Pharmacokinetics: Drug ABSORPTION Flashcards

(59 cards)

1
Q

What is Pharmacology?

A
  • Science of chemicals (Drugs) that interact with the body
  • Biochemical/physiological effects on cells, tissues + organs
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2
Q

What are the 2 parts/principles of Pharmacology

A
  1. Pharmacokinetics
  2. Pharmacodynamics
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3
Q

Explain the difference between Pharmacokinetics & Pharmacodynamics

A
  1. Pharmacokinetics = What the body does to the drug, with time
  2. Pharmacodynamics = What the drug does to the body
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4
Q

What do the MADE principles stand for in Pharmacokinetics?

A
  • M = Metabolism
  • A = Absorption
  • D = Distrubution
  • E = Excretion
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5
Q

Does Pharmacodynamics have a dose-response relationship, or Pharmacokinetics?

A

Pharmacodynamics

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6
Q

What is the Mechanism of Action, when talking about Pharmacodynamics?

A

How drugs interact with:
1. Receptors
1. Enzymes
1. Cellular targets
To produce their biological effects

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7
Q

11 basic steps..

Basic stuff.

List the general way that an oral drug would go through the body, from mouth > anus.

A
  1. Mouth/oral cavity
  2. Oesophagus
  3. Stomach
  4. Small Intestine
  5. Muscosal lining
  6. Bloodstream
  7. Large Intestine
  8. Kidneys
  9. Colon
  10. Rectum
  11. Anus
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8
Q

What is drug absorption?

A
  1. How the drug reaches the circulation
  2. From point of entry
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9
Q

What is the method that most drugs diffuse across membranes + travel around the body?

A

Passive diffusion

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10
Q

Why do IV drugs avoid the absorption process?

A
  1. Because their point of entry is directly into the bloodstream
  2. So don’t require absorption!
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11
Q

Is Passive diffusion from a high > low concentration gradient or low > high?

A
  • High > low concentration gradient
  • Because it takes more effort to go from low > high = requiring active transport/energy

  • Adam says to think about Febreeze air freshners!
  • As they come from a compacted tight cynlinder, almost urging to come out!
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12
Q

Why do drugs that are administered subcutaneously take longer to be absorbed by the body, than IM?

A

Because IM is more vascular than SC!

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13
Q

7 ..

How are IM drugs absorbed?

A
  1. Absorbed into muscles >
  2. Tissues >
  3. Intracellular compartments >
  4. Extracellular compartments >
  5. Interstital fluid >
  6. Capillaries >
  7. Veins
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14
Q

Most drugs are absorped + distrubuted around the body using Passive diffusion.

What is Passive diffusion?

A
  1. The passing of chemicals/drugs from a High > low concentration gradient
  2. Through a lipid layer of the cell
  3. So the drug has to be either Lipid-soluble or Lipophilic!
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15
Q

Why should IM drugs be more water-soluble than lipid-soluble?

A
  • Because water-soluble drugs are easier to pass through the muscular natural barriers
  • Whereas lipid-soluble is harder
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16
Q

Does Passive transport/diffusion require lipid-soluble or water-soluble drugs?

A
  • Lipid-soluble
  • Due to their lipid membranes
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17
Q

Describe the difference between Hydrophobic v Hydrophilic Phospholipid bi-layer membranes in Simple, Facilitated + Active transport systems.

In very basic terms!

A
  • Hydrophobic = Hate water, so they repell it
  • Hydrophilic = Love water, so they attract it
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18
Q

The phospholipid bi layer of the cell has 2 sides, one is Hydrophilic + the other is Hydrophobic.

Are they either:

A) Hydrophilic outside of the cell + Hydrophobic **inside the cell.
OR
B) Hydro
phobic** outside of the cell + Hydrophilic inside the cell.

A

B) Hydrophobic outside of the cell + Hydrophilic inside the cell.

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19
Q

Name the 4 types of Ions, that pass through channels

A
  1. Hydrogen
  2. Potassium
  3. Chloride
  4. Calcium
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20
Q

What do Calcium ions do?

A

Activate myosin in the muscle fibres

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21
Q

Do Ion channels have selective pores on the cell membranes?

A

Yes

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22
Q

What do Ion channels do?

A
  1. They allow the ready transfer of ions
  2. Down their ELECTRO-CHEMICAL gradients
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23
Q

Name the 2 types of Ion channels

A
  1. Voltage gated (De-polarising)
  2. Ligand gated (Polarising)
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24
Q

Which are de-polarising + which aren’t?

A) Ligand gated Ion channels
B) Voltage gated Ion channels

A
  1. Ligand gated ion channels = de-polarising
  2. Voltage gated ion channels = polarising
25
If **Ligand** gated Ion channels are **polarising**, which do they have to do to open?
**Bind** with a ***specific*** Ligand
26
If **Voltage** gated Ion channels are **de-polarising**, which do they have to do to open?
1. They have to **reach** their specific membrane **voltage** potential/**threshold** 3. Reaching de-polarisation 4. Then opens
27
What **type** of **gate** does this Ion channel have?
**Voltage** gated
28
What **type** of **gate** does this Ion channel have?
**Ligand** gated
29
Is this Ligand or an Voltage gated Ion channel?
Voltage gated
30
Is this Ligand or an Voltage gated Ion channel?
Ligand gated
31
Is there **more** Sodium or Potassium on the outside of a **Ligand**-gated Ion channel?
1. More **Sodium** on **outside** 2. More **Potassium** on **Inside**
32
Why is there ***more*** **Sodium** on the outside of the cell, than **Potassium**? (In Ligand gated Ion channels)
1. Beause **Sodium** (Na+) is **more postively charged** 1. Than Potassium (K+) 2. Due to the ***Sodium-Potassium pump*** 3. To **maintain** a **membrane potential** 4. Creating a rapid membrane potential
33
Where can you find Ligand-gated Ion channels?
At **Neuromuscular** ***junctions***
34
What is **Active** Transport?
1. **Transfer** of substances **AGAINST** their **concentration gradients** 2. From **Low** > high 3. Utilising ***special carrier molecules***, in the membrane 4. Requiring **ATP** (energy)
35
Name an example of Active Transport
Sodium-Potassium pump
36
Name the most common pump that uses Active Transport
Sodium pump
37
What is this?
The Sodium pump
38
What **type** of **pump** do ***Local Anaesthetics*** use to block painfull nerve transmissions?
The Sodium pump!
39
What is **Bioavailability**?
* The **proportion** of administered drug * **Reaching** the ***Systemic circulation***
40
What is the **%** of **Bioavailability** following an **IV** injection?
**100**%
41
What **type** of **coating** on tablets/capsules **increases** bioavailability?
**Enteric** coatings
42
True or False. When a drug is given orally, the proportion of the dose reaching the systemic circulation increases with different drugs and from animal to animal.
False. When a drug is given orally, the proportion of the dose reaching the systemic circulation **varies** with different drugs and from animal to animal.
43
What **bodily factor** can **affect** the **absorption** of drugs, when administering to that area?
1. **Blood** **supply**! 2. The ***higher*** the blood supply, the ***quicker*** it works
44
Name the **6** factors that affect **Oral** drug **absorption**
1. Drug **formulation** *(**Hydro**philic/**Lipo**philic v **Ionised**/**Non**-ionised)* 2. **Stability** to ***acid*** + ***enzymes*** 3. **GUT MOTLITY** 4. **Food** in the stomach 5. **DEGREE** of **1st**-**PASS** metabolism 6. **Health** status *(CV, GI or Hepatic)*
45
What **type** of **Ion** ***channels*** are associated with terms '***Hydrophilic***' + '***Lipophilic***'?
* **Ligand** gated Ion channels * *Ligand = Lipid = Passive diffusion*
46
What **type** of **Ion** ***channels*** are associated with terms '***Ionised***' + '***Non-Ionised***'?
* **Voltage** gated Ion channels * *(Voltage = Polarisation = Active transport)*
47
What does **Ionised** mean?
The substance has a an **electrical charge**
48
Can charged/Ionised substances pass the Postassium-Sodium pump?
No
49
What does **taking away** an electron do to a substance?
Makes it **postively** charged
50
What does **adding** an electron do to a substance?
Make it **negatively** charged
51
Why would ***gut motility*** affect the **rate** at which a drug is **absorbed** into the body? For example, a Bunny with Ileus, who has recieved oral medication?
1. The Bunny will not move due to the **pain** + ileus = **reduced or absent** gut motility 2. Drugs **stay longer in SI**, **not** being ***distrubuted***, ***dissolved*** or ***absorbed*** 3. ***Reducing*** circulating **drug blood levels**, possible ***degrading*** the **drug** 2. Causing little to **no peristalsis** 3. **Halting** gut motility + **blood flow**
52
If there is a **high % degree** of **first-pass metabolism** when administering an **oral** drug, what affect will this have?
* Might **not reach** the ***target organ*** * As **high %** = ***large portion*** of the drug is ***metabolised*** by the **Liver** * ***Before reaching*** the ***Systemic circulation*** * ***Reducing*** the drug's ***bioavailability*** * Occurs after **oral** admin, where absorbed drug > **Hepatic portal vein > Liver**
53
What is **First-pass** metabolism?
1. When a ***large portion*** of the drug is **EXTENSIVELY** ***metabolised*** by the **Liver** 1. ***Before reaching*** the ***Systemic circulation*** 1. ***Reducing*** the drug's **bioavailability** 1. Usually occuring after **oral** admin, where absorbed drug > **Hepatic portal vein > Liver**
54
Describe the **5** stages of Oral absorption of drugs
1. Mouth > **SI** for ***absorption*** 2. Passing **across** **GI** ***mucosa*** 3. Entering **Hepatic Portal circulation** 4. To Liver 5. Where the **First-Pass** effect occurs
55
What is this?
The **Hepatic Portal Vein** System
56
Why are **lipid soluble** drugs **absorbed across** the **SI** ***mucosa*** more rapidly?
1. Passive diffusion 2. **High surface area**
57
How can **food in the stomach** be beneficial to drug **absorption**?
Because it can **protect** the drug from **extensive** drug **breakdown**
58
How might the following **effect** the **bioavailability** of a drug? A) V+ B) Poor Liver function
A) **V+** = **Can't absorb** drug, as can't reach stomach > SI > to enter Hepatic portal vein circulation > for metabolism B) **Poor Liver function** = **Can't metabolise** the drug + more at risk of an ***overdose***
59
Why do **Water-soluble** parenteral drugs work **faster**?
* Beause they **don't** have to **cross membranes** * They can mix with the bodily fluids, causing rapid absorption around the body