Name: Zalameda, Erika Therese T.

Program/Year/Section: BSN 2A

Drug Diary

Antiparkinsonism
Antiparkinsonism: Anticholinergics
Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Benztropine Benztropine is an agent Used to treat - Rapid heart - Assess therapeutic effectiveness.
Mesylate with anti-muscarinic and symptoms of rate Clinical improvement may not be
(Cogentin) antihistaminic effects. Its Parkinson’s - Constipation evident for 2–3 d after oral drug is
main mechanism of disease or - Vomiting started.
action is presented by involuntary - Nausea - Monitor I&O ratio and pattern.
the selective inhibition of movements due - Dry mouth Advise patient to report difficulty in
dopamine transporters to the side effects - Confusion urination or infrequent voiding.
but it also presents of certain - Memory Dosage reduction may be indicated.
affinity for histamine and psychiatric drugs problems - Closely monitor for appearance of
muscarine receptors. (antipsychotics - Visual S&S of onset of paralytic ileus
It is widely known that such as hallucination including intermittent constipation,
benztropine is a potent chlorpromazine / - abdominal pain, diminution of bowel
inhibitor of presynaptic haloperidol). Nervousness sounds on auscultation, and
carrier-mediated - Depression distention.
dopamine transport. As - Numbness - Monitor for and report muscle
well, it is known to be an in fingers weakness or inability to move certain
analog of atropine and - Blurred muscle groups. Dosage reduction
hence, it has a large vision may be needed.
affinity for muscarinic - Dilated - Supervise ambulation and use bed
receptors M1 in the pupils side rails as necessary.
human brain. Once - Problems - Report immediately S&S of CNS
bound, benztropine with urination depression or stimulation. These
blocks the activity of the usually require interruption of drug
therapy.
 muscarinic receptors - Allergic
mainly in the striatum. reaction such
The increased as skin rash
advantage of - Abdominal
benztropine lays on the cramps
antagonism of - Tiredness
acetylcholine activity - Fever
which corrects the
imbalance between
dopamine and
acetylcholine in
Parkinson patients.
Biperiden HCI Parkinsonism is thought For use as an - Dry mouth, - Monitor BP and pulse after IV
(Akineton) to result from an adjunct in the nose, throat administration. Advise patient to
imbalance between the therapy of all - Blurred make position changes slowly and in
excitatory (cholinergic) forms of vision stages, particularly from recumbent
and inhibitory parkinsonism and - Drowsiness to upright position.
(dopaminergic) systems control of - Euphoria - Monitor for and report immediately:
in the corpus striatum. extrapyramidal - Mental confusion, drowsiness,
The mechanism of disorders Disorientation dizziness, agitation, hematuria, and
action of centrally active secondary to - Urinary decrease in urinary flow.
anticholinergic drugs neuroleptic drug retention - Assess for and report blurred vision.
such as biperiden is therapy. - Dizziness - Monitor I&O ratio and pattern.
considered to relate to - Constipation - Note: Biperiden usually reduces
competitive antagonism - Nausea muscle rigidity. In patients with
of acetylcholine at - Vomiting severe parkinsonism, tremors may
cholinergic receptors in - Agitation increase as spasticity is relieved.
the corpus striatum, - Disturbed
which then restores the behavior
balance. - Decreased
sweating
 - Difficult or
painful
urination
- Involuntary
movements
- Slow heart
rate
- Reduction in
rapid eye
movement
(REM) sleep

Antiparkinsonism: Dopaminergics
Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Carbidopa - Carbidopa is an inhibitor This combination - Anorexia - Monitor patient’s vital signs and
Levodopa of the DDC which in medication is - Nausea electrocardiogram. Orthostatic
(Sinemet) order, inhibits the used to treat - Vomiting hypotension may occur during early
peripheral metabolism of symptoms of - Dysphagia use of levodopa and bromocriptine.
levodopa. Parkinson’s - Fatigue Instruct patient to rise slowly to avoid
DDC is very important in disease or - Dizziness faintness.
the biosynthesis of L- Parkinson-like - Headache - Observe for weakness, dizziness,
tryptophan to serotonin symptoms (such - Dry Mouth or syncope, which are symptoms of
and the modification of as shakiness, - Bitter taste orthostatic hypotension.
L-DOPA to dopamine. stiffness, difficulty - Twitching - Administer carbidopa-levodopa
DDC can be found in the moving). - Blurred (Sinemet) with low- protein foods.
body periphery and in Parkinson’s vision High-protein diets interfere with drug
the blood-brain barrier. disease is thought - Insomnia transport to the CNS.
The action of carbidopa to be caused by - Dark urine - Observe for symptoms of
is focused on peripheral too little of a parkinsonism.
DDC as this drug cannot naturally - Urge patient not to abruptly
cross the blood-brain occurring discontinue the medication.
barrier. Hence, it will substance Rebound parkinsonism (increased
prevent the metabolism (dopamine) in the
 of levodopa in the brain. Levodopa symptoms of parkinsonism) can
periphery but it will not changes into occur.
have any activity on the dopamine in the - Inform patient that urine may be
generation of dopamine brain, helping to discolored and will darken with
in the brain. control exposure to air. Perspiration also
Levodopa by various movement. may be dark. Explain that both are
routes crosses the blood Carbidopa harmless but clothes may be stained.
brain barrier, is prevents the - Advise patient to avoid chewing or
decarboxylated to form breakdown of crushing extended- release tablets.
dopamine. This levodopa in the
supplemental dopamine bloodstream so
performs the role that more levodopa
endogenous dopamine can enter the
cannot due to a brain. Carbidopa
decrease of natural can also reduce
concentrations and some of
stimulates dopaminergic levodopa's side
receptors. effects such as
nausea and
vomiting.

Antiparkinsonism: Dopamine Agonists

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Amantadine HCI The mechanism of its For the - Nausea - Monitor effectiveness. Note that
(Symmetrel) antiparkinsonic effect is chemoprophylaxi - Stomach with parkinsonism, maximum
not fully understood, but s, prophylaxis, upset response occurs within 2 weeks–3
it appears to be and treatment of - Diarrhea mo. Effectiveness may wane after 6–
releasing dopamine from signs and - Constipation 8 weeks of treatment; report change
the nerve endings of the symptoms of - Loss of to physician.
brain cells, together with infection caused appetite - Monitor and report: Mental status
stimulation of by various strains - Dizziness changes; nervousness, difficulty
norepinephrine of influenza A - Drowsiness concentrating, or insomnia; loss of
response. It also has virus. Also for the - Headache seizure control; S&S of toxicity,
 NMDA receptor treatment of - Sleep especially with doses above 200
antagonistic effects. The parkinsonism and problems mg/d.
antiviral mechanism drug-induced (Insomnia) - Establish a baseline profile of the
seems to be unrelated. extrapyramidal - Strange patient's disabilities to accurately
The drug interferes with reactions. dreams differentiate disease symptoms and
a viral protein, M2 (an - Nervous drug-induced neuropsychiatric
ion channel), which is feeling adverse reactions.
needed for the viral - Dry mouth - Monitor vital signs for at least 3 or 4
particle to become - Dry nose d after increases in dosage; also
"uncoated" once it is - Blurred monitor urinary output.
taken inside the cell by vision - Lab tests: pH and serum
endocytosis. - Loss of electrolytes.
balance or - Monitor for and report reduced
coordination salivation, increased akinesia or
rigidity, and psychological
disturbances that may develop within
4–48 h after initiation of therapy and
after dosage increases with
parkinsonism.
Bromocriptine The dopamine For the treatment - Dizziness - Monitor vital signs closely during
Mesylate D2 receptor is a 7- of galactorrhea - Spinning the first few days and periodically
(Parlodel) transmembrane G- due to sensation throughout therapy.
protein coupled receptor hyperprolactinemi - Mild - Lab tests: Periodic CBC, liver
associated with a, prolactin- drowsiness functions and renal functions with
Gi proteins. In dependent - Tiredness prolonged therapy.
lactotrophs, stimulation menstrual - Mild - Monitor for and report psychotic
of dopamine D2 receptor disorders and headache symptoms and other adverse
causes inhibition of infertility, - Depressed reactions in Parkinson's patients
adenylyl cyclase, which prolactin- mood because larger doses are used.
decreases intracellular secreting - Sleep - Improvement in Parkinson's
cAMP concentrations adenomas, problems disease may be noted in 30–90 min
and blocks IP3- prolactin- (Insomnia) following administration of
dependent release of dependent male - Dry mouth
Ca2+ from intracellular hypogonadism, - Stuffy nose bromocriptine, with maximum effect
stores. Decreases in as adjunct - Upset in 2 hours.
intracellular calcium therapy to surgery stomach - Make position changes slowly and
levels may also be or radiotherapy - Nausea in stages, especially from lying down
brought about via for acromegaly or - Vomiting to standing, and to dangle legs over
inhibition of calcium as monotherapy - Stomach bed for a few minutes before walking.
influx through voltage- is special cases, pain Lie down immediately if light-
gated calcium channels, as monotherapy - Loss of headedness or dizziness occurs.
rather than via inhibition in early appetite - Do not drive or engage in other
of adenylyl cyclase. Parkinsonian - Diarrhea potentially hazardous activities until
Additionally, receptor Syndrome or as - Constipation response to drug is known.
activation blocks an adjunct with - Cold feeling - Avoid exposure to cold and report
phosphorylation of levodopa in or numbness the onset of pallor of fingers or toes.
p42/p44 MAPK and advanced cases in your fingers - Note: Patients taking bromocriptine
decreases MAPK/ERK with motor to suppress postpartum lactation
kinase phosphorylation. complications. may have temporary rebound breast
Inhibition of MAPK Bromocriptine enlargement and pain following drug
appears to be mediated has also been withdrawal.
by c-Raf and B-Raf- used off-label to
dependent inhibition of treat restless legs
MAPK/ERK kinase. syndrome and
Dopamine-stimulated neuroleptic
growth hormone release malignant
from the pituitary gland is syndrome.
mediated by a decrease
in intracellular calcium
influx through voltage-
gated calcium channels
rather than via adenylyl
cyclase inhibition.
Stimulation of dopamine
D2 receptors in the
nigrostriatal pathway
 leads to improvements in
coordinated muscle
activity in those with
movement disorders.

Antiparkinsonism: MAO-B Inhibitors

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Selegiline HCI Although the Monotherapy for - Abnormal, - Monitor vital signs, particularly
(Eldepryl) mechanisms for initial treatment of involuntary during period of dosage adjustment.
selegiline's beneficial Parkinson's movements Report alterations in BP or pulse.
action in the treatment of disease, as well - Nausea Indications for discontinuation of the
Parkinson's disease are as an adjunct - Abdominal drug include orthostatic hypotension,
not fully understood, the therapy in pain hypertension, and arrhythmias.
selective, irreversible patients with a - Dry mouth - Monitor all patients closely for
inhibition of monoamine decreased - Fainting behavior changes (e.g.,
oxidase type B (MAO-B) response to - Irregular hallucinations, confusion,
is thought to be of levodopa/carbido heartbeats depression, delusions).
primary importance. pa. Also used for - Confusion - Do not exceed the prescribed drug
MAO-B is involved in the the palliative - Generalized dose.
oxidative deamination of treatment of mild pain - Report symptoms of MAO inhibitor-
dopamine in the brain. to moderate - Headache induced hypertension (e.g., severe
Selegiline binds to MAO- Alzheimer's - headache, palpitations, neck
B within the nigrostriatal disease and at Hypertension stiffness, nausea, vomiting)
pathways in the central higher doses, for - Sleep immediately to physician.
nervous system, thus the treatment of problems - Do not drive or engage in potentially
blocking microsomal depression. (Insomnia) hazardous activities until response to
metabolism of dopamine - Mood drug is known.
and enhancing the changes - Make positional changes slowly and
dopaminergic activity in - Dizziness on in stages. Orthostatic hypotension is
the substantial nigra. standing possible as well as dizziness, light-
Selegiline may also - Urinary headedness, and fainting.
increase dopaminergic retention - Do not breast feed while taking this
activity through - Vomiting drug without consulting physician.
 mechanisms other than - Heartburn
inhibition of MAO-B. At - Diarrhea
higher doses, selegiline - Constipation
can also inhibit - Weakness
monozmine oxidase - Runny or
type A (MAO-A), stuffy nose
allowing it to be used for - Back pain
the treatment of - Mouth sores
depression. or ulcers
- Pain with
swallowing
Rasagiline The precise For the treatment - Depressed - Monitor for new onset hypertension
(Azilect) mechanisms of action of of the signs and mood or hypertension that is not
Rasagiline is unknown. symptoms of - Sleep adequately controlled after starting
One mechanism is idiopathic problems therapy.
believed to be related to Parkinson’s (Insomnia) - Avoid tyramine-rich foods
its MAO-B inhibitory disease as initial - Strange - Monitor for drowsiness or
activity, which causes an monotherapy and dreams sleepiness
increase in extracellular as adjunct - Involuntary - Mild hepatic impairment: reduce
levels of dopamine in the therapy to muscle dose; moderate to severe hepatic
striatum. The elevated levodopa. movements impairment (Child-Pugh score ≥7):
dopamine level and - Loss of not recommended
subsequent increased appetite - Monitor for hallucinations, psychotic
dopaminergic activity - Weight loss or compulsive behaviors; consider
are likely to mediate - Indigestion reduce dose or discontinue if
rasagiline's beneficial - Stomach develops.
effects seen in models of pain - Monitor for melanoma
dopaminergic motor - Nausea
dysfunction. - Vomiting
- Constipation
- Joint pain or
stiffness
- Rash
 - Cough
- Flu
symptoms
- Dry mouth
- Swelling in
your hands or
feet

Antiparkinsonism: COMT Inhibitors

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Tolcapone The precise mechanism Used as an - Sleep Lab tests: Monitor liver functions
(Tasmar) of action of tolcapone is adjunct to disturbances monthly for first 3 months, every 6
unknown, but it is levodopa/carbido - Excessive weeks for the next 3 months, and
believed to be related to pa therapy for the dreaming periodically thereafter.
its ability to inhibit COMT symptomatic - Diarrhea Monitor PT and INR carefully when
and alter the plasma treatment of - Dizziness given concurrently with warfarin.
pharmacokinetics of Parkinson's - Vomiting Monitor carefully for and immediately
levodopa, resulting in an Disease. This - Increased report S&S of hepatic impairment
increase in plasma drug is generally sweating (e.g., jaundice, dark urine).
levodopa reserved for - Do not engage in hazardous
concentrations. The patients with Hallucination activities until response to drug is
inhibition of COMT also parkinsonian s known. Avoid use of alcohol or
causes a reduction in syndrome - Confusion sedative drugs while on tolcapone.
circulating 3-OMD as a receiving - Irregular Rise slowly from a sitting or lying
result of decreased levodopa/carbido heartbeat position to avoid a rapid drop in BP
peripheral metabolism of pa who are with possible weakness or fainting.
levodopa. This may lead experiencing Nausea is a common possible
to an increase symptom adverse effect especially at the
distribution of levodopa fluctuations and beginning of therapy.
into the CNS through the are not Do not suddenly stop taking this
reduction of its responding drug. Doses must be gradually
competitive substrate, 3- adequately to or reduced over time.
OMD, for transport are not
 mechanisms. Sustained candidates for Notify physician promptly about any
levodopa concentrations other adjunctive of following: Increased loss of muscle
presumably result in therapies. control, fainting, yellowing of skin or
more consistent eyes, darkening of urine, severe
dopaminergic diarrhea, hallucinations.
stimulation, resulting in
greater reduction in the
manifestations of
parkinsonian syndrome.
Entacapone The mechanism of Used as an - Nausea - Monitor carefully for hyperpyrexia,
(Comtan) action of entacapone is adjunct to - Vomiting confusion, or emergence of
believed to be through its levodopa / - Diarrhea Parkinson's S&S during drug
ability to inhibit COMT in carbidopa in the - Constipation withdrawal.
peripheral tissues, symptomatic - Unwanted / - Monitor for orthostatic hypotension
altering the plasma treatment of uncontrolled & worsening of dyskinesia or
pharmacokinetics of patients with movements hyperkinesia.
levodopa. When idiopathic - Increased - Lab tests: Hgb and serum ferritin
entacapone is given in Parkinson's sweating levels with prolonged therapy.
conjunction with Disease who - Drowsiness - Take with levodopa/carbidopa; not
levodopa and an experience the - Dizziness effective alone.
aromatic amino acid signs and - - Do not discontinue abruptly;
decarboxylase inhibitor, symptoms of end- Lightheadedn gradually reduce dosage.
such as carbidopa, of-dose "wearing- ess upon - Exercise caution when rising from a
plasma levels of off". standing sitting or lying position because
levodopa are greater - Tiredness faintness/dizziness can occur.
and more sustained than - Dry mouth - Exercise caution with hazardous
after administration of - Gas activities until reaction to the drug is
levodopa and an - Abdominal known.
aromatic amino acid or stomach - Harmless brownish-orange
decarboxylase inhibitor pain discoloration of urine is possible.
alone. It is believed that - Back pain - Report unusual adverse effects
at a given frequency of (e.g., hallucinations/unexplained
levodopa administration, diarrhea).
these more sustained - Brownish
plasma levels of orange
levodopa result in more colored urine
constant dopaminergic - Falling
stimulation in the brain, asleep
leading to a greater
reduction in the
manifestations of
parkinsonian syndrome.
 Muscle Relaxant

Muscle Relaxant: Centrally – Acting Muscle Relaxants

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Baclofen Baclofen is an effective Baclofen is - Drowsiness - Supervise ambulation. Initially, the
(Lioresal) and widely used administered for - Dizziness loss of spasticity induced by baclofen
antispastic agent with a the relief of signs - Weakness may affect patient's ability to stand or
spinal site of action. Its and symptoms of - Tiredness walk.
mechanism of action and spasticity - Headache - Lab tests: baseline and periodic BP,
pharmacological resulting from - Trouble weight, blood sugar, hepatic function
properties are different multiple sclerosis, sleeping tests, and urine.
from the effects of other particularly for the - Nausea - Monitor for adverse neuropsychiatric
antispastic agents. In relief of flexor - Increased or genitourinary symptoms that
addition, baclofen has spasms and urination resemble those of the underlying
central sites of action, associated pain - Constipation disease. Assess them carefully and
shown by its adverse and clonus, in report to the physician.
event profile and general addition to - Observe carefully for side effects:
CNS depressant muscular rigidity. mental confusion, depression,
properties. GABA-B Patients receiving hallucinations. Older adults are
receptors interact with this drug should especially sensitive to this drug.
signal transduction have reversible - Monitor patients with epilepsy closely
pathways and spasticity for for possible loss of seizure control.
neurotransmitter baclofen to
systems. Baclofen promote the
exerts an antinociceptive restoration of
effect. The clinical residual function.
significance of this This drug is not
warrants further indicated in the
research data for treatment of
clarification. Baclofen skeletal muscle
depresses spasm caused by
monosynaptic and rheumatic
polysynaptic reflex disorders. The
 transmission, by various efficacy of
actions, and possibly baclofen in
including the stimulation stroke, cerebral
of GABAβ-receptors. palsy, and
This stimulation results Parkinson's
in the inhibition of disease has not
excitatory been determined
neurotransmitter and, therefore,
(glutamate and baclofen is not
aspartate) release, recommended for
which may normally these conditions
contribute to pain and
spasticity. Although
baclofen is an analog of
the inhibitory
neurotransmitter
gamma-amino-butyric
acid (GABA), there are
no conclusive data
indicating GABA
systems are involved in
its clinical effects.
Cyclobenzaprine The exact mechanism of Cyclobenzaprine - Blurred - Monitor serum liver enzyme levels of
(Flexeril) action of is indicated as a vision patients taking dantrolene and
cyclobenzaprine has not short-term (2-3 - Constipation carisoprodol. Report elevated levels of
been fully elucidated in weeks) adjunct - Dry mouth liver enzymes such as alkaline
humans, and much of therapy, along - Tachycardia phosphatase (ALP), alanine
the information available with rest and - Urinary aminotransferase (ALT), and gamma-
regarding its mechanism physical therapy, retention glutamyl transferase (GGT).
has been ascertained for relief of muscle - Drowsiness - Record vital signs. Report abnormal
from early animal spasm associated - Dizziness results.
studies. There is some with acute, painful - Headache - Observe for CNS side effects (e.g.,
evidence that musculoskeletal - Fever dizziness).
cyclobenzaprine exerts conditions. It has - Abdominal - Teach patient that the muscle
its effects at the not been found pain relaxant should not be abruptly
supraspinal level, effective in the - Vomiting stopped. Drug should be tapered over
specifically within the treatment of - Diarrhea 1 week to avoid rebound spasms.
locus coeruleus of the spasticity - Flatulence - Advise patient not to drive or operate
brainstem, with little-to- originating from - Erectile dangerous machinery when taking
no action at cerebral or spinal dysfunction muscle relaxants. These drugs have a
neuromuscular junctions cord disease, or sedative effect and can cause
or directly on skeletal spasticity in drowsiness.
musculature. Action on children with - Inform patient that most of the
the brainstem is thought cerebral palsy. centrally acting muscle relaxants for
to result in diminished Cyclobenzaprine acute spasms are usually taken for no
activity of efferent alpha is also longer than 3 weeks.
and gamma motor occasionally used - Teach patient to avoid alcohol and
neurons, likely mediated off-label for CNS depressants. If muscle relaxants
by inhibition of reducing pain and are taken with these drugs, CNS
coeruleus-spinal or sleep depression may be intensified.
reticulospinal pathways, disturbances in - Advise patient that these drugs must
and ultimately patients with be used cautiously for pregnant or
depressed spinal cord fibromyalgia. nursing patients. Check with health
interneuron activity. care provider.
More recently it has
been suggested that
inhibition of descending
serotonergic pathways
in the spinal cord via
action on 5-HT2
receptors may contribute
to cyclobenzaprine’s
observed effects.
Muscle Relaxant: Direct – Acting Muscle Relaxants
Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Dantrolene Dantrolene depresses For use, along - Muscle - Monitor for therapeutic effectiveness.
Sodium excitation-contraction with appropriate weakness Improvement may not be apparent
(Dantrium) coupling in skeletal supportive - Drowsiness until 1 week or more of drug therapy.
muscle by binding to the measures, for the - Dizziness - Monitor vital signs during IV infusion.
ryanodine receptor 1, management of - Low energy Also monitor ECG, CVP, and serum
and decreasing the fulminant - Tired feeling potassium.
intracellular calcium hypermetabolism - Injection site - Supervise ambulation until patient's
concentration. of skeletal muscle reactions reaction to drug is known. Relief of
Ryanodine receptors characteristic of (Pain, spasticity may be accompanied by
mediate the release of malignant redness or some loss of strength.
calcium from the hyperthermia swelling) - Note: Most common adverse effects
sarcoplasmic reticulum, crises in patients - Diarrhea are generally transient, lasting up to 14
an essential step in of all ages. Also - Constipation d after initiation of therapy. Keep
muscle contraction. used -Nausea physician informed.
preoperatively, - Vomiting - Monitor patients with impaired
and sometimes - Stomach cardiac or pulmonary function closely
postoperatively, pain for cardiovascular or respiratory
to prevent or - Problems symptoms such as tachycardia, BP
attenuate the with speech changes, feeling of suffocation.
development of - Difficulty - Monitor for and report symptoms of
clinical and with balance allergy and allergic pleural effusion:
laboratory signs or walking Shortness of breath, pleuritic pain, dry
of malignant - Headache cough.
hyperthermia in - Confusion - Alert physician if improvement is not
individuals judged - Vision evident within 45 d. Drug may be
to be malignant problems discontinued because of the possibility
hyperthermia - Sleep of hepatotoxicity (see Appendix F).
susceptible. problems - Lab tests: Perform baseline and
(Insomnia) regularly scheduled hepatic function
- Sweating tests (alkaline phosphatase, AST,
- Drooling
- Urinating ALT, total bilirubin), blood cell counts,
more than and renal function tests.
usual - Monitor bowel function. Persistent
diarrhea may necessitate drug
withdrawal. Severe constipation with
abdominal distention and signs of
intestinal obstruction have been
reported.
 Narcotics

Narcotics: Narcotic Agonists

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Morphine Morphine-6-glucuronide Used for the - Drowsiness - Assess the source, quality, and
(Roxanol, is responsible for management of - Dizziness severity of the patient’s pain and keep
Astomorph) approximately 85% of chronic, moderate - Tiredness in mind that pain is a subjective
the response observed to severe pain. - Constipation experience. A patient’s report of pain
by morphine Opioids, including - Stomach should be believed.
administration. Morphine morphine, are pain - Use non-opioid analgesics when
and its metabolites act effective for the - Nausea possible.
as agonists of the mu short term - Vomiting - Giving an opioid along with a non-
and kappa opioid management of - Sweating opioid may increase analgesic effects
receptors. The mu- pain. Patients - Feelings of and allow a lower dose of opioid to be
opioid receptor is taking opioids extreme given.
integral to morphine's long term may happiness or - Monitor the patient’s vital signs and
effects on the ventral need to be sadness mental status regularly. Report if the
tegmental area of the monitored for the pulse is below 50 beats per minute in
brain. Morphine's development of adults or 110 beats per minute in
activation of the reward physical infants.
pathway is mediated by dependence, - Monitor for decreased respirations.
agonism of the delta- addiction - Opioids may decrease the patient’s
opioid receptor in the disorder, and cough reflex. Therefore, it is important
nucleus accumbens, drug abuse. to have the patient turn, cough, and
while modification of the deep breath regularly to prevent
respiratory system and atelectasis.
addiction disorder are - Give the opioid drug at least 30-60
mediated by agonism of minutes prior to activities or painful
the mu-opioid receptor. procedures.
- Monitor the patient closely when an
opioid is given as sedation for a painful
procedure.
 - Opioids may also cause urinary
retention. Monitor the patient’s intake
and output, palpate the suprapubic
area of the abdomen for bladder
distention, ask the patient about any
voiding problems, pain in the bladder
area, a sensation of not completely
emptying the bladder, or any unusual
odors in the urine.
- If the patient is confined to bed, use
side rails and safety measures to
prevent a fall when receiving opioids.
Provide assistance with ambulation
and transfers.
Meperidine Meperidine is primarily a A prescription - - May cause alterations in mentation,
(Demerol) kappa-opiate receptor medicine used to Lightheadedn hypotension, constipation, nausea,
agonist and also has treat the ess vomiting
local anesthetic effects. symptoms of - Dizziness - Assess BP, pulse, and respiratory
Meperidine has more moderate to - Weakness rate prior to administration and
affinity for the kappa- severe pain. - Headache frequently during administration
receptor than morphine. Demerol may be - Extreme - Use caution if patient is receiving
Opiate receptors are used alone or with calm MAOIs
coupled with G-protein other - Mood - Narcan (naloxone) is the antidote for
receptors and function medications. changes opioid agonists
as both positive and Demerol belongs - Nausea - Can cause seizure
negative regulators of to a class of drugs - Vomiting - May increase pancreatic enzyme
synaptic transmission called Synthetic, - Stomach levels
via G-proteins that Opioids, Opioid pain or - Assess bowel function
activate effector Analgesics. cramps
proteins. Binding of the - Constipation
opiate stimulates the - Dry mouth
exchange of GTP for - Flushing
GDP on the G-protein - Sweating
complex. As the effector - Changes in
system is adenylate vision
cyclase and cAMP - Tremors
located at the inner - Loss of
surface of the plasma appetite
membrane, opioids - Seizure
decrease intracellular - Breathing
cAMP by inhibiting that stops
adenylate cyclase. during sleep
Subsequently, the
release of nociceptive
neurotransmitters such
as substance P, GABA,
dopamine, acetylcholine
and noradrenaline is
inhibited. Opioids also
inhibit the release of
vasopressin,
somatostatin, insulin and
glucagon. Opioids close
N-type voltage-operated
calcium channels (OP2-
receptor agonist) and
open calcium-dependent
inwardly rectifying
potassium channels
(OP3 and OP1 receptor
agonist). This results in
hyperpolarization and
reduced neuronal
excitability.
Narcotics: Narcotic Agonist – Antagonist
Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Pentazocine The preponderance of Used to relieve - Nausea - Monitor therapeutic effect. Tolerance
(Talwin) evidence suggests that moderate to - Dizziness to analgesic effect sometimes occurs.
pentazocine severe pain. - Psychologic and physical dependence
antagonizes the opioid Pentazocine is in Lightheadedn have been reported in patients with
effects by competing for a class of ess history of drug abuse, but rarely in
the same receptor sites, medications - Vomiting patients without such history.
especially the opioid mu called opiate - Euphoria Addiction liability matches that of
receptor. (narcotic) - Injection site codeine.
analgesics. It reactions - Be aware that pentazocine may
works by - Hard lump produce acute withdrawal symptoms
changing the way - Skin in some patients who have been
the brain and dimpling receiving opioids on a regular basis.
nervous system - Ulceration
respond to pain. - Sweating
- Flushing
- Itching
- Shortness of
breath
-
Hallucination
s
- Sleepiness
- Headache
- Confusion
-
Disorientation
Nalbuphine Nalbuphine is a kappa- Nalbuphine is - Flushing - Assess respiratory rate before drug
(Nubain) opioid receptor agonist FDA indicated for (warmth, administration. Withhold drug and
and a partial mu-opioid moderate to tingling, notify physician if respiratory rate falls
receptor antagonist. severe pain in redness) below 12.
Analgesic properties are where the patient - Nausea
mediated through requires an opioid - Vomiting - Watch for allergic response in
agonist activity at agent, and other - Stomach persons with sulfite sensitivity.
the kappa-opioid alternative cramps or - Administer with caution to patients
receptor. Because of this treatments have pain with hepatic or renal impairment.
unique mixed agonist- been insufficient. - Upset - Monitor ambulatory patients;
antagonist opioid Non-FDA stomach nalbuphine may produce drowsiness.
receptor activity of approved uses of - Dizziness - Watch for respiratory depression of
nalbuphine, it provides nalbuphine - Spinning newborn if drug is used during labor
analgesia with less do exist such as sensation and delivery.
nausea, pruritus, and treatment of labor - Dry mouth - Avoid abrupt termination of
respiratory depression pain, opioid- - Bitter or nalbuphine following prolonged use,
when compared to induced urinary unpleasant which may result in symptoms similar
morphine. retention, opioid- taste in your to narcotic withdrawal: nausea,
induced mouth vomiting, abdominal cramps,
respiratory - Sweating lacrimation, nasal congestion,
depression, and - Skin itching piloerection, fever, restlessness,
pruritus or burning anxiety.
associated with sensation
neuraxial opioid - Rash
use. - Headache
-
Nervousness
-
Restlessness
- Depression
- Strange
dreams
- Slurred
speech
- Blurred
vision
Narcotics: Narcotic Antagonist
Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Naloxone Naloxone is a Naloxone nasal - Flushing - Observe patient closely; duration of
(Narcan) competitive inhibitor of sprays are - Dizziness action of some narcotics may exceed
the µ-opioid receptor. indicated for the - Tiredness that of naloxone. Keep physician
Naloxone antagonizes emergency - Weakness informed; repeat naloxone dose may
the action of opioids, treatment of an - be necessary.
reversing their effects. If opioid overdose Nervousness - May precipitate opiate withdrawal if
a patient has not taken or suspected - administered to a patient who is opiate
opioids, naloxone does opioid overdose. Restlessness dependent.
not have a significant Intramuscular, - Irritability - Note: Narcotic abstinence symptoms
effect on patients. intravenous, and - Body aches induced by naloxone generally start to
subcutaneous - Diarrhea diminish 20–40 min after
injections are - Stomach administration and usually disappear
indicated for pain within 90 min.
complete or - Nausea - Monitor respirations and other vital
partial reversal of - Fever signs.
opioid - Chills - Monitor surgical and obstetric
depression, - patients closely for bleeding.
diagnosis of Goosebumps Naloxone has been associated with
known or - Sneezing abnormal coagulation test results.
suspected opioid - Shortness of Also observe for reversal of analgesia,
overdose, and as breath which may be manifested by nausea,
an adjunct - Runny nose vomiting, sweating, tachycardia.
therapy in the
treatment of
septic shock.
Sublingual tablets
and films are
formulated with
buprenorphine for
the treatment of
opioid
 dependence.
Naloxone is also
formulated with
pentazocine as
an oral tablet for
severe pain.
Naloxone has
been used off-
label for the
treatment of
neuraxial opioid-
induced pruritus.
Naltrexone Naltrexone is a pure Used as an - Nausea - Lab tests: Check liver function before
(Re Via) opiate antagonist and adjunct to a - Headache the treatment is started, at monthly
has little or no agonist medically - Dizziness intervals for 6 months, and then
activity. The mechanism supervised - periodically as indicated.
of action of naltrexone in behavior Nervousness - Note: Naltrexone therapy may put
alcoholism is not modification - Fatigue you in danger of overdosing if you use
understood; however, program in the - Insomnia opiates. Small doses even at frequent
involvement of the maintenance of - Vomiting intervals will give no desired effects;
endogenous opioid opiate cessation - Anxiety however, a dose large enough to
system is suggested by in individuals who - Drowsiness produce a high is dangerous and may
preclinical data. were formerly be fatal.
Naltrexone is thought to physically - It may be possible to transfer from
act as a competitive dependent on methadone to naltrexone. This can be
antagonist at mc, κ, and opiates and who done after gradual withdrawal and
δ receptors in the CNS, have successfully final discontinuation of methadone.
with the highest affinity undergone - Report promptly onset of signs of
for the μ receptor. detoxification. hepatic toxicity (see Appendix F) to
Naltrexone competitively Also used for the physician. The drug will be
binds to such receptors management of discontinued.
and may block the alcohol - Do not self-dose with OTC drugs for
effects of endogenous dependence in treatment of cough, colds, diarrhea, or
opioids. This leads to the conjunction with a analgesia. Many available
antagonization of most behavioral preparations contain small doses of an
of the subjective and modification opioid. Consult physician for safe
objective effects of program. drugs if they are needed.
opiates, including - Tell a doctor or dentist before
respiratory depression, treatment that you are using
miosis, euphoria, and naltrexone.
drug craving. The major - Wear identification jewelry indicating
metabolite of naltrexone, naltrexone use.
6-β-naltrexol, is also an - Do not breast feed while taking this
opiate antagonist and drug without consulting physician.
may contribute to the
antagonistic activity of
the drug.
 Anti-Migraine

Anti – Migraine: Ergot Derivatives

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Ergotamine Ergotamine acts on For use as - Nausea - Monitor adverse GI effects. Nausea
Tartrate migraine by one of two therapy to abort - Vomiting and vomiting are adverse reactions
(Ergomar) proposed mechanisms: or prevent - Dizziness that occur in about 10% of patients
1) activation of 5- vascular - Spinning after they take ergotamine. Patient
HT1D receptors located headache, e.g., sensation may need an antiemetic. Consult with
on intracranial blood migraine, - Weakness physician.
vessels, including those migraine variants, - Itching - Monitor patients with PVD carefully
on arterio-venous or so called for development of peripheral
anastomoses, leads to "histaminic ischemia.
vasoconstriction, which cephalalgia". - Monitor long-term effectiveness.
correlates with the relief Patients receiving high ergotamine
of migraine headache, doses for prolonged periods may
and 2) activation of 5- experience increased frequency of
HT1D receptors on headaches, fatigue, and depression.
sensory nerve endings Discontinuation of the drug in these
of the trigeminal system patients results in severe withdrawal
results in the inhibition of headache that may last a few days.
pro-inflammatory - Overdose symptoms: Nausea,
neuropeptide release. vomiting, weakness and pain in legs,
numbness and tingling in fingers and
toes, tachycardia or bradycardia,
hypertension or hypotension, and
localized edema.
Dihydroergotamine DHE has several Dihydroergotamin - Nasal - Monitor cardiac status, especially
(Migranal) proposed mechanisms e (DHE) in all congestion or when large doses are given.
which may contribute to formulations is irritation - Monitor for and report numbness and
its therapeutic efficacy indicated for the - Changes in tingling of fingers and toes, extremity
as an abortive therapy in acute treatment of your sense of weakness, muscle pain, or intermittent
migraines. Firstly, DHE's migraine with or taste claudication.
s agonist action on 5- without aura in - Sore throat - Take at first warning of migraine
hydroxytryptamine adults. As an - Nausea headache.
(5HT) 1b receptors in the injection, DHE is - Vomiting - Lie down in a quiet, darkened room
smooth muscle of the also indicated for - Dizziness for several hours after drug
cranial vasculature may the acute - Fatigue administration for best results.
provide relief via treatment of - Runny or - Report immediately if any of the
vasoconstriction of the cluster headache stuffy nose following S&S develop: Chest pain,
blood vessels which episodes. - Nosebleeds nausea, vomiting, change in
typically become dilated DHE is not - Headache heartbeat, numbness, tingling, pain or
due to the release of indicated for - Drowsiness weakness of extremities, edema, or
CGRP during migraine migraine - Anxiety itching.
attacks. DHE's off-target prevention or the - Depression - Do not breast feed while taking this
action at alpha- management of - Cold sweats drug without consulting physician.
adrenergic receptors hemiplegic or - Pain,
may further contribute basilar migraine. soreness,
via this mechanism. The burning,
remaining mechanisms tingling or
are thought to provide dryness in
relief through the effects your nose or
on the neurogenic throat
causes of migraine
symptoms. Agonist
action by DHE on 5-
HT1b and 5-
HT1d receptors inhibits
nociceptive signaling
through the
ventroposteromedial
thalamus to the
trigeminal sensory
neurons. Further action
on 5-HT1b and 5-
HT1d receptors with the
addition of agonist
activity on 5-HT1f in the
trigeminal nucleus
caudalis decreases
afferent signaling to
trigeminal sensory
neurons which
contributes to central
sensitization. The
success of experimental
compounds selectively
targeting the 5-
HT1f receptor lends
support to this
mechanism. Lastly,
action at 5-
HT1d receptors on
trigeminal nerve
terminals inhibits the
release of vasoactive
neuropeptides thought
to contribute to pain and
inflammation during a
migraine attack. DHE is
known to have 10-fold
less potency at the 5-
HT1b receptor than its
predecessor ergotamine
which reduces the
incidence of vascular
side effects.
Anti – Migraine: Triptans
Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Sumatriptan Sumatriptan is an indicated for the - Mild - Assess for side-effects of tingling,
(Imitrex) agonist of 5-HT1B and treatment of headache burning, numbness, flushing or feeling
5-HT1D. This agonism migraines with or (not a of pressure.
leads to constriction of without auras in migraine) - Assess stress level and
cranial blood vessels patients 12 years - Pain or mechanisms for coping with migraine.
and inhibits the release of age and older. chest - Assess avoidance of factors
of pro-inflammatory Sumatriptan tightness predisposing to migraine, such as
neuropeptides. nasal powder, - Pressure or caffeine and chocolate, and give
Sumatriptan decreases nasal spray, heavy feeling appropriate advice.
carotid arterial blood subcutaneous in any part of - Provide a calm environment during
flow, but increases blood injection, and your body migraine attack.
flow velocity in the tablets are - Weakness - Assess therapeutic response and
internal carotid artery indicated to treat - Feeling hot need for second dose.
and middle cerebral migraines with or or cold
artery. without auras in - Dizziness
adults. One of the - Spinning
subcutaneous sensation
formulations of - Drowsiness
sumatriptan is - Nausea
also indicated to - Vomiting
treat cluster - Drooling
headaches in - Unusual
adults, while the taste in your
other mouth after
subcutaneous using nasal
formulation is not. spray
-
Burning/num
bness/pain/irr
itation in your
nose or throat
 after using
nasal spray
- Flushing
(warmth,
redness or
tingling under
the skin)
Zolmitriptan Zolmitriptan blocks both Indicated for the - Dizziness - Monitor for therapeutic effectiveness:
(Zomig) vascular phenomena. Its acute treatment of - Numbness Relief or reduction of migraine pain
agonist action upon the migraine with or and tingling within 1–4 h.
5-HT1D receptor ends without auras in - Weakness - Monitor cardiovascular status
the aseptic inflammation patients aged 18 - Drowsiness carefully following first dose in patients
by inhibiting the release and over. - Warm or at risk for CAD (e.g., postmenopausal
of vasoactive peptides. cold women, men >40 y, persons with
The dilatation of sensation known CAD risk factors) or coronary
meningeal vessels - Nausea artery vasospasms.
disappears due to the - Heaviness - Perform periodic cardiovascular
stimulation of sensation evaluation and ECG with long-term
zolmitriptan of 5-HT1B - Dry mouth use.
receptors. As this drug - Indigestion - Report to physician immediately
crosses the blood brain - Difficulty chest pain, nausea, or tightness in
barrier, zolmitriptan has swallowing chest or throat that is severe or does
both peripheral and - Spinning not quickly resolve.
central actions over the sensation
spinal trigeminal (vertigo)
nucleus, which is rich in - Sweating
5-HT1B/D receptors.
Thus, the mechanism of
action of zolmitriptan is
double. On the one
hand, zolmitriptan acts
peripherally inhibiting
dilatation and
 inflammation of cranial
vessels. On the other,
zolmitriptan exhibits a
central nociceptive
action in the brainstem
nuclei. This dual action
of zolmitriptan on
migraine pain is
completed with its
beneficial effects on
nausea and vomiting,
due to its binding to the
nucleus of the tractus
solitarius, the center for
control of vomiting.

Anti – Migraine: Serotonin Antagonists

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Methysergide Methysergide is Used exclusively - Nausea - All patients receiving Sansert
(Sansert) serotonin antagonists to treat episodic - Vomiting (methysergide maleate) should
acts on central nervous and chronic - Heartburn remain under constant supervision of
system (CNS), which migraine and for - Abdominal the physician and be examined
directly stimulates the episodic and pain regularly for the development of
smooth muscle leading chronic cluster - Diarrhea fibrotic or vascular complications.
to vasoconstriction. headaches. - Constipation - Sansert (methysergide maleate) has
Some alpha-adrenergic Methysergide is - Drowsiness been specifically designed for the
blocking activity has one of the most - Dizziness prophylaxis of vascular headache and
been reported. effective - has no place in the management of the
Suggestions have been medications for Lightheadedn acute attack
made by investigators as the prevention of ess - Intended for use as a preventive
to the mechanism migraine, but is - Weakness agent in the treatment of vascular
whereby Methysergide not intended for - Poor headaches. It should not be used for
produces its clinical the treatment of coordination acute
effects, but this has not an acute attack, it - Insomnia Migraine attacks. If, after a 3-week trial
been finally established, is to be taken - Rash period, Sansert (methysergide
although it may be daily as a - Facial maleate) has not been effective in
related to the anti- preventative flushing decreasing the frequency or intensity
serotonin effect. medication. - Weight gain of headaches, it is unlikely that longer
or loss administration of Sansert
- Muscle or (methysergide maleate) will be
joint aches or beneficial.
discomfort - It should be taken with meals. Weight
- General gain may necessitate modification of
feeling of diet.
being unwell
(malaise)
- Fatigue
- Backache
- Fever
- Urinary
problems
- Leg pain or
swelling
- Shortness of
breath
- Numbness
or cold feeling
in the
extremities
- Hair loss
 Anesthetics

Anesthetics: General (IV)

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Thiopental Thiopental binds at a For use as the - Coughing - Monitor vital signs q3–5min before,
(Pentothal) distinct binding site sole anesthetic - Sneezing during, and after anesthetic
associated with a agent for brief (15 - Hiccups administration until recovery and into
Cl- ionopore at the minute) - Slowed postoperative period, if necessary.
GABAA receptor, procedures, for breathing - Report increases in pulse rate or
increasing the duration induction of - Slow heart drop in blood pressure. Hypovolemia,
of time for which the anesthesia prior rate cranial trauma, or premedication with
Cl- ionopore is open. to administration - Cardiac opioids increases potential for apnea
The post-synaptic of other arrhythmias and symptoms of myocardial
inhibitory effect of GABA anesthetic - Prolonged depression (decreased cardiac output
in the thalamus is, agents, to sleepiness and arterial pressure).
therefore, prolonged. supplement and recovery - Shivering, excitement, muscle
regional - Shivering twitching may develop during recovery
anesthesia, to period if patient is in pain.
provide hypnosis
during balanced
anesthesia with
other agents for
analgesia or
muscle
relaxation, for the
control of
convulsive states
during or
following
inhalation
anesthesia or
local anesthesia,
in neurosurgical
 patients with
increased
intracranial
pressure, and for
narcoanalysis
and
narcosynthesis in
psychiatric
disorders.
Propofol The action of propofol Used for induction - Hypotension - Monitor hemodynamic status and
(Diprivan) involves a positive and/or - Pauses in assess for dose-related hypotension.
modulation of the maintenance of breathing - Take seizure precautions. Tonic-
inhibitory function of the anesthesia and (Apnea) clonic seizures have occurred
neurotransmitter gama- for management lasting 30 – following general anesthesia with
aminobutyric acid of refractory 60 seconds propofol.
(GABA) through GABA- status epilepticus. - Movement - Be alert to the potential for drug
A receptors. - Injection site induced excitation (e.g., twitching,
burning / tremor, hyper clonus) and take
stinging / pain appropriate safety measures.
- Respiratory - Provide comfort measures; pain at
acidosis the injection site is quite common
during especially when small veins are used.
weaning
-
Hypertriglycer
idemia
-
Hypertension
- Rash
- Itching
- Irregular
heartbeat
(Arrhythmia)
 - Slow heart
rate
- Cardia
output
decreased
(concurrent
opioid use
increases
incidence)
- Fast heart
rate

Anesthetics: General (Inhalational)

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Sevoflurane Sevoflurane induces a Used for induction - Cough - Check the time of administration
(Ultane) reduction in junctional and maintenance - Dizziness - Monitor vital signs
conductance by of general - Drowsiness - Monitor all the body systems
decreasing gap junction anesthesia in - Increased - Continuous monitoring of pulse
channel opening times adult and amount of oximetry
and increasing gap pediatric patients saliva - Postural Blood Pressure should be
junction channel closing for inpatient and - Nausea taken
times. Sevoflurane also outpatient - Shivering - Take note of the time that the drug
activates calcium surgery. - Vomiting has expired
dependent ATPase in
the sarcoplasmic
reticulum by increasing
the fluidity of the lipid
membrane. It also
appears to bind the D
subunit of ATP synthase
and NADH
dehydrogenase and also
binds to the GABA
 receptor, the large
conductance
Ca2+ activated
potassium channel, the
glutamate receptor, and
the glycine receptor.
Halothane Halothane causes For the induction - Nausea - Note that Children are at greater risk
(Fluothane) general anaethesia due and maintenance - Vomiting for complications after anesthesia
to its actions on multiple of general - Chills (e.g. laryngospasm, bronchospasm,
ion channels, which anesthesia. May - Headache aspiration, etc.)
ultimately depresses be administered - Abnormal - Nursing care should include support
nerve conduction, by the heart rhythm and reassurance; assessment of child
breathing, cardiac nonrebreathing - Decreased for any skin breakdown related to
contractility. Its technique, partial lung function immobility, and safety precautions.
immobilizing effects rebreathing, or - Decreased - Adult patients should receive
have been attributed to closed technique. oxygen in the education about what will happen
its binding to potassium The induction tissues or during administration of anesthesia.
channels in cholinergic dose varies from blood Expected body reactions should also
neurons. Halothane's patient to patient - Hepatitis be explained.
effect are also likely due but is usually - Kidney - Continuously reassure adult patients
to binding to NMDA and within the range damage during the time that they are aware of
calcium channels, of 0.5% to 3%. - Malignant their surroundings but they are unable
causing hyperthermia to speak.
hyperpolarization. - Problems - Most general anesthetics are not
with recommended during pregnancy
circulation because of potential adverse effects to
- Yellowing of the fetus.
skin or eyes - Note that Older adults are more
(jaundice) susceptible to adverse effects (e.g.
CNS, CV, and dermatological effects).
- At risk for developing toxicity
because of possible hepatic and renal
impairment.
 - Safety measures should be instituted
(e.g. side rails, call light, ambulation
assistance, and skin care).
Longer monitoring and regular
orienting and reassuring is essential.
After general anesthesia, it is
important for nurses to promote
vigorous pulmonary toilet to decrease
the risk of pneumonia.

Anesthetics: Local (Esters)

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Procaine Procaine acts mainly by Indicated for the - Allergic - Be aware that reactions during dental
(Novocaine) inhibiting sodium influx production of reaction procedure are usually mild, transient,
through voltage gated local or regional - Difficulty and produced by epinephrine added to
sodium channels in the analgesia and breathing local anesthetic (e.g., headache,
neuronal cell membrane anesthesia by - Closing of palpitation, tachycardia, hypertension,
of peripheral nerves. local infiltration the throat dizziness).
When the influx of and peripheral - Swelling of - Use procaine with epinephrine with
sodium is interrupted, an nerve block the lips, caution in body areas with limited
action potential cannot techniques. tongue or blood supply (e.g., fingers, toes, ears,
arise and signal face nose). If used, inspect particular area
conduction is thus - Chest pain for evidence of reduced perfusion
inhibited. The receptor - Slow or (vasospasm): Pale, cold, sensitive
site is thought to be irregular skin.
located at the heartbeats - Hypotension is the most important
cytoplasmic (inner) - Dizziness or complication of spinal anesthesia.
portion of the sodium drowsiness Risk period is during first 30 min after
channel. Procaine has - Anxiety or induction and is intensified by changes
also been shown to bind restlessness in position that promote decreased
or antagonize the - Nausea venous return, or by preexisting
function of N-methyl-D- - Vomiting hypertension, pregnancy, old age, or
aspartate (NMDA) - Trembling hypovolemia.
 receptors as well as - Shaking
nicotinic acetylcholine - Seizures
receptors and the (convulsions)
serotonin receptor-ion
channel complex.
Tetracaine Tetracaine is an ester- Ophthalmic - Mild - Recovery from anesthesia to the
(Pontocaine) type anesthetic and tetracaine is stinging, pharyngeal area is complete when
produces local indicated for the burning or patient has feeling in the hard and soft
anesthesia by blocking for procedures itching where palates and when muscles in the
the sodium ion channels requiring a rapid the medicine faucial (tonsillar) pillars contract with
involved in initiation and and short- acting is applied stimulation.
conduction of neuronal topical ophthalmic - Skin - Do not give food or liquids until these
impulses. anesthetic. tenderness or normal pharyngeal responses are
The combination redness present (usually about 1 hr. after
lidocaine and - Numbness anesthetic administration). The first
tetracaine patch in places small amount of liquid (water) should
is indicated for where the be given under supervision of care
local dermal medicine is provider.
analgesia for accidentally - Be aware that increased blood
superficial applied concentration of the drug may result
dermatological - Severe from excess application of tetracaine
procedures and burning, to the skin (to relieve pruritus or
superficial venous stinging, burning), application to debrided or
access. The swelling, or infected skin surfaces, or too rapid
combination other irritation injection rate.
lidocaine and of the treated - High blood concentrations of
tetracaine cream skin tetracaine can lead to adverse
is intended to - Oozing, systemic effects involving CNS and
provide topical blistering or CV systems: Convulsions, respiratory
local analgesia for any signs of arrest, dysrhythmias, cardiac arrest.
superficial infection
dermatological - Dizziness
procedures. - Drowsiness
 - Nausea
- Vomiting
- Slow, fast or
irregular
heartbeats

Anesthetics: Local (Amides)

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Dibucaine Local anesthetics block For production of - Contact
- Use OTC preparations as directed.
(Nupercainal) both the initiation and local or regional dermatitis Always review package instructions.
conduction of nerve anesthesia by - Sensitivity to
- Discontinue if irritation or rectal
impulses by decreasing infiltration sunlight bleeding (following use of rectal
the neuronal techniques such (Photosensiti preparations) develops and consult
membrane's as percutaneous vity) physician.
permeability to sodium injection and - Flushing - Hemorrhoids can be caused or
ions through sodium intravenous - Eye / skin worsened by constipation, excessive
channel inhibition. This regional irritation straining at stool, excessive standing,
reversibly stabilizes the anesthesia by - Nausea sitting, and coughing.
membrane and inhibits peripheral nerve - Vomiting - Physician may prescribe sitz baths
depolarization, resulting block techniques - Diarrhea 3–4 times/d to reduce the swelling and
in the failure of a such as brachial - Chest pain pain of hemorrhoids.
propagated action plexus and - Palpitations- Note: Medication is intended for
potential and intercostal and by temporary relief of mild to moderate
subsequent conduction central neural itching or pain. Seek medical advice
blockade. techniques such for continuing discomfort, pain,
as lumbar and bleeding, or sensation of rectal
caudal epidural pressure.
blocks. - Do not breast feed while taking this
drug without consulting physician.
Bupivacaine Local anesthetics such Indicated for the - Abnormal - Monitor for signs of inadvertent
(Marcaine, as bupivacaine block the production of heart rhythms intravascular injection, which can
Sensorcaine) generation and the local or regional - Anxiety produce a transient "epinephrine
conduction of nerve anesthesia or response" (increased heart rate or
impulses, presumably by analgesia for - systolic BP or both, circumoral pallor,
increasing the threshold surgery, for oral Apprehension palpitations, nervousness) within 45
for electrical excitation in surgery - Back pain seconds in the unsedated patient and
the nerve, by slowing the procedures, for - Blurred an increase by 20 bpm or more in
propagation of the nerve diagnostic and vision heart rate for at least 15 seconds in
impulse, and by reducing therapeutic - Cardiac sedated patient.
the rate of rise of the procedures, and arrest - Vasoconstrictor-containing solution
action potential. for obstetrical - should be administered cautiously, if
Bupivacaine prevents procedures. Cardiovascul at all, to areas with end arteries (e.g.,
depolarization by Bupivacaine is ar collapse digits, penis) or to areas that have a
binding to the indicated to - Chest pain compromised blood supply; ischemia
intracellular portion of induce post- - Chills or and gangrene can result. Inspect
sodium channels and surgical analgesia shivering areas for evidence of reduced
blocking sodium ion in adults for up to - Confusion / perfusion because of vasospasm:
influx into neurons. In 72 hours following disorientation pale, cold, sensitive skin.
general, the progression arthroscopic - Convulsions - Note: Systemic reactions (toxicity)
of anesthesia is related subacromial (seizures) are more apt to occur in children or
to the diameter, decompression - Dizziness older adults and may develop rapidly
myelination and by administration - Drowsiness or be delayed for as long as 30 min
conduction velocity of into the - Constricted after administration.
affected nerve fibers. subacromial pupils - Monitor for toxicity: CNS stimulation
Clinically, the order of space under - Fast heart (unusual anxiety, excitement,
loss of nerve function is direct rate restlessness) usually occurs first,
as follows: (1) pain, (2) arthroscopic - Feeling followed by CNS depression
temperature, (3) touch, visualization. unusually hot (drowsiness, unconsciousness,
(4) proprioception, and Bupivacaine, - Gasping respiratory arrest). However, because
(5) skeletal muscle tone. together with the - Headache stimulation is apt to be transient or
The analgesic effects of NSAID - absent, drowsiness may be the first
Bupivacaine are thought Meloxicam, is Hypertension sign in some patients (especially
to potentially be due to indicated for the - Impaired children and older adults).
its binding to the production of heart function - Monitor BP and fetal heart rate
prostaglandin E2 postsurgical (myocardial continuously during labor because
receptors, subtype EP1 analgesia in adult depression) maternal hypotension may
(PGE2EP1), which patients for up to - Loss of accompany regional anesthesia.
inhibits the production of 72 hours following consciousnes Place mother on left side with legs
prostaglandins, thereby bunionectomy, s elevated.
reducing fever, open inguinal - Hypotension - Monitor cardiac and respiratory
inflammation, and herniorrhaphy or - Metallic status continuously in patients
hyperalgesia. total knee taste receiving retrobulbar and dental
arthroplasty. - Nausea blocks.
- Tremors
- Urinating
less than
usual or not at
all
- Vomiting
- Weak pulse
 Neuromuscular Blockers

Neuromuscular Blockers: Depolarizing

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Succinylcholine Succinylcholine is a Indicated as an - Jaw rigidity - Lab tests: Obtain baseline serum
(Anectine) depolarizing adjunct to general - Hypotension electrolytes. Electrolyte imbalance
neuromuscular blocker, anesthesia, to - Muscle (particularly potassium, calcium,
meaning it causes a facilitate tracheal fasciculation magnesium) can potentiate effects of
prolonged period of intubation, and to may result in neuromuscular blocking agents.
membrane provide skeletal postoperative - Be aware that transient apnea
depolarization in order to muscle relaxation pain usually occurs at time of maximal drug
exert its therapeutic during surgery or - Muscle effect (1–2 min); spontaneous
effects. It binds to the mechanical relaxation respiration should return in a few
post-synaptic cholinergic ventilation. resulting in seconds or, at most, 3 or 4 min.
receptors found on respiratory - Have immediately available:
motor endplates, depression to Facilities for emergency endotracheal
thereby inducing first the point of intubation, artificial respiration, and
transient fasciculations breathing assisted or controlled respiration with
followed by skeletal cessation oxygen.
muscle paralysis. (apnea) - Monitor vital signs and keep airway
- Respiratory clear of secretions.
depression
- Salivary
gland
enlargement

Neuromuscular Blockers: Non – Depolarizing

Name of the Drug Mode of Action Indication Side Effects Nursing Considerations
Rocuronium Rocuronium acts by For inpatients and - Nausea - Assess for the mentioned cautions
(Zemuron) competing for outpatients as an - Vomiting and contraindications (e.g. drug
cholinergic receptors at adjunct to general - Swelling or allergies, hepatic and renal
the motor end-plate. This anesthesia to discomfort at impairment, etc.) to prevent any
action is antagonized by facilitate both untoward complications.
acetylcholinesterase rapid sequence the injection - Perform a thorough physical
inhibitors, such as and routine site assessment (e.g. weight, neurological
neostigmine and tracheal - Sleepiness status, vital signs, heart sounds, bowel
edrophonium. intubation, and to or sounds, etc.) to establish baseline
Rocuronium acts by provide skeletal lightheadedn data before drug therapy begins, to
competitively binding to muscle relaxation ess determine effectiveness of therapy,
nicotinic cholinergic during surgery or - Mild itching and to evaluate for occurrence of any
receptors. The binding of mechanical or skin rash adverse effects associated with drug
vecuronium decreases ventilation. - High or low therapy.
the opportunity for blood - Inspect skin color and evidence of
acetylcholine to bind to pressure pressure areas or breakdown which
the nicotinic receptor at (Hypertensio could result when movement ceases.
the postjunctional n or - Monitor laboratory test results
membrane of the Hypotension) (e.g. liver and renal function tests) to
myoneural junction. As a determine possible need for a
result, depolarization is reduction in dose and evaluate for
prevented, calcium ions toxicity.
are not released and
muscle contraction does
not occur. Evidence also
suggests that
nondepolarizing agents
can affect ACh release.
It has been hypothesized
that nondepolarizing
agents bind to
postjunctional ("curare")
receptors and may
therefore interfere with
the sodium and
potassium flux, which is
responsible for
depolarization and
 repolarization of the
membranes involved in
muscle contraction.
Atracurium Atracurium antagonizes For use, as an - Skin flushing - Lab tests: Baseline serum
(Tracrium) the neurotransmitter adjunct to general - Redness electrolytes, acid–base balance, and
action of acetylcholine anesthesia, to - Injection site renal function as part of preanesthetic
by binding competitively facilitate reactions assessment.
with cholinergic receptor endotracheal - Hives - Note: Personnel and equipment
sites on the motor end- intubation and to - Itching required for endotracheal intubation,
plate. This antagonism is provide skeletal - Wheezing administration of oxygen under
inhibited, and muscle relaxation - Shortness of positive pressure, artificial respiration,
neuromuscular block during surgery or breath and assisted or controlled ventilation
reversed, by mechanical - Allergic must be immediately available.
acetylcholinesterase ventilation. reactions - Evaluate degree of neuromuscular
inhibitors such as - Inadequate blockade and muscle paralysis to
neostigmine, musculoskele avoid risk of overdosage by qualified
edrophonium, and tal block individual using peripheral nerve
pyridostigmine. - Low blood stimulator.
pressure - Monitor BP, pulse, and respirations
(hypotension) and evaluate patient's recovery from
- Fast or slow neuromuscular blocking (curare-like)
heart rate effect as evidenced by ability to
breathe naturally or to take deep
breaths and cough, keep eyes open,
lift head keeping mouth closed,
adequacy of hand-grip strength. Notify
physician if recovery is delayed.
- Note: Recovery from neuromuscular
blockade usually begins 35–45 min
after drug administration and is almost
complete in about 1 hr.