08/21 Intro To Pharm Flashcards

1
Q

What are exogenous chemicals?

A

Chemicals that originate outside of the body

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2
Q

What are endogenous chemicals?

A

Chemicals that originate inside of the body.

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3
Q

Who coined the phrase “The dose makes the poison” ?

A

Paracelsus

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4
Q

Why is the phrase “the dose makes the poison” important?

A

It hones in on the idea that any drug, even one typically used for “good”, can be harmful (poisonous) when the dose is too high.

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5
Q

Why is the phrase “the dose makes the poison” important?

A

It hones in on the idea that any drug, even one typically used for “good”, can be harmful (poisonous) when the dose is too high.

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6
Q

What is Pharmacodynamics?

A

the study of what the drug does to the body
I.e. You give a drug and see the HR go down

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7
Q

What is Pharmacokinetics?

A

The study of what the body does to the drug.
I.e. what is the half life of the drug d/t the liver being able to break it down, Can the BBB stop the drug from entering the brain.

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8
Q

What is Pharmacogenomics?

A

The study of a person’s genetics to predict how well the person will respond to a certain drug or drugs

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9
Q

What is an Agonist?

A

A drug that elicits a response from the receptor when it is bound to that receptor.

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10
Q

What is a ligand?

A

A molecule or atom that binds to a receptor causing changes in the cell signaling.
I.e. endogenous or exogenous drugs

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11
Q

What response do exogenous agonists typically elicit?

A

The same response you would expect from an endogenous agonist.
I.e. Endogenous Epinephrine vs exogenous epinephrine.

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12
Q

What does an antagonist do?

A

It blocks the endogenous ligand from binding to the receptor, or it blocks that receptor from functioning. It essentially shuts down the receptor- blocks it.

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13
Q

What are the categories of organic compounds?

A

Carbohydrates, lipids, proteins, nucleic acids

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14
Q

What are the characteristics that determine receptor interactions?

A

Correct Shape and size (lock and key)
Correct Electrical Charge
Correct Atomic composition

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15
Q

What is the strongest bond in the biological system?

A

Covalent bond

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16
Q

what is an electrostatic bond?

A

A bond that is created from charges (Negative to positive)

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17
Q

What is a covalent bond?

A

A bond created from 2 molecules sharing electrons

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18
Q

What is a hydrophobic bond?

A

A bond created between a non-polar (no charge) drug and a non-polar receptor site. these drugs are water-fearing and are soluble in lipids.

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19
Q

What is the relationship between bond strength and specificity?

A

Inverse
The stronger the bond the less specific. (Covalent)
The weaker the bond, the more specific.
(Hydrophobic)

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20
Q

What are most Receptors made of?

A

Proteins

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21
Q

What is an isomer?

A

Molecules that have the same chemical equation, but a different arrangement of atoms (a different shape)
I.e. fructose and glucose have the same c6h1206 but a different shape, and therefore have different effects on the body.

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22
Q

What is an optical isomer?

A

A mirror image of isomers. 2 molecules that have the same chemical equation but different physical structure.
*Think gloves

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23
Q

What is a racemic mixture?

A

A 50:50 mixture of two optical isomers.
I.e. R ketamine and S ketamine.

24
Q

What is an active site on a receptor?

A

The site on a receptor where, typically, the native ligand would bind.

25
Q

Are there other binding sites on a receptor besides the active site, and what do they do?

A

Yes, they act in different ways. Some close the active site where a ligand cannot bind. Some may enhance the active site in a way that makes a ligand bind better.

26
Q

What are the drugs that bind to sites on a receptor called that are NOT the active site?

A

Allosteric

27
Q

What is the classification of ligand that binds to an active site on a receptor?

A

Orthosteric

28
Q

What does ADME stand for?

A

Absorption
Distribution
Metabolism
Excretion

29
Q

What is the EC 50?

A

The point on a graph where the concentration of the drug elicits 50% of the effect.

30
Q

What is the Kd 50?

A

The point on a graph where 50% of the receptors are bound to the drug give.

31
Q

Why does the Kd not equal the EC50?

A

Because a drug can bind to 25% of the receptors and elicit a 50% effect. The amount of receptors bound does not directly correlate to the same percentage of effect.

32
Q

What does a high or low Kd on a graph mean in terms of receptor affinity?

A

Low Kd= high drug/receptor affinity
High Kd= low drug/receptor affinity

33
Q

What does an allosteric activator do?

A

It is a drug that binds somewhere outside of the active site and elicits a response in the active site to bind more easily to the agonist.

34
Q

What does giving an increasing dose of an agonist + an allosteric activator do?

A

It shifts your graph to the left. It elicits an even greater response than the normal agonist, increasing the maximum effect of the agonist drug.

35
Q

What is a competitive inhibitor?

A

A subtype of antagonist that competes for the active site on the receptor.

36
Q

What does giving an increasing dose of an agonist + a competitive inhibitor antagonist do?

A

It shifts your graph to the right, meaning you will need more and more agonist drug to overcome the antagonist and eventually see the same response as an agonist drug by itself.

37
Q

What is an allosteric inhibitor?

A

An Antagonist that binds outside of the active site and is NONcompetative. (Because it binds outside of the active site)

38
Q

Can an allosteric inhibitor be surmounted?

A

No, because it binds outside of the active site and therefore can never be overtaken by the orthosteric agonist.

39
Q

What does giving an increasing dose of an agonist + an allosteric inhibitor do?

A

It shifts the graph WAY to the right, never reaching the normal agonist limits. Meaning it blocks the effects of the agonist.

40
Q

What is an agonist mimic or indirect agonist?

A

A drug that works down the cascade of events to increase the effects of an agonist.

41
Q

Associate competitive with

A

Surmountable. You can give more agonist and eventually outcompete the antagonist.

42
Q

Associate non-competitive with

A

Insurmountable. No matter how much agonist you give, the agonist will never win.

43
Q

What is an example of a orthosteric insurmountable antagonist?

A

An antagonist that binds at the orthosteric space and creates a covalent bond.

44
Q

A Partial agonist acts as an ______ in the presence of a full agonist

A

Antagonist

45
Q

What are 2 other mechanisms of antagonism besides binding to a receptor?

A

Administrating the opposite charge. I.e. overdose one negatively charged heparin you counteract with positively charge Protamine. Nothing to do with a receptor.

Physiologic- squelching the effect of drug 1. I.e. Epinephrine vs. aceytlcholine. Epi binds to beta receptors to speed up HR but acetylcholine works on muscarinic receptors to slow HR down.

46
Q

What is an inverse agonist?

A

A drug that favors the inactive form of the receptor. Acting like an antagonist because is shuts the receptor down so no cascade effect can happen.

47
Q

What is a partial agonist?

A

An Agonist that does not bind well to the receptor and therefore only elicits a partial effect.

48
Q

Briefly describe the history of Pharmacology.

A

Imhotep: First physician

Hippocrates: Father of western medicine

Asclepius: god of medicine, has a rod
Confused with
Caduceus: rod of Hernes the Greek messenger god

Materia Medica- a composition of botany and how effects the body (first textbook)
Attributed to Dioscorides.

Paracelsus: Father of toxicity . Famous quote

Modern day: Drug trials and Clinical testing

49
Q

What is Toxicology?

A

The study of poisons, its’ effects and detections.

50
Q

What is the difference between toxins and poisons?

A

Poisons are NON-biological. Toxins come from living organisms.

51
Q

Define Stereoisomerism

A

It’s a form of isomerism in which molecules have the same molecular formula and sequence of bonded atoms, but different spatial orientation.

52
Q

What is the Emax?

A

The maximum effect a drug can have when the drug is concentrated in the blood.

53
Q

What is the Emax?

A

The maximum effect a drug can have when the drug is concentrated in the blood.

54
Q

What is the Emax?

A

The maximum effect a drug can have when the drug is concentrated in the blood.

55
Q

What is Bmax?

A

The highest point on the graph when 100% of the receptors are bound to the drug.