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Flashcards in 3/15 pharm Deck (111)
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1

Clearance can be impaired w/defects in which systems?

cardiac, renal, hepatic.

2

Clearance
-equation:

Cl = (rate of elim of drug)/(plasma drug conc.)
Cl = (Vd)*(Ke)
Cl = (Q)*(Er)

Q = flow to that organ (ie. liver)
Er = extraction ratio

3

Loading dose
-equation

Loading dose = (Cp)(Vd) / (F)

Cp = target plasma concentration at steady state
F = bioavailability

4

Maintenance dose (MD)
-equation

MD = (Cp)(Cl)(t) / F

t = dosage interval (time between doses), if not administered continuously.
*If continuous, leave t out. You will also know its IV so F = 1. B/c only IV is continuous.

5

In liver or renal disease, does maintenance dose inc. or dec.?

Dec.
-less being cleared, so less dose needed.

6

Which drugs follow zero-order elimination?
-mnemonic?

-Phenytoin, Ethanol, and Aspirin (at high or toxic concentrations).

-PEA. (A pea is round, shaped like the “0” in
“zero-order.”)

7

Capacity-limited elimination
-0 or 1st order?

0 order elim.

8

Flow-dependent elimination
-0 or 1st order?

1st order elim.

9

Phase I drug metabolism

P450 system
-Reduction, oxidation, hydrolysis.

10

Phase II drug metabolism

Conjugation (Glucuronidation, Acetylation, Sulfation)

11

Which is most common P450 enzyme?

CYP3A4 = most common

12

Name 3 drugs that might cause trouble in a slow acetylator.
-which would also have a bimodal pop. distribution.

-hydralazine, isoniazid, procainamade

*HIP: its not hip to be a slow acetylator.

13

What kind of antagonist is ketamine?

-ketamine (noncompetitive antagonist) on NMDA receptors.

14

Therapeutic index:
-equation:

TI = Toxic dose/Effective dose
*high therapeutic index is good b/c that means theres a big difference btwn toxic and effective doses.

15

Whats good, a high or low therapeutic index?

High.
-Safer drugs have higher TI values.

16

Is the therapeutic index the same as therapeutic window?

No, b/c the therapeutic window would never extend all the way until the toxic dose.

17

Some receptors that respond to autonomic neurotrasmitters/drugs receive NO nerve innervation (must get ligand through blood).
-can you name these uninnervated autonomic receptors?

-muscarinic receptors on endothelium of blood vessels
-adrenoreceptors on apocrine sweat glands
-alpha-2 and beta adrenoreceptors in blood vessels.

18

para/pre, sym/pre: all release what?

ACh

19

All ganglia have what type of receptor?

Nicotinic: ligand-gated ion channels.

20

Do all sym/post release NE?

NO
-adrenal medulla releases NE and epi.
-sym/post release ACh that innervate sweat glands & piloerector muscles. These = sympathetic cholinergic.

21

sympathetic cholinergic

sym/post that releases ACh
-innervate sweat glands & piloerector muscles.

22

All glands have what receptors on them?

muscarinic
-even sweat glands that have sym/post innervation: these sym/posts dump ACh, not NE (sympathetic cholinergic).

23

adrenal medulla & sweat glands = part of sym nervous system but are innervated by _______ fibers.

cholinergic

24

Nicotinic ACh receptors
-what type of receptor is it?

-ligand-gated Na/K channels.

25

which receptors are more sensitive to activation, alpha or beta?

beta

26

Epi: acting more on alpha1 or beta2?
-low dose =
-high dose =

-low dose - acts more on beta-2
-high dose - acts more on alpha-1

*remember, beta-receptors are more sensitive.

27

Ciliary muscle innervation:

-muscarinic
-its NOT dual innervated.

*if there is an effect on accomodation, its a muscarinic (agonist or antagonist) drug

28

Cycloplega = what is it, what can cause it?

paralysis of ciliary muscles = M-antagonist

29

Gs => inc. cAMP => PKA => phosphorylates MLC kinase.
-whats the result?

smooth muscle relaxation
-hence beta-2 (Gs) causing smooth muscle relaxation in lungs.

30

Hemicholinium
-mech:
-use:

-Prevents reuptake of choline so you have less in nerve terminal so you make less ACh and release less ACh.
*NO CLINICAL USE.