Basic Principles

Question 0

Actions of body on drug

Answer 0

Pharmacokinetics

Question 1

Actions of drug on body

Answer 1

Pharmacodynamics

Question 2

Passive movement of non protein bound drugs between blood and extravascular space through small water filled pores
Affected by DRUG CONCENTRATION and CHARGE

Answer 2

Aqueous diffusion
Permeation
Pharmacokinetics

Question 3

Exceptions to aqueous diffusion

Answer 3

Brain
Testes
Eye
Placenta

Question 4

Most important limiting factor for permeation in the BBB and placenta

Answer 4

CONCENTRATION
Lipid Diffusion
Pharmacokinetics

Question 5

Transport NOT GOVERNED BY FICK’s LAW is limited by

Answer 5

CAPACITY
Transport by special carriers
Pharmacokinetics

Question 6

Endocytosis is limited by

Answer 6

CAPACITY

Question 7

Fick’s Law of Diffusion

Answer 7

C1-C2 x surface area x (permeability coefficient/thickness)

Question 8

Implications of Fick’s Law

Absorption is faster in

Answer 8

LARGER SA SI>stomach

THINNER MEMBRANES lungs>skin

Question 9

Partial avoidance of first pass effect

Answer 9

Rectal
SRV: IMV to PV
MRV: IIV to IVC
IRV: IPV to IIV to IVC

Question 10

Slowest route of administration

Answer 10

Topical

Question 11

More evaporation

Less evaporation

Answer 11

Tinctures

Ointments

Question 12

Acidic drugs are bound to

Basic drugs are bound to

Answer 12

Albumin

Orosomucoid

Question 13

Reversible
Shift to R - inc potency - add more S
Examples

Answer 13

Competitive antagonist

Propanolol B blocker and Isoproterenol B agonist

Question 14

Irreversible
Downward shift - Emax lowered
Examples?

Answer 14

Norepinephrine and phenoxybenzamine

Question 15

Binds to a different receptor causing the opposite effect

Examples?

Answer 15

Physiologic antagonists

Histamine and epinephrine

Question 16

Propanolol and thyroid hormone

Answer 16

Inverse agonist
Reduces constitutive activity
Binds with the same receptor to produce opposite effect

Question 17

Interacts directly with drug

Answer 17

Chemical antagonists
Dimercaprol for lead poisoning
Pralidoxime for organophosphate poisoning

Question 18

Tachyphylactic drugs

Answer 18

MED students Love to watch CNN in HD
Metoclopramide
Ephedrine
Dobutamine
LSD
Calcitonin
Nitroglycerin
Nicotine
Hydralazine
Desmopressin

Question 19

Tolerance examples

Answer 19

Depletion of thiol cofactors in nitroglycerin

- glutathione

Question 20

Idiosyncratic drug response

Answer 20

Aplastic anemia / chloramphenicol

Cataracts / allopurinol

Question 21

Vd
Blood
ECF
Tissue

Answer 21

Low
Med
High

Question 22

Amount Vd

Answer 22

Amount of drug in body / plasma drug concentration

Liver and kidney dependent

Question 23

Clearance

Answer 23

Rate of drug elimination / plasma drug concentration

Question 24

Steady state

Answer 24

4-5 half lives

Question 25

Half life

Answer 25

0.693 x vd / cl

Question 26

Maintenance dose

Answer 26

Cl x desired plasma concentration / bioavailability | Vd is NOT involved

Question 27

Cl is NOT involved

Answer 27

Loading dose

Question 28

Corrected dose | Renal disease or reduced cardiac output

Answer 28

Average dose x (Clcr / 100ml/min)

Question 29

Clcr

Answer 29

(Wt x (140-age)) / (72 x serum crea) | x 0.85 in females

Question 30

Phase 1 reactions | CYP3A4 and CYP2D6

Answer 30

``` More water soluble HORDe Hydrolysis Oxidation Reduction Deamination ```

Question 31

Phase 2 reactions

Answer 31

Conjugation to polar groups

Question 32

CP450 Inducers

Answer 32

``` Ethyl Booba takes Phen-Phen and Refuses Greasy Carb Shakes Ethanol Barbidurates Phenytoin Rifampin Griseofulvin Carbamazepine St. John's Wort/Smoking ```

Question 33

CP450 Inhibitors

Answer 33

``` Inhibitors Stop Cyberkids from Eating Grapefruit QV Isoniazid Sulfonamides Cimetidine Erythromycin Grapefruit Quinidine Valproic acid ```

Question 34

Administration of single doses of the agent up to the lethal level in at least 2 species

Answer 34

Acute toxicity | Animal testing

Question 35

Animal testing Acute toxicity Subacute and chronic testing

Answer 35

Pharmacologic profile

Question 36

Reproductive toxicity

Answer 36

Teratogenesis devt defects Mutagenesis heritable Carcinogenesis malignancy

Question 37

A Pregnant Animal Studies Pregnant Human Studies

Answer 37

Safe Safe Folic acid and thyroid hormones

Question 38

B Pregnant Animal Studies Pregnant Human Studies

Answer 38

Safe None Unsafe Safe Zidovudine

Question 39

C Pregnant Animal Studies Pregnant Human Studies

Answer 39

Unsafe None None None Aspirin

Question 40

D Pregnant Animal Studies Pregnant Human Studies

Answer 40

Unsafe Unsafe ACE inhibitors Anti convulsants

Question 41

X Pregnant Animal Studies Pregnant Human Studies

Answer 41

Unsafe Unsafe Statins, OCP, Clomiphene, Misoprostol, High dose Vit A

Question 42

Teratogens | ACE inhibitors

Answer 42

Fetal renal damage

Question 43

In vitro test for mutagenicity

Answer 43

Ames test

Question 44

In vivo test for mutagenicity

Answer 44

Dominant lethal test

Question 45

``` Clinical trials Phase 1 Phase 2 Phase 3 Phase 4 ```

Answer 45

Is it safe? Normal volunteers Except cancer and toxic agents Is it effective? Sick volunteers Is it better? Postmarketing

Question 46

Bioequivalent

Answer 46

Comparable bioavailability | Similar times to achieve peak blood concentrations