Picazo, Drol Susej Z.
BSN 2-A-4
Pharmacology
CLASSIFICATION DRUGS PHARMACODYNAMICS
Sedative-hypnotics Ultrashort- Thiopental, a barbiturate,
(Barbiturates) acting: is used for the induction
Thiopental of anesthesia prior to the
sodium use of other general
anesthetic agents and for
induction of anesthesia
for short surgical,
diagnostic, or therapeutic
procedures associated
with minimal painful
stimuli. Thiopental is an
ultrashort-acting
depressant of the central
nervous system which
induces hypnosis and
anesthesia, but not
analgesia. It produces
hypnosis within 30 to 40
seconds of intravenous
injection. Recovery after
a small dose is rapid, with
some somnolence and
retrograde amnesia.
Repeated intravenous
doses lead to prolonged
anesthesia because fatty
W7 Course Task
PHARMACOKINETICS INDICATIONS SIDE EFFECTS INTERACTIONS NURSING
CONSIDERATIONS
Absorption – Rapidly For use as the Adverse reactions The metabolism of Monitor vital signs q3–
absorbed. Distribution – Not sole anesthetic include respiratory Acetaminophen can 5min before, during,
available. Metabolism – agent for brief depression, be increased when and after anesthetic
Thiopental is extensively (15 minute) myocardial combined with administration until
metabolized, primarily in the procedures, for depression, cardiac Thiopental. recovery and into
liver, resulting in only 0.3% of induction of arrhythmias, postoperative period,
an administered dose being anesthesia prior prolonged The risk or severity if necessary.
excreted unchanged in the to administration somnolence and of adverse effects
urine. Ring deculturation leads of other recovery, sneezing, can be increased Report increases in
to the generation of an active anesthetic coughing, when pulse rate or drop in
metabolite, pentobarbital, that agents, to bronchospasm, Acetophenazine is blood pressure.
exists in concentrations supplement laryngospasm, and combined with Hypovolemia, cranial
approximately 3-10% that of regional shivering. Thiopental. trauma, or
the parent concentration. anesthesia, to Anaphylactic and premedication with
Thiopental and pentobarbital provide hypnosis anaphylactoid Thiopental may opioids increases
are also subject to both during balanced reactions to increase the central potential for apnea
oxidation and hydroxylation to anesthesia with Pentothal (thiopental nervous system and symptoms of
carboxylic acids and alcohols, other agents for sodium) (Thiopental depressant (CNS myocardial depression
respectively, all of which are analgesia or Sodium for Injection, depressant) activities (decreased cardiac
pharmacologically inert. muscle USP) have been of Aclidinium. output and arterial
Elimination – Not available. relaxation, for the reported. Symptoms, pressure).
control of e.g., urticaria,
convulsive states bronchospasm, Shivering, excitement,
during or vasodilation and muscle twitching may
following edema should be develop during
inhalation managed by
 tissues act as a reservoir; anesthesia or conventional means. recovery period if
they accumulate local anesthesia, patient is in pain.
Pentothal in in neurosurgical Rarely, immune
concentrations 6 to 12 patients with hemolytic anemia
times greater than the increased with renal failure and
plasma concentration, intracranial radial nerve palsy
and then release the drug pressure, and for have been reported.
slowly to cause narcoanalysis
prolonged anesthesia. and
narcosynthesis in
psychiatric
disorders.
Short-acting: Secobarbital, a Absorption – For the Short- CNS: Anxiety, CNS depressants: Assess patient for
Secobarbital barbiturate, is used for Not available. term treatment of clumsiness, Additive depressant signs and symptoms
the induction of Distribution – intractable confusion, effects of barbiturate toxicity,
anesthesia prior to the Not available. insomnia for depression, corticosteroids, oral including dyspnea,
use of other general Metabolism – patients dizziness, anticoagulants: severe confusion,
anesthetic agents and for Not available. habituated to drowsiness, Decreased plasma and severe
induction of anesthesia Elimination – barbiturates. hangover, headache, levels of these drugs drowsiness. Notify
for short surgical, Barbiturates are metabolized insomnia, irritability, with decreased prescriber
diagnostic, or therapeutic primarily by the hepatic lethargy, effectiveness immediately if they
procedures associated microsomal enzyme system, nervousness, appear because
with minimal painful and the metabolic products are nightmares, barbiturate toxicity
stimuli. Little analgesia is excreted in the urine and, less paradoxical may
conferred by barbiturates; commonly, in the feces. stimulation, syncope be life-threatening.
their use in the presence CV: Hypotension
of pain may result in EENT:
excitation. Laryngospasm Expect prescriber to
GI: Anorexia, provide patient with
constipation, nausea, the least possible
vomiting quantity of
MS: Arthralgia, secobarbital to
muscle weakness minimize the
RESP: Apnea, risk of acute or
bronchospasm, chronic overdosage.
respiratory For patients who are
depression depressed, drug-
SKIN: Jaundice dependent, or suicidal
Other: Drug or who have a history
dependence, weight of drug abuse,
 loss institute precautions to
prevent drug hoarding
and overdosage.

Intermediate Butabarbital potentiates Absorption – Butabarbital is Central nervous Most reports of Assess for adverse
acting: GABAergic neurons while Not available. indicated for use system/psychiatric: clinically significant effects. Older adults
Butabarbital inhibiting neuronal Distribution – as a sedative or Agitation, confusion, drug interactions and debilitated
acetylcholine and Not available. hypnotic. hyperkinesia, ataxia, occurring with the patients sometimes
glutamate receptors to Metabolism – Butabarbital CNS depression, barbiturates have manifest excitement,
produce sedation. Data regarding the metabolism should not be nightmares, involved confusion, or
Butabarbital is an of butabarbital in humans are used to treat nervousness, phenobarbital. depression. Children
intermediate acting not readily available. In dogs, insomnia for psychiatric However, the also may react with
barbiturate with a butabarbital undergoes longer than 2 disturbance, application of these paradoxical
duration of action of metabolism to a final weeks. hallucinations, data to other excitement. Side rails
approximately 6-8 hours. glucuronide metabolite. insomnia, anxiety, barbiturates appears may be advisable.
The therapeutic index is Elimination – Barbiturates dizziness, thinking valid and warrants Report these
quite wide as doses vary such as butabarbital are abnormality. serial blood level reactions to physician.
considerably from patient predominantly eliminated in Respiratory: determinations of the
to patient. Patients the urine. In dogs, 3-5% of the Hypoventilation, relevant drugs when
should be counselled dose is eliminated in the urine apnea. there are multiple
regarding the risk of as the unchanged parent therapies.
worsening insomnia, compound. Cardiovascular:
drowsiness, falls, and Bradycardia,
complex behaviour while hypotension,
not fully awake. syncope.

Gastrointestinal:
Nausea, vomiting,
constipation.

Other reported
reactions: Headache,
 hypersensitivity
(angioedema, skin
rashes, exfoliative
dermatitis), fever,
liver damage.

Long acting: Phenobarbital, the Absorption – For the treatment CNS: Anxiety, Anticoagulants: Be aware that
Phenobarbital longest-acting Absorbed in varying degrees of all types of depression, Decreased phenobarbital
barbiturate, is used for its following oral, rectal or seizures except dizziness, anticoagulant activity shouldn’t be given
anticonvulsant and parenteral administration. The absence drowsiness, during third trimester
sedative-hypnotic salts are more rapidly seizures. headache, irritability, CNS depressants: of pregnancy because
properties in the absorbed than are the acids. lethargy, Additive depressant repeated
management of all The rate of absorption is mood changes, effects use can cause
seizure disorders except increased if the sodium salt is paradoxical dependence in
absence (petit mal). ingested as a dilute solution or stimulation, sedation, corticosteroids: neonate. It also
taken on an empty stomach. vertigo Enhanced shouldn’t be given to
Distribution – CV: Bradycardia, metabolism of breastfeeding women
Not available. hypotension corticosteroids because it
Metabolism – Hepatic (mostly EENT: Miosis, ptosis possibly requiring may cause CNS
via CYP2C19). GI: Constipation, dosage adjustment depression in infants.
Elimination – diarrhea, nausea,
Not available. vomiting Use I.V. route
GU: Decreased cautiously in patients
libido, impotence, with CV disease,
sexual dysfunction hypotension,
MS: Arthralgia, bone pulmonary disease, or
tenderness shock
RESP: because drug may
Bronchospasm, cause adverse
respiratory hemodynamic or
depression respiratory effects.
SKIN: Dermatitis,
photosensitivity, Know that because
rash, urticaria drug can cause
Other: Injection-site respiratory
phlebitis (I.V.), depression,
physical and respiratory rate and
psychological depth should be
dependence. assessed before use,
especially in patient
 with
bronchopneumonia,
pulmonary disease,
respiratory
tract infection, or
status asthmaticus.

Give elixir undiluted or

mix with fruit juice,
milk, or water. Use a
calibrated device to
measure doses.

If necessary, crush
tablets and mix with
fluids or food.
Sedative-hypnotics Flurazepam Flurazepam, a Absorption – For short-term Dizziness, The metabolism of Monitor effectiveness.
(Benzodiaze- benzodiazepine and intermittent drowsiness, light-
Flurazepam hydrochloride is Flurazepam can be Hypnotic effect is
pines) derivative, is a hypnotic use in patients headedness,
agent which does not rapidly (30 minutes) absorbed with recurring staggering, ataxia increased when apparent on second or
appear to decrease insomnia and and falling have
from the gastrointestinal tract. combined with third night of
dream time as measured poor sleeping occurred, particularly
by rapid eye movements Distribution – habits. in elderly or Abatacept. consecutive use and
(REM). Furthermore, it debilitated persons.
Not available. continues
decreases sleep latency Severe sedation,
and number of Metabolism – lethargy, Acemetacin may
awakenings for a disorientation and decrease the
Flurazepam is rapidly 1–2 nights after drug
consequent increase in coma, probably excretion rate of
total sleep time. metabolized and is excreted indicative of drug Flurazepam which is stopped (drug has a
intolerance or could result in a
primarily in the urine. Both long half-life).
overdosage, have higher serum level
hydroxyethyl flurazepam (the been reported. Supervise ambulation.
major metabolite) and N- Residual sedation and
desalkyl flurazepam are active. drowsiness are
The N-desalkyl metabolite is relatively common.
slowly excreted in the urine as Excessive
the conjugated form. drowsiness, ataxia,
Elimination –
Flurazepam is rapidly
metabolized and is excreted
primarily in the urine. Less
than 1% of the dose is
excreted in the urine as N1-
desalkyl-flurazepam.
vertigo, and falling
occur more frequently
in older adults or
debilitated patients.
Monitor drug ingestion
if patient has a history
of drug abuse.
Prolonged use of
large doses can result
in psychic and
physical dependence.
Lab tests: Obtain
blood counts and liver
and kidney function
with repeated use.
Be aware that
withdrawal symptoms
have occurred 3 d
after abrupt
discontinuation after
prolonged use and
include worsening of
insomnia, dizziness,
blurred vision,
 anorexia, GI upset,
nasal congestion,
paresthesias.

Sedative-hypnotics Zolpidem Effects on the central Absorption – This drug is CNS: Abnormal Barbiturates, Use zolpidem
(Nonbenzodia- nervous system (CNS) Zolpidem is rapidly absorbed indicated for the
thinking, chlorpromazine, cautiously in patients
zepines) from the gastrointestinal tract. short-term
This drug has CNS In a single-dose crossover treatment of aggressiveness, general anesthetics, with additional
depressant effects, which study in 45 healthy subjects insomnia in
amnesia, asthenia, opioid agonists, disorders because it
may include somnolence, given 5 and 10 mg zolpidem adults
decreased alertness, tartrate tablets, the average characterized by ataxia, behavioral other CNS isn’t known if zolpidem
sedation, drowsiness, peak zolpidem concentrations difficulties with
changes, complex depressants, therapy might
dizziness, and other (Cmax) were 59 and 121 sleep initiation.
changes in psychomotor ng/mL, respectively, occurring behaviors (such as phenothiazines, aggravate these
function. Due to the at a mean time (Tmax) of 1.6
sleep driving), tramadol, tricyclic conditions, especially
above effects, the FDA hours for both doses.
has recommended an Distribution – confusion, decreased antidepressants: conditions with
initial dose of zolpidem 0.54 to 0.68 L/kg (in humans).
level Possibly respiratory
(immediate-acting) is a In patients with long term renal
single dose of 5 mg for insufficiency who were not yet of consciousness or increased CNS impairment.
women and a single dose on hemodialysis, the volume of depression and
inhibition, dizziness,
of 5 or 10 mg for men, distribution was found to reduced
immediately before increase significantly, AUC drowsiness, psychomotor Administer zolpidem
bedtime with at least 7-8 increased by 60%, and half-life function
euphoria, just before patient’s
hours remaining before nearly doubled.
the planned time of Metabolism – hallucinations, bedtime because drug
awakening. Refer to Zolpidem is metabolized to
headache, insomnia, has a rapid onset of
product labeling for three pharmacologically by
detailed information. various hepatic cytochrome lethargy, paradoxical action.
P450 (CYP) isoenzymes,
CNS stimulation
mainly CYP3A4, but also
CYP1A2 and CYP2C9. (including agitation, Expect patient to
Although zolpidem is heavily receive no more than
euphoria,
metabolized, all three a 1-month supply of
metabolites are inactive. hallucinations, zolpidem for
hyperactivity, and outpatient therapy.
The major metabolic routes in
humans are oxidation of the nightmares), suicidal
 methyl group on the phenyl ideation,
ring or the methyl group on the
vertigo, worsening of
imidazopyridine moiety, to
depression
produce carboxylic acids
(metabolites I and II), and
hydroxylation of one of the
imidazopyridine groups (to
produce metabolite X).
Another less common pathway
is by the oxidation of the
methyl groups on the
substituted amide.
Elimination –
Zolpidem tartrate tablets are
converted to inactive
metabolites that are eliminated
mainly by renal excretion.
Sedative-hypnotics Chloral hydrate None Absorption – Mainly used as a Central Nervous Aceclofenac may Chloral hydrate is not
Rapidly absorbed in the GI hypnotic in the intended for relief of
System decrease the
tract following oral or rectal treatment of pain. When used in
administration. Chloral hydrate insomnia; excretion rate of the presence of pain,
and its active metabolite, however, it is it may cause
Occasionally a Chloral hydrate
trichloroethanol, have been only effective as excitement and
detected in CSF, umbilical a hypnotic for patient becomes which could result in delirium.
cord blood, fetal blood, and short-term use. somnambulistic and
he may be a higher serum level.
amniotic fluid. May be used as Do not discontinue
Distribution – a routine disoriented and
abruptly following
Not available. sedative incoherent and show
prolonged use.
Metabolism – preoperatively to paranoid behavior. The protein binding
Sudden withdrawal
Metabolized by the liver and decrease anxiety Rarely, excitement, of Acenocoumarol
from dependent
erythrocytes to form and cause tolerance, addiction, can be decreased
patients may produce
trichloroethanol, an active sedation and/or delirium, drowsiness, when combined with
delirium, mania, or
metabolite. This reaction is sleep with staggering gait, Chloral hydrate.
convulsions.
catalyzed by alcohol respiration ataxia,
dehydrogenase and other depression or lightheadedness,
Monitor for S&S of
enzymes. Oxidation of chloral cough reflex vertigo, dizziness,
allergic skin reactions,
hydrate and trichloroethanol to nightmares, malaise,
which may occur
trichloroacetic acid in the liver mental confusion and
within several hours or
and kidneys also occurs to a hallucinations have
as long as 10 d after
lesser extent. Trichloroethanol been reported.
drug administration.

Anesthetics Gas: Methohexital, a
(General) Methohexital barbiturate, is used for
the induction of
anesthesia prior to the
use of other general
anesthetic agents and for
induction of anesthesia
for short surgical,
diagnostic, or therapeutic
procedures associated
with minimal painful
stimuli. Little analgesia is
conferred by barbiturates;
their use in the presence
of pain may result in
excitation.
also undergoes
glucuronidation to produce an Evaluate patient's
inactive metabolism. response to chloral
Elimination – hydrate and continued
Trichloroethanol, need for the drug.
trichloroethanol glucuronide,
and trichloroacetic acid are
excreted in the urine. Some
trichloroethanol glucuronide
may be secreted into bile and
excreted in the feces.
Absorption – Methohexital is Cardiovascular Methohexital may Monitor signs of
The absolute bioavailability indicated for use laryngeal spasm and
Circulatory increase the central
following rectal administration as an bronchospasm,
of methohexital is 17%. intravenous depression, nervous system including tightness in
Distribution – anaesthetic. It the throat and chest,
thrombophlebitis, depressant (CNS
Not available. has also been wheezing, cough, and
Metabolism – commonly used hypotension, depressant) activities severe shortness of
Metabolism occurs in the liver to induce deep breath. Notify
tachycardia, of Aclidinium.
through demethylation and sedation. physician or nursing
oxidation. Side-chain oxidation peripheral vascular staff immediately if
is the most important these reactions occur.
collapse, and Methohexital may
biotransformation involved in
termination of biologic activity. convulsions in increase the
Elimination – hypotensive activities
association with of Aldesleukin.
Excretion occurs via the
kidneys through glomerular cardiorespiratory
filtration.
arrest
Respiratory
Respiratory
depression (including
apnea),
cardiorespiratory
arrest,

Volatile liquids: Halothane is a general
Halothane
inhalation anesthetic
used for induction and
maintenance of general
anesthesia. It reduces the
blood pressure and
frequently decreases the
pulse rate and depresses
respiration. It induces
muscle relaxation and
reduces pains sensitivity
by altering tissue
excitability. It does so by
decreasing the extent of
gap junction mediated
cell-cell coupling and
altering the activity of the
laryngospasm,
bronchospasm,
hiccups, and
dyspnea
Neurologic
Skeletal muscle
hyperactivity
(twitching), injury to
nerves adjacent to
injection site, and
seizures
Absorption – For the induction As with other agents As with other agents Nursing care should
and maintenance
Not available. of this type, of this type, include support and
of general
Distribution – anesthesia. halothane halothane reassurance;
Not available. anaesthesia has anaesthesia has assessment of child
Metabolism – been shown to been shown to for any skin
Halothane is metabolized in trigger a skeletal trigger a skeletal breakdown related to
the liver, primarily by CYP2E1, muscle muscle immobility, and safety
and to a lesser extent by hypermetabolic state hypermetabolic state precautions.
CYP3A4 and CYP2A6. leading to high leading to high Halothane is widely
Elimination – oxygen demand and oxygen demand and used for children,
Not available. the clinical syndrome the clinical syndrome especially those with
known as malignant known as malignant respiratory
hyperthermia (MH). hyperthermia (MH). dysfunction because it
The syndrome The syndrome tends to produce
includes non specific includes non specific bronchial dilation.
features such as features such as
hypercapnia, muscle hypercapnia, muscle
 channels that underlie the rigidity, tachycardia, rigidity, tachycardia,
action potential. tachypnoea, tachypnoea,
cyanosis, cyanosis,
arrhythmias and arrhythmias and
unstable blood unstable blood
pressure. An pressure. An
increase in overall increase in overall
metabolism may be metabolism may be
reflected in an reflected in an
elevated elevated
temperature. temperature.
Treatment includes Treatment includes
discontinuation of discontinuation of
triggering agents, triggering agents,
administration of administration of
intravenous intravenous
dantrolene sodium dantrolene sodium
and application of and application of
supportive therapy. supportive therapy.

Anesthetics Tetracaine None Absorption – Ophthalmic Hypersensitivity The risk or severity Recovery from
(Regional) Systemic absorption of
tetracaine is Reactions: of adverse effects anesthesia to the
anaesthetic from the
combination cream is directly indicated for the Unpredictable can be increased pharyngeal area is
related to the duration and
for procedures adverse reactions (ie, when Acetazolamide complete when patient
surface area of application.
Although peak plasma requiring a rapid hypersensitivity, is combined with has feeling in the hard
concentrations for lidocaine
and short- acting including Tetracaine. and soft palates and
were measured, plasma levels
for tetracaine could not be topical anaphylaxis) are when muscles in the
determined due to low levels ophthalmic extremely rare. faucial (tonsillar)
(<0.9 ng/mL).
anesthetic. Tetracaine may pillars contract with
Distribution –
Tetracaine is rapidly increase the central stimulation.
hydrolyzed in the plasma;
therefore, volume of The combination nervous system
distribution could not be lidocaine and depressant (CNS Do not give food or
determined.
Metabolism – tetracaine patch depressant) activities liquids until these
Tetracaine is rapidly is indicated for of Aclidinium. normal pharyngeal
hydrolyzed by plasma
esterases to the following local dermal responses are present
primary metabolites: para- analgesia for (usually about 1 h
aminobenzoic acid and
diethylaminoethanol. The superficial after anesthetic
activity of both metabolites is dermatological administration). The
unspecified.
Elimination – procedures and first small amount of
Not available. superficial liquid (water) should
venous access. be given under
The combination supervision of care
lidocaine and provider.
tetracaine cream
is intended to Be aware that
provide topical increased blood
local analgesia concentration of the
for superficial drug may result from
dermatological excess application of
procedures. tetracaine to the skin
(to relieve pruritus or
burning), application
to debrided or infected
skin surfaces, or too
 rapid injection rate.

High blood
concentrations of
tetracaine can lead to
adverse systemic
effects involving CNS
and CV systems:
Convulsions,
respiratory arrest,
dysrhythmias, cardiac
arrest.

Anesthetics Lorazepam The effect of lorazepam Absorption – Lorazepam is CNS: Amnesia, Aminophylline, Be aware that
(Moderate in GABA-A receptors Readily absorbed with an FDA-approved anxiety, ataxia, theophylline: parenteral form of
sedation) produces an increase in absolute bioavailability of 90% for the short-term coma, confusion, Possibly reduced lorazepam is
the frequency of opening when given orally. When relief of anxiety delusions, sedative effects of contraindicated in
of the chloride ion intramuscularly administered a symptoms depression, lorazepam premature infants
channel. However, for its dose of 4 mg, lorazepam is related to anxiety dizziness, because the
effect to generate, the completely and rapidly disorders and drowsiness, Clozapine: Increased formulation contains
neurotransmitter is absorbed and achieves a anxiety euphoria, risk of ataxia, benzyl alcohol,
required. The maximal serum concentration associated with extrapyramidal delirium, excessive increasing risk of
anticonvulsant properties of 48 ng/ml in 15-30 minutes. depressive symptoms, fatigue, salivation, gasping syndrome,
of lorazepam are thought When administered orally, the symptoms such headache, hypotension, kernicterus, and
to be related to the time to attained maximum as anxiety- hypokinesia, marked sedation, toxicity.
binding to voltage- concentration is observed to associated irritability, malaise, and respiratory Lorazepam should be
dependent sodium insomnia. It is as nervousness, used with extreme
channels in which the
sustained repetitive firing
gets limited by the slow
recovery of sodium
channels due to the
benzodiazepine effect.
be of 2 hours. well used as an seizures, slurred arrest caution in neonates
Distribution – anesthesia speech, suicidal because although the
The reported volume of premedication in ideation, tremor, CNS depressants: amount of benzyl
distribution of lorazepam is 1.3 adults to relieve unsteadiness, vertigo Additive CNS alcohol is well below
L/kg. It is important to mention anxiety or to CV: Chest pain, depression, that associated with
that due to the lipophilicity of produce palpitations, potentially fatal toxicity, a total daily
lorazepam, it does not sedation/amnesia tachycardia respiratory metabolic load of
redistribute as fast in the brain. and for the EENT: Blurred vision, depression benzyl alcohol from
Metabolism – treatment of diplopia, dry mouth, combined sources
Lorazepam is hepatically status increased salivation, may increase the risk
metabolized by CYP450 epilepticus. photophobia of toxicity.
isoenzymes and extensively ENDO: Syndrome of
conjugated to the 3-0-phenolic inappropriate ADH
glucuronide. GI: Abdominal pain, Before starting
This is an inactive metabolite constipation, lorazepam therapy in
and is eliminated mainly by the diarrhea, elevated a patient with
kidneys. liver enzymes, depression, make
Elimination – jaundice, sure he already takes
When a single 2 mg oral dose nausea, thirst, an
is given to healthy subjects, vomiting antidepressant,
88% of the administered dose because of the
is recovered in urine and 7% increased risk of
was recovered in feces. From suicide in patients with
the excreted dose in urine, the untreated depression.
major form is the glucuronide
version that represents 74%
Be aware that the
while only 0.3% of the dose is
combination of

Anesthetics (Local) Long acting: Bupivacaine is a widely
Bupivacaine
used local anesthetic
agent. Bupivacaine is
often administered by
spinal injection prior to
total hip arthroplasty. It is
also commonly injected
into surgical wound sites
to reduce pain for up to
20 hours after surgery. In
comparison to other local
anesthetics it has a long
duration of action. It is
also the most toxic to the
recovered as unchanged general anesthesia
lorazepam. and sedation drugs
like lorazepam used
during
procedures or
surgeries in pregnant
women in their third
trimester is not
recommended
because it
may affect brain
development in the
fetus.
Absorption – Bupivacaine is Reactions to The metabolism of The metabolism of
Systemic absorption of local indicated to Sensorcaine Bupivacaine can be Bupivacaine can be
anesthetics is dose- and produce local or (bupivacaine HCl) increased when increased when
concentration-dependendent regional are characteristic of combined with combined with
on the total drug administered. anesthesia or those associated with Abatacept. Abatacept.
Other factors that affect the analgesia for other amide-type
rate of systemic absorption surgery, for oral local anesthetics. A The risk or severity The risk or severity of
include the route of surgery major cause of of adverse effects adverse effects can
administration, blood flow at procedures, for adverse reactions to can be increased be increased when
the administration site, and the diagnostic and this group of drugs is when Bupivacaine is Bupivacaine is
presence or absence of therapeutic excessive plasma combined with combined with
epinephrine in the anesthetic procedures, and levels, which may be Acetophenazine. Acetophenazine.
solution. for obstetrical due to overdosage,
Distribution – procedures. unintentional
heart when administered Not available. intravascular
in large doses. This Metabolism – Bupivacaine is injection, or slow
problem has led to the Amide-type local anesthetics indicated to metabolic
use of other long-acting such as bupivacaine are induce post- degradation.
local metabolized primarily in the surgical
anaesthetics:ropivacaine liver via conjugation with analgesia in
and levobupivacaine. glucuronic acid. The major adults for up to
Levobupivacaine is a metabolite of bupivacaine is 72 hours
derivative, specifically an 2,6-pipecoloxylidine, which is following
enantiomer, of mainly catalyzed via arthroscopic
bupivacaine. Systemic cytochrome P450 3A4. subacromial
absorption of local Elimination – decompression
anesthetics produces Only 6% of bupivacaine is by administration
effects on the excreted unchanged in the into the
cardiovascular and urine. subacromial
central nervous systems. space under
At blood concentrations direct
achieved with therapeutic arthroscopic
doses, changes in visualization.
cardiac conduction,
excitability,
refractoriness,
contractility, and
peripheral vascular
resistance are minimal.
However, toxic blood
concentrations depress
 cardiac conduction and
excitability, which may
lead to atrioventricular
block, ventricular
arrhythmias and to
cardiac arrest, sometimes
resulting in fatalities. In
addition, myocardial
contractility is depressed
and peripheral
vasodilation occurs,
leading to decreased
cardiac output and
arterial blood pressure.
Following systemic
absorption, local
anesthetics can produce
central nervous system
stimulation, depression,
or both.

Moderate- Excessive blood levels of
acting:
lidocaine can cause
Lidocaine
changes in cardiac
output, total peripheral
resistance, and mean
Absorption – Lidocaine is an CNS: Agitation; CNS: Agitation; Use caution when
In general, lidocaine is readily anesthetic of the anxiety; anxiety; administering
absorbed across mucous amide group apprehension; apprehension; lidocaine to patients
membranes and damaged skin indicated for confusion; difficulty confusion; difficulty with compromised
but poorly through intact skin. production of myocardial function
arterial pressure. With The agent is quickly absorbed local or regional speaking; speaking; because
central neural blockade from the upper airway, anesthesia by disorientation; disorientation; of risk of electrolyte
these changes may be tracheobronchial tree, and infiltration dizziness; dizziness; disturbances or fluid
attributable to the block of alveoli into the bloodstream. techniques such drowsiness; drowsiness; overload.
autonomic fibers, a direct And although lidocaine is also as percutaneous euphoria; euphoria;
depressant effect of the well absorbed across the injection and hallucinations; hallucinations; Observe for
local anesthetic agent on gastrointestinal tract the oral intravenous lethargy; light- lethargy; light- respiratory depression
various components of bioavailability is only about regional headedness; headedness; after bolus injection
the cardiovascular 35% as a result of a high anesthesia by malignant malignant and during I.V.
system, and/or the beta- degree of first-pass peripheral nerve hyperthermia; hyperthermia; infusion of lidocaine.
adrenergic receptor metabolism. After injection into block techniques paresthesia; paresthesia;
stimulating action of tissues, lidocaine is also such as brachial seizures; sensation seizures; sensation Keep life-support
epinephrine when rapidly absorbed, and the plexus and of cold, of cold, equipment and
present. The net effect is absorption rate is affected by intercostal and by heat, or numbness; heat, or numbness; vasopressors nearby
normally a modest both vascularity and the central neural tremors; twitching; tremors; twitching; during I.V. use in case
hypotension when the presence of tissue and fat techniques such unconsciousness unconsciousness of respiratory
recommended dosages capable of binding lidocaine in as lumbar and CV: Bradycardia, CV: Bradycardia, depression or other
are not exceeded. the particular tissues. caudal epidural cardiac arrest, cardiac arrest, reactions.
Distribution – blocks. hypotension, new or hypotension, new or Hypersensitivity
The volume of distribution worsening worsening reactions, including
determined for lidocaine is 0.7 arrhythmias, arrhythmias, anaphylaxis, have
to 1.5 L/kg. tachycardia tachycardia occurred with
Metabolism – EENT: Blurred vision, EENT: Blurred lidocaine-containing
Lidocaine is metabolized diplopia, oral vision, diplopia, oral solutions.
predominantly and rapidly by hypoesthesia, hypoesthesia,
the liver, and metabolites and tinnitus tinnitus
Carefully check
unchanged drug are excreted GI: Nausea, vomiting GI: Nausea, vomiting
prefilled syringes
by the kidneys. HEME: HEME: before using. Use only
Biotransformation includes Methemoglobinemia Methemoglobinemia syringes labeled “for
oxidative N-dealkylation, ring MS: Dysarthria, MS: Dysarthria, cardiac arrhythmias”
hydroxylation, cleavage of the muscle weakness, muscle weakness, for I.V. administration.
amide linkage, and myalgia myalgia
conjugation. N-dealkylation, a RESP: Respiratory RESP: Respiratory
major pathway of arrest or depression arrest or depression
biotransformation, yields the Other: Anaphylaxis; Other: Anaphylaxis;
metabolites other less severe other less severe
monoethylglycinexylidide and hypersensitivity hypersensitivity
glycinexylidide. The reactions; injection- reactions; injection-
pharmacological/toxicological site site
actions of these metabolites burning, irritation, burning, irritation,
are similar to, but less potent petechiae, redness, petechiae, redness,
than, those of lidocaine HCl. stinging, swelling, stinging, swelling,
Elimination – and tenderness. and tenderness.
The excretion of unchanged worsened pain worsened pain
lidocaine and its metabolites
occurs predominantly via the
kidney with less than 5% in the
unchanged form appearing in
the urine. The renal clearance
is inversely related to its
protein binding affinity and the
pH of the urine. This suggests
by the latter that excretion of
lidocaine occurs by non-ionic

Short-acting: Procaine is an anesthetic
Procaine agent indicated for
production of local or
regional anesthesia,
particularly for oral
surgery. Procaine (like
cocaine) has the
advantage of constricting
blood vessels which
reduces bleeding, unlike
other local anesthetics
like lidocaine. Procaine is
an ester anesthetic. It is
metabolized in the
plasma by the enzyme
pseudocholinesterase
through hydrolysis into
para-aminobenzoic acid
(PABA), which is then
excreted by the kidneys
into the urine.
diffusion.
Absorption – Absorption – CNS: Confusion, CNS: Confusion, Obtain body tissue
Not available. Not available. dizziness, dysphasia, dizziness, dysphasia, and fluid samples for
Distribution – Distribution – hallucinations, hallucinations, culture and sensitivity
Not available. Not available. headache, lethargy, headache, lethargy, tests as ordered
Metabolism – Metabolism – sciatic sciatic before giving first
Hydrolysis by plasma Hydrolysis by nerve irritation, nerve irritation, dose. Expect to begin
esterases to PABA plasma esterases seizures seizures drug therapy before
Elimination – to PABA CV: Labile blood CV: Labile blood test results are known.
With normal kidney function, Elimination – pressure, palpitations pressure,
the drug is excreted rapidly by With normal EENT: Black “hairy” palpitations Reconstitute vials of
tubular excretion. kidney function, tongue, oral EENT: Black “hairy” penicillin for injection
the drug is candidiasis, tongue, oral with D5W, or sodium
excreted rapidly stomatitis, taste candidiasis, chloride for injection,
by tubular perversion stomatitis, taste or sterile
excretion. GI: Abdominal pain, perversion water for injection.
diarrhea, elevated GI: Abdominal pain,
liver enzymes diarrhea, elevated Administer penicillin at
(transient), liver enzymes least 1 hour before
indigestion, (transient), other antibiotics.
nausea, indigestion,
pseudomembranous nausea,
Inject I.M. form deep
colitis pseudomembranous
into large muscle
GU: Acute interstitial colitis
mass. Apply ice to
nephritis, vaginal GU: Acute interstitial
relieve pain.
candidiasis nephritis, vaginal
MS: Muscle twitching candidiasis
SKIN: Rash MS: Muscle twitching
Other: Electrolyte SKIN: Rash
imbalances; Other: Electrolyte
injection-site imbalances;
necrosis, pain, or injection-site
redness necrosis, pain, or
redness