ADME overview Flashcards
Absorption requires SOLUBILILZATION. TRUE OR FALSE?
TRUE
Drugs that are more hydrophilic are more likely to be dissolved than those that are hydrophobic. TRUE OR FALSE
TRUE
Ionization does not determine solubilization. TRUE OR FALSE?
FALSE
Ph does not determine rate of ionization. TRUE OR FALSE?
FALSE
What is thermodynamic solubility?
Refers to how soluble a drug is if left in solution to come to equilibrium
What is kinetic solubility?
Refers to how quickly a drug dissolves in solution
What is pinocytosis transport of drug?
When cell membrane invaginates the drug
What is Paracellular transport pf drug?
Transport of drug between different cells
What is Lipid diffusion transport of drug?
Movement of drug directly across cell membrane
What is Aquaporin transport of drug?
Drugs can move across ion channels
What is carrier transport of drug?
These are proteins that can transport certain drugs
What does fick’s law describe?
The flux of drug across the membrane i.e how many moles of the drug is moving across the membrane per unit time
Absorption is determined by POLARITY AND LIPOHILICITY. TRUE OR FALSE?`
TRUE
What re the factors affecting GI absorption?
- Anatomical factors
- pH
- Permeability and solubility
- Binding to other material in GI tract
- Gastric emptying
- Metabolism
What is permeability dependent on?
- Solubility in membrane lipid
- Mobility in membrane lipid
- Molecular mass ( Reduces permeability)
what is the pH partition hypothesis?
uncharged molecules preferentially cross membrane (there are exceptions to this)
what is distribution?
The reversible transfer of a drug between different tissues in the body
Many drugs exert their effect in interstitial water or intracellular water. TRUE OR FALSE?
TRUE
Only unbound drug moves between compartments.TRUE OR FALSE?
TRUE
Blood-brain barrier restricts access to CNS. TRUE OR FALSE?
TRUE
Blood-brain barrier DOES NOT prevents
water-soluble drugs from
reaching the CNS. TRUE OR FALSE?
FALSE
What are Perfusion limited drugs?
These are drugs where the membrane presents little permeability barrier - this is the case for lipophilic drugs
What are permeability limited drugs?
Are drugs where membrane present significant permeability barrier- this is the case for polar drugs that are affected by charge
Blood flow does not control the distribution of drug, its the permeability of the membrane to those drugs that affects their distribution. TRUE OR FALSE?
TRUE
Drugs may bind to blood cells, tissue proteins and plasma protein. TRUE OR FALSE?
TRUE
What does serum albumin mostly bind?
Acidic drugs
What doe a1 acid glycoprotein mostly bind?
Basic drugs
Only unbound drug exerts a pharmacodynamic effect. TRUE OR FALSE?
TRUE
What does the one compartment model mean?
The drug can diffuse into all the tissues at the same time
What does the two compartment model mean?
Drug can distribute into one compartment more rapidly than in another compartment
Elimination is both metabolism and excretion. TRUE OR FALSE?
TRUE
What is metabolism?
The conversion of drug to another chemical
Which organ is the major site of metabolism?
Liver
What occurs in Phase I in metabolism?
conversion to more reactive form to allow conjugation
What occurs in Phase II in metabolism?
conjugation with another biomolecule to increase solubility to
allow excretion
Some drugs may be excreted unchanged
Some drugs may not undergo phase II
ARE THESE STATEMENTS TRUE OR FALSE?
TRUE
Oxidation and reduction both occurs in phase 1 of metabolism. TRUE OR FALSE?
TRUE
95% of reactions does not occur by cytochrome P450. TRUE OR FALSE?
FALSE
List the different types of isoforms of cyp and describe their uses.
3A4 - most commonly associated with drug metabolism
2D6 - shows greatest variability between different people
Apart from cytochromes there no other enzymes that can catalyze metabolism. TRUE OR FALSE?
FALSE
Biotransformation can render a drug more reactive: - aids conjugation - makes more harmful TRUE OR FALSE?
TRUE
What is Excretion?
the irreversible removal of drug from the
body
List the different Routes of excretion
- Urine
- Bile
- Sweat
- Milk
- Exhaled breath
What are the Processes involved in
renal excretion?
- Filtration in Renal corpuscle
- Active secretion in the tubule
- Reabsorption in the tubule