Pharmacology for Dentistry

88 Section 2/ Drugs Acting on CNS

INDOLE DERIVATIVES

INDOMETHACIN

It is indole acetic acid derivative possess-
ing potent antiinflammatory property and
having a good analgesic and antipyretic ac-
tion also. Mechanism of action is same as
other NSAIDs.

It is readily absorbed from the GI tract,
99% bound to plasma proteins, distributed
into synovial fluid, the central nervous sys-
tem, placenta and breast milk. It is
metabolised in the liver to glucuronide con-
jugates, excretion of metabolites is predomi-
nantly in the urine with some amount ap-
pearing in the faeces.

Adverse effects include nausea, vomiting,
anorexia, gastric bleeding, diarrhoea, dizzi-
ness, frontal headache, confusion, depression,
psychosis, hallucination, leukopenia, epigas-
tric distress and rarely aplastic anaemia.

It is used in rheumatoid arthritis, osteo-
arthritis, ankylosing spondylitis and gout.

SULINDAC

It is a fluorinated derivative of in-
domethacin, has longer duration of action
and is used orally. It is prodrug, converted
to active sulfide metabolite.

PROPIONIC ACID DERIVATIVES

The drugs like ibuprofen, flurbiprofen,
ketoprofen etc. possess antiinflammatory

property similar to aspirin but toxicity and
adverse effects are fewer and of lesser in-
tensity. These preparations alone and in

combination with other NSAIDs are used for
treatment of inflammatory disorders,

muscle spasm and rheumatic disorders.

They are all well absorbed orally and are

highly bound to plasma proteins (90-99%).

Metabolized largely in liver by hydroxyla-

tion and glucuronide conjugation and ex-

creted in urine as well as in bile.

Adverse effects include nausea, vomit-

ing, epigastric discomfort, dizziness, head-

ache, skin rash and thrombocytopenia.

It is indicated in rheumatoid and osteo-

arthritis, ankylosing spondylitis, mild to

moderate pain including dysmenorrhoea,

soft tissue injuries, fractures and postopera-

tive analgesia.

FLURBIPROFEN

It is NSAID used in musculoskeletal and

joint disorders. It acts by inhibition of

cyclooxygenase.

It is readily absorbed from GI tract and

is 99% bound to plasma proteins.

Metabolised mainly by hydroxylation and

conjugation and excreted in urine.

KETOPROFEN

It is an inhibitor of cyclooxygenase with

analgesic, antiinflammatory and antipyretic

properties.

Readily absorbed from the GI tract. Food

slows the rate of absorption but not the total

bioavailability. Extensively bound to plasma

proteins and substantial concentrations are

found in synovial fluid. Metabolised mainly

by conjugation with glucuronic acid and ex-

creted mainly in the urine.

NAPROXEN

After oral administration, it is fully

absorbed. It is 99% bound to plasma pro-