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Q5 LONG ANSWER 10M ★ High-yield

Classify anthelmintic drugs. Describe the antiamoebic drugs and the treatment of visceral leishmaniasis.

Pharmacology · 2nd Professional — Para-Clinical

Anthelmintics — Classification and Mechanisms

DrugMechanismChief uses
Albendazole, mebendazoleBind parasite beta-tubulin and prevent microtubule assembly, blocking glucose uptake; the worm is immobilised and diesAscaris, hookworm, Trichuris, Enterobius; albendazole also for neurocysticercosis and hydatid disease; broad and well tolerated
IvermectinOpens glutamate-gated chloride channels in invertebrate nerve and muscle, causing paralysis; these channels are absent in man, and the drug does not cross the intact blood–brain barrierStrongyloides, onchocerciasis, filariasis, scabies, head lice
Diethylcarbamazine (DEC)Alters microfilarial surface, promoting phagocytosisLymphatic filariasis — the mainstay of India’s elimination programme; causes a mazzotti-like reaction from dying microfilariae
PraziquantelIncreases membrane permeability to calcium, causing sustained contraction and tegument damageAll schistosomes, tapeworms (Taenia, Diphyllobothrium), neurocysticercosis, liver flukes
Pyrantel pamoateDepolarising neuromuscular blocker in the worm — spastic paralysisAscaris, hookworm, Enterobius; must not be combined with piperazine, which acts oppositely
NiclosamideUncouples oxidative phosphorylationTapeworms; not absorbed

CLINICAL PEARL

Killing the worm can be more dangerous than the worm itself. Dying parasites release antigen, producing the mazzotti reaction in onchocerciasis, and in neurocysticercosis the inflammatory response around dying cysts causes cerebral oedema and seizures. That is why corticosteroids and anticonvulsants are given alongside albendazole in neurocysticercosis, and why treatment is avoided in ocular cysticercosis.

Mass Drug Administration and Programmes

  • Soil-transmitted helminths — India’s National Deworming Day gives albendazole to all children twice yearly, improving growth, haemoglobin and school attendance at negligible cost
  • Lymphatic filariasis — annual mass administration of DEC with albendazole, increasingly the triple regimen with ivermectin, has brought India close to elimination
  • Treat the whole household in enterobiasis, and repeat after 2 weeks, since reinfection is the rule
  • Sanitation and footwear matter more than any drug in the long term for soil-transmitted helminths

Antiamoebic and Antiprotozoal Drugs

DrugSite of actionNotes
Metronidazole, tinidazoleTissue amoebicide — acts on trophozoites in the gut wall, liver and other tissuesA prodrug reduced to a cytotoxic intermediate only in anaerobic organisms — the basis of selectivity. Amoebic liver abscess, invasive dysentery, giardiasis, trichomoniasis, and anaerobic bacterial infection. Metallic taste, nausea, peripheral neuropathy with prolonged use, and a disulfiram-like reaction with alcohol
Diloxanide furoate, paromomycinLuminal amoebicide — acts on cysts in the gut lumenMust follow metronidazole in invasive amoebiasis to clear intestinal carriage and prevent relapse; also used alone for asymptomatic cyst passers
NitazoxanideBroad antiprotozoalCryptosporidium, Giardia
Pentamidine, suramin, melarsoprolTrypanosomiasis—
  • Invasive amoebiasis always requires both — a tissue amoebicide to treat the disease and a luminal amoebicide to eradicate the source. Giving metronidazole alone leaves cysts in the gut and relapse follows

Drugs for Visceral Leishmaniasis

  • Kala-azar remains endemic in Bihar, Jharkhand, West Bengal and Uttar Pradesh, and India has committed to its elimination
  • Liposomal amphotericin B — now first-line; a single-dose regimen is effective and is the basis of the elimination programme
  • Miltefosine — the first effective oral agent; causes vomiting and diarrhoea, and is teratogenic with a long half-life, so contraception is required for months afterwards
  • Paromomycin — intramuscular, cheap; used in combination regimens
  • Pentavalent antimonials (sodium stibogluconate) — formerly standard, now abandoned in Bihar because of widespread resistance; cardiotoxic and pancreatotoxic
  • Combination and single-dose regimens reduce cost, duration, resistance and the need for hospital admission — all decisive for a programme in rural India

Common Helminth Infections and Their Treatment

InfectionDrug of choice
Ascariasis, hookworm, trichuriasisSingle-dose albendazole 400 mg
Enterobiasis (pinworm)Albendazole or mebendazole, repeated after 2 weeks, treating the whole household
StrongyloidiasisIvermectin — essential before immunosuppression, since hyperinfection syndrome is often fatal
Lymphatic filariasisDEC with albendazole, increasingly with ivermectin as triple therapy
NeurocysticercosisAlbendazole with corticosteroids and anticonvulsants; imaging first, and ocular lesions excluded
Hydatid diseaseAlbendazole with surgery or pair (puncture, aspiration, injection, reaspiration)
TaeniasisPraziquantel or niclosamide
SchistosomiasisPraziquantel
Scabies and pediculosisTopical permethrin; oral ivermectin for crusted scabies and outbreaks

Applied Aspects

  • Give albendazole with a fatty meal for systemic disease such as neurocysticercosis and hydatid, since absorption is otherwise poor; for intestinal worms absorption does not matter
  • Add corticosteroids before albendazole in neurocysticercosis, and treat seizures; imaging must precede treatment, and ocular lesions must be excluded
  • Warn about alcohol with metronidazole during and for 48 hours after
  • Follow every course of metronidazole for amoebiasis with a luminal amoebicide
  • Ivermectin is contraindicated in heavy Loa loa infection because of fatal encephalopathy, and is avoided in young children and pregnancy
  • Deworming is cheap, safe and one of the highest-value public health measures available in India, with measurable effects on nutrition, anaemia and school performance
  • Screen and treat for Strongyloides before corticosteroids or other immunosuppression in anyone from an endemic area; hyperinfection syndrome carries a very high mortality
  • Praziquantel is given with food and causes transient abdominal pain and dizziness; it must not be used in ocular cysticercosis
  • Treat the household and wash bedding in enterobiasis; treating the index child alone guarantees reinfection
  • Sanitation, safe water and footwear prevent soil-transmitted helminth infection permanently, while deworming only clears the current burden — both are needed, and only one is a drug
  • Amoebic liver abscess rarely needs drainage; metronidazole alone usually suffices, and aspiration is reserved for large left-lobe or impending-rupture lesions
  • Distinguish amoebic from pyogenic liver abscess before treating — serology, the clinical picture and the response to metronidazole all help, and the management differs
  • Mass drug administration works only with high coverage, sustained over several rounds; partial coverage neither interrupts transmission nor justifies the effort
  • Ivermectin has a remarkable safety record and has been given to hundreds of millions in onchocerciasis programmes, which is why its role in filariasis elimination has expanded
  • Anthelmintics are among the safest drugs in the pharmacopoeia, which is what makes mass administration to whole populations of children defensible — the benefit is modest per child but the risk is close to zero
  • Albendazole is avoided in the first trimester but is given in later pregnancy in endemic areas, where hookworm anaemia does more harm than the drug

All questions in Antimicrobials: TB, Fungal, Viral & Antiparasitic

  1. Q1Classify antitubercular drugs. Describe the first-line drugs with their mechanisms and adverse effects, the standard regimens and drug-resistant tuberculosis. ★
  2. Q2Classify antimalarial drugs by stage of action. Describe chloroquine, the artemisinins and the other agents. ★
  3. Q3Classify antifungal drugs. Describe amphotericin B and the azoles with their uses and adverse effects. ★
  4. Q4Describe the antiviral drugs and the principles of antiretroviral therapy. ★
  5. Q5Classify anthelmintic drugs. Describe the antiamoebic drugs and the treatment of visceral leishmaniasis. ★
  6. SN1Describe isoniazid with its mechanism, acetylation polymorphism, adverse effects and uses. ★
  7. SN2Describe rifampicin with its mechanism, uses, adverse effects and interactions. ★
  8. SN3Describe the antileprotic drugs and WHO multidrug therapy. Add a note on lepra reactions. ★
  9. SN4Describe chloroquine with its mechanism, uses, adverse effects and resistance. ★
  10. SN5Explain the rationale for artemisinin-based combination therapy and describe the regimens used in India. ★
  11. SN6Describe amphotericin B with its mechanism, formulations, uses and toxicity. ★
  12. SN7Describe the drugs used in visceral leishmaniasis and the basis of the elimination programme in India.

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