artesunate (Rx)

Brand and Other Names:
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injection, lyophilized powder for reconstitution

  • 110mg/vial
  • Not FDA approved nor commercially available in US; however, CDC has taken action to ensure IV artesunate is available through an expanded use investigational new drug (IND) protocol
  • CDC malaria hotline (770-488-7788): Call to obtain IV artesunate; call 770-488-7100 evenings or weekends and ask for CDC malaria expert

Malaria

CDC IND protocol: Indicated as first-line treatment for severe malaria

Consider treating with oral antimalarials while waiting for IV artesunate; when IV artesunate arrives, discontinued oral antimalarials

2.4 mg/kg IV at 0 hr, 12 hr, 24 hr, and 48 hr

Follow-on drug therapy

  • Administer follow-on drug after IV artesunate regimen completed (eg, artemether/lumefantrine, atovaquone/proguanil, doxycycline, mefloquine)
  • Patients who still cannot tolerate oral medications after completing artesunate treatment may continue artesunate IV qDay (not to exceed total course of 7 days) or switch to IV doxycycline or clindamycin for 7 days

Dosage Forms & Strengths

injection, lyophilized powder for reconstitution

  • 110mg/vial
  • Not FDA approved nor commercially available in US; however, CDC has taken action to ensure IV artesunate is available through an expanded use investigational new drug (IND) protocol
  • CDC malaria hotline (770-488-7788): Call to obtain IV artesunate; call 770-488-7100 evenings or weekends and ask for CDC malaria expert

Malaria

CDC IND protocol: Indicated as first-line treatment for severe malaria in infants and children

Consider treating with oral antimalarials while waiting for IV artesunate; when IV artesunate arrives, discontinued oral antimalarials

≥20 kg: 2.4 mg/kg IV at 0 hr, 12 hr, 24 hr, and 48 hr

<20 kg: 3 mg/kg IV at 0 hr, 12 hr, 24 hr, and 48 hr

Follow-on drug therapy

  • Administer follow-on drug after IV artesunate regimen completed (eg, artemether/lumefantrine, atovaquone/proguanil, doxycycline, mefloquine)
  • Patients who still cannot tolerate oral medications after completing artesunate treatment may continue artesunate IV qDay (not to exceed total course of 7 days) or switch to IV doxycycline or clindamycin for 7 days
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Adverse Effects

>10%

Anorexia on Day 1-2 (34%)

Dizziness, nausea on Day 1-2 (15-16%)

1-10%

Diarrhea on Day 1-2 (1%)

Frequency Not Defined

Urticaria

Rash

Hemoglobinuria

Seizures

Neuropsychiatric reactions

Reversible neurologic changes

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Warnings

Contraindications

Hypersensitivity to artemisinins

Cautions

Rare, delayed post-artemisinin hemolytic anemia reported; monitor for up to 4 wk after treatment; patients with higher parasitemias may be more prone to hemolytic anemia

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Pregnancy & Lactation

Pregnancy

May administer to pregnant women in second and third trimesters

Data are limited for first trimester of pregnancy; no harmful effects have been observed

Animal studies

  • Causes fetal toxicity in rats and rabbits resulting in fetal resorption and abortion
  • Low incidence of cardiac malformations and skeletal defects also observed

Clinical considerations

  • Severe malaria is life-threatening for pregnant women and their fetuses, and artesunate should not be withheld if quinidine is unavailable, contraindicated, ineffective, and/or not tolerated

Lactation

Limited distribution into human breast milk

LactMed (Toxnet.mlm.nih.gov) states limited information indicates that a maternal dose of 200 mg PO produced low levels in milk and would not be expected to cause any adverse effects in breastfed infants, especially if aged >2 months

Withholding breastfeeding for 6 hr after dose should markedly reduce amount infant receives

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

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Pharmacology

Mechanism of Action

Artemisinin derivative

Mechanism of antimalarial action has been hypothesized to involve an iron-mediated cleavage of the endoperoxide bridge, which produces oxygen radicals, which then react with nearby molecules, interfering with parasite function

Pharmacokinetics

Half-life, elimination: 1 hr (dihydroartemisinin)

Metabolites: Dihydroartemisinin, active

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Administration

IV Preparation

Provided as sterile dry-filled powder with diluent for reconstitution, phosphate buffer

Withdraw 11 mL diluent and inject into artesunate vial; gently swirl for 5-6 minutes to dissolve

Resulting solution: 10 mg/mL

Administer within 1 hr of reconstitution

IV Administration

Administer as slow IV over 1-2 minutes through a 0.8-micron hydrophilic polyethersulfone filter

Storage

Unopened vials: Store at 2-10°C (35-50°F)

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Images

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Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
  • Manage and view all your plans together – even plans in different states.
  • Compare formulary status to other drugs in the same class.
  • Access your plan list on any device – mobile or desktop.

The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.