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PTVI > Med Chem Test 3 > Flashcards

Med Chem Test 3 Flashcards

1
Q

Which of the following are non-nicotine therapites for smoke cessation?

A. Nicorette gum

B. Bupropion (Zyban)

C. Nicotine Lozenge

D. Nicotine inhaler (Nicotrol Inhaler)

E. Nicotine Nasal Spray (Nicotrol)

F. Varenicline (Chantix)

A

B, F

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2
Q

Cigarette smoke contains more than _____ compounds

A. 4

B. 40

C, 400

D. 4000

A

D

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3
Q

Nicotine contains ___ which is responsible for inducing the enzymes 1A1, 1A2, 2E1 etc.

A. TLC

B. PAH (Polycyclic Aromatic Hydrocarbons)

C. Methamphetamines

D. Dopamine

A

B

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4
Q

What causes the addiciton in tobacco

A. Nicotine

B. Methamphetamines

C. MAO inhibitors

D. Tar

E. A and C

A

E.

MAO inhibitors in tobacco act in synergy with nicotine to induce addiction (slide text)

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5
Q

Nicotine is known as an____ that is ____ at higher pHs.

A. Acid, Ionized

B. Alkaloid (basic), unionized

C. Alkaloid (basic), ionized

D. Acid, unionized

A

B.

Nicotine has high pKa of 7.8 so at higher pHs it will remain unionized (uncharged) but at lower pHs it will become ionized (charged)

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6
Q

The red functional group in nicotine’s structure is known as a(n)____ and the blue functional group in nicotine’s structure is knonw as a(n)____.

A. Pyrrolidine, Pyridine

B. Pyrrolidine, Pyrazine

C. Pyrrolidine, Pyrimidine

E. Pyrrolidine, Furan

A

A

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7
Q

T/F Nicotine absorption is NOT pH dependent

A

F.

At basic pHs nicotine is more readily absorbed since it is unionized (uncharged) and can cross lipophilic barriers more easily into systemic circulation.

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8
Q

Nicotine is ___ bioavailable in acidic environments (lower pH) and ___ bioavailable in basic environments (higher pH).

A. More, Less

B. Less, More

A

B

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9
Q

Tobacco smoke is pH buffered and kept at a ___ pH in order to ___ absorption

A. Higher, Decrease

B. Higher, Increase

C. Lower, Decrease

D. Lower, Increase

A

B

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10
Q

Which receptors does nicotine act on?

A. Beta 1 receptors

B. Alpha 1 receptors

C. Beta 2 receptors

D. Alpha 2 receptors

E. nAChR receptors

A

E

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11
Q

In the structure of nicotine the circled group is a ___ that allows it to exist as an ___

A. Chiral, R/S isomer

B. Non-chiral, R/S isomer

A
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12
Q

When nicotine activates ____ receptors it triggers the release of ____, which ultimately leads to addiction.

A. Alpha 1, Serotonin

B. Beta 1, Dopamine (DA)

C. nAChR, Dopamine (DA)

D. nAChR, Serotonin

A

C

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13
Q

Regarding addiciton, what substance in the body is the primary reason why tobacco can become so addicting?

A. Nicotine

B. Tar

C. PAH

D. Dopamine

E. Serotonin

A

D.

Nicotine is the reason why dopamine is released in the body but dopamine release is ultimately the culprit behind the addiction. (Reward sensation)

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14
Q

Nicotine is metabolized by the enzyme _____

A. CYP1A1

B. CYP3A4

C. CYP2A6

E. UGT

A

C

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15
Q

The enzyme CYP2A6 can have slow and rapid polymorphisms. We would expect a rapid metabolizer to have ___ blood concentrations of Nicotine.

A. Increased

B. Decreased

C. Unchanged

A

B.

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16
Q

A heavy smoker is someone who requires ____ nicotine to get the reward sensation (dopamine release). As a result it can be assumed that heavy smokers are ____ CYP2A6 metabolizers.

A. More, Rapid

B. Less, Rapid

C. More, Slow

D. Less, Slow

A

A

If you are a rapid CYP2A6 metabolizer then you will remove nicotine from the body faster so they people will have to smoke more in order to get the reward sensation of dopamine release. AKA heavy smokers.

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17
Q

When you have low CYP2A6 activity, ____ metabolism will become more important for removing nicotine from the body.

A. CYP3A4

B. CYP2D6

C. UGT (Glucuronidation)

D. Sulfation

A

C

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18
Q

If the patient does not stop smoking while on nicotine therapy then nicotine____ can occur

A. Withdrawal

B. Deficiency

C. Toxicity

D. Reistance

A

C

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19
Q

Nicotine replacement therapy is meant to deliver ___ and safer doses of nicotein to mitigate (lessen) withdrawal symptoms.

A. Low

B. High

C. Medium

A

A

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20
Q

Nicotine patches will ___ release nicotine into the bloodstream and the skin absorbs it and acts as a reservoir after the patch has been removed.

A. Rapidly

B. Slowly

A

B

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21
Q

Regarding Nicotine Gum, any nicotine that is swallowed is going to be exposed to a(n) ____ environment and become ____ and as a result ____ bioavailable.

A. Acidic, Ionized, Less

B. Basic, Ionized, Less

C. Acidic, Ionized, More

D. Basic Ionized, more

A

A

Nicotine has a high pKa of 7.8 and when swallowed it is put into an acidic environment (stomach) where it will become ionized (charged) and will not be able to cross into systemic circulation.

22
Q

Oral nicotine such as the gum or lozenge is absorbed by the ___ of the mouth.

A. Tongue

B. Buccal Mucossa

C. Nasal passages

D. Gums

A

B.

The reason they tell people to “park” the gum between the cheeks of the mouth is because that is where the buccal mucossa are located and they can absorb the nicotine from there. It also avoids the 1st pass effect and GI side effects.

23
Q

Drinking something acidic before using nicotine gum or lozenges will result in ____ bioavailability of the nicotine.

A. Increased

B. Decreased

A

B.

The mouth will become acidic due to the acidic food/beverage and cause the nicotine to become ionized and unabsorbed as a result. Needs to be unionzied to pass through the mucosa and through lipophilic barriers.

24
Q

T/F Nicotine inhalers (nicotrol inhaler) is meant to mimic the act of smoking for smokers.

A

T

25
Q

T/F Nicotine nasal spray is meant to mimic the rapid administration (absorption profile) of nicotine that is seen in cigarettes.

A

T

26
Q

Based on the chart provided on nicotine absorption profiles, which nicotine replacement therapy closely mimics the absorption profile of cigarettes?

A. Gum

B. Tablet

C. Inhaler

D. Spray

A

D.

The absorption profile is very similar just smaller. The nasal spray has the MOST RAPID absorption profile of nicotine than any other nicotine replacement therapy.

27
Q

Which of these sites can nicotine be absorbed?

A. Skin

B. Lung

C. Urinary bladder

D. GI

E. All of the above

A

E

28
Q

Which of the following statments is NOT true?

A. Nicotine is converted to it’s hydrophilic form when placed in an acidic environment

B. Nicotine is converted to it’s lipophilic form when placed in a basic environment

C. Uncharged species of nicotine are lipophilic and more readily absorbed

D. When nicotine is absored through the lung tissue it is no longer pH-dependent and is only dependent on concentration gradient.

E. Nicotine absorption at the lung tissue is dependent on pH and the concentration gradient.

A

D

When someone smokes small tar droplets flow into the lungs and deposit on the alveloli and stick there. Each droplet contains nicotine and forms a concentration gradient that allows the nicotine to pass through the wall of the alveoli into the blood (since there is more in the alveoli and less in the blood). Also if the pH is basic at the alveoli (which it is) then the drug will remain unionized and lipophilic and can pass through the alevoli and into the blood stream.

29
Q

When looking at the metabolism of nicotine what kind of reaction is occuring from the starting molecule (nicotine) to it’s active metabolite (Cotinine)?

A. Methylation

B. C-Oxidation

C. Glucuronidation

E. Sulfation

A

B

30
Q

When looking at this particular metabolism of Nicotine, what is the enzyme responsible for its metabolism?

A. CYP2A6

B. CYP3A4

C. COMT

D. SULT

A

A

31
Q

What kind of reaction is occuring here between these two molecules?

A. Methylation

B. C-Oxidation

C. COMT

D. SULT

A

B

32
Q

What kind of metabolism is nicotine undergoing?

A. N-Oxidation

B. N-methylation

C. N-glucuronidation

D. O-glucuronidation

A

A

33
Q

What kind of metabolism is nicotine undergoing here?

A. N-Oxidation

B. N-Methylation

C. O-Glucuronidation

D. N-Glucuronidaiton

A

B

34
Q

What kind of metabolism is occuring here in nicotine?

A. N-Methylation

B. N-Oxidation

C. C-Oxidation

D. A and C

A

D

35
Q

What enzyme is responsible for the N-oxidation occuring here?

A. FMO

B. MAO

C. CYP2A6

D. UGT

A

A

36
Q

What enzyme is responsible the c-oxidation of nicotine?

A. FMO

B. MAO

C. CYP2A6

D. UGT

A

C

For methylation he also says N-methyltransferase

37
Q

What kind of metabolism is happening with the active Nicotine metabolite, Cotinine?

A. N-Methylation using 2A6

B. N-Glucuronidation using SULT

C. N-Glucuronidation using UGT

D. N-Oxidation using FMO

A

C

38
Q

What series of reactions is occuring in order to get from the active Cotinine metabolite to the inactive metabolite?

A. C-Hydroxylation (oxidation), O-Glucuronidation

B. C-Reduction, O-Glucurondation

C. C-Hydroxylation (oxidation, N-Glucuronidation

D. C-Reduction, N-Glucuronidation

A

A

39
Q

What enzyme is causing this reaction to occur?

A. 2A6

B. MAO

C. FMO

D. UGT

A

D

40
Q

Based on the structure circled in Varenicline it can be infered that:

A. Varenicline is a pyradine derivative of Cytisine

B. Varenicline is a pyrazine derivative of Cytisine

C. Varenicline is a pyrimidine derivative of Cytisine

A

B

Remember that Pyradine has only one Nitrogen with double bonds.

Pyrazine has two Nitrogens with double bonds on opposite sides

41
Q

T/F Varenicline only partially activates nAChR receptors but has a high affinity for them (long duration of action)

A

T

42
Q

When looking at the metabolism of Varenicline what enzyme is responsible for the metabolite?

A. FMO

B. MAO

C. UGT

D. 2A6

A

C

43
Q

T/F Based on the diagram most varenicline is excreted unchanged and it is important a patient has good renal function.

A

T

44
Q

What is bupropion known as?

A. Amino-Ketone

B. Amino acid

C. Quinoline

D. Piperazine

A

A

Just remember the amino group and the ketone and it will be known as an amino-ketone

45
Q

The structure on the right is what is responsible for stimulating effects. The ___ group in red and the ketone on bupropion prevents the molecule from being converted into that so the stimulating effects are not seen.

A. T-butyl

B. Isopropyl

C. Propyl

D. Butyl

A

A

46
Q

What is the name of the strucutre on the right resemble?

A. Phenethylamine

B. Pyrazine

C. Pyrimidine

D. Amino Acid

A

A.

Just remember the aromatic phenyl group and the Amine group at the top. Then it resembles the Phenethylamine

47
Q

The T-butyl group prevents ____ and thus prevents the conversion of bupropion to an amphetamine-like compound, phenethylamine.

A. N-Oxidation

B. N-Dealkylation

A

B

48
Q

Starting from the circled compounds what kind of reaction is occuring here?

A. T-Butyl hydroxylation (Forming Major metabolite OH-bupropion)

B. T-Butyl Reduction (Forming Major metabolite OH-bupropion)

A

A

49
Q

T/F Based on the picture provided it can be concluded that the majority of bupropion’s activity is done through the active metabolites generated from reduction and hydroxylation.

A

T

50
Q

Swalowed drops of nicotine reaching the stomach…

A. Become highly bioavailable

B. Readily enter systemic circulation

C. Exhibit extreme lipophilicity

D. Possess an overall neutral charge

E. Exhibit poor bioavailability

A

E

51
Q
A

PTVI (5 decks)

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