Leoprime
Leoprime Uses, Dosage, Side Effects, Food Interaction and all others data.
Leoprime is an 8-aminoquinoline antimalarial which eliminates the exoerythrocytic forms of malarial parasite Plasmodium vivax, Plasmodium ovale and Plasmodium falciparum by disrupting mitochondria and binding to DNA.
Leoprime's mechanism of action is not well understood. It may be acting by generating reactive oxygen species or by interfering with the electron transport in the parasite. Also, although its mechanism of action is unclear, primaquine may bind to and alter the properties of protozoal DNA.
Leoprime is an antimalarial agent and is the essential co-drug with chloroquine in treating all cases of malaria. In the blood, malaria parasites break down a part of the red blood cells known as haemoglobin. When this happens haemoglobin is divided into two parts; haem and globin. Haem is toxic to the malaria parasite. To prevent it from being damaged, the malaria parasite produces an chemical which converts the toxic haem into a non-toxic product. Leoprime acts by interfering with a part of the parasite (mitochondria) that is responsible for supplying it with energy. Without energy the parasite dies. This stops the infection from continuing and allows the person to recover. Leoprime kills the intrahepatic form of Plasmodium vivax and Plasmodium ovale, and thereby prevents the development of the erythrocytic forms that are responsible for relapses (it also kills gametocytes). Leoprime is not used in the prevention of malaria, only in the treatment. It has insignificant activity against the asexual blood forms of the parasite and therefore it is always used in conjunction with a blood schizonticide and never as a single agent. Leoprime has gametocytocidal activity against all plasmodia, including P. falciparum.
| Trade Name | Leoprime |
| Availability | Prescription only |
| Generic | Primaquine |
| Primaquine Other Names | Primachin, Primachina, Primachinum, Primaquin, Primaquina, Primaquine, Primaquinum |
| Related Drugs | doxycycline, clindamycin, hydroxychloroquine, sulfamethoxazole / trimethoprim, Bactrim, Plaquenil, Bactrim DS, dapsone, Cleocin |
| Type | Tablet |
| Formula | C15H21N3O |
| Weight | Average: 259.3467 Monoisotopic: 259.168462309 |
| Groups | Approved |
| Therapeutic Class | Anti-malarial drugs |
| Manufacturer | Leo Pharma |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Leoprime phosphate is used for the radical cure (prevention of relapse) of vivax malaria.
Leoprime is also used to associated treatment for these conditions: Malaria caused by Plasmodium ovale, Malaria caused by plasmodium vivax, Plasmodium Infections, Pneumocystis Jirovecii Pneumonia
How Leoprime works
Leoprime's mechanism of action is not well understood. It may be acting by generating reactive oxygen species or by interfering with the electron transport in the parasite. Also, although its mechanism of action is unclear, primaquine may bind to and alter the properties of protozoal DNA.
Dosage
Leoprime dosage
Leoprime phosphate is recommended only for the radical cure of vivax malaria, the prevention of relapse in vivax malaria, or following the termination of chloroquine phosphate suppressive therapy in an area where vivax malaria is endemic. Patients suffering from an attack of vivax malaria or having parasitized red blood cells should receive a course of chloroquine phosphate, which quickly destroys the erythrocytic parasites and terminates the paroxysm. Leoprime phosphate should be administered concurrently in order to eradicate the exoerythrocytic parasites in a dosage of 1 tablet (equivalent to 15 mg base) daily for 14 days.
Should be taken with food. Take with meals to avoid GI discomfort.
Side Effects
Abdominal pain, gastric distress, nausea, vomiting; methaemoglobinaemia, haemolytic anaemia (in patients with G6PD deficiency), mild anaemia, leucocytosis; HTN, cardiac arrhythmias, prolonged QT interval on ECG, accommodation disturbance. Rarely, leucopenia, agranulocytosis.
Precaution
Patient with G6PD deficiency, NADH methaemoglobin reductase deficiency. Childn. Pregnancy and lactation.
Interaction
Enhanced effect with other drugs that prolong the QT interval.
Food Interaction
- Take with food. Food decreases irritation.
Leoprime Drug Interaction
Major: procaine penicillinUnknown: aspirin, zolpidem, RHO Immunoglobulin , dexamethasone, dextran, low molecular weight, acetaminophen, phenytoin, valproic acid, multivitamin, thiamine, cyanocobalamin, riboflavin, pyridoxine, ascorbic acid, ergocalciferol, cholecalciferol, phytonadione, phytonadione, zinc sulfate
Leoprime Disease Interaction
Major: G-6-PD/NAPD methemoglobin deficiency, granulocytopenia
Half Life
3.7-7.4 hours
Pregnancy & Breastfeeding use
Pregnancy Category C. Safe usage of Leoprime Phosphate in pregnancy has not been established. Leoprime is contraindicated in pregnant women. Even if a pregnant woman is G6PD normal, the fetus may not be. Animal data show toxicity to reproduction.
Lactation: It is not known whether Leoprime is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Leoprime, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Contraindication
Acutely ill patients suffering from systemic disease manifested by tendency to develop granulocytopenia (e.g. rheumatoid arthritis, lupus erythematosus). Concurrent use with other potentially haemolytic drugs or depressants of myeloid elements of the bone marrow. Concomitant admin with mepacrine.
Acute Overdose
Symptoms of overdosage of Leoprime phosphate include abdominal cramps, vomiting, burning epigastric distress, central nervous system and cardiovascular disturbances, including cardiac arrhythmia and QT interval prolongation, cyanosis, methemoglobinemia, moderate leukocytosis or leukopenia, and anemia. The most striking symptoms are granulocytopenia and acute hemolytic anemia in G6PD deficient patients. Acute hemolysis occurs, but patients recover completely if the dosage is discontinued.
Storage Condition
Store at 25° C. Protect from light.
Innovators Monograph
You find simplified version here Leoprime
Leoprime contains Primaquine see full prescribing information from innovator Leoprime Monograph, Leoprime MSDS, Leoprime FDA label
