Basic Principles of Pharmacology Flashcards

1
Q

Endobiotics

A

agents normally produced within the body that are used therapeutically

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2
Q

Xenobiotics

A

agents NOT normally produced within the body

*Largest proportion of medications

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3
Q

Pure Food and Drug Act

A

Label active ingredients (1906)

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4
Q

Harrison Narcotic Act

A

Ban OTC sale of addictive drugs (1914)

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5
Q

Food, Drug, and Cosmetic Act

A

Document safety

Label inactive ingredients (1938)

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6
Q

Durham-Humphrey Amendments to Food, Drug and Cosmetic Act

A

2 categories of drugs created:
1)Legend Drugs-need prescription
2)OTC Drugs
(1951)

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7
Q

Kefauver-Harris Amendments to Food, Drug and Cosmetic Act

A

Must demonstrate effectiveness (1962)

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8
Q

Controlled Substances Act

A

-Schedule 1: Drugs w/out legal use
-Schedule 2: Drugs w/highest abuse potential
-Schedule 3-5: Decreasing abuse potential
(1970)

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9
Q

Dietary Supplement Health & Education Act

A

Removed vitamins, minerals, herbals, botanicals, amino acids, and metabolites from FDA control

  • No longer approved/regulated by FDA
  • No responsibility for ensuring effectiveness
  • Manufacturer responsible for ensuring safety
  • Marketing and Advertising restrictions implemented
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10
Q

Name the 3 Categories of OTC Drug Safety

A

Category 1: Safe and Effective
Category 2: Not safe, Not Effective, or Both
Category 3: Safety and effectiveness inconclusive

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11
Q

Development and Marketing of New Drugs

A

1) Preclinical Trials: Checks effects and safety in animals
2) Clinical Studies (Require FDA approval)
- Phase 1: Initial dose range and safety w/healthy volunteers
- Phase 2: Efficacy in diseased volunteers and effective dose
- Phase 3: Compare w/best current treatment
3) New Drug Application (NDA) (Require FDA approval)
- Phase 4: Post-marketing monitoring for rare adverse effects

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12
Q

What is First Pass Effect?

A

A phenomenon in which a drug gets metabolized at a specific location in the body that results in a reduced concentration of the active drug upon reaching its site of action or the systemic circulation.
Often the Liver.

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13
Q

Name the 5 ways drugs move across the cell layers.

A

1) Passive Diffusion
2) Facilitated Diffusion
3) Active Transport
4) Aqueous Diffusion
5) Pinocytosis/Exocytosis

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14
Q

What is Passive Diffusion?

A

Movement from high concentration to low concentration via lipid solubility

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15
Q

What is Facilitated Diffusion?

A

Movement down the concentration gradient via a membrane carrier protein *No energy source

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16
Q

What is Active Transport?

A

Movement against the concentration gradient via membrane carrier protein *REQUIRES energy source

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17
Q

What is Aqueous Diffusion?

A

Movement via channels between cells

  • Glomerulus filtration has the largest gaps
  • BBB has NO gaps
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18
Q

What is Pinocytosis? What is Exocytosis?

A
  • Method by which a cell absorbs small particles outside the cell and brings them inside
  • Process by which the contents of a cell vacuole are released to the exterior through fusion of the vacuole membrane with the cell membrane
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19
Q

Is the Henderson-Hasselbalch equation below for Acids or Bases?
pH=pKa +log([ionized]/[non-ionized])

A

Acids

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20
Q

Is the Henderson-Hasselbalch equation below for Acids or Bases?
pH=pKa +log([non-ionized]/[ionized])

A

Bases

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21
Q

Write the Ionization equation for Acids

A

HA πŸ” H+ + A-

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22
Q

Write the Ionization equation for Bases

A

BH+ πŸ” B + H+

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23
Q

Acids are (Ionized/Non-Ionized) in Acidic pHs?

A

Non-Ionized

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24
Q

Bases are (Ionized/Non-Ionized) in Acidic pHs?

A

Ionized

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25
Q

What substituents make drugs behave as weak organic bases?

A

Amine groups (-NH2)

26
Q

What substituents make drugs behave as weak organic acids?

A

Carboxyl groups (-COOH) and Hydroxyl groups (-OH)

27
Q

According to the pH Partition Hypothesis of Drug Diffusion, weak organic acids and bases cross biomembranes more readily in the (Ionized/Non-ionized) and (Lipid-Soluble/Water-Soluble) form.

A

Non-Ionized

Lipid-Soluble

28
Q

Are weak acids better absorbed at pHs BELOW or ABOVE their pKa?

A

BELOW

29
Q

Are weak bases better absorbed at pHs BELOW or ABOVE their pKa?

A

ABOVE

30
Q

Name 2 Solute-Carrier (SLC) Transporters.
What is their function?
What kind of transporters are they?

A

-Organic Anion Transporters (OATs): Influxers of weak organic acids
-Organic Cation Transporters (OCTs): Influxers of weak organic bases
ACTIVE Transporters w/Indirect Energy source

31
Q

What are ABC Transporters?
What is their function?
What kind of transporters are they?

A

ATP Binding Cassette Transporters: contain ATPase and are Effluxers of weak organic acids and bases
*These included MRPs, MDRs, and P-glycoproteins
ACTIVE Transporters w/Direct Energy source

32
Q

True/False

Plasma Protein binding to drugs does not cause Drug-Drug Interactions.

A

False

33
Q

What drugs can cross the BBB?

Lipid-Soluble or Water-Soluble

A

Lipid-Soluble

34
Q

What is Pharmacodynamics?

A

The study of how drugs have effects on the body. This involves the Drug-Receptor Interaction.

35
Q

What is Pharmacokinetics?

A

The study of drug absorption, distribution, metabolism, and excretion.

36
Q

What is a Quantal drug response?

A

All or None! They either work or they don’t!

Ex: Anti-arrhythmics, Anti-convulsants

37
Q

What is a Graded drug response?

A

Continually increasing or decreasing responses

Ex: Anti-hypertensives, Anti-diabetic agents

38
Q

What is ED50?

A

Effective Dose 50: dose of drug which produces a response in 50% of the population

39
Q

Define Efficacy

A

A drugs ability to activate the receptors and get a response.

40
Q

Define Potency

A

The amount of drug required to get an ED50 response

*Less drug required for response, More Potent the drug

41
Q

What is Therapeutic Index?

A

The difference between the ED50 and the TD50 (Toxic Dose in 50% of the population).
TI is written as a ratio=> TD50/ED50

42
Q

What is an Agonist?

What is an Antagonist?

A

Agonist is a drug that, by itself, produces a response

Antagonist is a drug that, by itself, produces no response but prevents the agonist response

43
Q

What is an Inverse Agonist?

A

A drug that interacts at the receptor to produce an inhibitory response

44
Q

Define Competitive Antagonist

A

A drug that competes with agonists, usually for a common binding site in a receptor.

  • Increasing the agonist dose can overcome the antagonist drug
  • Effects are REVERSIBLE
45
Q

Define Non-competitive Antagonist

A

A drug that binds to an allosteric (non-agonist) site on the receptor to prevent activation of the receptor.
*Effects are IRREVERSIBLE

46
Q

What is tachyphylaxis?

A

A decreased response to a drug after administration that develops in minutes

47
Q

What 3 ways can drug action be terminated?

A

1) Redistribution: drug literally moves away from the receptor site (Ex: Anesthetics)
2) Biotransformation (aka Metabolism): converts substances into different compounds
3) Excretion: primary means of reducing drug concentration in tissues by removing drug through kidney, liver, or lungs (gases only)

48
Q
Which of the following are Biotransformation/Metabolism reactions?
CYPs (Cytochrome P450s)
OATs (Organic Anion Transporters)
MAOs (MonoAmine Oxidases)
Cholinersterases
UGTs (Glucuronyl Transferases)
OCTs (Organic Cation Transporters)
STs (Sulfotransferases)
A
CYPs (Cytochrome P450s)
MAOs (MonoAmine Oxidases)
Cholinersterases
UGTs (Glucuronyl Transferases)
STs (Sulfotransferases)
49
Q

What is an Active Metabolite?

A

Drug metabolite that has significant activity (sometimes greater than the parent compound)

50
Q

What is a Prodrug?

A

An inactive/relatively inactive precursor drug that is converted to a more active compound by enzymes

51
Q

How do inhibitors modulate metabolism and therefore drug level?

A
Decrease metabolism (inhibit CYPs) and Increase drug levels
*Common mechanism of Drug-Drug interactions!
52
Q

What are some common inhibitors of drug metabolism?

A

Imidazoles (cimetidine, ketoconazole)
Macrolide antibiotics (erythromycin)
Grapefruit juice

53
Q

How do activators modulate metabolism and therefore drug level?

A
Increase metabolism (activate CYPs) and Decrease drug levels
*Common mechanism of Drug-Drug interactions!
54
Q

What are some common activators of drug metabolism?

A

Ethanol
Phenytoin
Phenobarbital
Pesticides

55
Q

How can filtration (aka kidney excretion) of a drug be increased?

A

Increased urinary volumes (w/saline, diuretics, ect.)
Increased blood flow to the kidneys
Altering the pH gradient w/in the lumen of the kidneys

56
Q

Where does filtration of drugs occur in the kidney?

A

Glomerulus

*Limited by Drug size and Protein binding of drugs

57
Q

Are hydrophilic or lipophilic drugs more easily excreted via the kidneys?

A

Hydrophilic Drugs are more easily excreted via the kidneys

58
Q

True/False

The kidneys have Active Transporters located in the Proximal Tubules that facilitate drug excretion.

A

True

  • Active transporters include the SLC Transporters (OATs and OCTs) and the ABC Transporters (MRPs)
  • Glucuronyl Transferases (UGTs) and Sulfotransferases (STs) create anion metabolites which also helps facilitate excretion by Active Transporters
59
Q

How does Probenecid effect Drug excretion by the kidneys?

A

Probenecid (anti-gout agent) is a competitive inhibitor of OATs causing decreased excretion of other drugs

60
Q

How does Cimetidine effect Drug excretion by the kidneys?

A

Cimetidine (anti-histamine agent) is a competitive inhibitor of OCTs causing decreased excretion of other drugs

61
Q

Describe the Enterohepatic Circulation.

A

Process of a drug or metabolite in the liver is secreted into the bile, stored in the gall bladder, and subsequently released into the small intestine, where the drug can be reabsorbed back into circulation and subsequently returned to the liver.
*Certain enzymes in the GI tract can reactivate the drug