Justeen Pharmaceauticals Limited

TERTEL -150 INJECTION

Arteether 150mg/2ml

• DESCRIPTION

  TERTEL - 150 INJECTION (Arteether) is a synthetic derivative of artemisinin, a product of Chinese plant Artemisia annua.

  TERTEL - 150 (Arteether) is fast acting blood schizonticide specifically indicated for the treatment of chloroquine resistant P. falciparum malaria and cerebral malaria cases.

  TERTEL - 150 INJECTION (Arteether) is developed by Central Drug Research Institute (C.D,R.I.) Locknow and Themis Medicare Limited after extensive preclinical, clinical and toxicological studies.

• COMPOSITION

  Each 2ml ampoule of TERTEL - 150 INJECTION contains:
  Arteether: 15Omg.
  Arachis Oil: q.s.
  

• PHARMACOLOGY

  Arteether is fast acting blood schizonticidal agent for P.falciparum Malaria at the erythrocytic stage.

  Arteether is concentrated in parasitized erythroctytes. The functional group responsible for antimalarial activity of 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 (lY) oxo species which rips apart the parasitic cells.

  It is proposed that Arteether inhibits the protein synthesis and alter the ribosomal organisation and endoplasmic reticulum. Arteetbet also acts on the membranes of the parasites through lipid peroxidation.

• PHARMACOKINETICS

  Main metabolite of 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 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, spleenornegaly, hypotension and coma were treated with Arteether. Most of the cases became afebrile within 36 hours with the use of antipyretic drugs and parasite free with 72 hours.

  The cure rate in uncomplicated malaria was nearly 100 and in complicated P. falciparum malaria about 90. Recrudescence was less than 7%.

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

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

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

• INDICATIONS

  TERTEL - 150 INJECTION (Arteether) is indicated for use in severe P.falciparum malaria including cerebral and as second line treatment in cholroquine.

• CONTRAlNDICATION

  TERTEL - 150 INJECTION (Arteether) is contraindicated in patients hypersensitive to artemisinin derivatives.

• DOSAGE AND ADMINISTRATION

  Tertel - 150 Injection (Arteether) is for intramuscular use only.

  Adult:

  • 150 mg i.e. 1 ampoule of TERTEL - 150 INJECTION (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 condition, deep intramuscularly in the upper-external quadrant of the buttock. No other drug should be mixed in the same syringe.

• OVERDOSE

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

• PRECAUTIONS

  Since no clinical data is available for the use of 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 know whether Arteether is excreted in human milk, because many drugs are excreted in human milk, a caution should be exercised while using Arteether.

• DRUG INTERACTIONS

  TERTEL - 150 INJECTION (Arteether) does not interfere with the action of other commonly used drugs for treatment of P.falciparum malaria. eg Quinine and can be administered along with these drugs for the treatment of severe forms of malaria. (Except for other Artemisinin Derative like Artesunate and Artemether)

• ADVERSE EFFECTS

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

  In the multi centric trials of TERTEL - 150 INJECTION (Arteether) involving 478 patients suffering from P.falciparum malaria, no significant side effects were observed.

• STORAGE

  Protect from Iight. Store in cool place.

• PRESENTATION

  3 x 2 ml ampoules.