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Pharmacology - pharmacokinetics > Lecture 1 > Flashcards

Lecture 1 Flashcards

1
Q

Pharmacokinetics definition

A

What the body does to the drug: absorption, distribution, biotechs formation (metabolism), excretion
ADME

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2
Q

Pharmacodynamics

A

What the drug does to the body: drug action and effects

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3
Q

what are the 3 diff types of drug names?

A

INN, proprietary name, company/compound code

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4
Q

what might proprietary name suggest?

A

drug effect

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5
Q

what are the 2 stages of drug development?

A

pre clinical and clinical

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6
Q

what are the phases of preclinical stage?

A

phase 1. isolation/synthesis
phase 2. screening and determination of acute toxicity (LD50)
phase 3. pharamcological studies
phase 4. studies of subchronic (1month), chronic (6month), toxicity or teratogenic/mutagenic/cancerogenic effects

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7
Q

what are the phases of the clinical stage?

A

phase 1. human pharmacology
phase 2. therapeutic exploration
phase 3. therapeutic confirmation (random trials)
phase 4. therapeutic use (post-marketing studies)

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8
Q

what are the 3 ways drug can be absorbed by the body?

A
  • passive diffusion (common; aqueous and lipid)
  • carrier mediated transport (facilitated, active - primary and secondary)
  • endo/exocytosis
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9
Q

what does fick’s law show?

A

passive flux of molecules down a conc. gradient

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10
Q

where does aqueous diffusion occur in the body?

A
  • large aqueous compartments such as interstitial space, cytosol
  • in aqueous pores of blood vessels
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11
Q

what kind of drug molecules do not permeate most vascular aqueous pores?

A

those bound to large plasma proteins (albumin etc.)

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12
Q

can protein bound drug be cleared? why?

A

no because they can’t enter the glomerulus

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13
Q

what is the most important limiting factor for drug permeation?

A

lipid diffusion

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14
Q

what does henderson-hasselbalch equation show?

A

ration of lipid soluble weak acid/base to water soluble weak acid/base

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15
Q

what is pKa?

A

pH at which durg is 50% ionised and 50% unionised

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16
Q

are unionised molecules lipid or water soluble?

A

lipid because they are not charged and thus can corss the phosolipid bilayer; it is absorbed by the body

17
Q

are ionised molecules lipid or water soluble?

A

water because they are charged and can’t cross the membrane; goes w/the water of the body and is excreted via urine

18
Q

at what pH are weak acids in the lipid soluble form?

A

acidic pH

19
Q

at what pH are weak bases in the lipid soluble form?

A

alkaline pH

20
Q

what form are weak acids in at a basic pH?

A

water soluble

21
Q

what form are weak bases in at an acidic pH?

A

water soluble

22
Q

examples of weak acids?

A

aspirin, penicilin, cephalosporine, loop diuretics, phenobarbitone

23
Q

examples of weak bases?

A

local anesthetics, morphine, PCP, atropine, amphetamine

24
Q

what are the 3 types of carrier molecules?

A

selective, saturable, inhibitable

25
Q

what are the 2 types of carrier families?

A

ABC (ATP binding cassette)

SLC (solute carrier)

26
Q

what family does transporters of facilitated diffusion belong to?

A

SLC

27
Q

what is example of facilitated diffusion?

A

glucose into muscle/fat cells via GLUT 4 transporter (SLC)

28
Q

what family does transporters of primary active transport belong to?

A

ABC; their intracellular loops have ATPase activity

29
Q

what family does transporters of secondary active transport belong to?

A

SLC

30
Q

what is bioavailability?

A

measure of the fraction of administered dose of a drug that reaches systemic circulation unchanged

31
Q

why is bioavailability of an ingested drug lowered?

A
  • may be not completely absorbed

- might undergo first pass metabolism in liver/intestinal wall

32
Q

what is the effective barrier to orally administered drugs?

A

epithelial lining of the GIT

Pharmacology - pharmacokinetics (1 decks)

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