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05 Pharmacology

The document discusses the role of inflammation as the body's protective response and outlines the types, signs, and chemicals involved in the inflammatory process. It details the mechanisms of action for non-steroidal anti-inflammatory drugs (NSAIDs) and steroidal anti-inflammatory drugs, their indications, side effects, and contraindications. Additionally, it highlights the use of analgesics for pain relief, particularly in pregnancy and breastfeeding.

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15 views23 pages

05 Pharmacology

The document discusses the role of inflammation as the body's protective response and outlines the types, signs, and chemicals involved in the inflammatory process. It details the mechanisms of action for non-steroidal anti-inflammatory drugs (NSAIDs) and steroidal anti-inflammatory drugs, their indications, side effects, and contraindications. Additionally, it highlights the use of analgesics for pain relief, particularly in pregnancy and breastfeeding.

Uploaded by

drabdullahpharmd
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PPTX, PDF, TXT or read online on Scribd
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DRUGS USED TO TREAT PAIN

AND INFLAMMATION

Dr. Haji Bahadar, PhD, Assistant Professor


KMU-IPMS
WHAT IS INFLAMMATION?
Inflammation is the body's protective response to
injury.
Physical: Burns, Frostbite, Physical injury
Biological: Infection by pathogens
Chemical: toxin or toxicant
Immune system activation
Types: Acute and chronic
SIGNS OF INFLAMMATION
 Pain - the inflamed area is likely to be painful
.Chemicals that stimulate nerve endings are
released, making the area much more
sensitive.
 Redness - this is because the capillaries are

filled up with more blood than usual.


 Immobility - there may be some loss of

function.
 Swelling - caused by an accumulation of

fluid.
 Heat - more blood in the affected area

makes it feel hot to the touch.


SYNTHESIS OF PROSTAGLANDINS

 Synthesis of prostaglandins: Arachidonic acid


is the primary precursor of the prostaglandins

 Arachidonic acid is present as a component of


the phospholipids of cell membranes.
 Free arachidonic acid is released from tissue

phospholipids by the action of phospholipase


A2 via a process controlled by hormones
 There are two major pathways in the synthesis

of the eicosanoids from arachidonic acid, the


cyclooxygenase and the lipoxygenase
pathways
Rheumatoid arthritis
CHEMICALS INVOLVED
 Cytokines (fever sensitizing)
 Histamine (swelling sensitizing)

 Prostaglandins (pain sensitizing)


PAIN
 Pain is an unpleasant sensory and emotional
experience associated with actual or
potential tissue damage.
 Pain has many causes – cancer, injury,

infection, surgery – and people experience


pain in many different ways.
Analgesics

Non-opioid
Opioid analgesics
analgesics or NSAIDs
CYCLOOXYGENASE PATHWAY
 COX-1 is an enzyme that regulates normal
cellular processes,
1. Gastric protection,

2. Vascular homeostasis,

3. Platelet aggregation

4. Reproductive and kidney functions


 COX-2 is expressed in tissues such as the

brain, kidney, and bone. Its expression at


other sites is increased during states of
chronic inflammation
NONSTEROIDAL ANTI-INFLAMMATORY DRUGS
(NSAIDS) TRADE NAMES (DRUG MANNUAL)

1. Non selective COX


inhibitors
 Aspirin

 Diclofenac

 Indomethacin
2. COX-2 inhibitors
Selective COX-2 inhibitors are a type of non-
 Ketorolac
steroidal anti-inflammatory drug (NSAID) that
 Meloxicam directly targets cyclooxygenase-2, COX-2,
 Piroxicam an enzyme responsible
 Fenoprofen for inflammation and pain. Targeting
 Flurbiprofen selectivity for COX-2 reduces the risk
of peptic ulceration. Drugs are
 Ibuprofen
celecoxib, rofecoxib
 Ketoprofen

 Naproxen

 Paracetamol

(no anti inflammatory)


STEROIDAL ANTI INFLAMMATORY
DRUGS
 Steroid is an organic compound with
four rings.
 The steroid core structure is composed

of seventeen carbon atoms, bonded in


four "fused" rings.
DIFFERENCE BETWEEN NON STEROID
AND STEROID STRUCTURES

Aspirin Dexamethasone
MECHANISM OF ACTION

During inflammation prostaglandins are


produced which stimulate peripheral nerve
endings producing pain impulses that are carried
to the CNS. NSAIDs cause the inhibition of COX-
1/2, decreasing prostaglandin synthesis. Aspirin
irreversibly inhibit cyclooxygenase. The other
NSAIDs are all reversible inhibitors of
cyclooxygenase.
INDICATIONS
 Headache (nonmigraine)

 Muscle aches and pain


 Toothache
 Dysmenorrhea
 Joint Pain (osteoarthritis)
 Inflammation
 Removal of acne(salicylic acid)
Salicylic acid 6 % topical gel
SIDE EFFECTS
• Nausea due to erosion of stomach lining
• Decrease cytoprotective mucus secretion.
SIDE EFFECTS
 Vomiting
 Peptic ulcer disease

 Gastrointestinal bleeding

 Prolong bleeding time (Aspirin)

 Hepatotoxicity (elevated serum enzymes like

alkaline phosphatase, serum glutamic-


pyruvic transaminase SGPT or ALT)
(Paracetamol)
 Hypersensitivity (in sensitive patients)- rash,

laryngeal edema, asthma (Aspirin)


 Kidney damage
CONTRAINDICATIONS
 Severe hepatic diseases (Aspirin, diclofenac,
paracetamol)
 Vitamin K deficiency (Aspirin)

 Hemophilia (bleeding disorder) (Aspirin)

 Children (Aspirin) causing Reye syndrome(self)

 Patients receiving anticoagulants such as warfarin

and heparin (aspirin)


 Asthma (aspirin)
ANTIPYRETIC ACTION
 Antipyretic action: Fever occurs when the
set-point of the anterior hypothalamic
thermoregulatory center is elevated. This can
be caused by PGE2 synthesis, which is
stimulated when endogenous fever-
producing agents (pyrogens), such as
cytokines, are released from WBCs that are
activated by infection, hypersensitivity,
malignancy, or inflammation. The NSAIDs
lower body temperature in patients with
fever by impeding PGE2 synthesis and
release
ANALGESICS AND PAIN RELIEF IN PREGNANCY
AND BREASTFEEDING

 Paracetamol
 Mefanamic acid

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