PHM 424 MIDTERM EXAM
What are the two antidiarrheal agents that are derivatives of meperidine?
-loperamide
-diphenoxylate
What are the chemical characteristics of H2RA's?
-Imidazole structure important for binding to receptor.
-C-4 methyl group on imidazole ring
-4-atom side chain of sulfur, carbon, oxygen. Sulfur increases potency
How is the active metabolite of metronidazole formed?
-Hydroxylation of the 2-methyl group 2-hydroxy-methylmetronidazole.
-Oxidation to metronidazole acetic acid.
What are the characteristics of Δ1- corticoids?
prednisone & prednisolone
-1-dehydro derivatives of cortisone
-Known as Δ1-corticoids, containing an additional double bond between positions 1 and 2.
What are the characteristics of amino-salicylates?
-Synthetic salicylic acid derivatives.
-High affinity for connective tissues containing elastin
-Active moiety is salicylate anion
What does the addition of lipophilic groups do to amino-salicylates?
, - increases anti-inflammatory activity
Which functional group contained on multicyclic opioids is responsible for binding to µ and κ
receptors?
-phenol
Which functional group MUST be present on Ciprofloxacin for it to be active?
- MUST be fluorinated to be active
What are the amino-salicylate drugs used to treat Inflammatory Bowel Diseases?
-sulfasalazine
-olsalazine
-mesalamine
What are the metabolic products of Sulfasalazine?
5-ASA
sulfapyridine
-5-ASA
What are the two antidiarrheal agents that are derivatives of meperidine?
-loperamide
-diphenoxylate
What are the chemical characteristics of H2RA's?
-Imidazole structure important for binding to receptor.
-C-4 methyl group on imidazole ring
-4-atom side chain of sulfur, carbon, oxygen. Sulfur increases potency
How is the active metabolite of metronidazole formed?
-Hydroxylation of the 2-methyl group 2-hydroxy-methylmetronidazole.
-Oxidation to metronidazole acetic acid.
What are the characteristics of Δ1- corticoids?
prednisone & prednisolone
-1-dehydro derivatives of cortisone
-Known as Δ1-corticoids, containing an additional double bond between positions 1 and 2.
What are the characteristics of amino-salicylates?
-Synthetic salicylic acid derivatives.
-High affinity for connective tissues containing elastin
-Active moiety is salicylate anion
What does the addition of lipophilic groups do to amino-salicylates?
, - increases anti-inflammatory activity
Which functional group contained on multicyclic opioids is responsible for binding to µ and κ
receptors?
-phenol
Which functional group MUST be present on Ciprofloxacin for it to be active?
- MUST be fluorinated to be active
What are the amino-salicylate drugs used to treat Inflammatory Bowel Diseases?
-sulfasalazine
-olsalazine
-mesalamine
What are the metabolic products of Sulfasalazine?
5-ASA
sulfapyridine
-5-ASA
