Introduction to Pharmacology

Question 1

What is an adverse drug reaction?

Answer 1

A response to a drug which is noxious and unintended, and which occurs at doses normally used in man

Question 2

List 4 factors that may predispose patients to develop ADRS.

Answer 2

1. Use of unlicensed and off-label prescribing
2. Different pharmacokinetic and pharmacodynamics
3. Overdosing
4. Under-reporting: studies show that between 45%-92% of ADRs are identified

Question 3

List 8 medications involved in adverse events requiring an ED visit.

Answer 3

1. Insulin (most common)
2. Antibiotics
3. Anticoagulants
4. Aspirin
5. Ibuprofen
6. Acetaminophen
7. Hydrocodone
8. Intentional overdoses

Question 4

What is the true rate of adherence for appropriate drug use?

Answer 4

50%

Question 5

What are the adherence rates if medication is dosed 1x/day? 2x/day? 3x/day?

Answer 5

1x/day = 73%
2x/day = 70%
3x/day = 52%

Question 6

List 3 steps of the pre-clinical development process of a drug.

Answer 6

1. Target Audience or Disease is identified
2. Chemists generate compounds
3. Pharmacologists perform testing on cells and animals

Question 7

What are the 4 phases of the drug development process?

Answer 7

Phase I: Safety
Phase 2: Safety and Effectiveness
Phase 3: Safety and Effectiveness
Phase 4: Safety (Post-marketing Surveillance)

Question 8

What takes place during phase 3 of the drug development process?

Answer 8

Phase 3: Safety and Effectiveness

Large studies are performed in different countries and populations to assess differences in drug metabolism

Question 9

What takes place during phase 4 of the drug development process?

Answer 9

Post marketing surveillance: drug is being monitored after being released on the marked, for ARDS

Question 10

One should not take a drug until it has been out on the market for at least ____ years.

Answer 10

2 years

Question 11

True or False: Drug naming is consistent.

Answer 11

False

Based on source, chemistry, effects, and regulation

Question 12

What class of drugs are named based on their pharmacotherapuetic action?

Answer 12

Anti-hypertensive drugs

Question 13

What class of drugs are named based on their pharmacological action?

Answer 13

Diuretics

Question 14

What class of drugs are named based on their molecular target?

Answer 14

Beta blockers

Question 15

List the 4 process involved with the pharmacokinetics of a drug.

Answer 15

ADME

1. Absorption
2. Distribution
3. Metabolized
4. Elimination

Question 16

List 6 things that influence the absorption of a drug.

Answer 16

1. Physiochemical properties
2. non-ionized are absorbed better, and acids are absorbed better in low pH (bases are absorbed better in higher pH)
3. Lipid/water coefficient K: lipid soluble drugs are absorbed better
   blood flow to the site of administration
4. Dosage Form: liquid faster than capsules
5. Temperature: higher temps facilitate absorption
6. Exercise

Question 17

Drugs should be taken ____ exercise.

Answer 17

AFTER

Question 18

The distribution of a drug depends on where _____ and presence of ______.

Answer 18

1. Blood flows

2. Plasma proteins (albumin)

Question 19

Why is there decreased drug distribution in patients with liver disease?

Answer 19

Drugs bound to albumin are no longer free to act at target organ.

In liver disease there is low albumin and thus greater free drug availability -leads to toxicity

Question 20

What is volume of distribution? Equation?

Answer 20

Hypothetical concept to describe where the drug exists in the body

Vd = [dose]/[plasma concentration]

Question 21

Describe the difference between a small vs large volume of distribution.

Answer 21

Small Vd : drug will be confined to the plasma compartment –stays mainly in blood stream (eg. heparin and warfarin).

Large Vd: drug can easily pass through the lipid membranes and are distributed widely around the body.

Question 22

What is drug metabolism?

Answer 22

Modifies drug to facilitate excretion (filtered through glomerulus and the excreted in urine)

Question 23

Most drugs are eliminated through the ______.

Answer 23

Kidneys

Question 24

What is bioavailability? What type of drugs are 100% bioavailable?

Answer 24

% of given dose that reaches the systemic circulation.

Drugs given IV are 100% bioavailable

Question 25

Enzyme _____ drugs increase the activity of the enzymes responsible for its metabolism.

Answer 25

Induction

Question 26

Enzyme _____ drugs decrease the activity of the enzymes responsible for its metabolism.

Answer 26

Inhibition

Question 27

What is first order elimination?

Answer 27

Rate of elimination is proportionate to the concentration (a constant % of drug is lost per unit of time)

Question 28

Drugs with first-order elimination have a characteristic ____.

Answer 28

half-life of elimination (t1/2) Time it takes for the concentration to decrease to half the value it had at the start of the dosing interval

Question 29

What is zero order elimination?

Answer 29

A constant amount of drug is lost per unit time.

Question 30

Any drug given through the mouth or into any part of the GI tract is considered ____.

Answer 30

Enteral

Question 31

______ proteins allow the selective passage of specific ions when the ion channel is open.

Answer 31

Transmembrane spanning proteins

Question 32

What is the difference between an agonist and a partial agonist?

Answer 32

1. Agonist is a compound that binds to a receptor and produces a biological response 2. Partial agonist produces a response but cannot produce 100% of the response even at a high dose

Question 33

A _____ blocks or reverses the effect of agonists.

Answer 33

ANTAGONIST

Question 34

List 3 things that decline with age that affect pharmacokinetics.

Answer 34

1. Liver function 2. Renal Clearance 3. Maintenance dose should decrease

Question 35

Why should the maintenance dose decrease with age?

Answer 35

Metabolizing drugs becomes more difficult with age, thus older individuals have more active drug in their blood stream, warranting for a decrease in dosage.

Question 36

True or False: Medication should be taken AFTER exercise. Why or why not?

Answer 36

TRUE Should be taken after exercise because the drug may not be metabolized effectively in the body if taken before exercise due to decrease blood flow to the kidney and liver.

Question 37

List 2 areas that receive decreased blood flow during exercise.

Answer 37

Kidneys | Liver

Question 38

What 3 areas receive increasing blood flow during exercise?

Answer 38

Heart Skin Muscles

Question 39

What types of drugs should be given DURING exercise? Why?

Answer 39

Transdermal patches Why?: increase in heat and blood flow to the skin will result in greater absorption of drugs given transdermally

Question 40

In general expect ____ fold increase in plasma drug levels especially at temperatures higher than ____ degrees C.

Answer 40

1.5-2.5 fold increase 30 degrees C

Question 41

Slowing of gastric emptying when exercise intensity reaches ____ VO2max---delays absorption. Why?

Answer 41

70% Delays absorption because the drug is subjected to degradation from acid secondary to decreased blood flow to the digest tract during exercise.

Question 42

Exercise reduces ____ which results in more rapid drug elimination.

Answer 42

Volume of distribution (Vd)

Question 43

The clearance of ______ ratio drugs depends on blood flow so during exercise there is less metabolism.

Answer 43

High hepatic extraction

Question 44

The clearance of ______ ratio drugs are not affected by change in blood flow during exercise but may be affected by level of fitness.

Answer 44

Low hepatic extraction