DRUGS AFFECTING THE
CENTRAL NERVOUS
SYSTEM
Chap. 11, 13, 15, 16, 17
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
BRAIN AND SPINAL CORD

PRIMARY FUNCTION – CONTROLS AND
COORDINATES THE BODY AND BODY
SYSTEMS

DRUGS CAN: ALTER BEHAVIOR /
CONSCIOUSNESS
› BY STIMULATING OR DEPRESSING CNS – FOR
DESIRED AFFECT
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A
substance (norepinephrine,
acetylcholine, dopamine, or hormone)
that is released when the terminal
axon of a presynaptic neuron is
excited and acts by exciting or
inhibiting a target cell.
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
DEPRESS CNS

STIMULATE CNS – DRUGS CAN
◦ DRUGS CAN CAUSE THE BRAIN TO BE CALM 
SLEEP  ANESTHESIA  COMA  DEATH
◦ STIMULATE RESPIRATIONS
◦ KEEP A PATIENT AWAKE
◦ DEPRESS APPETITE
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
ACUTE V. CHRONIC PAIN
› ACUTE OCCURS QUICKLY, IS SHORT IN DURATION
 USUALLY CAN BE RESOLVED
› CHRONIC – LONGER LASTING, USUALLY AT LEAST 3
MONTHS IN DURATION
 POSSIBLY WILL NOT GO AWAY

PAIN IS THE SIXTH (6th) VITAL SIGN
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CAUSES OF PAIN / DISCOMFORT
◦ TRAUMA
◦ TISSUE DAMAGE
◦ PRESSURE ON TISSUE AND NERVES
◦ INFLAMMATION OF TISSUES AND
NERVES
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◦ MASSAGE
◦ POSITION CHANGE
◦ BIOFEEDBACK
◦ EXERCISE
◦ NON-OPOID ANALGESICS
◦ ANTIDEPRESSANTS
◦ Opioid ANALGESICS
◦ STEROIDS
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
Pain relievers that contain opium,
derived from the opium poppy or
chemically related to opium

Very strong pain relievers

Very addicting
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codeine sulfate
 meperidine HCl (Demerol)
 methadone HCl (Dolophine)
 morphine sulfate
 propoxyphene HCl
 hydromorphone
 oxycodone
 fentanyl
 Many Others

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Bind to an Opioid receptor in the
brain
 Cause an analgesic response
(reduction of pain sensation)

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
Main use: to alleviate moderate to
severe pain

Often given with adjuvant drugs to
assist primary drugs with pain relief
◦ Muscle relaxant
◦ Sedative
◦ Alternate with non-narcotic analgesic
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
Opioids’ are also used for:
◦ Cough center suppression
◦ Treatment of diarrhea
◦ Balanced anesthesia
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

Known drug allergy
Severe asthma
Use with extreme caution if:
 Respiratory insufficiency
 Elevated intracranial pressure
 Morbid obesity
 Sleep apnea
 Paralytic ileus
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

Euphoria
CNS depression
◦ Leads to respiratory depression
◦ Most serious adverse effect






Nausea and vomiting
Urinary retention
Diaphoresis and flushing
Pupil constriction (miosis)
Constipation
Itching
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
A common physiologic result of
chronic Opioid treatment

Result: larger dose is required to
maintain the same level of analgesia
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
Physiologic adaptation of the body to the
presence of an Opioid

Opioid tolerance and physical dependence
are expected with long-term Opioid treatment
and should not be confused with psychologic
dependence (addiction)
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
A pattern of compulsive drug use
characterized by a continued craving
for an Opioid and the need to use the
Opioid for effects other than pain
relief
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
Misunderstanding of these terms leads to
ineffective pain management and contributes
to the problem of undertreatment

Physical dependence is seen when the
Opioid is abruptly discontinued or when an
Opioid antagonist is administered
 Opioid withdrawal/Opioid abstinence
syndrome
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Reverse the effects of these drugs
on pain receptors
 Bind to a pain receptor and exert
no response
 Also known as competitive
antagonists

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ANALEPTICS
 naloxone (Narcan)
 naltrexone (Revia)
 These drugs bind to opiate receptors
and prevent a response
 Used for complete or partial reversal of
Opioid-induced respiratory depression
Regardless of withdrawal symptoms,
when a patient experiences severe
respiratory depression, an Opioid
antagonist should be given.
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
ADMINISTER MEDICATION VERY SLOWLY
◦ ANTICIPATE PATIENT RESPONSE TO TREATMENT

MONITOR PATIENT VERY CLOSELY
◦ VITAL SIGNS, RESPIRATORY RATE, PULSE OX

CONTINUE TO MONITOR CLOSELY
◦ ½ LIFE OF NARCAN = 60 – 90 MINUTES
◦ ½ LIFE OF MORPHINE = 2 – 4 HOURS
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Symptoms of “Abstinence Syndrome”
 Pulmonary edema
 Withdrawal symptoms
 Nausea
 Vomiting
 Agitation
 Anxiety
 Confusion
 Pain
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


Oral forms should be taken with food to
minimize gastric upset
Ensure safety measures, such as
keeping side rails up, to prevent injury
Withhold dose and contact physician if
there is a decline in the patient’s
condition or if vital signs are abnormal,
especially if respiratory rate is less than
10 to 12 breaths/min
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
Check dosages carefully
 Follow proper administration
guidelines for IM injections, including
site rotation
 Follow proper guidelines for IV
administration, including dilution and
rate of administration
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


Constipation is a common adverse effect
and may be prevented with adequate fluid
and fiber intake
Instruct patients to follow directions for
administration carefully and to keep a
record of their pain experience and
response to treatments
Patients should be instructed to change
positions slowly to prevent possible
orthostatic hypotension
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




Decreased complaints of pain
Decreased severity of pain
Increased periods of comfort
Improved activities of daily living,
appetite, and sense of well-being
Decreased fever (acetaminophen)
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
Contact physician immediately if vital
signs change, patient’s condition
declines, or pain continues

Respiratory depression may be
manifested by respiratory rate of less
than 10 breaths/min, dyspnea,
diminished breath sounds, or shallow
breathing
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 Opioid agonist
 Schedule II narcotic
 Pregnancy Category C
 Given orally or parenterally
 Half life 2 – 4 hours
 Used for severe pain (chronic or acute)
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Indications
Relief of severe/acute/chronic pain,
analgesia during labor.

Morphine is the drug of choice for pain
due to Myocardial Infarction, dyspnea from
pulmonary edema not resulting from
chemical respiratory irritant.
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 Contraindications
Severe respiratory depression, acute/severe
asthma, severe hepatic/renal impairment. Used
with extreme caution in COPD, hypoxia, head
injury, increased intracranial pressure
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
Drug-Drug Interactions
◦ Use with EXTREME CAUTION in patients taking
MAOIs
◦ Increased CNS depression and hypotension with
alcohol, sedatives, hypnotics, barbiturates, tricyclic
antidepressants, antihistamines
◦ May INCREASE the anticoagulant effect of
Warfarin (Coumadin)
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› CNS

Impaired judgment
 Drowsiness (decrease in LOC)
 Decrease in respiratory effort
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Gastrointestinal
◦ Dry mouth
◦ Nausea, vomiting
◦ Decreased intestinal peristalsis
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CARDIOVASCULAR (CV)
› Bradycardia
› Vasodilation
› Tachycardia
› Flushing
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
GENITOURINARY
◦ URINARY RETENTION

ALLERGIC
◦ RASH
◦ ITCHING

RESPIRATORY
◦ RESPIRATORY DEPRESSION
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
Concurrent use of:
 Kava kave
 Valerian root
 Camomile
◦ Can result in increased CNS depression
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IV
PO
IM
IN (intra-nasal)
SC (SQ)
TRANSDERMAL
EPIDURAL
RECTAL
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
INTRAVENOUS
› Effective within 5 – 10 min. Of administration
› Most common route (in hospitalized patients)
› Frequently administered as patient controlled
analgesia (PCA)
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
DOUBLE LOCK SYSTEM
› TIME
› AMOUNT

NURSE MUST DOCUMENT:
› AMOUNT USED
› EFFECTIVENESS
› VITAL SIGNS INCLUDING RESPIRATIONS
› ANY UNTOWARD EFFECTS
› TEACH FAMILY ABOUT USE AND ABUSE
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
Catheter is placed into the epidural space to
inject a narcotic or anesthetic drug
◦ Obstetrics
◦ Surgical procedures
◦ Pain management

Catheter may be left in for follow up injections by
physician or patient controlled analgesia
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
SEVERE PAIN – CHRONIC PAIN
› FENTANYL PATCH (DURAGESIC) MOST COMMON
 Slower onset but more consistent pain relief
 Patch usually changed every 72h
 Treated just as any other narcotic – must account for
every patch
 Patch must be dated, timed and signed when placed
 Old patch must be removed when the new one is
placed
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
Assess effectiveness of medication
◦ Use the 0 – 10 scale to measure intensity of
pain

Assess for adverse effects
◦ Assess rate, depth, and rhythm of
RESPIRATIONS

Provide for patient safety
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



Blocks acetylcholine at the neuro-muscular
junction
Produces paralysis
Does NOT effect LOC
Drugs include:
◦ Pancuronium
◦ Succinycholine
◦ Vecuronium
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
Used for uncomfortable procedures such as:
◦
◦
◦
◦


Colonoscopy
Endoscopy
X-ray procedures
Minor surgery
Patient is unconscious but still able to protect
their airway
Amnesia is common
 midazolam (Versed)
 lorazepam (Ativan)
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Chapter 13
CNS depressants and
muscle relaxants
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 Sedative effect:
◦ Given during waking hours
 May cause drowsiness
 Hypnotic effect:
◦ Given at bedtime with the purpose of inducing
sleep
MAY BE THE SAME DRUG GIVEN AT
DIFFERENT DOSAGES
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
Prototype
› Diazepam (Valium)
 Antianxiety, anticonvulsant, sedative/hypnotic,
skeletal muscle relaxant
 Schedule IV drugs – Moderate potential for abuse
 Pregnancy category D
 Half-life 20-50 hours (metabolites also cause
sedation up to 100 hours)
 Drug of choice to treat status epilepticus (sustained
seizures)
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alprazolam (Xanax)
 chlordiazepoxide (Librium)
 flurazepam (Dalmane)
 lorazepam (Ativan)
 midazolam (Versed)
 triazolam (Halcion)

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
MECHANISM OF ACTION
◦ Binds with benzodiazepine receptors in nerve
cells of the brain; these cells also have binding
sites for GABA (gamma-aminobutyric acid)
which is an inhibitory neurotransmitter.

Excitatory v. Inhibitory transmitters
◦ Excitatory – Norepinephrine
◦ Inhibitory - GABA
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
Benzodiazapines and barbiturates work by
increasing the action of gaba in the brain

Gaba is an amino acid that inhibits nerve
transmissions in the brain
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
Indications – Not all drugs are appropriate
for all uses
◦ Antianxiety
◦ Hypnotic
◦ Anticonvulsant
◦ Preoperative sedation
◦ Prevent DTs in alcohol withdrawal
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 Contraindications
◦ Respiratory depression
◦ Liver disorder
◦ Kidney disorder
◦ History of alcohol or drug abuse
◦ Used cautiously with other CNS
depressants
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
Drug-Drug interactions
◦ Cimetidine, hormonal contraceptives, disulfiram,
fluoxetine, isoniazid, ketoconazole, metoprolol,
propoxyohene, propranolol, and valproic acid may
enhance the effects of sedatives by decreasing their
metabolism.
◦ May decrease the efficacy of levodopa
◦ Rifampin, barbiturates may increase the metabolism of
benzodiazepines, decreasing their effectiveness.
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
Herbal products to avoid when using
benzodiazepines
◦ Kava kava
◦ Valerian root
◦ Camomile

CAN INCREASE SEDATION

THIS APPLIES TO ALL CNS DEPRESSANTS
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
Adverse Effects
◦ CNS depression – drowsiness,
lightheadedness
◦ Paradoxical effects – insomnia, excitation
◦ Respiratory depression
◦ Hypotension
◦ Constipation/diarrhea
◦ Nausea, vomiting
◦ Rash
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
REVERSAL AGENT FOR OVERDOSE OF
BENZODIAZEPINES:
FLUMAZENIL
◦ INDICATED FOR THE REVERSAL OF MODERATE
SEDATION OR GENERAL ANESTHIA
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
ASSESS PATIENT WITH FOCUS ON REASON FOR
GIVING SEDATION
› ANXIETY
› NERVOUSNESS

REASSESS PATIENT FOR RESPONSE TO DRUG
› SEDATIVE Q 4-6 H
› HYPNOTIC AT BEDTIME

MONITOR VS AND POTENTIAL FOR DEPRESSION
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
Patient with a history or current use of
recreational drugs or alcohol abuse

Respiratory compromise

Pregnancy or lactation
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
Administer accurately
◦ Teach patient about expected effects and
possible side effects
◦ Provide for patient safety

Observe for therapeutic effects
◦ Decrease in anxiety
◦ Positive signs of sleep
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
Observe for adverse effects
◦ Excessive sedation
◦ Hypotension

Observe for drug interactions
◦ Concurrent use of other cns depressants
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ALCOHOL
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
Stimulant and depressant
◦ Stimulates the adrenal gland
◦ Depresses the CNS

Physical manifestations
◦
◦
◦
◦
◦
Acts as a diuretic
Increases gastric acidity
Cardiomyopathy
Peripheral vasodilation
Electrolyte imbalance
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
Delirium tremens – Latin for “shaking frenzy”

Abrupt alcohol (ETOH) withdrawal

Mismatch between excitatory (norepinephrine)
and inhibitory (GABA) receptors in the brain
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◦ Confusion
◦ Diarrhea
◦ Insomnia
◦ Disorientation
◦ Agitation
◦ Fever
◦ Tachycardia
◦ Hypertension
◦ Visions of insects
◦ Severe anxiety
◦ Fear of death
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
Many safety issues

Do not mix with other CNS depressants

Monitor patients’ liver function

Patient may have altered clotting factors

Patient may have withdrawal symptoms
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PSYCHOTHERAPEUTIC
MEDICATIONS
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
A group of mental disorders characterized
by a vague uneasy feeling of discomfort
or dread. The symptoms of anxiety
prevent the individual from normal
functioning . can be an exaggerated
response to an actual event or anxiety
unrelated to an identifiable event or
condition.
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◦ Panic disorder
◦ Generalized anxiety disorder
◦ Obsessive-compulsive disorder
◦ Post-traumatic stress disorder
◦ Simple phobia
◦ Social phobia
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Tricyclic antidepressants
 Benzodiazepines
 MAOIs
 Buspirone
 SSRIs

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 Mechanism
of action – unknown
◦ Interacts with serotonin and dopamine in
the brain
◦ No muscle relaxant effects
◦ No anticonvulsant effects
◦ Does not cause sedation
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
Uses / indications
◦ Short term management of anxiety disorders
◦ Not appropriate for immediate relief – may
take several weeks to see effects
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
Side effects
◦ Dizziness, nausea, headache, anxiety,
fatigue, insomnia

Contraindications
◦ Renal/hepatic failure
◦ Use of MAOIs
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ANTIDEPRESSANTS
AND MOOD
STABILIZERS DRUGS
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 Monoamine
neurotransmitter
dysfunction
◦ Deficiency of norepinephrine and/or serotonin.
◦ Balance, integration and interactions among
norepinephrine, serotonin, and other
neurotransmission systems is an important
etiological factors.
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 Neuroendocrine
factors
◦ AN INCREASE IN CRF (corticotropin releasing
factor/hormone) HAS BEEN NOTED IN
PATIENTS WITH DEPRESSION.
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
Tricyclic antidepressants

Monoamine oxidase inhibitors

Selective serotonin reuptake inhibitors

Unclassified drugs
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



imipramine (Tofranil) prototype
nortriptyline (Pamelor)
amitryptyline (Elavil)
desipramine (Norpramin)
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

First generation of antidepressant therapy
Mechanism of action
› Corrects the imbalance in the neurotransmitter concentrations of
serotonin and norepinephrine at the nerve endings in the CNS.
This is done by blocking the reuptake of the neurotransmitters and
thus causing these neurotransmitters to accumulate at the nerve
endings.
› Also have nonselective receptor antagonism causing
many side effects.
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
Indications
◦ Depression
◦ Childhood enuresis(bed wetting)
 Imipramine
◦ Obsessive compulsive disorder
 Clomipramine
◦ Chronic pain syndromes
 Neuropathic pain (trigeminal neuralgia)
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
Adverse effects
◦ Sedation
◦ Impotence
◦ Orthostatic hypotension
◦ Disturbs cardiac conduction
◦ Delayed micturation
◦ Edema
◦ Muscle tremors
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
Interactions
◦ WHEN TAKEN WITH MAOIs MAY RESULT IN
INCREASED THERAPEUTIC LEADING TO TOXIC
EFFECTS (HYPERPYRETIC CRISIS)
◦ TCAs can inhibit the metabolism of warfarin,
resulting in an increase in anticoagulation
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
Toxicity and management of overdose
◦ TCA overdoses are fatal 70% - 80% of the time
◦ Death usually results from seizures or dysrhythmias
◦ THERE IS NO SPECIFIC ANTIDOTE FOR TCAs
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
First generation of antidepressant drugs
◦ Highly effective
◦ Many side effects and drug/drug, drug/food
interactions
◦ Disadvantage: potential to cause hypertensive
crisis when taken with tyramine
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phenelzine (Nardil)
 tranylcypromine (Parnate)

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
Inhibit the MAO enzyme system in the CNS

Amines (dopamine, serotonin, norepinephrine) are
not broken down, resulting in higher levels in the
brain

Result: alleviation of symptoms of depression
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
Depression, especially types characterized by
symptoms such as increased sleep and appetite
depression that does not respond to other drugs
such as tricyclics
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Tachycardia
 Dizziness
 Insomnia
 Anorexia
 Blurred vision

Palpitations
 Drowsiness
 Headache
 Nausea
 Impotence

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
Symptoms appear 12 hours after
ingestion

Tachycardia, circulatory collapse,
seizures, coma

Treatment: protect brain and heart,
eliminate toxin
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Ingestion of foods and/or drinks with
the amino acid tyramine leads to
hypertensive crisis, which may lead
to cerebral hemorrhage, stroke,
coma, or death
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Avoid foods that contain tyramine!





Aged, mature cheeses (cheddar, blue, Swiss)
Smoked/pickled or aged meats, fish, poultry (herring,
sausage, corned beef, salami, pepperoni, pâté)
Yeast extracts
Red wines (Chianti, burgundy, sherry, vermouth)
Italian broad beans (fava beans)
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Concurrent use of MAOIs and SSRIs may
lead to serotonin syndrome
 If the decision is made to switch to an
SSRI, there must be a 2- to 5-week “washout” period between MAOI therapy and
SSRI therapy

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Delirium
Tachycardia
Hyper-reflexia
Shivering
Agitation
Sweating
Muscle spasms
Coarse tremors
More severe cases
Hyperthermia
Renal failure
Rhabdomyolysis
Dysrhythmias
Seizures
DIC
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fluoxetine (Prozac)
paroxetine (Paxil)
sertraline (Zoloft)
fluvoxamine (Luvox)
citalopram (Celexa)
escitalopram (Lexapro)
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
Fewer adverse effects than tricyclics and
MAOIs

Very few drug-drug or drug-food interactions

Still takes about 4 to 6 weeks to reach
maximum clinical effectiveness
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0
Mechanism of action
 Selectively inhibits serotonin reuptake
 Little or no effect on norepinephrine or
dopamine reuptake
 Result in increased serotonin concentrations
at nerve endings
Advantage over tricyclics and MAOIs: little or
no effect on cardiovascular system
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1

INDICATIONS
◦ Depression
◦ Bipolar disorder
◦ Obesity
◦ Eating disorders
◦ Obsessive-compulsive
disorder
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3
Body System
Effects
CNS
Headache, dizziness,
tremor, nervousness,
insomnia,* fatigue
Nausea, diarrhea,
constipation, dry mouth
Sexual dysfunction,
* weight gain,* weight
loss, sweating
GI
Other
* Most common and bothersome
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4
Duloxetine (Cymbalta)
 Venlafaxine (Effexor)

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
Indicated
◦ For depression and general anxiety disorder
◦ Also pain associated with diabetic peripheral
neuropathy

Contraindicated
◦ CONCURRENT USE OF MAOIs
◦ Angle closure glaucoma
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
Drug Interactions
◦ Highly bound to plasma proteins
◦ Compete with other protein-binding
drugs, resulting in more free, unbound
drug to cause a more pronounced
drug effect
◦ Inhibition of cytochrome P-450 system
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
bupropion
◦ Wellbutrin, zyban
 Commonly prescribed for smoking cessation

maprotiline
◦ Similar to TCAs

Mirtazapine
◦ Remeron
 Often prescribed to enhance appetite
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





Comprehensive patient history
Complete medication history
Monitor patient for therapeutic effects
Monitor patients for adverse effects
Education of patient on drug expectations
and adverse effects
Educate patient regarding drug-drug, drug-food
and drug-herbal interactions
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
lithium carbonate
 Eskalith, lithobid
◦ MOA – not completely understood
 Managed using serum levels
◦ Indications – mania, bipolar disorder
◦ Adverse effects
 vomiting, diarrhea, drowsiness, difficult
coordination, hand tremors, muscle twitching,
mental confusion
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
Monitor serum lithium levels
◦ Therapeutic levels are 1.0 – 1.5 meq/L


Lithium is eliminated intact by the kidneys.
Encourage fluids to completely eliminate the
drug
Monitor for therapeutic and adverse effects
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
A severe mental disorder characterized by
disordered thought process and often
bizarre thinking.
 Hypoactivity or hyperactivity
 Agitation
 Aggressiveness
 Hostility
 Social withdrawal
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
Antipsychotic AKA Neuroleptic:
◦ Any drug that modifies or treats psychotic
behaviors usually by blocking dopamine
receptors in the brain
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Thioxanthenes
thiothixene (Navane)
Phenylbutylpiperidines
haloperidol (Haldol)
Dihydroindolones
molindone (Moban)
Dibenzodiazepines
loxapine (Loxitane)
Benisoxazoles
Risperidone
Quinolinine
Aripiprazole (Abilify)
Phenothiazines
Chlorpromazine (Thorazine)
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
Schizophrenia
◦ Long half-life facilitates better compliance
by patients

Long-term treatment of psychosis

Can be given either IV or po
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
Seizures

Extrapyramidal reactions

Blurred vision, dry eyes

Neuroleptic malignant syndrome

Tartive dyskinesia
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
A potentially fatal syndrome with symptoms:
◦
◦
◦
◦
◦
◦
◦
◦
Hyperthermia
Catatonic rigidity
Altered mental status
Profuse sweating
Rhabdomyolysis
Renal failure
Seizures
Death
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8
◦ Involuntary contractions of oral and facial
muscles
◦ Choreoathetosis (wavelike movements of
extremities)
◦ Occurs with continuous long-term
antipsychotic therapy (esp. phenothiazines)
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◦ Involuntary muscle symptoms similar to
those of Parkinson’s disease
◦ Akathisia (distressing muscle
restlessness)
◦ Acute dystonia (painful muscle spasms)
◦ Treated with benztropine (Cogentin) and
trihexyphenidyl (Artane)
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
Recognizing extrapyramidal symptoms

http://www.youtube.com/watch?v=WAg2iLEWVh0
&playnext=1&list=PLFA09E8C6FCF4EC70&featur
e=results_main
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clozapine (Clozaril)
 risperidone (Risperdal)
 olanzapine (Zyprexa)
 quetiapine (Seroquel)
 ziprasidone (Geodon)
 aripiprazole (Abilify)

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Block dopamine receptors in the brain
(limbic system, basal ganglia)—areas
associated with emotion, cognitive
function, motor function
 Dopamine levels in the CNS are
decreased
 Result: tranquilizing effect in psychotic
patients

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◦ Reduced effect on Prolactin levels
 Stimulates mammary glands to produce milk
◦ Lower risk of
 Neuroleptic malignant syndrome
 Extrapyramidal adverse effects
 Tartive dyskinesia
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
Treatment of serious mental illnesses
◦
◦
◦
◦


Bipolar affective disorder
Depressive and drug-induced psychoses
Schizophrenia
Autism
Movement disorders (such as Tourette’s
syndrome)
Some medical conditions
◦ Nausea, intractable hiccups
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Body System
CNS
Cardiovascular
Dermatologic
Adverse Effects
Sedation, delirium
Orthostatic hypotension,
syncope, dizziness,
EKG changes
Photosensitivity, skin
rash, hyper-pigmentation,
pruritus
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Body System
Adverse Effects
GI
Dry mouth, constipation
GU
Urinary hesitancy or
retention, impaired
erection
Hematologic
Leukopenia and
agranulocytosis
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Body System
Metabolic/endocrine
Adverse Effects
Galactorrhea,
irregular menses,
increased appetite,
polydipsia
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
Before beginning therapy, assess both the
physical and emotional status of patients

Obtain baseline vital signs, including postural BP
readings

Obtain liver and renal function tests
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
Assess for possible contraindications to
therapy, cautious use, and potential drug
interactions

Assess LOC, mental alertness, potential
for injury to self and others

Check the patient’s mouth to make sure
oral doses are swallowed
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
Provide simple explanations about the drug,
its effects, and the length of time before
therapeutic effects can be expected

Abrupt withdrawal should be avoided

Advise patients to change positions slowly to
avoid postural hypotension and possible
injury
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
The combination of drug therapy and
psychotherapy is emphasized because patients
need to learn and acquire more effective coping
skills

Only small amounts of medications should be
dispensed at a time to minimize the risk of
suicide attempts

Simultaneous use of these drugs with alcohol or
other CNS depressants can be fatal
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
Skeletal muscle relaxants are used to decrease
muscle spasm or spasticity that occurs in certain
neurologic and musculoskeletal disorders.
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
Indications
› Relief of painful musculoskeletal
conditions
 Muscle spasms
 Management of spasticity of severe
chronic disorders
 Multiple sclerosis, cerebral palsy
› Work best when used along with
physical therapy
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
Muscle spasms
◦ Sudden involuntary muscle contraction
◦ Can occur secondary to trauma, inflammation,
sprains, strains, arthritis, spinal disorders
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


MECHANISM OF ACTION
Act to relieve pain associated with skeletal
muscle spasms
Majority are central acting
◦ CNS is the site of action
◦ Similar in structure and action to other CNS
depressants

Direct acting
◦ Acts directly on skeletal muscle
◦ Closely resembles GABA (an inhibitory
neurotransmitter)
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baclofen (Lioresal)
 cyclobenzaprine (Flexeril)
 carisoprodol (Soma)
 metaxalone (Skelaxin)
 methocarbamol (Robaxin)


tizanidine (Zanaflex)

DIRECT ACTING
 dantrolene (Dantrium)
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
Muscle spasticity
◦ Spasticity involves increased muscle tone or
contraction
◦ Can occur secondary to spinal cord injury,
multiple sclerosis, cerebral palsy, muscular
dystrophy
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
Extension of effects on CNS and skeletal
muscles
◦ Euphoria
◦ Lightheadedness
◦ Dizziness
◦ Drowsiness
◦ Fatigue
◦ Muscle weakness, others
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
Nursing implications
◦ Monitor therapeutic response to medication
◦ Monitor for adverse reactions
◦ Nursing diagnosis appropriate to specific
patient
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Anticonvulsants
Antiseizure drugs
Antiepileptic drugs
(AEDs)
Chapter 15
MEDICATION TO
CONTROL SEIZURES
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
A brief episode of abnormal electrical activity of
nerve cells in the brain
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4

GOAL OF TREATMENT
◦ Control seizures without causing undue sedation
and experiencing minimal adverse reactions
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5
DRUGS TO CONTROL
SEIZURES
CARBAMAZAPINE
TEGRETOL
CLONAZEPAM
KLONOPIN
FOSPHENYTOIN
CEREBYX
GABAPENTIN
NEURONTIN
CHLORAZEPATE
LORAZEPAM
DIAZEPAM
VALIUM
PHENYTOIN
(PROTOTYPE)
LUMINAL
VALPROIC ACID
TRANXENE
PHENOBARBITAL
ATIVAN
DILANTIN
DEPAKENE
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
FIRST USED IN 1903
› PHENOBARBITAL
 MOST COMMONLY PRESCRIBED FOR STATUS
EPILEPTICUS
 MORE OFTEN USED IN NONINDUSTRIALIZED
COUNTRIES BECAUSE OF LOW COST
 CLINICAL CLASSIFICATION – ANTICONVULSANT,
HYPNOTIC
 LONG HALF-LIFE
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
Classification
◦ Anticonvulsant
◦ Antiarrhythmic

MOA
◦ Stabilize neuronal membranes in the motor
cortex of the brain. Limits the spread of
seizure activity
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
Contraindications
› Seizures caused by hypoglycemia or high fever

Side effects
› Drowsiness, lethargy, confusion, slurred speech
› Gingival hyperplasia
› Fever, rash, lymphadenopathy

Monitor serum dilantin levels
› 10 -20 mcg/ml IS THERAPEUTIC


Monitor liver function
Decreases many drug levels including oral
contraceptives
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0

NURSING CONSIDERATIONS
◦ REVIEW HISTORY OF SEIZURES
◦ INITIATE SEIZURE PRECAUTIONS
◦ PATIENT EDUCATION
 WHAT TO EXPECT FROM MEDICATION
 DO NOT EVER OMIT A DOSE
 MUST MAINTAIN THERAPEUTIC BLOOD LEVELS OR
SEIZURES WILL RECUR
◦ SEE “NURSING PROCESS – ASSESSMENT” P.238
◦ DOCUMENT TYPE AND CHARACTER OF SEIZURE
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
Classification:
◦ Anticonvulsant
◦ Vascular headache suppressant

Mechanism of action
◦ Increases levels of gaba in the CNS

Adverse reactions
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
Adverse reactions
 Agitation
 Dizziness
 Headache
 Insomnia
 Sedation
 Visual disturbances
 Tremor
 Ataxia
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
Classification – anticonvulsant

Mechanism of action
◦ Alters ion transport in the CNS

Indicated for short term management of
generalized seizures, status epilepticus

Parenteral administration only
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
Indications – treatment of clonic-tonic, mixed and
complex seizures

Mechanism of action – decreases synaptic
transmission in the CNS by affecting sodium
channels in the neurons
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
Adverse reactions
 Ataxia
 Drowsiness

Drug-drug interactions
◦ Many

Drug food interactions
◦ Grapefruit juice increases serum levels and increases
the drug effects (toxicity?)

THERAPEUTIC SERUM DRUG LEVELS – 4-12mcg/ml
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7
DRUGS FOR
PARKINSON’S
DISEASE
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
Progressive, degenerative neurologic
disorder caused by a imbalance between
acetylcholine and dopamine in the brain
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
Signs and symptoms
› Shuffling gait
› Fine tremors
› Muscle rigidity
› Slurred speech
› Emotionless facial expression (mask-like)
› Difficulty chewing and swallowing
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
Anticholinergic drugs

Antihistamines

Dopaminergic’s
◦ Direct acting dopamine receptor agonists
◦ Indirect acting dopamine receptor agonists
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
benztropine, procyclidine, trihexyphenidyl
◦ Drugs that block the effects of acetylcholine
 As dopamine decreases, acetylcholine
increases causing muscle tremors and
rigidity (more pronounced at rest)
 Pill rolling
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
Anticholinergic effects DECREASE:
◦ Salivation
◦ Tearing of the eyes,
◦ Urination
◦ Diarrhea
◦ Increased GI motility
◦ Emesis (vomiting)
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
Contraindications
◦ Known drug allergy
◦ GI or bladder obstruction
◦ Cardiac disease
◦ Glaucoma
◦ Myasthenia gravis
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
Used for their anticholinergic effects
◦ diphenhydramine (Benadryl)
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
Direct acting medication increase the levels of
dopamine at the synapse.
› bromocriptine – dopamine agonist
› pergolide – dopamine agonist
› pramipexole - dopamine agonist
› levodopa – dopamine replacement
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
Indirect acting increase dopamine levels by inhibiting
enzymes that break down dopamine
› Carbidopa – inhibits enzyme AADC
› Entacapone – COMT inhibitor
› Tolcapone – COMT inhibitor
› Selegiline – MAOI

Others
› Amantadine – synthetic antiviral
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
Levodopa (prototype)
◦ Precursor to dopamine
 Dopamine does not cross the blood-brain barrier.
Can cross as levodopa and is then converted to
dopamine

Carbidopa
◦ Prevents the conversion of levodopa to dopamine in
the peripheral tissues
◦ Does not cross the blood brain barrier
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
ACTION OF MAO
◦ Primary roll is the catabolism or breakdown of
catecholamines such as dopamine, norepinephrine
and epinephrine. Also breaks down serotonin.
 Rasagiline (azilect)
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
Catechol-o-methytransferase
◦ A naturally occurring enzyme in the body that
breaks down dopamine molecules
◦ By inhibiting this enzyme, the action of
levodopa is prolonged
◦ Medications:
 tolcapone (Tasmar)
 entacapone (Comtan)
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Drowsiness

Confusion


Orthostatic hypotension


Dystonia
Dyskinesia
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
Risk for injury due to postural hypotension
◦ Rise slowly from sitting or lying position

Difficulty with communication

Safety issues r/t unsteady, shuffling gait

Never stop meds abruptly

Take meds on time

Watch for adverse reactions
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
ON – OFF:
Disease is worsening, too little dopamine is
present

WEARING OFF:
Gradual worsening of Parkinson’s symptoms as
the drugs lose their effectiveness
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5