Apex- Pharmacodynamics Flashcards

1
Q

Pharmacokinetics

A

What the BODY does to the drug

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2
Q

Pharmacodynamics

A

What the Drug does to the body

> potency, efficacy, dose-response curve slope, agonist, antagonist, ED50, LD50, Theraputic index, stereochemistry

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3
Q

Chemistry term to describe the drugs specific shape, size, and characteristics which allow it to bind to a certain receptor.

A

Stereospecificity

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4
Q

A drug that binds to a receptor and fully enhances the response of that receptor

A

Full agonist

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5
Q

A drug that sit’s on a specific receptor, doesn’t activate it, but blocks an agonist from binding to it.

A

Antagonist

> it doesn’t tell the cell to do anything

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6
Q

Difference between competitive and non-competitive antagonists

A
  1. Competitive = reversible ; wants to compete, can lose and be overridden by increasing concentrations of agonists
    * Rocuronium competes with ACH at the NMJ
  2. Noncompetitive = irreversible binding; “not worth my time to even compete with you, I sit and stay, I win, you lose”
    * Aspirin inhibits the Cox-1 enzyme fro the entire life of the platelet (7-10days)
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7
Q

If the patient receives a competitive antagonists, will the dose-response curve shift to the right or left?

A

Right > because it will require MORE of the AGONIST to exert it’s effects

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8
Q

What happens with the dose response curve with noncompetitive agonists?

A

It shifts down and resembles a partial agonist

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9
Q

What might continuous administration of an agonist cause? Up or down regulation of receptors?

A

Down regulation - body senses the overstimulation of the target receptors and tries to fix it by not producing as many receptors

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10
Q

Continuous administration of an antagonist may cause up/down regulation of receptors?

A

Up-regulation. Body senses under stimulation of these receptors and wants to equilibrate by making more receptors

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11
Q

What law describes a drug binding to a receptor?

A

The law of mass action

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12
Q

Partial agonist AKA: ________
Example
How does it work

A

Agonist-Antagonist
Ex. Suboxone/ Nalbuphine
Binds to a receptor and PARTIALLY turns it on
>can block the effects of agonist by competing for binding sites

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13
Q

What kind of drug binds to a receptor and directly causes the opposite effect of a full agonist
Example?

A

Inverse agonist

(Not antagonist bc the antagonists just sit there and don’t cause any effect directly)

Epi- full agonist- binds to B1 > increased cAMP
Propranolol- inverse agonist - binds to B1- decreased levels of cAMP

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14
Q

Chemical term to describe a drug that binds in one place but works somewhere else

A

Allosteric

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15
Q

Dose- response curve: what represents how many of the receptors must be occupied to exert a clinical effect?

A

The slope

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16
Q

Dose response curve: what represents the dose required to achieve the clinical effect? X or Y axis

A

X-axis (bottom/horizontal) (slope)

17
Q

Dose-response curve- which part represents the ability of the drug itself to elicit a clinical effect? X or Y axis

A

The Y-axis (vertical)

18
Q

What is ED50 vs ED90?

A

The dose required to elicit a given clinical effect in 50%/90% of the population

(Dose response curves)

19
Q

With dose-response curves, once the plateau phase is reached, what would happen if you give more drug? Would it increase the effect?

A

No increase in effect , just increase in risk of toxicity

20
Q

Which drug is more potent (see dose response curve pic)

A

Drug A - less dose (x/bottom axis) is required to achieve the same effect of drug B

21
Q

With a dose-response curve, if the drug has an increased affinity for the receptor, which way will it shift?

A

To the left

>increased affinity = increased receptors to occupy to elicit the response

22
Q

See this dose-response curve. If these drugs are narcotics, what assumptions can be made about drugs A and B

A

Both drugs elicit a response but drug A elicits a greater response (greater analgesia)

23
Q

Which goes where ? Agonist, Inverse agonist, partial agonist, antagonist

A

Agonist - binds and enhances normal response
Partial agonist- binds and half ass enhances the normal response
Antagonist - binds to a receptor and prevents binding from other agents
*DOES NOT DIRECTLY EVOKE A CLINICAL RESPONSE!
Inverse agonist- binds to a receptor causing the opposite effect of its normal response
Ex) H1 & H2 blockers

24
Q

How is the therapeutic index of a drug measured?

A

LD50/ED50

  • ED50 - dose of a drug that elicits the intended clinical effect in 50% of the population
  • LD50 - dose of a drug that will kill 50% of the population
25
Q

What is the ED50 a measure of?

A

Potency

26
Q

What is a division of stereochemistry where the molecules have a center of 3-dimensional asymmetry?
What does the asymmetry stem from?

A

Chirality

-asymmmetry stems from the tetrahedral bonding of a carbon

27
Q

A molecul with 1 chiral carbon will exist as how many enantiomers?

A

Two

> the more chiral carbons in a molecule, the more enantiomers

28
Q

What are chiral molecules that are non-superimposable, mirror images of one another?

A

An Enantiomers

29
Q
Dextrorotary vs levorotarory enantiomers.
Which one is:
\+/-
R/S
Clockwise/counterclockwise
A

DEXTRO + R Clockwise
> think if you see DEXTER, your time (clockwise) is positively Running out

LEVO - S Counterclockwise
>think Levo loves being Silly (counterclockwise) , negative spin

30
Q

What kind of mixtures contain 2 enantiomers in equal amounts?

A

Racemic mixture

31
Q

About how many of the drugs we administer are enantiomers? How many of them are prepared as racemic mixtures? Exceptions (2)

A

1/3 are enantiomers
Almost all of them are prepared as racemic mixtures
Except : Levobupivacaine & Ropivacaine (Single enantiomers) (LEaVe the ROPe)

32
Q

12 Racemic mixtures

A
Bupivacaine 
Desflurane
Isoflurane
Ibuprofen
Ketamine
Ketorolac
Methohexital 
Methadone
Morphine
Mepivacaine
Prilocaine
Thiopental
33
Q

Is S-Bupivacaine more or less toxic than R-bupivacaine or the racemic mixture?

A

S-Bupivacaine = Levo-bupivacaine

Levo, Less cardiotoxic