Chapter 8 Objectives

Question 1

What are the two major categories of analgesics?

Answer 1

Centrally-acting opioid (narcotic) analgesic

Peripherally-acting non-opioid analgesic

Question 2

What are eight other classes of drugs that have been used to provide pain relief in certain circumstances?

Answer 2

1. Alpha 2-adrenergic agonists (clonidine)
2. Beta-blockers (antagonists)
3. Ca++ channel blockers (antagonists)
4. TCA’s (tricyclic antidepressants)
5. Serotonin rc agonists (SSRI’s)
6. Na+ channel blockers (local anesthetics)
7. General vasoconstrictors: ergotamine (sympathomimetic)
8. Sedatives and anxiolytics

Question 3

Define opiate/opioid.

Answer 3

Naturally occurring mu-receptor agonists derived from opium to include opium, morphine, and codeine.
***Opioids, natural(opiates) or synthetic, are all mu-receptor agonists.

Question 4

Define narcotics.

Answer 4

Pertaining to or producing narcosis. Any schedule 1 controlled substance regulated by the CSA of 1973 to include heroin, methamphetamine, and LSD.

Question 5

What are the therapeutic effects of opioid analgesics?

Answer 5

Pain relief properties and cough suppression.

Question 6

What are common side effects of opioids and give an example of how they can be used therapeutically?

Answer 6

Sedation to the point of respiratory depression, urinary retention, constipation, and euphoria (individual variations). Example: constipation to treat diarrhea, treatment of anxiety.

Question 7

Define NSAID.

Answer 7

A group of widely used aspirin-like drugs know as non-steroidal antiinflammatory inhibitors. Aspirin was the first discovered, followed by other “salicylates”. Over 20 Rx medicines of this type available. Used to block the eicosanoids; prostaglandins (PG) & thromboxanes.

Question 8

Why is aspirin considered the prototype of NSAID’s?

Answer 8

It was the first of it’s class to inhibit part of the inflammatory pathway called the arachidonic acid (AA) cascade. Steroids were already known to do this so it is the first in its class of NSAID’s

Question 9

What effect do NSAID’s have on the arachadonic acid (AA) cascade?

Answer 9

Work by blocking a group of localized hormones called eicosanoids (prostaglandins, thromboxanes, and leukotrienes. These are formed in response to trauma and control many normal body processes like pain, inflammation, fever, and muscle cramps.

Question 10

What are the drug properties of NSAID’s?

Answer 10

Analgesia(inhibition of prostaglandins), anti-inflammation(inhibition of PG’s), antipyresis(fever reduction), and anticoagulation(prevent platelet aggregation; mainly aspirin).

Question 11

Name 3 common salicylates.

Answer 11

aspirin/acetylsalicylic acid(Bayer), magnesium salicylate(Doan’s pills), and sodium salicylate(Alka-Seltzer, Pepto-Bismol)

Question 12

Describe 4 therapeutic effects of aspirin.

Answer 12

Same as NSAID’s except platelet inhibition. Analgesia, Anti-inflammation, Antipyresis, & Anticoagulation.

Question 13

What are common side effects of aspirin?

Answer 13

Peptic ulcer disease (PUD; because of inhibition of “protective prostaglandins”), GI bleeding, ringing of the ears, Reye’s syndrome

Question 14

Reye’s syndrome

Answer 14

Associated with aspirin. A disorder of the liver and brain. Occurs in children under 16 while taking salicylates during a viral infection.

Question 15

Describe the mechanism of COX-2 inhibitors.

Answer 15

Only found in areas of inflammation compared to COX-1 which are found throughout the body. Have fewer adverse gastric effects. Long term use has shown higher incidence of stroke & heart attack. All but one drug (Celebrex) have been removed from the market.

Question 16

Name the properties of the drug acetaminophen that make it unique.

Answer 16

Derived from coal tar, part of a drug class called aniline analgesics(only one still in use today). Action at the molecular level is still unknown but may suppress the COX-2 enzyme similarly to Celebrex. Not grouped with NSAID’s due to unknown mechanism of action. Causes very little stomach irritation & no measurable platelet effect.

Question 17

What is the most commonly used over-the-counter drug for the safe & effective treatment of pain(analgesic) and fever(antipyretic)?

Answer 17

acetaminophen

Question 18

What are 2 reasons why nonnarcotic & narcotic drugs are often used together in combination analgesics?

Answer 18

1. Combining peripherally acting drugs (NSAID’s) with centrally acting drugs (opioids) has a synergistic, potentiating effect.
2. Fewer of each type of drug can be used which often means fewer side effects.
   * **Problems arise when consumers don’t look at labeling.

Question 19

Describe the major toxicity from combining acetaminophen products to produce an overdose.

Answer 19

Overdose occurs frequently due to the wide use of the drug in OTC products. Causes liver damage & is one of the leading causes of liver failure. Parents need to be especially careful.

Question 20

What drug classes/categories (other than NSAIDs or opioids) are used to treat migraine headaches and other pain syndromes?

Answer 20

ergotamine (powerful vasoconstrictor), beta-blockers and CCB, TCA and SSRI antidepressants, and a few antiseizure & antipsychotic drugs are also used.

Question 21

Serotonin (5-HT-1B receptor agonist) triptan drugs

Answer 21

The most helpful group of medications for the treatment of vascular headaches, Imitrex(sumatriptan) was the first and is the prototype.