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Lecture 8 Presentation

Nonsteroidal anti-inflammatory drugs (NSAIDs) are used to treat pain, fever, and inflammation, with various indications including musculoskeletal pain and postoperative pain. They are categorized based on their chemical structure and selectivity, with both non-selective and COX-2 selective inhibitors available. NSAIDs have notable pharmacokinetic properties and potential adverse effects affecting multiple organ systems, necessitating careful monitoring and consideration of contraindications.

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3 views

Lecture 8 Presentation

Nonsteroidal anti-inflammatory drugs (NSAIDs) are used to treat pain, fever, and inflammation, with various indications including musculoskeletal pain and postoperative pain. They are categorized based on their chemical structure and selectivity, with both non-selective and COX-2 selective inhibitors available. NSAIDs have notable pharmacokinetic properties and potential adverse effects affecting multiple organ systems, necessitating careful monitoring and consideration of contraindications.

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alifoli202020
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© © All Rights Reserved
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Pharmacology

Of Non-steroid anti-inflammatory
drugs
Dr. BABAYEVA SVETLANA M.
Associate-professor, Department of Pharmacology, Azerbaijan Medical University
e-mail: svetlana.babayeva@amu.edu.az
Nonsteroidal anti-inflammatory drugs
• NSAIDs are a class of medications used to treat pain, fever, and other
inflammatory processes. This activity describes the indications,
mechanism of action, administration, adverse effects,
contraindications, monitoring, and important points for providers
regarding NSAIDs.
• NSAIDs are a drug class use as antipyretic, anti-inflammatory, and
analgesic agents. These effects make NSAIDs useful for treating
muscle pain, dysmenorrhea, arthritic conditions, pyrexia, gout,
migraines, and used as opioid-sparing agents in certain acute trauma
cases.
• Indications for NSAIDS include the following:
• Inflammatory conditions
• Chronic joint disease
• Musculoskeletal pain
• Headache
• Menstrual pain
• Dental pain
• Postoperative mild to moderate pain
•
NSAIDs are typically divided into groups based on
their chemical structure and selectivity:
• Non-selective COX1,2 blockers:
• Salicylates: Acetylsalicylic acid, sodium salicylate, salicylic acid, Methyl
salicylate, phenyl salicylate, mesalazine, diflunisal
• Para-aminophenol derivatives: acetaminophen (paracetamol)
• Pyrazolone derivatives: aminopyrine, methamisole (analgin),
propiphenazone, Phenylbutazone, oxyphenbutazone
• Phenylpropionic acid derivatives: (profenes) ibuprofen, naproxen, fenbufen,
• Thiaprofen, ketoprofen, phenoprofen.
• Phenylacetic acid derivatives: Diclofenac sodium, Nabumetone,
phenclofenac
• Indoleacetic acid derivatives: Indometacin, Tolmetin, Ketorolac,
Sulindac
• Phenamic acid derivatives: Mephenamic acid, Fluphenamic acid,
Tolphenamic acid,
• Oxycams: Piroxicam, Tenoxicam, Procuazone, Azapropazone
• COX-2 inhibitors:
• 1. COX-2 selective inhibitors: Celecoxib, Valdecoxib, Etherecoxib
Rofecoxib
• 2. Non-selective COX-2 inhibitors: Nimesulide, Meloxicam, Etodolac
•:
• III. Drugs of different groups:
• 1. Gold drugs: crizanol, auranofin, myocrysin
• 2. Bee venom preparations: apizatron, virapin, ungapevin, apifor,
apitoxin
• 3. Drugs based on snake venom: vipraxin, nayaxin, viprosal, nizvisal,
nazatox
• 4. Various anti-inflammatory agents: dimethyl sulfoxide
(dimethoxide), bischofit
• Topical NSAIDs are also available for use in acute tenosynovitis, ankle
sprains, and soft tissue injuries
Mechanism of action of
NSAIDs
Figure 1. Arachidonic
acid pathway showing
production of
prostaglandins from
membrane
phospholipids. The
leukotriene pathway is
responsible to the
group of patients with
NSAIDs–sensitive
asthma.
A wide variety of NSAIDs are available with different degrees of inhibition
of COX-1 and COX-2. Their degree of each isoenzyme inhibition determines
their side-effect profile.
Pharmacokinetic properties
The majority of NSAIDS are administered orally
They are weak organic acids and are therefore absorbed rapidly in the
stomach and small intestine.
The stomach has a lower pH than the small intestine and therefore,
more drug is in the more absorbable unionised form
NSAIDs have a high bioavailability due to limited first-pass hepatic
metabolism.
They are highly protein-bound molecules and as a result can displace
other protein-bound medications leading to increased free drug
concentrations and increased risk of adverse events (eg, displacement
of warfarin from albumin leading to an increased risk of bleeding).
Bioconversion is mostly hepatic with metabolites excreted in the urine.
• Adverse effects of NSAIDs
• NSAIDs have well-known adverse effects affecting the gastric mucosa,
renal system, cardiovascular system, hepatic system, and hematologic
system.
• Gastric adverse effects ,.
• Renal adverse effects ,
• Cardiovascular adverse effects can also be increased with NSAID use;
these include MI, thromboembolic events, and atrial fibrillation.
Diclofenac seems to be the NSAID with the highest reported increase in
adverse cardiovascular events.
• Respiratory adverse effects
• Hepatic adverse effects
• Hematologic adverse effects ,
• Bone Healing ,
Acetilsalicylic acid

Pharmacological effects: Side effects:


• Antiinflammatory (high dose) • Gastrointestinal irritation
• Analgetic (moderate dose) • Salicylism: tinnitus, vertigo, J.. hearing-
• Antipyretic (moderate dose) often first signs of toxicity
• Antiplatelet (low dose) • Bronchoconstriction
• Reye syndrome: encephalopathy
• hemorrhage
• Chronic use: associated with renal
dysfunction
• Drug interactions: ethanol (i gastrointestinal
bleeding) and warfarin (i effects), and
uricosurics ( J.. effects)
Acetaminophen - COX-III inhibitor (CNS)
• Mechanisms
- No inhibition of COX in peripheral tissues and lacks significant
antiinflammatory
Effects
Equivalent analgesic and antipyretic activity to ASA due to inhibition
of cyclooxygenases
• Comparisons with ASA:
No antiplatelet action
Not implicated in Reye syndrome
- No effects on uric acid
Not bronchospastic (safe in NSAID hypersensitivity and asthmatics)
- Gastrointestinal distress is minimal at low to moderate doses
Other NSAIDs

• Reversible inhibitors of COX 1 and


COX 2, with analgesic, antipyretic, and
antiinflammatory actions, include:
• metamizol
• Ibuprofen Naproxen
• diclofenac
• Indomethacin
• Ketorolac
• Sulindac Nabumeton
COX 2 Inhibitors:
Selective: Celecoxib
• Compared with conventional NSAIDs, it is no more effective as
an antiinflamrnatory agent.
• Primary differences are:
- Less gastrointestinal toxicity
- Less antiplatelet action
• However, it may possibly exert prothombotic effects via
inhibition of endothelial cell function (MI and strokes) .
• Cross-hypersensitivity between celecoxib and sulfonamides
COX 2 Inhibitors: Compared with conventional NSAIDs, it is no more
effective as an antiinflamrnatory agent. Primary differences are:
- Less gastrointestinal toxicity
- Less antiplatelet action

• Semi-selective: • Selective:
Meloxicam Celecoxib - it may possibly exert
prothombotic effects via inhibition of
Nimesulid endothelial cell function (MI and
strokes)
Etodolac
Rofecoxib
Etericoxib
Valdecoxib

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