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Pharmacology (PHA 3112 B) > Pharmacokinetics + Pharmacodynamics > Flashcards

Pharmacokinetics + Pharmacodynamics Flashcards

Midterm 1 Review

1
Q

What is pharmacology?

A

Science of the fate of drugs in the body and their biological actions within the body.

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2
Q

Primary drug action

A

Therapeutic effect
-Usually intended to be beneficial

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3
Q

Secondary drug action

A

Side effects
-can be desirable, undesirable, or neutrla
-If unwanted side effects occur; usually called adverse reactions

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4
Q

Who regulates drugs?

A

The Food and Drugs Act (FDA)

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5
Q

Branches of the FDA

A

Natural health products
Biological
Pharmaceutical
Food
^(Above 3 are all under the Food and Drug Regulations)
Cosmetics
Devices

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6
Q

3 main uses for drugs?

A
  1. the Dx, Tx and prevention or diseases or it’s Sx’s
    2.Restoring/correcting organic functions
    3.Disinfection in places where food is
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7
Q

What kind of effect do drugs give?

A

Local or systemic

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8
Q

Device

A

Aimed at the functioning of a body part

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9
Q

What is considered to be a drug?

A

Pharmaceutical, biologics (biologically-derived products), disinfectants, natural health products

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10
Q

Pharmaceuticals can be either…?

A

Prescription or non-prescription

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11
Q

Biologics come from…?

A

Living organisms or their cells
-Often made using biotechnology

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12
Q

Biologics include…

A

-Blood and blood products
-Viral +bacterial vaccines
-Cells, tissues, organs
-Antibodies
-Gene therapies

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13
Q

What are biologics used for?

A

To treat disease and medical conditions like;
-Anemia
-Diabetes
-Psoriasis
-Rheumatoid arthritis
-Inflammatory bowel disease (IBD)
-Hormone deficiency
-Some forms of cancer

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14
Q

Natural health products include…

A

Vitamin and mineral supplements
-Therapeutic claims made

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15
Q

Pharmacology started out as…

A

Potions, elixers, herbal remedies and evolved through centuries of trial and error

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16
Q

Botanists

A

Screen natural materials

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17
Q

Chemists

A

Extract and purify these natural materials (ex. morphine from opium) so that the active ingredient could be synthesized

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18
Q

Sources of drugs

A

1.Natural preparations (Ex. Opium)
2.Purified components (Ex. Morphine)
3.Derivatives of natural products (Ex. Heroin)
4.Totally synthesized compounds (Ex. Fentanyl)

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19
Q

3 main drug nomenclatures

A
  1. Chemical name (Ex. Ortho-acetoxybenzoic acid)
  2. Generic name (international nonproprietary name) (INN) (Ex. Acetyl salicylic acid - ASA)
  3. Brand/Trade name (Ex. Aspirin)
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20
Q

Innovator Drugs

A

Also = Brand name drug
-Patent protected for 20 years, once expired any other pharmaceutical company can market the drug without the same brand name

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21
Q

Generic drug (not to be confused with generic name)

A

Also called subsequent entry drug
-Contains the same active ingredients as the original brand name drug approved for sale
-Often sold under a name that incorporates the generic name (often with an added prefix representing the company)

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22
Q

For biological products, generic drugs (subsequent entry drugs) are also called…?

A

-Biosimilar products

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23
Q

Does everything we eat flow through the liver? T/F?

A

True

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24
Q

The Liver can’t tell the difference between good and bad chemicals so it will breakdown it all (sometimes inactivating medications we take) T/F?

A

True

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25
Q

What happens when a drug enters the body? (Acetaminophen tablet PO)

A

1.Once the drug goes into solution it is absorbed from the digestive tract into systemic circulation
2.Reversible binding to plasma proteins and circulation/distribution in the body
3.Most drugs bind to specific receptors
4.Transformation/metabolism (by liver)
5.Kidney’s, lungs, intestines can eliminate drug
^The above process influences the speed of onset and duration of drug effects

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26
Q

Metabolites

A

Substance produced when the body (likely the liver) breaks down a drug
-Can be Active or Inactive

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27
Q

What does Albumin (the mist abundant plasma protein in the body) do?

A

Helps fluid from leaking out of your blood vessels (capillaries) into other tissues

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28
Q
A
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29
Q

Where is bile released into?

A

The duodenum

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30
Q

How do most drugs work?

A

By binding to receptors

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31
Q

Drugs are absorbed through which intake routes…?

A

Oral intake, inhalation, injection

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32
Q

Distribution of drugs takes place in the…?

A

Blood vessels (circulation) attach receptors

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33
Q

Drug transformation happens where?

A

the liver is the site of biotransformation (some other sites not listed)

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34
Q

Elimination of drugs happens by which routes?

A

feces, exhalation, urine, sweat, saliva

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35
Q

Pharmacokinetics

A

Study of factors determining the concentration of a drug at the receptor site, as a function of time and dose administered
ADME (absorption, distribution, metabolism, excretion)

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36
Q

Pharmacodynamics

A

Study of the biochemical and physiological mechanisms by which drugs produce their effects (Includes mechanism of action)

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37
Q

Pharmacokinetics vs. pharmacodynamics

A

Pharmacokinetics: What the body does to the drug
Pharmacodynamics: What the drug does to the body

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38
Q

A-Absorption Routes of administration

A

IV
IM
SC
PO
PR
IA
SL (Sublingual - under the tongue)
Inhalation
Topical
Transdermal
Vaginal
Opthalmic

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39
Q

Intravascular vs. extravascular

A

Intravascular doesn’t require any absorption
Extravascular route requires absorption

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40
Q

Intravascular routes

A

Intravenous
Intra-arterial

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41
Q

Extravascular routes

A

Oral, rectal, IM, SC

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42
Q

Transdermal route means?

A

In the nose (Ex. Spray)

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43
Q

Inhalation meaning?

A

Being pushed right into the lungs, not the nose, (Ex. Inhaler)

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44
Q

Enteral (gastrointestinal) routes of administration

A

-Under the tongue (PO, SL - don’t swallow)
-Pr

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45
Q

Parenteral (Injection) routes of administration

A

SC
IM
IV
IA

46
Q

A.C

A

Before meals

47
Q

ad lib.

A

As much as desired; freely (rarely used for meds. mainly for food - different than prn)

48
Q

B.I.D

A

Twice a day

49
Q

H.S, QHS

A

H.S= At bedtime
QHS= Every bedtime

50
Q

P.C

A

After meals

51
Q

P.V

A

Vaginally

52
Q

q

A

Every; per

53
Q

q.d

A

Every day

54
Q

q.i.d

A

4 times a day

55
Q

t.i.d

A

Three times a day

56
Q

Applying drugs on a surface - Topical administration

A

-Direct application to where it must act
Ex. skin creams, ointments, nasal sprays (inhalation is different), vaginal applications, eye drops

57
Q

Simplest mode of administration=

A

Topical

58
Q

Ointment vs. cream

A

Ointment is more oily (ex. vaseline, polysporne)
-Still glistens on the skin after rubbed in
-Stays on the surface of the skin mainly - that’s what you want an ointment for
Cream is when you rub it in and it disappears (sinks into the skin)

59
Q

Applying drugs on a surface - Transdermal administration

A

-Is a patch you put on your skin
-Gradual absorption through intact skin; variable absorption (proportional to lipid solubility, blood flow)
-Often can be a route for poisoning (ex. insecticides)
-Ex. Hormone treatment, nicotine, fentanyl, nitroglycerin

60
Q

Administration by inhalation

A

-Rapid access to general circulation via the lungs
-Ex. anesthesia for surgery, bronchodilators for asthma (salbutamol)

61
Q

Perfusion

A

-When you give the med. drop by drop

62
Q

Enteral (gastrointestinal) - Oral P.O

A

-Most common route of administration
-Exposure to intestinal and liver metabolism before gaining access to systemic circulation
-Absorbed like nutrients and travel through the liver before gaining access to systemic circulation

63
Q

Oral - Tablets/capsules

A

-Active ingredient + excipients (Inactive ingredients) (ex. starch, color, preservatives, coating)
-Take with sufficient liquid (100mL)
-Some should not be split or crushed (enteric-coated, slow/extended release, gelatin capsules)

64
Q

Why are some pills coated?

A

To protect the stomach from the pill or to protect the pill from the acid of the stomach

65
Q

Woul a drug that is highly destroyed by the liver be taken by mouth (P.O)?

A

No. (Ex. nitroglycerin never taken P.O, taken s.l instead)

66
Q

Oral - Liquids (3 types)

A

Emulsions: mix of water/oil
Suspensions: Insoluble matter in water, mix well before dispensing (ex. sand in water)
Tincture/elixir: Alcohol-based (used to extract active components from plants)

67
Q

Hepatic portal system route taken

A
  1. Small intestine absorbs products of digestion
    2.Nutrient molecules travel in hepatic portal vein to liver
    3.Liver monitors blood content
    4.Blood enters general circulaton by way of hepatic vein
68
Q

How the sublingual route works

A

Gets drained from under the tongue by veins in the neck to the superior vena cava (of the heart) good for pills that act directly on the heart

69
Q

Veins into and back out of the liver

A

Hepatic portal vein into the liver and hepatic vein out of the liver

70
Q

Enteral (gastrointestinal) routes of administration - Sublingual

A

-Absorption through the oral mucosa
-The point of it is to avoid the liver
-Bypasses first-pass liver metabolism
Ex. nitroglycerin used for the Tx of angina

71
Q

Bucco-gingival

A

-Drug dissolves between gums and cheek

72
Q

Enteral routes of administration - Rectal (p.r)

A

-Useful in cases of nausea, vomiting or local issues
Ex. anti-inflammatory drugs for hemorrhoids

73
Q

First pass metabolism

A

Enzymatic activity that can transform a drug in the way IN
Ex. can have elevated first pass metabolism
-Can be first pass liver, intestinal, pulmonary, hepatic metabolism

74
Q

I.v injection, common example

A

Adrenaline/epinephrine (same thing)

75
Q

I.m injection, common example

A

Diazepam

76
Q

S.c injection, example

A

Insulin

77
Q

Intravenous administration

A

-Most direct route
-Requires extra vigilance (esp. in 1st hour after administration)

78
Q

Why is the intravenous route risky?

A

-High concentrations = increased risk of toxicity
-Risk of injection site infection
-Phlebitis: Caused by hypertonic solution or direct effect of drug
-Accidental extravascular administration (go through the blood vessel to the other side into surrounding tissue)
-Air embolism

79
Q

Intra-arterial perfusion

A

-Used for some chemotherapeutics
-Lysis of blood clots

80
Q

Parenteral administration via central venous catheter (PICC line)

A

Point is to get access to major blood supply carries

81
Q

Intraosseous administration

A

The bone marrow cavity (ex. tibia, humerus, sternum) is used as a non-collapsible vascular entry point
-Used in resuscitation of critically ill adult patients if rapid and timely peripheral intravenous cannot be established or has failed

82
Q

Possible complications of intraosseus administration?

A

Extravasation, infection and fracture

83
Q

What is concentration the relationship of?

A

Concentration is the relationship between quantity and volume

84
Q

Therapeutic range

A

Anywhere above the threshold
-Where you feel the effects

85
Q

Why does drug concentration in the blood drop?

A

Because of metabolism

86
Q

T-max

A

The time required for the drug to get to the maximum concentration in the blood

87
Q

Threshold

A

The onset of action can begin to occur at the threshold (lowest amount of the drug in the blood to feel effects start)

88
Q

Phlebitis

A

Inflammation of a vein near the skin of the surface

89
Q

4 principles of bioavailability

A

Absorption - bioavailability
Distribution - volume of distribution
Metabolism - Half-life
Elimination - Clearance

90
Q

Bioavailability F =

A

The fraction of unchanged drug (unmodified and still active) that reaches the systemic circulation

91
Q

What is ideal bioavailability?

A

100% (no losses between site of administration and systemic circulation)

92
Q

F < 100% can mean…?

A

-Some of the drug is lost before reaching the heart
-Lost before intestinal absorption (ex. diarrhea)
-Lost by modification of the drug by intestinal or hepatic metabolism (enzymes)
-Lost because transporters return the drug to the gastrointestinal tract (into bile, small intestines)

93
Q

Systemic circulation means?

A

The blood that’s leaving the heart to fill the body

94
Q

If a drug has an elevated first pass metabolism, does it have increased or decreased bioavailability?

A

Decreased because (ex. 90% destroyed by the liver, 10% not) then drug has been changed a lot and not much left to distribute

95
Q

Is bioavailability on the way in or out?

A

IN!!!!!!!!!!!!!

96
Q

Oral availability is 50% compared to IV route T/F?

A

True

97
Q

How is bioavailability calculated?

A

AUC Proportional dose x F/clearance
-By comparing the amount of drug absorbed over time from the route of administration of interest to the amount of drug absorbed over time when the same dose is given by intravenous route

98
Q

AUC (Area under the curve) is directly proportional to the clearance of the drug T/F?

A

False

99
Q

The larger the dose of the drug the smaller the area under the curve T/F?

A

False

100
Q

If clearance is high, drug concentration will be lower in the body T/F?

A

True, because high clearance means normally functioning kidney’s and liver so drug concentrations in the body will be lower because the drug is eliminated by the kidney’s and liver doing it’s job)
-Reverse if kidney’s/liver are damaged

101
Q

If the AUC is larger, then bioavailability is less T/F?

A

False

102
Q

If rate of gastric emptying is slow then bioavailability is increased tTF?

A

False. If rate of gastric emptying is slow then bioavailability is reduced (ex. reduced absorption surface, destruction by low pH/gastric enzymes)

103
Q

If rate of intestinal emptying (or intestinal motility) is low (statsis), bioavailability can’t be increased anymore since it’s at maximum T/F?

A

True

104
Q

If rate of intestinal emptying is high (ex. diarrhea), bioavailability will be increased T/F?

A

False

105
Q

Will there be increased absorption if the intestinal surface is reduced due to inflammation or surgical ressection?

A

No. The reverse is true. There will be decreased absorption in that case.

106
Q

Can hepatic metabolism be increased or decreased?

A

-Yes it can be increased by inducers of enzymatic activity.
-It can be decreased by educers such as in cases of decreased hepatic function due to severe liver disease or effects of chemicals that inhibit hepatic metabolism
-Ex. Nitroglycerin would be heavily impacted by changes in hepatic metabolism because it’s highly metabolized by the liver

107
Q

The nutrient and caloric content, volume and temperature of the meal can all affect what?

A

Factors that affect a drug’s ability to be able to disssolve, it’s permeability (ability to cross the cell membranes) and speed of travel (transit) in the GI system are all affected
-Ex. Large volumes of liquids tend to distend the stomach and accelerate gastric emptying, whereas high-calories, high-fat meals are more likely to slow gastric emptying
-ALL OF THESE FACTORS CAN AFFECT THE BIOAVAILABILITY OF A DRUG ADMINISTERED VIA THE ORAL ROUTE

108
Q

When things hang around in the stomach is bioavailability increased or decreased?

A

Decreased

109
Q

The larger the surface area - the more layers/chances of absorption (ex. liver has less then intestines) T/F?

A

True

110
Q
A

Pharmacology (PHA 3112 B) (1 decks)

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