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SRNA4TopicsAnesthesia > M&M PharmPrinciples > Flashcards

M&M PharmPrinciples Flashcards

1
Q

Process by which drug moves from site of admin to bloodstream

A

Absorption

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2
Q

Absorption is influenced by characteristics of drugs such as

A

Solubility
Pka
site of absorption
dose

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3
Q

Fraction reaching systemic circulation is

A

Bioavailability

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4
Q

Preferentially absorbed form of the drug is

A

nonionized

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5
Q

Acidic environment favors Absorption of (AAA)

A

Acidic drugs

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6
Q

Basic environment favors ABSORPTION of

A

Basic drugs

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7
Q

This route may be limited by first pass metabolism by the liver

A

Oral

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8
Q

Routes bypasses liver and first pass metabolims

A

SL or buccal

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9
Q

Provide prolonged continuous administration

A

Transdermal

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10
Q

What is the effective barrier to all but SMALL, highly potent lipid soluble drugs

A

Stratum Corneum

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11
Q

SC and IM injection depends on what

A

Diffusion from the site of injection to the circulation

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12
Q

During SC and IM , diffusion from the site of injection to the circulation depends on what

A

Blood flow to the area

Carrier vehicle

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13
Q

Which one is absorbed faster, solution, or suspensions?

A

SOLUTIONS

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14
Q

Irritating preparations can causes

A

pain and tissue necrosis

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15
Q

IV injections and absorption

A

Bypasses the process of absorption because the drug is placed directly into the bloodstream

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16
Q

The process of circulation of a drugs in the blood throughout the body is

A

Distribution

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17
Q

Name all the highly perfused organs?

A 
Brain
Heart
Liver 
Endocrine glands
Kidneys
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18
Q

Less perfused organs are? what is the significance?

A

Fat and skin ; equillibrate more slowly because of low blood flow.

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19
Q

What law do drug molecule obey?

A

law of mass action

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20
Q

Explain the law of MASS ACTION that drug molecule obey? (Gradient)

A

When plasma concentration exceeds the concentration in tissues, drugs moves from plasma to tissue. When the plasma concentration is less than the concentration in the tissue, drugs moves from TISSUE back to PLASMA

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21
Q

Binds many acidic drugs what protein?

A

Albumin

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22
Q

Binds many BASIC drugs what protein

A

Alpha 1 acid glycoprotein (AAG)

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23
Q

Diseases where albumin is decreased?

A

Renal
Liver,
Chronic CHF
malignancies

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24
Q

Alpha 1 acid glycoprotein (AAG) are increased in

A

TRAUMA( including surgery)
Infection
MI
Chronic pain

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25
Q

Alpha 1 acid glycoprotein (AAG) are decreased in

A

Pregnancy

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26
Q

The apparent volume into which a drugs has been distributed is called its

A

Volume of distribution (Vd)

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27
Q

How is Vd determined?

A

dose divided by concentration : Vd = Dose/concentration

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28
Q

Most anesthetic drugs are lipophillic or hydrophillic

A

liphophillic

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29
Q

Most anesthetic drugs are liphophillic resulting in a Vd that

A

Exceeds total body water .

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30
Q

What is total body water?

A

~ 40 L

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31
Q

The Vd of fentanyl is about

A

350L

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32
Q

The Vd of propofol may exceed

A

5000L

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33
Q

The chemical alteration of a drug is the ______aka____

A

biotranformation; metabolism

34
Q

Primary organ of metabolism

A

liver

35
Q

The primary end products of metabolism characteristics?

A

INACTIVE and WATER SOLUBLE

36
Q

What drugs characteristics allows excretion by the kidney?

A

WATER SOLUBLE

37
Q

Metabolism can be divided into 2 reactions

A

Phase I and Phase II

38
Q

What happens during phase I reaction? name them

A

Convert drugs into a MORE POLAR metabolites through Oxidation, reduction or HYDROLYSIS

39
Q

What happens during phase II reaction? name the process involved?

A

Phase II couples or CONJUGATE a parent drug or a phase I metabolite with an ENDOGENOUS SUBSTRATE, to form a water-soluble metabolites that are eliminated in urine or stool.

40
Q

Example of endogenous substrate that may be used by phase II reaciton

A

GLUCORONIC ACID

41
Q

Can a phase I metabolites be excreted without undergoing PHASE II biotransformation?

A

YES

42
Q

Can a Phase II reaction precede or occur without a phase I reaction?

A

YeS

43
Q

Volume of plasma of blood CLEARED of drug per unit of time is

A

HEPATIC CLEARANCE

44
Q

What is hepatic clearance?

A

BLOOD FLOW times the HEPATIC EXTRACTION RATIO

Clearance = Q x E

45
Q

What is the hepatic extraction ratio?

A

Fraction of drug entering the liver that is metabolized.

46
Q

If the extraction ration is 50%, what is hepatic clearance

A

It is half of liver blood flow.

47
Q

Principal organ of excretion

A

Kidneys

48
Q

Kidneys: explain what happens with ionized and unionized fraction of the drug?

A

Ionized fraction of Drug EXCRETED IN URINE

NONionized fraction of drugs get REABSORBED in the RENAL TUBULES

49
Q

What part of kidney are nonionized drugs absorbed at

A

RENAL tubules.

50
Q

The rate of elimination of a drug from kidney excretion is the

A

Renal clearance

51
Q

Renal clearance formula

A

Clearance = Q x E (renal extraction ratio)

52
Q

What is enterohepatic circulation?

A

DRUG excreted into the bile and THEN REABSORBED in the intestine

53
Q

Multi-compartment models provide

A

Mathematical framework to relate drugs dose to a drug concentration overtime

54
Q

2 compartment drug model phases

A

Distribution or ALPHA phase

Elimination or BETA phase

55
Q

Explain the distribution or alpha phase

A

After an initial bolus , there is a RAPID drop in concentration over the first few minutes as drugs quickly DIFFUSES into PERIPHERAL compartments

56
Q

2 compartment graph explanation
x-axis
Y-axis
SHAPE

A

X-axis is the –> TIME after dose
y-axis is the –> PLASMA Concentration
STEEP drop then slow downward slope

57
Q

Explain the Elimination or beta phase

A

Continued drop in concentration but LESS STEEP decline in plasma concentration

58
Q

What is pharmacodynamics

A

How drugs affects the body

59
Q

Concepts of pharmacokinetics are

A 
ADME 
Absorption
Distribution
Metabolism
Excretion
60
Q

Concepts of PHARMACODYNAMICS are (PET)

A

POTENCY
EFFICACY
Therapeutic window

61
Q

What does the dose response curve explain?

A

relationship between drug dose and pharmacologic effect

62
Q

The shape of drug dose and pharmacological effect is

A

SIGMOIDAL in a log scale.

63
Q

The sigmoidal shape of the dose response curve means that

A

a certain amount of drug must be present before there is any measurable physiologic response.

64
Q

The left side of the dose response curve is flat until

A

the drug concentration reaches a minimum threshold.

65
Q

The right side of the dose response curve is flat until

A

reflecting the MAXIMUM physiological response of the body.

66
Q

What is the therapeutic window defined as

A

Difference between the concentration associated with a desired therapeutic effect and the concentration associated with a toxic drug response.

67
Q

Therapeutic index is

A

Toxic concentration / therapeutic coencentration

68
Q

What are drug receptors usually made of

A

Usually macromolecules typically proteins that bind a drug and mediate the drug response.

69
Q

Bind a drug

A

Agonist

70
Q

Reverses the effects of the agonist

A

Antagonist

71
Q

Occurs when the ANTAGONIST competes with THE AGONISTS for the binding site , each displacing the other.

A

COMPETITIVE ANTAGONISM

72
Q

WHEN the ANTAGONISTS through COVALENT BINDING or another process PERMANENTLY impaired the drug’s access to the receptor?

A

NONCOMPETITIVE ANTAGONISM

73
Q

Drugs effect is governed by what?

A

FRACTION of receptors occupied

74
Q

Fraction of receptors occupied is based on

A

concentration of drug
Concentration of a receptor
AFFINITY of drug to the receptor.

75
Q

What is the RECEPTOR occupancy importance

A

the first step in mediating the drug effect.

76
Q

Binding of a drug to a receptor can trigger MULTIPLE STEPS including

A

opening or closing of ion channel
activating of a G protein
activating an intracellular kinase
Interaction directly with a cellular structure, binding directly to DNA

77
Q

Prolonged binding and activation of a receptor may lead to (PROLONGED AGONIST)

A

HYPO reactivity (desensitization) and TOLERANCE

78
Q

If the binding of Endogenous ligand is chronically blocked, receptors may proliferate, resulting in (PROLONGED ANTAGONIST)

A

HYPERREACTIVITY and INCREASED SENSITIVITY.

79
Q

Beta-blockers cause subtype-specific upregulation such that nonselective beta-blockers increase the density of both.

A

beta1- and beta2-adrenoceptors whereas beta1-selective antagonists upregulate only beta1-adrenoceptors

80
Q

Chornic BETA blockers, As a consequence of increased sympathetic tone, cardiac beta-receptors are down-regulated in the

A

failing ventricle and dilated cardiomyopathy.

81
Q

However, in the presence of acute myocardial ischemia there is rapid upregulation of beta-receptors in the presence of _____________which forms the basis of beta blockade therapy for treatment of ACS.

A

elevated circulating catecholamines,

SRNA4TopicsAnesthesia (47 decks)

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