Alternate Name(s):
Artesunic acid
Classification:
Antimalarial; Anti-Protozoal agent; Artemisinin derivative
Original Date:
August 2009
Revised Date:
August 2017
Indications:
- Treatment for severe and complicated malaria and infections due to chloroquine-resistant or multi-drug resistant strains of malaria
Reconstitution and Stability:
US product (Walter Reed supply):
- Available as 110 mg/vial sterile powder with diluent (phosphate buffer) for reconstitution.
- Refrigerate vials (2-10 C). Buffer may be stored at room temperature or refrigerated (phosphate crystals may form in the buffer at low temperatures - use only if solution is clear and colourless after gentle warming)
- Withdraw 11.5 mL from vial of phosphate buffer into a 20 mL syringe
- Attach a 0.2 micron filter to syringe containing phosphate buffer
- Add 11.5 mL of phosphate buffer, through the filter, slowly (against vial wall) into each vial of 110 mg artesunate to get 10 mg/mL
- Gently swirl for 5 - 6 minutes until completely dissolved.
- Stable 1 hour after reconstitution. Administer as soon as possible following reconstitution or further dilution. Discard unused solution.
- For IM administration: use the same preparation, dilution and dosage as for IV administration
Chinese product (Artesun):
- Available as 120 mg/vial with diluent (sodium bicarbonate 50 mg/mL ampoule) and 0.9% NaCl ampoule
- Store at room temperature. Protect from light.
- Reconstitute vial with 2 mL of sodium bicarbonate solvent (provided ampoule)
- Shake for several minutes (not too vigorously) until powder is complete dissolved and solution is clear. Discard if solution not clear or a precipitate is present.
- For IV administration: Add 10 mL 0.9 % NaCl (provided vial) to the reconstituted solution to get 10 mg/mL
- Shake to mix well. Solution should be clear. Discard if solution appears cloudy or a precipitate is present.
- Stable 1 hour after reconstitution. Administer as soon as possible following reconstitution or further dilution. Discard unused solution.
- For IM administration: Add 4 mL 0.9% NaCl (provided vial) to the reconstituted solution to get 20 mg/mL
Compatibility:
- Solutions Compatible: D5W, 0.9% NaCl
- Incompatible: Water for injection (no data)
Administration:
(For approved routes of administration by nursing personnel, refer to Policy for the Administration of Intravenous Medications.)
| SC | NO |
| IM |
YES -if IV access cannot be obtained - into anterior thigh - may need to divide dose and inject in several sites US product - 10 mg/mL Chinese product - 20 mg/mL |
| IV Direct | YES - preferred Usual dilution: with 5 mL D5W or 0.9% NaCl prior to injection Infusion time: over 1 - 2 minutes |
| IV Intermittent Infusion | NO |
| IV Continuous Infusion | NO |
Dosage:
(For neonatal dosages, refer to Neonatal IV Drug Manual.)
Pediatric/Adult:
- 2.4 mg/kg IV at 0, 12, 24 and 48 hours (total of 4 doses = 9.6 mg/kg)
- First dose should be admininistered STAT
- Obese patients should be dosed based on actual body weight (no maximum dose)
- Dose adjustment not required in renal or liver dysfunction
- An oral agent is required as follow-on therapy within 4 hours after last dose of IV artesunate ie. Malarone (atovaquone /proguanil)
Potential hazards of parenteral administration:
- Very well tolerated in adults and children. Observe patient for 30 minutes following administration for signs of an allergic reaction
- Hypersensitivity : allergic reactions (rash, urticaria, swelling, watery eyes, shortness of breath, chest pain, anaphylaxis)
- Cardiovascular: bradycardia, heart block
- Gastrointestinal: anorexia, taste alteration, nausea, vomiting, diarrhea
- Central nervous system: dizziness, lightheadedness, headache
- Reversible decrease in reticulocyte count
- Increased liver enzymes
Notes:
- Artesunate is not marketed in Canada & falls under the jurisdiction of the Special Access Program (SAP) therefore requires a verbal consent from a parent which must be documented in the patient's medical chart before administration
- No known drug interactions at this time but note that it is a derivative of artemisinin which is metabolized via cytochrome P450 2B6
- Pregnancy -IV quinine preferred in the first trimester& IV artesunate is the drug of choice in the second and third trimester (Canadian Malaria Network July 2009)
- Artesunate is converted in the body to its active metabolite, dihydroartemisinin
- US product (Walter Reed supply): vials have the date manufactured and do not have a specified expiry date, as testing of the product is ongoing
- Chinese product (Artesun): expiration date as per package