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Non-Narcotic Analgesics: Brusas, Mylene
Non-Narcotic Analgesics: Brusas, Mylene
Brusas,Mylene D.
WHAT IS PAIN?
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ACUTE PAIN
Results from injury, disease or
inflammation.
Often comes on suddenly, can be
diagnosed and treated, and is usually self-
limited.
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CHRONIC PAIN
A disease by itself.
It is made worse by environmental and
psychological factors. Persists over time and
is resistant to medical treatment.
Pain management is an integral part of
treating chronic pain.
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INTRODUCTION
TO
NSAIDs
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Non-Narcotic pain relievers are
commonly called NSAIDs Non-
Steroidal Anti-Inflammatory
Drugs.
These drugs act at the local site
of injury to reduce inflammation
and to block nociceptors.
NSAIDs block COX.
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COX Inhibitors
COX or Cyclooxygenase is an enzyme which is
used to synthesize prostaglandins which cause
pain and inflammation.
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CLASSIFICATIONS
OF
NSAIDs
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NON-SELECTIVE
COX INHIBITORS
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INTRODUCTION:
Nonselective COX Inhibitors inhibit both COX-1 and
COX-2;
Prototype: ASA
Used as analgesics and for long-term treatment of
pain and inflammation from arthritis.
Significant effects on:
- Pain
- Inflammation
- Blood Platelets
- GI Tract
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NON-SELECTIVE COX INHIBITORS EXAMPLES
(CATEGORIES)
Salicylates Aspirin
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PHARMACOLOGICAL
ACTIONS
O Analgesic, antipyretic and anti-inflammatory
actions.
O Signs of inflammation:
Pain,
Tenderness,
Swelling,
Vasodilation
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PHARMACOKINETICS
O Absorbed from the stomach and small
intestines
O Poor water solubility
O Rapidly de-acetylated to release salicylic
acid to became an active form
O Bound to plasma proteins: 80%
O VDL: 0.17 L/kg
O ½ of anti-inflammatory dose: 8 to 12 hours
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ADVERSE EFFECTS
Side effects:
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ADVERSE EFFECTS
Hypersensitivity and idiosyncrasy
Rashes
Urticaria
Rhinorrhoea
Angioedema
Asthma
Anaphylactic reaction
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ADVERSE EFFECTS
Anti-inflammatory doses (3 to 5 g/day)
Syndrome salicylism- dizziness
Tinnitus
Vertigo
Reversible impairment of hearing and vision
Excitement and mental confusion
Hyperventilation
“Reye’s syndrome” in children
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ADVERSE EFFECTS
Acute salicylate poisoning (>50 mg/dL)
Vomiting
Dehydration
Electrolyte imbalance
Acidotic breathing
Restlessness, delirium
Hallucination, hyperpyrexia
Convulsions
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USES
Analgesic
Antipyretic
Acute rheumatic fever
Rheumatiod arthritis/ Osteoarthritis
Pregnancy: induced HTN and pre-eclampsia
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PROPIONIC ACID
DERIVATIVES
O Ibuprofen: 1st member of the class to be introduces
in 1969 as a better tolerated alternative to ASA.
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ADVERSE EFFECTS
Gastric discomfort, nausea and vomiting
Gastric erosion and occult blood loss
CNS side effects:
Headache
Dizziness
Blurring of vision
Tinnitus and depression
Rashes, itching and other hypersensitivity
phenomena
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USES
IBUPROFEN
Analgesic and antipyretic
Musculoskeletal disorders
Indications:
Soft tissue injuries, fractures
Vasectomy
Tooth extraction
Postpartum and postoperatively
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USES
NAPROXEN
Strong anti-inflammatory activity
Inhibits leucocyte migration
Acute gout: 750mg
Rheumatoid arthritis and Ankylosing
spondylitis
Suppress platelet function (longer t ½)
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USES
KETOPROFEN
Anti-inflammatory action
Additional action to stabilize lysosomes and
inhibits LOX
FLUBIPROFEN
Anti-inflammatory
Used in ocular anti-inflammatory
Longer acting
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FENAMATE
MEFENAMIC ACID
Analgesic, antipyretic and weaker anti-
inflammatory drug
Inhibits synthesis of PGs
ADVERSE EFFECTS:
Diarrhea
Epigastric distress
Skin rashes, dizziness
Hemolytic anemia (rare)
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OXICAMS
PIROXICAM
As a long-acting potent NSAID
Anti-inflammatory potency and good
analgesic-antipyretic action
A non-selective COX inhibitor
Inhibits platelet aggregation
Decreases IgM rheumatoid factor
TENOXICAM
A congener of Piroxicam with similar uses.
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PYROLO-PYROLLE
DERIVATIVE
KETOROLAC
Acetic acid derivative
Potent analgesic and modest anti-
inflammatory activity
Indicated for post-operative pain
Inhibits PG synthesis
Rapid absorption
High plasma protein bound
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Plasma t ½: 5 to 7 hours
INDOLE DERIVATIVE
INDOMETHACIN
An Acetic acid derivative
A potent anti-inflammatory drug with prompt
antipyretic action
Highly potent inhibitor of PG synthesis
Pharmacokinetics:
90% bound to plasma protein
Partial metabolized in liver
Excreted by kidney
Plasma t ½: 2 to 5 hours
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PYRAZOLONES
METAMIZOL
Potent analgesic and antipyretic
Poor anti-inflammatory and not uricosuric
S/E:
Agranulocytosis
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PYRAZOLONES
PROPIPHENAZONE
Similar properties to Metamizol
Claimed to be better tolerated
Agranulocytosis has not been reported.
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ARYL-ACETIC ACID
DERIVATIVE
DICLOFENAC SODIUM
An analgesic-antipyretic-antiinflammatory
drug.
Inhibits PG synthesis
Antiplatelet action is not applicable
99% protein bound
Metabolized and excreted both in urine and
bile
Plasma t ½: 2 hours
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SELECTIVE
COX-2
INHIBITORS
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SELECTIVE COX-2
INHIBITORS
O Inhibits COX-2 selectively
O Reduce PGI2 production by vascular
endothelium
O DO NOT SUPPRESS
COX-1
TXA2
O Avoided in patients with:
History of Ischemia Heart disease
HTN
Cardiac failure
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SELECTIVE COX-2
INHIBITORS
CELECOXIB
Anti-inflammatory, analgesic and antipyretic
In rheumatoid arthritis: as effective as
Naproxen and Diclofenac
S/E:
Abdominal pain
Dyspepsia
Mild diarrhea, rashes, edema
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SELECTIVE COX-2
INHIBITORS
ETORICOXIB
Highest COX-2 selectively inhibitor
Once-a-day treatment of:
Osteo-arthritis
Rheumatoid arthritis
Acute gouty arthritis
Ankylosing spondylitis
Acute dental surgey pain
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PARA-AMINO PHENOL
DERIVATIVES
O Action:
The central analgesic action of Paracetamol
Weak peripheral anti-inflammatory
Good antipyretic
Does not affect platelet function or clotting
factors and is not uricosuria.
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PARA-AMINO PHENOL
DERIVATIVES
O Pharmacokinetics
Well absorbed orally
Excreted by urine
Plasma t ½: 2 to 3 hours
O Adverse Effects:
Nausea and Rash
Leukopenia (Rare)
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