PHARMACOLOGY SPUP MEDICINE

ANTI-MALARIAL DRUGS
Leon Caculitan, MD April, 2018
EXIMIUS
2021
CHEMOTHERAPY FOR MALARIAMarch 2019
Anti-Protozoal Drugs 3. Gametocides: Drug that kill sexual stages and prevent transmission to
Drug Classification: mosquitoes.
1. Tissue Schizonticides: Drugs that eliminate developing or dormant liver forms. Radical Cure: Elimination of both hepatic and erythrocytic stages.
2. Blood Schizonticides: Drugs that act on erythrocytic parasites. NOTE: No one available agent can reliably affect a radical cure.

DRUG ANTI-MALARIAL ACTION MODE OF ACTION CLINICAL USE ADVERSE EFFECTS OTHERS
CHLOROQUINE Chloroquine is a highly effective After traversing the erythrocytic and At high doses, some toxic effects RESITANCE:
- is a synthetic 4 blood Schizonticide. It's also plasmodial membranes, Chloroquine occur such as gastro-intestinal Chloroquine resistant P.
aminoquinoline formulated as moderately effective is upset, pruritis, falciparum exhibit
the phosphate salt for against gametocytes of P. vivax, concentrated in the organism's headache and blurred vision. multigenic alternations
oral use. P. ovale and P. malariae. acidic food vacuoles. Chloroquine Discoloration of the nail beds and that confer a
Chloroquine is not active against specifically binds to heme released mucous membranes high level of resistance.
PHARMACOKINETICS: liver stage parasites. from the digestion of the host cells' may be seen on chronic When a chloroquine
Chloroquine is a rapidly and hemoglobin, preventing its administration. Rare reactions resistant organism is
completely absorbed polymerization to hemozin (a include hemolysis in G6PD encountered,
following oral administration. pigment). The increased pH and deficient persons, seizures, therapy usually consists of
It concentrates in erythrocytes accumulation of the agranulocytosis and ECG an orally administrated
and some tissues. Thus it has a toxic heme result in oxidative changes. Patients with psoriasis combination of quinine,
very large apparent volume of damage to the membranes, leading or porphyria should not be pyrimethamine and a
distribution. to lysis of both the treated with chloroquine, sulfonamide,such as
The drug also penetrates into parasite and the RBC. because an acute attack may be sulfadoxine
the CNS and traverses the provoked.Chloroquine is
placenta. considered safe in pregnancy.
Chloroquine is dealkylated by
the hepatic mixed function
oxidase system and is
principally excreted in the
urine.

QUININE Quinine is a rapidly acting, highly Quinine and quinidine interfere with 1. Parenteral treatment of 1. Cinchonism: A syndrome
- is derived from the bark of effective blood schizonticide. It's heme polymerization resulting in the severe falciparum malaria. causing nausea, vomiting, tinnitus
the cinchona tree. Quinidine is gametocidal death of Quinine or quinidine is the and vertigo is the
the against P. vivax and P. ovale. It's the erythrocytic form of the treatment of choice for major adverse effect. These
dextrorotatory stereoisomer of NOT effective against liver stage plasmodial parasite. severe falciparum malaria. effects are reversible and are not
quinine. Taken orally, Quinine parasites. 2. Oral treatment of considered to be
is well distributed falciparum malaria. Quinine reasons for suspending therapy.
throughout the body and can is appropriate first line 2. Positive Coombs test for
reach the fetus. therapy hemolytic anemia. Quinine
for uncomplicated treatment should be
falciparum malaria. Quinine suspended.
is commonly used with 3. Hemolysis with G6PD
doxycycline to shorten deficiency.
quinine's duration of use and 4. Potentiation of neuromuscular
limit toxicity. blocking agents and elevation of
digoxin levels

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EXIMIUS
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PRIMAQUINE 1. Eradicates primary - Primaquine is a tissue 1. Drug induced hemolytic Contraindications

- Primaquine is a synthetic 8- exoerythrocytic forms of P. schizonticide. Anemia in patients with 1) Patients should be
aminoquinoline. It's well falciparum and P. vivax. - Metabolites of it are believed to genetically low levels of tested for G6PD
absorbed on oral 2. Eradicates secondary act as oxidants that are glucose 6 phosphate deficiency before
administration and is not exoerythrocytic forms of responsible for the schizonticidal dehydrogenase. primaquine is prescripted.
concentrated in tissues. It's recurring malarias (P. vivax action as well as for the 2. Abdominal discomfort When the patient is
rapidly oxidized to many and hemolysis and especially when administrated in deficient in G6PD,
compounds. 3. P. ovale). Primaquine is the methemoglobinemia combination with treatment strategies may
only agent that can lead to encountered as toxicities. chloroquine. consist of (1)
radical cures of P. vivax and 3. Occasional withholding therapy, (2)
P. ovale malaria, which may methemoglobinemia. treating patients with
remain in the liver after the 4. Rarely granulocytopenia and standard dosing for 14
erythrocytic form of the agranulocytosis days (3)
disease is eliminated. treating with weekly
4. Destroys in the blood the primaquine for 8 weeks.
gametocytic forms of all 4 2) During pregnancy
plasmodia. Inhibitors of Folate
5. It is not effective against the synthesis:
erythrocytic stage of 36.8
malaria.

PYRIMETHAMINE  Against erythrocytic forms of - Pyrimethamine inhibits 1. Fansidar is used to treat

- adequately absorbed, susceptible strains of all 4 plasmodial dihydrofolate chloroquine –resistant
bound to plasma proteins and human malaria species. reductase at much lower falciparum malaria.
has an  It also acts as a strong concentrations than those 2. Fansidar is used as
elimination half-life of about sporontocide in the needed to inhibit the presumptive therapy of
3.5 days. It's extensively mosquito's gut when the mammalian enzyme. falciparum malaria.
metabolized before excretion. mosquito ingests it with the - The inhibition deprives the 3. Pyrimethamine, in
Fansidar is a fixed combination blood of the human host. protozoan of tetrahydrofolate – combination with
of the sulfonamide sulfadoxine  Thus it's a blood a cofactor required in the de sulfadiazine is first line
and pyrimethamine Schizonticide and novo synthesis of purines and therapy for
sporontocide. pyrimidines and in the thetreatment of
interconversion of certain amino toxoplasmosis. If
acids. megaloblastic anemia
occurs with
pyrimethamine
treatment, it may be
reversed with
Leucovorin.

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ANTI-MALARIAL DRUGS
Leon Caculitan, MD April, 2018
EXIMIUS
2021
March 2019
Drugs for treatment of Nematodes: Drugs for the treatment of trematodes:
 Mebendazole  Prazyquantel
 Pyrantel Pamoate
 Thiabendazole Drugs for the treatment of cestodes:
 Ivermectin  Niclosamide
 Diethylcabamazine  Albendazole
Mechanism of Action Pharmacokinetics Clinical use Side effect Contraindications
Diethylcarbamazine treatment of filariasis because of its ability to immobilize
microfilariae.
Pyrantel pamoate - depolarizing neuromuscular poorly absorbed orally & exerts its - effective in the treatment of infections caused by mild & include
blocking agent, causing effects in the intestinal tract roundworms, pinworms &hookworms nausea,
persistent activation of the - paralyzed worm is then expelled from the host’s vomiting &
parasites nicotinic receptors. intestinal tract. diarrhea.
Thiabendazole - targets the parasite’s Cl channel Thiabendazole is effective against: Pregnancy
receptors. (1) strongyloidiasis
- Chloride influx is enhanced & (2) cutaneous Larva migrans
hyperpolarization occurs, (3) trichinosis.
resulting in paralysis
Niclosamide - to inhibition of the parasite’s - A laxative is administered prior to The drug is lethal for the cestode’s scolex & segments of
mitochondrial anaerobic oral administration of niclosamide cestodes, but not for the ova.
phosphorylation of ADP, which to purge the bowel of all the dead 1. Diphyllobothrium latum
produces energy in the form of segments & so preclude digestion 2. T. saginata,
ATP. & liberation of the ova, which may 3. T.solium
lead to cysticercosis 4. H. nana.
Praziquantel - increase the permeability of - rapidly absorbed after oral 1. Schistosomiasis: drug of choice of all forms of include ocular
trematode & cestode cell administration & distributes into schistosomiasis (S. haematobium, S. mansoni & S. drowsiness, cysticercosis.
membrane to calcium, resulting the CSF. japonicum). dizziness & GIT
in paralysis, dislodgement & - High levels occur in the bile. The 2. Other trematodes infections e.g. clonorchiasis. upsets. not
death. drug is extensively metabolized & 3. Taeniasis & diphyllobothriasis: results in high cure rates recommended
excreted through the urine & bile. for T. saginata, T. solium & D. latum. for pregnant
4. Neurocysticercosis: albendazole is now the preferred women or nursing
drug. mothers.
5. Hymenolepis nana: drug of choice for H. nana
infections
Mebendazol - inhibits microtubule synthesis in - Little of an oral dose (that is It is the drug of choice in the treatment of infections by: abdominal pain pregnancy
nematodes thus irreversibly chewed) is absorbed by the 1. Whipworm (Trichuris trichiura). & diarrhea. &children under 2
impairing glucose uptake. body, unless it is taken with a high 2. Pinworm (Enterobius vermicularis). years.
- Affected parasites are expelled fat meal. 3. Hookworm (Ancylostoma duodenale).
with feces - It undergoes 1st pass metabolism 4. Roundworm (Ascaris lumbricoides).
to inactive compounds.
Albendazole - inhibits microtubule synthesis & - It is erratically absorbed after oral 1. Cysticercosis (caused by Taenia Solium larvae). Treatment of The drug
glucose uptake in nematodes. administration & undergoes 2. Hydatid disease ( caused by Echinococcus granulosis) hydatid disease shouldn’t be
extensive 1st pass metabolism, (3 months) has given during
including formation of sulfoxide, a risk of pregnancy or to
which is also active Albendazole hepatotoxicity children under 2
& its metabolites are primarily & rarely, years of age.
excreted in the urine. agranulocytosis
or
pancytopenia.
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ANTI-MALARIAL DRUGS
Leon Caculitan, MD April, 2018
EXIMIUS
2021
March 2019

TRANSCRIBERS Smile 1 of 1
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ANTI-MALARIAL DRUGS
Leon Caculitan, MD April, 2018
EXIMIUS
2021
March 2019

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