Falcitar
Falcitar Uses, Dosage, Side Effects, Food Interaction and all others data.
Falcitar is a potent and rapidly-acting blood schizontocide derived from the leaves of the chinese herb, Armesia annua. The exact mode of action is not clear but clinical studies have confirmed the effectiveness of artesunate in P. vivax and falciparum malaria.
Falcitar is an artemisinin derivative that is metabolized to DHA, which generates free radicals to inhibit normal function of Plasmodium parasites. It has a short duration of action due to its short half life, and a moderate therapeutic index. Patients should be counselled regarding the risk of post treatment hemolytic anemia and hypersenstivity.
| Trade Name | Falcitar |
| Availability | Prescription only |
| Generic | Artesunate |
| Artesunate Other Names | Artesunate, Artesunato, Artesunatum, Artesunic acid |
| Related Drugs | doxycycline, clindamycin, hydroxychloroquine, Plaquenil, Cleocin |
| Type | Injection |
| Formula | C19H28O8 |
| Weight | Average: 384.425 Monoisotopic: 384.178417862 |
| Protein binding | Artesunate and its metabolite DHA are approximately 93% protein bound in plasma. Artesunate can bind to serum albumin. |
| Groups | Approved, Investigational |
| Therapeutic Class | Anti-malarial drugs |
| Manufacturer | Micro Labs |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Falcitar can quickly and reliably control the acute attack of malaria. It is suitable to salvage the patients with pernicious malaria and treat P. falciparum malaria and P. vivax malaria. It is effective against malaria caused by chloroquine resistant strain of plasmodium falciparum.
Falcitar is also used to associated treatment for these conditions: Acute Uncomplicated Plasmodium Falciparum Malaria, Malaria, Cerebral, Severe Malaria
How Falcitar works
Falcitar is metabolized to the active DHA. the endoperoxide bridge of DHA reacts with heme, generating free radicals which inhibit protein and nucleic acid synthesis of the Plasmodium parasites during all erythrocytic stages. Reactions with these free radicals can also lead to alkylation of parasitic proteins such as a calcium adenosine triphosphatase and EXP1, a glutathione S-transferase.
Dosage
Falcitar dosage
Adult: 5 days treatment: on the 1st day 2 tablets twice and 2nd day onward 1 tablet twice daily for remaining 4 days
Children:
- 1-3 years: 5 days treatment: on the 1st day ½ tablet twice and 2nd day onward ¼ tablet twice daily for remaining 4 days
- 4-5 years: 5 days treatment: on the 1st day 1 tablet twice and 2nd day onward ½ tablet twice daily for remaining 4 days
- 6-12 years: 5 days treatment: on the 1st day ½ tablet twice, 2nd day 1 tablet twice and 3rd day onward ½ tablet twice daily for remaining 3 days
Prophylmcis: 100 mg tablet once a week, from 1 week before entering malarial areas, to 4 weeks after leaving the area.
Side Effects
Transient and reversible reticulocytopaenia, drug fever, rash, bradycardia, transient 1st-degree heart block and reversible elevation of serum transaminases.
Toxicity
Data regarding overdoses of artesunate are rare. Patients experiencing an overdose may present with pancytopenia, melena, seizures, multiorgan failure, and death. Treat overdose with symptomatic and supportive measures.
Precaution
Hepatic or renal insufficiency; Pregnancy and lactation.
Interaction
Antimalarial potentiating action seen with mefloquine, primaquine and tetracycline. Additive effect with chloroquine. Antagonistic effect with pyrimethamine and sulphonamides.
Food Interaction
No interactions found.Falcitar Drug Interaction
Unknown: acetylcysteine, amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, epinephrine, aspirin, celecoxib, ubiquinone, ubiquinone, glutamic acid, lysine, acetaminophen, fluoxetine, bioflavonoids, thiamine, cyanocobalamin, ascorbic acid, cholecalciferol, menaquinone, zinc sulfate, ondansetron
Volume of Distribution
The volume of distribution of artesunate is 68.5L while the volume of distribution of DHA is 59.7L.
Elimination Route
The Cmax of artesunate is 3.3µg/mL while the Cmax of the active metabolite DHA is 3.1µg/mL. The AUC of artesunate is 0.7µg*h/mL while the AUC of DHA is 3.5µg*h/mL. After intravenous artesunate, DHA has a Tmax of 0.5-15 minutes in adult patients and 21-64 minutes in pediatric patients. Intramuscular artesunate has a Tmax of 8-12 minutes. Infants less than 6 months old will have a higher AUC due to an undeveloped UGT metabolic pathway.
Half Life
The elimination half life of artesunate is 0.3h with a range of 0.1-1.8h. The elimination half life of DHA is 1.3h with a range of 0.9-2.9h. Half life after intramuscular administration is 48 min in children and 41 min in adults.
Clearance
The clearance of artesunate is 180L/h while the clearance of DHA is 32.3L/h.
Elimination Route
The main route of elimination in humans is unknown. In rats, a dose of artesunate is 56.1% eliminated in the urine and 38.5% in the feces.
Pregnancy & Breastfeeding use
Pregnancy category is not classified. FDA has yet not classified the drug into a specific pregnancy catagory.
Contraindication
Hypersensitivity.
Innovators Monograph
You find simplified version here Falcitar
Falcitar contains Artesunate see full prescribing information from innovator Falcitar Monograph, Falcitar MSDS, Falcitar FDA label
FAQ
What is Falcitar used for?
Falcitar is a medication used to treat malaria. The intravenous form is preferred to quinine for severe malaria. Often it is used as part of combination therapy, such as artesunate plus mefloquine.
How safe is Falcitar?
Intravenous Falcitar was safe and effective in treating severe malaria in adults in the United States, researchers reported in Clinical Infectious Diseases.
What are the common side effects of Falcitar?
Common side effects of Falcitar are include:
- Hives.
- Rash.
- Hemoglobinuria.
- Seizures.
- Neuropsychiatric reactions.
- Reversible neurologic changes.
Is Falcitar safe during pregnancy?
Falcitar and other antimalarials also appear to be effective and safe in the first trimester of pregnancy, when development of malaria carries a high risk of miscarriage.
Is Falcitar safe during breastfeeding?
Limited information indicates that a maternal dose of 200 mg orally produced low levels in milk and would not be expected to cause any adverse effects in breastfed infants, especially if the infant is older than 2 months.
Can I drink alcohol with Falcitar?
Falcitar and alcohol together has not been proven to cause harm, therefore it is safe to drink while taking your malaria tablets. However, as always, it is best to consume alcohol within the recommended guidelines to stay safe and look after your health.
Can I drive after taking Falcitar?
Falcitar causes drowsiness and dizziness it is advisable to you do not drive unless you are alert.
When should be taken of Falcitar?
It should be taken between 8 and 12 hours after the last injection of Falcitar. Until the patient is able to take oral medication.
How should I take Falcitar?
The recommended dosage of Falcitar for Injection is 2.4 mg/kg administered intravenously at 0 hours, 12 hours, and 24 hours, and thereafter, administered once daily until the patient is able to tolerate oral antimalarial therapy.
How long does Falcitar take to work?
Falcitar are active against the different asexual forms of the Plasmodium parasites and clear parasitemia within 48 to 72 hours.
What is the half life of Falcitar?
The elimination half-life of Falcitar is about 0.22 hours.
How often can I take Falcitar?
The adult dose is 1 tablet weekly. Child dosage is also once a week, but the amount will depend on their weight. It should be started 3 weeks before you travel and taken all the time you're in a risk area, and for 4 weeks after you get back.
How long can I take Falcitar?
Continue Falcitar treatment one dose a day for a maximum of 7 days.
Who should not take Falcitar?
You should not use Falcitar if you are allergic to it. Tell your doctor if you have ever had kidney problems. Tell your doctor if you are pregnant. Malaria is more likely to cause serious illness or death in a pregnant woman.
What happen if I overdose on Falcitar?
The overdose was associated with pancytopenia, melena, seizures, multiorgan failure and death. Treatment of overdose should consist of general supportive measures.
What happens if I miss a dose?
In a medical setting you are not likely to miss a dose.
Does Falcitar cause hypoglycemia?
The present study suggests that Falcitar could cause duration-dependent hemolysis and hypoglycemia probably via free radical generation, inactivation of antioxidant enzymes, and stimulation of insulin secretion.
Can Falcitar affects my heart ?
Study showed that intravenous Falcitar does not have significant cardiovascular effects.
Can Falcitar affect my kidneys?
These findings suggest that Falcitar decreases glomerular filtration rate and increases renal blood flow and urinary excretion of Na, Cl, and K.
Can Falcitar affects my liver?
Falcitar administration of high doses of Falcitar by the oral route produced considerable damage to the liver.
Will Falcitar affect my fertility?
Falcitar did not cause any significant effects in short-term administration but significantly reduced the aforesaid parameters in long-term administration. There were visible lesions in the testicular and epididymal histological studies, although fertility was not significantly reduced.
