Pharm (Fall 2025) > Test 1 > Flashcards

Test 1 Flashcards

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1
Q

What is the main historical approach to pharmacology before the 17th century?

A

Trial and error, using experimentation and observation

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2
Q

Who was Imhotep?

A

A recorded physician and architect of the great pyramids in Ancient Egypt

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3
Q

What is the significance of the Rod of Asclepius?

A

It is a symbol of the profession of medicine

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4
Q

What does ‘the dose makes the poison’ refer to?

A

The concept introduced by Paracelsus related to toxicology and therapeutic index

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5
Q

What are the four main categories of pharmacology?

A
  • Pharmacodynamics
  • Pharmacokinetics
  • Pharmacogenomics
  • Toxicology
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6
Q

Define pharmacodynamics.

A

What the drug does to the body clinically

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7
Q

Define pharmacokinetics.

A

What the body does to the drug

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8
Q

What is pharmacogenomics?

A

The study of how genes determine drug interactions with the body

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9
Q

What is toxicology?

A

The study of undesirable effects of chemicals

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10
Q

Define agonist.

A

A substance that mimics a natural endogenous ligand in the body

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11
Q

Define antagonist.

A

A substance that blocks a drug or ligand

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12
Q

What is the difference between toxins and poisons?

A

Toxins are from living organisms; poisons are from nonliving sources

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13
Q

What is meant by ‘lock and key’ in drug-receptor interactions?

A

A drug’s specific structure fits one receptor

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14
Q

Rank the bond strengths from strongest to weakest.

A
  • Covalent
  • Electrostatic
  • Hydrophobic
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15
Q

What is a racemic mixture?

A

Two different isomers of the same drug

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16
Q

What is stereoisomerism?

A

Optical isomers that are mirror images and can have different effects

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17
Q

Define receptor.

A

A protein on the cell surface that interacts with drugs and endogenous ligands

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18
Q

What is Emax?

A

The maximal efficacy of a drug

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19
Q

What does EC50 represent?

A

The concentration of a drug that produces 50% of its maximal effect

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20
Q

Differentiate between a competitive inhibitor and an allosteric inhibitor.

A
  • Competitive inhibitor: competes for the active site
  • Allosteric inhibitor: binds elsewhere and is insurmountable
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21
Q

Define physiologic antagonism.

A

Drugs that act at different receptors to cancel each other’s effects

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22
Q

What is efficacy in pharmacology?

A

The greatest response a drug can deliver

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23
Q

What is potency?

A

The concentration/dose of a drug required to produce 50% of its maximal effect

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24
Q

Define partial agonist.

A

A drug that binds to a receptor with less affinity, producing a weaker response

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25
What is an inverse agonist?
A drug that binds to a receptor and favors its inactive form
26
What is the role of drug carriers?
To bind to drugs and facilitate their transport without altering them
27
Calculate the therapeutic index.
Therapeutic index = median toxic dose (TD50) / median effective dose (ED50)
28
What happens when pH < pKa for weak acids?
The protonated form is favored and is uncharged
29
What are the four main causes of drug variation?
* Genetics * Physiology * Underlying disease * Absorption rate
30
What is the Henderson Hasselbalch equation used for?
To correlate pH to pKa and predict the charge on drugs
31
Define monoclonal antibodies.
Antibodies produced by clones of a single parent cell, targeting specific diseases
32
What does 'MAb' signify?
It indicates a monoclonal antibody
33
What is the role of the FDA?
Oversees drug development and ensures safety and efficacy before marketing
34
List the differences in regulation between prescription and OTC drugs.
* Prescription drugs: tightly regulated, require health professional guidance * OTC drugs: assumed low risk, but can be harmful in excess
35
What are the steps to bring a prescription drug to market?
* Find lead compound * In vitro studies * Animal testing * IND submission * Clinical testing (Phases 1-3) * NDA submission * Post-marketing surveillance
36
What are G-protein coupled receptors (GPCRs)?
Receptors that bind guanine nucleotides and activate intracellular signaling
37
What are the components of a G-protein?
* Alpha * Beta * Gamma
38
Describe the cell signaling process.
Receptor converts an external signal into an internal effect
39
What is the significance of second messengers?
They act as intermediaries between activated receptors and cellular responses
40
What happens to the intracellular alpha subunit of GCPR upon ligand binding?
The alpha subunit undergoes a conformational change and exchanges GDP for GTP ## Footnote This change allows the alpha subunit to dissociate from the beta/gamma dimer and regulate downstream effectors.
41
What are second messengers?
Intracellular molecules that act as intermediaries between an activated receptor and the cellular response ## Footnote They are produced through enzymatic activity of G-proteins.
42
List the most common second messengers.
* cAMP * cGMP * Ca++ * DAG * IP3
43
Define desensitization in pharmacology.
The response to a drug diminishes when given continuously or repeatedly ## Footnote This can occur due to various molecular mechanisms.
44
Differentiate between ligand gated and voltage gated ion channels.
Ligand gated channels open upon ligand binding, while voltage gated channels open due to changes in transmembrane potential ## Footnote Ligand gated channels are very fast; examples include nicotinic acetylcholine receptors.
45
What are ionotropic and metabotropic ion channels?
* Ionotropic: Requires two identical ligands to open the channel; the ion channel and receptor are the same * Metabotropic: Activates GPCR to open a separate ion channel; faster than metabotropic but not as fast as ionotropic
46
What types of ligands bind to receptors inside the cell?
Lipid soluble or uncharged ligands ## Footnote Examples include gases and steroids.
47
List the pharmacokinetic variables.
* Absorption * Distribution * Metabolism * Excretion
48
Describe the four ways a drug can cross barriers.
* Aqueous diffusion * Lipid diffusion * Special carriers * Endocytosis/Exocytosis
49
Define Volume of Distribution (Vd).
The amount of drug in the body compared to the concentration in the blood
50
What does Clearance (CL) predict?
The rate of elimination in relation to drug concentration
51
What is the definition of Concentration (C) in pharmacokinetics?
The amount of drug in blood required to achieve the desired effect
52
What is the Rate of Elimination (ROE)?
Clearance multiplied by concentration
53
Define Target Concentration (TC).
The concentration of the drug in blood when it is producing the desired effect
54
What is Half-life (T1/2)?
The time required to reduce the drug concentration in the body to half its level
55
Define Bioavailability (F).
The proportion of a drug that enters systemic circulation when introduced into the body
56
What is capacity limited elimination?
A zero-order elimination process dependent on saturation of elimination mechanisms
57
What is flow dependent elimination?
Elimination that depends on blood flow to the organ and the extraction ratio
58
What is the relationship between Vd and drug distribution?
A high Vd indicates the drug is likely to distribute widely in the body
59
What remains constant in first-order elimination?
Clearance (CL) remains constant; ROE and concentration vary
60
List routes of drug administration.
* IV * IM * SQ * Rectal * PO * Inhalation * Transdermal
61
Describe the first pass effect.
The process where drugs absorbed from the gastrointestinal tract pass through the liver before entering systemic circulation
62
What are the major phase I metabolic reactions?
* Oxidation * Reduction * Hydrolysis
63
What are phase II metabolic reactions?
* Glucuronidation * Sulfation * Acetylation
64
What is the role of cytochrome P450 in drug metabolism?
It catalyzes oxidation reactions that increase drug polarity and solubility
65
What does 'wild type' CYP enzymes refer to?
The normal version of CYP enzymes found most often in the population
66
What is hepatic enzyme induction?
The process by which some drugs enhance the amount of CYP enzymes present
67
What is hepatic enzyme inhibition?
The process that decreases or irreversibly inhibits P450 enzyme activity
68
What factors can affect drug clearance?
* Kidney function * Liver function * Blood flow * Albumin concentration * Protein binding capability
69
Define the term 'prodrug'.
An inactive form of a drug that is metabolically converted into an active form
70
What is the significance of toxic byproducts of metabolism?
They can overwhelm normal pathways of excretion and lead to overdose
71
What is the mechanism of hepatic enzyme induction?
Some drugs enhance the amount of CYP enzymes, leading to increased enzyme presence.
72
What occurs when Drug A induces enzyme activity for Drug B?
Increased metabolism of Drug B due to induction from Drug A.
73
What is the effect of inhibition on P450 enzymes?
Decreases or irreversibly inhibits P450 activity.
74
What is the role of Brussel sprouts in drug metabolism?
Inducer of CYP1A2, which metabolizes warfarin, resulting in less warfarin effect.
75
List the biggest CYP metabolizers of drugs and their percentages.
* CYP2B6: 8% * CYP2D6: 20% * CYP3A4: 50%
76
How is acetaminophen metabolized at normal doses?
Metabolized to harmless products.
77
What happens to acetaminophen during an overdose?
Metabolized to hepatotoxic products.
78
List additional factors affecting drug metabolism.
* Diet * Charcoal broiling * Grapefruit juice * Environment * Age & sex * Disease state * Genetics
79
Define pharmacogenomics.
The study of how a person’s genetic make-up influences their response to medications.
80
What is the importance of pharmacogenomics in personalized medicine?
Allows for drug optimization, drug safety, correct dosage, and reduces trial and error prescribing.
81
What are polymorphisms and their effect on warfarin?
Variations can make individuals less or more responsive to warfarin.
82
Name a drug that may require dosage adjustments in specific genetic populations.
Warfarin.
83
What gene is involved in the metabolism of warfarin?
CYP2C9 and V-Kor1 gene.
84
What is the consequence of CYP2C9 *2 and *3 variants?
Lead to reduced metabolism and higher drug concentrations.
85
What is the significance of genetic testing for 6-mercaptopurine?
Helps determine appropriate dosing to avoid severe/fatal side effects.
86
What type of cancer is trastuzumab (Herceptin) used to treat?
HER2 positive breast cancer.
87
What is the role of drug transporters in cells?
Regulate entry and exit of drugs, target organs, eliminate drugs, and protect cells.
88
What is the function of drug efflux transporters?
Pump drugs and xenobiotics out of the cell.
89
What is the substrate specificity of most efflux transporters?
Broad substrate specificity.
90
What are the most important ABC transporters?
* ABCB1 * ABCC * ABCG
91
What is the primary site of exclusion in the blood-brain barrier?
Vascular epithelium with tight junctions.
92
What cells surround the vascular endothelium in the blood-brain barrier?
* Astrocytes * Pericytes
93
What is the role of ABC transporters in the blood-brain barrier?
Pump substances out of the brain to protect it.
94
What is the pathway of Tylenol in the gut before biotransformation?
Enters through the gut, into the bloodstream, and is sent to the liver.
95
What happens to Tylenol after hepatic metabolism?
Converted to non-toxic glucuronide and excreted into bile.
96
Fill in the blank: Drug transporters help ______ drugs into specific organs.
[target]
Pharm (Fall 2025)
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