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Intro to Pharmacology > Basics 2 > Flashcards

Basics 2 Flashcards

1
Q

Drug discovery

A

Disease target, molecular design/screening, congeners/me too drugs.
Must be tested in animal and human trials, chronic toxicity not usually required
Drug discovery is very expensive and time consuming.

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2
Q

Animal testing: General screening tests for:

A 
pharmacological effects
hepatic/renal functioning
blood/urine tests
gross and histopathologic exams
reproductive effects
toxicity
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3
Q

What is acute toxicity?

A

Admin of a single dose of the agent up to lethal dose i at least 2 species. usually 1 rodent and 1 non-rodent
sub ac

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4
Q

What is sub acute toxicity?

A

2-4 weeks, at least 2 species

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5
Q

What is chronic toxicity?

A

6-24 mos, at least 2 species

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6
Q

Repro toxicity: what is teratogenic?

A

Effect on the In Utero Development of an organism resulting in abnormal structure or function-generally not heritable.

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7
Q

Repro toxicity: what is mutagenic?

A

Effect on the inheritable characteristics of a cell or organism-mutation in DNA.

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8
Q

What is AMES test?A

A

Standard IN VITRO test for mutagenicity-used for toxicity!

Uses salmonella bacteria, and also used in carcinogenesis test.

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9
Q

What is Dominant Lethal Test?

A

IN VIVO! test for toxicity. Males are exposedto substance and abnormalities looked for in progeny

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10
Q

FDA approval: Investigational New Drug (IND)

A

requires animal data, application for FDA approval to carry out new drug trials in humans

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11
Q

FDA approval:New Drug Application (NDA)

A

Application for FDA approval to market a new drug for ordinary clinical use-requires data from clinical trials as well as animal data.

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12
Q

Clinical Trials: phase I

A

studies safety of medication and treatment.
20-80 participants
up to several months

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13
Q

Clinical Trials: phase II

A

Studies the efficacy.
100-300 participants
up to 2 years

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14
Q

Clinical Trials: phase III

A

Studies safety, efficacy, and dosing.
1-3K participants
1-4 years

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15
Q

Clinical Trials: phase IV

A

Studies the long-term effectiveness; cost effectiveness.
Thousands of participants
1 yr+

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16
Q

Drug patents:

A

patent applications usually submitted during animal testing, 20 yrs non competition allowance.
After 20 yrs, generics are allowed into the market, but prove BIOEQUIVALENCE

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17
Q

Orphan Drugs?

A

Used for rare diseases. Uncommon in R&D b/c cost may not outweigh profit-> may be some federal incentives like grants etc.

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18
Q

Schedule I

A

No currently accepted medical use in the US. a lack of accepted safety for use under medical supervision, and a HIGH POTENTIAL FOR ABUSE. i.e. heroin, LSD, marajuana,peyote, ecstasy etc

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19
Q

Schedule II

A

High potential for abuse, may lead to severe psychological or physical dependence. ie codeine, amphetamine, phenobarbitol

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20
Q

Schedule III

A

Less potential for abuse-moderate to low physical dependence or high psychological dependence. hydrocodone anabolic steroids

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21
Q

Schedule IV

A

Low potential for abuse relative to schedule III. ie ativan, alprazolam

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22
Q

Schedule V

A

Low potential for abuse, relative to schedule IV and consists primarily of preparations containing limited qtys of certain narcotics. i.e. cough meds containing no more than 200mg codeine per 100 mL= robitussin

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23
Q

What is an analog?

A

Drug whose structure is related to another drug. i.e. extra hydrogen, hydroxyl, or methyl group.
Chemical and biological properties may be quite different.
“similar” drugs with similar properties

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24
Q

What is a congener?

A

substance synthesized by essentially the same synthetic chemical runs and the same procedures as another drug. ie tires. . . .
Congeners and analogs placed into same schedule . ..”designer drugs”

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25
Q

Route of Administration (ROA)

A

ROA chosen may have profound effect upon the speed and efficiency with which the drug acts. The properties of a drug will determine in which way it can or must be given: solubility, pH effects

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26
Q

Enteral routes-Drugs placed directly into GI tract

Benefits?

A 
Sublingual-placed under tongue
Oral-swallowing
Buccal-placed in cheek
Rectum-absorption through rectum
Convenient, outpatient, less expensive
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27
Q

Aspects of Enteral routes: Mouth

A

thin epithelium
short transit time
most are swallowed and absorbed in GI tract
some absorbed sublingually or buccally

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28
Q

Aspects of Enteral routes: Stomach

A 
Rich blood supply
Acid environment
Transit time highly variable
Some absorption of drug may occur in the stomach, but most reaches intestines
Tablet disintegration takes time
Some drugs are acid sensitive
Irritation develop
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29
Q

Aspects of Enteral routes: Small intestine

A

Huge SA
ph gradient 4.5-8
Enzyme secretions
Most of drugs absorbed here

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30
Q

Aspects of Enteral routes: Colon

A

Bacterial actions
Less absorption
Some drugs actually act on the colon

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31
Q

Aspects of Enteral routes: Rectum

A

Use in unconscious patient or child

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32
Q

Oral Administration advantages include:

A

Convenient:self-administered, pain free, easy
Absorption:along whole length of GI tract
Cheap:compared to most parenteral routes
Low risk of systemic infections
Antidotes for toxicities and overdose (activated charcoal)

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33
Q

What is the first pass effect?

A

hepatic metabolism of the drug when it is absorbed through gut an delivered to the liver via the portal circulation. The greater the first pass effect, the less agent will reach systemic circulation when the agent is administered orally

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34
Q

How might reduced liver function affect first pass effect?

A

More drug will go into circulation!

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35
Q

What are the primary enzymes that will affect first pass metabolism?

A

GI lumen, Gut wall enzymes, bacterial enzymes, hepatic enzymes

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36
Q

What is bioavailability?

A

BIOAVAILABILITY= fraction of an administered dose of unchanged drug that reaches the systemic circulation

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37
Q

Oral preparations: what is Enteric coated?

A

Chemical envelope that resists the action of the fluids and enzymes in the stomach, but dissolve regularly in the upper intestine.
Beneficial for drugs that are acid unstable or irritating to stomach.

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38
Q

Oral preparations: what is extended release?

A

Special coatings or ingredients that control how fast the drug is released into the body.
Helpful w/ compliance issues; no peaks or troughs

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39
Q

What are some advantages to sublingual/buccal administration

A

Rapid absorption,
drug stability,
avoids first pass effect

40
Q

What are some disadvantages to sublingual/buccal administration?

A

Inconvenient
Smaller doses
Unpleasant taste of some drugs

41
Q

What are the advantages of Rectal admin?

A

Unconscious patients and children
If patient is nauseas or vomitting
Easy to terminate exposure
Good for drugs affecting the bowel-laxatives

42
Q

What are some disadvantages of Rectal Admin?

A

absorption may be variable
can be extremely dangerous and painful
Irritating drugs are contraindicated

43
Q

What is pulmonary administration?

A

Drugs inhaled as gases, aerosols, or as powders

44
Q

What are some advantages used for parenteral administration?

A

Drugs that poorly absorbed from the GI tract
Drugs unstable in GI tract
Unconscious patients
Quick onset of action
High bioavailability-more control over dosing

45
Q

What are some disadvantages to parenteral administration?

A

Irreversible
May cause pain or fear
May cause local tissue damage
May cause infections

46
Q

What angles are used for injections?

A

Intradermal: 15-20 degree angle
Subcutaneous:45 degree angle
Intramuscular: 90 degree angle

47
Q

What are some advantages of intravenous administration?

A

Bolus or continuous
Most reproducible and predictable
Watch for bolus effect: too large->death
High plasma conc achievable

48
Q

What are some disadvantages of intravenous administration?

A

Cannot be recalled (overdose)
May inadvertently introduce pathogens
May induce hemolysis, precipitate blood constituents or cause other adverse reactions

49
Q

What are some advantages of intramuscular administration?

A

Second most controllable
Absorptive time variable with local blood flow
Can be given in aqueous solns that are absorbed rapidly or in DEPOTS/reservoir
Suspension of the drug in a nonacqueous vehicle that slowly diffuses out of muscle and releases drug.-useful for neuroleptic and contraceptive drugs

50
Q

What are some disadvantages of Intramuscular admin?

A 
Absorption is dependent on flow
Slower than IV 
Painful
Limited volume
Nerve damage
Sterile or infected abscesses reported
51
Q

What are some advantages of Subcutaneous admin?

A

Slower than IV
Minimizes risk of hemolysis or thrombosis compared to IV
May be more constant slower and more sustained effects compared to IV

52
Q

What are some disadvantages to subcutaneous admin?

A

Use only non-irritating drugs.
Sometimes a minute amount of EPI is added to limit the area of action via vasoconstriction.
Useful for insulin pumps in diabetic patients

53
Q

What is inhalation?

A

Rapid, quick effect, Systemic absorption may occur.
Most addictive route.
Too small of particles aren’t retained, and too large particles impact tissues.
ORAL- Good for asthma, COPD
NASAL-good for nasal decongestants

54
Q

Other parenteral: what is intrathecal admin?

A

Bypasses BBB. Can be risky, but essential for some diseases like meningitis.

55
Q

Other parenteral: what is Intraperitoneal admin?

A

Directly into body cavity

mostly in animals

56
Q

Other parenteral: what is Intraosseous?

A

Into bone marrow-used in Europe.

57
Q

What is topical administration?

A

Mucosal membranes-eye drops,nasal etc
Skin-dermal rubbing of oil/ointment-local axn
Transdermal-Absorption of drug trough systemic action: stable blood levels, no first pass metabolism, drug must be potent or patch becomes too large.

58
Q

Onset of action:

A

the period b/w the moment of drug introduction to the organism and the beginning of its action.

59
Q

Onset of action:IV,IO

A

30-60 secs

60
Q

Onset of action:Endotracheal, Inhalation

A

2-3 mins

61
Q

Onset of action: Sublingual

A

3-5 mins

62
Q

Onset of action: Intramuscular

A

10-20 mins

63
Q

Onset of action: Subcutaneous

A

15-30 mins

64
Q

Onset of action: Rectal

A

5-30 mins

65
Q

Onset of action: Ingestion

A

30-90 mins

66
Q

Onset of action:transdermal (topical)

A

variable, minutes-hours

67
Q

What is duration of action?

A

period that specific effects of drug maintained

68
Q

What is therapeutic window?

A

Distance b/w minimum therapeutic and minimum toxic doses of drug

69
Q

What is Maximal effect?

A

Greatest response that can be produced by a drug “peak effect” varies from person to person

70
Q

What is pulmonary administration?

A

Drugs inhaled as gases, aerosols, or as powders

71
Q

What are some advantages used for parenteral administration?

A

Drugs that poorly absorbed from the GI tract
Drugs unstable in GI tract
Unconscious patients
Quick onset of action
High bioavailability-more control over dosing

72
Q

What are some disadvantages to parenteral administration?

A

Irreversible
May cause pain or fear
May cause local tissue damage
May cause infections

73
Q

What angles are used for injections?

A

Intradermal: 15-20 degree angle
Subcutaneous:45 degree angle
Intramuscular: 90 degree angle

74
Q

What are some advantages of intravenous administration?

A

Bolus or continuous
Most reproducible and predictable
Watch for bolus effect: too large->death
High plasma conc achievable

75
Q

What are some disadvantages of intravenous administration?

A

Cannot be recalled (overdose)
May inadvertently introduce pathogens
May induce hemolysis, precipitate blood constituents or cause other adverse reactions

76
Q

What are some advantages of intramuscular administration?

A

Second most controllable
Absorptive time variable with local blood flow
Can be given in aqueous solns that are absorbed rapidly or in DEPOTS/reservoir
Suspension of the drug in a nonacqueous vehicle that slowly diffuses out of muscle and releases drug.-useful for neuroleptic and contraceptive drugs

77
Q

What are some disadvantages of Intramuscular admin?

A 
Absorption is dependent on flow
Slower than IV 
Painful
Limited volume
Nerve damage
Sterile or infected abscesses reported
78
Q

What are some advantages of Subcutaneous admin?

A

Slower than IV
Minimizes risk of hemolysis or thrombosis compared to IV
May be more constant slower and more sustained effects compared to IV

79
Q

What are some disadvantages to subcutaneous admin?

A

Use only non-irritating drugs.
Sometimes a minute amount of EPI is added to limit the area of action via vasoconstriction.
Useful for insulin pumps in diabetic patients

80
Q

What is inhalation?

A

Rapid, quick effect, Systemic absorption may occur.
Most addictive route.
Too small of particles aren’t retained, and too large particles impact tissues.
ORAL- Good for asthma, COPD
NASAL-good for nasal decongestants

81
Q

Other parenteral: what is intrathecal admin?

A

Bypasses BBB. Can be risky, but essential for some diseases like meningitis.

82
Q

Other parenteral: what is Intraperitoneal admin?

A

Directly into body cavity

mostly in animals

83
Q

Other parenteral: what is Intraosseous?

A

Into bone marrow-used in Europe.

84
Q

What is topical administration?

A

Mucosal membranes-eye drops,nasal etc
Skin-dermal rubbing of oil/ointment-local axn
Transdermal-Absorption of drug trough systemic action: stable blood levels, no first pass metabolism, drug must be potent or patch becomes too large.

85
Q

Onset of action:

A

the period b/w the moment of drug introduction to the organism and the beginning of its action.

86
Q

Onset of action:IV,IO

A

30-60 secs

87
Q

Onset of action:Endotracheal, Inhalation

A

2-3 mins

88
Q

Onset of action: Sublingual

A

3-5 mins

89
Q

Onset of action: Intramuscular

A

10-20 mins

90
Q

Onset of action: Subcutaneous

A

15-30 mins

91
Q

Onset of action: Rectal

A

5-30 mins

92
Q

Onset of action: Ingestion

A

30-90 mins

93
Q

Onset of action:transdermal (topical)

A

variable, minutes-hours

94
Q

What is duration of action?

A

period that specific effects of drug maintained

95
Q

What is therapeutic window?

A

Distance b/w minimum therapeutic and minimum toxic doses of drug

96
Q

What is Maximal effect?

A

Greatest response that can be produced by a drug “peak effect” varies from person to person

Intro to Pharmacology (4 decks)

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