Simplotan

Each vaginal suppository contains tioconazole 100 mg and Simplotan 150 mg. It also contains witepsol as excipient.

Trichomoniasis

Simplotan is indicated for the treatment of trichomoniasis caused by Trichomonas vaginalis. The organism should be identified by appropriate diagnostic procedures. Because trichomoniasis is a sexually transmitted disease with potentially serious sequelae, partners of infected patients should be treated simultaneously in order to prevent re-infection.

Giardiasis

Simplotan is indicated for the treatment of giardiasis caused by Giardia duodenalis (also termed G. lamblia) in both adults and pediatric patients older than three years of age.

Amebiasis

Simplotan is indicated for the treatment of intestinal amebiasis and amebic liver abscess caused by Entamoeba histolytica in both adults and pediatric patients older than three years of age. It is not indicated in the treatment of asymptomatic cyst passage.

Bacterial Vaginosis

Simplotan is indicated for the treatment of bacterial vaginosis (formerly referred to as Haemophilus vaginitis, Gardnerella vaginitis, nonspecific vaginitis, or anaerobic vaginosis) in non-pregnant women.

Other pathogens commonly associated with vulvovaginitis such as Trichomonas vaginalis, Chlamydia trachomatis, Neisseria gonorrhoeae, Candida albicans and Herpes simplex virus should be ruled out.

To reduce the development of drug-resistant bacteria and maintain the effectiveness of Simplotan Tablets and other antibacterial drugs, Simplotan Tablets should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.

Simplotan (Simplotan) is an antibiotic that fights bacteria in the body.

Simplotan is used to treat certain infections caused by bacteria, such as infection of the intestines or vagina. It is also used to treat certain sexually transmitted infections.

Simplotan may also be used for purposes other than those listed in this medication guide.

Usual Adult Dose for Trichomoniasis

2 g orally once with food

The sexual partners should be treated with the same dose at the same time.

Usual Adult Dose for Giardiasis

2 g orally once with food

Usual Adult Dose for Amebiasis

Intestinal: 2 g orally once a day with food for 3 days

Amebic liver abscess: 2 g orally once a day with food for 3 to 5 days

Usual Adult Dose for Bacterial Vaginosis

Nonpregnant, adult women: 2 g orally once a day with food for 2 days or 1 g orally once a day with food for 5 days

Usual Pediatric Dose for Trichomoniasis

2 g orally once with food

The sexual partners should be treated with the same dose at the same time.

Usual Pediatric Dose for Giardiasis

3 years or older: 50 mg/kg (up to 2 g) orally once with food

Usual Pediatric Dose for Amebiasis

3 years or older:

Intestinal: 50 mg/kg (up to 2 g) orally once a day with food for 3 days

Amebic liver abscess: 50 mg/kg (up to 2 g) orally once a day with food for 3 to 5 days

Close monitoring is recommended when treatment durations exceed 3 days.

Renal Dose Adjustments

No adjustment recommended

Liver Dose Adjustments

No data available for dosing adjustments for Simplotan. However, caution should be used in dosing patients with severe hepatic dysfunction due to reduction of metabolic elimination of metronidazole in this patient population.

Dose Adjustments

No adjustment recommended

Precautions

Convulsive seizures and peripheral neuropathy have been reported. The drug should be discontinued if patient experiences abnormal neurological symptoms. Simplotan should be administered cautiously to patients with diseases of the central nervous system.

Simplotan may produce transient leukopenia and neutropenia, However no persistent hematological abnormalities attributable to Simplotan have been observed clinically. If retreatment is necessary, total and differential leukocyte counts are recommended.

Alcoholic beverages should be avoided during and for 3 days after Simplotan therapy.

Animal studies have revealed carcinogenicity with another agent in the nitroimidazole class (metronidazole). Therefore, unnecessary use of Simplotan should be avoided.

Simplotan is contraindicated during the first trimester of pregnancy.

Simplotan is contraindicated in women who are breastfeeding. Interruption of breastfeeding is recommended for the duration of treatment and for 72 hours following the last dose.

To reduce the risk of development of drug resistant organisms, antibiotics should only be used to treat or prevent proven or suspected infections caused by bacteria. Culture and susceptibility information should be considered when selecting treatment or, if no data are available, local epidemiology and susceptibility patterns may be considered when selecting empiric therapy. Patients should be advised to avoid missing doses and to complete the entire course of therapy.

Dialysis

Hemodialysis: On the day of hemodialysis, if Simplotan is administered prior to hemodialysis, an additional dose equivalent to one-half of the original dose should be administered after the end of hemodialysis.

Peritoneal dialysis: Data not available

Other Comments

Bioavailability is not affected by food.

For patients unable to swallow tablets, Simplotan tablets may be crushed in artificial cherry syrup and administered with food. The oral suspension may be prepared as follows:

1. Crush four 500 mg oral tablets to a powder with mortar and pestle.

2. Add about 10 mL cherry syrup to the powder and mix until smooth.

3. Transfer the suspension to a graduated amber container.

4. Use several small rinses of cherry syrup to transfer any remaining drug in the mortar to the final suspension for a total volume of 30 mL.

The oral suspension should be shaken well before each administration. The oral suspension of crushed tablets in artificial cherry syrup is stable for 7 days at room temperature.

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

Hypersensitivity to Simplotan, other 5-nitroimidazole derivatives or to any of the excipients of Simplotan.

As with other drugs of similar structure, Simplotan is also contraindicated in patients having or with a history of blood dyscrasias, although no persistent hematologic abnormalities have been noted in clinical or animal studies.

Use in pregnancy: Simplotan crosses the placental barrier. Since the effects of compounds of this class on fetal development are unknown, the use of Simplotan during the 1st trimester is contraindicated. There is no evidence that Simplotan is harmful during the latter stages of pregnancy, but its use during the 2nd and 3rd trimesters requires that the potential benefits be weighed against possible hazards to the mother or fetus.

Use in lactation: Simplotan is distributed in breast milk. Simplotan may be present in breast milk for >72 hrs after administration. Women should not nurse during and for at least 3 days after having discontinued taking Simplotan.

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

• Take Simplotan by mouth with food.
• If you have trouble swallowing the tablets, check with your doctor or pharmacist.
• If you take cholestyramine, do not take it at the same time you take Simplotan. Talk with your doctor about how you should take cholestyramine with Simplotan.
• If more than one dose of Simplotan is required, continue using Simplotan for the full course of treatment in order to clear up your infection completely, even if you feel better in a few days. Do not miss any doses.
• If you miss a dose of Simplotan, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

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

Use: Labeled Indications

Amebiasis: Treatment of intestinal amebiasis and amebic liver abscess caused by Entamoeba histolytica in adults and pediatric patients older than 3 years.

Limitations of use: Not indicated for the treatment of asymptomatic cyst passage.

Bacterial vaginosis: Treatment of bacterial vaginosis (formerly referred to as Haemophilus vaginitis, Gardnerella vaginitis, nonspecific vaginitis, or anaerobic vaginosis) in adult women.

Giardiasis: Treatment of giardiasis caused by Giardia duodenalis (also termed Giardia lamblia) in adults and pediatric patients older than 3 years.

Trichomoniasis: Treatment of trichomoniasis caused by Trichomonas vaginalis; treat partners of infected patients simultaneously to prevent reinfection.

Off Label Uses

Helicobacter pylori eradication

Based on the American College of Gastroenterology Clinical Guideline for the Treatment of Helicobacter pylori Infection, Simplotan is an effective and recommended component of a multiple-drug regimen for the treatment of this condition.

Prophylaxis against sexually transmitted diseases following sexual assault

Based on the Centers for Disease Control and Prevention (CDC) sexually transmitted diseases treatment guidelines, Simplotan, in combination with ceftriaxone and azithromycin, is a recommended regimen for prophylaxis against sexually transmitted diseases following sexual assault in adolescents and adults.

Urethritis, nongonococcal (persistent and recurrent)

Based on the CDC sexually transmitted diseases treatment guidelines, Simplotan is effective and recommended as treatment for recurrent and persistent urethritis for men who have sex with women and who live in areas where T. vaginalis is prevalent. Compliance with initial regimen and lack of reexposure to an untreated sex partner should be excluded prior to use. Sex partners should be referred for evaluation and appropriate treatment.

See also:
What other drugs will affect Simplotan?

Although not specifically identified in studies with Simplotan, the following drug interactions were reported for metronidazole, a chemically-related nitroimidazole. Therefore, these drug interactions may occur with Simplotan.

Potential Effects Of Simplotan On Other Drugs

Warfarin And Other

Oral Coumarin Anticoagulants

As with metronidazole, Simplotan may enhance the effect of warfarin and other coumarin anticoagulants, resulting in a prolongation of prothrombin time. The dosage of oral anticoagulants may need to be adjusted during Simplotan co-administration and up to 8 days after discontinuation.

Alcohols, Disulfiram

Alcoholic beverages and preparations containing ethanol or propylene glycol should be avoided during Simplotan therapy and for 3 days afterward because abdominal cramps, nausea, vomiting, headaches, and flushing may occur. Psychotic reactions have been reported in alcoholic patients using metronidazole and disulfiram concurrently. Though no similar reactions have been reported with Simplotan, Simplotan should not be given to patients who have taken disulfiram within the last two weeks.

Lithium

Metronidazole has been reported to elevate serum lithium levels. It is not known if Simplotan shares this property with metronidazole, but consideration should be given to measuring serum lithium and creatinine levels after several days of simultaneous lithium and Simplotan treatment to detect potential lithium intoxication.

Phenytoin, Fosphenytoin

Concomitant administration of oral metronidazole and intravenous phenytoin was reported to result in prolongation of the half-life and reduction in the clearance of phenytoin. Metronidazole did not significantly affect the pharmacokinetics of orally-administered phenytoin.

Cyclosporine, Tacrolimus

There are several case reports suggesting that metronidazole has the potential to increase the levels of cyclosporine and tacrolimus. During Simplotan co-administration with either of these drugs, the patient should be monitored for signs of calcineurin-inhibitor associated toxicities.

Fluorouracil

Metronidazole was shown to decrease the clearance of fluorouracil, resulting in an increase in side-effects without an increase in therapeutic benefits. If the concomitant use of Simplotan and fluorouracil cannot be avoided, the patient should be monitored for fluorouracil-associated toxicities.

Potential Effects Of Other Drugs On Simplotan

CYP3A4 Inducers And Inhibitors

Simultaneous administration of Simplotan with drugs that induce liver microsomal enzymes, i.e., CYP3A4 inducers such as phenobarbital, rifampin, phenytoin, and fosphenytoin (a pro-drug of phenytoin), may accelerate the elimination of Simplotan, decreasing the plasma level of Simplotan. Simultaneous administration of drugs that inhibit the activity of liver microsomal enzymes, i.e., CYP3A4 inhibitors such as cimetidine and ketoconazole, may prolong the half-life and decrease the plasma clearance of Simplotan, increasing the plasma concentrations of Simplotan.

Cholestyramine

Cholestyramine was shown to decrease the oral bioavailability of metronidazole by 21%. Thus, it is advisable to separate dosing of cholestyramine and Simplotan to minimize any potential effect on the oral bioavailability of Simplotan.

Oxytetracycline

Oxytetracycline was reported to antagonize the therapeutic effect of metronidazole.

Laboratory Test Interactions

Simplotan, like metronidazole, may interfere with certain types of determinations of serum chemistry values, such as aspartate aminotransferase (AST, SGOT), alanine aminotransferase (ALT, SGPT), lactate dehydrogenase (LDH), triglycerides, and hexokinase glucose. Values of zero may be observed. All of the assays in which interference has been reported involve enzymatic coupling of the assay to oxidation-reduction of nicotinamide adenine dinucleotide (NAD+↔ NADH). Potential interference is due to the similarity of absorbance peaks of NADH and Simplotan.

Simplotan, like metronidazole, may produce transient leukopenia and neutropenia; however, no persistent hematological abnormalities attributable to Simplotan have been observed in clinical studies. Total and differential leukocyte counts are recommended if re-treatment is necessary.

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

Applies to Simplotan: oral tablet

As well as its needed effects, Simplotan (the active ingredient contained in Simplotan) may cause unwanted side effects that require medical attention.

Major Side Effects

If any of the following side effects occur while taking Simplotan, check with your doctor immediately:

Rare

• Change in consciousness
• cough
• difficulty breathing
• loss of consciousness
• noisy breathing
• shortness of breath
• tightness in chest
• wheezing

• Black, tarry stools
• bleeding gums
• blood in urine or stools
• burning, numbness, tingling, or painful sensations
• chest pain
• chills
• difficulty swallowing
• fast, irregular, pounding, or racing heartbeat or pulse
• fever
• hives
• increased transaminase levels
• large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
• lower back or side pain
• nausea
• painful or difficult urination
• pale skin
• pinpoint red spots on skin
• reddening of the skin, especially around ears
• seizures
• sore throat
• sores, ulcers, or white spots on lips or in mouth
• swelling of eyes, face, or inside of nose
• swollen glands
• ulcers
• unsteadiness or awkwardness
• unusual bleeding or bruising
• unusual tiredness or weakness
• weakness in arms, hands, legs, or feet

Minor Side Effects

Some Simplotan side effects may not need any medical attention. As your body gets used to the medicine these side effects may disappear. Your health care professional may be able to help you prevent or reduce these side effects, but do check with them if any of the following side effects continue, or if you are concerned about them:

More common:

• Bitter taste
• metallic taste

• Acid or sour stomach
• belching
• cramps
• difficulty having a bowel movement (stool)
• dizziness
• general feeling of discomfort or illness
• headache
• heartburn
• indigestion
• loss of appetite
• pain or discomfort in chest, upper stomach, or throat
• vomiting
• weight loss

• Body aches or pain
• coating on tongue
• congestion
• depression
• dryness or soreness of throat
• hoarseness
• mood or mental changes
• runny nose
• tender, swollen glands in neck
• voice changes

• Abnormal liver
• darkened urine
• diarrhea
• difficulty in moving
• feeling of constant movement of self or surroundings
• giddiness
• lightheadedness
• muscle pain or stiffness
• pain, swelling, or redness in joints
• sensation of spinning
• shakiness and unsteady walk
• sleepiness
• sleeplessness
• swelling or inflammation of the mouth
• tongue discoloration
• trembling, or other problems with muscle control or coordination
• trouble sleeping
• unable to sleep
• white or brownish vaginal discharge
• white patches in the mouth or throat or on the tongue