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Intro to Pharmacology > Basics 2 > Flashcards

Basics 2 Flashcards

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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
Route of Administration (ROA)
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
26
Enteral routes-Drugs placed directly into GI tract Benefits?
``` Sublingual-placed under tongue Oral-swallowing Buccal-placed in cheek Rectum-absorption through rectum Convenient, outpatient, less expensive ```
27
Aspects of Enteral routes: Mouth
thin epithelium short transit time most are swallowed and absorbed in GI tract some absorbed sublingually or buccally
28
Aspects of Enteral routes: Stomach
``` 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 ```
29
Aspects of Enteral routes: Small intestine
Huge SA ph gradient 4.5-8 Enzyme secretions Most of drugs absorbed here
30
Aspects of Enteral routes: Colon
Bacterial actions Less absorption Some drugs actually act on the colon
31
Aspects of Enteral routes: Rectum
Use in unconscious patient or child
32
Oral Administration advantages include:
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)
33
What is the first pass effect?
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
34
How might reduced liver function affect first pass effect?
More drug will go into circulation!
35
What are the primary enzymes that will affect first pass metabolism?
GI lumen, Gut wall enzymes, bacterial enzymes, hepatic enzymes
36
What is bioavailability?
BIOAVAILABILITY= fraction of an administered dose of unchanged drug that reaches the systemic circulation
37
Oral preparations: what is Enteric coated?
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.
38
Oral preparations: what is extended release?
Special coatings or ingredients that control how fast the drug is released into the body. Helpful w/ compliance issues; no peaks or troughs
39
What are some advantages to sublingual/buccal administration
Rapid absorption, drug stability, avoids first pass effect
40
What are some disadvantages to sublingual/buccal administration?
Inconvenient Smaller doses Unpleasant taste of some drugs
41
What are the advantages of Rectal admin?
Unconscious patients and children If patient is nauseas or vomitting Easy to terminate exposure Good for drugs affecting the bowel-laxatives
42
What are some disadvantages of Rectal Admin?
absorption may be variable can be extremely dangerous and painful Irritating drugs are contraindicated
43
What is pulmonary administration?
Drugs inhaled as gases, aerosols, or as powders
44
What are some advantages used for parenteral administration?
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
What are some disadvantages to parenteral administration?
Irreversible May cause pain or fear May cause local tissue damage May cause infections
46
What angles are used for injections?
Intradermal: 15-20 degree angle Subcutaneous:45 degree angle Intramuscular: 90 degree angle
47
What are some advantages of intravenous administration?
Bolus or continuous Most reproducible and predictable Watch for bolus effect: too large->death High plasma conc achievable
48
What are some disadvantages of intravenous administration?
Cannot be recalled (overdose) May inadvertently introduce pathogens May induce hemolysis, precipitate blood constituents or cause other adverse reactions
49
What are some advantages of intramuscular administration?
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
What are some disadvantages of Intramuscular admin?
``` Absorption is dependent on flow Slower than IV Painful Limited volume Nerve damage Sterile or infected abscesses reported ```
51
What are some advantages of Subcutaneous admin?
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
What are some disadvantages to subcutaneous admin?
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
What is inhalation?
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
Other parenteral: what is intrathecal admin?
Bypasses BBB. Can be risky, but essential for some diseases like meningitis.
55
Other parenteral: what is Intraperitoneal admin?
Directly into body cavity | mostly in animals
56
Other parenteral: what is Intraosseous?
Into bone marrow-used in Europe.
57
What is topical administration?
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
Onset of action:
the period b/w the moment of drug introduction to the organism and the beginning of its action.
59
Onset of action:IV,IO
30-60 secs
60
Onset of action:Endotracheal, Inhalation
2-3 mins
61
Onset of action: Sublingual
3-5 mins
62
Onset of action: Intramuscular
10-20 mins
63
Onset of action: Subcutaneous
15-30 mins
64
Onset of action: Rectal
5-30 mins
65
Onset of action: Ingestion
30-90 mins
66
Onset of action:transdermal (topical)
variable, minutes-hours
67
What is duration of action?
period that specific effects of drug maintained
68
What is therapeutic window?
Distance b/w minimum therapeutic and minimum toxic doses of drug
69
What is Maximal effect?
Greatest response that can be produced by a drug "peak effect" varies from person to person
70
What is pulmonary administration?
Drugs inhaled as gases, aerosols, or as powders
71
What are some advantages used for parenteral administration?
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
What are some disadvantages to parenteral administration?
Irreversible May cause pain or fear May cause local tissue damage May cause infections
73
What angles are used for injections?
Intradermal: 15-20 degree angle Subcutaneous:45 degree angle Intramuscular: 90 degree angle
74
What are some advantages of intravenous administration?
Bolus or continuous Most reproducible and predictable Watch for bolus effect: too large->death High plasma conc achievable
75
What are some disadvantages of intravenous administration?
Cannot be recalled (overdose) May inadvertently introduce pathogens May induce hemolysis, precipitate blood constituents or cause other adverse reactions
76
What are some advantages of intramuscular administration?
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
What are some disadvantages of Intramuscular admin?
``` Absorption is dependent on flow Slower than IV Painful Limited volume Nerve damage Sterile or infected abscesses reported ```
78
What are some advantages of Subcutaneous admin?
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
What are some disadvantages to subcutaneous admin?
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
What is inhalation?
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
Other parenteral: what is intrathecal admin?
Bypasses BBB. Can be risky, but essential for some diseases like meningitis.
82
Other parenteral: what is Intraperitoneal admin?
Directly into body cavity | mostly in animals
83
Other parenteral: what is Intraosseous?
Into bone marrow-used in Europe.
84
What is topical administration?
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
Onset of action:
the period b/w the moment of drug introduction to the organism and the beginning of its action.
86
Onset of action:IV,IO
30-60 secs
87
Onset of action:Endotracheal, Inhalation
2-3 mins
88
Onset of action: Sublingual
3-5 mins
89
Onset of action: Intramuscular
10-20 mins
90
Onset of action: Subcutaneous
15-30 mins
91
Onset of action: Rectal
5-30 mins
92
Onset of action: Ingestion
30-90 mins
93
Onset of action:transdermal (topical)
variable, minutes-hours
94
What is duration of action?
period that specific effects of drug maintained
95
What is therapeutic window?
Distance b/w minimum therapeutic and minimum toxic doses of drug
96
What is Maximal effect?
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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