This Presentation gives you the pharmacology of different antimalarial drugs and Newer advances such as Vaccine

1. Dr . Naveen Avula
Assistant professor
Dept. of pharmacology
GIMSR

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

5. Therapeutic uses:(RED LIP)
 Malaria
 Rheumatoid arthritis
 Extraintestinal (Hepatic) amoebiasis, Giardiasis
 Discoid lupus Erythematosis
 Lepra reaction
 Infectious mononucleosis
 Photogenic reactions
5

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

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

13. Adverse effects:
 GI intolerance
 Neuropsychiatric disturbances
 Conduction defects – bradycardia
 Teratogenicity
 DDIs: Halofantrine, Quinine, Chloroquine.
13

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

17. Inhibitors of Folate synthesis

18. Antibiotics
 Tetracycline, doxycycline, clindamycin
 Inhibits protein synthesis
 Used only in combinations
 Active against Erythrocytic schizonts
18

19. Artemisinin derivatives
 Qinghaosu (artemisia annua)
Artesunate, artemether, dihydroartemisinin
Antimalarial activity:
 Rapid acting blood schizontocide
 No effect on hepatic stages
19

21. Adverse effects:
 Nausea, vomiting, diarrhoea
 Irreversible neurotoxicity
 Used in pregnancy
21

22. Artemisinin Combination Therapy
 Rapid clinical and parasitological cure.
 High cure rates and low recrudescence rate.
 No parasite resistance.
 Good tolerability profile.

24. Rx of uncomplicated malaria: