Pharmacology: Non Opiates

Front 1

Actions from stimuli to cell

Back 1

• Stimuli=physical, chem., bacterial, hormonal
• →arachidonic acid—cyclooxygenase 1 and 2
• cyclo 1→produce prostaglandins→physiological/protective(good!)
• cyclo 2→prostaglandins→pathological response (bad!)

Front 2

Physiologic Response

Back 2

• Cyclo 1→protect the body
o GI-decrease gas, increase mucous production, increase blood flow to GI tract
o Renal-maintain blood flow
o Smooth muscle-blood flow

Front 3

Pathological response

Back 3

• Not good
o Cause inflammation
o Vasodilitation (swelling at pain site)
o Edema
o Warmth (temp increase)
o White blood cells
o Cytokins→increase inflammatory and pain response

Front 4

Non Opiate Mechanism

Back 4

• NOT selective
• Cyclooxygenase blockers (BOTH 1 and 2)
o Block phys and path sites

Front 5

Acertlsalicyclic Acid (ASA)

Back 5

• Prototype Aspirin
• Analgesic-will relieve mild pain (1-3)
• Anti-inflammatory
• Antipyretic-decrease temp at hypothalamus
o Causes some sweating
• Antithrombotic-stop clotting

Front 6

Anti-thrombotic effect of ASA

Back 6

• Bind irreversible to platelets for the rest of the platelets life
• Platelets last 7-10 days
• →bound→wont aggregate/stick together to form clots

Front 7

Therapeutic use of ASA

Back 7

• Relieve mild pain
• Reduce fever

Front 8

ASA adverse effects

Back 8

• Longer you take it and higher dose→more adverse
o Tinnitus-reversable hearing loss
o Reye’s syndrome-high BP→brain damage/death
• Associated w giving to kids under 12 years old
 For virus
o N/V
o GI-ulceration, bleeding
o Pregnancy-birth defects
o ASA sensitive asthma
o poisoning

Front 9

Proper dose of ASA

Back 9

• For analgesic (pain relieving use)-2 pills (325x2=650mg_ every 4-6 hours PRN
• Antipyretic use (decrease temp)-1-2 pills every 4-6 hours as fever>101
• Antithrombotic-85 mg a day (baby aspirin)

Front 10

Overdose of ASA

Back 10

• If within 1hr/1.5 hr→do gastric lavage (tube in esophagus)
• Over hr→not a lot can be done but support patient
o Confusion, sweating hyperventilation (breath faster to blow off CO2 to compensate for rise in acid)
o Stupor, life threatening

Front 11

Non Stroidal Anti Inflammatory Drugs (NSAID

Back 11

• PROTOTYPE-ibuprofen (advil)

Front 12

Advil

Back 12

• NSAID
• Analgesic
• Anti-inflammatory
• Antipyretic (reduce fever)
• Anti thrombotic (reduce clotting)

Front 13

Anti thrombotic effect of NSAID

Back 13

• Bind to platelet ONLY as long as the drug is in circulation
• Have to take it every 4 hours to prevent MI

Front 14

Advil vs Aspirin

Back 14

• Platelets bound only while advil in circulation
o Platelets bound to aspirin for platelet life
• Advil-OK for children under 12
o Aspirin-NOT OK
• Advil-preganacy use unsure→contact doctor
o Aspirin-NOT OK
• Advil-more expensive
• Advil not proven to be more affective

Front 15

Adverse effects of NSAID

Back 15

• CNS-
• GI-NV, gastric ulceration and bleeding
• Liver-toxicity
• Kidneys-damage
• Bad for eyes
• Bleeding risk with interactions with steroids, alcohol, etc

Front 16

Acetaminophen

Back 16

• Prototype-acetaminophen (Tylenol)
• Metabolized in liver→excreted in kidneys

Front 17

Therapeutic effects of tylenol

Back 17

• Analgesic- mild pain relief
• Antipyretic-fever reducer
• NO anti-inflammatory effect
• LITTLE effect on platelets
• LITTLE gastric irritation

Front 18

Uses for acetaminophen

Back 18

• People who don’t tolerate NS and aspirin
• Children under 12
• Children w viruses
• People who don’t need anti-inflammatory effect

Front 19

adverse drug effects for acetaminophen

Back 19

• Hepatic or renal toxicity
• Rash, uticaria, nausea

Front 20

overdose of tylenol

Back 20

• 30 tablets
• within half hr→gastric lavage
• after hr→feel like virus (flu like symtoms)
o →24 hrs later→jaundice, hepatoxicity→elevated liver enzymes
• renal failure and death

Front 21

Muscomyst

Back 21

• Liver protective
• Help from toxicity
• Give to patients who OD on Tylenol

Front 22

Cox2 inhibitors

Back 22

• PROTOTYPE: celecoxib (celebrex)
• Selective cox 2 inhibitoy (allow protective response to continue)
• Analgesic
• Anti-inflammatory
• A little better w stomach protection
• PROBLEM:
o Increases platelet activity→clotting happens more readily
o →increase MI or stroke risk
• black box warning for patients at risk for those things