Meflokhin (Mefloquinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Other synthetic antibacterial agents

Included in the formulation
  • Lariam®
    pills inwards 
    Hoffmann-La Roche Ltd.     Switzerland
  • Meflokhin
    pills inwards 
    FARMZASCHITA NPC, GP     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    P.01.B.C.02   Meflokhin

    Pharmacodynamics:

    Hematocide. It acts on erythrocyte forms of malaria pathogens: Plasmodium falciparum, Plasmodium vivax, circulating schizonts Plasmodium malariae and Plasmodium ovale. Not effective against gamonts Plasmodium falciparum and hepatic histoshysonts Plasmodium vivax. Has antimalarial effect.

    Pharmacokinetics:

    Well absorbed from the gastrointestinal tract (eating significantly increases the speed and increases the degree of absorption by 40%). It is distributed into blood, urine, cerebrospinal fluid and tissues, accumulates in erythrocytes (at a concentration 2 times that of plasma), penetrates into breast milk in low concentrations (3-4% of the dose). The connection with plasma proteins is very high (98%). It is subject to partial biotransformation in the liver with the formation of 2 metabolites. The half-life is 15-33 days. Displayed kidneys (15% unchanged) and with feces (in the form of metabolites, very slowly, the tendency for cumulation, sub-therapeutic concentrations may persist in the blood for several months).

    Indications:

    · Treatment and prevention of malaria.

    · Preventing malaria before leaving for regions with a high risk of infection.

    · Emergency therapy for suspected malaria and inability to seek emergency medical care.

    ICD-10

    I.B50-B64.B54   Malaria, unspecified

    I.B50-B64.B52   Malaria caused by Plasmodium malariae

    I.B50-B64.B51   Malaria caused by Plasmodium vivax

    I.B50-B64.B50   Malaria caused by Plasmodium falciparum

    Contraindications:

    · Individual intolerance.

    · Epileptic and other convulsive seizures.

    · Acute psychosis.

    Carefully:

    · Pregnancy, I trimester.

    · Mental diseases.

    · Severe liver dysfunction.

    · Age under 2 years or body weight up to 15 kg.

    Pregnancy and lactation:

    Recommendations FDA category C. Contraindicated in the II and III trimesters of pregnancy. With caution in the I trimester. The drug is not recommended during breastfeeding. When choosing it as a chemoprophylaxis for women of reproductive age, it is recommended that contraceptives be used throughout the period of admission and 3 months after discontinuation.

    Dosing and Administration:

    The drug should be taken orally after eating, with plenty of water.

    The daily dose is 15-25 mg / kg (on average for an adult - 1-1.5 g), in one or two or three doses with an interval of 6-8 h.When malaria symptoms appear, adults are recommended to take 3 tablets at one time, then 6-8 hours (in the absence of side effects) - 2 more tablets, and after 6-8 hours - 1 more tablet.

    For the prevention of malaria for 2-3 weeks before the proposed trip to the epidemic-threatening area of ​​malaria, prescribe 5 mg / kg once a week.

    Side effects:

    In preventive doses, patients are usually well tolerated mefloquine, it rarely causes serious side effects (more often when taking therapeutic doses), but differential diagnosis of the side effects of mefloquine and the symptoms of acute malaria can be difficult.

    Blood: leukopenia, leukocytosis, thrombocytopenia.

    Cardiovascular system: extrasystole, lability of arterial pressure, vascular collapse, tachycardia, palpitation, bradycardia, arrhythmias, atrioventricular blockade, quinidine-like effect on the heart.

    Digestive system: nausea, vomiting, diarrhea, abdominal pain, decreased appetite.

    Nervous system: dizziness, headache, convulsions, depression (requires the abolition of mefloquine), psychotic or paranoid conditions, drowsiness, insomnia (6% of patients when using therapeutic doses), nightmares, neuropathy, paresthesia, anxiety, memory impairment, confusion (requires the abolition of mefloquine), hallucinations, encephalopathy.

    Skin: skin rash, exanthema, alopecia.

    Organs of the senses: visual disturbances, tinnitus, vestibular and labyrinthine disorders.

    Allergic reactions: urticaria, pruritus, multiforme exudative erythema (including Stevens-Johnson syndrome).

    Others: muscle cramps, myasthenia gravis, myalgia, arthralgia, asthenia, weakness, fever, chills, increased transaminase activity, hypercreatininaemia.

    Overdose:

    In case of an overdose, nausea, vomiting, system dizziness, abdominal pain, disruption of the central and peripheral nervous system, cardiovascular system are observed. The specific antidote is unknown.

    Treatment: induction of vomiting or gastric lavage, with vomiting and diarrhea - correction of water-salt metabolism, careful monitoring (for ≥24 h) of hemodynamic parameters, electrocardiogram and neuropsychic status, symptomatic therapy (artificial ventilation may be required).

    Interaction:

    β-Adrenoblockers, blockers of slow calcium channels - it is possible to increase the inhibition of conduction and excitability of the cardiac muscle with parallel application.

    Anticonvulsants (carbamazepine, phenobarbital, phenytoin, valproic acid) - it is possible to reduce their concentration in the blood plasma with parallel application, worsening control of seizures; it is necessary to monitor the content of anticonvulsants in blood plasma and the corresponding correction of their dose.

    Vaccine for the prevention of typhoid fever - it is possible to reduce the effectiveness of immunization in parallel with mefloquine; The vaccination must be completed within 3 days or more before the first dose of mefloquine.

    Halofantrine - possible development of life-threatening arrhythmias due to lengthening of the interval Q-T; combine or prescribe immediately after mefloquine should not be.

    Quinidine, quinine - possible development of sinus bradycardia, lengthening of the interval Q-T or cardiac arrest, an increased risk of seizures. If combined therapy is necessary, careful monitoring of the patient's condition is necessary; it is not recommended to appoint mefloquine earlier than 12 hours after the last dose of quinidine or quinine.

    Chloroquine - may increase the risk of seizures.

    Special instructions:

    May increase the risk of seizures in patients with epilepsy. During treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Instructions
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