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Pharmacology basics Flashcards

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1
Q

Pharmacology is

A

the study of the interactions between a drug and organism (body, enzyme, etc)

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2
Q

Pharmacodynamics is

A

the study of how a drug affects the organism (biochemical, physiological, and molecular effects)

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3
Q

Pharmacokinetics is

A

the study of how the organism affects the drug

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4
Q

What is included within pharmacodynamics? (5 things)

A

Site of Action
Mechanism of Action
Receptor Binding
Postreceptor Effects
Chemical Interactions

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5
Q

What can pharmacodynamics be affected by? (3 things)

A

Disease or Disorder
Age
Drug–Drug interactions

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6
Q

In regard to pharmacodynamics, what are the three receptor subtypes?

A

Enzymes
Ion Channels
Membrane receptors

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7
Q

When drugs bind, what kind of chemical interactions can they go through? Which one do we like, and which do we typically avoid? (four things).

A

Electrostatic interactions are what we prefer (it occurs with intermolecular forces, always will have van Der Waals, hydrogen bonding prominent)

Hydrophobic interactions

Covalent bonds – typically avoid; intramolecular force; irreversible, can be problematic, shuts down receptor; certain bonds can cause DNA mutations

Stereospecific interactions (enantiomers) r, s, e, z
Some receptors are specific, some are not - this could lead to bad side effects with stereoisomers

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8
Q

The drug acts as a what to the receptor?

A

Ligand

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9
Q

What were the three drug properties discussed in class? What do we want in a drug?

A

Affinity – how well the drug binds to the receptor

Efficacy – how well the drug produces its desired effect

Potency – term used to compare the relative affinity of competing drugs

–

We want a drug to have high affinity, and high specificity.

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10
Q

What are the categories of drugs? (2)

A

Agonists – bind and activate receptors

Antagonists – bind, but do not activate receptors

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11
Q

Drugs can bind in two ways to a receptor. What two ways are those?

A

Competitive – bind reversibly

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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12
Q

What is pharmacokinetics, and how does concentration come in to play? What does us help us understand?

A

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

Concentration affects the ability of the drug to give its desired effect

Helps to better understand the following:
Drug administration
Therapeutic dosing
Time intervals between drug dosing
Toxic dosing

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13
Q

Adding what to a drug stops it from being oxidized without adding much weight or changing properties?

A

Fluorine

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14
Q

What methods of administration are available? Which is not very efficient? Which is the fastest? Which bypasses first pass effect?

A

Enteral (oral) – through the intestines; not very efficient, lose a lot of drug

Parenteral – other than the intestine (four below)
Intramuscular
Subcutaneous
Intravenously – fastest; bypass first pass effect
Inhalation

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15
Q

Absorption rate determines what?

A

Time to maximal concentration at the receptor to produce peak effect.

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16
Q

What is bioavailability?

A

how much of the administered drug is actually absorbed. (typically used for oral administration)

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17
Q

What are the 8 factors affecting bioavailability?

A

Molecular weight of the drug

Drug formulation

Drug stability (especially pH sensitivity)

First pass metabolism (typically in the liver)

Blood flow

Gastric emptying (food slows this process)

Intestinal motility

Drug interactions

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18
Q

What is distribution?

A

Effectiveness of the movement of the drug throughout the body

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19
Q

What are the 6 things distribution is influenced by?

A

Blood

Total body water

Extracellular fluids

Lymphatic fluids

Cerebrospinal fluids

Protein-binding

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20
Q

What do drug solubility properties help us determine?

A

help determine ability of drug to be distributed to the desired receptor site.

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21
Q

What must be done to a drug to make it more soluble? Can it be too soluble?

A

The drug has to be more ionized; can’t be too soluble, otherwise it will have a hard time crossing membranes.

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22
Q

What is metabolism, and what does it do? What does it have the potential to do?

A

Breakdown of drugs into metabolites

Prodrugs – convert from inactive form to active form
Typically inactivates the drug ahead of excretion

Has the potential to lead to the formation of toxic metabolites

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23
Q

What are two common processes of metabolism? Which is MORE common?

A

Hydrolysis (esters, amides, and nitriles) – typically in pancreas, etc

REDOX reactions (Cytochrome P450 enzymes in the liver) – most common

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24
Q

What is excretion?

A

Removal of the drug and its metabolites from the body

25
Q

What is the purpose of excretion?

A

Helps to prevent toxic buildup of the drug in the body

26
Q

What are the four main routes of excretion?

A

Kidneys (majority of drugs)

Feces (unabsorbed drug or metabolites from bile)

Lungs (inhaled anesthetic drugs)

Sweat (not very common)

27
Q

Where does the majority of metabolism take place? How about excretion?

A

Liver - metabolizes most

Kidney - excretes most

28
Q

When do most drugs fail?

A

During the discovery phase of drug development

29
Q

What % of drugs fail in clinical testing?

A

~90%

30
Q

What is the ratio of drugs that make it to market vs those that don’t?

A

1:10,000

31
Q

What are the 8 steps of drug development in order, with time frame?

A

Target validation (1.5 years)

Compound screening (1.5 years)

Lead optimization (1.5 years)

Pre-clinical test (1 year)

Phase I (1.5 years)

Phase II (2.5 years)

Phase III (2.5 years)

Approval to launch (1.5 years)

32
Q

What is done during drug development: Target validation

A

Disease models

Target identification

Target validation

33
Q

What is done during drug development: Compound Screening

A

Visual screening

HTS

34
Q

What is done during drug development: Pre-Clinical testing & Lead optimization

A

SAR

Drug like properties

Solubility

Permeability

ADME

Plasma PK

Efficacy

Toxicity

35
Q

What is done during drug development: Phase I

A

PK

Dose escalation

Toxicity

36
Q

What is done during drug development: Phase II/III

A

Dose

Efficacy

Toxicity

37
Q

What are the two areas in drug development that most drugs fail?

A

Target validation & Phase II (ADME/Efficacy)

38
Q

What is lipinski rule of 5?

A

describes drug potential for a new chemical entity (NCE)

Used as a tool to measure a NCE’s potential bioavailability

10:500:5 (less than 10 hydrogen bond acceptors, less than 500 MW, cLogP less than 5)

39
Q

What is Lipinski rule of 5 based on?

A

Hydrogen bond donors (typically amines and alcohols)

Hydrogen bond acceptors (total number of N, O, and F)

Molecular weight (MW) = 500 or less**

Calculated Partition Coefficient (cLogP)

40
Q

If a rule within Lipinski rule of 5 is violated, what does it typically (but not always) mean?

A

Violation of more than one “rule” predicts a NCE (new chemical entity) is non-orally available/probably won’t be good drug

41
Q

What is cLogP?

A

measure/ratio of solubility of drug in oil vs water (octenol & water)

42
Q

What does a cLogP of less than 5 mean?

A

Crosses membranes easily

43
Q

What functional groups are linked to increased toxicity due to metabolites?

A

Aromatic anilines

Nitroaromatics

Aliphatic halides

Polycyclic aromatic hydrocarbons

Thiophenes

44
Q

What is drug efficacy directly related to?

A

Concentration of the drug at its site of action

45
Q

What should be considered when deciding concentration of a drug?

A

Drug concentration must be high enough to elicit the desired effect, but not too high to cause negative effects.

46
Q

Drugs must cross membranes throughout the entirety of ADME. What does that look like?

A

Absorption – enter into blood stream
Distribution – contact with receptor
Metabolism – leave receptor and move to liver (or other metabolism site)
Excretion – passage to kidneys for removal

47
Q

What drugs might use passive transport? How about active transport?

A

Passive - small, uncharged drug

Active - large, charged drug

48
Q

What is passive diffusion?

A

Transport across a membrane from area of high concentration to area of low concentration (requires no energy)

49
Q

What drugs use passive diffusion?

A

Low molecular weight drugs have an easier time crossing membranes

50
Q

What is passive diffusion dependent on? (in regard to absorption of drugs)

A

Absorption of drugs into the bloodstream is dependent on the acid/base properties of the drug and the pH at the site of absorption

51
Q

What is active transport?

A

Transport of a drug across a concentration gradient. Uses energy

52
Q

What does active transport require?

A

Requires the aid of membrane-bound proteins to recognize the drug for transport. Requires energy.

53
Q

What is influx?

A

Transport into the cell

54
Q

What is efflux?

A

Transport out of the cell

55
Q

What happens in active transport with high drug concentrations?

A

Transport plateaus due to a limited number of transport proteins available. This can lead to competition with structurally similar compounds.

56
Q

What is drug transport and distribution affected by?

A

Size & charge of the drug molecule.

57
Q

What size is considered a small drug?

A

<50 Da (bulk flow/passive transport; Pelphrey said they can be interchangeable)

58
Q

What size is considered a lipophilic drug?

A

50-500 Da (Passive transport)

59
Q

What size of a charged drug would require active transport?

A

> 50 Da

Chemistry (3 decks)

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