EXAM 2: Anticonvulsant Medicinal
Chemistry Exam Questions with All
Accurate Answers.
What are the ideal administration characteristics of anticonvulsant drugs? - Answer rapid
onset
long duration of action
Many of the standard anti-epileptic drugs contain what structure? - Answer ureide
Barbituate - Answer -three ketones
-6 membered rings
Hydantoin - Answer -NH group
-5 membered ring
Oxazolidinediones - Answer
Succinimide - Answer
What is the mechanism of action of phenytoin? - Answer binds to Na+ channel; inhibition of
repetitive firing and spread of seizures
How many hydrogen bonding sites does phenytoin have? - Answer 3
Phenytoin is ionized/unionized as physiological pH. - Answer unionized
-poor H2O solubility
-nonlinear kinetics
T/F: Phenytoin can be given IM. - Answer FALSE
, -prodrug form (Fosphenytoin) is converted to phenytoin in the body
Ethotoin - Answer -phenyl substituent at 5C is replaced by a H
-the NH at C3 becomes ethyl group
---less toxic; less effective; more sedation
Mephenytoin - Answer -ethyl group at C5 instead of phenyl
-the NH at C3 is methylated
---more sedation
The _____________________ metabolite of mephenytoin contributes to both efficacy and
toxicity. - Answer 5-phenyl-5-ethyldantoin
(N-methyl removed)
What is the mechanism of action of carbamazepine? - Answer acts on Na+ channels to prevent
spread of seizure
-autoinduction of metabolism
The metabolites of carbamazepine are: - Answer 10,11-epoxide (active); more toxic
10,11-hydroxy (inactive)
Iminoquinone - Answer
What is the mechanism of action of oxcarbazepine? - Answer blocks Na+ channel recovery;
additional action on Ca2+/K+ channels
-it is the 10-keto analog of CBZ
The pharmacological activity of oxcarbazepine is due to: - Answer 10-
monohydroxycarbazepine metabolite
Barbituates are lipophilic/hydrophilic and weak acids. - Answer lipophilic
-well distributed in brain
Chemistry Exam Questions with All
Accurate Answers.
What are the ideal administration characteristics of anticonvulsant drugs? - Answer rapid
onset
long duration of action
Many of the standard anti-epileptic drugs contain what structure? - Answer ureide
Barbituate - Answer -three ketones
-6 membered rings
Hydantoin - Answer -NH group
-5 membered ring
Oxazolidinediones - Answer
Succinimide - Answer
What is the mechanism of action of phenytoin? - Answer binds to Na+ channel; inhibition of
repetitive firing and spread of seizures
How many hydrogen bonding sites does phenytoin have? - Answer 3
Phenytoin is ionized/unionized as physiological pH. - Answer unionized
-poor H2O solubility
-nonlinear kinetics
T/F: Phenytoin can be given IM. - Answer FALSE
, -prodrug form (Fosphenytoin) is converted to phenytoin in the body
Ethotoin - Answer -phenyl substituent at 5C is replaced by a H
-the NH at C3 becomes ethyl group
---less toxic; less effective; more sedation
Mephenytoin - Answer -ethyl group at C5 instead of phenyl
-the NH at C3 is methylated
---more sedation
The _____________________ metabolite of mephenytoin contributes to both efficacy and
toxicity. - Answer 5-phenyl-5-ethyldantoin
(N-methyl removed)
What is the mechanism of action of carbamazepine? - Answer acts on Na+ channels to prevent
spread of seizure
-autoinduction of metabolism
The metabolites of carbamazepine are: - Answer 10,11-epoxide (active); more toxic
10,11-hydroxy (inactive)
Iminoquinone - Answer
What is the mechanism of action of oxcarbazepine? - Answer blocks Na+ channel recovery;
additional action on Ca2+/K+ channels
-it is the 10-keto analog of CBZ
The pharmacological activity of oxcarbazepine is due to: - Answer 10-
monohydroxycarbazepine metabolite
Barbituates are lipophilic/hydrophilic and weak acids. - Answer lipophilic
-well distributed in brain
