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    MIMS Version 22-23 Important

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    Ftm Ashe Sariol
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    MIMS Version 22-23 Important

    Uploaded by

    Ftm Ashe Sariol
    9 views16 pages
    Version 2

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    Version 2

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    9 views16 pages

    MIMS Version 22-23 Important

    Uploaded by

    Ftm Ashe Sariol
    Version 2

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    of 16

    ANTHELMINTIC

    DRUGS

    Prepared by: Mary Blessa M. Sabate, RPh


    ▪ Nematodes, trematodes, and cestodes are three major groups of
    helminths (worms) that infect humans.

    ▪ Anthelmintic drugs are aimed at metabolic targets that are present in


    the parasite but either are absent from or have different characteristics
    than those of the host.
    ▪ Most anthelmintics target eliminating the organisms from the host, as
    well as controlling spread of infections.
    DRUGS FOR THE TREATMENT OF
    NEMATODES (ROUNDWORMS)

    Nematodes are elongated roundworms that possess a complete digestive system.


    They cause infections of the intestine as well as the blood and tissues.
    1. MEBENDAZOLE
    ▪ A synthetic benzimidazole compound
    ▪ It is a first-line agent for the treatment of infections caused by
    whipworms (Trichuris trichiura), pinworms (Enterobius vermicularis),
    hookworms (Necator americanus and Ancylostoma duodenale) and
    roundworms (Ascaris lumbricoides).
    ▪ MOA: inhibiting the assembly of the microtubules in the parasite and
    also by irreversibly blocking glucose uptake
    ▪ A/E: abdominal pain and diarrhea
    ▪ CI: should be avoided in pregnancy [however, in mass prevention or
    treatment programs, certain agents (ex: mebendazole or albendazole)
    may be used in the second or third trimester.]
    2. PYRANTEL PAMOATE
    ▪ Pyrantel pamoate is also effective in the treatment of infections caused
    by roundworms, pinworms, and hookworms.
    ▪ MOA: It acts as a depolarizing, neuromuscular-blocking agent, causing
    release of acetylcholine and inhibition of cholinesterase, leading to
    paralysis of the worm. The paralyzed worm releases its hold on the
    intestinal tract and is expelled.
    ▪ A/E: nausea, vomiting, and diarrhea.
    Characteristics of and therapy for commonly
    encountered nematode infections.
    3. IVERMECTIN

    ▪ Ivermectin is the drug of choice for the treatment of cutaneous larva migrans,
    strongyloidiasis, and onchocerciasis (river blindness).
    ▪ It is also useful in the treatment of pediculosis (lice) and scabies.]
    ▪ MOA: It targets the glutamate-gated chloride channel receptors. Chloride influx is
    enhanced, and hyperpolarization occurs, resulting in paralysis and death of the worm.
    ▪ The drug is given orally and does not readily cross the blood–brain barrier.
    ▪ CI: Ivermectin should not be used in pregnancy.
    ▪ The killing of the microfilaria in onchocerciasis can result in a dangerous Mazzotti
    reaction (fever, headache, dizziness, somnolence, and hypotension).
    ▪ The severity of this reaction is related to parasite load. Antihistamines or steroids may
    be given to ameliorate the symptoms.
    4. DIETHYLCARBAMAZINE

    ▪ Diethylcarbamazine is the drug of choice for filariasis caused by


    infection with Wuchereria bancrofti and Brugia malayi.
    ▪ It is rapidly absorbed following oral administration with meals and is
    excreted mainly in the urine.
    ▪ A/E: fever, nausea, vomiting, arthralgia & headache
    ▪ [Note: It can accelerate blindness and cause severe Mazzotti reactions
    in patients with onchocerciasis. It should be avoided in patients with this
    disorder.]
    DRUGS FOR THE TREATMENT OF
    TREMATODES (FLUKES)

    The trematodes (flukes) are leaf-shaped flatworms that are generally


    characterized by the tissues they infect (liver, lung, intestinal or blood).
    1. PRAZIQUANTEL
    ▪ Praziquantel is an agent of choice
    for the treatment of all forms of
    schistosomiasis, other trematode
    infections, and cestode infections
    such as taeniasis.
    ▪ It is also used off-label in the
    treatment of cysticercosis
    (caused by Taenia solium larvae).

    ▪ MOA: Permeability of the cell


    membrane to calcium is increased,
    causing contracture and paralysis
    of the parasite.
    ▪ Praziquantel should be taken with food and not chewed due to a bitter taste.
    ▪ It is rapidly absorbed after oral administration and distributes into the cerebrospinal fluid (CSF).
    ▪ A/E: dizziness, malaise, and headache as well as gastrointestinal upset.
    ▪ DRUG INTERACTIONS:
    ✔ Dexamethasone, phenytoin, rifampin, and carbamazepine may increase the metabolism of
    praziquantel.
    ✔ Cimetidine causes increased praziquantel levels.
    ▪ CONTRAINDICATIONS:
    ✔ Contraindicated for the treatment of ocular cysticercosis, because destruction of the organism
    in the eye may cause irreversible damage.
    DRUGS FOR THE TREATMENT OF
    TREMATODES (FLUKES)

    The cestodes, or “true tapeworms,” typically have a flat, segmented body and attach to the host’s
    intestine.
    Like the trematodes, the tapeworms lack a mouth and a digestive tract throughout their life cycle.
    1. NICLOSAMIDE

    ▪ Niclosamide is an alternative to praziquantel for the treatment of


    taeniasis, diphyllobothriasis, and other cestode infections.
    ▪ MOA: It inhibits the mitochondrial phosphorylation of adenosine
    diphosphate (ADP) in the parasite, making it lethal for the cestode’s
    scolex and segments but not for the ova. Anaerobic metabolism may
    also be inhibited.
    ▪ A laxative is administered prior to oral administration to purge the bowel
    of all dead segments and to enhance digestion and liberation of the
    ova.
    ▪ Alcohol should be avoided within 1 day of niclosamide use.
    2. ALBENDAZOLE

    ▪ MOA: inhibits microtubule synthesis and glucose uptake in nematodes


    and is effective against most nematodes known.
    ▪ Its primary therapeutic application, however, is in the treatment of
    cestodal infestations, such as cysticercosis and hydatid disease
    (caused by larval stage of Echinococcus granulosus).
    ▪ Albendazole is also very effective in treating microsporidiosis, a
    fungal infection.
    ▪ Albendazole is erratically absorbed after oral administration, but
    absorption is enhanced by a high-fat meal.
    ▪ The drug distributes widely, including the CSF.
    ▪ When used in short-course therapy (1 to 3 days) for nematodal
    infestations, adverse effects are mild and transient and include
    headache and nausea.
    ▪ Treatment of hydatid disease (3 months) has a risk of hepatotoxicity
    and, rarely, agranulocytosis or pancytopenia.
    ▪ Medical treatment of neurocysticercosis is associated with
    inflammatory responses to dying parasites in the CNS, including
    headache, vomiting, fever, and seizures.

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