Presentation On Non-Steroidal Anti-Inflammatory Drugs

Presented by: Mahwish Nasir

CELECOXIB DRUG CATEGORY : Coxib(cox-2-inhibitor)

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KETOROLAC TROMETHAMINENonselective Cox inhibitor

DRUG CATEGORY : NSAID Previous Drug

Celecoxib

DRUG DESCRIPTION:Celecoxib is chemically designated as 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzene sulfonamide and is a diaryl-substituted pyrazole. It has the following chemical structure:

MECHANISM OF ACTION:Celecoxib is a highly selective COX-2inhibitor , about 10 – 20 times more selective for COX -2 than for COX-1 .

COX-2 selective inhibitors , were developed in an attempt to inhibit prostacyclin synthesis.

It is done by COX-2 ISO enzyme Induced at sites of inflammation without affecting the action of the constitutively active “house keeping” COX-1 ISO enzyme found in the GI tract, kidneys, and platelets.

COX-2 inhibitors have analgesic, anti-pyretic, and anti-inflammatory effects similar to those of non-selective NSAIDs.

Celecoxib

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CelecoxibINDICATIONS:

Rheumatoid arthritis Osteoarthritis

DOSAGE:

Osteoarthritis (adults): 200mg capsule once daily or in two divided doses.

Increase to 200mg twice daily if necessary. Maximum 400mg daily.

CHILDREN: not recommended.

Rheumatoid arthritis (adults): 200 to 400mg daily.

CHILDERN: not recommended.

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Celecoxib

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PHARMACOLOGY:

Pharmacokinetics:

HALF-LIFE(hours): 11

URINARY EXCRETION: 27%

Pharmacodynamics:

The Coxib continue to be investigated to determine whether their effects on prostacyclin production could lead to a prothrombotic state.

It causes no more edema or renal effects than other members of NSAIDs group.

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Celecoxib

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CONTRA-INDICATION:

History of hypersensitivity to sulphonamides or NSAIDs.Active peptic ulceration or GI bleeding.Severe renal or hepatic impairment.Severe congestive heart failure.Safe-use during pregnancy or lactation is not advisable.

Precautions:

Risk of hypovolaemia in elderly patient ( > 65 yrs).Left ventricular dysfunction.

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Celecoxib

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INTERACTIONS:Diuretics Anti-hypertensive ACE inhibitorsAnti-coagulantsLithium CyclosporineRifampicinBarbituratesFluconazoleMethotrexate

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SIDE-EFFECTS:Fluid retentionGI upsetDizziness InsomniaSkin rash

Celecoxib

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AVAILABLE BRANDS AND PRICES: CELART(Hilton) Price:Caps 100mg:10’s: 97.75Caps 200mg:10’s: 148.75

CELBEXX (Getz-pharma)Price:Caps: 100mg: 20’s :102.00Caps: 200mg: 20’s: 170.00

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KETOROLAC TROMETHAMINE

Mechanism of action: It is an NSAID promoted for systemic use. It inhibits prostaglandin biosynthesis.

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DRUG DESCRIPTION: Ketorolac is potent analgesic but only a moderately effective anti-inflammatory drug. It is one of the few NSAIDs approved for Perenteral administration.

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Indications: Short -term management of moderate to severe post- operative pain.

Available dosage forms:

Oral: 10mg tablets

Perenteral: 10-30mg per ml for IM or Iv injection.

Ophthalmic: 0.5 % solution.

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Dosage regimen:

Adults: Initially 10mg by IM or bolus IV daily for upto2 days. Maximum 90mg daily for up to 2 days.

Elderly: Initially 10mg by IM or bolus Iv injection then 10-30mg every 4-6

hours. Maximum 60mg daily for 2 days.Children: Under 16 yrs, not recommended.

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Contra-indication: Peptic ulcer GI or cerebrovascular bleeding Coagulation disorders Asthma Renal impairment Hypovolaemia during dehydration Pregnancy & Lactation: Safe use during pregnancy and lactation is not advisable. ( NOTE: unless expected benefit outweighs potential risk.)

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PHARMACOLOGY:Pharmacokinetics:

HALF-LIFE(hours): 4-10 URINARY EXCRETION: 58%

Pharmacodynamics: The drug does appear to have significant analgesic efficacy and has been used successfully

to replace morphine in some situations involving mild to moderate post surgical pain. When used with an opioid, it may decrease the opioid requirement by 25 to 50%.

Precautions: Homeostasis Allergic disease Cardiac dysfunction

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Interaction:AnticoagulantsLithium FrusemideOxypentifyllineNSAIDsMethotrexate

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Side effects: Abnormal liver function tests Acute renal failure Bronchospasm Anaphylaxis Pain at injection site Ulcers Wound hemorrhage GI disturbances Dizziness

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AVAILABLE BRANDS AND PRICES:TORADOL(Roche) Price: Inj 30mg :5×1ml : 455.50 TORAPAN (Duopharma)Price:Inj 30mg :10×1ml : 589.68.

KETOROLAC TROMETHAMINE

References

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REFRENCES:

KatzungPharma guide

Goodman Gilman

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