Anti - Inflammatory Drugs Flashcards
What is an example of an autacoid and what causes its release?
Tissue injury causes the release of autocoids. An example is prostaglandins
What do autacoids cause?
Vasodilation, increased vascular permeability, chemotaxis, pain
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) - Mechanism of Action
Also known as Cyclooxygenase Inhibitors
Inhibits cyclooxygenase (COX)
What is COX
COX is the enzyme that converts arachidonic acid into prostanoids
It induces an undesirable inflammatory effect
What are the 4 properties of NSAIDs
Analgesic
Anti-inflammatory
Antipyretic (fever reducing)
Antirheumatic (arthritis treatment)
NSAID - Indication
- Mild to moderate pian
- Acute gout
- Various bone, joint, and muscle pain
- Osteo/rheumatoid/juvenile arthritis
- Dysmenorrhea (menstrual cramps)
- Fever
etc
What does the Antipyretic property of NSAID inhibit?
Prostaglandin E2 within the hypothalamus (where the temperature is controlled)
What is the role of Non-selective NSAIDs?
To inhibit COX-1 and COX-2
- Alleviate mild to moderate pain
- Inflammatory disorders (arthritis, bursitis)
Examples of Non-Selective NSAIDs
Acetylsalicylic acid (ASA, ASPIRIN)
Ibuprofen (Motrin, Advil)
Naproxen (Aleve)
Can be combine with mild opioids (codeine) or caffeine
What is the standard NSAID?
Acetylsalicylic acid (ASA, Aspirin)
Made in 1899
What are the 4 properties of ASA?
- Anti-inflammatory
The reduction in tissue levels of prostaglandins may be responsible for ASA’s analgesic and anti-inflammatory effects. - Analgesic
“” - Antipyretic
- ASA lowers body temperature mainly through inhibition of prostaglandin E1 synthesis in the brain. Heat production is not affected but dissipation of heat is enhanced via increased blood flow through the skin and sweating. - Antiplatelet
Inhibition of thromboxane A2 synthesis which plays an essential role in platelet aggregation. ASA prevents thromboxane A2 formation by inhibiting COX. This is irreversible and lasts the lifetime of a platelet (8 days)
Platelet Activation Balance
Balance between TXA2 and PGI2
Platelets - Endothelial cells
Prothrombotic - Anti-thrombotic
TXA2 - PGI2/NO
ASA - Contraindications
Pregnancy - in late trimester connected with low weight, intracranial bleed, and even death
- Also excreted in breast milk
Influenza and chickenpox in kids/teens to avoid *Reye’s syndrome
Bleeding disorders, 1 week pre op, and in renal/hepatic dysfunction patients
What are the symptoms of Reye’s syndrome?
- Vomiting
- Liver damage
- CNS problems (encephalopathy) including confusion, seizures, coma.
Salicylate Toxicity - Drugs and Symptoms
Caused by ASA, Na salicylate, Mg salicylate
Adult symptoms:
- Tinnitus and hearing loss
Children
- Hyperventilation and CNS effects