Pharmacodynamics Flashcards

1
Q

What is a ligand?

A

A molecule that can bind to a complex with a receptor to produce a response. Can be endogenous or exogenous

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2
Q

List in order from weakest to strongest bonds (4 of them)

A

Van De Waals, Hydrogen, Ionic, Covalent

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3
Q

What is a Van De Waals bond?

A

2 molecules with electrostatic attraction will have a weak bond

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4
Q

What is a hydrogen bond?

A

Occur frequently when you have a molecule with a negative charge that has an electrostatic attraction to a positively charged hydrogen molecule

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5
Q

What is an ionic bond?

A

a positively charged ion and a negatively charged ion form a double bond

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6
Q

What is a covalent bond?

A

a chemical bond that involved sharing of electrons between atoms. Irreversible. Strongest bond

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7
Q

Explain a ligand gated receptor

A

A ligand binds to receptors and allows passage through the phospholipid bilayer. ex. acetylcholine receptors

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8
Q

Explain a G-protein coupled receptor

A

A ligand binds and causes structural changes to the G protein inside the cell. It becomes activated, finds an effector protein and causes a response. Ex. GABA receptors

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9
Q

Explain an enzyme linked receptor

A

A drug or hormone binds causes an enzyme to be activated inside the cell. That enzyme travels to an effector protein, and causes an affect. ex. tyrosine kinase

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10
Q

Explain Intracellular receptor

A

Something can pass through the phospholipid bilayer because: it lacks polarity (non-ionized), small enough to go directly through

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11
Q

What is the Law of Mass Action?

A

Drug + Receptor = Drug-receptor complex

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12
Q

What are the affects of the Law of Mass Action?

A

Elimination, concentration

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13
Q

What is the X axis on a drug-response curve?

A

Dose or Concentration

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14
Q

What is the Y axis on a drug-response curve?

A

Result or Effect

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15
Q

What is the Emax?

A

Maximal amount of effect

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16
Q

What does a full agonist do and what is an example?

A

Binds to a receptor and mimics an endogenous ligand. Reaches full Emax. Ex: Fentanyl (IV narcotics)

17
Q

What does a partial agonist do and what is an example?

A

Binds to a receptors and partially activates a response Doesn’t reach full emax. It competitively blocks other agonists. Ex. nalbuphine.

18
Q

Describe competitive agonist:
Reversible or irreversible antagonism?
Increased concentration can or cannot overcome effect?

A

They bind to a receptor and block activity. Increasing drug concentration will kick antagonist blocker off.
Reversible antagonism
CAN overcome

19
Q

Describe competitive agonist:
Reversible or irreversible antagonism?
Increased concentration can or cannot overcome effect?

A

Binds to a receptor, blocks it, drugs cannot offset it.
Irreversible antagonism (Covalent bond)
CANNOT overcome

20
Q

What is an inverse agonist?

A

It binds to a receptor and does the opposite effect ex. flumazenil

21
Q

What is potency?

A

The amount of drug needed to produce an effect

22
Q

What is efficacy?

A

Ability of a drug to produce a physiologic or clinical effect. More important than potency. We want drugs that WORK.

23
Q

How do you calculate therapeutic index?

A

ToxicDose50/EffectiveDose50

24
Q
Combination Therapy: 
Addition:
Synergism:
Potentiation:
Antagonism:
A

Addition: 1 + 1=2
Synergism: 1 + 1 = 3
Potentiation: 1 + 0 = 3
Antagonism: 1 + 1 =0

25
Q

Explain addition:

A

using 2 different drugs, you get expected results. Usually have the same mechanism of action

26
Q

Explain synergism:

A

using 2 different drugs results in a greater effect. Ex. fentanyl and versed

27
Q

Explain potentiation:

A

Combining a drug that normally doesn’t have an effect with a drug that has an expected effect and the effect is greater. Ex. NSAIDS and Coumadin

28
Q

Explain antagonism:

A

Combine 2 drugs and get no results, they cancel each other out. Ex. protamine and heparin

29
Q

What is down regulation?

A

Requires increased dose to have same effect. Physiologic tolerance. Ex: caffeine, nicotine, opiods, alcohol

30
Q

What is tachyphylaxis?

A

an acute rapid decrease in response to a drug after its administration.

31
Q

What is stereochemistry?

A

Study of 3D structures of molecules

32
Q

What is a chiral model?

A

Molecules with 3D asymmetry. Almost always centered around carbon.

33
Q

What is enantiomerism?

A

Pairs of molecules that are mirror images of each other

34
Q

What is a racemic mixture?

A

50/50 mixture of “left” and “right-handed” enantiomers of a chiral molecule