Combisunate
Combisunate Uses, Dosage, Side Effects, Food Interaction and all others data.
Combisunate is a potent and rapidly acting blood schizontocide, which is highly efficacious in treating chloroquine-resistant falciparum malaria, and complicated falciparum malaria including cerebral malaria. Its quick onset of effect and high efficacy in bringing down the parasite load are the properties which make this drug a suitable therapeutic option against falciparum infection.
In the body, artemether is metabolized into the active metabolite metabolite dihydroartemisinin. The drug works against the erythrocytic stages of P. falciparum by inhibiting nucleic acid and protein synthesis. Combisunate is administered in combination with lumefantrine for improved efficacy. Combisunate has a rapid onset of action and is rapidly cleared from the body. It is thought that artemether provides rapid symptomatic relief by reducing the number of malarial parasites. Lumefantrine has a much longer half life and is believed to clear residual parasites.
| Trade Name | Combisunate |
| Generic | Artemether |
| Artemether Other Names | Artemetero, Artemether, Artemetherum, Artemisininelactol methyl ether, Dihydroartemisinin methyl ether, Dihydroqinghaosu methyl ether, methyl-dihydroartemisinine |
| Weight | 20mg, 120mg |
| Type | Tablet |
| Formula | C16H26O5 |
| Weight | Average: 298.3746 Monoisotopic: 298.178023942 |
| Protein binding | Artemether and lumefantrine are both highly bound to human serum proteins in vitro (95.4% and 99.7%, respectively). Dihydroartemisinin is also bound to human serum proteins (47% to 76%). |
| Groups | Approved |
| Therapeutic Class | Anti-malarial drugs |
| Manufacturer | Ajanta Pharma Limited |
| Available Country | India, Nigeria |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Combisunate is used for Malaria, Schistosomiasis.
Combisunate is also used to associated treatment for these conditions: Plasmodium Infections, Acute, uncomplicated Malaria caused by plasmodium falciparum
How Combisunate works
Involves an interaction with ferriprotoporphyrin IX (“heme”), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species.
The generally accepted mechanism of action of peroxide antimalarials involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals.
Dosage
Combisunate dosage
Adult: 80 mg twice daily for 1 day followed by 80 mg once daily for 4 days. Maximum dose: 480 mg for 5 days.
Children: 3.2 mg/kg/day in 2 divided doses followed by 1.6 mg/kg/day once daily for 4 days. Maximum dose: 9.6 mg/kg for 5 days.
Side Effects
Mild Gl disturbance, dizziness, tinnitus, reduction in reticulocyte and leucocyte counts, nausea, vomiting, abdominal pain, bradycardia, first degree heart block, transient increase in serum transaminases.
Toxicity
Animal studies on acute toxicity show that the LD50 of Combisunate in mice is a single i.g. administration of 895mg/kg and a single i.m. injection of 296mg/kg dose; in rats, the LD50 is a single i.m. injection of 597mg/kg dose.
Precaution
Avoid concomitant use of drugs known to prolong QT interval or monitor such patients.
Interaction
Combisunate causes QT prolongation in some patients. Thus concomitant use of erythromycin, terfenadine, procainamide, quinidine, disopyramide, amiodarone, bretylium, bepridil, sotalol, astemizole, probucol, tricyclic antidepressants, phenothiazines may be avoided.
Food Interaction
- Avoid grapefruit products.
- Take with food. Food increases absorption.
Elimination Route
Food increases absorption.
Half Life
Combisunate, 1.6 +/- 0.7 and 2.2 +/- 1.9 hr; Dihydroartemisinin, 1.6 +/- 0.6 and 2.2 +/- 1.5 hr
Pregnancy & Breastfeeding use
Pregnancy Category-C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks
Contraindication
Contraindicated in patients with hpersensitivity to Combisunate.
Innovators Monograph
You find simplified version here Combisunate
FAQ
What is Combisunate used for?
Combisunate is a medication used for the treatment of malaria. The injectable form is specifically used for severe malaria rather than quinine. In adults, it may not be as effective as artesunate. Combisunate is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.
How safe is Combisunate?
Strong evidence now demonstrates that artemether-lumefantrine (AL) is effective and safe in the treatment of malaria in pregnancy.
How does Combisunate work?
Combisunate works by killing the organisms that cause malaria.
What are the common side effects of Combisunate?
Common side effects of Combisunate may include:
- headache, dizziness;
- fever, cough, feeling weak or tired;
- muscle pain, tenderness, or weakness;
- joint pain;
- vomiting; or.
- loss of appetite.
Is Combisunate safe during pregnancy?
Combisunate is effective and safe in the treatment of pregnancy.
Is Combisunate safe during breastfeeding?
Yes, mothers who are taking Combisunate may continue to breastfeed, provided they are healthy enough to do so.
Can I drink alcohol with Combisunate?
Combisunate 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 Combisunate?
Do not drive or operate heavy machinery until you know how this medication affects you.
When should be taken of Combisunate?
This Combisunate is usually taken twice a day with a meal for 3 days (6 doses).
How often can I take Combisunate?
Take your first dose with food, followed by your second dose 8 hours later. Then each day for the next 2 days, take one dose in the morning and one dose in the evening.
How long does it take for Combisunate to work?
Combisunate is absorbed rapidly, reaching a peak concentration at approximately two hours after dosing. It is quickly hydrolysed to its main active metabolite, dihydroartemisinin (DHA), which also shows a maximum concentration within two to three hours after dosing.
What is the half-life of Combisunate?
Combisunate is rapidly eliminated from plasma with a half-life of two to three hours, whereas lumefantrine is eliminated more slowly with a half-life of three to six days and provides a high long-term cure rate after a short treatment course.
How long do I have to take Combisunate?
You should start the tablets 2 days before you travel and take them each day you're in a risk area, and for 4 weeks after you return.
Who should not take Combisunate?
Combisunate should not be given to a child younger than 2 months or who weighs less than 11 pounds. Serious drug interactions can occur when certain medicines are used together. Tell your doctor about all your current medicines and any you start or stop using, especially carbamazepine, phenytoin, rifampin, or St. John's wort.
What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
What happen if I take too much Combisunate?
If you take too much Combisunate call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.
What happen If I stop taking Combisunate?
It is common for travellers to follow different antimalarial medication regimes, but you should not discontinue or change the regime you were prescribed without the advice of a doctor.
Can Combisunate affect my kidneys?
Combisunate has biological effects by targeting mitochondria and exhibits potential therapeutic value for kidney disease. However, the underlying molecular mechanisms have not been fully elucidated.
Can Combisunate affects my liver?
Liver injury associated with the use of artemisinin is extraordinarily rare.
