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RUSVM Pharmacology > Muscle Relaxants and AEDs > Flashcards

Muscle Relaxants and AEDs Flashcards

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1
Q

What are the anti-tremorogenic and sedating drugs

A

Methocarbamol
Guaifenasin
Dantrolene

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2
Q

What re the antiepilieptic drugs

A 
Diazepam and midazolam 
Phenobarbital 
Bromide 
Levetricetam 
Zonisamide
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3
Q

What is the site of action of dantrolene?

A

Peripheral -muscle cells

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4
Q

What is the site of action of guaifensin?

A

Central -> spinal cord

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5
Q

What is the site of action of methocarbamol

A

Central -> spinal cord

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6
Q

What is the MOA of dantrolene?

A

Peripherally acting muscle relaxant -> acts on the muscle cell

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7
Q

T/F: dantrolene crosses the BBB

A

F

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8
Q

What is the drug of choice for treatment of malignant hyperthermia (hypermetabolic syndrome)

A

Dantrolene

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9
Q

What is hypermetabolic syndrome

A

Idiosyncratic drug reaction
Hyper metabolic rxn on skeletal muscle -> rhabdomyolysis

Life threatening hyperthermia, hyperkalemia, and cell death
Multiple organ dysfunction syndrome (MODS)

Often fatal

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10
Q

__________ are very toxic to dogs and can lead to malignant hyperthermia

A

Hops

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11
Q

What are the clinical uses of dantrolene

A

Malignant hyperthermia

Tetanus –> cause muscle relaxation

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12
Q

What is the MOA of methocarbamol?

A

Blockade of nerve impulse transmission in the spinal cord

Cross the BBB

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13
Q

What is the main clinical use of methocarbamol?

A

Reduce muscle spasm (approved in cat, dog, and horse)

  • > tetanus
  • > intoxication (tremorogenic)

Treatment of acute inflammatory or traumatic conditions (eg intervertebral disk disease )

Functional urethral obstruction/urinary retention (less common use)

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14
Q

What is the half life of methocarbamol

A 
Relatively short (1-2hrs) 
Shorter when given IV
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15
Q

How is methocarbamol administered

A

Oral or IV

Irritating if administered IM/SQ -> not recommended

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16
Q

Strychnine, metaldehyde, pyrethrin(cat) and some toxic molds are treated with ____________ to reduce treorogenic toxins

A

Methocarbamol

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17
Q

What are the side effects of methocarbamol ?

A

Sedation, salivation, weakness, lethargy, and ataxia

Caution using injectable form with renal disease

Avoid extravasation and administer IV slowly

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18
Q

What is the MOA of Guaifensin

A

Centrally-acting muscle relaxant and expectorant (break up a cough)

Blocks nerve impulse transmission in spinal cord, brain stem and subcortical areas of the brain -> cross BBB

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19
Q

What is the onset and duration of guaifensin

A

Rapid onset and short duration (10-20min)

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20
Q

What are the clinical uses of guaifensin ?

A

Intubation -> relax pharyngeal and laryngeal muscles

Procedural sedation in horse and cattle
-> Guaifensin + Xylazine + ketamine (triple drip)

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21
Q

What are precautions to using guaifensin

A

High concentration causes hemolysis

Cattle more sensitive than horse

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22
Q

______________ drug is contraindicated in horse receiving guaifensin

A

Physostigmine

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23
Q

________ is a clinical manifestation of abnormal electrical activity in the brain (uncontrolled firing of neurons)

A

Seizure

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24
Q

_________ is a chronic syndrome of seizures occurring intermittently over months to years

A

Epilepsy

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25
__________________ is 'true epilespy' and is genetic
Idiopathic
26
______________ epilepsy has intracranial vs extra-cranial causes
Acquired/symptomatic
27
________________ seizures is when more than one seizure occurs within a 24hr period with recovery inbetween
Cluster
28
____________________ is when you have repeated seizures without full recovery between them or a single seizure that lasts > 5mins
Status epilepticus (SE)
29
_____________ drugs prevent or treat seizures
Anticonvulsants
30
_______________ drugs generally refers to maintenance management of epileptic seizures
Antiepileptic drugs (AED)
31
_____________ seizures do not respond to therapeutic doses of AEDs
Refractory
32
_______________ seizures occur at periodic intervals during treatment course with AEDs
Breakthough
33
What are the types of seizures
Generalized - convulse - non-convulsive (absent) Partial - simple (lateralizing motor activity, no loss of consciousness) - complex (altered motor activity and consciousness)
34
What is the major excitatory neurotransmitter in the brain?
Glutamate -> depolarization | -interact with NMDA, AMPA and kainate receptors
35
What is the major inhibitory neurotransmitter in the brain
GABA (hyperpolarization) | -interact with GABA receptor (Gprotein coupled)
36
Pyrethrum, rhododendrons, spider, and scorpion bites effect the ___________ channels and will cause (excitation or inhibition) of neurons
Sodium (inhibits inactivation of Na channel) | Excitation
37
Organophosphate and carbamate cause ___________________ stimulation leading to increased neuronal excitation
Cholingergic
38
Clads, amanita mushrooms, and algae cause _____________stimulation that leads to increased neuronal stimulation
Glutamtergic
39
Caffeine, therophyline, aminophylleine, and theobromine cause ________________ toxicosis leading to increased neuronal excitation
Methylxanthine
40
Strychnine has _______________ antagonism causing decreased neuronal inhibition
Glycine -> a inhibitory neurotransmitter
41
What are the three main ways of AED action?
Reduction of excitatory transmission Enhancement of inhibitory process Modulation of membrane cation conductance
42
How can an AED reduce excitatory transmission?
Decrease excitatory neurotransmitters: Glutamate | Na channel blockade
43
How can an AED enhance inhibitory processes ?
Increase inhibitory neurotransmitter : GABA | Hyperpolarize postsynaptic membrane (GABAa: chloride permeability)
44
How can an AED modulate membrane cation conductance
Block voltage-gated inward positive currents: Na or Ca Increase outward positive current: K
45
What are the therapeutic goals of an AED
Emergency (acute) treatment - seizure in progress - risk of kindling seizures Maintenance (chronic) treatment - reduce frequency or severity of seizures - reduce time between breakthrough seizures (if occurring) and reduce severity/duration
46
What is the drug of choice to stop a seizure in progress?
Diazepam (intranasal or per rectum)
47
What is the onset and duration of diazepam?
``` Rapid (immediate) Short duration (2-4hrs) ```
48
What drug can be used to stop a seizure in progress if there is not IV access?
Midazolam (IM)
49
What two benzodiazepines can be used in acute therapy of seizures
Diazepam | Midazolam
50
What drug can be used in acute therapy of a seizure that is neuroprotective, but it will have a slower onset but a longer duration than benzodiazepines
Phenobarbital (IV) Will also have sedative effect because it is a barbiturate
51
What drugs will mask seizure activity but does not have true anticonvulsant effects?
Propofol or Alfaxalone (IV)
52
What is a con to using propofol to control seizures
Very rapid but short acting | Airway protection required -> intubate
53
How can seizures be controlled at home?
Diazepam intranasally or rectally Controlled substance-> legalities to consider Cannot be stored in a plastic container/syringe (will bind plastic)
54
When should a patient receive maintenance therapy for seizures?
Treatable underlying cause of seizure has been ruled out Status epilepticus Cluster seizures Seizure starts within a week of head injury More than 2-3 seizures in 6-12months
55
Why can diazepam not be given orally to cats?
Hepatotoxicity
56
Cats give bromide are at risk for developing _________
Asthma/ pneumonitis
57
T/F: dantrolene crosses the BBB
F | Peripherally active muscle relaxant
58
What is given to treat tremorogenic toxicity, such as topical permethrin in cats?
Methocarbamol
59
What are the 3 main causes of a seizure?
``` Intracranial lesion (symptomatic epilespy) Extracrainial lesion (reactive epilepsy) Primary disorder (idiopathic disorder) ```
60
What features does the ideal AED have?
Effective -> broad spectrum regardless of underlying cause Safe Long half life-> SID or BID Anti-epileptogenic effects Enteral and parenteral Affordable/sustainable for long time use
61
What are the AEDs?
Phenobarbital Bromide Levetricetam Zonisamide
62
What is the most common first-line AED for chronic therapy?
Phenobarbital (oral and IV)
63
What is the MOA of phenobarbital?
GABA agonist | -> potentiates the inhibitory effects of GABA by binding and prolonging opening of Cl- channels
64
how is phenobarbital metabolized?
Liver POTENT inducer of hepatic microsomal enzymes (cytochrome P450) and metabolized through this system May develop tolerance due to enzyme induction (monitor levels) and may increase rate of degradation of other drugs using this pathway
65
What are precautions to using phenobarbital ?
``` PU/PD/PP Sedation(transient) Elevated liver enzymes - high ALP-> induced by steroid and phenobarbital - high ALT -> liver damage ```
66
What AED is the least appropriate for a patient with liver damage/dysfunction
Phenobarbital
67
What is the MOA of bromide?
Alters Cl- transport across neuronal cell membranes | Anticonvulsant -salt/chemical powder
68
Who is bromide use contraindicated in and why?
CAT | Asthma like change that can cause acute respiratory distress
69
How is bromide excreted?
Unchanged by kideny
70
What is the duration of bromide
Long half life (24days)-> 2-3months to reach steady state (shortened if loading dose used)
71
What are precautions to bromide use?
Interfere with Cl- on serum chemistry-> reads as false high Changes in Cl- ion concentration can significantly interfere with bromide levels (increased Cl- causes increased Br excretion in kidney) -> keep salt intake constant Asthma like change (contraindicated in cats!) Plasma drug concentration monitoring
72
What can be seen with bromism?
Bromism= toxicity with overdose of bromide Severe sedation and neurological signs -> treat with 0.9%NaCl to promote excretion Pancreatitis (range of GI signs)
73
What is the MOA of Levetricetam?
We think it binds to synaptic vesicle protein SV2A -> decrease neurotransmitter release But we dont really know so.. just FYI
74
What is the duration of action of levetricetam ?
Very short half life (3-4hrs)
75
How is levetricetam excreted?
Unchanged in the urine
76
What is the preferred treatment of seizures due to hepatic encephalopathy ?
Levetricetam
77
Is therapeutic blood level monitoring required for levetricetam ?
Nope
78
What are the clinical uses of levetricetam ?
IV for acute seizure treatment Oral dose for maintenance therapy Pulse therapy around breakthrough seizures -> given 3-5days following a breakthrough seizure Tolerated in cats and doggos
79
What are precautions to using levetricetam ?
Sedation/ataxia-> dose dependent (transient with oral therapy) Inappetence, salivation, lethargy in cats Caution with decreased renal clearance Tolerance
80
What is the MOA of Zonisamide
Inhibits voltage-gated sodium channels ->stabilize neurons | NOT on GABA receptors
81
Where is zonisamide excreted
Urine (80%) | Liver
82
Do you need to monitor therapeutic blood levels of zonisamide?
Nope
83
What are the clinical uses of zonisamide?
Oral capsule only Adjunct AED agent (2nd or 3rd line add-on drug) for maintenance therapy In Cato and doggo
84
What are precautions to using zonisamide ?
Well tolerated overall - hepatopathy - GI signs and somnolence (depression) in cats Sulfonamides chemical structure - idiosyncratic rxn - monitor CBC after initiating treatment
85
What drugs do we monitor therapeutic drug levels?
Phenobarbital and bromide (kBr)
86
What drug has anticonvulsant effects through inhibition of voltage-gated sodium channels in the CNS
Zonisamide
87
What AED has the shortest and longest half life in doggo?
Longest- bromide | Shortest- levetiracetam
88
Why is bromide contraindicated for use in cats?
Bronchopulmonary changes

RUSVM Pharmacology (18 decks)

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