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Chemistry Me > Pharmacology Basics (Exam 4) > Flashcards

Pharmacology Basics (Exam 4) Flashcards

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1
Q

What is pharmacology?

A

The study of the interactions between a drug and organism

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2
Q

What is pharmacodynamics?

A

The study of the biochemical, physiological, and molecular effects of drugs on the body

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3
Q

What is pharmacokinetics?

A

The study of absorption, distribution, metabolism, and exretion of drugs from the body.

And toxicity according to professor.

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4
Q

What 5 things does the study of pharmacodynamics include?

A
  1. site of action
  2. mechanism of action
  3. receptor binding
  4. postreceptor effects
  5. chemical interactions
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5
Q

What 3 things can affect the pharmacodynamics of a drug?

A
  1. disease or disorder
  2. age
  3. drug-drug interactions
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6
Q

What are the 3 receptor subtypes?

A
  1. enzymes
  2. ion channels
  3. membrane receptors
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7
Q

What are 4 ways that drugs bind to the receptor (chemically)?

A
  1. electrostatic interactions (intermolecular forces)
  2. hydrophobic interactions
  3. covalent bonds
  4. stereospecific interactions (enantiomers)
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8
Q

What are the 3 properties of drugs?

A
  1. affinity: how well a drug binds to the receptor
  2. efficacy: how well the drug produces its desired effect
  3. potency: a term used to compare the relative affinity of competing drugs
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9
Q

What are the 2 categories of drugs/ligands (in terms of how they bind)?

A
  1. agonists: bind and activate receptors
  2. antagonists:
    a. competitive: bind reversibly
    b. non-competitive: either binds irreversibly or binds to create allosteric effects that diminish an agonist’s ability to bind to a different receptor
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10
Q

What 4 things does the study of pharmacokinetics help us better understand?

A
  1. drug administration
  2. therapeutic dosing
  3. time intervals between drug dosing
  4. toxic dosing
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11
Q

What are the 2 methods of drug administration?

A
  1. Enteral (oral): through the intestines
  2. Parenteral: other than the instestine
    a. IM
    b. Subq
    c. IV
    d. inhalation
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12
Q

The rate of what determines the time to maximal concentration at the receptor to produce peak effect?

A

absorption

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13
Q

What is bioavailability?

A

How much of the administered drug is actually absorbed (typically oral administration)

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14
Q

Factors affecting bioavailability (8)

A
  1. molecular weight
  2. drug formulation
  3. drug stability (especially pH sensitivity)
  4. first pass metabolism (liver)
  5. blood flow
  6. gastric emptying (food slows this process)
  7. intenstinal motility
  8. drug interactions
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15
Q

What types of things influence the effectiveness of the movement of the drug throughout the body (6)?

A
  1. blood
  2. total body water
  3. ECF
  4. lymphatic fluids
  5. cerebrospinal fluids
  6. protein binding
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16
Q

This property helps determine the ability of a drug to be distributed to the desired receptor site

A

solubility

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17
Q

Prodrugs convert from ______ to ______

A
  • inactive form, active form
  • typically inactivated ahead of excretion
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18
Q

What are the 2 common reactions by which a drug is metabolized?

A
  1. hydrolysis (esters, amides, nitriles)
  2. REDOX reactions (cytochrome P450 enzymes in the liver)
19
Q

What is excretion, and how is it helpful to the body?

A
  • removal of the drug AND its metabolites from the body
  • helps to prevent toxic buildup of the drug in the body
20
Q

What are the 4 main routes for excretion?

A
  1. kidneys
  2. feces
  3. lungs
  4. sweat
21
Q

Which phase of the drug development process do most drugs fail?
What percentage fail clinical testing?

A
  • The discovery phase
  • 90%
22
Q

What is the “Lipinski rule of 5”?

A
  • describes a drugs potential for a new chemical entity (NCE)
  • used as a tool to measure the NCE’s potential bioavailability
23
Q

What criteria is the “Lapinski rule of 5” based on (4)?
What predicts that a NCE is non-orally available?

A
  1. hydrogen bond donors (typically amines and alcohols), hydrogen bond acceptors (just count total number of N, O) <10 total
  2. molecular weight (MW): <500 da
  3. calculated Partition Coefficient (cLogP) <5
  4. Contains no more than 1 toxicophore

Violation of more than one “rule” indicates it is non-orally available

24
Q

T/F: low MW drugs with a low cLogP can easily cross membranes

A

True

25
Q

Potential drug compounds must have a mix of _____ and _____ groups

A

hydrophilic, lipophilic

26
Q

Which 5 functional groups have been linked to increased toxicity due to their metabolites?

A
  1. Aromatic anilines
  2. Nitroaromatics
  3. Aliphatic halides
  4. Polycyclic aromatic hydrocarbons
  5. thiophenes
27
Q

What is a drugs efficacy directly related to?

A

The concentration of the drug at its site of action. Concentration must be high enough to elicit the desired effect, but not too high to cause negative effects.

28
Q

What is passive diffusion? Does it require energy?

A

Transport across a membrane from an area of high concentration to an area of low concentration. Requires no energy.

29
Q

T/F: high MW drugs have an easier time crossing membranes

A

False. Low MW drugs have an easier time crossing membranes

30
Q

Absorption of drugs into the bloodstream is dependent on what 2 things?

A
  1. acid/base properties
  2. the pH at the site of absorption
31
Q

What is active transport? Does it require energy?

A

Transport of a drug across a concentration gradient.
Requires the aid of membrane-bound proteins to recognize the drug
Requires energy

32
Q

Drugs of this size (daltons) are transported by bulk flow

A

<50 Da

33
Q

Lipophilic drugs of this size (daltons) are transported by active transport

A

50-500 Da

34
Q

Ionized drugs of this size (daltons) are transported by active transport

A

> 50 Da

35
Q

5 examples that are considered structural alerts in drug development

A
  1. Aromatic anilines
  2. Nitroaromatics
  3. Aliphatic halides
  4. Polycyclic aromatic hydrocarbons
    5.Thiophenes
36
Q

Intramolecular forces strongest to weakest

A
  1. Ion-ion
  2. Ion-dipole
  3. Hydrogen
  4. Dipole-dipole
  5. Van der Waals
37
Q
A

Aromatic analines (Toxicophore)

38
Q
A

Nitroaromatics (Toxicophore)

39
Q
A

Aliphatic halides (Toxicophore)

40
Q
A

Thiophenes (Toxicophore)

41
Q
A

Polycyclic aromatic hydrocarbons (Toxicophore)

42
Q

A molecule that is _______ or ______ must go through active transport.

A

> 500 g/mol; charged

43
Q

In order to undergo passive transport, a molecule must be ______ and ______.

A

<50 g/mol; uncharged

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