Intro to Pharmacology

Question 1

What are the 4 things describe by pharmacokinetics (as opposed to pharmacodynamics)?

Answer 1

1) Absorption
2) Distribution
3) Metabolism
4) Excretion

Question 2

What does pharmacodynamics describe?

Answer 2

Mechanism of action (MOA)

Question 3

What are the two primary types of absorption?

During what methods of administration does each occur? What effects does each have?

Answer 3

1) Intravascular: directly administered into blood
-Systemic
2) Extravascular: all other sites of administration
-Local & systemic

Question 4

1) GI dissolution of drugs administered orally is dependent on what?
2) Most drugs will move from the ___________ to the _____________ via the _____________________.

Answer 4

1) Solubility of drug
2) duodenum; liver; hepatic portal vein

Question 5

What are the two types of transport that allow drugs to leave the gut wall?

Answer 5

1) Passive diffusion across gut wall
2) Active transport via transporter proteins

Question 6

1) Define bioavailability
2) What is it calculated as?

Answer 6

1) Percentage of drug that reaches systemic circulation from site of administration
2) Area under the plasma concentration time curve (AUC)

Question 7

1) Define distribution
2) What 5 factors is it dependent on?

Answer 7

1) Process of drugs moving from systemic circulation to tissues / organs / non-plasma fluids
2) Lipophilicity, molecular weight, solubility, ionization and protein binding (i.e., albumin)

Question 8

1) Define volume of distribution (Vd)
2) How is it calculated?

Answer 8

1) The area of the body in which the drug has been distributed
2) Amnt of drug in body/ concentration of drug in plasma)

Question 9

1) What is the Vd of warfarin? Why?
2) What is the Vd of chloroquine? Why?

Answer 9

1) 8L; warfarin is highly protein bound
2) 15,000L; lipophilic and sequestered in fatty tissue

Question 10

1) What is drug metabolism?
2 Why does it occur?

Answer 10

1) Drug is converted from original form to more hydrophilic metabolite
2) To increase excretion of the compound

Question 11

1) What is the primary site of metabolism?
2) Via what?
3) What phase of metabolism is this?

*(highlighted on ppt)

Answer 11

1) Liver
2) CYP P450 isoenzymes
3) Phase I

Question 12

True or false: most drug metabolizing enzymes exhibit clinically relevant genetic polymorphisms

Answer 12

True

Question 13

1) Define substrate
2) Define inducer
3) Define inhibitor

Answer 13

1) The substance on which an enzyme acts
2) A substance that is capable of activating the transcription of a gene by combining with and inactivating a genetic repressor
3) A substance which slows down or prevents a particular chemical reaction or other process or which reduces the activity of a particular reactant, catalyst, or enzyme

Question 14

List and define the types of drug interactions in order of severity (greatest to least)

Answer 14

1) Contraindicated
2) Major: may be life-threatening and/ or req. medical intervention to minimize or prevent serious adverse ffects
3) Moderate: may result in exacerbation of the pts condition and/ or req. an alteration in therapy
4) Minor: would have limited clinical effects; may incl. an increase in the freq. or severity of side effects (but gen. no maj. alteration in therapy)
5) Unknown

Question 15

1) What is the mnemonic to remember the strongest inducers?
2) What is the mnemonic to remember the strongest inhibitors?
3) Is this an element of pharmacokinetics or dynamics?

*(this is on EVERY EXAM)

Answer 15

1) PS PORCS
2) G PACMAN
3) Pharmacokinetics

Question 16

What are the strongest inducers?

*(this is on EVERY EXAM)

Answer 16

Phenytoin
Smoking
Phenobarbital
Oxcarbazepine
Rifampin (and rifabutin / rifapentine)
Carbamazepine
St. John’s Wort

PS PORCS

Question 17

What are the strongest inhibitors?

*(this is on EVERY EXAM)

Answer 17

Grapefruit
PIs (protease inhibitors)
Azoles
C–cyclosporin & cimetidine
Macrolides –not azithromycin
Amiodarone (and dronedarone)
Non-DHP CCBs (diltiazem and verapamil)

G PACMAN

Question 18

1) Carbamazepine, an inducer, is a ____________ substrate.
2) It gets metabolized by _____________.
3) And it induces _____________, ____________, _____________, ______________ and a few other CYPs that aren’t as relevant.

Answer 18

1) CYP3A4
2) CYP3A4
3) CYP1A2, CYP2C19, CYP2C9, CYP3A4

Question 19

1) Does Fluconazole metabolize very well?
2) ____% of the dose is excreted renally unchanged.
3) It can inhibit what 3 CYPs?

Answer 19

Fluconazole
2) 80%
3) CYP2C19, CYP2C9 and CYP3A4.

Question 20

Define excretion and the 6 places it can occur in the body

Answer 20

Elimination of drug via:
1) Kidneys (urine)
2) Liver (bile)
3) Gut (feces)
4) Lungs (respiratory droplets)
5) Breasts (lactation)
6) Skin (sweat)

Question 21

1) Define clearance (CL).
2) How is it calculated?

Answer 21

1) Rate of drug removal in plasma over time
2) Rate of Elimination (ke) / Concentration

Question 22

1) True or false: Most drugs will be eliminated at a constant rate (i.e., first-order elimination).
2) Define Saturable kinetics (Michaelis-Menten)

Answer 22

1) True
2) Start with first-order elimination, but switch to zero-order elimination when metabolism becomes saturated (some drugs do this)

Question 23

1) Define half-life.
2) How is it calculated?

Answer 23

1) The time required for the drug concentration to decrease by 50%
2) t1/2 = 0.693 / ke

Question 24

1) Define steady state
2) How long does it usually take to reach this?

Answer 24

1) The rate of drug intake equals the rate of drug elimination
2) About 5 half-lives to reach steady state

Question 25

1) What question does pharmacodynamics answer?
2) Give an example

Answer 25

1) “How does this drug work?”
2) Hydrocodone: mu opioid agonist; decreases sensation of pain

Question 26

1) Metoprolol is a _____________ antagonist that ______________ heart rate.
2) What is this description an example of?

Answer 26

1) beta 1; decreases
2) Pharmacodynamics

Question 27

1) Define “legend” in a pharmacology context
2) What are the two types?

Answer 27

1) Requires prescription (Rx) for purchase in US
2) Non-scheduled and scheduled

Question 28

1) Give examples of non-scheduled drugs
2) Define OTC

Answer 28

1) Inhalers, antibiotics, anticoagulants, etc
2) No Rx required

Question 29

Give examples of each level of scheduled drugs

Answer 29

1) Schedule I – LSD
2) Schedule II – USP manufactured cocaine or illegal cocaine, stimulants, opioids, others
3) Schedule III-V – benzodiazepines, sleeping pills, others

Question 30

1) OTC drugs are GRAS; what does this mean?
2) OTC drugs have strict “labeling” requirements regarding claims about what 2 things?

Answer 30

1) GRAS = generally regarded as safe
2) Structure and function

Question 31

1) What 3 groups regulate US drugs?
2) Which of these groups only focuses on controlled substances?

Answer 31

1) FCC, FDA, and DEA
2) DEA

Question 32

Give 12 examples of different types of drug formulations.

Answer 32

1) Oral dissolvable tablet
2) Lozenges
3) Sublingual or buccal tablets, films or sprays
4) Nasal sprays
5) Creams, ointments, gels or topical solutions
6) Ointments are (most lipophilic)
7) Injections (SUBQ, IM, IV)
8) Chewable tablets
9) Tablets and capsules(long-acting or instant)
10) Granules
11) Patches
12) Suppositories and enemas

Question 33

1) What type of drug formulation is the most lipophilic?
2) What are the 3 primary types of injections?
3) What are the 2 main types of tablets and capsules?

Answer 33

1) Ointments
2) SUBQ, IM, IV
3) Long-acting or instant release

Question 34

1) What is the gold standard of experimental studies?
2) Why?
3) What are the two ways this type of study can be designed?

Answer 34

1) Randomized controlled trials (RCT)
2) Show cause and effect
3) Parallel or crossover study design

Question 35

1) What does intent-to-treat design include?
2) What does per protocol design include?
3) Which of these is preferred?

Answer 35

1) All subjects in trial(preferred)
2) Excludes subjects that dropped out the trial OR deviated from the protocol

Question 36

For each of the 3 main phases of FDA drug development studies, describe their purpose, subjects, scope, & length of time

Answer 36

1) Phase 1: Safety, PD, PK; healthy volunteers (usually); 20-80 subjects; 6-12 months
2) Phase 2: Safety and efficacy (dose response); intended population; 100-300 subjects; 1-2 years
3) Phase 3: Safety and efficacy at specified dose and determining labeling; wide range of intended population; 100s-1000s of subjects; 2-3 years

Question 37

What may phase IV studies be used for?

Answer 37

1) Drugs seeking new indications
2) Cmbination phases for cancer drugs
3) IIa & IIb studies to respectively evaluative proof of concept or well-controlled target populations

Question 38

1) Define pharmacoeconomics
2) What does its research do?

Answer 38

1) A collection of descriptive and analytic techniques for evaluating pharmaceutical interventions.
2) Identifies, measures and compares the costs and consequences of pharmaceutical products and services.

Question 39

Define pharmacogenetics

Answer 39

Examines inherited variations in genes that dictate drug response and explores ways that the variation can be used to predict whether a patient will have a good, bad or no response to a drug.

Question 40

1) What indication(s) is Clopidogrel assoc. with? What genotype and what’s the recommendation?
2) What is the clinical significance?

Answer 40

1) Acute coronary syndromes, PAD, Stroke; CYP2C19 genotype; consider alt. treatments for poor metabolizers
2) Clopidogrel isa prodrug; poor metabolizers exhibit higher cardiovascular outcomes compared to normal or extensive metabolizers.

Question 41

1) What indication(s) is Carbamazepine assoc. with? What genotype and what’s the recommendation?
2) What is the clinical significance?

Answer 41

1) Seizures, neuralgia; HLA-B1502 for Asian patients; if positive, do not use unless benefit > risk
2) Serious dermatologic reactions with positive HLA-B1502 allele (SJS or TEN)

Question 42

1) What indication(s) is Herceptin assoc. with? What genotype and what’s the recommendation?
2) What is the clinical significance?

Answer 42

1) Breast and gastric cancer; HER2/neu oncogene; if positive, can use drug
2) HER2/neu over-expression required for use.

Question 43

List the Ophthalmic and otic sig codes

Answer 43

A = ear
O = eye
D = right
S = left
U = both

Question 44

Translate “Ciprofloxacin / dexamethasone (Ciprodex) for Oititis externa IV gtts AS BID x 7 days for ear infection” into normal language

Answer 44

(Intravenous drops??) in left ear twice a day for 7 days

Question 45

1) What does i subq Qday mean?
2) How would you abbreviate one by mouth twice daily ?
3) What does i PR QID mean?
4) How would you abbreviate two by mouth three times daily?

Answer 45

1) One subcutaneous injection once daily
2) i PO BID
3) One per rectum four times daily
4) ii PO TID

Question 46

1) What does APAP mean?
2) What does ASA mean?
3) How would you abbreviate “hours” in an Rx?
4) What does i PO q 8° mean?

Answer 46

1) APAP = acetaminophen
2) ASA = aspirin
3) Degree sign (°)
4) Once by mouth once every 8 hours

Question 47

1) How do you write a sig?

Answer 47

1) Dose – route – frequency – indication

Question 48

Eye drop counseling:
1) Generally, wait __________________ after administration before administering a second drop or different drug with ophthalmic medications
2) Should they be shaken or inverted?
3) Why should the pt not touch the applicator tip?
4) Should you occlude the eye after administration? If not, why? If so, for how long?

Answer 48

1) 5 to 10 minutes
2) Drugs must be gently shaken or inverted prior to use
3) Sterility may be compromised and cause bacterial keratitis
4) Occlude the eye after administration for one minute

Question 49

Eye drop counseling:
1) Whether or not a pt removes / reinserts their contacts depends on what?
2) Drugs with ______________________ require a 15-minute wait prior to reinsertion.
3) What formulation is generally not used while wearing contacts?

Answer 49

1) Formulation
1) benzalkonium chloride (BAK)
2) Ointments

Question 50

What should you tell patients to do regarding ear drops? Why?

Answer 50

Roll in hand prior to use; if drops are too cold they may cause vertigo

Question 51

What Phase 1 CYPs are associated w the most genetic polymorphisms?

Answer 51

CYPs:
1) 3A4/5/7
2) 2E1
3) 2D6
4) 2C19
5) 2C9
6) 1A1/2
7) 2C8/9
(not sure if we need to know more or not)

Question 52

Explain the difference between first-order and zero-order kinetics

Answer 52

First order = a certain percentage each hour
Zero-order = a certain amount (mg) each hour

Question 53

List the 4 types of metabolizers and specify which is normal

Answer 53

1) Poor metabolizers
2) Intermediate metabolizer
3) Extensive metabolizer (normal)
4) Ultra metabolizer

Question 54

True or false: with Rxs, use leading zeros, but not trailing zeros

Answer 54

True