NEUROLOGIC AND
NEUROMUSCULAR
AGENTS
Prof. Felma G. Garcia
Our Lady of Guadalupe Colleges
College of Nursing
CNS STIMULANTS AND
DEPRESSANTS
An Overview
Let us try to compare the effects of drinking
coffee and any alcoholic beverage….
CNS Medications
Stimulants (Uppers)
Speeds up the CNS
Feeling of extreme energy
Depressants (Downers)
Slows down the function of the CNS
Feeling of relaxation
CNS STIMULANTS
CNS Stimulants
Key Action: Stimulate the function of the CNS
• Increases the heart rate, blood pressure and Amphetamines
brain function
Anorexiants
Major Indications: Lipase Inhibitors
• Attention deficit hyperactivity disorder (ADHD)
Analeptics
• Narcolepsy
• Reversal of respiratory distress Respiratory stimulants
Attention deficit/hyperactivity disorder
(ADHD)
Cause
• dysregulation of serotonin, norepinephrine and dopamine
Incidence
• children before age 7 and may extend up to adolescence; more common in boys
Manifestations
• Inattentiveness, inability of concentrate, restlessness (fidgety), hyperactivity
(excessive and purposeless activity), inability to complete tasks, impulsivity, poor
coordination and learning disability
Narcolepsy
• Excessive drowsiness
• Falling asleep during normal
waking activities
• Sleep paralysis
Amphetamines
Drug Names
• Amphetamine (Adderall) ,
• Dextroamphetamine (Dexedrine),
• Metamphetamine (Desoxyn)
Action
• stimulate release of neurotransmitters –
norepinephrine and dopamine – from the brain and
sympathetic nervous system
• Stimulates the cerebral cortex of the brain
Indications
• ADHD
• Narcolepsy
Amphetamines
Drug effects Side effects / Adverse reactions
• euphoria • restlessness
• Alertness • insomnia
• tachycardia
• hypertension
Causes adverse effects on the CNS, • heart palpitations
cardiovascular, gastrointestinal and • dry mouth
endocrine system • anorexia
• weight loss
• diarrhea
• constipation
• impotence
Amphetamine-Like Drugs
• Methylphenidate (Ritalin) and Dexmethylphenidate (Focalin)
• Increases attention span and cognitive performance (reading, memory) and
decreases impulsiveness, hyperactivity and restlessness to a child ADHD
• Treats narcolepsy - modafinil (Provigil)
Methylphenidate (Ritalin)
Therapeutic Effects
• To correct hyperactivity caused by ADHD, increase attention
span, and control narcolepsy
Mode of action
• Modulation of serotogenic pathways by affecting changes in
dopamine transport
Side effects
• anorexia, vomiting, diarrhea, insomnia, dizziness,
nervousness, restlessness, irritability, tremors, euphoria,
blurred vision, headache, increased hyperactivity,
abdominal pain, anemia, upper respiratory infection
Methylphenidate (Ritalin)
Adverse Reactions
• Tachycardia, hypertension, growth suppression, palpitations, seizures, transient weight loss
in children
• Life-threatening: exfoliative dermatitis, stroke, thrombocytopenia, hepatotoxicity
Contraindications
• Hyperthyroidism, anxiety, history of seizures, coronary artery disease, hypertension,
Tourette’s syndrome, glaucoma, psychosis and mental depression
Nursing Considerations
• Determine history of heart disease, hypertension,
hyperthyroidism, parkinsonism, or glaucoma.
• Assess mental status (mood, affect and aggressiveness).
• Monitor vital signs.
• Evaluate height, weight and growth of children. Monitor
weight twice a week and report weight loss.
• Assess CBC before and during therapy.
• Teach patient to take drug 30 to 45 minutes before meals.
• Administer 6 hours or more before sleep because it may
cause insomnia.
Nursing Considerations
• Encourage use of sugarless gum to relieve dry mouth.
• Advise patient to avoid driving and using hazardous
equipment when experiencing tremors, nervousness or
increased heart rate.
• Teach patient not to abruptly discontinue the drug; dose
must be tapered off to avoid withdrawal symptoms.
• Observe patient for withdrawal symptoms such as nausea,
vomiting, weakness, and headache.
• Teach patient to avoid foods that contain caffeine and
alcohol.
Anorexiants
Appetite suppressants
Drug Name diethylpropion HCl (Tenuate)
Indication for short-term appetite suppression to cause weight loss
stimulates the satiety center in the hypothalamic and limbic
Action areas of the brain
long-term use can lead to nervousness, restlessness,
Side-effects irritability, insomnia, heart palpitations and hypertension.
Lipase Inhibitors
• Replaces anorexiants as the drug of choice for weight loss
• Action
• decrease GI absorption of dietary fats; excrete fats in feces leading to weight loss
• Side-effects
• Oily spotting, fecal urgency and incontinence, steatorrhea, flatus with discharge,
headache, nausea, vomiting, and abdominal cramping
• Hypoglycemia may occur in diabetic patients.
Analeptics
Action
• Acts on the brainstem and medulla to stimulate respiration
Indications
• newborn with respiratory distress
xanthines (methylxanthines)
• caffeine citrate (Cafcit); theophylline
Side-effects and adverse reactions
• Nervousness, restlessness, tremors, twitching, palpitations and insomnias
• Diuresis, GI irritation (nausea, diarrhea), and tinnitus
Respiratory Stimulants
Drug name: Doxapram (Dopram)
Indication
• used to treat respiratory depression caused by drug overdose, preanesthetic and
postanesthetic respiratory depression and chronic obstructive pulmonary disease
(COPD)
Side-effects
• hypertension, tachycardia, tremors, spasticity and hyperactive reflexes
CNS DEPRESSANTS
CNS Depressants
• Key Action: cause varying degrees of
depression or reduction in functional
Sedative-hypnotics
activity within the CNS
General anesthetics
Opioid and nonopioid analgesics
Anticonvulsant
Antipsychotics
Antidepressants
SEDATIVE-HYPNOTICS
Insomnia
Nonpharmacologic Interventions
• Inability to fall or • Arise at a specific hour in the morning
remain asleep
• Take a few or no daytime naps
• Most common sleep
• Avoid smoking and food that contain caffeine and
disorder occurs more
alcohol 6 hours before bedtime.
frequently in women
and increases with • avoid heavy meals or strenuous exercise before bedtime.
age
• Take a warm bath, listen to quiet music, or perform other
• Medical Management: soothing activities before bed.
Sedative-Hypnotics
• Drink warm milk before bedtime.
Sedative-Hypnotics
Sedative – diminishes physical and mental responses at lower dosages but does not
affect consciousness.
Hypnotic – produces “natural” sleep
• Often used to produce hypnotic effect but with very high dose can produce anesthesia
Indications
• Temporary treatment of insomnia, decrease anxiety and increase relaxation and/or sleep
before diagnostic or surgical procedures
Side-effects and Adverse Reactions
• Hangover, REM rebound, dependence, tolerance, excessive depression, respiratory
depression and hypersensitivity
Sedative-Hypnotics
• Usually for short-term use to prevent drug dependence
and drug tolerance.
• Dose should be tapered down to avoid withdrawal
symptoms.
• Lowest dose should be taken to obtain sleep.
• Contraindicated to pregnant patient and those with
respiratory disorders because the drug causes respiratory
depression.
• Ramelteon (Roserem) is the only major sedative-
hypnotic approved for long-term use for the treatment of
chronic insomnia.
Classification of Sedative-Hypnotics
Barbiturates
Benzodiazepines
Nonbenzodiazepines
Miscellaneous agents
Barbiturates
Actions Nursing Considerations
• Reversibly depress excitable tissues,
suppress REM and stage III/IV sleep when • Perform baseline assessment of vital
used for hypnosis signs (most especially respiration),
• Degree of depression can range from
degree of alertness, state of arousal and
mild sedation to coma and death motor function
• Do not combine with alcohol, narcotics
Side-effects and other sedative-hypnotics because it
• Hangover, blurred vision, transient may further depress the CNS.
hypotension on arising, sedation,
decreased alertness and lethargy
Adverse effects
• Excessive use or abuse, paradoxical
response, hypersensitivity (hives, rash,
pruritus) and blood dyscrasias
Barbiturates
Long-acting phenobarbital and mephobarbital
Used to control seizures in epilepsy
Intermediate- Butabarbital (Butisol)
acting Useful as sleep sustainers for maintaining long periods of sleep
Short-acting Secobarbital (Seconal) and pentobarbital (Nembutal)
Used primarily for sedation preoperatively
Ultrashort- Thiopental sodium (Pentothal)
acting Used as general anesthetic
Pentobarbital
• Used for sedation, sleep or preanesthesia
• Increases hepatic enzyme action causing an
increased metabolism and decreased effect of
drugs such as oral anticoagulants,
glucocorticoids, tricyclic antidepressants
and quinidine.
• May cause hepatotoxicity if taken with large
doses of acetaminophen
SAFETY!!! Preventing Medication Error
Do not confuse phenobarbital (a long acting barbiturate used to control seizures)
with pentobarbital (an ultrashort-acting barbiturate used as a general anesthetic)
Benzodiazepines
• Used primarily as hypnotics and to alleviate anxiety
Drug Names
Action Alprazolam (Xanax)
• Increase the action of the inhibitory neurotransmitter Flurazepam (Dalmane)
gamma-aminobutyric acid (GABA) to the GABA receptors Temazepam (Restoril)
thereby reducing excitability of neuron. Triazolam (Halcion)
Side-effects Estazolam (ProSom)
• Drowsiness, hangover, blurred vision, sedation, lethargy, Quazepam (Doral)
decreased level of alertness Lorazepam (Ativan)
Diazepam (Valium)
Adverse Effects
• Confusion, agitation, amnesia and hepatotoxicity
Benzodiazepines
Nursing Considerations
• Obtain drug history of current drugs and herbs patient is taking, especially CNS depressants,
which would potentiate respiratory depression and hypotensive effects.
• Assess vital signs especially respiration and blood pressure.
• Assess renal function. Renal impairment could prolong drug action.
• Use bed alarm for older adults and patients receiving a hypnotic for the first time. Confusion
may occur and injury may result.
• Examine patient’s skin for rashes.
• Encourage patient to avoid alcohol and antidepressant, antipsychotic and opioid drugs while
taking benzodiazepines which can further increase the risk for respiratory depression.
Benzodiazepines
Nursing Considerations
• Warn patient that certain herbs (kava-kava and valerians) may interact with
benzodiazepines. Herbal supplement may need to be discontinued.
• Advise patient not to drive a motor vehicle or operate a machinery.
• Advise patient to report adverse reactions such as cognitive changes and
paradoxical reactions.
• Teach patient that benzodiazepines should be gradually withdrawn. Withdrawal
symptoms such as tremors and muscle twitching occur if discontinued abruptly.
• For benzodiazepine overdose, the antagonist flumazenil (Romazicon) can be given.
Alprazolam (Xanax)
Action
• CNS depression, binds receptors in limbic
system and reticular formation, increases
GABA to GABA receptors, shift of Side effects
chloride ions leads to less excitability and • lethargy, drowsiness, dizziness,
stabilizes neuronal membranes. headache, constipation, memory
impairment, increased appetite, blurred
Indication vision, decreased libido, paradoxical
• Anxiety and panic disorder reactions
Contraindications
• Respiratory depression, acute alcohol Adverse Reactions
intoxication, psychotic reactions, recent
• Depression, impaired coordination
respiratory depressants, hypersensitivity
Nonbenzodiazepines
Prototype: zolpidem (Ambien)
• Used for short-term treatment (less than 10 days) of insomnia
Contraindications
• Hypersensitivity to benzodiazepines, respiratory depression, lactation
Side-effects
• Drowsiness, lethargy, headache, hot flashes, hangover, irritability, dizziness, ataxia,
visual disturbances, anxiety, mental depression, nausea and vomiting, erectile
dysfunction
Adverse reactions
• Tolerance, psychological or physical dependence, sleep-related behavior, hypotension,
angioedema dysrhythmias, suicidal ideation
Nonbenzodiazepines
Nursing Considerations:
• Assess baseline vital signs and laboratory tests (AST, ALT, bilirubin)
• Monitor VS and check for signs of respiratory depression
• Advise patient to take nonbenzodiazepines before bedtime
• Drowsiness may result from taking these drugs so caution while driving is advised
Melatonin Agonists
• Prototype: Ramelteon (Rozerem)
• Action
• targets melatonin receptors to regulate
circadian rhythm in the treatment of
insomnia; decreases REM sleep
• Adverse effects
• drowsiness, dizziness, fatigue, headache,
nausea and suicidal ideation
Sedative-Hypnotics
Geriatric Consideration
• Barbiturates increase CNS depression and confusion in older adults and should not
be taken for sleep.
• Short- to intermediate-acting benzodiazepines are safer for older adults. Long-
acting benzodiazepines should be avoided.
• Advise them to take prescribed benzodiazepines not more than four times a week
to avoid side effects and drug dependency.
ANESTHETICS
Anesthetics
General Anesthetics Local / Regional Anesthetics
• Depress the CNS, alleviate pain and • Block pain at the site without loss of
cause loss of consciousness consciousness
• Nitrous oxide – first anesthetic agent
known as the “laughing gas”
General Anesthetics
Mechanisms of action
• The lipid structure of cell membranes is altered
resulting in impaired physiologic function.
• The inhibitory neurotransmitter gamma-
aminobutyric acid (GABA) is activated to its
receptor that pushes chloride ions. This
decreases the fire action potentials of the
neurons
• The ascending reticular activating system is
altered and the neurons cease to transmit
information (stimuli) to the brain.
Balanced Anesthesia
Refers to the combination of drugs that are frequently used in general anesthesia
which include the following:
1. A hypnotic agent given the night before
2. Premedication with an opioid analgesic or benzodiazepine (e.g. midazolam
[Versed]) plus an anticholinergic (e.g. atropine) given about 1 hour before
surgery to decrease secretions
3. A short-acting barbiturate (e.g. thiopental sodium [Pentothal])
4. An inhaled gas – often combination of nitrous oxide and oxygen
5. A muscle relaxant is given as needed
Balanced Anesthesia
Advantages
• Minimizes cardiovascular problems
• Decreases the amount of general anesthetic needed
• Reduces possible postanesthesia nausea and vomiting
• Minimizes the disturbance of organ function
• Decreases pain
Stages of General Anesthesia
• Begin with consciousness and ends with loss
Analgesia / Induction consciousness
• Produces a loss of consciousness caused by
Excitement or delirium depression of the cerebral cortex
• As anesthesia deepens, respirations become
Surgical more shallow and respiratory rate is increased
• Toxic stage where respirations are lost and
Medullary paralysis circulatory collapse occurs
General Anesthesia
Inhalation Anesthetics Intravenous Anesthetics
• Gas or volatile liquids administered as • Used for rapid induction stage of
gas anesthesia
• Usually combined with a barbiturate, a • IV anesthetics have rapid onsets and short
strong analgesic and a muscle relaxant duration of action
• Adverse effects
• Respiratory depression, hypotension, • Adverse effects
dysrhythmias, hepatic dysfunction, • Respiratory and cardiovascular depression
malignant hyperthermia
• Examples
• Examples • Thiopental sodium (Pentothal), droperidol
• halothane (Flouthane), enflurane (Innovar), etomidate (Amidate), ketamine
(Ethrane), isoflurane (Forane), desflurane hydrochloride (Ketalar), midazolam
(Suprane) and sevoflurane (Ultane) (Versed), propofol (Diprivan)
Regional Anesthetics
Topical Anesthetics
• Applied to mucous membranes, broken or unbroken
skin surfaces
• In the form of solution, liquid spray, ointment, cream,
gel or powder
Local Anesthetics
• Procaine hydrochloride (Novocain), lidocaine
hydrochloride (Xylocaine), bupivacaine (Marcaine)
Spinal Anesthesia
• Administration of local anesthetic in subarachnoid
space at the third or fourth lumbar space
