Fundamentals Tutorial Week 2

Concerning drug receptor interaction, the constant Kd refers to:

G protein-coupled receptors are characterised by:

Which of these is NOT an effect that follows receptor activation?
a. Increase in intracellular cAMP levels
b. Increase in intracellular calcium levels
c. Increase in intracellular IP3 levels
d. Increase in intracellular ATP levels

Which statement is TRUE regarding competitive receptor antagonism?

a. Competitive antagonism is based on reversible antagonist binding at the receptor active site.
b. With competitive antagonism, maximal drug effect is lower
c. With competitive inhibition, maximum drug effect cannot be obtained, even at high agonist concentrations
d. With competitive inhibition, the dose-effects curve is shifted to the left

How is GABA channel changing nerve membrane polarity?

Which drug exerts much of its effects through intracellular receptors?
Select one:
a. Phenytoin
b. Diazepam
c. Fluticasone
d. Flumazenil

Which of the following statements is NOT TRUE regarding the binding site of a receptor?

a. The binding site is normally a hollow or cleft in the surface of a receptor
b. The binding site is normally hydrophobic in nature
c. Ligands fit into binding sites and bind to the functional groups within it
d. Receptor binding site contains amino acids which are important to the binding process

Which of the following reactions is catalyzed by a protein kinase?

a. Phosphorylation of alcohol groups in protein substrates
b. Hydrolysis of phosphate groups in protein substrates
c. Phosphorylation of alcohol groups in carbohydrates
d. Hydrolysis of phosphate groups in ATP and GTP

What determines the degree of movement of a drug between body compartments?

describe drug minimal effective concentration (MEC)?

What indicates amount of a drug absorbed per amount administered?

Bioavailability is a percentage of administered drug that reaches the systemic circulation via a given route as compared to which route?

Given a graph of plasma drug concentration versus time, what part of the graph would be used to calculate bioavailability?

Drug biotransformation Phase I makes drugs ____ polar for metabolism and Phase II makes
drugs ____ polar for excretion

Which of the following is NOT a liver Phase II substrate?

a. Glucuronic acid
b. Sulphate
c. Acetate
d. Alcohol C

Which of the following is the equilibrium dissociation constant, where the concentration of free drug is at half-maximal binding?

Which of the following is increased in intracellular concentration due to signalling molecule
IP3?
Select one:
a. K+
b. Ca++
c. Cl-
d. Na+

Which direction would a PARTIAL agonist shift the dose-response curve when compared to a full
agonist?

Which of the following is NOT an action of the body on a drug?

a. Absorption
b. Distribution
c. Metabolism
d. Drug side effects

What is the correct order of bond strength, from strongest to weakest?