INTRODUCTION
ANALGESICS
A drug that selectively relieves pain by
acting in CNS or on peripheral pain
mechanism, without significantly altering
consciousness.
ANAESTHESIA
Anaesthesia means loss of sensation.
Anaesthetic agent is one which bring about
loss of all modalities of sensation,
particularly pain, along with a reversible
loss of consciousness.
PAIN (ALGESIA)
An unpleasant sensory and emotional
experience associated with actual or
potential tissue damage or described in terms
of such damage.
CLASSIFICATION
Divided into 2 groups:
1. Opioid Analgesics
-Narcotics/Morphine like analgesics
2. Non Opioid Analgesics
-NSAIDs/Non narcotic/aspirin like
analgesics
B. Prefential COX-2 inhibitors
- Nimesulide
- Meloxicam
- Nabumetone
C. Selective COX-2 inhibitors
- Valdecoxib
- Celecoxib
- Rofecoxib
D. Analgesics with poor Anti inflammatory
action-
Paraminophenol derivative
- Paracetamol (Acetaminophen)
4.Pyrazolone derivative
- Metamizol, Propiphenazone
6.Benzoxazocine derivative
- Nefopam
MECHANISM OF ACTION OF
NSAIDS
Prostaglandins synthesis inhibiton
Membrane phospholipids
Phospholipase A
Arachidonic acid
Cyclo oxygenase
PG G
2
+ PG H
2
Isomerases
Thromboxane
sythetase
Prostacyclin
synthetase
PG E
2
, PG D
2
, PG F TX A2
TX B
2
PG I
2
PG E
2
, PG D
2
, PG F TX A
2
MEPHENAMIC ACID
Anthranilic acid derivative
Adverse effect: Diarrhoea, skin rashes,
dizziness & other CNS manifestation
Orally absorbed & t ½ is 2-4 hrs
Uses: Analgesic in muscle, joint & soft tissue
pain, dysmenorrhoea, rheumatoid & osteoarthritis
Dose: 250-500 mg TDS
Commercially available as:
Medol, Meftal - 250, 500 mg tab.
DICLOFENAC SODIUM
Aryl-acetic acid derivative
Well absorbed orally
Plasma t ½ - 2 hrs
Adverse effects: Epigastric pain, nausea,
headache, dizziness, rashes
Uses: Rheumatoid arthritis, ankylosing
spondylitis, dysmenorrhea, post traumatic & post
inflammatory conditions
Dose: 50mg TDS, then BD oral, 75mg deep i.m
Commercially available as:
Voveran, Diclonac, Movonac : 50 mg tab.
Diclomax : 25, 50 mg tab.
PIROXICAM
Oxicam derivative
Long acting potent NSAID
Good analgesic-antipyretic action
Metabolised in liver ; excreted in urine & bile
Plasma t ½ is 2 days
Side effects : heart burn, nausea & anorexia
Use as short term analgesic & long term anti
inflammatory drug – rheumatoid & osteo arthritis,
ankylosing spondylitis, acute gout, musculoskeletal
injuries,dysmenorrhoea etc
Dose: 20mg BD for 2 days followed by 20mg OD
Commercially available as-
Dolonex, Pirox, Piricam : 10, 20 mg cap.
KETOROLAC
Pyrrolo-pyrrole derivative
Potent analgesic & modest anti inflammatory
Rapidly absorbed after oral & i.m administration
Plasma t ½ is 5-7 hrs
Adverse effects: Nausea, abdominal pain,
dyspepsia, ulceration, loose stools, drowsiness,
headache, dizziness, nervousness, pruritis, pain &
fluid retention
Not be given to patients on anticoagulants
USES:
-Postoperative & acute musculoskeletal pain: 15-30
mg i.m or i.v every 4-6 hrs
-Used for renal colic, migraine, pain due to bony
metastasis
-Orally in a dose of 10-20 mg 6 hrly.
-Commercially available as –
Ketorol, Zorovon, Ketanov, Torolac : 10mg tab.
NIMESULIDE
Preferential COX-2 inhibitors
Used for short lasting painful inflammatory
conditions like sports injuries, sinusitis, ear nose
throat disorders, dental surgery, bursitis, low
backache, dysmenorrhoea, post operative pain,
osteoarthritis & for fever
Completely absorbed orally, excreted in urine, t ½
of 2-5 hrs
Adverse effects:
- Epigastralgia, heart burn, nausea, loose motions,
rash pruritus.
- Hematuria & fulminant hepatic failure in few cases
Useful in asthmatics, bronchospasm or intolerance to
aspirin & other NSAIDs
Dose: 100 mg BD
Commercially available as-
Nimulid, Nimegesic, Nise, Nobel, Nimodol : 100mg
tab.
ROFECOXIB
Selective COX-2 inhibitor.
Effective in osteoarthritis, rheumatoid arthritis,
dysmenorrhoea, dental, post operative & acute
musculoskeletal pain at dose of 12.5-25 mg OD
daily
Side effects mild g.i complaints, headache &
dizziness
Well absorbed orally & t ½ of 17 hrs
Avoided in presence of severe hepatic or renal
disease
Dose: 12.5-25 mg OD
Commercially available as-
Rofact, Rofegesic, Rofibax : 12.5, 25 mg tab.
PARACETAMOL
Para-amino phenol derivative
Actions: Good & promptly acting antipyretic
Well absorbed orally
Plasma t ½ is 2-3 hrs
Safe & well tolerated
Nausea & rashes occur occasionally
Analgesic nephropathy- years of heavy ingestion
Acute paracetamol poisoning:
- In small children with glucuronide conjugating
ability
-Nausea, vomiting, abdominal pain, liver tenderness
-Centrilobular hepatic necrosis accompanied by renal
tubular necrosis & hypoglycemia, may progress to
coma
-Jaundice after 2 days
Treatment: Vomiting induced, activated
charcoal given, N-acetylcystein 150mg/kg infused
iv over 20hrs, alternatively, 75mg/kg orally every
4-6 hrs for 2-3 days.
USES:
-First choice analgesic for osteoarthritis
-Best drug to be used as antipyretic
-Over the counter analgesic for headache,
musculoskeletal pain, dysmenorrhoea, etc
-Much safer than aspirin
-Does not prolong bleeding time
-Used in all age groups, pregnant & lactating
women, in other disease states & in patients in
whom aspirin is contraindicated
-No significant drug interactions
SYNERGISTIC EFFECT
When the action of one drug is facilitated or
increased by the other, they are said to be
synergistic.
ADDITIVE SYNERGISM
Combiflam : ibuprofen+ paracetamol (400 + 325mg)
Dolokind plus : aceclofenac + paracetamol (100
+500 mg)
Diclozee plus : diclofenac Na + acetoaminophen (50
+ 500 mg)
Diclomol : diclofenac Na + acetoaminophen (50 +
500 mg)
Serazee plus : diclofenac K + seratiopeptidase (50
+10 mg)
Ibugesic plus : ibuprofen+ paracetamol (400 +
325mg)
Asonac-SR plus : aceclofenac + paracetamol +
seratiopeptidase (100 + 500 + 15mg )
TOPICAL NSAIDs
Topical formulations are available for application
over painful joints and muscles.
•Osteoarthritis
•Sprains
•Sports injuries
•Backache
Preparations
Diclofenac 1% gel : voveron emulgel, diclonac gel.
Ibuprofen 10% gel : ribufen gel.
Ketoprofen 2.5% gel : rhofenid gel.
Nimesulide 1% gel : nimulid trans gel.
Piroxicam 0.5% gel : dolonex gel, minicam gel.
GENERAL CONTRAINDICATIONS
Ulcer
Asthma
Patient with nasal polyp
Diabetes
Gout
Influenza (Reye’s syndrome)
Hypo coagulation state
Chronic allergic disorders
Chronic liver disease
Renal failure
Salicylate allergy
Breast feeding mothers
Pregnancy
CONCLUSION
Nature of problem along with consideration of risk
factors in an individual patient directs the initial
selection
Drugs differ quantitatively in producing different
side effects
Large inter individual differences
REFERENCES
Essentials of Medical Pharmacology,
K. D Tripathy, 5
th
edition
Pharmacology & Pharmacotherapeutics,
R. S. Satoskar,18
th
edition
Textbook of oral medicine,
Burkett’s, 11
th
edition