1. Dr . Naveen Avula
Assistant professor
Dept. of pharmacology
GIMSR
2.
3.
4. Chloroquine
Drug of choice for both treatment and chemoprophylaxis
Highly effective blood schizontocide (suppressive)
Not effective against liver forms
Mechanism of action:
Haeme hemozoin
Resistance:
Due to mutations in PfCRT
4
polymerase
6. Adverse effects:
Uncommon-nausea, vomiting, abdominal pain,
blurring of vision, urticaria
Rare: impaired hearing, psychosis, seizures,
agranulocytosis, bleaching of hair.
Long term use-
Irreversible ototoxicity, myopathy, retinopathy,
peripheral neuropathy.
6
7. Contraindications & precautions
Psoriasis and porphyria
Visual field abnormalities
With metoclopramide – extrapyramidal side effects
Safe in pregnancy
7
8. Primaquine
Drug of choice for eradication of hypnozoites
Antimalarial action:
Active against hepatic forms of all parasites
Also gametocidal against all four species
No action on asexual forms of RBC
8
9. Mechanism of action:
Generates toxic reactive species and interferes with electron transport
Therapeutic uses:
Radical cure of vivax & ovale (combined with chloroquine)
Chemoprophylaxis –daily treatment
Gametocidal action-single dose
Pneumocystitis jiroveci – with clindamycin
9
10.
11. Tafenoquine& Bulaquine
It has long plasma t1/2: 16-19days
In phase 3 clinical trials ,1-3 day treatment (along with CQ) has achieved
up to 100% relapse prevention.
Likely to emerge as single dose radical curative.
12. Mefloquine
Potent blood schizontocide, not tissue schizonticide or gametocide
Indications:
Mainly used for chemoprophylaxis-weekly dose
Combined with artesunate for uncomplicated chloroquine resistant
falciparum
12
14. Quinine
Alkaloid from Cinchona bark.
Important drug for cerebral and chloroquine resistant falciparum malaria
Anti malarial action:
Rapid acting blood schizonticidal against all four species
Gametocidal for P.vivax and P.ovale but not P.falciparum
14
15. Adverse effects:
Severe GI irritation
Cinchonism
Hypoglycaemia
toxic amblyopia
Myocardial depression
Idiosyncracy
Black water fever
15
16. Therapeutic uses:
Severe falciparum malaria.
Babesiosis: with clindamycin
Myotonia congenita
Nocturnal leg cramps
16