Pharmacokinetics and Pharmacodynamics

Question 1

Pharmacokinetics

Answer 1

This is what the body does to the drug. ADME is an acronym that sums up the main focal points in PK

Question 2

Explain ADME

Answer 2

Administration: This part focuses on the passage of drug from its site of ingestion to the blood stream
Distribution: This focuses on how the drug distributes throughout our vascular system to site of action/intracellular fluid.
Metabolism: digestion of the drug
Excretion

Question 3

Pharmacodynamics

Answer 3

Pays attention to what the drug does to the body

Question 4

What are the most common types of drug receptor bonds?

Answer 4

ionic, hydrophobic, van der waal bonds because they are weak bonds and are reversible, which are the most common types of drug-receptor interactions

Question 5

What does the mechanism of bonding look like?

Answer 5

it will resemble a lock and key relationship because a drug will bind only to certain types of receptors depending on if it is the appropriate shape that will fit the receptor shape.

After the drug is bound, a signaling cascade is triggered and the biological response will commence.

Question 6

What needs to happen in order for there to be a successful drug receptor bond?

Answer 6

1. The drug needs to be given at an appropriate concentration
2. The proper biological fit
3. Chemical specificity and enantiomers

Question 7

Affinity

Answer 7

The strength of the D-R interaction

Question 8

Emax aka Efficacy

Answer 8

this is the max effect a drug illicit

Question 9

EC50 aka potency

Answer 9

the drug concentration that will illicit half of the max effect

Question 10

Agonists

Answer 10

These are drugs that enhance or mimic the actions of endogenous compound

Question 11

Types of Agonists

Answer 11

Full Agonist: this will bound to all the Rs and illicit the max expected effect
Partial agonist: They will bind to all the Rs but only illicit half the effect
positive allosteric modulator: enhance the effects of endogenous compounds and they have their own binding site that is not where the endogenous compound binds. The key for them is that they enhance the effects but at a lower dosage

Question 12

Explain how the positive allosteric modulator binds to the receptor

Answer 12

They will bind to a completely different site than the endogenous ligand spot

Question 13

What is the effect of the positive allosteric modulator on the response curve?

Answer 13

it will shift the response curve to the left because the entire point of positive allosteric modulators is that they illicit more of a response at lower dosages

Question 14

Antagonists

Answer 14

These are drugs that inhibit the actions of endogenous compounds by interrupting or preventing the biological signalling cascade from being triggered

Question 15

Types of Antagonists

Answer 15

Pharmalogical: drug that will block the binding of D-R interaction
Chemical: 2 compounds that interact to prevent the effect of an active drug
Physiological: Interaction of two drugs with opposing effects

Question 16

Competitive Antagonist

Answer 16

• antagonist that will compete against a ligand or an agonist for the receptor binding site so it physically stops the signalling cascade taking the spot of the drug.

Question 17

What can overcome a competitive antagonist?

Answer 17

the addition of Ag and this will cause a rightward shift in the dose curve because in order to illicit the same effect, you require more of the dose to be present

Question 18

Non-competitive Antagonist

Answer 18

These are negative allosteric modulators and they will bind to a site unique to the D-R spot.
and may involve irreversible covalent bonding

Question 19

What will non-competitive antagonists impact

Answer 19

It will cause a decrease in the EC50 (potency) and Emax (efficacy) because the drug’s natural effect will be hindered because regardless of the dosage, it will be able to illicit a strong enough effect

Question 20

What is the difference between Antagonists and blockers/inhibiters

Answer 20

Antagonists only involve drugs acting on receptors

inhibiters and blockers can be drugs that act via other methods (transporters/inhibiting enzymes) or they can be antagonists at receptors