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PMP 102 Drugs & Medicines > Drug Metabolism and Kinetics > Flashcards

Drug Metabolism and Kinetics Flashcards

1
Q

Pharmaceutical Phase

A

Disintegration of the pill / capsule in gastrointestinal
tract (GI), release of the drug, dissolution of drug

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2
Q

Pharmacokinetic Phase

A

Absorption from GI tract into bloodstream and
what the body does to the drug

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3
Q

Pharmacodynamic Phase

A

Mechanism by which the drug interacts with the
molecular target. What the drug does to the body

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4
Q

Pharmacokinetics required by a drug

A
  • Absorbed well by the body
  • Reaches target easily
  • Not modified, inactivated, or removed from the body
    too quickly
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5
Q

Pharmacodynamics required for a drug

A
  • Effective at targeting the
    disease process
  • Not toxic
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6
Q

Potency

A
  • Dose required to achieve the effect.
  • Measured as the 50% effective concentration (EC50).
  • Units of concentration
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7
Q

Efficacy

A
  • The maximal effect.
  • Measured as “response.”
  • Usually a percentage
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8
Q

ADME

Absorption

A
  • Process of drug entering the body and therapeutic agent entering the blood
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9
Q

ADME

Distribution

A
  • Drug may reversibly leave the bloodstream and distribute into the interstitial and intracellular
    fluids of various compartments in the
    body
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10
Q

ADME

Metabolism

A

chemical conversion of drug
molecules

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11
Q

ADME

Elimination

A
  • Clearance of drugs and
    metabolites from the body (urine, bile,
    faeces)
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12
Q

Absorbtion adminstration method

Intravenous

A
  • Polar charged and high molecular weight drugs
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13
Q

Absorbtion adminstration method

Intramuscular

A
  • Oily vehicles that are irritating
  • Neutral chemicals
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14
Q

Absorbtion adminstration method

Inhaled

A
  • Neutral molecules
  • Highly volatile
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15
Q

Absorbtion adminstration method

Topical and subcutaneous

A
  • Neutral molecules
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16
Q

Factors Affecting Drug Absorption

Solubility

A
  • Drugs need to be water-
    soluble to pass into the blood for
    distribution
17
Q

Factors Affecting Drug Absorption

Ionisation

A

Drugs need to be close to
neutral to pass through membranes

18
Q

Factors Affecting Drug Absorption

Stability

A

Drugs need to be chemically
stable until they reach their site of
action

19
Q

Factors Affecting Distribution

Plasma solubility

A

Including binding to plasma proteins (bind and release)

20
Q

Factors Affecting Distribution

Lipophilicity

A
  • Balance between water and fat solubility.
  • Influences drug levels in blood, muscles, adipose tissue, and organs
21
Q

Factors Affecting Distribution

Perfusion

A
  • Level of blood flow to a tissue.
  • Major organs e.g. well perfused
  • Brain is a special case – blood-brain barrier more difficult to reach
22
Q

Elimination

A
  • Get metabolites and exogenous
    molecules out of their system
  • Drug is removed without metabolism, the process is called excretion
23
Q

Metabolism

A
  • Metabolic enzymes attack drug molecules forming metabolites
  • Metabolites may be inactive, less active or even more active than parent drug molecules
  • Side effects and toxicity
24
Q

Why is the metabolism of drugs required

A
  • Designing new drugs which do not form unacceptable metabolites
  • Designing pro-drugs / understanding pre-drug strategy
  • Understanding half-lives and tailoring drug action
25
Q

Minor metabolites

A
  • Accumulation of minor
    metabolites can be extremely toxic
26
Q

Exreation of Polar Drugs

A
  • Kidneys will excreate polar drugs at a faster rate
27
Q

Excreation of Non-polar Drugs

A
  • Needs to be chemically modified to make them more hydrophilic so they can
    be eliminated more easily
28
Q

Phase I Transformations

A
  • Mostly in liver
  • Chemical Modifications
  • Oxidation, Reduction, Hydrolysis
29
Q

CYP- P450 Reactions

A
  • Haemoproteins (contain haem)
  • Located in the liver cells
  • Split molecular oxygen so one of the oxygen atoms is introduced into the drug, the other ends up in water
30
Q

1 - lowest order of oxidation

Oxidation of carbon

A
  • Oxidation of exposed alkyl groups & exposed regions of cycloalkyl rings
  • Exposed CH3 molecule and alkyl substitution
  • Most ecposed hydrogen the one opposing the R group
31
Q

2 oxidation level

Oxidation of carbon

A
  • CH3 opposing the the R group on the benzene to alcohol to carbocylic acid

PMP 102 Drugs & Medicines (56 decks)

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