Drugs online research references
Arzneimittelforschung. 1999 Oct;49(10):843-8.
Anti-inflammatory activity of 2-acyl-5(3)-hydroxytetrahydro-1H-pyrazole derivatives.
Zelenin KN, Bezhan IP, Pastushenkov LV, Gromova EG, Lesiovskaja EE, Chakchir BA, Melnikova LF.
Department of Chemistry of Military Medical Academy, St. Petersburg, Russia.
The anti-inflammatory effects of five pyrazolidine derivatives on white mice and laboratory rats were studied using models of thermal aseptic inflammation and inflammation induced by injection of carragenin and histamine, as well as models of "cotton-ball granuloma" and epinephrine (adrenaline)-induced pulmonary edema. These effects were compared with those of the most commonly used non-steroid anti-inflammatory drugs, such as phenylbutazone (CAS 50-33-9) and diclofenac (CAS 15307-79-6). It was found that the pyrazolidine compounds studied induced a pronounced anti-inflammatory effect by inhibiting both the proliferative and exudative phases of inflammation. At the same time, as compared to natural non-steroid anti-inflammatory drugs, these compounds had a lower toxicity and induced neither gastric ulcers nor suppression of hemopoiesis.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10554662&dopt=Abstract
Life Sci. 2000 Jan 21;66(9):791-802.
Antinociceptive properties of the methanolic extract and two triterpenes isolated from Epidendrum Mosenii stems (Orchidaceae).
Ferreira J, Floriani AE, Filho VC, Delle Monache F, Yunes RA, Calixto JB, Santos AR.
Nucleo de Investigacoes Quimico-Farmaceuticas (NIQFAR)/CCS, Universidade do Vale do Itajai, SC, Brazil.
The antinociceptive effect of the methanolic extract (ME) and two triterpenes isolated from E. mosenii (Orchidaceae) has been investigated in chemical and thermal models of nociception in mice. The ME of E. mosenii (0.3-30 mg kg(-1), i.p. or 50-400 mg kg(-1), p.o.) produced dose-related, significant and long-lasting (4 to 6 h) inhibition of acetic acid-induced abdominal constriction, with ID50 values of 3.9 and 137.0 mg kg(-1), respectively. Pholidotin and 24-methylenecycloartenol isolated from E. mosenii (0.1-3.0 mg kg(-1), i.p.) also produced marked and dose-related inhibition of acetic acid-induced pain, with ID50 values of 0.9 and 1.1 mg kg(-1). However, these compounds and the ME were about 3- to 13-fold more potent at the level of ID50 than diclofenac when assessed in acetic acid-induced abdominal constriction. The ME of E. mosenii in the same range of doses produced dose-related inhibition of both phases of formalin-induced licking, with mean ID50 values for the first and the second phases of 0.9, 122.0 mg kg(-1) and 0.7, 258.0 mg kg(-1), respectively by i.p. or p.o. routes. In addition, the ME (0.3-30 mg kg(-1), i.p., or 50-400 mg kg(-1), p.o.) also caused dose-related inhibition of capsaicin-induced neurogenic pain with mean ID50 values of 5.2 and 130.0 mg kg(-1), respectively. Treatment of animals with naloxone (5 mg kg(-1), i.p.) completely reversed the antinociceptive effect caused by morphine (5 mg kg(-1), s.c.) and that caused by ME of E. mosenii (1 mg kg(-1), i.p.) when assessed against either phase of the formalin-induced pain. Furthermore, when assessed in the hot-plate test, ME (100 mg kg(-1), i.p.) and morphine (10 mg kg(-1), s.c.) caused significant increase in response latency. However, ME given daily for to 7 consecutive days did not develop tolerance to itself nor did it induce cross-tolerance to morphine. Taken together these data demonstrate that the ME of E. mosenii elicited pronounced antinociception, when assessed by i.p. or p.o. routes, against several models of pain. Its actions involve, at least in part, an interaction with opioid system, seeming no to be related with a non-specific peripheral or central depressant actions. Finally, the active principle(s) responsible for the antinociceptive action of E. mosenii is likely related to the presence of the triterpenes.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10698354&dopt=Abstract
Arzneimittelforschung. 2000 Mar;50(3):275-80.
Prediction of the efficacy of cutaneously applied nonsteroidal anti-inflammatory drugs from a lipophilic vehicle.
Wenkers BP, Lippold BC.
Institut fur Pharmazeutische Technologie, Heinrich-Heine-Universitat, Dusseldorf, Germany.
The maximum cutaneous fluxes of 12 nonsteroidal anti-inflammatory drugs (NSAIDs), determined in a preceding study from the lipophilic vehicle light mineral oil in vivo on 24 healthy volunteers, were related to data concerning their intrinsic activities. From the multiplication of the relative intrinsic activities with the relative maximum fluxes, both related to indometacin (CAS 53-86-1) as standard, the percutaneous activities result as parameters for the prediction of the efficacy of cutaneous preparations with NSAIDs. According to the results of the calculations, the percutaneous activities of ibuprofen (CAS 15687-27-1) and nabumetone (CAS 42924-53-8) from lipophilic vehicles are remarkable because of their very high maximum fluxes. NSAIDs with still high percutaneous activities are ketoprofen (CAS 22071-15-4), naproxen (CAS 22204-53-1), piroxicam (CAS 36322-90-4) and diclofenac (CAS 15307-86-5). In contrast, the systemically highly effective NSAIDs indometacin and acemetacin (CAS 53164-05-9) show rather low percutaneous activities, when applied in lipophilic vehicles. Especially nabumeton and also tenoxicam (CAS 59804-37-4), both not yet commercially used cutaneously, can be recommended for lipophilic skin preparations.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10758781&dopt=Abstract
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