3/27/17 Prostanoids & Anti Inflammatory Drugs SMITH TEST #3 Flashcards
What is the body’s normal protective response to an injury, irritation, or even surgery?
-Acute inflammation
What has a purpose to eliminate the initial cause of cell injury, clear out necrotic cells and tissues damaged from the original insult and the inflammatory process, and to initiate tissue repair?
-Acute inflammation
What is the goal of therapy with anti-inflammatory drugs?
- Decrease inflammation
- Decrease Pain
- Arrest tissue damage
- Preserve function
What type of inflammation uses innate immunity?
-Acute inflammation
What type of inflammation uses adaptive immunity?
-Chronic inflammation
What is the duration for acute inflammation?
-Short (days)
What type of inflammation uses the cardinal signs of pain, heat, redness, swelling, and loss of function?
-Acute inflammation
What type of inflammation does not have to have any of the cardinal signs?
-Chronic inflammation
What type of inflammation uses neutrophils and macrophages?
-Acute inflammation
What type of inflammation uses Lymphocytes (B and T cells), Macrophages, and fibroblasts?
-Chronic inflammation
If you have fluid exudation and edema what type of inflammation do you have?
-Acute inflammation
If you have fibrosis and angiogenesis what type of inflammation do you have?
-Chronic inflammation
If you have a high grade fever will you have acute or chronic inflammation?
-Acute inflammation
What are the primary mediators for acute inflammation?
- Vasoactive amines (serotonin, histamine)
- Eicosanoids (prostaglandins, thromboxane)
What are the three major classes of anti-inflammatory drugs?
- NSAIDS
- Glucocorticoids
- DMARDs
Which major class of anti-inflammatory drugs inhibit cyclooxygenase enzymes?
-NSAIDs
Which major class of anti-inflammatory drugs inhibit phospholipase A2 (PLA2)?
-Glucocoriticoids
Which major class of anti-inflammatory drugs is prednisone, and cortisone found in?
-Glucocorticoids
What do Biologic DMARDs inhibit?
-TNF
What is an oxygenated product of poly-unsaturated long-chain fatty acids (arachidonic acid) known as?
-Eicosanoids
What type of crine fashion do eicosanoids act in
- Autocrine
- Paracrine
Eicosanoids are what type of proteins?
-G-coupled proteins
Prostanoids is a subclassification of what?
-Eicosanoids
What are three types of prostanoids?
- Prostaglandins
- Thromboxanes
- Prostacyclins
What type of prostanoid is a mediator of inflammatory and anaphylactic reactions?
-Prostaglandins
What type of prostanoid is a mediator of vasoconstriction?
-Thromboxanes
What type of prostanoid is active in the resolution phase of inflammation?
-Prostacyclins
What are five things that prostanoids have a major biological effect on?
- Smooth muscle
- Platelets and blood cells
- Nerve terminals
- Endocrine organs
- Adipose tissue
What COX selective inhibitors do not inhibit platelet aggregation or cause GI upset/ulceration?
-COX-2
Is Aspirin a selective or nonselective COX inhibitor?
It is a nonselective COX-1 and COX-2 inhibitor
What is the only NSAID to inhibit both COXs in an irreversible manner?
-Aspirin
What does antipyretic mean?
-Reduce fever
What does analgesic mean?
-Reduce pain
What three things can aspiring do?
- Antipyretic
- Analgesic
- Anti-inflammatory
Who should you avoid giving aspirin to?
- CHildren with Reye syndrome
- People is NSAID allergies
- People with hemophilia
What is aspirin valued primarily for?
-Anti-platelet aggregation effects
What NSAID is a derivative of propionic acid?
-Ibuprofen
What three effects does Ibuprofen have?
- Analgesic
- Antipyretic
- Anti-inflammatory
What drug interferes with the antiplatelet effect of low-dose aspirin rendering aspirin less effective for MI and stroke prevention if taken together?
-Ibuprofen
For ibuprofen to have an anti-inflammatory effect what amount do you have to take?
> 2400 mg/day
What NSAID is available in slow-release formulation and is “all day strong”?
-Naproxen
If you give NSAIDs to children who are recovering from a viral-induced illness what might they develop?
-Reye syndrome
What type of COX inhibitor or Celecoxib?
-COX-2 selective
What NSAID drug has no effect on platelet aggregation?
-Celecoxib
What drug is known as a non-aspirin pain reliever?
-Acetominophen
Is acetominophen an NSAID?
-No it is not an anti-inflammatory
Should you use acetominophen is someone who has liver disease?
-No
What drug prevents conversion of membrane phospholipids to arachidonic acid by inhibiting the phospholipase A2 enzyme?
-Glucocorticoids
What drugs block the prostaglandin pathway only?
-COX inhibitors
What are three short to medium acting GCs?
- Hydrocortisone
- Cortisone
- Prednisone
What is a long acting GC?
-Dexamethasone
What drugs are used clinically to treat diseases caused by an overactive immune system?
-Glucocorticoids
What is the mechanism of action of Prednisone?
-Blocks phospholipase A2, thus shuts down immune responses
What is the 1st line DMARD for RA (Rheumatoid arthritis)?
-Methotrexate
What is the mechanism of methotrexate?
-Inhibits transformylase & thymidylate synthetase
What is a major contraindication of methotrexate?
-Do not use in pregnancy
Methotrexate can cause a risk of serious, life threatening adverse effects, and they are increased if taking what other type of drug?
-NSAIDs
What drug is a prodrug that acts through its main metabolite, 6-thioguanine, to strongly suppress DNA synthesis and production?
-Asathioprine (imuran)
What type of DMARD is a large molecule?
-Biologic DMARDs
What is the mechanism of Abatacept (a Biologic DMARD)?
- Acts as fusion protein to prevent activation of T-cells
What drug do you use for the treatment of RA in patients whom have failed or are inadequately responding to anti-TNFalpha therapy?
-Abatacept
What is the mechanism of Adalimumab (Humira)?
-Prevents ligand from binding to TNFalpha receptor
What are five different TNF alpha inhibiting biologic DMARDs?
- Infliximab (Remicade)
- Adalimumab (Humira)
- Certolizumab pegol (Cimzia)
- Golimumab (Simponi)
