[The analgesic and antipyretic effects of a non-steroidal anti-inflammatory drug, oxaprozin, in experimental animals].
FUSAO AMANUMAS. OkuyamaSeiichi OrikasaShinichi HashimotoChizuko YamadaT SakagawaYukako TsutsuiY TarumotoH AiharaTsutomu Kameyama
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Abstract:
The analgesic and antipyretic effects of oxaprozin were investigated in comparison with those of indomethacin, ibuprofen, phenylbutazone and aspirin. On the various writhing tests in mice, the analgesic effect of oxaprozin was about 2 to 9 times more potent than those of ibuprofen, phenylbutazone and aspirin. On the other hand, the analgesic and antipyretic effects of oxaprozin in rats were roughly equivalent to those of aspirin, but less effective than those of the other drugs tested. On the urate synovitis test in dogs, only oxaprozin showed a prophylactic effect. Therefore, The effect of oxaprozin in mice and dogs was more potent than ibuprofen, phenylbutazone and aspirin. The metabolic rate of oxaprozin in rats is 3.5 and 7.2 times more rapid than in mice and dogs, respectively, and its blood level in rats is low. Moreover, the biological half-life of oxaprozin is 39 to 43 hr and 49 to 69 hr in dogs and humans, respectively. From these results, it is suggested that oxaprozin is more potent than ibuprofen, phenylbutazone and aspirin, and in clinical use, it is a long acting anti-inflammatory drug.Keywords:
Ibuprofen
Antipyretic
Anti-inflammatory
Tail flick test
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Diclofenac
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Acetaminophen
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Aspirin remains the agent of first choice, but ibuprofen, fenoprofen, naproxen and tolmetin are useful drugs in rheumatoid arthritis. Ibuprofen and fenoprofen are also approved for use in osteoarthritis. Each shares anti-inflammatory, analgesic and antipyretic properties with aspirin, phenylbutazone and indomethacin. The nonsteroidal anti-inflammatory agents have fewer minor side effects than aspirin and fewer major side effects than indomethacin or phenylbutazone. The patient must understand that drugs are but one part of a comprehensive management program.
Ibuprofen
Antipyretic
Anti-inflammatory
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Antipyretic
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Caffeine has been found to potentiate the acute anti-inflammatory activity of aspirin, indomethacin, and phenylbuta-zone, but not the activity of sodium salicy-late or hydrocortisone, in the carrageenan pleurisy or hindlimb models of inflammation in the rat. The mobilization of inflammatory cells was not affected by aspirin in the presence or absence of caffeine.
Carrageenan
Anti-inflammatory
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Analgesic, antipyretic and anti-inflammatory activities of newly synthesized spirobarbitunylphenothiazines viz 10-[7, 11-Di(4-4' dimethoxphenyl)-3-oxo-9-methylaminoimino-2, 4-diazaspiro [5.5] undecane 1, 5 dione] acetylphenothiazine (test drug A) and 10-[7, 11-Di (N.N-dimethylaminophenyl)-3-oxo-9-methylaminoimino-2, 4-diazaspiro [5, 5] undecane-1, 5 dione] acetylphenothiazine (test drug B) have been screened in Swiss mice and Wistar rats. The peripheral analgesic activity of test drugs A and B was investigated by acetic acid induced writhing test in Swiss mice while the central analgesic action was assessed by hot-wire (tail flick test) of the analgesiometer and tail-clip test in Wistar rats. Antipyretic activity was assessed on Brewer's yeast induced pyrexic model while antiinflammatory activity was seen on carrageenan induced hind paw oedema. Analgesic activity was found to be only of peripheral type as there was reduction of 66% in writhing responses by test drugs A and B in dose of 80 mg/kg in mice. No change in the tail flick responses was observed on analgesiometer or by tail clip by both the test drugs. Reduction of 1.5 to 2.0 degrees C in rectal temperature was observed in pyretic rats by test drugs A and B in dose of 80 mg/kg. 80% reduction in paw volume was noted in 80 mg/kg dose of both the test drugs which was comparable to the anti-inflammatory activity of 300 mg/kg, p.o. of phenylbutazone.
Antipyretic
Tail flick test
Carrageenan
Anti-inflammatory
Rectal temperature
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The analgesic and antipyretic effects of oxaprozin were investigated in comparison with those of indomethacin, ibuprofen, phenylbutazone and aspirin. On the various writhing tests in mice, the analgesic effect of oxaprozin was about 2 to 9 times more potent than those of ibuprofen, phenylbutazone and aspirin. On the other hand, the analgesic and antipyretic effects of oxaprozin in rats were roughly equivalent to those of aspirin, but less effective than those of the other drugs tested. On the urate synovitis test in dogs, only oxaprozin showed a prophylactic effect. Therefore, The effect of oxaprozin in mice and dogs was more potent than ibuprofen, phenylbutazone and aspirin. The metabolic rate of oxaprozin in rats is 3.5 and 7.2 times more rapid than in mice and dogs, respectively, and its blood level in rats is low. Moreover, the biological half-life of oxaprozin is 39 to 43 hr and 49 to 69 hr in dogs and humans, respectively. From these results, it is suggested that oxaprozin is more potent than ibuprofen, phenylbutazone and aspirin, and in clinical use, it is a long acting anti-inflammatory drug.
Ibuprofen
Antipyretic
Anti-inflammatory
Tail flick test
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In continuation of our efforts to discover novel nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) as potentially "Safe NSAIDs," we report herein the design, synthesis and evaluation of 21 new NO-NSAIDs of commonly used NSAIDs such as aspirin, diclofenac, naproxen, flurbiprofen, ketoprofen, sulindac, ibuprofen and indomethacin. These prodrugs have NO-releasing disulfide linker attached to a parent NSAID via linkages such as an ester (compounds 9-16), a double ester (compounds 17-24), an imide (compounds 25-30) or an amide (compounds 31-33). Among these NO-NSAIDs, the ester-containing NO-aspirin (9), NO-diclofenac (10), NO-naproxen (11), and the imide-containing NO-aspirin (25), NO-flurbiprofen (27) and NO-ketoprofen (28) have shown promising oral absorption, anti-inflammatory activity and NO-releasing property, and also protected rats from NSAID-induced gastric damage. NO-aspirin compound 25, on further co-evaluation with aspirin at equimolar doses, exhibited comparable dose-dependent pharmacokinetics, inhibition of gastric mucosal prostaglandin E(2) (PGE(2)) synthesis and analgesic properties to those of aspirin, but retained its gastric-sparing properties even after doubling its oral dose. These promising NO-NSAIDs could therefore represent a new class of potentially "Safe NSAIDs" for the treatment of arthritic pain and inflammation.
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Phenacetin
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Ibuprofen
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新規非ステロイド性抗炎症剤EB-382の鎮痛および解熱作用について検討した．EB-382はacetic acid，phenylquinoneおよびacetylcholineの各種起炎剤によるマウスwrithingに対してibuprofenとほぼ同程度の抑制作用を示したが，phenylbutazoneの作用は弱かった．EB-382はラットにおけるRandall-Selitto法および硝酸銀誘発関節炎の炎症性疼痛に対して著しい鎮痛作用を示し，その効力はibuprofenおよびphenylbutazoneよりも遥かに優れていた．EB-382はラットの正常足における疼痛およびマウス熱板法において何ら作用を示さなかった．EB-382は，マウス酵母誘発慢性炎症性疼痛およびadjuvant関節炎疼痛に対して著しい鎮痛作用を示し，その効力はibuprofenおよびphenylbutazoneよりも遥かに優れていた．EB-382はラット酵母発熱に対してibuprofenとほぼ同程度の解熱作用を示したが，正常体温に対してはaminopyrineと異なり，何ら作用を及ぼさなかった．以上，EB-382は鎮痛・解熱剤として臨床上有用な薬剤となり得ることが示唆された．
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The influence of single oral dose of anti-inflammatory, antipyretic and analgesic agents on urinary enzymes was investigated in rats as a indicator of nephrotoxic effect. Urinary LDH activity was significantly elevated by aspirin, ketophenylbutazone, aminopyrine, phenacetin and acetaminophen. These drugs increased also H/M ratio of LDH isoenzymes. Although other test drugs have no effect on LDH in urine phenylbutazone and indomethacin elevated GPT and Al-P, oxyphenbutazone did γ-GT and anthranilic acid derivatives did Al-P and γ-GT. Other drugs such as sodium salicylate, ibufenac, ibuprofen, bucolome, aminopropylone, sulfinpyrazone, benzydamine and mepirizole did not significantly influence any enzyme activities measured in urine.
Antipyretic
Phenacetin
Ibuprofen
Acetaminophen
Oxyphenbutazone
Anthranilic acid
Sulfinpyrazone
Anti-inflammatory
Sodium salicylate
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