Roko

Roko® (Roko) is indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. Roko® (Roko hcl) is also indicated for reducing the volume of discharge from ileostomies.

Roko slows the rhythm of digestion so that the small intestines have more time to absorb fluid and nutrients from the foods you eat.

Roko is used to treat diarrhea. Roko is also used to reduce the amount of stool in people who have an ileostomy (re-routing of the bowel through a surgical opening in the stomach).

Roko may also be used for purposes not listed in this medication guide.

(1 capsule = 2 mg)

Patients should receive appropriate fluid and electrolyte replacement as needed.

Acute Diarrhea

Adults: The recommended initial dose is 4mg (two capsules) followed by 2 mg (one capsule) after each unformed stool. Daily dose should not exceed 16mg (eight capsules). Clinical improvement is usually observed within 48 hours.

Children: In children 2 to 5 years of age (20 kg or less), the non-prescription liquid formulation (Roko® (Roko hcl) A-D 1 mg/5 mL) should be used; for ages 6 to 12, either Roko® (Roko hcl) Capsules or Roko® (Roko hcl) A-D Liquid may be used. For children 2 to 12 years of age, the following schedule for capsules or liquid will usually fulfill initial dosage requirements:

Recommended First Day Dosage Schedule

Two to five years: 1 mg t.i.d. (3mg daily dose) (13 to 20 kg) Six to eight years: 2 mg b.i.d. (4mg daily dose) (20 to 30 kg) Eight to twelve years: 2mg t.i.d. (6mg daily dose) (greater than 30 kg)

Recommended Subsequent Daily Dosage

Following the first treatment day, it is recommended that subsequent Roko® (Roko hcl) doses (1 mg/10 kg body weight) be administered only after a loose stool. Total daily dosage should not exceed recommended dosages for the first day.

Chronic Diarrhea

Children: Although Roko® (Roko hcl) has been studied in a limited number of children with chronic diarrhea; the therapeutic dose for the treatment of chronic diarrhea in a pediatric population has not been established.

Adults: The recommended initial dose is 4 mg (two capsules) followed by 2 mg (one capsule) after each unformed stool until diarrhea is controlled, after which the dosage of Roko® (Roko hcl) should be reduced to meet individual requirements. When the optimal daily dosage has been established, this amount may then be administered as a single dose or in divided doses.

The average daily maintenance dosage in clinical trials was 4 to 8 mg (two to four capsules). A dosage of 16 mg (eight capsules) was rarely exceeded. If clinical improvement is not observed after treatment with 16 mg per day for at least 10 days, symptoms are unlikely to be controlled by further administration. Roko® (Roko hcl) administration may be continued if diarrhea cannot be adequately controlled with diet or specific treatment.

Children under 2 Years

The use of Roko (Roko hcl) in children under 2 years is not recommended. There have been rare reports of paralytic ileus associated with abdominal distention. Most of these reports occurred in the setting of acute dysentery, overdose, and with very young children less than two years of age.

Elderly

No formal pharmacokinetic studies were conducted in elderly subjects. However, there were no major differences reported in the drug disposition in elderly patients with diarrhea relative to young patients. No dosage adjustment is required for the elderly.

Renal Impairment

No pharmacokinetic data are available in patients with renal impairment. Since the metabolites and the unchanged drug are mainly excreted in the feces, no dosage adjustment is required for patients with renal impairment.

Hepatic Impairment

Although no pharmacokinetic data are available in patients with hepatic impairment, Roko (Roko hcl) should be used with caution in such patients because of reduced first pass metabolism..

How supplied

Capsules - each capsule contains 2 mg of Roko. The capsules have a light green body and a dark green cap with "JANSSEN" imprinted on one segment and "Roko" on the other segment. Roko® (Roko hcl) capsules are supplied in bottles of 100.

NDC 50458-400-10.........(100 CAPSULES)

Store at 15°-25°C (59°-77°F).

Janssen Pharmaceutica Inc. Revised September 1996, July 1998. FDA Rev date: 10/21/2005

See also:
What is the most important information I should know about Roko?

Roko (Roko hcl) is contraindicated in patients with a known hypersensitivity to Roko or to any of the excipients.

Roko (Roko hcl) is contraindicated in patients with abdominal pain in the absence of diarrhea.

Roko (Roko hcl) is not recommended in infants below 24 months of age.

Roko (Roko hcl) should not be used as the primary therapy:

- in patients with acute dysentery, which is characterized by blood in stools and high fever,

- in patients with acute ulcerative colitis,

- in patients with bacterial enterocolitis caused by invasive organisms including Salmonella, Shigella, and Campylobacter,

- in patients with pseudomembranous colitis associated with the use of broad- spectrum antibiotics.

Use Roko solution as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Roko solution by mouth with or without food.
• Use the measuring cup that comes with Roko solution. Ask your pharmacist for help if you are unsure of how to measure your dose.
• Drinking extra fluids is recommended while you have diarrhea. Check with your doctor if you have questions.
• If you miss a dose of Roko solution, take it as soon as you remember. Continue to take it as directed by your doctor or on the package label.

Ask your health care provider any questions you may have about how to use Roko solution.

This medication is used to treat sudden diarrhea (including traveler's diarrhea). It works by slowing down the movement of the gut. This decreases the number of bowel movements and makes the stool less watery. Roko is also used to reduce the amount of discharge in patients who have had an ileostomy. It is also used to treat ongoing diarrhea in people with inflammatory bowel disease.

Roko treats only the symptoms, not the cause of the diarrhea (e.g., infection). Treatment of other symptoms and the cause of the diarrhea should be determined by your doctor.

Do not use in children younger than 6 years unless directed by your doctor. This medication should not be used in infants younger than 24 months.

How to use Roko (Roko)

If you are using the over-the-counter product to self-treat, read all the directions on the product package before taking this medication. If your doctor has prescribed this medication, follow your doctor's directions and the directions on your prescription label.

Take this medication by mouth, usually after each loose stool or as directed by your doctor. Shake the bottle well before each use. Measure each dose carefully using the attached measuring cup. Do not use a household spoon since you may not get the correct dose.

The dosage is based on your condition and response to treatment. In children, dosage is also based on age and weight. Adults should not use more than 8 milligrams in 24 hours if self-treating, or 16 milligrams in 24 hours if under a doctor's direction.

Improper use of this medication (overuse or abuse) - or use with certain other medications - may cause serious harm, such as fast/irregular heartbeat or death. Do not increase your dose, take it more often, or use it for longer than directed. Be sure to tell your doctor or pharmacist about all the products you use (including prescription, nonprescription, and herbal products).

Diarrhea can cause a serious loss of body water (dehydration). Drink plenty of fluids and minerals (electrolytes) to replace what is lost. Tell your doctor right away if you develop signs of dehydration (e.g., extreme thirst, decreased urination, muscle cramps, weakness, fainting). You may also need to change to a bland diet during this time to reduce irritation to your stomach/intestines. Consult your doctor or pharmacist for more information.

Tell your doctor if your diarrhea does not improve after 2 days, if your condition worsens, or if you develop new symptoms. If you develop blood in the stool, fever, or an uncomfortable fullness/swelling of the stomach/abdomen, or if you think you may have a serious medical problem, seek immediate medical attention.

If you are taking this medication under your doctor's direction for ongoing diarrhea, tell your doctor if your diarrhea continues after 10 days of treatment.

See also:
What other drugs will affect Roko?

Desmopressin: Roko-Roko Oxide may increase the serum concentration of Desmopressin. Monitor therapy

Eluxadoline: Roko-Roko Oxide may enhance the constipating effect of Eluxadoline. Monitor therapy

Erdafitinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of Haloperidol. Monitor therapy

Lasmiditan: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Avoid combination

Lumacaftor and Ivacaftor: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. Lumacaftor and Ivacaftor may increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Monitor therapy

QuiNIDine: May enhance the CNS depressant effect of Roko-Roko Oxide. Roko-Roko Oxide may enhance the QTc-prolonging effect of QuiNIDine. QuiNIDine may increase the serum concentration of Roko-Roko Oxide. Monitor therapy

Ramosetron: Roko-Roko Oxide may enhance the constipating effect of Ramosetron. Monitor therapy

Ranolazine: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Consider therapy modification

See also:
What are the possible side effects of Roko?

Clinical Trial Data

The adverse effects reported during clinical investigations of Roko® (Roko) are difficult to distinguish from symptoms associated with the diarrheal syndrome. Adverse experiences recorded during clinical studies with Roko® (Roko hcl) were generally of a minor and self-limiting nature. They were more commonly observed during the treatment of chronic diarrhea.

The adverse events reported are summarized irrespective of the causality assessment of the investigators.

1) Adverse events from 4 placebo-controlled studies in patients with acute diarrhea The adverse events with an incidence of 1.0% or greater, which were reported at least as often in patients on Roko as on placebo, are presented in the table below.

The adverse events with an incidence of 1.0% or greater, which were more frequently reported in patients on placebo than on Roko, were: dry mouth, flatulence, abdominal cramp and colic.

2) Adverse events from 20 placebo-controlled studies in patients with chronic diarrhea

The adverse events with an incidence of 1.0% or greater, which were reported at least as often in patients on Roko as on placebo, are presented below in the table below.

The adverse events with an incidence of 1.0% or greater, which were more frequently reported in patients on placebo than on Roko were: nausea, vomiting, headache, meteorism, abdominal pain, abdominal cramp and colic.

3) Adverse events from seventy-six controlled and uncontrolled studies in patients with acute or chronic diarrhea

The adverse events with an incidence of 1.0% or greater in patients from all studies are given in the table below.

Post -marketing experience

The following adverse events have been reported:

Skin and subcutaneous tissue disorders

Rash, pruritus, urticaria, angioedema, and extremely rare cases of bullous eruption including erythema multiforme, Stevens-Johnson syndrome and Toxic Epidermal Necrolysis have been reported with use of Roko (Roko hcl).

Immune system disorders

Isolated occurrences of allergic reactions and in some cases severe hypersensitivity reactions including anaphylactic shock and anaphylactoid reactions have been reported with the use of Roko (Roko hcl).

Gastrointestinal disorders

Dry mouth, abdominal pain, distention or discomfort, nausea, vomiting, flatulence, dyspepsia, constipation, paralytic ileus, megacolon, including toxic megacolon.

Renal and urinary disorders

Urinary retention

Nervous system disorders

Drowsiness, dizziness

General disorders and administrative site conditions

Tiredness

A number of the adverse events reported during the clinical investigations and post- marketing experience with Roko are frequent symptoms of the underlying diarrheal syndrome (abdominal pain/discomfort, nausea, vomiting, dry mouth, tiredness, drowsiness, dizziness, constipation, and flatulence). These symptoms are often difficult to distinguish from undesirable drug effects.

Drug Abuse And Dependence

Abuse

A specific clinical study designed to assess the abuse potential of Roko at high doses resulted in a finding of extremely low abuse potential.

Dependence

Studies in morphine-dependent monkeys demonstrated that Roko at doses above those recommended for humans prevented signs of morphine withdrawal. However, in humans, the naloxone challenge pupil test, which when positive indicates opiate-like effects, performed after a single high dose, or after more than two years of therapeutic use of Roko® (Roko), was negative.

Orally administered Roko® (Roko hcl) (Roko formulated with magnesium stearate) is both highly insoluble and penetrates the CNS poorly.

One of the long-acting synthetic antidiarrheals; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally. [PubChem]