Pharmacology L4

Question 1

How do drugs reach their target tissue

Answer 1

Through the blood

Question 2

What are the general routes of drug administration

Answer 2

! Oral
! Intravenous
! Intra-arterial
! Intramuscular
! Subcutaneous
! Inhalation
! Topical
! Sublingual
! Buccal
! Rectal

Question 3

What is ‘First-Pass Hepatic Elimination’

Answer 3

a pass through the liver, which may cause an
inactivation of the drug via biotransformation

Question 4

What is the time course of drug concentation

Answer 4

Initially, drug conc is at its highest but it starts to decrease as time goes

Question 5

Time course of drug concentration consists of:

Answer 5

-absorption
-distribution
-elimination

Question 6

Absorption

Answer 6

Uptake from stomach and intestines into blood

Question 7

Distribution(α-phase)

Answer 7

Systemic distribution into body tissues

Question 8

Elimination (β-phase)

Answer 8

Elimination from body by biotransformation and excretion

Question 9

External and internal barriers of the body to drug absorption

Answer 9

GI-tract barrier
Respiratory tract barrier
Oral mucosa barrier
Skin barrier
Blood-brain barrier

Question 10

GI tract barrier

Answer 10

The intestinal epithelium with brush border serves as a barrier for orally administered drugs. The brush border contains microvilli that increase the surface area for absorption of nutrients and drugs.

Question 11

Respiratory tract barrier

Answer 11

Cilia-bearing epithelium in the respiratory tract helps trap foreign particles and prevent them from entering the lungs

Question 12

Oral mucosa barrier

Answer 12

The non-keratinized squamous epithelium lining the oral cavity provides a barrier for sublingual and buccal drug administration.

Question 13

Skin barrier

Answer 13

The keratinized squamous epithelium in the skin provides a barrier for transdermal drug delivery

Question 14

Blood-brain barrier

Answer 14

The pore-lacking CNS endothelia in the blood-brain barrier helps protect the brain from harmful substances.

Question 15

Drugs may traverse biomembranes by

Answer 15

• Gradient diffusion
• Carrier transport
• Vessicular transport
• Surface receptor

Question 16

What is gradient diffusion used for

Answer 16

For lipophilic not hydrophilic substances

Question 17

How does gradient diffusion occur

Answer 17

• Diffusion (passive transport)
• Facilitated diffusion (passive transport)
• Active transport

Question 18

Diffusion (passive transport)

Answer 18

Is the movement of a solute down a gradient. A transport protein is not needed

Question 19

Facilitated diffusion (passive transport)

Answer 19

is movement down a gradient with the aid of a transport protein

Question 20

Active transport

Answer 20

movement against a gradient with the aid of a transport protein

Question 21

Membrane-associated proteins as drug targets

Answer 21

• integral receptor protein
• ion channel protein
• ion pump protein

Question 22

Carrier-mediated transport through membranes occur by

Answer 22

transporter proteins

Question 23

What are transporter proteins

Answer 23

specialized proteins found in the cell membrane that are responsible for transporting drugs into and out of the cell. Transporter proteins function by binding a solute on one side of the membrane and undergoing a conformational change that allows the molecule or ion to be transported across the membrane to the other side.

Question 24

Types of transporter proteins

Answer 24

-uniporter
-symporter
-antiporter

Question 25

Uniporter

Answer 25

These transporter proteins transport a single solute in one direction across the membrane

Question 26

Symporter

Answer 26

transport two or more solutes in the same direction across the membrane.

Question 27

Antiporter

Answer 27

transport two or more solutes in opposite directions across the membrane.

Question 28

Receptor-mediated endocytosis

Answer 28

Receptor-mediated endocytosis is a process by which cells take up specific molecules from the extracellular fluid by binding to receptors on the cell surface and transporting them into the cell.

Question 29

Why is drug binding to plasma proteins like albumin important

Answer 29

since the concentration of the free drug determines the intensity of the pharmacological effect

Question 30

Depending on the particular physicochemical properties of a drug, the distribution of a pharmacological substance will be restricted to the:

Answer 30

-Vasculature Blood -Extracellular spaces -Intracellular spaces -Tissue receptors

Question 31

What is biotransformation

Answer 31

a protective mechanism of the body to promote the efficient removal of potentially harmful substances

Question 32

How can biotransformation affect a drug negatively

Answer 32

chemical modification of xenobiotic substances may also cause a loss of pharmacological potency or biological function of a drug.

Question 33

Phase I biotransformation reactions

Answer 33

Oxidation; Reduction; Alkylation; Hydrolytic cleavage

Question 34

Phase II biotransformation reactions

Answer 34

Conjugation reactions with glucoronic acid or sulfuric acid

Question 35

Excretory kidney function

Answer 35

The chemical derivatives of drugs or chemically unchanged drugs are eliminated in the urine. drugs with a molecular mass of less than 5,000 Da pass through the vascular walls of the glomerular capillaries.