Niclosamide (Oral-Local)


VA CLASSIFICATION
Primary: AP200{02}

Commonly used brand name(s): Niclocide.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).

Not commercially available in Canada.



Category:


Anthelmintic (oral-local)—

Indications

Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.

Accepted

Diphyllobothriasis (treatment)—Niclosamide is indicated in the treatment of diphyllobothriasis caused by Diphyllobothrium latum (broad or fish tapeworm). {02} {03}

Hymenolepiasis (treatment)—Niclosamide is indicated in the treatment of hymenolepiasis caused by Hymenolepis nana (dwarf tapeworm) and [H. diminuta (rat tapeworm)] . {02} {03} {06}

Taeniasis (treatment)—Niclosamide is indicated in the treatment of taeniasis caused by Taenia saginata (beef tapeworm) and [T. solium (pork tapeworm)] . {02} {03}

[Dipylidiasis (treatment)]—Niclosamide is used in the treatment of dipylidiasis caused by Dipylidium caninum (dog and cat tapeworm). {08} {09}

—Although niclosamide is effective in the treatment of cestode infections caused by T. solium , it causes disintegration of the proglottids with release of viable eggs into the intestinal lumen. Since this may theoretically result in cysticercosis, quinacrine, which expels T. solium intact, may be preferred by some medical experts even though it may be less convenient to administer and is more toxic. However, quinacrine commonly causes vomiting, which may predispose to egg activation in the gastrointestinal lumen. {08}

—Niclosamide is effective only in the treatment of intestinal cestodes.

—Not all species or strains of a particular helminth may be susceptible to niclosamide.

Unaccepted
Niclosamide is not effective against cysticercosis.


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    327.12 {04}

Mechanism of action/Effect:

Inhibits oxidative phosphorylation in mitochondria of cestodes; anaerobic metabolism, on which many cestodes are dependent, may also be inhibited; scolex and proximal proglottids are rapidly killed on contact; scolex is loosened from intestinal wall and may be digested. {03}

Absorption:

Not significantly absorbed from the gastrointestinal tract. {07}

Elimination:
    Fecal. {07}


Precautions to Consider

Carcinogenicity

Although carcinogenicity studies have not been done, long-term feeding of the ethanolamine salt of niclosamide to rats and mice has not shown that niclosamide is carcinogenic. {03}

Mutagenicity

Studies have not been done. {03}

Pregnancy/Reproduction
Fertility—
Studies in rats and rabbits given 25 times the human therapeutic dose and studies in mice given 12 times the human therapeutic dose have not shown that niclosamide causes impaired fertility. {01} {03}

Pregnancy—
Adequate and well-controlled studies in humans have not been done.

Studies in rats and rabbits given 25 times the human therapeutic dose and studies in mice given 12 times the human therapeutic dose have not shown that niclosamide causes adverse effects in the fetus. {01} {03}

FDA Pregnancy Category B.

Breast-feeding

It is not known whether niclosamide is distributed into breast milk. However, problems in humans have not been documented.

Pediatrics

Appropriate studies on the relationship of age to the effects of niclosamide have not been performed in children up to 2 years of age. However, no pediatrics-specific problems have been documented to date in children over the age of 2. {03}


Geriatrics


No information is available on the relationship of age to the effects of niclosamide in geriatric patients.

Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problem exists
Hypersensitivity to niclosamide

Patient monitoring
The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; » = major clinical significance):

» Stool examinations    (may be required approximately 1 month and 3 months following treatment with niclosamide to determine efficacy or proof of cure; where expulsion of the tapeworm[s] is uncertain, stool examinations for the presence of ova or segments of the worm[s] may be required periodically; no patient should be considered cured unless stool examinations have been negative for 3 months {03})




Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention only if they continue or are bothersome
Incidence less frequent (1 to 3%) {03} {08}
    
Gastrointestinal disturbances (abdominal or stomach cramps or pain; diarrhea; loss of appetite; nausea or vomiting)

Incidence rare
    
Dizziness or lightheadedness
    
drowsiness
    
itching of the rectal area
    
skin rash
    
unpleasant taste





Overdose
For specific information on the agents used in the management of niclosamide overdose, see:
   • Laxatives (Local) monograph.
For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center (see Poison Control Center Listing ).

Treatment of overdose
Recommended treatment consists of the following: {03}


To decrease absorption:
Administering a fast-acting laxative and enema.

Not inducing vomiting.



Supportive care:
Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation.



Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Niclosamide (Oral).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Hypersensitivity to niclosamide

Proper use of this medication
No special preparations or additional measures (e.g., dietary restrictions or fasting, concurrent medications, purging, or cleansing enemas) required before, during, or immediately after therapy

Taking on an empty stomach or after a light meal (for example, breakfast)

Chewing or crushing tablets; in young children, crushing tablets and mixing with small amount of water to form a paste

» Proper storage

For beef, fish, and dwarf tapeworms
» Compliance with full course of therapy; second course may be required

» Proper dosing
Missed dose: Taking as soon as possible; not taking if almost time for next dose; do not double doses

Precautions while using this medication

For beef, fish, and dwarf tapeworms
Regular visits to physician to check progress

Checking with physician if no improvement within a few days


General Dosing Information
No special preparations or additional measures (e.g., dietary restrictions or fasting, concurrent medications, purging, or cleansing enemas) are required before, during, or immediately after treatment with niclosamide.

Niclosamide should preferably be taken after a light meal (for example, breakfast). However, it may also be taken on an empty stomach (either 1 hour before or 2 hours after a meal).

In Diphyllobothrium latum (broad or fish tapeworm) and Taenia saginata (beef tapeworm) infections in which proglottids and/or ova persist for 7 days after treatment, a second course of niclosamide may be administered.

In Hymenolepis nana (dwarf tapeworm) infections, both mature cestodes and cysticerci (larvae) are found in the intestine. Cysticerci maturing in the intestinal wall are generally resistant to niclosamide. Therefore, therapy should be continued for 7 days to cover adequately all stages of maturation. A second course of niclosamide may be administered 7 to 14 days after initial treatment if necessary.

To prevent the development of cysticercosis in the treatment of T. solium (pork tapeworm) infections, a magnesium sulfate or other saline purge should be administered approximately 1 to 2 hours after niclosamide. This may also aid in the identification of the tapeworm by permitting the expulsion of an intact scolex. {03}


Oral Dosage Forms

Note: Bracketed uses in the Dosage Forms section refer to categories of use and/or indications that are not included in U.S. product labeling.

NICLOSAMIDE CHEWABLE TABLETS

Usual adult and adolescent dose
Diphyllobothrium latum, [Dipylidium caninum], Taenia saginata, and [T. solium] infections
Oral, 2 grams as a single dose. {03} May be repeated in seven days if required.

Hymenolepis nana and [H. diminuta] infections
Oral, 2 grams once a day for seven days. May be repeated in seven to fourteen days in H. nana infections if required.

Note: Some medical experts recommend a dose of 2 grams as a single dose the first day, then 1 gram once a day for the next six days for Hymenolepis nana and [H. diminuta] infections.



Usual pediatric dose
Diphyllobothrium latum, [Dipylidium caninum], Taenia saginata, and [T. solium] infections
Children 11 to 34 kg of body weight: Oral, 1 gram as a single dose. {03} May be repeated in seven days if required.

Children over 34 kg of body weight: Oral, l.5 grams as a single dose. {03} May be repeated in seven days if required.

Hymenolepis nana and [H. diminuta] infections
Children 11 to 34 kg of body weight: Oral, 1 gram as a single dose the first day, then 500 mg once a day for the next six days. {03} May be repeated in seven to fourteen days in H. nana infections if required.

Children over 34 kg of body weight: Oral, l.5 grams as a single dose the first day, then 1 gram once a day for the next six days. {03} May be repeated in seven to fourteen days in H. nana infections if required.


Note: Children under 2 years of age—Dosage has not been established. {03}


Strength(s) usually available
U.S.—
{02}{03}

500 mg (Rx) [Niclocide (sodium saccharin)]

Canada—
Not commercially available. {05}

Packaging and storage:
Store below 30 °C (86 °F), in a well-closed container, unless otherwise specified by manufacturer.

Auxiliary labeling:
   • Chew or crush tablets before swallowing.
   • Continue medication for full time of treatment (dwarf tapeworm infections).



Revised: 06/23/1995



References
  1. Niclocide (Miles). In: PDR Physicians' desk reference. 42nd ed. 1988. Oradell, NJ: Medical Economics Company, 1988: 1460.
  1. Niclocide (Miles). In: PDR Physicians' desk reference. 49th ed. 1995. Montvale, NJ: Medical Economics Data Production Company, 1995: 1683-4.
  1. Niclocide package insert (Miles—US), Rev 8/88, Rec 4/89.
  1. Fleeger CA, editor. USAN 1989. USAN and the USP dictionary of drug names. Rockville, MD: The United States Pharmacopeial Convention, Inc., 1988: 382.
  1. Ching HL. Fish tapeworm infections (diphyllobothriasis) in Canada, particularly British Columbia. Can Med Assoc J 1984 May 1; 130: 125-7.
  1. Gilman AG, Goodman LS, Rall TW, Murad F, editors. Goodman and Gilman's the pharmacological basis of therapeutics. 7th ed. New York: Macmillan, 1985: 104-5.
  1. McEvoy GK, editor. AHFS Drug information 88. Bethesda, MD: American Society of Hospital Pharmacists, 1988: 40-1.
  1. Pearson RD, Hewlett EL. Niclosamide therapy for tapeworm infections. Ann Intern Med 1985 April; 102 (4): 550-1.
  1. Hamrick HJ, Drake Jr R, Jones HM, et al. Two cases of dipylidiasis (dog tapeworm infection) in children: update on an old problem. Pediatrics 1983; 72(1): 114-7.
Hide
(web2)