ACTIVON INJECTION

VETERINARY MEDICINE   

SCHEDULING STATUS

S4

COMPOSITION

Each ml contains:     Diprenorphine HCl 12 mg

Preservative:              Chlorocresol 0,1 % m/v         

CATEGORY AND CLASS OF MEDICINE

C 1.3.2 Opioid antagonist

PHARMACOLOGICAL ACTION

Diprenorphine is a relatively potent antagonist of the oripavine series that binds with equal affinity to µ-, δ- and κ-opioid receptors. Although its action is much closer to that of an antagonist and it is routinely used as a reversal agent for potent opioid agonists, it does retain some agonistic activity. Diprenorphine has no analgesic activity in rodents and primates, suggesting a lack of agonistic activity at the µ-opioid receptors although some agonistic activity has been found at κ-opioid receptors in these species. 

PHARMACOKINETIC AND PHARMACODYNAMIC PROPERTIES

Diprenorphine has a quick onset of action following administration and is rapidly metabolized. When given intramuscularly, it takes 10-20 minutes to reverse the effects of etorphine while intravenous administration shows a faster onset of action of 2-5 minutes. In mice treated with etorphine, the antagonistic effect of diprenorphine peaked 30 minutes after subcutaneous administration with a duration of action exceeding 90 minutes.

INDICATIONS

ACTIVON is indicated for the reversal of CAPTIVON (etorphine HCl) immobilization in wildlife animals.

CONTRAINDICATIONS

None recorded. 

WARNINGS

Opioids may be less effective if wildlife animals are to be re-immobilized within 24 hours following treatment with ACTIVON, and an alternative immobilization protocol should be considered in such cases.

The safety of ACTIVON in pregnant and lactating wildlife animals has not been established. 

ACTIVON residue studies have not been conducted in wildlife animals and consequently, human and predator consumption of carcasses from animals treated with ACTIVON is not advisable.

DOSAGE AND DIRECTIONS FOR USE

Administration by intravenous or intramuscular injection is recommended. Refer to the table below for ACTIVON dosing. 

Wildlife species CAPTIVON 98 dose ACTIVON dose
Elephant, rhino and giraffe 1 mg 3-5 mg 
Other 1 mg 2-3 mg

SIDE EFFECTS AND SPECIAL PRECAUTIONS FOR USE

ACTIVON may produce sedation and other opioid effects due to its partial agonistic activity. A degree of sedation may persist following reversal of CAPTIVON with ACTIVON and this should be considered when using ACTIVON in prey species that are to be released in predator areas. In white rhino, ACTIVON does not antagonize the effects of CAPTIVON completely and the animal may remain partially narcotized for up to eight hours following the administration of ACTIVON.

Accidental exposure to ACTIVON could have serious effects on humans due to the high concentration of the medicine. The following precautions should be taken by veterinarians when using ACTIVON:

  • Do not work with ACTIVON unaccompanied. 
  • Wear gloves when handling ACTIVON. Ensure water or an appropriate irrigation solution is available to treat accidental exposure of the skin or eyes.
  • Once the required dose of ACTIVON has been withdrawn from the vial, the needle should be immediately discarded into a closed container or sharps bin. 
  • ACTIVON should not be used in blowpipes or similar devices where the medicine solution is pressurized. 
  • ACTIVON should not be used as an antagonist in the event of accidental human exposure to CAPTIVON.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT 

Overdosing with ACTIVON may cause continued immobilization due to its partial agonistic activity.

IDENTIFICATION

A clear, colourless solution free from visible particulate matter. 

PRESENTATION

ACTIVON is supplied in a 10 ml amber vial with a grey stopper and a silver aluminium. 

STORAGE INSTRUCTIONS

Store at or below 25 °C. 

Protect from light. 

Once the rubber stopper has been pierced, the contents of the vial must be used within two weeks. 

KEEP OUT OF REACH OF CHILDREN AND UNINFORMED PERSONS. 

REGISTRATION NUMBER 

93/1.3.2/8

NAME AND BUSINESS ADDRESS OF HOLDER OF CERTIFICATE OF REGISTRATION

Wildlife Pharmaceuticals (Pty) Ltd

38 Wilkens Street

Rocky Drift

White River 1240

South Africa