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Anesthesia Pharm. I > Module 2 > Flashcards

Module 2 Flashcards

1
Q

The insertion of a molecule of water into another molecule, which forms an unstable intermediate compound that subsequently splits apart.

Barash Ch. 11

A

Hydrolysis

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2
Q

The primary way amides, such as lidocaine and other amide local anesthetics, and esters, such as succinylcholine, are metabolized.

Barash Ch. 11

A

Hydrolytic reactions

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3
Q

Reactions that remove electrons from a molecule.

Barash Ch. 11

A

Oxidation

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4
Q

The single most important enzyme, accounting for 40% to 45% of all CYP-mediated drug metabolism.

Barash Ch. 11

A

CYP3A4

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5
Q

Enzymatic reactions that metabolize drugs can be classified into (_____) and (_____) biotransformation reactions.

Barash Ch. 11

A

Phase I / Phase II

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6
Q

True or False?

The passive elimination of drugs by passive glomerular filtration is a very efficient process.

Barash Ch. 11

A

False

The passive elimination of drugs by passive glomerular filtration is a very INefficient process

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7
Q

What determines the concentration of a drug in the plasma or at the site of drug effect?

A

Pharmacokinetics

[Stoelting ch 2]

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8
Q

A result from genetic modifications in metabolism; interactions with other drugs; or disease in the liver, kidney, or other organs of metabolism?

A

Pharmacokinetic Variability

[Stoelting ch2]

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9
Q

What is the time frame of initial distribution after bolus injection?

A

Within 1 minute

Stoelting ch 2

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10
Q

A compartment physically composed of those elements of the body that dilute the drug within the first minute after injection. Consists of Vessel Rich Group (VRG)

A

Central compartment

[Stoelting ch 2]

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11
Q

Many anesthetic drugs are highly ___________ soluble and poorly soluble in _______.

A

Fat; water

[Stoelting ch 2]

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12
Q

Protein binding affects the ________ of drugs as well as the _______.

A

Distribution; potency

[Stoelting ch 2]

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13
Q

Most acidic drugs bind to___________. while most basic drugs bind to ________.

A

Albumin; alpha 1 acidic glycoprotein

[ Stoelting ch 2]

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14
Q

The 4 basic pathways of metabolism are?

A 
Phase 1
- oxidation
- reduction
- hydrolysis
Phase 2 
- conjugation

Stoelting ch 2

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15
Q

The CYP450 enzyme is involved in what phase of metabolism?

A

Phase 1

Stoelting ch 2

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16
Q

The rate of metabolism for most anesthetic drugs is proportional to drug ____________, rendering the clearance of the drug constant.

A

Concentration

Stoelting ch 2

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17
Q

The rate at which drug flows out of the liver must be the rate at which the drug flows in to the liver, minus the rate at which the liver ______ the drug.

A

Metabolizes

Stoelting ch 2

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18
Q

Renal excretion of drug involves what 3 things?

A

A) glomerular filtration
B) active tubular secretion
C) passive tubular reabsorption

Stoelting ch 2

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19
Q

Nonionized molecules are usually _______ soluble and can diffuse across cell membranes.

A

Lipid

[Stoelting ch 2]

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20
Q

The ______molecule is poorly lipid soluble and cannot penetrate lipid cell membranes easily.

A

Ionized

[Stoelting ch 2]

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21
Q

The reason for the large differences in the pharmacological effect of oral and IV drug doses.

A

First-pass hepatic effect

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22
Q

Route of drug administration that permits a rapid onset of drug effect due to bypassing the liver and preventing the first-pass hepatic effect.

A

Sublingual/ buccal route
Intravenous

(Stoelting ch 2)

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23
Q

What organ excretes the most amount of drugs?

A

Renal system

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24
Q

What is the formula for renal excretion?

A

Filtration - reabsorption + secretion at the level of the nephron

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25
Q

What is the definition of a nephron

A

It is the functional unit of the kidney

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26
Q

The liver is the most important organ for metabolism of drugs. Hepatic drug clearance depends on what three factors?

Barash Ch. 11

A
  1. The intrinsic ability of the liver to metabolize a drug
  2. Hepatic blood flow
  3. The extent of binding of the drug to blood components
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27
Q

Where do drugs enter the nephron?

A

Afferent arteriole

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28
Q

After a drug goes through the afferent arteriole in the nephron where does go?

A

Bowman’s capsule

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29
Q

When a drug is not filtered in the kidney where does it go?

A

Efferent Arteriole

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30
Q

Can a drug be secreted more then once in the kidney?

A

Yes, if the drug is not secreted it will branch to the peritubular capillaries and allows the drug to be secreted again if it was not filtered.

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31
Q

True/False Does filtration care if a drug is metabolized?

A

False, the only thing that filtration cares about is if the drug is free and not bound to anything. Generally speaking, polar and ionized.

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32
Q

If a drug is unbound in the kidney where can it be filtered out at?

A

Glomerulus site

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33
Q

Is albumin in the urine a good or bad thing?

A

Bad! It is used as a marker for diabetics to determine the progression of kidney disease in the urine. High number of albumin is bad

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34
Q

Is it good or bad for reabsorption of a drug at the glomerulus?

A

Bad, it is important not to reabsorb the drug. The point of metabolism is to process a drug in a way that is more readily eliminated.

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35
Q

What is the entire point of metabolism?

A

To prevent reabsorption, make a drug more readily eliminated.

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36
Q

Does the body prefer lipid soluble drugs or water soluble

A
  • Lipid soluble drugs bypass the GI tract and allows is to get reabsorbed into the body.
  • Easily passes cell membrane with increased lipophilicity.
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37
Q

True or False?

All else being equal, an increase in the volume of distribution of a drug will increase its elimination half-life; while an increase in elimination clearance will decrease elimination half-life.

Barash Ch. 11

A

True

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38
Q

Most drugs must pass through cell membranes to reach their sites of action. Consequently, drugs tend to be relatively (_____), rather than (____).

Barash Ch. 11

A

lipophilic/hydrophilic

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39
Q

The theoretical volume of blood from which a drug is completely and irreversibly removed in a unit of time.

Barash Ch. 11

A

Elimination clearance/drug clearance/ rate of elimination. Expressed as mass/time.

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40
Q

Which highly perfused core circulatory components receive the highest relative distribution of cardiac output, and therefore, are the initial organs to reach equilibrium with plasma drug concentrations? (Vessel Rich Group)
(five organs)

Barash Ch. 11

A

The brain, lungs, heart, liver and kidneys.

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41
Q

What does the liver do to the molecule?

A

The liver metabolizes molecules and makes them more polar, more readily eliminated from the body.

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42
Q

Why is a polar molecule good?

A

More polar molecules prevent reabsorption.

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43
Q

What is ion trapping

A

Systematic administration of a weak base, such as opioid, can result in accumulation of ionic drug in the environment of the stomach

(The ph and the charge can be changed to prevent reabsorption)

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44
Q

Is reabsorption always bad?

A

No, reabsorption of electrolytes is good but reabsorption of the drug is not

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45
Q

What is secretion

A

The way the body releases the drug into the urine

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46
Q

What is the rate of elimination

Formula

A

Elimination (Mass/time) = Clearance (volume/time) * (mass/volume) concentration. *Notice how units cancel to derive elimination as mass/time.

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47
Q

What is GFR

A

Flow rate of blood that is being filtered.

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48
Q

Where can creatine be found in the body ?

A

The muscles

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49
Q

What does creatinine measure

A

Kidney function

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50
Q

What is the best test to measure kidney function

A

24-hr urine collection

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51
Q

What is the gold standard for measuring kidney function

A

The measurement of inulin because it is freely filtered precise measurement of GFR. Rarely used.

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52
Q

What classifies chronic kidney disease

A
  • Kidney problem > 3 months
  • GFR< ml/min
  • Increase in creatinine and decrease in GFR
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53
Q

What is the easiest way to determine kidney disease

A
  • Decreased GFR

- Increased Serum Creatinine

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54
Q

What does enzyme induction do

A

It increases drug metabolism

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55
Q

What does competitive inhibition do

A

Decrease drug metabolism

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56
Q

Where does metabolism occur

A

At the level of the enzyme

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57
Q

Why do drug reactions occur

A

Secondary to change in enzyme activity

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58
Q

What enzyme is responsible for more than 50% of unexpected drug reactions

A

CYP3A4

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59
Q

What increases drug metabolism?

A

Enzyme inducers

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60
Q

What happens when you make more enzyme

A

Rate of drug metabolism is increased. It increases VMAX (maximum rate of metabolism). A VMAX that can no longer increase indicated enzyme saturation.

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61
Q

What is enzyme induction?

A

It increases the rate of metabolism, leads to increase in metabolites.

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62
Q

What happens if drug metabolism increases?

A

Drug concentration decreases.

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63
Q

Do chronic alcoholics make more or less enzymes ?

A

They make more so it increases the rate of metabolism.

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64
Q

What is competitive inhibition

A

Constrains drug metabolism, increases plasma drug concentration.

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65
Q

What happens in the presence of competitive inhibitors

A

Decreases the rate of drug metabolism, will decrease the dosage required.

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66
Q

What are two consequences of competitive inhibitor’s

A
  1. Decreases metabolism so it makes less metabolites (this is good if metabolites are toxic)
  2. If Metabolites are increased the drug concentration causes more side effects to occur
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67
Q

What is the most commonly prescribed drug in the US?

A

Statins

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68
Q

What is a statin

A

It is a cholesterol lowering agent

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69
Q

Where are statins metabolized at

A

CYP3A4-metabolite

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70
Q

What does more than one glass of grapefruit juice do to a person who is taking a Statin

A

Having more than one glass of grapefruit juice, especially at night, inhibits the CYP3A4 gene, which increases the amount of statin in the body

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71
Q

What is CYP3A4 inhibited by ?

A

Furanocumarins

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72
Q

What type of antacid should you not take with statins

A

H2 blockers

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73
Q

What do you H2 blockers do to your stomach when you’re taking a Staten

A

It takes the protons and pumps it out creating a hydrochloric acid

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74
Q

What are three molecules that bind to the Parietal cell

A

Histamine, acetylcholine, and gastrin

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75
Q

What is a specific name of an H2 blocker that inhibits the CYP3A4 gene and it increases Statin concentration in the body

A

Cimetidine

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76
Q

What do macrolides treat

A

Upper respiratory infections

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77
Q

What is MACE

A

Macrolides, azithromycjn, clarithromycin, erythromycin

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78
Q

Which mycin can you give a patient who is taking a statin and why

A

Azithromycin because it does not have CYP3A4 inhibition

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79
Q

What is Pharmogemonics

A

It is the study of how genetic factors affect drug metabolism. As with Asian glow

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80
Q

What is Asian glow

A

Eastern Asians have a predisposition when drinking alcohol that gives them an allergic reaction

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81
Q

In what regións in Asia do people commonly encounter Asian glow

A

Koreans, Taiwanese, and Japanese

Eastern Asian

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82
Q

What causes the Asian glow to occur

A

It is a release of histamine and prostaglandin that widen the arteries in veins causing a flushing appearance
(Vasodilation)

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83
Q

How can you treat Asian glow

A
  1. Avoid drinking
  2. Can use a anti-histamine (cimetidine)
  3. Before you start drinking alcohol take a Zantac, or aspirin to decrease the production of prostaglandins
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84
Q

Which route of a drug is able to directly enter the systemic circulation, able to bypass the metabolically active intestinal mucosa, and the hepatic first-pass metabolism?

Barash Ch. 11

A
  • Sublingual

- Intravenous

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85
Q

Direct injection of local anesthetics and opioids into the intrathecal space bypasses the limitations of drug (___) and drug (___) of any other route of administration.

Barash Ch. 11

A

Absorption / distribution

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86
Q

The large surface area of the pulmonary alveoli available for exchange with the large volumetric flow of blood found in the pulmonary capillaries makes (___) administration an extremely attractive method by which to administer drugs.

Barash Ch. 11

A

Inhalational / Inhalation

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87
Q

True or False?

Once the concentration of drug in the brain tissue is higher than the plasma concentration of drug, there is a reversal of the drug concentration gradient so that the lipophilic drug readily diffuses back into the blood and is redistributed to the other tissues that are still taking up drug.

Barash Ch. 11

A

True

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88
Q

Pharmacokinetic term that describes all the processes that remove a drug from the body.

Barash Ch. 11

A

Elimination

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89
Q

Most drugs that are excreted unchanged from the body are (____) and therefore readily pass into urine or stool.

Barash Ch. 11

A

Hydrophilic

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90
Q

What enzymatic reaction that metabolizes a drug, which tends to transform a drug into one or more polar and potentially excretable compounds?

Barash Ch. 11

A

Phase I biotransformation reactions

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91
Q

What enzymatic reaction that metabolizes a drug to transform the original drug by conjugating a variety of endogenous compounds to a polar functional group of the drug, making the metabolite even more hydrophilic.

Barash Ch. 11

A

Phase II biotransformation reactions

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92
Q

Most common enzyme involved in phase 2 metabolism

A

UGTs- (UDP- Glucuronosyltransferase)- Glucuronidation reaction.

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93
Q

Enzymes involved in phase 2 metabolism.

A

UGTs (UDP- Glucuronosyltransferase)involved in Glucuronidation reaction., ( GSTs (Glutathione-s-transferase) involved in Glutathione conjugation, NATs(N-acetyltransferase) leads to Acetylation , SULTs (Sulfotransferase) leads to sulfation.

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94
Q

Acetaminophen is metabolized by which phase reaction.

A

95% of tylenol is metabolized by phase 2 enzymes.

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95
Q

Enzyme famous for polymorphism.

A

CYP2D6 (CODEINE)

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96
Q

First order kinetics.

video-9

A 
Rate of metabolism is proportional to drug concentration.
Half life(Time to metabolise 50% of drug) is constant.
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97
Q

What is zero order kinetics.

A

Rate of metabolism becomes independent of drug concentration. Rate of drug metabolism is constant. Rate of drug elimination is constant. Drug can build up in the body leads to toxicity

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98
Q

Name three drugs reach zero order kinetics quickly

VIDEO-9

A

Aspirin, phenytoin & ETOH

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99
Q

What is elimination half life

A

Time it take to eliminate 50% of the drug in the body.

95% of drug is always eliminate after 4.5 half-lives

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100
Q

Formula to calculate elimination half life

A

0.693/ke (first order elimination constant)
OR
0.693xVd/cl
Vd is volume of distribution and cl is clearance

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101
Q

What is clearance

A

Volume of plasma that gets filtered of drug/Time

unit is L/hr or ml/min

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102
Q

How to calculate Rate of elimination

A

Rate of elimination = clearancexplasma drug concentration

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103
Q

what is total clearance.

A

CL total= CL renal+ CL hepatic +CL lungs.

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104
Q

Clinical use of GFR (glomerular filtration rate)

A

GFR is used to to estimate changes in the renal clearance of drugs. Used as an indicator to select drug dose and choice .

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105
Q

DRUG CLEARANCE VS ELIMINATION.

A

Drug elimination refers to the irreversible removal of drug from the body by all routes of elimination. The declining plasma drug concentration observed after systemic drug absorption shows that the drug is being eliminated from the body but does not indicate which elimination processes are involved.

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106
Q

Total clearance

A

Renal clearance-urine
Hepatic clearance- Bile
Pulmonary clearance- Air

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107
Q

What are the main factors that affect tissue distribution of drugs? KT

A

Body composition, regional blood flow, and drug affinity for plasma proteins/tissue components.

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108
Q

The behavior of molecules with weak-moderate lipophilicity in obese patients is…. KT

A

Predictable as these drugs are mainly distributed in lean tissues and their doses based on ideal body weight. Ex: vecuronium and lithium.

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109
Q

Obesity can significantly alter….. KT

A

Tissue distribution and elimination of drugs, and may necessitate modified loading and/or maintenance doses of various drugs.

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110
Q

Obesity is defined as ….. KT

A

An excess of fat tissue compared with normal values for age and gender

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111
Q

An individual was said to be obese when …… KT

A

The actual bodyweight exceeds the IBW by more than 20%

112
Q

Body mass index (BMI) is…. kT

A

Bodyweight (in kg) divided by the square of the height in metres

113
Q

The BMI of an overweight person is…. KT

A

≥25 to 29.9 kg/m2

114
Q

The BMI of an obese person is………. KT

A

≥30 kg/m2.

115
Q

Obesity is divided into 3 classes: KT

A

Moderate (BMI 30.0 to 34.9), severe (BMI 35.0 to 39.9) and morbid (BMI ≥ 40.0).

116
Q

How has the prevalence of obesity changed in the past 15 years? KT

A

Obesity has increased by

between 10 and 40%. Most pronounced in young women.

117
Q

Obesity affects which stages of pharmacokinetics? KT

A

Distribution and elimination/clearance

118
Q

The main factors that affect the distribution of drugs in tissues are… KT

A

Body composition, regional blood flow and binding to plasma proteins

119
Q

Obese individuals have a larger absolute …… KT

A

Lean body mass (LBM), as well as fat mass, compared to normal healthy individuals of the same age, gender and height.

120
Q

Anthropometric calculation of Lean Body Mass….KT

A

LBM (kg) = a × TBW (kg) – b × [TBW/height (cm)]2

where a and b are 1.10 and 120 for men and 1.07 and 148 for women.

121
Q

Blood flow in fat is typically.. KT

A

Poor and accounts for only 5% of cardiac output compared to 22% in lean tissue and 73% in the viscera.

122
Q

The livers of obese individuals frequently suffer from … KT

A

Fatty infiltration Ex: nonalcoholic steatohepatitis

123
Q

Obese individuals may be at an increased risk of… KT

A

CYP2E1-mediated toxicity of environmental agents.

124
Q

maintenance dosage of propofol for obese patients may be established on the same basis as …… KT

A

For lean patients, taking into account the TBW. There is no extra accumulation of Propofol in obese patients.

125
Q

Fentanyl in obese patients… KT

A

Is distributed at least as extensively in the excess body mass as in the lean tissues, and the loading dose should account for total body mass.

126
Q

The longer t1⁄2β of fentanyl elimination in obese patients suggests that …. KT

A

Maintenance doses should be prudently reduced in these individuals

127
Q

Remefentanil doses for obese individuals should …. KT

A

Be calculated on the basis of IBW

128
Q

Neuromuscular blockers are ….. KT

A

Polar and hydro- philic

129
Q

IBW should be used to calculate ….. KT

A

doses of vecuronium in obese patients

130
Q

Rocuronium should be administered to obese pa- tients on the basis of ……. KT

A

IBW and not TBW.

131
Q

What is phase one when Asian flush occurs in the body

A

First the enzyme is ash (alcohol dehydrogenase)- take ethanol (ETOH)
And forms acetaldehyde, which make the molecule more polar

132
Q

What is the normal gene in the body the metabolizes alcohol and is the abnormal gene for an Asian person

A

Normal = ALDH*1

Abnormal = ALDH*2

133
Q

Why does Asian flushing occur ?

A

One parent has the abnormal gene ALDH*2 and passes it to the child

134
Q

If only one parent passes the bad gene ALDH*2 to the child what kind of molecule is it

A

It is heterozygous and it is 100 times slower

135
Q

What happens if both parents pass along the bad gene ALDH*2

A

The molecule is then homozygous and alcohol would make the child EXTREMELY sick

136
Q

If someone has a heterozygous can they drink alcohol

A

They will still get sick but if they still drink they would be able to develop a tolerance and reaction would not be as bad

137
Q

What is important to warn the patient who have a heterozygous gene and build up tolerance to alcohol?

A

They are at higher risk for developing esophageal cancer because they have the bad gene in their genetic makeup

138
Q

What is disulfiram

A

It is a competitive inhibitor of the ALDH*2 gene and is used as an alcohol deterrent that will cause the person to get extremely ill if the drink alcohol.
It is used as a treatment for alcoholism

139
Q

Which route of a drug is able to directly enter the systemic circulation, able to bypass the metabolically active intestinal mucosa, and the hepatic first-pass metabolism?

Barash Ch. 11

A

Sublingual

140
Q

Direct injection of local anesthetics and opioids into the intrathecal space bypasses the limitations of drug (___) and drug (___) of any other route of administration.

Barash Ch. 11

A

Absorption / distribution

141
Q

The large surface area of the pulmonary alveoli available for exchange with the large volumetric flow of blood found in the pulmonary capillaries makes (___) administration an extremely attractive method by which to administer drugs.

Barash Ch. 11

A

Inhalational / Inhalation

142
Q

True or False?

Once the concentration of drug in the brain tissue is higher than the plasma concentration of drug, there is a reversal of the drug concentration gradient so that the lipophilic drug readily diffuses back into the blood and is redistributed to the other tissues that are still taking up drug.

Barash Ch. 11

A

True

143
Q

Pharmacokinetic term that describes all the processes that remove a drug from the body.

Barash Ch. 11

A

Elimination

144
Q

Most drugs that are excreted unchanged from the body are (____) and therefore readily pass into urine or stool.

Barash Ch. 11

A

Hydrophilic

145
Q

What enzymatic reaction that metabolizes a drug, which tends to transform a drug into one or more polar and potentially excretable compounds?

Barash Ch. 11

A

Phase I biotransformation reactions

146
Q

What enzymatic reaction that metabolizes a drug to transform the original drug by conjugating a variety of endogenous compounds to a polar functional group of the drug, making the metabolite even more hydrophilic.

Barash Ch. 11

A

Phase II biotransformation reactions

147
Q

What is pharmacokinetics?

[V1-6]

A

How does the drug concentration change as it moves through the different compartments of your body

“what your body does to the drug”

148
Q

What is absorption?

[V1-6]

A

The process of a substance entering the systemic circulation

149
Q

Where does absorption take place in the body?

[V1-6]

A

Where absorption occurs depends on route of administration.
• If you take a drug orally – GI tract
• If you take an inhaler - lungs

150
Q

What is distribution?

[V1-6]

A

The dispersion of a substance throughout fluids and tissues of the body; Process of going from vascular space to extravascular space

151
Q

Where does distribution take place?

[V1-6]

A

Starts taking place in vascular space (plasma) and goes to extravascular space (fat, muscle, interstitial space)

152
Q

What is metabolism?

[V1-6]

A

The irreversible transformation of parent compounds into daughter compounds.

Enzymes do this biotransformation process to transform it into a more polar molecule and get it ready for elimination

153
Q

Where does metabolism take place?

[V1-6]

A

Liver

sometimes in the intestines as well

154
Q

What is elimination?

[V1-6]

A

The removal of substances from the body

155
Q

Where does elimination take place?

[V1-6]

A

Kidneys (most of the time)

156
Q

What is bioavailability?

[V1-6]

A

The fraction of the administered dose that’s reaches the systemic circulation

157
Q

What are the two main determinants of bioavailability?

[V1-6]

A

Properties of the drug and route of administration

158
Q

What is the bioavailability of a drug given IV?

[V1-6]

A

1 because the drug is given directly into circulation

159
Q

Volume of distribution

[V1-6]

A

Vd = total mass absorbed / [Concentration of plasma]

160
Q

What is volume of distribution (Vd) used for in clinical practice?

[V1-6]

A

helps providers figure out how much total drug they need to give to reach a desired plasma concentration

161
Q

Two clinical conditions that affect Vd

[V1-6]

A

Protein deficiency (low albumin levels) and increased capillary permeability (septic shock)

162
Q

Do we measure extravascular concentration or intravascular concentration to determine Vd?

[V1-6]

A

Intravascular

163
Q

Where in the liver cells does metabolism take place?

[V1-6]

A

smooth endoplasmic reticulum

164
Q

Routes of administration that do NOT undergo first pass metabolism

[V1-6]

A

Sublingual, IM, IV

165
Q

Two routes of administration that are subject to first pass metabolism

[V1-6]

A

oral and rectal

166
Q

Three possible outcomes of metabolism

[V1-6]

A

1) active molecule becomes inactive and vice versa
2) toxic to nontoxic metabolite and vice versa
3) molecule becomes more water soluble

167
Q

Drug properties that impact Vd

[V1-6]

A

Size of drug–Large drugs will stay in plasma, thus have a low Vd;
Binding–Plasma protein binding = low Vd, Extravascular protein binding = high Vd; Hydrophilic or lipophilic—Lipophilic (extravascular) = high Vd, Hydrophilic (stays in plasma) = low Vd

168
Q

What the body “does” to the drug

PPT

A

Pharmacokinetics

169
Q

Pharmacokinetics describes the __________,__________,___________, & _____________ of drugs.

PPT

A

Absorption, distribution, metabolism and elimination (ADME)

170
Q

The plasma or serum concentration range within which a drug is likely to produce its effects.

PPt

A

Therapeutic Range (TR)

171
Q

Describes the relationship between drug concentration and the response.

PPT

A

Pharmacodynamics

172
Q

process by which a drug proceeds from the site of administration to the site of measurement (usually blood, plasma, or serum)

PPT

A

Absorption

173
Q

process of reversible transfer of drug to and from the site of measurement (between blood and tissue)

PPT

A

Distribution

174
Q

process by which a drug is structurally changed for purposes of detoxification and elimination

PPT

A

Metabolism

175
Q

the irreversible loss of drug from site of measurement

PPT

A

Elimination (Excretion)

176
Q

The fraction of administered drug that reaches general circulation.

PPT

A
  • Bioavailability
177
Q

Bioavailability is influenced by

PPT

A

gut function, gut perfusion (CHF), route of administration, first-pass metabolism

178
Q

Combined action of intestinal and liver enzymes on drugs, or loss of a drug given orally, before it reaches systemic circulation.

PPT

A

First-Pass effect

179
Q

Benefits of Oral route administration

PPT

A

Non-invasive, most common, increases patient compliance

180
Q

Disadvantages of oral route administration

PPT

A

Not appropriate for all drugs, GI side effects, dosing frequency of some drugs

181
Q

Benefits and disadvantages of topical route of administration.

PPT

A

Treats local areas, decreases systemic effects, slow onset, not useful for most drugs

182
Q

Benefits and disadvantages of rectal route of administration

PPT

A

useful in unconscious patients, absorption is unpredictable, avoids first pass metabolism by the liver

183
Q

Benefits and disadvantages of Sub cutaneous & IM injections

PPT

A

Provides steady absorption of drugs, limited to non-irritating compounds, can cause tissue necrosis

184
Q

Affects how drugs are administered and supplied

PPT

A

Solubility

185
Q

Solubility is measured as a ratio of

PPT

A

oil to water partition coefficient

186
Q

Oil used in most medications is called

PPT

A

Octanol

187
Q

Medications must be ________ to cross the lipid bilayer.

PPT

A

Lipophilic

188
Q

The larger the solubility ratio the

PPT

A

More lipid soluble the substance is

189
Q

Solubility of anesthetic gases is measure using what

PPT

A

Blood to gas partition coefficient

190
Q

Most drugs are absorbed by

PPT

A

Passive diffusion

191
Q

Most drugs are salts of

PPT

A

Weak acids or weak bases

192
Q

Drugs are preferentially absorbed in which form

PPT

A

Unionized form

193
Q

The fraction of the drug available in unionized form depends on

PPT

A

The Dissociation Constant (pKa) & the pH of the environment

194
Q

The more ________, the higher the absorption

PPT

A

Lipophilic

195
Q

The pH at which ionized and unionized forms are in a 1:1 ratio

PPT

A

pKa

196
Q

pH is defines as

PPT

A
  • log [H+]
197
Q

pH for weak acids to be absorbed

PPT

A

LOW

198
Q

pH for weak bases to be absorbed

PPT

A

High

199
Q

With weak acids as pH increases, % ionized form ________

PPT

A

increases

200
Q

With weak bases as pH increases, % ionized form __________

PPT

A

Decreases

201
Q

The active form of the drugs

PPT

A

Unionized form

202
Q

In weak bases if pH>pKa than what form predominates

PPT

A

Unionized

203
Q

In weak bases if pH

A

Ionized

204
Q

In weak acids if pH

A

Unionized

205
Q

In weak acids if pH>pKa than what form predominates

PPT

A

Ionized

206
Q

Most drugs move across membranes by

PPT

A

simple diffusion

207
Q

The rate at which drugs diffuse through membranes is given by what equation

PPT

A

Fick’s equation

208
Q

Diffusion rate is dependent on __________ and __________

A
  1. [drug]
  2. gradient across a membrane

(Fick’s equation)

209
Q

drug properties that effect their transfer across membranes

PPT

A
  1. Molecular size
  2. degree of ionization
  3. lipid solubility
  4. protein binding
210
Q

Other factors that effect the transfer of drugs across membranes

PPT

A
  1. Blood flow to target tissue

2. [gradient] of drug across membranes

211
Q

Transports drug molecule to site of activity

PPT

A

Vasculature

212
Q

Carrier mediated process, moves down the concentration gradient

PPT

A

Facilitated Diffusion

213
Q

Carrier mediated, requires energy, can move against concentration gradient

PPT

A

Active Transport

214
Q

Passive diffusion ________ be saturated

PPT

A

CANNOT

215
Q

Two main plasma proteins that drugs bind to

PPT

A

Albumin & Alpha1-acid glycoprotein

216
Q

Protein Bound drugs stay in

PPT

A

the intravascular space

217
Q

Patients with hypoproteinemia are more sensitive to IV drugs as a result of

PPT

A

Decreased protein binding

218
Q

_______% of circulation thiopental is protein-bound

PPT

A

65-85%

219
Q

Administration route that bypasses absorption

PPT

A

IV

220
Q

Organs that have enzymes that metabolize drugs

PPT

A

Liver, GI tract, Lung

221
Q

Metabolites may be

PPT

A

active or inactive

222
Q

Active metabolite of codeine

PPT

A

morphine

223
Q

metabolism that makes the drug more polar and water soluble

PPT

A

Phase I Reactions

224
Q

Phase 1 reactions include

PPT

A

oxidation, reduction, and hydrolysis

225
Q

Phase II reactions are

PPT

A

conjugation reactions

226
Q

Examples of Phase II conjugation reactions

PPT

A

Glucuronidation, acetylation,

sulfation

227
Q

The const common phase II conjugation reaction

PPT

A

Glucuronidation

228
Q

______ acetylators are more prone to toxicity with amides

PPT

A

SLOW (50% caucasians)

229
Q

Population that has a high percent of fast acetylators

PPT

A

Asian

230
Q

Phase I metabolism is enzymatic therefore it can be

PPT

A

Saturated

231
Q

Metabolism of drugs in hepatocytes of the liver occurs in

PPT

A

Smooth endoplasmic reticulum (SER)

232
Q

loss of electrons

PPT

A

Oxidation

233
Q

Gain of electrons

PPT

A

Reduction

234
Q

Addition of -OH group to a molecule

PPT

A

Hydroxylation

235
Q

Break down of molecules by the addition of water

PPT

A

Hydrolysis

236
Q

When a drug increases the amount of available enzymes

PPT

A

Induction

237
Q

Induction results in

PPT

A

shorter half-life

238
Q

Phase II reactions are also known as

PPT

A

synthetic reactions

239
Q

Common phase II reactions involve the attachment of __________ to the molecule, rendering the compound water soluble

PPT

A

a sugar group

240
Q

Orally given drugs are carried via portal vein circulation to the liver where they are metabolized

PPT

A

First Pass metabolism

241
Q

What is the most important patient specific factor factor that influences elimination

PPT

A

Renal Function

242
Q

Elimination occurs through 2 processes

PPT

A

Metabolism & excretion

243
Q

Irreversible loss of a drug in the chemically unchanged form

PPT

A

Excretion

244
Q

The primary site of excretion

PPT

A

Kidney

245
Q

Rate of drug removal at a given time

PPT

A

Clearance (CL)

246
Q

Theoretical volume of plasma that is completely cleared of drug at a given time

PPT

A

Clearance (CL)

247
Q

Units of clearance

PPT

A

mL/min

248
Q

formula used to calculate creatinine clearance

PPT

A

Cockroft-Gault equation

249
Q

Creatinine clearance (CLcr) is needed in order to determine

PPT

A

Dosing regimen

250
Q

Relates to the amount of the drug in the body to the concentration of the drug in the plasma

PPT

A

Volume of Distribution (Vd)

251
Q

Hypothetical value that tells us about distribution characteristics of a drug

PPT

A

Apparent volume

252
Q

Formula for Vd

PPT

A

Dose/Cp0

253
Q

Units for Vd

A

L/kg

254
Q

Used to determine if a drug is removed by dialysis

PPT

A

Vd

high Vd are not removed effectively

255
Q

Time it takes for the drug concentration in the plasma to fall by one half

PPT

A

Elimination Half-Life (t1/2 beta)

256
Q

How many half-lives does it take for a drug to reach a steady state

PPT

A

4 to 5 half lives (Video says 4.5)

257
Q

Have a proportionally larger extracellular fluid (ECF) volume than adults

PPT

A

Neonates (up to 18 months)

258
Q

ECF in adults

A

~ 20%

259
Q

ECF in neonates

A

~ 40%

260
Q

A higher Vd results in

PPT

A

Longer time for elimination

261
Q

In the Two-compartment model the central compartment (VRG) can be sampled through

PPT

A

the blood

262
Q

In the two compartment model, this compartment cannot usually be sampled

PPT

A

Peripheral compartment

263
Q

In _________, a constant amount of drug is eliminated per unit time.

PPT

A

Zero Order Kinetics

264
Q

In zero order kinetics, __________ can occur as a result of constant drug elimination regardless of drug concentration.

PPT

A

Accumulation

265
Q

In First order Kinetics a ____________ is eliminated per unit time.

PPT

A

Constant fraction

266
Q

Most drugs undergo which kinetics

PPT

A

First order Kinetics

267
Q

In the first order kinetics two compartment model the fast decline in [drug plasma] represents (curvilinear part of graph)

PPT

A

distribution from central to peripheral compartment

268
Q

In the first order kinetics two compartment model the slow decline in [drug plasma] represents (linear part of graph)

PPT

A

Elimination

269
Q

Formula for T1/2beta

PPT

A

0.693Vd/Cl

270
Q

What is the value for the proportionality constant

PPT

A

0.693

271
Q

Elimination constant

PPT

A

Ke

272
Q

Formula to T1/2

PPT

A

T1/2 = 0.693/Ke

273
Q

Css represents where the rate of infusion = the rate of ___________

PPT

A

Elimination

274
Q

The time necessary for plasma drug concentration to fall by 50% or other percentage after a continuous infusion of specific duration.

PPT

A

Context Sensitive Half-Time

275
Q

How far plasma concentration must decrease to reach levels compatible with awakening.

PPT

A

Time to recovery

Anesthesia Pharm. I (4 decks)

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