Falcigo injection (Artesunate)

Artesunate is a water-soluble hemisuccinate derivative of artemisinin. It is unstable in neutral solution and the injectable formulation must be prepared immediately before use in 5% (w/v) sodium bicarbonate solution to produce the salt sodium artesunate. After parenteral administration, it is rapidly hydrolysed to the active metabolite dihydroartemisinin. The oral formulation is probably hydrolysed completely before entering the systemic circulation. Artesunate has been reported to clear fever in patients with severe falciparum malaria 16-25 hours after parenteral administration.

Artesunate Uses

Artesunate is used to treat chloroquine resistant malaria and complicated malaria like cerebral malaria.

• orally: treatment of uncomplicated falciparum malaria in areas where there is evidence of chloroquine, pyrimethamine/sulfadoxine, mefloquine and quinine resistance. It should always be administered together with mefloquine in full therapeutic dose.

• parenterally: treatment of severe falciparum malaria in areas where there is evidence of quinine resistance. Radical cure is then effected with a full course of an effective oral antimalarial.

How it works

Artesunate belongs to class of medications called anti-malarial. It acts by producing free radicals which kills the malarial parasite (plasmodium).

How to take artesunate 50 mg tablets

Always take artesunate tablets exactly as your doctor or health care provider has told you. Artesunate 50 mg tablets are usually taken in combination with another medicine to treat malaria. Artemisinin-based combination therapy (act) in combination therapy in adults and children, artesunate should be given at 4 mg/kg body weight once daily for three days (range 2-10 mg/kg; 200 mg per day in adults). Artesunate dosing scheme in combination therapy (treatment duration 3 days) age no of tablets per day (dose) 1-6 years 1 tablet once daily (50 mg/day) 7-13 years 2 tablets once daily (100 mg/day) older than13 years 4 tablets once daily (200 mg/day)

Oral administration

Adults and children over 6 months: 5 mg/kg orally on the first day followed by 2.5 mg/kg on the second and third days in combination with mefloquine (15 mg/kg) in a single dose on the second day. In a few areas, a higher dose (25 mg/kg) of mefloquine may be required for a cure to be obtained.

Parenteral administration

The powder for injection should be reconstituted with 5% sodium bicarbonate and diluted in an equal volume of physiological saline or 5% (w/v) glucose. It should be administered immediately by either intravenous or intramuscular injection.

A loading dose of 2 mg/kg should be followed by 1 mg/kg after 4 hours and 24 hours. Thereafter a dose of 1 mg/kg should be given daily until the patient is able to tolerate oral artesunate or for a maximum of 7 days.

If you use more artesunate 50 mg tablets than you should if you have taken too many tablets or if someone accidentally swallows some, there is no immediate danger. However, you should contact your doctor, health care provider or the nearest hospital emergency department for further advice. If you forget to take artesunate 50 mg tablets when artesunate 50 mg tablets is normally to be taken once daily (in combination therapy): if you accidentally miss a dose take the missed dose as soon as possible. Make sure you take the next dose least 8 hours but not more than 24 hours after that dose. If your next regular dose is scheduled more than 8 hours after the dose made up for, then simply take your normal dose when it is due. Do not take a double dose to make up for forgotten individual doses. When artesunate 50 mg tablets is normally to be taken twice daily: if you accidentally miss a dose, take the missed dose as soon as possible. Take the next regular dose as scheduled. If you notice only when your next dose is due, you may take a double dose to make up for the forgotten individual dose. If you stop taking artesunate 50 mg tablets make sure that the medicine is administered for as long as your doctor has told you, even if you are feeling better. If you stop the medicine too soon, your infection may not be completely cured. This may result in relapse of your malaria symptoms, and possibly increased problems in treating malaria should you get it again. You should not stop treatment unless your doctor or health care provider tells you to.

Contraindications

Oral artesunate should not be used during the first trimester of pregnancy.

Precautions

Parenteral artesunate should be used for the treatment of severe falciparum malaria only where there is evidence that the antimalarial efficacy of quinine is declining. The powder for injection is difficult to dissolve and care should be taken to ensure that it is completely dissolved before parenteral administration. It should always be used immediately following reconstitution. If the solution is cloudy or a precipitate is present, the parenteral preparation should be discarded.

Use in pregnancy

Little experience has been gained with the use of this drug in pregnancy but the parenteral preparation should not be withheld if it is considered life-saving to the mother.

Adverse effects

Drug-induced fever can occur. Neurotoxicity has been observed in animal studies but not in humans. In view of the uncertainty about toxic effects, caution should be exercised when more than one 3-day treatment is given. Cardiotoxicity has been observed following administration of high doses. How to store artesunate 50 mg tablets keep out of the reach and sight of children. Do not store above 30ºc, store in the original packaging. Do not use artesunate 50 mg tablets after the expiry date which is stated on the carton after exp. The expiry date refers to the last day of that month. Do not use artesunate 50 mg tablets if you notice any visible sign of deterioration. Medicines should not be disposed of via waste water or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.

Expert advice

• Do not start or continue the artesunate tablets and consult your doctor if you are allergic (hypersensitive) to artesunate.
• Do not start or continue the artesunate tablets and consult your doctor you are in first 3 months of pregnancy  or if you are breast feeding.
• Do not drive or operate machinery after taking artesunate because you may feel sleepy.

Before you take artesunate do not take artesunate 50 mg tablets

If you are hypersensitive (allergic) to artesunate or to any of the other ingredients of artesunate 50 mg tablets (see section 6, what artesunate 50 mg tablets contains), take special care with artesunate 50 mg tablets if you have experienced rash or urticarial reaction to artesunate before, you should not be treated with artesunate 50 mg tablets, if avoidable, since this has been associated with recurrence of symptoms and occasionally with the development of severe allergic reactions

Frequently asked questions

Q. What artesunate is and what it is used for

Artesunate 50 mg tablets is used for the treatment of uncomplicated cases of malaria. Artesunate 50 mg tablets is indicated only for attacks due to plasmodium falciparum (a particular type of malaria parasite), against which the medicine is active. It reduces the number of malaria parasites in your body. Your doctor has found that you have malaria and so has prescribed the tablets to treat your malaria infection. For complete cure it is important that you complete the prescribed dose as advised by your doctor, health care worker or pharmacist.

Q. Is artesunate/falcigo safe during pregnancy or breastfeeding?

No. Artesunate (also available as falcigo) should not be given during 1st trimester of pregnancy. During second and third trimester and breastfeeding, the drug can be used only if benefit outweighs the risk. Patients should follow the advice of the doctor regarding its use.patients should follow the advice of the doctor regarding its use.

Q. Is artesunate banned in india?

No, it is available in india with doctor’s prescription only.

Q. What is artesunate amodiaquine/ winthrop/artesunate injection?

These are trade names of artesunate containing products. It is used for the treatment of malaria. Patients should follow the advice of the doctor regarding its use.

Q. Why is artesunate better than quinine?

Intramuscular or intravenous injection of artesunate has shown better treatment effects than quinine. Always consult your doctor regarding its use.

Q. Does artesunate contain sulphur?

No, it does not contain sulphur.

Q. How does artesunate work?

It acts by producing free radicals which kills the malarial parasite (plasmodium) q. Where does artesunate come from? It is derived from artemisinin tree.