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- Pharmacology For Artesunate + Mefloquine
Artesunate + Mefloquine Pharmacology
Artesunate + Mefloquine
About Artesunate + MefloquineN/AMechanism of Action of Artesunate + MefloquineN/APharmacokinets of Artesunate + MefloquineN/AOnset of Action for Artesunate + MefloquineN/ADuration of Action for Artesunate + MefloquineN/AHalf Life of Artesunate + MefloquineN/ASide Effects of Artesunate + MefloquineN/AContra-indications of Artesunate + MefloquineN/ASpecial Precautions while taking Artesunate + MefloquineN/APregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with caution
NEONATES:ContraindicatedIndications for Artesunate + MefloquineTreatment of uncomplicated P. falciparum malaria.Interactions for Artesunate + MefloquineN/ATypical Dosage for Artesunate + MefloquineN/ASchedule of Artesunate + MefloquineN/AStorage Requirements for Artesunate + MefloquineN/AEffects of Missed Dosage of Artesunate + MefloquineN/AEffects of Overdose of Artesunate + MefloquineN/AArtesunate
About ArtesunateA semi-synthetic derivative of artemisinin, a sesquiterpene lactone potent blood schizonticide, Anti malarial.Mechanism of Action of ArtesunateThis antimalarial drug binds tightly to parasitized erythrocyte membranes. Its endoperoxide bond is responsible for antimalarial activity. Release of an active oxygen species (free radicals) from this bond kills the parasite if accumulated in the erythrocytic cells. It also suppresses the production or activity of antioxidant enzymes in the erythrocytes, causing lysis of the parasitic cell due to the highly reactive free oxygen radicals.Pharmacokinets of ArtesunateAbsorption- Rapidly absorbed after administration
Distribution- Widely distributed in the body. High concentration is seen in liver, kidney and intestine
Metabolism- Metabolized in the liver to its metabolites
Excretion- Excreted through urine and feces
Onset of Action for ArtesunateN/ADuration of Action for ArtesunateN/AHalf Life of ArtesunateN/ASide Effects of Artesunate1. Dizziness
2. Itching
3. Vomiting
4. Abdominal pain
5. Flatulence
6. Headache
7. Bodyache
8. Diarrhoea
9. Tinnitus
10. Alopecia
11. Macular rash
12. Neutropenia
13. Convulsions
14. Skin rash
15. Pruritis
Contra-indications of Artesunate1. Hypersensitivity to the drug or any ingredients of it
2. G6PD deficiency
3. Immunocompromised patients.
Special Precautions while taking ArtesunateParenteral artesunate should be used for the treatment of severe falciparum malaria only where there is evidence that the antimalarial efficacy of quinine is declining.Pregnancy Related InformationContraindicated (1st trimester)Old Age Related InformationMay be used.Breast Feeding Related InformationUse with cautionChildren Related InformationMay be usedIndications for Artesunate1.Uncomplicated falciparum malaria (in areas where there is evidence of chloroquine, pyrimethamine/sulfadoxine, mefloquine and quinine resistance).
2. Severe falciparum malaria (in areas where there is evidence of quinine resistance)
Interactions for ArtesunateNULL
Typical Dosage for ArtesunateAdults-
Oral-
Monotherapy:
4mg/Kg loading dose on the first day followed by 2mg/Kg once a day for 6 days
Combination therapy:
4mg/Kg once a day for 3 days plus mefloqine (15mg or 25mg of base per Kg) as a single dose or split dose on the second and/or third day.
Intramuscular-
2.4mg/Kg followed by 1.2mg/Kg at 12 and 24 hours then 1.2mg/Kg daily for 6 days.
Intravenous-
2.4mg/Kg on the first day followed by 1.2mg/Kg daily
Note: The speed for intravenous injection is 3-4 ml per minute
Schedule of ArtesunateHStorage Requirements for ArtesunateStore in a cool dry dark place.Effects of Missed Dosage of ArtesunateTake the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.Effects of Overdose of ArtesunateGive symptomatic and supportive treatmentMefloquine
About MefloquineA synthetic quinine analogue, Antimalarial.Mechanism of Action of MefloquineThe exact mechanism of action of Mefloquine is not known. Malarial parasites digest their own haemoglobin and release highly toxic heme.This free haeme cause membrane lysis and kill the parasite.
Pharmacokinets of MefloquineAbsorption: It is orally well absorbed after oral administration. Distribution: It is distributed in protein bound form and concentrated in melanin containing cells. Metabolism: some drugs undergo metabolism in the liver. Excretion: It is excreted mainly through urine.Onset of Action for MefloquineA few daysDuration of Action for MefloquineN/AHalf Life of Mefloquine2 - 3 weeksSide Effects of Mefloquine1.Nausea
2.Vomiting
3.Diarrhoea
4.Abdominal cramps
5.Bitter taste
5.Ataxia
6.Dizziness
7.Hallucination
8.Pruritis
Contra-indications of Mefloquine1.Hypersensitivity to Mefloquine
2.Epilepsy
3.Anxiety disorder
4.PsychosisSpecial Precautions while taking Mefloquine1.Hepatic dysfunction
2.Renal impairment
3.Heart failure
4.Do not drive or operate machines during or up to 3 week
5.Epilepsy
6.Psychiatric problems
Pregnancy Related InformationContraindicated.Old Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with caution
NEONATES: contraindicated
Indications for Mefloquine1.Malaria (Treatment and prophylaxis of malarial infections)Interactions for MefloquineBeta adrenergic blockers: Cardiac arrest may occur with concurrent mefloquine.
Chloroquine: Risk of convulsion may be increased.
Quinine or Quinidine: Do not use concurrently with mefloquine.
Valproic acid: Loss of seizure control and lower than expected valproic acid blood levels.
Typical Dosage for MefloquineAdult: Treatment of Malaria: 25 mg base / kg body weight in single or divided dose; Maximum dose: 1.5 g
Prophylaxis: 250 mg of salt /week taken 2 week before entering an endemic area and 4 weeks after leaving.
Children: 10 - 25 mg / kg body weight / week in single dose
Schedule of MefloquineHStorage Requirements for MefloquineThe drug should be stored in cool dark place. Keep out of the reach of children.Effects of Missed Dosage of MefloquineTake the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose.Effects of Overdose of MefloquineGive supportive measures and treatment. Induce emesis or gastric lavage has to be done
Home Delivery for Artesunate + Mefloquine in Your City
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Artesunate + Mefloquine is a generic medicine name and there are several brands available for it. Some of the brands for artesunate + mefloquine might be better known than artesunate + mefloquine itself. If the pharmacy that's willing to deliver medicines to your home doesn't have artesunate + mefloquine in stock, you can ask for one of the branded alternatives for artesunate + mefloquine.