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Intro to Pharmaceuticals > Ch. 2-Drugs and their Targets > Flashcards

Ch. 2-Drugs and their Targets Flashcards

0
Q

chemical barrier

A

fluids, may affect solubility and ionization (charge) of the drug

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1
Q

anatomical barriers

A

membranes that prevent the drug from reaching its intended site of action

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2
Q

biochemical barriers

A

transport proteins, enzymes, and receptors resulting in movement of the drug, destruction of the drug, or production of target or unintended response
-ex) not enough transporters to move the drug, it won’t reach its target and is ineffective

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3
Q

drug actions depend on 3 properties

A

physiochemical properties, chemical properties, and stereochemistry

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4
Q

physiochemical properties of drugs

A

solubility, ionization, etc that influence how well the drug is absorbed and where it travels

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5
Q

chemical properties of drugs

A

resonance structure and inductive effects that play role in drug’s ability to bind

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6
Q

stereochemistry

A

shape and size of molecule that can influence how drug interacts with targets and if it can produce the right response

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7
Q

Can a drug create or confer a new biological function?

A

no, it can only increase or decrease the normal function

-ex) ibuprofen inhibits enzyme that synthesizes substances that cause inflammation

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8
Q

Proteins are needed for what in the body?

A

structure, function, and regulation of cells, tissues, and organs

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9
Q

What roles do proteins have?

A

regulating activation of genes, relaying signals between cells, driving metabolic processes, etc

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10
Q

4 Structures of protein

A

primary, secondary, tertiary, quaternary

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11
Q

primary structure of protein

A

sequence of amino acids that make up protein

-looks like string of beads

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12
Q

secondary structure of protein

A

determined by hydrogen bonding between amino acids to form alpha-helix or beta-sheets

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13
Q

tertiary structure of protein

A

highly organized, 3-D shape with distinct inside and outside; unfolded or folded
-has several binding sites where molecules can bind

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14
Q

quaternary structure of protein

A

2-6 polypeptide chains or subunits, often form a channel for entry into the cell
-acetylcholine receptor has 5 subunits that form a channel for sodium ions

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15
Q

4 Regulatory Protein Targets

A
  1. receptor proteins
  2. ion channel proteins
  3. enzymes
  4. transporters
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16
Q

receptor proteins

A
  • receive and process signals from other cells

- ex)Zyrtec blocks H1 receptor (histamine receptor)

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17
Q

ion channel proteins

A
  • control passage of solutes and ions in and out of cell

- ex) Novocain blocks sodium ion channel proteins to prevent pain signals

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18
Q

enzymes

A
  • catalyze reactions

- ex) Celebrex inhibits COX2 enzyme to prevent synthesis of substances that cause inflammation

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19
Q

transporters

A
  • bring materials in and out of cells

- ex) Prozac inhibits serotonin transporter (doesn’t move out of brain) resulting in elevated mood to relieve depression

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20
Q

agonist

A

initiates activity

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21
Q

antagonist

A

resists activity

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22
Q

blockers

A

block ion channels so certain ions cannot enter the cell

23
Q

modulators

A

change the size of the opening in an ion channel

24
Q

ligand

A

ion or molecule that binds to protein to form a complex (anything that binds to receptor)

  • endogenous: already inside the body such as neurotransmitters
  • exogenous: introduced into the body as a drug
25
Q

pharmacophore

A

simplest structure that will bind to the target

-doesn’t take into account the different barriers or toxicity

26
Q

3 groups of pharmacophore

A

vector groups, carrier groups, and vulnerable groups

27
Q

vector groups

A

direct the drug to its site of action and can help minimize toxicity
-classified further as carrier groups and vulnerable groups

28
Q

carrier groups

A

part of vector group

-control ionization and influence absorption, distribution, and excretion

29
Q

vulnerable groups

A

part of vector group

-susceptible to enzyme action and responsible for determining drug’s metabolism

30
Q

analog

A

compound with same or similar pharmacophore as the lead, with differences in other parts of the molecule

31
Q

complementarity

A

physiochemical and steric

-determine strength of the type of interaction

32
Q

physiochemical complementarity

A

several weaker noncovalent bonds attracting and keeping the two molecules together

  • initial attraction between protein and ligand by long-range force such as ionic interaction between opposite charges
  • short range forces (hydrogen bonds and van der Waals forces) hold them together as ligand gets closer
33
Q

hydrophobic interaction

A

critical for protein-ligand interactions

-hydrophobic portion of ligand propels it from the water to the protein

34
Q

electrostatic complimentarity

A

makes sure the ligand has the correct charged atoms for the interaction to occur so the wrong molecules don’t bind to active site

35
Q

Region A of pharmacophore-The Amine Function

A

carries positive charge and can form ionic bond to negative site on receptor

36
Q

Region A of pharmacophore-The R Group

A

size of R group increases, alpha receptor binding decreases and beta receptor binding increases

  • hydrophobic binding also increases
  • ex) R group changes from hydrogen to isopropyl group-drug only binds to beta receptors
37
Q

what is most important for alpha receptor binding and activation?

A

ionic bonding

38
Q

what is most important for beta receptor binding and activation?

A

hydrophobic binding

39
Q

Region D-The Catechol Function

A

hydrophobic region of molecule, attracted to hydrophobic region of active site
-removing or replacing with less hydrophobic group reduces ability to bind to alpha and beta receptors

40
Q

Region B-The alpha Carbon

A

inserting methyl group decreases alpha and beta receptor binding and activation
-physically interferes with ability of amine to bind to complementary active site

41
Q

steric complementarity

A

determines shape and size that fit into shape of target on active site

42
Q

stereoisomer

A

same molecular formula and sequence but different spatial arrangement
-can have dramatically different chemical, physical, and biological properties

43
Q

chirality

A

geometric property, something can’t be superimposed on its mirror image

44
Q

geometric isomers

A

restricted rotation around a bond

-cis and trans isomers

45
Q

racemic mixtures

A

sample of compound that contains all its possible stereoisomers in equal propertions

46
Q

isosterism

A

similarity in physicochemical properties bc of similarities in electron structures

47
Q

bioisosterism

A

application of isosterism, allows the drug formula to be changed to improve the effect
-ex) Propanolol slows heart rate but is lipid soluble. modified to be Pindolol which is less lipid soluble

48
Q

How does sulfonamide kill bacteria?

A

it is an isomer of PABA (para-aminobenzoic acid) which forms from folic acid and bacteria want to eat it. give the body sulfonamide and the bacteria eat it and can’t synthesize DNA to form new bacteria

49
Q

How does ranitidine work?

A

it is an H2 blocker, and H2 is mainly present in the stomach. it causes excess stomach acid to be formed. ranitidine blocks the H2 receptors, inhibiting formation of stomach acid

50
Q

For a drug to work, it has to be soluble in what?

A

balance between water soluble and lipid soluble

51
Q

lipophilic

A

lipid-loving
they dissolve in lipids
cells and tissues contain lipids, and most drugs need to pass through those lipids

52
Q

hydrophilic

A

water-loving
dissolves in water
most of the body is made of water, drug needs to dissolve in it so it can be transported throughout the body to its site of action

53
Q

ionization

A

ability of a molecule to gain or lose electrons

54
Q

Why is ionization important?

A

if a particle is charged, it won’t cross the cell membrane and it affects the structure, absorption, and distribution

55
Q

efficacy

A

how effective something is

-how much of a drug you would need to produce the desired response

56
Q

affinity

A

attraction, how compatible two molecules are and if they’ll stay together

Intro to Pharmaceuticals (10 decks)

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