Routes of administration and dosage forms Flashcards

1
Q

How can we deliver drugs to the body?

A

-oral: swallowed
-sublingual/buccal
-topical
-transdermal
-rectal
-vaginal
-inhalation
-IV
-IM
-SubQ

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2
Q

Why are there different forms of drug delivery to the body?

A

-drug properties
-onset of action
-patient acceptance
-ease of use
-cost

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3
Q

What route of administration is convenient and often the cheapest?

A

oral (po) - swallowed

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4
Q

What are the absorption characteristics of the oral route?

A

-slow absorption
-absorption primarily occurs in intestines
-subject to first-pass effect
-gastric emptying and GI motility important

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5
Q

What can be added or medications taken orally to protect the stomach and the drug?

A

a coating

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6
Q

What is the first-pass effect?

A

medication goes into liver where it is metabolized and broken down some before it enters blood stream–less % goes into bloodstream than what initially went in

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7
Q

What are the different formulations of substances that can be taken via the oral route?

A

-tablets
-capsules (soft gel caps/hard caps)
-ODT (orally dissolving tablet)
-liquids
-lozenges

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8
Q

What are the different types of liquids that can be taken via the oral route?

A

-suspensions
-elixirs
-syrups
-solutions

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9
Q

What type of liquid is created when a powder and liquid are mixed together?

A

suspension

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10
Q

What type of liquid contains alcohol and usually isn’t given to kids?

A

elixirs

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11
Q

What type of liquid is heavily sugared?

A

syrups

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12
Q

What type of liquid is when a liquid is added to powder to create a substance that doesn’t separate?

A

solution

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13
Q

What type of route of administration can a drug be taken that has a delayed ore extended release?

A

oral (po)

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14
Q

What are the characteristics of delayed/extended release substances?

A

-slow, uniform absorption over an extended period of time

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15
Q

What are delayed/extended release substances great for?

A

drugs that have a short half-life

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16
Q

What are the advantages of delayed/extended release medications?

A

-improved compliance
-lower peak levels = less side effects

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17
Q

What are the disadvantages of delayed/extended release medications?

A

-dosage from failure/dumping
-inappropriate administration (cutting/crushing)
-cost

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18
Q

What is the route of administration where the drug is placed under the tongue (SL) or between the cheek/lip and gums?

A

sublingual (SL) and buccal

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19
Q

What does the sublingual (SL) and buccal route of administration avoid?

A

first-pass effect; direct absorption to systemic venous circulation

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20
Q

What type of onset do sublingual (SL) and buccal drugs have?

A

quick onset

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21
Q

What is the route of administration where the drug is applied to the skin or mucous membrane (eye, ear, nose, throat, vagina)?

A

topical

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22
Q

What are topical medications used for?

A

local effect

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23
Q

What are generally not a concern for topical medications?

A

systemic effects

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24
Q

What is the route of administration where the drug is applied topically and is intended to produce a systemic effect?

A

transdermal

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25
Q

What does transdermal route of administration avoid?

A

first-pass effect

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26
Q

What are the considerations when it comes to using transdermal medications?

A

-skin is tough to penetrate-absorption will be slow
-drug must reach capillary bed to be effective systemically
-degree of absorption depends on lipophilicity of drug, surface area exposed, presence of abrasion, occlusion, vehicle

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27
Q

What type of route of administration has a partial, not full, avoidance of first-pass effect?

A

rectal (pr)

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28
Q

When medications are taken rectally, the absorption is often what?

A

incomplete or irregular

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29
Q

Rectally administered medications may be what?

A

systemic or local

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30
Q

Rectally administered medications would be good for who?

A

sometimes kids, people who can’t swallow, someone throwing up, someone in a coma

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31
Q

What does the vaginal route of administration avoid?

A

first-pass effect

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32
Q

What becomes problematic when taking medications vaginally?

A

retaining dosage forms due to vaginal fluid clearance

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33
Q

Why are some medications given vaginally?

A

it has good blood supply and surface area

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34
Q

In what route of administration is the drug quickly and well-absorbed due to the lungs having a large surface area and has an immediate effect?

A

inhalation

35
Q

What does the inhalation route avoid?

A

first-pass effect

36
Q

What is a great why to deliver medication directly to the lungs and is sometimes used sytemically?

A

inhalation

37
Q

What are the characteristics of intravenous (IV) route of administration?

A

-100% bioavailability
-fast onset
-bolus or continuous dosing
-not appropriate for patient self-care

38
Q

What does 100% bioavailability mean?

A

the fraction of a dose that reaches systemic circulation is unchanged (not getting broken down initially)

39
Q

What is the only true 100% bioavailable course of administration?

A

Intravenous (IV)

40
Q

What does bolus mean?

A

one time

41
Q

What does intramuscular (IM) administration avoid?

A

firs-pass effect

42
Q

What must the drug permeate for systemic absorption for intramuscular (IM) administration?

A

capillary walls (increasing blood flow will increase absorption)

43
Q

Who will show unexpected results when taking a medication via IM route?

A

obese or emaciated patients

44
Q

What is the absorption rate of IM medications?

A

absorption is fast; may be slowed by suspending in oil, using microspheres

45
Q

What route of administration has a slower absorption than IM?

A

subcutaneous (SC, SQ) because you are putting it in the skin, not directly into the muscle, so it has longer to travel)

46
Q

What does the subcutaneous route avoid?

A

first-pass effect

47
Q

The absorption rate of subcutaneous medications may be altered by what?

A

-particle size
-protein complexation
-addition of vasoconstrictors
-pH

48
Q

What are other routes of administration?

A

-intrathecal
-intraosseous
-intra-arterial

49
Q

What route delivers drug right to the CNS?

A

intrathecal

50
Q

What route delivers drugs in to the bone where the bone marrow drains into venous system and is seen often in the ER and peds where access may be difficult?

A

intraosseous

51
Q

What route is uncommon, requires special training, is when there is a quick withdrawal of needle and immediate pressure is required?

A

intra-arterial

52
Q

What can be used if patent has no patent venous access?

A

intra-arterial

53
Q

What carries the risk of capillary bed destruction and loss of perfusion possible?

A

intra-arterial

54
Q

What route is appropriate for vasodilators?

A

antra-arterial

55
Q

What is floxuridine an example of where the antineoplastic is delivered directly to the liver vis the hepatic artery?

A

intra-arterial

56
Q

What are the pros of parenteral administration?

A

-better absorption
-quick or immediate onset
-IM and SC can be modified to create slow/delayed onset

57
Q

What are the cons of parenteral administration?

A

-training
-cost
-comfort
-sterility
-equipment

58
Q

What should you look at when choosing a route and formulation?

A

-efficacy (local/systemic; general patient health)
-side effects
-desired onset and length of therapy
-cost
-compliance issues (lifestyle, acceptability, ability to administer drug)

59
Q

What is the drug discovery process

A
  1. target discovery
  2. chemical library screening
  3. lead optimized
  4. pre-clinical animal studies
  5. clinical trials
  6. market entry
60
Q

When you think you have invented a drug, you need to administer it to how many different animal species?

A

2

61
Q

The two different animal species used in a study are typically what?

A

one rodent, one non-rodent

62
Q

What are you looking for in animal studies of a new drug?

A

general toxicity- increase doses until lethal

63
Q

After looking at general toxicity of a drug in animal studies, what do you look at?

A

subacute (2-4 weeks) and chronic (6-24 months) toxicity testing

64
Q

What has to be further investigated in animal studies of a new drug?

A

any negative effects

65
Q

After you do animal studies of a new drug, you can submit what?

A

IND (investigational new drug)

66
Q

How many days does the FDA have to evaluate applicants who submitted an IND?

A

30 days

67
Q

If your IND is approved, you can begin working on what?

A

clinical trials

68
Q

What occurs in phase I clinical trials?

A

-first trial in humans (10-100 people)
-normally healthy volunteers, occasionally patients with rare/advanced illnesses

69
Q

What is tested in phase I of clinical trials on humans?

A

safety and tolerability

70
Q

What occurs in phase II clinical trials?

A

-first trial in patients (50-500 people)
-patients with illness

71
Q

What is being tested in phase II of clinical trials on patients?

A

efficacy and dose range

72
Q

What occurs in phase III clinical trials?

A

-large scale multi-site (few hundred to few thousand people)
-patients with illness

73
Q

What is being tested in phase III of clinical trials in patients?

A

-confirms efficacy, compare to older therapies, continue to evaluate safety

74
Q

After phase III of clinical trials, what is submitted?

A

NDA (new drug application)

75
Q

After you submit an NDA and it is approved, what do you move onto?

A

phase IV trial where it is the post-marketing surveillance (thousands of patients)

76
Q

When is a patent for a drug usually started?

A

around time of IND

77
Q

How long does a patent last?

A

20 years

78
Q

How long is usually left in a patent when a drug is officially approved?

A

10-14 years

79
Q

What act prohibited mislabeling and adulteration of food and drugs?

A

Pure food and drug act of 1906

80
Q

What act established regulations for use of opium, opioids, and cocaine?

A

Harrison Narcotics act of 1914

81
Q

What act make it so drugs were tested for safety and purity?

A

Food, drug, and cosmetics act of 1938

82
Q

What act made it so companies had to provide proof of efficacy as well as safety for new drugs?

A

Kefauver-harris amendment 1962

83
Q

What act amended food, drug, and cosmetics act to establish standards for dietary supplements but not to allow FDA to apply same standard as for drugs?

A

dietary supplement and health education act of 1994