Primaquine

Primaquine Uses, Dosage, Side Effects, Food Interaction and all others data.

Primaquine 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.

Primaquine'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.

Primaquine 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. Primaquine 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. Primaquine 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). Primaquine 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. Primaquine has gametocytocidal activity against all plasmodia, including P. falciparum.

Primaquine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Primaquine
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
Weight	7.5mg, , 15mg, 26.5mg
Type	Tablet, Oral Tablet
Formula	C₁₅H₂₁N₃O
Weight	Average: 259.3467 Monoisotopic: 259.168462309
Groups	Approved
Therapeutic Class	Anti-malarial drugs
Manufacturer	Zydus Cadila Healthcare Ltd, Ethical Laboratories (pvt) Ltd, , Phapros
Available Country	India, Canada, Pakistan, United States, Indonesia
Last Updated:	September 19, 2023 at 7:00 am

Uses

Primaquine phosphate is used for the radical cure (prevention of relapse) of vivax malaria.

Primaquine 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 Primaquine works

Dosage

Primaquine dosage

Primaquine 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. Primaquine 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.

Primaquine 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 Primaquine Phosphate in pregnancy has not been established. Primaquine 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 Primaquine 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 Primaquine, 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 Primaquine 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.