Dynamics

Front 1

4 patters of drug distribution

Back 1

1-largely in vascular system-bound to plasma proteins
2-uniformly in water
3-Conc. in 1 or more sites(may not be site of action)
4- 1,2,3-MOST COMMON

Front 2

What cell makes BBB

Back 2

endothelial cells

Front 3

Loratadine vs Diphenhydramine

Back 3

Loratadine doesnt cross BBB-nondrowsey

Diphen-Does-Drowesy

Front 4

Memb transporter acts as eflux carriers

Back 4

P-glycoprotein

Organic Anion Transporter Polypepti
(OATP)

Front 5

what Increases local permeability

Back 5

Menigeal inflamm.

Encephalic inflamm.

Front 6

Placental Drug transfer depends upon?

Back 6

Lipid Solubility
Degree of plasma binding
Degree of Ionization

Front 7

What is Fetal pH
What does it cause

Back 7

7.0-More acidic than mothers
-Ion trapping

Front 8

Drug transform may render a drug ______, ________, or ____________

Back 8

Benefical, harmful, or ineffective

Front 9

Xenobiotics

Back 9

Foreign subst that enters body

Front 10

Drug metabolism

Back 10

biochem rxns alter drug to be excreted or recycled

Front 11

4 ways drugs are altered into more polar

Back 11

1-Active Drug--->Inactive drug
2. AD--->Excretable drug
3. Inactive prodrug ---->Active drug
4. Unexcretable drug---> excretable

Front 12

Major site of Biotransform.
other significant sites

Back 12

Liver
Kidney, GI tract, skin, and lungs

Front 13

First Pass effect (Phenomenon)

Back 13

Orally admin drug is immedi. inactivated

bypass by IV

Front 14

Phase I rxns

Back 14

Hydrolytic
Oxidative
Reductive

Front 15

Phase II rxns

Back 15

adding Glucoronic acid, sulfate conjugates

Front 16

MFO

Back 16

family of Hemes, monooxygenases
adds one O from O2 to group

Front 17

P450 gets its name from?

Back 17

P=pigment
450=450 nm in reduced form

Front 18

What is P450 associated with

Back 18

NADPH-CYP450-Reductase

Front 19

Where are CYP's in the cell

Back 19

Smooth E.R.

Front 20

Responsable for metabo. of 50% of drugs

Back 20

CYP 3A4

Front 21

1A2-what does it metab also?

Back 21

Activity increased in smokers
-imipramine, warfarin, cipro

Front 22

2C9

Back 22

Absent in !% of whites

Front 23

2C19
what does it metab also?

Back 23

Absent in 15-20% asians
2-5% whites
-Diazepam to Nordiazepam

Front 24

2D6
what does it metab also?

Back 24

Absent in 7% of whites
-Metab. Codeine to morphine

Front 25

2E1

Back 25

Increas. by alcohol

Front 26

Phase II occurs where?
what functional groups?

Back 26

cytosol
-Glucoronic acid
-Acetate
-Sulfate
-Gluthathione
-Amino Acids

Front 27

Inducers of P450?

Back 27

2B1-phenobarb
3A-isoniazid
2E1-ethanol
1A1-pollutants

Front 28

Inhib of P450?

Back 28

Cimetidine
Ketoconazole
Secobarbital
(causes toxic levels)

Front 29

Grapefruit juice inhibits?
chemical name?

Back 29

3A4
Narangenin

Front 30

Where is 3A4 found?
which one is inhib by G.F.J

Back 30

Liver and Intest. wall
-Intest. wall

Front 31

Inhibitors of 3A4

Back 31

Ketoconazole, diltiazem, erythromycin, and narangenin(G.F.)

Front 32

Inducers of 3A4

Back 32

Carbamazepine
rifampicin

Front 33

Golmerular filt. filters?

Back 33

molecules of low mol weight <60,000
most drugs unless bound to proteins

Front 34

Normal GFR?

Back 34

110 to 130mL/min (180 L/DAY)

Front 35

Prox reabsorbs
Requires?

Back 35

Water
energy and carrier

Front 36

Distal tubule

Back 36

passive excretion
reabs. lipid soluble drugs

Front 37

Excretion pathway that is quantitatively unimportant

Back 37

sweat
saliva
tears

Front 38

First Order Kinetics

Back 38

Most drugs follow
rate is prop to amt of drug in body

half life is constant

Front 39

Zero Order

Back 39

Rate is constant and fixed-indep of dosage entering ex ethanol
Half life not constant

Front 40

Vd

Back 40

Volum of Distrib
Amt of drug in body to concen. of drug in plasma or blood
high Vd= high lipid solub
low Vd= lipid insolub

Front 41

Formula for Vd

Back 41

Vd= dose of drug/ [drug] in plasma

Front 42

Compartments in L

Back 42

ICF-25-28
ECF-13-16
Plasma-3-4

Front 43

CL equation

Back 43

CL= Rate of Elim/ C plasma

Front 44

system Cl

Back 44

Cl sys= Cl renal + Cl hepatic +Cl lungs

Front 45

Half life formula

Back 45

T 1/2= .7(Vd)/ CL

Front 46

Significance of Half Life

Back 46

-indic first order eliminat mech.
-design dosage regimens
-prolonged half life=disease or alt of mech.

Front 47

What always gives 100% bioavail.

Back 47

IV
-used to compare against oral route

Front 48

Bioavail effected by?

Back 48

Route of admin
extent of absorp.
First pass effect

Front 49

criteria to be bioequivalence

Back 49

-same active ingred.
-identical in strength and conc.
-same rates and extent of bioavail.

Front 50

Dosing rate formula

Back 50

DR=CL x Desired plasma C

Front 51

Steady rate occurs when?
time relationship to dosage

Back 51

after 4 to 5 half lives
time is independent of dosage

Front 52

Loading Dose

Back 52

LD=Vd x desired plasma C

Front 53

ADME

Back 53

Absorbed
Distributed
Metab.
Eliminated

Front 54

Pharmokinetics

Back 54

dose-circ-distrib-metab or excret

Front 55

Pharmacodynamics

Back 55

Therapuetic action
-toxicity
-Efficacy

Front 56

Absorption

Back 56

Pass of drug thru cells into gen circul.

Front 57

Distribution

Back 57

Blood to ECF of cells

Front 58

Metab

Back 58

drugs into hepatic tissues

Front 59

What determines kinetic prop?

Back 59

Polarity

Front 60

Absorption rate and effic depend upon?

Back 60

route of admin.

Front 61

what route of admin is erratic and incomplete

Back 61

rectal 50% bypasses liver

Front 62

Pharm Equivalents

Back 62

Same active ingred., strength or conc, dosage form and route of admin