TROBICIN- spectinomycin hydrochloride and water
Function and Efficacy
CLINICAL PHARMACOLOGY
TROBICIN Sterile Powder is rapidly absorbed after intramuscular injection. A single, two-gram injection produces peak serum concentrations averaging about 100 mcg/mL at one hour; a single, four-gram injection produces peak serum concentrations averaging 160 mcg/mL at two hours. Average serum concentrations of 15 mcg/mL for the two-gram dose and 31 mcg/mL for the four-gram dose were present eight hours after dosing. Spectinomycin hydrochloride is an inhibitor of protein synthesis in the bacterial cell; the site of action is the 30S ribosomal subunit. Definitive in vitro N. gonorrhoeae For specific information regarding susceptibility test interpretive criteria and associated test methods and quality control standards recognized by FDA for this drug, please see: https://www.
Microbiology
Spectinomycin hydrochloride is an inhibitor of protein synthesis in the bacterial cell; the site of action is the 30S ribosomal subunit. Definitive in vitro N. gonorrhoeae
Indication
TROBICIN Sterile Powder is indicated in the treatment of acute gonorrheal urethritis and proctitis in the male and acute gonorrheal cervicitis and proctitis in the female when due to susceptible strains of Neisseria gonorrhoeae. To reduce the development of drug-resistant bacteria and maintain the effectiveness of TROBICIN Sterile Powder and other antibacterial drugs, TROBICIN Sterile Powder 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.
Usage and Dosage
DOSAGE AND ADMINISTRATION
TROBICIN Sterile Powder, 2 grams: reconstitute with 3. 2 mL of Sterile Water for Injection, USP. Shake vials vigorously immediately after adding Sterile Water for Injection, USP and before withdrawing dose. It is recommended that disposable syringes and needles be used. A 20-gauge needle is recommended. Intramuscular injections should be made deep into the upper outer quadrant of the gluteal muscle. Adults (Men and Women)em dashInject 5 mL intramuscularly In geographic areas where antibiotic resistance is known to be prevalent, initial treatment with 4 grams (10 mL) intramuscularly is preferred. The 10-mL injection may be divided between two gluteal injection sites.
Preparation of Drug for Intramuscular Injection
TROBICIN Sterile Powder, 2 grams: reconstitute with 3.2 mL of Sterile Water for Injection, USP . Shake vials vigorously immediately after adding Sterile Water for Injection, USP and before withdrawing dose. It is recommended that disposable syringes and needles be used. A 20-gauge needle is recommended.
Dosage
Intramuscular injections should be made deep into the upper outer quadrant of the gluteal muscle. Adults (Men and Women)em dashInject 5 mL intramuscularly In geographic areas where antibiotic resistance is known to be prevalent, initial treatment with 4 grams (10 mL) intramuscularly is preferred. The 10-mL injection may be divided between two gluteal injection sites.
Label
Adverse Reactions
The following reactions were observed during the single dose clinical trials: soreness at the injection site, urticaria, dizziness, nausea, chills, fever and insomnia. During multiple dose subchronic tolerance studies in normal human volunteers, the following were noted: a decrease in hemoglobin, hematocrit and creatinine clearance; elevation of alkaline phosphatase, BUN and SGPT. In single and multiple dose studies in normal volunteers, a reduction in urine output was noted. Extensive renal function studies demonstrated no consistent changes indicative of renal toxicity. A few cases of anaphylaxis or anaphylactoid reactions have been reported. If serious allergic reactions occur, the usual agents (epinephrine, corticosteroids, and/or antihistamines) should be available for emergency use. In cases of severe anaphylaxis, airway support and oxygen may also be required.
Precautions
The use of TROBICIN Sterile Powder is contraindicated in patients previously found hypersensitive to it.
Special Population Medication
Pregnancy:
Spectinomycin was not teratogenic or embryocidal when orally or subcutaneously administered to rats at doses of 300 mg/kg/day (equivalent to the recommended maximum human dose based on mg/m 2 2
Nursing Mothers
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when spectinomycin is administered to a nursing woman.
Pediatric Use
Safety and effectiveness in the pediatric population have not been established. ( See WARNINGS
Storage
Store unreconstituted product at controlled room temperature 20° to 25°C (68° to 77°F) [see USP]. Store prepared suspension at controlled room temperature 20° to 25°C (68° to 77°F) and use within 24 hours.
Other Information
Susceptibility Testing
For specific information regarding susceptibility test interpretive criteria and associated test methods and quality control standards recognized by FDA for this drug, please see: https://www.fda.gov/drugs
WARNINGS
Spectinomycin hydrochloride is not effective in the treatment of syphilis. Antibiotics used in high doses for short periods of time to treat gonorrhea may mask or delay the symptoms of incubating syphilis. Since the treatment of syphilis demands prolonged therapy with any effective antibiotic, patients being treated for gonorrhea should be closely observed clinically. All patients with gonorrhea should have a serologic test for syphilis at the time of diagnosis. Patients treated with spectinomycin hydrochloride should have a follow-up serologic test for syphilis after three months.
Carcinogenesis,Mutagenesis, Impairment of Fertility
Genotoxicity of spectinomycin hydrochloride was evaluated in six assay test systems including two Ames tests, two micronucleus tests in mice, unscheduled DNA synthesis in rat primary hepatocytes, and a chromosomal aberration test in Chinese hamster ovary cells. Spectinomycin was not shown to be mutagenic or genotoxic in these tests. No adverse effects on fertility or general reproductive performance were observed when spectinomycin was administered subcutaneously to rats at dose levels up to 300 mg/kg (equivalent to the recommended maximum human dose based on mg/m 2 2
OVERDOSAGE
Information on overdosage in humans is not available. Hemodialysis has been reported to aid in the removal of intravenously administered Kusumi R, Metzler C, Fass R; Pharmacokinetics of Spectinomycin in Volunteers with Renal Insufficiency, Chemotherapy,