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CHEMISTRY > ORGANIC MEDICINAL CHEMISTRY > Flashcards

ORGANIC MEDICINAL CHEMISTRY Flashcards

1
Q
  • Practice of medicinal chemistry devoted to the discovery of drugs and development of new drugs
A

ORGANIC MEDICINAL CHEMISTRY

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2
Q

Food Drug and Cosmetic Act R.A#

A

RA 3720

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3
Q
  • A relatively small region of a macromolecule w/c may be: Isolatable enzyme, Structural or functional component of cell membrane, Specific intracellular substances (w/c a drug binds to produce a physiologic response)
A

RECEPTOR

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4
Q

Selection of structure components, the steric, electronic, & solubility characteristics of a drug w/c makes it interchangeable w/ drugs of the same pharmacologic class

A

ISOSTERISM

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5
Q

Grp of cmpds or atoms having the same # and arrangement of electrons

A

ISOSTERES

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6
Q

“Biotransformation”

A

DRUG METABOLISM

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7
Q

Advantages of PRODRUGS

A
  • Mask bitterness

- Incr. absorption of drug leading to higher plasma conc.

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8
Q

Cmpds that are inactive in native form but easily metabolized to the active agent

A

PRODRUGS

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9
Q

Paracetamol toxic from

A

NAPQI

N-acetyl-Pbenzoquinone

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10
Q

PHASE 1 OF METABOLISM

A

FUNCTIONALIZATION

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11
Q

Involves oxidation, reduction and hydrolysis

A

FUNCTIONALIZATION

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12
Q

Most common & important in drug metabolism

A

OXIDATION

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13
Q

Enzyme that adds O2 to the substrae

A

Cytochrome P450

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14
Q

Most dominant isoform of Cytochrome P450

A

Cyp3A4

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15
Q

Isoform of enzyme Cytochrome P450 that is for metabolism of antidepressant drugs

A

Cyp2D6

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16
Q

SUSCEPTIBILITY RULE

A

Esters > Thioesters > Carbonyls > Amide > Carbamate > Ureide

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17
Q

PHASE 2 OF METABOLISM

A

CONJUGATION

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18
Q

Attachment of small polar endogenous molecules such as glucuronic acid, sulfate and amino acids & etc. to the Phase 1 metabolites or parent drugs

A

CONJUGATION

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19
Q

Main enzyme responsible for attaching polar endogenous molecule to the Phase 1 metabolites

A

TRANSFERASES

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20
Q

Most common conjugation pathway

A

GLUCORONIDATION

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21
Q

Enzyme for GLUCORONIDATION

A

UDP-Glucoronosyltransferase

22
Q

Enzyme that is underdeveloped in neonates that cx Gray-baby syndrome

A

UDP - Glucuronosyltransferase

23
Q

Cofactor of UDP - Glucuronosyltransferase

A

Glucoronic acid

24
Q

Enzyme for SULFATION

A

Sulfotransferase

25
Q

Cofactor of Sulfotransferase

A

3’-Phosphoadenosyl-5’Phosphosulfate PAPS

26
Q

Example of drugs in SULFATION

A

Methyldopa, Albuterol, Terbutaline, Acetaminophen, Phenacetin MATA-Ph

27
Q

1st mammalian drug metabolite isolate

A

HIPPURIC ACID

28
Q

Enzyme for AMINO ACID CONJUGATION

A

N-acyltransferase/ Amino acid transferase

29
Q

Cofactor of N-acyltransferase/Amino acid transferase

30
Q

Enzyme for GLUTATHIONE CONJUGATION

A

Glutathione-S-transferase

31
Q

Cofactor of Glutathione-S-transferase

A

Glutathione

32
Q

Final metabolite in GLUTATHIONE CONJUGATION

A

Mercapturic acid

33
Q

Metabolism for N-containing drugs

A

ACETYL CONJUGATION

34
Q

Enzyme for ACETYL CONJUGATION

A

N-acetyltransferase NAT

35
Q

Cofactor of NAT

A

Acetyl-CoA

36
Q

Example of drugs in ACETYL CONJUGATION

A

Hydralazine, Isoniazid, Procainamide, Sulfonamides HIPS

37
Q

Important in the biosynthesis of Epi & melatonin & in the catabolism of catecholamines

A

METHYL CONJUGATION

38
Q

Enzyme for METHYL CONJUGATION

A

Methyltransferases

COMT

39
Q

Cofactor for Methyltransferases

A

S-Adenosinemethionine SAM

40
Q

Locally used anti infectives

A

GERMICIDES

41
Q

SUBTYPES OF GERMICIDES

A

Antiseptic

Disinfectant

42
Q

ALCOHOL common names

A

Ethanol
Gray Alcohol
Wine spirit

43
Q

ALCOHOL common names

A

Ethanol
Gray Alcohol
Wine spirit
Spiritus vini Retificatus

44
Q

Rendered unfit for use in intoxication beverages due to added: Methanol & benzene

A

DENATURED ALCOHOL

45
Q

Astringent, rubefacient, mild local anesthetic bc of its pulling effect

A

RUBBING ALCOHOL

46
Q

99% ethanol by wt.; Lab solvent

A

DEHYDRATED ALCOHOL/ABSOLUTE ALCOHOL

47
Q

Sterilize temp. - sensitive medical equipment and pharmaceuticals that cannot be autoclaved

A

ETHYLENE OXIDE

48
Q

Disinfectant and embalming fluid

A

FORMALDEHYDE/FORMALIN

49
Q

Sterilizing function for equipment & instruments that cannot be autoclaved

A

GLUTARALDEHYDE

50
Q

The ratio of a disinfectant to the dilution of phenol required to kill a given strain of the bacterium, under carefully controlled conditions over a given period

A

PHENOL COEFFICIENT

CHEMISTRY (5 decks)

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