General Flashcards
Permissive drug
1) Allows other drugs to reach their full capacity
2) Cortisol for norepinephrine (cortisol increases alpha 1 receptors)
Decreased drug responsiveness with repeated administration
Tachyphylaxis
Combination of two drugs that creates an effect that is equal to the sum of the effects from the individual drugs
Additive
Combination of two drugs that creates an effect greater than the sum of the individual drugs effects
Synergistic
Drug used for cyanide poisoning?
1) Amyl nitrite
2) Thiosulfate
Drug used for iron poisoning?
1) Deferoxamine (chelating agent)
Drug used for arsenic poisoning? What does arsenic inhibit?
1) Dimercaprol
2) Lipoic acid (results in Pyruvate dehydrogenase and alpha ketoglutarate impairment)
How many drug half lives does it take for it to be completely removed from the system?
1) 4-5 half lives
How do you calculate a half life?
t1/2 = (V x .7)/Clearance
Study of drug effects and their mechanism of action; “What drugs do to you”
Pharmacodynamics
Quantitative descriptions of the time course of drug and drug metabolite; “What the body does to the drug”
Pharmacokinetics
What is inversely related to the affinity of an enzyme to its substrate?
Km
- Low Km = High affinity (seen in hexokinase)
What does a high Km mean?
Low affinity for substrate
Proportional to enzyme concentration
Vmax
What are the x and y axis on a lineweaver burk plot
1) X axis = 1/S(concentration substrate)
2) y axis = 1/V
As the y intercept increases on the lieweaver burk plot what happens to Vmax
1) Vmax decreases
Inhibitor that resembles the substrate, binds to the active site, increases Km (decreases affinity)
Competitive inhibitor
How can a competitive inhibitor be overcome?
Increase the substrate
Inhibitor that does not resemble the substrate, does not bind to the active site, decreases the Vmax
Non-competitive inhibitor
Fraction of administered drug that reaches the systemic circulation unchanged
Bioavailability (F)
What is the bioavailablility of an IV drug
100% (all of it reaches the systemic circulation unchanged)
How do you calculate volume of distribution
V = amount of drug in body divided by plasma drug concentration
What order of elimination are half lives only applicable to?
1) First order elimination
How do you calculate Clearance of a drug?
Cl = rate of elimination divided plasma concentration
How do you calculate a loading dose?
Loading dose = Cp x (Vd/F)
- Cp = target plasma concentration
- F = bioavailability
How do you calculate maintenance dose?
Maintenance dose = Cp x CL/F
Elimination rate that is constant regardless of target plasma concentration; Decreases linear with time
Zero order elimination
What drugs have zero order elimination?
Think: PEA (pea is round, shaped like the 0 in zero order)
1) Phenytoin
2) Ethanol
3) Aspirin (at high or toxic concentration)
Elimination rate that is directly proportional to concentration of drug
First order elimination
What determines whether a drug is reabsorbed or excreted in the urine?
1) If the drug is in its neutral form
How do you ensure a weak acid is excreted in the urine? weak base?
1) Make the urine basic (give bicarb) so that it remains in its ionized form
2) Make the urine acidic (give ammonium chloride) so that it becomes ionized
What phase of drug metabolism includes reduction, oxidation, and hydrolysis with P-450
Phase I
what is the result of phase I drug metabolism?
Production of water-soluble metabolites
What phase of drug metabolism is lost as we grow older
Phase I
What phase of drug metabolism includes conjugation yielding very polar, inactive metabolites
Phase II