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45 Cards in this Set

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What is an Analgesic?

Drugs used for the relief of pain.



Non-opiod Analgesics

-Tylenol


-NSAIDS



Pain Threshold

Level of stimulus needed to create a pain sensation

Acetaminophen - Mechanism of Action

Antipyretic


Analgesic




Inhibits prostaglandin synthesis in the CNS


DOES NOT work on inflammation.



Acetaminophen - Adverse Effects

Rare at therapeutic levels




Interacts with Alcohol, Warfarin




Acute Toxicity


Liver damage and death due to hepatic necrosis.



Treatment of Acetaminophen Toxicity

Mucomyst (Acetylcysteine) - if given within 10 hours, then 100% prevention of severe liver injury.

COX 1 and 2 Enzymes

COX1 found in all tissues and is helpful: housekeeping enzyme.



COX2: Shows up during inflammation

What class of drugs are Cyclooxygenase inhibitors?

NSAIDS




NOT TYLENOL

COX1

Converts arachidonic acid into prostaglandins.



Beneficial!


Protects gastric mucosa, supports renal function, and promotes platelet aggregation

COX2

Harmful


Mediates inflammation, sensitizes receptors to painful stimuli.



First Generation NSAIDS

Inhibit both COX 1 and 2 nonselectively.

Aspirin- Therapeutic Uses

Suppressed Inflammation


Analgesic


Antipyretic


Suppression of platelet aggregation



Aspirin- Adverse Effects

GI Effects


Increased bleeding


Renal Impairment


Salicylism


Reye's Syndrome

Reye's Syndrome

Use of Aspirin for children, increased child mortality rate



Encephalopathy and Fatty Liver degeneration





Aspirin Drug Interactions

Warfarin: Gastric Hemorrhage - both affect blood clotting; high risk of bleeding


Glucocorticoids: Gastric Ulcers


Alcohol: Gastric Bleeding


Ibuprofen: Decreases anti-platelet effect of Aspirin



Salicylism

Aspirin Overdose: Tinnitus, irratibility, dizziness

Ibuprofen

One of the First Generation NSAIDS

Helps with fever, arthritis, dysmennorea

Naproxen

One of the first generation of NSAIDS


Prolonged half lives, so dosing is less frequent

Indocin

First generation NSAID


Arthritis, gout

Toradol

Ketorolac (generic name)


Used only for short term therapy - High kidney toxicity


usually used in cesarean section

Celebrex (celecoxib)

Selective COX-2 Inhibitor


Suppresses inflammation


Less GI side effects





Side effects of celebrex

Linked to CV events


Increased risk of bleeding with coumadin


Cannot take if a sulfa allergy is present

What is an opiod

An analgesic that has properties similar to morphine

Opioid receptors

2 types


Mu and Kappa

Mu Receptors

an opioid receptor responsible for analgesia, respiratory depression, euphoria and sedation



Kappa Receptor

an opioid receptor also responsible for analgesia and sedation

Pure Opioid Agonists

Morphine

Demerol


Fentanyl



Opioid Agonist-Antagonist

Work as antagonists at the mu receptor, but as agonists at the kappa receptor.




Provides low abuse potential, but less analgesic effects

Opioid Antagonists

Acts to block receptors completely


Narcan

Morphine: Mechanism of Action

Mimics actions of endogenous opioids


Works on Mu receptors



Morphine: Therapeutic Use

Pain relief for a variety of reasons


Post-op pain


Cancer


Constant, dull pain.

Morphine: Pharmacokinetics

Can be given PO, IM, IV


NOT lipid soluble


Inactivated by hepatic metabolism

Morphine: Adverse Effects

Respiratory Depression


Constipation (anticholinergic)


Orthostatic Hypotension


Urinary retention


Emesis


Sedation


Increase in intercranial pressure

Morphine: Dependence issues

Tolerance


Physical Dependence: Abstinence syndrome


Sweating, anorexia, irritability, nausea



Morphine: Drug Interactions

CNS Depressants: Alcohol, Benzos


Anticholinergic Drugs: Antihistimines


Hypotensive Drugs


Opioid Antagonists

Morphine Toxicity

Pinpoint Pupils


Respiratory Depression


Coma

What are examples of strong opiods?

Fentanyl


Demerol


Methadonne


Heroin


Dilaudid

Methadone

Strong opioid agonist


Used in alcohol withdrawl


Can become addicted

Demerol

Strong Opioid agonist


Used post surgery

Fentanyl

Mostly transdermal, really easy to abuse

Dilaudid

Small doses can give high amounts of pain relief.

Codeine

Opioid Agonist


Metabolized into a stronger drug in the body - similar to morphine


Has a lot of side effects - anticholinergic effects

Oxycodone

Opioid agonist


Opioid with tylenol



Darvocet

Opioid agonist


more lethal that other moderate opioids



Tramadol

Non-opioid analgesic