Revised: 21 January 2009
AN: 01283/2008
SUMMARY OF PRODUCT CHARACTERISTICS
January 2009
1.
NAME OF VETERINARY MEDICINAL PRODUCT
Oralject Sedazine Acepromazine (1.20% w/v) Oral Paste Transquilliser For
Horses
2.
QUALITATIVE AND QUANTITATIVE COMPOSITION
ACTIVE SUBSTANCE
Acepromazine maleate 12mg/ml,
(equivalent to 8.9mg/ml acepromazine base)
EXCIPIENTS
Propyl Parahydroxybenzoate 0.15mg/ml
Methyl Parahydroxybenzoate 0.65mg/ml
For full list of excipients, see section 6.1.
3.
PHARMACEUTICAL FORM
Oral Paste.
Yellow coloured paste.
4.
CLINICAL PARTICULARS
4.1
Target Species
The product is recommended only for use in horses.
4.2
Indications for Use, Specifying the Target Species
4.2.1
At low doses, as a tranquilliser to quieten excitable, nervous, hard to
handle horses during training, transport and confinement.
4.2.2
At higher doses, as a sedative to reduce excitement and stress during
various veterinary procedures, e.g. dentistry, shoeing, clipping and
minor surgery.
4.2.3
Doses higher than those recommended should never be used, since
there is a ceiling to the sedative effect attainable; higher than
recommended doses are likely merely to prolong the
duration of the sedative action.
Revised: 21 January 2009
AN: 01283/2008
4.3
Contra-indications
4.3.1
Do not administer to breeding stallions. Paralysis of the retractor penis
muscle has been associated with the use of parenterally administered
acepromazine in horses.
4.4
Special Warnings for Each Target Species
4.4.1
Do not administer in conjunction with other depressant or hypotensive
agents.
4.5
Special Precautions For Use
Special precautions for use in animals
4.5.1
Acepromazine has caused paraphimoses sometimes as a sequel to
priapism. When administered to male horses (geldings or stallions) use
the lowest dose recommended to produce the desired effect.
4.5.2
Whilst the product is not intended for routine use as an anaesthetic
premedication, situations may arise where general anaesthesia is
required in the 4-6 hours following use of the product. Care should be
taken to reduce the induction dose of other premedications and
anaesthetic agents, particularly parenteral barbiturates to avoid
potentiation and additive depressant effects.
4.5.3
Acepromazine has little, if any, analgesic effect, so that painful
procedures must be avoided particularly where animals are known to
have unpredictable temperaments. Therefore, the usual precautions
should be maintained when handling sedated horses.
4.5.4
Administer with great caution, and at low dose rates only, to debilitated
horses in states of hypovolaemia, anaemia and shock or with
cardiovascular disease.
4.5.5
The safety of use of the product in young foals or aged horses has not
been evaluated.
4.5.6
Care must be taken when administering repeated doses to horses with
hepatic disease, as evidence of accumulation and prolonged effect of
acepromazine has been observed in animals.
4.5.7
Horses should not, in any circumstances, be ridden within 36 hours of
administration of a clinical dose.
4.5.8
Horses medicated with acepromazine retain auditory and visual acuity.
Loud sounds and rapid movements should be avoided when handling
sedated horses.
Revised: 21 January 2009
AN: 01283/2008
Special precautions for the person administering the veterinary
medicinal product to animals
Avoid contact with eyes and skin.
Persons with sensitive skin or in continuous contact are advised to wear
impermeable gloves.
In the event of accidental skin or eye contact, wash/irrigate the affected
area thoroughly with clean, running water.
In the event of accidental ingestion or if eye/skin irritation persists, seek
medical attention and show the product label to the doctor.
Wash hands and exposed skin thoroughly after use.
Other precautions
No other precautions applicable.
4.6
Adverse reactions (frequency and seriousness)
4.6.1
Acepromazine is an adrenoceptor blocking drug and this causes
hypotension and lowered PCV.
4.6.2
Acepromazine administration is additive to the action of other
depressants, and will potentiate general anaesthesia.
4.7
Use During Pregnancy,Lactation or Lay
4.7.1
Do not administer the product to pregnant mares.
4.7.2
Phenothiazine compounds are excreted in small amounts into the milk
of lactating humans and animals.
No adverse effects in suckling foals have been reported.
4.8
Interaction With Other Medicinal Products and Other Forms of
Interaction
4.8.1
Do not use this product in conjunction with organophosphates, and/or
procaine hydrochloride, as it may enhance activity and potential toxicity.
4.8.2
Tranquillisers are additive to the actions of other depressants, and will
potentiate general anaesthesia. Care should be taken to reduce doses
of other premedications and anaesthetic agents, particularly parenteral
barbiturates so as to avoid potentiation and additive depressant effects.
4.8.3
Epinephrine (adrenaline) is contra-indicated in the treatment of acute
hypotension produced by overdosage of acepromazine maleate, since
further depression of systemic blood pressure can result. Other
pressoramines, such as norepinephrine (noradrenaline) or
neosynephrine, should be administered to reverse the hypotensive
effects.
Revised: 21 January 2009
AN: 01283/2008
4.9
Amount(s) to be administered and administration route
For oral administration on a bodyweight basis.
4.9.1
General Dose Range
1-2 graduations per 450kg bodyweight.
4-10ml per 450kg bodyweight (to give 0.13mg to 0.26mg
Acepromazine base per kg bodyweight).
4.9.1.1
4.9.1.2
The recommended dose required to obtain the ideal result may
vary depending on the individual temperament of the animal.
The higher dose rate is recommended for horses that are
excitable, hard to handle, or have known unpredictable temperaments.
4.9.1.3
Exceeding the recommended dose will not necessarily
intensify the effect of the product. For best results, avoid excitement
or stimulation of the horse prior to oral administration.
4.9.1.4
The tranquillisation effect may be more pronounced if food
(and water) is limited for a period of up to three hours before
administration.
4.9.1.5
On an empty stomach, tranquillisation effect will be apparent
within 30-40 minutes, and with a duration of up to 12 hours. On a full
stomach, full tranqullisation effect will be apparent within 30-40
minutes or longer with a duration of 10-12 hours.
Revised: 21 January 2009
AN: 01283/2008
4.9.1.6
The following table provides a guideline for the clinical
application of the product.
Degree of
Sedation
(Application)
Mild
tranquillisation
(training,
transport,
confinement,
new
surroundings)
Medium
tranquillisation
(training,
education,
minor
dentistry,
shoeing,
transport,
mares during
breeding)
Heavy
sedation
(Major
dentistry,
clipping, minor
surgery)
4.9.2
Dose Rate
Onset Time
Peak Effect
Total Duration
1ml per 100kg
bodyweight
before or after
feeding
30-40 minutes
2-4 hours
8-10 hours
1.5ml per
100kg
bodyweight
before or after
feeding
40-60 minutes
2-5 hours
10-12 hours
2ml per 100kg
bodyweight
before feeding
60-80 minutes
80 minutes to
6 hours
12 hours
Repeat Dosing
Normally horses will receive a single dose of the product. On the rare
occasions that repeat dosing is required the dosing interval should be 3648 hours.
4.9.3
corner
Administration Technique
The following administration technique will ensure accurate dosage, with
minimum wastage of paste. Remove cap from nozzle, turn ring until the
required dose appears on the left margin of ring. Insert nozzle into
of horse’s empty mouth, deposit paste on back of horse’s tongue. Lift
horse’s chin and hold mouth closed for a few seconds to ensure the full
dose is swallowed. Replace cap on nozzle.
Revised: 21 January 2009
AN: 01283/2008
4.10
Overdose (symptoms, emergency procedures, antidotes), if necessary
4.10.1
Symptoms
Symptoms of overdose are consistent with the hypotensive state, with
reduced blood pressure, increased heart rate, depression, incoordination
and collapse.
4.10.2
Emergency Procedure
The dose rate of noradrenaline to correct overdosage with sustained
hypotensive effect is 2-4mg in 250ml 5% dextrose in water, via slow
intravenous drip infusion, until hypotension is reversed.
The reversing effect of noradrenaline is likely to be transient, with up to a
10 minute duration, and repeated doses of noradrenaline will normally be
required when hypotensive signs reappear. The temperature, heart rate
and clinical signs of the overdosed animal must be monitored with
appropriate measures taken to avoid hyperthermia and symptoms of
shock.
4.10.3
Antidotes
There are no specific antidotes available to quickly reverse the effects of
overdosage.
4.11
Withdrawal Period(s)
Not to be used in horses intended for human consumption.
Treated horses may never be slaughtered for human consumption.
The horse must have been declared as not intended for human
consumption under national horse passport legislation.
5.
PHARMACOLOGICAL PROPERTIES
Summary of Presentation of Active Ingredients
Pharmacotherapeutic group: Antipsychotics
ATV Vet Code: QN05AA04
Acepromazine maleate is a central nervous system depressant, derived
from phenothiazine, which primarily acts by interference with, or blockage
of, dopamine receptors within the central nervous system.
5.1
Pharmacodynamic Properties
The pharmacodynamic action of acepromazine maleate is similar to other
phenothiazine derived sedative agents.
Revised: 21 January 2009
AN: 01283/2008
5.1.1
The mechanism of action results from interference with, or blockage of,
dopamine receptors on extrapyramidal sites in the brainstem, basal
ganglia, hypothalamus and limbic system of the Central Nervous System.
It provides a dose dependent tranquillising, relaxant and sedative effect. It
produces an hypotensive state without analgesic action. It’s action is
additive to other hypotensive agents.
5.2
Pharmacokinetic Properties
5.2.1
Absorption
5.2.1.1
Acepromazine maleate is readily absorbed from the
gastrointestinal tract of horses.
5.2.1.2
Due to the relatively low dose rates administered orally in
horses to exert clinical sedative effects, blood levels cannot be
accurately measured with present technology. However, the relative
degree of sedative effect, which reflects gastrointestinal absorption
patterns, has been monitored. At a dose rate of 0.13 mg/kg orally as a
paste, onset of sedation occurred within 40 minutes,reaching a
maximum clinical sedation between 120-180 minutes after
administration, with a duration of hypotensive effect of 10-12 hours.
5.2.1.3
The tranquillisation and sedative effect may be more
pronounced if food and water is limited for up to three hours before
dosing. At oral dose rates between 0.13 to 0.26 mg/kg, administered
on an empty stomach 15-30 minutes prior to feeding, tranquillisation is
apparent within 30-40 minutes, peaking at 2 hours with a duration of
up to 12 hours. At similar dose rates, administered on a full stomach
after feeding, tranquillisation effects develop between 40-60 minutes,
peaking at between two to three hours, with a duration of 10-12 hours.
5.2.2
Distribution
5.2.2.1
Administration of paste prior to feeding on an empty stomach
achieves a faster onset of action, earlier peak effect, but a similar total
duration of clinical sedation as the same dose rate given directly after
feeding.
5.2.2.2
The active, acepromazine maleate, following intravenous
administration has a plasma half life of 4.5 hours. No biodistribution
data is currently available following oral dosage of the product.
5.2.3
Biotransformation
Acepromazine maleate is extensively metabolised in the liver by hepatic
microsomal activity, with the majority of the dose being transformed into
predominantly sulfoxide and hydroxyl metabolites prior to excretion in the
urine.
Revised: 21 January 2009
AN: 01283/2008
5.2.4
Elimination
The half life following intravenous administration is 4.5 hours.
5.2.4.1
The principal route of excretion is via the urine, with up to 5
metabolites being identified in horse urine following routine
administration. The main metabolites are 2-(1-hydroxyethyl)
promazine sulfoide, 2-(1-hydroxyethyl) promazine,
7-hydroxyacepromazine and 2-(1-hydroxyethyl)-7-hydroxypromazine.
These metabolites are excreted for up to 72 hours after a single oral
dosage.
6.
PHARMACEUTICAL PARTICULARS
6.1
List of excipients
Propyl Parahydroxybenzoate
Methyl Parahydroxybenzoate
Liquid Paraffin
Polysorbate 80
Silicon Dioxide precipitated
Water Purified
6.2
Incompatabilities
The product is recommended as a sole therapeutic medication to be
administered directly by oral syringe to a horse’s mouth.
6.3
Shelf Life
Shelf life of the veterinary medicinal product as packaged for sale; 2 Years.
6.4
Special Precautions for Storage
Do not store above 25o C.
Replace cap on partly used syringes prior to storage.
Replace cap on nozzle after use.
6.5
Nature and Composition of immediate packaging
30ml dial-a-dose (graduated in 5 mL increments) white opaque high
density polyethylene syringe closed with low density polyethylene push fit
caps.
Revised: 21 January 2009
AN: 01283/2008
6.6
Special Precautions for the Disposal of unused veterinary medicinal
product or waste materials derived from the use of such products, if
appropriate
Any unused veterinary medicinal product or waste materials derived from
such veterinary medicinal products should be disposed of in accordance
with local requirements.
7.
MARKETING AUTHORISATION HOLDER
7.1
Vetsearch International (UK) Limited
52/54 Oswald Road, Scunthorpe
North Lincolnshire DN15 7PQ
UK
8.
MARKETING AUTHORISATION NUMBER(S)
VM 06036/4001
9.
DATE OF FIRST AUTHORISATION
Date of Approval: 24th January 1990
10.
DATE OF REVISION OF THE TEXT
January 2009