Iodoquinol (Oral-Local)



INN:

Diiodohydroxyquinoline {13}

BAN:
Diiodohydroxyquinoline {13}

VA CLASSIFICATION
Primary: AP109
{05}
Commonly used brand name(s): Diodoquin; Diquinol; Yodoquinol; Yodoxin.

Other commonly used names are
diiodohydroxyquin and diiodohydroxyquinoline. {13}


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



Category:


Antiprotozoal—

Indications

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

Accepted

Amebiasis, intestinal (treatment)—Iodoquinol is indicated alone as a primary agent in the treatment of intestinal amebiasis in asymptomatic carriers (cyst passers) of Entamoeba histolytica {06} {18}.

[Amebiasis, extraintestinal (treatment)]1—Iodoquinol is used concurrently or sequentially with metronidazole in the treatment of extraintestinal (invasive) amebiasis. {18}

[Balantidiasis (treatment)]1—Iodoquinol is used as a secondary agent in the treatment of balantidiasis caused by Balantidium coli {18}.

—Not all species or strains of a particular organism may be susceptible to iodoquinol.

Unaccepted
Iodoquinol is not effective alone in the treatment of extraintestinal (invasive) amebiasis. {03}

1 Not included in Canadian product labeling.



Pharmacology/Pharmacokinetics

Physicochemical characteristics:

Chemical group—
    Halogenated 8-hydroxyquinoline. {01}
Molecular weight—
    396.95 {11}

Mechanism of action/Effect:

The exact mechanism of action of iodoquinol is unknown. Iodoquinol acts against the trophozoites of Entamoeba histolytica . Iodoquinol produces its amebicidal effect at the site of infection, since it is poorly absorbed from the gastrointestinal tract and can reach high concentrations in the intestinal lumen. {03}

Absorption:

Poorly absorbed after oral administration. {07}

Elimination:
    Fecal; less than 10% of the dose is recovered in the urine, mostly as glucuronides. {07} {15}


Precautions to Consider

Cross-sensitivity and/or related problems

Patients hypersensitive to chloroxine, iodine, pamaquine, pentaquine, primaquine, or other 8-hydroxyquinolines(e.g., clioquinol) may be hypersensitive to this medication also. {08} {16}

Pregnancy/Reproduction

Problems in humans have not been documented.

Breast-feeding

It is not known whether iodoquinol is distributed into breast milk. {06} However, problems in humans have not been documented.

Pediatrics

Children may be more susceptible to the side effects of 8-aminoquinolines, such as optic atrophy, optic neuritis, and peripheral neuropathy, especially with prolonged high-dose therapy. {14} {15}


Geriatrics


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


Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With diagnostic test results
» Thyroid function tests{06}    (iodoquinol may increase protein-bound serum iodine concentrations, reflecting a decrease in 131I uptake; this effect may persist for as long as 6 months after discontinuation of therapy)


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 problems exist
» Hepatic disease{06}{17}    (iodides should be used with caution in patients with hepatic disease)


Hypersensitivity to iodoquinol, chloroxine, iodine, pamaquine, pentaquine, primaquine, or other 8-hydroxyquinolines{06}
Optic neuropathy, pre-existing{06}    (iodoquinol may cause optic neuritis when given in large doses and could worsen pre-existing optic neuropathy)


» Renal disease{14}    (iodides should be used with caution in patients with renal disease)


Thyroid disease{06}    (iodoquinol may interfere with thyroid function tests and may cause goiter)




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
Incidence less frequent {06} {14}
    
Fever or chills
    
hypersensitivity (skin rash, hives, or itching)
    
thyroid gland enlargement (swelling of neck)

With prolonged, high doses of 8-hydroxyquinolines
—children may be more susceptible{07}{14}{15}
    
Optic atrophy (blurred vision or any change in vision)
    
optic neuritis (decreased vision or eye pain )
    
peripheral neuropathy (numbness, tingling, pain, or weakness in hands or feet)
    
subacute myelo-optic neuropathy (blurred vision or any change in vision, clumsiness or unsteadiness, increased weakness, or muscle pain)



Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent {06}
    
Gastrointestinal disturbances (diarrhea; nausea or vomiting; stomach pain)

Incidence less frequent {06}
    
Headache
    
itching of the rectal area





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

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

Before using this medication
»   Conditions affecting use, especially:
Hypersensitivity to iodoquinol, chloroxine, iodine, pamaquine, pentaquine, primaquine, or other 8-hydroxyquinolines





Use in children—Children may be more likely to develop side effects, such as optic atrophy, optic neuritis, and peripheral neuropathy, especially with long-term, high-dose therapy

Other medical problems, especially hepatic or renal disease

Proper use of this medication
» Taking after meals to minimize possible gastrointestinal irritation

Crushing tablets and mixing with applesauce or chocolate syrup if unable to swallow tablets

» Compliance with full course of therapy

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

» Proper storage

Precautions while using this medication
» Caution if blurred vision or loss of vision occurs

» May interfere with thyroid function tests during and for 6 months following therapy


Side/adverse effects
Signs of potential side effects, especially fever or chills, hypersensitivity, thyroid gland enlargement, optic atrophy, optic neuritis, peripheral neuropathy, and subacute myelo-optic neuropathy


General Dosing Information
Iodoquinol should be taken after meals to minimize possible gastrointestinal irritation.

Prolonged high-dosage therapy with 8-hydroxyquinolines may cause optic neuritis, optic atrophy, peripheral neuropathy, or subacute myelo-optic neuropathy, especially in children.

The course of therapy may be repeated after a 2- to 3-week interval, if necessary.


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.

IODOQUINOL TABLETS USP

Usual adult and adolescent dose
Amebiasis, intestinal; or
[Balantidiasis]1
Oral, 630 or 650 mg three times a day for twenty days.
{06}{18}

Usual adult prescribing limits
Up to 2 grams daily. {18}

Usual pediatric dose
Amebiasis, intestinal; or
[Balantidiasis]1


Oral, 10 to 13.3 mg per kg of body weight, or 333.3 mg per square meter of body surface, three times a day for twenty days. Dose should not exceed 1.95 grams in twenty-four hours.
{06}{07}{18}

Strength(s) usually available
U.S.—


210 mg (Rx) [Yodoxin{02}{06}]


650 mg (Rx) [Diquinol{08}{12}] [Yodoquinol{05}{19}] [Yodoxin{02}{06}][Generic]{04}{09}

Canada—


210 mg (Rx) [Diodoquin{07}{10}]


650 mg (Rx) [Diodoquin{07}{10} (scored)]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a well-closed container.

Auxiliary labeling:
   • Continue medication for full time of treatment.
   • Take after meals.



Revised: 03/25/1996



References
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  1. Yodoxin (Glenwood). In: PDR Physicians' desk reference. 49th ed. 1995. Montvale, NJ: Medical Economics Data Production Company, 1995: 1114.
  1. Panel comments on monograph draft of Iodoquinol (Oral-Local), 12/3/86.
  1. Iodoquinol (Generic). In: Red book 1995. Montvale, NJ: Medical Economics Data, 1995: 288.
  1. Yodoquinol (Liquipharm). In: Red book 1995. Montvale, NJ: Medical Economics Data, 1995: 469.
  1. Yodoxin (Glenwood). In: PDR Physicians' desk reference. 43rd ed. 1989. Oradell, NJ: Medical Economics Company, 1989: 1008.
  1. Diodoquin (Searle). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 23rd ed. Ottawa: Canadian Pharmaceutical Association, 1988: 272.
  1. Diquinol(CMC). In: Red book 1989. Montvale, NJ: Medical Economics Company, 1989: 290.
  1. Iodoquinol (Generic). In: Red book 1989. Montvale, NJ: Medical Economics Company, 1989: 404.
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  1. Diquinol (CMC-Cons). In: Red book 1995. Montvale, NJ: Medical Economics Data, 1995: 217.
  1. Fleeger CA, editor. USP dictionary of USAN and international drug names. Rockville, MD: The United States Pharmacopeial Convention, Inc., 1996: 368.
  1. Reynolds JEF, editor. Martindale, the extra pharmacopeia. 29th ed. London: The Pharmaceutical Press, 1989: 662.
  1. AMA Drug evaluations. 6th ed. Chicago: American Medical Association, September 1986: 1579.
  1. Chloroxine (Capitrol, Westwood). In: PDR Physicians' desk reference. 44th ed. 1990. Oradell, NJ: Medical Economics Company, 1990: 2280.
  1. Markell EK, Voge M, John DT. Medical parasitology. 7th ed. Philadelphia: WB Saunders Co., 1992: 38.
  1. Mandell GL, Douglas RG, Bennett JE, editors. Principles and practice of infectious diseases. 3rd ed. New York: Churchill Livingstone, Inc., 1990: 402–3, 406.
  1. Yodoquinol (Liquipharm). In: Red book 1992. Montvale, NJ: Medical Economics Data, 1991: 625.
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