indomethacin,tolmetin,kitorolac
TRANSCRIPT
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
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.
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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.
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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.
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.