lecture 1

Question 1

Intracellular Receptors

Answer 1

• Bind ligands that are very LIPOPHILIC
• Liigand diffuses through cell membranes to interact with its receptor

Question 2

Receptors with Intrinsic enzymatic activity

Answer 2

• Single membrane spanning domain
• Ligand binds to extracellular domain that turns on switch inside the cell

–> commonly activates protein and lipid kinase cascades that leads to protein phosphatases

Question 3

receptors that directly associate with intracellular enzymes

Answer 3

transmembrane receptor associated with enzyme

• receptor can associate with kianses or proteases

Question 4

Ligand-gated ion channel

Answer 4

• binding of a ligand to the channel opens up the pore
• allows ions to move down concentration gradient

Question 5

7-membrane spanning receptor

Answer 5

• G-protein
• coupling to G-protein liberates one of the subunit that turns on downstream signaling events

Question 6

describe the variation of receptor availability

Answer 6

• Receptor availability is dynamic
• Continued STIMULATION/ACTIVATION of receptor leads to DOWNREGULATION (DECREASE drug-induced response)
• Continued exposure of a recetpor to INHIBITOR may cause UPREGULATION (Observation of phsyiological response despite presence of inhibitor)

Question 7

define Potency

Answer 7

• Measurement of drug dose used to compare the relative affinity and effectiveness of two or more drugs
• most conveniently done by comparing the EC50 of two or more agents

(EC50 = concentration of drug that produces a half maximal effect)

Question 8

define eficacy

Answer 8

• the maximal effect a drug can induce (Emax)

Question 9

define Bmax and Kd

Answer 9

• Bmax = maximum binding/all receptors are full
• Kd = ligand concentration at a point where 1/2 your receptors are free (represents the affinity of a ligand for tis receptors)

Question 10

define pharmacy

Answer 10

science and profession concerned with the preparation, storage, dispensing and proper utilization of drug products

Question 11

define pharmacology

Answer 11

pharmacology is the biomedical science concerned with the interaction of chemical substances with living cells, tissues and organisms. It is particularly concerned with the mechanisms by which drugs counteract the manifestations of disease

Question 12

define toxicology

Answer 12

Toxicology is the science of poisons and toxicity. It focuses on the harmful effects of drugs and other chemicals and on the mechanisms by which toxic agents produce pathological changes, disease and death.

Question 13

define pharmacokinetics

Answer 13

divison of pharmacology focused on processes that affect drug concentration in the body. These processes include absorption, distribution, metabolism and elimination. Kinetic parameters will AFFECT the DRUF BIOAVAILABILITY

Question 14

define pharmacodynamics

Answer 14

division of pharmacology focused on how a drug produces an effect. Area of interest when studying pharmacodynamics would include drug targets or receptors, signal transduction pathways regulated by drugs and the physiological and therapeutic effects caused by particular agent

Question 15

describe phase 1

Answer 15

• Limits of safe dosing range
• small number of subjects
• Is it safe?

Question 16

phase 2

Answer 16

• Does it work?
• relatively small number of subjects (more than phase 1)

Question 17

phase 3

Answer 17

• well controlled, more patients (randomized double-blind study)
• larger number of people

Question 18

phase 4

Answer 18

• monitor during clinical use
• postmarketing surveillance

Question 19

animal testin

Answer 19

• experimentation
• drug characterization (molecular, cellular etc)
• TOXICITY (MINIMAL LETHAL DOSE)