lecture4&5 Flashcards

1
Q

what form of an acid can transverse the membrane

A

the protonated form

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2
Q

what form of a base can transverse a membrane

A

the unprotonated form

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3
Q

what does the Henderson Hasselbalch equation tell us about drugs

A

it will give us a clue as to how much is protonated and so how much of the acid can transverse the membrane

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4
Q

where do weak acids get absorbed

A

more likely in the stomach

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5
Q

where do weak bases get absorbed

A

more likely in the intestines

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6
Q

what cardiac factors impact distribution

A

cardiac output, regional blood flow, capillary permeability, binding to plasma proteins.

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7
Q

what are the four main factors of distribution

A

cardiovascular, tissue binding, drug molecule size, and lipid solubility.

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8
Q

what is biotransformation

A

reaction or metabolism of drugs can be categorized as phase 1 or phase 2. these can convert a parent compound into an active or inactive metabolite.

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9
Q

what is phase 1 biotransfromation

A

generates a more polar molecule by exposing a functional group on parent group readies for phase 2 FORMS METABOLITE ACTIVE OR NOT

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10
Q

what is phase 2 biotransformation

A

reaction yield a more water soluble conjugated product to be excreted. CONJUGATED

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11
Q

what kind of reactions happen in phase1

A

oxidation reductive and hydrolytic

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12
Q

what kind of reactions happen in phase2

A

glucuronidation, sulfation, acetylation, methylation,

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13
Q

what is the first pass effect

A

that drugs absorbed by stomach or intestine will be carried by portal vein to the liver.

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14
Q

what is the primary mechanism of drug elimination

A

renal excretion

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15
Q

what processes effect renal excretion

A

GFR binding to plasma proteins, alklinization or acidification of urine

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16
Q

what is another route for more lipophilic drugs to be excreted

A

fecal excretion

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17
Q

what are the key parameters that impact drug dosage in patients

A

volume of distribution and clearance

18
Q

what is volume of distribution

A

the measure of the space in the body available to contain the drug. This is a theoretical number

19
Q

what is clearance

A

measure of the ability of the body to eliminate a drug

20
Q

what is volume of distribution as a formula

A

V=amount of drug in body/concentration of drug in blood or plasma. A high volume suggest the drug is moving but a low volume suggests little movement.

21
Q

what is the formula for clearance

A

CL=rate of elimination/concentration

22
Q

what is zero order elimination

A

this is when the elimination process is at capacity or saturated, so its independent of concentration. Linear on a normal scale nonlinear on a log scale

23
Q

what is first order elimination

A

non saturated process you will remove a fraction of the drug is removed every time period. Ie 50% every two hours non linear on a normal scale linear on a log scale

24
Q

what is flow dependent elimination

A

an organ has a high capacity but needs the right flow to get the drug there. Looks like first order kinetics

25
Q

what is capacity limited elimination

A

a point where the drug has saturated the elimination capacity of the system, but in dosage exceeds elimination this could lead to toxicity. Looks like zero order kinetics

26
Q

how does volume of distibution effect half life

A

the larger the volume of dist. The longer the half life

27
Q

how does clearance effect half life

A

the slower the clearance the longer the half life of the drug.

28
Q

what is the acuumulation factor

A

AF=1/fraction lost in one dosing interval. Only works if dosing is less than four half lives.

29
Q

what is the bioavailability

A

the amount of drug that reaches the systemic circulation. IV will be 100%

30
Q

what is the extraction ratio formula

A

ER= clearance of liver/hepatic blood flow or Q. the close to 1 the more its extracted and less is available.

31
Q

what is the bioavailability formula

A

F=extent of absorption of the gut or f, x [1-ER]

32
Q

what is steady state concentration Css

A

the point where what is reaching the blood is what is leaving the blood

33
Q

what is the formula for steady state

A

Css=dosing rate/Clearance or CL ti will take 4-5 half lives to reach the Css and is independent of the dose and dosing rate and only dependent of the half life of the drug.

34
Q

what is the maintenance dose

A

dose needed to maintain a steady state concentration in order to determine a maintenance dose the dosing rate must first be determined.

35
Q

what is the formula for dosing rate

A

ClxTC or target concentration this is for an IV dose, for oral does it would be Dosing rate/ F oral or bioavalibility

36
Q

what is the formula for maintenance dose

A

dosing rate x Dosing interval

37
Q

what happens to concentrations as the dosing interval increases

A

it will increase the peak and decease the trough concentrations which might or might not effect the patient.

38
Q

what is the loading dose

A

an initial dose that can be given in order to achieve the target concentration rapidly.

39
Q

what is the formula for loading dose

A

LD=V x TC / F

40
Q

how many half lives does it take for a drug concentration to be considered negligable?

A

4-5 half lives.