Pharmacology Flashcards
What are the four pharmacokinetic phases?
- Administration or Absorption (into circulation)
- Distribution (circulation to target tissues),
- Metabolism (inactivation, usually in the liver),
- Excretion (elimination through biliary secretion, breast milk, saliva, tears and sweat).
What is the difference between pharmacokinetics and pharmacodynamics?
Pharmacokinetics describes what the body does to medications.
Pharmacodynamics describes what the medication does to the body.
What is a narrow therapeutic window (therapeutic index)?
A drug with a narrow therapeutic window means that the concentration of drug required to exert the preferred response is very close to the concentration at which toxic events are likely.
What is drug tolerance?
Drug tolerance occurs when the body makes adaptations due to the constant presence of the drug, and thus the effectiveness of the drug diminishes over time with chronic use.
An athlete who has built up tolerance to a drug should be tapered off of it under MD supervision.
In general, NSAIDs all work by blocking a key mediator of inflammation:
prostaglandins.
Categories of NSAIDs include:
- Aspirin,
- Non-acetylated salicylates (salsalate),
- First-generation NSAIDs (ibuprofen),
- COX-2 inhibitor (celecoxib/Celebrex).
NSAIDs reduce inflammation by inhibiting the enzyme, __________, and thus inhibiting the production of __________.
cyclooxygenase type-2 (COX-2)
prostaglandins
Aspirin, NSAIDs, and salicylates inhibit both COX-2 and COX-1. Inhibition of COX-1 leads to
gastrointestinal adverse effects include dyspepsia, heartburn, nausea, abdominal pain, peptic ulcer and gastrointestinal bleeding.
Yearly in the US, (number) hospitalizations and (number) deaths are due to first-generation NSAIDs.
100,000
16,500
What is considered “chronic NSAID use”?
> 10days
Non-acetylated salicylates and the COX-2 inhibitors have a (lower or higher) risk of gastrointestinal complications?
lower
What are some advantages of topical NSAIDs, such as diclofenac (Flector Patch®, Voltaren Gel®, Pennsaid®), which don’t produce COX-1 inhibition?
Good levels of pain relief in acute sprains, strains, and overuse injuries similar to that of oral NSAIDs, without the common gastrointestinal problems.
Which NSAIDs act as anti-coagulants (have antiplatelet effects)?
Which NSAIDs don’t?
First-generation NSAIDs
Non-acetylated salicylates and the COX-2 inhibitors
Which drugs target pain without effects on inflammation?
Acetaminophen
Opioid Analgesics
What puts the liver at additional risk for an athlete that is using acetaminophen?
older,
have hepatitis,
consume alcohol daily, or
exceed four grams per day
What is the primary accidental overdosed drug in the US?
What is the maximum gram dosage per 24-hour period?
Acetaminophen
4 grams
Opioid medications include:
How do opioids work?
morphine,
codeine,
hydrocodone,
oxycodone and others
They mimic endogenous endorphins, which are neurotransmitters that modulate pain transmission to the brain and spinal cord and induce euphoria. They alter the perception of pain, but do not block inflammation (prostaglandins) or mediate the cause of pain.
What are side effects of opioid use?
Sedation, fatigue, lethargy, drowsiness, dizziness, impaired judgment and/or inability to concentrate.
Constipation, allergic reaction, respiratory distress, hives, anaphylaxis.
What is the general time frame for opioid withdrawal symptoms?
Symptoms usually occur within 6-10 hours after the last dose, and peak on day 2 or 3. Symptoms of withdrawal may last for up to 5 days following the last dose.
What are localized side effects of inhaled corticosteroids?
oropharyngeal candidiasis (thrush) dysphonia (difficulty speaking)
How do rescue inhalers, such as abuterol or levalbuterol, operate?
They stimulate beta-2 receptors on the smooth muscle surrounding bronchioles, causing immediate bronchodilation and quick reversal of acute shortness of air.
Adverse effects of inhaled bronchodilators include:
tremor, nervousness, dizziness, headache, nausea, and tachycardia
How long do short-acting bronchodilators last, as compared to long-acting bronchodilators?
2-3 hours
12 hours
Exercise-induced bronchospasm is due to:
Not warming up
Breathing in cold air
