Systems I Exam 3 ALL

CYP450 enzymes

Aliphatic hydroxylation

Aliphatic hydroxylation

Aromatic hydroxylation

N-Dealkylation

N-Dealkylation

N-Deamination

Deamination

N-Oxidation

N-Oxidation

S-Oxidation

S-Oxidation

Epoxidation

Epoxidation

Reduction

Hydrolysis

Hydrolysis

Glucuronidation

Sulfation

Acetylation

Acetylation

Methylation

Amino acid conjugation

Two enzymes for amino acid conjugation

Acyl synthetase and transacetylase

Glutathione

Acetylation

Glucuronidation

Sulfation

Glucuronidation

Sulfation

Converts acetaminophen to NAPQI

CYP2E1

Glutathione conjugation

Specific binding

Saturation binding study

Which drug has a higher affinity?

Drug A

Which drug has a higher affinity?

Drug A

Which drug has a higher affinity

Drug A

Which drug binds more receptors?

Drug A

What does the blue line represent?

Partial agonist

Which drug has a higher affinity?

Drug A

Which drug binds more receptors?

Drug B

Which drug is more efficacious?

Drug B

What does the top line represent?

Agonist

What does the middle line represent

Baseline activity

What does the bottom line represent?

Inverse agonist

Which drug is more potent?

Drug A

Which drug is the most potent?

Drug R

What is drug Z an example of?

Partial agonist

Most drugs produce their effects by interacting with ______ within cells or on cell surfaces

Targets

A drug ______ can be a molecule such as a protein, a lipid molecule, or DNA

Target

Common ________ for drugs include receptor proteins, ion channel proteins, enzymes, and transporters

Targets

Molecules on the cell surface or inside the cell that bind to hormones, neurotransmitters, or drugs to initiate a cellular response

Receptor proteins

Pores in the cell membrane that regulate the flow of ions, which can be opened or blocked by drugs

Ion channel proteins

Proteins that catalyze biochemical reactions, which drugs can inhibit or activate

Enzymes

Proteins that actively move substances across cell membranes

Transporters

It is important to note that some drugs do not have ____ specific target and may produce their effects through less targeted mechanisms

One

These drugs produce effects by changing the physical or chemical environment of a biological system rather than binding to a receptor or enzyme

Nonspecific

Antacids act nonspecifically by neutralizing the _____

Acid

______ drugs can result in changes in pH, osmolarity, and surface tension

Nonspecific

Many drugs target ______ to either activate or inhibit their function

Enzymes

The drug (inhibitor) binds to the same active site as the natural substrate

Competitive

The drug (inhibitor) binds to a different site (allosteric site), changing the enzyme’s shape and reducing its effectiveness

Non-competitive

________ are the target for drugs most of the time; binding usually changes its activity

Receptors

These can be extracellular or intracellular

Receptors

Drugs that exert osmotic effects are typically highly _________ and cannot easily cross cell membranes

Hydrophilic

Drugs that exert osmotic effects change the osmolarity of a solution, causing _____ to shift

Fluid

A hydrophilic alcohol used as a diuretic to rapidly reduce intracranial pressure or treat cerebral edema

Mannitol

Increase urine production

Diuretic

This remains in the blood, increasing its osmolarity, which draws excess fluid from the brain tissue into the blood and then the renal tubules, increasing the excretion of water in urine

Mannitol

Mannitol doesn’t directly interact with a __________

Receptor

This mechanism involves a drug changing the structure of proteins, typically by breaking chemical bonds

Protein denaturation

Used as an inhalational agent to treat respiratory conditions; acts as a disulfide breaking agent to reduce viscosity of mucus and make it easier to expel

NAC

This is used as an oral treatment for acetaminophen overdose because it serves as a precursor to glutathione, an important detoxifying cofactor

NAC

Antacids work by chemically ________ stomach acid, thereby increasing the pH of the stomach

Neutralizing

Examples are calcium carbonate and sodium bicarbonate

Antacids

This mechanism refers to compounds that are selectively toxic to foreign organisms or cells

Selective toxicity

Examples of selective toxicity

Germicides and disinfectants

These work by altering the surface tension between a liquid and a gas or another liquid

Surfactants

A natural lung surfactant replacement given to babies burn prematurely; composed of phospholipids, neutral lipids, and hydrophobic surfactant-associated proteins B and C

Intrasurf

Intrasurf reduces surface tension in the ______ of the lungs, preventing them from collapsing and allowing the premature baby to breathe easier

Alveoli

Surfactant, a mixture of lipids and proteins, lowers the _______ _______ between the wet lining of the alveoli and the air inside them

Surface tension

Surfactant lowers the _______ properties of water in the alveoli which helps them remain stable by preventing collapse and bursting

Cohesive

Without adequate surfactant, the strong ______ forces of water molecules lining the alveoli create a high surface tension

Cohesive

High surface tension can lead to alveoli ________

Collapse

High surface tension makes it extremely difficult to re-_______ the lungs with each breath

Inflate

Adequate _______ allows alveoli to stay properly open at various sizes throughout the breathing cycle

Surfactant

The definition of a receptor depends on the _______

Context

The component of a cell that interacts with a drug and initiates a chain of biochemical events leading to the drug’s therapeutic or toxic effects

Receptor

Receptors cause something to _____ inside the cell in addition to binding

Change

For a drug to bind to a receptor, there must be precise _________ involving chemical groups and the there-dimensional shape

Compatibility

The three-dimensional _____ of the drug must fit precisely into the receptor site, like a lock and key

Shape

A _________ shape will not bind effectively, while a complementary shape will

Mismatched

Various types of ______ chemical bonds form between the drug and receptor including ionic bonds, hydrogen bonds, and van der waals

Weak

Strongest type of bond; involves the sharing of electrons

Covalent

Involves the electrostatic attraction between a positively charged atom and a negatively charged atom (transfer of electrons)

Ionic

A weak interaction between a hydrogen atom covalently bonded to an electronegative atom (like N or O) and another electronegative atom

Hydrogen bond

Weak interactions between non-polar groups, often involving aromatic rings

Hydrophobic

The weakest interactions, arising from temporary fluctuations in electron distribution

Van der Waals

Drug-receptor binding usually involves a combination of _______ ____ bonds, including ionic, hydrogen, hydrophobic, and Van der Waals

Multiple weak

We usually want __________ and reversible interactions for drug-receptor binding

Non-covalent