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Principles of Drug Action > Test 2 > Flashcards

Test 2 Flashcards

1
Q

Agonist

A

Mimics Physiological ligand

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2
Q

Antagonist

A

Binds to part of the receptor and inhibits ligand binding.

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3
Q

Agonist differ in…

A

Affinity (1/Kd), efficacy, and or potency.

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4
Q

Partial agonist

A

Has affinity for receptor but only elicits partial response.

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5
Q

Surmountable antagonism

A

Comp inhibition reduces receptor sensitivity to agonist but does not diminish max function.

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6
Q

Biased agonist

A

Works same as agonist but only elicits a certain part of the signal transduction

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7
Q

Constitutive activity

A

Tone made by spontaneous change or receptor from rested to active states without agonist.

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8
Q

Inverse agonist

A

Lowers the constitutive activity

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9
Q

When high spare receptor

A

Graph looks like competitive inhibition, Affinity shifts right first, then later Efficacy falls when used and we see it is irreversible.

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10
Q

Functional groups control…

A

solubility, route of administration, binding, mode of action, metabolism, duration, and adverse effects.

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11
Q

FG electronic effect

A

Measures ability to donate or pull away electrons. Effected by resonance and inductive effect.

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12
Q

Inductive effect

A

How easily an atom or FG can attract electrons from other groups. Leads to H bonding.

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13
Q

Oxygen

A

Is EWG except when by resonance capable group like phenyl ring

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14
Q

Electron donating groups

A

Push electrons towards more electronegative atom. FGs with lone pairs can do this

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15
Q

Electron withdrawing groups

A

Most important in medchem. CF3 is most powerful EWG. Acids good EWG.

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16
Q

FG ionization…

A

increases hydrophilicity

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17
Q

An acid…

A

Proton donor. More pos hydrogen = more acidic

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18
Q

A Base…

A

Proton acceptor. More electron density, more basic

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19
Q

Aldehyde

A

Will not be in drug molecules because it forms covalent bonds with nuleophiles

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20
Q

Carboxylic acids

A

Good at ionizing. Will react with bases to make salts with high water solubility. EWG make them more acidic. EDG Destabilize and reduce it.

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21
Q

Esters

A

Only H bond accept

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22
Q

Amides

A

Cannot H bond accept because lone pair is in resonance with carbonyl.

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23
Q

Amines

A

Hydrogen bond donors and acceptors. When rpotonated cannot HBA. Can HBD stronger.

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24
Q

Ketones

A

Participate in hydrongen, DD and DI binding. Mostly H bonding.

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25
Q

Alchols

A

Inter/intramolecular H bonding. Bond to H2O. Terminal OH on long C chain less soluble.

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26
Q

Phenols

A

Weak organic acids

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27
Q

halogenated hydrocarbond

A

Major use is in anesthetics.

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28
Q

Aromatic hydocarbond

A

E clouds above and below ring. Van der waals and Pi Pi stacking. Aromatic rings flat and can fit where cyclohexane rings cannot.

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29
Q

Heterocycles

A

Can change around Nitrogen and whatnot. Allows tuning of H donating and accepting.

30
Q

Pharmacophore

A

Active constituents of drugs.

31
Q

Ionized

A

When an acidic FG loses its proton and becomes negatively charged (conjugate base). Or when a basic FG Gains proton and is pos charged.

32
Q

Acidity factors

A

Inorganic more acidic than organic. Resonance in a ring makes more acidic.

33
Q

Basic factors

A

Resonance pulling E density away makes less basic. More E density being pushed on say N, more basic.

34
Q

Ionization constant

A

Equilibrium between ionized and un-ionized. Ka or Pka

35
Q

%ionized =

A

100/

1+10^(Pka-ph)

36
Q

pH = PKa

A

When acid or base is 50% ionized

37
Q

Structure Influence on PKa

A

Electornegativity, H-A bond strength (weaker more acidic), A- stability, Resonance.

38
Q

Henderson H.

A

PKa= pH + log (acid form/Base form) Then to get % ionized, =(acid form/total) * 100%

39
Q

Dealing with basic FG

A

The conjugate acid is the ionized form of the basic FG. PKa refers to the conjugate acid.

40
Q

Ionization

A

Protonation or deprotonation to get charged molecule. 85% of drugs.

41
Q

Binding to active site

A

Un-ionized- H bonds, gets out of stomach

Ionized- Influence salt bridge strength and H bonds, wont get out of stomach.

42
Q

Ph and drug absorption

A

Drugs absorbed passively when unionized.

43
Q

Bioavailabliity %F

A

How quickly and how much of a particular drug reaches the blood supply. 20% Considered minimum.

44
Q

Extent of ionization controls…

A

Absorption, receptor binding, plasma protein binding, CNS penetration, and solubility.

45
Q

Drugs are hydrophobic in general

A

Binding sites are also hydrophobic

46
Q

Ethalpy gains can come from…

A

Van der waals bonding from pi pi stacking, or between alkyl, aryl, and halogen groups

47
Q

Entropy gains are achieved when…

A

Water molecules are displaced from active site and return to randomness.

48
Q

What increases order (reduces entropy) in water?

A

Adding hydrophobic compound. Lead to neg delta S, and pos G. Not favored.

49
Q

Increased entropy leads to what?

A

A negative value of G and hence a gain in energy

50
Q

If i compound is too lipophilic it may?

A

Be insoluble in aqueous, bind too strongly to plasma protein, distribute inside of lipid layers and not reach inner cell.

51
Q

LogP

A

Lipophilicity measurement of neutral compound

52
Q

Distribution coefficient LogD

A

Lipophilicity of an ionized compound

53
Q

Something that increases lipophilicity?

A

Replacing a hydrogen with a halogen.
Removing quinoline N to give carbocylcic ring.
Adding O adjacent to an N in ring.

54
Q

Why is CF3 so lipophilic?

A

Cannot be Ionized. Very E withdrawing. Reduces H bonding strength around it.

55
Q

Ways to measure molecular size

A

MW, E density, polar surface area, van der waals surface, molar refractivity.

56
Q

Rotatable bond

A

Any single non ring bond, attached to a non terminal and non hydrogen atom.

57
Q

Lipinskis rule of 5

A

MW less than 500, logP less than 5, less than 5 H bond donors, less than 10 H bond acceptors. Verber, Less than 10 rotatable bonds.

58
Q

DMPK

A

Drug metabolism, pharmacokinetics, and pharmacodynamics.

59
Q

ADMET

A

Absorption, distribution, metabolism, Excretion

60
Q

Factors that affect absorption.

A

Solubility, acid stability, permeability, metabolism.

61
Q

Phase 1 metabolism

A

Producing a new chemical group on a molecule.

Oxidation, reduction, hydrolysis

62
Q

Phase 2 metabolism

A

Addition of endogenous ligand to the molecule.

Glucuronidation, amino acids, acetylation, sulfation, and gluthionine conjugation.

63
Q

Mechanism based pharmacology

A

Activation of target causes unwanted effects. Not seen in in vitro tests.

64
Q

Reactive metabolites

A

Are electrophiles that mind bind to DNA and proteins leading to toxic effects

65
Q

Drugs most susceptible to Interaction

A

Compounds with loW F% and high first pass metabolism. CYP drugs.

66
Q

Bioisosteres

A

Substituents or functional groups that have similar chemical and/or physical properties and produce similar biologic properties

67
Q

Conformational isomers (rotamers)

A

The non identical spacial arrangement of atoms and groups in a molecule that result from rotating around a single bond. Ex. Trans ACH bind muscarinic and Gauche binds nicotinic

68
Q

Geometric isomers

A

Result of restricted rotation around a chemical bond. Not mirror images and have different properties.

69
Q

Optical isomers

A

Compounds containing at leas one chiral center.

70
Q

Enantiomers

A

One of two stereoisomers that are non super-impossable mirror images of each other. Can have way different binding and potency.

71
Q

Eutomer

A

The most active isomer delivering the desired effect.

72
Q

Diasteromers

A

Molecules that are not super impossable and non-mirror images due to containing more than one chiral center.

Principles of Drug Action (2 decks)

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