The effects of some nonsteroidal anti-inflammatory drugs on experimental induced gastric ulcers in rats

Batu, Özlem; Erol, Kevser

doi:10.1007/s10787-007-1605-1

Cited by 19 publications

(19 citation statements)

References 27 publications

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“…On the basis of 50% inhibitory concentration values obtained from in vitro and rat studies, it has been claimed that dipyrone might elicit a selective COX-2 inhibition that could explain why use of dipyrone, in contrast to aspirin and other NSAIDs, is not associated with an increased risk of gastrointestinal bleeding [23,24]. Acetaminophen inhibits both COX-1 and COX-2 weakly in vitro.…”

Section: Discussionmentioning

confidence: 99%

Acute Effects of Dipyrone on Renal Function in Patients with Cirrhosis: A Randomized Controlled Trial

Zapater

Llanos

Barquero

et al. 2014

Basic Clin Pharma Tox

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Use of non-steroidal anti-inflammatory drugs in cirrhosis has been associated with impairment of renal function based on its ability to inhibit the renal production of prostaglandins. Renal effects of dipyrone in patients with cirrhosis have not been evaluated. We aimed to assess the renal effect of therapeutic doses of dipyrone used for short periods of time in patients with cirrhosis. Twenty-nine patients with cirrhosis were included in an observer-blind clinical trial. Patients were randomized to receive three times a day oral acetaminophen (500 mg; N = 15) or dipyrone (575 mg; N = 14) for 72 hr. Serum and urine samples were obtained at baseline, 48 and 72 hr, and cystatin C, creatinine, aldosterone, 6-keto-Prostaglandin-F1 alpha and prostaglandin E2 were measured. Cystatin C and creatinine levels remained comparable in patients treated with acetaminophen and dipyrone. Urine and serum prostaglandins concentrations were significantly decreased at 72 hr in patients treated with dipyrone regardless of the status of ascites. One patient with ascites treated with dipyrone required a paracentesis and developed renal insufficiency. We conclude that dipyrone and acetaminophen did not reduce renal function when used for short periods of time (up to 72 hr) in patients with cirrhosis. However, considering that dipyrone lowered renal vasodilator prostaglandins synthesis, acetaminophen appears as the safest choice with respect to kidney function in cirrhosis.Patients with advanced cirrhosis show a hyperdynamic circulation, characterized by an enhanced splanchnic blood flow, arterial vasodilatation and hypervolaemia, together with an increased reabsorption of sodium and water related with a marked activation of neurohormonal vasoconstrictor systems such as the sympathetic nervous and renin-angiotensin systems [1,2]. In fact, angiotensin II reduces renal blood flow and renal excretory function by directly constricting the renal vascular smooth muscle and by facilitating renal sympathetic tone. This detrimental effect can partly be counteracted by renal prostaglandin production through their local vasodilating effects [2,3].Patients with cirrhosis show an increased production of prostaglandin E2 (PGE2) in the medullary and juxtamedullary vessels of kidney that has been associated with relative

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Section: Discussionmentioning

confidence: 99%

Acute Effects of Dipyrone on Renal Function in Patients with Cirrhosis: A Randomized Controlled Trial

Zapater

Llanos

Barquero

et al. 2014

Basic Clin Pharma Tox

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“…Berenguer et al (2002) did not demonstrate any effect of multiple administration of metamizole on experimentally induced gastric ulcer in rats. Moreover, Batu and Erol (2007) proved experimentally that the drug might have a protective effect against some types of gastric ulcers. They demonstrated that metamizole decreased the ulcer index of rats with histamine-and diethyldithiocarbamate-induced gastric ulcer, but it did not change the ulcer index of rats with stress-induced gastric ulcer.…”

Section: Side Effectsmentioning

confidence: 99%

“…Their results suggest that the common factor engaged in the protective effect of the drug could be its ability to increase synthesis and/or release of gastric mucus. In addition, some of the protective effect of metamizole may be paradoxically due to its ability to increase the gastric PGE 2 content (Batu and Erol 2007). Thus, regarding the influence on the digestive tract, metamizole seems to be much safer than NSAIDs.…”

Section: Side Effectsmentioning

confidence: 99%

Pharmacological characteristics of metamizole

Jasiecka¹,

Maślanka²,

Jaroszewski³

2014

Polish Journal of Veterinary Sciences

129

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Metamizole (dipyrone) is a popular analgetic, non-opioid drug, commonly used in human and veterinary medicine. In some cases, this agent is still incorrectly classified as a non-steroidal anti-inflammatory drug (NSAID). Metamizole is a pro-drug, which spontaneously breaks down after oral administration to structurally related pyrazolone compounds. Apart from its analgesic effect, the medication is an antipyretic and spasmolytic agent. The mechanism responsible for the analgesic effect is a complex one, and most probably rests on the inhibition of a central cyclooxygenase-3 and activation of the opioidergic system and cannabinoid system. Metamizole can block both PG-dependent and PG-independent pathways of fever induced by LPS, which suggests that this drug has a profile of antipyretic action distinctly different from that of NSAIDs. The mechanism responsible for the spasmolytic effect of metamizole is associated with the inhibited release of intracellular Ca 2+ as a result of the reduced synthesis of inositol phosphate. Metamizole is predominantly applied in the therapy of pain of different etiology, of spastic conditions, especially affecting the digestive tract, and of fever refractory to other treatments. Co-administration of morphine and metamizole produces superadditive, antinociceptive effects. Metamizole is a relatively safe pharmaceutical preparation although it is not completely free from undesirable effects. Among these side-effects, the most serious one that raises most controversy is the myelotoxic effect. It seems that in the past the risk of metamizole-induced agranulocytosis was exaggerated. Despite the evidence showing no risk of teratogenic and embryotoxic effects, the drug must not be administered to pregnant women, although it is allowed to be given to pregnant and lactating animals. This paper seeks to describe the characteristics of metamizole in the light of current knowledge.

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“…Представляет собой производное пиразолона (Brogden, 1986 . В свете того, что мы знаем сегодня, последняя классифика-ция представляется ошибочной, так как в отличие от НПВС механизм, через который действует мета-мизол, опирается на ингибирование центральной циклооксигеназы-3 (ЦОГ-3), активацию и модуля-цию системы опиоидных нейропептидов и системы каннабиноидов [3,4]. Метамизол является проле-карством, которое спонтанно распадается после перорального введения на структурно родственные соединения пиразолона.…”

Section: ам овечкин 2001unclassified