Ibasunate Dihydroartemisinin and Piperaquine Phosphate Capsules

IBASUNATE

Dihydroartemisinin 40 mg and Piperaquine Phosphate 320 mg Capsules

 

Composition

Each soft gelatin capsule contains

Dihydroartemisinin 40 mg

Piperaquine Phosphate 320 mg

Excipients q.s.

Approved colours used in capsule shell.

 

Pharmacology and Pharmacokinetics

Mode of action of Dihydroartemisinin

Dihydroartemisinin mainly interferes with the membrane structures of trophozoites (erythrocytic asexual forms), i.e. whorled food vacuole membrane, distended mitochondria, swollen nuclear membrane, dissociation of ribosomes from endoplasmic reticulum leading to cytoplasmic vacuolization and autophagocytosis. In additional biochemical depression of protein synthesis and nucleic acid synthesis are exhibited.

Upon oral administration Dihydroartemisinin is rapidly absorbed and maximum blood concentration attained 1 hour afterward, with a half-life of about 4 hours. It is widely distributed in the liver, kidneys and bile. Approximately 80% is excreted through the urine and feces within 24 hrs after administration. It is metabolized to two inactive metabolites, deoxydihydroartemisinin and dihydroxydilhydroarternistnin.

 

Mode of action of Piperaquine Phosphate

Experimental results show that PQP interferes with physiological function of the food vacuole membrane of the trophozoites leading to autophagocytosis of the parasites. It has no marked effect on the ring forms, immature or mature schizonts and the male or female gametocytes. Upon oral administration about 80-90% is absorbed within 24 hrs. It is widely distributed in the body mainly in the liver, kidneys, lungs and spleen. About 25% of the total dose is partitioned in the liver within 8 hours of intake. Elimination is very slow with the half-life of about 9.4 days. It is excreted through bile by hepatoenteral circulation.

 

Indications

Treatment of all kinds of malarias even malaria caused by multi-resistant Plasmodium falciparum.

 

Contraindications

Ibasunate is not recommended for use in women during the first 3 months of pregnancy.

 

Administration

Ibasunate should be administered orally over three consecutive days for a total of three doses taken at the same time each day.

 

Dosage

As directed by the Physician or as per the insert or chart given below.

Age (Years) < 6 Years old 6-16 Years old > 16 years old
Day 1 1 Capsule 2 Capsules 3 Capsules
Day 2 1 Capsule 2 Capsules 3 Capsules
Day 3 1 Capsule 2 Capsules 3 Capsules
Total 3 Capsules 6 Capsules 9 Capsules

Warning

This medicine is for only those Children / Patients that can swallow the soft gelatin capsules.

 

Overdose

Overdose have severe consequences in children.

There may be chance for hypotension, apnea, seizures, arrythmias, progressing to cardiac arrest due to overdose.

In cases of suspected overdose, symptomatic and supportive therapy should be given as appropriate.

 

Warnings

If a patient vomits within 30 minutes of taking Ibasunate ,the whole dose should be re-administered; if a patient vomits within 30-60 minutes, half the dose should be re-administered. Re-dosing with lbasunate should not be attempted more than once. If the second dose is vomited alternative antimalarial therapy should be instituted. If a dose is missed, it should be taken as soon as realised and then the recommended regime will continued until the full course of treatment has been completed. No more than two courses of lbasunate may be given within a 12 month period. A second course of Ibasunate should not be given within 2 months after the first course due to the long elimination half-life of piperaquine.

 

Pregnancy

It does not recommend this product for treatment of malaria in the 1st trimester except when considered lifesaving for the mother and other antimatarials are unsuitable.

Because of limited safety data, this product should only be used in the 2nd and 3rd trimesters when other treatments are considered unsuitable.

 

Lactation

Excretion of Ibasunate through breast milk has not been established.

 

Adverse Reactions

1 Nausea or vomiting may occur occasionally with incidence of less than 6%.

2 No noticeable side effect of Dihydroartemisinin is reported. The Dihydroartemisinin would, for certain individuals bring effects of greater or lesser severity for example, a reversible reduction in reticulocyte counts.

3 Possible side-effect of PQP include mild dizziness, vertigo, headache, nausea, vomiting and abdominal discomfort. Reversible leucopenia was infrequently reported; dyspnea and palpitations were also reported but not further specified.

 

Precautions

Do not exceed the stated dosage.

 

Storage

Store below 25°C in a cool and dry place.

Protect from light and moisture.

 

Packaging

Blister pack of 9 soft gelatin capsules in a carton.

 

NAFDAC Reg. No.: B4-4786

 

Manufactured in India by

Olive Healthcare

197/2 Athiyawad Dabhel Village

DAMAN 396 210 (U.T.) India

www.olivehealthcare.co.in

export.department@olivehealthcare.co.in

 

Marketed in Nigeria by

ELBE PHARMA NIGERIA LIMITED

1, African Church Close,

Off Coker Road,

Ilupeju, Lagos, Nigeria.

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