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Presentation On Non-Steroidal Anti-Inflammatory Drugs. Presented by: Mahwish Nasir. CELECOXIB DRUG CATEGORY : Coxib(cox-2-inhibitor). Next Drug. KETOROLAC TROMETHAMINE Nonselective Cox inhibitor DRUG CATEGORY : NSAID. Previous Drug.

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Presentation Transcript
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Presentation On

Non-Steroidal Anti-Inflammatory Drugs

Presented by: Mahwish Nasir

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CELECOXIB

DRUG CATEGORY : Coxib(cox-2-inhibitor)

Next Drug

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KETOROLAC TROMETHAMINE

  • Nonselective Cox inhibitor
  • DRUG CATEGORY : NSAID

Previous Drug

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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.

Next

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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 orNSAIDs.
  • 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

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Celecoxib

INTERACTIONS:

  • Diuretics
  • Anti-hypertensive
  • ACE inhibitors
  • Anti-coagulants
  • Lithium
  • Cyclosporine
  • Rifampicin
  • Barbiturates
  • Fluconazole
  • Methotrexate

Next

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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
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KETOROLAC TROMETHAMINE

Mechanism of action:

  • It is an NSAID promoted for systemic use.
  • It inhibits prostaglandin biosynthesis.

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.

Next

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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.

Continue

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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

Next

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KETOROLAC TROMETHAMINE

Interaction:

  • Anticoagulants
  • Lithium
  • Frusemide
  • Oxypentifylline
  • NSAIDs
  • Methotrexate

Next

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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

Next

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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

refrences

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REFRENCES:
  • Katzung
  • Pharma guide
  • Goodman Gilman
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