Beether Alpha Beta Arteether Injection

BEETHER

ᾀ-β ARTEETHER INJECTION

 

DESCRIPTION

BEETHER (ᾀ-β Arteether) is a synthetic derivative of artemisinin, a product of Chinese plant Artemisia annua.

BEETHER (ᾀ-β Arteether) is fast acting blood schizonticide specifically indicated for the treatment of chloroquine resistant P. Falciparum malaria and cerebral malaria cases.

 

COMPOSITION

Each 2 ml contains

ᾀ-β Arteether 150 mg

Arachis oil B.P. q.s.

 

PHARMACOLOGY

ᾀ-β Arteether is fast acting blood schizonticidal agent for P. falciparam Malaria at the erythrocytic stage.

Arteether is concentrated in parasitized erythrocytes. The functional group responsible for antimalaria activity of ᾀ-β Arteether is “endoperoxide bridge”. The researchers believe that iron from the digested haemoglobin of the parasite’s victim reduces this bridge releasing a highly reactive free radical iron (IV) oxo species which rips apart the parasitic cells.

It is proposed that ᾀ-β Arteether inhibites the protein synthesis and after the ribosomal organization and endoplasmic reticulum.

ᾀ-β Arteether also acts on the memebranes of the parasites through lipid peroxidation.

 

PHARMACOKINETICS

Main metabolite of ᾀ-β Arteether is Dihydroartemisinin. The half life of Dihydroartemisinin is more than 20 hours. The elimination of the drug is through hepatic metabolism and gets eliminated at a low rate as compared to other artemisinin derivatives.

 

CLINICAL DATA

In multicentric clinical evaluation of ᾀ-β Arteether in complicated and uncomplicated P. falciparum malaria, a total of 267 patients of uncomplicated P. falciparum malaria, having fever with chill/rigor and 211 patients of complicated P. falciparum malaria having fever, headache, vomiting, diarrhoea, convulsions, renal impairment, severe anaemia, spleenomegaly, hypotension and coma were treated with ᾀ-β Arteether. Most of the cases became afebrila within 36 hours without the use of antipyretic drugs and parasite free within 72 hours. The cure rate in uncomplicated malaria was nearly 100% and in complicated P. falciparum malaria about 90%. Recrudescence was less than 7%.

ᾀ-β Arteether is more lipophilic and has the advantage of greater accumulation in brain tissue, hence a potential drug for the treatment of cerebral malaria.

ᾀ-β Arteether, also exhibits gametocytocidal action on P. falciparum which will be an added advantage in cutting down the transmission of P. falciparum malaria.

ᾀ-β Arteether is well tolerated and compliance is very good with virtually no drug related side effects.

 

INDICATION

BEETHER (ᾀ-β Arteether) is indicated for use in severe P. falciparum malaria including cerebral and as a second line treatment in chloroquine resistant malaria. No cross resistance detected with Chloroquine.

 

CONTRAINDICATION

BEETHER (ᾀ-β Arteether) is contraindicated in patients hypersensitive to artemisinin derivates.

 

DOSAGE AND ADMINISTRATION

BEETHER (ᾀ-β Arteether) injection is for INTRAMUSCULAR USE ONLY.

Adult

150 mg i.e. 1 ampoule of BEETHER (ᾀ-β Arteether) once daily for 3 consecutive days or as directed by the physician.

Children

3 mg/kg per day administered by intramuscular injection over a 3 day period or as directed by the physician. The injection must be given in aseptic conditions, deep intramuscularly in the upper-external quandrant of the buttock.

No other drug should be mixed in the same syringe.

 

OVERDOSE

The pre-clinical studies of ᾀ-β Arteether have shown that LD50 value is more than 1000 mg/kg, whereas the maximum dose injected in adults is about 2.5 mg/kg per day. This confirms that the safety window for the dose administered is very wide. Hence this study concludes that ᾀ-β Arteether is well tolerated even when overdose is administered.

 

PRECAUTIONS

Pregnancy

Since no clinical data is available for the use of ᾀ-β Arteether during pregnancy, it should be used with caution in pregnant women, if the potential benefits justify the potential risk to the foetus.

Nursing mother

It is not known whether ᾀ-β Arteether is excreted in human milk, because many drugs are excreted in human milk, caution should be exercised while using ᾀ-β Arteether.

 

DRUG INTERACTIONS

BEETHER (ᾀ-β Arteether) does not interfere with the action of other commonly used drugs for treatment of P. falciparum malaria, e.g. Quinine and can be administered along with these drugs for the treatment of severe form of malaria.

(Except for other Artemisinin Derivative like Artesunate Artemether)

 

ADVERSE EFFECTS

Neurotoxicity is the common side effect associated with all artemisinin compounds in high doses.

Neurotoxicity in manifests as gait disturbances, loss of spinal cord pain responses, incoordination, respiratory depression, convulsions and cardio respiratory arrest.

Other side effects are nausea, dizziness and depressed GIT activity. Clinical, neurological, electro-cardiographic and biochemical abnormally were seen.

In the multi centric trails of ᾀ-β Arteether involving 478 patients suffering from P. falciparum malaria, no significant side effects were observed.

 

STORAGE

Protect from light. Store in cool place.

 

PRESENTATION

3 x 2 ml ampoules.

 

NAFDAC Reg. No.: A4-7153

 

Manufactured by

Malcur Laboratories Limited

46/4-7, Village: Zak, Tal: Degham

Dist: Gandinager-382330

Gujarat, India.

 

Manufactured for

Nicholson Healthcare

(A Division of Schwitz Biotech)

CM01, Saya Apartments, New Sai Baba Temple, Ghadoda,

Ahmedabad-61, Gujarat, India

 

Marketed by

Kingzy Pharmaceuticals Ltd.

142 Okporo Road, Port Harcourt,

Rivers State, Nigeria.