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biopharm > final review of earlier modules > Flashcards

final review of earlier modules Flashcards

1
Q

describe competitive inhibitors

A

compete with substrate for same active site
alter km and kcat

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2
Q

describe non competitive inhibitors

A

bind to diff location prevent ES formation
alter k cat and vmax

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3
Q

describe uncompetitive inhibitors

A

binds to ES, alters ES structure prevents catalysis
alters Km, Kcat, Vmax

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4
Q

what is Km

A

concentration of substrate at 1/2 vmax, enzyme efficiency

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5
Q

what is Vmax

A

maximum velocity of the reaction

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6
Q

what is Kcat

A

turnover rate, how efficiently ES into products

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7
Q

what is Kd

A

binding between E + S

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8
Q

what is an irreversible inhibitor

A
  • binds covalently, alters conformation or disables function group
  • penicillin
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9
Q

2 methods of receptor signalling

A

1) binding of messenger changes conformation allowing another molecule to bind or be released

2) binding of messenger changes conformation of receptor allowing or destroying catalytic function

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10
Q

what is an agonist

A
  • binds to active site in the same place messenger would
  • induces shape change which sends out a signal
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11
Q

what is a partial agonist

A

1) non ideal conformational change, leads to a weaker signal produced than agonist and lasts for certain duration

2) binds in more than one way (agonist + antagonist)

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12
Q

what is an antagonist

A
  • Drug binds to receptor in such a way that an abnormal shape change is produced. This results in no signal transmitted. The drug prevents the messenger from binding, preventing signal from being produced.
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13
Q

what is an allosteric agonist

A
  • binds to different location on receptor
  • alters active site making it easier for messenger to bind
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14
Q

what is an inverse antagonist

A
  • reversal in receptor function
  • only if receptor has background activate (signal in absence of messenger
  • antagonist shuts off background signal
  • apparent reversal
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15
Q

phase 1 clinical trial

A
  • max safety dose
  • 100 patients
  • VOLUNTEERS
  • less than 1 year
  • 30% fail
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16
Q

phase 2 clinical trial

A
  • safety, efficacy
  • max effective dose
  • 200-300 patients
  • less than 1 year
  • 70% fail
17
Q

phase 3 clinical trial

A
  • safety, efficacy
  • monitor rare side effects
  • thousands of patients
  • less than 1 year
  • 70% fail
18
Q

4 types of excipients

A
  • non medicinal ingredients, usually from food industry
  • stabilizers: acid/base protect from degradation due to oxygen
  • preservatives : prevent bacteria or mold
  • disintegrates: help deliver drug, starch
  • flavours: sweetness for kids, safety in adult medication
  • colours: safety and identification
  • fillers: ensure correct dosing, cellulose, MgSO4
19
Q

4 types of formulation

A

-pills, capsules, liquids
- digested orally

topical cream, patch, nasal spray, eyedrops
- bypass liver, if ingested may not reach bloodstream fast enough

20
Q

4 requirements for animal testing

A

2 species
1 must be primate
show that drug is bioavailable (gets in body)
must use relevant dose

21
Q

solvent exposed binding pockets

A

see doc

22
Q

how does bacteria overcome b-lactam

A
  • b lactamase
  • opens b lactam ring, drug can no longer inhibit peptidase
23
Q

how to overcome bacterial resistance

A
  • add larger group to side chain of penicillin
  • no longer fits into b lactamase, can’t be deactivated
  • fits into transpeptidase and inhibits it
24
Q

what is a classical isostere

A
  • same valency + similar size
  • helps determine if groups important for binding or not
25
Q

what is a non classical isostere

A
  • similar bio or chem properties
  • differ in steric and electronics
26
Q

what was the first commercially successful drug and how did it work

A
  • sulfanilamide
  • competitive inhibitor (competes with PABA for active site)
  • inhibits bacteria enzyme from forming co enzymes F needed for growth
27
Q

3 amino acids in catalytic triad and functions

A
  • aspartic acid
  • histidine
  • serine
28
Q

role of oxyanion hole

A

stabilize -ve oxygen in tetrahedral intermediate

29
Q

lipinski rule of 5

A

if 2 or more: not bioavailable

SHOULD NOT HAVE
- more than 5 h bond donors
- more than 10 h bond acceptors
- molecular weight > 500
- C/ log p > 5, MlogP > 4.15
- Log D 1 < x< 3

biopharm (8 decks)

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