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PSYC 475 > Principles of pharmacology part 1 > Flashcards

Principles of pharmacology part 1 Flashcards

1
Q

what is pharmacology?

A

the study of the actions of drugs and
their effects on a living organism

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2
Q

Name 3 specialized areas of pharmacology

A
  1. Neuropharmacology
  2. Psychopharmacology
  3. Neuropsychopharmacology
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3
Q

what is neuropharmacology the study of?

A

drug-induced changes to nervous
system

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4
Q

what is psychopharmacology the study of?

A

drug-induced changes in mood,
thinking, and behavior

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5
Q

what is Neuropsychopharmacology the study of?

A

identify chemicals that can
alter disturbed behavior

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6
Q

What is drug action?

A

Is the specific molecular changes produced when a drug binds to a particular target site or receptor

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7
Q

What is drug effect means?

A

the alterations in physiological or psychological functions

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8
Q

what are two types of drug effect?

A
  1. Therapeutic effect
  2. Side effects
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9
Q

what is the therapeutic effect?

A

it’s an effect where a drug produces desired physical or
behavioral changes

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10
Q

what does it mean to have a Side-Effects?

A

anything that is a non-therapeutic effect. an effect that wasn’t desired physically or behaviorally

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11
Q

what kind of compound is a placebo?

A

pharmacologically inert compound

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12
Q

what kind of effect might a placebo have?

A

may have a therapeutic effect and side effect

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13
Q

what four reasons explain placebo effects?

A

1.Pavlovian conditioning - cues in the environment
2.Positive expectations - an optimistic outlook
3.Social learning - observing another individual anticipating a positive outcome
4. Genetics

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14
Q

what is a nocebo effect?

A

patients experience an adverse effects if they expect or are worried about the adverse effect

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15
Q

why are placebos essential in experimental design?

A

It eliminates the influence of expectation from the experiment’s participants

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16
Q

what is a double-blind experiment?

A

neither patient nor observer knows what treatment the participant has received

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17
Q

what does pharmacokinetics refer to?

A

refers to the movement of drugs into, through,
and out of the body. what the body does with the drug.

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18
Q

Explains the 5 steps on how the drug moves throughout the body. in other words how pharmacokinetics occurs?

A

starts from the site of administration (1)

the drug moves through cell membranes to be absorbed into the blood (2)

where it circulates to all cells in the body. Some of the drug molecules may bind to inactive sites such as plasma proteins or storage depots (3),

and others may bind to receptors in target tissue. Bloodborne drug molecules also enter the liver (4),

where they may be transformed into metabolites and travel to the kidneys and other discharge sites for ultimate excretion (5) from the body

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19
Q

what does bioavailability mean?

A

amount of drug in the blood that is free to bind at
specific target sites

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20
Q

what are the five pharmacokinetic factors determining drug action?

A
  1. Routes of administration
  2. Absorption and distribution
  3. Binding
  4. Inactivation
  5. Excretion
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21
Q

Explain routes of administration

A

how and where a drug is administered determines how
quickly and how completely it is absorbed into the blood

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22
Q

Explain absorption and distribution

A

most drugs must pass through a variety of cell
membranes and enter the blood plasma to reach the desired site of action

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23
Q

what happens during the “binding” to the drug

A

the drug binds to active target sites (receptors), to plasma proteins, or may be stored
temporarily in bone or fat (inactive)

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24
Q

what happens during inactivations

A

also known as biotransformation. occurs primarily as a result of metabolic processes in the liver influencing both the intensity and the duration of drug effects

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25
Q

what happens during excretion

A

liver metabolites are eliminated from the body with the urine or feces (some drugs are excreted in an unaltered form by the kidneys)

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26
Q

when a drug is orally administrated, what is the drugs route through the body?

A

drug must pass through stomach or intestine wall to reach blood capillaries; must be resistant to destruction by stomach acid and enzymes

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27
Q

what is the purpose of first-pass metabolism?

A

is an evolutionarily beneficial function because
potentially harmful chemicals

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28
Q

what does it mean to go through the first-pass metabolism?

A

it means that ingested chemicals have to pass via the portal vein to the liver, where they are altered by enzymes before passing to the general circulation

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29
Q

what is intravenous(IV) drug administration? what is a danger of?

A

rapid and accurate injection; drug goes directly into bloodstream; danger of overdose

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30
Q

what is intramuscular drug administration?

A

injection: slower, more even absorption over time

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31
Q

what is subcutaneous drug administration?

A

injection: just below the skin; drug pellets can be used to deliver hormones such as contraceptives

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32
Q

what does it mean to be an enteral route of administration?

A

it means that the use of the gastrointestinal tract is involved

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33
Q

what are methods of administration for enteral?

A

oral and rectal

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34
Q

what is the parenteral route?

A

an administration that does not use the alimentary canal, such as injection or pulmonary administration(inhalation).

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35
Q

what is inhalation?

A

when the drug is absorbed by passing through the lungs

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36
Q

what is the purpose of rectal administration?

A

the drug may avoid some first-pass metabolism – effective in infants, vomiting, unconscious

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37
Q

what is the route of administration for intraperitoneal? what is meant for?

A

injection: into peritoneal cavity – mostly used
for laboratory animals.

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38
Q

what is the sublingual route?

A

under the tongue; rapid absorption into capillaries;
avoids first-pass metabolism

39
Q

what is topical routes of administration? what kind of effect does it have?

A

method that involves an application to a specific body surface or mucus membranes, and local effects

40
Q

what is intranasal?

A

route of administration that has a local effect but moves rapidly into blood; avoids first-pass metabolism; bypasses blood-brain barrier

41
Q

what is the transdermal route?

A

through the skin with skin patches; avoids first-pass metabolism

42
Q

what is the epidural route?

A

injection into epidural space, in the spinal cord; bypasses blood-brain
barrier

43
Q

what are the advantages and disadvantages of oral route of administration?

A

Advantage - Safe; self-administered; economical; no
needle-related complications

Disadvantage - low and highly variable absorption; subject to first-pass metabolism; less-predictable blood levels

44
Q

what are the advantages and disadvantages of Intravenous route of administration?

A

Advantage - Most rapid; most accurate blood
concentration

Disadvantage - Overdose danger; cannot be readily reversed; requires sterile needles and medical technique

45
Q

what are the advantages and disadvantages of Intramuscular (IM) route of administration?

A

Advantage - Slow and even absorption

Disadvantage - Localized irritation at site of injection; needs sterile equipment

46
Q

what are the advantages and disadvantages of Subcutaneous (SC) route of administration?

A

Advantage - Slow and prolonged absorption

Disadvantage - Variable absorption depending on blood flow

47
Q

what are the advantages and disadvantages of Inhalation route of administration?

A

Advantage - Large absorption surface; very rapid onset;
no injection equipment needed

Disadvantage - Irritation of nasal passages; inhaled small particles may damage lungs

48
Q

what are the advantages and disadvantages of Topical route of administration?

A

Advantage - localized action and effects; easy to self-administer

Disadvantage - May be absorbed into general circulation

49
Q

what are the advantages and disadvantages of Intranasal route of administration?

A

Advantage - Ease of use; local or systemic effects; very
rapid; no first-pass metabolism; bypasses
blood–brain barrier

Disadvantage - Not all drugs can be atomized; potential irritation of nasal mucosas

50
Q

what are the advantages and disadvantages of Transdermal route of administration?

A

Advantage - Controlled and prolonged absorption

Disadvantage - Local irritation; useful only for lipid-soluble drugs

51
Q

what are the advantages and disadvantages of Epidural route of administration?

A

Advantage - Bypasses blood–brain barrier; very rapid
effect on CNS

Disadvantage - Not reversible; needs trained anesthesiologist; possible nerve damage

52
Q

what methods of drug administration influence the beginning(onset) of drug action?

A

Route of administration alters the rate of absorption and thus blood levels of the drug available to bind to a specific target site(bioavailability)

also, peak levels reflect the absorption rate and metabolism in the liver. such that the higher the peak, the faster the absorption over time.

53
Q

what are four multiple factors that modify drug absorption?

A
  1. route of administration
  2. drug concentration
  3. solubility and ionization of the drug
  4. rate of transport across cell membranes - bilayers of phospholipids molecules
54
Q

what drugs move through the cell membrane and how do they move through it?

A

Lipid-soluble drugs move through cell membranes by passive diffusion

55
Q

what direction is movement across the membrane for drugs that are lipid-soluble?

A

Diffusion is from higher to lower concentration (concentration gradient)

56
Q

what the purpose of having lipid soluble drugs?

A

Lipid solubility increases absorption and facilitates entry into the brain.

In other words, the faster the diffusion means increase in absorption. therefore increasing how easily it will pass lipid barriers to enter the brain

57
Q

why are more drugs not lipid soluble?

A

Most drugs are weak acids or bases that partially ionize in water

58
Q

what are the advantages of non-ionized drugs?

A

Non-ionized form is more lipid soluble; can pass cell membranes and enter the blood more easily

59
Q

when the drug enters the blood stream, what does the distribution look like?

A

Once a drug enters the blood it is quickly delivered to areas with high blood flow

60
Q

what happens to the plasma and drug when there is a high concentration of a drug?

A

plasma levels fall as the drug is absorbed into those areas, and thus will initially have a high drug concentration compared to the blood

then due to the high concentration, the drug is redistributed until it reaches equilibrium in all tissues

61
Q

what can drug redistribution do?

A

it can terminate drug action

62
Q

what the function of fenestration in typical capillary?

A

allows large molecules to pass through

63
Q

how do capillaries influences the drug distribution?

A

Since blood capillaries have numerous pores, most drugs can move from blood and enter body tissues regardless of lipid solubility, unless they are bound to
protein

64
Q

what difference does the brain capillary have compared to a typical capillary? how does this change distribution of materials?

A

Brain capillaries: endothelial cells are
fused by tight junctions instead of having fenestrations; most materials move by special transporters or if they are lipid-soluble

65
Q

what does the blood-brain barrier limit? what does this mean in terms of permeability?

A

The blood–brain barrier limits the movement of ionized molecules from the blood to the brain.

the blood-brain barrier is selectively permeable, and not impermeable

66
Q

what are brain capillaries surrounded by? what’s the purpose of this?

A

Brain capillaries are surrounded by extensions of astroglia (astrocytes) –essential to maintaining the blood-brain barrier

67
Q

what is the of the blood the brain receives? what of drugs within that blood?

A

The brain receives ~ 20% of the blood that
leaves the heart

if the drug is lipid-soluble they are readily distributed to brain tissue

68
Q

what is the placental barrier?

A

separation of blood circulation between mother
and fetus at the placenta

69
Q

what are two damaging effects on the fetus if a harmful drug transfer from mother to child. Give examples of those harmful drugs

A

Acute toxicity – where opiates, alcohol, and other drugs; action can be prolonged after birth due to slow metabolism

Teratogenic effects – agents causing developmental abnormalities; depends on time of exposure – most severe in early pregnancy

70
Q

give two examples of teratogenic effects

A
  1. Accutane (treatment for acne)
  2. thalomid - It was originally intended as a sedative or
    tranquilizer. Used for treating other conditions (colds, flu, nausea and morning sickness in pregnant women)
71
Q

what are drug depots? give examples

A

a place where there is a binding of drugs to inactive sites. these include several plasma proteins, with albumin being most important.

72
Q

what three things happens when a drug binds to a depot?

A

1.Reduces concentration of drug at action sites

2.Nonselective binding can cause competition between
drugs and possible overdose (phenytoin x aspirin)

3.Bound drug molecules cannot be altered by liver enzymes - prolongs time drug is in the body (THC)

73
Q

what is biotransformation?

A

(metabolism) and excretion eliminate drugs
from the body.

74
Q

what is half-life?

A

amount of time required for removal of 50% of the drug (t½);

75
Q

what does half-life determine when administering a drug?

A

Half-life determines the time interval between doses

76
Q

what is first-order kinetics of drug clearance?

A

Exponential elimination of drug from the blood. such that, exponential elimination means that a constant 50% of free drug in the blood is removed in each time interval

77
Q

with respect to clearance, what happens when blood levels are high?

A

When blood levels are high, clearance is faster, as blood levels drop, rate of clearance is reduced

78
Q

with respect to first-order kinetics of drug clearance. what happens when the drug levels are high in concentration?

A

clearance of that drug is faster. since you are talking half of that

79
Q

what we want when we administer a drug?

A

a desired drug level. such that we have a steady state in plasma level

80
Q

where do most of biotransformation occur?

A

the liver

81
Q

what are the two types of biotransformation? what are these phases responsible for?

A

Phase one metabolism
- oxidation, reduction or hydrolysis occurs
- makes metabolite less lipid soluble
- metabolite can be less reactive or more reactive

Phase two
- synthetic reaction - products are ionized, water soluble, and biologically inactive

82
Q

what is CYP450(cytochrome) responsible for?

A

enzyme family is responsible for oxidizing most psychoactive drugs

83
Q

what is responsible for inactive psychoactive drugs?

A

Glucuronide conjugation is particularly important for inactivating psychoactive drugs

84
Q

summarize the affects of biotransformation

A

the two phases of drug biotransformation ultimately produce one or more inactive metabolites, which are water soluble, so they can be excreted more readily than the parent drug. Metabolites formed in the liver are returned to the circulation and are subsequently filtered out by the kidneys, or they may be excreted into bile and eliminated with the feces. Metabolites that are active return to the circulation and may have additional action on target tissues before they are further metabolized into inactive products

85
Q

what are factors that influence rate of biotransformation?

A
  1. enzyme induction
  2. enzyme inhibition
  3. drug competition
  4. individual differences in age, gender, and genetics
86
Q

what triggers enzyme induction, give examples? what does enzyme induction do?

A

when there is a repeated use of drug, enzyme induction occurs, meaning that there is an increases number of enzymes; increases rate of metabolism

ex. heavy smokers and antidepressant

87
Q

what does enzyme inhibition do?

A

reduces metabolism of other drugs that use the same enzyme. therefore increased drug effect and increased potential for toxicity – grapefruit juice

88
Q

what is drug competition?

A

elevated levels of one drug reduces metabolism of the second

89
Q

what is the most important route of elimination of a drug?

A

kidney then urine

90
Q

what does liver biotransformation of a drug do?

A

turns the drug into s into ionized (water-soluble) molecules traps the metabolites in the kidney tubules, so they can be excreted along with waste products in the urine

91
Q

what does pH of urine influence? how might this knowledge be useful?

A

affects drug reabsorption(back to the blood) in kidney tubules. this is useful to know because altering the pH is used to treat drug toxicity

92
Q

what do kidneys do? what cant they do it for?

A

filter materials from the blood, unless large or bound to plasma proteins

93
Q

explain how the kidney is pH-dependent?

A

if its weakly acidic, means that its ionized, therefore it will be reabsorbed. however, if its weakly basic, it will be readily excreted

PSYC 475 (12 decks)

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