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Medication Review
Central Nervous System (CNS).
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Medication Review, Central Nervous System (CNS)
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Definitions
Antipsychotics
Therapeutic Classes
Antidepressants
Sedative Hypnotics
Skeletal Muscle Relaxants
Antianxiety Agents
(Anxiolytics)
Anticonvulsants
CNS Stimulants
Narcotic Analgesics
Anti-Parkinson's Agents
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Definitions
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Dependence
An altered state where continued administration of the drug is necessary to prevent physical
and psychological withdrawal systems
Addiction
A pattern of compulsive use characterized by overwhelming involvement with drug use and
abuse
Tolerance
The need for larger doses or an increase in the number of doses to achieve the desired
response
May develop after repeated or chronic administration of the drugs
Example: Some with chronic pain increase dose of analgesic
Physiology
The CNS is composed of the brain and spinal cord
Example: Burn your finger, goes to spinal cord to brain, brain says "move finger"
Involved in integrating and deciphering all incoming messages and sending responses to the
organs and tissues of the body
Co-ordinates muscle movements, visualization, temperature regulation, pain and sensation
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Therapeutic Classes
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Sedative Hypnotics
Uses
Short-term use (days to a few weeks) for insomnia, not for long term use
Long-term use (months or years), long-term use can cause drug-induced abnormalities in
the patient's sleep cycle
Antidotes for overdoses of stimulants
In combination with analgesics in painful situations
Preoperative anesthetics
Mechanism of Action
Not sure, but is though to reduce the activity of the brain and spinal cord
Side Effects
Drowsiness
Addiction
Tolerance & dependence
Respiratory and cardiac depression (with high doses)
Examples
Benzodiazepines:
Flurazepam (Dalmane)
Alprazolam (Xanax)
Lorazepam (Ativan)
Diazepam (Valium)
Oxazepam (Serax)
Midazolam (Versed)
Temazepam (Restoril)
Triazolam (Halcion)
Estazolam (ProSom)
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Clonazepam(Klonopin) used to treat epilepsy seizures
Barbiturates:
Secobarbital (Seconal)
Amobarbital (Amytal)
Pentobarbitol (Nembutal)
Primidone (Mysoline)
Miscellaneous:
Zolpidem Tartrate (Ambien)
Chloral Hydrate (Noctec)
Alcohol
Diphenhydramine (Benadryl, Compoz, Nytol, Sominex)
Eszopiclone (Lunesta)
Skeletal Muscle Relaxants
Uses
Relieve muscle spasm associated with muscle inflammation and injury
Useful in neuromuscular disorders such as Multiple Sclerosis and Cerebral Palsy
Mechanism of Action
Not understood, but may block nerve response within the spinal column. This has an effect
of reducing, muscle tone and relieving muscle spasm and tension
Side Effects
Drowsiness
Addiction
Tolerance and dependence
Respiratory and cardiac depression (with high doses)
Examples
Diazepam (Valium)
Cyclobenzaprine (Flexeril)
Methocarbamol (Robaxin)
Baclofen (Lioresal)
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Chlorzoxazone (Parafon Forte)
Carisoprodol (Soma)
Metaxalone (Skelaxin)
Tizanidine(Zanaflex)
Orphenadrine(Norflex)
Anticonvulsants
Uses
Epilepsy:
Seizures accompanied by loss or disturbance of consciousness and possibly abnormal body
movements (convulsions)
Needs to be individualized by dose and addition of other anticonvulsant agents
Prevent the occurrence of seizures, they do not cure the disease
Mechanism of Action
Control the excessive discharge of signals from the brain (seizures)
Side Effects
Drowsiness
Slurred speech
Addiction
Tolerance and dependence
Respiratory and cardiac depression (with high doses)
Examples
The anticonvulsant drug chosen depends on the type of seizure the patient has (e.g. partial
vs. generalized onset seizures). Valium and Ativan are the drugs of choice to treat a life
threatening seizure disorder called Status Epilepticus
Phenobarbital
Phenytoin (Dilantin)
Carbamazepine (Tegretol)
Valproic acid and its derivatives
(Depakene, Depakote)
Gabapentin (Neurontin)
Lamotrigine (Lamictal)
Clonazepam (Klonopin) a benzodiazepine
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Clorazepate (Tranxene)
Ethosuximide (Zarontin)
Oxcarbazepine (Trileptal)
Felbamate (Felbatol)
Lamotrigine (Lamicta)
Levetiracetam (Keppra)
Tiagabine (Gabitril Filmtabs)
Topiramate (Topamax)
Primidone (Mysoline)
Trimethadione (Tridione)
Narcotic Analgesics
Uses
Relief of moderate to severe pain
Cough suppressant
Severe diarrhea
Mechanism of Action
Bind to specific receptors within the brain and depress certain parts of the CNS to cause
pain relief, respiratory depression, decreased GI motility, and suppression of cough
Side Effects
Drowsiness
Constipation
Nausea/vomiting
Addiction, tolerance and physical an psychological dependence
Overdoses can cause respiratory depression, profound coma, and pinpoint pupils (narcotic
antagonists are used to treat overdoses - Naloxone (Narcan)
Examples
Single Agents:
Codeine
Morphine Sulfate (MS Contin, Roxanol)
Oxycodone (Roxicodone)
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Nalbuphine (Nubain)
Meperidine (Demerol)
Fentanyl (Duragesic) (Actiq lozenges on a stick)
Hydromorphone (Dilaudid)
Remifentanil (Ultiva)
Pentazocine (Talwin)
Levorphanol (Levo-Dromoran)
Propoxyphene (Darvon)
Butorphanol (Stadol)
Combination Products:
Acetaminophen with Codeine (Tylenol with Codeine)
Hydrocodone and Acetaminophen (Lorcet, Lortab, Vicodin)
Propoxyphene and Acetaminophen (Darvocet-N, Propacet, Wygesic)
Oxycodone and Acetaminophen (Percocet, Roxicet)
Oxycodone and Aspirin (Percodan)
Antipsychotics
Uses
Relieve the signs and symptoms of psychoses (e.g. Schizophrenia)
Have a much better effect on the positive symptoms of psychosis:
Auditory and visual hallucinations, agitation, suspiciousness, felling of persecution, ideas of
reference, and intrusion of unwanted thoughts
Noncompliance is the leading cause of recurrent positive psychotic symptoms in those
patients who initially responded
Negative symptoms include emotional apathy, extreme inattentiveness, and social
withdrawal
Some analgesic, antiemetic, antinausea, and antihistaminic effects
Mechanism of Action
Originally, it was proposed that these drugs block dopamine (a chemical in the brain)
receptors in the brain
Chemically effects unknown
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Side Effects
Sedation
Extrapyramidal symptoms (abnormal body movements) - with typicals
Anticholinergic symptoms
Orthostatic hypotension
Abnormal heart rhythms (arrhythmia's)
Examples
Typical:
Haloperidol (Haldol)
Chlorpromazine (Thorazine)
Prochlorperazine (Compazine)
Fluphenazine (Prolixin - Permitil)
Thioridazine (Mellaril)
Thiothixene (Navane)
Trifluoperazine (Stelazine)
Atypical:
Clozapine (Clozaril)
Risperidone (Risperdal )
Olanzapine (Zyprexa)
Antipiprazole (Abilify)
Quetiapine (Seqroquel)
Antidepressants
Uses
Treat severe depression
Mechanism of Action
Exact mechanism unknown
Appear to increase neurotransmitters in the brain (Norepinephrine and serotonin)
Usually takes 3-6 weeks for these drugs to relieve the depression
Side Effects
Sedation
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Anticholinergic
Abnormal heart rhythm
Seizures
Examples
Tricyclic antidepressants (TCAs):
Amitriptyline (Elavil)
Desipramine (Norpramin)
Imipramine (Tofranil)
Nortriptyline (Pamelor)
Trimipramine (Surmontil)
Clomipramine (Anafranil)
Mirtazpine (Remeron)
Serotonin-reuptake inhibitors:
Fluoxetine (Prozac)
Venlafaxine (Effexor)
Paroxetine (Paxil)
Sertraline (Zoloft)
Fluvoxamine (Luvox)
Citalopram (Celexa)
Escitalopram (Lexapro)
Serotonin and Norepinephrine reuptake inhibitors
Duloxetine (Cymbalta)
Miscellaneous:
Trazodone (Desyrel)
Nefazodone (Serzone)
Bupropion (Wellbutrin)
Lithium (Eskalith, Lithobid, Lithonate)
Monoamine oxidase inhibitors:
Phenelzine (Nardil)
Tranylcypromine (Parnate)
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Important to do a drug interaction check
Manic-depressive disorder:
Periods of elation, followed by periods of depression
Drugs used to moderate mood swings
Lithium Carbonate (Eskalith, Lithonate)
Alzheimer disease:
Alzheimer is an illness that makes it hard for people to remember, think, and use language.
It can make them act strange.
Uses
Treat Alzheimer
T
Mechanism of action
NMDA Receptor antagonists
Cholinesterase inhibitors
Side Effects
Dizziness
Confusion
Insomnia
Nausea
Agitation
Coughing
Fatique
Abdnormal thinking
NMDA Receptor antagonists
Example: Memantine (Namenda)
Cholinesterase inhibitors
Examples:
Tacrine (Cognex)
Donepezil (Aricept)
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Rivastigmine (Exelon)
Antianxiety Agents (Anxiolytics)
Uses
To relieve nervousness and tension in normal or neurotic patients
Have muscle-relaxing capabilities
Some have anticonvulsant activity
Mechanism of Action
Benzodiazepines work by binding to and affecting certain receptors and neurotransmitters
(GABA) in the brain
The second-generation drug, Buspirone, has an effect at the serotonin and dopamine
receptors
Side Effects
Drowsiness
Dizziness
Fatigue
Abrupt termination of high does can cause coma, convulsions, and death
Examples
Benzodiazepines:
Alprazolam (Xanax)
Lorazepam (Ativan)
Diazepam (Valium)
Oxazepam (Serax)
Flurazepam (Dalmane)
Midazolam (Versed)
Miscellaneous:
Buspirone (BuSpar)
Doxepin (Sinequan)
Hydroxyzine (Atarax)
CNS Stimulants
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Uses
To improve mental function, elevate mood, overcome fatigue, and produce a general feeling
of well being
Narcolepsy
Hyperkinesis (Attention Deficit Hyperactivity Disorder - ADHD in children)
Anorexiants ( Management of Obesity)
Mechanism of Action
Amphetamines stimulate activity and are mediated by the release of Norepinephrine and
Dopamine in the brain
Pemoline and Methylphenidate's action is unknown
Side Effects
Dependence
Increased blood pressure
Increased respiratory rate
Stomach upset
Examples
Caffeine
Methylphenidate (Ritalin)
Dextroamphetamine (Dexadrine)
Pemoline (Cylert)
Adderall (Amphetamine Mixture)
Modafinil (Provigil)
Dexmethylphenidate (Focalin)
Examples of Anorexiants
Benzphetamine (Didrex)
Phentermine (Adipex-P)
Anti-Parkinson's Agents
Uses
To treat the shaking, rigidity, salvation, and slowing of initial movements associated with
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Parkinson's disease
Mechanism of Action
Parkinson's is a disease characterized by loss of dopamine manufacturing neurons. There
is an imbalance in the brain between Acetylcholine (increased) and dopamine (decreased)
Anticholinergics decrease the amount of CNS Acetylcholine
Drugs such as Levodopa increase the amount of dopamine in the CNS
Amantadine augments dopamine release from presynaptic nerve terminals and inhibits
dopamine reuptake
Side Effects
Anticholinergics:
Dry mouth
Blurred vision
Constipation
Hallucinations
Memory impairment
Amantadine:
Dizziness
Insomnia
Nervousness
Irritability
Confusion
Nausea and vomiting
Constipation
Levodopa:
Nausea and vomiting
Confusion
Depression
Restlessness
Postural hypotension
Arrhythmias
Examples
Levodopa/Carbidopa (Sinemet)
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Bromocriptine (Parlodel)
Amantadine (Symmetrel)
Pergolide (Permax)
Pramipexole (Mirapex)
Ropinirole (Requip)
Selegiline (Eldepryl)
Benztropine (Cogentin)
Special Note
Alcohol and other CNS depressants can have additive CNS depressant effects and
concomitant use should be avoided
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