Fundamentals of Pharmacology (Pharmocodynamics/kinetics) (LO1) Flashcards

1
Q

Pharmacokinetics

A

what the body does to the drug

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2
Q

ADME

A

determine how and how much of a drug arrives at its target body tissues and how long it exerts its therapeutic effect

(A) Absorption
(D) Distribution
(M) Metabolism
(E) Excretion

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3
Q

Absorption

A

refers to the transfer of medication from its site of administration into the body to specific target organs and tissues

The  rate of absorption  determines the  onset  of action

The extent of absorption  determines the  intensity  of action

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4
Q

factors affecting the absorption of a medication including

A

Solubility of the drug

Concentration of the drug

pH of the body

Site of absorption

Absorbing surface area

Blood supply to absorption site

Medication’s bioavailability (the amount of medication that is still active once it reaches it’s target tissue)

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5
Q

Distribution

A

As a drug passes through the body, its form and its concentration in the tissues influences the effect it will have

Plasma protein binding is an important mechanism of distribution

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6
Q

bound drug

free drug

A

bound drug: Plasma protein binding is an important mechanism of distribution.

Drugs are bound in variable degrees to proteins or become stored in fatty tissues

free drug: Only those drug particles that are not bound can be active in the cells

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7
Q

metabolism (biotransformation)

A

changes a drug into forms that can be used by the body or which can be readily excreted (or both)

Metabolism occurs immediately and most often in the liver.

first pass effect: the liver inactivates some medications and some can only be given parenterally

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8
Q

Excretion

A

A drug and its metabolites must be excreted

If a drug is excreted more slowly than it is administered, accumulation occurs causing adverse effects and toxicity.

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9
Q

Drug Half-Life

A

represents the time required for the amount of the drug in the blood serum to diminish by one-half

the concentration (M) of a drug in the blood during a period of time after administration of a single dose

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10
Q

The  minimum effective concentration (MEC) or therapeutic index

A

is a term indicating the lowest concentration of drug in the blood able to produce a therapeutic effect

useful in determining adequate dosages

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11
Q

The therapeutic range describes

A

the range between MEC and the toxic concentration where the drug can seriously harm the client

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12
Q

Onset of Action

A

is the time after administration when the drug reaches the MEC and begins to produce its effects

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13
Q

Principles Related to Onset of Action

A

Route of administration

sometimes a loading or priming dose is given to achieve the MEC quickly

Some drugs have a latency period

peak effect  occurs when blood level is highest

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14
Q

The duration of action

The termination of action

A

–The duration of action–
is usually defined as how long the medication can be expected to remain above the minimum level to provide the effects

it is the time the blood level is above the MEC

-The termination of action-
the amount of time after the concentration level falls below the minimum level to the time it is eliminated from the body

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15
Q

Duration of action of :

  • fentanyl (Sublimaze®),
  • meperidine (Demerol®),
  • morphine,
  • acetaminophen (Tylenol®),
A

fentanyl (Sublimaze®), 1–2 hours

meperidine (Demerol®), 2–4 hours

morphine, 3-7 hours

acetaminophen (Tylenol®), 4–6 hours

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16
Q

Principles Related to Duration of Action

A

Short acting drugs must be given frequently.

Duration of action can be maintained by giving drugs at regular intervals (maintaining the blood level).

Duration can be used to help predict the time of next dose.

Occasionally a drug’s effects may persist even after it has been excreted.

Duration is influenced by pharmacokinetics and can vary with different routes of administration.

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17
Q

Sites of Elimination

A

Kidneys (main site of elimination)

GI tract

Perspiration

Respiration

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18
Q

Pharmacodynamics

A

what the drug does to the body

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19
Q

Drugs either alter the ——- —- or change the —— — — — —-

A

Drugs either alter the cell environment or change the rate of cell functions

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20
Q

the receptor theory of drug action

A

Drugs “attach” to cells because their molecular structure matches

All cell receptors will be exposed to the drug circulating in the blood stream but only those that fit (visualize a lock and key) will bind to each other

If many receptors are available, we can increase the drug dosage and thus drug effect.

If few receptors are available, increasing the drug dosage will have no effect.

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21
Q

the cell is said to be receptive to the drug if…

A

If at least three sites on the surfaces of both drug and cell match

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22
Q

what are receptors usually made of

A

cellular proteins or nucleic acids but can be enzymes, carbohydrate residues, and lipids

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23
Q

Agonist

A

a drug that directly alters the rate of a cellular process

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24
Q

Affinity for the target tissue

A

An agonist has a natural tendency to bind with the receptor

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25
Q

Efficacy

A

ability to initiate drug action

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26
Q

Partial agonists 

A

are agonists that produce only moderate effect.

They occupy a receptor site and produce moderate effect

prevent any other drug from binding to those receptor sites.

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27
Q

Antagonists

A

do not alter cellular rates or environments. 

they compete with agonists to occupy the same receptor site

If successful in binding more tightly, the antagonist will prevent the agonist from acting

Antagonists are often given to act as antidotes

excreted more rapidly than the agonist they oppose, therefore have short-lived actions and must be administered repeatedly to prevent toxicity from recurring

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28
Q

Numerous factors affect an individual’s response to drugs, including:

A
Age 
Weight 
Gender 
Environment 
Time of administration 
Condition of the patient 
Genetic factors 
Psychologic factors
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29
Q

Types of Responses

A

predictable

unpredictable

iatrogenic

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30
Q

Predictable response

A

extensive research to determine the therapeutic action (desired effect) of a drug

in order for a response to be classed as predictable it must have occurred in 50% of the population

going to be some potential negative results that may occur (side effects)

Through research and testing, most side effects can be anticipated

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31
Q

Unpredictable response

A

If the response seen is unique to that patient and not seen in other patients in a similar setting, the response is classed as an  idiosyncrasy

When medications are given in successive doses or in conjunction with other medications, we can see unpredictable responses as well

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32
Q

 idiosyncrasy

A

an abnormal or unusual response to a drug

33
Q

Tolerance

A

decreased effects of a drug due to long term use

These patients will build a tolerance to that medication resulting in the need for a higher than normal dose to achieve the same result

34
Q

Cross-tolerance

A

drug tolerance in which patients who takes a medication for an extended period of time can build up a tolerance to other medications in the same class

35
Q

Tachyphlaxis

A

condition where patient rapidly becomes tolerant to a medication

36
Q

Drug dependence

A

a physical or emotional need for drug

37
Q

Cumulative effect

A

occurs when several does of a medication are administered or when absorption occurs more quickly than elimination

If repeat doses are given too quickly, a cumulative effect may result, causing possible nontherapeutic effects

38
Q

Summative effect

A

the process where multiple medications can produce a response that the individual medications alone do not produce

If two medications of similar effect are given to a patient

39
Q

Synergism

A

combined action of two drugs that is greater than the sum of their individual responses

40
Q

Potentiation

A

enhanced action of the drug by another administered concurrently

41
Q

Iatrogenic response

A

is an adverse condition that is inadvertently induced in a patient by the treatment given

An example of this would be a patient developing an urinary tract infection after the insertion of urinary catheter.

42
Q

in the metabolic phase The liver can act on a drug in 2 phases

A

Phase1: the enzymes may oxidize the drug or bind it with oxygen molecules and can also hydrolyze the medication; both causes medication to be more soluble with water

Phase 2: the medication molecules combine with a chemical found in the body (known as conjugation reaction)

43
Q

excretion occurs primarily through the kidneys 3 mechanisms

A

Glomelur filtration
Tubular secretion
Partial reabsorption

44
Q

Glomelur filtration

A

a passive process in which blood flows through the glomeruli of the kidneys

a differential in pressure forces waste away from the blood into the capsule where it is transported for excretion

45
Q

Tubular secretion

A

an active transport process in which medications are bound to specific transporters aiding in their elimination

46
Q

Partial reabsorption

A

this occurs when some amount of the drug is reabsorbed after being filtered

47
Q

Medications cause their action on the body by four mechanisms:

A

They may bind to a receptor site

They may change physical properties of cells

They may chemically combine with other chemicals

They may alter a normal metabolic pathway

48
Q

A medication molecule witll have 1 of 2 effects when it binds to a receptor site

A

It may stimulate the receptor site to cause the response it normally does (agonist)

It may block the receptor site from being stimulated by other chemical mediators and inhibit the normal response (antagonist)

49
Q

The autonomic nervous system

A

is composed of nerve fibers that send impulses from the CNS to smooth muscles, cardiac muscles, and glands

50
Q

The autonomic nervous system (ANS) consists of two further subdivisions:

A

Parasympathetic  nervous system

Sympathetic  nervous system

51
Q

Nerve fibers associated with the parasympathetic system originate

A

from the spinal cord at the level of the cervical and sacral regions

52
Q

Parasympathetic nervous system is responsible for actions such as:

A

Decreased heart rate

Decreased cardiac contractile force

Decreased blood pressure

Increased circulation to digestive organs

Increased peristalsis

Constriction of the pupils

Bronchoconstriction

53
Q

The principle neurotransmitter of the parasympathetic nervous system is

A

acetylcholine

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54
Q

acetylcholine

A

Acetylcholine is very short lived.

within seconds of release it is deactivated by another chemical called acetylcholinesterase

55
Q

Within the parasympathetic nervous system there are two main types of acetylcholine receptors

A

nicotinic and muscarinic

56
Q

Muscarinic receptors

A

are primarily responsible for parasympathetic overactivity responses

57
Q

Muscarinic responses and what reverses them

A

including bradycardia, miosis (pinpoint pupils), sweating, blurred vision, tearing, wheezing, SOB, coughing, vomiting, abdominal cramps, diarrhea

atropine reverses them

58
Q

nicotinic receptors

A

are primarily responsible for sympathetic overactivity response and neuromuscular disfunction

causes muscular contractions

opened by nicotine

59
Q

nicotinic responses

A

responses include tachycardia, hypertension, dilated pupils, muscle fasciculation (involuntary twitching etc) and muscle weakness

60
Q

cholinergic receptors

A

these receptors respond to acetylcholine

nicotinic and muscarinic

61
Q

parasympathomimetic  or cholinergic agonists

A

producing effects that resemble (mimic) the stimulation of the parasympathetic nervous system

If a medication binds to and stimulates those receptors

62
Q

parasympatholytic  or anticholinergic

A

blocking effects or producing effects that resemble interruption of the parasympathetic nervous system

If a medication blocks the actions of the parasympathetic nervous system

ex: atropine

63
Q

Nerve fibers associated with the sympathetic system originate

A

from the spinal cord at the level of the thoracic and lumbar regions

64
Q

Sympathetic nervous system is responsible for actions such as:

A

Increase heart rate

Increase blood pressure

Peripheral vasoconstriction

Increase circulation to vital organs

Sweat gland stimulation

65
Q

The principle neurotransmitters of the sympathetic nervous system are

A

catecholamines
 norepinephrine 
epinephrine

66
Q

Within the sympathetic nervous system there are two main types of receptors

A

adrenergic  and  dopaminergic.

67
Q

Dopaminergic receptors

A

are believed to cause renal, coronary, and cerebral artery dilation

68
Q

Adrenergic receptors

A

are the receptors that are most common within the sympathetic nervous system

the receptors stimulated by prehospital medications

69
Q

Adrenergic receptors 4 classes

A

Alpha1
Alpha2
Beta1
Beta2

70
Q

where are the following receptors primarily located

Alpha 1
Alpha 2
Beta 1
Beta 2

A

Alpha 1: on peripheral blood vessels

Alpha 2: on nerve endings

Beta 1: within the cardiovascular system

Beta 2: on bronchial smooth muscle

71
Q

Alpha 1 stimulation results in:

A

Peripheral vasoconstriction

Mild bronchoconstriction

Increased metabolism

Stimulation of sweat glands

72
Q

Alpha 2 stimulation results in:

A

Control release of neurotransmitters

73
Q

Beta 1 stimulation results in:

A

Increased heart rate (positive chronotropic)

Increased strength of cardiac contraction (positive inotropic)

Increased cardiac conduction (positive dromotropic)

74
Q

Beta 2 stimulation results in:

A

Bronchodilation

Peripheral vasodilation

75
Q

sympathomimetic  or adrenergic agonists

A

If a medication binds to and stimulates any of the adrenergic receptors

76
Q

what do sympathomimetic or adrenergic agonists do

A

producing effects that resemble the stimulation of the sympathetic nervous system

77
Q

sympatholytic or adrenergic antagonist

A

blocking effects or producing effects that resemble interruption of the sympathetic nervous system

78
Q

Selective beta blockers

A

bind and block only beta 1 or beta 2 receptors

79
Q

non-selective beta blockers

A

would block both beta 1 and beta 2 receptors