EXAM 4 Flashcards

1
Q

Pharmacodynamics (definition, includes what, affected by what)

A
  • study of effects of drugs on body
  • includes: 1) site of action, 2) mechanism of action, 3) receptor bindings, 4) post-receptor effects, 5) chemical interactions
  • affected by: 1) disease/disorder, 2) age, 3) drug-drug interactions
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2
Q

Receptor subtypes

A

1) enzymes
2) ion channels
3) membrane receptors

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3
Q

Chemical interactions that affect drug binding

A

1) electrostatic interactions (intermolecular forces)
2) hydrophobic interactions
3) covalent bonds
4) stereospecific interactions (enantiomers)

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4
Q

Pharmacokinetics affect the following: (4)

A

1) drug administration
2) therapeutic dosing
3) time intervals between drug dosing
4) toxic dosing

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5
Q

Factors affecting bioavailability: (8)

A

1) MW of drug
2) drug formulation
3) drug stability (pH sensitivity)
4) first pass metabolism (liver)
5) blood flow
6) gastric emptying (food slows process)
7) intestinal motility
8) drug interactions

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6
Q

Distribution of a drug (influenced by 6 things)

A

1) blood
2) total body water
3) extracellular fluids
4) lymphatic fluids
5) cerebrospinal fluids
6) protein binding

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7
Q

hydrolysis metabolizes what types of bonds?

A
  • esters
  • amides
  • nitriles
  • occurs in the pancreas
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8
Q

REDOX metabolizes with what?

A
  • cytochrome P450 (liver)
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9
Q

main routes of excretion (4):

A
  • kidneys (majority)
  • feces (unabsorbed/metabolites from bile)
  • lungs (anesthetics)
  • sweat (not common)
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10
Q

Lipinski rule of 5

A
  • describes drug potential for a new chemical entity (NCE) that is used as a tool too measure potential bioavailability
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11
Q

Lipinski rule of 5 based on:

A
  • H bond donors (amines/alcohols)
  • H bond acceptors (total number of N, O and F)
  • MW
  • calculated partition coefficient (cLogP)

violation of more than 1 rule = not orally available

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12
Q

lipophilic moiety

A

charge transfer

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13
Q

hydrophilic moiety

A
  • h bonding
  • van der waals
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14
Q

ester linkage

A
  • dipole interaction
  • van der Waals interaction
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15
Q

functional groups with increased toxicity (5)

A
  • aromatic anilines
  • nitroaromatics
  • aliphatic halides
  • polycyclic aromatic hydrocarbons
  • thiophenes
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16
Q

absorption of drugs into bloodstream is dependent on 2 things:

A

1) acid/base properties of the drug
2) pH at site of absorption

17
Q

ionized drug

A

> 50 Da
require active transport

18
Q

small drugs

A

< 50 Da
bulk flow

19
Q

lipophilic drugs

A

50 - 500 Da
passive transport

20
Q

Lewis

A
  • acid –> e acceptor
  • base –> e donor
21
Q

Bronsted-Lowry

A
  • acid –> proton donor
  • base –> proton acceptor
22
Q

strong acid

A
  • completely ionize in water
  • have weak conjugate bases
  • HCl, HBr, HI, HClO4, H2SO4, HNO3
23
Q

weak acid

A
  • partially ionize in water
  • strong conjugate bases
  • HF, H2CO3, H3PO4, organic acids (carboxylic acids, protonated drugs)
24
Q

strong base

A
  • completely ionize in water
  • LiOH, NaOH, KOH, Sr(OH)2, Ca(OH)2, Ba(OH)2
25
Q

weak base

A
  • partially ionize in water
  • Mg(OH)2, transition metal hydroxides, NH3
26
Q

amphoteric

A
  • can act as either a base or acid
  • water
27
Q

water constant

A
  • measure of self ionization of water
28
Q

pH vs pOH

A
  • inverse relationship
29
Q

acid strength is relative and depends on ___

A

the ability of the group to give up a proton (known as the pKa)

30
Q

the lower the pKa, the more ___.

A

acidic

31
Q

Buffers are a solution that contain what?

A
  • weak acid and its conjugate base
  • weak base and its conjugate acid
32
Q

define buffer capacity

A

each buffer has a limit to the amount of acid/base that can be added before the buffer loses its ability to change

(buffers resist change in pH when strong acids/bases are added in limited quantity)

33
Q

how is blood pH controlled

A

function of the buffer systems of the body in combination with the respiratory and renal system

34
Q

three main buffer systems

A
  • bicarbonate
  • phosphate
  • protein buffer systems
35
Q

respiratory system

A

directly impacts the carbonic acid buffer system through control of blood CO2 levels

36
Q

renal system

A

regulated by various buffer systems and works to remove H ions through the kidneys

37
Q

T/F
the charge of a drug compound is one factor that can dictate the movement of acid/base drugs across a membrane

A

T

38
Q

Henderson Hasselbalch equation determines what

A

the amount of charged species at a particular pH