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Pharmacology II: Exam 2
NSAIDs & Gout
30
Other
Graduate
04/23/2010

Additional Other Flashcards

 


 

Cards

Term

Aspirin:

 

Class?

 

Effects?

 

Mechanism of action?

 

What's it called wo acetyl group?

 

Effects?

Definition

- COX inhibitor

 

- Inhibits synthesis of prostaglandins, thromboxane, prostacyclin

 

- Binds irreversibly, noncompetitive

- Adds acetyl group to amino acid R-group to COX (B) (inhibitor)

 

- Salicylic acid

 

- Antiinflamatory

-Analgesic

-Antipyretic

-Platelet inhibiton

Term

Salicylic acid:

 

Class?

 

 

Definition

- COX (C) inhibitor

 

Term

Acetaminophen (Tylenol):

 

Class?

 

Mechanism of action?

 

Effects?

 

Use?

 

 

Definition

- Non selective COX inhibitor

 

- COX-1&2 inhibition

 

- Analgesic

- Antipyretic

- (Blocks prostaglandin production in hypothalamus)

 

- Alternative to aspirin

Term

Ibuprofen (Motrin, Advil):

 

Class?

 

Why used?

 

Effects?

 

 

Definition

- Nonselective COX inhbitor

 

- Lowest SE

- Less platelet effects

- Less bleeding & GI symptoms

 

- Similar to aspirin

 

Term

Celecoxib (Celebrex):

 

Class?

 

Use?

Definition

- Selective COX inhibitor

- Reversible COX-2 inhibitor

 

 

Term

Gold sodium thiomalate (Myochriysine):

 

Class?

 

Use?

Definition

- Gold salt

 

- Manage rheumatoid arthritis

Term

Prednisone (Deltasone):

 

Use?

 

Effects?

 

When used?

Definition

- Antirheumatic

 

- Induces lipocortin -> inhibits phospholipase A2 & arachidonic acid

- (inhibits production of cytokines, interleukins & tumor necrosis factors)

 

- RA flare-ups

Term

Methotrexate (Rheumatrex):

 

Use?

 

Effects?

 

 

Definition

- Antirheumatic

 

- Inhibits folate reductase -> ↓ folate for DNA synthesis

Term

Probenecid (Benemid):

 

Use?

 

Effect?

Definition

- Prevent gout

 

- Prevents tubular reabsorption

Term

Allopurinol (Zyloprim):

 

Use?

 

Mechanism of action?

Definition

- Prevent gout

 

- Inhibit xanthine oxidase -> blocks formation of uric acid

Term

Colchicine:

 

Use?

 

Mechanism of action?

Definition

- Treat gout

 

- Binds tubulin -> inhibits assembly of micro tubules & motility of inflammatory leukocytes

Term

What is rheumatoid arthritis caused by?

 

Signs/symptoms?

 

What immune responses are involved?

Definition

- Autoimmune 

 

- Chronoic & progressive inflammation & destruction of joints in hands, wrists & feet

- Cardiopulmonary, neurological & ocular inflammation

-> Deformity, disability, death

 

- Humoral

- Cellular

 

Term

What causes osteoarthritis?

 

Signs/symptoms?

 

Effects?

Definition

- Degenerative, weight bearing on joints

 

- Inflammation

- Thinning/destruction of cartridge layer of joints

 

- Bone erosion -> stiffness, pain & muscle weakness

Term

What causes gout?

 

Effects?

 

Where?

 

Signs/symptoms?

Definition

- Overproduction/under excretion of uric acid

 

- Hyperuricemia

-Formation of crystals of monosodium urate monohydrate

 

- Joints & renal tubules

 

- Joint inflammation due to mechanical irritation by urate crystals

Term

Site of action for rheumatoid arthritis drugs:

 

Glucocorticoids?

 

NSAIDs?

 

Methotrexate?

 

Etanercept & inflixmab?

Definition

- Activation of T cells

- Release of IL-2

 

- Activation of macrophages

 

- Production of autoimmune antibodies

 

- Activation of macrophages

- Induction of cytotoxic T cels

- Activation of B cells

Term
What is the role of prostaglandins/related autocoids in pain?
Definition

- Sensitize sensory nerves 

- Amplify pain sensations

Term

What is the role of prostaglandins/related autocoids in inflammation?

 

Definition

- Promote inflammation by stimulation of chemotaxis (from inflammatory cells)

- Vasodilation & ↑ vascular permeability -> edema

Term

What is the role of prostaglandins/related autocoids in fever (above 37)?

 

What drug is used to treat fever?

 

How does it work?

 

NSAIDs do no produce what kind of effect on fever?

 

Definition

- Alter thermoregulatory mechanism in hypothalamus -> new set point 

- Fever by constriction of skin BV

 

- NSAIDs

 

- Inhibit prostaglandin synthesis in hypothalamus

 

- Not nypothermic

Term
Major effects of leukotrienes?
Definition

- VSM: vasoconstriction/vasodilation

- NVSM: Contraction

- Inflammation (↑ vascular permeability)

Term
Major effects of prostaglandin E?
Definition

- VSM: Vasodilation

- Relaxation (bronchioles), contraction (uterus)

- Inhibit GI secretion

Term

Major effects of prostaglandin F?

 

Definition

- VSM: Vasoconstriction 

- NVSM: Contraction (bronchial & uterus)

- (↑ aqueous humor outflow)

Term

Major effects of prostaglandin I?

 

Definition

- VSM: Vasodilation

- NVSM: Contraction

- Inhibition of platelet aggregation

 

Term

Major effects of thromboxane A2?

 

Definition

- VSM: Vasoconstrictor

- NVSM: Contraction

- Stimulate platelet aggregation

Term
What is the role of COX-2 inhibitor?
Definition

- Anti-inflammatory w less GI toxicity

 

Term
Describe the antithrombotic effect of NSAID (aspirin):
Definition

- Irriversible nonselective COX 1 & 2 inhibitor

- Binds to active site (amino acid R group) of COX B

Term
What is the difference between aspirin, Acetaminophen (Tylenol) & ibuprofen (Advil)?
Definition

- Aspirin: irreversible inhibitor of COX 1 & 2. Antiinflamatory, analgesic, antipyretic, platelet effects.

- Acetaminophen: weak COX 1 & 2 inhibition. Antipyretic, Analgesic (pain) .

- Ibuprofen: same as aspirin, less platelet effect. Less bleeding & GI symptoms.

Term

What are the causes of gout?

 

What are the signs & symptoms?

 

What are the 2 types?

 

What are the 2 therapeutic approaches aim to treat gout?

Definition

- Inborn uric acid metabolism dysfunction

 

- Urate crystals deposite in joints, ligaments, skin & kidney

 

- Overproduction

- Under secretion

 

- Treat inflammation

- Treat hyperuricemia

Term
How does allpurinol work in prevention of gout?
Definition
- Prevents conversion to xanthine & plasma uric acid by inhibiting xanathine oxidase
Term

How does probenecid, sulfinpyrazone & salicylates work in prevention of gout?

Definition
- Prevent tubular reabsorption
Term

 

How does diuretics & salicylates work in prevention of gout?

 

Definition
- Prevents tubular secretion
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