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
What does transdermal route of administration avoid?
first-pass effect
26
What are the considerations when it comes to using transdermal medications?
-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
27
What type of route of administration has a partial, not full, avoidance of first-pass effect?
rectal (pr)
28
When medications are taken rectally, the absorption is often what?
incomplete or irregular
29
Rectally administered medications may be what?
systemic or local
30
Rectally administered medications would be good for who?
sometimes kids, people who can't swallow, someone throwing up, someone in a coma
31
What does the vaginal route of administration avoid?
first-pass effect
32
What becomes problematic when taking medications vaginally?
retaining dosage forms due to vaginal fluid clearance
33
Why are some medications given vaginally?
it has good blood supply and surface area
34
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?
inhalation
35
What does the inhalation route avoid?
first-pass effect
36
What is a great why to deliver medication directly to the lungs and is sometimes used sytemically?
inhalation
37
What are the characteristics of intravenous (IV) route of administration?
-100% bioavailability -fast onset -bolus or continuous dosing -not appropriate for patient self-care
38
What does 100% bioavailability mean?
the fraction of a dose that reaches systemic circulation is unchanged (not getting broken down initially)
39
What is the only true 100% bioavailable course of administration?
Intravenous (IV)
40
What does bolus mean?
one time
41
What does intramuscular (IM) administration avoid?
firs-pass effect
42
What must the drug permeate for systemic absorption for intramuscular (IM) administration?
capillary walls (increasing blood flow will increase absorption)
43
Who will show unexpected results when taking a medication via IM route?
obese or emaciated patients
44
What is the absorption rate of IM medications?
absorption is fast; may be slowed by suspending in oil, using microspheres
45
What route of administration has a slower absorption than IM?
subcutaneous (SC, SQ) because you are putting it in the skin, not directly into the muscle, so it has longer to travel)
46
What does the subcutaneous route avoid?
first-pass effect
47
The absorption rate of subcutaneous medications may be altered by what?
-particle size -protein complexation -addition of vasoconstrictors -pH
48
What are other routes of administration?
-intrathecal -intraosseous -intra-arterial
49
What route delivers drug right to the CNS?
intrathecal
50
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?
intraosseous
51
What route is uncommon, requires special training, is when there is a quick withdrawal of needle and immediate pressure is required?
intra-arterial
52
What can be used if patent has no patent venous access?
intra-arterial
53
What carries the risk of capillary bed destruction and loss of perfusion possible?
intra-arterial
54
What route is appropriate for vasodilators?
antra-arterial
55
What is floxuridine an example of where the antineoplastic is delivered directly to the liver vis the hepatic artery?
intra-arterial
56
What are the pros of parenteral administration?
-better absorption -quick or immediate onset -IM and SC can be modified to create slow/delayed onset
57
What are the cons of parenteral administration?
-training -cost -comfort -sterility -equipment
58
What should you look at when choosing a route and formulation?
-efficacy (local/systemic; general patient health) -side effects -desired onset and length of therapy -cost -compliance issues (lifestyle, acceptability, ability to administer drug)
59
What is the drug discovery process
1. target discovery 2. chemical library screening 3. lead optimized 4. pre-clinical animal studies 5. clinical trials 6. market entry
60
When you think you have invented a drug, you need to administer it to how many different animal species?
2
61
The two different animal species used in a study are typically what?
one rodent, one non-rodent
62
What are you looking for in animal studies of a new drug?
general toxicity- increase doses until lethal
63
After looking at general toxicity of a drug in animal studies, what do you look at?
subacute (2-4 weeks) and chronic (6-24 months) toxicity testing
64
What has to be further investigated in animal studies of a new drug?
any negative effects
65
After you do animal studies of a new drug, you can submit what?
IND (investigational new drug)
66
How many days does the FDA have to evaluate applicants who submitted an IND?
30 days
67
If your IND is approved, you can begin working on what?
clinical trials
68
What occurs in phase I clinical trials?
-first trial in humans (10-100 people) -normally healthy volunteers, occasionally patients with rare/advanced illnesses
69
What is tested in phase I of clinical trials on humans?
safety and tolerability
70
What occurs in phase II clinical trials?
-first trial in patients (50-500 people) -patients with illness
71
What is being tested in phase II of clinical trials on patients?
efficacy and dose range
72
What occurs in phase III clinical trials?
-large scale multi-site (few hundred to few thousand people) -patients with illness
73
What is being tested in phase III of clinical trials in patients?
-confirms efficacy, compare to older therapies, continue to evaluate safety
74
After phase III of clinical trials, what is submitted?
NDA (new drug application)
75
After you submit an NDA and it is approved, what do you move onto?
phase IV trial where it is the post-marketing surveillance (thousands of patients)
76
When is a patent for a drug usually started?
around time of IND
77
How long does a patent last?
20 years
78
How long is usually left in a patent when a drug is officially approved?
10-14 years
79
What act prohibited mislabeling and adulteration of food and drugs?
Pure food and drug act of 1906
80
What act established regulations for use of opium, opioids, and cocaine?
Harrison Narcotics act of 1914
81
What act make it so drugs were tested for safety and purity?
Food, drug, and cosmetics act of 1938
82
What act made it so companies had to provide proof of efficacy as well as safety for new drugs?
Kefauver-harris amendment 1962
83
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?
dietary supplement and health education act of 1994