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Non MSK OCS > pharmacology > Flashcards

pharmacology Flashcards

1
Q

What is pharmacodynamics?

A

the study of what the drug does in the body, including mechanism by which a drug exerts its effect on the body
- includes distribution and metabolism

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2
Q

What is a drugs mechanism of action?

A

how the drug produces its effects, not the site of action

  • sequential steps following drug binding to receptor
  • followed by signal transduction steps
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3
Q

what is a drugs site of action

A

location in the body where the drug exerts its therapeutic effect

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4
Q

what is the most common way to classify drugs

A

According to their mechanism of action

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5
Q

What role do receptors play int he drug therapeutic decision making

A
  1. primary determinate in does size and effect
  2. selectivity of drug actions
  3. mediate action of agonist and antagonist
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6
Q

What is the difference between an agonist and antagonist drug

A
  • agonist bind to a receptor and mimic the effect of the endogenous signaling compound
  • antagonist bind to the receptor and block the actions of the endogenous signaling compound
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7
Q

what is drug potency

A

measure of the strength, or concentration, of a drug required to produce a specific effect
- the greater the potency the less the drug is needed and the lower the change of an ADR

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8
Q

what is a drug’s maximum efficacy

A

the extent or degree of an effect that can be achieved

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9
Q

what is ceiling effect

A

increasing dose no longer produces a response

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10
Q

What is drug efficacy

A

The ability of a drug to accomplish the desired outcome

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11
Q

What is the difference between a graded dose response curve and a quantal dose response curve

A
  1. Graded - depiction of observed effects of a drug as a function of its dose in individuals, single test subjects or homogenous populations. The dose is slowing increased and the response is observed
  2. Quantal - a predetermined drug effect is set (median effective ED50 or median toxic TD50) and a population is provided with increasing doses. Each person is classified in has or does not have the predetermined effect.
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12
Q

What is the purpose of dose response curves

A

they are used to study the effects of a drug in order determine to proper therapeutic dosing

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13
Q

What is the therapeutic index of a drug

A
  • a quantal dose response variable
  • ratio of individuals achieving median effect dose (ED50) producing the desired response to individuals achieving the median toxic dose (TD50) producing the negative drug effect
  • greater the ratio the safer the drug
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14
Q

what are the different pathways of drug adverse reactions (3)

A
  1. mechanism based - extension of the drugs principal pharmacological actions
  2. off target - consequences of the drugs molecules not drug actions - hepatoxicity of acetaminophen is an example
  3. idiosyncratic - interaction of the drug with unique HOST factors and do not occur in the population at large
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15
Q

What drug characteristics will predict its ability to move in the body

A

Molecular…

  1. size
  2. shape
  3. ionization
  4. lipid solubility
  5. ability to bind to serum and tissue protein
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16
Q

What are the primary barriers to drug movement in the body

A

Membranes (capillary, GI, blood-brain, cellular)

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17
Q

What variables predicts a drugs ability to passively diffuse across a membrane

A
  1. diffuse along concentration gradients
  2. solubility in the lipid bilayer or permeability coefficient
  3. membrane surface area
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18
Q

What is permeability coefficient

A

how well a drug travels through the lipid bilayer
- dependent on participation coefficient (degree of innate lipid solubility) and degree of ionization (greater the ionization the more effect it takes to get through the membrane)

19
Q

What is the Flick low of diffusion

A

formula for describing passive diffusion across a plasma membrane

  • difference in concentration between outside and inside
  • surface area exposed to the drug
  • permeability coefficient
  • distance across membrane
20
Q

What are the key factors impacting a drug’s ionization

A
  1. the pH of the body fluids which the drug is dissolved

2. ionization constant of the drug itself

21
Q

how does the pH of the body fluid in which the drug is absorbed impact drug movement across membranes

A
  1. acidic drugs are non-ionized by acidic fluid thereby increasing their absorption rate (stomach acid makes them easier to absorb)
  2. basic drugs are non-iononzid by basic fluid such as the upper GI tract
  3. the drug will also tend to accumulate in areas where their ionization increased due to the decreased ability to cross the membrane
22
Q

what is bioavailability

A

fraction of unchanged drug reaching the systemic circulation following administration by any route

23
Q

what is first pass effect

A

a phenomenon of drug metabolism whereby the concentration of a drug is greatly reduced before it reaches the systemic circulation (metabolized or filtered out by liver)

24
Q

what is the difference between enteral and parenteral administration of a drug

A

enteral - oral, sublingual or rectal

parenteral - inhalation, IV, SQ, IV, TD, topical

25
Q

What is drug distribution

A

the process of molecules moving into and out of the various tissues of the body

26
Q

What is apparent volume of distribution and how does it effect drug distribution

A
  • it is a measure of apparent space in the body available to contain a drug
  • it is a ratio of the amount of drug administered to the concentration of the drug in the plasma
  • hydration impacts this variable, dehydration will cause the drug to be retained in the blood due to a greater concentration of drug binding proteins
  • hyperhduration can distribute greater loads of the drug to the target tissues
27
Q

What is drug biotransformation

A

chemical change that takes place in a drug following administration

28
Q

what are metabolites

A

the stuff comes off of the parent drug after it is biotranformed (typically they are more polar/less lipid soluble and more easily excitable)

29
Q

what are the different cellular mechanisms of drug biotransformation

A
  1. oxidation - addition of oxygen molecule or removal of hydrogen molecule
  2. reduction - removal of oxygen or addition of hydrogen
  3. hydrolysis - original compound broke in to separate parts
  4. conjugation - addition of endogenous substances
30
Q

how does liver function impact drug biotransformation

A
  • liver is the primary way of removing drugs from the blood stream
  • low liver function can increase the impact of the drug
  • drugs requiring the same liver enzyme to remove can result increased drug effect
31
Q

How many half lives are required to clear 90% of a drug

A

4-5x

32
Q

what is drug clearance

A

a measure of the body’s ability to eliminate a drug

33
Q

Drug elimination occurs by what processes

A
  1. clearance - rate of removal of the active form of the drug form the body and can occur via excretion and metabolism
  2. excretion - physical removal of the drug from the body via
34
Q

Describe relative organ blood flow at react versus with exercises

A
  • at rest blood volume 27% in liver 22% in Kidneys

- exercises changes to 3% liver, 3% kidney 71% muscle

35
Q

How does exercise impact drug effect

A

shifts in blood flow to different organs or regions of the body will change drug pharmokinetics

36
Q

how does exercise impact renal blood flow and drugs that are eliminated by the kidney

A

Decreases renal blood flow

- drugs such as atenolol have increased plasma concentration with exercise

37
Q

What are the drug administration routes, bioavailiablity adn charateristics

A
  1. IV, 100%, most rapid
  2. IM, 75-<100, large volumes but can be painful
  3. SC, 75-<100, smaller volume, can be painful
  4. oral, 5-<100 most convenient high first pass effect
  5. rectal30-<100, less first pass than oral
  6. inhal, 5-<100, often rapid onset
  7. transderm, 80<100 slow but low first pass
38
Q

What determines a drug’s therapeutic effect or adverse reaction?

A

Interaction with receptors

39
Q

What are the three functions of receptors as they relate to drugs

A
  1. determine quantitative relations between does or concentration of drugs
  2. responsible of selectivity of drugs
  3. mediate actions of both pharmacological agonist and antagonist
40
Q

what is the difference between an agonist and antagonist drug?

A
  1. agonist - binds to a receptor and produces a cellular response
  2. antagonist - binds to a receptor and blocks a cellular response
41
Q

What are pharmacokinetics?

A

how the drug enters the body and the body works in terms of absorption, distribution, metabolism (biotransformation) and elimination (DAME)

42
Q

Why is would understanding pharmacokinetics be important for PT’s

A

Many of the things we do will charge pharmacokinetic variables

43
Q

What are the active pathways for drugs to cross membranes?

A
  1. active transport
  2. endocytosis
  3. facilitated diffusion

Non MSK OCS (4 decks)

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