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Pharmacology > Basics Part 1 > Flashcards

Basics Part 1 Flashcards

1
Q

What are drugs?

A

No matter what you call them, drugs are chemical compounds

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2
Q

Chemical name -

7-chloro-2-methylamino-5-phenyl-3H-1,4-benzodiazepine-4-oxide

A

Generic name - chlordiazepoxide

Proprietary, or trade name - Librium

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3
Q

What are drug sources?

A
  • Natural sources
  • Synthetic sources
  • Recombinant DNA
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4
Q

What are Natural Sources?

A

quinine, penicillin, and salicylate

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5
Q

What are Synthetic sources?

A

Barbiturate, sulfonamide, and benzodiazepine.

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6
Q

What are Recombinant DNA?

A

Insulin, growth hormone, cetuximab.

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7
Q

What are methods for identifying compounds?

A

Traditional uses

Screens of large numbers of compounds for activity in disease model

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8
Q

What are FDA standards?

A

Safety, Effectiveness, and Approved uses

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9
Q

What is the movement of drugs?

A
  • into the body (absorption)
  • to the target (distribution)
  • out of the body (metabolism/excretion)
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10
Q

What are the barriers to transit?

A

Cell membranes and connections between cells.

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11
Q

Passive diffusion — will it dissolve in a lipid bilayer?

A

Drug moves passively through membrane down a concentration gradient.

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12
Q

What is lipid solubility?

A

Hydrophilic, hydrophobic, and very hydrophobic

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13
Q

What is the capillary endothelium in the brain consisting of very tightly linked cells called?

A

blood brain barrier

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14
Q

Do drugs cross the placenta?

A

The capillary endothelial
cells in the placenta are loosely connected –
allowing free exchange of molecule

• Drugs cross the placenta

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15
Q

Can drugs pass the plasma membrane?

A

• Some drugs can cross the plasma membrane and
be absorbed through cellular barriers

• This is important when reaching targets in the
brain or within the cell

• Mechanisms include passive diffusion (most
common), facilitated diffusion, and active transport

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16
Q

What is Enteral?

A

Oral dose

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17
Q

What is absorption?

A

Absorption
For a drug to act, it must first get into the blood stream. For an oral dose, this involves movement across layers of cells that line the GI tract and blood vessels.

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18
Q

Enteral –oral doses

Drugs given orally must be absorbed from the stomach and/or intestine. These are unique environments.

A
  • Stomach is very acidic due to HCl secretion
  • Some drugs are unstable in acid
  • Time in stomach is variable so absorption in stomach is variable
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19
Q

Is the small intestine acidic?

A

stomach environment - enteric coatings

Small intestine is less acidic and has high absorptive area

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20
Q

What is the enteric coating?

A

stomach environment - enteric coatings
• Enteric coating dissolves slowly
• Prevents stomach – drug contact
• Protects either drug or stomach

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21
Q

What must the oral dose do in order to get into the blood stream?

A

Oral doses must cross out of the GI tract into the blood stream to get to the target. To do this, the drug must disintegrate and dissolve first.

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22
Q

What is dissolution?

A

Dissolution
• Some preparations dissolve rapidly
• Others provide sustained release —
convenience but there are safety issues too

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23
Q

What is a measure of absorption of an oral dose?

A

Absorption
a measure of absorption of an oral dose of drug into the bloodstream is “bioavailability”.
Note: not relevant to injected doses.
Some drugs are well absorbed orally, and some are not.
Those that are well absorbed are said to have high bioavailability.

Chemically equivalent forms produced by different manufacturers are often referred to as generic drugs.
It is possible for two preparations of the same drug to have different bioavailabilities.

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24
Q

What does bioequivalent?

A

a measure of absorption of drug into the bloodstream is “bioavailability”.

Two formulations that have the same bioavailability are said to be bioequivalent.

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25
Q

What does parenteral mean?

A

parenteral – other than oral delivery

Most common is intravenous. Other routes as well:
• subcutaneous
• intramuscular
• transdermal 
• inhalational
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26
Q

intentional — intramuscular injection can be used to make drug storage reservoirs or “depots”

A

parenteral – other than oral delivery
Improper treatment or mixture incompatibilities can produce drug precipitation to form unwanted suspensions
This can lead to embolism

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27
Q

What is distribution?

A

Distribution — where does the drug go after absorption?

Common distributions:

  • plasma
  • extracellular fluid
  • total fluid
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28
Q

What does measuring dilution after does allow?

A

Measuring the dilution of a drug after dosing allows an estimation of how the drug is distributed in the body.

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29
Q

For a given amount of drug administered: larger dilution indicates a larger volume in which the drug is diluted, the __________.

A

volume of distribution.

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30
Q

Sometimes the drug is not evenly distributed but instead gloms onto a particular site. This can involve an appreciable amount of drug, and the drugs is said to form _________.

A

a “depot”.

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31
Q

Depots increase the apparent volume of distribution- free drug is very dilute.
Depots of drugs can involve association with – _______, Cells, _______

A

Proteins, Cells, Fat

32
Q

Sometimes drugs can be displaced from their depots by other drugs. This _________ free drug concentration, and increases concentration of drug that can act at the target
This is one type of drug-drug interaction

A

increases

33
Q

Removal of drugs from the bloodstream is often referred to as _________. This is because one can think of the blood as being “cleared” of drug.

A

Clearance

34
Q

What are two important clearance mechanisms?

A

Metabolic clearance -

Excretion -

35
Q

What is metabolic clearance?

A

Metabolic clearance - removes drug by transforming it into a new compound.

Metabolic clearance
• Can vary between individuals
• Metabolism of one drug can sometimes be affected by another drug
• Liver metabolism is lower in elderly and newborns
• Unless dosage is adjusted, reduced clearance leads to higher blood levels

36
Q

oxidation to make a new compound can _____ drug activity

A

end

37
Q

oxidation to make a new compound can _______ a pro-drug

A

activate

38
Q

Metabolic clearance:
• Allows the body to break down _________ compounds

  • Produces derivatives that are more _____ and more ________
  • Aids in kidney excretion of the drug ________.
A

Foreign

Polar and hydrophilic

metabolites

39
Q

Anything orally absorbed goes directly to the __________

This is known as a _____________

A

Liver

portal circulation

40
Q

After passing through the liver, the absorbed nutrients and chemicals enter the ___________. If a compound is poorly metabolized almost all of it will get into circulation.

A

general circulation

41
Q

Renal Excretion

Many drugs are excreted either unchanged or as metabolites by the kidney.
The kidney is most effective in excretion of small molecules that are _____________. That is: small, ________ compounds.

A

not lipid soluble

small, polar compounds

42
Q

Lipid soluble drugs are ___________ in the nephron and escape back into the circulation during fluid reabsorption.
These drugs are excreted, but not concentrated by the kidney

A

not concentrated

43
Q

With _____________ there is a fixed rate of elimination.

A

zero order elimination

44
Q

The rate of elimination of most drugs is proportional to the drug concentration. This kind of elimination is called _____________.

A

first order elimination

45
Q

With first order elimination there is no fixed rate of elimination. Instead, elimination is described by the drug ____________.

A

half life, or T1/2

46
Q

With first order elimination, the rate of elimination is _____________ to the blood concentration

A

proportional

47
Q

As drug concentration in the body rises, so does the rate of __________

A

elimination

48
Q

In practice, drugs are usually given at a steady dosage schedule ( for example, 1 capsule every x hours). Drug concentration in the body rises until the rate of elimination equals the ____________.

A

rate of administration

49
Q

What are the actions of a drug at its target?

A

PHARMACODYNAMICS

50
Q

Receptors

A

Receptors
• Receptors are almost always protein molecules.
• The binding of a drug to its receptor is usually a reversible process.
• Binding requires a precise fit between the drug molecule and the receptor.

51
Q

Receptors

A
  • Affinity
  • Specificity
  • Intrinsic Activity
52
Q

The shape and chemical properties of a drug are critical in _________ to the receptor

A

binding

53
Q

What are two important clearance mechanisms?

A

Metabolic clearance- Liver
and
Excretion-Kidney

54
Q

How does metabolic clearance remove drug

A

transforms it into a new compound through oxidation. Oxidation can also make a new compound to end drug activity.

inactive to active

or

active to inactive

55
Q

A drug with low affinity, you will need

A

higher concentrations of the drug.

56
Q

What is the KD?

A

The KD is the concentration of the drug of half of the max binding. KD is inversely related to affinity. So, a drug that binds with high affinity will have a low KD.

57
Q

If a compound is subject to liver metabolism, the amount getting into the circulation is reduced
This is called a ________
For a strong first pass effect, none of the drug reaches the circulation

A

first pass effect

58
Q

Renal Excretion

Many drugs are excreted either unchanged or as metabolites by the kidney.
The kidney is most effective in excretion of small molecules that are __________.
That is: small, polar compounds.

A

not lipid soluble

59
Q

With _______ elimination, the rate of elimination is proportional to the blood concentration

A

first order

60
Q

Lipid soluble drugs are ______ concentrated in the nephron and escape back into the circulation during fluid reabsorption.
These drugs are excreted, but not concentrated by the kidney

A

not

61
Q

Some drugs are moved directly into the nephron by ____________.

A

active transporters

active transporters pump drug into urine.

62
Q

The rate of elimination of most drugs is proportional to the drug ________. This kind of elimination is called first order elimination.

A

concentration

63
Q

With continued dosing, blood levels rise, elimination rises, and steady state occurs when the __________ matches rate of input

A

rate of elimination

64
Q

In practice, drugs are usually given at a steady dosage schedule ( for example, 1 capsule every x hours). Drug concentration in the body rises until the rate of _________ equals the rate of _____________.

A

elimination, administration

65
Q

What is the strength of the interaction between a drug and its receptor. The higher of this means tighter binding.

A

AFFINITY

66
Q

What is it when a drug binds to only one kind of receptor, or multiple receptor types?

A

SPECIFICITY

67
Q

What is Intrinsic activity?

A

Intrinsic Activity
(what happens to the receptor when drug binds)

Drugs can enhance or block the activity of receptors

  • Agonists (activators) = full intrinsic activity
  • Antagonists (blockers) = no intrinsic activity
  • Partial Agonists = intermediate intrinsic activity
68
Q

What is a drug with a high intrinsic activity called?

A

agonist

agonist activate the receptors that they bind to.

69
Q

Dose response curves
• Increased drug concentration/_____ gives higher receptor occupancy

  • As receptor occupancy by drug increases, the response increases
  • Eventually receptors become ________ by drug
A

dose, saturated

70
Q

All-or-none responses require an approach in which groups are given different doses.
The percent responding to each dose is recorded, and plotted.

A

Therapeutic index:

lethal dose/ effective dose

We want a lethal dose to be huge and an effective dose to be smaller.

71
Q

Dose response curves
• We measure potency of a drug by the amount it takes to produce a half maximal response.
• This is the ______ if measuring drug level as a concentration
• ED50 if measured as a dosage.

A

EC 50

72
Q

Difference between polar and non-polar drugs

A

Polar drug doesn’t get into the bloodstream easily and Non-Polar drugs are able to get into the bloodstream easier.

73
Q

Tolerance

Distribution tolerance

  • Some drugs will induce the production of __________ that degrade the drug
  • Over time the liver is better able to destroy a given dose, and does so more rapidly
  • The net effect is lower circulating blood levels of the drug, because it is degraded faster
  • Classic case is barbiturate sleeping test in rats – over time the barbiturate is less and less effective
A

liver enzymes

74
Q

Tolerance

Pharmacodynamic tolerance

  • Most receptors _________ their responses
  • In other words, the more a receptor system is activated, the less it responds
  • Involves many mechanisms, but net effect is the same: less response to a given dose after repeated use
  • Classic case is opiates and tolerance
  • Or tolerance to odors like perfumes, etc
A

auto regulate

75
Q

ADVERSE EFFECTS - “SIDE EFFECTS”

Predictable
Side effects

• Unwanted effects that are well known to occur
Overdose
• Generally produces exaggerated intended effect or increased side effect
• Examples:
Drugs that reduce blood pressure may produce disastrously low blood pressure in overdose – too much desired effect
Morphine overdose produces cessation of breathing. Respiratory depression is a normal side effect

A

ADVERSE EFFECTS - “SIDE EFFECTS”
Less predictable
Allergies / Hypersensitivity
• Only a problem for some people, but can be very
serious or fatal “Idiosyncratic reactions”
• Unwanted effects that are so uncommon that they appear unique to an individual
• These are actually rare unrecognized side effects
• Everyone has a different genetic makeup – goal is to predict unwanted effects based on genomic testing

Pharmacology (5 decks)

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