Nizoral Topical

Generic Name: ketoconazole topical (kee toe KOE na zole)

Brand Names: Extina, Kuric, Nizoral A-D, Nizoral Topical, Xolegel

What is Nizoral Topical (ketoconazole topical)?

Ketoconazole topical is an antifungal medication. Ketoconazole topical prevents fungus from growing on your skin.

Ketoconazole topical is used to treat fungal infections of the skin such as athlete's foot, jock itch, ringworm, and seborrhea (dry, flaking skin).

Ketoconazole topical is available as a cream, gel, and as a shampoo. The shampoo is used for the treatment of dandruff.

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

What is the most important information I should know about Nizoral Topical (ketoconazole topical)?

Use this medication for the entire length of time prescribed by your doctor. Your symptoms may get better before the infection is completely treated. Do not use bandages or dressings over the treated skin areas, unless your doctor has told you to. Avoid getting this medication in your eyes, nose, or mouth.

Wait at least 20 minutes after applying this medicine before you use cosmetics or sunscreen on the treated skin area. Do not wash the treated skin for at least 3 hours after applying ketoconazole topical.

Call your doctor if your condition does not improve within 2 weeks, or if your symptoms get worse.

Stop using ketoconazole topical and call your doctor if you have severe burning, irritation, redness, pain, or oozing where the medicine is applied. Ketoconazole topical gel is flammable. Do not use it while you are smoking or near an open flame. Do not use this medication on a child younger than 12 years old.

What should I discuss with my healthcare provider berfore using Nizoral Topical (ketoconazole topical)?

Do not use this medication if you are allergic to ketoconazole. FDA pregnancy category C. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether ketoconazole topical passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. Do not use this medication on a child younger than 12 years old.

How should I apply Nizoral Topical (ketoconazole topical)?

Use this medication exactly as it was prescribed for you. Do not use the medication in larger amounts, or use it for longer than recommended by your doctor. Follow the instructions on your prescription label.

Do not use this medication for any skin condition that has not been diagnosed by a doctor.

Wash your hands before and after using this medication.

Clean and dry the affected area. Apply a thin layer of the cream or gel to the affected skin area as directed. This medicine is usually used for only 2 to 4 weeks.

Wait at least 20 minutes after applying this medicine before you use cosmetics or sunscreen on the treated skin area. Do not wash the treated skin for at least 3 hours after applying ketoconazole topical.

Do not use bandages or dressings over the treated skin areas, unless your doctor has told you to.

Use the shampoo twice per week, unless your doctor has told you otherwise. Apply enough shampoo to create a lather and massage the scalp for 1 minute. Rinse thoroughly and repeat, leaving the lather on for an additional 3 minutes. Then rinse it off completely. Allow at least 3 days to pass between uses of ketoconazole shampoo.

Use this medication for the entire length of time prescribed by your doctor. Your symptoms may get better before the infection is completely treated.

Call your doctor if your condition does not improve within 2 weeks, or if your symptoms get worse.

Store ketoconazole topical at room temperature away from moisture and heat. Ketoconazole topical gel is flammable. Do not use it while you are smoking or near an open flame.

What happens if I miss a dose?

Use the medication as soon as you remember. If it is almost time for the next dose, skip the missed dose and use the medicine at the next regularly scheduled time. Do not use extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medicine, or if anyone has accidentally swallowed it.

An overdose of ketoconazole topical applied to the skin is not expected to produce life-threatening symptoms.

What should I avoid while using Nizoral Topical (ketoconazole topical)?

Avoid getting this medication in your eyes, mouth, and nose, or on your lips. If it does get into any of these areas, wash with water.

Avoid covering treated skin areas with tight-fitting, synthetic clothing (such as nylon or polyester) that doesn't allow air to circulate to your skin. If you are treating your feet, wear clean cotton socks and sandals or shoes that allow for air circulation. Keep your feet as dry as possible.

Avoid using other skin or hair products that can cause irritation, such as harsh soaps or shampoos or skin cleansers, hair coloring or permanent chemicals, hair removers or waxes, or skin products with alcohol, spices, astringents, or lime. Do not use other medicated skin products unless your doctor has told you to.

Nizoral Topical (ketoconazole topical) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using ketoconazole topical and call your doctor if you have any of these serious side effects:

• 
  

  severe itching, burning, or irritation where the medicine is applied;

  
  


• 
  

  oily or dry scalp, mild hair loss;

  
  


• 
  

  redness, pain, or oozing of treated skin areas; or

  
  


• 
  

  eye redness, swelling, or irritation.

  
  

Less serious side effects include:

• 
  

  mild skin itching or irritation;

  
  


• 
  

  dry skin; or

  
  


• 
  

  headache.

  
  

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Nizoral Topical (ketoconazole topical)?

There may be other drugs that can affect ketoconazole topical. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

More Nizoral Topical resources

• Nizoral Topical Side Effects (in more detail)
• Nizoral Topical Use in Pregnancy & Breastfeeding
• 2 Reviews for Nizoral Topical - Add your own review/rating

• Extina Consumer Overview


• Extina Topical Advanced Consumer (Micromedex) - Includes Dosage Information


• Extina Foam MedFacts Consumer Leaflet (Wolters Kluwer)


• Extina Prescribing Information (FDA)


• Kuric Cream MedFacts Consumer Leaflet (Wolters Kluwer)


• Nizoral A-D Shampoo MedFacts Consumer Leaflet (Wolters Kluwer)


• Xolegel Prescribing Information (FDA)


• Xolegel Consumer Overview


• Xolegel Gel MedFacts Consumer Leaflet (Wolters Kluwer)

Compare Nizoral Topical with other medications

• Cutaneous Candidiasis
• Dandruff
• Seborrheic Dermatitis
• Tinea Corporis
• Tinea Cruris
• Tinea Pedis
• Tinea Versicolor

Where can I get more information?

• Your pharmacist can provide more information about ketoconazole.

See also: Nizoral Topical side effects (in more detail)

Indocolir

Indocolir may be available in the countries listed below.

Ingredient matches for Indocolir

Indometacin

Indometacin is reported as an ingredient of Indocolir in the following countries:

• Germany


• Turkey

International Drug Name Search

Chloramphenicol Sodium Succinate

Class: Chloramphenicol
VA Class: AM150
CAS Number: 56-75-7
Brands: Chloromycetin Sodium Succinate

• 
  

  Serious and fatal blood dyscrasias (aplastic anemia, hypoplastic anemia, thrombocytopenia, granulocytopenia) can occur after short-term or prolonged therapy.^a Chloramphenicol-associated aplastic anemia (terminating in leukemia) has been reported.^a (See Hematologic Effects under Cautions.)

  
  


• 
  

  Use only when other potentially less hazardous anti-infectives cannot be used or would be ineffective.^a Do not use for trivial infections or when not indicated (e.g., for colds, influenza, throat infections, prophylaxis).^a

  
  


• 
  

  It is essential that adequate blood studies be performed during chloramphenicol treatment.^a While such studies may detect early peripheral blood changes (e.g., leukopenia, reticulocytopenia, granulocytopenia) before they become irreversible, such studies cannot be relied on to detect bone marrow depression prior to development of aplastic anemia.^a

  
  


• 
  

  To facilitate appropriate blood studies and observation, patient should be hospitalized while receiving chloramphenicol.^a

  
  

Introduction

Antibacterial; broad-spectrum antibiotic used only in serious infections caused by susceptible bacteria when less hazardous anti-infectives are ineffective or contraindicated.^{132 a}

Uses for Chloramphenicol Sodium Succinate

Meningitis

Treatment of meningitis caused by susceptible bacteria, including Neisseria meningitidis, Haemophilus influenzae, or Streptococcus pneumoniae.^{106 112 132 144 149 a} Generally used only when penicillins and cephalosporins are contraindicated or ineffective.^{101 102 104 105 106 132 149} A regimen of ampicillin and chloramphenicol may be used as an alternative to cefotaxime or ceftriaxone for treatment of H. influenzae meningitis.¹³²

Do not use for treatment of meningitis caused by penicillin-resistant S. pneumoniae^{132 149} unless the chloramphenicol minimum bactericidal concentration (MBC) is ≤4 mcg/mL.^{132 149}

Do not use for treatment of meningitis caused by Listeria monocytogenes¹⁴⁴ or gram-negative bacilli.¹⁴⁷

Anthrax

Alternative for treatment of anthrax†,^{165 166 170} especially anthrax meningoencephalitis.^{165 166}

Component of multiple-drug parenteral regimens recommended for treatment of inhalational anthrax that occurs as the result of exposure to B. anthracis spores in the context of biologic warfare or bioterrorism.^{164 167} Initiate treatment with IV ciprofloxacin or doxycycline and 1 or 2 other anti-infective agents predicted to be effective (e.g., chloramphenicol, clindamycin, rifampin, vancomycin, clarithromycin, imipenem, penicillin, ampicillin);^{164 167} if meningitis is established or suspected, use IV ciprofloxacin (rather than doxycycline) and chloramphenicol, rifampin, or penicillin.¹⁶⁴

Brucellosis

Treatment of brucellosis†; used with or without streptomycin as an alternative to a tetracycline regimen.¹⁰⁶

Burkholderia Infections

Treatment of infections caused by Burkholderia cepacia† (e.g., in cystic fibrosis patients, immunocompromised patients).¹⁰⁶ Co-trimoxazole considered drug of choice; chloramphenicol, ceftazidime, or imipenem are alternatives.¹⁰⁶

Treatment of glanders† caused by B. mallei; used in conjunction with streptomycin as an alternative to tetracycline and streptomycin.¹⁰⁶

Treatment of melioidosis† caused by B. pseudomallei; used in a multiple-drug regimen with doxycycline and co-trimoxazole.^{106 154} Ceftazidime or imipenem monotherapy may be preferred.^{106 152 153 154 156} B. pseudomallei is difficult to eradicate and relapse of melioidosis is common.^{152 153 154 156}

Chlamydial Infections

Treatment of psittacosis† (ornithosis) caused by Chlamydia psittaci.^{106 132} Alternative to tetracyclines.¹⁰⁶

Clostridium Infections

Alternative to penicillin G or clindamycin for treatment of infections caused by Clostridium perfringens†.^{106 132}

Ehrlichiosis

Treatment of ehrlichiosis† caused by Ehrlichia chaffeensis.^{106 159 160} Recommended as an alternative to tetracyclines,¹⁰⁶ but efficacy has not been established.^{132 159}

Plague

Alternative for treatment of plague† caused by Yersinia pestis, including naturally occurring or endemic plague or pneumonic plague that occurs following exposure to Y. pestisin the context of biologic warfare or bioterrorism.^{106 132 133 168} Regimen of choice is streptomycin (or gentamicin) with or without doxycycline.^{106 132 168 170} Alternatives include doxycycline (or tetracycline), chloramphenicol, co-trimoxazole (may be less effective than other alternatives), or ciprofloxacin (or another fluoroquinolone).^{132 168 170}

Treatment of plague meningitis; drug of choice.^{132 170}

Rat-bite Fever

Alternative to penicillin G for treatment of rat-bite fever† caused by Streptobacillus moniliformis or Spirillum minus.¹³²

Rickettsial Infections

Alternative to tetracyclines for treatment of Rocky Mountain spotted fever and other rickettsial infections.^{102 104 105 106 132 135}

Tularemia

Alternative to streptomycin (or gentamicin) for treatment of tularemia† caused by Francisella tularensis,^{106 132 133 169} including naturally occurring or endemic tularemia or tularemia that occurs following exposure to F. tularensis in the context of biologic warfare or bioterrorism.^{169 170}

Typhoid Fever

Treatment of typhoid fever caused by susceptible Salmonella typhi.^{106 132 134 136 139 140 a} Drugs of choice are third generation cephalosporins (e.g., ceftriaxone, cefotaxime) or fluoroquinolones (e.g., ciprofloxacin, ofloxacin); chloramphenicol is an alternative.^{106 132 139 150 151}

Do not use to treat S. typhi carriers.^{101 104 110 112 a}

Vibrio Infections

Treatment of cholera† caused by Vibrio cholerae.^{106 123 128 129 130} Alternative to tetracyclines;^{123 128 129 130 132} used as an adjunct to fluid and electrolyte replacement in moderate to severe disease.^{106 132}

Chloramphenicol Sodium Succinate Dosage and Administration

General

Because differences between therapeutic and toxic plasma concentrations of chloramphenicol are narrow and because of interindividual differences in metabolism and elimination of the drug, most clinicians recommend that plasma concentrations of chloramphenicol be monitored in all patients.^{101 102 104 105 107 108 109 114 115} Some experts suggest chloramphenicol dosage be adjusted to maintain plasma concentrations at 5–20 mcg/mL.^{101 102 104 105 107 108}

Administration

Chloramphenicol is administered IV.^a Do not administer IM since this route may be ineffective.^a

Administer IV chloramphenicol no longer than necessary; change to an oral regimen of another appropriate anti-infective as soon as practical.^a

Repeated courses of chloramphenicol should be avoided if at all possible.^a

IV Administration

Reconstitution

Reconstitute vial containing 1 g of chloramphenicol by adding 10 mL of an aqueous diluent (e.g., sterile water for injection, 5% dextrose injection) to provide a solution containing 100 mg/mL.^a

Rate of Administration

Inject calculated dose IV over a period of ≥1 minute.^a

Dosage

Available as chloramphenicol sodium succinate; dosage expressed in terms of chloramphenicol.^a

Pediatric Patients

General Dosage for Neonates

IV

25 mg/kg daily given in 4 equally divided doses every 6 hours during the first 2 weeks of life.^{102 112 a} Full-term neonates >2 weeks of age may receive 50 mg/kg daily given in 4 equally divided doses every 6 hours.^a

General Dosage for Children >1 Month of Age

IV

50 mg/kg daily given in equally divided doses every 6 hours.^{102 112 132 a}

Up to 100 mg/kg daily may be required in infections caused by less susceptible organisms or if necessary to achieve adequate CSF concentrations.^{112 132 a} However, because of concern that toxic chloramphenicol concentrations may occur with this high dosage, some clinicians suggest that 75 mg/kg daily be used initially in the treatment of these infections.^{102 105} Dosage should be reduced to 50 mg/kg daily as soon as possible.^{112 a}

General Dosage for Pediatric Patients with Immature Metabolic Processes

IV

25 mg/kg daily will usually produce therapeutic blood concentrations in young infants and other pediatric patients in whom immature metabolic functions are suspected.^a

Monitoring chloramphenicol plasma concentrations is particularly important in these patients.^a

Anthrax†

Treatment of Anthrax (Inhalational, GI, Meningeal, Septicemia)†

IV

50–75 mg/kg daily given in 4 divided doses.¹⁶⁵

Meningoencephalitis caused by B. anthracis may require 1 g every 4 hours.¹⁶⁶

Used in multiple-drug regimens that initially include IV ciprofloxacin or IV doxycycline and 1 or 2 other anti-infectives predicted to be effective.^{164 167}

Duration of treatment is 60 days if anthrax occurred as the result of exposure to anthrax spores in the context of biologic warfare or bioterrorism.^{164 167}

Plague†

IV

25 mg/kg 4 times daily for 10 days for treatment of pneumonic plague† that occurs as the result of exposure to Y. pestis in the context of biologic warfare or bioterrorism.¹⁶⁸

Initial loading dose of 25 mg/kg followed by 15 mg/kg 4 times daily for 10–14 days for treatment of plague meningitis.¹⁷⁰

Tularemia†

IV

15 mg/kg 4 times daily given for 14–21 days for treatment of tularemia† that occurs as the result of exposure to F. tularensis in the context of biologic warfare or bioterrorism.¹⁶⁹

Typhoid Fever

IV

50 mg/kg daily in equally divided doses every 6 hours given for 14–15 days.^{134 139 140}

Adults

General Adult Dosage

IV

50 mg/kg daily given in equally divided doses every 6 hours.^{102 112 a}

In infections caused by less susceptible organisms or if necessary to achieve adequate CSF concentrations, up to 100 mg/kg daily may be required.^{112 c} However, because of concern that toxic plasma chloramphenicol concentrations may occur with this high dosage, some clinicians suggest that 75 mg/kg daily be used initially in the treatment of these infections.^{102 105} Dosage should be reduced to 50 mg/kg daily as soon as possible.^{112 c}

Anthrax†

Treatment of Anthrax (Inhalational, GI, Meningeal, Septicemia)†

IV

50–100 mg/kg daily in 4 divided doses.¹⁶⁵

Meningoencephalitis caused by B. anthracis may require 1 g every 4 hours.¹⁶⁶

Used in multiple-drug regimens that initially include IV ciprofloxacin or IV doxycycline and 1 or 2 other anti-infectives predicted to be effective.^{164 167}

Duration of treatment is 60 days if anthrax occurred as the result of exposure to anthrax spores in the context of biologic warfare or bioterrorism.^{164 167}

Plague†

IV

25 mg/kg 4 times daily given for 10 days for treatment of pneumonic plague† that occurs as the result of exposure to Y. pestis in the context of biologic warfare or bioterrorism.¹⁶⁸

Initial loading dose of 25 mg/kg followed by 15 mg/kg 4 times daily given for 10–14 days for treatment of plague meningitis.¹⁷⁰

Tularemia†

IV

15 mg/kg 4 times daily given for 14–21 days for treatment of tularemia† that occurs as the result of exposure to F. tularensis in the context of biologic warfare or bioterrorism.¹⁶⁹

Typhoid Fever

IV

50 mg/kg daily in equally divided doses every 6 hours given for 14–15 days.^{134 139 140}

Prescribing Limits

Pediatric Patients

Maximum 25 mg/kg daily in 4 divided doses in neonates <2 weeks of age.^a Higher dosage in these neonates should be used only to maintain blood concentrations within a therapeutically effective range.^a

Special Populations

Hepatic Impairment

Reduce dosage in proportion to the degree of impairment.^a Closely monitor plasma chloramphenicol concentrations, especially in pediatric patients.^a

Renal Impairment

Reduce dosage in proportion to the degree of impairment.^a Closely monitor plasma chloramphenicol concentrations, especially in pediatric patients.^a

Cautions for Chloramphenicol Sodium Succinate

Contraindications

• 
  

  Known hypersensitivity to chloramphenicol.^a

  
  


• 
  

  History of previous toxic reaction to chloramphenicol.^a

  
  


• 
  

  Trivial infections or when not indicated (e.g., colds, influenza, throat infections, prophylaxis).^a

  
  

Warnings/Precautions

Warnings

Hematologic Effects

Serious and potentially fatal blood dyscrasias (aplastic anemia, hypoplastic anemia, thrombocytopenia, granulocytopenia) reported with both short-term and prolonged use.^a An irreversible type of bone marrow depression leading to aplastic anemia with a high mortality rate has occurred.^a

Dose-related, reversible bone marrow depression may occur.^a This type of bone marrow depression is characterized by vacuolization of erythroid cells, reduction in reticulocytes and leukopenia, and usually responds promptly to discontinuance of chloramphenicol.^a

Hematologic function should be evaluated prior to and approximately every 2 days during chloramphenicol therapy.^a Consider that such studies do not exclude the possible later appearance of the irreversible type of bone marrow depression.^a

Discontinue chloramphenicol if reticulocytopenia, leukopenia, thrombocytopenia, anemia, or any other blood study findings attributable to the drug occur.^a

Sensitivity Reactions

Hypersensitivity Reactions

Fever, macular and vesicular rash, angioedema, urticaria, and anaphylaxis may occur.^a

General Precautions

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of chloramphenicol and other antibacterials, use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.^a

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing.^a

Chloramphenicol may be initiated pending results of in vitro susceptibility testing, but should be discontinued if the causative organism is found to be susceptible to potentially less hazardous anti-infectives.^a A decision to continue use of chloramphenicol rather than switching to a less hazardous anti-infective should be based on severity of the infection, susceptibility of the causative organism to the other anti-infectives, and efficacy of the various drugs in the specific infection type.^a

Repeated courses of chloramphenicol should be avoided if at all possible.^a Treatment should not be continued longer than required to produce a cure with little or no risk or relapse.^a

Superinfection

Possible emergence and overgrowth of nonsusceptible bacteria or fungi.^a Discontinue drug and institute appropriate therapy if superinfection occurs.^a

CNS Effects

Headache, mild depression, metal confusion, and delirium have been reported.^a

Optic and peripheral neuritis reported, usually following long-term therapy.^a Promptly discontinue chloramphenicol if this occurs.^a

Sodium Content

Contains approximately 52 mg (2.25 mEq) of sodium per g of chloramphenicol sodium succinate.^a

Specific Populations

Pregnancy

Category C.^a

Lactation

Distributed into milk; discontinue nursing or the drug.^a

Pediatric Use

Use with caution in premature and full-term neonates and infants because of potential for gray syndrome toxicity.^a

Gray syndrome can be fatal within a few hours of symptom onset; symptoms include abdominal distension (with or without emesis), progressive pallid cyanosis, and vasomotor collapse (frequently accompanied by irregular respiration).^a Syndrome may be reversible if drug discontinued at early evidence of symptoms.^a

Immature metabolic processes in neonates and infants may result in excessive chloramphenicol concentrations.^a Adjust dosage accordingly and monitor blood concentrations at appropriate intervals.^a

Hepatic Impairment

Excessive chloramphenicol concentration may occur in patients with impaired hepatic function.^a Decrease dosage accordingly.^a Determine chloramphenicol concentrations at appropriate intervals.^a

Renal Impairment

Excessive chloramphenicol concentrations may occur in patients with impaired renal function.^a Decrease dosage accordingly.^a Determine chloramphenicol concentrations at appropriate intervals.^a

Common Adverse Effects

Hematologic effects (blood dyscrasias, bone marrow depression); GI effects (nausea, vomiting, glossitis, stomatitis, diarrhea, enterocolitis).^a

Interactions for Chloramphenicol Sodium Succinate

Specific Drugs

Drug	Interaction	Comments
Antianemia agents	Possible delayed response to iron preparations, vitamin B12, or folic acidc	Concomitant use of iron preparations, vitamin B12, or folic acid should be avoided if possiblec
Anticoagulants, oral	Possible increased anticoagulant effect;c chloramphenicol may impair utilization of prothrombin or decrease vitamin K production by intestinal bacteriac
β-Lactam antibiotics	In vitro evidence of antagonism with penicillins or cephalosporinsc	Concomitant use with penicillins or cephalosporins not recommendedc
Myelosuppressive agents	Potential additive bone marrow depressiona c	Avoid concomitant use with other drugs that may cause bone marrow depressiona c
Phenobarbital	Possible decreased chloramphenicol concentrationsc	Monitor chloramphenicol concentrations in patients receiving concomitant phenobarbitalc
Rifampin	Possible decreased chloramphenicol concentrations103

Chloramphenicol Sodium Succinate Pharmacokinetics

Absorption

Bioavailability

Inactive until chloramphenicol sodium succinate is hydrolyzed in vivo to active chloramphenicol, presumably by esterases in liver, kidneys, and lungs.^{102 107}

Bioavailability following IV administration varies; there is considerable interindividual variation in plasma chloramphenicol concentrations.^{101 102 107 109 114}

Distribution

Extent

Widely distributed into most body tissues and fluids, including saliva, ascitic fluid, pleural fluid, synovial fluid, and aqueous and vitreous humor.^c Highest concentrations attained in liver and kidneys.^c

CSF concentrations may be 21–50% of concurrent plasma concentrations in patients with uninflamed meninges and 45–89% of concurrent plasma concentrations in patients with inflamed meninges.^c

Crosses the placenta and is distributed into milk.^a

Plasma Protein Binding

Approximately 60%.^c

Elimination

Metabolism

Chloramphenicol sodium succinate hydrolyzed to active chloramphenicol, presumably by esterases in liver, kidneys, and lungs.^{102 107} Rate and extent of hydrolysis is highly variable.^{101 102 107 109 114}

Chloramphenicol inactivated principally in the liver by glucuronyl transferase.^c

Elimination Route

Eliminated in urine by glomerular filtration or active tubular secretion.^c Approximately 30% of an IV dose excreted unchanged in urine, but fraction excreted in urine varies considerably and may range from 6–80% in neonates and children.^{102 107 109}

Half-life

Adults with normal renal and hepatic function: plasma half-life 1.5–4.1 hours.^{101 104 107}

Neonates and infants: plasma half-life ≥24 hours in neonates 1–2 days of age and approximately 10 hours in those 10–16 days of age.^c Premature infants and neonates have immature mechanisms for glucuronide conjugation and excretion which results in higher and more prolonged chloramphenicol concentrations.^c

Special Populations

Patients with impaired hepatic function: plasma half-life prolonged.^c

Patients with impaired renal function: plasma half-life not substantially prolonged, but half-lives of the inactive conjugated metabolites may be prolonged.^c

Stability

Storage

Parenteral

Powder for Injection

15–25°C.^a

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility^HID

Compatible
Dextran 40,000
Dextran 6% in dextrose 5%
Dextran 6% in sodium chloride 0.9%
Dextrose–Ringer’s injection combinations
Dextrose–Ringer’s injection, lactated, combinations
Dextrose 5% in Ringer’s injection, lactated
Dextrose–saline combinations
Dextrose 5% in sodium chloride 0.9%
Dextrose 2½, 5, or 10% in water
Fat emulsion 10%, intravenous
Fructose 10% in sodium chloride 0.9%
Fructose 10% in water
Invert sugar 5 and 10% in sodium chloride 0.9%
Invert sugar 5 and 10% in water
Ionosol products
Normosol M in dextrose 5% in water
Normosol R
Ringer’s injection
Ringer's injection, lactated
Sodium chloride 0.45 or 0.9%
Sodium lactate (1/6) M

Drug Compatibility

Admixture CompatibilityHID

Compatible
Amikacin sulfate
Aminophylline
Ascorbic acid injection
Calcium chloride
Calcium gluconate
Colistimethate sodium
Cyanocobalamin
Dimenhydrinate
Dopamine HCl
Ephedrine sulfate
Heparin sodium
Hydrocortisone sodium succinate
Kanamycin
Lidocaine HCl
Magnesium sulfate
Metaraminol bitartrate
Methyldopate HCl
Methylprednisolone sodium succinate
Metronidazole
Metronidazole HCl with sodium bicarbonate
Nafcillin sodium
Oxacillin sodium
Oxytocin
Penicillin G potassium
Penicillin G sodium
Pentobarbial sodium
Phenylephrine HCl
Phenlephrine HCl with sodium bicarbonate
Phytonadione
Plasma protein fraction
Potassium chloride
Promazine HCl
Ranitidine HCl
Sodium bicarbonate
Sodium bicarbonate with phenylephrine HCl
Thiopental sodium
Verapamil HCl
Vitamin B complex with C
Incompatible
Chlorpromazine HCl
Hydroxyzine HCl
Polymyxin B sulfate
Prochlorperazine edisylate
Prochlorperazine mesylate
Promethazine HCl
Vancomycin

Y-Site CompatibilityHID

Compatible
Acyclovir sodium
Cyclophosphamide
Enalaprilat
Esmolol HCl
Foscarnet sodium
Hydromorphone HCl
Labetalol HCl
Magnesium sulfate
Meperidine HCl
Morphine sulfate
Nicardipine HCl
Perphenazine
Tacrolimus
Incompatible
Fluconazole

Actions and SpectrumActions

• 
  

  Usually bacteriostatic in action, but may be bactericidal in high concentrations or against highly susceptible organisms.^c

  
  


• 
  

  Inhibits protein synthesis in susceptible organisms by binding to 50S ribosomal subunits.^c Also inhibits protein synthesis in rapidly proliferating mammalian cells; reversible bone marrow depression reported during chloramphenicol therapy may occur because of inhibition of protein synthesis in mitochondria of bone marrow cells.^c

  
  


• 
  

  Inactive until chloramphenicol sodium succinate is hydrolyzed in vivo to active chloramphenicol.^{102 107}

  
  


• 
  

  Spectrum of activity includes many gram-positive and -negative aerobic bacteria, many anaerobic bacteria, and some other organisms (e.g., Rickettsia, Chlamydia, and Mycoplasma).^c Inactive against fungi and viruses.^c

  
  


• 
  

  Gram-positive aerobes: active against Streptococcus pneumoniae and other streptococci.^{104 110 c} Also active in vitro against Bacillus anthracis.^{161 167}

  
  


• 
  

  Gram-negative aerobes: active against some strains of Brucella, Burkholderia mallei, B. cepacia, Francisella tularensis, Haemophilus influenzae, Neisseria meningitidis, Proteus mirabilis, Salmonella, and Shigella,^{104 110} Vibrio cholerae, and Yersinia pestis,^{171 172}

  
  


• 
  

  Anaerobes: active against Bacteroides fragilis, Clostridium, Fusobacterium, Prevotella melaninogenica, and Veillonella.^{104 110}

  
  


• 
  

  Resistance has been reported in staphylococci, S. pneumoniae,^{126 131} Escherichia coli, H. influenzae,^{104 110 125} Neisseria meningitidis, Salmonella, and Shigella.¹⁴²

  
  

Advice to Patients

• 
  

  Advise patients that antibacterials (including chloramphenicol) should only be used to treat bacterial infections and not used to treat viral infections (e.g., the common cold).^a

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.^a

  
  


• 
  

  Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.^a

  
  


• 
  

  Importance of advising patients of other important precautionary information.^a (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Chloramphenicol Sodium Succinate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	For injection	1 g (of chloramphenicol)*	Chloramphenicol Sodium Succinate Sterile	American Pharmaceutical Partners
			Chloromycetin Sodium Succinate	Monarch

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

100. Freundlich M, Cynamon H, Tamer A et al. Management of chloramphenicol intoxication in infancy by charcoal hemoperfusion. J Pediatr. 1983; 103:485-7. [IDIS 175139] [PubMed 6886919]

101. Bartlett JG. Chloramphenicol. Med Clin North Am. 1982; 66:91-102. [PubMed 7038343]

102. Shalit I, Marks MI. Chloramphenicol in the 1980s. Drugs. 1984; 28:281-91. [IDIS 193569] [PubMed 6386425]

103. Prober CG, Jadavji T, Soldin SJ. Effect of rifampin on chloramphenicol levels. N Engl J Med. 1985; 312:788-9. [IDIS 198165] [PubMed 3974656]

104. Standiford HC. Tetracyclines and chloramphenicol. In: Mandell GL, Douglas RG Jr, Bennett JE, eds. Principles and practice of infectious diseases. 2nd ed. New York; John Wiley & Sons; 1985:206-16.

105. Marks MI, LaFerriere C. Chloramphenicol: recent developments and clinical indications. Clin Pharm. 1982; 1:315-20. [IDIS 154494] [PubMed 6764390]

106. Anon. The choice of antibacterial drugs. Med Lett Drugs Ther. 2001; 43: 69-78.

107. Ambrose PJ. Clinical pharmacokinetics of chloramphenicol and chloramphenicol succinate. Clin Pharmacokinet. 1984; 9:222-38. [IDIS 186221] [PubMed 6375931]

108. Mulhall A, de Louvois J, Hurley R. Chloramphenicol toxicity in neonates: its incidence and prevention. BMJ. 1983; 287:1424-7. [IDIS 178991] [PubMed 6416440]

109. Kauffman RE, Miceli JN, Strebel L et al. Pharmacokinetics of chloramphenicol and chloramphenicol succinate in infants and children. J Pediatr. 1981; 98:315-20. [IDIS 137940] [PubMed 7463235]

110. Kucers A, Bennett NM. The use of antibiotics. 3rd ed. London: William Heineman Medical Books Ltd; 1979:420-56.

112. Parke-Davis. Chloromycetin sodium succinate (sterile chloramphenicol sodium succinate) for intravenous administration prescribing information (dated 1996 Aug). In: Physicians’ desk reference. 52nd ed. Montvale, NJ: Medical Economics Company Inc; 1998:2081-2.

113. Shann F, Linnemann V, Mackenzie A et al. Absorption of chloramphenicol sodium succinate after intramuscular administration in children. N Engl J Med. 1985; 313:410-4. [IDIS 203367] [PubMed 4022068]

114. Sack CM, Koup JR, Smith AL. Chloramphenicol pharmacokinetics in infants and young children. Pediatrics. 1980; 66:579-84. [IDIS 123431] [PubMed 7432844]

115. Nahata MC, Powell DA. Chloramphenicol serum concentration falls during chloramphenicol succinate dosing. Clin Pharmacol Ther. 1983; 33:308-13. [IDIS 168659] [PubMed 6825386]

116. Brown TH, Alford HR. Antagonism by chloramphenicol of broad-spectrum β-lactam antibiotics against Klebsiella pneumoniae. Antimicrob Agents Chemother. 1984; 25:405-7. [IDIS 184272] [PubMed 6375551]

117. Centers for Disease Control. Rocky mountain spotted fever—United States, 1988. MMWR Morb Mortal Wkly Rep. 1989; 38:513-5. [PubMed 2501644]

118. Fishbein DB. Treatment of Rocky Mountain spotted fever. JAMA. 1988; 260:3192.

119. Asmar BI, Prainito M, Dajani AS. Antagonistic effect of chloramphenicol in combination with cefotaxime of ceftriaxone. Antimicrob Agents Chemother. 1988; 32:1375-8. [IDIS 248089] [PubMed 3195999]

120. Dance DA, Wuthiekanun V, Chaowagul W et al. Interactions in vitro between agents used to treat melioidosis. J Antimicrob Chemother. 1989; 24:311-6. [PubMed 2681117]

121. French GL, Ling TKW, Davies DP et al. Antagonism of ceftazidime by chloramphenicol in vitro and in vivo during treatment of gram negative meningitis. BMJ. 1985; 291:636-7. [IDIS 205179] [PubMed 3928061]

122. Cephalosporins interactions: chloramphenicol. In: Hansten PD, Horn JR. Drug interactions: clinical significance of drug-drug interactions. 6th ed. Philadelphia: Lea & Febiger; 1989:213-4.

123. Swerdlow DL, Ries AA. Cholera in the Americas: guidelines for the clinician. JAMA. 1992; 267:1495-9. [PubMed 1371570]

124. Flegg P, Cheong I, Welsby PD. Chloramphenicol: are concerns about aplastic anemia justified? Drug Safety. 1992; 7:167-9.

125. Jorgensen JH. Update on mechanisms and prevalence of antimicrobial resistance in Haemophilus influenzae. Clin Infect Dis. 1992; 14:1119-23. [PubMed 1600014]

126. Friedland IR, Klugman KP. Failure of chloramphenicol therapy in penicillin-resistant pneumococcal meningitis. Lancet. 1992; 339:405-8. [IDIS 291433] [PubMed 1346668]

127. Islam A, Butler T, Nath SK et al. Randomized treatment of patients with typhoid fever by using ceftriaxone or chloramphenicol. J Infect Dis. 1988; 158:742-7. [IDIS 263618] [PubMed 3171225]

128. Saraswathi K, Deodhar LP. A study of V. cholerae strains isolated in Bombay. J Postgrad Med. 1990; 36:128-30. [PubMed 2102910]

129. Willke A, Arman D, Tolunay C. [Susceptibility of Vibrio cholerae El-Tor strains to various antibiotics]. Mikrobiyol Bul. 1988; 22:101-4. [PubMed 3273600]

130. Khan MM, Ara F, Yousuf MO et al. Outbreak of gastroenteritis in different areas of Pakistan. J Pak Med Assoc. 1989; 39:151-4. [PubMed 2504955]

131. Syrogiannopoulos GA, Grivea IN, Beratis NG et al. Resistance patterns of Streptococcus pneumoniae from carriers attendng day-dare centers in Southwestern Greece. Clin Infect Dis. 1997; 25:188-94. [IDIS 392202] [PubMed 9332508]

132. Committee on Infectious Diseases, American Academy of Pediatrics. 2000 Red book: report of the Committee on Infectious Diseases. 25th ed. Elk Grove Village, IL: American Academy of Pediatrics; 2000:192-3,234-6,262-72,396-401,450-60,473-5,489-93,501-6,618-20,656.

133. Centers for Disease Control and Prevention. Human plague—India, 1994. MMWR Morb Mortal Wkly Rep. 1994; 43:689-91. [PubMed 8084331]

134. Islam A, Butler T, Kabir I et al. Treatment of typhoid fever with ceftriaxone for 5 days or chloramphenicol for 14 days: a randomized clinical trial. Antimicrob Agents Chemother. 1993; 37:1572-5. [IDIS 318762] [PubMed 8215265]

135. Walker DH. Rocky mountain spotted fever: a seasonal alert. Clin Infect Dis. 1995; 20:11

Ampicillin Solution

Pronunciation: AM-pi-SIL-in
Generic Name: Ampicillin
Brand Name: Ampicillin

Ampicillin Solution is used for:

Treating and preventing infections caused by certain types of bacteria.

Ampicillin Solution is a penicillin antibiotic. It works by killing sensitive bacteria by interfering with formation of the bacteria's cell wall while it is growing. This weakens the cell wall and it ruptures, resulting in the death of the bacteria.

Do NOT use Ampicillin Solution if:

• you are allergic to any ingredient in Ampicillin Solution or to any other penicillin antibiotic (eg, amoxicillin)


• you are taking a tetracycline antibiotic (eg, doxycycline)


• you have mononucleosis ("mono")


• you have recently received or will be receiving live oral typhoid vaccine

Contact your doctor or health care provider right away if any of these apply to you.

Before using Ampicillin Solution:

Some medical conditions may interact with Ampicillin Solution. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have a stomach infection or diarrhea


• if you have had a severe allergic reaction (eg, severe rash, hives, difficulty breathing, dizziness) to a cephalosporin (eg, cephalexin) or other beta-lactam antibiotic (eg, imipenem)

Some MEDICINES MAY INTERACT with Ampicillin Solution. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Tetracyclines (eg, doxycycline) because they may decrease Ampicillin Solution's effectiveness


• Probenecid because it may increase the risk of Ampicillin Solution's side effects


• Allopurinol because the risk of skin rash may be increased


• Anticoagulants (heparin, warfarin) or methotrexate because the risk of their side effects may be increased by Ampicillin Solution


• Aminoglycosides, birth control pills, or live oral typhoid vaccine because their effectiveness may be decreased by Ampicillin Solution

This may not be a complete list of all interactions that may occur. Ask your health care provider if Ampicillin Solution may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Ampicillin Solution:

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

• Ampicillin Solution is usually given as an injection at your doctor's office, hospital, or clinic. If you will be using Ampicillin Solution at home, a health care provider will teach you how to use it. Be sure you understand how to use Ampicillin Solution. Follow the procedures you are taught when you use a dose. Contact your health care provider if you have any questions.


• Do not use Ampicillin Solution if it contains particles, is cloudy or discolored, or if the vial is cracked or damaged.


• Use Ampicillin Solution on a regular schedule to get the most benefit from it. Using Ampicillin Solution at the same time each day will help you remember to use it.


• If Ampicillin Solution is given intravenously (IV) or intramuscularly (IM), it should be given within 1 hour of mixture. After 1 hour, it begins to lose its potency.


• To clear up your infection completely, use Ampicillin Solution for the full course of treatment. Keep using it even if you feel better in a few days.


• Keep this product, as well as syringes and needles, out of the reach of children and pets. Do not reuse needles, syringes, or other materials. Ask your health care provider how to dispose of these materials after use. Follow all local rules for disposal.


• If you miss a dose of Ampicillin Solution, use 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 use 2 doses at once.

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

Important safety information:

• Ampicillin Solution only works against bacteria; it does not treat viral infections (eg, the common cold).


• Be sure to use Ampicillin Solution for the full course of treatment. If you do not, the medicine may not clear up your infection completely. The bacteria could also become less sensitive to this or other medicines. This could make the infection harder to treat in the future.


• Long-term or repeated use of Ampicillin Solution may cause a second infection. Tell your doctor if signs of a second infection occur. Your medicine may need to be changed to treat this.


• If vomiting or diarrhea occurs, you will need to take care not to become dehydrated. Contact your doctor for instructions.


• Mild diarrhea is common with antibiotic use. However, a more serious form of diarrhea (pseudomembranous colitis) may rarely occur. This may develop while you use the antibiotic or within several months after you stop using it. Contact your doctor right away if stomach pain or cramps, severe diarrhea, or bloody stools occur. Do not treat diarrhea without first checking with your doctor.


• Some injectable penicillins contain sodium. Contact your doctor if you are on a salt-restricted diet or if your condition could be worsened with an increase in salt intake (eg, congestive heart failure).


• Hormonal birth control (eg, birth control pills) may not work as well while you are using Ampicillin Solution. To prevent pregnancy, use an extra form of birth control (eg, condoms).


• Diabetes patients - Ampicillin Solution may cause the results of some tests for urine glucose to be wrong. Ask your doctor before you change your diet or the dose of your diabetes medicine.


• Lab tests, including white blood cell counts and kidney function tests, may be performed while you use Ampicillin Solution. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.


• Use Ampicillin Solution with extreme caution in CHILDREN younger than 10 years old who have diarrhea or an infection of the stomach or bowel.


• PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Ampicillin Solution while you are pregnant. Ampicillin Solution is found in breast milk. If you are or will be breast-feeding while you use Ampicillin Solution, check with your doctor. Discuss any possible risks to your baby.

Possible side effects of Ampicillin Solution:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Black, "hairy" tongue; inflammation and redness of the tongue; mild diarrhea; nausea; second infection; vomiting.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); bloody stools; chills; fever; itching; muscle pain; pain, redness, or swelling at the injection site; severe diarrhea; stomach pain/cramps; vaginal irritation or discharge.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Ampicillin side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include diarrhea; nausea; seizures; vomiting.

Proper storage of Ampicillin Solution:

Ampicillin Solution is usually handled and stored by a health care provider. If you are using Ampicillin Solution at home, store Ampicillin Solution as directed by your pharmacist or health care provider. Keep Ampicillin Solution out of the reach of children and away from pets.

General information:

• If you have any questions about Ampicillin Solution, please talk with your doctor, pharmacist, or other health care provider.


• Ampicillin Solution is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Ampicillin Solution. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Ampicillin resources

• Ampicillin Side Effects (in more detail)
• Ampicillin Use in Pregnancy & Breastfeeding
• Drug Images
• Ampicillin Drug Interactions
• Ampicillin Support Group
• 3 Reviews for Ampicillin - Add your own review/rating

Compare Ampicillin with other medications

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Drug List:

Utira-C Tablets

Dosage Form: tablet, sugar coated
Utira-C Tablets

Utira-C Tablets Description

Each tablet for oral administration contains:

Hyoscyamine Sulfate……...12 mg

Methenamine.....81.6 mg

Phenyl Salicylate.....36.2 mg

Sodium Phosphate Monobasic…..40.8 mg

Methylene Blue.....10.8 mg

Other Ingredients: Calcium Sulfate, Carnauba Wax, D & C Red #27  lake, Dicalcium Phosphate, FD&C Blue #1 Lake, Gelatin, Hypromellose, Kaolin, Magnesium Silicate, Magnesium Stearate, Microcrystalline Cellulose, Mineral Oil, Pharmaceutical Glaze, Polyethylene Glycol, Polyvinylpyrrolidone, Sugar and Titanium Dioxide.

Hyoscyamine Sulfate. [101- 31-5] [3(s)-endo)-α(Hydroxymethyl benzeneacetlc acid 8- methyl-8-azabicyclo [3.2.1] oct- 3-yl ester; 1αH,5 αH-tropan-3 α-ol(-)-tropate (ester);3 α-tropanyIS-(-)-tropate; I-tropic acid ester with tropine; 1- tropine tropate. Hyoscyamine Sulfate is an alkaloid of belladonna. Exists as a white crystalline powder. Its solutions are alkaline to litmus. Affected by light, it is slightly soluble in water; freely soluble in alcohol; sparingly soluble in ether.

C17H23N03 • H2S04 • 2H20

MW = 712.85

Methenamine. [100-97-0] 1,3,5,7- Tetraazatricyclo [3.3.1.13•7] decane; hexamethyenetetramine; HMT; HMTA; hexamine. 1,3,5,7- tetraazaadamantane hexamethylenemine; Uritone; Urotropin. C6H12N4; mol wt 140.19; C 51.40%, H 8.63%, N 39.96%. Methenamine (hexamethylenetetramine) exists as colorless, lustrous crystals or white crystalline powder. Its solutions are alkaline to litmus. Freely soluble in water, soluble in alcohol and in chloroform.

Phenyl Salicylate. [118-55-8] 2-Hydroxybenzoic acid phenyl ester; Salol. C13H10O3 ; mol wt 214.22, C 72.89%, H 4.70%, 0 22.41%. Made by the action of phosphorus oxy-chloride on a mixture of phenol and salicylic acid. Phenyl Salicylate exists as white crystals with a melting point of 40-43° C. It is very slightly soluble in water and freely soluble in alcohol.

Sodium Phosphate Monobasic. [7558-80-7] Sodium biphosphate; sodium dihyrdogen phosphate; acid sodium phosphate; monosodium orthophosphate; primary sodium phosphate; [H2Na04P:] mol wt 119.98. H 1.68%,   Na 19.16%, 0 53.34%, P 25.82%. Monohydrate, white, odorless slightly deliquesce crystals or granules. At 100º loses all its water; when ignited it converts to metaphosphate. It is freely soluble in water and practically insoluble in alcohol. The aq soln is acid. PH of 0.1 molar aq soln at 25°: 4.5.

Methylene Blue. [61-73-4] 3,7-bis(dimethylamino) phenothiazin-5-ium chloride; C.I. Basic Blue 9; methylthioninium chloride; tetramethylthionine chloride; 3,7-bis( dimethylamino) phenazathionium chloride. Methylene Blue (Methylthionine chloride) exists as dark green crystals. It is soluble in water and in chloroform; sparingly soluble in alcohol.

C16H18CIN3S· 3H20 MW  =373.9

Utira-C Tablets - Clinical Pharmacology

Hyoscyamine Sulfate is a parasympatholytic which relaxes smooth muscles and thus produces an antispasmodic effect. It is well absorbed from the gastrointestinal tract and is rapidly distributed throughout body tissues. Most is excreted in the urine within 12 hours, 13% to 50% being unchanged. Its biotransformation is hepatic. Its protein binding is moderate.

Methenamine degrades in an acidic urine environment releasing formaldehyde, which provides bactericidal or bacteriostatic action. It is well absorbed from the gastrointestinal tract. 70% to 90% reaches the urine unchanged at which point it is hydrolyzed if the urine is acidic. Within 24 hours it is almost completely (90%) excreted; of this at pH 5, approximately 20% is formaldehyde. Protein binding-some formaldehyde is bound to substances in the urine and surrounding tissues. Methenamine is freely distributed to body tissue and fluids but is not clinically significant as it does not hydrolyze at pH greater than 6.8.

Phenyl Salicylate releases salicylate, a  mild analgesic for pain.

Methylene Blue possesses weak antiseptic properties. It is well absorbed by the gastrointestinal tract and is rapidly reduced to leukomethylene blue which is stabilized in some combination form in the urine. 75% is excreted unchanged.

Sodium Phosphate Monobasic, an acidlfier, helps to maintain an acid pH in the urine necessary for the degradation of methenamine.

Indications and Usage for Utira-C Tablets

Indicated for the treatment of symptoms of irritative voiding. Indicated for the relief of local symptoms, such as inflammation, hypermotility, and pain, which accompany lower urinary tract infections. Indicated for the relief of urinary tract symptoms caused by diagnostic procedures.

Contraindications

Hypersensitivity to any of the ingredients. Risk benefits should be carefully considered when the following medical problems exist: Cardiac disease (especially cardiac arrhythmias, congestive heart failure, coronary heart disease, mitral stenosis); gastrointestinal tract obstructive disease; glaucoma; myasthenia gravis; acute urinary retention may be precipitated in obstructive uropathy (such as bladder neck obstruction due to prostatic hypertrophy).

Warnings

Do not exceed recommended dosage. If rapid pulse, dizziness, or blurring of vision occurs, discontinue use immediately.

KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN. IN CASE OF ACCIDENTAL OVERDOSE, SEEK PROFESSIONAL ASSISTANCE OR CONTACT A POISON CONTROL CENTER IMMEDIATELY.

Precautions

General

Cross sensitivity and/or related problems - patients intolerant of belladonna alkaloids or salicylates may be intolerant of this medication also. Delay in gastric emptying could complicate the management of gastric ulcers.

Information for Patients

There have been no studies to establish the safety of prolonged use in humans. No known long-term animal studies have been performed to evaluate carcinogenic potential.

Laboratory Tests

Interactions

Drug Interactions

Because of this product's effect on gastrointestinal motility and gastric emptying, it may decrease the absorption of other oral medications during concurrent use such as: urinary alkalizers; thiazide diuretics (may cause the urine to become alkaline reducing the effectiveness of Methenamine by inhibiting its conversion to formaldehyde); antimuscarinics (concurrent use may intensify antimuscarinic effects of Hyoscyamine Sulfate because of secondary antimuscarinic activities of these medications); antacids/ antidiarrheals (may reduce absorption of Hyoscyamine Sulfate, concurrent use with antacids may cause urine to become alkaline, reducing effectiveness of Methenamine by inhibiting its conversion to formaldehyde). Doses of these medications should be spaced 1 hour apart from doses of Hyoscyamine Sulfate; antimyasthenics (concurrent use with Hyoscyamine Sulfate may further reduce intestinal motility); ketoconazole (patients should be advised to take this combination at least 2 hours after ketoconazole); monoamine oxidase (MAO) inhibitors (concurrent use may intensify antimuscarinic side effects), opioid (narcotic analgesics may result in increased risk of severe constipation); sulfonamides (these drugs may precipitate with formaldehyde in the urine, increasing the danger of crystalluria). Patients should be advised that the urine may become blue to blue green and the feces may be discolored as a result of the excretion of Methylene Blue.

Drug/Laboratory Test Interactions

Carcinogenesis, Mutagenesis, Impairment of Fertility

Pregnancy

Teratogenic Effects

Pregnancy Category C - Hyoscyamine Sulfate and Methenamine cross the placenta. Studies have not been done in animals or humans. It is not known whether Utira™-C Tablets cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Utira™-C Tablets should be given to a pregnant woman only if clearly needed.

Nonteratogenic Effects

Labor and Delivery

Nursing Mothers

Problems in humans have not been documented, however, Methenamine and traces of Hyoscyamine Sulfate are excreted in breast milk. Accordingly, Utira™-C Tablets should be given to a nursing woman only if clearly needed.

Pediatric Use

Infants and young children are especially susceptible to the toxic effect of the belladonna alkaloids.

Geriatric Use

Use with caution in elderly patients as they may respond to usual doses of Hyoscyamine Sulfate with excitement, agitation, drowsiness, or confusion.

Adverse Reactions

Cardiovascular - rapid pulse, flushing

Central Nervous System- blurred vision, dizziness

Respiratory - shortness of breath or trouble breathing

Genitourinary - difficulty micturition, acute urinary retention

Gastrointestinal - dry mouth, nausea/vomiting

Drug Abuse and Dependence

A dependence on the use of Utira -C has not been reported and due to the nature of its ingredients, abuse of UtiralTM-C is not expected.

Controlled Substance

Abuse

Dependence

Overdosage

By exceeding the recommended dosage of Utira™-C, symptomology related to the overdose of its individual active ingredients may be expected as follows:

Hyoscyamine Sulfate: Symptoms associated with an overdosage of Utira™-C, will most probably be manifested in the symptoms related to overdosage of the alkaloid Hyoscyamine Sulfate. Such symptoms as dryness of mucous membranes; dilation of pupils, hot, dry, flushed skin; hyperpyrexia; tachycardia; palpitations; elevated blood pressure; coma; circulatory collapse and death from respiratory failure can occur due to overdosage of these alkaloids.

Methenamine: If large amounts of the drug (2-8 g daily) are used over extended periods (3-4 weeks), bladder and gastrointestinal irritation, painful and frequent micturition, albuminuria and gross hematuria may be expected.

Methylene Blue: Symptoms of Methylene Blue overdosage associated with the overdosage of Utira™-C are not expected to be discernible from those associated with other active ingredients in UtiraTM-C.

Phenyl Salicylate: Symptoms of Phenyl Salicylate overdosage include burning pain in throat and mouth, white necrotic lesions in the mouth, abdominal pain, vomiting, bloody diarrhea, pallor, sweating, weakness, headache, dizziness and tinnitus. The symptoms, however, are not expected to be discernible from those associated with the other active ingredients in Utira™-C.

Sodium Phosphate Monobasic: Symptoms of Sodium Biphosphate overdosage may include diarrhea, dehydration, and electrolyte imbalances.

Treatment: Emesis or gastric lavage. Slow intravenous administration of physostigmine in doses of 1 to 4 mg (0.5 to 1 mg in children), repeated as needed in one to two hours to reverse severe antimuscarinic symptoms. Administration of small doses of diazepam to control excitement and seizures. Artificial respiration with oxygen if needed for respiratory depression. Adequate hydration. Symptomatic treatment as necessary.

Utira-C Tablets Dosage and Administration

Adults: One tablet orally 4 times per day followed by liberal fluid intake. Older children: Dosage must be individualized by physician. Not recommended for use in children 6 years of age or younger.

How is Utira-C Tablets Supplied

UtiraTM-C is an oval, purple tablet imprinted with "HAW 513" on one side, available in bottles of 100 tablets, NDC 63717-513-01, and samples of 20 tablets, NDC 63717-513-99.

STORAGE

Preserve and dispense in a tight, light- resistant container as defined in the USP/NF with a child-resistant closure. Store at room temperature, USP.

PACKAGE/LABEL PRINCIPAL DISPLAY PANEL

UTIRA-C  hyoscyamine sulfate 0.12mg, methenamine 81.6 mg, phenyl salicylate 36.2 mg, sodium phosphate monobasic 40.8 mg, methylene blue 10.8 mg  tablet, sugar coated

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 63717-513 Route of Administration ORAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength HYOSCYAMINE SULFATE (HYOSCYAMINE) HYOSCYAMINE SULFATE 0.12 mg SODIUM PHOSPHATE, MONOBASIC, MONOHYDRATE (COLFOSCERIL PALMITATE) SODIUM PHOSPHATE, MONOBASIC, MONOHYDRATE 40.8 mg PHENYL SALICYLATE (PHENYL SALICYLATE) PHENYL SALICYLATE 36.2 mg METHENAMINE (METHENAMINE) METHENAMINE 81.6 mg METHYLENE BLUE (METHYLENE BLUE) METHYLENE BLUE 10.8 mg

Inactive Ingredients Ingredient Name Strength CALCIUM SULFATE 46.4 mg CARNAUBA WAX 0.02 mg D&C RED NO. 27 1 mg ANHYDROUS DIBASIC CALCIUM PHOSPHATE 102 mg FD&C BLUE NO. 1 0.9 mg GELATIN 1.6 mg HYPROMELLOSE 8.2 mg KAOLIN 33.6 mg MAGNESIUM STEARATE 4 mg CELLULOSE, MICROCRYSTALLINE 50.28 mg MINERAL OIL 1.4 mg SHELLAC 3 mg POLYETHYLENE GLYCOL 1.4 mg POVIDONE K30 1 mg SUCROSE 117 mg TITANIUM DIOXIDE 6.7 mg

Product Characteristics Color PURPLE Score no score Shape OVAL Size 435mm Flavor Imprint Code HAW;513 Contains

Packaging # NDC Package Description Multilevel Packaging 1 63717-513-99 20 TABLET In 1 BLISTER PACK contains a BOTTLE (63717-513-01) 1 63717-513-01 100 TABLET In 1 BOTTLE This package is contained within the BLISTER PACK (63717-513-99)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
Unapproved drug other		09/01/2005

Labeler - Hawthorn Pharmaceuticals (118049704)

Registrant - Contract Pharmacal Corporation (057795122)

Establishment
Name	Address	ID/FEI	Operations
Contract Pharmacal Corporation		057795122	MANUFACTURE

Revised: 03/2010Hawthorn Pharmaceuticals

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