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Chapter 6
Anesthetics,
Analgesics, and
Narcotics
Chapter 6 Topics
• Divisions of the Nervous System
• Major Neurotransmitters
• Anesthesia
– General Anesthesia
– Local Anesthesia
• Pain Management
• Migraine Headaches
Learning Objectives
• Understand the central and peripheral nervous
systems, their functions, and their relationship to
drugs.
• Become aware of the role of neurotransmitters.
• Learn how drugs affect body systems and where
they work in the body.
• Understand the concepts of general and local
anesthesia, and know the functions of these
agents.
Learning Objectives
• Define the action of neuromuscular blocking
agents in reducing muscle activity.
• Distinguish between narcotic and nonnarcotic
analgesia.
• Become familiar with the various types of
agents for migraine headaches.
Divisions of the Nervous System
• Central Nervous System
– Brain
– Spinal cord
• Peripheral Nervous System
– Nerves
– Sense organs
Divisions of the Nervous System
• Central Nervous System
1. Brain receives information
2. Evaluates information
3. Sends out a response
• Peripheral Nervous System
Divisions of the Nervous System
• Central Nervous System
• Peripheral Nervous System
– Somatic Nervous System
– Autonomic Nervous System
Divisions of the Nervous System
• Central Nervous System
• Peripheral Nervous System
– Somatic Nervous System
Voluntary action: skeletal muscle contraction and
movement
– Autonomic Nervous System
Involuntary activities: respiration, circulation,
digestion, sweating
Autonomic Nervous System
Review
The nervous system has two
components. What are they?
Review
The nervous system has two components. What
are they?
Answer
– Central nervous system (CNS)
– Peripheral nervous system (PNS)
Major Neurotransmitters
•
•
•
•
•
Acetylcholine
GABA
Dopamine
Epinephrine
Serotonin
Major Neurotransmitters
• Acetylcholine (ACh)
– Smooth muscle, cardiac muscle, and
exocrine glands
– Anticholinergics block ACh receptors
•
•
•
•
GABA
Dopamine
Epinephrine
Serotonin
Major Neurotransmitters
• Acetylcholine
• GABA (gamma-aminobutyric acid)
Regulates message delivery system of
the brain
• Dopamine
• Epinephrine
• Serotonin
Major Neurotransmitters
• Acetylcholine
• GABA
• Dopamine
Acts on the CNS and kidneys
• Epinephrine
• Serotonin
Major Neurotransmitters
• Acetylcholine
• GABA
• Dopamine
• Epinephrine
– Acts on cardiac and bronchodilator
receptors
– Known as Adrenaline
• Serotonin
Major Neurotransmitters
•
•
•
•
Acetylcholine
GABA
Dopamine
Epinephrine
• Serotonin
– Acts on smooth muscle and gastric mucosa
(causes vasoconstriction)
– Emotional responses: depression, anxiety
Communication by
Neurotransmitters
Neurotransmitters are released from one
axon and received by another neuron’s
dendrites.
Discussion
What are three important
types of receptors in the study
of drugs?
Discussion
What are three important types of receptors
in the study of drugs?
Answer
– Alpha
– Beta-1
– Beta-2
Types of Receptors
• Alpha
Vasoconstriction, raise BP
• Beta-1
Heart stimulation
• Beta-2
Vasodilation and bronchodilation
Drug Effects on Receptors
Drugs can have two types of effects on
receptors.
– Stimulating, causing a reaction
– Blocking, preventing a reaction
• Dopamine blocking
• Anticholinergics
Anticholinergic Side Effects
•
•
•
•
•
•
Decreased GI motility
Decreased sweating
Decreased urination
Dilated pupils
Dry eyes
Dry mouth
Anesthesia
In the “old days” the following were used for
anesthesia.
Anesthesia
In the “old days” the following were used for
anesthesia.
–
–
–
–
–
Alcohol
Drugs
Ice for numbing
Blow to the head
Strangulation
Anesthesia
Now, anesthesia is designed to focus on
specific systems, such as
Anesthesia
Now, anesthesia is designed to focus on
specific systems, such as
• Nervous system
• Skeletal system
• Respiratory system
• GI system
• Endocrine system
• Hepatic system
• Cardiovascular system
Anesthesia
Goals of Balanced Anesthesia
– Amnesia
Anesthesia
Goals of Balanced Anesthesia
– Amnesia
– Adequate Muscle
Relaxation
Anesthesia
Goals of Balanced Anesthesia
– Amnesia
– Adequate Muscle Relaxation
– Adequate Ventilation
Anesthesia
Goals of Balanced Anesthesia
– Amnesia
– Adequate Muscle Relaxation
– Adequate Ventilation
– Pain Control
Types of Anesthesia
• General
• Local
Types of Anesthesia
•General
• Local
Discussion
What are some of the indicators
used to assess general anesthesia?
Discussion
What are some of the indicators used
to access general anesthesia?
Answer: Blood pressure,
hypervolemia, oxygen level,
pulse, respiratory rate, tissue
perfusion, urinary output
General Anesthesia
Preanesthetic Medications
–
–
–
–
Control sedation
Reduce postoperative pain
Provide amnesia
Decrease anxiety
General Anesthesia
Malignant Hyperthermia
– Side effect of anesthesia
• Fever of 110°F or more
• Life threatening
– Treatment: dantrolene (Dantrium)
Warning!
Always check
expiration date.
Drug List
Inhalant Anesthetics
•
•
•
•
•
desflurane (Suprane)
enflurane (Ethrane)
halothane
isoflurane (Forane)
nitrous oxide
Inhalant Anesthesia Side Effects
• Causes reduction in blood pressure
• May cause nausea and vomiting
nitrous oxide
• Causes analgesia only; no amnesia or
relaxation
• May be given alone or may be given
with more powerful anesthetics to
hasten the uptake of the other agent(s)
• Commonly used for dental procedures
• Rapidly eliminated
desflurane (Suprane)
• Has rapid onset and recovery
• Often used in ambulatory surgery
General Anesthesia
• Often dispensed by IV drip
• Very lipid soluble
Drug List
Injectable Anesthetics
•
•
•
•
•
•
•
etomidate (Amidate)
fentanyl (Duragesic, Sublimaze)
fentanyl-droperidol
ketamine (Ketalar)
morphine
propofol (Diprivan)
sufentanil (Sufenta)
Drug List
Injectable Anesthetics
Barbituates
– methohexital (Brevital)
– thiopental (Pentothal)
Benzodiazepines
– diazepam (Valium)
– lorazepam (Ativan)
– midazolam (Versed)
propofol (Diprivan)
• Used for maintenance of anesthesia,
sedation, or treatment of agitation
• Has antiemetic properties
–
–
–
–
Drowsiness
Respiratory depression
Motor restlessness
Increased blood pressure
Injectable Anesthesia
Dispensing Issues
Warning!
Diprivan (anesthetic) and Diflucan
(antifungal) may be confused.
This mix-up could be life-threatening.
fentanyl
• Dosage Forms
– IV (Sublimaze)
– patch (Duragesic)
– lozenge (Actiq) for children
• Used extensively for open-heart
surgery due to lack of cardiac
depression
Benzodiazepines
• Used for induction, short procedures, and
dental procedures
• Useful in controlling and preventing
seizures induced by local anesthetics
• midozolam (Versed)
– fastest onset of action
– greatest potency
– most rapid elimination
Antagonist Agents
Antagonist agents reverse
benzodiazepine and narcotic
overdose.
Drug List
Antagonist Agents
• flumazenil (Romazicon)
• nalmefene (Revex)
• naloxone (Narcan)
flumazenil (Romazicon)
• Antagonizes benzodiazepines by competing
for receptor site
• Used for complete or partial reversal
naloxone (Narcan)
• Competes for opiate receptor sites
• Has a shorter duration of action than
narcotics, so it must be given repeatedly
Neuromuscular Blocking Agents
• Causes immediate skeletal muscle
relaxation.
– Short Duration
– Intermediate Duration
– Extended Duration
• Used to facilitate endotracheal intubation.
– Allows for easier insertion of endotracheal
tube.
– Keeps airway open.
Drug List
Neuromuscular Blocking
Agents
•
•
•
•
•
•
•
atracurium (Tracrium)
cisatracurium (Nimbex)
mivacurium (Mivacron)
pancuronium
rocuronium (Zemuron)
succinylcholine (Quelicin)
vecuronium (Norcuron)
Neuromuscular Blocking Agents
Dispensing Issues
Warning!
• Very expensive
• Be conscious of storage requirements
• Store away from look-alike and drugs
succinylcholine (Quelicin)
• Often called “sux.”
• Only depolarizing agent. All others work as
competitive antagonists to ACh receptors.
• Persistent depolarization at motor endplate.
• Causes sustained, brief period of flaccid
skeletal muscle paralysis.
Reversal of Neuromuscular Blocking
Agents
• Increases the action of acetylcholine by
inhibiting acetylcholinesterase
• Used for reversal of nonpolarizing agents
Drug List
Anticholinesterase Agents
• edrophonium (Enlon)
• neostigmine (Prostigmin)
• pyridostigmine (Mestinon)
Types of Anesthesia
• General
•Local
Local Anesthesia
Relieves pain without altering
alertness or mental function.
Local Anesthesia
Variety of Dosage Forms
–
–
–
–
–
–
Topical
Superficial injection (infiltration)
Nerve block
IV
Epidural
Spinal
Discussion
Local anesthetics are classified
by their chemistry into two
classes.
What are they?
Discussion
Local anesthetics are classified by
their chemistry into two classes.
What are they?
Answer
– Esters
– Amides
Local Anesthesia
Esters
– Short acting
– Metabolized in the plasma and tissue fluids
– Excreted in urine
Local Anesthesia
Amides
– Longer acting
– Metabolized by liver enzymes
– Excreted in urine
Drug List
Local Anesthesia
Esters
• benzocaine (Americaine)
• chloroprocaine (Nesacaine)
• dyclonine (Cēpacol Maximum Strength)
• procaine (Novocain)
• tetracaine (Cēpacol Viractin, Pontocaine)
Drug List
Local Anesthesia
Amides
• bupivacaine (Marcaine)
• levobupivacaine (Chirocaine)
• lidocaine (L-M-X, Solarcaine, Xylocaine)
• lidocaine-epinephrine (Xylocaine w/ Epinephrine)
• lidocaine-prilocaine (EMLA)
• mepivacaine (Carbocaine)
Discussion
What functions are lost with
local anesthetics?
Discussion
What functions are lost with local anesthetics?
Answer
–
–
–
–
–
Pain perception
Temperature
Touch sensation
Proprioception
Skeletal muscle tone
Discussion
Under what conditions would
a local anesthetic be used over
a general anesthetic?
Discussion
Under what conditions would a local
anesthetic be used over a general
anesthetic?
Answer: It is chosen when a
well-defined area of the body is
targeted.
Pain Management
What is pain?
– A protective mechanism to warn of damage or
the presence of disease
– Part of the normal healing process
Managing pain can be a challenge.
Discussion
What are the classifications of
pain?
Discussion
What are the classifications of pain?
Answer
– Acute
– Chronic
• Nonmalignant
• Malignant
Pain Management
Acute Pain
• Associated with trauma or surgery
• Easier to manage by treating the cause
• Has a beginning and an end
Pain Management
Chronic Pain
• No end to the pain
• Patients may have a sense of helplessness and
hopelessness
• Affects different aspects of life
–
–
–
–
Physical
Psychological
Social
Spiritual
Pain Management
Chronic Nonmalignant Pain
• Cause may be diagnosed or undiagnosed
• Pain lasts for more than 3 months
• Patients may have signs and symptoms of
depression
Pain Management
Chronic Malignant Pain
• Accompanies malignant disease
• Often increases in severity with disease
progression
Major Sources of Pain
Source
Area
Involved
Characteristics
Treatment
Somatic
body
framework
throbbing,
stabbing
narcotics,
NSAIDS
Visceral
kidneys,
intestines,
liver
Nerves
aching,
throbbing,
sharp, crampy
burning,
numbing,
tingling
narcotics,
NSAIDS
Neuropathic
antidepressants,
anticonvulsants
Sympathetically overactive no pain should nerve blockers
Mediated
sympathetic be felt
system
Pain Management
Narcotic
• Pain-modulating chemical derived from
opium or is synthetically produced
• Also called opioid
• Causes insensibility or stupor
• Mainly effects on CNS and GI tract
• Lesser effects on peripheral tissues
Pain Management
Natural Opioids
• Endorphins, enkephalins, and dynorphins
• Produced by the brain in response to pain
stimuli
• When receptors are activated
– causes decreased nerve transmission
– sensation of pain is diminished
• Opioids bind to these same receptors
Discussion
What are the three effects of
narcotics?
Discussion
What are the three effects of
narcotics?
Answer
– Analgesia
– Sedation
– Euphoria and Dysphoria
Pain Management
Effects of Narcotics
• Analgesia
Reduce pain from most sources
Pain Management
Effects of Narcotics
• Analgesia
Reduce pain from most sources
• Sedation
Decrease anxiety and cause drowsiness
Pain Management
Effects of Narcotics
• Analgesia
Reduce pain from most sources
• Sedation
Decrease anxiety and cause drowsiness
• Euphoria and Dysphoria
– Can cause feelings of well-being and disquiet or
restlessness
– Potential for tolerance and dependence
Pain Management
Patient-Controlled Analgesia Pump
– Patient controls (within limits) when and how
often medication is administered
– Allows for better pain control
Pain Management
Analgesic Ladder
1. Onset of mild to moderate pain
Administer acetaminophen (APAP) or an
NSAID
Pain Management
Analgesic Ladder
1. Onset of mild to moderate pain
Administer acetaminophen (APAP) or an NSAID
2. Adequate relief is not achieved in Step 1
Administer NSAID plus a “weak” opioid
(codeine)
Pain Management
Analgesic Ladder
1. Onset of mild to moderate pain
Administer acetaminophen (APAP) or an NSAID
2. Adequate relief is not achieved in Step 1
Administer NSAID plus a “weak” opioid
(codeine)
3. Adequate relief is not achieved in Step 2
Administer a strong opioid (morphine)
Pain Management
Chronic opioid therapy has a low risk of
addiction when used appropriately.
Discussion
What is the difference between
addiction and dependence?
Pain Management
• Dependence
Physical and emotional reliance on a drug
• Addiction
Compulsive disorder
Pain Management
Symptoms of Addiction
• Preoccupation with drugs
• Refusal of medication tapers
• Strong preference for a specific opioid
• Decrease in ability to function
• Medication is typically not taken as prescribed
• Have a tendency to visit many different doctors
and pharmacies in order to get the drug(s)
Narcotic
Dispensing Issues
Warning!
Pharmacy technicians have a legal and moral
responsibility to alert pharmacist of suspected
abuse and addiction.
Pain Management
Patients are more successful overcoming
addiction if withdrawal symptoms are handled
appropriately.
Drug List
Addiction Treatment
• buprenorphine (Buprenex, Subutex)
• buprenorphine-naloxone (Suboxone)
• methadone (Dolophine)
methadone (Dolophine)
• Uses
– Detoxification
– Maintenance of narcotic addiction
• Dispensed in clinics or in hospitals
• Binds to opiate receptors without giving a
euphoric feeling
Discussion
What are the pros and cons of
methadone clinics?
Pain Management
Combinations of narcotics and nonnarcotics is
common.
– Enhances relief
– Facilitates use of lower doses
– Decreases side effects
Pain Management
Warning!
Combinations can be dangerous if the ASA or
APAP dose is overlooked.
Technicians should be aware of this risk and
assess each prescription for possible toxic doses.
Narcotic Analgesics
Varying dose requirements due to
–
–
–
–
Severity of pain
Individual response to pain
Patient’s age and weight
Presence of concomitant disease
Narcotic Analgesics
• Many different dosage forms and strengths
are available.
• Goal: Patient comfort
• Key to reaching goal: Constant
reassessment
• Side effects should be anticipated and
minimized for patient comfort
Narcotic Analgesic Side Effects
–
–
–
–
–
–
–
Mental confusion
Reduced alertness
Nausea/vomiting
Dry mouth
Constipation
Inflammatory process
Bronchial constriction
Drug List
Narcotic Analgesics
•
•
•
•
•
•
APAP-codeine (Tylenol With Codeine)
hydrocodone-APAP (Lortab, Vicodin)
hydromorphone (Dilaudid)
meperidine (Demerol)
morphine (MS Contin)
oxycodone (OxyContin)
Drug List
Narcotic Analgesics
•
•
•
•
•
•
•
oxycodone-APAP (Endocet, Percocet, Tylox)
oxycodone-ASA (Endodan, Percodan)
oxymorphone (Numorphan)
pentazocine (Talwin)
pentazocine-naloxone (Talwin NX)
propoxyphene (Darvon)
propoxyphene-APAP (Darvocet-N 100)
Narcotic Analgesic
Dispensing Issues
Warning!
• Be careful of multiple strengths.
• Lortab and Lorabid can be confused. Pay
attention to dosing schedule.
• Morphine sulfate and magnesium sulfate are
often confused.
Migraine Headaches
Migraine
– Severe, throbbing, vascular
headache
– Recurrent unilateral head pain
– Combined with neurologic and
GI disturbances
Migraine Headaches
• 90% of migraine sufferers report nausea.
• Sensitivity to light, sound, and stimulation
are also common.
Migraine Headaches
Components of classic migraine (all five not
experienced by every migraine sufferer):
–
–
–
–
–
Prodrome
Aura
Headache
Headache relief
Postdrome
Migraine Headaches
Prodrome
Symptom indicating the onset
Migraine Headaches
Aura
Subjective sensation or motor phenomenon that
precedes and marks the onset of a migraine attack
•
•
•
•
•
•
Flashing lights
Shimmering heat waves
Bright lights
Dark holes in visual fields
Blurred or cloudy vision
Transient loss of vision
Migraine Headaches
Headache and Headache Relief
Headache generally dissipates in six hours, but
may last one to two days
Migraine Headaches
Postdrome
Knowing the headache is gone
Migraine Headaches
Serotonin appears to be involved in cause.
– Decreased levels = excessive vasodilation in
cranial arteries = headache.
– By stimulating serotonin receptors,
vasoconstriction will occur thereby alleviating
the migraine.
Migraine Headaches
Causative Factors
• Diet
• Stress
• Depression
• Sleep habits
• Certain
medications
• Hormonal
fluctuations
• Atmospheric
changes
• Environmental
irritants
Migraine Headaches
Initial Treatment
• Identifying and eliminating triggers
Ex: red wine, caffeine, certain foods, bright
lights
• If attacks are still frequent, drug therapy
may be indicated
Discussion
Migraine drug therapy can be
divided into two classes. What
are they?
Discussion
Migraine therapy can be divided into two
drug classes. What are they?
Answer
– Prophylactic Therapy
– Abortive Therapy
Migraine Headaches
• Prophylactic Therapy
Attempts to prevent or reduce recurrence
• Abortive Therapy
Migraine Headaches
• Prophylactic Therapy
Attempts to prevent or reduce recurrence
• Abortive Therapy
– Treats acute migraine attacks
– Taken after headache occurs, at first sign of a
headache
Migraine Headaches
• Prophylactic Therapy
– Anticonvulsants
– Beta blockers
– Calcium channel
blockers
– Estrogen
– Feverfew
– NASAIDs
– SSRIs
– Tricyclic
antidepressants
• Abortive Therapy
– Simple analgesics
– NSAIDs
– Ergotaminecontaining
medications
– Other drugs
Drug List
Migraine Headaches
Triptans—Selective 5-HT Receptor Agonists
• almotriptan (Axert)
• eletriptan (Relpax)
• frovatriptan (Frova)
• naratriptan (Amerge)
• rizatriptan (Maxalt, Maxalt-MLT)
• sumatriptan (Imitrex)
• zolmitriptan (Zomig)
sumatriptan (Imitrex)
• Binds to serotonin receptors causing
vasoconstriction of blood vessels in the dura
• Use at first sign of headache
• Available in injection, nasal spray, and
tablet
rizatriptan (Maxalt-MLT)
• Sublingual tablet, quickly absorbed
• Has most rapid onset of action of all oral
migraine therapies
• May receive relief after 30 minutes
• Maxalt is not absorbed as quickly as
Maxalt-MLT
Drug List
Migraine Headaches
Ergot Preparations
• dihydroergotamine (D.H.E. 45, Migranal)
• ergotamine (Ergomar)
• ergotamine-caffeine (Cafergot)
Drug List
Migraine Headaches
Antiemetic Agents
• chlorpromazine (Thorazine)
• metoclopramide (Reglan)
• prochlorperazine (Compazine)
metoclopramide (Reglan)
• Reduces nausea and vomiting
• Enhances absorption of other antimigraine
products
• Metoclopramide (Reglan) and aspirin have
been prescribed together instead of using
sumatriptan (Imitrex)
Drug List
Migraine Headaches
Opiod Analgesic
• butorphanol (Stadol, Stadol NS)
Beta Blocker
• propranolol (Inderal)
butorphanol (Stadol, Stadol NS)
• Nasal spray is used more commonly than
injection
• Has analgesic properties for moderate-tosevere pain
• Can be addictive and abused
• A controlled substance in some states
Drug List
Migraine Headaches
Other
• butalbital-APAP-caffeine (Fioricet)
• butalbital-ASA-caffeine (Fiorinal)
• isometheptene-dichloralphenazone-APAP
(Midrin)
• tramadol (Ultram)
Migraine Agents
Dispensing Issues
Warning!
Tramadol and Toradol could be confused. Be
sure of which drug is being prescribed.
tramadol (Ultram)
• High success rate when given with NSAIDs
(ibuprofen)
• Has slow onset of action
• Is not a controlled substance, but has shown
potential for addiction
isometheptene-dichloralphenazineacetaminophen (Midrin)
• Has fewer side effects than ergotamines, but
may be less effective
• Combination of analgesic, sedative, and
vasoconstrictor
Discussion
What are some of the issues facing
migraine sufferers and the medication
that is used?
Discussion
What are some of the issues facing migraine
sufferers and the medication that is used?
Answer
– N/V
– 0.5-2 hour onset of action
– side effects of medications