Pharm 1 Flashcards
(81 cards)
Pharmacokinetics
what the body does to the drug
-ADME
-Concentration of drug in plasma
Pharmacodynamics
what the drug does to the body
- concentration of drug at site of action
- drug effect
Absorption
How administered drugs are absorbed into the body (depends on route).
- Bioavailability bc of first pass
Distribution
How drugs are distributed to the site of action
Depends on: Protein binding, solubility, perfusion to area
Metabolism
Biotransformation of the drug from active form to inactive form (liver-CYP450 enzyme)
Excretion
How the drug leaves the body -> through sweat, bowels, and urine
BEERs Criteria
Used to determine potentially inappropriate medications used in older adults (65+)
Common medications (beta blockers) are on list
Medicare D does not cover so may need GENERIC form
Receptor abundance
age related
Peds and gero = less receptors
Receptor affinity
age related
can change over time
Agonists
CREATES RESPONSE
- Dose dependent
- Dependent on receptor sensitivity
- Full agonist = 100% of desired effect
- Partial agonist = Partial response
Antagonists
creates NO BIOLOGICAL RESPONSE
- Blocks receptors from agonists
- Competes for receptor sites
- Noncompetitive sites
Ex. Beta blockers
Pregnant woman Physiologic Changes
-fat distribution
-hormonal changes
-increased blood volume (dilutional effect)
-Decreased albumin % (less protein to bind to drug, INC free drug circulating)
-Decreased intestinal motility and increased gastric acid
Factors PROMOTING transfer through placenta
-Lipid solubility (Hydrophobic)
-Smaller, lighter molecules
-Unbound or “free drug”
Factors INHIBITING transfer through placenta
-Highly ionized molecules
-Larger, heavier molecules (hydrophilic)
-Drugs with high protein binding
Therapeutic Window
The range of drug concentration in blood between minimally effective and toxic level
-Pill count and patient diary can help monitor adherence
LD50
lethal dose in 50% of recipients
ED50
effective dose in 50% of recipients
Half life
Time required for 50% of the drug to be eliminated from the body
How many half lives is a drug considered fully cleared?
4-5
If the half life is 10 hours, then each 10 hours _____% of what is remaining will be eliminated
50%
Older adults renal function
lower GFR - slower eliminating waste - Longer half-life - inc free drug - inc risk for toxicity
Factors that interfere with elimination
- Renal failure - increases half life–> dose less
- Hepatic disease - impacts prodrugs (CYP450 enzymes) increases half life
- Exercising regularly vs. intermittently (increases blood flow, GI motility, body-temp increased which increases gastric absorption
Properties that affect gastric absorption
GI motility - increased gastric emptying means less breakdown and decreased motility means it sits in the gut longer leaving more time for absorption
Bioavailability
Rate and extent a drug is absorbed from a tablet/capsule and is available at the site of action
Ex. 250mg oral drug -> first pass -> 125 enters the blood = 50% bioavailability