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Pharm > Antiepileptics & Neurologically Active Drugs > Flashcards

Antiepileptics & Neurologically Active Drugs Flashcards

1
Q

How do you ensure a single dose missed will not result in sub-therapeutic plasma concentrations

A

Dosing at 1/2 the drugs elimination half-time

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2
Q

Carbamazepine

A

MOA: inhibition of Na & Ca channel

Targeted seizure: nonconvulsive/convulsive, Partial/generalized

Dosage: 10-40 mg/kg per day in 2-3 divided doses

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3
Q

Gabapentin

A

MOA: inhibition of Ca channels; decreases synaptic Glutamate release

Target seizures: Partial & Generalized

Dosage: 10-60 mg/kg per day

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4
Q

Phenobarbital

A

MOA: inhibits GABA & excitatory postsynaptic actions of glutamate; prolongs Cl channel opening (limits sprees of sz & increases sz threshold)

Targeted seizures: all EXCEPT nonconvulsive primary generalized

Dosage: 2-5 mg/kg per day everyday or in 2 divided doses

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5
Q

Phenytoin

A

MOA: Na ion channel blockade, Ca ion channels, NMDA receptors

Targeted seizures: partial & generalized

Dosage: 3-4 mg/kg per day in 3 divided doses
“Long duration so single daily dosage”??

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6
Q

Topiramate

A

MOA: Na ion channel blockade, enhanced GABA activity, Glutamate antagonism, Ca ion channel blockade

Targeted seizures: partial & generalized tonic-clonic, absence sz

Dosage: 500-3,000 mg per day in 2-4 divided doses

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7
Q

Valproate

A

MOA: Na ion channel blockade, Ca ion channels

Targeted seizures: all primary generalized epilepsies and all convulsive epilepsies

Dosage: 500- 3,000 mg per day in 2-4 divided doses

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8
Q

The ONLY agent requiring routine monitoring

A

Phenytoin

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9
Q

Factors that may facilitate the spread of a seizure focus into areas of the normal brain:

A 
Blood glucose concentrations
PaO2
PaCO2
pH
Endocrine function
Stress
Fatigue
Electrolyte balance
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10
Q

What happens if the spread of a seizure focus is extensive enough the entire brain is activated?

A

Tonic-clinic seizure w/ unconsciousness

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11
Q

Frontal lobe

A

Controls muscle movements, thinking, and judgement

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12
Q

Parietal lobe

A

Controls sense of touch, response to pain and temperature, and understanding of language

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13
Q

Occipital lobe

A

Controls vision

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14
Q

Temporal lobe

A

Controls hearing and memory

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15
Q

Cerebellum

A

Controls balance

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16
Q

Brain stem

A

Controls breathing and regulates heartbeat

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17
Q

How do antiepileptic drugs control seizures?

A

By decreasing neuronal excitability
Or
By enhancing inhibition of neurotransmitters

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18
Q

Selectively blocks the T-type calcium ion current which is thought to act as a pacemaker for the thalamus neurons and may be important in absence seizures

A

Ethosuximide

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19
Q

Drugs used for partial seizures w/ acceptable side effects

A 
Carbamazepine
Lamotrigine
Oxcarbazepine
Topiramate
Zonisamide
Phenytoin
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20
Q

drugs used to treat generalized seizures

A

Valproate
Lamotrigine
Tompiramate

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21
Q

Drugs effective in tx of generalized non convulsive seizures & especially absence seizures

A

Ethosuximide
Lamotrigine
Valproate

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22
Q

______ & _______ have more than double the risk of fetus w/ congenital malformations (spina bifida)

A

Valproate; Carbamazepine

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23
Q

Carbamazepine characteristics

A

O: rapid oral

P: 2-6 hrs

D: plasma elimination half-time is 8-24 hrs

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24
Q

Carbamazepine E/M

A

Plasma elimination half-time 8-24 hrs

B/c of it’s metabolism, increased dosing may be needed in 2-4 wks

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25
Carbamazepine considerations
70-80% protein bound Side effects: sedation, vertigo, diplopia, N/V, chronic diarrhea Rare but life threatening: SIADH, Aplastic anemia, Thrombocytopenia, Hepatocellular & cholestatic jaundice, oliguria, HTN, cardiac dysrhythmias, WBC suppression High plasma conc. has arginine vasopressin hormone like actions resulting in hyponatremia
26
Drugs that inhibit metabolism of carbamazepine enough to cause toxic effects: (6)
``` Cimetidine Propoxyphene Diltiazem Verapamil Isoniazid Erythromycin ```
27
Ethosuximide MOA
Acts by decreasing voltage-dependent Ca conductance in thalami neurons
28
Ethosuximide indications
Drug of choice for suppression of absence (petit mal) epilepsy in pts who do not also have tonic-clonic seizures
29
Ethosuximide E/M
M: hepatic microsomes enzymes E: 25% excreted unchanged in urine
30
Ethosuximide dosage
20-30 mg/kg
31
Phenobarbital indications
Long acting. Effective against ALL seizure types except nonconvulsive primary deneralized seizures
32
Phenobarbital pharmacokinetics
PO absorption slow but nearly complete Peak conc: 12-18 hrs Plasma protein binding: 48%-54%
33
Phenobarbital E/M
E: 25% by pH-dependent renal excretion M: remainder inactivated by hepatic microsomal enzymes
34
Phenobarbital plasma concentration
10-40 mcg/ml
35
Phenytoin plasma concentrations
Seizure control: 10-20 mcg/ml Dig-induced cardiac dysrhythmias: 0.5-1.0mg/kg IV q 15-30 min (max 15mg/kg)- 8-16 mcg/ml
36
Valproic acid indications
Effective in tx of all primary generalized and all convulsive epilepsies
37
What causes Parkinson’s Disease?
Results from loss of dopaminergic neurons in the substantia nigra pars compacta region of the basal ganglia
38
Where is dopamine located?
80% located in basal ganglia, mostly in the caudate nucleus and putamen
39
% of protein binding for Gabapentin
0%
40
Meds relying on renal excretion & may need adjusting according to renal fx
``` Gabapentin Pregabalin Levetiracetam Vigabatrin Zonisamide ```
41
Drug clearance & elimination half-times that take hours
Carbamazepine (8-24 hrs) Valproate (7-17 hrs) Primidone (4-12 hrs) Gabapentin (6 hrs)
42
Drug clearance and elim. Half-times that take days
Phenytoin (9-40 hrs avg 24hrs) Lamotrigine (25 hrs) Phenobarbital (72-144 hrs) Zonisamide (50-70 hrs)
43
All antiepileptic drugs may be associated w/ drug interactions resulting in interactions of plasma drug concentrations EXCEPT:
Gabapentin Levetiracetam Vigabatrin
44
Highly bound protein drugs:
Phenytoin (90%) Valproate (>80%) Carbamazepine (70-80%)
45
________ can result in increased plasma concentrations of unbound antiepileptics resulting in toxicity despite therapeutic levels
Hypoalbunemia (except in pregnancy)
46
Which drug produces nhibitory effect on AP ONLY by delaying reactivation of Na channels during high frequency neuronal firing?
Primidone
47
Drugs that act on both Na and Ca channels
Phenytoin Carbamazepine Valproate Lamotrigine
48
Patients develop a tolerance & sedation is common side effect of this drug
Clonazepam
49
This drug is reserved for selected pts w/ uncontrolled seizures d/t its side effects
Felbamate
50
This drug is a recent benzo derivative that does not cause sedation & can be used long term bc tolerance is uncommon
Clobazam
51
Carbamazepine accelerates metabolism of: (5)
``` Ethosuximide Valproic acid Corticosteroids Anticoagulants Antipsychotics ```
52
decreases frequency of seizures associated w/ Lennox-Gastaut Syndrome & myotonic & atonic forms of epilepsy Used principally for poorly controlled partial and secondarily generalized seizures
Felbamate
53
Felbamate MOA may involve ____, ____, & ___ voltage-gated currents
NMDA, GABA, Ca
54
Keto analogue of carbamazepine that provides equivalent seizure control w/ fewer S/E. Does NOT induce hepatic microsomal enzymes or displace other drugs from plasma protein binding
Oxcarbazepine
55
PO & IV Juvenile myoclonic epilepsy & partial & generalized convulsive seizures Binds to presynaptic Ca channels to reduce NT release Minimal protein binding & no drug interaction
Levetiracetam
56
Acts by stabilizing Na channels, preventing release of aspartame & glutamate Partial or generalized seizures & children w/ Laennox-Gastaut syndrome
Lamotrigine
57
Phenobarbital MOA
GABA, inhibition of glutamate Limits spread of sz activity and increases sz threshold
58
______ causes tolerance to sedation (requires more) with chronic therapy
Phenobarbital
59
Accelerated metabolism of many lipid soluble drugs
Phenobarbital
60
High therapeutic index & not accompanied by excessive sedation Can be given acutely to achieve effective plasma concentrations w/in 20 min
Phenytoin
61
Should not exceed 50mg/min in adults or 1-3mg/kg in peds to prevent severe hypotension and cardiac arrhythmias
Phenytoin
62
With Phenytoin, a greater fraction remains unbound in _____, _____, & _____
Neonates; hypoalbuminemia; uremic pts
63
With Phenytoin, concentrations <10mcg/ml follow ____ order kinetics & elim. H/t is 24 hrs
First
64
With phenytoin, concentrations >10mcg/ml follow ____ order kinetics and elim becomes dose dependent
Zero
65
Gingival hyperplasia is the most common side effect of?
Phenytoin
66
Valproic acid pharmacokinetics
Peak plas. Conc.: 1-4 hrs Elim h/t: 7-17 hrs Therapeutic plasm conc: 50-100 mcg/ml
67
Hepatotoxicity can occur in children under 2 with this drug
Valproic acid
68
Infrequent S/E of valproic acid
Sedation & ataxia
69
May have falsely high positive ketone results
Valproic acid & levodopa
70
Valproic acid can displace ____ & ____ from protein binding sites resulting in increased pharmacological effects by the displaced drugs
Phenytoin; diazepam
71
What can cause plasma concentrations of phenobarbital to increase 50%. If you see these 2 drugs together, d/c which one?
Valproic acid; phenobarbital
72
Valproic acid does or does not interfere with oral contraceptives?
Does not
73
____ acts as an inhibitory neurotransmitter while ____ acts as an excitatory neurotransmitter
Dopamine; ACh
74
Crosses BBB and is converted to dopamine Replenishes dopamine stores in basal ganglia Usually administered with a peripheral decarboxylase inhibitor
Levodopa
75
How do decarboxylase inhibitors work with levodopa?
They maximize entrance of levodopa into brain before it is converted to dopamine
76
What meds should not be stopped for surgery?
Seizure meds Beta Blockers Levodopa
77
Most common s/e with levodopa and dopamine agonists
Nausea and hypotension
78
metabolites color urine red then black upon exposure to air
Levodopa
79
May cause false positive coomb’s test
Levodopa
80
This drug can cause severe skeletal muscle rigidity and pulmonary edema in Parkinson’s patients. Has produce Parkinson’s disease like syndrome in otherwise healthy patients
Droperidol | Sudden antagonism of Dopamine
81
____ increases metabolism of Levodopa in the circulation before it can enter CNS in doses as low as 5 mg
Vitamin B
82
These drugs slow elimination of carbidopa-levodopa increasing plasma concentration 10-15%
COMT inhibitors (Tolcapone or Entacapone)
83
Bromocriptine
Synthetic dopamine agonist | Extensive first-pass hepatic metabolism with >90% excreted in bile
84
CNS stimulant used for resp depression Vt causes > increase in minute ventilation than breathing frequency 1mg/kg IV is similar to that produced by PaO2 of 38 mmHg
Doxapram

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