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DRUGS ACTING ON THE CENTRAL NERVOUS SYSTEM

Neurotransmitters (NT)- group of chemical substances released by neurons to stimulate other

neurons or muscle or gland cells.
Action Potential (AP)- travels the length of the axon and causes release of neurotransmitter into
the synapse
Re-uptake - reabsorption of a neurotransmitter by a neurotransmitter transporter

Excitatory NT
causes Depolarization
(influx of positive ion)
↑↑↑ action potential
↑↑↑ response
Inhibitory NT
causes Hyperpolarization
(influx of negative ion)
↓↓↓ action potential
↓↓↓ response

If the neuron is Dopaminergic If the neuron is Serotonergic If the neuron is Adrenergic If the neuron is GABAergic
NT: DOPAMINE (DA) NT: SEROTONIN (5-HT) NT: NOREPINEPHRINE NT: GABA
(5-Hydroxy tryptamine) Gamma-aminobutyric
Receptor Receptor acid
Receptor
Depolarization Depolarization Receptor
Hyperpolarization Depolarization
Hyperpolarization Response: Hyperpolarization
Response: Sympathetic
Cognition Response: GABA - major inhibitory
response
Mood regulation Mood regulation neurotransmitter
↑ Pleasure & reward ↓ feeling of
seeking behavior depression and Metabolizing enzyme:
anxiety Monoamine Response:
Addiction
Body movements ↑ happiness Oxidase (MAO) Producing a calming
and coordination ↓ libido (sex drive) Catechol O-methyl effect
Promotes sleep transferase (COMT)
Metabolizing enzyme: Digestive functions Metabolizing enzyme:
Monoamine GABA-transaminase
Oxidase (MAO) Metabolizing enzyme:
Catechol O-methyl Monoamine
transferase (COMT) Oxidase (MAO)

OVERVIEW OF DISEASES
PSYCHOSIS
↑ dopamine INSOMIA
DEPRESSION
↑ serotonin ↓ GABA ANXIETY
↓ Norepinephrine
↓ Melatonin ↓ GABA
PARKINSON’S DISEASE ↓ Serotonin
↑ Orexin ↓ Serotonin
↓ dopamine ↓ Dopamine
↑ Histamine

CNS STIMULANTS CNS DEPRESSANTS

Numerous drugs can stimulate the CNS, but Drugs that are central nervous system depressants
medically approved use of these drugs is limited to cause varying degrees of depression within the
the treatment of Attention Deficit / Hyperactivity CNS.
Disorder (ADHD), Narcolepsy, Obesity & reversal of The degree of depression depends primarily on the
respiratory distress. drug and the amount of drug taken
These drugs can calm hyperkinetic children and Class: Sedative-Hypnotics, General anesthetics,
help them focus on one activity for a longer period. Analgesics, Anticonvulsants, Antipsychotics,
Antidepressants.
 CNS STIMULANTS Therapeutic Action
Redirect and excite arousal stimuli from the RAS. Acting as both cortical and RAS stimulants
Majority of CNS stimulants are controlled possibly by increasing catecholamine release
substances so it is important for patients to be from presynaptic neurons, CNS stimulants are
taught how to secure them to prevent inappropriate able to increase stimulation of postsynaptic
use and distribution. neurons.
The paradoxical calming effect of these drugs
in hyperkinetic children is thought to be
DRUGS related to the increased stimulation of an
AMPHETAMINES immature RAS leading to an ability to be more
Amphetamine (Adderall), Dextroamphetamine selective in response to coming stimuli.
(Dexidrine), Methamphetamine (Desoxyn)
MOA: Stimulate release of DA & NE causing euphoria
Indications
and alertness
Indications: ADHD, narcolepsy Attention-deficit disorders
CI: Hyperthyroidism, agitated states Narcolepsy
AE/SE: Dry mouth, Impotence
NR: Monitor vital signs, monitor weight, offer fluids,
provide reassurance, report extreme restlessness/ Contraindications & Cautions
insomnia, monitor for withdrawal, no caffeine, Caution should be used with extended-release
alternative therapies to help sleep preparations because they differ markedly in
timing and effectiveness.
AMPHETAMINE LIKE DRUGS Children should be assessed carefully and
Methylphenidate (Ritalin), Atomoxetine (Strattera), challenged periodically for the necessity of
Modafinil (Provigil) continuing the drug.
MOA: Produces CNS and respiratory stimulation Cautious use of these drugs for pregnant and
with weak sympathomimetic activity lactating women is implemented because of
Indications: ADHD, narcolepsy potential adverse effects to fetus or neonate.
CI: Hyperexcitable states Reduced doses of drugs for older adults are
AE/SE: Hyperactivity, Tremors required because this population is more
NR: same as for amphetamines susceptible to drug adverse effects.
Hypersensitivity
ANOREXIANT Marked anxiety, agitation, tension and severe
Benzphetamine (Dexadrine) - OTC fatigue, glaucoma.
Silbutramine (Meridian) - RX Cardiac disease, hypertension
MOA: Stimulates CNS activity, suppresses appetite History of seizures
CI: < 12 years old History of drug dependence including
AE/SE: Irritability alcoholism
NR: Monitor length of time being treated, teach Pregnancy, lactation (potential adverse effects
patient diet management, encourage exercise on the fetus or neonate)
ANALEPTIC
Caffeine, Theophylline Side Effects / Adverse Effects
MOA: Affects brainstem, spinal cord, and cerebral
cortex, Relaxes bronchial smooth muscle, Increases CNS: nervousness, insomnia, dizziness,
heart rate and blood pressure, Stimulates headache, blurred vision, difficulty with
respirations accommodation
Indication: Used for newborns with apnea CV: hypertension, arrhythmias, angina
AE/SE: Necrotizing enterocolitis (rare but deadly) GI: anorexia, nausea, weight loss
NR: Do not take before bedtime, increased urine Skin rashes are common reactions
output Physical and psychological dependence

RESPIRATORY CNS STIMULANT

Doxapram (Dopram) Nursing Responsibilities
MOA: Low dose --> Stimulates carotid receptors
Arrange to interrupt the drug periodically in
High dose --> stimulates respiratory center in
children to determine whether symptoms
medulla, produces generalized CNS stimulation
recur and therapy should be continued.
Indication: Respiratory depression caused by drug
Arrange to dispense the least amount of drug
overdose, COPD, Pre & postanesthetic res-dep.
possible to minimize risk of overdose and
CI: used with caution for neonatal apnea
abuse.
AE/SE: Laryngospasm (rare but deadly)
Administer drug before 6 PM as ordered to
NR: Monitor for signs of overdose, frequently assess
reduce the incidence of insomnia.
IV site
Monitor weight, CBC, and ECG to ensure early
detection of adverse effects and proper
Drug-Drug Interactions interventions.
MAOIs: increased risk of adverse effects and Provide safety measures (e.g. adequate
increased toxicity lighting, raised side rails, etc.) to prevent
Guanethidine: decreased in antihypertensive injuries.
effects Educate client on drug therapy to promote
TCAs, phenytoin: increased drug levels understanding and compliance.
 CNS DEPRESSANTS

Sedative-hypnotics Antipsychotics Anticonvulsants Analgesics General Anesthetics

H
Y Anxiety D Insomnia
P E
E P
R Limbic System O Wakefulness/ Wakefulness/
P L
O ↑GABA ↓GABA A Arousal Arousal
L R
A
R ↑ 5-HT ↓ 5-HT I
I Z OREXIN HISTAMINE
Z Sympathetic NS A
A T Hypothalamus
T I
I O
O N GABA MELATONIN
N

Wakefulness/ Sleep
Arousal
↑ HR & BP Tremors Diaphoresis ↑ Resp rate

SEDATIVE-HYPNOTICS cause a dose-dependent depression of the CNS function, inducing

sedation, sleep, and unconsciousness with increasing dose.
ANXIOLYTICS
Barbiturates
MOA: Inhibit impulse conduction in the ascending RAS, depress cerebral cortex, alter cerebral
function, and depress motor nerve input. Increases the influx of a negative ion (Cl) causing
hyperpolarization.
Indication: Control of tonic-clonic, status epilepticus, and psychomotor seizures. Prevention of
seizures during neurosurgery. Barbiturates are controlled substances due to high abuse potential.
CI: Hypersensitivity, Pregnancy & Lactation, Debilitated patients, Impaired hepatorenal function,
Coma, Depression, Psychoses
AE/SE: GU: urinary retention, loss of libido
CNS: depression, confusion, drowsiness, lethargy, fatigue, sedation, hypnosis, anesthesia, deep coma
CV: arrhythmias, changes in blood pressure
GI: constipation, dry mouth, anorexia
Others: physical dependence, withdrawal symptoms, severe dermatological reactions
Interactions: Alcohol: increased risk of CNS depression | Ginkgo: increased risk of serious adverse effects

Ultra-short acting: Thiopental (hypnosis & anesthesia)

Short acting: Secobarbital (insomnia)
Long-acting: Narrow Therapeutic Index
Phenobarbital depresses lower brainstem, cerebral cortex, and motor conduction
Mephobarbital used in tonic-clonic and absence seizures. Also used as an anxiolytic or hypnotic.
Mephobarbital is commonly associated with CNS and GI effects. It can also cause circulatory
collapse and apnea which makes it less desirable compared to other antiseizure agents.

Benzodiazepines
MOA: Act primarily in the limbic system and RAS so it can also cause muscle relaxation and relief of
anxiety without substantially affecting the functions of the cortex. Increases the influx of a negative
ion (Cl) causing hyperpolarization.
Indication: Used as adjunct to treatment of status epilepticus and severe recurrent convulsive
seizures. Also used to manage epilepsy in patients who require intermittent use to control bouts of
increased seizure activity. It can be used as agent to relieve anxiety before operative interventions.
CI: Hypersensitivity, Pregnancy & Lactation, Debilitated patients, Impaired hepatorenal function,
Coma, Depression, Psychoses
AE/SE: CNS: depression, confusion, drowsiness, lethargy, fatigue
CV: arrhythmias, changes in blood pressure
GI: constipation, dry mouth, anorexia
GU: urinary retention, loss of libido
Others: physical dependence, withdrawal symptoms
Interactions: Alcohol: increased risk of CNS depression

Short acting: Midazolam, Triazolam

Intermediate acting: Lorazepam, Oxazepam, Alprazolam, Temazepam
Long acting: Diazepam, Clonazepam, Flurazepam
 Miscellaneous Nursing Responsibilities
Z-Drugs (No anxiolytic effect) Avoid alcohol, antidepressants, antipsychotic,
Zaleplon and opioid drugs while taking benzodiazepine.
Zolpidem (SE: Headache) Respiratory depression may occur when these
Eszopiclone drugs are combined
Stress management –counseling, relaxation
Melatonin receptor agonist techniques, referrals for mastery of biofeedback,
Ramelteon meditation, express feelings, channeling toward
positive realistic goals
Buspirone - partial agonist of 5-HT receptors Fostering health maintenance –discuss med,
Chloral hydrate - mild hypnotic used for how it benefits, stress non- pharmacologic
insomnia interventions, compliance, provide significant
Suvorexant - Orexin receptor antagonist other information, adverse effects and serious
Diphenhydramine - Antihistamine adverse effects.
SSRIs Written Record –record of monitoring
SNRIs Please refer to “Antidepressants” parameters, assess understanding

Benzodiazepines P ANXIOLYSIS SSRI

Alprazolam R SNRI
Clonazepam N
Acute Anxiety Chronic Anxiety
Diazepam PRN BENZO
Lorazepam Generalized Anxiety Disorder or
Oxazepam Social Anxiety Disorde BUSPIRONE
Panic-Attack Anxiety Disorde

HYPNOSIS

Stress/Anxiety Mild-Moderate Sleep Depression

Related Insomnia Insomnia Induction Related Insomnia

Benzodiazepines Z-Drugs Melatonin Agonist 5-HT Agonist

Flurazepam Eszopiclone Ramelteon / Antihistamine
Temazepam Zolpidem Orexin Antagonist (TCAs)
Zaleplon Suvorexant Doxepin
↓ residual Mirtazapine
drowsiness Trazadone

PSYCHOSIS / SCHIZOPRENIA

MESOCORTICAL PATHWAY MESOLIMBIC PATHWAY

Ventral Tegmental Area (VTA)

Nucleus Accumbens
Prefrontal cortex

Ventral Tegmental Area (VTA)

↑ Dopamine in D2 Receptor

↓ Dopamine in D1 Receptor
Positive Symptoms
Most antipsychotics block the changes in thoughts and
Negative Symptoms dopamine 2 receptor. feelings that are “added on” to
things that are “taken away” or Decreasing the dopamine in the a person's experiences
reduced Mesolimbic pathway. Treating Delusions
reduced motivation the positive symptoms Hallucinations
reduced intensity of Disorganized Speech or
emotion Behaviour
 Referred to as neuroleptics or major tranquilizers. Prescribed to treat
ANTIPSYCHOTICS schizophrenia and to reduce the symptoms associated with psychotic
conditions such as bipolar, psychotic depression, senile psychoses,
various organic psychoses, and drug-induced psychoses.

Typical Antipsychotics / 1st Generation Antipsychotics

Developed in 1950s
MOA: Block dopamine receptors, preventing dopamine from stimulating the postsynaptic neurons.
Indication: Schizophrenia and manifestations of other psychotic disorders including hyperactivity,
combative behavior, and severe behavioral problems. Some antipsychotics are approved for
treatment of bipolar disorder. Useful when new medications are ineffective.
AE/SE: Hypotension, anticholinergic effects, and extrapyramidal side effects (EPS)

Haloperidol (Haldol)
Chlorpromazine (Thorazine)

Atypical Antipsychotics / 2nd Generation Antipsychotics

Approved for use in the 1990s
This category of drugs has also been of great value in studying the pathophysiology of
schizophrenia and other psychoses.
MOA: Block both dopamine and serotonin receptors (This dual blocking action help relieve
neurological adverse effects associated to typical antipsychotics)
Indication: are used for treatment of severely ill patients with schizophrenia but are unresponsive
to standard drugs. It also reduces the risk of recurrent suicidal behaviors in patients with
schizophrenia and schizoaffective disorders

Risperidone (Risperdal) is commonly used for treatment of irritability and aggression in children
and adolescents with autism
Clozapine (Clozaril) was categorized as the first atypical antipsychotic drug
Olanzapine (Zyperea), Quetiapine (Seroquel), Aripiprazole

Adverse Effects / Side Effects

Extrapyramidal Effects: Dystonia, akathisia, tardive dyskinesia, Parkinson’s-like symptoms,
unwanted movements, ataxia, muscle breakdown, rigidity, tremors, and seizures are some major
effects of this category of drugs. Neuroleptic malignant syndrome may occur as well.
Effects on the Central Nervous System: Drowsiness, sedation, and hypnosis occur. Confusion,
vertigo, syncope, disturbed sleep, nightmares, and agitation are also reported by various
studies. Dementia, amnesia, and loss of memory are some adverse effects. Suicidal ideation in
old and young with increased mania, anxiety, agitation, violent behavior, and depression can also
be seen in people taking these drugs.
Effects on the Cardiovascular System: Cardiomyopathy is noted in nine out of every 100,000
people using clozapine. Alteration in electrocardiogram (ECG) readings, chest pain, angina,
myocarditis, palpitation, tachycardia, edema, phlebitis, and arrhythmias are serious adverse
effects. Myocardial infarction (heart attack) occurs in only 1% of people using this category of
drug. Orthostatic hypotension—the medical name for the fuzzy feeling you get when standing up
to quickly—is very common.
Hepatic (Liver) Effects: These agents increase the serum concentration of alkaline
aminotransferase. Reversible liver cell hyperplasia, increase in bilirubin, jaundice, drug induced
hepatitis, and necrosis have been recorded in studies.
Gastrointestinal Effects: Constipation, dry mouth, anorexia, weight gain, increases in pancreatic
enzymes, epigastric distress, abdominal cramps, dyspepsia, heartburn, and nausea are some
common adverse effects.
Genitourinary (Urinary and Reproductive) Effects: Impotence, delayed and premature
ejaculation, testicular swelling, priapism, increased or decreased libido, virginal itching, enuresis,
polyuria, breast engorgement, galactorrhea, and anorgasmia have been reported.
Other Effects: Cases of blurred vision, hot flashes, dry throat, nasal congestion, severe
hyperglycemia, numbness, chills, glaucoma, leukopenia, neutropenia, hyperlipidemia,
agranulocytosis, and respiratory depression have been reported.
Pregnancy and Lactation: Antipsychotic drugs can be used in pregnant females since they have
shown no teratogenic (development of the fetus or embryo) effects in animal studies. Drugs like
clozapine and olanzapine have shown no harm to the fetus. However, during lactation, the
metabolites may be disturbed in the milk and could harm the newborn.
 Contraindications
Presence of diseases that can be exacerbated by dopamine-blocking effects
CNS depression, circulatory collapse, Parkinsons’ disease, coronary disease, severe
hypotension, bone marrow suppression, blood dyscrasias. Exacerbated by drug effects
QTc interval prolongation. Contraindicated to mesoridazine, thioridazine, and ziprasidone; can
lead to serious cardiac arrhythmias
Dementia. Use is associated with increased risk of CV events and death
Glaucoma, peptic ulcer, urinary or intestinal obstruction. Exacerbated by anticholinergic effects
of antipsychotics
Seizure disorders. Possible severe neurosensitivity can lower seizure threshold in patients with
thyrotoxicosis
Active alcoholism. Antipsychotics can potentiate CNS depression
Immunosuppression, cancer. Caution is applied because antipsychotics can result to bone
marrow suppression and blood dyscrasias
Pregnancy, lactation. Potential adverse effects on the fetus or neonate
Caution is used in children younger than 12 years of age who have chicken pox or a CNS infection
because children are more likely to develop dystonia and this could cause confusion in the
diagnosis of Reye’s syndrome.

Nursing Responsibilities
Do not allow patient to crush or chew sustained-release capsules as this will speed up
absorption and may cause toxicity.
Keep patient in recumbent position for 30 minutes if administering parenteral forms to reduce
risk of orthostatic hypotension.
Monitor CBC results to arrange to discontinue the drug at signs of bone marrow suppression.
Monitor blood glucose levels with long-term use to detect development of glucose intolerance.
Provide comfort measures (e.g. positioning of legs and arms for dyskinesia, sugarless candy and
ice chips for dry mouth, voiding before taking drugs for urinary hesitancy or retention, etc.) to
help patient tolerate drug effects.
Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
Educate client on drug therapy to promote understanding and compliance.

Interactions Withdrawal Symptoms

Anti-anxiety drugs and other CNS depressants Withdrawal from antipsychotics should be
Antidepressants slow and gradual. A period of at least 15–
Hypotensive agents 30 days should be considered for this
Anticholinergic agents purpose. Nausea, vomiting, psychotic
Anticoagulants symptoms, hypertension, and sleep
Levodopa disturbances might come back if sudden
Carbidopa discontinuation of therapy occurs.
Alcohol
Valproic acid
Lithium
Drugs affecting seizure threshold
Smoking

SEIZURE / EPILEPSY
collection of different syndromes, all of which
is characterized by sudden discharge of
excessive electrical energy from nerve cells
located within the brain.
Nature of seizures depends on the location of
the cells that initiate the electrical discharge
as well as the neural pathways which were
stimulated. Seizures can be primary (no
underlying cause) or secondary (brought
about by external factors like head injury)
Too much excitation or too little inhibition
Glutamate - major excitatory
neurotranmistter
 Types of Seizure
Generalized Seizures : These seizures are characterized by a massive electrical activity that begins in
one area of the brain and rapidly spread to both hemispheres. It is usually accompanied by loss of
consciousness. It is further classified into five types:
Tonic-clonic seizure(grand mal) : It involves involuntary muscle contraction (tonic) followed by
relaxation appearing as an aggressive spasm (clonic), loss of consciousness, and confusion and
exhaustion in the early recovery period
Absence seizure (petit mal) : It is an abrupt and brief (3-5 s) period of loss of consciousness
common in children (starting at age 3) but frequently disappears by puberty. This seizure does not
usually involve muscle contractions.
Myoclonic seizure : It is characterized by short, sporadic periods of muscle contractions that last
for several minutes. It is relatively rare.
Febrile seizure : Self-limited seizure related to very high fevers and usually involves tonic-clonic
seizures. This type most frequently occurs in children.
Jacksonian Seizures: Begins in one area of the brain and involve only one part of the body but this
later on spread to other parts until a generalized tonic-clonic seizure has developed.

Partial (Focal) Seizures : These are characterized by seizures that originate from one area of the brain
which do not spread to other parts. It can be further classified into two:
Simple Partial Seizure: It occurs in a single area of the brain and may involve a single muscle
movement or sensory alteration.
Complex Partial Seizure: It is a type which occurs by late teenage years and involves a series of
reactions or emotional changes and complex sensory changes (hallucinations, mental distortion,
personality changes, loss of consciousness, and loss of social inhibition). Motor changes may
include involuntary urination, chewing motions, and diarrhea.

Status epilepticus is a state in which seizures rapidly recur with no recovery between seizures. It is
potentially the most dangerous of seizures.

ANTICONVULSANTS /ANTISEIZURE / ANTIEPILEPTIC

Sedative-Hypnotics
Barbiturates Please refer to “Sedative-hypnotics/Anxiolytics”
Benzodiazepine

Hydantoins
MOA: Stabilize the CNS nerve membranes by decreasing the excitability and hyperexcitability of
ionic channels in the cell membrane to stimulation. Decreasing the conduction through nerve
pathways reduce the tonic-clonic, muscular, and emotional responses to stimulation.
Indication: Control of tonic-clonic and psychomotor seizures, prevention of seizures during
neurosurgery, control of status epilepticus. Less likely to cause sedation which makes them the drug
of choice for patients who are not willing to tolerate sedation and drowsiness. However, this class
have severe adverse effects that benzodiazepines have replaced them in many situations.
CI: Hypersensitivity, Pregnancy & Lactation, Debilitated patients, Impaired hepatorenal function,
Coma, Depression, Psychoses
AE/SE: CNS: depression, confusion, drowsiness, lethargy, fatigue
CV: arrhythmias, changes in blood pressure
GI: constipation, dry mouth, anorexia
GU: urinary retention, loss of libido
Cellular toxicity is characterized by severe liver toxicity, bone marrow suppression, gingival
hyperplasia, and serious dermatological reaction (e.g. hirsutism, Steven-Johnson syndrome).
Interactions: Alcohol: increased risk of CNS depression
Evening primrose: increased risk of seizures
Ginkgo: increased risk of serious adverse effects together with phenytoin
Phenytoin (Dilantin) - also used as an antiarrhythmic due to it’s Na channel blocking activity.

Succinimides
Ethosuximide
MOA: Act in inhibitory neuronal systems and suppress the electroencephalographic pattern
associated with absence seizures. Acts by decreasing positive ion (Ca) influx through the calcium
channel
Indication: Most frequently used to treat absence seizures and reduction of frequency of attacks
CI: Same with those discussed for hydantoins
AE/SE: CNS: depression, drowsiness, fatigue, ataxia, insomnia, headache, blurred vision
GI: decreased GI activity, nausea, vomiting, anorexia, weight loss, GI pain, constipation or
diarrhea
Direct chemical irritation of the skin and bone marrow: bone marrow suppression, fatal
pancytopenia, urticarial, alopecia, Steven-Johnson’s syndrome
Ethosuximide has relatively few adverse effects compared with may antiseizure agents.
Interaction: Primidone = decreased primidone serum levels
 Succinimides cont.
Nursing responsibilities:
Monitor for adverse effects and provide appropriate supportive care as needed to help patient
cope with these effects.
Monitor CBC results to detect bone marrow suppression early and provide prompt intervention.
Discontinue the drug at any sign of hypersensitivity reaction, liver dysfunction, and severe skin
rash to limit reaction and prevent potentially serious reactions.
Provide comfort measures (e.g. positioning of legs and arms for dyskinesia, sugarless candy and
ice chips for dry mouth, voiding before taking drugs for urinary hesitancy or retention, etc.) to
help patient tolerate drug effects.
Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
Educate client on drug therapy to promote understanding and compliance.

Miscellaneous
Carbamazepine - For tonic-clonic, partial, simple, and complex seizures. Used in treating seizures
unresponsive to other anticonvulsants. Now approved to treat bipolar disorder.
Valproic acid - For psychomotor, myoclonic, absence, and tonic-clonic seizures. Also approved for
bipolar disorder and migraine prophylaxis. Avoid during pregnancy.
Acetazolamide - For grand mal, petit mal (absence), and focal seizures. Maintain adequate fluid intake to
prevent renal impairment. Also used as a diuretic and treatment for glaucoma.
Gabapentin - Used as adjunctive therapy for partial seizures. Promotes GABA release. It's also taken for
nerve pain, which can be caused by different conditions, including diabetes and shingles.
Lamotrigine - For partial and tonic-clonic seizures. Also used for treatment of Lennox-Gastaut syndrome
in adults and children. Blocks sodium influx. May be given with other anticonvulsants.
Levetiracetam - For complex partial seizures. For adjunctive and monotherapy.
Topiramate - For partial seizures and generalized tonic-clonic seizures. Inhibits
calcium channels and increases action of GABA.
Magnesium sulfate - To control seizures in toxemia of pregnancy caused by eclampsia or
preeclampsia.
Pregabalin - For partial seizures and neuralgia. It's also taken for nerve pain, which can be caused by
different conditions, including diabetes and postherpetic neuralgia

is mostly a subjective experience of unpleasant sensation and emotional experience.

PAIN People respond to pain differently because of cultural differences, learned experiences,
and environmental stimuli.

A-delta and C-fibers are two sensory nerves that respond to stimulation by generating nerve impulses
that produce pain sensations.

Acute Pain – is caused by tissue injury. It is the type of pain which makes the person aware of the
injury and leads him to seek for care and education about the injury and how to take care for it.
Chronic Pain – is a constant or intermittent pain that keeps occurring long past the time the area
would be expected to heal. This is the type that can interfere with activities of daily living.

Pain Classification According to Source

Nociceptive Pain – caused by direct pain receptor stimulus
Neuropathic Pain – caused by nerve injury
Psychogenic Pain – associated with emotional, psychological, or behavioral stimuli

Analgesics are medications that relieve pain. They work either by

ANALGESICS reducing inflammation or by changing the way the brain processes and
perceives pain. Side effects include heartburn, nausea, and headaches.
Non-narcotics
Indication: used to treat acute or persistent pain that is mild to moderate. They also may be used in
combination with other medications or therapies to treat moderate to severe pain.
available over-the-counter or with prescription
Acetaminophen (Tylenol), NSAIDs, Bupivacaine (Postsurgical analgesia)
Acetaminophen/NSAIDs + Caffeine = Synergistic effect

Acetaminophen
MOA: Antipyretic = Acts directly on the thermoregulatory cells of the hypothalamus
Analgesic = Mechanism of action related to analgesic effects is not certain
AE/SE: Hepatotoxic
Antidote: N-acetylcysteine
Signa: For pain - PRN For Fever - take q4-6h if temp is >37.5 (Max of 4000mg/day)
OPIOID RECEPTORS
Mu-receptors: primarily pain-blocking receptors; also account for respiratory depression,
euphoria, and development of physical dependence.
Beta-receptors: modulate pain transmission by reacting with enkephalins in the periphery
Kappa-receptors: associated with some analgesia, pupillary constriction, sedation, and
dysphoria
Sigma-receptors: pupillary dilation, hallucinations, psychoses with narcotic use
Delta-receptor: Spinal analgesia & modulation of hormone and neurotransmitter release

Opioid agonist used for other properties:

Loperamide & Diphenoxylate - Antidiarrheal
Dextromethorphan - Antitussive

Narcotics / Opioids
Narcotic Agonists – react with opioid receptors in the CNS; cause analgesia, sedation, or
euphoria. They are classified as controlled substances because they have potential for physical
dependence.
Indication: Relief of moderate to severe acute pain or chronic pain; preoperative medication;
component of combination therapy for severe chronic pain; intraspinal to reduce intractable pain.
Narcotic agonists are pregnancy category B except oxycodone (category C) so it might be the drug of
choice if one is needed during pregnancy.
Narcotics used in labor include morphine, meperidine, and oxymorphone
Methylnaltrexone bromide (Relistor) is the treatment for opioid-induced constipation in palliative
care patients who are no longer responding to traditional laxatives.
Other opioid analgesics: Codeine, Hydrocodone, Hydromorphone, Oxycodone, Fentanyl,
Methadone, Tramadol, Heroin
CI: Hypersensitivity, Diarrhea (caused by toxic poisons), Respiratory dysfunction, Recent GI/GU
surgery, Head injuries, alcoholism, delirium tremens, cerebral vascular disease, Liver & Renal
dysfunction, Pregnancy & Lactation
AE/SE: CNS: light-headedness, dizziness, psychoses, anxiety, fear, hallucinations, pupil constriction,
impaired mental processes, GI: nausea, vomiting, constipation, biliary spasm, GU: ureteral spasm,
urinary retention, hesitancy, loss of libido, Others: sweating, physical and psychological dependence,
Narcotic-induced respiratory center depression: respiratory depression with apnea, cardiac arrest,
shock
Interactions: Barbiturates, phenothiazines, MAOIs: increased likelihood of respiratory depression,
hypotension, and sedation or coma , SSRI, MAOI, TCA, St. Johns Wort: increased risk of potentially
life-threatening serotonin syndrome if taken with tapentadol, the newest narcotic agonists that
blocks norepinephrine reuptake in the CNS
Narcotic Agonists-Antagonists – stimulate certain opioid receptors but block other such
receptors. They exert similar analgesic effect with that of morphine but they have less potential
for abuse. However, they are associated with more psychotic like reactions.
Indication: Relief of moderate to severe pain; preanesthetic medication and a supplement to
surgical anesthesia. May be desirable for relieving chronic pain in patients who are
susceptible to narcotic dependence.
Buprenorphine, Butorphanol, Nalbuphine, Pentazocine
Nursing responsibilities:
Perform baseline and periodic pain assessments with patient to monitor drug
effectiveness and provide appropriate changes in pain management protocol as needed.
Have a narcotic antagonist and equipment for assisted ventilation readily available when
administering this drug IV to provide patient support in case of severe reaction.
Monitor timing of analgesic doses. Prompt administration may provide a more acceptable
level of analgesia and lead to a quicker resolution of the pain.
Provide non-pharmacological pain measures like breathing exercises, back rubs, and
stress reduction to increase drug effectiveness and reduce pain.
Provide comfort measures (e.g. small, frequent meals for GI upset) to help patient
tolerate drug effects.
Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
Educate client on drug therapy to promote understanding and compliance.
Narcotic Antagonists – bind strongly to opioid receptors without causing receptor activation.
They block opioid receptor effects as well as effects of too much opioids in the system.
Indication: Indicated for complete or partial reversal of narcotic depression; diagnosis of
suspected opioid overdose.
Naloxone, Naltrexone
Nursing responsibilities:
Maintain open airway and provide artificial ventilation and cardiac massage as needed to
support the patient.
Administer vasopressors as ordered and as needed to manage narcotic overdose.
Administer naloxone challenge before giving naltrexone because of the serious risk of
acute withdrawal
Provide comfort measures to help patient cope with withdrawal syndrome
Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
Ensure that patients receiving naltrexone have been narcotic-free for 7-10 days to
prevent severe withdrawal syndrome
Educate client on drug therapy to promote understanding and compliance.
 MIGRAINE Unilateral throbbing (usually temporal), Nausea, Vomiting, Photophobia
HEADACHE Caused by inflammation and dilation of cranial blood vessels (constriction precedes
the migraine which is the blow out of the vessels)
Preventive treatments(prevent vasoconstriction) for migraine:
Beta blockers: Propranolol (Inderal), Atenolol (Tenormin)
Anticonvulsants: Gabapentin (Neurontin), Topiramate (Topamax), Valproic acid (Depakote)
Tricyclic antidepressants : Amitriptyline (Elavil), Imipramine (Tofranil)
Treatment for cessation
Analgesics (for migraine and cluster) Selective Serotonin Receptor Agonists
1. Opioid Triptans -Sumatriptan, Naratriptan, Zolmitriptan
2. NSAIDS Inhibits vasodilation of cerebral blood vessels
3. Combinations (hydrocodone with ibuprofen) Inhibits inflammation of meninges
AE/SE: Hypertension, Paresthesia, hot or cold
Ergot Alkaloids (for migraine) sensation, malaise/fatigue, chest pain, dizziness,
Ergotamine tartrate (Ergostat) flushing
Action: Vasoconstricts

General & Local are a diverse group of drugs that are used in the management of pain;
Anesthetic are drugs used to cause complete or partial loss of sensation

Anesthesia
Classification:
1. General anesthetics – depress the CNS, alleviate pain & cause loss of consciousness
2. Local – block pain at the site where the drug is administered

Stages & Depth of Anesthesia:

Stage 1: Analgesia - patient has decreased awareness of pain sometimes with amnesia;
consciousness may be impaired but not lost
Stage 2: Excitatory - Patient is delirious and excited; Amnesia occurs, reflexes are enhanced, and
respiration is typically irregular; retching and incontinence may occur
Stage 3: Surgical - Patient is unconscious and has no pain reflexes; respiration is very regular, and
BP is maintained
Stage 4: Medullary Depression - Patient develops severe respiratory and CVS depression that
requires mechanical and pharmacologic support

Anesthesia Protocols:
Induction - the time from administration of a potent anesthetic to development of effective anesthesia
Maintenance - provides sustained anesthesia
Recovery - time from discontinuation of anesthetic until consciousness and protective reflexes return

For minor procedures:

• Conscious sedation techniques (IV agents with local anesthetics)

For more extensive surgical procedures:

• IV drugs to induce the anesthetic state, inhaled anesthetics (with or without IV agents) to maintain
an anesthetic state, and neuromuscular blocking agents to effect muscle relaxation

Assessment of depth of anesthesia during surgery:

• Vital sign monitoring
• Cerebral monitoring (EEG)

General Anesthetic
MOA:
Increase inhibitory (GABA) synaptic activity
Inhaled anesthetics, Barbiturates, BZDs, Etomidate, and Propofol
Decrease excitatory (glutamate or ACh) synaptic activity
Inhaled anesthetics (Nicotinic receptor antagonists)
Ketamine (NMDA receptor antagonist)

Inhaled Anesthetics
Nitrous Oxide, Desflurane, Sevoflurane, Isoflurane, Enflurane, Halothane, Methoxyflurane

Intravenous Anesthetics
Propofol, Fospropofol, Barbiturates, Benzodiazepines, Etomidate, Ketamine, Opioid analgesics

Local Anesthetic
MOA: blockade of voltage-gated sodium channels

Cocaine, Procaine, Lidocaine, Bupivacaine, Prilocaine

 Affective Disorders vs Depression
Affective disorder : A person’s mood goes far beyond the normal “ups and downs”
Depression : Severe and long-lasting feelings of sadness beyond the precipitating event
BIOGENIC AMINE THEORY OF DEPRESSION
Depression results from deficiency of monoamine; norepinephrine (NE), dopamine, or serotonin (5HT)
Monoamine oxidase (MAO) may break them down to be recycled or restored in the neuron
Rapid fire of neurons may lead to their depletion
The number or sensitivity of postsynaptic receptors may increase, depleting neurotransmitter levels
Signs and Symptoms of Depression
Low energy level
Sleep disturbances
Lack of appetite
Limited libido
Inability to perform activities of daily living
Overwhelming feelings of sadness, despair,
hopelessness, and disorganization

Antidepressants

Tricyclic Antidepressants (TCAs)

MOA: Reduce the reuptake of 5HT and NE into nerves
Indication: Relief of symptoms of depression, used for
patients with sleep disorders, treatment of enuresis,
chronic pain. All TCAs are similar, Choice depends on
individual response to the drug and tolerance of adverse
effects.
CI: Hypersensitivity, recent MI, myelography, pregnancy, and lactation. CV disease, angle closure
glaucoma, urinary retention, and manic depression.
AE/SE: Sedation, sleep disturbances, fatigue, hallucinations, ataxia, dry mouth, constipation, nausea,
and vomiting
Interactions: MAOIs, cimetidine, fluoxetine, ranitidine, and oral anticoagulants

Amitriptyline, Nortriptyline , Imipramine Desipramine, Doxepin, Clomipramine

Monoamine Oxidase Inhibitors (MAOIs)

MOA: Irreversibly inhibit MAOs, allowing norepinephrine, serotonin, and dopamine to accumulate
in the synaptic cleft
Indication: Treatment of patients with depression who are unresponsive to or unable to take other
antidepression agents
Pharmacokinetics: Cross placenta and enter breast milk
CI: Hypersensitivity, pheochromocytoma, CV disease, headaches, and renal or hepatic impairment
AE/SE: Dizziness, excitement, nervousness, mania, hyperreflexia, tremors, confusion, insomnia,
agitation, liver toxicity, nausea, vomiting, diarrhea or constipation, anorexia, weight gain, dry
mouth, and abdominal pain
Drug Interactions:
Other antidepressants: hypertensive crisis and coma
Methyldopa: sympathomimetic effects increase
Insulin or oral antidiabetic agents: additive hypoglycemia
Food Interaction: Tyramine rich foods (cheese, wine, beer, chicken, liver, banana) → will cause
hypertensive crisis

Isocarboxazid (Marplan) : Used for patients who do not respond to or cannot take newer, safer
antidepressants
Phenelzine (Nardil) : Used for some patients who do not respond to newer, safer antidepressants
Tranylcypromine (Parnate) : Used for adult outpatients with reactive depression

Selective Serotonin Reuptake Inhibitors (SSRIs)

The newest group of antidepressant drugs. Do not have the many adverse effects associated with
TCAs and MAOIs but is associated with congenital abnormalities.
MOA: Specifically block the reuptake of 5HT, with little to no known effect on NE
Indication: Depression, OCD, panic attacks, bulimia, PMDD, posttraumatic stress disorders, social
phobias, and social anxiety disorders
AE/SE: Headache, drowsiness, dizziness, insomnia, anxiety, tremor, and agitation
Interaction: MAOIs, TCAs increase therapeutic and toxic effect (Serotonin Syndrome)
Fluoxetine, Paroxetine, Citalopram, Sertraline
 Serotonin Norepinephrine Reuptake Inhibitors (SnRIs)
Venlafaxine, Desvenlafaxine, Duloxetine, Milnacipran
MOA: Inhibit the reuptake of monoamines, serotonin and norepinephrine.
Indication: Major depression, neuropathies, and fibromyalgia. Also used in the treatment of
generalized anxiety, stress urinary incontinence, and vasomotor symptoms of menopause.

Miscellaneous
Bupropion (Wellbutrin, Zyban), Mirtazapine (Remeron), Nefazodone (Serzone),
Trazodone (Desyrel), Venlafaxine (Effexor)

Mood Disorders
Mental health problem that mainly affects the person’s emotional state
It is a disorder characterized by long period of extreme happiness, extreme
loneliness, or both
Mood regulation: 5-HT, Dopamine, NE

Mixed Disorders:
• Bipolar disorder: Mania and Major depression
• Cyclothymia: Dysthymia and Hypomania

Bipolar Disorder
• Formerly known as manic-depressive illness or manic depression
• A mental disorder that causes unusual shifts in mood

Mood Stabilizers

Lithium
Trade name : Eskalith, Lithane, Lithonate, Lithobid
MOA:
Alteration of ion transport in muscle and nerve cells; increase receptor sensitivity to serotonin.
Alters sodium transport in nerve and muscle cells
Inhibits the release of norepinephrine and dopamine—but not serotonin—from stimulated
neurons
Increases the intraneuronal stores of norepinephrine and dopamine slightly
Decreases intraneuronal content of second messengers
Indication: treat bipolar manic depressive psychosis
CI: Liver and renal disease, pregnancy, lactation, severe cardiovascular disease, severe
dehydration, brain tumor or damage , sodium depletion, children 12 years old and below.
AE/SE: headache, lethargy, drowsiness, dizziness, tremors, slurred speech, dry mouth, anorexia,
vomiting diarrhea, polyuria, hypotension abdominal pain, muscle weakness and restlessness.
Urinary incontinence, clonic movements, stupor, azotemia, leukocytosis, nephrotoxicity
cardiac dysrhythmias, circulatory collapse

Nursing Responsibilities
Observe for signs and symptoms of depression: mood changes, insomnia, apathy, or lack of
interest in activities
Monitor vital signs : orthostatic hypotension is common
Monitor for suicidal tendencies when marked depression Is present.
Evaluate client’s urine output and body weight. Fluid volume deficit may occur as a result of
polyuria.
Observe client for fine and gross motor tremors and presence of slurred speech which are signs
of adverse reaction
Check client’s cardiac status. Loss of fluids and electrolytes may cause cardiac dysrhythmias
Monitor for signs of lithium toxicity.

Miscellaneous
Drugs that increase the serum concentration of Lithium - Thiazide Diuretics, ACE Inhibitors, NSAIDs
Valproic Acid - for mania
Carbamazepine, Lamotrigine - used as prophylaxis and treatment of mania
Antipsychotics - for acute mania
 Parkinson’s Disease
Parkinson’s Disease is a chronic, progressive neurological disorder with rhythmic tremors as its initial
manifestation. These tremors lead to rigidity and weakness which interfere with the ability to maintain
posture.
Other manifestations include bradykinesia (extremely slowed movements), shuffling gait, drooling, and
slow and slurred speech. Cranial nerve affectations lead to a mask-like expression.
It is important to note that Parkinson’s does not affect the higher levels of cerebral cortex so
intelligence and other brain functions at the same level are intact.
The actual cause of Parkinson’s is not known but the manifestations are directly related to the damaged
neurons in the basal ganglia of the brain. Neuronal damage is thought to be caused by viral infections,
head trauma, brain infections, atherosclerosis, and drug and environmental exposures.
Parkinsonism is referred to as the Parkinson’s disease-like extrapyramidal symptoms which are
associated to particular drugs or brain injuries’ adverse effects.

used for management of signs and symptoms of

Antiparkinsonism Agents Parkinson’s disease, a progressive, chronic neurological
disorder primarily characterized by lack of coordination.

There is no known treatment for Parkinson’s as of present and drug therapy remains to be the
primary treatment.
The goal of the therapy is to restore the balance between decreasing dopamine levels (has
inhibitory effect on the neurons of the basal ganglia) and increasing acetylcholine (excitatory).

Dopaminergic Agents
Drugs that increase the effects of dopamine at receptor sites.
Therapeutic Action
Dopamine does not cross the blood-brain barrier so other drugs with actions similar to
dopamine and those that increase its concentration in the substantia nigra (area responsible
for muscle tone) must be used. This is one way of restoring the balance between stimulatory
and inhibitory neurotransmitters.
Levodopa, the precursor of dopamine is the mainstay of treatment for Parkinson’s. It crosses
the blood-brain barrier and is converted into dopamine. When combined with carbidopa, the
enzyme dopa-decarboxylase is inhibited from metabolizing levodopa, leading to higher levels
that can cross the barrier.
Indications
Dopaminergic are indicated for the relief of the signs and symptoms of idiopathic Parkinson’s
disease.
Levodopa is the drug of choice and acts as a replacement therapy.
Amantadine is an antiviral drug that increases release of dopamine.
Apomorphine directly binds with postsynaptic dopamine receptors.
CI:
Hypersensitivity, Angle-closure glaucoma, Lactation, Pregnancy, Suspicious skin lesions.
CV disease, bronchial asthma, psychiatric disorders
Hepatorenal diseases
Apomorphine can increase risk of hypotension and prolonged QT interval.
Levodopa is associated with development of melanoma
AE/SE:
CNS: anxiety, nervousness, headache, malaise, fatigue, confusion, mental changes, blurred
vision, muscle twitching, and ataxia
CV: arrhythmias, hypotension, palpitation
Respiratory: bizarre breathing patterns
GI: anorexia, nausea, vomiting, dysphagia, constipation or diarrhea
GU: urinary retention
Others: flushing, increased sweating, hot flashes
 Dopaminergic Agents cont.
Interactions:
MAOI: Increased therapeutic effects and risk of hypertensive crisis. MAOI should be stopped 14
days before beginning dopaminergic therapy.
Vitamin B6, phenytoin: decreased levodopa efficacy
Over-the-counter vitamins: decreased dopaminergic effectiveness
Nursing Responsibilities:
Decrease dose of drug as ordered if therapy has been interrupted to prevent systemic
dopaminergic effects.
Evaluate disease progress and signs and symptoms periodically for reference of disease
progress and drug response.
Give drug with meals to alleviate GI irritation if present.
Monitor bowel function and institute bowel program if constipation is severe.
Have patient void before taking the drugs to decrease risk of urinary retention.
Monitor laboratory test results (renal and liver function, CBC) to detect early signs of
dysfunction.
Provide comfort measures to help patient tolerate drug effects.
Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
Educate client on drug therapy to promote understanding and compliance.

Anticholinergics
are synthetic drugs which have been developed to achieve a greater affinity for cholinergic
receptor sites in the CNS. Drugs that inhibit the effects of acetylcholine at receptor sites of
substantia nigra and corpus striatum.
Therapeutic Action:
Returns the balance to the basal ganglia and reduces the severity of rigidity, akinesia, and tremors.
Peripheral anticholinergics reduce drooling and other secondary effects of parkinsonism.
Indications:
Adjunctive therapy for Parkinson’s disease (idiopathic, atherosclerotic, and postencephalitic)
Indicated for patients who no longer respond to levodopa.
Contraindications and Cautions:
Hypersensitivity, Angle-closure glaucoma, GI and GU obstruction, prostatic hypertrophy,
Myasthenia gravis
Tachycardia, dysrhythmia, hyper or hypotension. Blocking the parasympathetic system may
cause a dominance of sympathetic stimulatory activity
Hepatic dysfunction, Lactation & Pregnancy
AE/SE:
CNS: disorientation, confusion, memory loss, agitation, nervousness, delirium, dizziness, light-
headedness, weakness
CV: tachycardia, palpitations, hypotension
EENT: blurred vision, photophobia, pupil dilation, blocking of lens accommodation
GI: dry mouth, nausea, vomiting, paralytic ileus, constipation
GU: urinary retention and hesitancy Others: flushing, reduced sweating Interactions
TCAs, phenothiazines: increased risk of potentially fatal paralytic ileus and toxic psychoses
Antipsychotics: decreased antipsychotic therapeutic effectiveness because of central
antagonism of two agents
Nursing Responsibilities:
Administer drug with caution for patients exposed in hot weather or environments because
patients are at increased risk for heat prostration due to decreased ability to sweat.
Give drug with meals to alleviate GI irritation if present.
Monitor bowel function and institute bowel program if constipation is severe.
Have patient void before taking the drugs to decrease risk of urinary retention.
Monitor laboratory test results (renal and liver function) to detect early signs of dysfunction.
Provide comfort measures to help patient tolerate drug effects.
Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
Educate client on drug therapy to promote understanding and compliance.
Evaluate disease progress and signs and symptoms periodically for reference of disease
progress and drug response.
Benztropine & Trihexyphenidyl

MYASTHENIA GRAVIS
Characterized by weakness and rapid fatigue of
any of the muscles under your voluntary control.
The cause of myasthenia gravis is a breakdown in
the normal communication between nerves and
muscles.
There is no cure for myasthenia gravis, but
treatment can help relieve signs and symptoms
such as weakness of arm or leg muscles, double
vision, drooping eyelids, and difficulties with
speech, chewing, swallowing and breathing.
MYASTHENIA GRAVIS MANAGEMENT
Nursing management:
Provide rest in-between nursing care interventions.
Admin. Meds on time and evenly spaced intervals to prevent relapse.
Make the most of energy peaks.
Plan diet and food intake around ability to swallow.
Stress need for frequent rest periods.
Establish resp. and neuro. Baseline.
Medical Management:
Pyridostigmine (Mestinon) : Orally active cholinesterase inhibitor. Increases the amount of
acetylcholine at the neuromuscular junction. Enhances Communication between nerves and
muscles.
Corticosteroids- these inhibit the immune system
Immunosuppressants- to alter immune system. ( these can increase risk for infection)
cyclosporine/mycophenolate
Atropine: for bradycardia. This med will pick up the heart rate.
Edrophonium (Tensilon): The tensilon test is an injection used to diagnose MG. Prolongs the
muscle stimulation and temporarily improves strengths, increased strength following an
injection of tensilon suggests a diagnosis of MG.

MUSCLE SPASM
Spasms of skeletal muscles are most common and are often due to overuse and muscle fatigue,
dehydration, and electrolyte abnormalities. The spasm occurs abruptly, is painful, and is usually short-
lived. It may be relieved by gently stretching the muscle.
Muscle spasm is a disturbance to the normal flow of information in the CNS caused by diseases,
infections, toxins, and injuries can lead to disturbances ranging from spasms to paralysis. Results from
violent and painful involuntary muscle contraction usually caused by muscle overstretching, joint
wrenching, and tendon or ligament tearing. When this happens, the injured area floods sensory impulses
to the spinal cord and it responds by eliciting intense muscle contraction. Pain from muscle spasms is
due to lactic acid accumulation that occurs when blood flow is cut off during contractions. Sensory
impulses continue to flood and a vicious cycle of contraction develops.
Muscle spasticity occurs when damaged neurons are within the CNS rather than the peripheral areas.
The site of damage makes this abnormality permanent. There is an interruption in the balance of
excitatory and inhibitory influences within the CNS which can lead to hypertonia (excessive muscle
stimulation) and consequent contractures and structural changes. There is now loss of coordinated
muscle activity.
Diseases associated with muscle spasm: Multiple sclerosis & Cerebral Palsy
Ex
cit
at
or
yI
nt
ern

Tizanidine
eu
ron

Alpha-2

Diazepam

Baclofen

CENTRALLY-ACTING MUSCLE RELAXANTS

MUSCLE RELAXANTS PERIPHERALLY-ACTING MUSCLE RELAXANTS

Centrally-Acting Muscle Relaxants / Spasmolytics

Baclofen, Diazepam, Tizanidine, Carisoprodol, Chlorzoxazone
work in the CNS to interfere with reflexes that cause muscle spasms. They essentially destroy
or lyse spasms. Other modalities of spasm and pain relief like rest, heat application, and
physical therapy are used in addition to these drugs.
MOA: The exact mechanism of action of skeletal muscle relaxants is not fully understood but it
is thought that it involves the participation of upper or spinal interneurons. It inhibits
monosynaptic and polysynaptic spinal reflexes. Other than that, it is a CNS depressant.
Indication: Primary indication is relief of discomfort associated with acute, painful
musculoskeletal conditions as adjunct to rest, physical therapy, and other measures.
Alleviation of signs and symptoms of spasticity, may be of use in spinal cord injuries or spinal
cord diseases.
CI: Hypersensitivity, skeletal muscle spasms caused by rheumatic disorders, history of epilepsy,
cardiac dysfunction, condition marked by muscle weakness, hepatic & renal dysfunction.
Baclofen is not indicated for treatment of spasticity that contributes to locomotion, upright
function, or increased function. Blocking this spasticity results in loss of these functions.
CAMR / Spasmolytics cont.
AE/SE:
CNS: depression, drowsiness, fatigue, weakness, confusion, headache, insomnia.
CV: hypotension, arrhythmias o GI: nausea, dry mouth, anorexia, constipation.
GU: urinary frequency, enuresis, urinary urgency
Chlorzoxazone may turn urine into purple-red color.
Tizanidine has been associated with liver toxicity and hypotension in some patients.
Baclofen is tapered over 1-2 weeks to prevent development of psychoses and
hallucinations.
Interaction: Other CNS depressants, alcohol --> increased CNS depression
Nursing Responsibilities:
Provide additional spasm and pain relief like rest periods, heat application, NSAIDs as
ordered, and positioning to augment the effects of the drug at relieving the musculoskeletal
discomfort.
Discontinue drug at any sign of liver and renal dysfunction to prevent severe toxicity.
Monitor respiratory status to evaluate adverse effects and arrange for appropriate dose
adjustment or discontinuation of the drug.
Provide comfort measures to help patient tolerate drug effects.
Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
Educate client on drug therapy to promote understanding and compliance.

Peripherally-Acting Muscle Relaxants

Directly-Acting on Skeletal Muscle
Dantrolene
enter the muscle to prevent muscle contraction directly
MOA: Dantrolene acts within skeletal muscle fibers and interfere with calcium ion release from
the muscle tubules. Therefore, the fibers are prevented from contracting. It does not interfere
with neuromuscular transmission and does not affect skeletal muscle surface membrane.
Indications:
Children
Safety and effectiveness not established in children.
Dantrolene is used to treat upper motor neuron spasticity in children.
Dose should be accurately calculated based on body weight and it increases over time.
Children are at increased risk of CNS and GI toxicity.
Adult
They should be cautioned to avoid activities that require alertness (e.g. driving) because
drugs can cause confusion and drowsiness.
Pregnant and lactating women should be advised to use contraception and alternative
method of feeding, respectively.
Premenopausal women are at increased risk for hepatotoxicity in association with use of
dantrolene.
Older adults
They are more likely to experience adverse effects associated with these drugs.
Older women who are receiving hormone replacement therapy have the same risk for
hepatotoxicity with premenopausal women in association with use of dantrolene.
CI: Hypersensitivity, spasticity that contributes to locomotion, upright position, increased
function. Active hepatic disease, pregnancy & lactation.
Women and patients older than age 35. Caution is applied because of increased risk of
potentially fatal hepatocellular disease
Respiratory depression & cardiac disease
AE/SE: CNS: drowsiness, fatigue, weakness, confusion, headache, insomnia, visual disturbances
GI: GI irritation, diarrhea, constipation, abdominal cramps
GU: urinary frequency, enuresis, urinary urgency , crystalline urine with pain or burning on
urination
Others: acne, abnormal hair growth, rashes, photosensitivity, abnormal sweating, chills,
myalgia
Dantrolene can cause direct hepatocellular damage and potentially fatal hepatitis
Interaction: Estrogens: increased incidence of hepatocellular toxicity if used with dantrolene
Neuromuscular junction blockers, lincosamides, quinidine, magnesium sulfate,
anticholinesterase, succinylcholine, polymyxin, aminoglycosides --> additive effects
Nursing Responsibilities:
Monitor intravenous access sites of dantrolene for potential extravasation because drug is
alkaline and very irritating to tissues.
Periodically discontinue dantrolene for 2-4 days as ordered to monitor therapeutic
effectiveness.
Discontinue drug at any sign of liver dysfunction to prevent adverse effects.
Provide comfort measures to help patient tolerate drug effects.
Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
Educate client on drug therapy to promote understanding and compliance.

Drugs Acting at the Neuromuscular Junction

Botulinum toxins/Botox are associated with anaphylactic reactions characterized by headache,
dizziness, muscle pain, paralysis. Assess area before administering botulinum toxins because
area with active infection will be exacerbated by injection.
Other drugs: Succinylcholine, Atracurium, Tubocurarine, Pancuronium, Rocuronium
 ALZHEIMER’S DISEASE

Alzheimer’s disease (AD) is a progressive and irreversible,

degenerative, fatal disease and is the most common form of
dementia among older people.

Dementia is a brain disorder that seriously affects a person’s

ability to carry out daily activities. It usually begins after age 60
and the risk goes up as you get older. Risk is also higher if a family
member has the disease.

Clinical Manifestations:
Memory impairment. Impaired ability to learn new information or to recall previously learned
information.
Impairment in abstract thinking, judgment, and impulse control.
Impairment in language ability, such as difficulty naming objects. In some instances, the individual may
not speak at all (aphasia).
Personality changes are common.
Impaired ability to perform motor activities despite intact motor abilities (apraxia).
Disorientation. Patient may feel disoriented regarding current place, time, o names of persons they are
close with.
Wandering. Because of disorientation, patient with dementia may often wander from one place to
another.
Delusions are common (particularly delusions of persecution).

ALZHEIMER’S DRUG THERAPY

Orient client. Frequently orient client to reality and surroundings. Allow client to have familiar objects
around him or her; use other items, such as a clock, a calendar, and daily schedules, to assist in
maintaining reality orientation.
Encourage caregivers about patient reorientation. Teach prospective caregivers how to orient client to
time, person, place, and circumstances, as required. These caregivers will be responsible for client
safety after discharge from the hospital.
Enforce with positive feedback. Give positive feedback when thinking and behavior are appropriate, or
when client verbalizes that certain ideas expressed are not based in reality. Positive feedback increases
self-esteem and enhances desire to repeat appropriate behavior.
Explain simply. Use simple explanations and face-to-face interaction when communicating with client.
Do not shout message into client’s ear. Speaking slowly and in a face-to-face position is most effective
when communicating with an elderly individual experiencing a hearing loss.
Discourage suspiciousness of others. Express reasonable doubt if client relays suspicious beliefs in
response to delusional thinking. Discuss with the client the potential personal negative effects of
continued suspiciousness of others.
Avoid cultivation of false ideas. Do not permit rumination of false ideas. When this begins, talk to client
about real people and real events.
Observe client closely. Close observation of client’s behavior is indicated if delusional thinking reveals
an intention for violence. Client safety is a nursing priority.