors are used to control safe operation and to document individual drug consumption. ⋯ Demand analgesia is described not only as an effective therapeutic concept but also as an interesting tool for pain research (influences on pain perception, comparison of analgesic potencies etc.). It is strongly suggested from the results that treatment of acute pain ought to be more individualized than it is now in routine practice.
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Arzneimittel Forsch · Jan 1984
A quantitative analysis of steric and hydrophobic effects in ribonucleoside diphosphate reductase inhibition by thiosemicarbazones.
Ribonucleoside diphosphate reductase (RDR) inhibitory activity of 2-formylpyridine and 1-formylisoquinoline thiosemicarbazones is quantitatively analysed in relation to a steric parameter (van der Waals volume, VW) and the hydrophobic parameter logP. The activity is found to be significantly correlated with VW and very poorly with logP. On the basis of this, it is inferred that RDR inhibition by thiosemicarbazones is very sensitive to steric effects and is little influenced by the hydrophobic character of the molecules.
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The spinal application of opiates is followed by a long-lasting and strong pain relief. This action is based upon the binding of opiates to specific opiate receptors situated in the substantia gelatinosa of the spinal cord. Two possible approaches exist - intrathecally or epidurally. ⋯ The epidural opiate analgesia has proven good results with few side effects in the treatment of postoperative pain, pain of multiple rib fractures and other thoracic trauma or cancer pain. In obstetrics analgesia by spinal opiates was disappointing. Mode of action, possible side effects and the results of epidural opiates are discussed.