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2S PCL&T 1st shift > Unit 1 > Flashcards

Unit 1 Flashcards

1
Q

Study of substances that interact with living systems through chemical processes by binding to regulatory molecules and activating/inhibiting normal body processes

A

Pharmacology

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2
Q

Science of substances used to prevent/diagnose/treat disease

A

Medical Pharmacology

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3
Q

Branch of pharmacology dealing with undesirable effects of chemicals on living systems

A

Toxicology

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4
Q

Body to Drug; Absorption, distribution, elimination of drugs

A

Phamacokinetics

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5
Q

Actions of chemical on organism

A

Pharmacodynamics

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6
Q

Science of drug preparation and the medical uses of drugs, precursor to pharmacology developed around end of 17th century

A

Material Medica

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7
Q

Developed experimental physiology and pharmacology

A

Francoi Magendi

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8
Q

began to develop the methods of experimental physiology and pharmacology

A

François Magendie and his student Claude Bernard

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9
Q

Biological substrate of drug action

A

Receptor

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10
Q

Receptors for which no ligand has been discovered and whose function can only be surmised

A

Orphan Receptor

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11
Q

Relation of individuals genetic makeup and response to specific drugs, relationships between receptor families and evolution of receptor proteins

A

Pharmacogenomics

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12
Q

(2) small segments of RNA that interfere with protein synthesis with extreme selectivity

A

SiRNAs and miRNAs
Small interfering RNAs and micro RNAs

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13
Q

short nucleotide chains synthesized to be complementary to natural RNA/DNA, can interfere with readout of genes and transcription of RNA

A

ANOs
Antisense oligonucleotides

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14
Q

Any substance that brings about change in biological function through chemical actions

A

Drug

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15
Q

Interact with other drugs directly

A

Chemical Antagonist

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16
Q

Interact exclusively with water molecules

A

Osmotic Agents

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17
Q

Drugs that are exclusively harmful

A

Poison

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18
Q

Poisons of biological origin, synthesized by plants/animals

A

Toxin

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19
Q

Very weak, important for highly lipid soluble drugs

A

Hydrophobic Bonds

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20
Q

True or False: drugs that bind weakly to receptors are more selective

A

True

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21
Q

Drugs with 2 chiral centers have __ diastereomers

A

4

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22
Q

True or False: an entantiomer has different potency than another according to best fit and duration

A

True

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23
Q

True or False: most drugs are one active isomer rather than a racemic mixture

A

False

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24
Q

Kd, concentration for 50% saturation of receptors, inversely proportional to affinity of drug for receptors

A

dissociation constant

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25
Q

Makes final change and may be in receptor molecule or separate, sometimes with a coupling mechanism

A

Effector

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26
Q

Bind and activate receptor to directly/indirectly cause effect

A

Agonist

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27
Q

Bind receptor to compete and prevent binding by other molecules

A

Antagonist

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28
Q

True or False: action of the antagonist can be overcome by increasing dosage of the agonist

A

True

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29
Q

Bind to same receptor but don’t prevent agonist from binding; may enhance or inhibit action of agonist

A

Allosteric Drugs

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30
Q

True or False: action of allosteric drug can be overcome by increasing agonist concentration

A

False

31
Q

Thermodynamic property; in absence of agonist some receptors are in active form and have same effect as agonist-induced activity

A

Constitutive Activity

32
Q

Constitutive activity depends on receptor _____, concentration of ____ molecules, and number of _____

A

Density, coupling, effectors

33
Q

At saturating concentration activate receptor-effector systems to max extent and shift all receptors to active pool

A

Full Agonist

34
Q

Bind same receptors and activate but do not evoke same response regardless of concentration, don’t fully stabilize active receptor form as effectively, low intrinsic activity of

A

Partial Agonist

35
Q

True or False: partial agonists act as agonists if no full agonist is present or antagonist if full agonist is present

A

True

36
Q

Fix fraction of active and inactive receptor in same amounts as if there were no drug present, no change in activity is observed, prevent agonist action

A

Antagonist

37
Q

Drug has stronger affinity for inactive receptor than active, reduced constitutive activity and result in opposite effect of agonists

A

Inverse Agonist

38
Q

Not until the concepts of rational therapeutics, especially that of the __________, were reintroduced into medicine—only about 60 years ago—did it become possible to adequately evaluate therapeutic claims.

A

controlled clinical trial

39
Q

3 General Principles

A

1) that all substances can under certain circumstances be toxic;
2) that the chemicals in botanicals (herbs and plant extracts, “nutraceuticals”) are no different from chemicals in manufactured drugs except for the much greater proportion of impurities in botanicals; and
3) that all dietary supplements and all therapies promoted as health-enhancing should meet the same standards of efficacy and safety as conventional drugs and medical therapies

40
Q

T/F: there should be artificial separation between scientific medicine and “alternative” or “complementary” medicine.

A

False, there should be no artificial separation

41
Q

To interact chemically with its receptor, a drug molecule must have the (4)

A

appropriate size, electrical charge, shape, and atomic composition.

42
Q

aspirin, atropine

A

solid drugs

43
Q

nicotine, ethanol

A

liquid drugs

44
Q

nitrous oxide, nitric oxide, xenon

A

gaseous drugs

45
Q

fluoride, lithium, iron, and heavy metals

A

inorganic elements

46
Q

T/F Many organic drugs are weak acids or bases

A

True

47
Q

What is the range of MW most drugs have?

A

100 - 1000

48
Q

To achieve such selective binding, it appears that a molecule should in most cases be at least __ MW units in size

A

100

49
Q

T/F Drugs much larger than MW 1000 do not diffuse readily between compartments

A

True

50
Q

T/F: Very large drugs (usually proteins) must often be administered orally into the compartment where they have their effect

A

False, it is administered directly

51
Q

3 Major types of Chemical forces/bonds:

A

Covalent, Electrostatic, Hydrophobic

52
Q

vary from relatively strong linkages between permanently charged ionic molecules to weaker hydrogen bonds and very weak induced dipole interactions

A

Electrostatic Bonds

53
Q

the phenomenon of _____ is so common in biology that more than half of all useful drugs are chiral molecules; that is, they can exist as enantiomeric pairs.

A

chirality (stereoisomerism)

54
Q

implies the ability to predict the appropriate molecular structure of a drug on the basis of information about its biologic receptor.

A

Rational drug design

55
Q

Drug (D) + ___ → drug-receptor-effector complex → effect

A

receptor-effector (R)

56
Q

D + R → drug-receptor complex → __ → effect

A

effector molecule

57
Q

D + R → D-R complex → activation of __ → effector molecule → effect

A

coupling molecule

58
Q

Inhibition of metabolism of __ → increased activator action on an effector molecule → increased effect

A

endogenous activator

59
Q

final change in function is accomplished by an__.

A

effector mechanism

60
Q

Some drugs mimic agonist drugs by __ the molecules responsible for terminating the action of an endogenous agonist

A

inhibiting

61
Q

This effect, occurring in the absence of agonist, is termed

A

constitutive or basal activity

62
Q

the presence of the antagonist at the receptor site will block access of agonists to the receptor and prevent the usual agonist effect. Such blocking action can be termed as

A

neutral antagonism

63
Q

the drug will reduce any constitutive activity, thus resulting in effects that are the opposite of the effects produced by conventional agonists at that receptor. Such drugs are termed as

A

inverse agonists

64
Q

To function as a receptor, an __ molecule must first be selective in choosing ligands (drug molecules) to bind

A

endogenous

65
Q

an inactive precursor chemical that is readily absorbed and distributed must be administered and then converted to the active drug by biologic processes—inside the body. Such a precursor chemical is called a

A

prodrug

66
Q

This requires that the drug be __ into the blood from its site of administration and __ to its site of action, __ through the various barriers that separate these compartments.

A

absorbed, distributed, permeating

67
Q

__ can be very important in facilitating transport and permeation, eg, by encapsulating the active agent in liposomes and in regulating release, as in slow release preparations.

A

Drug vehicles

68
Q

Drugs may diffuse passively through (4)

A
  1. Aqueous Diffusion
  2. Lipid Diffusion
  3. Special Carriers
  4. Endocytosis and Exocytosis
69
Q

This diffusion occurs within the larger aqueous compartments of the body (interstitial space, cytosol, etc) and across epithelial membrane tight junctions and the endothelial lining of blood vessels

A

Aqueous Diffusion

70
Q

most important limiting factor for drug permeation because of the large number of lipid barriers that separate the compartments of the body

A

Lipid diffusion

71
Q

These exist for many substances that are important for cell function and too large or too insoluble in lipid to diffuse passively through membranes, eg, peptides, amino acids, and glucose

A

Special carrier molecules

72
Q

This process is responsible for the transport of vitamin B12, complexed with a binding protein (intrinsic factor) across the wall of the gut into the blood.

A

Endocytosis

73
Q

responsible for the secretion of many substances from cells.

A

exocytosis

2S PCL&T 1st shift (1 decks)

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