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ANALGESIC DRUGS
PRESENTER
C.NKAKA
CLASSIFICATION
• Non- steroidal anti-inflammatory drugs (
NSAIDs)
• Weak opiods
• Strong opiods
• Non-opiod analgesics
NON- STEROIDAL ANTI-INFLAMATORY
DRUGS ( NSAIDs)
• Salicylates ( e.g. acetylsalicylic acid )
• Paracetamol
• Cyclo-oxygenase (COX) inhibitors
Selective COX-2 compounds
Non Selective COX compounds.
COX-2 SELECTIVE COMPOUNDS
• Rofecoxib.
• Celecoxib.
• Meloxicam.
• Etodolac.
• Nabumetone.
NON COX-2 SELECTIVE COMPOUNDS.
• Diclofenac.
• Ibuprofen
• Piroxicam.
• Ketoprofen.
Weak opiods
• Codeine.
• Dihydocodeine.
• Dextropropoxyphene.
Strong opiods
• Morphine.
• Pethidine.
• Dextromoramide.
• Dipipanone.
• methadone
NON-OPIOD ANALGESICS
• Nefopam
CHOICE OF ANALGESICS
• For mild pain Non-narcotic analgesics or
NSAIDs are used such as:
Paracetamol.
Ibuprofen.
Diclofenac.
CHOICE OF ANALGESICS
• For moderate pain ,Narcotic (opiod)
analgesics, low –efficacy opiods are used such
as:
Codeine.
Dihydocodeine.
Dextropropoxyphene.
Pentazocine
CHOICE OF ANALGESICS
• For severe pain, high-efficacy opiod are used
such as:
Morphine
Diamorphine
Pethidine
Buprenorphine
An additional NSAID is useful if there's an
additional tissue injury component e.g. gout, bone
metastasis.
CHOICE OF ANALGESIC
• overwhelming acute pain
High-efficacy opiod plus a sedative/ anxiolytic
such as diazepam.
High –efficacy opiod plus a phenothiazine
tranquillizer such as chlorpromazine,
levomepromazine,
NONSTEROIDAL ABTI-INFLAMATORY
DRUGS
Mode of action
They work by blocking prostaglandin synthesis.
This is due to inhibition of the enzyme Cyclo-
oxygenase. Some NSAIDs are specific whereas
others are none specific.
USES OF NSAIDs
• Analgesia.
• Anti-inflammatory.
• Antipyretic action.
• Antiplatelet function.
USES
• Prolongation of gestation and labour.
• Patency of ductus arteriosus
• Primary dysmenorrhoea.
ADVERSE REACTIONS
• Gastric and intestinal mucosal damage
• Sodium and fluid retention
• Urticuria, rhinitis, and asthma occur in
susceptible individuals.
INTERACTIONS
• ACE inhibitors and angiotensin 11 antagonists
:there is risk of renal impairment and
hyperkalaemia.
• Quinolone antimicrobials: convulsions may
occur if NSAIDs are co administered.
• Anticoagulants and Antiplatelet agents reduce
platelet adhesiveness and GI tract damage by
NSAIDs increase risk of bleeding.
INTERACTIONS
• Fluconazole raises the plasma of Celecoxib
• Effect of antihypertensive drugs reduced due
to sodium and fluid retention.
• Ritonavir may raise the concentration of
piroxicam; NSAIDs may increase the
heamatological toxicity from Zidovudine.
Pharmacology of Individual NSAIDs
ASPIRIN
ACTION
• Has antipyretic, anti-inflammatory and
analgesic properties.
• Blocks prostaglandin synthesis .
ASPIRIN
INDICATIONS
• Mild to moderate pain
• Pyrexia
• Prophylaxis of cerebrovascular disease or
myocardial infarction
• Inflammatory condition
DOSE
Inflammatory /analgesia
• Adults: 300-900mg every 4-6 hours when
necessary, maximum 4g daily.
Secondary prevention of thrombotic
cerebrovascular disease or cardiovascular
• 75mg - 300mg daily. after myocardial
infarction 150mg daily. following bypass
surgery,75mg to 100mg daily.
ADVERSE EFFECTS
• Gastric irritation and bleeding.
• Asthmatic attacks and skin reactions.
• Reyes syndrome in some children with viral
infection.
• Salicylism-deafness, dizziness, tinnitus,
confusion, vomiting and hyperventilation.
• Metabolic acidosis
cautions
• Asthma
• Allergic disease
• Impaired renal or hepatic function
• Dehydration
• pregnancy
CONTRAINDICATIONS
• Gastro-intestinal ulceration
• Children under 12 years of age ( except for
juvenile arthritis) due to association with
Reyes syndrome
• Breastfeeding
• Heamophilia and other bleeding disorders
• History of hypersensitivity to aspirin
• Concurrent anticoagulant therapy.
DRUG INTERACTIONS
•
• ALCOHOL-likely to cause gastritis
• ANTICOAGULANTS-Increases bleeding
• ANTACIDS-excretion of aspirin increased in
alkaline urine
• ANTIEPILEPTICS-Phenytoin, valproate effect
enhanced.
• COTICOSTEROIDS-increased risk of bleeding and
peptic ulceration.
Paracetamol
Paracetamol
ACTION
• It has weak anti-inflammatory properties.
• Antipyretic,
• Analgesic
Indications
• Mild to moderate pain
• Pyrexia
• Alternative for patients who are sensitive to
aspirin
Dose
• Adults: 500mg -1g every 4-6 hours when
necessary, maximum 4g daily.
SIDE EFFECTS
• It causes kidney and liver damage on
prolonged use or overdose.
Cautions
• Impaired kidney or liver function
• alcoholism
INTERACTIONS
• ANTICOAGULANTS-enhances the effect of
warfarin after regular use.
• METOCLOPROMIDE &DEMPERIDONE
absoption of paracetamol is enhanced.
Ibuprofen
ACTION
• Has antipyretic, anti-inflammatory and
analgesic properties.
• Blocks prostaglandin synthesis .
Ibuprofen
INDICATIONS
• Fever and pain in children
• Mild to moderate pain including
dysmenorrhoea
• Postoperative analgesia
Dose
Adult:1.2- 1.8g in 3-4 divided doses preferably
after meals increased to a aximum of 2.4g
daily
Maintenance dose of 0.6 – 1.2g daily may be
adequate
Children:20mg/kg body weight daily in divided
doses. Not recommended for children under
75kg.
Side effects, cautions and
contraindications
• Same as for aspirin
End of presentation

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ANALGESIC DRUGS-1.ppt