Lectures 1-2
This is intended to heal or relieve a disorder.
What is medical therapy.
In a graded response curve, as the dosage of the drug is increased, the magnitude of this also increases.
What is physiological response.
This type of ligand will bind to a different site on the receptor and prevents the receptor from responding to a ligand.
Bonus: This is what an allosteric antagonist will impact.
What is non-competitive/allosteric antagonism.
Bonus: reduce efficacy, but not potency.
D in LADME.
Distribution
These types of parenteral administration has less than 100% bioavailability.
What are transdermal, nasal, and inhalational.
A. Hydrophobic
B. Hydrophilic
What is hydrophobic.
What is lower affinity of drug to receptor.
See Separate Document.
Highest potency
Lowest Efficacy.
This is the definition of bioavailability.
The proportion of a drug that enters circulation after administration.
Define bioequivalent and therapeutic equivlence.
Bioequivalent - two products pharmaceutically equivalent and biovailabilities equivalent so drug effects essentially the same. (ex: brand drug vs. generics)
Therapeutic equivalence - drug same pharmacological effect w/o being chemically equivalent.
What is voltage gated ion channel.
This is the concentration of a drug in which 50% of receptors are bound.
What is EC50.
This type of ligand binds to the receptor that is already in an active state and stabilizes and inactivates it, thus reducing basal activity.
What is inverse agonist.
Major routes of elimination are:
This is a major carrier protein for hydrophobic molecules in the plasma.
What is albumin.
A. 4.5
B. 5.5
C. 6.5
D. 7.5
E. 8.5
A. 4.5
Remember acids negatively charged when lose proton, so want the majority of the acid to be protonated which would be a neutral charge and more easily absorbed than a charged molecule.
narrow
TD50/ED50
An antagonist that functions on a completely different receptor causing a physiological effect that is opposite the action of an agonist is this type of antagonism.
What is functional antagonism.
Example of this is bronchodilation to reverse the effects of bronchoconstriction. (2 different receptors)
These enteral routes largely avoid first pass metabolism.
What are sublingual and buccal. Rectal can as well depending on insertion location.
This is an efflux pump that can be found in many cell types that pumps toxic substances (ie xenobiotics) back into intestinal lumen.
What is p-glycoprotein.
You have a weak base, pKa 7.6, that you need to eliminate via the urine. Which pH do you need your urine to ensure maximum elimination of the base?
A. 5.6
B. 6.6
C. 7.6
D. 8.6
E. 9.6
A. 5.6
Think of this in reverse of absorption, once you get the molecule across into the lumen, you want the molecule to be charged which will keep it from traveling back across into the body. Bases are charged when protonated, so the lower the pH of the urine, the more charged the base.
This is the difference between a quantal dose response curve and a graded response curve.
Quantal dose response curve refers to the population.
See separate document.
Lowest potency.
Competitive Antagonist
Partial Agonist
Bonus: enteral or parenteral?
What is subcutaneous.
Bonus: Parenteral
Transfer of the drug from site of delivery to blood stream is absorption. This is another term for blood plasma.
Bonus: This route directly delivers to the blood plasma.
What is central compartment.
Bonus: IV