Neurological and neuromuscular Pharm

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  1. phenobarbital (Luminal)
    Barbiturate (GABAa receptor agonist)
    • Therapeutic class: antiseizure; sedative
    • Preg: D
    • MOA: Long acting barb, potentiates GABA neurotransmitter which suppresses abnormal neuronal discharge and causes CNS depression.
    • Indications: Seizures, insomnia
    • Contraindications: severe uncontrolled pain, pre-existing CNS depression, porphyria (Red blood cell proteins), severe respiratory depression, dyspnea, COPD caution, glaucoma.
    • Adverse: drowsiness, vitamin deficiencies, laryngospasms, severe respiratory depression(hypersensitivity), coma/ death. 
    • Alerts: should not be used with other CNS depressants-may lead to life threatening respiratory depression. Also increases the metabolism of other drugs decreasing effectiveness, soft tissue irritant-vesicant.
  2. diazepam (Valium)
    Benzodiazepine (GABAa receptor agonist)
    • Therapeutic class: antiseizure
    • Preg: D
    • MOA: binds to GABA receptors-chloride channels throughout the CNS, suppresses neuronal activity and subsequent impulses that might be transmitted to the reticular activating system. Potentiates GABA.
    • Indications: seizures, muscle spasms
    • contraindications: when given IM should be avoided for shock, coma, depressed vital signs, OB patients, infants less than 30 days, or within 14 days of an MAOI
    • Adverse: More SE with IM use: hypotension, muscular weakness, tachycardia, respiratory depression.
    • Alerts: avoid concurrent use with other CNS depressants. increases levels of phenytoin in bloodstream which may lead to phenytoin toxicity.
    • Antidote: flumazenil
  3. phenytoin (Dilantin) 
    Hydantoin (suppress sodium influx)
    • Therapeutic class: antiseizure; antidysrhythmic
    • Preg: D
    • MOA: desensitizing sodium channels in the CNS which prevents the spread of disruptive electrical charges in brain.  also has antidysrhythmic activity similar to lidocaine. 
    • Indications: seizures
    • contraindications: rashes, seizures due to hypoglycemia, sinus bradycardia and heart blocks
    • Adverse: May cause dysrhythmias, bradycardia, V-fib, severe hypotension, hyperglycemia, headaches, nystagmus, ataxia, confusion slurred speech, paradoxical nervousness, twitching and insomnia, (agranulocytosis and aplastic anemia)
    • Alerts: Interacts with many drugs and when combined with tricyclic antidepressants may trigger seizures. Can lower dexamethasone levels in the body. No reversal for this medication. only mix with saline when given IV-D5 will cause percipitation-most antiseizure medications require 2 forms of birth control.
  4. valpoic acid (Depakene, Depakote)
    Valproate
    • Therapeutic class: Antiseizure drug
    • Preg: D
    • MOA: similar action to that of phenytoin, also similiar effects on GABA and calcium channels such as the succinimides and benzo. 
    • Indications:  seizures, mixed type seizures, absence seizures, migraines and treatment of bipolar disorder.
    • Contraindications: hepatic disease, bleeding dysfunctions, pancreatitis, metabolic disorders.
    • Adverse: sedation, drowsiness, GI upset, prolonged bleeding time, visual disturbances, muscle weakness, tremor, bone marrow suppression weight gain, abdominal cramps, rash, alopecia, pruritus, hepatotoxicity, agitation.
    • Alerts:  many drug interactions, potentiation of CNS depressants, concurrent use of clonazepam (klonopin) may cause absence seizures, can increase phenytoin levels as well.may result in fatal hepatic failure, monitor liver tests.
  5. ethosuximide (Zarontin)
    Succinmides (suppress calcium influx)
    • Therapeutic class: antiseizure 
    • Preg: C
    • MOA: depresses activity of neurons in motor cortex by increasing neuronal threshold by suppressing calcium influx.
    • Indications: drug of choice for petit mal seizures (absence)
    • contraindications: Kidney or liver disease, children younger than 3 years of age. 
    • adverse: may impair mental and physical abilities, psychosis or extreme mood swings, depression, SI, behavioral changes are prominent in pt with history of psych illness, dizziness, headache, lethargy, fatigue, ataxia, sleep disturbance, bone marrow suppression, blood dyscrasias, systemic lupus erythematosus. 
    • Alerts: increases phenytoin serum levels, causes valproic acid levels to fluctuate as well. Must taper off-abrupt withdrawal may cause a seizure. 
  6. levodopa, carbidopa, entacapone (Stalevo)
    Dopaminergic drugs (Parkinsons disease)
    • Therapeutic class: Antiparkinson
    • Preg: C
    • MOA: restores the neurotransmitter dopamine in areas of the brain, to increase its effect its combined with two other drugs (carbidopa and entacapone) this prevents enzymatic breakdown-may take up to several months for a therapeutic effect.
    • Indications: parkinsons
    • Contraindications: Hx of melanoma, suspicious pigmented lesions, should be avoided with cases of severe psychoneurosis or within 14 days of MAOI. 
    • Adverse: uncontrolled movements, dyskinesia, N/V, loss of appetite, orthostatic hypotension. 
    • Alert: must be tapered off if toxicity develops, abrupt withdrawal can produce acute parkinsonism, avoid taking with high protein meals.
  7. benztropine (Cogentin)
    anticholinergic ( cholinergic receptor blocker)
    • Therapeutic class: antiparkinson
    • Preg: C
    • MOA: blocks excess cholinergic stimulation of neurons in corpus striatum. 
    • Indications: Parkinsonism symptoms, EPS
    • Contraindications: glaucoma, myasthenia gravis(autoimmune disorder that causes muscle weakness), obstructive disorders of GU and GI tracts.
    • Adverse: anticholinergic SE,
    • Alerts: Many drug interactions.
    • Antidote: physostigmine 1-2mg Sq or IV, will reverse symptoms of anticholinergic intoxication.
  8. donepezil (Aricept)
    acetylcholinesterase inhibitor (Alzheimers)
    • Therapeutic class: alzheimers disease drug
    • Preg: C
    • MOA: improves memory in cases of mild to moderate alzheimer's by enhancing effects of acetylcholine in neurons. 
    • Indications: Alzheimers
    • Contraindications: Gi bleeds and jaundice
    • Adverse: N/V, diarrhea, darkened urine, insomnia, syncope, depression, headaches, irritability, muscle cramps, arthritis,  increased libido, hot flashes, blurred vision. 
    • Alert: will cause anticholinergics to be less effective. Has many drug interactions.
  9. Drugs used for MS?
    • immunomodulators
    • immunosuppressants
    • potassium channel blockers
  10. Immunomodulators
    interferon beta (Avonex, Betaseron)
    and
    Glatiramer (Copaxone)
    • Decreases number of lesion detected
    • will cause flu-like symptoms, but usually well tolerated.

    synthetic protein that stimulates myelin-thought to curb the body's attack on the myelin covering and reduces symptoms.
  11. Immunosuppressants 
    Mitoxantrone (Novantrone)
    • used for progressive-relapsing MS
    • Primarily a chemo drug; toxicity concerns
    • cardiotoxicity, dysrhythmias, SOB
  12. Ginkgo biloba can do what?
    can interact with most of the anti seizure meds
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Neurological and neuromuscular Pharm
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