Transcript Presentation On Non-Steroidal Anti-Inflammatory Drugs Presented by: Mahwish Nasir CELECOXIB DRUG CATEGORY : Coxib(cox-2-inhibitor) Next Drug.

Presentation On
Non-Steroidal Anti-Inflammatory Drugs
Presented by: Mahwish Nasir
CELECOXIB
DRUG CATEGORY : Coxib(cox-2-inhibitor)
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KETOROLAC TROMETHAMINE
Nonselective Cox inhibitor
DRUG CATEGORY : NSAID
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Celecoxib
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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.
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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.
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Celecoxib
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
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
INTERACTIONS:
Diuretics
Anti-hypertensive
ACE inhibitors
Anti-coagulants
Lithium
Cyclosporine
Rifampicin
Barbiturates
Fluconazole
Methotrexate
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Celecoxib
SIDE-EFFECTS:
Fluid retention
GI upset
Dizziness
Insomnia
Skin rash
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Celecoxib
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
KETOROLAC TROMETHAMINE
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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.
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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.
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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.
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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.)
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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
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KETOROLAC TROMETHAMINE
Interaction:
Anticoagulants
Lithium
Frusemide
Oxypentifylline
NSAIDs
Methotrexate
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KETOROLAC TROMETHAMINE
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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KETOROLAC TROMETHAMINE
AVAILABLE BRANDS AND PRICES:
TORADOL(Roche)
Price:
 Inj 30mg :5×1ml : 455.50
TORAPAN (Duopharma)
Price:
Inj 30mg :10×1ml : 589.68.
References
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REFRENCES:
Katzung
Pharma guide
Goodman Gilman