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Pharmacology #1 > Module A-2 > Flashcards

Module A-2 Flashcards

1
Q

Kinetic vs dynamic vs biophase figure

A
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2
Q

Figure relating pH and PKa

A
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3
Q

Pre-systemic elimination

A

Elimination by GI system before it can get to systemic circulation
-stomach acids hydrolyze drug
-enzymes from GI wall deactivate drug
-liver bio transforms drug before it reaches effect site

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4
Q

Properties impacting kinetics

A

-molecular size
-drug transporters
-degree ionization
-lipid solubility

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5
Q

Properties impacting kinetics

A

-molecular size
-drug transporters
-degree ionization
-lipid solubility

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6
Q

Key points of Oral

A

-Degree of ionization impacts absorption
-low bioavailability
-liver first pass

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7
Q

pKa

A

pH at which drug will be 50% ionized and non-ionized

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8
Q

Characteristics of non-ionized drugs

A

-lipid soluble
-hepatic metabolism
-no renal excretion

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9
Q

Characteristics of ionized drugs

A

-water soluble
-renal excretion
-do not cross lipid barriers

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10
Q

Bioavailability

A

Extent to which drug reaches effector site
-solubility (lipids vs aqueous)
-molecular weight
-pH
-pKa
-perfusion/blood flow to effector site

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11
Q

Ion trapping

A

Non-ionized drugs cross a lipid barrier and become ionized on the other side due to a change in pH and cannot cross back over-can quickly lead to toxicity

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12
Q

Two compartment model

A

Drug is first distributed to the vessel rich group (central compartment) and then redistributed to the the peripheral compartment or metabolized/excreted

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13
Q

Volume of distribution

A

Apparent volume in which drug has been distributed after it has been introduced
Variables:
-drug size
-carrier molecules
-disease states (burns, liver disease, pregnancy)
-solubility

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14
Q

Large Vd (>0.67 L/kg)

A

Widely distributed, likely lipophilic- think propofol

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15
Q

Small Vd (<0.4 L/kg)

A

Likely stays in plasma, highly hydrophilic, rocuronium

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16
Q

Oxidation

A

Loss of an electron

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17
Q

Reduction

A

Gain of an electron

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18
Q

Hydrolysis

A

Adding water to a compound to cleave it into acid and alcohol

19
Q

Conjugation

A

Addition of a functional group to create more ionized compound at physiological pH

20
Q

Phase 1 reactions

A

-increase polarity
-Primarily P450
-oxidation/reduction/hydrolysis

21
Q

Phase 2 reactions

A

Conjugation- covalently links drug/metabolite with highly polar molecule to make water soluble and inactive

22
Q

Glucuronidation & common drugs

A

Phase 2 reaction-addition of glucuronic acid
Propofol
Midazolam
Morphine

23
Q

Other Phase 2 reaction examples

A

N-acetylation
Glutathione-S-transferases

24
Q

Elimination half life

A

Time for plasma concentration to drop by half in elimination phase of plasma concentration curve

25
Q

Context sensitive half time

A

Time to decrease by 50% from infusion that maintained a constant concentration (context is time of infusion)

26
Q

Distribution half life

A

Amount of time to decrease by 50% in distribution phase of plasma concentration curve

27
Q

First order kinetics

A

Drugs are eliminated at a constant fraction per unit time

28
Q

Zero order kinetics

A

Drugs are eliminated at a constant AMOUNT per unit time
-commonly seen in overdose

29
Q

Clearance

A

Volume of blood from which drug is completely eliminated per unit of time
-NOT amount of drug eliminated
Clearance=blood flow*extraction ratio

30
Q

High Extraction ratio

A

> 0.7 Reliant on hepatic blood flow- considered high clearance drugs

31
Q

Low extraction ratio

A

<0.3 Dependent on hepatic liver enzymes for extraction and changes in hepatic perfusion have no impact on

32
Q

Ionization
Acid in acid

A

Non ionized

33
Q

Ionization
Bases in bases

A

Non ionized

34
Q

Ionization
Acids in base

A

Ionized

35
Q

Ionization
Bases in acid

A

Ionized

36
Q

Drug A is an acidic compound with pKa of 7.1. It is put in acidic environment of 6.0

A

7.1-6=1.1 therefore 99/1 percent

Acid in acid so 99% non-ionized

37
Q

Drug B is an acid with pKa of 5, put in 7.4

A

2.4 so 99%
Ionized!!

38
Q

Drug C is a base with pKa of 7.8, in 7.4

A

0.4 so 75/25
Base in more acidic environment so it is 75% ionized and 25% non-ionized

39
Q

Other clearance factors…

A

Age- GFR declines, hepatic blood flow decreases, neonates have poor renal function
Gender- receptor sensitivity differences…
Liver disease- alters Vd

40
Q

Absorption:

A

How a drug moves from its site of delivery into the bloodstream

41
Q

Exponential Decay

A

The decay/decreases is proportional to the size of the quantity of interest

42
Q

Plasma protein binding: three facts- name abundant types of

A

Albumin & alpha 1 acid glycoproteins are most abundant

Bound protein is NOT pharmacologically active

Unbound protein is available for receptor binding

43
Q

Primary goal of metabolism/biotransformation

A

Make inactive & water soluble for excretion

44
Q

Common enzyme in phase two reactions

A

Transferase

Conjugation adds a functional group (ie it transfers a functional group)

Pharmacology #1 (15 decks)

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