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Org Chem PACOP > 251-300 > Flashcards

251-300 Flashcards

1
Q

Which of the following statements is correct regarding Phase ll reactions?
l.These are reactions in which the functional groups of the original drug(or metabolite)are masked by conjugation reaction
ll.These reactions require both a high-energy molecules and an enzyme
lll.High-energy molecules consist of a coenzyme bound to the endogenous substrate,the parent drug,or the drug’s phase l metabolite.
lV.Most conjugates are highly polar and unable to cross cell membranes,making them almost almost always pharmacology inactive and of little or no toxicity.

A

l,ll,lll,lV

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2
Q

Which of the following statements correctly describes Glucuronidation reaction?
l.It is the most common conjugation pathway because of readiy available supply of glucuronic acid as well as a large variety of functional groups,which can enzymatically react with this sugar derivative.

ll.The high energy form of glucuronic acid is Uridine monophosphate glucuronic acid and the enzyme involve in these reaction is glucuronyl transferase.

III.Druds that posses hydroxyl or carboxyl functional groups readily undergo glucurinidation to form esters and ethers,respectively.

lV.The addition of the glucuronide moiety greatly increases the hydrophilicity of the molecule which makes it highly reabsorbed by the renal tubes.

A

l,ll only

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3
Q

Which of the following conjugation reactions requires 2’-phosphoadenosine-5’- phosphosulfate molecule?
A) Glutathione conjugation
B) Acetylation
C) Methylation
D) Sulfate conjugation
E) Amino acid conjugation

A

D) Sulfate conjugation

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4
Q

Which of the following conjugation reactions require the formation of the high-energy molecule AcetylCoA
A) Glutathione conjugation
B) Acetylation
C) Methylation
D) Sulfate conjugation
E) Amino acid conjugation

A

Acetylation

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5
Q

Which of the following conditions can greatly affect the metabolism of a certain drug?
A) Congestive heart failure
B) Deficiency of certain dietary minerals
C) Deficiency of vitamins
D) Increase drug dosage
E) All of the above

A

All of the above

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6
Q

Which of the following drug administration route bypasses first-pass effect
A) Oral administration
B) Intravenous administration
C) Sublingual administration
D) A and B
E) B and C

A

B and C

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7
Q

Which of the following metabolites would be the least likely urinary excretion product of acetaminophen?
A) Ether glucuronide
B) Sulfate conjugate
C) N-acetyl-p-benziminoqiunoneimine
D) Unchange drug
E) N-acetyl-p-benziminoquinoneimine with glutathione

A

Unchange drug

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8
Q

Which of te following statements correctly describes the first and second generation Sulfonylureas? (See structure below)
l.First and second generation Sulfonylureas have a bulk aliphatic substituent on the nonsufonyl have relatively simple aromatic
ll.First generation Sulfonylureas have relatively simple aromatic substituents such as methyl,amino,acetyl,chloro
lll Second generation Sulfonylureas have a larger aromatic substituent
lV.First generation Sulfonylureas are more potent than second generation

A

l,ll,lll only

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9
Q

Which of the following is not the first generation sulfonylurea
A) Glyburide
B) Glipizide
C) Glimperide
D) All of the choices
E) None of the choices

A

All of the choices

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10
Q

Which of the following is the first generation sulfonylurea
A) Glyburide
B) glipizide
C) Glimperide
D) All of the choices
E) None of the choices

A

None of the choices

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11
Q

This drug has been highly effective against Schistoma mansoni.It is activated via esterification to a biological ester that spontaneously dissociates to an electrophlie,which alkylates the helminth DNA,leading to irreversible inhibition of nucleic acid metabolism.
A) Praziquantel
B) Oxaminiquine
C) Ivermectin
D) Pyrantel
E) Mebendazole

A

Oxaminiquine

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12
Q

This drug acts as a depolarizing neuromuscular blocking agent that acts as a depolarizing neuromuscular blocking agent that activates nicotinic receptors and inhibits cholinesters,ultimately leading to worm paralysis.It is used as apamoate salt,which is quite insoluble and,as a result,is not readiy absorbed improving the usefulness of the drug for the treatment of intestinal helminthes.
A) Praziquantel
B) Oxaminiquine
C) Ivermectin
D) Pyrantel
E) Mebendazole

A

Pyrantel

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13
Q

A drug that belongs to a class of 16-membered macrocyclic lactones extracted from Streptomyces avermitilis used in the treatment of various nematode infections.It acts either as a GABA agonist or as an inducer of chloride ion influx,leading to hyperpolarization and muscle paralysis.
A)Praziquantel
B)Oxaminiquine
C)Ivermectin
D)Pyrantel
E)Mebendazole

A

Ivermectin

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14
Q

It is an isoquinoline derivative with most of the biological activity found in the levo enantiomer.The compound has no activity against nematodes,but is highly effective against cestodes and trematodes.Its mechanism of action appers to involve calcium ion redistribution either directly or indirectly and inhibition of phosphoinositide metabolism
A) Praziquantel
B) Oxaminiquine
C) Ivermectin
D) Pyrantel
E) Mebendazole

A

Praziquantel

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15
Q

Buspirone,a long chain arylpiperazine derivative,is an anxiolytic agent that is a partial agonist to
A)5HT1A receptor
B)5HT4 receptor
C)5HT3 receptor
D)5HT2A
E)5HT1D

A

5HT1A receptor

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16
Q

Sumatriptan and other indeleaklylamine derivatives used in the treatment of migraine is an agonist at which of
the following receptors.
A) 5HT1A receptor
B) 5HT4 receptor
C) 5HT3 receptor
D) 5HT2A
E) 5HT1D

A

5HT1D

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17
Q

. 267-268, refer to the following reaction pathway
A)l,ll,lll,lV
B)l,ll only
C)lll,lV only
D)l,lll
E)ll,lV

A

lll,lV only

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18
Q

Which of the givem reactions can be classified as Phase ll metabolism?
A)l,ll,lll,lV
B)l,ll only
C)lll,lV only
D)l,lll
E)ll,lV

A

I and II only

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19
Q

Which of the following drugs would most likely undergo nitroreduction?
A)Chloramphenicol
B)Procaine
C)Lidocaine
D)Sulfasalazine
E)All of the above

A

Chloramphenicol

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20
Q

Which of the following drugs would most likely undergo azoreduction
A)Chloramphenicol
B)Procaine
C)Lidocaine
D)Sulfasalazine

A

Sulfasalazine

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21
Q

Which of the following drugs would most likely undergo ester hydrolysis
A)Chloramphenicol
B)Procaine
C)Lidocaine
D)Sulfasalazine
E)All of the above

A

Procaine

22
Q

Which of the following drugs would likely undergo amide hydrolysis
A)Chloramphenicol
B)Procaine
C)Lidocaine
D)Sulfasalazine
E)All of the above

A

Lidocaine

23
Q

This conjugation pathway is extremely important in preveting toxicity from a variety of electrophilic agents.It produces a mercaptopuric acid derivative upon reaction with an electrophile
A)Glutathione conjugation
B)Acetylation
C)Methylation
D)Sulfate conjugation
E)Amino acid conjugation

A

Glutathione conjugation

24
Q

S-adenosylmethionine is required for the conjugation reaction
A)Glutathione conjugation
B)Acetylation
C)Methylation
D)Sulfate conjugation
E)Amino acid conjugation

A

Methylation

25
Q

Meperidine can undergo which of the following metabolic pathway?
I. Hydroxylation at thr aromatic ring
II. Ester hydrolysis
III. N-oxidation
IV. N-dealkylation

A

I,II,III,IV

26
Q

Which of the following selective estrogen receptor modulators (SERMs) and antiestrogens has a
triphenylethylene structure used to treat early and advanced breast carcinoma in post menopausal women?
A. raloxifene
B. Fulvestrant
C. Tamoxifen
D. Clomiphene
E. None of the above

A

Tamoxifen

27
Q

Which of the following SERMs and antiestrogen is a benzothiophene derivative that has been approved for the prevention and treatment of osteoporosis in menopausal women? It has antagonist properties on the endometrium and breast tissue and agonist properties on bone and cardiovascular system?
A. raloxifene
B. Fulvestrant
C. Tamoxifen
D. Clomiphene
E. None of the above

A

raloxifene

28
Q

Which of the following SERMs and antiestrogen is an antagonist structurally on the estradiol structure which is
used in the treatment of women who have had disease progression after prior antiestrogen property?
A. raloxifene
B. Fulvestrant
C. Tamoxifen
D. Clomiphene
E. None of the above

A

Fulvestrant

29
Q

Which of the following drugs is not a nonsteroidal aromatase inhibitor?
A. Letrozole
B. Aminoglutethimide
C. Exemestane
D. A and B only
E. B and C only

A

Exemestane

30
Q

Which of the following drugs is a nonsteroidal aromatase inhibitor?
A. Letrozole
B. Aminoglutethimide
C. Exemestane
D. A and B only
E. B and C only

A

A and B only

31
Q

An aromatase inhibitor used mainly in the treatment of cushing’s syndrome
A. Letrozole
B. Aminoglutethimide
C. Exemestane
D. A and B only
E. B and C only

A

Aminoglutethimide

32
Q

What is the probable mechanism of action of diuretic drug with the following structure?
A. It increases intraluminal osmotic pressure, causing water to pass from the body into the tubules.
B. It can induce dieresis by inhibiting the formation of carbonic acid within the proximal and tubular cells to limit the number of hydrogen ions available to promote sodium reabsortion
C. It inhibits the Na+/Cl- symportar located in the distal convulated tubule
D. It inhibits Na+/K=/Cl- transport system in the thick ascending limb loop of henle
E. It inhibits sodium and water reabsorption by competitive inhibition of aldosterone

A

It increases intraluminal osmotic pressure, causing water to pass from the body into the tubules.

33
Q

What is the probable mechanism of action of a diuretic drug with the following structure?
A. It increases intraluminal osmotic pressure, causing water to pass from the body into the tubules.
B. It can induce dieresis by inhibiting the formation of carbonic acid within the proximal and tubular cells to limit the
number of hydrogen ions available to promote sodium reabsortion
C. It inhibits the Na+/Cl- symportar located in the distal convulated tubule
D. It inhibits Na+/K=/Cl- transport system in the thick ascending limb loop of henle
E. It inhibits sodium and water reabsorption by competitive inhibition of aldosterone

A

It inhibits the Na+/Cl- symportar located in the distal convulated tubule

34
Q

What is the probable mechanism of action of a diuretic drug with the following structure?
A. It increases intraluminal osmotic pressure, causing water to pass from the body into the tubules.
B. It can induce dieresis by inhibiting the formation of carbonic acid within the proximal and tubular cells to limit the number of hydrogen ions available to promote sodium reabsortion
C. It inhibits the Na+/Cl- symportar located in the distal convulated tubule
D. It inhibits Na+/K=/Cl- transport system in the thick ascending limb loop of henle
E. It inhibits sodium and water reabsorption by competitive inhibition of aldosterone

A

It can induce dieresis by inhibiting the formation of carbonic acid within the proximal and tubular cells to limit the number of hydrogen ions available to promote sodium reabsortion

35
Q

What is the probable mechanism of action of a diuretic drug with the following structure?
A. It increases intraluminal osmotic pressure, causing water to pass from the body into the tubules.
B. It can induce dieresis by inhibiting the formation of carbonic acid within the proximal and tubular cells to limit the
number of hydrogen ions available to promote sodium reabsortion
C. It inhibits the Na+/Cl- symportar located in the distal convulated tubule
D. It inhibits Na+/K=/Cl- transport system in the thick ascending limb loop of henle
E. It inhibits sodium and water reabsorption by competitive inhibition of aldosterone

A

It inhibits Na+/K=/Cl- transport system in the thick ascending limb loop of henle

36
Q

Which of the following analgesic agent is 2 to 3 times more potent than morphine as analgesic and also known
as heroin?
A. Tramadol hydrochloride
B. Normorphine
C. Diphenoxylate
D. Nalbuphine
E. Diacetylmorphine Hydrochloride

A

Diacetylmorphine Hydrochloride

37
Q

Which of the following drugs represent a fragment of codeine’s structure, consisting of the phenyl and
cyclohexane rings? This drug possesses opioid activity but has other analgesic activity that is not reversed by
naloxone.
A. Tramadol hydrochloride
B. Normorphine
C. Diphenoxylate
D. Nalbuphine
E. Diacetylmorphine Hydrochloride

A

Tramadol hydrochloride

38
Q

This drug prepared by N-demethylation of morphine and has about one-fourth as active as morphine in
producing analgesia but has a much lower physical dependence capacity
A. Tramadol hydrochloride
B. Normorphine
C. Diphenoxylate
D. Nalbuphine
E. Diacetylmorphine Hydrochloride

A

Normorphine

39
Q

Also known as Ncyclobutylmethylnoroxymorphone hydrochloride, this drug is analgesia of the agonistantagonist type with little or no abuse liability.
A. Tramadol hydrochloride
B. Normorphine
C. Diphenoxylate
D. Nalbuphine
E. Diacetylmorphine Hydrochloride

A

Nalbuphine

40
Q

This drug has a strong structural relationship to the meperidine type analgesics and has the ability to inhibit
excessive gastrointestinal motility.
A. Tramadol hydrochloride
B. Normorphine
C. Diphenoxylate
D. Nalbuphine
E. Diacetylmorphine Hydrochloride

A

Diphenoxylate

41
Q

Which of the following modifications can affect the onset , degree and duration of insulin activity?
A. Rearrangement of amino acid residues at the N- and C- terminus at the B chain of insulin
B. Changing the insulin crystal type (ex. From crystalline to amorphous)
C. Addition of modifying protein such as protamine
D. Changing the site of injection
E. All of the above

A

All of the above

42
Q

This is the only insulin analogue with a C14 fatty acid attached to an amino residue in the B chain of insulin
A. Lispro
B. Aspart
C. Glulisine
D. Glargine
E. Detemir

A

Detemir

42
Q

A highly purified protein containing 165 amino acids manufactured from a strain of E. coli bearing a genetically engineered plasmid containing an interferon alfa 2a gene from leucocytes. This drug is used in patients 18 years or older for treatment of hairy cell leukemia and chronic myelogenous leukemia.
A. Roferon-A
B. Interon
C. Aldesleukin
D. Rituximab
E. Gemtuzumab Ozogamicin

A

Roferon-A

43
Q

A highly purified protein containing 165 amino acids manufactured from a strain of E. coli bearing a genetically engineered plasmid containing an interferon alfa 2a gene from leucocytes. This drug is used in patients 18 years or older for treatment of hairy cell leukemia and chronic myelogenous leukemia.
A. Roferon-A
B. Interon
C. Aldesleukin
D. Rituximab
E. Gemtuzumab Ozogamicin

A

Interferon

44
Q

A highly purified protein produced by E.coli containing a plasmid with alfa 2b gene. This product is indicated
for hairy cell leukemia and also useful in treating malignant melanoma.
A. Roferon-A
B. Interon
C. Aldesleukin
D. Rituximab
E. Gemtuzumab Ozogamicin

A

Aldesleukin

45
Q

It is also known as interleukin 2 or T-cell growth factor. This product when administered stimulates T-cell growth and regulation, proliferation and immunoglobulin production in B lymphocytes macrophage activity enhancement
A. Roferon-A
B. Interon
C. Aldesleukin
D. Rituximab
E. Trastuzumab

A

Gemtuzumab Ozogamicin

46
Q

A genetically engineered chimeric monoclonal antibody directed against CD20 antigen on malignant B
lymphocytes
A. Roferon-A
B. Interon
C. Aldesleukin
D. Rituximab
E. Gemtuzumab Ozogamicin

A

Rituximab

47
Q

A type of immunobiological that contains a solution of antibodies derived from the serum of animals immunized with specific antigens.
A. Toxoid
B. vaccine
C. Anti toxin
D. Intravenous immune globulin
E. Immune globulin

A

Anti toxin

48
Q

A product derived from blood plasma of a donor pool similar to the IG pool but prepared so it is suitable for IV use. It is primarily use for replacement therapy in primary Ab deficiency disorders and for the treatment of kawasaki’s disease.
A. Toxoid
B. vaccine
C. Anti toxin
D. Intravenous immune globulin
E. Immune globulin

A

Intravenous immune globulin

49
Q

A modified bacterial toxin that has been made non toxic but remains the ability to stimulate the formation of
antitoxin.
A. Toxoid
B. vaccine
C. Anti toxin
D. Intravenous immune globulin
E. Immune globulin

A

Toxoid

Org Chem PACOP (6 decks)

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