What are the common side effects of mefloquine. How does mefloquine prevent malaria. Who should avoid taking mefloquine. What are the FDA warnings for mefloquine. How long can mefloquine side effects last.

What is Mefloquine and How Does it Prevent Malaria?

Mefloquine, formerly sold under the brand name Lariam® in the United States, is an antimalarial medication used to prevent and treat malaria. It is a round, white tablet taken once a week by travelers and military personnel in malaria-endemic regions such as parts of Africa, South America, Asia, Iraq, and Afghanistan.

Malaria is a serious infectious disease transmitted by mosquitoes. Mefloquine works by killing the malaria parasites in the blood, preventing the disease from taking hold. It is particularly useful for individuals who cannot take other antimalarial medications like doxycycline or atovaquone-proguanil.

How effective is mefloquine in preventing malaria?

Mefloquine is highly effective at preventing malaria when taken as directed. Its once-weekly dosing schedule makes it convenient for long-term use. However, its efficacy must be weighed against potential side effects, which can be significant for some individuals.

Common Side Effects of Mefloquine

While mefloquine is an effective antimalarial drug, it can cause various side effects. The most commonly reported adverse reactions include:

• Nausea
• Vomiting
• Diarrhea
• Dizziness
• Difficulty sleeping
• Bad dreams

These symptoms are typically mild and may not necessitate discontinuation of the medication. However, patients should consult their healthcare provider if they experience persistent or concerning side effects.

Can mefloquine cause more severe side effects?

Yes, more severe side effects can occur with mefloquine use. These may include:

• Convulsions or seizures
• Restlessness
• Confusion
• Unusual behavior
• Mood changes
• Agitation
• Suicidal thoughts or behavior

The frequency of these more serious side effects is not fully understood, but they warrant immediate medical attention if experienced.

FDA Warnings and Black Box Alert for Mefloquine

In 2013, the U.S. Food and Drug Administration (FDA) issued a safety alert for mefloquine and added a black box warning to its label. This is the FDA’s strongest warning and highlights significant safety concerns.

What specific warnings did the FDA issue for mefloquine?

The FDA warning emphasized two main categories of potential side effects:

1. Neurologic effects: These can include dizziness, loss of balance (vestibular problems), and tinnitus (ringing in the ears).
2. Psychiatric effects: These may involve anxiety, paranoia, depression, and hallucinations.

Importantly, the FDA noted that these neurologic or psychiatric side effects can occur at any time during drug use and may persist for months or even years after discontinuation of mefloquine.

Who Should Avoid Taking Mefloquine?

Despite its effectiveness in malaria prevention, mefloquine is not suitable for everyone. Individuals with certain medical conditions should not take this medication:

• Those with psychiatric conditions, including:
  • Active depression
  • Recent history of depression
  • Generalized anxiety disorder
  • Psychosis
  • Schizophrenia
  • Other major psychiatric disorders
• People with seizure disorders (epilepsy)
• Individuals with certain heart conditions, particularly irregular heartbeat and conduction problems
• Those taking specific medications, as advised by a healthcare provider

Are there special considerations for people with liver problems?

Yes, individuals with liver problems or those who consume alcohol or take medications affecting the liver may take longer to eliminate mefloquine from their bodies. This can potentially increase the risk or duration of side effects.

Long-Term Effects and Duration of Mefloquine Side Effects

One of the most concerning aspects of mefloquine use is the potential for long-lasting side effects. According to the FDA warning, neurologic and psychiatric side effects may persist for months or even years after stopping the medication.

How long can mefloquine side effects last?

The duration of mefloquine side effects can vary greatly between individuals. Some may experience short-term effects that resolve quickly after discontinuing the medication. Others, however, have reported persistent symptoms lasting months or years. This variability underscores the importance of careful monitoring and prompt reporting of any adverse effects to a healthcare provider.

Recent Research on Mefloquine Use and Health Outcomes

Ongoing research continues to shed light on the effects of mefloquine use, particularly among military personnel. Recent studies published by the Department of Veterans Affairs (VA) and the Department of Defense have provided valuable insights:

What have recent studies revealed about mefloquine use in military populations?

Two key studies have contributed to our understanding:

1. Schneiderman et al. (2018) examined associations between antimalarial medication use and health among U.S. veterans of the wars in Iraq and Afghanistan.
2. Eick-Cost et al. (2017) investigated neuropsychiatric outcomes after mefloquine exposure in U.S. military service members.

These studies help to quantify the risks associated with mefloquine use and inform policy decisions regarding its administration to military personnel.

Alternatives to Mefloquine for Malaria Prevention

Given the potential risks associated with mefloquine, it’s important to consider alternative antimalarial medications. Several options are available, each with its own risk-benefit profile.

What are some alternatives to mefloquine for preventing malaria?

Common alternatives to mefloquine include:

• Doxycycline: An antibiotic taken daily that also provides protection against some other infections.
• Atovaquone-proguanil (Malarone): A combination drug taken daily that is generally well-tolerated.
• Chloroquine: Used in areas where chloroquine-resistant malaria is not present.
• Primaquine: Can be used for short-term travel to areas with predominantly P. vivax malaria.

The choice of antimalarial medication depends on various factors, including the specific destination, length of stay, individual health status, and potential drug interactions.

Seeking Help for Mefloquine-Related Health Concerns

If you have taken mefloquine and are experiencing concerning side effects, it’s crucial to seek appropriate medical care. This is particularly important for symptoms that persist after discontinuing the medication.

Where can veterans seek help for mefloquine-related health issues?

Veterans concerned about mefloquine use or experiencing potential side effects should:

1. Consult with their primary care provider or a VA healthcare professional.
2. Consider reaching out to the Veterans Crisis Line at 1-800-273-8255 (press 1) or through online chat if experiencing suicidal thoughts.
3. Discuss their concerns with a mental health professional, especially if experiencing persistent neuropsychiatric symptoms.

Early intervention and comprehensive care can help manage and potentially mitigate long-term effects of mefloquine use.

Monitoring and Reporting Mefloquine Side Effects

Proper monitoring and reporting of mefloquine side effects are crucial for individual patient care and broader public health efforts. Both healthcare providers and patients play important roles in this process.

How should patients monitor and report mefloquine side effects?

Patients taking mefloquine should:

• Keep a detailed record of any side effects experienced, including their onset, duration, and severity.
• Report any side effects to their healthcare provider promptly, even if they seem minor.
• Be aware of the potential for delayed onset of side effects and continue monitoring after discontinuing the medication.
• Consider reporting serious side effects to the FDA’s MedWatch program, which helps track adverse events related to medications.

Healthcare providers should maintain vigilance in monitoring patients on mefloquine and report any significant adverse events to appropriate authorities.

Future Directions in Antimalarial Research and Development

The challenges associated with mefloquine use highlight the ongoing need for safer and more effective antimalarial medications. Research efforts continue to focus on developing new drugs and improving existing ones.

What are some promising areas of antimalarial drug research?

Current areas of focus in antimalarial research include:

1. Development of new drug compounds that target different stages of the malaria parasite’s life cycle.
2. Exploration of combination therapies that may offer improved efficacy and reduced side effects.
3. Investigation of novel drug delivery methods to enhance effectiveness and reduce adverse reactions.
4. Research into malaria vaccines, which could potentially provide long-term protection without the need for regular medication.

These research efforts aim to provide safer alternatives to drugs like mefloquine while maintaining or improving efficacy in malaria prevention and treatment.

Mefloquine (Lariam®) – Public Health

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Mefloquine (Lariam®)

Malaria is a serious infectious disease transmitted by mosquitoes. Malaria is found in Iraq, Afghanistan, and many areas in Africa, South America, and Asia.

Mefloquine is a round, white tablet taken once a week that can help prevent malaria for travelers. It is administered to both military personnel, including those serving in Iraq and Afghanistan, and civilians, although it is used less than it has been in the past.

Mefloquine is used based on recommendations from the Centers for Disease Control and Prevention. The brand Lariam® is no longer sold in the United States, although other brands of mefloquine are available. Mefloquine is particularly helpful for those who are unable to take other medications to prevent malaria such as doxycycline and atovaquone-proguanil.

Mefloquine side effects

The most commonly reported side effects from mefloquine are nausea, vomiting, diarrhea, dizziness, difficulty sleeping, and bad dreams. These symptoms are usually mild and may not cause people to stop taking the medicine. However, consult with your prescribing provider if you are concerned. Other side effects include convulsions or seizures, restlessness, confusion, and unusual behavior. People with liver problems, or those who drink alcohol or take medicines that affect the liver, may take longer to eliminate mefloquine from the body.

Recent scientific literature has suggested side effects including mood changes, bad or vivid dreams, agitation, suicidal thoughts, and suicidal behavior. How often these side effects occur is not fully understood. Contact a health care provider as soon as possible if you experience any side effects.

Although it is very effective at preventing malaria, individuals with the following conditions should not take mefloquine:

• Psychiatric conditions including active depression, a recent history of depression, generalized anxiety disorder, psychosis, schizophrenia, or other major psychiatric disorders. 
• Seizure disorders (epilepsy)
• Certain heart conditions (irregular heartbeat and conduction problems)
• Those taking certain medications, as advised by a health care provider

Mefloquine was approved by the Food and Drug Administration (FDA) in May 1989. In 2013, the FDA published a safety alert on mefloquine and added a black box warning (its strongest warning) to the drug label.  The FDA notice pointed out that neurologic side effects can include dizziness, loss of balance (vestibular problems), or ringing in the ears (tinnitus).   The safety alert also discussed psychiatric side effects which can include feeling anxious, mistrustful (paranoia), depressed, or having hallucinations (seeing or hearing things that are not there).   Neurologic or psychiatric side effects may occur at any time during drug use, and may last for months to years after the drug is stopped. 

If you are thinking about suicide, seek appropriate care immediately. Contact the Veterans Crisis Line at 1-800-273-8255 (press 1) or through online chat.

Recent Research

VA and the Department of Defense published the following research findings:

Schneiderman AI, Cypel YS, Dursa EK, Bossarte R. Associations between use of antimalarial medications and health among U. S. Veterans of the wars in Iraq and Afghanistan. Am J Trop Med Hyg 2018.

Eick-Cost AA, Hu Z, Rohrbeck P, Clark LL. Neuropsychiatric outcomes after mefloquine exposure among U.S. military service members. Am J Trop Med Hyg 2017; 96: 159-166.

Health concerns?

If you are concerned about mefloquine use, or have short or long-term potential side effects from taking mefloquine, talk to your health care provider.

VA offers a variety of health care benefits to eligible Veterans. Not enrolled in the VA health care system? Find out if you qualify for VA health care.

Compensation benefits for health problems

Veterans may file a claim for disability compensation for health problems they believe are related to mefloquine use during military service. VA decides these claims on a case-by-case basis. File a claim online.

Learn more about VA benefits.

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Resources

• Mefloquine (CDC)
• Revised Mefloquine Labeling (CDC)
• Mefloquine Drug Safety (FDA)
• Malaria
• Malaria field guide

Contact

Health Care
877-222-8387

Benefits
800-827-1000

TDD (Hearing Impaired)
800-829-4833

Mefloquine Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Warnings:

Mefloquine may cause mental/mood or nervous system problems. Tell your doctor right away if you have any of these serious side effects, including: mental/mood changes (such as anxiety, depression, restlessness, confusion, hallucinations, suicidal thoughts/attempts), ringing in the ears, dizziness, lightheadedness, loss of balance, or trouble sleeping. These side effects may continue to occur even after stopping mefloquine and certain side effects (such as dizziness, ringing in the ears, loss of balance) may become permanent. This medication should not be used to prevent malaria in people who have mental/mood disorders (such as depression, schizophrenia).

Warnings:

Mefloquine may cause mental/mood or nervous system problems. Tell your doctor right away if you have any of these serious side effects, including: mental/mood changes (such as anxiety, depression, restlessness, confusion, hallucinations, suicidal thoughts/attempts), ringing in the ears, dizziness, lightheadedness, loss of balance, or trouble sleeping. These side effects may continue to occur even after stopping mefloquine and certain side effects (such as dizziness, ringing in the ears, loss of balance) may become permanent. This medication should not be used to prevent malaria in people who have mental/mood disorders (such as depression, schizophrenia).

… Show More

Uses

How to use Mefloquine HCL

Read the Medication Guide provided by your pharmacist before you start taking mefloquine and each time you get a refill. If you have any questions, ask your doctor or pharmacist. Carry the information wallet card with you at all times.

Take this medication by mouth as directed by your doctor. Take it with food or milk to prevent stomach upset. Do not take the medication on an empty stomach. Take each dose of this medication with a full glass (8 ounces or 240 milliliters) of water. If you have trouble swallowing the medication, the tablet may be crushed and placed in a small amount of water, milk, or other beverage.

For children, the dosage is based on their weight. Early vomiting may occur in children after taking mefloquine. If vomiting occurs in your child after taking this medication, call the doctor right away to see if your child needs to take another dose of the medication. If vomiting continues, check with your doctor for a different medication to use in place of mefloquine.

When using this medication to prevent malaria, it is usually taken once a week. The first dose of this medication should be taken one week before travel, or as directed by your doctor.

Take this medication as prescribed for the full course of treatment. It is important that you do not miss any doses and that you take the drug on a regularly scheduled basis. Remember to take it on the same day each week.

Upon returning from the malaria area, you should keep taking this medication for 4 more weeks. If you are unable to finish this course of mefloquine, contact your doctor.

If this medication is being used for prevention of malaria, it is important to understand that it is still possible to contract the disease. Tell your doctor right away if you develop a fever. Malaria is best treated if therapy is started early.

Side Effects

See also Warning section.

Stomach upset/pain, loss of appetite, nausea/vomiting, headache, muscle pain, or diarrhea may occur. If any of these effects last or get worse, tell your doctor promptly.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: nausea/vomiting that doesn’t stop, loss of coordination, numbness/tingling/pain of hands or feet, vision changes, unusual tiredness, dark urine, yellowing skin/eyes.

Get medical help right away if you have any very serious side effects, including: fast/slow/irregular heartbeat, fainting, seizures.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before taking mefloquine, tell your doctor or pharmacist if you are allergic to it; or to quinine or quinidine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: mental/mood disorders (such as depression, anxiety, schizophrenia), seizures, heart problems, liver disorder.

This drug may make you dizzy or lose your balance. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Mefloquine may cause live bacterial vaccines (such as typhoid vaccine) not to work well. Tell your health care professional that you are using mefloquine before having any immunizations/vaccinations.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

This drug passes into breast milk. Consult your doctor before breast-feeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Some products that may interact with this drug include: artemether-lumefantrine, beta-blockers (such as atenolol, propranolol), chloroquine, halofantrine, ketoconazole, quinidine, quinine, drugs for seizures (such as phenytoin, valproic acid), ziprasidone.

Do not take halofantrine or ketoconazole for 15 weeks after your last dose of mefloquine.

Other medications can affect the removal of mefloquine from your body, which may affect how mefloquine works. Examples include rifamycins (such as rifabutin), azole antifungals (such as itraconazole), among others.

Does Mefloquine HCL interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

Do not share this medication with others.

It is important to wear protective clothing, insect repellent, and use bednets when trying to prevent malaria.

If you are taking this medication for a long time, lab and/or medical tests (such as eye exams, liver function) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Store at room temperature away from light and moisture. Do not store in bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Images

mefloquine 250 mg tablet

Color: whiteShape: ovalImprint: b 171

This medicine is a white, oval, scored, tablet imprinted with “b 171”.

mefloquine 250 mg tablet

Color: off-whiteShape: roundImprint: 54 111

This medicine is a white, oval, scored, tablet imprinted with “b 171”.

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Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Active substance MEFLOKIN (MEFLOQUINUM) | Compendium – drug reference book

• Pharmacological properties
• Indications MEFLOKHIN
• Application of MEFLOKIN
• Contraindications
• Side effects
• Special instructions
• Interactions
• Overdose
• Diagnosis
• Recommended alternatives
• Trade names

Medicinal preparations containing the active substance MEFLOKHIN

Lariam

tablets 250 mg, № 8

Roche

Prices in pharmacies

antimalarial drug. Mefloquine acts on asexual intracellular forms of human malaria pathogens: Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae and Plasmodium ovale. Mefloquine is effective against malaria pathogens resistant to other antimalarial drugs, such as chloroquine, proguanil, pyrimethamine, and the combination of pyrimethamine with sulfonamides. Cases of resistance have been described P. falciparum to mefloquine, mainly in Southeast Asia. Cross-resistance to mefloquine and halofantrine was noted.

Eating significantly accelerates the rate and extent of absorption, increasing bioavailability by approximately 40%. C _max in blood plasma are reached in 6-24 hours (on average after 17 hours) after a single dose of mefloquine.

When taken orally at a dose of 250 mg once a week, the equilibrium maximum plasma concentration (1000–2000 µg/l) is reached after 7–10 weeks.

The volume of distribution of mefloquine is about 20 L/kg, indicating penetration of the drug into many tissues. Mefloquine can accumulate in erythrocytes containing malaria parasites at concentrations approximately twice those in blood plasma. Plasma protein binding is about 98%. The MIC of mefloquine is about 600 µg/l.

Crosses the placenta. In minimal amounts passes into breast milk.

Two mefloquine metabolites have been identified in humans. The main metabolite (2,8-bis-trifluoromethyl-4-quinoline carboxylic acid) is inactive against P. falciparum .

T _½ mefloquine is from 2 to 4 weeks (average about 3 weeks). The total clearance is about 30 ml / min. Most of mefloquine and its metabolite are excreted in bile and feces. Age-dependent changes in the pharmacokinetics of mefloquine are not observed. The pharmacokinetics of mefloquine may change in acute malaria. With long-term antimalarial prophylaxis, the half-life of mefloquine does not change.

Treatment and prevention of malaria. Mefloquine is particularly indicated for the treatment of malaria caused by P. falciparum strains , resistant to other antimalarial drugs. It can also be prescribed for the treatment of P. vivax malaria and malaria of mixed etiology.

Malaria prophylaxis with mefloquine is recommended for travelers traveling to malaria-endemic areas, especially areas at high risk of infection with strains of P. falciparum that are resistant to other antimalarial drugs.

Emergency therapy (self-help). Mefloquine is recommended for self-administration as an emergency treatment for suspected malaria if urgent medical attention is not possible.

by mouth after meals with plenty of liquid.

Treatment. The total therapeutic dose of mefloquine for non-immune individuals is 20–25 mg/kg. For individuals with partial immunity, a lower total dose of 15 mg/kg may be sufficient.

Thus, non-immune persons weighing more than 45 kg should receive a total of 1250–1500 mg mefloquine, and partially immune persons of the same body weight 750–1000 mg mefloquine. If the patient vomits within 30 minutes after taking the drug, the full dose of mefloquine should be re-taken. If vomiting occurs 30-60 minutes after ingestion, an additional ¹ / 2 doses are prescribed.

After treatment of P. vivax malaria, relapse prevention with aminoquinoline derivatives (eg primaquine) is indicated to eliminate hepatic forms of Plasmodium.

If a full course of treatment with mefloquine after 48-72 hours does not lead to an improvement in the patient’s condition, it is necessary to decide on the appointment of another agent. In severe acute malaria, mefloquine may be given after an initial IV course of quinine therapy of at least 2 to 3 days. Most drug interactions leading to the development of side effects can be prevented if mefloquine is administered no earlier than 12 hours after the last dose of quinine.

In areas with multidrug-resistant malaria, initial treatment with artemisinin or its derivatives, followed by mefloquine, if possible, may be appropriate.

Prevention. The prophylactic dose of mefloquine is approximately 5 mg/kg body weight once a week. For adults and children weighing >45 kg, this corresponds to approximately 250 mg of mefloquine once a week. In children and adults weighing <45 kg, the daily dose is reduced accordingly. The first time the drug should be taken no later than 1 week before arrival in a malaria-endemic region. If this is not possible, it is necessary to prescribe a loading dose of the drug. For adults weighing >45 kg, it is 250 mg/day for 3 consecutive days, and then 250 mg once a week. Weekly doses of mefloquine should always be taken on the same day of the week. To reduce the risk of malaria after leaving an endemic region, prophylaxis is continued for another 4 weeks.

Emergency self-care. Mefloquine can be recommended for self-administration in cases where emergency medical care is not possible. Self-treatment should begin with a dose of about 15 mg/kg. If medical care continues to be unavailable for 24 hours, and severe adverse reactions to the drug do not appear, after 6-8 hours, you can take the second part of the total therapeutic dose. Patients weighing >60 kg should take another 250 mg 6-8 hours after the second dose. Patients should be advised to consult a doctor even if after self-treatment they feel completely recovered.

Hypersensitivity to mefloquine or related agents (quinine, quinidine). Mefloquine should not be prescribed for prophylactic purposes to persons who have a history of psychosis or seizures.

Nausea, vomiting, dizziness, imbalance, headache, drowsiness, insomnia, nightmares, diarrhea, abdominal pain are the most commonly reported. Adverse reactions during prophylaxis with mefloquine are usually mild and decrease with continued use. Less common are motor and sensory neuropathy (including with paresthesia), convulsions, visual disturbances, tinnitus, vestibular disorders, anxiety, anxiety, depression, memory loss, confusion, hallucinations, psychotic or paranoid reactions, isolated cases of encephalopathy; arterial hypo- or hypertension, flushing, fainting, tachycardia, palpitations, bradycardia, arrhythmia, extrasystole, isolated cases of AV blockade; skin rash, erythema, urticaria, pruritus, hair loss, isolated cases of erythema multiforme, Stevens-Johnson syndrome; muscle weakness, muscle cramps, myalgia, arthralgia; asthenia, general malaise, weakness, fever, chills, anorexia; transient increase in transaminase activity, leukopenia or leukocytosis, thrombocytopenia. Due to the large T _½ mefloquine side effects may develop or persist up to several weeks after the last dose of the drug.

mefloquine may increase the risk of seizures in patients with epilepsy. Therefore, mefloquine can be prescribed to such patients only for the purpose of treatment and if there are absolute indications for its use.

In patients with impaired liver function, the excretion of mefloquine may be slowed down, as a result of which the concentration of the agent in the blood plasma increases.

If anxiety, depression, restlessness or impaired consciousness develop during prophylactic use, mefloquine should be discontinued.

Limited experience with mefloquine in children under 3 months of age or <5 kg.

concomitant use of mefloquine and other related compounds (quinine, quinidine and chloroquine) may cause ECG changes and increase the risk of seizures. Because of the risk of potentially life-threatening prolongation of the Q-Tc interval, halofantrine should not be administered with or after mefloquine.

Administration of mefloquine to patients taking anticonvulsants (such as valproic acid, carbamazepine, phenobarbital, or phenytoin) may impair their anticonvulsant effect by decreasing their plasma concentrations. In some cases, dose adjustment of anticonvulsants may be required.

If mefloquine is administered concomitantly with oral live typhoid vaccines, a decrease in the immunogenicity of the latter cannot be excluded. Therefore, vaccination with live attenuated vaccines should be completed no later than 3 days before the first dose of mefloquine.

overdose of mefloquine may develop the symptoms listed in the SIDE EFFECTS section, but more pronounced. Gastric lavage, monitoring of cardiac function (including ECG) and neuropsychiatric status for at least 24 hours are recommended. If necessary, symptomatic and supportive measures are taken, in particular aimed at eliminating disorders of the cardiovascular system.

Mefloquine – description of the substance, pharmacology, use, contraindications, formula

Contents

• Structural formula

• Russian name

• English name

• Latin name

• chemical name

• Gross formula

• Pharmacological group of the substance Mefloquine

• Nosological classification

• CAS code

• pharmachologic effect

• Characteristic

• Pharmacology

• The use of the substance Mefloquine

• Contraindications

• Application restrictions

• Side effects of Mefloquine

• Interaction

• Overdose

• Dosage and administration

• Precautionary measures

• Trade names with the active substance Mefloquine

Structural formula

Russian name

Mefloquine

English name

Mefloquine

Latin name

Mefloquinum ( born 901 90 Mefloquini)

Chemical name

(R*,S*)-(±)- alpha-2-Piperidinyl-2,8-bis-(trifluoromethyl)-4-quinolinemethanol (and in hydrochloride form)

Gross formula

C ₁₇ H ₁₆ F ₆ N ₂ O

Pharmacological group of the substance Mefloquine

Other synthetic antibacterial agents

Nosological classification

ICD-10 code list

• B50 Plasmodium falciparum malaria

• B51 Plasmodium vivax malaria

• B52 Malaria due to Plasmodium malariae

• B54 Malaria, unspecified

CAS code

53230-10-7

Pharmacological action

Pharmacological action –

antimalarial , antiprotozoal .

Description

Powder of bitter and slightly burning taste.

Pharmacology

High hematoschizontocidal activity against Plasmodium falciparum and P. vivax, not effective against gamonts P. falciparum and hepatic histoschizonts P. vivax, may affect circulating schizonts P. ovale and P. malariae.

Resistance can develop fairly quickly. Resistant strains are found in areas where the drug has never been used before. It has a quinidine-like effect on the heart.

Well absorbed when taken orally, especially with food – food increases the absorption rate and increases bioavailability by 40%. max”>C _max is reached in 7-24 hours. Plasma concentration after a single appointment at an average therapeutic dose (250 mg) is 290-340 ng / ml, stationary concentration is 560-1250 ng / ml, which is much higher than the MIC for P. falciparum (200-300 ng/mL). About 98% binds to plasma proteins, concentrates in erythrocytes. The volume of distribution is about 20 l / kg, it penetrates through the BBB, the placenta, into breast milk. Decomposed in the liver with the formation of an inactive carboxylic acid metabolite and alcohol. Slowly excreted in the form of biotransformation products through the gastrointestinal tract (mainly). 1/2″>T _1/2 is 13 to 33 days, total Cl is 30 ml/min. Has a tendency to cumulation, can be detected in plasma within 1 month after discontinuation. Gives a therapeutic effect when taken weekly for 4 weeks after leaving the endemic zone.

Use of the substance Mefloquine

Malaria (mild to moderate treatment, prophylaxis) caused by chloroquine-resistant, pyrimethamine-sulfadoxine-resistant or multidrug-resistant strains Plasmodium falciparum; prevention of malaria due to P. vivax, P. ovale, P. malariae, before leaving for regions with a high risk of infection with strains Plasmodium falciparum, resistant to other antimalarial drugs; emergency treatment for suspected malaria and the impossibility of seeking urgent medical care.

Contraindications

Hypersensitivity, epileptic and other convulsive seizures, acute psychoses.

Application restrictions

Pregnancy, mental illness, severe liver dysfunction, age less than 2 years or body weight less than 15 kg.

Side effects of the substance Mefloquine

When using prophylactic doses: transient gastrointestinal disorders (nausea, vomiting, epigastric pain, diarrhea), headache, dizziness, fainting, extrasystole, unstable changes in laboratory parameters (leukocytosis, thrombocytopenia, increased blood transaminases), reversible neuropsychiatric disorders (convulsions, depression, psychosis). When using therapeutic doses: severe dyspepsia, fatigue, neuropsychiatric disorders (dizziness, headache, visual disturbances, tinnitus, insomnia, anxiety, anxiety, agitation, depression, disorientation, memory loss, confusion, hallucinations, acute psychoses or seizures), decrease or increase in blood pressure, tachycardia or bradycardia, transient disturbances in the rhythm and conduction of the heart, rashes, alopecia, pruritus, urticaria, erythema multiforme, changes in laboratory parameters.

Interaction

Enhances the inhibition of conduction and excitability of the heart muscle caused by beta-blockers, quinine, quinidine, halofantrine, calcium channel blockers. Reduces the antiepileptic activity of valproic acid, sodium divalproate, immunogenicity of live typhoid vaccines. Chloroquine, quinine increase the risk of seizures.

Overdose

Symptoms: nausea, vomiting, systemic dizziness, abdominal pain, disorders of the central and peripheral nervous systems, cardiovascular system.

Treatment: induction of vomiting and gastric lavage, symptomatic therapy. Long-term monitoring of hemodynamic parameters, ECG, neuropsychic status is required.

Dosage and administration

Inside, after eating, drinking plenty of water, milk or other liquids; pre-crushing of the tablet is acceptable. The total dose is 15-25 mg / kg (on average for an adult – 1-1.5 g), in one or 2-3 doses with an interval of 6-8 hours. When symptoms of malaria appear, adults are recommended to take 3 tablets at once, then after 6-8 hours (in the absence of side effects) – 2 more tables, and after 6-8 hours – 1 more table. For the prevention of malaria, 2-3 weeks before the expected arrival in a malaria-prone area, 5 mg / kg is prescribed once a week; in some cases, it is acceptable to take 1 week of the usual prophylactic dose, or immediately upon arrival, taking high doses (adults 250 mg daily for 3 days, then 1 time per week). After leaving the dangerous area, the prophylactic reception is continued for another 4 weeks.

Precautions

Patients should seek medical advice even if self-treatment seems to make a full recovery. In the first trimester of pregnancy, it can be prescribed if the benefit from the intended course outweighs the potential risk to the fetus. Women of childbearing age during the period of therapy need reliable methods of contraception. It is not recommended to use in severe forms of malaria (the effect comes slowly and parenteral administration is impossible).