33.antiamoebic, antihelmintic, anticancer and antimalarial drugs

Anti malarial drugs

1. Antimalarial
drugs

2. Malaria – a protozoal infection - P.vivax, P.ovale
P.falciparum & P.malariae
Antimalarial drugs (examples) –
•Proguanil, Pyrimethamine
•Primaquine
•Chloroquine
•Mefloquine
•Quinine
•Artemisinin derivatives, Atovaquone
•Sulfadoxine, Doxycycline

3. Chloroquine:
MOA –

•Basic drug – taken up by the acidic food vacuoles of
susceptible plasmodia
•‘Drug-heme’ complex – toxic & kills the parasite
Haemoglobin
heme (toxic)
hemozoin (non-toxic
to plasmodium)
heme polymeraseChloroquine

4. Uses:
Malaria
Hepatic amoebiasis
Lepra reaction
Rheumatoid arthritis
Infectious mononucleosis
Discoid lupus erythematosus

5. Adverse effects:
Nausea, vomiting, headache
Skin rashes, itching, visual disturbances
Parenteral administration – hypotension, confusion,
cardiac arrhythmias &
convulsions
Prolonged administration – irreversible
retinopathy
& ototoxicity
Myopathy, cardiomyopathy, neuropathy &
psychiatric
disturbances

6. Anti-amoebic
drugs

7. Amoebiasis – a protozoal infection – Entamoeba
histolytica
Antiamoebic drugs (examples) -
•Nitroimidazoles – Metronidazole, Tinidazole
Secnidazole, Ornidazole
•Emetine , Dehydroemetine
•Chloroquine
•Diloxanide furoate
•Iodoquinol
•Tetracyclines, Paromomycin, Erythromycin

8. Uses of nitroimidazoles:
Amoebiasis
Trichomonas vaginitis
Giardiasis
Anaerobic infections
i. Anaerobic brain abscess
ii. Pseudomembranous colitis
iii. Vincent’s angina
iv. H.pylori infection
Guinea worm infestation

9. Adverse effects :
Gastrointestinal – anorexia, nausea, metallic taste,
epigastric distress, abdominal cramps
Allergic reactions – skin rashes, urticaria, itching &
flushing
CNS – dizziness, vertigo, confusion, irritability,
headache & rarely convulsions
Disulfiram-like reaction if taken with alcohol –
nausea, vomiting, abdominal cramps, headache &
flushing

10. Anthelmintic
drugs

11. Anthelmintics –
Drugs used in the treatment of infections with
helminths in the intestinal tract or tissues of the body
Examples :
•Mebendazole
•Albendazole
•Diethylcarbamazine
citrate (DEC)
•Ivermectin


•Praziquantel
•Pyrantel pamoate
•Piperazine
•Niclosamide

12. Mebendazole
Uses :
 Intestinal nematode infestation - roundworm,
hookworm, whipworm, pinworm & mixed worm
infestation
Adverse effects :
GI side effects
Skin rashes, itching, drug fever

13. Uses :
Intestinal nematode infestation - roundworm,
hookworm, whipworm, pinworm, threadworm &
mixed worm infestation
 Neurocysticercosis
 Hydatid disease
 Filariasis
Albendazole

14. Adverse effects :
GI disturbances
Headache, dizziness, fever & weakness
Loss of hair
Pancytopenia

15. Diethylcarbamazine citrate (DEC)
Uses :
 Filariasis
 Tropical eosinophilia
Adverse effects:
Drug-induced effects – anorexia, nausea, vomiting,
headache & dizziness
Parasite-induced effects – due to release of proteins from
dying parasites
Mazzotti reaction – fever, skin rashes, severe itching, chest
pain, muscle & joint pain, keratitis, lymphadenitis ,
eosinophilia & proteinuria

16. Anticancer
drugs

17. Examples
•Cyclophosphamide
•Cisplatin, carboplatin
•Methotrexate, 6-mercaptopurine
•5-Fluorouracil
•Vinblastine, Vincristine
•Docetaxel, Paclitaxel
•Etoposide, Irinotecan
•Doxorubicin, Bleomycin
•Imatinib

18. Hormones and their antagonists:
Glucocorticoids - prednisolone
Estrogens - ethinyl estradiol
Antiestrogens - tamoxifen
Antiandrogens - flutamide
5α-reductase inhibitors - finasteride
GnRH analogues - nafarelin , abarelix
Progestins - hydroxyprogesterone-caproate

19. 1.Bone marrow suppression:
2. Immunosuppression
3. GIT :
Nausea and vomiting
Diarrhoea, stomatitis, GI bleeding & ulcers
• Leukopenia, agranulocytosis
• Thrombocytopenia, aplastic anemia
General toxicities

20. 4.Skin and hair : alopecia, dermatitis, rashes

5.Gonads
Oligozoospermia – males
Amenorrhea – females
6.Foetus
Abortion and fetal death
7. Hyperuricemia, gout
8. Carcinogenicity

21. Thank you