Module 10 Flashcards

1
Q

Pharmacodynamic can be affected by?

A

-age
-disease or disorder
-drug-drug interaction

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2
Q

Pharmacodynamic includes:

A
  • site of action
  • MOA
  • receptor binding
  • post-receptor effect
  • chemical interaction
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3
Q

Receptor subtypes include:

A
  • enzymes
  • Ion channels
  • membrane receptors
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4
Q

type of chemical interactions that drugs use to bind to receptors?

A

electrostatic interactions (INTERmolecular forces)

hydrophobic interactions

covalent bonds

stereospecific interactions (enantiomers)

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5
Q

Drug properties

A

Affinity
efficacy
potency

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6
Q

Affinity

A

how well the drug binds to the receptor

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7
Q

efficacy

A

how well the drug produces its desired effect

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8
Q

potency

A

term used to compare the relative affinity of competing drugs

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9
Q

Categories of Drugs

A

Agonist
antagonists (competitive and non-competitive)

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10
Q

Methods of drug administration

A

enteral (oral), parenteral (other than intestine) that include: intramuscular, subQ, IV, Inh

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11
Q

What determines the time to maximal concentration at the receptor to produce peak effect?

A

absorption rate

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12
Q

Bioavailability definition:

A

how much of the administered drug is actually absorbed (esp. in oral meds)

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13
Q

Factors that affect bioavailability?

A

MW
drug formulation
drug stability
1st pass metabolism
blood flow
gastric emptying
intestinal motility
drug interaction (polypharm)

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14
Q

What influences volume distribution?

A

blood,
total body H20,
ECF,
lymphatic fluids,
cerebrospinal fluids,
protein-binding

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15
Q

What are prodrugs?

A

convert from inactive form to active form

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16
Q

Two common chemical reactions of drugs being metabolized?

A

hydrolysis (esters, amides, nitriles)
REDOX reactions (P450)

17
Q

What are the major routes of excretion?

A

kidney, feces, lungs, and sweat

18
Q

What % of drugs fail in clinical testing?

A

90%

19
Q

How many years is the drug development process?

A

usually 13 year process

20
Q

Lipinski Rule of 5 used for?

A

used as a tool to measure a new chemical entity’s potential bioavailability

&

describes drug potential for a new chemical entity

21
Q

Lipinski rule of 5 include?

A

hydrogen bond donor
hydrogen bond acceptors
MW
cLogP

22
Q

What does more than one rule violation mean for the Lipinski Rule of 5?

A

(NCE) new chemical entity is non-orally available

23
Q

Low ___ drugs with a low __ can easily cross cell membranes?

A

MW ; cLogP

24
Q

What are the structural alerts? (5) why?

A

functional groups that have been linked to increased toxicity due to their metabolites.

aromatic anilines
nitroaromatics
aliphatic halides
polycyclic aromatic hydrocarbons
thiophenes

25
Q

drug ___ is directly related to the concentration of the drug at its _____.

A

efficacy; site of action

26
Q

Drug size and transport

A

Small drugs (<50 Da) = bulk flow
lipophilic drugs (50-500 Da) = passive transport

27
Q

Drug charge and transport

A

ionized drugs (>50 Da) = active transport

28
Q

What determines ability of drug to be distributed to the desired receptor sites?

A

Drug solubility properties

29
Q

Don’t for get men in black (Bioavailability)

A

D- drug formulation, stability, interactions
F - first pass metabolism
G - gastric emptying
M - molecular weight of drug
I - intestinal motility
B - blood flow

30
Q

no more than _____ hydrogen bond acceptors/donors (lipniski rule)

A

10

31
Q

Hydrogen bond acceptors (lipinski rule)

A

total # of N and O

F is only for metabolic reasons, not included in this category per Dr. P

32
Q

hydrogen bond donors (lipinski rule)

Functional groups

A

amines and alcohols

(Can give away a hydrogen)

33
Q

What MW will allow passive diffusion?

A

MW less than 500

34
Q

cLogP and diffusion

A

less than 5 will predict drug will cross the membrane via passive diffusion.

35
Q

What two compounds must be present in potential drugs?

A

a mix of hydrophilic and lipophilic groups.

36
Q

drug concentration that is too high can elicit?

A

negative effects

37
Q

Da unit =

A

g/mole

38
Q

bulk flow =

A

passive transport (interchangeable term)