Overview of Pharmacology: Part 2 Flashcards

1
Q

Distribution

A

Process by which the drug becomes available to body fluids and body tissues

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2
Q

Distribution process

A

Blood flow to tissues > Exiting the vascular system > Entering the cells

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3
Q

Protein binding

A

Drugs are distributed in the plasma > bound to protein

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4
Q

Only _____ _____ are active and can create a pharmacologic effect

A

Free drugs

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5
Q

Competition exists between drugs for…

A

Protein binding sites

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6
Q

When a drug is bound to albumin, it..

A

Does nothing

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7
Q

Bioavailability

A

The amount of drug available for use by the body (free drug)

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8
Q

What does the protein do over time?

A

Releases the drug, allows for a certain amount to be present at any given time

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9
Q

When two drugs compete for binding to albumin…

A

One loses and has a much higher level of free drug in the blood

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10
Q

In protein-binding competition, Coumadin (warfarin)….

A

Will always lose and be in high amounts in the blood

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11
Q

Drug metabolism

A

Process by which the body inactivates or bio transforms the drug

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12
Q

Primary site of drug metabolism

A

Liver

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13
Q

Usually a drug has been ___ by the time it is metabolized

A

Used

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14
Q

Hepatic Enzyme System is AKA

A

Cytochrome P450 Family

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15
Q

P450 System

A

Group of 12 closely related enzyme families, performs drug metabolism in liver

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16
Q

How are the enzymes named?

A

CYP1, CYP2, etc

CYP2D6

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17
Q

Every single P450 enzyme..

A

Has a group of drugs that it metabolizes

18
Q

If you give two drugs at the same time that are metabolized by the same enzyme…

A

One will be metabolized and one will not

19
Q

Does drug metabolism always result in the breakdown of drugs?

A

No! It can also result in the synthesis of molecules larger than the parent drug

20
Q

Consequences of drug metabolism

A
Accelerated renal excretion
Drug inactivation 
Decreased toxicity
Increased toxicity
Activation of prodrugs
Increased therapeutic action
21
Q

Increased therapeutic action (liver)

A

Ex: when codeine is metabolized in the liver, it becomes chemically similar to morphine

22
Q

Activation of prodrugs (liver)

A

Prodrugs are given as physiologically inert drugs, converted in the liver to active drugs (Dopamine for Parkinson’s)

23
Q

Increased toxicity (liver)

A

Ex: Tylenol taken in too large of a dose follows a metabolic pathway that creates metabolites that destroy the liver (Ibuprofen is similar w/ kidney)

24
Q

Factors in drug metabolism

A

Age
Induction of drug-metabolizing enzymes
First-pass effect
Competition between drugs

25
Q

An infant’s liver enzyme system does not even mature until…

A

6 months

26
Q

Induction of drug metabolizing enzymes example

A

Phenytoin: old anti seizure medication, induces the P450 enzymes so that any drug given will get metabolized quickly

27
Q

First pass effect

A

Oral drug goes through GI, then hepatic portal vein to liver, liver metabolizes certain amount of drug before it has even been to the tissues

28
Q

The higher the first-pass effect…

A

The higher the dose necessary

29
Q

First pass effect explains the difference between dosages in…

A

Oral vs. IV

30
Q

Excretion (methods)

A
Renal (main excretor) 
Breast milk
Bile
Lungs
Sweat / saliva
31
Q

Why do we want anesthetic patients to wake up?

A

So that they can breathe deeply and excrete the drug via the respiratory route

32
Q

Plasma drug levels (3 levels)

A

Minimum effective concentration
Therapeutic range
Toxic concentration

33
Q

Minimum effective concentration

A

Plasma drug level below which therapeutic effects will not occur

34
Q

Therapeutic range

A

Objective of drug dosing

35
Q

There is a window between…

A

MEC and toxic concentrations- we prefer this to be large

36
Q

Loading dose

A

Takes a while to get into therapeutic range, we give a larger amount of drug to get patient into therapeutic range

37
Q

Drug Half-life

A

The time takes for one half of the drug concentration to be eliminated

38
Q

Repeated dosing of medications can help cause..

A

Plateau levels, reducing fluctuations

39
Q

Morphine has a half life of 3 hours. If 50 mg were given at noon…

A

3pm- 25mg
6pm-12.5mg
9pm-6.25mg

40
Q

Pharmacodynamics

A

What the drug does to the body