Antimalarial drugs

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

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

Uses:

Malaria

Hepatic amoebiasis

Lepra reaction

Rheumatoid arthritis

Infectious mononucleosis

Discoid lupus erythematosus

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

Anti-amoebic drugs

Amoebiasis – a protozoal infection – Entamoeba

histolytica

Antiamoebic drugs (examples) - • Nitroimidazoles – Metronidazole, Tinidazole Secnidazole, Ornidazole• Emetine , Dehydroemetine• Chloroquine• Diloxanide furoate• Iodoquinol• Tetracyclines, Paromomycin, Erythromycin

Uses of nitroimidazoles:AmoebiasisTrichomonas vaginitisGiardiasisAnaerobic infections i. Anaerobic brain abscess ii. Pseudomembranous colitis iii. Vincent’s angina iv. H.pylori infectionGuinea worm infestation

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

Anthelmintic drugs

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

Mebendazole

Uses : Intestinal nematode infestation -

roundworm, hookworm, whipworm, pinworm & mixed

worm infestation

Adverse effects : GI side effects Skin rashes, itching, drug fever

Uses : Intestinal nematode infestation -

roundworm, hookworm, whipworm, pinworm, threadworm & mixed worm infestation

Neurocysticercosis Hydatid disease Filariasis

Albendazole

Adverse effects :

GI disturbances Headache, dizziness, fever &

weakness Loss of hair Pancytopenia

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

Anticancer drugs

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

Hormones and their antagonists: Glucocorticoids - prednisolone

Estrogens - ethinyl estradiol

Antiestrogens - tamoxifen

Antiandrogens - flutamide

5α-reductase inhibitors - finasteride

GnRH analogues - nafarelin , abarelix

Progestins - hydroxyprogesterone-caproate

1.Bone marrow suppression:

2. Immunosuppression

3. GIT :Nausea and vomitingDiarrhoea, stomatitis, GI bleeding &

ulcers

• Leukopenia, agranulocytosis

• Thrombocytopenia, aplastic

anemia

General toxicities

4.Skin and hair : alopecia, dermatitis, rashes 5.GonadsOligozoospermia – malesAmenorrhea – females

6.Foetus Abortion and fetal death

7. Hyperuricemia, gout

8. Carcinogenicity

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