ANTIMALARIAL DRUGS

 Anopheles Mosquito

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 ANTIMALARIALS
1. ARTEMISININ and its derivatives
• Artemisinin – Limited to oral use
• Artesunate – oral, IV, IM, rectal
• Artemether – oral, IM, rectal
Combined with drugs such as mefloquine ,
lumefantrine (Coartem), amodiaquine ,
piperaquine (Duo-Cotecxin), and pyronaridine
(Pyramax). =Artemisinin-based Combination
Therapy (ACT)
Mxn: Fast acting blood schizonticide on all species,
kill the parasites-not well known

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 ARTEMISININ……..
Uses: •Standard for RX of uncomplicated P.
falciparum
S/E (fairly well tolerated)
• GIT disturbance (nausea, vomiting,
diarrhea)
• Irreversible neurotoxicity w/ high doses.
• Avoid in pregnancy

NB: WHO discourages monotherapy

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 Artemisia annua plant

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 2. Sulfonamide-pyrimethamine
Pyrimethamine
● Pyrimethamine interferes with tetrahydrofolic
acid synthesis from folic acid - folate needed
to synthesize DNA
Acts slowly against all erythrocytic stage of all
species of plasmodium.
Adm: oral
Elimination: long t1/2 -(allows once a week
dosing)
S/E
GIT irritation
Rashes, itching
Teratogenic in animals (use if benefits
outweigh risk in pregnancy)
Always supplement folic acid if antifolates are
5
used in pregnancy
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 Sulphonamide-pyrimethamine
Uses:
Malaria prophylaxis e.g. pregnancy
Toxoplasmosis - a parasitic disease caused by
the protozoan Toxoplasma gondii(combined
with sulfadiazine or clindamycin and folic acid)
Examples
FANSIDAR = SULPHADOXINE + PYRIMETHAMINE
METAKELFIN = SULPHALENE + PYRIMETHAMINE

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 3. PROGUANIL
●A slowly acting blood schizonticide against
all 4 forms of plasmodium
Adm: oral & adequately absorbed.
Elimination: t1/2 – long (once daily dosing)
S/E
GIT irritation, Skin rash, Mouth ulcers &
Alopecia
Uses:
Prophylaxis of malaria – (alternative to
mefloquine)
Dose: 2 tabs daily.

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 4. QUININE & QUINIDINE
● Quinine is a natural white crystalline alkaloid
having antipyretic (fever-reducing),
antimalarial, analgesic (painkilling), and
anti-inflammatory properties and a bitter taste
Quinidine is an antimalarial schizonticide and
an antiarrhythmic agent ; it is the isomer of
quinine
MOA: not well known, but rapid blood
schizonticide against all 4 species.
Adm: oral, parenteral
Abs: rapid, impaired by Al3+ containing antacids
Distribution: wide & with extensive protein-
binding hence a loading dose is required.
Elimination:
8 Liver
Nursing Pharmacology
metabolism, renal excretion (NB. Monitor
05:13 PM
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19th-century illustration of Cinchona calisaya
 S/E
1.Cinchonism – a combination of –Tinnitus,
visual disturbance, dizziness, headache, nausea
Serious S/E
2. Audio-visual disturbance
3. Hypersensitivity reactions
4. Hypoglycemia (stimulates insulin release, felt
most in pregnancy)
5.GIT irritation
6. Hematological abnormalities – hemolysis,
leukopenia, agranulocytosis, thrombocytopenia
7. Thrombophlebitis at site of infusion
8. Mild uterine contractions (esp. 3rd trimester)
9. Hypotension – with rapid infusion

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 Quinine……
Precautions/ avoid in:
Severe cinchonism (discontinue therapy)
Auditory or visual problems
Presence of myasthenia gravis
Cardiac abnormalities
Patients who have recently received
mefloquine
D/I
Mefloquine (increases quinine toxicity) – do
not co-administer
Quinine raises the plasma conc. of Warfarin
and Digoxin

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 Quinine:
Uses:
1. Severe falciparum malaria (DOC,
parenteral)
2. Babesiosis (Babesia microti) Babesiosis is
a malaria-like parasitic disease caused by
infection with Babesia- DOC in combination
with clindamycin
3. Nocturnal leg cramps
Dose:
P.O= 600mg TDS *1/52
IV infusion: loading with 20mg/kg(max.1.4g)
then 10mg/kg(max.700mg) TDS over 4
hours.
NB: When patient can swallow, switch to oral
12 drug
Nursingto complete 7 days therapy.
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 5. MEFLOQUINE
●Strong blood schizonticide
Adm: oral (produces severe local irritation with
parenteral use)
Absorption: good but slow
Distribution: extensively in tissues
Elimination: t1/2- long
• Some metabolism, Biliary excretion mainly.
S/E
●GIT irritation, Sleep disorders
●Behavioral (Neuropsychiatric) disturbance
●Hepatic damage, arrhytmias
●Leukopenia and thrombocytopenia

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 MEFLOQUINE
C/I – in the presence or History of
1.Cardiac conduction defects
2. Epilepsy
3. Neuropsychiatric disorders
4. Hypersensitivity (to related drugs) e.g.
Quinine, quinidine or halofantrine (do not co-
administer)
Uses:
1.Chemoprophylaxis=1 tab(250mg) weekly.
● NB.co-administer with primaquine for
radical cure of P. vivax & ovale)

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 6. HALOFANTRINE
●Rapid blood schizonticide against all 4 species
Administration: oral
Absorption: variable, enhanced with meals
(especialy fatty foods)- but take on empty
stomach to avoid high plasma conc.
associated with toxicities
S/E
• GIT irritation • Headache, cough
• Pruritus, rash • Mild hepatic damage
• Cardiac conduction defects – arrhythmias,
death
• Embryotoxic in animals

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 HALOFANTRINE……
C/I
Persons with cardiac conduction defects
Persons recently on mefloquine
Pregnancy
Uses:
Treatment of falciparum malaria (NOT for
chemoprophylaxis)
Dose: >40kg= 500mg TDS- QID (max 6 tabs)
<40kg=8mg/kg QID( max 24mg/kg).

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 8. PRIMAQUINE
The only drug against hypnozoites (dormant
state in liver. It is also gametocidal
Adm: oral (NEVER give parenteral –lead to
severe hypotension)
Abs: adequate
S/E
GIT distress - take w/ food
Hemolysis and methemoglobinemia esp in
G6PDH deficiency
Serious S/E
Hematological abnormalities – leucopenia,
agranulocytosis,
Cardiac arrhythmias

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 PRIMAQUINE…..
C/I
Those at risk of granulocytopenia,
methemoglobinemia (Methemoglobin is an
oxidized form of hemoglobin that has a
decreased affinity for oxygen).
In pregnancy
Uses:
Radical cure of P. vivax & ovale infections (add
a schizonticide too)
Terminal prophylaxis (after end of travel) to
eradicate any liver forms
Alternative for mild Pneumocystis jiroveci
infection (along w/ clindamycin)

Dose: 15mg OD (PO) for 2-3 weeks.

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 9. AMODIAQUINE (Camoquin, Flavoquine)
The mode of action of amodiaquine has not
yet been determined.
Adm: oral
S/E
•Agranulocytosis, hepatotoxic, peripheral
neuropathy, visual disturbances.
Aminoquinolines depress cardiac muscle,
impair cardiac conductivity, and produce
vasodilatation with resultant hypotension.
Uses:
•Sensitive strains of malaria
•(don’t use for prophylaxis due to its S/E)
Dose: 600mg (PO) OD X 3/7

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 10. Antibacterials used as antimalarials –
E.g.Tetracycline, doxycycline, clindamycin
Are SLOW schizonticides– hence never use
alone for treatment.
Uses:
Treatment of falciparum malaria in conjunction
with other drugs e.g. quinine
Chemoprophylaxis of malaria (Doxycycline).

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 WHO guidelines
Artemisinin-based combination therapies
(ACTs) are the recommended treatments for
uncomplicated P. falciparum malaria.
Severe malaria is a medical emergency.
For adults, artesunate IV or IM: OR
artemether or quinine is an acceptable
alternative if parenteral artesunate is not
available.
Give parenteral antimalarials in the treatment
of severe malaria for a minimum of 24 h

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 The End….

Thank
you!!
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