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level: Prodrugs & Conjugation

Questions and Answers List

level questions: Prodrugs & Conjugation

Question	Answer
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 plasma	esterases
It is inactive and activated by hydrolysis plasma esterases to chlorampenicol / prednisolon	1 Prodrug Chloramphenicol Hemisuccinate Na Salt 2 Prodrug Prednisolon Hemisuccinate Na Salt
It is inactive and activated by hydrolysis by intestinal esterases to chloramphenicol / clindamycin	1 Prodrug Chloramphenicol Palmitate 2 Prodrug Clindamycin Palmitate
It is inactive and activated by hydrolysis by plasma esterases to carbenicillin	1 Prodrug Carbenicillin Indanyl Ester
PHASE II is also called what?	Conjugation Reaction
The most common conjugation pathway	Glucuronidation
Classes of Glucuronides	1 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 conjugated	UDP glucuronosyltransferase
It leads Neonates to Gray Baby Syndrome	Chloramphenicol (Chloroptic)
Attributable to to their inability to conjugate bilirubin with glucuronic acid	Neonatal jaundice
Enzymes involved in the Formation of B-glucuronides	1 Phosphorylase 2 UDPG Dehydrogenase 3 UDP-Glucuronyl-transferase
Occurs less frequently than does glucuronidation	Sulfate 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-hydroxyarylamides	1 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 primates	1 Glycine and Glutamine 2 Glycine conjugate 3 Glutamine conjugate
Glycine conjugate of Aspirin	Salicyluric acid
Its thiol functions as scavenger of harmful electrophilic parent drugs or their metabolites	Glutathione
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 melatonin	Methylation