Absorption Flashcards

1
Q

What is BIOACCESSIBILITY? What are the two sources for it?

A

The availability of a molecule to enter an organism from the environment.

  1. The organism has access to the molecule
  2. Environmental pollution + biodegradation
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2
Q

While BIOAVAILABILITY is how much of a xenobiotic that gets into the body to the SOA, BIOACCESSIBILITY is the different _____ of the xenobiotic the body encounters. Give examples.

A

Forms

Prescription drugs, food alternative meds, cosmetic + household cleaners

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3
Q

What is the difference between BIOACCUMULATION and BIOMAGNIFICATION?

A

In both cases, toxic chemicals bond are stored in fatty tissues/organs instead of being secreted out in animals.

BIOACCUMULATION: takes place in a single organism over the span of its life. Older animals have a higher level of chemical.

BIOMAGNIFICATION; the toxic chemicals transfer from lower trophic levels to higher trophic levels within a food web, resulting in a higher concentration in predators.

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4
Q

What are the two routes of exposure/administration? How are they different? Give examples of both.

A

Enteral (alimentary) and Parenteral (extra-alimentary)

Enteral involves the gastrointestinal tract and is done through ORAL, SUBLINGUAL/BUCCAL, and RECTAL.

The parenteral involves substances unstable in the GI tract and is done through INJECTIONS, INHALATIONS, and TRANSDERMAL exposures.

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5
Q

(T/F) One of the advantages of parenteral exposure is that it has quick effects while a disadvantage is that it decreases the likelihood of getting the drug into the right tissue.

A

False, it has quick effects and it increases the likelihood of getting the drug into the right tissue because it is more precise.

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6
Q

What are the three physical factors that influence absorption of a xenobiotic? What do they all dictate?

A
  1. Substance properties
  2. Matrix properties
  3. Route of exposure/administration

Blood flow, surface area and contact time.

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7
Q

The greater the blood flow, the _____ the absorption of a drug. The greater the surface area and time for absorption, the _______ the absorption.

A

Greater; greater

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8
Q

Pick one from each pair in where a greater absorption of a xenobiotic would occur and briefly explain why:

  1. Intestine vs subcutaneous tissue
  2. Intestine vs stomach
A
  1. Greater absorption in intestine than subcutaneous tissue because HIGHER BLOOD FLOW. Organs that need more oxygen have a higher blood flow.
  2. Intestine has a LARGER surface area which also means LARGER CONTACT TIME, so greater absorption in intestine than stomach.

*residence time in intestine is 4-8 times longer than stomach

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9
Q

What are the five elements of the digestive system? Briefly explain them.

A
  1. Digest - break molecules into small molecules
  2. Secrete - active release of a substance
  3. Absorb - movement of nutrients into stomach from GI tract or intestinal cells after digestion
  4. Excrete - elimination of non-absorbed or metabolic wastes
  5. Protect
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10
Q

The gastrointestinal tract is a flexible muscular tube extending from the _______ to the ______ that is surrounded by the body. Many things pass through the GI tract without being absorbed and if they are not absorbed, they are not _____ our body.

A

Mouth; Anus; Inside

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11
Q

(T/F) The organisms that live in our digestive tract only have positive impacts on absorption and health.

A

False, can also have negative impacts.

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12
Q

What is the difference between Mechanical digestion
and Chemical digestion for ORAL (enteral) drugs?

A

Mechanical digestion begins in the mouth where molecule is broken into smaller pieces to increase SA with water added to it. Then, peristalsis lubricates food and moves it into stomach. NO change in chemical nature of drug.

Chemical digestion also begins in the mouth through the saliva’s enzymes. Digestive “juices” break down complex drug molecules into their chemical building blocks. Process is completed in the small intestine.

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13
Q

Match the following terms regarding digestive “juices.”

  1. Saliva
  2. Gastric juice
  3. Bile
  4. Pancreatic juice
  5. Epithelial cell secretions

A. in STOMACH made up of water, mostly PROTEASES and HCL to break down food. Protected by gastric mucosa.
B. in the INTESTINE produced by liver and released by gall bladder. Acts as a EMULSIFIER (e.g. micelles of lipophilic molecules created in an aqueous env are broken down to be absorbed by epithelial cells).
C. made of enzymes
D. in the MOUTH with a slightly basic pH that neutralizes acid. Has AMYLASE and LIPASE.
E. in the INTESTINE with enzymes and bicarbonate

A

Saliva - in the MOUTH with a slightly basic pH that neutralizes acid. Has AMYLASE and LIPASE.

Gastric juice - in STOMACH made up of water, mostly PROTEASES and HCL to break down food. Protected by gastric mucosa.

Bile - in the INTESTINE produced by liver and released by gall bladder. Acts as a EMULSIFIER (e.g. micelles of lipophilic molecules created in an aqueous env are broken down to be absorbed by epithelial cells).

Pancreatic juice - in the INTESTINE with enzymes and bicarbonate

Epithelial cell secretions - made of enzymes

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14
Q

Small intestine is the _______ site of chemical absorption, while large intestine is the ________ site of chemical absorption.

A

Primary
Secondary

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15
Q

Nutrients and xenobiotics reach the blood and lymph via the intestinal _______ cells.

A

Epithelial

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16
Q

What are the four ways xenobiotics reach the blood and lymph via epithelial cells?

A

1) Transcellular
2) Paracellular
3) Transcytosis
4) Absorption into lymph

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17
Q

Match the following terms to their definitions regarding chemical absorption:
1) Transcellular
2) Paracellular
3) Transcytosis
4) Absorption into lymph

A. receptor mediated endocytosis where the molecule is released on the other side of the cell. Limited by size, lipophilicity and SA.
B. molecules (usually lipophilic) pass through epithelial cells using active/passive transport
C. done via M-cells pd Peyer’s.
D. molecules transfer across an epithelium by passing through the intercellular space (cracks) between the cells. Limited by size and lipophilicity (small + polar)

A

Transcellular - molecules (usually lipophilic) pass through epithelial cells using active/passive transport

Paracellular - molecules transfer across an epithelium by passing through the intercellular space (cracks) between the cells. Limited by size and lipophilicity (small + polar)

Transcytosis - receptor mediated endocytosis where the molecule is released on the other side of the cell. Limited by size, lipophilicity and SA.

Absorption into lymph - done via M-cells pd Peyer’s.

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18
Q

Unabsorbed materials in the small intestine is partially or completely absorbed by _______ in the large intestine. The remaining unabsorbed is ______.

A

Microflora

Feces

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19
Q

Match the transit time of a xenobiotic according to the organs:

  1. less than a minute
  2. 1-2 hours
  3. 7-8 hours
  4. 12-14 hours

A. small intestine
B. large intesine
C. mouth
D. stomach

A

Less than a minute - mouth
1-2 hours - stomach
7-8 hours - small intestine
12-14 hours - large intestine

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20
Q

First pass metabolism includes the HEPATIC PORTAL SYSTEM, what are the four steps of it?

A
  1. Small intestine absorbs products of digestion
  2. Nutrient molecules travel in hepatic portal vein to liver
  3. Liver monitors blood content
  4. Blood enters general circulation
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21
Q

Briefly describe first pass metabolism and how it reduces BIOAVAILABILITY.

A

First pass metabolism is a process where a drug administered by the MOUTH (oral) is absorbed from the GI tract (small intestine) and is transported to the LIVER via the HEPATIC PORTAL VIEN where it is metabolized. The drug is metabolized into its inactive forms, reducing the bioavailability by causing only some of the active drug to reach the SOA.

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22
Q

(T/F) All enteral forms of drug administration/exposure (oral, sublingual, buccal + rectal) undergo first pass metabolism.

A

False! Only oral undergoes first pass metabolism!

23
Q

What are the advantages of Enteral Oral administration/exposure of drugs?

if you can know at least 5, ill be proud of you <3

A
  • most common + convenient
  • not invasive
  • local + systemic delivery
  • slow delivery into circulation which avoids spike and reduces toxicity
  • dose can be increased
  • large SA for absorption
  • toxicity can be reduced + reversed
24
Q

What are the disadvantages of Enteral Oral administration/exposure of drugs?

if you can know at least 5, ill be proud of you <3

A
  • easy access for toxins
  • variable rate of absorption
  • patient might not comply
  • first-pass effects (metabolized before reaching SOA)
  • patient must be capable
  • poor absorption of lipophilic molecules
  • digestive enzymes/gastric acidity can destroy drugs
25
Q

Match the following terms to their definition
1) Sublingual
2) Buccal
3) Oral spray

A. drug is between CHEEK + GUMS and is diffused through ORAL MUCOSA into the capillary network to enter systemic circulation
B. faster than sublingual and buccal, is diffused through ORAL MUCOSA into the capillary network to enter systemic circulation
C. drug is placed UNDER THE TONGUE and is diffused through ORAL MUCOSA into the capillary network to enter systemic circulation

A

Sublingual - drug is placed UNDER THE TONGUE and is diffused through ORAL MUCOSA into the capillary network to enter systemic circulation

Buccal - drug is between CHEEK + GUMS and is diffused through ORAL MUCOSA into the capillary network to enter systemic circulation

Oral spray - faster than sublingual and buccal, is diffused through ORAL MUCOSA into the capillary network to enter systemic circulation

26
Q

What are the advantages of Enteral - Sublingual, Buccal & Oral spray administration/exposure of drugs?

if you can know at least 5, ill be proud of you <3

A
  • rapid absorption (emergency treatment)
  • avoids first pass metabolism
  • avoids digestive enzymes + gastric acidity
  • excess drug can be removed from mouth
  • non-invasive
  • convenient, economical
27
Q

What are the disadvantages of Enteral - Sublingual, Buccal & Oral spray administration/exposure of drugs?

if you can know at least 5, ill be proud of you <3

A
  • easy access for toxins
  • uncommon
  • only small doses
  • can’t use for drugs causing vasoconstriction of mucosa
  • repeated exposure can damage oral mucosa
  • can irritate oral mucosa
  • unpleasant taste
  • patient may not comply
  • no effects if swallowed
28
Q

Position in rectum influences drug absorption. While the superior rectal vein drains into the _______ circulation into the _____, the middle and lower vein drains into the _______ vena cava to the _____.

A

portal; liver

inferior; heart

29
Q

What are the advantages of Enteral - Rectal administration/exposure of drugs?

if you can know at least 5, ill be proud of you <3

A
  • useful when oral administration is impractical (unable to swallow, coma, prior to x-rays, children, elderly, etc)
  • antiemetics; used when other drug induces vomiting/irritates stomach
  • excess drug can be removed
  • can partially avoid first pass metabolism
  • avoids GI enzymes and pH
30
Q

What are the disadvantages of Enteral - Rectal administration/exposure of drugs?

if you can know at least 5, ill be proud of you <3

A
  • patient preferences
  • absorption is imperfect and unpredictable (don’t know which blood supply drug gonna go to)
  • degree of metabolism variable
  • repeated exposure can damage rectal mucosa
  • can irritate rectal mucosa
  • unsure patient compliance
31
Q

What is Parenteral - Intravenous (iv)?

A

Injection of drug directly into the circulation. It bypasses 1st pass metabolism and absorption and is the FASTEST ROUTE OF SYSTEMIC DELIVERY.

32
Q

What are the advantages of parenteral - intravenous (iv)?

if you know 5, ill be proud of you <3

A
  • precise and accurate
  • immediate onset of action (EMERGENCY situations)
  • can be controlled + adjusted
  • useful for comatose/unconscious organisms
  • can be used if drug induces vomitting/irritates stomach
  • avoids first pass & GI tract
  • assures patient compliance
33
Q

What are the disadvantages of parenteral - intravenous (iv)?

if you know 5, ill be proud of you <3

A
  • greater risk of adverse effects + discomfort/fear
  • high conc. attained rapidly
  • irreversible
  • elevated risk of addition
  • local irritation
  • risk of air emboli or particulate material
  • pH must match body fluids
  • limited volume to avoid phlebitis (blood clot), pain and necrosis (death of tissue)
  • skilled personnel and must be sterile because of risk of infection = expensive
  • limited types of formulations
34
Q

(T/F) IV offers highest peak drug concentrations (Tmax) to bloodstream.

A

True!

35
Q

Match the following parenteral administrations to their definitions:

1) Intramuscular
2) Subcutaneous
3) Intraperitonial
4) Intra-articular
5) Intravenous
6) Intraosseous
7) Intracardiac

A. substance injected into fatty acids below the skin (rich blood supply, fewer nerves)
B. substance injected directly into the circulation
C. substance injected into the heart muscle. e.g. adrenaline for heroin overdose. VERY risky
D. substance injected into the bone marrow.
infusion into cavity rapidly enters circulation via extensive network of sinusoidal capillaries. Used in LIFE SUPPORT
E. substance injected into the peritoneum (body cavity); frequent use in animals when IV isn’t possible
F. substance injected deep between the layers of large skeletal muscles with lots of capillaries (rich blood supply, fewer nerves)
G. substance injected into the joint to treat inflammation/pain in the joint

A

Intramuscular - substance injected deep between the layers of large skeletal muscles with lots of capillaries (rich blood supply, fewer nerves)

Subcutaneous - substance injected into fatty acids below the skin (rich blood supply, fewer nerves)

Intraperitonial - substance injected into the peritoneum (body cavity); frequent use in animals when IV isn’t possible

Intra-articular - substance injected into the joint to treat inflammation/pain in the joint

Intravenous - substance injected directly into the circulation

Intraosseous - substance injected into the bone marrow.
infusion into cavity rapidly enters circulation via extensive network of sinusoidal capillaries. Used in LIFE SUPPORT

Intracardiac - substance injected into the heart muscle. e.g. adrenaline for heroin overdose. VERY risky

36
Q

What are the two types of preparations used for intramuscular? What is the difference between the two in regards to absorbtion?

A

AQUEOUS and DEPOT preparations.

Absorption from aqueous solution is VERY FAST. There is a rapid diffusion through extracellular fluids and capillary endothelium to circulation.

Absorption from depot preparations is SLOW. Non-aqueous vehicle diffuses out of muscle, leaving drug to precipitate at site of injection, where the drug dissolves slowly. Sustained-release formulations.

37
Q

What are the intramuscular injection sites for children?

A
  1. Vastus lateralis muscle
  2. Deltoid muscle
38
Q

What are the intramuscular injection sites for adults?

A
  1. Deltoid muscle
  2. Buttock
  3. Anterolateral thigh (fastest absorption site cos biggest)
39
Q

What are the advantages of parenteral - intramuscular (im)?

if you know 5, ill be proud of you <3

A
  • rapid onset of actions
  • more predictable than po route
  • more convenient than iv route (slower onset/practical outside of clinics)
  • can rotate between injection sites to reduce irritation
  • can be used when drug induces vomiting or irritates stomach
  • avoids first pass & GI tract
  • assures patient compliance when not self administered
  • route of choice in animals
40
Q

What are the disadvantages of parenteral - intramuscular (im)?

if you know 5, ill be proud of you <3

A
  • only small volumes (<3 mL)
  • risk of improper disposition in nerve, vasculature, fat, or connective tissue
  • not suitable for emergency situations
  • local irritation
  • risk of air emboli or particulate materials
  • pH must match body fluids
  • skilled personnel and must be sterile because of risk of infection = expensive
41
Q

Parenteral - Subcutaneous has similar pros and cons to Parenteral - Intramuscular. What are some pros and cons differ from im?

A

-slower absorption and distribution.
-it also requires absorption but because there is less blood supply and greater innervation, it is more painful.
-limited to a very small volume (<1.5mL)
-subcutaneous is not always injections
-very suitable for depot preparations

42
Q

What are the advantages of parenteral - intraperitonial (ip)?

if you know 5, ill be proud of you <3

A
  • rapid absorption and onset of action
  • large volume can be injected
  • can be used when drug induces vomiting or irritates stomach
  • avoids first pass and GI tract
  • route of choice in research animals
43
Q

What are the disadvantages of parenteral - intraperitonial (ip)?

if you know 5, ill be proud of you <3

A
  • irritant substances can cause peritonitis (inflammation of the peritoneum)
  • risk of improper disposition into or puncturing of GI and abdominal organs
  • other risks associated with needles; must be sterile, skilled personnel, expensive, etc.
44
Q

What is commonly used to treat arthritis?

What is its duration of action inversely proportion to?

A

Anti-inflammatory steroids such as CORTICOSTEROIDS through intra-articular injection.

Solubility

45
Q

What are the advantages of parenteral - intra-articular?

A
  • direct local administration
  • avoids first pass and GI tract
  • well establish with low risk of serious effects
46
Q

What are the disadvantages of parenteral - intra-articular?

A
  • required advanced technical skill
  • risk of damage to articular cartilage and joint
  • other risks associated with needles
47
Q

Epidural injection, a highly PAINFUL, RISKY + INVASIVE method of parenteral administration, injects substance into the ______ space. This space is between the ________ and ______ sac, which surrounds the ______ cord.

A

epidural

vertebrae; dural sac

spinal

48
Q

What are the three primarily systemic routes of parenteral administration?

A
  1. Intravenous
  2. Intramuscular
  3. Subcutaneous
49
Q

Match the following non-injecting parenteral methods of administration with their definitions:

  1. Inhalation
  2. Intranasal
  3. Topical

A. drugs sprayed into the nostrils which can hold up to 20 mL of volume of liquid, gas and aerosols. Rich blood supply and rapid absorption. Nasal mucosa more permeable than GI mucosa.
B. drug goes from MOUTH TO LUNGS. It is dispersed across extensive respiratory tract mucous membranes and pulmonary epithelium with a larger SA and rich blood supply.
C. drugs applied or sprayed or dropped in external body surfaces. Transdermal circulation delivers to systemic circulation at a pre-determined and controlled rate. Absorption proportion to lipid solubility of drugs.

A

Inhalation - drug goes from MOUTH TO LUNGS. It is dispersed across extensive respiratory tract mucous membranes and pulmonary epithelium with a larger SA and rich blood supply.

Intranasal - drugs sprayed into the nostrils which can hold up to 20 mL of volume of liquid, gas and aerosols. Rich blood supply and rapid absorption. Nasal mucosa more permeable than GI mucosa.

Topical - drugs applied or sprayed or dropped in external body surfaces. Transdermal circulation delivers to systemic circulation at a pre-determined and controlled rate. Absorption proportion to lipid solubility of drugs (hydrophilic substances poorly absorbed).

50
Q

What are the advantages of parenteral - inhalation?

A
  • rapid absorption and systemic circulation
  • 7-10 seconds to reach the brain
  • almost as fast as iv
  • convenient
  • non invasive
  • very good for local pulmonary delivery
  • avoids first pass metabolism
  • avoids GI enzymes and pH –> stability
51
Q

What are the disadvantages of parenteral - inhalation?

*also similar to intranasal

A
  • if substance not absorbed and deposited, mechanism of toxicity
  • easy access for toxins
  • irreversible
  • difficult to regulate amount delivered
  • elevated risk of addiction
  • can irritate pulmonary mucosa
  • can have unpleasant taste
  • relatively uncommon
  • limited formulations
52
Q

What are the advantages of parenteral - transdermal?

A
  • convenient
  • self administration, compliance
  • stable plasma concentration
  • non-invasive
  • allows removal of source
  • effective for substances with: short half-life, narrow therapeutic window, and poor oral bioavailability
  • avoids first pass metabolism
  • avoids GI enzymes and pH –> stability
  • emerging technologies
53
Q

What are the disadvantages of parenteral - transdermal?

A
  • poor diffusion of large and lipophilic compounds
  • can irritate skin and mucosa
  • crystallization can lead to local toxicity
  • systemic side effects
54
Q

(T/F) Intranasal, Inhalation, and Ophthalmic are also considered topical routes of parenteral administration.

A

True!