33.antiamoebic, antihelmintic, anticancer and antimalarial drugs
Post on 18-Aug-2015
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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
Thank you
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