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Phenytoin (Dilantin), Fosphenytoin (Cerebyx) are _______ channel inhibitors. Which one is a prodrug and which one is active?
- Na+
- Fosphenytoin is a prodrug and is converted to
- Phenytoin, the active drug
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Phenytoin (Dilantin) & Fosphenytoin (Cerebyx), Na+ channel inhibitors, are hepatically metabolized by and inducers of ____________________.
CYP3A4, 2C9, 2C19
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Phenytoin uses ________ kinetics, where ________ amount of drug eliminated per unit of time and the rate of drug elimination is _______ drug concentration.
- zero-order
- constant
- independent of
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What does a small increase in the dose of Phenytoin mean?
a large increase in plasma concentration
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TI of Phenytoin including free and protein-bound.
10-20 mcg/m
-
TI of free Phenytoin.
1-2 mcg/m
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Make sure to watch total levels and _______ and also _______ with Phenytoin.
-
Boxed warning (IV only) of Phenytoin.
severe hypotension and cardiac arrhythmias (infusion rate dependent); do not administer rapidly
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The anticonvulsant drug, ____________ can be administered faster.
Fosphenytoin (prodrug)
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SE of Phenytoin.
- SJS
- Hirsutism, gingival hyperplasia, acne
- Alteration of vitamin D metabolism (osteoporosis)
- hematological abnormalities
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Carbamazapine is an autoinducer & potent inducer of ________.
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Carbamazepine (Tegretol) exhibits _________ kinetics; Phenytoin exhibits ______ kinetics.
-
Boxed warnings for Carbamazepine (Tegretol).
- Serious dermatological reactions (SJS/TEN)
- Aplastic anemia
- agranulocytosis
-
Carbamazepine (Tegretol) is associated with what AE?
- Cholestatic jaundice
- hyponatremia
-
TI for Carbamazepine (Tegretol).
6–12 mcg/mL
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_________ has a similar MOA as Phenytoin, but is less protein bound and has less DIs.
Lamotrigine (Lamictal)
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Why is it important to slowly titrate Lamotrigine (Lamictal).
Too fast can = rash (SJS)
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NA+ channel inhibitor assoc with blood dyscrasias such as neutropenia & thrombocytopenia.
Lamotrigine (Lamictal)
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First order kinetics mean a constant ________ of the drug is elminated per unit of time and that the rate of drug elimination is __________ drug concentration.
-
First order kinetics mean a constant ________ of the drug is elminated per unit of time and that the rate of drug elimination is __________ drug concentration.
-
Lacosamide (Vimpat) should be used with caution with what type of pt?
with cardiac arrhythmias
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How is Gabapentin eliminated?
100% RENALLY
-
Common AE of Gabapentin.
- CNS depression, dizziness
- peripheral edema
-
_________ and ________ are anticonvulsants but not very effective for seizures.
- Gabapentin
- Pregabalin (Lyrica)
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_________ is more potent than Gabapentin.
Pregabalin (Lyrica)
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AE of Pregabalin (Lyrica)
Angioedema, peripheral edema
-
The only K+ channel inhibior available.
Ezogabine (Potiga)
-
Boxed warning for Ezogabine (Potiga).
- retinal abnormalities
- potential vision loss
-
Which anticonvulsant can cause urinary retention, neuropsychiatric events, & QT prolongation?
Ezogabine (Potiga)
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Common AE of all anticonvulsants.
CNS depression
-
How is Ezogabine (Potiga) metabolized?
glucorinidation & acetylation
-
Boxed warning: permanent vision loss (anticonvulsant).
Vigabatrin (Sabril)
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Stimulation of D1 receptors is ________; stimulation of D2 receptors is _________.
-
Dopamine stimulates the ________ pathway, enabling moment; and will inhibit the ________ pathway.
-
Levadopa is converted to dopamine in the CNS, but also in the __________ which can cause _________.
-
Why is carbidopa administered with Levodopa?
- Carbidopa inhibits conversion of Levadopa to dopamine in the periphery (otherwise, w/o carbidopa only 1-3% reaches CNS).
- Carbidopa does not cross BBB, so now more levadopa can cross and be converted to dopamine
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Sinemet most effective for Parkinsons, but what is the downfall?
- Pt's build a tolerance, so higher doses are needed
- "on" and "off" moments
- can lead to dyskinesias
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AE of Dopamine receptor agonists
- sedation
- vivid dreams, hallucinations
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Selegiline (Eldepryl) and rasagiline (Azilect) are __________ inhibitors.
MAO-B
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Tolcapone (Tasmar) and entacapone (Comtan) are __________ inhibitors. Which one works peripherally only?
- COMPT (an enzyme that breaks down dopamine)
- entacapone
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Trihexyphenidyl (Artane) and benztropine (Cogentin) can reduce _________ by antagonizing the _________ receptors.
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Most atypical antipsychotics are more effective at treating negative symptoms, but _________ is more effective than haloperidol at treating positive symptoms.
Risperidone
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Lower potency typical antipsychotics have more _______ effects than D2-related effects.
off-target
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___________ of dopamine improves negative symptoms.
agonism
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_________ of dopamine improves positive symptoms.
antagonism
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Side effects from blocking D2 (higher potency especially): will increase _______ symptoms and will cause ________.
-
40% D2 saturation will cause ______.
akathisia
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60% D2 saturation will improve _______.
positive symptoms
-
80% D2 saturation will cause _______.
dystonias
-
Acute EPS.
- dystonia (muscle stiffness)
- akathisia (restlessness)
-
Chronic EPS.
- pseudoparkinsonism
- tardive dyskinesia
-
What can be used to tx akathisia (restlessness)?
BB (propanolol)
-
What can be used to tx pseudoparkinsonism (rigidity, bradykinesia, tremor)?
anticholinergics; amantadine (releases dopamine)
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What can be used to tx dystonia (muscle stiffness)?
- anticholinergics restore balance
- benzos relax muscles
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S/S of NMS.
- fever (hyperthermia)
- muscle rigidity (tx w/ dantrolene, bromocriptine)
- increased CPK, myoglobin (renal failure - hydration)
- delirium
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Clozapine and Olanazapine are metabolized by _______, so smoking increases metabolism.
1A2
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MANY CNS drugs are metabolized by _______.
CYP2D6
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