TELAZOL- tiletamine hydrochloride and zolazepam hydrochloride injection, powder, for solution

Telazol by

Drug Labeling and Warnings

Telazol by is a Animal medication manufactured, distributed, or labeled by Zoetis Inc.. Drug facts, warnings, and ingredients follow.

Drug Details [pdf]

SPL UNCLASSIFIED SECTION

100 mg/mL total
(equivalent to 50 mg/mL tiletamine and 50 mg/mL zolazepam)
For Intramuscular and Intravenous injection in Dogs
For Intramuscular injection only in Cats

CAUTION

Federal (USA) law restricts this drug to use by or on the order of a licensed veterinarian.

DESCRIPTION

TELAZOL (tiletamine and zolazepam for injection) is a nonnarcotic, nonbarbiturate, injectable anesthetic agent for dogs and cats. Chemically, TELAZOL is a combination of equal parts by weight of base of tiletamine hydrochloride (2-[ethylamino]-2-[2-thienyl]-cyclohexanone hydrochloride), an arylaminocycloalkanone dissociative anesthetic, and zolazepam hydrochloride (4-[o-fluorophenyl]-6, 8-dihydro-1,3,8- trimethylpyrazolo [3, 4-e][1,4] diazepin-7 [1H]-1- hydrochloride), a nonphenothiazine diazepinone having minor tranquilizing properties. The product is supplied sterile in vials. The addition of 5 mL diluent produces a solution containing the equivalent of 50 mg tiletamine base, 50 mg zolazepam base and 57.7 mg mannitol per milliliter. This solution has a pH of 2 to 3.5 and is recommended for deep intramuscular injection.

INDICATIONS

Dogs
TELAZOL is indicated in dogs for restraint and minor procedures of short duration (30 min. avg.) requiring mild to moderate analgesia. Minor surgery is considered to be laceration repair, draining of abscesses, castrations and other procedures requiring mild to moderate analgesia. (See Dogs under Dosage and Administration.) TELAZOL administered intravenously is indicated in dogs for induction of anesthesia followed by maintenance with an inhalant anesthetic.

Cats
TELAZOL is indicated in cats for restraint or for anesthesia combined with muscle relaxation.

DOSAGE AND ADMINISTRATION

The dose is determined by the total combined concentration of 100 mg/mL (see HOW SUPPLIED)

Dogs

Intramuscular (IM) For Restraint and Minor
Procedures of Short Duration Requiring Mild to
Moderate Analgesia:
In healthy dogs, an initial intramuscular
dosage of 3 to 4.5 mg/lb (6.6 to 9.9 mg/kg)
TELAZOL is recommended for diagnostic
purposes; 4.5 to 6 mg/lb (9.9 to 13.2 mg/
kg) for minor procedures of short duration,
such as treatment of lacerations and wounds,
castrations and other procedures requiring mild
to moderate analgesia. When supplemental
doses of TELAZOL are required, such individual
supplemental doses should be less than the
initial dose, and the total dose given (initial
dose plus supplemental dose or doses)
should not exceed 12 mg/lb (26.4 mg/kg). The
maximum safe dose is 13.6 mg/lb (29.92 mg/
kg). (See Animal Safety.) Results from TELAZOL
anesthesia in dogs will be more satisfactory
if the procedures are completed within one
hour and if the procedures can be completed
following single dose administration. In order to
maintain at least a 2X margin of safety in dogs,
the use of this product is limited to procedures
that call for low doses (see Indications). Studies
show that there is variation in response to
different dosages of TELAZOL and that low
doses do not give adequate levels of anesthesia,
and in some instances do not give adequate
analgesia, for extensive procedures.

Intravenous (IV) For Induction of Anesthesia
Followed by Maintenance with an Inhalant
Anesthetic:
In dogs, for induction of anesthesia, administer
TELAZOL intravenously at 1-2 mg/lb (2.2-4.4 mg/
kg) body weight to effect. TELAZOL should be
administered slowly, over 30-45 seconds; after
approximately 30-60 seconds, the dog’s level
of consciousness, muscle relaxation, and jaw
tone should be assessed to determine the
ability to intubate. If after waiting 60 seconds
the dog’s level of anesthesia is not sufficient for
successful intubation, additional TELAZOL may be
administered; the total dose should not exceed
2 mg/lb (4.4 mg/kg) body weight.

Cats

In healthy cats, an initial TELAZOL dosage of 4.4 to
5.4 mg/lb (9.7 to 11.9 mg/kg) IM is recommended
for such procedures as dentistry, treatment of
abscesses, foreign body removal and related
types of surgery; 4.8 to 5.7 mg/lb (10.6 to
12.5 mg/kg) for minor procedures requiring
mild to moderate analgesia, such as repair of
lacerations, castrations and other procedures of
short duration. Initial dosages of 6.5 to 7.2 mg/
lb (14.3 to 15.8 mg/kg) are recommended for
ovario hysterectomy and onychectomy. When
supplemental doses of TELAZOL are required,
such individual supplemental doses should be
given in increments that are less than the initial
dose, and the total dose given (initial dose plus
supplemental doses) should not exceed the
maximum allowable safe dose of 32.7 mg/lb
(72 mg/kg). (See Animal Safety.)

General Dosing Information

Fasting prior to induction of general anesthesia with
TELAZOL is not essential; however, when preparing
for elective surgery, it is advisable to withhold food
for at least 12 hours prior to TELAZOL administration.
As with other injectable anesthetic agents, the
individual response to TELAZOL is somewhat
varied, depending upon the dose, general physical
condition and age of the patient, duration of the
surgical procedure, and any preanesthetics used.
Therefore, recommendations for dosage regimens
cannot be fixed absolutely. Specific dosage
requirements must be determined by evaluation
of the health status and condition of the patient
and of the procedure to be performed.
Recovery varies with the age and physical
condition of the animal and the dose of TELAZOL
administered. Recovery is extended with high
dose or multiple injections, particularly in cats.

Intramuscular injection in dogs and cats:
There may be pain on injection. This is especially
prevalent in cats.
Following a single, deep intramuscular injection
of TELAZOL in cats and dogs, onset of anesthetic
effect usually occurs within 5 to 12 minutes.
Muscle relaxation is optimum for approximately
the first 20 to 25 minutes after TELAZOL is
administered, and then diminishes.
Repeated doses increase the duration of the
effect of TELAZOL but may not further diminish
muscle tone. The quality of anesthesia with
repeated doses varies because the ratio of the two
components within the animal’s body changes
with each injection. This is due to the difference
in the rates of metabolism and elimination of the
two components. The quality of anesthesia will
be improved and more predictable if the entire
dose is given as a single injection rather than in
several doses. The best method of evaluating
the depth of TELAZOL anesthesia is to monitor
the patient for deliberate conscious response to
nociceptive stimuli.
If adequate anesthesia is not produced by the
recommended dosage regimen, supplemental
anesthesia or another agent is indicated. This
includes the use of barbiturates and volatile
anesthetics. When used concurrently with TELAZOL
the dosage of these agents should be reduced.

PREPARATION OF SOLUTION FOR ADMINISTRATION

To each vial add 5 mL sterile water for injection,
USP. Slight agitation will facilitate complete
reconstitution. The resultant solution will contain
100 mg total TELAZOL per one milliliter (50 mg
tiletamine and 50 mg zolazepam per mL).
Discard unused solution after 7 days when stored
at room temperature or after 56 days when kept
refrigerated. Only use clear solution. Color of
solution may vary from colorless to light amber.

CONTRAINDICATIONS

The use of TELAZOL is contraindicated in dogs and cats with pancreatic disease. TELAZOL is excreted predominantly by the kidneys. Preexistent renal pathology or impairment of renal function may be expected to result in prolonged duration of anesthesia. TELAZOL should not be used in dogs and cats with severe cardiac or pulmonary dysfunction. Because the teratogenic potential of TELAZOL is unknown, it should not be used in pregnant bitches or queens at any stage of pregnancy. Also, a study has shown that TELAZOL crosses the placental barrier and produces respiratory depression in the newborn; therefore, its use for Cesarean section is contraindicated.

WARNINGS

FOR USE IN DOGS AND CATS ONLY. 

When using TELAZOL for induction of anesthesia,
patients should be continuously monitored.
Facilities for the maintenance of a patent airway,
artificial ventilation and oxygen supplementation
should be available.
Pulmonary edema has been reported to occur in
cats with the use of TELAZOL. Signs and symptoms
include dyspnea, lethargy, anorexia and abnormal
behavior. Deaths have been reported occasionally
in severely affected individuals. Cats should be
observed closely for any signs and symptoms
which may suggest pulmonary edema so that
appropriate therapy may be instituted.
The principal route of excretion of both
components in the cat is the urine; therefore,
TELAZOL is not recommended for use in cats
suffering from renal insufficiency.
Balance studies in dogs indicated extensive
biotransformation of both components with less
than 4% of the dose excreted unchanged in the
urine.
TELAZOL is excreted predominantly by the
kidneys. Preexistent renal pathology or
impairment of renal function may be expected to
result in prolonged duration of anesthesia.
Phenothiazine-derivative drugs should not
be used with TELAZOL at dosages indicated
for intramuscular (IM) injection because the
combination produces respiratory and myocardial
depression, hypotension and hypothermia.
The safe use of TELAZOL in pregnant animals
or on reproduction has not been established.
TELAZOL crosses the placental barrier and causes
respiratory depression in the neonate.

PRECAUTIONS

The dosage of TELAZOL should be reduced in
geriatric dogs and cats, in animals in debilitated
condition and in animals with impairment of
renal function. Death has occurred in both cats
and dogs following intramuscular TELAZOL
administration. Preexisting pulmonary disease,
renal disease (see Contraindications and
Warnings) and shock were causally implicated at
necropsy; however, death was drug attributable
in at least one dog (of 1072) and one cat (of 1095).
Intravenous TELAZOL has been demonstrated
to be safe in a field study in dogs when used in
conjunction with phenothiazine-derivative drugs
(acepromazine) administered at dosages from
0.04-0.06 mg/kg IM.
Cats and smaller dogs with small body masses
in relation to large body surfaces should be
protected from heat loss during TELAZOL
anesthesia. Body temperature should be
monitored, and supplemental heat may be
required to control hypothermia. As with
other anesthetics, it is prudent to provide for
hemostasis during any surgical procedure.
During TELAZOL anesthesia, athetoid movement
may occur. This athetosis should not be mistaken
for lack of anesthesia nor is it indicative of lack
of analgesia. Do not give additional anesthesia
in an attempt to abolish the athetoid movement.
Efforts to eliminate athetoid movement with
additional doses of TELAZOL can result in
anesthetic overdosage.
TELAZOL does not abolish laryngeal, pharyngeal,
pinnal, palpebral, and pedal reflexes, and may
not be adequate as the sole anesthetic for
surgical procedures in these areas. Endotracheal
tubes are not well tolerated in connection with TELAZOL anesthesia in the cat and their use may
result in impaired respiration. After removal of
the tube, normal respiration should resume.
The stimulation of surgical procedures aids in
maintaining adequate ventilation. The anesthetized
patient must be monitored throughout the
procedure, and if cardiopulmonary problems do
occur, measures must be taken to assure that
alveolar ventilation and cardiovascular functions are
maintained.
The eyes normally remain open with the pupils
dilated. The use of a bland ophthalmic ointment is
advisable to protect the corneas from desiccation.
The concurrent use of chloramphenicol will
prolong the duration of anesthesia in cats.
Copious salivation may occur during TELAZOL
anesthesia. Ptyalism may be controlled in dogs
and cats by administering atropine sulfate, USP,
0.02 mg/lb (0.04 mg/kg) body weight (IV, IM,
or SC) as concurrent medication. Exaggerated
swallowing, reflex action and accumulation of
saliva may give rise to vomiting and retching.

ADVERSE REACTIONS

For Restraint and Minor Procedures of Short
Duration Requiring Mild to Moderate
Analgesia
Respiratory depression may occur following
administration of high doses of TELAZOL. If at any
time respiration becomes excessively depressed
and the animal becomes cyanotic, resuscitative
measures should be instituted promptly. Adequate
pulmonary ventilation using either oxygen or room
air is recommended as a resuscitative measure.
Adverse reactions reported include emesis during
emergence, excessive salivation, transient apnea,
vocalization, erratic recovery and prolonged
recovery, excessive tracheal and bronchial
secretions when atropine sulfate, was not given
before anesthesia, involuntary muscular twitching,
hypertonicity, cyanosis, cardiac arrest, pulmonary
edema and muscle rigidity during surgical
procedures. Central nervous system stimulation and
convulsions have also been reported. Tachycardia
frequently occurs, particularly in the dog. This rise
in heart rate usually lasts about 30 minutes. Either
hypertension or hypotension may also occur.
Insufficient anesthesia has been reported in dogs.
Death has been reported in dogs and cats following
TELAZOL administration.

Intravenous Induction of Anesthesia followed by
Maintenance with Inhalant Anesthesia in Dogs
In a field study to assess the effectiveness and
safety of TELAZOL administered intravenously
at 1-2 mg/lb (2.2-4.4 mg/kg) for the induction of
anesthesia followed by maintenance with inhalant
anesthesia in dogs, 144 dogs were intravenously
administered TELAZOL (See Effectiveness).
Sixteen adverse reactions occurred during the
study: nystagmus (5), emesis (4), diarrhea (2), and
one occurrence each of hypersalivation, urticarial,
anorexia, hyperthermia, and lethargy. All adverse
reactions resolved by the end of the study.
Physiologic abnormalities related to general
anesthesia were transient and not severe.
Post-induction apnea (time from induction to
first inspiration ≥30 seconds) was observed in
49.3% of dogs across all treatment groups with a
mean duration of one minute. The highest overall
frequency and duration of post-induction apnea
was in the alpha2-agonist + opioid groups.
Overall, 36 dogs received assisted ventilation.
Assisted ventilation was needed most frequently
early in the procedure (at procedure start,
possibly after an apneic period) then decreased
in frequency as the procedure continued.
Sixteen dogs experienced oxygen saturation
(SpO2) ≤90 mmHg: 7 in the alpha2-agonist +
opioid groups, 6 in the phenothiazine + opioid
groups, and 3 in the opioid alone groups.
Twenty-five dogs had a temperature ≥103°F
during the study, with 12 of these occurring
prior to preanesthetic administration only. Of the
remaining 13 dogs, 7 were in the alpha2-agonist +
opioid groups, 5 were in the opioid alone groups,
and 1 in the phenothiazine + opioid groups.
One dog was reported with hyperthermia as an
adverse reaction in the alpha2-agonist + opioid
treatment groups. The dog became excitable
during recovery and its temperature elevated to
105.7°F. Hyperthermia resolved with treatment
of IV fluids and cooling.

Twenty-seven dogs experienced temperatures
≤96°F at one or more timepoints. Most dogs
received supplemental heat during surgery.
Fifty-nine dogs had mean blood pressure
(BP) values ≤60 mmHg. These values are
spread among all treatment groups. No dogs
were reported with adverse reactions due to
hypotension or hypertension in any dose groups.
Elevated or low BP values were transient.
Ventricular premature depolarizations were
noted in 3 dogs in the alpha2-agonist + opioid
group. This transient rhythm disturbance is
not uncommon in dogs receiving alpha2-
agonists or inhalant anesthetics. One dog in the
phenothiazine + opioid group showed transient
ST depression that could have been due to
cardiac hypoxia. All dogs recovered normally.
For a copy of the Safety Data Sheet (SDS) or
to report adverse reactions call Zoetis Inc. at
1-888-963-8471. Additional information can be
found at www. Zoetis.US.com.
For additional information about adverse drug
experience reporting for animal drugs, contact
FDA at 1-888-FDA-VETS or http://www.fda.gov/
AnimalVeterinary/SafetyHealth.

CLINICAL PHARMACOLOGY

Mechanism of Action

TELAZOL is a rapid-acting anesthetic combination
of tiletamine hydrochloride and zolazepam
hydrochloride. Tiletamine hydrochloride is a
dissociative anesthetic agent whose pharmacologic
action is characterized by profound analgesia,
normal pharyngeal-laryngeal reflexes and
cataleptoid anesthesia. The anesthetic state
produced does not fit into the conventional
classification of stages of anesthesia, but instead
TELAZOL produces a state of unconsciousness
which has been termed “dissociative’’ anesthesia in
that it appears to selectively interrupt association
pathways to the brain before producing somesthetic
sensory blockade.
Cranial nerve and spinal reflexes remain active;
however, these reflexes must not be confused
with inadequate anesthesia. Analgesia results
from apparent selective interruption of sensory
inputs to the brain and usually persists after the
anesthetic effect has subsided.
Protective reflexes, such as coughing and
swallowing, are maintained under tiletamine
anesthesia. Other reflexes, e.g., corneal, pedal,
are maintained during tiletamine anesthesia,
and should not be used as criteria for judging
depth of anesthesia. The eyes normally remain
open with the pupil dilated. It is suggested that
a bland ophthalmic ointment be applied to the
cornea if anesthesia is to be prolonged.
Used alone, tiletamine hydrochloride does
not provide adequate muscle relaxation for
abdominal surgical procedures. When combined
with zolazepam hydrochloride, good muscle
relaxation is generally attained during the phase
of deep surgical anesthesia.

Pharmacokinetics
The pharmacokinetics of TELAZOL injectable
solution was evaluated in 12 healthy adult
Beagle dogs, following a single intravenous (IV)
administration of 2.2 mg/kg bodyweight, which
is equivalent to 1.1 mg/kg for both tiletamine
hydrochloride and zolazepam hydrochloride.
After administration of 2.2 mg/kg TELAZOL IV,
the initial mean concentration of tiletamine (C0)
was 1018 ng/mL, the systemic clearance (CL)
was 6223 mL/kg/h, the area under the curve to
the last measured concentration (AUC 0-last) was
178 ng*hr/mL, and steady state volume of
distribution (Vss) was 3250 mL/kg. The mean
elimination half-life of tiletamine was 0.87 hours.
For zolazepam, the mean C0 was 2594 ng/mL, CL
was 1993 mL/kg/h and Vss was 604 mL/kg. The mean
elimination half-life of zolazepam was 0.41 hours.
The mean C0 and AUC0-t(last) were approximately
2.5 and 3 times, respectively, greater for zolazepam
than for tiletamine. However, the mean half-life
(T1/2) of tiletamine was approximately 2.5 times
longer than for zolazepam, resulting in quantifiable
plasma concentrations up to 2 hours longer.
Pretreatment with an alpha-2 agonist or
phenothiazine followed by inhalant isoflurane
has been shown to increase in the initial
concentration of both tiletamine and zolazepam.

EFFECTIVENESS

Dogs
Preanesthesia
In a field study conducted at 6 veterinary hospitals,
144 dogs of various breeds, ranging in age from
4 months to 14 years (mean age 5 years) and
body weights from 1.2- 85.5 kg, were enrolled for
completion of a veterinary procedure requiring
anesthesia. Dogs were preanesthetized with a
phenothiazine + opioid, an opioid alone, or an
alpha2-agonist + opioid at the study Investigator’s
discretion based on individual patient needs.
Approximately 20 minutes later, dogs were
intravenously administered TELAZOL at 1-2 mg/lb
(2.2-4.4 mg/kg) ‘to effect’ of anesthesia and
were intubated. After induction, dogs received
either isoflurane or sevoflurane for anesthetic
maintenance for at least 30 minutes. Procedures
conducted included dental prophylaxis with or
without extractions (64), ovariohysterectomy
(31), castration (18), and mass removal (14).
Upon completion of the procedure, dogs were
monitored in recovery for 4 hours, then followed at
home for 2-4 days, monitoring for the presence of
abnormal clinical signs.
Of 144 dogs enrolled in the study, 142 (98.6%)
were successfully intubated after intravenous
administration of TELAZOL at a mean dosage of
1.2 mg/lb (2.7 mg/kg). The mean dosage range was
lowest in the alpha2-agonist + opioid preanesthetic
treatment group (0.9 mg/lb; 2 mg/kg) and highest
in the opioid alone preanesthetic group (1.8 mg/lb;
3.9 mg/kg).
Overall induction quality evaluated on a scale
of acceptable, intermediate, or unacceptable
was acceptable in 131/142 (91.6%) dogs and
intermediate in 12/143(8.4%) dogs. On a scale of
good, fair, or poor, study participants rated the
quality of recovery from anesthesia as good in
75% of dogs (118/144) and fair in 18.1% (26/144).
In an overall assessment of anesthesia, considering
induction, maintenance, and recovery, was scored
as excellent or good in 128/144 (88.9%) of dogs.
Three dogs (2.1%) were rated with an overall
assessment of anesthesia as poor, and for these
dogs, recovery was also rated poor. Physiologic
measurements of heart rate, respiratory rate,
body temperature, oxygen saturation, and blood
pressure during anesthetic induction, maintenance,
and recovery showed that the administration of
TELAZOL did not severely impact these variables.
A variety of concomitant treatments were used
during the study including intravenous fluid
solutions, non-steroidal anti-inflammatory
medications, antimicrobials, and antiparasitics that
were consistent with routine canine practice.

ANIMAL SAFETY

TELAZOL has a wider margin of safety in cats
than in dogs. Dogs have survived repeated
IM dosage regimens of 13.6 mg/lb (30 mg/kg)
(maximum safe dose) for eight successive days.
This is approximately two times the maximum
recommended therapeutic dose. Cats have
survived IM dosage regimens of up to 32.7 mg/
lb (72 mg/kg) (maximum safe dose) on alternate
days for seven episodes. This is 4.6 times the
maximum recommended therapeutic dose for
cats. However, these reports should not obviate
prudent anesthetic practices. Some degree of
tolerance has been reported. This tolerance
appears to be species-variable.

Cats

In cats, the duration of effect of zolazepam exceeds
that of tiletamine so that as the animal recovers
there is a greater degree of tranquilization than
anesthetization. There is a slight lowering of blood
pressure during the first hour after injection.
Heart rate and electrocardiogram readings are
unaffected by TELAZOL (tiletamine and zolazepam
for injection). Arterial pO2 levels are decreased
three minutes after injection but usually return to
normal within 15 to 35 minutes.

Dogs
In dogs, the duration of effect of tiletamine
exceeds that of zolazepam so there is a lesser
degree of tranquilization than anesthetization in
this species. The total effect of TELAZOL in dogs is
of shorter duration than in cats.
Following administration of TELAZOL in dogs, a
marked, persistent tachycardia occurs within two
minutes following either 4.5 or 9 mg/lb (10 or
20 mg/kg) TELAZOL intramuscularly. Stroke volume
decreases proportionately to the increased rate
at the 4.5 mg/lb (10 mg/kg) dose, with little
change in net cardiac output. There is an initial
increase in systolic blood pressure, with a slight
drop in pressure within five minutes. The systolic
blood pressure remains at this decreased level
throughout the duration of the anesthetic effect.
Diastolic pressure increases throughout this same
period. Following a 9 mg/lb (20 mg/kg) dose
of TELAZOL in dogs, the relationship between
stroke volume and heart rate is disproportionate,
with a resultant substantial decrease in cardiac
output. Contractility and mean blood pressure are
decreased, indicating direct myocardial depression.
Ventricular function is adequate. During surgical
manipulations, tachycardia and hypertension may
be observed, and may be brought on by sympathetic
reaction to painful stimuli. Epinephrine is markedly
less arrhythmogenic in animals under TELAZOL
anesthesia than in those under halothane anesthesia.
During TELAZOL anesthesia, the assurance of
a patent airway is greatly enhanced by virtue
of maintaining pharyngeal-laryngeal reflexes.
During the first 15 minutes after intramuscular
administration of 9 mg/lb (20 mg/kg) of TELAZOL,
the respiratory rate is doubled while the tidal
volume is decreased to less than one-half of control
values. Arterial pO2 levels also decrease. This may
be evidenced by hypoxemia and cyanosis. The
pulmonary function usually returns to normal within
35 minutes after the administration of TELAZOL.

Preanesthetic Compatibility Study in Dogs
Six healthy Beagle dogs (3 males and 3 females),
at least 8 months of age, ranging in body
weight between 5.6 and 9.4 kg, were fitted
with a telemetry device that captured systemic
arterial blood pressures, electrocardiogram, and
body temperature. Each dog received a total of
6 treatments with at least a 7-day washout between
periods. During each period, dogs received
1 of the following 6 preanesthetics prior to the
TELAZOL administration: placebo (0.9% saline),
acepromazine low dose (0.1 mg/kg body weight
[BW]), acepromazine high dose (1.1 mg/kg BW),
dexmedetomidine low dose (125 mcg/m2 body
surface area [BSA]), dexmedetomidine high dose
(375 mcg/m2 BSA), or butorphanol (0.4 mg/kg BW).
Blood samples were collected at intubation, end
of isoflurane administration, and after anesthesia
when the dogs were able to walk. Plasma
concentrations of tiletamine and zolazepam were
measured using a validated method. Preanesthetic
treatment with high dose acepromazine and both
high and low doses of dexmedetomidine resulted
in substantial increases in plasma concentrations
of tiletamine and zolazepam at intubation. The
increase in the tiletamine plasma concentrations
was approximately 2X higher for the high dose of
acepromazine and 2.7 to 4.5X higher for the low
and high doses of dexmedetomidine, respectively,
compared to saline. The increase in zolazepam
plasma concentrations was 1.5X higher for the
high dose acepromazine, and 1.8 to 2.8X higher
for the low and high doses of dexmedetomidine,
respectively, compared to saline.
No information on the dose-sparing of TELAZOL
was obtained during the study because the dogs
were given the full initial half-dose (2.2 mg/kg) and
not actually administered TELAZOL ‘to effect’. The
average total dose of test article administered to
the dogs was 2.6 mg/kg for the saline group and
2.2 mg/kg for the other treatment groups. One
dog (saline group) required more than the initial
2.2 mg/kg bolus to achieve intubation at the first
attempt.
Without preanesthesia (saline group), dogs
retained a strong cough reflex, chewing motions,
tachycardia and increased muscle tone during
intubation. With preanesthesia, half of the dogs
in the high dose dexmedetomidine group had
no laryngeal reflex response to intubation and
all experienced post-intubation apnea. The postintubation
apnea suggests that the 2.2 mg/kg dose
of TELAZOL was higher than necessary in some
groups.
All dogs in all treatment groups achieved successful
anesthetic plane following TELAZOL administration
and were intubated and induced to isoflurane
anesthesia uneventfully. The quality of intubation,
and occurrence and severity of adverse reactions
(e.g., apnea and bradypnea) following TELAZOL
administration and intubation revealed differences
among preanesthetic treatment groups. The
cardiovascular and respiratory changes observed
were typical of each preanesthetic medication used
in combination with TELAZOL. Acepromazine and
isoflurane administration decreased arterial blood
pressure. Dexmedetomidine decreased heart rate.
Intubation transiently increased heart rate and/or
blood pressure (sympathetic stimulations). Mild to
severe respiratory depression was observed after
TELAZOL administration and each preanesthetic
agent. Adverse reactions were manageable with
appropriate care.

STORAGE CONDITIONS

Store at controlled room temperature 20° to 25°C (68° to 77°F). Discard unused solution after 7 days when stored at room temperature or after 56 days when kept refrigerated. Only use clear solution. Color of solution may vary from colorless to light amber.

HOW SUPPLIED

TELAZOL (tiletamine and zolazepam for injection) is available in individual vials of 5 mL solution when reconstituted. The addition of 5 mL diluent produces a solution containing the equivalent of 50 mg tiletamine base, 50 mg zolazepam base and 57.7 mg mannitol per milliliter.

10 mL vial -100 mg/mL total (equivalent to 50 mg/mL tiletamine and 50 mg/mL zolazepam) when reconstituted

SPL UNCLASSIFIED SECTION

Approved by FDA under NADA # 106-111

zoetis

Distributed by:
Zoetis Inc.
Kalamazoo, MI 49007

Revised: June 2019

40027682

PRINCIPAL DISPLAY PANEL - 5 mL Bottle Label

INGREDIENTS AND APPEARANCE

TELAZOL 
tiletamine hydrochloride and zolazepam hydrochloride injection, powder, for solution

Product Information
Product Type	PRESCRIPTION ANIMAL DRUG	Item Code (Source)	NDC: 54771-9050
Route of Administration	INTRAMUSCULAR	DEA Schedule	CIII

Active Ingredient/Active Moiety
Ingredient Name	Basis of Strength	Strength
TILETAMINE HYDROCHLORIDE (UNII: 99TAQ2QWJI) (TILETAMINE - UNII:2YFC543249)	TILETAMINE	50 mg  in 1 mL
ZOLAZEPAM HYDROCHLORIDE (UNII: 45SJ093Q1N) (ZOLAZEPAM - UNII:G1R474U58U)	ZOLAZEPAM	50 mg  in 1 mL

Inactive Ingredients
Ingredient Name	Strength
MANNITOL (UNII: 3OWL53L36A)	57.7 mg  in 1 mL

Packaging
#	Item Code	Package Description	Marketing Start Date	Marketing End Date
1	NDC: 54771-9050-1	1 in 1 CARTON
1		5 mL in 1 BOTTLE

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NADA	NADA106111	04/09/1982

Labeler - Zoetis Inc. (828851555)