Presentation On Non-Steroidal Anti-Inflammatory Drugs Presented by: Mahwish Nasir

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

KETOROLAC TROMETHAMINE Nonselective Cox inhibitor DRUG CATEGORY : NSAID Previous Drug

Celecoxib Drug Description Indication & Dosage Pharmacology Contra-Indications & Precautions Interactions Side effects Available Brands & Prices

Celecoxib Main Menu DRUG DESCRIPTION: MECHANISM OF ACTION: 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. Next

Celecoxib Main Menu INDICATIONS: 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. Next

Celecoxib PHARMACOLOGY: Main Menu Pharmacokinetics: Pharmacodynamics: 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. Next

Celecoxib CONTRA-INDICATION: Main Menu Celecoxib 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. Next

Celecoxib INTERACTIONS: Diuretics Anti-hypertensive ACE inhibitors Main Menu Celecoxib INTERACTIONS: Diuretics Anti-hypertensive ACE inhibitors Anti-coagulants Lithium Cyclosporine Rifampicin Barbiturates Fluconazole Methotrexate Next

Celecoxib SIDE-EFFECTS: Fluid retention GI upset Dizziness Insomnia Main Menu Celecoxib SIDE-EFFECTS: Fluid retention GI upset Dizziness Insomnia Skin rash Next

AVAILABLE BRANDS AND PRICES: Main Menu Celecoxib AVAILABLE BRANDS AND PRICES: CELART(Hilton) Price: Caps 100mg:10’s: 97.75 Caps 200mg:10’s: 148.75 CELBEXX (Getz-pharma) Caps: 100mg: 20’s :102.00 Caps: 200mg: 20’s: 170.00

KETOROLAC TROMETHAMINE Drug Description Indication & Dosage Contra-Indications Pharmacology & Precautions Interactions Side effects Available Brands & Prices

KETOROLAC TROMETHAMINE Main Menu KETOROLAC TROMETHAMINE 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. Mechanism of action: It is an NSAID promoted for systemic use. It inhibits prostaglandin biosynthesis. Next

KETOROLAC TROMETHAMINE Main Menu KETOROLAC TROMETHAMINE 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. Continue

KETOROLAC TROMETHAMINE Main Menu KETOROLAC TROMETHAMINE 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. Next

KETOROLAC TROMETHAMINE Main Menu KETOROLAC TROMETHAMINE 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.) Next

KETOROLAC TROMETHAMINE Main Menu KETOROLAC TROMETHAMINE 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 Next

KETOROLAC TROMETHAMINE Main Menu KETOROLAC TROMETHAMINE Interaction: Anticoagulants Lithium Frusemide Oxypentifylline NSAIDs Methotrexate Next

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

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

Main Menu REFRENCES: Katzung Pharma guide Goodman Gilman