CARTEF 20/120 (Artemether and Lumefantrine powder for oral suspension)

🧪 Composition

Each 5 ml suspension after reconstitution contains:

• Artemether – 20 mg
• Lumefantrine USP – 120 mg
• Excipients – q.s.
• Colour – Sunset Yellow FCF

⚙️ Properties

Artemether is the most active derivative of the Artemisinines, a new class of antimalarial drugs derived from Artemisinin. The latter compound is extracted from the plant Artemisia Annua, and Artemether is prepared semi-synthetically. Lumefantrine is a synthetic aryl amino alcohol similar to mefloquine and halofantrine.

🎯 Indications

CARTEF 20/120 Oral Suspension is indicated for the treatment of malaria in children, caused by all forms of Plasmodium, including severe malaria caused by multiple drug-resistant strains of P. falciparum.

🔬 Pharmacological Properties

Pharmacodynamics

• Both components have distinct action sites in the malarial parasite.
• Artemether’s endoperoxide bridge generates singlet oxygen and free radicals—cytotoxic to plasmodia.
• Morphological changes in parasitic membranes are due to free-radical action.
• Lumefantrine interferes with polymerization processes.
• In vitro tests suggest both reduce nucleic acid synthesis and inhibit protein synthesis.
• Artemether acts as a blood schizonticide and clears gametocytes in clinical trials.

Pharmacokinetics

• Artemether:

  • Rapid absorption (therapeutic levels in 60–90 mins)
  • Metabolized to Dihydroartemisinin (DHA)
  • Elimination half-life: 2–4 hours
  • Plasma protein binding: ~50%
  • Distribution equal between cells and plasma

• Lumefantrine:

  • Absorption influenced by lipids and food (10% when fasting, 100% with normal diet)
  • N-debutylated in liver; metabolite is 5–8× more potent
  • Protein binding: ~95%
  • Elimination half-life: 4–6 days
  • Excreted via bile and feces

🧴 Direction for Reconstitution

To make 60 ml suspension:

1. Add 45 ml boiled and cooled water.
2. Invert bottle and shake until powder is dispersed.
3. Slowly add more water up to the mark on the bottle.
4. Shake well before use.
5. Store reconstituted suspension in refrigerator (2°C to 8°C).
6. Use within 7 days.
7. Second dose: 8 hours after first dose.
8. Administer with food, preferably fatty meals.

If vomiting occurs within 1 hour of dosing, repeat the dose immediately.
Take dosage exactly as recommended to prevent recurrence of infection.

⚠️ Pharmaceutical Precautions & Contraindications

• Contraindicated in individuals hypersensitive to Artemether or Lumefantrine.
• No strict contraindication for Artemether in children.
• Caution in patients on QT-prolonging drugs (macrolides, fluoroquinolones, imidazoles).
• Use in pregnancy only if essential—especially in cerebral malaria.
• Not recommended during breastfeeding; wait at least one-week post-treatment before resuming.

🔄 Drug Interactions

• No specific negative interactions observed.
• Artemether enhances activity of other antimalarials.
• Avoid grapefruit juice—it retards metabolism of some antimalarials.

🚨 Side Effects

• Artemether:

  • Virtually no side effects
  • Transient lab abnormalities (e.g., rise in transaminases, drop in reticulocytes)
  • Possible transient abdominal pain, tinnitus, diarrhea at high doses

• Lumefantrine:

  • ECG pattern may be influenced by prior use of halofantrine or quinine
  • Consider monotherapy with Artemisinin derivatives in severe cases

• Common side effects:

  • Rash
  • Sleep disturbances
  • Nausea
  • Diarrhea
  • Coughing

Seek medical attention if symptoms persist.

🧊 Storage

• After reconstitution: store in refrigerator (2°C–8°C)
• Consume within 7 days
• Keep out of reach of children
• Store below 30°C, protected from light and moisture

SHAKE WELL BEFORE TAKING EACH DOSE

📦 Presentation

A 60 ml bottle of dry powder with insert, packed in a carton.
Made in India