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Medicinal Chemistry I > Final Drugs and Diseases > Flashcards

Final Drugs and Diseases Flashcards

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1
Q

Pellagra is the deficiency of …

A

niacin (vitamin B3)

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2
Q

Niacin is an important precursor for ___

A

NAD+ and NADP+

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3
Q

Niacin is vitamin __

A

B3

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4
Q

Which disease state causes pts to have rough skin and the 3D’s ( dermatitis, dementia and diarrhea)?

A

Pellagra

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5
Q

If a person has a deficiency in transferring hydride ions (H-) they will get what disease?

A

Pellagra

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6
Q

NAD+ plus H+ plus 2e-&raquo_space; NADH
NADP+ plus H+ plus 2e-&raquo_space; NADPH
These equation shows the transfer of _____

A

hydride ions

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7
Q

FAD plus 2H+ plus 2 electrons&raquo_space;> FADH2
This equation shows the transfer of ___

A

hydrogen atoms

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8
Q

Ariboflavinosis is the deficiency in ____

A

Riboflavin (vitamin B2)

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9
Q

Riboflavin is vitamin __

A

B2

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10
Q

If a person has a deficiency in transferring hydrogen atoms, they will get what disease?

A

Ariboflavinosis

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11
Q

Which disease state causes pts to have angular cheilitis, itchy eyes, light sensitivity, dermatitis around mouth and anemia?

A

Ariboflavinosis

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12
Q

What mitochondrial mutation result in a rare form of diabetes?

A

defect in oxidative phosphorylation

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13
Q

Defect in oxidative phosphorylation result in what in the rare form of diabetes?

A

Low ATP in the cell therefore causing insulin NOT to be released

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14
Q

T/F High ω-6 to ω-3 fatty acids lead to cardiovascular disease.

A

True

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15
Q

Essential fatty acids include

A

omega 6 and omega 3

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16
Q

Omega __ : Linoleate 18:2 →Arachidonate 20:4 (AA)

A

6

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17
Q

Omega __ : Linoleate 18:2 → a- Linoleate 18:3 (fish oils) →Eicosapentaenoic acid (EPA) 20:5 → Docosahexaenoic acid (DHA)
22:6

A

3

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18
Q

What insulin sensitizers decrease insulin resistance, a phenomenon that occurs with high blood levels of free fatty acids which causes obesity in type 2 diabetes?

A

Thiazolidinediones such as Rosiglitazone (Avandia) and Pioglitazone (Actos)

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19
Q

MOA of Thiazolidinediones

A

They stimulate PPARy which regulates gene expression such as PEPCK
and other systems like GLUT-4, a glucose transporter in fat cells.

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20
Q

What type of drugs lower cholesterol?

A

Statins

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21
Q

MOA of statins

A

inhibits HMG-CoA
reductase that forms mevalonate

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22
Q

Examples of statins

A

lovastatin (mevacor) and rosuvastatin (crestor)

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23
Q

4 major lipoproteins

A
  1. Chylomicrons
  2. VLDL
  3. LDL
  4. HDL
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24
Q

function of lipoproteins

A

transport TG (triglycerides) and cholesterol from one tissue to another

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25
Q

where are chylomicrons synthesized?

A

intestines

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26
Q

where is VLDL synthesized?

A

liver

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27
Q

where is LDL synthesized?

A

liver and blood (highest amount of cholesterol)

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28
Q

where is HDL synthesized?

A

liver

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29
Q

Atherosclerosis and Coronary heart disease: are correlated with what 4 things?

A
  1. serum cholesterol
  2. deposition of cholesterol
  3. cholesterol ester
  4. lipoproteins containing apo-B
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30
Q

So when someone has elevated ___ and normal ___ or vice versa or both are elevated there will be elevated cholesterol levels which is
unhealthy

A

VLDL, LDL

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31
Q

Low HDL or high LDL (VLDL) is very bad because …

A

there will be a high amount of cholesterol injected into the body and very little harvested back.

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32
Q

what serum cholesterol causes Atherosclerosis and Coronary heart disease.

A

low HDL and high LDL (VLDL)

33
Q

what are the 3 polyunsaturated fatty acids (PUFAs) that lower blood cholesterol?

A
  1. eicosapentaenoic (EPA)
  2. docosahexaenoic (DHA)
  3. Omacor
34
Q

Jaundice is caused by:

A
  1. The accumulation of bilirubin due to liver disease ( liver cancer, hepatitis)
  2. blocked bile secretion (due to pancreatic cancer, gallstones)
  3. the lack of UDPGT (Crigler-Najjar)
35
Q

infant jaundice is centered on ___ which is toxic.

A

4Z, 15E ( bilirubin)

36
Q

treatment of infant jaundice

A

phototherapy

37
Q

what are the 2 steps of heme being degraded to bilirubin?

A
  1. Heme oxygenase linerarizes heme to create biliverdin (green compound, seen in a bruise)
  2. Biliverdin reductase converts biliverdin to bilirubin (yellow compound that travel bound to serum albumin in the bloodstream)
38
Q

Major pigment of urine come from bilirubin being degraded to ___

A

urobilin

39
Q

urobilin is further degraded by intestinal microbiota to _____

A

stercobilin ( major pigment of feces)

40
Q

HMG-CoA reductase inhibitors

A

Statins (e.g. Lovastatin (Mevacor) and Rosuvastatin (Crestor))

41
Q

Drugs that decrease VLDL synthesis

A

Fenofibrate (Tricor) and Niacin (Nicotinic Acid)

42
Q

What drug is a resin that absorb bile acids and in pts with high cholesterol/LDL, converts more cholesterol to bile acid?

A

cholestyramine (questran)

43
Q

Pyridoxal phosphate (PLP) is an active form of vitamin __ involved in transaminations

A

B6

44
Q

Porphyrias are a result of enzyme deficiency along the porphyrin (heme) biosynthesis
pathway that starts with ____ and ___resulting in a heme.

A

succinyl-CoA, glycine

45
Q

T/F Porphyrias causes a buildup of precursors in RBC, body fluids, and the liver.

A

true

46
Q

Accumulation of precursor uroporphyrinogen leads to ….
A. urine being pink to dark purple
B. Urine being red
C. teeth being red under UV
D. skin is sensitive to UV light
E. craving for heme (vampire myth)

A

A. urine being pink to dark purple
C. teeth being red under UV
D. skin is sensitive to UV light
E. craving for heme (vampire myth)

47
Q

most common type of porphyria

A

acute intermittent

48
Q

rate-limiting step of purine synthesis

A

Glutamine-PRPP amindotransferance

49
Q

Glutamine-PRPP amindotransferance may be inhibited by what anticancer drugs?

A

6-mercaptopurine and 6-thioguanine

50
Q

what two things provide the atoms to create a ring for pyrimidine synthesis to then attach to a ribose 5-phosphate.

A

Aspartate and carbamoyl phosphate

51
Q

UMP is phosphorylated to __ then it is converted to
___

A

UTP, CTP

52
Q

______is the target for anti cancer drugs such as 5-fluorouracil (5FU), floxuridine and capecitabine

A

Thymidylate synthase

53
Q

5-fluorouracil (5FU), floxuridine and capecitabine are ___ inhibitors of thymidylate synthase

A

irreversible

54
Q

what anti cancer drugs irreversible inhibit thymidylate synthase?

A

5-fluorouracil (5FU) , floxuridine and capecitabine

55
Q

_______ is blocked by anticancer drugs such as methotrexate which is very
toxic

A

Dihydrofolate reductase (DHFR)

56
Q

Dihydrofolate reductase (DHFR) is blocked by anticancer drugs such as ____ which is very
toxic

A

methotrexate

57
Q

Dihydrofolate reductase (DHFR) reduces __ to ___ which is required in both purine and pyrimidine synthesis

A

DHF (dihydrofolate) , THF (tetrahydrofolate)

58
Q

Lesch-Nyhan disease: total lack of ____ , that is used in the salvage pathway to convert purines and their nucleosides to mononucleotides.

A

HGPRT

59
Q

symptoms of Lesch-Nyhan disease

A
  1. severe mental disabilities
  2. deposits of orange sand-like crystals in the diapers of infants with this condition
60
Q

Gout is caused by an excess of ___

A

uric acid

61
Q

symptoms of gout

A
  1. painful joints (toes) due to deposits of sodium urate crystals
62
Q

gout primarily affects males or females

A

males

63
Q

Gout may involve
A. overproduction or genetic under-excretion of uric acid
B. overconsumption of fructose
C. HGPRT deficiency from the salvage pathway
D. overconsumption of lactose

A

A. overproduction or genetic under-excretion of uric acid
B. overconsumption of fructose
C. HGPRT deficiency from the salvage pathway

64
Q

How can gout be treated (diet related) ?

A
  1. avoidance of purine rich foods (seafood,liver)
  2. avoidance of fructose
65
Q

How can gout be treated (drug related) ?

A
  1. xanthine oxidase inhibitors e.g. allopurinol (Zyloprim) and febuxostat (Uloric)
  2. administration of porcine uric acid oxidase (uricase, Krystexxa)
66
Q

examples of endocrine hormones that are released to blood and carried to their target cells

A

insulin and glucagon

67
Q

examples of paracrine hormones that are released into extracellular space, diffuses to a nearby target (act locally)

A

Eicosanoids: prostaglandins, thromboxanes, and leukotrienes

68
Q

paracrine hormones are produced from ______ via _________

A

arachidonic acid, phospholipase A2

69
Q

____: affects the cell where they are produced, but can bind to surface
receptors. Very lipophilic

A

Autocrine

70
Q

______: bind to receptors that span the membrane and induce
conformational change that produces a secondary messenger. Causes signal amplification and affects many targets.

A

Extracellular hormones

71
Q

Extracellular hormones

A

peptide and amine

72
Q

Peptide hormones

A

insulin, glucagon, somatostatin

73
Q

Insulin is synthesized ….

A

on the ribosome of Beta cells of the pancreas as preproinsulin

74
Q

which is the correct order?
A. preproinsulin→proinsulin→matured insulin
B. proinsulin →matured → preproinsulin
C. matured → preproinsulin → proinsulin
D. proinsulin → preproinsulin→ →matured insulin

A

A. preproinsulin→proinsulin→matured insulin (5.8 kDa)

75
Q

Insulin has __ AA

A

51

76
Q

the B chain is the same in pigs and cows but
we do not use the cows due to “____”.

A

mad cow disease

77
Q

Amine hormone

A

epinephrine (adrenaline)

78
Q

epinephrine (adrenaline) and norepinephrine are ___ hormones

A

catecholamine b

Medicinal Chemistry I (2 decks)

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