The pharmacologic activity of ketorolac tromethamine.

Ketorolac tromethamine is a highly potent member of a class of compounds having both analgesic and antiinflammatory activity. In animal pain models using underlying inflammation, ketorolac markedly inhibited the pain response and increased the pain threshold; it did not exhibit any narcotic or central nervous system depressant effects. It was also active in rat models of acute and chronic inflammation and pyresis.

11-Deoxy-11 alpha,12 alpha-methanoprostaglandin E2, a potent, short-acting bronchodilator.

11-Deoxy-11 alpha,12 alpha-methanoprostaglandin E2 (1b) and the corresponding methyl ester 7a were highly potent, but short acting, bronchodilators both by the intravenous (80 and 10 times PGE2, respectively) and aerosol (2 and approximately 1 times PGE2) routes, as measured by the Konzett-Rössler assay. The 11 beta,12 beta-methano compound 15a was two orders of magnitude less active than 7a. In rhesus monkeys anesthetized by aerosol administration, 1b was 10-50% as potent as, and had a duration of action similar to, PGE1 in the inhibition of methacholine-induced increases in airway resistance.

The analgesic and anti-inflammatory profile of ketorolac and its tromethamine salt.

Ketorolac tromethamine[(+/-)-5(benzoyl)-2,3-dihydro-1N-pyrrolizine-1-carboxylic acid tris hydroxymethylaminomethane salt] is a highly potent member of a new class of compounds having analgesic and anti-inflammatory activity. When given orally in tests involving underlying inflammation it was a potent analgesic, whereas it was inactive in tests for narcotic activity. It was also highly active orally in rat models of acute and chronic inflammation and pyresis.

The analgesic and anti-inflammatory profile of (+/-)-5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2a]pyrrole-1-carboxylic acid (RS-37619).

RS-37619 showed highly potent analgesic activity when given p.o. in tests utilizing underlying inflammation.

The anti-inflammatory and analgesic profile of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid (tiopinac).

Tiopinac displayed marked anti-inflammatory activity when given p.o. in rat models of acute and chronic inflammation.