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33 Cards in this Set

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  • Back
What gets trapped in urine and is cleared quickly?
Ionized species
What drugs are weak acids? How does this affect their elimination?
- Ex: phenobarbital, methotrexate, aspirin
- Weak acids are trapped in BASIC environments
How do you treat an overdose of a weak acid drug (eg, phenobarbital, methotrexate, aspirin)?
Bicarbonate
What drugs are weak bases? How does this affect their elimination?
- Ex: amphetamines
- Trapped in ACIDIC environment
How do you treat an overdose of a weak base drug (eg, amphetamines)?
Treat overdose of weak base with ammonium chloride
What are the phases of drug metabolism?
- Phase I
- Phase II
What happens in phase I drug metabolism? What does it yield?
- Reduction
- Oxidation
- Hydrolysis with cytochrome P-450
- Usually yields slightly polar, water-soluble metabolites (often still active)
What happens in phase II drug metabolism? What does it yield?
- Conjugation (glucuronidation, acetylation, sulfation)
- Usually yields very polar, inactive metabolites (renally excreted)
What phase of drug metabolism do geriatric patients lose first?
Phase I
- Reduction
- Oxidation
- Hydrolysis w/ cytochrome P-450
What phase of drug metabolism do geriatric patients usually still have?
Phase II
- Conjugation (glucuronidation, acetylation, sulfation)

Geriatric patients have GAS
What type of abnormal drug metabolism in a patient causes greater side effects from certain drugs? Why?
Slow acetylators - decreased rate of metabolism
What is meant by drug "efficacy"?
Maximal effect a drug can produce
What is meant by drug "potency"?
Amount of drug needed for a given effect
What are some examples of high efficacy drug classes?
- Analgesic (pain) meds
- Antibiotics
- Antibiotics
- Antihistamines
- Decongestants
What mediates increased potency of a drug?
Increased affinity for receptor
What are some examples of high potency drug classes?
- Chemotherapeutic (cancer) drugs
- Anti-hypertensive (blood pressure) drugs
- Lipid-lowering (cholesterol) drugs
What is the effect of a competitive antagonist on potency and efficacy?
- Shifts curve to right (decreased potency)
- No change in efficacy
- Shifts curve to right (decreased potency)
- No change in efficacy
How can you overcome a competitive antagonist?
Increase the concentration of agonist substrate
Increase the concentration of agonist substrate
What is the effect of a non-competitive antagonist on potency and efficacy?
Shifts curve down (decreased efficacy)
Shifts curve down (decreased efficacy)
How can you overcome a non-competitive antagonist?
Cannot be overcome by increasing agonist substrate concentration
Cannot be overcome by increasing agonist substrate concentration
What is the effect of an irreversible antagonist on potency and efficacy?
Shifts curve down (decreased efficacy)
How can you overcome an irreversible antagonist?
Cannot be overcome by increasing agonist substrate concentration
What is the effect of a partial agonist on potency and efficacy?
- Acts at same site as full agonist, but with lower maximal effect (decreased efficacy)
- Potency is an independent variable
- Acts at same site as full agonist, but with lower maximal effect (decreased efficacy)
- Potency is an independent variable
What is the relationship of flumazenil to diazepam?
Competitive antagonist at GABA receptor
Competitive antagonist at GABA receptor
What is the relationship of ketamine to glutamate?
Non-competitive antagonist at NMDA receptor
Non-competitive antagonist at NMDA receptor
What is the relationship of phenoxybenzamine to norepinephrine?
Irreversible competitive antagonist on α receptors
What is the relationship of buprenorphine on morphine
Partial agonist at opioid µ receptors
What measurement is used to assess drug safety?
Therapeutic Index
Therapeutic Index
How do you calculate the therapeutic index (TI)?
TI = (TD50 / ED50) = (median toxic dose) / (median effective dose)

TITE: Therapeutic Index = TD50 / ED50
What is the therapeutic window?
Measure of clinical drug effectiveness for a patient
Measure of clinical drug effectiveness for a patient
What relative Therapeutic Index value do safer drugs have?
Higher Therapeutic Index values
Higher Therapeutic Index values
What are some drugs with low Therapeutic Index values?
- Digoxin
- Lithium
- Theophylline
- Warfarin
What value often replaces TD50 in animal studies?
LD50 (lethal median dose)