PDA II exam 3 eico

Question 1

Describe the pathways and function of eicosanoids and relate them to the pharmacological action of drugs (3)

Answer 1

Eicosanoids function in diverse physiological systems and pathological processes such as: mounting or inhibiting inflammation, allergy, fever and other immune responses; regulating the abortion of pregnancy and normal childbirth; contributing to the perception of pain; regulating cell growth; controlling blood pressure

roduced by three primary enzymatic pathways: cyclooxygenase (COX), lipoxygenase (LOX) and cytochrome P450 (CYP)

Question 2

name

Selective Cox-2 Inhibitor (NSAID):

Non-selective Cox Inhibitors (NSAIDs):

Analgesic & Antipyretic:

drugs

Answer 2

Selective Cox-2 Inhibitor (NSAID):

Celecoxib (Celebrex ®)

Non-selective Cox Inhibitors (NSAIDs):

Aspirin

Ibuprofen

Naproxen

Analgesic & Antipyretic:
Acetaminophen (Rx: N-acetylcysteine)

Question 3

Nociceptors and pain management

Answer 3

Nociceptors: Transduction of Pain

Ion channels opened by:

Strong mechanical stimulation, temperature extremes, oxygen deprivation, chemicals

Question 4

Mediators derived from phospholipids

Answer 4

The main phospholipid-derived mediators are the eicosanoids (prostanoids and leukotrienes) and platelet-activating factor (PAF).

Phospholipids ——-phospholipase A2—> arachidonic acid

Arachidonate is metabolized

by cyclo-oxygenases (COX-1 or COX-2) to prostanoids

by 5-lipoxygenase to leukotrienes.

Arachidonic acid is the precursor of eicosanoids (prostaglandins, thromboxanes, and leukotrienes).

Question 5

Describe the therapeutic effects of NSAIDs including acetaminophen (2)

Answer 5

NSAIDs such as aspirin and ibuprofen block the formation of prostaglandins and thromboxanes by inhibiting cyclooxygenase (prostaglandin H2 synthase)

NSAIDs block the production of certain body chemicals that cause inflammation. NSAIDs are good at treating pain caused by slow tissue damage, such as arthritis pain. NSAIDs also work well fighting back pain, menstrual cramps and headaches.

Question 6

Production of protaglandins (PG’S)

Question 7

why can acetylsalicyclic acid (ASA) exacerbate asthma attack?

Answer 7

When medications such as NSAIDs or aspirin block the COX-1 enzyme, production of thromboxane and some anti-inflammatory prostaglandins is decreased, and in patients with aspirin-induced asthma, this results in the overproduction of pro-inflammatory leukotrienes, which can cause severe exacerbations of asthma

Question 8

Interventions into the pain pathway

Three broad groups:

Answer 8

Nonsteroidal anti-inflammatory drugs (NSAIDs)

• Opioids
• Adjuvants

antidepressants
anti-seizure medications
CNS antispasmodics
sedatives or anti-anxiety medications botulinum toxin A

Question 9

NSAIDS—Side Effects GI complications

Answer 9

COX-1 is constitutively expressed and is involved in physiological functions such as gastric protection and hemostasis