What is the mechanism of action of mefloquine?
Mechanism of Action: Membrane-bound mefloquine may inhibit merozoite invasion and interact with proteins involved with parasite membrane lipid trafficking and nutrient uptake. Mefloquine binds to haem, forming a complex that may also be toxic to the parasite.
What is mefloquine toxicity?
Mefloquine is also known to cause anxiety, paranoia, hallucinations, depression, restlessness, confusion, and unusual behavior. In more serious cases symptoms can include suicidal behavior, committing suicide, severe anxiety, paranoia, hallucinations, depression, feeling restless, insomnia, and abnormal dreams.
How does mefloquine work in the body?
Mefloquine works by attacking the Plasmodium parasites once they have entered the red blood cells. It kills the parasites and prevents them from multiplying further.
Which of the following is an adverse reaction of mefloquine?
Among subjects who received mefloquine for treatment, the most frequently observed adverse experiences included: dizziness, myalgia, nausea, fever, headache, vomiting, chills, diarrhea, skin rash, abdominal pain, fatigue, loss of appetite, and tinnitus.
How does mefloquine prevent malaria?
About mefloquine Malaria is a disease which is passed on to humans by infected mosquitoes. A parasite called plasmodium lives inside the stomachs of infected female mosquitoes and is passed on to humans by a bite. Mefloquine works by killing the parasites passed into your body from the bites of the infected mosquitoes.
Does mefloquine have side effects?
What is the mechanism of action of chloroquine in malaria?
The major action of chloroquine is to inhibit the formation of hemozoin (Hz) from the heme released by the digestion of hemoglobin (Hb). The free heme then lyses membranes and leads to parasite death.
What is the pathophysiology of malaria?
All the manifestations of malarial illness are caused by the infection of the red blood cells by the asexual forms of the malaria parasite and the involvement of the red cells makes malaria a potentially multisystem disease, as every organ of the body is reached by the blood.
How does mefloquine work against malaria?
What type of drug is mefloquine?
Mefloquine (also known as mefloquine hydrochloride) is an antimalarial medicine. It is available in the United States by prescription only. It is available as a generic medicine and used to be sold under the brand name Lariam. It is available in tablets of 228mg base (250mg salt).
Is mefloquine an antagonist or agonist?
The results indicate that mefloquine has affinity for specific 5-HT and dopamine receptors, and in assays of receptor function, is a partial agonist at the 5-HT2A receptor, a full agonist at 5-HT2C receptors, and an antagonist at the dopamine D3 receptor.
Can you overdose on mefloquine?
Mefloquine Overdose If you take too much mefloquine, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.
How does malaria become resistant to chloroquine?
Resistance to chloroquine of malaria strains is known to be associated with a parasite protein named PfCRT, the mutated form of which is able to reduce chloroquine accumulation in the digestive vacuole of the pathogen.
What is pathogenesis of Plasmodium falciparum?
The pathogenesis of human P falciparum infection is a complex interplay of parasite-induced RBC alterations2 and microcirculatory abnormalities,12 accompanied by local and systemic immune reactions, resulting in multiple clinical forms of variable severity.
What class of drug is mefloquine?
Mefloquine is in a class of medications called antimalarials. It works by killing the organisms that cause malaria.
Which is the most probable mechanism of Plasmodial resistance to chloroquine?
What is the pathogenesis of malaria parasite?
Life cycle — Human malaria occurs by transmission of Plasmodium sporozoites via a bite from an infected female anopheline mosquito (figure 1). The sporozoites travel from the salivary glands of the mosquito through the bloodstream of the host to the liver, where they invade hepatocytes.
What is the pathogenesis of Plasmodium?
PATHOGENESIS. Severe malaria is predominantly caused by Plasmodium falciparum because of its ability to induce infected red blood cell (RBC) cytoadherence to the vascular endothelium and consequent end-organ dysfunction.
Some studies suggest that mefloquine specifically targets the 80S ribosome of the Plasmodium falciparum, inhibiting protein synthesis and causing subsequent schizonticidal effects. 4 There are other studies in the literature with limited in vitro data on mefloquine’s mechanism of action. 8, 11
Is mefloquine use linked to intoxication-induced psychosis?
Abstract Mefloquine use has been linked to severe gastrointestinal and neuropsychiatric adverse effects, including cognitive disturbances, anxiety, depression, psychosis, and violence.
What is the retinoid hypothesis of mefloquine toxicity?
The retinoid hypothesis could be tested clinically by comparing cases of mefloquine toxicity and untreated controls in terms of retinoid profiles (retinol, retinyl esters, percent retinyl esters, and retinoic acid). Subject to such tests, retinoid profiling could provide an indicator for assessing mefloquine-associated adverse effects.
Is mefloquine maternally toxic?
At the same doses, Mefloquine was also embryotoxic in mice and rabbits. All of these findings were observed at doses that were maternally toxic. Mefloquine is excreted in human milk in small amounts, the activity of which is unknown.