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Medicinal Chemistry
Designs or discovers new drugs, modifies drug chemistry to improve drug
Pharmacology
Study a drug's effect on the body, determine mechanism of action, determine how and why a drug is toxic
Pharmaceutics
Design new drug forms, optimize a drug's formulation to improve threptic outcomes
Pharmacokinetics
Studies drug metabolism, measures the rate of excretion, Use math to optimize dosing
What are the core areas of pharmacy?
Medicinal chemistry, Pharmacology, Pharmaceutics, Pharmacokinetics
What are the drug barriers?
Anatomical, Chemical, and Biochemical
What is an anatomical barrier?
A physical barrier blocking entry (ex. skin, GI tract, ect.)
What is a chemical barrier?
Body chemistry that degrades the drug's function (ex stomach acid)
What is a biochemical barrier?
A biological agent that actively works against the drug (ex enzymatic breakdown, drug pumping protiens)
What is 1 common way to create new drugs?
Modify and older non-marketed "lead" cmpd
What are the targets for most drugs?
Endogenous proteins
3 MULTIPLE CHOICE OPTIONS
What makes a drug work?
The drug must be an analogue for the endogenous ligand
What is a pharmacophore?
The region of the drug that directly binds to the target
What is a commonality between drugs within a family?
They have similar pharmacophores
What is physiochemical complementarity?
The size of the binding site and drug match, charges complement each other (ie + charge on drug has a - counterpart on the target)
What is stereochemical complementarity?
The shape of drug and its site must match (same orientation)
What are the most common bonds and interaction between a drug and its target?
Hydrogen and Ionic bonds as well as hydrophobic interactions
What is a rare drug-target interaction?
Covalent bonds
What is a racemic drug?
Contains both enantiomers of a drug
What is a eutomer?
Only the enantiomerically active portion of a drug?
What is a distomer?
Only the enantiomerically inactive portion of a drug?
What enantiomer is the prefix Lev- denoting on a drug?
L-isomer (levorotatory, counterclockwise rotation)
What enantiomer is the prefix Dex- denoting on a drug?
D-isomer (dextrorotatory, clockwise rotation)
What enantiomer is the prefix Ar- denoting on a drug?
R-isomer
What enantiomer is the prefix Es- denoting on a drug?
S-isomer
What is a prodrug?
A drug that is administered in an inactive state but is activated in the body
What is a common enzyme used to activate prodrugs?
Esterase in the blood
What are some chem groups that increase lipophilicity?
Halogens (F, Cl, Br)
Alkyl groups (methyl, ethyl, ect)
Aromatic groups
What is SAR?
Structure Activity Relationship, the study of the relationships between functional groups of a drug and the interactions with a target as well as how the body handles them
What is Bioisosterism?
Elements or groups that can be analogues for each other because of similarities in number of electrons or shape and size
What is an electrolyte?
Any substance that ionizes in water resulting in availability to conduct electricity
Why is drug ionization important to know?
Drugs dissolve better when Ionized however, especially with the GI tract, drugs are absorbed better when unionized
What is a pKa value?
The pH at which a molecule is 1/2 unionized and 1/2 ionized
What occurs to a weak acid when the pH > pKa?
More ionized (acid)
What happens to a weak acid when the pH < pKa?
Less ionized (acid)
What happens to a weak base when the pH > pKa?
Less ionized (base)
What happens to a weak base when the pH < pKa?
More ionized (base)
What is the approximate pH of the in vivo environment?
~7.4
A weak base drug has a pKa of 9.1, how much drug will be ionized?
98.04%
3 MULTIPLE CHOICE OPTIONS
A weak acid drug has a pKa of 4.2, How much drug will be ionized?
99.94%
3 MULTIPLE CHOICE OPTIONS
A drug salt uses a Chloride ion to stabilize it's structure, is it a weak acid or base?
Weak base
A drug uses a Potassium ion to stabilize its structure, is it a weak acid or base?
Weak acid
Why are buffers used in drug forms?
To make the dosage form comfortable to take (eye drops) as well as stabilizing the pdt
What does amphoteric mean?
A drug containing both acidic and basic groups
Why might you not want a drug to disintegrate once taken?
You have an extended-release dosage form
What are the properties of a Crystalline drugs?
Shelf-stable, narrow melting range, low intrinsic solubility, neatly arranged atoms
What are the properties of Amorphous drugs?
Not very shelf-stable, wide melting range, high intrinsic solubility, disordered atoms
Why are salt forms of drugs preferred?
Dissolves faster, easier to crystalize
Why do we want a balance between lipo and hydrophilicity?
Availability in multiple dosage forms, successful delivery to target, and it will spend enough time in the body to be effective
What happens if drugs are too hydrophilic?
They are too polar to reach the target and are excreted too quickly to be effective
What happens if drugs are too lipophilic?
Doesn't dissolve well, is painful/ difficult to inject
What does the partition coefficient measure?
How lipo/ hydrophilic a drug is
If logP > 0 then the drug is?
Lipophilic
If logP < 0
Hydrophilic
What is the optimal logP range?
0 - 3.5
What does the apparent partition coefficient measure?
The actual lipo/ hydrophilicity of a weak acid or base drug in vivo conditions
What happens to the apparent partition coefficient of a weak acid when pH increases?
Papp decreases
What happens to the apparent partition coefficient of a weak base when pH increase?
Papp increases
What are the 3 methods of Cellular Transport?
Passive diffusion
Carrier-mediated transport
Endo/ Exocytosis
What is passive diffusion?
Diffusion of a drug across a cell membrane without the assistance of a transporter
What is Carrier-mediated transport?
A transporter protein is provided naturally by the cell
What is Endo/ Exocytosis?
A drug being inffluxed/ effluxed via a vesicle
What are the factors affecting the rate of Passive Diffusion?
MW (higher means slower)
Viscosity (higher viscosity means slower)
Temperature (higher temp means faster)
What does Fick's Law calculate?
The rate of passive drug diffusion
What is the most common mechanism for drug transport?
Passive diffusion
What is Ion trapping?
A weak base/ acid swaps between charged and neutral forms. The neutral form diffuses across the membrane and is trapped in the cell as an ion
Where do weak acid drugs tend to accumulate?
basic tissues
Where do weak base drugs tend to accumulate?
acidic tissues
Do fetuses have higher or lower blood pH?
Lower, more acidic blood pH
What are the types of Carrier-mediated transport?
active (energy required)
facilitated (concentration gradient required)
How are drugs able to use Carrier-mediated transport?
They hitch a ride by acting like common molecules
What is facilitated diffusion?
Carrier protein allows drug to move down the concentration gradient without the use of ATP
What are the factors affecting the rate of facilitated diffusion?
Affinity of drug for carrier,
Concentration gradient
Number of carriers available
What is active transport?
Carrier protein allows drug to move against concentration gradient using energy
What are the factors affecting the transport rate of active transport?
Affinity of drug for carrier
Number of carrier available
What are the types of active transport?
uniporter
antiporter
symporter
What protein is a common cause of drug efflux problems?
P-glycoprotein
Why might drug efflux decrease the effectiveness of drugs?
Reverses GI absorption of oral drugs
"Rotating Door" for drugs (they enter and are immediately pumped out)
reduce the amount of time drugs can take effect
Why is Vesicular Transport becoming more important?
Large protein-based molecules and vaccines use this method of transport
What is the most common type of tissue drugs are transported across?
Epithelial cells
What are endothelial tissues?
Epithelial cells that form blood vessels
What are the methods drugs transport across epithelial cells?
Paracellular and Transcellular
What is Paracellular transport?
Drugs slip between cells instead of going through cells, this is uncommon due to drug size
What is Transcellular transport?
Drugs pass through cells
Why are endothelial cells easy for drugs to move across?
They have "leaky" junctions between cells
What barrier is hardest to overcome for a drug?
Blood Brain Barrier
What is true about drugs that can cross the Blood Brain Barrier?
High lipophilicity and/or a substrate for a transporter in the Blood Brain Barrier
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