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Pharmacokinetics > Lecture 2: Routes of Drug Administration > Flashcards

Lecture 2: Routes of Drug Administration Flashcards

1
Q

t/f route of administration

has a dramatic effect on the time course of a drug in the body

A

treu

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2
Q

what is the most common route of drug delivery?

A

oral

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3
Q

what are the 3 types of enteral drug administration?

A
  1. oral
  2. buccal / sublingual
  3. rectal
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4
Q

what is the primary absorption site for oral drugs?

A

small intestine

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5
Q

drug absorption and effects of oral drugs are determined by what three things?

A
  1. physiological factors
  2. chemical/physical factors
  3. drug formulation
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6
Q

what are the physiological factors that can influence oral drug absorptin>

A

pH, gastric emptying

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7
Q

what are the chemical/physical factors that can influence oral drug administration?

A

molecular weight and ionization

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8
Q

do liquids or solids tend to be better absorbed when given by the oral route?

A

liquids

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9
Q

why does molecular weight and ionization matter in absorption>

A

they have an effect on how well a drug is moved across membrane

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10
Q

blood draining from gastrointestinal organs and spleen flows into the ___ circulation and ___(organ) before reaching the general circulation

A

portal; liver

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11
Q

blood draining from the intestines, stomach, pancreas, and spleen drains into the __ and will then move to the __ where drugs can be subject to metabolism before reaching the systemic circuit

A

portal vein; liver.

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12
Q

first pass metabolism describes the metabolism of a drug as it passes through the ____ and ___ before reaching the __

A

intestinal wall and liver; systemic circuit

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13
Q

first pass metabolism can reduce __

A

amount of active drug that reaches the systemic circuit

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14
Q

t/f metabolism can both activate and inactive drugs

A

true

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15
Q

the buccal route is the location of the __

A

membranes of the cheeks and behind the lips

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16
Q

the sublingual route is the location of the __

A

under the rogue

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17
Q

drugs in the buccal/sublingual route first pass through the __ epithelium to the ___ membrane which is reach in __ and __ that will transport the drug directly to the systemic circuit

A

stratified oral; submucosal; collagen and blood vessels

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18
Q

are drugs that are administered buccally and sublingually subject to first pass metabolism?

A

no

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19
Q

nicotine absorbs better in the mouth than the stomach, why is this?

A

pH

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20
Q

both the buccal and sublingual routes are ___, but the sublingual space has a ___

A

non-keratinized; thinner epithelium

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21
Q

what are 4 properties of the SL route that increase absorption?

A
  1. thinner epithelium
  2. immersion in saliva
  3. higher blood flow
  4. less propensity to swallow
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22
Q

what are the 3 rectal veins that drain blood from the rectum?

A

superior, middle and inferior rectal veins

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23
Q

the superior rectal veins drains into the ___ and therefor __ undergo 1st pass metabolism

A

portal vein; does

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24
Q

the middle and inferior rectal veins drains into the __ and therefor __ undergo 1st pass metabolism

A

vena cava; do NOT

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25
Q

what is a benefit of rectal administration?

A

reduces 1st pass metabolism (but does not completely eliminate)

26
Q

drug absorption in the rectal route is highly dependent on the ___ of the drug administered as this determines which veins are likely to absorb the drug

A

placement within the rectum

27
Q

what are the 3 types of parenteral admin?

A
  1. intravenous
  2. subcutaneous
  3. intramuscular
28
Q

list 5 advantages of intravenous administration

A
  1. no barrier to absorption
  2. rapid achievement of high drug concentration
  3. rapid onset of action
  4. precise delivery and controlled dose
  5. can deliver large volumes
29
Q

subcutaneous injects into the __

A

fatty tissue under the skin

30
Q

absorption form SC/IM sites is said to be __ rate limited, meaning it depends on __

A

perfusion, rate of blood flow away from the site

31
Q

blood vessels have pores called ___ that allows the ___ diffusion of drug rapidly

A

fenestrae, passive

32
Q

is there any barrier to blood absorption in the SC/IM route?

A

no

33
Q

oral administration absorption is ___ rate limited

A

permeability

34
Q

the __ supply impacts the effects of SC drugs

A

vascular supply

35
Q

at the IM site of administration, there is little impedance to movement of a drug into blood flow, even for __ and __ drugs

A

polar and ionized

36
Q

when administered IM, drugs are absorbed independently of ___and molecular size up to ___ g/mol

A

pKa (ionization); 5000

37
Q

which has higher blood flow, gluteal or deltoid?

A

deltoid

38
Q

if a drug is ____g/mol or larger, it is too large to be absorbed through the fenestra of the BV, therefore must enter through the ___ pathway

A

20 000; lymphatic

39
Q

lymph flow is much ___ than blood flow, absorption timeline of __

A

slower; several hours

40
Q

what are two benefits of drug distribution through the lymph?

A

slow transport allows for amount to be maintained at near constant amount and reducing the number of times it needs to be administered

41
Q

what are the 4 topical delivery routes?

A
  1. percutaneous
  2. ocular
  3. nasal
  4. inhalation
42
Q

what is percutaneous delivery?

A

delivering a drug to the place immediately below the point of application

43
Q

the percutaneous route if mainly designed for __ effects (ex: ___), but can also be used for ___ (ex:___)

A

local: hydrocortisone; systemic: nicotine and nitroglycerine patches

44
Q

what is a benefit of the percutaneous route?

A

can administer directly to desired site while minimizing the side effects of it affecting the body systemically

45
Q

percutaneous is also known as __

A

transdermal

46
Q

provide an example of a drug that is delivered transdermally to have systemic effects

A

fentanyl (applied to skin too treat systemic pain)

47
Q

why might lidocaine for pain relief be given percutaneously?

A

in large doses, it can be linked to toxicity and acadian arrest, therefore want to eliminate large systemic exposure

48
Q

list 4 factors that may affect variability of transdermal patches

A
  1. temperature
  2. sweating
  3. age
  4. skin thickness
49
Q

for fentanyl, an increase in temperature does what to the absorption rate?

A

increases

50
Q

ocular admin is reserved for only __ delivery

A

local

51
Q

give an example of a drug that is delivered ocularly an what it is used to treat

A

topical agents (beta antagonists) that reduce intraocular pressure in glaucoma

52
Q

beta antagonists can adversely affect ___ / __ function in patients with __, ___. ___

A

cardiac/pulmonary; heart failure, bradycardia, COPD

53
Q

nasal drug administration has historically been used to __ delivery, but recent investigations indicate that it may be useful for __ delivery

A

local; systemic

54
Q

nasal exposure may allow for __ exposure due the the ___ channels

A

brain exposure; olfactory

55
Q

give an example of a nasally administersed drug that has been traditionally given IV, but has shown to reach effective concentration in 10 min through nasal route

A

midazolam

56
Q

what is a benefit of being able to administer via nose rather than IV

A

less invasive

57
Q

the inhalation route is used to treat diseases of the __

A

lungs

58
Q

administration via the inhalation route minimizes the __while lowering the __

A

required dose; systemic concentration and associated risk

59
Q

what makes the lungs a great delivery system? 3

A
  1. rich blood supply to areolar epithelium for gas exchange
  2. highly permeable membrane
  3. provides favourable conditions for rapid and efficient absorption of systemically acting agents such as volatile aneshtetic s
60
Q

nicotine is absorbed fastest through which route? what is the impact of this?

A

inhalation, makes smoking more addictive than chewing

61
Q

give an example of topical inhalation drug

A

corticosteroids

Pharmacokinetics (3 decks)

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