Universal reference book for medicines
Product name: LARIAM (LARIAM)

Active substance: mefloquine

Type: Antimalarial drug

Manufacturer: F.Hoffmann-La Roche (Switzerland)
Composition, form of production and packaging
Tablets
1 tab.

mefloquine (in the form of hydrochloride) 250 mg

4 things.
- packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2010.

PHARMACHOLOGIC EFFECT

Lariam - hematocid, acts on asexual intracellular erythrocyte forms of human malaria pathogens: Plasmodium falciparum, Plasmodium vivax , on the circulating schizonts of Plasmodium malariae and Plasmodium ovale .
Not active against liver stages of parasites. Effective against malaria pathogens resistant to other antimalarial drugs, for example, chloroquine, proguanil, pyrimethamine and combinations of pyrimethamine with sulfonamides.
For P. falciparum , development of resistance to mefloquine is possible, mainly in Southeast Asia.
In some regions cross-resistance between mefloquine and halofantrine, mefloquine and quinine has been noted.
The drug does not cause hemolysis associated with insufficiency of glucose-6-phosphate dehydrogenase.

PHARMACOKINETICS

Suction

Absolute bioavailability of mefloquine after oral administration was not evaluated (absent in / in form).
Bioavailability of the tablet form is more than 85% of that when the solution is taken orally. Food intake significantly speeds up the rate and increases the degree of absorption by 40%. The average time to achieve C maxmefloquine after a single dose is 17 h (6-24 h). Cmax in plasma, measured in μg / l, is approximately equal to the dose taken, measured in mg (for example, a single dose of 1000 mg gives a Cmax of about 1000 μg / l). After a regular intake of 250 mg mefloquine 1 time / week C ss max , equal to 1000-2000 μg / l, is achieved after 7-10 weeks. To achieve 95% effectiveness of prevention, a concentration of mefloquine in the blood, equal to 620 ng / ml.
Distribution

V d mefloquine 20 l / kg, which indicates the penetration of the drug in many tissues.
It accumulates in red blood cells, inside of which there are malarial parasites, in concentrations about twice that of plasma ones. Penetrates through the placental barrier, as well as into breast milk. Communication of the preparation with plasma proteins 98%.
Metabolism

Metabolized with the formation of 2 metabolites: the main metabolite, 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, and alcohol.
The main metabolite is inactive against P. falciparum, appears in the plasma 2-4 hours after a single oral intake of the drug, its C max in plasma is 50% higher than those of mefloquine and is achieved in 2 weeks. After that, the decrease in the concentrations of the main metabolite and mefloquine in plasma occurs at the same rate. AUC of the main metabolite is 3-5 times higher than that of the parent drug. Another metabolite, alcohol, is present in very small quantities.
Excretion

The mean T 1/2 mefloquine for 3 weeks (2 to 4 weeks) does not change with prolonged antimalarial prophylaxis.
It is excreted as metabolic products mainly with bile and feces. The total clearance, most of which is hepatic, is 30 ml / min. Excretion of unmodified mefloquine and its main metabolite by the kidneys composes about 9% and 4%, respectively. Other metabolites in the urine are not detected.
Pharmacokinetics in special cases.

Children and elderly patients : age does not affect the pharmacokinetics of mefloquine.

Pharmacokinetic studies in patients with renal insufficiency have not been carried out, since very small amounts of the drug are excreted with the kidneys.
In any significant amounts of mefloquine and its main metabolite with the help of hemodialysis are not deduced. Dose adjustments for hemodialysis patients are not required.
Hepatic insufficiency: in patients with impaired hepatic function, the excretion of mefloquine can be slowed down, so that the plasma concentrations of the drug increase.

Pregnancy does not have a clinically significant effect on the pharmacokinetics of mefloquine.

The race .
Pharmacokinetic differences are of very little clinical importance in comparison with the immune status of an infected patient and a sensitive pathogen.
INDICATIONS

- treatment of mild and moderate forms of malaria caused by P. falciparum strains, resistant to other antimalarial drugs, P. vivax, and malaria of mixed etiology;

- malaria prophylaxis for people moving to malaria-dangerous regions, especially in regions with a high risk of infection with P. falciparum strains resistant to other antimalarial drugs;

- first aid (self-help): self-administration as an emergency therapy for suspected malaria, if urgent medical assistance is not possible.

DOSING MODE

Inside, after eating, squeezed a large amount of fluid (at least 200 ml), in 2-3 hours.

Mefloquine has a bitter and slightly burning taste.
Tablets should be swallowed whole. When prescribed to children or persons who can not swallow the whole tablet, it can be crushed and dissolved in a small amount of water, milk or other beverage.
Tablets should not be removed from the blister until the intake, as they are sensitive to moisture.

Prevention

Adults and children weighing more than 45 kg: 5 mg / kg (250 mg, 1 tablet Lariam) 1 time / week.

Adults and children with a body weight of 30 to 45 kg - 3/4 tablets, children with a body weight of 20 to 30 kg - 1/2 tablets, children with a body weight of 10 to 20 kg - 1/4 tablets, children with weight body from 5 to 10 kg - 1/8 tablets.

Weekly doses of Lariam should be taken always on the same day of the week.
The first time the drug should be taken at least a week before arriving in a malaria-endemic region. If this is not possible, it is necessary to prescribe a shock dose of the drug. For adults weighing more than 45 kg, it is 1 tablet of Lariam (250 mg) per day for 3 consecutive days, and then - 1 tablet / week. To reduce the risk of malaria after leaving the endemic region, prevention continues for another 4 weeks. If the patient is taking other medications, it is advisable to begin prophylaxis 2-3 weeks before departure to ensure that the concomitant medication is well tolerated.
Treatment

The recommended total therapeutic dose of mefloquine is 20-25 mg / kg.

Body weight, kg Total dose, tab.
Dose distribution for receptions 1
5-10 1/2 - 1

10-20 1-2

20-30 2-3 2 + 1

30-45 3-4 2 + 2

45-60 5 3 + 3

> 60 6 3 + 2 + 1

1 Distribution of the total therapeutic dose for 2-3 doses with an interval of 6-8 hours can reduce the frequency and severity of side effects.

The experience of using total doses exceeding 6 tablets in individuals with very large excess body weight is not.

Dosage in special cases

For individuals with reduced immunity, residents of malaria-endemic regions may have a smaller overall dose.

If within 30 minutes after taking the drug the patient has vomiting, you should repeatedly take a full dose of Lariam.
If vomiting occurs after 30-60 minutes after ingestion, an additional half of the dose is prescribed.
After the treatment of malaria caused by P. vivax, the prevention of relapses with preparations that are derivatives of 8-aminoquinoline (for example, primaquine) is indicated to eliminate the hepatic forms of plasmodia.

If the full course of treatment with Lariam in 48-72 hours does not lead to an improvement in the patient's condition, it is necessary to decide on the appointment of another remedy.

If malaria develops in the course of prophylaxis with Lariam, the doctor should carefully consider which drug to choose for therapy.
For the appointment of halofantrine, see "Special instructions" and "Interactions".
In severe acute malaria, Lariam can be administered after an initial IV course of quinine therapy lasting at least 2-3 days.
Most drug interactions leading to the development of side effects can be prevented by taking Lariam at least 12 hours after the last dose of quinine.
In regions with multiresistant pathogens of malaria, initial treatment with artemisinin or its derivatives may be appropriate, followed, if possible, by Lariam therapy.

Independent emergency therapy

The initial dose of Lariam for patients with a body weight of 45 kg or more is 15 mg / kg (3 tablets, 750 mg).
If medical care remains inaccessible for 24 hours and there are no serious side effects, then after 6-8 hours, the second part of the total therapeutic dose of 500 mg can be taken (for patients with a body weight of 45 kg or more, 2 tablets). Patients with a body weight of more than 60 kg 6-8 hours after repeated taking should take another pill.
To confirm or exclude a presumptive diagnosis, patients should be advised to see a doctor even if, after self-treatment, they feel completely recovered.

SIDE EFFECT

When taking Lariam in doses prescribed for the treatment of acute malaria, there may be side effects similar to those of the underlying disease.

The incidence of adverse events during mefloquine prophylaxis is comparable to that of other chemoprophylaxis regimens.
The profile of side effects of mefloquine is characterized by the prevalence of reactions from the neuro-psychic sphere.
The most frequent side effects are usually mild and decrease with continued use of the drug.
These include nausea, vomiting, fecal incontinence, diarrhea, abdominal pain, dizziness, imbalance, headache, drowsiness, insomnia, nightmares.
Less common are the following side effects.

From the side of the central nervous system and the peripheral nervous system: sensory and motor neuropathies, paresthesia, tremor, ataxia, convulsions, agitation, anxiety, anxiety, depression, panic attacks, memory impairment, confusion, hallucinations, aggressive, psychotic and paranoid reactions, in rare cases - suicidal ideas (their connection with the drug is not established), rarely - encephalopathy.

From the cardiovascular system : a decrease or increase in blood pressure, hot flashes, fainting, chest pain, tachycardia, palpitations, bradycardia, arrhythmia, incl.extrasystole, transient conduction disorders, rarely - AV blockade.

Dermatological reactions : skin rash, exanthema, erythema, urticaria, pruritus, edema, alopecia, rarely - multiforme exudative erythema, Stevens-Johnson syndrome.

Musculoskeletal system: myasthenia gravis, muscle cramps, myalgia, arthralgia.

From the sense organs: visual disturbances, disorders of the vestibular apparatus (dizziness), hearing impairment.

On the part of the hematopoiesis system: leukopenia or leukocytosis, thrombocytopenia, reduction of hematocrit.

Other : shortness of breath, malaise, weakness, fever, sweating, chills, loss of appetite, transient increase in hepatic transaminase activity.

Because of the large T 1/2 mefloquine, side effects can develop or persist up to several weeks after the last administration of the drug.

CONTRAINDICATIONS

- Depression;

- psychoses;

- schizophrenia;

- anxiety states;

- convulsions (including in the anamnesis);

- Pregnancy;

- co-administration with halofantrine, administration of halofantrine after mefloquine therapy;

- Hypersensitivity to the components of the drug or drugs close to it (quinine, quinidine).

With caution : hepatic insufficiency, I trimester of pregnancy, the period of breastfeeding, mental illness, age under 6 months, body weight up to 5 kg, heart disease, age over 65, combination with quinine and quinidine.

PREGNANCY AND LACTATION

Contraindicated in the II and III trimesters of pregnancy.
With caution in the I trimester.
When mefloquine was used in doses 5-20 times higher than therapeutic for humans, it had teratogenic effects in mice and rats and embryotoxic effects in rabbits.However, the experience of clinical use of Lariam did not reveal any embryotoxic or teratogenic effects.
However, Lariam should be prescribed in the first trimester of pregnancy only if the intended benefit to the mother exceeds the potential risk to the fetus. Women of reproductive age should be treated only if reliable contraception is used during the entire period of mefloquine intake and 3 months after the last dose. But when there is a pregnancy against the background of chemo prophylaxis of malaria, Lariam does not testify to its interruption.
The activity of small amounts of mefloquine falling into breast milk is unknown.
During the period of breastfeeding, the drug is prescribed only if the intended benefit to the mother exceeds the potential risk for the child. In children whose mothers took Lariam during breast-feeding, no adverse reactions were noted.
APPLICATION FOR FUNCTIONS OF THE LIVER

There is no data on the use of Lariam in patients with impaired renal function.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

The drug is administered with caution to patients with hepatic insufficiency.

APPLICATION FOR CHILDREN

The drug is administered with caution to children under 6 months of age, as well as children weighing up to 5 kg (Lariam's experience in this category of patients is limited).

APPLICATION IN ELDERLY PATIENTS

The drug with caution is prescribed to patients older than 65 years.

SPECIAL INSTRUCTIONS

Lariam may increase the risk of seizures in patients with epilepsy.
Therefore, for such patients, the drug can be administered only for the purpose of treatment and in the presence of absolute indications for its use (see also "Interactions").
After quinine or quinidine, mefloquine can be taken no earlier than 12 hours later.
With a preventive appointment for a long time (taking the drug for more than 1 year is not desirable), periodic analysis of the liver function and ophthalmological examination is necessary.
Because of the danger of a potentially life-threatening lengthening of the QT interval, halophthrin can not be administered with or after Lariam.
There are no data on the use of Lariam after halophthrin.
With the development of anxiety, depression, anxiety or impaired consciousness with the preventive use of Lariam, the drug should be withdrawn.

The experience of using Lariam in children under the age of 6 months or with a weight of less than 5 kg is limited.

Influence on the ability to drive vehicles and work with machines and mechanisms

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.

OVERDOSE

Symptoms: Lariam overdose is characterized by a manifestation of side effects in a more pronounced form.

Treatment: induce vomiting, rinse the stomach.
If necessary, conduct symptomatic and intensive supportive measures aimed at eliminating cardiovascular disorders. It is necessary to control hemodynamic parameters, ECG and neuro-psychic status for a minimum of 24 hours.
DRUG INTERACTION

Simultaneous reception of Lariam and quinine, quinidine and chloroquine can cause changes on the ECG and increase the risk of seizures.

The use of halofantrine after mefloquine leads to a significant elongation of the QTc interval (the QT interval, corrected for heart rate, is calculated by the formula: QTc = QT / RR 1/2 ).
When treating only mefloquine, there is no clinically significant prolongation of QTc. Simultaneous administration of other drugs that affect cardiac conduction (antiarrhythmic drugs, β-adrenoblockers, calcium channel blockers, antihistamines, in particular, H 1 -gistamine blockers, tricyclic antidepressants and phenothiazines) may also play a role in prolonging the QTc interval.
Reduces the effectiveness of anticonvulsants (valproic acid, carbamazepine, phenobarbital or phenytoin), reducing their concentrations in the plasma.
It is necessary to monitor the concentration of drugs in the plasma. In some cases, a dose adjustment of anticonvulsants may be required.
Lariam can reduce the immunogenicity of oral live typhoid vaccines when taken concomitantly, so vaccination with live attenuated vaccines should be completed at least 3 days before Lariam's first intake.

Other drug interactions Lariam unknown.
But people receiving other drugs, in particular, anticoagulants or hypoglycemic agents, must undergo medical supervision before leaving for an endemic region.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

Storage conditions:

Store at temperatures up to 30 ° C in a place protected from moisture out of the reach of children.

Shelf life:

3 years.

The drug should not be used after the expiry date indicated on the package.

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