indomethacin,tolmetin,kitorolac

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The NSAIDs are a group of chemically dissimilar agents that

differ in their antipyretic, analgesic, and anti-inflammatory

activities. They act primarily by inhibiting the cyclooxygenase

enzymes that catalyze the first step in prostanoid

biosynthesis. There are two types of NSAIDs: selective and

nonselective.

Indomethacin,Tolmetin and Ketorolac are the examples of

non selective NSAIDs

Lippincott

Remington

Solubility: 1 g in 50 ml alcohol,30 ml chloroform,40 ml ether,partially

soluble in water.

Pharmacokinetics: Indomethacin is well absorbed orally,rectal absorption is slow.It

is 90% bound to plasma proteins,partially metabolized in liver and excreated by kidney.

Therapeutic effect:Indomethacin is effective for relieving joint pain, swelling, and tenderness, increasing grip strength.

It also is very effective in the treatment of acute gout, although it is not uricosuric.

Good man and Gilman’s & Drugs.com

Pharmacological Properties:Indomethacin has prominent antiinflammatory and analgesic-antipyretic properties.

It is a potent inhibitor of the cyclooxygenases .

It has analgesic properties distinct from its antiinflammatory effects.

Adverse Effect:

Goodman & Gilman, Jaypee & KD Tripathi,Lippincott’s

Contraindication:Indomethacin is contraindicated in pregnency,in asthmatics and those with gastric ulers.

It may increase the symptoms associated with depressio or other psychiatric disturbness.

Preparations available:Indomethacin(generic name)

Oral:25,50 mg capsuls;75 mg sustained release capsul;25 mg/5 ml suspention.

Rectal:50 mg suppositories.

Modern Pharmacology with Clinical Application & Katzung Picture-Google image

Lippincott & Remington

Therapeautic effect:Tolmetin (tolmetin sodium;TOLECTIN) is used for the treatment

of-OsteoarthritisRheumatoid arthritisJuvenile rheumatoid arthritisIt also has been used in the treatment of ankylosing spondylitis.Tolmetin is a nonselective COX inhibitor

Mechanism:Tolmetin inhibits prostaglandin synthetase .

Goodman and Gilman’s

Side Effect:

Katzung ,Drugs.com,Lippincott(picture)

Overdose:Overdose symptoms may include-

NauseaVomiting Stomach pain

Preparation available:Tolmetin(generic Tolectin)Oral:200,600 mg tablets;400 mg capsuls.

Remington & Goodman& Gillman

Pharmacokinetic: Ketorolac has a rapid onset of action, extensive protein binding, and a short duration of action.

Oral bioavailability is about 80%. Urinary excretion accounts for about 90% of eliminated drug, with about 10% excreted unchanged and the remainder as a glucuronidated conjugate.

The rate of elimination is reduced in the elderly and in patients with renal failure.

Theaputic effect:o Inhibit PG synthesiso use in the treatment of postoperative paino topically use for allergic conjunctivitis.o It is frequently used in postoperative,dental and

musculoskeletal pain

Common Adverse Effects:

Contraindication:This agent is to be avoided in pediatric patients,patients with mild pain, and those with chronic conditions.

Example: KETOROL,ZOROVON,KETANOV,TOROLAC 30 MG TABLET.

KETLUR,ACULAR .5% eye drop.