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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
Q

Carbamazepine considerations

A

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

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26
Q

Drugs that inhibit metabolism of carbamazepine enough to cause toxic effects: (6)

A 
Cimetidine
Propoxyphene
Diltiazem
Verapamil
Isoniazid
Erythromycin
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27
Q

Ethosuximide MOA

A

Acts by decreasing voltage-dependent Ca conductance in thalami neurons

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28
Q

Ethosuximide indications

A

Drug of choice for suppression of absence (petit mal) epilepsy in pts who do not also have tonic-clonic seizures

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29
Q

Ethosuximide E/M

A

M: hepatic microsomes enzymes

E: 25% excreted unchanged in urine

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30
Q

Ethosuximide dosage

A

20-30 mg/kg

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31
Q

Phenobarbital indications

A

Long acting. Effective against ALL seizure types except nonconvulsive primary deneralized seizures

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32
Q

Phenobarbital pharmacokinetics

A

PO absorption slow but nearly complete

Peak conc: 12-18 hrs

Plasma protein binding: 48%-54%

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33
Q

Phenobarbital E/M

A

E: 25% by pH-dependent renal excretion

M: remainder inactivated by hepatic microsomal enzymes

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34
Q

Phenobarbital plasma concentration

A

10-40 mcg/ml

35
Q

Phenytoin plasma concentrations

A

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
Q

Valproic acid indications

A

Effective in tx of all primary generalized and all convulsive epilepsies

37
Q

What causes Parkinson’s Disease?

A

Results from loss of dopaminergic neurons in the substantia nigra pars compacta region of the basal ganglia

38
Q

Where is dopamine located?

A

80% located in basal ganglia, mostly in the caudate nucleus and putamen

39
Q

% of protein binding for Gabapentin

A

0%

40
Q

Meds relying on renal excretion & may need adjusting according to renal fx

A 
Gabapentin
Pregabalin
Levetiracetam
Vigabatrin
Zonisamide
41
Q

Drug clearance & elimination half-times that take hours

A

Carbamazepine (8-24 hrs)
Valproate (7-17 hrs)
Primidone (4-12 hrs)
Gabapentin (6 hrs)

42
Q

Drug clearance and elim. Half-times that take days

A

Phenytoin (9-40 hrs avg 24hrs)
Lamotrigine (25 hrs)
Phenobarbital (72-144 hrs)
Zonisamide (50-70 hrs)

43
Q

All antiepileptic drugs may be associated w/ drug interactions resulting in interactions of plasma drug concentrations EXCEPT:

A

Gabapentin
Levetiracetam
Vigabatrin

44
Q

Highly bound protein drugs:

A

Phenytoin (90%)
Valproate (>80%)
Carbamazepine (70-80%)

45
Q

________ can result in increased plasma concentrations of unbound antiepileptics resulting in toxicity despite therapeutic levels

A

Hypoalbunemia (except in pregnancy)

46
Q

Which drug produces nhibitory effect on AP ONLY by delaying reactivation of Na channels during high frequency neuronal firing?

A

Primidone

47
Q

Drugs that act on both Na and Ca channels

A

Phenytoin
Carbamazepine
Valproate
Lamotrigine

48
Q

Patients develop a tolerance & sedation is common side effect of this drug

A

Clonazepam

49
Q

This drug is reserved for selected pts w/ uncontrolled seizures d/t its side effects

A

Felbamate

50
Q

This drug is a recent benzo derivative that does not cause sedation & can be used long term bc tolerance is uncommon

A

Clobazam

51
Q

Carbamazepine accelerates metabolism of: (5)

A 
Ethosuximide
Valproic acid
Corticosteroids
Anticoagulants
Antipsychotics
52
Q

decreases frequency of seizures associated w/ Lennox-Gastaut Syndrome & myotonic & atonic forms of epilepsy

Used principally for poorly controlled partial and secondarily generalized seizures

A

Felbamate

53
Q

Felbamate MOA may involve ____, ____, & ___ voltage-gated currents

A

NMDA, GABA, Ca

54
Q

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

A

Oxcarbazepine

55
Q

PO & IV
Juvenile myoclonic epilepsy & partial & generalized convulsive seizures
Binds to presynaptic Ca channels to reduce NT release
Minimal protein binding & no drug interaction

A

Levetiracetam

56
Q

Acts by stabilizing Na channels, preventing release of aspartame & glutamate
Partial or generalized seizures & children w/ Laennox-Gastaut syndrome

A

Lamotrigine

57
Q

Phenobarbital MOA

A

GABA, inhibition of glutamate

Limits spread of sz activity and increases sz threshold

58
Q

______ causes tolerance to sedation (requires more) with chronic therapy

A

Phenobarbital

59
Q

Accelerated metabolism of many lipid soluble drugs

A

Phenobarbital

60
Q

High therapeutic index & not accompanied by excessive sedation

Can be given acutely to achieve effective plasma concentrations w/in 20 min

A

Phenytoin

61
Q

Should not exceed 50mg/min in adults or 1-3mg/kg in peds to prevent severe hypotension and cardiac arrhythmias

A

Phenytoin

62
Q

With Phenytoin, a greater fraction remains unbound in _____, _____, & _____

A

Neonates; hypoalbuminemia; uremic pts

63
Q

With Phenytoin, concentrations <10mcg/ml follow ____ order kinetics & elim. H/t is 24 hrs

A

First

64
Q

With phenytoin, concentrations >10mcg/ml follow ____ order kinetics and elim becomes dose dependent

A

Zero

65
Q

Gingival hyperplasia is the most common side effect of?

A

Phenytoin

66
Q

Valproic acid pharmacokinetics

A

Peak plas. Conc.: 1-4 hrs
Elim h/t: 7-17 hrs
Therapeutic plasm conc: 50-100 mcg/ml

67
Q

Hepatotoxicity can occur in children under 2 with this drug

A

Valproic acid

68
Q

Infrequent S/E of valproic acid

A

Sedation & ataxia

69
Q

May have falsely high positive ketone results

A

Valproic acid & levodopa

70
Q

Valproic acid can displace ____ & ____ from protein binding sites resulting in increased pharmacological effects by the displaced drugs

A

Phenytoin; diazepam

71
Q

What can cause plasma concentrations of phenobarbital to increase 50%. If you see these 2 drugs together, d/c which one?

A

Valproic acid; phenobarbital

72
Q

Valproic acid does or does not interfere with oral contraceptives?

A

Does not

73
Q

____ acts as an inhibitory neurotransmitter while ____ acts as an excitatory neurotransmitter

A

Dopamine; ACh

74
Q

Crosses BBB and is converted to dopamine

Replenishes dopamine stores in basal ganglia

Usually administered with a peripheral decarboxylase inhibitor

A

Levodopa

75
Q

How do decarboxylase inhibitors work with levodopa?

A

They maximize entrance of levodopa into brain before it is converted to dopamine

76
Q

What meds should not be stopped for surgery?

A

Seizure meds

Beta Blockers

Levodopa

77
Q

Most common s/e with levodopa and dopamine agonists

A

Nausea and hypotension

78
Q

metabolites color urine red then black upon exposure to air

A

Levodopa

79
Q

May cause false positive coomb’s test

A

Levodopa

80
Q

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

A

Droperidol

Sudden antagonism of Dopamine

81
Q

____ increases metabolism of Levodopa in the circulation before it can enter CNS in doses as low as 5 mg

A

Vitamin B

82
Q

These drugs slow elimination of carbidopa-levodopa increasing plasma concentration 10-15%

A

COMT inhibitors (Tolcapone or Entacapone)

83
Q

Bromocriptine

A

Synthetic dopamine agonist

Extensive first-pass hepatic metabolism with >90% excreted in bile

84
Q

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

A

Doxapram

Pharm (15 decks)

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