1 Nonsteroidal Anti-Inflammatory Drugs Flashcards

1
Q

NSAID – distinct pharmacologic properties:

A
  1. Ability to decrease inflammation
  2. Ability to relieve mild-to-moderate pain
  3. Ability to decrease elevated body temperature associated with fever
  4. Ability to decrease blood clotting by inhibiting platelet aggregation
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2
Q

Best representative of an NSAID is…

A

Aspirin – acetylsalicylic

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3
Q

Aspirin interferes with biosynthesis of…

A

prostaglandins

In 1970 aspirin was found to inhibit the synthesis of a group of compounds known as prostaglandins.

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4
Q

Prostaglandins

A

They are a group of lipid like compounds that exhibit a wide range of physiologic activities.

They appear to be hormones that act locally to help regulate cell function.

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5
Q

Which type of cells produce prostaglandins?

A

ALL the cells… except blood cells

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6
Q

Prostaglandins, thromboxanes, and leukotrienes are referred to as …

A

Eicosanoid

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7
Q

True or false: The 20-carbon fatty acid prostaglandin is derived from can be metabolized by one specific enzyme.

A

False: The 20-fatty acid can be metabolized by

several enzymes systems

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8
Q

Primary enzyme system involves the _____ enzyme, and synthesizes _________ and _________

A

Cyclooxygenase (COX)

prostaglandins and thromboxanes

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9
Q

Secondary enzyme involves the _____ enzyme, and synthesizes __________

A

lipoxygenase (LOX)

leukotrienes

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10
Q

A drug that blocks COX will eliminate all ________ and ________ synthesis in that cell

A

Prostaglandin and thromboxane

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11
Q

Aspirin are ________ inhibitors, they do not inhibit _______ enzyme

A

Aspirin are cyclooxygenase (COX)
inhibitors,

they do not inhibit lipoxygenase (LOX)enzyme

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12
Q

Leukotrienes mediate what?

A

airway inflammation.

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13
Q

Drugs have been developed to reduce leukotriene-mediated inflammation by blocking _____ enzymes, or by blocking leukotriene
receptors on _______ tissues

A

Block LOX enzymes

Or block receptors on respiratory tissues

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14
Q

Do prostaglandins increase or decrease with inflammation?

A

Increased prostaglandin synthesis is usually detected at the site of local inflammation

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15
Q

What are the roles of Eicosanoids in health and disease? How do you decrease these for treatment?

A

Treat with aspirin to decrease prostaglandins

  • Increased prostaglandins at sites of local inflammation
  • Mediate pain stimuli and increase sensitivity
  • Prostaglandins help elevate body temperature

Increased prostaglandin production accompanies dysmenorrhea

Thromboxanes cause platelet aggregation that result in blood clot formation

Other Pathologies:
• Hypertension 
•Colon Cancer 
• Asthma - increased blood flow 
• DM 
• MS- CNS inflammation
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16
Q

COX – 1: responsible for mediating ___________.

COX2 - produced in ______ cell.

A

COX – 1: responsible for mediating normal cell activity

COX2 - produced in injured cell

17
Q

Aspirin represents the major form of a group drugs known as …

A

the salicylates

18
Q

Aspirin and other NSAIDs are effective in treating:

A
• Mild-to-moderate  pain 
• Headache 
• Toothache 
• Diffuse  muscular aches and
soreness 
• RA 
• OA 
• Post-op (Toradol)
19
Q

The primary NSAID used in treating fever in Adults

A

Aspirin

20
Q

Aspirin is not recommended for use in children with …

A

Rye syndrome, a bleeding disorder

21
Q

Primary problem with Aspirin like drugs is _______.

Caused by the ______________________.

A

Primary problem is gastrointestinal damage.

Caused by the loss of prostaglandins in the mucosal lining

22
Q

What are the benefits of aspirin compared to other NSAIDS?

A
  • NSAIDs have less GI problems
  • NSAIDs are less toxic
  • NSAIDs need a prescription and cost
23
Q

COX 2 selective drugs _____ pain and inflammation

A

Decrease

24
Q

COX 2 selective drugs have ___________ on the stomach

A

No adverse effects

They’re coated and dont kill good prostaglandins

25
Q

COX2 selective drugs ________ platelets

A

Do not effect platelets because they leave thromboxins alone

26
Q

COX2 selective drugs are ______ for patients with prolonged bleeding

A

Prolonged

27
Q

COX2 selective drugs ________ risk of upper respiratory tract infections

A

Increase

28
Q

Acetaminophen (Tylenol) compared to aspirin or NSAIDs

A

Fever reducer: Tylenol= Aspirin

Analgesic: Tylenol: Aspirin

Anti-inflammatory: Aspirin> tylenol

Anticoagulant: Aspirin > Tylenol

GI health: Tylenol > Aspirin

Reye Syndrome: Tylenol > Aspirin

29
Q

What is the number 1 drug used to OA?

A

Tylenol

30
Q

Pharmacokinetics of NSAIDs and Acetaminophen

A

Aspirin absorbed in stomach and small intestine

80-90% bound to plasma proteins
10-20% distributed throughout body

Biotransformed in blood stream
Metabolites oxidized in the liver

People with preexisting liver disease or who are chronic alcohol abusers are susceptible to liver damage