Analgesics Presentation-1
Analgesics Presentation-1
Analgesics Presentation-1
ANALGESICS
Pathogenesis of pain
Intense stimulus (e.g. tissue injury)
releases substances that sensitize pain
receptors to mechanical, thermal, and
chemical stimulation.
• NSAIDs have
• analgesic,
• antipyretic
• anti-inflammatory effects.
b) Central mechanisms
◦ Prostaglandins act in the spinal cord and higher
centres to promote the transmission of pain
signals to the brain.
◦ They thus block the peripheral generation of
pain impulses mediated by prostaglandins and
other chemicals
NSAIDs
Indications??
NSAIDs
NSAIDs act on the hypothalamic thermo-regulating
center to produce peripheral vasodilation, via
prostaglandin synthesis inhibition.
They
can also be used for surgical and cancer pain (if
combined with opiods).
NSAIDs
A/E: GI effects, bleeding, hypersensitivity,
headache, dizziness, nephrotoxicity, fluid
retention.
Drug interactions:
◦ oral anticoagulants (↑bleeding).
◦ Other NSAIDs and aspirin (ulcers).
◦ Lithium (↑ lithium levels).
◦ Methotrexate (↑ methotrexate levels).
◦ Probenecid (inhibit renal excretion of drugs)
Salicylates
Used to relieve mild to moderate pain and reduce
inflammation and fever.
Receptors are located in the brain and spinal cord (μ, κ, δ , σ, and ε).
Histamine release
Pharmacokinetics
Well absorbed in the GIT.
Undergoes significant first pass hepatic metabolism (low
bioavailability of 20-30% ).
As a result there is a greater level of activity if morphine
is given IV.
Disadvantage of IV morphine:
Increased risk of tolerance (tolerance to one opiod can
lead to tolerance of other opiods).
Tolerance occurs through:
◦ Uncoupling of the receptors and 2nd messengers.
◦ Small rise in the # of 2nd messengers which are
activated by the receptor hence there is a lower
response.
◦ A decrease in the # of receptors.
OPIOD ANALGESICS
Dependence (usually accompanies the tolerance i.e. the
more tolerant you are, the more dependent you become).