Minocycline

Antibiotic Class:

Tetracyclines

Antimicrobial Spectrum:

Staphylococcus aureus, Streptococcus pneumonia, Streptococcus pyogenes, Streptooccus agalacticae, Campylobacter jejuni, Haemophilus influenzae, Neisseria gonorrhoeae, Neisseria meningitides,Clostridium spp., Peptostreptococcus spp., Peptococcus spp. Bacteroides melaninogenicus, Bacteroides fragilis

Mechanism of Action:

Inhibits bacterial protein synthesis by binding with the 30S ribosomal subunit.

Pharmacodynamics:

Tetracyclines produce a combination of concentration and time-dependent killing (AUC:MIC ratio).

Pharmacokinetics:

Dose of 200mg PO: Cmax: 2-3.5 mcg/mL; Tmax: 1-4 hours; Half-life: 11-26 hours; Volume of distribution: 60 L/kg; Table 3

Adverse Effects:

GI: epigastric burning, abdominal discomfort, nausea, vomiting, anorexia, diarrhea, esophagitis, esophageal ulcers, dysphagia, candidal superinfections

Teeth and bone: (dose/duration related) yellow discoloration of teeth, which turns into a gray-brown permanent discoloration, hypoplasia of enamel, teeth demineralization, skeletal growth retardation

Hepatotoxicity: rare, but fatal; intrahepatic cholestasis, jaundice, azotemia, acidosis, irreversible shock

Renal Toxicity: hyperphosphatemia, acidosis, polyuria, polydipsia

Photosensitivity and hyperpigmentation: red rash to blistering on sun-exposed areas; photoallergic reactions manifested by paresthesias of hands, feet, nose, photo-onycholysis

Auditory: tinnitus, hearing loss

Vision: visual disturbances

CNS: lightheadedness, dizziness, ataxia, drowsiness, headache

Dosage:

Oral: 50mg, 75mg, 100mg capsules

         50mg/5mL suspension

         50mg, 75mg, 100mg tablets

Dosing in adults (common indications):

Acne vulgaris: 200 mg IV or PO x 1, then 100 mg IV or PO q12h

Bartonellosis: 200 mg IV or PO x 1, then 100 mg IV or PO q12h

Brucellosis: 200 mg IV or PO x 1, then 100 mg IV or PO q12h

Chlamydial infection: 100 mg PO q12h x minimum 7 days

Cholera: 200 mg IV or PO x 1, then 100 mg IV or PO q12h

Rickettsial disease: 200 mg IV or PO x 1, then 100 mg IV or PO q12h

Psittacosis: 200 mg IV or PO x 1, then 100 mg IV or PO q12h

Dosing in pediatrics:

2-4 mg/kg divided q12h

Disease state based dosing:

Renal failure:  No dosing change necessary

Hepatic failure:  No dosing changes recommended at this time.

Contraindications/Warnings/Precautions:

Precautions: Usage in newborns, infants, and children less than 8 years of age; risk for tooth discoloration; Renal or liver impairment; Phototoxicity; Avoid in patients with systemic lupus erythematosus (SLE);

Drug Interactions:

Food: Decreased absorption of minocycline

Milk: Decreased absorption of minocycline

Oral contraceptives: Decreased contraceptive effectiveness

Warfarin: Increased warfarin effect

Table 6

Pregnancy:

Category D: Risk established, but benefits may outweigh risk.

Monitoring Requirements:

Therapeutic:  Culture and sensitivities, serum levels, signs and symptoms of infection, white blood cell count

Toxic: Hypersensitivity syndrome reaction, serum sickness like reaction or single organ dysfunction – Monitor: CBC, LFTs, urinalysis, urea, creatinine, chest radiograph; Drug-induced lupus: monitor antinuclear antibody and hepatic transaminases; General long-term therapy:  Liver and renal function tests, Hematopoietic studies

Brand names/Manufacturer: 

DynacinÒ/Medicis; MinocinÒ/Lederle; MinocyclineÒ/Generva; VectrinÒ/Warner Chilcott