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Non-Narcotic Analgesics

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.

 2 types of COX Inhibitors:


1. COX-1: Mediates GI Tract and Blood Platelets
2. COX-2: Inflammation
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GENERAL EFFECTS
OF NSAIDs
1. Reduction of inflammation;
2. Reduction of body temperature;
3. Reduction of pain without sedation;
4. Inhibition of platelet aggregation.

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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

Propionic Acid derivatives Ibuprofen, Naproxen Ketoprefen,


Flurbiprofen
Anthranilic acid derivative Mefenamic Acid

Aryl-acetic acid derivative Diclofenac

Pyrolo-pyrolle derivative Ketorolac

Indole derivative Indomethacin

Pyrozolone derivative Metamizol and


Propiphenazone
Oxicam Piroxicam and Tenoxicam
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SALICYLATES
O ASA (prototype)
O It is one of the OLDEST analgesic anti-
inflammatory drugs.
O It is rapidly converted to salicylic acid
which is responsible for most of the
actions.

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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:

 Nausea and vomiting


 Epigastric distress
 Gastric mucosal damage
 Peptic ulceration

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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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