Pyrrolo-Pyrrole Derivative

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Chapter: Essential pharmacology : Nonsteroidal Anti-inflammatory Drugs And Antipyreticanalgesics

Ketorolac : A novel NSAID with potent analgesic and modest anti-inflammatory activity. In postoperative pain it has equalled the efficacy of morphine, but does not interact with opioid receptors and is free of opioid side effects.


PYRROLO-PYRROLE  DERIVATIVE

 

Ketorolac

 

A novel NSAID with potent analgesic and modest anti-inflammatory activity. In postoperative pain it has equalled the efficacy of morphine, but does not interact with opioid receptors and is free of opioid side effects. Like other NSAIDs, it inhibits PG synthesis and relieves pain by a peripheral mechanism. In short lasting pain, it has compared favourably with aspirin.

 

Ketorolac is rapidly absorbed after oral and i.m. administration. It is highly plasma protein bound and 60% excreted unchanged in urine. Major metabolic pathway is glucuronidation; plasma t½ is 5–7 hours.

 

Adverse Effects

 

Nausea, abdominal pain, dyspepsia, ulceration, loose stools, drowsiness, headache, dizziness, nervousness, pruritus, pain at injection site, rise in serum transaminase and fluid retention have been noted.

 

Ketorolac has been used concurrently with morphine. However, it should not be given to patients on anticoagulants.

 

Use

 

Ketorolac is frequently used in postoperative, dental and acute musculoskeletal pain: 15– 30 mg i.m. or i.v. every 4–6 hours (max. 90 mg/ day). It may also be used for renal colic, migraine and pain due to bony metastasis.

 

Orally it is used in a dose of 10–20 mg 6 hourly for short term management of moderate pain. Ketorolac has been rated superior to aspirin (650 mg), paracetamol (600 mg) and equivalent to ibuprofen (400 mg). Continuous use for more than 5 days is not recommended. It should not be used for pre-anaesthetic medication or for obstetric analgesia.

 

KETOROL, ZOROVON, KETANOV, TOROLAC 10 mg tab, 30 mg in 1 ml amp.

 

KETLUR, ACULAR 0.5% eye drops; 1–2 drops 2–4 times a day for noninfective ocular inflammatory conditions.

 

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