ANTIMALARIAL DRUGS

DR. PRAVIN JOSHI

DRAVYA GUNA VIBHAG
G. S GUNE AYURVEDA COLLEGE AHMEDNAGAR
MALARIA
• An infection caused by a plasmodium parasite transmitted by the bite of infected mosquitoes.
• Four species are considered true parasites of humans, as they utilize humans almost exclusively as
a natural intermediate host:
• 1. P. falciparum,
• 2. P. vivax,
• 3. P. ovale
• 4. P. malariae.
• Transmission:Malaria mostly spreads to people through the bites of some infected female
Anopheles mosquitoes. Blood transfusion and contaminated needles may also transmit malaria.
• Symptoms are chills, fever and sweating, usually occurring a few weeks after being bitten.
TYPES OF MALARIA
PLASMODIUM PLASMODIUM VIVAX PLASMODIUM PLASMODIUM
FALCIPARUM MALRIARE OVULAE
Infections caused vivax previously Nephrotic syndrome ovale typically infects
by P. falciparum are considered as a (a chronic, severe young red blood cells,
the most likely to benign infection is kidney disease) can called reticulocytes.
progress to severe, now recognized as a result from chronic Giemsa stain reveals
potentially fatal cause of severe and or repeated infection Schuffner dots under
forms with central fatal malaria. with P. MALARIAE. light microscopy.
nervous system
involvement
LIFE CYCLE OF MALARIA
• HEPATIC STAGE (pre erythocytic ). : 1. Parasite localised in liver. and
• 2. Asymptomatic patient
• ERYTHROCYTIC STAGE: 1.parasite invade RBCs
• 2. patient develop fever cycle
• DEVELOPMENT OF SEXUAL FORMS: 1. occurs in mosquito
LIFE CYCLE OF MALARIA
 ANTIMALARIAL DRUGS

UNCOMPICATE COMPLICATED RADICAL

BASIC 1. ARTEMISININ 1.Primaquine

1. CHLOROQUINE DERIVATIVES
2. MEFLOQUINE 2.proguanil
2. Quinine
3..BULAQUINE
Sulphate +
Antibiotic
CHLOROQUINE
• Chloroquine is an antimalarial drug used to treat susceptible
infections with P. vivax, P. malariae, P. ovale, and P. falciparum.
• PD: Chloroquine inhibits the action of heme polymerase,
which causes the buildup of toxic heme in Plasmodium species.
• Route of administration Oral /IV
• Route of elimination: Chloroquine is predominantly eliminated
in the urine
• SIDE EFFECT: abdominal discomfort, nausea, vomiting, and
diarrhea. (treatment - PAN 40)
• DOSAGE:Adults—At first, 1000 milligrams (mg) once a day. Then,
500 mg 6 to 8 hours after the first dose, and 500 mg on the
second and third days of treatment.
MEFLORQUINE
• Mefloquine, Mefloquine is indicated for the treatment of mild to moderate cases of
malaria caused by Plasmodium falciparum and Plasmodium vivax. It is effective against
chloroquine-resistant forms of Plasmodium falciparum.
• PD: 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.19
Mefloquine is an antimalarial drug acting as a blood schizonticide, preventing and treating
malaria.
• Route of administration: Oral
• Route of elimination :Mefloquine is believed to be excreted in the bile and feces.
• SIDE EFFECT :Stomach upset/pain, loss of appetite, nausea/vomiting, headache,
muscle pain, or diarrhea may occur.
•
MEFLORQUINE
• DOSAGE: ORAL TABLET: 250mg
BULAQUINE
• PD:Bulaquine is a derivative aminoquinoline and has effective activity against the
liver stage of plasmodium falciparum and the dormant bodies of Plasmodium vivax and
Plasmodium ovale, inhibits protein synthesis in protozoa and polymerization of amino
acids by the plasmodia..
• Route of administration: Orals
• Route of elimination: Unknown
• SIDE EFFECTS: No significant side effects. The drug has a good
safety profile
• DOSAGE : The recommended dose is 25mg once daily for 5 days.
BULAQUINE
ARTEMISININ DERIVATIVES
• ARTESUNATE :Artesunate is an artemesinin derivative
indicated for the initial treatment of severe malaria.
• ARTEMETHER:An antimalarial agent used in combination with
lumefantrine for the treatment of acute uncomplicated malaria
caused by Plasmodium falciparum.
• ARTEETHER:ALSO KNOWN AS Artemotil, is a fast acting blood
schizonticide specifically indicated for the treatment of
chloroquine-resistant Plasmodium falciparum malaria and cerebral
malaria cases.
ARTESUNATE
• PD: inhibiting heme polymerization, generating ROS,
destabilizing parasite membrane, alkylating proteins and
inhibiting PfATP6
• ROUTE OF ADMINISTRATION: intravenous route
(IV) or intramuscular route (IM)
• ROUTE OF ELIMINATION Unknown (Mainly urine and
feaces in rats)
• SIDE EFFECTS :Back, leg, or stomach pains · bleeding
gums · bloating · blurred vision · chest tightness · chills ·
constipation
• DOSAGE:The recommended dosage of Artesunate for
Injection is 2.4 mg/kg administered intravenously at 0 hours, 12
hours, and 24 hours, and thereafter administered once daily until
the patient is able to tolerate oral antimalarial therapy.
ARTHEMETHER
• PD: The drug works against the erythrocytic stages of P. falciparum by inhibiting nucleic
acid and protein synthesis. Artemether is administered in combination with lumefantrine
for improved efficacy.
• ROUTE OF ADMINISTRATION:IM (INTRA MUSCULAR), ORAL
• ROUTE OF ELIMINATION: Unknown
• SIDE EFFECTS: Abdominal or stomach pain · chills · cough · fast, irregular, pounding,
or racing heartbeat or pulse · fever · headache · muscle aches · pale skin
• DOSAGE :80 mg in 1 ml ampoule (80 mg/ml), oily solution for IM injection. NEVER
ADMINISTER BY IV ROUTE.When the dose required is less than 1 ml, use a 1 ml syringe
graduated in 0.01 ml.
ARTHEMETHER
• ORAL DOSAGE:Adults and children 2 months of age and older weighing 35
kilograms or more—At first, 4 tablets as a single dose, then one dose (4 tablets) after 8
hours.
ARTEETHER
• PD :In the body, artemether is metabolized into the active metabolite metabolite
dihydroartemisinin. The drug works against the erythrocytic stages of P. falciparum by
inhibiting nucleic acid and protein synthesis.
• Route of administration: intramuscular injection
• Route of elimination: unknown
• SIDE EFFECTS :headache, general weakness, nausea, leg pain, chills, vomiting,
cough, pain at injection site, body ache, abdominal pain, dizziness, rigours and watery
diarrhoea.
• DOSAGE:The recommended dose schedule is 3.2 mg beta-arteether/kg body weight
on day 1, followed by 1.6 mg beta-arteether/kg on days 2 through 5.
ARTEETHER
Quinine sulphate+tetracycline
• PD -Quinine inhibits nucleic acid synthesis, protein synthesis, and glycolysis in
Plasmodium falciparum and can bind with hemazoin in parasitized erythrocytes
• Route of administration -oral (tablet)
• Route of elimination -Liver and urine
• SIDE EFFECTS - Blurred vision; change in color vision; changes in behavior;
confusion; diarrhea ; Anxiety; behavior change, similar to drunkenness .
• DOSAGE -30 mg/kg/day orally divided three times daily for 3-7 days, with
concomitant doxycycline, tetracycline, or clindamycin ·
Quinine sulphate+tetracycline
PRIMAQUINE
• PD: Primaquine acts by interfering with a part of the parasite (mitochondria) that is
responsible for supplying it with energy. Without energy the parasite dies. This stops the
infection from continuing and allows the person to recover.
• Route of administration: ORAL
• Route of elimination: Unknown
• SIDE EFFECTS :Back, leg, or stomach pains · black, tarry stools · bleeding gums ·
bluish-colored lips, fingernails, or palms · chest pain , hemolytic anemia
• DOSAGE :Adults— 15 milligrams (mg) once a day for 14 days.
PRIMAQUINE
PROGUANIL
• PD -exerts its antimalarial action by inhibiting parasitic dihydrofolate reductase enzyme.
It has causal prophylactic and suppressive activity against P. falciparum and cures the
acute infection. It is also effective in suppressing the clinical attacks of vivax malaria
• ROUTE OF ADMINISTRATION : SUSPENSION, TABLET (ORAL)
• ROUTE OF ELIMINATION : Unknown
• SIDE EFFECTS :stomach pain, nausea, vomiting, and headache.
• DOSAGE: Adults—1 gram of atovaquone and 400 mg of proguanil (4 adult strength
tablets) once daily as a single dose taken three days in a row
PROGUANIL
THANK YOU
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