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- Pharmacology For Artesunate + Sulphadoxine + Pyrimethamine
Artesunate + Sulphadoxine + Pyrimethamine Pharmacology
Artesunate + Sulphadoxine + PyrimethamineAbout Artesunate + Sulphadoxine + PyrimethamineN/AMechanism of Action of Artesunate + Sulphadoxine + PyrimethamineN/APharmacokinets of Artesunate + Sulphadoxine + PyrimethamineN/AOnset of Action for Artesunate + Sulphadoxine + PyrimethamineN/ADuration of Action for Artesunate + Sulphadoxine + PyrimethamineN/AHalf Life of Artesunate + Sulphadoxine + PyrimethamineN/ASide Effects of Artesunate + Sulphadoxine + PyrimethamineN/AContra-indications of Artesunate + Sulphadoxine + PyrimethamineN/ASpecial Precautions while taking Artesunate + Sulphadoxine + PyrimethamineN/APregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Artesunate + Sulphadoxine + PyrimethamineTreatment for all forms of malaria due to Plasmodium falciparum, Plasmodium vivax, Plasmodium ovale and Plasmodium malariae.Interactions for Artesunate + Sulphadoxine + PyrimethamineN/ATypical Dosage for Artesunate + Sulphadoxine + PyrimethamineN/ASchedule of Artesunate + Sulphadoxine + PyrimethamineN/AStorage Requirements for Artesunate + Sulphadoxine + PyrimethamineN/AEffects of Missed Dosage of Artesunate + Sulphadoxine + PyrimethamineN/AEffects of Overdose of Artesunate + Sulphadoxine + PyrimethamineN/A
ArtesunateAbout 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
4. Abdominal pain
11. Macular rash
14. Skin rash
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-
4mg/Kg loading dose on the first day followed by 2mg/Kg once a day for 6 days
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.
2.4mg/Kg followed by 1.2mg/Kg at 12 and 24 hours then 1.2mg/Kg daily for 6 days.
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 treatment
SulphadoxineAbout SulphadoxineAn ultra-long-lasting sulfonamide, Antimalarial with pyrimethamine.Mechanism of Action of SulphadoxineSulphadoxine is a structural analogs and competitive antagonists of para-aminobenzoic acid (PABA). They inhibit normal bacterial utilization of PABA for the synthesis of dihydrofolic acid, a compound that bacteria must be able to make in order to survive for the synthesis of folic acid, an important metabolite in DNA synthesis. It is usually given with Pyrimethamine in the treatment of Chloroquine resistant Plasmodium falciparum in a fixed dose formulation.Pharmacokinets of SulphadoxineAbsorption: Sulfadoxine is readily absorbed from the gastrointestinal tract. Distribution: It is distributed mainly in protein bound form. It is widely distributed to body tissues and fluids and it passes into the fetal circulation. Excretion: It is excreted very slowly in urine mainly in unchanged form.Onset of Action for SulphadoxineN/ADuration of Action for SulphadoxineN/AHalf Life of Sulphadoxine4 to 9 days.Side Effects of Sulphadoxine1. Brownish coloration of urine
2. Skin rashes
5. Localized swelling
6. Reddened eyes
9. Ringing in ears
10. Loss of appetite
11. Irritation of mouth and tongue
13. Abdominal pain
Contra-indications of Sulphadoxine1. Hypersensitivity to the drug or other ingredients it or other sulfonamides
2. Glucose-6-phosphate dehydrogenase (G6PD) deficiency
3. Kidney disease
4. Liver disease
6. Anemia or other blood problems
Special Precautions while taking Sulphadoxine1.Renal impairment
4.Drink lots of high calorie fluids such as cranberry juice and nectars, up to 2 quarts daily, to make sure you have adequate volume of urine to prevent dehydration.Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with caution
Indications for Sulphadoxine1. Malaria along with PyrimethamineInteractions for SulphadoxineN/ATypical Dosage for SulphadoxineAdult: Initially 2 g, followed by 1 to 1.5 g weekly.
Children: 250 mg - 1 g dose is depend on body weight of children.
Schedule of SulphadoxineHStorage Requirements for SulphadoxineStore at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from light.Effects of Missed Dosage of SulphadoxineTake 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 SulphadoxineGive symptomatic and supportive treatment. Induce gastric lavage. Treat with blood products if needed.
PyrimethamineAbout PyrimethamineFolic acid antagonist, Pyrimidine derivative, Antiprotozoal, Antimalarial.Mechanism of Action of PyrimethaminePyrimethamine binds to dihydrofolate reductase enzyme and inhibits the reduction of Dihydrofolic acid (DHFA) to Tetra hydrofolic acid (THFA) .This will interfere the synthesis of folic acid in malarial parasite.
Pharmacokinets of PyrimethamineAbsorption: It is well absorbed after oral administration.Distribution: It is widely distributed in the body in plasma protein bound form.Metabolism: It undergoes metabolism in the liver. Excretion: Excreted mainly through urine and also through breast milk.Onset of Action for Pyrimethamine30 - 60 minuteDuration of Action for Pyrimethamine8 - 10 hoursHalf Life of Pyrimethamine2 - 6 daysSide Effects of Pyrimethamine1.Nausea
Contra-indications of Pyrimethamine1.Hypersensitivity to Pyrimethamine
2.Megaloblastic anaemia caused by folic acid deficiency
Special Precautions while taking Pyrimethamine1. Hepatic dysfunction
2. Renal impairment
4. Patients with G -6-PD deficiency
Pregnancy Related InformationContraindicated.Old Age Related InformationUse with cautionBreast Feeding Related InformationContraindicated.Children Related InformationUse with cautionIndications for Pyrimethamine1. Malaria (treatment and chemoprophylaxis)
Interactions for PyrimethamineAntifolic drugs (e.g: Methotrexate, Sulphonamides TMP-SMZ): Do not use these agents while the patient is receiving sulfadoxine/pyrimethamine.
Typical Dosage for PyrimethamineAdult: Malaria: 50 mg once daily for 2 days followed by 25 mg once in 7 days for 2 - 3 months along with a Sulphonamide
Chemoprophylaxis: 25 mg once weekly for 2 - 3 months
Schedule of PyrimethamineHStorage Requirements for PyrimethamineThe drug should be stored in cool dark place. Protect away from sun light. Keep out of the reach of childrenEffects of Missed Dosage of PyrimethamineTake 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 PyrimethamineGive supportive measures and treatment. Gastric lavage has to be done followed by administration of cathartic. To control seizure Barbiturates can be given to the patient.Leucovorin is given to reduce the hematological side effect.
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