Introduction, Terminology, and Drug Classification Flashcards

1
Q

What is pharmacology?

A

the science that broadly deals with the physical and chemical properties, action, absorption, and fates of chemical substances termed drugs that modify biological function
- pharmakon = drug

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2
Q

Who is considered the Father of Chinese Medicine? What did he write?

A

Emporer Shen-Nung

Pen Tsao - list of herbal remedies considered the earliest compilation of drugs

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3
Q

What is Kahun Papyrus?

A

most ancient document on gynecology

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4
Q

Who is considered the father of medicine?

A

Hippocrates, who conducted systemic observations of his patients’ symptoms

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5
Q

Who was Theophrastus Bombastus von Hohenheim?

A

AKA Paracelsus - used drugs for specific and directed purposes

“All substances are poisons; the proper dose separates a poison from remedy

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6
Q

Who was Rudolph Buchheim?

A

German biochemist that established the first true experimental laboratory dedicated to pharmacology
- first “real” pharmacologist

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7
Q

What is the Pharmacopoeia?

A

official compilations of medicinal substances, their preparations, use, and dosages

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8
Q

What fueled the founding of the first veterinary colleges and hospitals?

A

response to epidemics of diseases, such as rinderpest

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9
Q

What are the 3 branches of pharmacology?

A
  1. Pharmacokinetics (PK) - study of the 4 key physiological processes that govern the time course of drug fate: Absorption, Distribution, Metabolism, Excretion - what the body does to the drugs
  2. Pharmacodynamics (PD) - study of cell/tissue responses and selective receptor affect - what drugs do to the body
  3. Pharmacogenetics (PG) - study of genetic determinants of response to drug therapy
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10
Q

What is a drug?

A

a molecule that interacts with specific molecular components of an organism to produce biochemical and physiologic changes/effects

(any chemical that can affect living processes)

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11
Q

What are the 3 major ways drugs are classified based on source?

A
  1. ORGANIC DRUGS: plants (digoxin, morphine, penicillin), animal (insulin, oxytocin)
  2. INORGANIC DRUGS: minerals (iron, calcium)
  3. SYNTHETIC DRUGS: most common
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12
Q

What are the 3 major ways that drugs are classified based on chemical structure?

A
  1. STEROIDS: derived from cholesterol (sex hormones, cortisol)
  2. GLYCOSIDES: (digoxin, digitoxin)
  3. BARBITURATES: derived from barbituric acid
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13
Q

What are the 3 major ways that drugs are classified based on biological effects?

A
  1. CARDIAC IONOTROPES: increase cardiac contractility (benazepril)
  2. NEUROMUSCULAR BLOCKERS: block transmission between a nerve muscle fiber
  3. ANTIMICROBIALS: bacteriostatic and bacteriocidal drugs
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14
Q

In what 3 ways can drugs be named?

A
  1. CHEMICAL NAME: IUPAC-given name that describes the drug using chemical nomenclature
  2. GENERIC NAME (nonproprietary): shortened name originating during drug development
  3. TRADE/BRAND NAME (proprietary): commercial name used for marketing - simple, catchy
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15
Q

What is the purpose of drug therapy?

A

induce a desired pharmacologic response

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16
Q

How is the degree of pharmacologic response controlled?

A

presence of drug concentration at the tissue (receptor)

17
Q

What processes regulate the absorption, distribution, and excretion of drugs in an animal?

A

processes that govern the movement of drugs across lipid-based biological membranes

18
Q

What are the 4 ways that drugs move through the body?

A
  1. bulk flow*
  2. passive diffusion*
  3. carrier-mediated transport
  4. endocytosis / pinocytosis
19
Q

What is bulk flow?

A

movement across the fenestrated capillaries of the body from plasma to tissue

20
Q

What is bulk flow dependent on? What is it independent of?

A

the concentration of drug dissolved in the plasma or tissue fluid (higher concentration = higher diffusion)

chemical nature of the of the drug

21
Q

What is the most common molecular weight of drugs?

A

< 350

22
Q

What is passive diffusion? What 5 things is it dependent on?

A

drug movement across cell membranes (transmembrane diffusion)

  1. lipid solubility
  2. environmental pH
  3. surface area
  4. thickness of the membrane to be transversed
  5. concentration of diffusible drug
23
Q

What is the most common method by which compouds move through the body?

A

passive diffusion

24
Q

What are the 2 major characteristics of drugs that affect their solubility?

A
  1. molecular weight
  2. partition coeficient (PC)
25
Q

What is the partition coefficient of a drug? What does a high number indicate?

A

the ratio determined by mixing the drug in a combination of water and an organic solvent (relative oil vs water affinity of a compound when it exists in its unionized form)

greater distribution, high lipid solubility, and greater ability of a drug to pass through the cell membrane

26
Q

According to pH, how are most drugs characterized?

A

most drugs are either weak acids or weak bases

27
Q

What is pKa?

A

pH at which 50% of the drug exists in the ionized state and 50% in the nonionized, lipid soluble state

28
Q

How does the environmental (host) pH affect a drug’s passive diffusion?

A

drugs will be more nonionized and more likely to diffuse into tissues when in a “like” environment (pH = pKa)

drugs will be trapped by ionization when present in an “unlike” environment

29
Q

How does drug absorption differ in the stomach and gut (intestine)?

A

STOMACH: weak acids are better absorbed in the acidic environment

GUT: weak bases are better absorbed in the alkaline environment

30
Q

What is the Hendersen-Hasselbalch equation?

A

equation used to calculate the percentage ionized of a drug or determine the concentration of a drug across a biological membrane

31
Q

What is carrier-mediated transport?

A

type of a diffusion where pH partitioning does not apply, and specialized membranes have specific carriers/transport systems/receptors

(can be active of passive)

32
Q

What are the 2 types of carrier-mediated transport?

A
  1. facilitated diffusion - passive transport (NO ATP) using a carrier protein to bind the drug and carry it across the membrane along with the concentration gradient
  2. active transport - using a specific carrier protein that uses ATP to move a drug across the membrane against the concentration gradient
33
Q

What are the main 2 things that carrier-mediated transport is dependent on? Why is this system used?

A

specificity and saturability

drugs normally cannot cross the membrane by passive diffusion because they are not lipophilic, so they need transporters

34
Q

In what 4 instances is carrier-mediated transport important?

A
  1. GI absorption of essential nutrients and drugs (beta-lactams)
  2. cellular uptake (glucose)
  3. removal of drugs from the CSF
  4. biliary and renal excretion of drugs
35
Q

What are 3 examples of facilitated diffusion?

A
  1. reabsorption of glucose by the kidney
  2. absorption of vitamin B12 from the intestine
  3. ion channels
36
Q

How can active transport be used after absorption?

A

removal of a drug after it has been absorbed (excretion/removal)

37
Q

What is the active transporter, P-glycoprotein?

A

AKA multidrug resistance protein, MDR1

ATP-driven efflux transporter encoded by MDR1/ABCB1, and highly expressed at the BBB, BTB, kidney, liver, intesting, and placenta to keep exogenous compounds out of critical tissues (Collies and Ivermectin)

38
Q

What is endocytosis/pinocytosis?

A

a compound binds to the surface of the membrane and the membrane invaginates and interiorized the compound

(not common of transmembrane passage for most drugs)

39
Q

Which one of the following statements is correct?

a. weak acids are better absorbed in alkaline environments
b. weak bases are better absorbed in acidic conditions
c. weak acids are better absorbed in the small intestine
d. weak bases are better absorbed int he stomach
e. weak bases are better absorbed in alkaline conditions

A

E