Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Intro to Pharmacology > Week 1 Lecture > Flashcards

Week 1 Lecture Flashcards

1
Q

The term Pharmacology came from the Greek word ?

A

“pharmakon” (drug)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Pharmacology can be defined as?

A

The science that studies the properties of chemicals
used as drugs for therapeutic purposes OR

Pharmacology is the science that broadly deals with the physical and chemical properties, action,
absorption, and fates of chemical substances termed drugs that modify biological function

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What does the body do to drugs?

A

Absorption Distribution Metabolism Excretion (ADME)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Pharmcokinetics is the study of the ____ key physiological processes that govern the ____ _____ of drug fate in the body. This specifically looks at?

A

four, time, course, what the body does to drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Pharmacodynamics (PD) is the study of ___/____ responses and selective _____ effect.
Specifically looks at ?

A

cell, tissue, receptor, what the drug(s) do to the body.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Pharmacogenetics is the study of _____ _____ of response to drug therapy.

Why is this field of study important?

A

genetic, determinants

Important b/c able to identify genetic responses to every drug (because can not use same treatment for everyone).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

A drug is defined as a molecule that interacts with ________ molecular components of an organism
to produce _______ and _______ changes/effects.

Any _____ can be a drug and can affect ______ processes.

Drugs can ______, ______, _____ or ____ disease (pharmacotherapeutics)

It could be a prescription or over the counter (OTC)

A

specific, biochemical, physiologic, chemical, living, prevent, mitigate, diagnose, treat

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

True or False: There is no unified system to classify drugs

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Drugs can be classified according to their ?

A

sources, chemical structures or biological effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are some examples of organic drugs that are sourced from plants?

A

Digoxin, morphine, penicillin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are some examples of drugs sourced from animals?

A

Insulin, oxytocin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What are some examples of inorganic drugs ?

A

Iron and calcium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are most of the drugs that we work with?

A

Synthetic drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are some examples of steroid drugs ?

A

Cholesterol, sex hormones, cortisol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What are two examples of glycoside drugs?

A

Digoxin and digitoxin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Barbituates are derived from?

A

Barbituric acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Cardiac ionotropes ______ cardiac contractility. An example of this type of drug is?

A

increase, benazepril

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Neuromuscular blockers block transmission between ?

A

a nerve muscle fiber.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Examples of Antimicrobial drugs are

A

Bacteriostatic and bacteriocidal drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Describe the three ways to name a drug.

A

Chemical name: describes the drug using chemical nomenclature.
Generic name (nonproprietary): shortened name originated during drug development.
Trade or brand name (proprietary): commercial name used for marketing. Simple catchy.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

The purpose of drug therapy is to ?,

A

induce a desired pharmacologic response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

For most drugs the degree of the pharmacologic response is related to the drug ________ at the _____ (_____).

A

concentration, tissue, receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

A drug crosses several ______ membrane barriers from its site of ________ to reach its
site of _____.

A

lipoidal, administration, action

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

The processes that govern the movement of drugs across lipid-based biological membranes
are important and regulate its ?

A

absorption, distribution and excretion from the animal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Drugs move through the body by four mechanisms. Which of these are the most important?

A
  1. Bulk flow
  2. Passive diffusion
  3. Carrier-mediated transport
  4. Endocytosis or pinocytosis

Bulk flow and passive diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Bulk flow is defined as movement across the _______ capillaries of the body from _____ to _____.
• Is dependent on the _______ of drug dissolved in the _____ or _____ fluid
• The ______ _____ of drug does not affect Bulk flow.
• Most drugs are characterized by a ______ _____ (__) < 350.

A

fenestrated, plasma, tissue, concentration, plasma, tissue, chemical nature, molecular weight, MW

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

True or False: If the drug is more concentrated, it has an easier time diffusing via bulk flow.

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Passive diffusion is defined as the movement of a across ____ _______ (_______
diffusion) and depends on what host and drug factors?

A

cell membranes, transmembrane

  1. Lipid solubility of the drug
  2. Environmental pH
  3. Surface area
  4. Thickness of the membrane to be tranversed (edematous V/S normal tissues)
  5. Concentration of diffusible drug
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

What is the most common method by which compounds move through the body?

A

Passive diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Lipid solubility of the drug is influenced by what drug characteristics?

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

A ratio greater than __ suggests greater distribution and high ______ _______.

A

1, lipid solubility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Most of drugs are either ?

A

weak acids or weak bases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Drug pka is defined as?

A

pKa = pH at which 50% of the drug exists in the ionized state and 50% in the nonionized, lipid-soluble state

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

A drug will be more _______ and more likely to ______ into tissues when present in a “____” environment.

Drugs will be trapped by ______ when present in an “unlike” environment.

A

nonionized, diffuse, like, ionization

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

If a drug was located in the stomach

Weak acids are better absorbed in _____ conditions
Weak bases are ______ absorbed in acidic conditions

A

acidic, poorly

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

If we were located in the gut…

Weak acids are poorly absorbed in ______ conditions

Weak bases are ______ absorbed in alkaline conditions

A

alkaline, better

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

The Henderson-Hasselbalch equation enables you to calculate the _______ ______ of a drug or to determine the _______ of a drug across a _______ _______.

A

percent (%) ionized, concentration, biological membrane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

If the drug is a weak acid:

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

If the drug is a weak base

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

Carrier-mediated transport

The laws of ______ and ___ partitioning do not govern transmembrane flux of drugs.

The body can exert control and selectivity over the chemicals that are allowed to enter.

A

diffusion, pH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

Facilitated diffusion is an example of ______ ______ transport. Active transport is an example of _______ ________ transport.

What is an example of facilitated diffusion?

A

carrier-mediated, carrier-mediated, Passive transport (nonactive)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

Drugs are normally not _________, so transporters help.

A

lipphyllic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

Transport systems are normally characterized by ______ and _______.
Drugs transported normally cannot cross the
membrane by ______ _______ because they
are not ________.

A

specificity, saturability, passive diffusion, lipophilic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

Carrier mediated transport is important for
the ___ absortion of essential ______ and ____ (e.g., β-lactams), ______ _____ (e.g., glucose), the _______ of drugs from the CSF, and ______ and _____ excretion of drugs

A

GI, nutrients, drugs, Cellular uptake, removal, biliary, renal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

Facilitated diffusion - Passive transport (nonactive)
• ______ protein binds to drugs and carries them across the membrane.
• It does not require ________ _____
• It does not operate _____ a concentration gradient

A

Carrier, cellular, energy, against

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

Facilitated diffusion - Passive transport (nonactive)
Examples?

A
  • Reabsorption of glucose by the kidney
  • Absorption of vitamin B12 from the intestine
  • Ion channels: Na+, Ca2+, Cl-, H+, K+
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
47
Q

Active transport
• Drug transport is conducted by ______ _____ _____ through the membrane
• It requires ______ _____ to move a drug against its concentration gradient. Energy is
driven by the ______ of adenosine triphosphate.

A

specific carrier proteins, cellular energy, hydrolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
48
Q

Active transport may also occur in the opposite direction to ______ a drug after it has been ______.

A

remove, absorbed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
49
Q

The MDR1 protein is also referred to as the ?
What role does MDR1 and ABC transporter play?
The MDR1 protein is encoded by?
How large is this protein?

MDR1 is highly expressed at the _____-_____ barrier, at the ______-_____ barrier and also in ______, ______, _______, and _______.

A
  1. P-Glycoprotein OR the multidrug resistance protein
  2. IDK
  3. multidrug-resistance gene MDR1/ABCB1
  4. 170 kDa

blood-brain, blood-testis, kidney, liver, intestine, placenta

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
50
Q

The function of MDR1 is to keep ______ compounds out of _______ tissues

A

exogenous, critical

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
51
Q

Endocytosis or pinocytosis is not a ?
Cells may absorb drugs by?
• A compound binds to the ______ of the membrane, the membrane _______
and ______ the compound.

A

primary mechanism
Endocytosis.
surface, invaginates, interiorizes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
52
Q

There are different methods available for administering drugs to animals

A

Enteral administration
Parenteral administration
Others

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
53
Q

What is the most common route of drug administration?

A

Enteral administration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
54
Q

Examples of enteral administration are?

A

oral
intrarumenal
rectal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
55
Q

Types of Parenteral administration

A

IV, IM, SC

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
56
Q

Which routes of administration are occasionally used?

A

Intraarterial
Intramedullary
Intracardiac
Intrathecal
Intrathoracic
Subarachnoid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
57
Q

Which routes of administration are common but less frequently used ?

A

Epidural
Intradermal
Intratracheal
IP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
58
Q

Other routes of administration are?

A

inhalation (pulmonary route)
topical (local application)
Oral transmucosal (OTM)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
59
Q

Choice of the route of administration is generally based on
• ________ properties of the drug
• _________ to be used
• __________ indications
• _________ of the disease
• Target _______

A

Physicochemical, Formulation, Therapeutic, Pathophysiology, species

60
Q

The _______ of administration might influence
the _____ and _____ of absorption but should
not influence the _______ or _____.

A

route, rate, extent, distribution, clearance

61
Q

The manufacturer‘s recommendations should ?

A

always be followed carefully.

62
Q

The purpose of drug therapy is to ?

A

induce a desired pharmacologic response

63
Q

For the most drugs the degree of the pharmacologic response is related to the drug _______ at the tissue (______) aka _____ _____.
A drug crosses several _______ _______ ______ from its site of administration to reach its site of action.

A

concentration, receptor, target site, lipoidal membrane barriers

64
Q

The processes that govern the movement of drug across lipid-based biological membranes are
important and regulate its ?

A

absorption, distribution and excretion from the animal.

65
Q

For the most drugs the magnitude of pharmacologic response is ________ related to the drug _________ at the tissue (_______). Since tissue samples cannot be collected easily, drug concentrations at the tissue site are
approximated by measuring “_____ _____ _______” (____)

A

proportionaly, concentration, receptor, plasma drug concentrations, PDCs

66
Q

Determinants of PDC
These movements largely, but not exclusively depend on _______ diffusion of the drug and include:
- Absorption from the site of _______ to _____ circulation
- Distribution of the drug from _____ circulation to ______ and back again
- Metabolism of the drug and its _____ from the body
- Excretion

A

passive, administration, systemic, systemic, tissues, elimination

67
Q

These movements are _____, occurring ______ and their effects determine ___ at any time during the dosing interval after _______ of a fixed dose

A

dynamic, simultaneously, PDC, administration

68
Q

Determinants of Plasma Drug Concentration (PDC)

After parenteral or oral administration, drug should be ______. Once in circulation, if they are not bound to _____ ______ they can be distributed. Elimination occurs by ______ metabolism and _____ or _____ excretion.

A

absorbed, plasma protein, hepatic, renal, biliary

The drug must be first absorbed after a drug administration.
Once in circulation, drug not bound to plasma protein (free
drug) is distributed into tissues, where it can be bound to
tissues or distributed back to circulation.
Elimination of the drug from the body occurs by hepatic
metabolism and renal or biliary excretion of the drug or its
metabolites.

69
Q

Absorption is defined as ?

A

the movement of the drug from the site of administration into the blood.

70
Q

All routes of administration except ____ involve an absorption process. Administrated drugs must cross _____ or _____ membranes before getting into the bloodstream

A

IV, one, more

71
Q

Oral (gastrointestinal absorption)

Main role of GI-tract is _____ and ______ ______. GI-Tract present a important degree of _______ relative to morphology and physiology. This causes a regional variations in drug ______.

A

digestion, nutrient, absorption, heterogeneity, absorption

72
Q

What is the major obstacle of gastrointestinal absorption?

A

The enormous interspecies diversity in comparative gastrointestinal anatomy and physiology. Also, drugs won’t be absorbed in the same way in different regions in the body.

73
Q

Most drugs reach systemic circulation after absorption from the ______ ______ because of the ____ surface area)

A

small intestine, large

74
Q

The rate and extent of drug absorption in the GI tract depend on:

o GI- ___
o Surface _____
o ______
o _______ of drug
o ________ and ________ of the mucosal epithelium
o Intestinal _____ _____

A

pH, area, Motility, Concentration, permeability, thickness, blood flow

75
Q

After GI absorption, drugs enter the _____ _____ and then the ______.

A

portal vein, liver

76
Q

Drugs that undergo first-pass metabolism may not reach _____ _____ in concentrations
sufficiently high to cause a _____.

A

systemic circulation, response

77
Q

In the oral cavity, the is the sublingual area is the route for _______ drugs. Example = ______. You can place ______ _______ or use ______ _______ (?) in the buccal mucosa.

A

systemic, nitroglycerin, polymer patches, feline oral sprays

78
Q

In the _________ and ______ portion of the stomach this part of the GI tract, it will be _____ ______ for drugs to be absorbed due to the _______ epithelium.

A

esophagus, cranial, more difficult, cornified

79
Q

The stomach contains ______ mucosa, which allows for ________. However surface _______ may be a barrier to some drugs. Furthermore, its ______ and ______ creates a ______ environment for drugs and therefore promotes promotes drug absorption _____ the GI tract.

A

simple, absorption, mucus, acidity, motility, hostile, down

80
Q

The SI is the primary site for most drug absorption due to ____ and ______ _____. ____ _____ is much greater here than it is in the stomach and the presence of _______ which increase SA. If there is no ______, then the drug would ____ be easily absorbed.

A

pH, epithelial lining, Blood, flow, microvilli, microvilli, not

81
Q

_______ have a higher permeability to
many drugs than humans.

A

Dogs

82
Q

Epithelial and bacterial biotransformation occurs in the?

This process is also called?

A

Small intestine, presystemic metabolism

83
Q

First pass effect is when drugs travel to the ______.

Second first-pass effect occurs in the ____. Not as important as ?.

A

liver, SI, hepatic metabolism

The epithelial cells of the intestine are endowed with the necessary enzymes for drug metabolism.

84
Q

Third first-pass effect is defined as?

A

Resident microbial population are capable of metabolizing specific drugs. This kind of metabolism are not as important as hepatic metabolism.

85
Q

In order for a drug to be absorbed across the intestinal mucosa, the drug must be first
dissolved in the ?

A

aqueous intestinal fluid

86
Q

List and define the important steps of (oral) gastrointestinal absorption.

A
  1. Disintegration= A solid dosage form (e.g. tablet) physically disperses so that its particles can
    be exposed to the Gastrointestinal fluid (GIF)
    Gastrointestinal fluid = GIF
  2. Dissolution = The drug molecules enter into solution, “pharmaceutical phase”
87
Q

Parenteral route

o Parenteral dosage forms are manufactured under strict guidelines that eliminate ________ and _______ contamination
o Sterile preparations must be administered using ______ techniques
o Dose must be ______
o ________ reactions are a possibility

A

microbial, particulate, aseptic, accurate, Painful

88
Q

Parenteral route

o The primary therapeutic parenteral routes are?
o The barrier to absorption is less than found in oral or topical delivery because ???
o The total drug dose is known and injected into ____ ______ ____. Systemic capillaries drain into the _______ circulation.

A

subcutaneous (SC) and intramuscular (IM), well perfused tissue, venous

89
Q

Parenteral routes bypass all of the body‘s ______ ______. If you are giving drugs orally, must go through ?

A

defensive mechanisms, stomach, SI, etc.

90
Q

SC and IM administration:
o Moderately irritating preparations can be injected _________ , but _____ reaction and
______ may become evident with time so must be careful when deciding.
o Duration of drug action for IM is ______ than IV but most often slightly ______ than SC administration
o Usually the rate of absorption from SC administration is _______ ______ than from IM sites

A

intramuscularly, tissue, necrosis, longer, shorter, slightly slower

91
Q

Parenteral route
Intraperitoneal (IP) administration
o The peritoneal absorption is very _______
o ____ injection is often used in toxicology in rodents
o _____ volumes can be administered
o There is a good “mixing” of the injection with the ______ _____
o The majority of drug absorbed after IP administration enters the ______ ____ and undergoes _____-pass hepatic metabolism

A

efficient, IP, Large, peritoneal fluid, portal vein, first

92
Q

Parenteral route
Intravenous administration (IV)
o It does not involve an ______ ______
o Immediately _____ blood levels and _____ _____ of action
o Drugs are administered directly into a ____ usually through IV catheter
o _______ fluid volume can be injected
o ______ solutions are preferable
o ________ and ______ solutions can be injected if done slowly and carefully

A

absorption process, high, rapid onset, vein, Large, Aqueous, Irritating, nonisotonic

93
Q

Inhalation (pulmonary route)
_______, _____ agents and _____ particles usually are rapidly absorbed from the ______ and _____ into the _________ circulation

A

Gases, volatiles, fine, airways, alveoli, pulmonary

94
Q

Particles less than 2 μm (produced by nebulization) are inspired into the ______ ____ and ____

A

terminal ducts, alveoli

95
Q

Particles less than ___ μm may reach the respiratory bronchioles.

A

5

96
Q

Particles 5 to 10 μm in size may reach the ______ respiratory tract and _____ airways

A

5, 10, upper, larger

97
Q

Inhalation (pulmonary route)
• Response is _____ because of the large _____ _____ of the lungs and large ____ ____ to the lungs.
• Cells lining the alveoli are very _____ and profusely bathed by _______.
• Compounds absorbed in the lung will enter the oxygenated _______ _____ that drain to the systemic arterial circulation
• Used for ______ ______ e. g. Isoflurane

A

rapid, surface area, blood flow, thin, capillaries, pulmonary veins, gas anesthesics

98
Q

Topical administration
o Drugs can be applied topically to the ______ and its ______
o Drugs can be applied to a variety of ________ _______

A

skin, adnexa, mucous membranes

99
Q

Topical administration routes:
Used routes?

A
  • Sublingual
  • Intravaginal
  • Intranasal
  • Intrauterine
  • Rectal
  • Preputial
  • Ocular
  • Aural (otic)

The achievement of effective systemic concentrations
are offen not required for what is an essentially local
therapeutic effect

100
Q

Oral trans-mucosal (OTM) or buccal drug administration
o Drugs are given by mouth with the intent of absorption occurring through the _______ of the mouth
o The major advantage is to avoid the _____-pass metabolism and bypass the ______ ____ environment

A

mucosa, first, harsh GI

101
Q

Bioavailability (F) is defined as the ________ of an administered dose of drug that reaches _____ ______

A

percentage, systemic circulation

102
Q

The bioavalability is determined only by comparing _____ levels of a drug after a particular route of administration with the levels achieved by ____ administration. Why?

A

plasma, IV, B/c when you use IV admin, 100% of drug reaches systemic circulation. This is the only route.

103
Q

F of an IV dose = ?

A

100% or 1

104
Q

All other routes of administration
will have an F =?

A

less than 1

105
Q

If 100 mg of a drug is administered orally and 70 mg is absorbed unchanged, the bioavailability is = ?

A

0.7 or 70%

106
Q

What is the bioavailability formula?

A

The amount of drug collected after administration by the route under study is divided by that
collected after IV administration
o When drug concentrations in blood are assayed, total absorption is determined by measuring
the area under the (concentration-time) curve (AUC)

Every time you want bioavailbility, you need to use this formula.

107
Q
A
108
Q

The greater the bioavailability or extent of absorption of a drug, the greater the ?

A

anticipated pharmacologic response

109
Q

Bioavailability is used to predict drug _______ after different routes of administration. If you have a good bioavailability, most of drug will reach ______ _______.

A

efficacy, systemic circulation

110
Q

Once a drug reaches the systemic circulation following any route of administration, it must be distributed from the _______ compartment to ________ tissues. This compartment is the ______.

A

central, peripheral, blood

111
Q

There are numerous tissues to which a drug may be distributed
• In some cases, drugs may be stored in ______ and ______ released back into the _____ circulation (low blood flow/mass ratio)
• If the animal is a food-producing species, such tissue storage may result in ______ in the edible meat products.

A

tissues, slowly, systemic, residues

112
Q

What are the major factors that determine drug distribution to and from tissues?

A
  1. Drug lipid solubility and its ability to penetrate cell membranes
  2. Regional blood flow (flow/mass ratio)
  3. Concentration gradient established between the blood and tissue
  4. The degree to which the drug is bound to plasma or tissue proteins
  5. The presence of transport proteins
113
Q

Which tissues have a high blood flow/mass ratio?

A

Brain, heart, liver, kidney, endocrine glands

114
Q

Which tissues have an intermediate blood flow/mass ratio?

A

Muscle, skin

115
Q

Which tissues have a low blood flow/mass ratio?

A

Adipose tissue, bone

116
Q

In the kidney, the renal cortex receives ____% of cardiac output. The renal medulla receives a _____ ______ of this blood flow.

A

25, small fraction.

117
Q

Following entry into the circulatory system a drug is distributed in association with _____ _____
• ____ _____ cells may also be responsible for transport of drugs but occurs seldom
• The transport of compounds by ____ is less important.

A

plasma proteins, Red blood, lymph

118
Q

The binding of lipid-soluble drugs to _____ _____ facilitates their circulation.

Weakly acidic drugs tend to bind to _______.

Weakly basic drugs tend to bind to ___________.

A

plasma proteins, albumin, alpha1-glycoprotein.

119
Q

There is a _______ (______) binding with most of therapeutic drugs. Why?
• A molecule bound to a plasma protein moves throughout the circulation until it ______
• ________ occurs when the _____ for another tissue component is ________ than that for the plasma protein.

A

reversible, noncovalent, B/c you want the drug to be dropped off at its target tissue.

dissociates, Dissociation, affinity, greater

120
Q
  1. The plasma protein binding can affect the _____ ______ since only the ______ drug is able to
    cross cell membranes. Why?
  2. What is the effect of plasma protein binding on a drug?
  3. The protein binding limits ______ _____. It slows the rates of _______
    and/or ______. Why?
A
  1. drug distribution, free, B/c binding to plasma protein allows them to travel through systemic circulation and reach target tissues. Once reach target tissues they must dissociate.
  2. Binding does not prevent a drug from reaching its site of action but slows it down.
    Effect on the response to a drug
  3. glomerular filtration, metabolism, secretion, Drugs can be filtered out if not bound to plasma protein.
121
Q

Protein binding are expressed in terms of ?

A

Percent of drug bound.

122
Q

What happens when a compound has a high affinity for a protein?

A

The percent of drug bound falls when the drug concentration exceeds the value that saturates the binding site.

123
Q

Binding capacity negatively affects?

A

Distribution of drug

124
Q

Competition for the same site on plasma proteins may have important consequences
specially when?

A

One of the potential ligands has a very high affinity

125
Q

If drug A were bound 98% and 10% of it is displaced by drug B, what is the amount of free drug A?

A

The amount of free drug A increases from 2% to 12%

126
Q

If Drug A were bound 30 % and 10% displaced by drug B, the result is ?

A

the amount of free drug A increases from 70% to 73%

127
Q

Define distribution equilibrium (DE)

A

DE, or steady-state, is defined as the amount of drug leaving plasma for tissues is equivalent to the
amount of drug leaving tissues for plasma.

128
Q

DE may not ever be achieved because ?

A

a drug is continually being eliminated. This is called pseudoequillibrium.

129
Q

DE is less likely to be achieved for drugs with a _____ ____-____, particularly when administered at a _____ dosing interval.

A

short half-life, long

130
Q

Drugs that accumulate (given at a dosing interval that is shorter than the half-life) are ______ likely to reach the a state of equilibrium between doses.

A

more

131
Q

Some organs have unique anatomic barriers to drug penetration. What is the most classic example? Explain.

A

Blood-brain barrier (BBB) This barrier has a glial cell layer interposed between the capillary endothelium and the nervous tissue. Only nonionized lipid-soluble compounds can penetrate this barrier. Similar considerations apply to ocular, prostatic, testicular, synovial, mammary gland and placental drug distribution.

132
Q

A few tissues possess selective transport mechanisms that accumulate specific chemicals ______ concentration gradients.

For example the blood-brain barrier has _____, -___ _____, and _______ ______. The blood-brain barrier also possesses drug efflux transport mechanisms that ________ drug from the ______ sites

A

against, glucose, L-amino acid, transferrin transporters, remove, protected

133
Q

Describe the MDR1 mutation in collies.

What is this disease characterized by?

A

The mutation causes a non-functional MDR1 protein at the blood brain barrier, which causes the passage of drugs into the CNS.

Neurotoxicity to ivermectin in MDR1 defect is characterized by: Depression, Ataxia, Somnolence, Salivation, Tremor, Coma, Death

134
Q

Depending on the ____ and the mechanism of _____, drugs that are MDR1 substrates can cause severe _______ leading to ____

A

dosis, action, depression, death

135
Q

In Ivermectin Sensitive Collies, there is a _______ of 4 nucleotides –> ?

Big difference is the size between the intact MDR1 and defective MDR1. The defective MDR1 is _____ in size.

A

deletion, premature stop-codon, 91 AS

136
Q

Define the volume of drug distribution

A

Vd is the volume to which a drug would have to be distributed if it were throughout the body in the same concentration as that measured in the plasma after IV administration of a known dose.

137
Q

Using the Vd formula, solve the following

Adding 5 g (5000 mg) of dextrose (considered the dose) to each of two beakers (A and B) containing a different and unknown volume of water. The dextrose is allowed to distribute equally throughout the beaker.

• If the concentration of beaker A is 5% ( 50 mg/mL), then the volume of water in the beaker
must be ?

• If the concentration of beaker B is 2.5% (25 mg/mL), then the volume of water in the beaker
is ?

A

100 mL ( Vd = 100 mL) , 200 mL

138
Q

Vd differences among species and ages can dramatically affect ?

A

PDC

139
Q

Diseases associated with ____ _____ or ____ are likely to increase the Vd of many drugs (and thus _______ PDC).

A

fluid retention, obesity, decrease

140
Q

______ or _____ _____ is likely to decrease Vd and thus increase PDC

A

Dehydration, weight loss

141
Q

The size of the apparent Vd may indicate the ____ _____ to which the drug is distributed

A

body compartment

142
Q

Any factor that increases Vd will tend to _____ PDC but prolong the ______ half-life and thus the ______ of drug in the body.

A

decrease, elimination, presence

143
Q

Drug redistribution is relevant only for drugs for ?

A

which an immediate effect can be realized (i.e., general anesthetics)

144
Q

Drugs showing the redistribution phenomenon are ?

A

highly lipid soluble

145
Q

The phenomenon of redistribution involves the rapid distribution of drugs to a ____-blood-flow organs such as the ____ followed by rapid ________ to _____ tissues and then to _____ tissues

A

high, brain, redistribution, lean, fatty

146
Q

___________ and _________ undergo a phenomenon of redistribution.

A

Thiobarbituates, propofol

147
Q

After a rapid IV bolus of thiobarbituates and propofol, these drugs distribute first into a ______ _______ _____ and ______ blood-flow organs. The drug effect rapidly terminates, primarily because?

Which animals tend to have prolonged recovery?

A

central blood pool, high,

of redistribution from the brain to lean tissues, such as muscle and continued redistribution to fatty tissues.

Hounds/animals that lack body fat.

Intro to Pharmacology (31 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions