Mef-Q Tablet 250 mg
Mef-Q Tablet 250 mg Uses, Dosage, Side Effects, Food Interaction and all others data.
Mef-Q Tablet 250 mg has been found to produce swelling of the Plasmodium falciparum food vacuoles. It may act by forming toxic complexes with free heme that damage membranes and interact with other plasmodial components.
Mef-Q Tablet 250 mg is an antimalarial agent which acts as a blood schizonticide. Mef-Q Tablet 250 mg is active against the erythrocytic stages of Plasmodium species. However, the drug has no effect against the exoerythrocytic (hepatic) stages of the parasite. Mef-Q Tablet 250 mg is effective against malaria parasites resistant to chloroquine. Mef-Q Tablet 250 mg is a chiral molecule. According to some research, the (+) enantiomer is more effective in treating malaria, and the (-) enantiomer specifically binds to adenosine receptors in the central nervous system, which may explain some of its psychotropic effects.
Sporozoites located in the salivary glands of mosquitoes infected with malaria parasites are introduced into the bloodstream of a human host during mosquito feeding. These sporozoites rapidly invade the liver, where they mature into liver-stage schizonts, rupturing and releasing 2,000 - 40,000 merozoites that invade red blood cells. Mef-Q Tablet 250 mg is an antimalarial drug acting as a blood schizonticide, preventing and treating malaria.
Trade Name | Mef-Q Tablet 250 mg |
Availability | Prescription only |
Generic | Mefloquine |
Mefloquine Other Names | Mefloquin, Mefloquina, Méfloquine, Mefloquine, Mefloquinum |
Related Drugs | doxycycline, clindamycin, hydroxychloroquine, Plaquenil, Cleocin, Vibramycin, Malarone |
Weight | 250 mg |
Type | Tablet |
Formula | C17H16F6N2O |
Weight | Average: 378.3122 Monoisotopic: 378.116682374 |
Protein binding | The binding of mefloquine to plasma proteins is over 98%. |
Groups | Approved, Investigational |
Therapeutic Class | Anti-malarial drugs |
Manufacturer | Renata Limited |
Available Country | Bangladesh |
Last Updated: | October 19, 2023 at 6:27 am |
![Mef-Q Tablet 250 mg Mef-Q Tablet 250 mg](https://www.medicinesfaq.com/media/png/mef-q-tablet.png)
Uses
Mef-Q Tablet 250 mg is used for-
- Acute Malaria Infections caused by Mef-Q Tablet 250 mg-susceptible strains of Plasmodium falciparum (both chloroquine- susceptible and resistant strains) or by P. vivax
- Prophylaxis of P. falciparum and P. vivax malaria infections
Mef-Q Tablet 250 mg is also used to associated treatment for these conditions: Malaria caused by Plasmodium falciparum, Malaria caused by plasmodium vivax
How Mef-Q Tablet 250 mg works
The mechanism of action of mefloquine is not completely understood. Some studies suggest that mefloquine specifically targets the 80S ribosome of the Plasmodium falciparum, inhibiting protein synthesis and causing subsequent schizonticidal effects. There are other studies in the literature with limited in vitro data on mefloquine's mechanism of action.
Dosage
Mef-Q Tablet 250 mg dosage
Adult:
- Malaria prevention: 1 tablet (250 mg) once per week starting 1-2 weeks before departure and continued for 4 weeks after leaving malarious area.
- Malaria treatment: 5 tablets (5 x 250 mg) in a single dose (up to max. 1.5 gm) or preferably in 2 divided doses 6 to 8 hours apart.
In Children 6 Months and Older:
- Malaria prevention: Approximately 5 mg/kg body weight once per week (250 mg for children weighing over 45 kg, decreasing in proportion to body weight for children weighing 45 kg or less).
- Malaria treatment: 20 to 25 mg/kg body weight which may be split into two doses 6 to 8 hours apart to reduce the occurrence or severity of adverse reactions.
Geriatric Use: Experiences have not identified differences in responses between the elderly and younger patients.
Should be taken with food. Best taken with meals & a full glass of water.
Side Effects
Among subjects who received Mef-Q Tablet 250 mg for prophylaxis of malaria, following side effects was observed:
- The most frequently observed sied-effects were vomiting, dizziness, syncope, extrasystoles and other complaints affecting less than 1%. Among subjects who received Mef-Q Tablet 250 mg for treatment, following side-effects was observed:
- The most frequently observed side-effects included : dizziness, myalgia, nausea, fever, headache, vomiting, chills, diarrhoea, skin rash, abdominal pain fatigue, loss of appetite, and tinnitus
Toxicity
The oral TDLO of mefloquine in humans is 11 mg/kg/2W (intermittent) and 880 mg/kg in the rat. Intraperitoneal LD50 in the rat is 130 mg/kg. Symptoms of an overdose with mefloquine may manifest as a worsening of adverse effects. In the case of an overdose, symptomatic and supportive care should be provided. There is no known antidote for an overdose with mefloquine. Monitor cardiac function by ECG, follow neuropsychiatric status for at least 24 hours, and provide treatment as required.
Precaution
Warnings: Mef-Q Tablet 250 mg may cause psychiatric symptoms in a number of patients, ranging from anxiety, paranoia, and depression to hallucinations and psychotic behavior. Rare cases of suicidal ideation and suicide have been reported though no relationship to drug administration has been confirmed. Mef-Q Tablet 250 mg should be used with caution in patients with a previous history of depression. Concomitant administration of Mef-Q Tablet 250 mg and quinine or quinidine may produce electrocardiographic abnormalities and may increase risk of convulsions.
Precautions: In patients with epilepsy, Mef-Q Tablet 250 mg may increase the risk of convulsions. Caution should be exercised with regard to activities requiring alertness and fine motor coordination such as driving, piloting aircraft and operating machinery. Mef-Q Tablet 250 mg should be used with caution in patients with psychiatric disturbances. In patients with impaired liver function the elimination of Mef-Q Tablet 250 mg may be prolonged, leading to higher plasma levels.
Interaction
Increased risk of ECG abnormalities with quinine or chloroquine, antihistamines, TCAs and phenothiazines. May increase risk of seizure with quinidine or quinine. Concomitant use with valproic acid, phenobarbital, carbamazepine and phenytoin may cause loss of seizure control and lower plasma levels of anticonvulsants. Increased risk of QT prolongation and arrhythmia with ketoconazole. Concomitant use with digoxin, Ca channel blockers, antiarrhythmics and β-blockers may increase the risk of cardiotoxicity. Increased risk of ventricular arrhythmias with amiodarone. Concomitant use with TCAs, SSRIs, buprion, antipsychotic, tramadol may increase the risk of convulsions. Increased plasma levels with metoclopromide. May compromise adequate immunisation by live typhoid vaccine. Vaccinations with attenuated live bacteria should be completed at least 3 days prior the 1st dose of mefloquine.
Food Interaction
- Avoid alcohol.
- Take with a full glass of water.
- Take with food. The presence of food significantly enhances the rate and extent of absorption, leading to about a 40% increase in bioavailability.
[Moderate] ADJUST DOSING INTERVAL: Food enhances the oral absorption and bioavailability of mefloquine.
The proposed mechanism is increased drug solubility in the presence of food.
In 20 healthy volunteers, administration of a single 750 mg oral dose of mefloquine 30 minutes following a high-fat meal increased the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of mefloquine by 73% and 40%, respectively, compared to administration in the fasting state.
The Cmax and AUC of the carboxylic acid metabolite were also increased by 35% and 33%, respectively, compared to fasting.
In addition, the time to reach peak plasma concentration (Tmax) of mefloquine was significantly shorter after food intake (17 hours) than in the fasting state (36 hours).
There was no difference in the elimination half-life of mefloquine and metabolite, or the Tmax for the metabolite.
MANAGEMENT: To ensure maximal oral absorption, mefloquine should be administered immediately after a meal with at least 8 ounces of water.
Mef-Q Tablet 250 mg Drug Interaction
Moderate: hydroxyzine, ciprofloxacin, dexamethasone, pregabalin, quetiapineUnknown: zolpidem, celecoxib, omega-3 polyunsaturated fatty acids, cyclobenzaprine, atovaquone / proguanil, acetaminophen, montelukast, oseltamivir, acetaminophen, cyanocobalamin, pyridoxine, ascorbic acid, cholecalciferol, alprazolam, cetirizine
Mef-Q Tablet 250 mg Disease Interaction
Major: psychosis/depression, seizuresModerate: ECG abnormalities, liver disease
Volume of Distribution
The apparent volume of distribution is in healthy adults is about 20 L/kg with wide tissue distribution. Various estimates of the total apparent volume of distribution range from 13.3 to 40.9L/kg. Mef-Q Tablet 250 mg can accumulate in erythrocytes that have been infected with malaria parasites.
Elimination Route
Mef-Q Tablet 250 mg is readily absorbed from the gastrointestinal tract; food significantly increases absorption and increases bioavailability by 40%. The bioavailability of tablets compared with the oral solution preparation of mefloquine is over 85%. Cmax is achieved in 6 to 24 hours in healthy volunteers after a single dose. Average blood concentrations range between 50 to 110 ng/ml/mg/kg. A weekly dose of 250 mg leads to steady-state plasma concentrations of 1000 to 2000 μg/L, after 7 to 10 weeks of administration.
Half Life
The terminal elimination half-life of mefloquine ranges from 0.9 - 13.8 days, according to one pharmacokinetic review. In various studies of healthy adults, the mean elimination half-life of mefloquine varied between 2 and 4 weeks, with a mean half-life of approximately 21 days.
Clearance
The systemic clearance of mefloquine ranges from 0.022 to 0.073 L/h/kg, with an increased clearance during pregnancy. Prescribing information mentions a clearance rate of 30 mL/min.
Elimination Route
Mef-Q Tablet 250 mg is believed to be excreted in the bile and feces. In healthy volunteers who have achieved steady-state concentrations of mefloquine, the unchanged drug was excreted at 9% of the ingested dose, and excretion of its carboxylic metabolite under was measured at 4% of the ingested dose. Concentrations of other metabolites could not be determined.
Pregnancy & Breastfeeding use
Use in Pregnancy: There is no adequate and well-controlled study in pregnant women. However, clinical experience with Mef-Q Tablet 250 mg has not revealed an embrytoxic or teratogenic effect. Mef-Q Tablet 250 mg should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Use in Nursing Mothers: Mef-Q Tablet 250 mg is excreted in breast milk in small amounts. the activity of which is unknown. Because of the potential for serious adverse reactions in nursing infants form Mef-Q Tablet 250 mg. a decision should be made whether to discontinue the drug taking into account the importance of the drug to the mother.
Contraindication
Use of Mef-Q Tablet 250 mg is contraindicated in patients with a known hypersensitivity to Mef-Q Tablet 250 mg or related compounds (e.g. quinine and quinidine). It should not be prescribed for prophylaxis in patients with active depression, a recent history of depression, generalized anxiety disorder, psychosis, or schizophrenia or other major psychiatric disorders, or with a history of convulsions.
Acute Overdose
In cases of overdosage with Mef-Q Tablet 250 mg, the symptoms may be more pronounced. The following procedure is recommended in case of overdosage:
- Induce vomiting or perform gastric lavage, as appropriate.
- Monitor cardiac function (if possible by ECG), neurologic and psychiatric status for at least 24 hours.
- Provide Symptomatic and intensive supportive treatment as required, particularly of cardiovascular disturbance.
- Treat vomiting or diarrhoea with standard fluid therapy.
Storage Condition
Store in a cool dry place. Protect from light.
Innovators Monograph
You find simplified version here Mef-Q Tablet 250 mg
Mef-Q Tablet 250 mg contains Mefloquine see full prescribing information from innovator Mef-Q Tablet 250 mg Monograph, Mef-Q Tablet 250 mg MSDS, Mef-Q Tablet 250 mg FDA label