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Pharmacology Exam 2 > 7 - Antiseizure Drugs > Flashcards

7 - Antiseizure Drugs Flashcards

1
Q

An event due to abnormally discharging cerebral neurons

A

Seizure

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2
Q

Recurrent seizures

A

Epilepsy

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3
Q

Abnormal electrical activity is limited to part of the brain/one cerebral hemisphere

A

Partial seizure

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4
Q

Seizure with no alteration of consciousness (consciousness is preserved)

A

Simple partial seizure

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5
Q

Seizure with altered consciousness, automatisms, & behavioral changes (consciousness is lost)

A

Complex partial seizure

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6
Q

Abnormal activity is occurs in the entire brain/both cerebral hemispheres

A

Generalized seizure

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7
Q

Seizure with increased muscle tone followed by spasms of muscle contraction & relaxation

A

Tonic-clonic seizure

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8
Q

Seizure with increased muscle tone

A

Tonic seizure

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9
Q

Seizure with rhythmic, jerking spasms

A

Myoclonic seizure

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10
Q

Seizure with sudden loss of all muscle tone

A

Atonic seizure

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11
Q

Seizure with brief loss of consciousness, with minor muscle twitches and eye blinking

A

Absence seizure

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12
Q

Which synapses have molecular targets for antiseizure drugs?

A

Excitatory glutamatergic & Inhibitory GABAergic synapses

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13
Q

Pathophysiology of Seizures at excitatory glutamateric synapse?

A

Increased excitatory amino acid (EAA) - glutamate
Increased Glu & Asp at start of seizure
Up-regulation of NMDA receptors
Increased EAA transmission & sensitivity to EAA

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14
Q

Pathophysiology of Seizures at inhibitory GABAergic synapse?

A

Decreased GABA
Decreased Cl- currents in response to GABA
Decreased binding of GABA and benzodiazepines
Decreased glutamate decarboxylase activity (synthesizes GABA)
Interfere with GABA causes seizures

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15
Q

What drugs stabilize Na+ channels?

A

(VLTPC: V Like To Proper Channel)

Valproic acid, Lamotrigine, Topiramate, Phenytoin, Carbamazepine

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16
Q

What drugs stabilize Ca2+ channels?

A

Ethosuximide, Valproic acid

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17
Q

What drugs enhance GABA transmission?

A

(BBVGVTF: BaBy V Gaba Vay Too Far)
Benzodiazepines (diazepam, clonazepam), Barbiturates (phenobarbital), Valproic acid, Gabapentin, Vigabatrin, Topiramate, Felbamate

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18
Q

What drugs inhibit EAA transmission?

A

Felbamate, Topiramate

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19
Q

What kind of seizures is Clonazepam used for?

A

Absence seizures

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20
Q

When a seizure lasts longer than 5 minutes or when seizures occur close together and the person doesn’t recover between seizures

A

Status Epilepticus

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21
Q

What are the different types of status epilepticus?

A

Convulsive & Non-convulsive

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22
Q

Which type of status epilepticus requires emergency treatment?

A

Convulsive status epilepticus

23
Q

What is Phenytoin’s MOA?

A

Inhibits Na+ channels of axons, decreasing influx of Na, also blocks Ca2+ channels at high doses

24
Q

Absorption of Phenytoin?

A

Oral absorption is less, poorly soluble in water, has high plasma protein binding

25
Q

Metabolism of Phenytoin?

A

First pass metabolism, follows zero order kinetics, metabolism occurs in liver by hydroxylation

26
Q

_______ exhibits genetic polymorphism. Responsible for variation in plasma concentration of drug by a given dose

A

Phenytoin

27
Q

What is the therapeutic plasma concentration of Phenytoin?

A

10-12 micrograms/mL

28
Q

Indications for Phenytoin?

A

1) Partial seizures: simple & complex
2) Generalized seizures: Tonic-clonic (Grandmal) and Status epilepticus
3) Arrhythmias (Digoxin toxicity)
4) Bipolar disorders

29
Q

Adverse effects of Phenytoin?

A

Nystagmus & Ataxia, Fetal hydantoin syndrome (cleft lip & cleft palate), Megaloblastic anemia

30
Q

What kind of drug is Fosphenytoin?

A

Prodrug, rapidly converts to phenytoin in body after I.V. or I.M. administration

31
Q

What are the pros of Fosphenytoin?

A

Avoids complications that come with Phenytoin (vein irritation, tissue damage, muscle necrosis, burning at site, need for lots of fluids)

32
Q

Are the toxicities of Fosphenytoin similar to Phenytoin?

A

Yes

33
Q

Indications of Fosphenytoin?

A

Admin. during Status Epilepticus

34
Q

What is the MOA of Carbamazepine?

A

Blocks Na+ channels of axons -> decreases A.P. frequency

35
Q

What are the indications for Carbamazepine?

A

Partial – simple & complex
Generalized - Tonic-clonic (grand mal seizures)
Trigeminal neuralgia
Bipolar disorder -> up regulate adenosine receptor -> block NE re-uptake

36
Q

What are Carbamazepine drug interactions?

A

Induces P450

Cimetidine & Isoniazid increase Carbamazepine

37
Q

What are the contraindications for Carbamazepine?

A

Pregnancy

38
Q

What are the adverse effects of Carbamazepine?

A 
Vertigo, Nystagmus, Ataxia, Diplopia
Sedation & Respiratory depression
Aplastic anemia - Granulocytopenia   
Megaloblastic anemia, Thrombocytopenia
Hepatotoxic
Teratogenic – Coarse facial features & Spina bifida. 
Exfoliate dermatitis
39
Q

MOA of Oxcarbazepine?

A

Blocks voltage-sensitive Na+ channels and may augment K+ channels

40
Q

What kind of drug is oxcarbazepine?

A

Considered a prodrug, its activity is attributed to monohydroxy metabolite

41
Q

What is the clinical use for Oxcarbazepine?

A

approved for monotherapy, or add-on therapy in partial seizures

42
Q

What are the adverse effects of Oxcarbazepine?

A

Some induction of P450 but much less than that seen with Carbamazapine
Sedating but otherwise less toxic than Carbamazapine

43
Q

What is the MOA for Eslicarbazepine?

A

Blocks Na+ channels of axons -> decreases A.P. frequency

44
Q

How often is Eslicarbazepine administered?

A

Once a day

45
Q

What is the MOA of Valproic Acid?

A

Blocks presynaptic Ca2+ influx in thalamus, blocks axonal Na+ channels, inhibits GABA transaminase -> increase of GABA, decrease Glutamate synthesis

46
Q

Indications of Valproic Acid?

A
  • Seizures: Generalized - Myoclonic, Atonic, Absence, Tonic-clonic
  • Migraine
  • Bipolar disorder
47
Q

Adverse effects of Valproic Acid?

A 
Ataxia, Tremor 			
Hepatotoxicity
Pancreatitis
Alopecia 			
Photosensitivity
Teratogenic (spina bifida)	
Thrombocytopenia
Inhibits platelets aggregation
48
Q

Contraindications for Valproic Acid?

A

Pregnancy

49
Q

Drug interactions with Valproic Acid?

A

Inhibits P450 enzymes

50
Q

What is the MOA of Lamotrigine?

A

Blocks voltage-sensitive Na+ channels

51
Q

What is the Clinical Use of Lamotrigine?

A

Partial seizures in adults and children. Adjuvant therapy
Generalized tonic-clonic, atonic, absence seizures. Adjuvant therapy
Lenox-Gastaut syndrome (LGS) – monotherapy
a syndrome characterized by multiple types of seizures in patients with mental retardation and other neurologic abnormalities.
Manic phase of bipolar disorder

52
Q

Metabolism of ________ is affected by Valproate, Carbamazapine, Phenobarbital, & Phenytoin

A

Lamotrigine

53
Q

Adverse Effects of Lamotrigine?

A

Less sedating than other AEDs
Severe dermatitis in 1-2% of pediatric patients
Cerebellar dysfunction, drowsiness, and rash, Stevens-Johnson syndrome.
Aseptic meningitis

Pharmacology Exam 2 (6 decks)

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