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Pharm 2060 > Module 2 > Flashcards

Module 2 Flashcards

1
Q

Pharmacokinetics

A

The study of drug movement in the body and what the body does to the drug

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2
Q

Four basic processes of pharmacokinetics

A

ADME: Absorption, Distribution, Metabolism, Excretion

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3
Q

Drug Absorption

A

The movement of the drug from the site of administration into the blood. Determines how intense the effect of the drug will be.

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4
Q

Rate of Absorption

A

Determines how quickly the drug effect will occur

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5
Q

6 Factors affecting absorption

A
  1. ) Rate of Dissolution
  2. ) Surface Area
  3. ) Blood Flow
  4. ) Lipid Solubility
  5. ) pH Partitioning
  6. ) Activity of Drug Transport Proteins
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6
Q

What is the effect on absorption for a drug with a fast rate of dissolution?

A

A drug with a fast rate of dissolution will have a faster onset of action than drugs with slow dissolution.

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7
Q

What is the major determinant for drug absorption?

A

Surface area

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8
Q

True or False: The larger the surface area, the faster the drug absorption is.

A

True

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9
Q

Which has greater surface area and why: Stomach or Small Intestine.

A

Stomach has folds called rugae while the small intestine has thousands of finger like projections called villi. The villi that line the intestine increase the surface area. So thus, the small intestine has a MUCH larger surface area then the stomach.

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10
Q

True or False: drug absorption is fastest in areas with low blood flow

A

False. Drug absorption is fastest in areas with HIGH blood flow. High blood flow helps to maintain a concentration gradient which drives absorption

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11
Q

How can blood flow be increased?

A

Exercise

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12
Q

How is blood flow decreased?

A

Heart failure, severe hypotension, hypothermia and circulatory shock

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13
Q

Drugs with _______ lipid solubility are absorbed ______ rapidly than water soluble drugs

A

High… More…

- Lipophilic drugs are able to cross the cell membrane whereas hydrophilic drugs can’t.

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14
Q

In regards to pH, when is drug absorption greatest?

A

Drug absorption is greatest when there is a difference between the pH at the site of administration and the blood such that the drug is ionized in the blood (prefers ionized state)

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15
Q

True or False: the activity of transport proteins do not play a role in drug absorption

A

False. Uptake drug transporters increase the absorption of drugs while efflux drug transporters decrease the absorption of drugs

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16
Q

What are the 8 major routes of drug administration?

A
  1. ) Oral (PO = “per os” which is latin for “by mouth”)
  2. ) Sublingual
  3. ) Transdermal
  4. ) Rectal
  5. ) Intravenous (IV)
  6. ) Subcutaneous (SubQ or SC)
  7. ) Intramuscular (IM)
  8. ) Pulmonary
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17
Q

Enteral Administration

A

Routes of administration involving the gastrointestinal tract

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18
Q

Parenteral Administration

A

Routes of administration that do not involve the gastrointestinal tract

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19
Q

Types of Enteral Administration

A

Oral, Rectal

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20
Q

Types of Parenteral Administration

A

Intravenous, Intramuscular, Subcutaneous

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21
Q

Types of “Other” Administration

A

Sublingual, Transdermal, Pulmonary

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22
Q

Is drug absorption greater in the intestine or the stomach?

A

Drug absorption is greater in the intestine

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23
Q

Drugs that are weak acids are best absorbed where?

A

In the intestine due to greater surface area. Even though the pH effects favour the acidic environment of the stomach, the small surface area makes the drug absorption poorer.

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24
Q

Besides a poor surface area, what other characteristic of the stomach results in poor drug absorption?

A

The stomach is covered with a thick layer of mucous which lessens drug absorption in the stomach.

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25
Q

When does the pharmaceutical phase occur?

A

After the patient swallows a tablet

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26
Q

Pharmaceutical Phase includes two different phases…

A

Disintegration Phase/Dissolution Phase

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27
Q

What happens if a drug does not fully disintegrate?

A

The absorption of the drug is reduced

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28
Q

Disintegration Phase includes…

A

Tablet -> Granules -> Smaller particles

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29
Q

Dissolution Phase includes…

A

Drug particles dissolve into gastric fluid

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30
Q

Gastric Emptying

A

The movement of the stomach contents into the intestine

31
Q

How does gastric emptying effect drug absorption?

A

Increased gastric emptying increases the rate of drug absorption

32
Q

Factors that increase gastric emptying:

A
  1. ) Taking medications on an empty stomach
  2. ) Taking medications with cold water
  3. ) Lying down on the right side
  4. ) High osmolality feeding (tube feeding)
  5. ) Taking a pro kinetic drug (a drug that increases GI motility)
33
Q

Factors that decrease gastric emptying:

A
  1. ) High fat meal
  2. ) Heavy exercise
  3. ) Lying down on the left side
  4. ) Taking a drug that inhibits the vagus nerve (ie. anticholinergic drugs)
34
Q

Enteric Coating

A

Drugs that are covered with a special coating that prevents their dissolution in the acidic environment of the stomach

35
Q

When does the enteric coating dissolve?

A

The coating will dissolve once the drug passes into the more alkaline duodenum

36
Q

Bioavailability

A

The fraction of a dose of drug that reaches the systemic circulation unchanged

37
Q

Bioavailability is influenced by:

A
  1. ) Drug formulation
  2. ) Route of administration
  3. ) Degree of metabolism
38
Q

List the order of bioavailable drugs from most bioavailable to least bioavailable

A
  1. ) Aqueous Solution
  2. ) Syrup
  3. ) Suspension
  4. ) Chewable Tablet
  5. ) Granules
  6. ) Capsules
  7. ) Compressed Tablet
  8. ) Enteric Coated Tablets
  9. ) Time Release Capsules
39
Q

Where is a sublingual drug administered?

A

Under the tongue

40
Q

Sublingual Absorption

A

The drug dissolves and is absorbed across the oral mucous. Venus drainage from the oral mucous is to the superior vena cave. Superior vena cava takes blood to the heart.

41
Q

What pathway do sublingual drugs avoid?

A

First pass metabolism through the liver

42
Q

What conditions must sublingual drugs have in order to be absorbed?

A

They must be lipophilic and uncharged

43
Q

Transdermal Administration

A

Drugs that penetrate the skin in forms of patches and creams

44
Q

True or False: all drugs can penetrate the skin.

A

FALSE! Not all drugs can penetrate through the skin.

45
Q

What does the epidermis provide to the skin?

A

A lipid barrier, preventing certain drugs from entering through the skin

46
Q

What drug characteristic allows drugs to penetrate the skin?

A

Drugs must be lipophillic to pass the lipid barrier

47
Q

Transdermal drugs must also be _______ in order to dissolve in the extracellular fluid.

A

Hypophilic. This allows them to move into the extracellular fluid which is mostly water!

48
Q

Transdermal Administration comes in the form of…

A

Patches, Ointments, Sprays or Lotions

49
Q

How is tolerance to transdermal drugs avoided?

A

Drug-free periods are enforced. Typically patches are removed 6-10 hours a day.

50
Q

5 Factors affecting transdermal absorption

A
  1. ) Thickness of Skin (absorption = 1/thickness)
  2. ) Hydration (absorption increased with increasing hydration of skin)
  3. ) Hair follicles (high number of hair follicles = better absorption due to the passing of barrier function in the epidermis)
  4. ) Application Area (surface area bigger, more absorption)
  5. ) Integrity of the Barrier (broken/cut skin = more absorption)
51
Q

When is Rectal Administration useful?

A

When the patient is unconscious or vomiting

52
Q

What percentage of rectally administered drugs bypass the liver?

A

50%

53
Q

Where is the drug administered?

A

The rectum, but more specifically the drug is inserted into the rectum as a suppository. This suppository dissolves and the drug crosses the rectal mucosa into the blood.

54
Q

What is the disadvantage of rectal administration?

A

Incomplete absorption as well as irritation of the rectal mucosa

55
Q

Intravenous drugs are administered by…

A

Injecting the drug directly into a peripheral vein

56
Q

Most commonly used veins for IV administration…

A

Back of the hand & the median cubital vein at the elbow

57
Q

2 ways an IV drug can be given to a patient:

A

Bolus & IV Drip

58
Q

IV Bolus

A

A single dose is administered over a short period of time (think needle)

59
Q

IV Drip

A

A drug is administered under continuous infusion over a prolonged period. Drugs are typically diluted in a “vehicle” such as saline in an IV bag

60
Q

Advantages of IV

A
  • No absorption barrieres (100% bioavailability)
  • Precise control of dosage
  • Can dilute low soluble drugs in a large volume
  • Irritant drugs (chemo) can be administered slowly to avoid side effects
61
Q

Disadvantages of IV

A
  • Expensive, invasive and inconvenient
  • Drug cannot be removed
  • Risk of infection and fluid overload
  • Risk of injecting wrong formulation (Mixing up with IM formulations)
62
Q

Subcutaneous Administration

A

Injected beneath the skin into the subcutaneous tissue

63
Q

What is a barrier to subcutaneous administration?

A

The capillary wall

64
Q

What type of drugs cannot be administered subcutaneously?

A

Irritant drugs. This will cause severe pain and/or tissue sloughing

65
Q

Intramuscular (IM)

A

Injected directly into muscle tissue

66
Q

Absorption of IM is dependent on…

A

The ability of the drug to pass through fenestrations in the capillary wall. Other determinants are blood flow and water solubility

67
Q

Advantages of IM

A
  1. ) Can be used for poorly soluble drugs

2. ) Can use it to administer depot preparations (drug absorption slowly over time)

68
Q

Disadvantages

A
  1. ) Pain/Discomfort

2. ) May cause local tissue and/or nerve damage if the injection is done improperly

69
Q

Factors that affect IM Absorption

A
  • Blood Flow (deltoid [shoulder] > vestus lateralis [thigh] > gluteal [ass])
  • Exercise increase blood flow, and thus absorption for IM drugs
70
Q

When is blood flow decreased?

A

Heart failure, severe hypotension and hypothermia

71
Q

Pulmonary Administration

A

Gaseous and volatile drugs can be inhaled and absorbed into the blood through the pulmonary epithelium

72
Q

Why is pulmonary administration very rapid?

A

This is due to the large surface area of the lung

73
Q

Examples of pulmonary drugs

A

Asthma inhaler, general anaesthetics, etc.

Pharm 2060 (5 decks)

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