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NSU AA Denver: Summer 2025 (2nd Semester) > Pharmacology I: Lecture I - Pharm Basics > Flashcards

Pharmacology I: Lecture I - Pharm Basics Flashcards

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1
Q

What is pharmacology?

A

The study of drug effects on biological systems.

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2
Q

What are the two major divisions of pharmacology?

A

Pharmacokinetics and Pharmacodynamics.

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3
Q

What are the primary goals of anesthetic pharmacology?

A

Provide analgesia, sedation, and muscle relaxation using multiple drugs.

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4
Q

What is a drug?

A

An exogenous chemical that alters physiological systems.

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5
Q

Can drugs be identical to natural substances?

A

Yes, such as insulin or potassium.

The compound in the body is called an Endogenous Compound

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6
Q

How were early drugs discovered?

A

Many originated from plant extracts. (e.g., opium contains morphine(alkaloids))

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7
Q

What is a receptor?

A

A macromolecule (often a protein) that drugs bind to in order to produce effects.

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8
Q

What is the commonly accepted theory as to how drugs work?

A

Drug-receptor interaction.

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9
Q

What does receptor affinity mean?

A

The strength of binding between a drug and its receptor.

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10
Q

Are most drug effects reversible?

A

Yes, ending when drug concentration and occupation of receptor sites diminish.

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11
Q

Are some drugs irreversible?

A

Yes, aspirin acetylates COX enzyme.

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12
Q

What is the dissociation constant (Kd)?

A

It reflects the tendency of the drug-receptor complex to break apart; lower Kd means higher affinity. Propensity of the drug to form a complex

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13
Q

What is pharmacodynamics?

A

The study of drug effects and mechanisms of action in the body.

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14
Q

What is efficacy?

A

The maximum response achievable from a drug (Emax). Reflects the ability of the agonist to activate a receptor. When a fraction of the occupied receptors is small, the physiologic effect can still be quite large if the efficacy is high.

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15
Q

What is potency?

A

The amount of drug required to achieve a defined effect.

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16
Q

What is ED50 or EC50?

A

The dose or concentration producing 50% of the drug’s maximal effect. The smaller the EC50 the less drug is required to produce the same effect

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17
Q

What is an agonist?

A

A drug that binds and activates a receptor.

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18
Q

What is a full vs partial agonist?

A

Full agonists have high efficacy, partial have limited efficacy even with full receptor occupancy.

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19
Q

What is an inverse agonist?

A

A drug that produces the opposite effect of an agonist.

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20
Q

What is an antagonist?

A

A drug that binds to a receptor but does not activate it, and prevents an agonist from stimulating the receptor

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21
Q

What is a competitive antagonist?

A

Binds to the same site as the agonist but can be displaced by high agonist concentration.

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22
Q

What is a non-competitive antagonist?

A

Binds to a different site and cannot be displaced by agonist.

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23
Q

What is an irreversible antagonist?

A

Can act at agonist site or not, reduce the number of receptors that can active

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24
Q

What is an indirect antagonist?

A

Occurs without receptor binding, Binds directly to agonist making it unable to bind, Examples: Protamine to inactivate heparin preventing activation of antithrombin; Suggamadex with Rocuronium

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25
What is tachyphylaxis?
Rapid decrease in drug response due to receptor desensitization.
26
What is ED50?
The dose producing a therapeutic effect in 50% of the population, Similar to MAC in VA
27
What is TD50?
Toxic dose in 50% of the population.
28
What is LD50?
Lethal dose in 50% of the population.
29
What are GPCRs?
G-protein-coupled receptors—largest receptor family; uses second messengers.
30
What drugs act via GPCRs?
* Opioids * Adrenergics * Antihistamines * Antiemetics * Atropine.
31
What are ligand-gated ion channels?
Receptors that open ion channels upon ligand binding altering electrical potential (e.g., GABA, nACh, glycine, 5-HT3).
32
Which anesthetics act on ion channels?
* GABAergic IV agents * VA agents * NM blockers * 5-HT3 antagonists.
33
What is receptor stereoselectivity?
Receptors may favor one stereoisomer over another (e.g., R-etomidate, Levobupivacaine, Cisatracurium is a diastereomer).
34
Why is stereoselectivity important?
It affects potency, efficacy, and toxicity of the drug.
35
What is pharmacokinetics?
The study of drug absorption, distribution, metabolism, and excretion. What the body does to the drug.
36
Why is pharmacokinetics important?
Pharmacokinetics and the dosage of drug administered determine the ultimate drug concentration at the site of action and thus the clinical effect. The major goal of pharmacokinetics is to understand and predict the time course of drug concentrations
37
Pharmacokinetics and compartment model?
Drug always move along concentration gradient; When higher in Central Compartment, the drug will distribute to into the peripheral
38
Main idea of Pharmacokinetics and Compartment model relationship?
The main idea is that drug elimination and distribution between compartments is described by rate constants (k), with assigned subscripts to indicate the direction of movement i.e. k1-2
39
What is the Distribution Phase?
Initial rapid decrease in concentration, drug movement from central to peripheral.
40
What is the Elimination Phase?
Slower decline in concentration, drug moves back into central and eventually eliminated.
41
What is bioavailability?
The fraction of drug reaching systemic circulation after administration.
42
What is the route a drug must take to take effect – causing a delay?
It must be transported close to the site of effect ; Penetrate into the tissue; Bind to a receptor; Elicit some intracellular process to achieve its effect
43
What affects absorption?
* Route * Blood flow * Solubility * Membrane permeability.
44
Which route has the highest bioavailability?
Intravenous (IV) = 100%.
45
What is Effect-Site Equilibration?
Delay between dosing and onset reflects time necessary for circulation of the drug to its site of action, time between dosing and clinical effect ex elderly have lower CO thus longer circulation time and delayed onset
46
What is the first-pass effect?
Liver metabolism of a drug before reaching systemic circulation.
47
Which tissues receive drugs first?
Vessel-rich group (brain, heart, liver, kidneys).
48
What determines drug distribution?
* Blood flow * Solubility * Concentration gradients.
49
What is the blood-brain barrier (BBB)?
A barrier that restricts entry to CNS; only non-ionized, lipid-soluble drugs cross easily.
50
What is the "reservoir effect"?
Some drugs accumulate in fat/muscle and release slowly over time.
51
What determines drug ionization?
pKa and environmental pH.
52
Why is ionization important?
Non-ionized forms are lipid-soluble and active; ionized forms are water-soluble and inactive.
53
What is most drugs pH and ionization?
Most drugs are weak acids or bases that exist as both ionized and non-ionized molecules.
54
What is the goal of drug metabolism?
Convert lipid-soluble drugs into water-soluble metabolites for excretion.
55
What are types of drug metabolism?
Active drug to inactive: Fentanyl Active drug to active metabolite: Morphine to Morphine-6-glucuronide Inactive prodrug to activated metabolite: Codeine to Morphine Drug to toxic metabolite: Meperidine to normeperidine leads to seizures
56
Where does a majority of metabolism primarily occur?
Liver (via CYP450 system). Phase I and Phase II reactions
57
What are Phase I reactions?
Oxidation, reduction, dehydrogenation, hydrolysis—make drugs more polar (uncover functional group); most by the Cytochrome P450
58
What are Phase II reactions?
Conjugation with polar molecules to enhance water solubility, ready to be eliminated
59
What is the CYP450 system?
Main liver enzyme family responsible for drug metabolism.
60
What are non-CYP enzymes involved in metabolism?
Esterases (e.g., carboxyl and choline) Cholinesterases: AChE, Plasma; Carboxylesterases: metabolize cocaine, meperidine, heroin
61
What drugs are metabolized by plasma cholinesterase?
Succinylcholine, remifentanil, mivacurium, Esmolol, Ester local anesthetics
62
What is extrahepatic metabolism?
Intestine: Same CYP enzymes as liver but less Kidney: 1/3 of propofol clearance via renal Brain: P450 activity is low Lung: Target organ of inhaled drugs
63
What factors affect metabolism?
Fetal & Neonatal: Decrease in CYP due to maturation; Pregnancy: Increase CYP activity Age: Phase 1 gradual decline, Phase 2 not seen Liver Disease: Reduced enzymatic activity
64
Goal of Metabolism?
The goal of metabolism is to convert active, lipid-soluble drugs into water-soluble, inactive metabolites; Caution not all metabolites are inactive!
65
What is elimination half-time?
Time it takes for drug concentration to fall by 50% during elimination phase.
66
How many half-lives until 98% elimination?
Approximately 6 half-lives. (within 2 weeks for most all drugs)
67
What is context-sensitive half-time?
Time for plasma concentration to fall by 50% after an infusion is stopped. Dependent on the drugs pharmacokinetics
68
What determines clearance?
Rate of elimination via hepatic metabolism and renal excretion.
69
What is clearance?
Volume of plasma cleared of drug by renal excretion and/or hepatic metabolism. (primarily CYP450)
70
What are non-organ clearance mechanisms?
* Hoffman elimination * Ester hydrolysis.
71
What is the first-pass effect?
Loss of drug via liver metabolism after GI absorption (oral route).
72
What routes avoid first-pass metabolism?
* Sublingual * Buccal * Transdermal * Rectal (distal) * IV * Intranasal.
73
What is the BA of Oral-Transmucosal?
~50-60%.
74
What is transdermal delivery used for?
Sustained plasma concentrations.
75
What is the rate-limiting step for absorption transdermal?
Thickness of stratum corneum.
76
What factors affect rectal absorption?
Onset is faster than oral route; Variable absorption based on proximal or distal administration; Lower rectum bypasses first-pass effects via draining into inferior vena cava
77
Does IM and SQ have a high or low BA?
High.
78
What are examples of trans-tracheal drugs?
* Atropine * Lidocaine * Isoproterenol * Epinephrine * Naloxone * Vasopressin * Valium.
79
What is the Intra-Nasal BA?
~50-70%, no first-pass.
80
What is pharmacogenetics?
The study of how genetic differences influence drug response.
81
Why is pharmacogenetics important?
Helps predict patient-specific efficacy and adverse drug reactions.
82
How do you convert mg to mcg?
1 mg = 1,000 mcg.
83
What is 1% solution in mg/mL?
10 mg/mL.
84
How do you dilute 10 mg of drug in 250 mL?
10 mg / 250 mL = 0.04 mg/mL or 40 mcg/mL.
85
What is the concentration of epinephrine 1:1,000?
1 mg/mL.
86
What is the concentration of 1:200,000 epinephrine?
5 mcg/mL.
87
What must a drug do first to initiate a physiologic effect?
Bind to a receptor and form a complex
88
What is the propensity of the drug-receptor complex to form called?
Affinity
89
What is the propensity to break down called?
Dissociation constant
90
What are most drug receptors?
Proteins in the plasma membrane that are involved in cell signaling (ex. G-protein-coupled receptors and ion channels)
91
Does drug binding equal drug effect?
No, it is governed by the characteristics constant called efficacy
92
What does affinity and efficacy give rise to?
Potency. Typically measured as effective concentration for 50% of maximal effect (EC50)
93
Depending on a drug's relative efficacies, how are they characterized?
Full, partial, or inverse agonists
94
What is a drug with receptor affinity, but no efficacy?
Antagonist
95
What is it called when a drug binds to receptors at distinct binding sites, resulting in complex receptor actions?
The interactions are called allosteric
96
What is signal transduction?
Process by which receptors transduce signals from extracellular messengers via second messengers to regular cell functions
97
What is the pharmacophore model?
Compatibility between chemical compound and a binding site
98
What determines the ability of a drug to bind to a particular site?
Depends on interactions determined by the chemical structure of the drug and binding site
99
What is posology?
Science of drug dosage (“dosology”)
100
What is the ultimate goal of clinical pharmacology?
Provide scientific foundation for rational posology (i.e. what is the right dosage for my patient)
101
What is Pharmacokinetics?
What body does to the drug, study of relationship between drug dose and drug concentration over time, dose-concentration relationship
102
What is Pharmacodynamics?
What the drug does to the body, study of relationship between drug concentrations and drug effects, concentration-effect relationship
103
What is the biophase?
The theoretical site of drug action or effect site.
104
Does blood plasma concentrations correlate well with drug effects?
No, especially during non-steady state conditions (after bolus injection or an infusion rate change)
105
Do remifentanil and propofol work synergistically?
Yes, so much less of each drug is needed to reach desired effect (a goal of modern anesthesia, to use combinations of drugs)
106
What is Volume of Distribution formula?
Vd = Amount of dose (mg)/ Concentration (mg/L) (MILLERS Basic Fig 4.1)
107
How is the volume of distribution formula refined for time?
Vd = Amount (t)/ Concentration (t) (MILLERS Basic Fig 4.2 Pic)

NSU AA Denver: Summer 2025 (2nd Semester) (24 decks)

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