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1. Pharmacology > Anticovalent Drugs > Flashcards

Anticovalent Drugs Flashcards

1
Q

Convulsion

A

Abnormal and sudden attack of involuntary muscular contractions and relaxations (motor activity)

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2
Q

Seizures

A

Episodes of neurological dysfunction from abnormal synchronous activity of neurons

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3
Q

Epilepsy

A

A group of recurrent CNS disorders: paroxysmal cerebral dysarrythmia
Signs: seizures, convulsions or fits

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4
Q

What is required for a animals to have epilepsy?

A

Abnormal, physical, sensory and autonomic activity
At least 2 unprovoked seizures
Unconsciousness

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5
Q

Intracranial causes of epilepsy

A

Neoplasm, inflammation, hydrocephalus, malformation, trauma

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6
Q

Extracranial causes of epilepsy

A

Hepatic/renal failure, hypoxia, toxicity, hypoglycemia, hypocalcemia

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7
Q

Seizures in vet med

A

Dogs: epilepsy inherited affected 0.5-6% population
In cats and other pets it’s rare

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8
Q

Higher incidence of epilepsy in ____________

A

Belgian Shepherd

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9
Q

Therapeutic success

A

Balance between efficacy and safety

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10
Q

Therapeutic considerations of anticonvulsants

A

Eradication not reasonable
Life-time therapy
Increased risk

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11
Q

When do you start anticonvulsant drugs?

A

Seizures more than 3 minutes
Cluster seizures
More than 1 month
Worsening seizure pattern

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12
Q

Excitatory NT

A

Hypopolarize
ACh
Glutamate **
Catecholamines

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13
Q

Inhibitory NT

A

Hyperpolarize
Gamma amino butyric acid*
Glycine

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14
Q

General cellular mechanisms of seizures

A

Altered membrane function: hypoxia and hypoglycemia
Altered mem. permeability: hypoxia, inflammation and tumors
Altered ECF electrolytes: increased K, decreased Ca
NT: increased excitatory

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15
Q

General mechanisms of seizures

A

Inappropriate neuronal discharge (inititation)
Recruitment
Synchronization
Propagation

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16
Q

What drugs enhance GABA inhibition

A

Increases GABAergic transmission
Barbiturates and Benzodiazepine

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17
Q

Important Barbiturates

A

Phenobarbital (luminal)
Primidone (Mysoline)

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18
Q

Important benzodiazepine drugs

A

Diazepam (valium)
Clonazepam (klonopin)

19
Q

Phenobarbital

A

Historic 1st choice chronic management
Increase GABA, decrease glutamine and Ca
Attenuates initiation, decreased progagation
100% F with long half life

20
Q

Phenobarbital drug interactions

A

Potent induction of CYP 450
Decreased clearance
Auto-induction in 2-4 weeks

21
Q

Phenobarbital behavioral side effects

A

Polyphagia, polydipsia, polyuria
Sedation (ataxia and grogginess)

22
Q

Phenobarbital in the bone marrow

A

Type B (allergic)- leukopenia
Requires 10-14 days or previous exposure

23
Q

Phenobarbital hepatotxocity

A

Type A (dose and duration dependent)
Limits maximum therapeutic range
Increased serum alk phos and bile acids
Decreased albumin and BUN

24
Q

Primidone (Mysoline)

A

Partial and generalized seizures

25
Q

Bromide

A

1st add-on
Common 1st choice for chronic conditions

26
Q

Diazepam

A

Historic 1st choice acute management
t 1/2= 2-4 hours in dogs
Treats status epilepticus/ emergency use
Given in bolus, rectum or infusion
Decreases spinal reflexes

27
Q

Diazepam in cats

A

For maintenance in cats but can cause hepatic necrosis

28
Q

Levetiracetam

A

New add-on against refractory epilepsy in dogs and cats
Prevents postoperative serizures in protosystemic shunt surgery in dogs

29
Q

PK of Levetiracetam

A

100% absorption and <10% protein binding
Cats t1/2= 3 h, dogs t1/2=3- 4.5

30
Q

Which bensodiazepine drugs are approved for long-term treatment?

A

Clonazepam (myclonic, atonic and absence seizures) and clorazepate (partial seizures)

31
Q

Na+ channel inhibitors

A

Anti-seizure drug
Blocks voltage-gated Na channels by selectively binding to channel in the inactive state and slowing the rate of recovery

32
Q

Phenytoin (Dilantin, Phenytek)

A

Occ. in horses for muscle disorders/ antiarrhythmic agent
Limited in vet use due to side effects and variable PK

33
Q

Valproic Acid (Depankene)

A

Increases GABA production and GABA metabolism
Dogs when refractory to other meds

34
Q

Valproic Acid PK

A

100% bioavailability
T 1/2 = 1-2.8 hours dogs

35
Q

T calcium channel

A

Found in heart and neurons
Short, small and low threshold

36
Q

L calcium channel

A

Muscle, neurons, endocrine cells, bone
Long, large and high threshold

37
Q

Gabapentin (neurontin)

A

Selective inhibition of v-g N type and T-type Ca2+ channels
Add on therapy in dogs and cats
t 1/2 = 2-4 hours in dogs and cats

38
Q

Pregabalin (lyrica)

A

Selective inhibition of v-g N type and T-type Ca2+ channels
Add on for partial and secondarily generalized seizures
Neuropathic pain, fibromyalgia in equine, canines and felines

39
Q

Felbamate

A

Add-on in dogs with t1/2 of 5-6 hours
Blocks voltage dependent Na+ channels
Inhibits Ca2+ channels

40
Q

What does Felbamate compete with

A

Glycone- binding site on NMDA glutamate receptor

41
Q

Bromide therapy

A

Liver disease (sole anticonvulsant)
t1/2 in dogs 25 days

42
Q

Bromide toxicosis in dogs and cats

A

CNS depression, weakness, ataxia, decreased proprioception
Polyphagia, PU/PD and behavior change in dogs
Respiratory signs (asthma)- cats

43
Q

Impact of short half-life compared to dosing interval

A

Fluctuation during dosing interval
No accumulation (shortens interval)
Clearing out quickly

44
Q

Impact of long half-life compared to dosing interval

A

Minimal fluctuation during dose interval
Protected against breakthrough seizures
Accumulation dramatic (steady-state in therapeutic range)

1. Pharmacology (29 decks)

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