Pharmacokinetics Questions Quiz! Trivia Test

2.

Which of the following are parenteral methods of administration (the others being enteral)?

Oral
Subcutaneous
Sublingual
Buccal
Intramuscular
Rectal
Intravenous
Intrathecal

Correct Answer(s)

A. Subcutaneous
A. Intramuscular
A. Intravenous
A. Intrathecal

Explanation

Enteral- via the gastrointestinal tract
Sublingual- under tongue
Buccal- under cheek
Rectal- where someone is vomiting, where a compound is volatile in the stomach (e.g. penicillin), less likely to be broken down, can be absorbed easily
Parenteral- Administered in some way other than by the gastrointestinal tract
Subcutaneous- Fatty layer under skin
Intramuscular
Intravenous
Intrathecal- Though membranes in the spinal olumn

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3

3.

By definition, when a medication is administered _______, its bioavailability is 100%.

Correct Answer(s)
intravenously

Explanation
Bioavailability = Area under curve (particular route)/Area under curve (IV)

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4

4.

Which of the following can be absorbed dermally?

Nicotine
Testosterone
Oestrogen
Insulin
Fentanyl (a strong opiate to control pain in the terminally ill)
Nitroglycerine (releases NO to treat angina)
Lidocaine (local anesthetic which blocks Na+ channels)
Morphine
Clonidine (high blood pressure treatment)

Correct Answer(s)

A. Nicotine
A. Testosterone
A. Oestrogen
A. Fentanyl (a strong opiate to control pain in the terminally ill)
A. Nitroglycerine (releases NO to treat angina)
A. Lidocaine (local anesthetic which blocks Na+ channels)
A. Clonidine (high blood pressure treatment)

Explanation

All the substances listed in the answer choices can be absorbed dermally. When a substance is absorbed dermally, it means that it can be absorbed through the skin and enter the bloodstream. This route of absorption is commonly used for medications such as nicotine patches, hormone creams (testosterone and estrogen), pain medications (fentanyl and morphine), and treatments for angina (nitroglycerine) and high blood pressure (clonidine). Lidocaine is a local anesthetic that can also be absorbed dermally and used to numb an area of the skin.

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2

5.

The partition coefficient logP=____

Log([solute in octanol]/[solute in unionised water])
Log([solute in unionised water]/[solute in octanol])
Log([solute in hexane]/[solute in unionised water])
Log([solute in unionised water]/[solute in hexane])

Correct Answer

A. Log([solute in octanol]/[solute in unionised water])

Explanation

A drug's distribution coefficient strongly affects how easily the drug can reach its intended target in the body, how strong an effect it will have once it reaches its target, and how long it will remain in the body in an active form. The distribution coefficient has a strong influence on ADME properties of the drug.

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3

6.

Drugs with a higher partition coefficient...

Are better orally absorbed
May be less likely to partition out of the bilayer again
Are always more selective
Are retained in the body for longer
Are less toxic
Are often extensively metabolised

Correct Answer(s)

A. Are better orally absorbed
A. May be less likely to partition out of the bilayer again
A. Are retained in the body for longer
A. Are often extensively metabolised

Explanation

Drugs with a higher partition coefficient are better orally absorbed because they can easily cross the lipid membranes in the gastrointestinal tract. They may be less likely to partition out of the bilayer again, meaning they have a higher tendency to stay within the cell membrane and exert their effects. These drugs are also retained in the body for longer periods of time, allowing for sustained therapeutic action. Additionally, drugs with higher partition coefficients are often extensively metabolized, which can contribute to their efficacy and safety profiles.

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2

7.

What is the advantage of prodrugs?

Greater oral bioavailability
Lower toxicity
Greater specificity
Higher potency

Correct Answer

A. Greater oral bioavailability

Explanation

Prodrugs offer the advantage of greater oral bioavailability. This means that prodrugs are more easily absorbed and utilized by the body when taken orally. They undergo specific chemical modifications that enhance their ability to be absorbed through the gastrointestinal tract and enter the systemic circulation. This allows for more efficient and effective delivery of the active drug to its target site. By increasing oral bioavailability, prodrugs can improve the therapeutic efficacy of the drug and potentially reduce the required dosage.

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6

8.

Why is the bioavailability of valaciclovir greater than aciclovir?

Greater partition coefficient
Can be transported by branched chain amino acid carriers
It is a prodrug

Correct Answer

A. Can be transported by branched chain amino acid carriers

Explanation

Valaciclovir can be transported by branched chain amino acid carriers, which allows for greater bioavailability compared to aciclovir. This means that valaciclovir can be more efficiently absorbed and utilized by the body, leading to higher levels of the active drug in the bloodstream. Aciclovir, on the other hand, does not have this specific transport mechanism, resulting in lower bioavailability. Additionally, valaciclovir is a prodrug, meaning it is converted into aciclovir in the body, which further enhances its bioavailability.

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2

9.

Which one of the following Phase I reactions are most commonly carried out by Cytochrome P450 enzymes?

Oxidation/hydroxylation
Dealkylation
Deamination
Hydrolysis
Reduction

Correct Answer

A. Oxidation/hydroxylation

Explanation

Phase I reactions are catabolic and often more chemically reactive
They mainly take place on the ER of the liver

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4

10.

Which of the following groups are drugs often conjugated to in Phase II metabolism?

Glucuronyl
Sulphate
Hydroxyl
Methyl
Acetyl
Amine
Glycyl
Glutathione

Correct Answer(s)

A. Glucuronyl
A. Sulphate
A. Methyl
A. Acetyl
A. Glycyl
A. Glutathione

Explanation

Phase II metabolism involves conjugation to a hydrohillic molecule such as glucuronate, sulphate, glycine and glutathione. The resulting molecule is often pharmacologically inactive and excreted via the bile or urine

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1

11.

How is caffiene metabolised?

1-N demethyation
3-N demethylation
5-N demethylation
7-N demethylation
Hydroxylation
Conjugation

Correct Answer(s)

A. 1-N demethyation
A. 3-N demethylation
A. 7-N demethylation
A. Hydroxylation

Explanation

Caffeine is metabolized in the liver by a series of enzymatic reactions. The primary pathway involves three steps: 1-N demethylation, 3-N demethylation, and 7-N demethylation. In the first step, the methyl group attached to the nitrogen atom at position 1 is removed. Then, in the second step, the methyl group attached to the nitrogen atom at position 3 is demethylated. Finally, in the third step, the methyl group attached to the nitrogen atom at position 7 is demethylated. Additionally, caffeine can also undergo hydroxylation, where a hydroxyl group is added to the molecule. These metabolic reactions help convert caffeine into its metabolites, which can be further processed and eliminated from the body.

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1

12.

The drug C__ is a prodrug that forms an active metabolite with an exposed _ group which covalently modifies a purinergic GPCR to prevent blood clots.

Correct Answer(s)
Clopidogrel, thiol

Explanation
Clopidogrel is a prodrug that undergoes metabolic activation to form an active metabolite. This active metabolite contains a thiol group, which is an important functional group for its mechanism of action. The thiol group covalently modifies a purinergic GPCR (G-protein coupled receptor), ultimately preventing blood clots. Therefore, Clopidogrel, with its thiol group, is the correct answer for the drug that forms an active metabolite with an exposed thiol group to prevent blood clots.

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2

13.

Tyrosine is __ to give tyramine, noradrenaline and 5-HT, the amino groups on which can be removed by _ to give an aldehyde which can then be oxidised to an _. Blocking of this pathway can lead to cheese syndrome by activating the ____ pathway.

Correct Answer(s)
Decarboxylated, monoamine oxidase, acid, sympathetic

Explanation
Tyrosine undergoes decarboxylation to give tyramine, noradrenaline, and 5-HT. The amino groups on these compounds can be removed by the enzyme monoamine oxidase to give an aldehyde. This aldehyde can then be oxidized to an acid. Blocking this pathway can lead to cheese syndrome by activating the sympathetic pathway.

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14.

Alcohol levels decrease:

Linearly
Exponentially
Parabolically

Correct Answer

A. Linearly

Explanation

Alcohol is oxides first by alcohol dehydrogenase then aldehyde dehydrogenase. Methanol is oxidised to formaldehyde by alcohol dehydrogenase but is not recognised by aldehyde dehydrogenase.

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9

Pharmacokinetics Questions Quiz! Trivia Test

What does ADME stand for? A_ D_ M_ E_

Quiz Preview

Which of the following are parenteral methods of administration (the others being enteral)?

By definition, when a medication is administered _______, its bioavailability is 100%.

Which of the following can be absorbed dermally?

The partition coefficient logP=____

Drugs with a higher partition coefficient...

What is the advantage of prodrugs?

Why is the bioavailability of valaciclovir greater than aciclovir?

Which one of the following Phase I reactions are most commonly carried out by Cytochrome P450 enzymes?

Which of the following groups are drugs often conjugated to in Phase II metabolism?

How is caffiene metabolised?

The drug C__ is a prodrug that forms an active metabolite with an exposed _ group which covalently modifies a purinergic GPCR to prevent blood clots.

Tyrosine is __ to give tyramine, noradrenaline and 5-HT, the amino groups on which can be removed by _ to give an aldehyde which can then be oxidised to an _. Blocking of this pathway can lead to cheese syndrome by activating the ____ pathway.

Alcohol levels decrease:

Pharmacokinetics Questions Quiz! Trivia Test

What does ADME stand for? A___ D___ M___ E___

Quiz Preview

Which of the following are parenteral methods of administration (the others being enteral)?

By definition, when a medication is administered _______, its bioavailability is 100%.

Which of the following can be absorbed dermally?

The partition coefficient logP=____

Drugs with a higher partition coefficient...

What is the advantage of prodrugs?

Why is the bioavailability of valaciclovir greater than aciclovir?

Which one of the following Phase I reactions are most commonly carried out by Cytochrome P450 enzymes?

Which of the following groups are drugs often conjugated to in Phase II metabolism?

How is caffiene metabolised?

The drug C____ is a prodrug that forms an active metabolite with an exposed ___ group which covalently modifies a purinergic GPCR to prevent blood clots.

Tyrosine is ____ to give tyramine, noradrenaline and 5-HT, the amino groups on which can be removed by _____ ____ to give an aldehyde which can then be oxidised to an ___. Blocking of this pathway can lead to cheese syndrome by activating the ____ pathway.

Alcohol levels decrease:

What does ADME stand for? A_ D_ M_ E_

The drug C__ is a prodrug that forms an active metabolite with an exposed _ group which covalently modifies a purinergic GPCR to prevent blood clots.

Tyrosine is __ to give tyramine, noradrenaline and 5-HT, the amino groups on which can be removed by _ to give an aldehyde which can then be oxidised to an _. Blocking of this pathway can lead to cheese syndrome by activating the ____ pathway.