© paradigm publishing, inc.1 chapter 8 drugs for central nervous system disorders
TRANSCRIPT
![Page 1: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/1.jpg)
© Paradigm Publishing, Inc. 1
Chapter 8
Drugs for Central Nervous System
Disorders
![Page 2: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/2.jpg)
© Paradigm Publishing, Inc. 2
Learning Objectives
• Develop an understanding of the physiologic processes that occur in epilepsy.
• Classify seizures and the goals of their therapy.
• Understand that specific drugs are used in different classes of seizures.
![Page 3: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/3.jpg)
© Paradigm Publishing, Inc. 3
Learning Objectives
• Be familiar with Parkinson disease and the drugs used in its treatment.
• Identify the drugs and goals of therapy for attention-deficit disorders.
• Realize that some drugs may be used for several disease states.
• Recognize drugs used to treat Alzheimer disease.
![Page 4: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/4.jpg)
4© Paradigm Publishing, Inc.
Epilepsy
• Common neurologic disorder with sudden and recurring (paroxysmal) seizures
• Caused by abnormal electrical impulses in the brain
• All epilepsy patients have seizures; not all with seizures have epilepsy
• 1% to 2% have chronic epilepsy
![Page 5: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/5.jpg)
5© Paradigm Publishing, Inc.
Seizures
• Disturbances of neuronal electrical activity that interferes with normal brain function
• Behavior change patient not aware of
• Conscious periods may or may not lose control over movement
• Loss of body control may affect one area or entire body
![Page 6: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/6.jpg)
6© Paradigm Publishing, Inc.
Convulsions
• Excessive firing of neurons can result in a convulsion– Involuntary contraction or series of
contractions of the voluntary muscles
![Page 7: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/7.jpg)
7© Paradigm Publishing, Inc.
Causes of Seizures
• Imbalance of excitatory and inhibitory neurotransmitters– GABA: excitatory– Glutamate: inhibitory– Other neurotransmitters can be involved
• Enzymes control neurotransmitter levels• Disruption in enzymes = disruption of
neurotransmitters
![Page 8: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/8.jpg)
8© Paradigm Publishing, Inc.
Causes of Seizures
• Alcohol or drug withdrawal• Epilepsy• High fever• Hypoglycemia, hyperglycemia• Infection (meningitis)• Neoplasm (brain tumor)• Trauma or injury (head, hematoma)
![Page 9: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/9.jpg)
9© Paradigm Publishing, Inc.
Two Classes of Seizures
• Partial– Simple partial– Complex partial
• Generalized– Tonic-clonic (was called grand mal seizure)– Absence (was called petit mal seizure)– Myoclonic– Atonic
![Page 10: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/10.jpg)
10© Paradigm Publishing, Inc.
Partial Seizures
• Localized in a specific area of the brain• Almost always results from injury to
cerebral cortex• Occurs in about 65% of people with
epilepsy• Can progress to generalized seizures
![Page 11: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/11.jpg)
11© Paradigm Publishing, Inc.
Two Classes of Partial Seizures
• Simple Partial– No loss of consciousness– May have muscle twitching or sensory
hallucinations
• Complex Partial– Impaired consciousness– Confusion, blank stare, and postseizure
amnesia
![Page 12: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/12.jpg)
12© Paradigm Publishing, Inc.
Generalized Seizures
• Involves both hemispheres of the brain, no specific location
• Four types
• Tonic-Clonic– Absence– Myoclonic– Atonic
![Page 13: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/13.jpg)
13© Paradigm Publishing, Inc.
Tonic-Clonic Seizures
• Tonic: body becomes rigid, patient may fall, lasts a minute or less
• Clonic: starts with muscle jerks, may be accompanied by shallow breathing, loss of bladder control, and excess salivation– Lasts a few minutes
![Page 14: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/14.jpg)
14© Paradigm Publishing, Inc.
Absence Seizures
• Interruption of activities by blank stare, rotating eyes, uncontrolled facial movements, rapid eye blinking, twitching or jerking of an arm or leg
• No generalized convulsions• Usually lasts 30 seconds or less• Most prevalent first 10 years of life. 50% of
children have tonic-clonic as grow older
![Page 15: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/15.jpg)
15© Paradigm Publishing, Inc.
Myoclonic Seizures
• Occurs with sudden, massive, brief muscle jerks which may throw patient down or nonmassive, quick jerks
• Consciousness is not lost
• Can occur during sleep
![Page 16: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/16.jpg)
16© Paradigm Publishing, Inc.
Atonic Seizures
• Begins with sudden loss of muscle tone and consciousness
• Patient may collapse, head drop, arm or leg may go limp
• Lasts few seconds to a minute, then patient can stand and walk again
![Page 17: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/17.jpg)
17© Paradigm Publishing, Inc.
Status Epilepticus
• Continuous tonic-clonic seizures, with or without return to consciousness
• Last at least 30 minutes
• High fever and lack of oxygen that can cause brain damage or death
![Page 18: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/18.jpg)
18© Paradigm Publishing, Inc.
Two Goals of Antiepileptic Therapy
• Seizure control or lessen the frequency
• Prevent emotional and behavioral changes that may result from seizures
![Page 19: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/19.jpg)
19© Paradigm Publishing, Inc.
Antiepileptic Drug Therapy
• Different seizure types require different drugs
• Start with monotherapy at low dose and increase slowly over 3 to 4 weeks
• Medication must be maintained at steady therapeutic levels
• If insufficient response, polytherapy can be considered
![Page 20: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/20.jpg)
20© Paradigm Publishing, Inc.
Antiepileptic Drug Therapy
• Newer drugs are seizure-specific• High potential for drug interactions• Anticonvulsants have narrow therapeutic
ranges• Minor dosage changes can result in loss of
seizure control or toxicity• Prescribers often write for the brand name
![Page 21: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/21.jpg)
© Paradigm Publishing, Inc. 21
Drug ListAnticonvulsants
– carbamazepine (Epitol, Tegretol)
– clonazepam (Klonopin)
– diazepam (Valium)
– divalproex (Depakote)
– ethosuximide (Zarontin)
![Page 22: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/22.jpg)
© Paradigm Publishing, Inc. 22
Drug ListAnticonvulsants
– fosphyenytoin (Cerebyx)
– gabapentin (Neurontin)
– lamotrigine (Lamictal)
– levetiracetam (Keppra)
– lorazepam (Ativan)
![Page 23: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/23.jpg)
© Paradigm Publishing, Inc. 23
Drug ListAnticonvulsants
– oxcarbazepine (Trileptal)
– phenobarbital (Luminal Sodium)
– phenytoin (Dilantin)
– pregabalin (Lyrica)
– primidone (Mysoline)
![Page 24: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/24.jpg)
© Paradigm Publishing, Inc. 24
Drug ListAnticonvulsants
– tiagabine (Gabitrol)
– topiramate (Topamax)
– valproic acid (Depakene)
– zonisamide (Zonegran)
![Page 25: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/25.jpg)
25© Paradigm Publishing, Inc.
Dispensing Issues of Anticonvulsants
• Prescribers often do not allow generic drugs
• Pharmacy technicians watch for DAW
• If computer changes drug to generic, technicians often change drug to brand
Warning!
![Page 26: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/26.jpg)
26© Paradigm Publishing, Inc.
carbamazepine (Epitol, Tegretol)
• Effect on sodium channels which may alter synaptic transmission
• Blood monitoring important
• Many interactions with other drugs
• Side effects can be serious
![Page 27: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/27.jpg)
27© Paradigm Publishing, Inc.
clonazepam (Klonopin)
• Prophylaxis of seizures
• Depresses nerve transmission in the motor cortex
• C-IV controlled substance (benzodiazepine)
![Page 28: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/28.jpg)
28© Paradigm Publishing, Inc.
gabapentin (Neurontin)
• Used as adjunct
• No significant drug interactions, well-tolerated, easy to use
• Used for many other disorders, particularly neuropathic pain
![Page 29: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/29.jpg)
29© Paradigm Publishing, Inc.
Dispensing Issues of Neurontin
• Sound-alike drugs, but different strengths– Neurontin, usually 100 mg– Noroxin (antibiotic), usually 400 mg
Warning!
![Page 30: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/30.jpg)
30© Paradigm Publishing, Inc.
lamotrigine (Lamictal)
• Add-on therapy for adults with partial seizures
• Blocks sodium channels which reduces neuron excitation
• Call physician immediately if rash appears, do not discontinue abruptly
![Page 31: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/31.jpg)
31© Paradigm Publishing, Inc.
Dispensing Issues of Lamictal
• Look-alike and sound-alike– Lamictal– Lamisil (terbinafine), antifungal– Lomotil (diphenoxylate-atropine),
diarrhea
Warning!
![Page 32: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/32.jpg)
32© Paradigm Publishing, Inc.
Dispensing Issues of Lamictal
• Black Box warning about fatal rashes, most serious warning
• Boxed warnings are special warnings about a drug highlighted in the FDA-approved product information
Warning!
![Page 33: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/33.jpg)
33© Paradigm Publishing, Inc.
phenytoin (Dilantin)
• May be used to prevent seizures• Promotes sodium outflow from cells,
stabilizing the neuronal membrane• Be cautious of drug interactions• IV phenytoin must be mixed carefully
![Page 34: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/34.jpg)
34© Paradigm Publishing, Inc.
Side Effects of Phenytoin: Dose Related
• Ataxia
• Diplopia
• Dizziness
• Drowsiness
• Encephalopathy
• Involuntary movements
![Page 35: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/35.jpg)
35© Paradigm Publishing, Inc.
Side Effects of Phenytoin: Non-Dose-Related
• Gingival hyperplasia
• Peripheral neuropathy (pain in extremities
• Vitamin deficiencies
![Page 36: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/36.jpg)
36© Paradigm Publishing, Inc.
pregabalin (Lyrica)
• Reduces release of neurotransmitters glutamate, norepinephrine, substance P
• Similar to gabapentin, more potent. Fewer side effects than other anticonvulsants
• Controlled substance, Schedule V
• Also approved to treat diabetic neuropathy
![Page 37: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/37.jpg)
37© Paradigm Publishing, Inc.
taigabine (Gabitrol)
• Blocks reabsorption of GABA, allowing it to bind to nerve cells which enhances normal brain activity
• Should be taken with food• Can cause seizures if patients who do not
have epilepsy use it off-label
• FDA has issued off-label use warning
![Page 38: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/38.jpg)
38© Paradigm Publishing, Inc.
topiramate (Topamax)
• Thought to block sodium channels which increases GABA activity and decreases glutamine activity
• Causes significant cognitive effects
• Drink fluids to decrease risk of kidney stones
![Page 39: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/39.jpg)
© Paradigm Publishing, Inc. 39
Discussion
Which neurotransmitters play the greatest role in seizures?
The neurotransmitters are glutamate (excitatory) and GABA (inhibitory).
![Page 40: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/40.jpg)
© Paradigm Publishing, Inc. 40
Terms to Remember
epilepsy
seizure
convulsion
partial seizure
generalized seizure
tonic-clonic seizure
![Page 41: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/41.jpg)
© Paradigm Publishing, Inc. 41
Terms to Remember
grand mal seizure
absence seizure
petit mal seizure
myoclonic seizure
atonic seizure
status epilepticus
![Page 42: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/42.jpg)
© Paradigm Publishing, Inc. 42
Terms to Remember
anticonvulsant
adjunct
ataxia
substance P
![Page 43: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/43.jpg)
43© Paradigm Publishing, Inc.
Parkinson Disease
• Characterized by tremor when resting, rigidity, and akinesia (absence of movement)
• Poor posture control, shuffling gait, loss of overall muscle control
• Usually affects people over 60
![Page 44: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/44.jpg)
44© Paradigm Publishing, Inc.
Physiology of Parkinson Disease
• Parkinson disease is result of alterations in the extrapyramidal system– Part of the CNS that controls motor activities
– Made up of the basal nuclei (basal ganglia)
• Most common extrapyramidal disease
• Parkinson has no definitive test, diagnosed by symptoms
![Page 45: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/45.jpg)
45© Paradigm Publishing, Inc.
Cutaway View of the Brain
![Page 46: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/46.jpg)
46© Paradigm Publishing, Inc.
Physiology of Parkinson Disease
• For normal muscle movement to be performed, 2 main neurotransmitters must be in balance– Dopamine (inhibitor)
– Acetylcholine (stimulator)
• In Parkinson disease, these neurotransmitters are not in balance
![Page 47: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/47.jpg)
47© Paradigm Publishing, Inc.
Dopamine and Parkinson Disease
• In the substania nigra, insufficient dopamine is released to counteract effects of Ach
• This causes excessive motor nerve stimulation
![Page 48: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/48.jpg)
48© Paradigm Publishing, Inc.
Substantia Nigra
![Page 49: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/49.jpg)
49© Paradigm Publishing, Inc.
Parkinson Disease Drug Therapy
• Improves functional ability and clinical status of patients
• Aims at symptomatic relief, does not alter disease process. No cure.
• Temporary or prolonged remission
• Side effects can be a problem
![Page 50: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/50.jpg)
© Paradigm Publishing, Inc. 50
Drug ListAnti-Parkinson Agents
– amantadine (Symmetrel)– benztropine (Cogentin)– bromocriptine (Parlodel)– entacapone (Comtan)– levodopa (Dopar)– levodopa-carbidopa (Sinemet)
![Page 51: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/51.jpg)
© Paradigm Publishing, Inc. 51
Drug ListAnti-Parkinson Agents
– levodopa-carbidopa-entacapone (Stalevo)
– pramipexole (Mirapex)– rasagiline (Azilect)– ropinirole (ReQuip)– selegiline (Eldepryl)– tolcapone (Tasmar)
![Page 52: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/52.jpg)
52© Paradigm Publishing, Inc.
levodopa (Dopar)
• Metabolized to dopamine in brain, but brain does not receive a full dose
• Very undesirable effects, including nausea, vomiting, cardiac arrhythmia
• After about 5 years of therapy, 2/3 of patients experience on-off phenomenon
![Page 53: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/53.jpg)
53© Paradigm Publishing, Inc.
levodopa-carbidopa (Sinemet)
• Probably most common drug used in Parkinson disease
• Carbidopa allows for lower doses of levodopa to be used which decreases side effects
![Page 54: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/54.jpg)
54© Paradigm Publishing, Inc.
rasagiline (Azilect)
• Monoamine oxidase inhibitor (MAOI), blocks breakdown of dopamine
• Initial therapy to improve symptoms
• Possible hypertensive crisis if patient consumes foods with tyramine (aged cheeses, cured meats, soy sauce)
![Page 55: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/55.jpg)
55© Paradigm Publishing, Inc.
entacapone (Comtan)
• Second in class of anti-Parkinson agents known as catechol-O-methyl transferase (COMT) inhibitors
• Indicated for patients who have a deteriorating response to levodopa
• Less toxic than tolcapone (Tasmar)
• Taken without regard to food
![Page 56: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/56.jpg)
© Paradigm Publishing, Inc. 56
Terms to Remember
Parkinson disease
basal nuclei
substantia nigra
on-off phenomenon
catechol-O-methyl transferase (COMT)
![Page 57: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/57.jpg)
57© Paradigm Publishing, Inc.
Other Central Nervous System Disorders
• Myasthenia gravis
• Attention-deficit hyperactivity disorder and attention-deficit disorder
• Amyotrophic lateral sclerosis (ALS)
• Multiple sclerosis (MS)
• Alzheimer disease
![Page 58: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/58.jpg)
58© Paradigm Publishing, Inc.
Myasthenia Gravis
• Autoimmune disorder of the neuromuscular junction
• ACh receptors are destroyed at the motor end plate
• Characterized by weakness and fatigability, especially of skeletal muscles
![Page 59: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/59.jpg)
59© Paradigm Publishing, Inc.
Motor End Plate
![Page 60: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/60.jpg)
60© Paradigm Publishing, Inc.
Presenting Signsof Myasthenia Gravis
• Ptosis (drooping eyelid)
• Diplopia (double vision)
• Dyarthria (speech)
• Dysphagia (swallowing)
• Extremity weakness
• Respiratory difficulty
![Page 61: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/61.jpg)
61© Paradigm Publishing, Inc.
Treatment of Myasthenia Gravis
• Acetylcholinesterase drugs can produce improvements in all forms of myasthenia gravis
• Drug therapy does not inhibit or reverse the immunologic flaw
![Page 62: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/62.jpg)
© Paradigm Publishing, Inc. 62
Drug ListAgents for Myasthenia Gravis
– azathioprine (Imuran)– cyclophosphamide (Cytoxan)– edrophonium (Enlon, Reversol)– neostigmine (Prostigmin)– pyridostigmine (Mestinon)
![Page 63: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/63.jpg)
63© Paradigm Publishing, Inc.
pyridostigmine (Mestinon)
• Blocks destruction of ACh
• Allows for ACh accumulation at the synaptic junction
• Take with food or milk and at same time each day
![Page 64: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/64.jpg)
64© Paradigm Publishing, Inc.
cyclophosphamide (Cytoxan)
• Prevents cell division by targeting the auto-immune portion of the disease
• Use chemotherapeutic precautions
![Page 65: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/65.jpg)
65© Paradigm Publishing, Inc.
Attention-Deficit Disorders
• Attention-Deficit Hyperactivity Disorder (ADHD)
• Attention-Deficit Disorder (ADD)
![Page 66: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/66.jpg)
66© Paradigm Publishing, Inc.
Attention-Deficit Hyperactivity Disorder (ADHD)
• Neurologic disorder characterized by hyperactivity, impulsivity, and distractability
• Symptoms can persist into adult life
• Most drugs used are amphetamines and amphetamine derivatives, C-II
![Page 67: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/67.jpg)
© Paradigm Publishing, Inc. 67
Drug ListAttention-Deficit Disorders Agents
– atomoxetine (Strattera)
– dexmethylphenidate (Focalin), C-II
– dextroamphetamine-amphetamine (Adderall), C-II
– lisdexamfetamine (Vyvanse)
![Page 68: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/68.jpg)
© Paradigm Publishing, Inc. 68
Drug ListAttention-Deficit Disorders Agents
– methylphenidate (Concerta, Daytrana Metadate, Metadate ER, Methylin, Ritalin, Ritalin-SR), C-II
– modafinil (Provigil, Sparlon)
![Page 69: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/69.jpg)
69© Paradigm Publishing, Inc.
Dispensing Issues of Attention-Deficit Disorders Agents
• ADHD drugs used for treatment as a group must provide a medication guide to patient or caretaker
• Technicians—check for mediation guide when drug is handed to patient or caretaker, even if drug is not C-II
Warning!
![Page 70: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/70.jpg)
70© Paradigm Publishing, Inc.
atomoxetine (Strattera)
• Nonstimulant indicated for treatment of ADHD in patients 6 years and older
• Controls impulsivity and activity
• Not a controlled substance, refills can be called in
![Page 71: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/71.jpg)
71© Paradigm Publishing, Inc.
methylphenidate (Concerta, Daytrana Metadate, Metadate
ER, Methylin, Ritalin, Ritalin-SR)
• Drug of choice to treat attention-deficit disorders
• CNS stimulant, C-II controlled substance• Improved dosage allows the drug to be
taken only in the morning• One form comes in a patch, improving
compliance
![Page 72: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/72.jpg)
72© Paradigm Publishing, Inc.
methylphenidate (Concerta)
• Dosed once a day, in morning
• Outer layer dissolves to release part of drug immediately
• Rest of drug is OROS tablet– Slowly releases through pores in tablet,
leaving a ghost
![Page 73: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/73.jpg)
73© Paradigm Publishing, Inc.
methylphenidate (Daytrana Metadate)
• Patch form of methylphenidate
• Worn for 9 hours, then removed
• Drug is in the adhesive
![Page 74: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/74.jpg)
74© Paradigm Publishing, Inc.
dextroamphetamine-amphetamine (Adderall)
• C-II controlled substance
• Effects last about 6 hours
• Primary side effect is depression as drug wears off
![Page 75: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/75.jpg)
75© Paradigm Publishing, Inc.
Dispensing Issues of Adderall
• Look-alike and sound-alike– Adderall (ADHD)– Inderal (propranolol), beta blocker used
to treat anxiety
Warning!
![Page 76: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/76.jpg)
76© Paradigm Publishing, Inc.
Modafinil (Provigil, Sparlon)
• Sparlon is nonstimulant medication
• Indicated for treatment of ADHD in patients 6 years and older
• Increases mental alterness
![Page 77: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/77.jpg)
77© Paradigm Publishing, Inc.
Amyotrophic Lateral Sclerosis (ALS)
• Also known as Lou Gehrig disease
• Progressive degenerative disease of the nerves
• Muscle weakness, paralysis, and eventually death
• Cause: excessive levels of glutamate
![Page 78: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/78.jpg)
© Paradigm Publishing, Inc. 78
Drug ListAgent for Amyotrophic Lateral Sclerosis
– riluzole (Rilutek)
![Page 79: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/79.jpg)
79© Paradigm Publishing, Inc.
riluzole (Rilutek)
• First drug approved for amyotrophic lateral sclerosis
• Inhibits release of glutamate
• Seems to improve survival rate by 3 months in some patients
![Page 80: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/80.jpg)
80© Paradigm Publishing, Inc.
Multiple Sclerosis (MS)
• Autoimmune disease in which myelin sheaths around nerves degenerate
• Patient loses use of muscles, and often eyesight is affected
• Some drugs can slow progression
• No cure
![Page 81: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/81.jpg)
© Paradigm Publishing, Inc. 81
Drug ListMultiple Sclerosis Agents
– baclofen (Lioresal)– glatiramer acetate (Copaxone)– interferon beta-1a (Avonex, Rebif)– interferon beta-1b (Betaseron)– mitoxantrone (Novantrone)– tizanidine (Zanaflex)
![Page 82: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/82.jpg)
82© Paradigm Publishing, Inc.
glatiramer acetate (Copaxone)
• Seems to block the autoimmune reaction against myelin that leads to nerve damage
• Decreases frequency of relapses
• Not been shown to slow disease progress
• Given everyday by subcutaneous injection
• Must be frozen
![Page 83: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/83.jpg)
83© Paradigm Publishing, Inc.
tizanidine (Zanaflex)
• Indicated to reduce muscle spasticity in MS and spinal cord injuries
• Oral drug
• Side effects: dry mouth, sedation, dizziness, and hypotension
![Page 84: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/84.jpg)
84© Paradigm Publishing, Inc.
Alzheimer Disease
• Progressive form of dementia
• Changes personality and behavior
• No treatments can cure or reverse
• Drugs can slow the disease
• Depression often treated with antidepressants according to symptoms
![Page 85: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/85.jpg)
85© Paradigm Publishing, Inc.
Progression of Alzheimer Disease
1. Memory deficit, forgetfulness, misplacements of ordinary items
2. Inability to complete complex tasks
3. Complete incapacitation, disorientation, and failure to thrive
![Page 86: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/86.jpg)
© Paradigm Publishing, Inc. 86
Drug ListAgents for Alzheimer Disease
– donepezil (Aricept)– galantamine (Razadyne)– ginkgo (many)– memantine (Namenda)– rivastigmine (Exelon)– tacrine (Cognex)
![Page 87: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/87.jpg)
87© Paradigm Publishing, Inc.
tacrine (Cognex)
• Cholinesterase inhibitor
• Most common side effect: increase in liver lab values
• Taken 4x a day on an empty stomach
• Side effects: nausea, vomiting
![Page 88: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/88.jpg)
88© Paradigm Publishing, Inc.
donepezil (Aricept)
• Convenient to use
• Few side effects
• Improves memory and alertness
• Give once a day at bedtime
![Page 89: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/89.jpg)
89© Paradigm Publishing, Inc.
Dispensing Issue of Aricept
• Look-alike and sound-alike– Aricept– Aciphex (rabeprazole), GERD
Warning!
![Page 90: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/90.jpg)
90© Paradigm Publishing, Inc.
memantine (Namenda)
• May have fewer side effects and better tolerated than other drugs
• Evidence that this drug slows advancement of Alzheimer disease
![Page 91: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/91.jpg)
© Paradigm Publishing, Inc. 91
Terms to Remember
myasthenia gravis
motor end plate
ptosis
diplopia
dysarthia
attention-deficit hyperactivity disorder (ADHD)
![Page 92: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/92.jpg)
© Paradigm Publishing, Inc. 92
Terms to Remember
amyotrophic lateral sclerosis (ALS)
Lou Gehrig disease
multiple sclerosis (MS)
Alzheimer disease
gingko
![Page 93: © Paradigm Publishing, Inc.1 Chapter 8 Drugs for Central Nervous System Disorders](https://reader036.vdocuments.net/reader036/viewer/2022062516/56649e055503460f94af1dce/html5/thumbnails/93.jpg)
© Paradigm Publishing, Inc. 93
Assignments
• Complete Chapter Review activities• Answer questions in Study Notes
document• Study Partner
– Quiz in review mode– Matching activities– Drug tables