Feccox Artemether and Lumefantrine Tablets

Feccox

Artemether and Lumefantrine Tablets

 

1 COMPOSITION

Each uncoated tablet contains:

Artemether 80 mg

Lumefantrine 480 mg

Excipients Q.S.

 

2 DESCRIPTION

FECCOX ARTEMETHER LUMEFANTEINE TABLETS contain a fixed combination of two antimalarial active ingredients, artemether, an artemisinin derivative, and lumefantrine. Both components are blood schizotocides. The chemical name of artemether is (3R,5aS,6R,8aS,9R,10S,12R,12aR)-10-methoxy- 3,6,9-trimethyldecahydro-3,12-epoxypyrano[4,3-j]-1,2-benzodioxepine. Artemether is a white, crystalline powder that is freely soluble in acetone, soluble in methanol and ethanol, and practically insoluble in water. It has the empirical formular C16H26O5 with a molecular weight of 298.4.The chemical name of lumefantrine is (1RS)-2-(dibutylamino)-1-{(9Z)-2,7-dichloro-9-[(4-chlorophenyI)methylene]-9H-fluorene-4-yl}ethanol. Lumefantrine is a yellow, crystalline powder that freely soluble in N,N-dimethylformamide, chloroform, and ethyl acetate; soluble in dichloromethane; slightly soluble in ethanol and methanol; and insoluble in water. It has the empirical formula C3OH32C13NO with a molecular weight of 528.9.

 

3 ROUTE OF ADMINISTRATION

FECCOX ARTEMETHER LUMEFANTRINE TABLETS are for oral administration.

 

4 INDICATIONS AND USAGE

FECCOX ARTEMEFHER LUMEFANTRINE TABLETS (artemether/lumefantrine) Tablets are indicated for treatment of acute, uncomplicated malaria infections due to Plasmodium falciparum in patients of 5 kg body weight and above. FECCOX ARTEMETHER LUMEFANTRINE TABLETS have been shown to be effective in geographical regions where resistance to chloroquine has been reported.

 

5 LIMITATIONS OF USE

FECCOX ARTEMETHER LUMEFANFRINE TABLETS are not approved for patients with severe or complicated P. falciparum malaria.

FECCOX ARTEMETHER LUMEFANTRINE TABLETS are not approved for the prevention of malaria.

 

6 DOSAGE AND ADMINISTRATION

FECCOX ARTEMETHER LUMEFANTRINE TABLETS should be taken with food. Patients with acute malaria are frequently averse to food. Patients should be encouraged to resume normal eating as soon as food can be tolerated since this improves absorption of artemether and lumefantrine.

For patients who are unable to swallow the tablets such as infants and children, FECCOX ARTEMETHER LUMEFANTRINE may be crushed and mixed with a small amount of water (one to two teaspoons) in a clean container for administration immediately prior to use.

The container can be rinsed with more water and the contents swallowed by the patient. The crushed tablet preparation should be followed whenever possible by food/drink (e.g. milk, formula, pudding, broth and porridge).

In the event of vomiting within 1 to 2 hours of administration, a repeat dose should be taken. If the repeat dose is vomited, the patient should be given an alternative antimalarial treatment.

 

6.2 dosage regimen

Weight in kg Total Tablets Dosage Regimen
35 kg and above   Day 1 Day 2 Day 3
  0 Hour 8 Hours 24 Hours 36 Hours 48 Hours 60 Hours
6 1 1 1 1 1 1

Second dose to be taken after 8 hours of first dose, better taken with food especially fatty meal.

 

6.3 Dosage in Patients with Hepatic or Renal Impairment

No specific pharmacokinetic studies have been carried out in patients with hepatic or renal impairment. Most patients with acute malaria present with some degree of related hepatic and/or renal impairment. Caution should be exercised when administering FECCOX ARTEMETHER LUMEFANTRINE TABLETSs in patients with severe hepatic or renal impairment.

 

7. DOSAGE FORMS AND STRENGTHS

FECCOX ARTEMETHER LUMEFANTRINE TABLETS contain 80 mg of artemether and 480 mg of lumefantrine. FECCOX ARTEMETHER LUMEFANTRINE TABLETS are supplied as yellow, oblong shaped, uncoated tablets.

 

8. PHARMACOLOGICAL ACTION

This medicine is an antimalarial. It is used to treat a certain type of malaria infection in adults and children who weigh at least 5kg. Artemether 80 mg and Lumefantrine 480 mg tablets contain two antimalarial drugs, artemether and lumefantrine in fixed dose, which work together to kill the malaria parasite (a tiny organism that is found inside the red blood cells). It is indicated only for the treatment of so called uncomplicated malarial attacks due to Plasmodium falciparum (a particular type of malaria parasite) against which the medicine is active. For complete cure it is important that you complete the prescribed dose as advised by your doctor, pharmacist or health care worker.

 

9 CONTRAINDICATIONS

9.1 Hypersensitivity

Known hypersensitivity to artemether, lumefantrine, or to any of the excipients of FECCOX ARTEMETIIER LUMEFANTRINE TABLETS

 

9.2 Strong CYP3A4 luducers

Co-administration of strong inducers of CYP3A4 such as rifampicin, carbamazepine, phenytoin and St. John’s wort with FECCOX ARTEMETHER LUMEFANTRINE TABLETS can result in decreased concentrations of artemether and/or lumefantrine and loss of antimalarial efficacy.

 

10 WARNING AND PRECAUTIONS

10.1 Prolongation of the QT Interval

Some antimalarials (e.g., halofantrine, quinine, quinidine) including FECCOX ARTEMETHER LUMEFANTRINE TABLETS have been associated with prolongation of the QT interval on the electrocardiogram. FECCOX ARTEMETHER LUMEFANTRINE TABLETS should be avoided in patients:

– With congenital prolongation of the QT interval (e.g., long QT syndrome) or any other clinical condition known to prolong the QTc interval such as patients with a history of symptomatic cardiac arrhythmias, with clinically relevant bradycardia or with severe cardiac disease.

– With a family history of congenital prolongation of the QT interval or sudden death.

– With known disturbances of electrolyte balance, e.g., hypokalemia or hypomagnesemia.

– Receiving other medications that prolong the QT interval, such as class IA (quinidine, procainamide, disopyramide), or class III (amiodarone, sotalol) antiarrhythmic agents; antipsychotics (pimozide, ziprasidone); antidepressants; certain antibiotics (macrolide antibiotics, fluoroquinolone antibiotics, imidazole, and triazole antifungal agents).

– Receiving medications that are metabolized by the cytochrome enzyme CYP2D6 which also have cardiac effects (e.g., flecainide, imipramine, amitriptyline, clomipramine).

 

10.2 Use of QT Prolonging Drugs and Other Antimalarials

Halofantrine and FECCOX ARTEMETHER LUMEFANTRINE TABLETS should not be administered within one month of each other due to the long elimination half-life of Iumefantrine (3-6 days) and potential additive effects on the QT interval. Antimalarials should not be given concomitantly with FECCOX ARTEMETHER LUMEFANTRINE TABLETS, unless there is no other treatment option, due to limited safety data.

 

10.3 Drug Interactions with CYP3A4

When FECCOX ARTEMETHER LUMEFANTRINE TABLETS are co-administered with substrates of CYP3A4 it may result in decreased concentrations of the substrate and potential loss of substrate efficacy. When FECCOX ARTEMETHER LUMEFANTRINE TABLETS are co-administered with an inhibitor of CYP3A4, including grapefruit juice it may result in increased concentrations of artemether and/or lumefantrine and potentiate QT prolongation. When FECCOX ARTEMETHER LUMEFANTRINE TABLETS are co-administered with inducers of CYP3A4 it may result in decreased concentrations of artemether and/or lumefantrine and loss of antimalaria efficacy.

 

10.4 Drug Interactions with CYP2D6

Administration of FECCOX ARTEMETHER LUMEFANTRINE TABLETS with drugs that are metabolized by CYP2D6 may significantly increase plasma concentrations of the co-administered drug and increase the risk of adverse effects. Many of the drugs metabolized by CYP2D6 can prolong the QT interval and should not be administered with FECCOX ARTEMETHER LUMEFANTRINE TABLETS due to the potential additive effect on the QT interval (e.g., ficcainide, imipramine, amimptyline, clomipramine).

 

10.5 Recrudescence

Food enhances absorption of artemether and lumefantrine following administration of FECCOX ARTEMETHER LUMEFANTRINE TABLETS. Patients who remain averse to food during treatment should be closely monitored as the risk of recrudescence may be greater.

In the event of recrudescent P. falciparum infection after treatment with FECCOX ARTEMETHER LUMEFANTRINE TABLETS, patients should be treated with a different antimalarial drug.

 

10.6 Hepatic and Renal Impairment

FECCOX ARTEMETHER LUMEFANTRINE TABLETS have not been studied for efficacy and safety in patients with severe hepatic and/or renal impairment.

 

10.7 Plasmodium Vivax Infection

FECCOX ARTEMETHER LUMEFANTRINE TABLETS have been shown in limited data to be effective in treating the erythrocytic stage of P. vivax infection. However relapsing malaria caused by P. vivax requires additional treatment with other antimalarial agents to achieve radical cure i.e., eradicate any hypiozoites forms that may remain dormant in the liver.

 

11 ADVERSE REACTIONS

11.1 Serious Adverse Reactions

Clinically significant adverse reactions reported in adults and/or children treated with the 6-dose regimen of FECCOX ARTEMETHER LUMEFANTRINE TABLETS which occurred in clinical studies, regardless of causality are listed below:

– Blood and lymphatic system disorders: eosinophilia

– Ear and labyrinth disorders: tinnitus

– Eye disorders: conjunctivitis

– Gastrointestinal disorders: constipation, dyspepsia, dysphagia, peptic ulcer

– General disorders: gait disturbance.

– Infections and infestations: abscess, acrodermatitis, bronchitis, ear infection, gastroenteritis, helminthic infection, hookwonn infection, impetigo, influenza, lower respiratory tract infection, malaria, nasopharyngitis, oral herpes, pneumonia, respiratory tract infection, subcutaneous abscess, upper respiratory tract infection, urinary tract infection.

 

12. USES

12.1 Pregnancy

Pregnancy: The Safety and efficacy of FECCOX ARTEMETHER LUMEFANTRINE TABLETS in the treatment of acute, uncomplicated malaria in pregnant women has not been established.

FECCOX ARTEMETHER LUMEFANTRINE TABLETS should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Pregnant rats dosed during the period of organogenesis at or higher than a dose of about half the highest clinical dose of 1120 mg artemether-lumefantrine per day (based on body surface area comparisons), showed increases in fetal loss, early resorptions and post implantation loss.

 

12.2 Nursing Mothers

It is not known whether artemether or lumefantrine is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when FECCOX ARTEMETHER LUMEFANTRINE TABLETS are administered to a nursing woman.

 

12.3 Pediatric Use

The safety and effectiveness of FECCOX ARTEMETHER LUMEFANTRINE TABLETS have been established for the treatment of acute, uncomplicated malaria in pediatric patients weighing 5kg or more. The safety and efficacy have not been established in pediatric patients who weigh less than 5kg.

 

12.4 Geriatric Use

In general, the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy in elderly patients should be considered when prescribing FECCOX ARTEMETHER LUMEFANTRINE TABLETS.

 

12.5 Hepatic and Renal Impairment

FECCOX ARTEMETHER LUMEFANTRINE TABLETS have not been proved for efficacy and safety in patients with severe hepatic and/or renal impairment. No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.

 

13 OVERDOSAGE

There is no information on overdoses of FECCOX ARTEMETHER LUMEFANTRINE TABLETS higher than the doses recommended for treatment. In cases of suspected overdosage, symptomatic and supportive therapy, which would include ECG and blood electrolyte monitoring, should be given as appropriate.

 

14. POSSIBLE SIDE EFFECTS

Like all medicines, Artemether 80mg and Lumefantrine 480mg Tablets can cause side effects, although not everybody gets them. When treating malaria, it is not always possible to differentiate between unwanted effects caused by Artemether 80mg and Lumefantrine 180mg Tablets, and those caused by any other medicines you may be taking at the same time. For this reason, it is important that you inform the doctor or health care provider of any change in your health.

The following side effects have been reported in patients treated with Artemether 80mg and Lumefantrine 480mg Tablets: The most commonly reported side effects (greater than 1 in every 10 patients treated) include headache, dizziness, feeling sick, vomiting, abdominal pain, loss of appetite, palpitations, pain in muscles and joints, fatigue and disturbed sleep.

Commonly (greater than 1 in every 100 patients treated) reported side effects include alterations to the electrocardiogram (ECG), tingling in hands and feet, problems with walking, cough, diarrhoea, itching, rash and insomnia.

Uncommon side effects (greater than 1 in every 1000 patients treated but less than 1 in 100): involuntary muscle jerks, coordination disturbances, altered liver function tests and drowsiness.

The following side effects have been reported in patients treated with Artemether 80mg and Lumefantrine 480mg Tablets. However frequency estimates for these effects are not available: hypersensitivity reaction, hives, rapid swelling of the face and throat (angioedema).

A similar side effect profile was reported for children. If any of the side effects gets serious or if you notice any side effects not listed in this leaflet, please tell your doctor, health care provider or pharmacist as soon as possible.

 

15 HOW SUPPLIED/STORAGE AND HANDLING

FECCOX ARTEMETHER LUMEFANTRINE TABLETS (artemether/lumefantrine) Tablets
80 mg/ 480 mg Tablets YELLOW COLOURED ROUND SHAPED UNCOATED TABLETS.

 

Storage

Store below 30°C. Protect from light.

Keep all medicines out of reach of children.

 

NAFDAC REG.NO.: B4-3409

Mfg Lic. No.: G/1369

 

Manufactured for

FECCOX PHARMA LTD.

No. 1/A, Airport Road, Kano, Nigeria.

feccox@yahoo.co.uk

Rc. No.: 255883

Under collaboration with

yatharthlifecare@gmail.com

 

Manufactured in India by

Brussels Laboratories Pvt. Ltd.

33, Changodar Ind. Estate, Sarkhej Bavia Road,

Changodar, Ahmedabad-382 210 (Gujarat)- India.