ST.

LUKE’S COLLEGE OF NURSING

1st Semester
School Year: 2021-2022

GENERAL DISCUSSION SCHEDULE

COURSE CODE : NCM 106

COURSE TITLE : Pharmacology
LESSON NUMBER : 04 – Central Nervous System (CNS) Medications
TIME ALLOTMENT : 6 Hours
PRESCRIBED FLO : Preferred: e-Learning (E1, E2)
Alternative: Modular (M2)

TOPIC LEARNING OUTCOMES:

After the end of the lesson, the student should be able to:

1. Review the anatomy and physiology of the central nervous system

2. Identify and discuss the various types of stimulants and depressants, as well as their nursing responsibilities and patient education
3. Discuss the pathophysiology of seizure and epilepsy, as well as identify and discuss the various types, nursing responsibilities and patient education of
anti-seizure and antiepileptic drugs
4. Discuss the pathophysiology Alzheimer’s Disease and Parkinson’s Disease, as well as identify and discuss the various types, nursing responsibilities and
patient education of Alzheimer and antiparkinsonian Drugs

1 Pharmacology 04 – Central Nervous System (CNS) Medications

 Activities Strategies TA Remarks
1 ATTENTION Open the class with updates on school matters and today’s topic 5 minutes

2 OBJECTIVE Discussion of the learning objectives for the day 5 minutes

3 RECALL Ask the class on what medications they or any family members usually take. Ask on 5 minutes
what they know about the medications they mentioned.
4 STIMULUS Deliver a 2-hour lecture 120 minutes

5 GUIDANCE Open the discussion for any inquiries from the class 5 minutes

6 PERFORMANCE Conduct a 10-item post-test 10 minuts

7 FEEDBACK Rationalize post-test answers 10 minutes

8 ASSESSING Conduct an pre-test 10 minutes

9 RETENTION Summarize the lesson, highlighting the salient points. 10 minutes

LESSON/TOPIC DISCUSSION

Learning Resources:
1. eBook
o Pharmacology: A Patient-Centered Nursing Process Approach, 9e by Linda E. McCuistion, Saunders (2017), Edition: 9
o Pharmacology and the Nursing Process by Lilley, L., Collins, S. & Snyder, J. (2017). 8th ed. St. Louis, Missouri: Elsevier.
o Mosby's 2020 Nursing Drug Reference, 33rd ed. by Linda Skidmore-Roth, St. Louis, MO : Elsevier (2020), Edition: 33
o Introducing Pharmacology: For Nursing and Healthcare by Roger McFadden, Routledge (2019), Edition: 3
o Pathophysiology and Pharmacology in Nursing (Transforming Nursing Practice Series) by Sarah Ashelford, Learning Matters (2019), Edition:
Second
o Lippincott NCLEX-RN Pharmacology Review by Hill
2. Scanned Reference Books
o PHARMACOLOGICAL REVIEWS Vol. 59, No. 4. 2007 by The American Society for Pharmacology and Experimental Therapeutics 70102/3301314
o Pharmacol Rev 59:289 –359, 2007
3. Online Resources

2 Pharmacology 04 – Central Nervous System (CNS) Medications

 o Philippine Drug Enforcement Agency. Laws and Regulations. https://pdea.gov.ph/laws-and-
regulations#:~:text=WHEREAS%2C%20by%20virtue%20of%20the,chemicals%20as%20provided%20in%20R.A.

LESSON 4 TOPICS:

1. The Central Nervous System (CNS)

2. Pain
3. Central Nervous System (CNS) Stimulants
4. Central Nervous System (CNS) Depressants
5. Anticonvulsants
6. Neuromuscular Medications
7. Opioid Analgesics
8. Non – Opioids Analgesics
9. Anesthesia
10. Anti-inflammatory Medications

ACTIVITY 1: INTRODUCTION

• Open the class with updates on school matters and today’s topic

ACTIVITY 2: PRE-TEST

DIRECTIONS: Read each question below and choose the letter that best describe the answer for each.

1. The client is prescribed phenytoin (Dilantin) for treatment of a seizure disorder. What precautions or instructions should be taught to this client?
a. “Do not take aspirin or aspirin-containing products while on this medication.”
b. “Avoid contact sports and heavy physical exercise while on this medication.”
c. “Avoid direct exposure to sunlight while on this medication.”
d. “Do not take warfarin (Coumadin) while on this medication.”

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 2. Which laboratory data should be monitored for a client prescribed a cholinesterase inhibitor, donepezil (Aricept)?
a. Serum electrolyte levels
b. Liver function tests
c. Complete blood cell count
d. Antinuclear antibodies

3. Pain can be acute or chronic?

a. True
b. False

4. The goal of pain management is:

a. Freedom from pain
b. Use the medication according to its indication
c. Prevent the occurrence of toxicity and dependency

5. The client who has experienced status epilepticus treated with IV diazepam has been ordered to receive phenytoin to prevent a recurrence. What statement
indicates that the client understands how to take this medication?
a. “I must drink at least 2 L of water daily.”
b. “This will stop me from getting an aura before a seizure.”
c. “I will not be able to be employed while taking this medication.”
d. “Even when my seizures stop, I will take this drug.”

6. What statement made by a client with newly diagnosed epilepsy indicates that further teaching concerning the drug regimen is necessary?
a. “I will avoid alcohol.”
b. “I will wear a medical alert bracelet.”
c. “I will let my doctor know about this drug when I receive a new prescription for other conditions.”
d. “I can miss up to two pills if I run out of them or they make me ill.”

7. A client presents with an acute exacerbation of multiple sclerosis. Which drug should the nurse be prepared to administer?
a. Baclofen
b. Betaseron
c. Dantrolene sodium
d. Methylprednisolone

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 8. A client with multiple sclerosis has been treated for 6 months with mitoxantrone (Novantrone). What clinical manifestation would alert the nurse to an
adverse effect of this medication?
a. Periorbital edema
b. Black, tarry stools
c. Crackles in the lungs
d. Nausea and vomiting after meals

9. The client with trigeminal neuralgia has received an injection of phenol into the gasserian ganglia. What clinical manifestation would the nurse expect to
find on physical assessment of this client?
a. Asymmetric movement of the face
b. No evidence of sensory or motor dysfunction
c. Inability to sense touch in the area affected by the injection
d. Inhibition of movement on the side of the face that is injected

10. The client is experiencing status epilepticus. Which of the following drugs should the nurse have ready to administer?
a. Atropine
b. Lorazepam
c. Propranolol
d. Theophylline

ACTIVITY 3: CENTRAL NERVOUS SYSTEM (CNS) MEDICATIONS

A. The Central Nervous System (CNS)

• Neuron - Receive stimuli and transmit action potentials
• Axons (Nerve Fibers)
o Slender processes of uniform diameter and may vary in length from a few millimeters to more than a meter
o Usually, there is only one unbranched axon per neuron
▪ Rare branches, if present, are called collateral axons
o Individual axons are surrounded by the endoneurium
o Groups of axons (fascicles) are bound together by the perineurium
o Fascicles form the nerve and are held together by the epineurium

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 • Remember!
o Bundles of processes are called nerve tracts in the CNS and nerves in the PNS
o Trigger zone is the part of the neuron where the axon originates
▪ Action potential is generated from the trigger zone
• Features of a Neuron
o Dendrites - receive signals from neighboring neurons
o Axon - transmit signals over a distance
o Axon terminal - transmit signals to other neuron dendrites or tissues
o Myelin sheath - speeds up signal transmission along the axon
• Action Potential - Electrical impulses due to a temporary shift (from negative to positive) in the neuron’s membrane caused by ions suddenly flowing in
and out of the neuron.
• When action potentials are received:
o Sensory cells: sight, hearing, and touch
o Complex mental activities: conscious thought, memory, and emotions
o Contraction of muscles and the secretion of certain glands
• Neurotransmitters
o Endogenous chemical messengers which transmits signals across a chemical synapse, from one neuron to another "target" neuron, muscle cell,
or gland cell.
o Neurotransmitters are released from synaptic vesicles in synapses into the synaptic cleft, where they are received by neurotransmitter
receptors on the target cells.
• Spinal Cord
o Major communication link between the brain and the PNS (spinal nerves)
o Integration of incoming information and produces responses through reflex mechanisms
• Spinal Nerves – 31 pairs of spinal nerves
o Eight cervical
o Twelve thoracic
o Five lumbar
o Five sacral
o One coccygeal
• Remember!
o Cervical and lumbosacral enlargements give rise to the spinal nerves of the limbs
o Nerves from the end of the spinal cord form the cauda quine

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 o Spinal nerves have specific cutaneous (skin) distributions called dermatomes
• Brain
o Contained in the cranial cavity
o Control center for many of the body’s functions
• Parts of the Brain:
o Brainstem
o Cerebellum
o Diencephalon
o Cerebrum
• Brainstem
o Connects the spinal cord and cerebellum to the remainder of the brain
o Contains 10 pairs of cranial nerves
o Damage to small areas of the brainstem can cause death.
• Medulla Oblongata
o Connected to the spinal cord and contains ascending and descending tracts
o Medullary nuclei regulate the heart, blood vessels, breathing, swallowing, vomiting, coughing, sneezing, hiccupping, balance and coordination
• Pyramid - Nerve fibers that carry voluntary muscle movement messages from cerebrum to spinal cord.
• Pons
o Superior to the medulla
o Ascending and descending tracts pass through the pons
o Connects the cerebrum and the cerebellum
o Pontine nuclei regulate breathing, swallowing, balance, chewing, and salivation
• Midbrain
o Superior to the pons
o Corpora quadrigemina consist of four colliculi
▪ Two inferior colliculi are involved in hearing
▪ Two superior colliculi in visual reflexes
o Substantia nigra and the red nucleus help regulate body movements
o Cerebral peduncles are the major descending motor pathway
• Reticular Formation
o Consists of nuclei scattered throughout the brainstem
o Regulates cyclic motor functions, such as breathing, walking, and chewing

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 o Reticular activating system maintains consciousness and regulates the sleep-wake cycle.
• Cerebellum
o Flocculonodular lobe
▪ Controls balance and eye movements
o Vermis and medial part of the lateral hemispheres
▪ Control posture, locomotion, and fine motor coordination
o Lateral hemispheres
▪ Involved with the planning, practice, and learning of complex movements
• Diencephalon
o Located between the brainstem and the cerebrum
o Consists of the
▪ Thalamus
▪ Subthalamus
▪ Epithalamus
▪ Hypothalamus
• Thalamus
o Consists of two lobes connected by the interthalamic adhesion
o All sensory input that reaches the cerebrum, except for the sense of smell, synapses in the thalamus
o Interacts with other parts of the brain to control motor activity
o Involved in emotions and pain perception
• Subthalamus
o Inferior to the thalamus
o Involved in motor function
• Epithalamus
o Superior and posterior to the thalamus.
o Habenular nuclei, which influence emotions through the sense of smell
o Pineal body, which may play a role in the onset of puberty and the sleep-wake cycle
• Hypothalamus - Main visceral control center of the body and is vitally important to overall body homeostasis.
• Functions of the Hypothalamus:
o Autonomic control center (heart rate, blood pressure, etc.)
o Center for emotional response/behavior
o Body temperature regulation

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 o Regulation of food intake
o Regulation of water balance
o Control of endocrine system functioning
o Mammillary bodies are reflex centers for olfaction
• Cerebrum
o Consists of two hemispheres, left and right, separated by the lontitudinal fissure.
o Responsible for complex sensory and neural functions and coordination of voluntary body movements.
• Lobes of the Cerebrum:
o Frontal lobes - Involved in voluntary motor function, motivation, judgement, aggression, sense of smell, mood, behavioral choices, planning,
personality, organization, attention, expressive language and word choice (Broca’s area)
o Parietal lobes - Receives sensory input, such as touch, pain, temperature, balance, and taste, size, shape, color identification, spatial and visual
perception
o Occipital lobes - Contains the visual centers
o Temporal lobes - Evaluates smell and hearing input, involved in short-term memory, abstract thought, processes language and communication
(Wernicke’s area), organization, sequencing, and emotional interpretation
o Insula - Located deep within the lateral fissure, controls emotion, homeostasis, perception, motor control, self-awareness, cognitive functioning,
and interpersonal experience.
• Basal Nuclei
o Include the corpus striatum (caudate and lentiform nuclei), subthalamic nuclei, and substantia nigra
o Important in controlling motor functions
• Limbic System
o Includes parts of the cerebral cortex, basal nuclei, the thalamus, the hypothalamus, and the olfactory cortex
o Involved in memory, reproduction, nutrition, emotional interpretation of sensory input, and emotions in general

B. Pain
• Pain
o “Unpleasant sensory and emotional experience associated with either actual or potential tissue damage.”
o Management should be individualized and has a constant evaluation throughout the treatment to determine the effectiveness of the pain medication.
o Pain is subjective; it involves psychological experience from the physiologic stimulation.
o Pain threshold – level of stimulus to produce a painful sensation.
o Pain tolerance – amount of pain the patient can handle.
o Ultimate goal of pain management: freedom from pain

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 • Classification of pain:
o Acute pain
▪ Sudden onset that last minutes to hours.
▪ Clinical Manifestation: tachycardia, sweating, pallor, increase blood pressure
o Chronic Pain
▪ Persistent or recurring that last 6 weeks or longer.
▪ Usually from long term illnesses

Type Location
Somatic Pain Skeletal muscles, ligaments, and joints
Visceral Pain Organs and smooth muscles
Superficial Pain Skin and mucous membrane
Vascular Pain Vascular and perivascular tissues
Referred Pain Pain extends to neighboring tissues
Neuropathic Pain Nerve pains
Phantom Pain Body part that has been removed (surgically/traumatically)
Cancer Pain Pressure to organs
Psychogenic Pain Psychological factors
Central Pain Tumors, trauma or inflammation to the brain
Table 4.1: Types of Pain

• Four processes of nociception (pain)

o Transduction – injured tissue emits chemical mediators to convey the signal of pain.
o Transmission – pain sensation travels from spinal cord to the brain.
o Perception of the brain – understanding and interpretation of pain by the brain
o Modulation – brain stem release neurotransmitters that block the pain impulses.
• Pain management ladder
1. Step 1: use of nonopioid (with or without adjuvant medication)
2. Step 2: use for mild to moderate pain; Opioids with or without non-opioiods and with or without adjuvants
3. Step 3: use for moderate to severe pain; Opioids with or without non-opioiods and with or without adjuvants
• Arachidonic Acid Pathway

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 o “Arachidonic acids released from phospholipids in cell membrane from the event/injury and metabolized by either prostaglandin (PG) pathway or
leukotriene (LT) pathway.”
o Prostaglandin – induces inflammation and promotes alteration in vascular responses.

Prostacyclin (PGI2)
Prostaglandin
(Cyclooxygenase)
Thromboxane A2
Arachidonic Acid

Leukotriene
Leukotriene
(Lipoxygenase)

Figure 5.1: Arachidonic Acid Pathway

C. Central Nervous System (CNS) Stimulants

• CNS Stimulants – Drugs that enhances the activities of neurotransmitters: dopamine, norepinephrine, serotonin
• Types of CNS Stimulants
o Amphetamines
o Analeptics
o Anorexiants
• Amphetamines
o Action: acts on cerebral cortex*, reticular activity system**
o Indication:
▪ ↑wakefulness in narcolepsy***
▪ ↑attention span, cognition
▪ ↓hyperactivity, impulsiveness, restlessness of ADHD
o Examples of Amphetamines:
▪ For ADHD
• Methamphetamine (Desoxyn)

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 • Amphetamine (Adderall)
• Dextroamphetamine (Dexedrine)
• Methylphenidate (Concerta, Ritalin)
▪ For Narcolepsy
• Modafinil (Provigil)
• Pemoline (Cylert)
• Analeptics
o Action: stimulates CNS by either increasing neuronal discharge or inhibiting neurotransmitters
o Indication:
▪ Reversal of anesthesia-induced respiratory depression
▪ Stimulate respiration in newborns
o Examples of Analeptics:
▪ Methylxanthines
▪ Aminophylline
▪ Theophylline
▪ Caffeine
▪ NoDoz
▪ Doxapram (Dopram)
• Anorexiants
o Action: suppress the appetite control center in the brain
o Indication: obesity
o Ex. Dextroamphetamine (Dexadrine)
• CNS Stimulants Drug Interactions:
o +Caffeine = ↑effects
o ↓effects of decongestants, antiHPN, barbiturates*
o May alter insulin effects
• CNS Stimulants Side effects/Adverse effects:
o Tachycardia, palpitations, dizziness, hypertension
o Sleeplessness, restlessness, nervousness, tremors, irritability
o ↑hyperactivity
o Anorexia, dry mouth, vomiting, diarrhea, weight loss
o Thrombocytopenia*

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 • CNS Stimulants Contraindications/Precautions:
o C: Glaucoma, severe CV disease
o P: psychosis, pregnant and breastfeeding women
o CNS Stimulants
• CNS Stimulants Nsx Action:
o Give before breakfast and lunch*
o Report arrhythmias, seizures, palpitations, liver problems
o Record ht, wt, and growth of children
o Avoid alcohol, caffeine
o Use sugarless gum to relieve dry mouth
o Do not stop abruptly; taper**

D. Central Nervous System (CNS) Depressants

• CNS Depressants
o Action: Drugs that have an CNS inhibitory effect
• Types of CNS Depressants:
o Sedatives
▪ Reduces nervousness, excitability, and irritability without causing sleep
o Sedative-hypnotics
▪ Low doses: calm the CNS without inducing sleep
▪ High doses: calm the CNS and causes sleep; also causes respiratory depression
• Classifications of CNS Depressants:
o Barbiturates
o Benzodiazepines
o Non-benzodiazepines
• Barbiturates
o Action: inhibits GABA*, which inhibits nerve impulses in the cerebral cortex; suppresses REM sleep**
o Indication: Hypnotics, sedatives, anticonvulsants, anesthesia
o Habit forming**; low therapeutic index
• Types of Barbiturates:
o Ultrashort-acting
▪ Used as a general anesthetic

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 ▪ Ex. thiopental sodium (Pentothal)
o Short-acting
▪ Induce sleep, controls convulsion, and no residual drowsiness
▪ Ex. pentobarbital (Nembutal), secobarbital (Seconal)
o Intermediate-acting
▪ Induce and sustain sleep, for convulsion, but causes residual drowsiness (hangover effect)
▪ Ex. amobarbital (Amytal), butabarbital (Butisol)
o Long acting
▪ Used to control seizures
▪ Ex. phenobarbital
• Remember! Barbiturates are notorious enzyme inducers; it stimulates liver enzymes, which speeds up drug metabolism resulting to shortened duration of
drug action
• Benzodiazepines
o Action: Interacts with GABA to reduce neuron excitability; do not suppresses REM sleep
o Indication: agitation, anxiety, alcohol withdrawal, pre-operative sedation, insomnia, seizure, skeletal muscle relaxation
• Types of Benzodiazepines
o Long acting
▪ Estazolam (Prosom)
▪ Flurazepam (Dalmane)
▪ Others
o Short-acting
▪ Temazepam (Restoril)
▪ Triazolam (Halcion)
• Remember! Benzodiazepines are the most frequently prescribed sedative-hypnotics because of their favorable drug effect
• Non-benzodiazepines
o Action: neurotransmitter inhibition
o Indication: treat short-term (<10 days) insomnia
o Ex. Zolpidem (Ambien), eszopiclone (Lunesta)
• CNS Depressants Drug interactions:
o Alcohol, antihistamines, benzodiazepines, opioids, tranquilizers, CNS depressants, MAOIs = ↑effect, ↓respirations with
o MAOIs will prolong effects of barbiturates
o ↓anticoagulant response, leading to possible clot formation

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 • CNS Depressants Side effects / Adverse effects:
o Residual drowsiness (“Hangover effect”)
o Headache, vertigo
o Fall hazard for frail elderly persons
o Drug dependence and tolerance
o Respiratory depression
o Withdrawal symptoms
• CNS Depressants Contraindication:
o Pregnancy
o uncontrolled pain
o acute intermittent porphyria*
• CNS Depressants Nsx Action:
o Assess health and drug Hx., monitor VS and I/O: including supine and erect BPs
o Give 15-30 min before bedtime
o Monitor “hangover effect, ” use with caution in elderlies, and ensure safety measures (fall risk)
o Avoid alcohol and other CNS depressants
o WOF rebound insomnia 3-4 weeks after drug being discontinued

E. Anticonvulsants
• Seizure Disorders
o Seizure – abnormal electric discharges from neurons characterized by loss of consciousness and convulsive movements
o Convulsion – sudden, violent, irregular movement of a limb or of the body, caused by involuntary contraction of muscles and associated especially
with brain disorders
o Epilepsy – chronic, recurrent occurrence of 2 or more unprovoked seizure episodes
• Anticonvulsants*
o Action: Suppress abnormal neuron firing, inhibiting seizure activities
o Indications: Tonic-clonic seizure*, status epilepticus**, complete partial seizures***, arrhythmias, trigeminal neuralgia****
• Classifications of Anticonvulsants:
o Suppress Na influx
▪ Phenytoin (Dilantin)
o Suppress Ca influx
▪ Valproic acid (Depakane), divalproex (Depakote)

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 o Enhance action of GABA*
▪ Clonazepam (Klonopin), gabapentin (Neurontin)
o Inhibit GABA degradation
▪ Vigabatrin (Sabril)
• Type of Anticonvulsants:
o Hydantoin
o Barbiturates
o Benzodiazepines
o Succinimides
• Hydantoin
o Most commonly used drug for seizure control: phenytoin
o Lesser toxic effects; non-addicting
o Should NOT be used in pregnancy
o Has a narrow therapeutic range
• Barbiturates
o For grand mal* acute episodes of status epilepticus
o Use long-acting barbiturate: phenobarbital
o Lesser teratogenic** effects than phenytoin
• Benzodiazepines
o Primary treatment for acute seizures: diazepam
o Short term effect; not for maintenance
o For petit mal seizures: clonazepam
o High degree of tolerance*
o Adjunctive therapy for treatment of partial seizures: clorazepate
• Succinimides
o Used to treat absence or petit mal seizures*
o May be used in combination with other anticonvulsants
• Anticonvulsants Drug interactions:
o +cimetidine (Tagamet), INH, sulfonamides = ↑effects
o +folic acid, antacids, calcium, sucralfate, antineoplastics, antipsychotics, primrose, ginkgo = ↓effects
o ↓effects of anticoagulants, oral contraceptives, antihistamines, dopamine, theophylline
• Anticonvulsants Side effect/adverse reactions:

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 o SE: Gingivitis, gingival hyperplasia, nystagmus, diplopia, dizziness, slurred speech, decreased coordination, alopecia
o AE: Thrombocytopenia, Stevens-Johnson syndrome*
• Anticonvulsants Contraindications:
o Pregnancy, sinus bradycardia, sinoatrial block, second- and third-degree AV block, Adam-Stokes syndrome**
• Anticonvulsants Nsx Action:
o Monitor serum drug levels (toxicity), glucose levels in DM, liver enzymes, CBC (platelet), ECG
o Administer with food
o Ensure safety during usage (fall risk)
o Avoid certain herbs, alcohol, and other CNS depressants
o For women taking oral contraceptives, advise to consider other methods
o Promote oral hygiene and dental check-ups
o Must be taken at same time every day, taper drug
o Warn of harmless pinkish red or brown urine

F. Neuromuscular Medications
• Myasthenia Gravis (MG) - Autoimmune disease caused by lack of nerve impulses and muscle responses at myoneural junction due to lack of acetylcholine
reaching cholinergic receptors
• Characteristics:
o Muscular weakness and fatigue
o Respiratory muscle paralysis, ptosis, difficulty chewing and swallowing
• Cholinesterase Inhibitors
o Action: transmission of neuromuscular impulses by preventing destruction of Ach – allows adrenergic response
o Indication: control and treat MG
• Specific actions of Cholinesterase Inhibitors
o Short-acting
▪ Neostigmine (Prostigmin)
o Ultrashort-acting for diagnosing MG
▪ Edrophonium (Tensilon)
o Intermediate acting
▪ Pyridostigmine (Mestinon)
• Specific Indication of Cholinesterase Inhibitors
o For Myasthenia crisis

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 ▪ Underdosed
▪ Severe muscle weakness
▪ Improves after edrophonium*
o For Cholinergic crisis
▪ Overdosed
▪ Severe muscle cramping
• Cholinesterase Inhibitors Side effects / Adverse effects:
o Pupil constriction
o GI distress, abdominal cramps
o Excess saliva, sweating
o Headache, dizziness, seizures
o Hypotension, bradycardia, dysrhythmias
o Bronchospasm, respiratory depression
• Cholinesterase Inhibitors Nsx Action:
o Administer doses on time
o Take drug before meals
o Monitor drug effectiveness
o Antidote for cholinergic crisis: atropine
• Multiple Sclerosis (MS) - Autoimmune disorder that attacks myelin sheath of nerve fibers
• Characteristics:
o Weakness or spasticity in extremities
o Diplopia
• Muscle Relaxants
o Provides relief of painful musculoskeletal conditions:
▪ Muscle spasms
▪ Management of spasticity of severe chronic disorders
▪ Multiple sclerosis, cerebral palsy
o Work best when used along with physical therapy
• Types of Muscle Relaxants
o Central acting: CNS
▪ Baclofen (Lioresal)
▪ Diazepam
▪ Carisoprodol (Soma)

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 ▪ Cyclobenzaprine (Flexeril)
▪ Methocarbamol (Robaxin)
o Direct acting: Skeletal muscle
▪ Dantrolene sodium
▪ Quinine
• Muscle Relaxants Side effects / Adverse effects:
o Drowsiness, sedation, dizziness, headaches, GI distress, fatigue, drug dependence
• Muscle Relaxants Nsx Action:
o Take with food
o Monitor VS, liver function
o Do not allow to drive
o Do not take longer than 3 weeks
o Do not stop abruptly: discontinue over 1 week to avoid rebound spasms
o Avoid alcohol and other depressants

G. Opioid Analgesics
• Opioid Drugs – Derived from opium plant that imitates natural narcotics. It is being utilized to relieve and decrease pain without causing the patient to
lose consciousness. Further, it also has antitussive and antidiarrheal properties.
• Types of opioids drugs:
o Agonist
▪ Binds to opiate receptor sites in the peripheral nervous system and in the CNS. When attached, the drug mimics the effects of natural
biochemical compounds that produce body’s natural pain reliever such as endorphins.
o Partial agonist (mixed opioid agonist-antagonist)
▪ Weakly antagonize the effects of agonists and others exert agonist to the other receptors.
▪ Weaker neurologic / pain reliever response as compared to agonists.
o Antagonist
▪ These are not pain medications; however, it blocks the effect of the opioid agonist and being used for reversal of drug reactions.
▪ In effect, it also reverses the analgesic effect of the opioid agonist.

AGONISTS MIXED ANTAGONIST

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 Morphine
Fentanyl
Nalbuphine Naloxone
Meperidine
Pentazacine Naltrexone
Codeine
Methadone

Table 4.2: Opioid Analgesics

• Liver metabolizes the opioid drugs, thus increases the liver enzymes.
• Also acts on the medulla oblongata which controls the respiration and coughing.
• Indications:
o Agonist
▪ Severe pain in acute, chronic and terminal illnesses.
o Mixed
▪ Given to limit dependency and toxic effects
o Antagonist
▪ Block the effect of opioids by occupying the receptor sites.
▪ Treatment for opioid overdose
• Contraindications:
o Drug allergy
o Severe asthma
o Hypotension
o Severe renal disease
o Increase ICP – decreases respiratory rate
o Head injuries
• Adverse Effects / Side Effects:
o Constipation
o Hypotension
o Nausea and vomiting
o Sedation and mental clouding
o Respiratory Depression
o Subacute overdose
o Urinary retention

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 o Pupil constriction
• Drug Interactions:
o Alcohol, antihistamines, barbiturates, benzodiazepines, phenothiazine, and CNS depressants will INCREASE the respiratory depressant effects.
o Monoamine oxidase inhibitors (MAOI) will increase respiratory depression and hypotension.
o MAOI + Meperidine = deep coma and death
• Nsx Action:
o Highly addictive.
o Opioid depresses the respiratory status.
o Withdrawal symptoms’ onset will depend on the half-life of the medication.
o Analgesic Ceiling Effect for Opioid Analgesics
o Opioid Tolerance: increases tolerance that makes the doses higher to main the therapeutic effect.
o Physical Dependency: physiologic adaptation of the body to the opioids
o Assessed for any drug allergies
o Monitor Vital Signs (Respiratory Rate) including Pain Scale
o Oral forms should be taken with foods.
o Encourage deep breathing exercises to promote lung expansion
o Instruct to change position slowly
o Keep naloxone and resuscitation equipment at bedside all the time.
o Increase fluid intake and fiber to soften the stool

H. Non – Opioids Analgesics

• Action
o Inhibit cyclooxygenase (COX) enzymes to prostaglandins.
o Blocks peripheral pain by inhibition of prostaglandin synthesis
o Peripheral-acting
o Inhibits pain receptors
o Promotes peripheral vasodilation to reduce fever
o All NSAIDs are absorbed in the GIT, metabolized in the liver, and excreted by the kidneys.

COX Inhibitor
COX 1
(Non-selective COX inhibitor)
• Protects stomach
• Increase risk of ulcers

21 Pharmacology 04 – Central Nervous System (CNS) Medications

 • Promotes coagulation • Increase risk of bleeding
(promotes TXA2)
COX 2 Inhibitors
COX 2 • Decrease risk of ulcers
(Nothing unique) • Increase coagulation:
• Risk for MI/Stroke

Table 4.3: Types Non-Steroidal Anti-inflammatory Drugs (NSAID)

• Indications:
o Relieves mild to moderate pain
▪ Rheumatoid and osteoarthritis (Most common – Ibuprofen)
o Antipyretics, anti-inflammatory
o Vascular headaches
o Platelet inhibitions
o Lowers body temperature by vasodilation (Anti pyretic); Drug of choice for fever.
o Weak anti-inflammatory effects
o Alternative for who cannot tolerate aspirin or has allergy. It also does not affect platelet functions
• Contraindications:
o Allergies with NSAIDs.
o High risk for bleeding
o Glucose-6-phosphate dehydrogenase (G6PD) deficiency
o Liver failure
o Not advised to pregnant women
• Side Effects / Adverse Effects:
o Rash,
o Bleeding (Internal)
o Nephrotoxicity
o Diarrhea, Nausea, vomiting, anorexia (gastrointestinal distress)
o Hepatotoxicity
o Reye’s Syndrome – when aspirin (salicylates) is given to children with chicken pox or flu-like symptoms
▪ Life threatening; causes neurologic deficits that can lead to coma and liver dysfunction.

22 Pharmacology 04 – Central Nervous System (CNS) Medications

 Acetic Acids Salicylates Para-aminophenol COX-2 Inhibitors Fenamic Acids Propionic Acids
(Nonselective COX (Nonselective COX (Selective COX (Nonselective COX (Nonselective COX
Inhibitors) Inhibitors) Inhibitor) Inhibitors) Inhibitors)
Diclofenac sodium Acetaminophen Naproxen
Paracetamol Celecoxib
(Voltaren) Aspirin Mefenamic Acid Ibuprofen
(Celebrex)
Indomethacin Ketorolac

Table 4.4: Non-Steroidal Anti-inflammatory Drugs (NSAIDS)

• Drug Interactions:
o Amplify the effects of anticoagulants, oral hypoglycemic agents
o High risk of toxicity with Calcium channel blockers
o Alcohol, corticosteroids increase GIT effects.
o Alcohol increases the risk for liver toxicity
• Nsx Action:
o Chronic salicylate intoxication also known as salicylism. Clinical manifestations are:
▪ Tinnitus and hearing loss
▪ Metabolic Acidosis and Respiratory Alkalosis
▪ Nausea, vomiting, and diarrhea
o Treatment Goal: to remove the salicylate from the GIT and prevent further absorptions
o Red blood cells (RBC), Hemoglobin, and Hematocrit may decrease if bleeding is present.
o Stop aspirin for 1 week before surgery
o Cautiously administer salicylates to asthmatics because of the risk of having bronchospasm.
o Cautiously administer NSAIDs to high risk of thrombotic events such as myocardial infarction or stroke
o Watch out for drug allergy.
o Watch out for signs and symptoms of bleeding.
o Assess auditory functions.
o Monitory CBC, platelet, Prothrombin time and hepatic and renal functions.
o Administer NSAIDs with foods.
o Do not chew or crush enteric coated tablets.
o Administer drug in liquid form for patients who have difficulty swallowing.
o Duration: less than 5 days for children; less than 10 days for adult.

23 Pharmacology 04 – Central Nervous System (CNS) Medications

 o Overdose can cause liver necrosis
o Acetaminophen overdose: 150mg/kg
o Antidote: Acetylcysteine (Fluimucil)

I. Anesthesia
• Anesthesia – Depresses central nervous system (CNS) or peripheral nervous system (PNS) which produces loss of consciousness, loss of responsiveness
to stimuli and muscle relaxation
• Action:
o Inhalation:
▪ Anesthesia absorbed by the blood through the lungs.
▪ Rapid distribution to organs
▪ Primarily works by depressing the CNS
o Parenteral:
▪ Lipid-soluble and well distributed to the body
▪ Overton-Meyer Theory – the greater the drug’s lipid solubility, the greater the effect.
▪ Crosses placenta and enter breast milk
▪ Occupy sites on receptors on the CNS and modifying release of neurotransmitters
▪ Depresses CNS, skeletal muscle relaxation
o Local:
▪ Absorption varies widely.
▪ Metabolites are excreted in the urine.
▪ Blocks nerve impulses at the point of contact.
o Topical:
▪ Applied over the intact skin or mucous membrane
▪ Little systemic absorption, however, with impaired skin integrity, it increases the systemic absorptions.
▪ Excreted in the urine
▪ Absorbed by the skin and acts on the nerve cell membrane and blocks transmission
• Indications:
o Inhalation:
▪ Surgeries – rapid onset
o Parenteral:
▪ Shorter surgical procedures (outpatient surgeries)
▪ Ketamine – induce profound sense of dissociation from environment

24 Pharmacology 04 – Central Nervous System (CNS) Medications

 ▪ Benzodiazepines – produce sedation or amnesia but does not relief pain.
o Local:
▪ Prevent or relieve at the specific area.
▪ Severe pain that topical anesthesia can’t relieve.
o Topical:
▪ Relieve or prevent pain (minor burn pain)
▪ Relieve itchiness and irritation
▪ Anesthetize before giving injection
▪ Numb mucosal surface (urinary catheter)
• Contraindications
▪ Inhalation:
▪ Hypersensitivity
▪ Liver disorder
▪ Malignant hyperthermia
o Parenteral:
▪ Drug allergy
▪ Pregnant
▪ Narrow angle glaucoma
▪ Malignant Hyperthermia
o Local:
▪ Drug allergy
o Topical:
▪ Drug allergy
• Side Effects / Adverse Effects
o Myocardial depression
o Respiratory depression
o Inhalation:
▪ Malignant Hyperthermia – sudden and lethal increase in body temperature.
o Parenteral:
▪ Ketamine – prolonged recovery, irrational behavior, excessive salivation and tearing
▪ Propofol – respiratory depression, bradycardia. Hypotension
▪ Thiopental – respiratory depression
▪ Fentanyl – CNS and respiratory depression, arrhythmias

25 Pharmacology 04 – Central Nervous System (CNS) Medications

 ▪ Midazolam – CNS and respiratory depression, hypotension
o Local:
▪ True allergic reactions are rare
▪ Anxiety, apprehension, restlessness, nervousness, disorientation, confusion
▪ Spinal headache – from spinal anesthesia
▪ Relieve by bedrest and conventional analgesics
o Topical:
▪ Hypersensitivity reactions
▪ Skin irritations
▪ Frostbite

General Anesthesia Local Anesthesia

Intravenous:
Inhalation:
• Barbiturates (thiopental) Amide: (with nitrogen) Ester: (with oxygen)
• Sevoflurane
• Benzodiazepines • Bupivaciaine • Procaine
• Desflurane
(midazolam) • Levobupivacane • Chloroprocaine
• Nitrous oxide (laughing
• Dissociatives (ketamine) • Lidocaine • Tetracaine
gas)
• Opiates (fentanyl)

Table 4.5: Anesthesia

• Drug Interactions:
o Inhalation:
▪ Combination with other CNS, Cardiac or respiratory depressants will increase depressant effects.
o Parenteral:
▪ Ketamine and nondepolarizing drugs increase neuromuscular effect and prolonged respiratory depression
▪ Barbiturates or opioids + Ketamine: prolong anesthesia time
▪ Anticholinergics – increases potential for confusion, tachycardia, constipation
o Co administered with Epinephrine – to constrict blood vessels and this in return, control local bleeding and reduces anesthesia absorption (due to
vasoconstriction) which prolongs anesthetic action at site.
• Nsx Action:
o Assess for drug allergies and risk factor for complication of anesthesia (smoking)

26 Pharmacology 04 – Central Nervous System (CNS) Medications

 o Explain the anesthesia period for preoperative, intraoperative and postoperative
o Encourage deep breathing exercises, coughing, early ambulation as postoperatively
o Monitor Vital signs and LOC, respiratory status, and pain status.
o Promote safety measures and precautions
o Depresses CNS, Cardiac and Respiratory functions
o Balance anesthesia – usage of minimal doses of multiple anesthesia to achieve desired effects
o Safer choice than general anesthesia for elderly patients, respiratory disorders such as COPD and myasthenia gravis.
o Explain the purpose of the therapy and intended effect.
o Monitor vital signs including pain

J. Anti-Inflammatory Medications
• Inflammation
o Reaction to tissue injuries
o This is caused by the release of histamine, serotonin, bradykinin, leukotrienes and prostaglandins
o The symptoms were caused by the vascular responses such as capillary, artery and venous dilation.
o Fluids and leukocytes migrate towards the injury site.
o Induced by Phospholipase A2
o Phospholipase A2 is stimulated by:
▪ Tissue injury
▪ Thrombin
▪ Bradykinin
▪ Angiotensin II
▪ Epinephrine
• Rheumatism – general term for disorders that is characterized by inflammation, degeneration or metabolic derangement connective tissues.
• Anti-inflammatory Medications:
o NSAIDs
o Steroids
o Disease-Modifying Anti-rheumatic Drugs
o Anti-Gout
• Corticosteroids
o Action:
o Suppresses immune responses and reduces inflammation, anti-stress and anti-allergic

27 Pharmacology 04 – Central Nervous System (CNS) Medications

 o Prevents the leakage of plasma from the capillaries and the migration of leukocytes
o Inhibit inflammation by the means of inhibiting the release of phospholipase A2 enzymes (which frees the phospholipid)
o Examples:
▪ Prednisone
▪ Celestone
▪ Hydrocortisone
▪ Dexamethasone
o Indications:
▪ Severe inflammations
▪ Immunosuppression
o Contraindications:
▪ Drug allergy
▪ Fungal infections
o Side effects / Adverse effects:
▪ Hyperglycemia
▪ Infection
▪ Weight gain and edema
▪ Cushing’s Syndrome
o Drug Interactions:
▪ Aspirin and NSAIDS + Corticosteroids = increased risk of GIT bleeding and ulceration
▪ Corticosteroids + Potassium losing diuretics = hypokalemia
▪ Dexamethasone decreases the effect of anticoagulants and antidiabetic medications
▪ Prednisone + Barbiturates, phenytoin and rifampin = decrease the effect of prednisone.
o Nsx Action:
▪ Cushing Syndrome: Moon face, puffy eyelids, edema in the feet, bruising, dizziness, bleeding and irregular menstrual cycle; these can be
result from long term glucocorticoids treatments.
▪ Live vaccines should not be given with this treatment.
▪ Abrupt withdrawal of drug can cause rebound inflammation, fever, depression, hypotension, hypoglycemia and adrenal insufficiency.
▪ Monitor for electrolytes, blood glucose levels.
▪ Monitor for daily weight, hypertension.
▪ Avoid individuals with infections
▪ Do not immediately stop the treatment after a long-term use.
▪ Give the medications during morning.

28 Pharmacology 04 – Central Nervous System (CNS) Medications

 ▪ Administer with food to prevent GIT irritation. Encourage food high in potassium.
• Disease-Modifying Anti-rheumatic Drugs (DMARs)
o Action
▪ Slows the progression of disease associated with arthritis.
▪ Slow onset of action that takes up to several weeks and usually take 3 to 6 months to see full effects. (Slow-acting anti-rheumatic drugs
(SAARDs))
▪ Exhibit anti-inflammatory, anti-arthritic, and immunomodulating effects and works by inhibiting the movement of the cells into the
damage tissue.
o Indications – Rheumatoid arthritis
o Contraindications:
▪ Active bacterial infection
▪ Active herpes zoster
▪ Active or latent tuberculosis
▪ Acute or chronic hepatitis B or C.

Non – Biologic Biologic DMARDs Gold Drug

DMARDs (Immunomodulators) Therapy
Adalimumab
Methotrexate Auranofin
Anakinra
Leflunomide (Ridaura)
Etanercept

Table 4.6: Disease-Modifying Anti-rheumatic Drugs (DMARDS)

o Side effects / Adverse effects

▪ Pancytopenia
▪ Infections
▪ Fatigue, nausea and vomiting and flu like symptoms
o Drug Interactions:
▪ Should not be used with other DMARDs or immunosuppressants
o Nsx Action:
▪ Report signs and symptoms of infections to physician.
▪ Do not administer live vaccines
▪ Monitor for complete blood count and liver enzymes

29 Pharmacology 04 – Central Nervous System (CNS) Medications

 ▪ Monitor injection site for pain, swelling and irritation.

• Anti-Gout Medications
o Action - Minimize inflammation by blocking uric acid absorptions and increases the uric acid excretion.
o Indications:
▪ Hyperuricemia
▪ Gout
o Contraindications – Renal or hepatic disease

Colchicine Allopurinol Probenecid

Anti-gout by reducing Uric acid
Uricosurics
inflammatory responses inhibitors

Table 4.7: Anti-Gout Medications

o Side effects / Adverse effects:

▪ Bone marrow suppression
▪ Uric acid stones
▪ Metallic taste
▪ Diarrhea, nausea and vomiting
o Drug Interactions:
▪ Aspirin can trigger the gout attack; aspirin with antigout medications causes elevated uric acid levels.
o Nsx Action:
▪ Avoid alcohol, foods high in purine.
▪ Encourage increase fluid intake to prevent kidney stones.
▪ Monitor liver functions.
▪ Take medications with food
▪ Acute attack of gout attacks:
• Use cautiously with cardiac, renal, GIT diseases
• If GIT symptoms occur (vomiting, nausea, diarrhea) withhold medications
• It can cause renal failure
▪ Prophylaxis in gout attack (Chronic gout):

30 Pharmacology 04 – Central Nervous System (CNS) Medications

 • Increases the effect of warfarin and oral hypoglycemic
• Do not take large doses of vitamin C because of the risk of having kidney stones.
• Limit exposure to sunlight -
▪ Mild GIT distress may occur; take with food to lessen distress:
• Aspirin interfere with uricosuric actions

ACTIVITY 4: DISCUSSION / EXERCISE

• Ask the class for any questions that they may have regarding the lecture.

ACTIVITY 5: POST TEST

DIRECTIONS: Read each questions below and choose the letter that best describe the answer for each.

1. A nurse is preparing a client newly diagnosed with multiple sclerosis for discharge home from a rehabilitation center. The client has been prescribed
cyclophosphamide and methylprednisolone. What should be included in a teaching plan for this client?
a. “Take hot baths.”
b. “Avoid people with colds.”
c. “Try to use physical aids such as walkers as little as possible.”
d. “You may discontinue these medications when your symptoms improve.”

2. The client with relapsing-remitting multiple sclerosis asks why continuous treatment with interferon beta-1a (Avonex) is necessary. What is the nurse’s
best response?
a. “This medication will help decrease the number and severity of relapses.”
b. “This medication is given weekly to halt progression of the disease.”
c. “This medication is given continuously for 1 year to effect cure.”
d. “This medication will protect your muscles from spasticity.”

3. The client with myasthenia gravis who is taking Tensilon develops a sudden increase in weakness, accompanied by an increase in heart rate from 76 to
100 beats/min and an increase in blood pressure from 122/72 to 152/82. What conclusion can the nurse make from these findings?
a. The client is experiencing a mixed crisis.
b. The client is experiencing myasthenic crisis.
31 Pharmacology 04 – Central Nervous System (CNS) Medications
 c. The client is experiencing cholinergic crisis.
d. The client’s condition is responding to treatment.

4. Nurse Joelle has instructed the client with myasthenia gravis to take drugs on time and to eat meals 45 to 60 minutes after taking the anticholinesterase
drugs. The client asks why the timing of meals is so important. What is the nurse’s best response?
a. “This timing allows the drug to have maximum effect, so it is easier for you to chew, swallow, and not choke.”
b. “This timing prevents your blood sugar level from dropping too low and causing you to be at risk for falling.”
c. “These drugs are very irritating to your stomach and could cause ulcers if taken too long before meals.”
d. “These drugs cause nausea and vomiting. By waiting for a while after you take the medication, you are less likely to vomit.”

5. Which of the following is an opioid analgesics?

a. Mefenamic Acid
b. Meperidine
c. Aspirin
d. Ketorolac

6. Which of the following is a local anesthetic?

a. Sevorane
b. Midazolam
c. Lidocaine
d. Dormicum

7. The client with myasthenia gravis in cholinergic crisis has been treated with atropine. What nursing intervention is a priority for this client?
a. Suctioning the client
b. Turning and positioning the client
c. Measuring urinary output every 30 minutes
d. Administering anticholinergic drugs on time

8. The nurse is teaching a child and the family about the medication phenytoin (Dilantin) prescribed for seizure control. Which of the following side effects is
most likely to occur?
a. Vertigo
b. Drowsiness

32 Pharmacology 04 – Central Nervous System (CNS) Medications

 c. Gum hyperplasia
d. Vomiting

9. A nurse is about to administer Naloxone hydrochloride (Narcan) to a client with known opioid overdose. Which of the following equipment should be
readily available at the bedside?
a. Suction machine.
b. Resuscitative equipment.
c. Nasogastric tube.
d. Dressing tray.

10. Nurse Frances is caring for a client with a history of epilepsy who suddenly begins to experience a tonic-clonic seizure and loses consciousness. What would
be her best action?
a. Restrain the client’s extremities.
b. Administer benzodiazepine as ordered.
c. Take the client’s blood pressure.
d. Place an airway into the client’s mouth.

ACTIVITY 6: SYNTHESIS / EXERCISE

• Summarize the lesson, highlighting the salient points.

Prepared by: Reviewed by: Approved by:

Dr. Tristan Jourdan C. Dela Cruz, RN Dennis Luis D. Abellera, RN MAN Dr. John Michael O. Lorena, RN
Lecturer, Pharmacology Academic Head Dean

33 Pharmacology 04 – Central Nervous System (CNS) Medications