OBAT-OBAT ANESTESI.

Dr Joko Murdiyanto SpAn MPH

 1.GENERAL ANESTHESIA

• General anesthesia provides rapid and

complete loss of sensation,It is characterized
by:
total analgesia (no pain)
unconsciousness deeper than sleep
loss of memory
complete muscle relaxation.
• General anesthesia usually requires more
than one drug. Multiple medications are used
to rapidly cause unconsciousness and muscle
relaxation and to maintain deep anesthesia.
• IV agents are usually administered first
because they act within a few seconds.
• After the patient loses consciousness, inhaled
agents are used to maintain the anesthesia.
• After the patient loses consciousness, inhaled
agents are used to maintain the anesthesia.
• This approach allows the dose of inhalation
anesthetic to be lower so that the procedure
is safer for the patient
General anesthesia occurs in distinct steps
or stages:
• Stage 1
Loss of pain, loss of general sensation, but the
patient may be awake
• Stage 2
Excitement and hyperactivity
The patient may try to resist, their heartbeat
and breathing may become irregular and blood
pressure can increase
The anesthesiologist will try to quickly move
through stage 2. Often an IV agent will be given
to calm the patient during this stage.
• Stage 3
Called surgical anesthesia
Skeletal muscles become relaxed,
cardiovascular and breathing activities
stabilize.
Eye movements slow down and the patient
becomes very still. This is the stage when
surgery begins and remains until the
procedure ends.
• Stage 4, or overdose
This is marked by hypotension or circulatory
failure. Death may result if the patient cannot
be revived quickly.
 Inhaled general anesthetics
• These agents are nonflammable,
nonexplosive gases or volatile liquids.
• One of their major advantages is that the
depth of anesthesia may be very quickly
changed by altering the concentration of the
agent.
• The median alveolar concentration (MAC) is a
term used to determine the potency of
various inhalation anesthetics.
• It is the median effective dose (ED50) of the
anesthetic, and is expressed as the % of the
gas in the mixture necessary to achieve an
anesthetic effect.
• The smaller the MAC, the more lipid soluble is
the anesthetic, and the lower the
concentration of the anesthetic needed to
produce anesthesia. Therefore, the more
potent is the anesthetic.
 Characteristic of the ideal inhaled anaesthetic
agent :
• Apleasant odor.
• Non-irritant.
• Low blood gas (rapid induction) and recovery).
• Chemically stable.
• Non-inflammable.
• Potent.
• Inert.
• Not metabolized.
• Non-toxic.
• Analgesic.
• Minimal depression of thr cardiovascular and respiratory
system
 Anesthetic MAC value
(in %)

• Isoflurane 1.2
• Sevoflurane 2.0
• Desflurane 6.0
• Nitrous oxide 100
• All of the inhalation anesthetics (except
nitrous oxide) are respiratory depressants.
• Isoflurane is more depressant than desflurane
and sevoflurane
• All 3 increase the resting partial pressure of
CO2 in arterial blood (PaCO2), increase the
apneic threshold, and decrease the ventilator
response to hypoxia.
• a. Nitrous oxide (laughing gas).
It is not very soluble in blood and tissues,
which enables it to move in and out of the
body very rapidly.
Used for dental procedures and brief
obstetrical and surgical procedures
It may also be used together with other
general anesthetics.
Nitrous oxide in higher doses has been found
to depress the heart.
 Volatile anesthetics

• These are liquid at room temperature,

converted into a vapor and inhaled

• The most commonly administered liquid

volatile agents in the U.S. are:
Desflurane (Suprane)
Sevoflurane (Ultane)
Isoflurane (Forane)
• Desflurane .
Advantages:
 rapid onset and recovery of anesthesia (useful for
outpatient procedures)
 one of least metabolized to toxic byproducts.
Disadvantages:
 low volatility, so requires a special vaporizer
 pungent and irritating to the airway (leading to more
coughing, laryngospasm, so it is not as useful for
extended surgical procedures)
• sevoflurane:
Advantages:
Rapid onset and very rapid recovery of
anesthesia (useful with children)
Not as pungent as desflurane (also useful with
children).
Has good bronchodilating properties and is
the agent of choice in patients with asthma,
bronchitis, and COPD. It has little effect on
the heart rate.
• Disadvantages:
Its metabolism results in F1- which may reach
toxic levels in kidneys.
In addition, carbon dioxide absorbents in
anesthesia machines degrade sevoflurane to a
fluorinated hydrocarbon, which is degraded by
renal lyase enzymes to a thioacylhalide.
This compound has been observed to cause
necrosis of the proximal tubule in rats.
• isoflurane:
Advantages:
 It causes peripheral vasodilation and increased coronary
blood flow (useful in patients with ischemic heart disease)
one of least metabolized to F1-.

Disadvantages:
 moderate solubility, so recovery from anesthesia may be
delayed.
 Isoflurane can make the heart “more sensitive” to circulating
catecholamines (like epinephrine).
 This could lead to a ventricular arrhythmia in patients with
heart disease who are given epinephrine in combination with
an anesthetic, or in chronically anxious, “Type A” patients
(they have higher circulating levels of endogenous
epinephrine).
 Intravenous anesthesia
• Intravenous anesthesia is used for the rapid
induction of, but not the maintenance of
anesthesia.
• The maintenance of anesthesia is with an
inhalation anesthetic
 Characteristic of ideal
intravenous induction.

• A smooth and rapid onset.

• A rapid recovery.
• No pain or injection.
• Minimal side-effects.
• No toxicity.
• 1. Benzodiazepines (BZ).
The 3 main drugs used in this category are
diazepam, lorazepam and midazolam.
They sedate, relieve anxiety, and control acute
agitation, therefore their primary indication is
for premedication.
They are inadequate for use in surgical
anesthesia “on their own”, and must therefore
be used with another anesthetic agent (i.e. an
inhalation anesthetic).
Diazepam (Valium).

This is the prototype drug of the BZ’s

It is water-insoluble, so IV use requires a nonaqueous
vehicle which can cause local irritation/pain

Midazolam (Versed).
Midazolam is water soluble, so drug of choice for IV
administration .
It has a more rapid onset and more rapid elimination than
the other BZ’s.
In addition, midazolam is the most potent amnestic
• Lorazepam (Ativan).

• It is water-insoluble, so IV use requires a

nonaqueous vehicle which can cause local
irritation/pain.
• It is a less potent amnestic than midazolam,
but a more potent amnestic than diazepam.

–
• 2. Barbiturates.
– The 3 main drugs used in this category are thiopental,
thiamylal, and methohexital.
– There is a more rapid onset and shorter duration of
action if there is a sulfur instead of oxygen atom at
position 2 (so, thiamylal and thiopental have more
rapid onset and shorter duration of action than
methohexital).
– None of these drugs provides analgesia or significant
muscle relaxation.
– Like most of the “older” drugs, barbiturates have a
worse toxicological profile than the benzodiazepines
– They all may cause coughing, laryngospasm,
bronchospasm, or apnea.
• a. Thiopental.
Thiopental, the flagship of the barbiturate
anesthetic group, has been a standard
anesthetic induction agent for more than 60
years and is the drug in this category, to which
all others are compared.
• b. Thiamylal.

Thiamylal is not significantly different from

thiopental in potency, incidence of laryngospasm,
respiratory depression, cardiotoxicity or recovery
time.
• c. Methohexitol.
• 3. Opioids.
The terms opioid and opiate are often used
interchangeably, but have different meanings.
An opiate is derived from the juice of the opium
poppy, Papaver Somniferum, which is commonly
called ‘White Poppy’ and ‘Herb of Joy’.
An opioid is a compound, either synthetic, or a
natural product which has morphine-like effects.
Opioids produce moderate sedation and profound
analgesia. They exert their effects by binding with
opioid receptors in the central nervous system.
Opioids may be used to supplement
anesthesia when other anesthetic drugs don’t
adequately control pain reactions.
They may be used as induction agents or as
the primary drug for the maintenance of
anesthesia when hemodynamic stability is
essential.
The high doses required to produce
unconsciousness do not depress the
myocardium, nor do they cause a significant
reduction in blood pressure.
Doses must be at least 10 times the dose used
for control of pain in ambulatory patients,
thus this is referred to as high dose opioid.
Opioids depress respiration by inhibiting the
responsiveness of the medullary respiratory
center to PCO2 and alter the rhythm of
breathing.
Consequently, it is necessary to assist
ventilation.
Since respiratory depression may extend into
the post-operative period as a result of drug
accumulation in the tissues, the use of opioids
whose clearances are slow remain most
appropriate for patients who are expected to
require p.o. ventilatory care.
• The opioids most commonly used are
fentanyl (Sublimaze)
sufentanil citrate (Sufenta)
alfentanil (Alfenta)
remifentanil (Ultiva)
• a. fentanyl (Sublimaze)
One of the most frequently used because of
how quickly it produces analgesi Fentanyl is a
potent synthetic opioid agonist with between
50-100 times the analgesic potency of
morphine.
• Fentanyl is used to aid induction and
maintenance of general anesthesia and to
supplement regional and spinal anesthesia.
• Fentanyl is preferred to morphine in
anesthesia due to its ability to maintain
cardiac stability.
• Fentanyl may be administered alone or in
combination with inhalation anesthetics,
local anesthetics, or benzodiazepines.
• b. sufentanil citrate (Sufenta)
Rapid induction of analgesia (similar to
Fentanyl)
• c. alfentanil (Alfenta).
Compared to fentanyl and sufentanil,
alfentanil has a shorter duration of action
because its high protein binding and relatively
low lipid solubility favor its sequestration in
plasma.
• d. remifentanil (Ultiva).
Remifentanil is ultra short acting and rapidly
cleared because it’s ester linkages are
susceptible to hydrolysis by esterases in
tissues and RBC’s.
• This converts the ester functional group into
an inactive carboxylic acid metabolite.
• This particular opioid is useful when dealing
with patients with liver or kidney failure.
• Less potent opioids such as morphine and
demerol have fallen into disfavor because of
their adverse effects when given in high doses.
• Morphine may produce hypotension and
bronchoconstriction as a consequence of its
histamine-releasing action.
• One of the most serious drawbacks of the
opioid anesthetics overall, is the possibility of
inadequate anesthetic depth.
• Signs of this include sweating, wrinkling of the
forehead, and opening of the eyes.
• To prevent this, the high dose opioid
techniques may be supplemented with
inhalation anesthetics or hypnotics such as
benzodiazepines (midazolam for shorter cases,
lorazepam for cases longer than 4 hours), or
more recently, propofol.
• However, the use of these may result in some
loss of cardiovascular stability.
• 4. Dissociative anesthetics.
This relates to a type of general anesthesia
that is characterized by amnesia, sedation,
and analgesia, although the patient appears to
be awake.
One of the dissociative anesthetics commonly
used is ketamine (Vetalar, Ketaset).
• Ketamine, is an N-methyl-D-aspartate (NMDA)
receptor antagonist.
• Ketamine blocks the ion channel in the
following diagram
• Ketamine blocks the ion channel in the
following diagram
• Ketamine has both very poor muscle
relaxation and analgesic activity.
• Ketamine may be used, along with diazepam
for cosmetic/reconstructive surgery
anesthesia.
• It is not widely used for anesthesia as it tends to
induce postoperative hallucinations.
• It is sometimes used as a recreational drug, but it
has a number of adverse effects:
 loss of coordination
 exaggerated sense of strength
 blank stare
 slurred speech
 A BBC report in May 2000 claimed that medical
research had shown that controlled tests on
ketamine users had revealed impaired memory
and mild schizophrenia several days after taking
the drug.
• Ketamine was classified as a Class C drug in
2005.
• Other class C drugs include cannabis and
anabolic steroids
• Ketamine plays an extensive role in the season
2 finale of House, M.D, titled “No reason”
• 5. Propofol (Diprivan)
From DI-isoPRopyl IV ANesthetic
chemical name: 2,6-diisopropylphenol
 Propofol is a sedative/hypnotic that can be used
for induction or maintenance of general
anesthesia.
 It is also used for sedating intubated,
mechanically ventilated patients.
 Analgesic effect is poor and addition of an
analgesic to the anesthetic regimen is necessary
for surgery.
 Advantages:
 Rapid induction and recovery times
 It can be given for prolonged periods without
resulting in prolonged recovery
• Disadvantages:
apnea
bradycardia and hypotension.
Propofol’s abuse as a recreational drug (it
produces euphoria) has been seen, in some
anesthesiologists who have access to the
drug.
 2.REGIONAL ANESTHESI
• 1.Local anesthesia.
• As the name implies, local anesthetics are
applied locally and function to block nerve
conduction.
• Recall that the concentration of sodium ions is
normally higher on the outside of neurons
than on the inside.
• A rapid flood of sodium ions into cells is
necessary for neurons to fire and conduct an
action potential.
• Local anesthetics act by blocking sodium
channels.
• This blocking is nonselective, which means
that both sensory and motor impulses are
affected.
• This blocking is brought about by the
anesthetic reversibly binding to and
inactivating sodium channels.
• Sodium influx through these channels is
necessary for the depolarization of nerve cell
membranes and subsequent propagation of
impulses along the course of the nerve.
• When a nerve loses depolarization and
capacity to propagate an impulse, the
individual loses sensation in the area supplied
by the nerve.
• All local anesthetics have an amine functional
group, an aromatic ring, and either an ester or
amide group linking them.
• amine
• aromatic ring
• ester
• amide
• Therefore, all local anesthetics are classified
as esters or amides.
• This is important because the amides are
chemically stable in vivo, whereas the esters
are subject to hydrolysis.
• In addition, the hydrolysis of an ester local
anesthetic leads to the formation of PABA,
which causes an allergic response in some
individuals.
• Local anesthetics may be administered
topically (i.e. nasal mucosa);
• through infiltration (injection into the dermis
and soft tissues located near peripheral nerve
endings);
• and in/near the spinal cord (includes caudal
block, epidural block, and spinal nerve block).
• Which local anesthetic should be used
generally depends on the duration of action of
the procedure.
• For short procedures, procaine would be
recommended.
• An intermediate duration of action is found
with cocaine, lidocaine, and mepivacaine.
• Long- acting local anesthetics include
bupivacaine (and levobupivacaine),
ropivacaine, and tetracaine.
• 2. Ester local anesthetics.
Commonly used local anesthetics containing
the ester functional group are benzocaine,
cocaine, procaine, and tetracaine.
a. procaine(Novocain)
• It is used for nerve block, epidural and spinal
anesthesia. Novocaine is generally not used in
dentistry anymore.
• b. benzocaine.
Topical use only
benzocaine (Solarcaine, Orajel, Lanacaine etc)
• It is used for minor mouth conditions (i.e
teething, canker sores) sore throat, sunburn,
and other minor skin conditions
• c. cocaine.
Cocaine is 2 times as potent as procaine. It is
used for ear, nose and throat procedures.
• d. tetracaine(Pontocaine).
Used for:
spinal anesthesia requiring 2 to 3 hours of
anesthesia
surface anesthesia of the eye, nose and
throat.
It is 16 times as potent as procaine.
• 3. Amide local anesthetics.
Commonly used local anesthetics containing
the amide functional group are bupivacaine,
lidocaine, mepivacaine, and ropivacaine.
a. bupivacaine(Marcaine) and
levobupivacaine (Chirocaine).
• These are used in infiltration and epidural
anesthesia. They are 16 times more potent
than procaine.
• Generally, they are more cardiotoxic than the
other long acting local anesthetics
• b. lidocaine.
• Used topically for minor dermatological
procedures (i.e skin tag removal)
• It is 4 times more potent than procaine and
has replaced procaine in the area of dental
anesthesia.
• c. mepivacaine (Carbocaine)
This local anesthetic is used for dental
procedures, surgical procedures and during
labor and delivery.
• d. ropivacaine (Naropin)
This is used for surgical procedures, including
caesarian sections. Although it is similar
pharmacologically to bupivacaine, it is less
cardiotoxic.
• 4. Adverse effects
a. Low concentration dosages:
dizziness
sleepiness
restlessness
• b. Higher concentration dosages:
muscular twitching
seizures
and hypotension (except for cocaine, which
can result in vasoconstriction and
hypertension, as well as cardiac arrhythmias).
 Tank for your attention

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