Intro To Pharm

Front 1

Intrathecal admininstration goes into?

Back 1

Subarachnoid space

Front 2

Transdermal drugs can penetrate if they are...?

Back 2

lipophillic

Front 3

Which form of a drug can cross membranes?

Back 3

NON-IONIZED

CHARGED CANNOT CROSS!
ONLY HA OR B

Front 4

If pKa is greater than pH, will drug be in protonated or nonprotonated form?

Back 4

pH is small = LOTS of H+
So drug will be protonated!!

Front 5

If pKa is smaller than pH?

Back 5

pH is large = no H+
so drug will be unprotonated

Front 6

four factors that impact drug distribution?

Back 6

CV (CO, flow, cap perm, plas prot)
Tissue binding
Drug size
Lipid sol

Front 7

What is phase 1 of biotransformation?

Rate limiting step? Primary organ?

Back 7

oxid, red, hydrolytic rxns
MAKE MORE POLAR

CYP enzymes = rate limiting (LIVER)

Front 8

What is phase 2 biotransformation?

Back 8

Conjugation to increase water sol, so can be excreted in bile/feces or back to blood for kidney excretion

Front 9

What is first pass effect?

Back 9

oral drugs absorbed by intestine go through portal vein to liver and exposed to metab enz (inactivated)

Front 10

Renal excretion is dependent on what three things?

Back 10

GFR
binding plasma prot
pH of urine

Front 11

Two mechanisms of excretion into feces?

Back 11

secreted into bile or removed from circ by GI entrocytes back into lumen! (some can be reabsorbed after gut flora work on it)

Front 12

What do intracellular receptors bind and what do they regulate?

Back 12

Lipophillic ligands and change gene activity(transcription)

Front 13

Receptors w/intrinsic enz activity have what types of activity?

Back 13

extracell portion binds and activates intracell enz activity: kinases and phosphatases

*Rec that directly assoc w/enz are similar

Front 14

Ligand-gated ion channel example?

Back 14

nic Ach Rec, hydrophillic core, only one subunit serves as receptor

Front 15

Do 7MSRs have intrinsic enz activity?

Back 15

can be g protein coupled, but not intrinsic enz activity

Front 16

What causes down and up regulation?

Back 16

DOWN = continued activ/stim
(may caused decreased response)

UP = continued inhibitor (increase receptors)

Front 17

What does Kd represent?

Back 17

point at which half the receptors are bound and half are free

represents the affinity of a ligand for its receptor

Front 18

The lower the Kd, the _____ the binding affinity of the drug.

Back 18

GREATER

because it takes less of a concentration to have half of the drug bound

Front 19

What are Emax and EC50?

Back 19

Emax = max effect of a drug
EC50 = concentartion of drug that produces half the max effect!

Front 20

What is potency?

Back 20

Relative affinity & effectiveness of 2+ drugs. SMALLER EC50 IS MORE POTENT!!!! reaches half max effect at smaller dose

Front 21

Efficacy?

Back 21

max effect a drug can have. At same concentration on X axis, one max will be higher

Front 22

What does a competitive agonist do to the EC50?

Back 22

Will SHIFT RIGHT, will reach effective doses at higher concentrations, because drug is competing with antag
(can still reach max if high dose)

Front 23

What does a noncompetitive inhibitor do?

Back 23

DECREASES MAX EFFECT! taking receptors out of commission, so can't be used by drug.

Front 24

Partial agonist?

Back 24

produces lower max response (physiol)
(as partial agonist binding increases, agonist binding decreases!)

won't be zero effect like non comp b/c "inhib" is agonist

Front 25

How do you calculate the THERAPEUTIC INDEX?

Is is better to have TI high or low?

Back 25

TI = toxic dose 50 / effective dose 50

GREATER TI = SAFER DRUG!!!!

Front 26

How much salicylic acid (aspirin; pKa =3) will be absorbed from the small intestine, which has a pH of 7?

Back 26

log Ha/A- = pKa -pH

= 3-7 = -4
antilog -4 = .0001 (ratio is 1/10000 so most of drug is UNPROTONATED)

Front 27

In the stomach (at pH = 2), what is the ratio of unionized to ionized aspirin (salicylic acid)?

Back 27

log Ha/A- = pKa -pH

3-2 = 1
antilog 1 = 10 (ratio is 10/1 so most of drug is PROTONATED)

Front 28

At a pH of 8, what is the ratio of unionized to ionized amphetamine (pKa=10)?

Back 28

log HB/B = pKa - pH

=10-8 = 2
antilog 2 = 100 (ratio of drug is 100/1 so most of drug is PROTONATED)

Front 29

log -2 =
log -1 =
log 0 =
log 1 =
log 2 =

Back 29

=.01
= .1
=1
= 10
= 100

Front 30

Intracellular rec:
Intrinsic Enz activ:
Ligand Gated
Enz Assoc
7TMR

Back 30

intracellular = estrogen, Vit A

Intrinsic enz = EGFR, IR, TGF-br

Ligand gated = Nic Ach rec

Direct assoc enz = IL3 Eryth, Leptin

7TMR = G prot, heptahelical, serpentine, B adren, Rhodopsin, Frizz and Smo

Front 31

Kd = R * L / RL

and if 1/2 rec bound

Back 31

R and RL cancel, Kd = ligand conc

Kd = Koff/Kon

Front 32

Max response of drug can be limited by what 3 things?

Back 32

receptor number, number of signaling molecules, how fast heart can beat

Front 33

What is extraction ratio and bioavailability calculations>

Back 33

E = (Dose IN - Dose OUT) / (Dose IN)

BAv = (1-E) Abs %

Front 34

Volume of Distribution?

Back 34

Vd = dose (mg) / Conc
(Conc is max in plasma after equil and before elim)

Front 35

C = 10mg/L
Vd = 20L

Back 35

Vd = mg / conc
20L = X / 10mg/L
X = 20L * 10 mg/L = 200 mg!

Front 36

Vd = .2L/Kg
Weighs = 70 kg
Vd for patient?

Back 36

.2L/kg x 70kg = 14L!!

Front 37

Drug = 100mg
Conc = 50 mg/L
Vd?

Back 37

Vd = 100mg / 50mg/L
Vd = 2L

Front 38

What happens to Cmax, rate absorption, and Tm with Varied dose absorption?

Back 38

Cmax increases
Tm and rate stay the same

i.e. you take 1x 200mg advil or 2 x 200 mg advil but they both work in 10 min

Front 39

What happens to Cmax, rate absorp, and Tm with Varied Rate?

And AUC's?

Back 39

If rate increases, Cmax increases and Time shorters BUT time increases and Cmax goes down for other but AUC ARE THE SAME!!!!!!!!!!!!!!!!

i.e. you take gel 200mg or solid 200mg, rate changes but same in body

Front 40

Two equations for Cl?

Back 40

Cl = Vd x Ke


Cl = Conc OUT/Conc IN x vol/time

Front 41

Flow limited Clearance?

Back 41

limiting factor is blood perfusion!
-binding insensitive

*clearnace how much fluid passes before ALL drug is removed?

Front 42

Capacity limited clearance?

Back 42

organ metab is limiting factor
BINDING INSENS = free fraction won't change rate of elim
BINDING SENS = will alter rate, high protein bound

Front 43

What is first order elimination?
v = Vm (D/Km+D)

Back 43

Conc low compared to Km ELIM is DEP on DOSE
elim constant % per time
*exp

Front 44

What is ZERO order elim?

Back 44

Saturation/Drug is high rel to Km
v = Vmax

ELIM INDEP OF DRUG CONC
*contant amt per time, linear

Front 45

Half life and Steady State?

Back 45

t 1/2 = .7/Ke

SS = t 1/2 (5)

1t = 50% accum,
2t = 75% accum
3t = 87.5% accum
4t = 93.75
5t = 96.88

Front 46

Decrease dosing interval (time between doses) does what to peak/troughs?

Back 46

Increased freq of drug makes diff between troughs and peaks narrow!
Diff between will become smaller

Front 47

What happens when you increase dose? to peaks and troughs?

Back 47

INCREASE! Both!

Front 48

What are the equations of LD and MD?

Back 48

LD = Css x Vd x (1/F)

MD = Css x Vd x Ke (1/F)
(Cl = Vd x Ke)