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Presented by: Mahwish Nasir Presented by: Mahwish Nasir.

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Presentation on theme: "Presented by: Mahwish Nasir Presented by: Mahwish Nasir."— Presentation transcript:

1 Presented by: Mahwish Nasir Presented by: Mahwish Nasir

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

3 KETOROLAC TROMETHAMINE Nonselective Cox inhibitor DRUG CATEGORY : NSAID Previous Drug

4 Celecoxib

5 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 NSAID s. Celecoxib Next Main Menu

6 Celecoxib 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 Main Menu

7 Celecoxib Next 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. Main Menu

8 Celecoxib Next 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. Main Menu

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

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

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

12 KETOROLAC TROMETHAMINE

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

14  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

15  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

16 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

17 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

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

19 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

20 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 Main Menu

21 REFRENCES:  Katzung  Pharma guide  Goodman Gilman Main Menu


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