Lariam

Lariam is a remedy for malaria. The active component of the drug is the substance methanolquinoline.

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Indications of the lariamah

It is used for treatment in the following cases:

• therapy for malaria occurring in an uncomplicated form (which is provoked by the action of plasmodium strains by falsiparum and other bacterial pathogens that have resistance to the rest of the antimalarial drugs);
• with malaria of mixed origin, or a bacterium-induced plasmodium Vivax;
• for the prevention of the development of malaria in persons who are going to visit regions in which there is a high risk of contracting it;
• as an emergency aid or self-help - to people who are suspected of malaria.

Release form

The release is carried out in tablets, 4 pieces inside the blister plate. The pack contains 2 blister packs.

Pharmacodynamics

Lariam influences asexual types of pathology (intra-erythrocyte origin). This list includes plasmodium Vivax and plasmodium falciparum, and in addition Plasmodium malariae and Plasmodium oval.

Along with this, the drug effectively acts against bacteria that have shown resistance to many other drugs. Among them, Proguanil with Chloroquine, and in addition Pyrimethamine and a combination of pyrimethamine with sulfonamides.

In the course of the tests, it was found that the stability of the plasmodium falsiparum for mefloquine is found mainly in South-East Asia, where bacteria are often resistant to a variety of known drugs. There is information about the cross-resistance of mefloquine with quinine and halophantrine substances.

Pharmacokinetics

The level of bioavailability is more than 85%. Eating with food increases the degree and speed of absorption, and in addition the bioavailability indicator (by about 40%). Peak values inside the plasma, which are about the same as the dose taken, reach after 6-24 hours. To obtain equilibrium indices inside the plasma (amounting to 1000-2000 μg / l) it is possible with the use of a medicine in the amount of 250 mg once a week for a period of 7-10 weeks.

The distribution volume of mefloquine is approximately 20 l / kg. The substance can pass into the tissues, through the placental barrier, and in small amounts enter into the mother's milk. Protein synthesis is 98%.

To achieve 95% of the preventive efficacy of drugs, it is required to achieve indices inside the bloodstream that are at least 620 ng / ml (inside the red blood cells containing malarial bacteria, these values should be 2 times higher).

Inside the body, mefloquine is transformed with the help of hemoprotein P450 3A4 into 2 decay products - carboxymethoxylocin with hydroxyfloquine. The main among them is 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, which has no activity against the plasmodium falsiparum bacterium.

The average indicator of the half-life is 3 weeks. Excretion is mainly carried out with feces, as well as bile. The total clearance level is 30 ml / minute (mainly inside the liver). With urine, 9% mefloquine is eliminated unchanged, and 4% of its main decay product.

Dosing and administration

Tablets are taken orally, they are consumed after meals, washed down with water (minimum 200 ml). The tablet needs to be swallowed whole, because it has a bitter taste and a bit burning. If the patient's inability to swallow the whole medicine is allowed to crush the tablet and add to the liquid that he drinks.

Use for the prevention of malaria.

The size of the adult dosage (and for children weighing from 45 kg) is equal to a maximum of 5 mg / kg once a week (taken on a strictly defined day). At a weight in the range of 30-45 kg, the dosage is 3/4 tab., With a weight of 20-30 kg - half the tablet, with a weight of 10-20 kg - a quarter of the tablet, and with a weight within 5-10 kg - a maximum of 0.125 tablets.

The first dose of Lariam should be taken before visiting a region in which the risk of contracting malaria is high (basically it is done in 7 days). If the dosage has not been taken beforehand, shock treatment is required - to use the one-time-once-weekly dose, dosage is required for 3 days in a row, and then reconstructed into the usual regimen. To reduce the likelihood of developing the disease after leaving the potentially dangerous area, even during the first month, it is necessary to take medicines in preventive mode. If a person is treated with other drugs, preventive maintenance should begin no later than 2-3 weeks before the trip to make sure the safety of the combination of medications.

Treatment with Lariam.

The total size of the standard dose that achieves the desired effect is 20-25 mg / kg, and can vary depending on the weight of the patient, and also be distributed with some variations (using a total medication dose of 2-3 doses with a gap of 6- 8 hours, side effects can be prevented).

Persons weighing more than 60 kg should take 6 tablets (in 3 receptions according to the 3 + 2 + 1 pill), and for people with a weight within 45-60 kg - 5 tablets (2 admission, scheme 3+ 2 tablets). At weight in a range of 30-45 kg it is necessary to take 3-4 tablets (in 2 receptions under the scheme 2 + 2 tablets). Weight 20-30 kg - 2-3 tablets (in 2 receptions, according to the scheme 2 + 1 tablet). At a weight of 10-20 kg take 1-2 tablets with one dose, and at a weight of 5-10 kg - also in 1 take 0.5-1 tablet.

Dose features in some situations:

• with weakened immunity, and in addition to people living in endemic malarial regions, you can take a reduced total dose;
• if the patient develops vomiting for up to half an hour after consuming the tablets, he needs to drink the full dosage again, and if vomiting begins in the 0.5-1 hour after taking - take an additional half of the dosage;
• if the infectious agent of malaria is the plasmodium Vivax to remove plasmodium from the liver, it is necessary to prevent the occurrence of relapses using the derivatives of 8-aminoquinoline substance (for example, Primachin);
• if there are no improvements after 48-72 hours after the completion of the full treatment course or when malaria develops during prevention, the doctor should choose another medicine;
• In severe forms of acute type of malaria, the drug is allowed to be consumed after a 2-3-day therapy with intravenous quinine. It is necessary to observe the interval between the applications of these drugs at least 12 hours to prevent the development of many pharmacological interactions;
• in areas where germs-pathogens have cross-resistance, the result may be a scheme with the initial use of artemisinin or its derivatives, and then using Lariam.

Self-medication.

It is required to take the initial dose - a minimum of 15 mg / kg. For example, with a weight of more than 45 kg - taking 3 tablets (dose is 750 mg). If it is not possible to receive medical care in the future and there are no negative manifestations, after 6-8 hours it is necessary to take the 2 nd half of the total dose - 2 tablets (the dose will be 500 mg). At a weight of more than 60 kg after another 6-8 hours in addition use another 1-well pill.

To exclude or confirm the diagnosis, you need to visit a doctor, even if you feel well.

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Use of the lariamah during pregnancy

Use Lariam in the 1st trimester is allowed only in situations where the likely benefit for a woman exceeds the risk of complications in the child.

Women who are in reproductive age, when using drugs, and also 3 months after the end of the course, should use reliable contraceptives. But with the conception that has already come during the treatment, the termination of pregnancy is not required.

Mefloquine passes into the mother's milk in small amounts. Because there is no information about its effect in such cases, it is required to refuse breastfeeding for the period of Lariam's admission.

Contraindications

Among the contraindications:

• anxiety or depression, as well as psychosis;
• a patient suffering from schizophrenia;
• the presence of convulsions (also if they have a history);
• therapy with Halofantrine, and in addition the appointment after using mefloquine (prolongation of the QT-interval values, which will be life-threatening) may occur;
• manifestations of intolerance with respect to elements of the drug or similar therapeutic agents-such as quinidine or quinine.

It is required to use the medicine with caution in the presence of liver failure or epilepsy (because it increases the likelihood of seizures), and in addition to people with mental disorders and heart pathologies. Also, caution is necessary when prescribing to infants under six months of age weighing less than 5 kg, and elderly people (over 65 years of age).

Side effects of the lariamah

During therapy in the acute stage of malaria, side effects, which are symptoms of the underlying pathology, may appear.

Most often, these disorders are noted (they are often expressed rather poorly, and their manifestation decreases during the course of treatment): vomiting, head and abdominal pain, diarrhea, nausea, incontinence, balance problems, diarrhea, nightmares, dizziness, and insomnia and a feeling of drowsiness.

Occasionally, the following complications and disorders occur:

• the state of depression, encephalopathy, motor or sensory-type neuropathy, ataxia, paresthesia with convulsions and tremor. There is a feeling of anxiety, agitation, confusion or anxiety, memory worsens, hallucinations and panic attacks develop, thoughts of suicide develop, as well as manifestations of a paranoid psychotic and aggressive nature;
• increased or decreased index of blood pressure, tachycardia, palpitations, bradycardia, hot flushes, and in addition extrasystole with arrhythmia. There may be AV blockades and transient problems with cardiac conduction;
• urticaria, rashes on the skin surface, swelling, exanthema, alopecia, itching, and erythema (this includes exudative polyforma) and Stevens-Johnson syndrome;
• Myalgia with myasthenia gravis, as well as arthralgia;
• may develop problems with hearing, vision or vestibular apparatus;
• thrombocyto- or leukopenia, a decrease in the amount of hematocrit and leukocytosis;
• a state of fever and a feeling of weakness, increased sweating, a feeling of chills and loss of appetite.

Due to the prolonged period of drug excretion, negative effects may persist and manifest themselves during a few more weeks after the end of drug administration.

Overdose

Among the characteristic signs of poisoning: increased severity of side effects.

Treatment in this case is as follows: induction of vomiting and gastric lavage, as well as symptomatic procedures. In addition, intensive activities are carried out to maintain the function of the CAS, monitor hemodynamic values and ECG parameters, as well as assess the patient's mental state (during the first day).

Interactions with other drugs

When combining Lariam with chloroquine, quinidine, and quinine, ECG changes can be observed, and the likelihood of seizures may increase.

Ca channel blockers, antiarrhythmic and antihistamines, tricyclics, β-adrenoblockers, phenothiazines, as well as histamine blockers (H1) affect the conduction processes inside the heart, and may affect the prolongation of QT-interval values.

Since the plasma values of valproate, carbamazepine and phenytoin with phenobarbital decrease with the combination with Lariam, which weakens their effectiveness, the dosage of these drugs may need to be changed.

The combination of the drug with live vaccines of typhoid for oral administration reduces the immunogenicity of the latter. Because of this, it is required to perform the vaccination at least 3 days before the start of Lariam use.

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Storage conditions

Lariat should be kept in a place protected from moisture. The temperature should not exceed + 30 ° C.

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Special instructions

Reviews

Lariam is a fairly popular drug, which is often used as a preventive measure against the development of malaria in the case of travel to countries with a high endemic level. Reviews about him are quite good, but because microbes-pathogens of malaria in different regions have differences (for example, in Sri Lanka), treatment or prevention is forbidden to perform on their own - they should be assigned only by a professional specialist who can assess the picture and choose the size of the dosage or any other medicine against malaria, if necessary.

Shelf life

Lariam can be used in the 3 years since the release of the drug.