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ANESTHESIA PHARM 1 > Basic Concepts of Physiology > Flashcards

Basic Concepts of Physiology Flashcards

1
Q

‘what the BODY does to drugs”

A

pharmacokinetics

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2
Q

absorption, distribution, metabolism, and excretion of drugs

A

pharmacokinetics

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3
Q

determines the concentration of a given drug at its target receptors, may reflect individual differences between patients

A

pharmacokinetics

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4
Q

“what a DRUG does to the body”

A

pharmacodynamics

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5
Q

intrinsic sensitivity/responsiveness of the body’s receptors to a drug

A

pharmacodynamics

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6
Q

chemical structure influences what plasma concentration of a drug is necessary to evoke a response

A

pharmacodynamics

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7
Q

INTRINSIC SENSITIVITY also varies among patients, and is determined by measuring the concentration needed for the desired effect because the sensitivity varies from person to person

A

pharmacodynamics

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8
Q
A

pharmacokinetics

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9
Q
A

pharmacodynamics

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10
Q
  • Specific protein molecule of lipid bilayer of cell membrane with which an administered drug interacts
  • interaction with drug causes changes in the cell to produce drug’s effects
A

receptor

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11
Q
  • Different types cause drugs to exert their effects in different ways
  • concentration (number) at site of action may change
A

receptor

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12
Q

___________ __________ receptors change conductance of cell, altering ion influx/efflux

A

voltage-sensitive

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13
Q

____________ ___________ receptors cause conformational change and thus alter cell membrane. Effects may INHIBIT or ENHANCE the functions of cells

A

ligand-gated

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14
Q

will cause downregulation of receptors to try and avoid the abundance of catecholamines

A

pheochromocytoma

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15
Q

___________ will upregulate the number of receptors. if you abruptly discontinue use, you will get an exaggerated effect

A

Beta antagonists

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16
Q

FOUR TYPES OF RECEPTORS

A
  1. MEMBRANE RECEPTORS
  2. LIGAND-GATED ION CHANNEL
  3. VOLTAGE-GATED ION CHANNEL
  4. ENZYME
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17
Q

ex: Beta-AR

A

membrane receptor

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18
Q

ex: GABAa

A

ligand-gated ion channel

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19
Q

ex: Na+ channel

A

voltage-gated ion channel

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20
Q

ex: phosphodiesterase inhibitors

A

enzyme

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21
Q

3D structural orientation of molecules

A

stereochemistry

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22
Q

2 molecules having the same chemical composition but different orientations around a central atom – mirror images

A

entantiomers

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23
Q
  • may bind to receptor sites differently, contribute to differnces in absoption, distribution, clearnce, potency, toxicity.
  • one may cause clinical effect, the other may cause side effects
A

entantiomers in racemic mixture

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24
Q

2 entantiomers present in EQUAL proportion

A

racemic mixture

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25
Q

“S” entantiomer: tetragenic, peripheral neuritis

“R” entantiomer: effective sedative, sleep med, and cure for morning sickness

A

Thalidomide

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26
Q
  • a drug that produces its clinical effect by binding to a receptor and activating it
  • mimetic
A

agonist

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27
Q
  • a drug that produces its clinical effect by binding to a receptor WITHOUT activating it and simultaneously prevents an agonist from stimulating it
  • blocking
A

antagonist

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28
Q

drug that combines directly with its receptor to trigger its physiologic response

A

direct-acting receptor agonist

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29
Q

drug that produces its physiologic response by:

  1. inducing the release/increasing the concentration of ENDOGENOUS substrate (neurotransmitter or hormone) at receptor site
  2. OR inhibits inactivation of neurotransmitter, (inhibiting reuptake or degadative metabolism)
  3. DRUG ITSELF DOES NO INTERACT WITH RECEPTOR
A

indirect-acting receptor agonist

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30
Q
  • Example of direct-acting receptor agonist
  • binds to alpha receptors in the peripheral vascular system and directly activates them to cause vasoconstriction
A

Phenylephrine

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31
Q

Example of indirect-acting receptor agonist

  • induces the RELEASE of norepinephrine from post synaptic nerve endings
  • denervation or depletion of teh neurotransmitter (after repeated doses, for example) will cause the administered drug to have less effect
A

ephedrine

amphetamines

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32
Q

receptor inhibition which can be overcome by INCREASING the concentration of the agonist at the receptor site (reversible blockade)

A

competitive receptor antagonism

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33
Q

receptor inhibition which CANNOT be overcome by increasing the concentration of the agonist (irreversible blockade)

A

noncompetitive receptor antagonism

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34
Q

drug response: unusually low dose triggers pharmoacological effect – very sensitive patients

A

hyperactive drug response

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35
Q

drug response: allergic to drug

A

hypersensitive drug response

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36
Q

drug response: patient requires large dose for desired effect, often due to chronic exposure (tolerance)

A

hyporeactive drug response

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37
Q

drug response: decreased effectiveness of a drug with multiple doses (ex. Ephedrine)

A

tachyphylaxis

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38
Q

drug response: second drug administered with the first will produce an effect EQUAL to the sum of the 2 doses if administered independently

A

additive drug response

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39
Q

drug response: 2 drugs administered together may produce a greater effect than either drug given alone

A

synergistic drug response

40
Q

drug response: 2 drugs administered together have LESSER effect than either given alone

A

antagonistic drug response

41
Q

drug response: pharmacologically inactive compounds designed to maximize the amount of active species that reaches its site of action (ACE inhibitors)

A

prodrug drug response

42
Q

route of administration: via the alimentary tract

  • oral (PO)
  • Sublingual
  • rectal
A

Enteral

43
Q

route of administration: “aside from” the alinentary tract

  • IV
  • IM
  • SC
  • pulmonary
  • intraarterial
  • intrathecal
  • nasal
  • transdermal, topical
A

parenteral

44
Q

routes of administration:

PO drugs from GI enter PORTAL VENOUS blood and travel to liver before being delivered to tissue

LIVER begins breakdown, accounting for differences between IV and PO administration of drug

A

oral administration of drugs

FIRST PASS HEPATIC METABOLISM

45
Q

routes of administration:

ADVANTAGES: convenient, cheap

DISADVANTAGES: GI irritation, destruction of drug by gastric acid, alterations with food

A

Oral administration:

FIRST PASS HEPATIC METABOLISM

46
Q

routes of administration: rapid absorption through buccal mucosa, no first pass metabolism

(nitroglycerine: if swallowed, NO EFFECT)

A

sublingual administration

47
Q

route of administration: absorbed into superior hemrrhoidal veins, good for vomitting pts and peds

A

rectal administration

48
Q

routes of administration: immediate onset, CANNOT RETRIEVE AN OVERDOSE

A

IV administration

49
Q

routes of administration: absorption rate depends on blood flow;nutrition for comatose or uncooperative pts

A

IM and SC administration

50
Q

routes of administration: volatile drugs and aerosols

A

pulmonary administration

51
Q

routes of administration: FEW DRUGS GIVEN THIS WAY!!! DON’T GIVE DRUGS THROUGH A-LINE!!!

A

intraarterial administration

52
Q

routes of administration: into CSF

A

intrathecal admnistration

53
Q

routes of administration: for LOCAL effect at application site

A

topical administration

54
Q

routes of administration: for SYSTEMIC effect but given on skin (patch)

A

transdermal administration

55
Q

Name each layer

A

epidermis

dermis

subcutaneous tissue

muscle (with vein)

56
Q

site-specific factors affecting absorption

1.

2.

3.

A
  1. blood flow from site
  2. surace area for absorption
  3. solubility of drug at site
57
Q

(theory) the body is composed of multiple compartments having calculated volumes

circulating blood

central nervous system

liver

fat

(etc.)

A

Compartment models

we can examine the pharmacokinetics of drugs we administer in terms of what compartments they travel to and what happens when they reach those compartments (clinical effect, metabolism, storage, etc.)

58
Q

components of 2-compartment model

1.

2.

A
  1. Central component
  2. Peripheral component
59
Q

2-compartment model: rapid uptake of drug

  • includes intravascular fluid and highly perfused tissues like the lungs, heart, brain, kidneys, and liver
  • 75% of cardiac output, 10% of body mass
A

Central compartment

60
Q

2-compartment model: slower uptake of drug

  • includes less vascular tissues like fat, bone, and inactive skeletal muscle
A

peripheral compartment

61
Q

drugs equilibrate between compartments and are eventually eliminated from the central compartment

A

2-compartment model

62
Q

(concept) the total approximation of all the compartments to which a drug goes

relates the amount of drug in the body to the concentration of drug in the blood or plasma

A

volume of distribution (Vd)

63
Q

indicates that a drug is extensively taken up by the tissues

A

large volume of distribution (Vd)

(the greater the Vd, the longer the elimination half-life)

64
Q

indicates that the majority of drug remains in plasma

A

small volume of distribution

65
Q

plasma concentration curve phases: immediately after administration of drug

movement from central to peripheral compartments

A

distribution phase

66
Q

plasma concentration curve phases: more gradual as drug is removed from circulation

A

elimination phase

67
Q

ex: drugs travel on proteins in the blood

1.

2.

A
  1. albumin
  2. alpha-1-acid glycoproteins
68
Q

protein binding: binds acidic drugs (eg, barbiturates)

A

albumin

69
Q

protein binding: binds basic drugs (eg, local anesthetics)

A

AGP (alpha-1-acid glycoproteins)

70
Q

proportional relation: protein binding vs. volume of distribution

A

degree of protein binding is INVERSELY PROPOTIONAL to volume of distribution

degree of protein binding = 1/Vd

71
Q

pharmacologic implication of drug-protein binding

1.

2.

3.

A
  1. only unbound drug crosses cell membranes to reach its site of action
  2. free drug is more readily available for elimination
  3. drug that is protein bound is NOT pharmacologically inert
72
Q

drug-protein binding: as soon as unbound drug leaves circulation, some drug will dissociate from binding sites, which tends to restore the free drug concentration

A

law of mass action

73
Q

what determines the degree of ionization of a drug?

A
  • pK of substrate
  • pH of surrounding fluid

whether or not a drug exists predominately in an ionized vs. nonionized state affects how well it permeates membranes

if a drug can’t diffuse through a cell membrane, its travel is limited

74
Q

____________ __________ drugs have:

  • impaired absorption from GI
  • limited hepatic metabolism
  • increased excretion (in unchanged form) facilitated by kidneys (drug will not be reabsorbed)
  • poor lipid solubility
A

highly ionized

75
Q

what form of ionization of a drug is more lipid soluble and can readily diffuse across a cell membrane?

A

non-ionized drugs

76
Q

what form of ionization of a drug is less lipid soluble and can not readily diffuse across a cell membrane?

A

ionized

77
Q

when ________ & _________ are __________, 50% of the drug exists in both the IONIZED and NONIONIZED from

A

when pK & pH are IDENTICAL

78
Q

ACIDIC drugs are _________ _________ at alkaline pH

ex., barbituates

A

highly ionized

79
Q

BASIC drugs are __________ ___________ at acidic pH

ex., opioids, local anesthetics

A

highly ionized

80
Q

if membrane separates areas of differing pHs, then the nonionized portion of a drug diffuses and equilibrates, but the ionized form does not, resulting in large concentration differences on either side of membrane

A

ion trapping

81
Q

ex., organ systems that induce ion trapping:

1.

2.

3.

A
  1. stomach
  2. renal tubules
  3. placenta

degree of ionization is different on each side of the membrane, and nonionized form equilibrates

82
Q

opioids and local anesthetics are ___________ drugs that ___________ the placenta to fetus.

Fetal pH is ________________, thus drug is converted to ________________ form and accumulates…can result in fetal distress

A

basic

cross

acidic

ionized

83
Q

chemical process where drug is altered in the body

A

biotransformation

84
Q

biotransformation: drug is converted to polar metabolite

  • oxydation, reduction, hydrolysis, acetylation
  • can result in activation, change, or inactivation of drug
A

metabolic biotransformation

Phase I

85
Q

biotransformation: drug forms conjugate with endogenous substrates (carbohydrates, amino acids) to form water soluble metabolites, readily excreted from body

results in loss of biological activity of a compound

A

metabolic biotransformation

phase II

86
Q

removal of drug from plasma

important concept to achieve steady state: want to dose amount that is leaving

A

clearance

87
Q

ester hydrolysis

A

clearance: kidneys

88
Q

hoffman elimination

A

clearance: liver

89
Q

ezymatic alteration of drug’s chemical structure

4 major types of reactions:

1.

2.

3.

4.

A

metabolism

  1. oxidation
  2. reduction
  3. conjugation
  4. hydrolysis
90
Q

refers to all the processes that remove drugs from the body, either excretion of unchanged drug or metabolism and subsequent excretion of metabolites

A

elimination

91
Q

a temperature- and pH-dependent process

(rate of degradation in vivo is highly influenced by body pH and temperature)

A

Hofmann eliminiation

92
Q

Hofmann elimination: an increase in body temp favors _______________

A

elimination

93
Q

Hofmann elimination: a decrease in temperature _____________ __________ _______________

A

slows down elimination

94
Q

clearance: drugs that are cleared efficiently by the liver are restricted in their rate of elimination not by intrahepatic process, but by

________________________________________

A

the rate at which they can be transported in the blood to the liver

95
Q

metabolism: typically conversion from ACTIVE, LIPID SOLUBLE drugs into ________________________________________

A

INACTIVE, WATER SOLUBLE metabolites

drugs must be transformed into hydrophilic metabolites for elimination

96
Q

drug clearance from liver dependent on:

1.

2.

3.

A
  1. hepatic blood flow
  2. intrinsic ability of liver to irreversibly eliminate drug from the blood
  3. the extent of drug binding to plasma proteins or other blood constituents

ANESTHESIA PHARM 1 (4 decks)

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