Topicycline

Action

Unknown. Thought to inhibit bacterial protein synthesis at level of 30S and 50S bacterial ribosomes and to alter cytoplasmic membrane of susceptible organisms.

Availability

Capsules: 250 mg, 500 mg

Indications and dosages

➣ Mild to moderate infections caused by susceptible organisms

Adults: 500 mg P.O. b.i.d. or 250 mg P.O. q.i.d.

➣ Severe infections caused by susceptible organisms

Adults: 500 mg P.O. q.i.d.

Children older than age 8: 25 to 50 mg/kg P.O. q.i.d.

➣ Syphilis in penicillin-allergic patients

Adults: 500 mg P.O. q.i.d. for 14 days

➣ Late syphilis (except neurosyphilis)

Adults: 500 mg P.O. q.i.d. for 28 days

➣ Leptospirosis when penicillin is contraindicated or ineffective

Adults: 1 to 2 g P.O. daily in two to four divided doses for 5 to 7 days

➣ Yaws

Adults: 1 to 2 g P.O. daily in two to four divided doses for 10 to 14 days

➣ Gonorrhea in penicillin-allergic patients

Adults: Initially, 1.5 g P.O., followed by 500 mg P.O. q 6 hours for 4 days, up to a total of 9 g

➣ Uncomplicated urethral, endocervical, or rectal infections caused by

Chlamydia trachomatis

Adults: 500 mg P.O. q.i.d. for 7 days

➣ Rickettsial and mycoplasmal infections

Adults: 1 to 2 g P.O. daily in two to four divided doses for 7 days

➣ Helicobacter pylori infection

Adults: In patients with active duodenal ulcer, 500 mg P.O. q.i.d. at meals and bedtime for 14 days, given with other drugs (such as metronidazole, bismuth subsalicylate, amoxicillin, or omeprazole)

➣ Brucellosis

Adults: 500 mg P.O. q.i.d. for 3 weeks, given with streptomycin I.M. b.i.d. during week 1 and streptomycin once daily during week 2

➣ Granuloma inguinale; chancroid

Adults: 1 to 2 g P.O. daily in two to four divided doses for 2 to 4 weeks

➣ Cholera

Adults: 500 mg P.O. q 6 hours for 48 to 72 hours

➣ Plague when streptomycin is contraindicated or ineffective

Adults: 2 to 4 g P.O. q.i.d. for 10 days

Children older than age 8: 30 to 40 mg/kg P.O. q.i.d. for 10 to 14 days

➣ Tularemia as an alternative to streptomycin

Adults: 1 to 2 g P.O. daily in two to four divided doses for 1 to 2 weeks

➣ Campylobacter infection

Adults: 1 to 2 g P.O. daily in two to four divided doses for 10 days

➣ Relapsing fever caused by Borrelia recurrentis

Adults: 1 to 2 g P.O. daily in two to four divided doses for 7 days or until patient is afebrile

➣ Adjunctive treatment of inflammatory acne

Adults and adolescents: 500 mg to 1 g P.O. q.i.d. for 1 to 2 weeks, decreased gradually to 125 to 500 mg P.O. daily

Dosage adjustment

• Renal impairment

Off-label uses

• Rosacea

• Anthrax

• Arthritis

• Lyme disease

• Sclerosing agent to control pleural effusions

Contraindications

• Hypersensitivity to drug, other tetracyclines, bisulfites, or alcohol (in some products)

Precautions

Use cautiously in:

• renal disease, hepatic impairment, nephrogenic diabetes insipidus

• cachectic or debilitated patients

• pregnant or breastfeeding patients (except in anthrax treatment)

• children younger than age 8 (except in anthrax treatment).

Administration

• Give with 8 oz of water at least 1 hour before or 2 hours after a meal (especially if it includes milk or other dairy products), antacids, laxatives, or antidiarrheal drugs.

Adverse reactions

CNS: paresthesia, benign intracranial hypertension

CV: pericarditis

EENT: abnormal conjunctival pigmentation, hoarseness, pharyngitis

GI: nausea, vomiting, diarrhea, loose bulky stools, esophageal ulcers, epigastric distress, enterocolitis, oral and anogenital candidiasis, stomatitis, black hairy tongue, glossitis, anorexia, pancreatitis

GU: dark yellow or brown urine, vaginal candidiasis, anogenital lesions

Hematologic: eosinophilia, hemolytic anemia, neutropenia, thrombocytopenia, thrombocytopenia purpura

Hepatic: fatty liver

Musculoskeletal: retarded bone growth, polyarthralgia

Respiratory: pulmonary infiltrates

Skin: photosensitivity, maculopapular or erythematous rash, increased pigmentation, urticaria, onycholysis

Other: permanent tooth discoloration (in children younger than age 8), tooth enamel defects, superinfection, hypersensitivity reactions including anaphylaxis, serum sickness-like reaction, exacerbation of systemic lupus erythematosus

Interactions

Drug-drug. Adsorbent antidiarrheals, antacids, calcium, cholestyramine, cimetidine, colestipol, iron, magnesium, sodium bicarbonate: decreased tetracycline absorption

Digoxin: increased digoxin blood level, greater risk of toxicity

Hormonal contraceptives: decreased contraceptive efficacy

Insulin: reduced insulin requirement

Lithium: increased or decreased lithium blood level

Methoxyflurane: increased risk of nephrotoxicity

Penicillin: decreased penicillin activity

Sucralfate: prevention of tetracycline absorption from GI tract

Warfarin: enhanced warfarin effects

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, amylase, aspartate aminotransferase, bilirubin, blood urea nitrogen: increased levels

Hemoglobin, neutrophils, platelets, white blood cells: decreased levels

Urinary catecholamines: false elevation

Drug-food. Dairy products, foods containing calcium: decreased drug absorption

Drug-behaviors. Alcohol use: decreased drug efficacy

Sun exposure: increased risk of photosensitivity

Patient monitoring

• Monitor for signs and symptoms of superinfection and hypersensitivity reaction.

• With long-term use, monitor CBC, liver function tests, and (in prepubertal patients) bone growth.

• Assess neurologic status. Stay alert for benign intracranial hypertension (especially in children).

Patient teaching

• Tell patient to take oral form with 8 oz of water at least 1 hour before or 2 hours after eating a meal, consuming dairy products, or taking antacids, laxatives, or antidiarrheal drugs. Advise him to take last daily dose at least 1 hour before bedtime.

• Stress importance of completing entire course of therapy as ordered, even after symptoms improve.

Caution patient not to use outdated tetracycline, because it may cause serious kidney disease.

• Teach patient to recognize and report signs and symptoms of yeast infection and other infections.

• With long-term therapy, tell patient he'll undergo regular blood testing. Advise parents that prepubertal child should have periodic bone X-rays.

• Caution patient to avoid alcohol during therapy.

• Tell parents that tetracycline use during tooth development period (last half of pregnancy, infancy, and childhood to age 8) may cause permanent yellow, gray, or brownish tooth discoloration.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and behaviors mentioned above.