Mitochondria: Requires constant Ca supply, able to quickly absorb after release
from intracellular stores
Unit 3: example of drug action
Inflammation Drug Targets
what is acute inflammation
an immediate response to injury that is short duration,
showing cardinal signs of inflammation:
rubor (redness), Calor (heat), Tumor (swelling), Dolor (pain), Functio laesa (loss of
function)
Mechanisms of acute inflammation
1. Exposure to an inflammatory insult
2. leads to activation of cells present at the site of exposure and release of
mediators
3. changes in blood flow and vessel wall permeability and recruitment and
activation of circulating cells which release mediators + plasma leakage,
bringing in more mediators
4. the inflammatory stimulus is removed and tissue resolution and repair issues
timeline of the inflammatory response
Principle of Pharmacology 68
, Pathways of inflammatory mediatory production
what is inflammation mediators
cause the vascular and cellular change, inflammatory pain and pruritus in
inflamed tissue
when pro-inflammatory mediators are released in excess, damage to the host
can occur, so anti-inflammatory drugs are needed
In response to injury or activation of the immune system, cytokines are released
or synthesised
e.g. TNF alpha, IL-1 → increase chemokine, adhesion molecules, inflammatory
mediators → increased vasodilation, pain, swelling, recruit inflammatory cell
how to control an inflammatory response
by targeting:
1. mediator synthesis
2. mediator directly
3. mediator receptors
Principle of Pharmacology 69
, 4. mediator signalling pathways
Overlapping actions of inflammatory mediators
Use of drugs to target inflammatory pathways
Anti-histamine
histamine
Stored in mast cells, platelets, basophils
H1 receptor is involved in inflammation
Massive histamine release causes hypersensitivity type 1 and anaphylactic
reaction
mode of action:
H1 anti-histamines block the action of histamine via competitive
antagonisms
clinical use:
Principle of Pharmacology 70
from intracellular stores
Unit 3: example of drug action
Inflammation Drug Targets
what is acute inflammation
an immediate response to injury that is short duration,
showing cardinal signs of inflammation:
rubor (redness), Calor (heat), Tumor (swelling), Dolor (pain), Functio laesa (loss of
function)
Mechanisms of acute inflammation
1. Exposure to an inflammatory insult
2. leads to activation of cells present at the site of exposure and release of
mediators
3. changes in blood flow and vessel wall permeability and recruitment and
activation of circulating cells which release mediators + plasma leakage,
bringing in more mediators
4. the inflammatory stimulus is removed and tissue resolution and repair issues
timeline of the inflammatory response
Principle of Pharmacology 68
, Pathways of inflammatory mediatory production
what is inflammation mediators
cause the vascular and cellular change, inflammatory pain and pruritus in
inflamed tissue
when pro-inflammatory mediators are released in excess, damage to the host
can occur, so anti-inflammatory drugs are needed
In response to injury or activation of the immune system, cytokines are released
or synthesised
e.g. TNF alpha, IL-1 → increase chemokine, adhesion molecules, inflammatory
mediators → increased vasodilation, pain, swelling, recruit inflammatory cell
how to control an inflammatory response
by targeting:
1. mediator synthesis
2. mediator directly
3. mediator receptors
Principle of Pharmacology 69
, 4. mediator signalling pathways
Overlapping actions of inflammatory mediators
Use of drugs to target inflammatory pathways
Anti-histamine
histamine
Stored in mast cells, platelets, basophils
H1 receptor is involved in inflammation
Massive histamine release causes hypersensitivity type 1 and anaphylactic
reaction
mode of action:
H1 anti-histamines block the action of histamine via competitive
antagonisms
clinical use:
Principle of Pharmacology 70
