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tetracycline (Sumycin, Actisite, Achromycin V)

 

Classes: Tetracyclines

Dosing and uses of Tetracycline

 

Adult dosage forms and strengths

capsule/tablet

  • 250mg
  • 500mg

syrup (extemporaneously prepared)

  • 125mg/5mL

 

Chronic Bronchitis, Acute Exacerbation

500 mg PO q6hr

 

Acne

250-500 mg PO q12hr

 

Ehrlichiosis

500 mg PO q6hr for 7-14 days

 

Vibrio Cholera

500 mg PO q6hr for 3 days

 

Malaria, Severe Treatment (Unlabeled)

500 mg PO q6hr for 7 days with quinidine gluconate

 

Dosage modifications

Renal impairment

  • CrCl 50-80 mL/min: Dose frequency q8-12hr
  • CrCl 10-50 mL/min: Dose frequency q12-24hr
  • CrCl <10 mL/min: Dose frequency q24hr

 

Dosing Considerations

Susceptible organisms

  • Acinetobacter spp, Actinomyces israelii, Afipia felis, Bacillus anthracis, Bacteroides spp, Bartonella bacilliformis, Bartonella quintana, Bordetella pertussis, Borrelia recurrentis, Brucella spp, Capnocytophaga canimorsus, Campylobacter jejuni, Chlamydia spp, Citrobacter spp, Coxiella burnetii, Eikenella corrodens, Escherichia coli, Francisella tularensis, Leptospira interrogans, Helicobacter pylori, Klebsiella spp, Listeria monocytogenes, Moraxella catarrhalis, Mycoplasma pneumoniae, Neisseria gonorrhoeae, Propionibacterium acnes, Rickettsiae, Shigella spp, Staphylococcus aureus, Streptococcus pneumoniae, Treponema pallidum, Ureaplasma urealyticum, Vibrio cholerae, Yersinia pestis, Yersinia enterocolitica, Yersinia pseudotuberculosis

 

Pediatric dosage forms and strengths

capsule/tablet

  • 250mg
  • 500mg

syrup

  • 125mg/5mL

 

General Dosing Guidelines

<8 years: Not recommended; tooth discoloration and enamel hypoplasia may occur with use in young children

>8 years: 25-50 mg/kg/day PO divided q6hr; not to exceed 3 g/day

 

Malaria, Severe Treatment (Unlabeled)

<8 years: Not recommended; tooth discoloration and enamel hypoplasia may occur with use in young children

>8 years: 25-50 mg/kg/day PO divided q6hr, not to exceed 250 mg/dose q6hr for 7 days with quinidine gluconate

 

Vibrio Cholera

Single dose: 25 mg/kg PO; not to exceed 1 g/dose

Multiple dose: 40 mg/kg/day PO divided q6hr for 3 days; not to exceed 2 g/day

 

Administration

Take on empty stomach; do not take with dairy products

 

Tetracycline adverse (side) effects

>10%

Discoloration of teeth and enamel hypoplasia (young children)

 

1-10%

Diarrhea

Nausea

Photosensitivity

 

<1%

Anorexia

Abdominal cramps

Antibiotic-associated pseudomembranous colitis

Bulging fontanels in infants

Diabetes insipidus syndrome

Esophagitis

Exfoliative dermatitis

Incr ICp

Pericarditis

Pseudotumor cerebri

Pancreatitis

Pruritus

Pigmentation of nails

Vomiting

 

Warnings

Contraindications

Documented hypersensitivity

Severe hepatic dysfunction

 

Cautions

Photosensitivity may occur with prolonged exposure to sunlight or tanning equipment

Reduce dose in renal impairment

Consider drug serum level determinations in prolonged therapy

Tetracycline use during tooth development (last half of pregnancy through age 8 years) can cause permanent discoloration of teeth

Fanconilike syndrome may occur with outdated tetracyclines

IV/IM no longer commercially available

 

Pregnancy and lactation

Pregnancy category: D (systemic), C (periodontal fiber)

Lactation: Enters breast milk; some manufacturers say do not nurse; however, AAP considers nursing compatible due to calcium chelation of drug and prevention of its absorption (long-term safety of prolonged exposure unknown)

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Tetracycline

Mechanism of action

Inhibits bacterial protein synthesis by binding with 30S and possibly 50S ribosomal subunit(s)

 

Absorption

Absorption: 75% (PO)

Peak plasma time: 2-4 hr (PO)

 

Distribution

Small amount appears in bile; relative diffusion from blood into CSF: good only with inflammation (exceeds usual MICs) CSF: blood level ratio: inflamed meninges: 25%

Protein bound: 65%

 

Elimination

Half-life: 8-11 hr (normal renal function); 57-108 hr (end-stage renal disease)

Excretion: Urine (60% as unchanged drug); feces (as active form)