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Here is the list of the most frequently asked questions about Alfaxan®. We hope that you will find this information useful in your every-day anaesthetic practice.

     
  What is Alfaxan®?
   
  How does Alfaxan® work?
   
  Which pre-meds can
be used with Alfaxan®?
   
  Why should Alfaxan® be injected slowly, over 60 seconds?
   
  Can I inject other drugs
in the same syringe?
     
  What happens if I inject
the drug extra-vascularly?
     
  Can Alfaxan® be used
to maintain anaesthesia?
     
  How safe is Alfaxan®?
     
  How is Alfaxan®
metabolised in the body?
     
  Does Alfaxan® cause
histamine release?
     
  Can Alfaxan® be
used in other species?
     
  Is Alfaxan® safe
to use in pregnancy?
     
  How is Alfaxan® different to
an alfaxalone / alfadolone anaesthetic combination?
     

If you cannot find the topic you are interested in amongst the questions and answers listed below, please contact us via email, by clicking here.

Alternatively please call our free dedicated Alfaxan® technical support line on:
0800 345 7560
(lines open from 9am to 5pm Monday to Friday).

References:

1.Jurox Pharmacovigilance Report JX9604-SR004

2.Data on file, Jurox study report no. JX9604.07-H003

3.Data on file, Jurox safety studies RD9604.03-H005, JX9604.07-H004

4.Data on file, Jurox study number RD9604.03-H002

5.Data on file, Jurox study number JX9604.07-H001

6.Data on file, Jurox studies number JX9604.03-E017, JX9604.03-C016, JX9604.07-H009 and JX9604.07-C006

7.Alfaxan® UK SPC

8.Data on file, Jurox study number JX9604.03/06 (dog) , RD9604.03/01 (cat)

Alfaxan® FAQ's


What is Alfaxan®
Top

Alfaxan® is an injectable anaesthetic agent for induction and maintenance of general anaesthesia in dogs and cats. Alfaxan® is a clear, colourless, aqueous solution of alfaxalone (3-α-hydroxy-5-α-pregnane-11,20-dione), a neuroactive steroid molecule with properties of a general anaesthetic.

Molecule

The alfaxalone molecule is solubilised in the Alfaxan® formulation using 2α- hydroxypropyl ß cyclodextrin. Cyclodextrins are complex polysaccharides derived from starch that supply a hydrophobic centre for lipophilic drugs like alfaxalone.

Unlike Cremaphor® EL, HPCD(2α-hydroxypropyl ß cyclodextrin) does not cause histamine release in dogs and cats.


How does Alfaxan® work?
Top

The primary mechanism for the anaesthetic action of alfaxalone is modulation of neuronal cell membrane chloride ion transport, induced by binding of alfaxalone to GABAA cell surface receptors.

Mechanism


Which pre-meds can be used with Alfaxan®?
Top

Table below contains pre-meds that are most commonly used with Alfaxan®.

Drug Class Examples
Phenothiazines acepromazine maleate
Benzodiazepines diazepam, midazolam hydrochloride,
Alpha-2-adrenoceptor agonists xylazine hydrochloride, medetomidine hydrochloride
Opiates buprenorphine hydrochloride, butorphanol tartrate,
morphine sulfate, methadone
NSAIDs carprofen, meloxicam

If your practice has its favourite pre-med combination for dogs and cats, please contact our free dedicated Alfaxan® technical support line on 0800 345 7560 (lines open from 9am to 5pm Monday to Friday) or click here if you wish to send us an email request instead. We will be happy to produce a custom-made, detailed Alfaxan® pre-med dosage chart for your practice, with doses in ml/kg.


Why should Alfaxan® be injected slowly, over 60 seconds?
Top

It takes about 20-30 seconds for Alfaxan® injected into the cephalic vein to reach the brain. If Alfaxan® is injected as a bolus, then less time is available for brain absorption of the alfaxalone needed to induce anaesthesia. A lower total amount of alfaxalone crosses the blood-brain barrier, but higher initial concentrations might be reached in the brain.

This has two consequences:
the higher initial concentration in the brain is more likely
to cause unwanted side-effects such as apnoea.
not all the drug will cross into the brain and the rest will re-distribute into the other tissues and will be wasted, resulting in shorter, less satisfactory anaesthesia.

By giving Alfaxan® slowly, over 60 seconds, one ensures that there is a steady increase in blood concentration (and therefore brain concentration), which leads to smoother induction into anaesthesia. The injection can be stopped when the brain concentration is just at the required level.


Can I inject other drugs in the same syringe?
Top

We do not recommend the concurrent injection of any drug in the same syringe.


What happens if I inject the drug extra-vascularly?
Top

Alfaxan® does not cause irritation if injected extra-vascularly1


Can Alfaxan® be used to maintain anaesthesia?
Top

Yes. Alfaxan® can be used to maintain anaesthesia either by ‘topping up’ as required or by constant rate infusion. Recommended dosages are listed in the table below.

DOG Maintenance
Cat Maintenance

Constant
rate
infusion

(6-7mg/kg/hour
of alfaxalone)

Bonus dose
each 10min
maintenance

(1.0-1.2mg/kg
of alfaxalone)

Constant
rate
infusion

(7-8mg/kg/hour
of alfaxalone)

Bonus dose
each 10min
maintenance

(1.1-1.3mg/kg
of alfaxalone)

Alfaxan® dose (kg/ml/hour)
Alfaxan® dose (kg/ml/every 10min)
Alfaxan® dose (kg/ml/hour)
Alfaxan® dose (kg/ml/every 10min)
0.6 - 0.7
0.1 - 0.12
0.7 - 0.8
0.11 - 0.13

Please refer to the Alfaxan® dosage chart for more information about “topping up” dosage rates. For further information about constant rate infusion dosages please click here.


How safe is Alfaxan®?
Top

Alfaxan® has a very wide safety margin:

In an acute tolerance study all dogs survived IV injection of Alfaxan® at 10 times (i.e. 20mg/kg BW) of the recommended clinical dose when administered adequate ventilatory support (intermittent positive pressure ventilation -IPPV) 2

In an acute tolerance study all cats survived IV injection of Alfaxan® at 5 times (i.e. 25mg/kg BW) of the recommended clinical dose when administered adequate ventilatory support (intermittent positive pressure ventilation – IPPV) 3


How is Alfaxan® metabolised in the body?
Top

Alfaxan® is metabolised rapidly in the liver. Alfaxalone has a very short plasma elimination half-life in dogs and cats4,5

Alfaxalone is completely cleared from the body within a few hours after single administration 4,5

When Alfaxan® is administered as a repeated bolus or as total intravenous anaesthesia (TIVA) as a continuous rate infusion, alfaxalone levels do not accumulate and recovery periods do not appear to be prolonged6. This supports the claim that the repeated use of the product over a short period of time (for procedures lasting for up to one hour7) does not present a risk of accumulation.


Does Alfaxan® cause histamine release?
Top

No, please see Figures 1 and 2 below for more information8. Normal histamine levels in dogs and cats are <1μmol/L and all the values in Figures 1 and 2 below are below 1μmol/L.

Figure 1: Normal histamine levels in dogs and cats are <1µmol/L and all the values in Figures 1 and 2 below are below 1µmol/L.

Figure1

Cats were dosed with Alfaxan® at a number of different doses (5, 10, 20 & 30mg/kg - up to 6 times the recommended clinical dose) and there was no significant rise in blood histamine levels.

Figure 2: Blood histamine levels in dogs dosed with 30mg/kg of Alfaxan® as an IV bolus injection.

Figure2

Dogs were dosed with Alfaxan® at 30mg/kg (15X the recommended dose) and there was no significant alteration in their blood histamine levels.


Can Alfaxan® be used in other species?
Top

While Alfaxan® is only licensed for use in cats and dogs there is information available about the use of Alfaxan® in other species. Please click here if you wish to receive more information.


Is Alfaxan® safe to use in pregnancy?
Top

The safety of Alfaxan® has not been established during pregnancy and lactation, in breeding animals or those intended for breeding in the future. However, studies using alfaxalone in pregnant mice, rats and rabbits have demonstrated no deleterious effects on gestation of the treated animals, or on the reproductive performance of their offspring.


How is Alfaxan® different to an
alfaxalone / alfadolone anaesthetic combination?
Top

The only active ingredient in Alfaxan® is alfaxalone, not a combination of alfaxalone and alfadolone.

The previously available commercial preparation of alfaxalone / alfadolone also contained Cremaphor-EL which has been shown to cause histamine release in cats and dogs. Alfaxan® contains 2-hydroxypropyl-b-cyclodextrin (HPBC) as the primary excipient, which does not cause histamine release.

Because of the above differences, Alfaxan® has different characteristics to an alfaxalone / alfadolone combination. The most noticeable differences are: Alfaxan® does not cause histamine release, provides smooth inductions, produces less “excitement” during recovery and has shorter duration of action.