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level: Prodrugs & Conjugation

Questions and Answers List

level questions: Prodrugs & Conjugation

QuestionAnswer
Prodrugs overcome some undesirable property such as __1 bitter taste 2 poor absorption 3 poor solubility 4 irritation of the site of injection
There is a presence of __ in many tissues and plasmaesterases
It is inactive and activated by hydrolysis plasma esterases to chlorampenicol / prednisolon1 Prodrug Chloramphenicol Hemisuccinate Na Salt 2 Prodrug Prednisolon Hemisuccinate Na Salt
It is inactive and activated by hydrolysis by intestinal esterases to chloramphenicol / clindamycin1 Prodrug Chloramphenicol Palmitate 2 Prodrug Clindamycin Palmitate
It is inactive and activated by hydrolysis by plasma esterases to carbenicillin1 Prodrug Carbenicillin Indanyl Ester
PHASE II is also called what?Conjugation Reaction
The most common conjugation pathwayGlucuronidation
Classes of Glucuronides1 O-, N-, S-, and C-
UDP-glucuronic acid contains what?D-glucuronic acid
Is closely associated with CYP450 so that Phase I products of drugs are efficiently conjugatedUDP glucuronosyltransferase
It leads Neonates to Gray Baby SyndromeChloramphenicol (Chloroptic)
Attributable to to their inability to conjugate bilirubin with glucuronic acidNeonatal jaundice
Enzymes involved in the Formation of B-glucuronides1 Phosphorylase 2 UDPG Dehydrogenase 3 UDP-Glucuronyl-transferase
Occurs less frequently than does glucuronidationSulfate conjugation -Involves three enzyme-catalyzed reactions
1 Sulfate conjugates can be hydrolyzed back to the parent compound by __ 2 __ plays an important role in the hepatoxicity and carcinogenecity of N-hydroxyarylamides1 sulfatases 2 Sulfoconjugation
In infants and young children where glucuronyltransferase activity is not well developed, have predominating __O-sulfate conjugation
In adults, the major urinary metabolite of the analgesic acetaminophen is the __O-glucuronide conjugate
1 Used by mammalian system to conjugate carboxylic acids particularly Aromatic acids and Arylalkyl acids 2 Common for mammals 3 Confine mainly to humans and other primates1 Glycine and Glutamine 2 Glycine conjugate 3 Glutamine conjugate
Glycine conjugate of AspirinSalicyluric acid
Its thiol functions as scavenger of harmful electrophilic parent drugs or their metabolitesGlutathione
Metabolism for drugs containing a primary amino group (aliphatic and aromatic amines)Acetyl Conjugation
1 They are rapid Acetylators (inadequate therapeutic response) 2 They are slow Acetylators (More likely to develop ADR)1 Eskimos and Asians 2 Egyptians and Western European Groups
Minor conjugation pathway, important in the biosynthesis of epinephrine and melatoninMethylation