U.S. Brand Names:
Dynacin®; Minocin®
Synonyms:
Minocycline Hydrochloride
Generic Available:
Yes: Capsule
Canadian Brand Names:
Alti-Minocycline; Apo-Minocycline®; Gen-Minocycline; Minocin®; Novo-Minocycline; PMS-Minocycline; Rhoxal-minocycline
Use:
Treatment of susceptible bacterial infections of both gram-negative and gram-positive organisms; treatment of anthrax (inhalational, cutaneous, and gastrointestinal); acne; meningococcal carrier state; Rickettsial diseases (including Rocky Mountain spotted fever, Q fever); nongonococcal urethritis, gonorrhea; acute intestinal amebiasis
Use - Dental:
Treatment of periodontitis associated with presence of Actinobacillus actinomycetemcomitans (AA); as adjunctive therapy in recurrent aphthous ulcers
Pregnancy Risk Factor:
D
Pregnancy Implications:
May cause permanent discoloration (brown-grey) of teeth. Animal studies indicate possible embryotoxicity.
Lactation:
Enters breast milk/not recommended (AAP rates "compatible")
Contraindications:
Hypersensitivity to minocycline, other tetracyclines, or any component of the formulation; pregnancy
Warnings/Precautions:
Avoid use during tooth development (children 8 years of age) unless other drugs are not likely to be effective or are contraindicated. May be associated with increases in BUN secondary to anti-anabolic effects. Avoid in renal insufficiency (associated with hepatotoxicity). CNS effects (lightheadedness, vertigo) may occur, potentially affecting a patient's ability to drive or operate heavy machinery. Has been associated (rarely) with pseudotumor cerebri. May cause photosensitivity.
Adverse Reactions:
>10%: Miscellaneous: Discoloration of teeth (in children)
1% to 10%:
Central nervous system: Lightheadedness, vertigo
Dermatologic: Photosensitivity
Gastrointestinal: Nausea, diarrhea
<1%: Abdominal cramps, acute renal failure, anaphylaxis, angioedema, anorexia, azotemia, diabetes insipidus, eosinophilia, erythema multiforme, esophagitis, exfoliative dermatitis, hemolytic anemia, hepatitis, hepatic failure, neutropenia, paresthesia, pericarditis, pigmentation of nails, pruritus, pseudotumor cerebri (blurred vision, bulging fontanels in infants, headache, increased intracranial pressure), rash, Stevens-Johnson syndrome, superinfection, thrombocytopenia, thyroid dysfunction (extremely rare), tinnitus, urticaria, vomiting
Overdosage/Toxicology:
Symptoms of overdose include diabetes insipidus, nausea, anorexia, and diarrhea. Treatment is supportive. Not dialyzable (0% to 5%).
Drug Interactions:
Calcium-, magnesium-, or aluminum-containing antacids, oral contraceptives, iron, zinc, sodium bicarbonate, penicillins, cimetidine: May decrease absorption of tetracyclines
Although no clinical evidence exists, tetracyclines may bind with bismuth or calcium carbonate, an excipient in bismuth subsalicylate, during treatment for H. pylori.
Digoxin: Tetracyclines may rarely increase digoxin serum levels.
Methoxyflurane anesthesia when concurrent with tetracyclines may cause fatal nephrotoxicity.
Oral contraceptives: Anecdotal reports suggesting decreased contraceptive efficacy with tetracyclines have been refuted by more rigorous scientific and clinical data.
Warfarin: Hypoprothrombinemic response may be increased with tetracyclines; monitor INR closely during initiation or discontinuation.
Ethanol/Nutrition/Herb Interactions:
Food: Minocycline serum concentrations are not altered if taken with dairy products.
Herb/Nutraceutical: Avoid dong quai, St John's wort (may also cause photosensitization).
Compatibility:
Stable in D5NS, D5W, LR, NS
Y-site administration: Compatible: Aztreonam, cisatracurium, cyclophosphamide, docetaxel, etoposide, filgrastim, fludarabine, gemcitabine, granisetron, heparin, hydrocortisone sodium succinate, linezolid, magnesium sulfate, melphalan, perphenazine, potassium chloride, remifentanil, sargramostim, teniposide, vinorelbine, vitamin B complex with C. Incompatible: Allopurinol, amifostine, hydromorphone, meperidine, morphine, piperacillin/tazobactam, propofol, thiotepa
Compatibility in syringe: Incompatible: Doxapram
Compatibility when admixed: Incompatible: Rifampin
Mechanism of Action:
Inhibits bacterial protein synthesis by binding with the 30S and possibly the 50S ribosomal subunit(s) of susceptible bacteria; cell wall synthesis is not affected
Pharmacodynamics/Kinetics:
Absorption: Well absorbed
Distribution: Majority deposits for extended periods in fat; crosses placenta; enters breast milk
Protein binding: 70% to 75%
Half-life elimination: 15 hours
Excretion: Urine
Dosage:
Children >8 years: Oral, I.V.: Initial: 4 mg/kg followed by 2 mg/kg/dose every 12 hours
Adults:
Infection: Oral, I.V.: 200 mg stat, 100 mg every 12 hours not to exceed 400 mg/24 hours
Acne: Oral: 50 mg 1-3 times/day
Dosage adjustment in renal impairment: Consider decreasing dose or increasing dosing interval with renal impairment.
Administration:
Oral: May be taken with food or milk. Administer with adequate fluid to decrease the risk of esophageal irritation and ulceration.
I.V.: Infuse slowly, usually over a 4- to 6-hour period.
Test Interactions:
May cause interference with fluorescence test for urinary catecholamines (false elevations)
Dietary Considerations:
May be taken with food or milk.
Patient Education:
Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take at intervals around-the-clock; may be taken with food. Complete full course of therapy; do not discontinue even if condition is resolved. May cause photosensitivity reaction (avoid sun, use sunblock, or wear protective clothing); nausea (small, frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); or diarrhea (boiled milk, buttermilk, or yogurt may help). Report rash or itching, unresolved nausea or diarrhea, change in urinary output (excess); or opportunistic infection (eg, fever, chills, sore throat, burning urination, fatigue). Pregnancy/breast-feeding precautions: Do not get pregnant while taking this medication. Consult prescriber for appropriate contraceptive measures. Consult prescriber if breast-feeding.
Dental Health: Effects on Dental Treatment:
Key adverse event(s) related to dental treatment: Discoloration of teeth (children). Opportunistic "superinfection" with Candida albicans; tetracyclines are not recommended for use during pregnancy or in children 8 years of age since they have been reported to cause enamel hypoplasia and permanent teeth discoloration. The use of tetracycline's should only be used in these patients if other agents are contraindicated or alternative antimicrobials will not eradicate the organism. Long-term use associated with oral candidiasis.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions:
No information available to require special precautions
Mental Health: Effects on Psychiatric Treatment:
Barbiturates and carbamazepine may decrease the effects of tetracyclines; tetracyclines may decrease lithium clearance resulting in an increase in serum lithium levels and potential lithium toxicity; monitor serum lithium levels
Dosage Forms:
Capsule, as hydrochloride: 50 mg, 75 mg, 100 mg
Dynacin®: 50 mg, 75 mg, 100 mg
Capsule, pellet-filled, as hydrochloride (Minocin®): 50 mg, 100 mg
Injection, powder for reconstitution, as hydrochloride (Minocin®): 100 mg
Tablet, as hydrochloride (Dynacin®): 50 mg, 75 mg, 100 mg
International Brand Names:
Acneclin® (AR); Akamin® (AU); Aknemin® (GB, NL); Akne-Puren® (DE); Aknin-Mino® (DE); Aknin-N® (CH); Aknoral® (CH); Aknosan® (DE); Alti-Minocycline (CA); Apo-Minocycline® (CA, ZA); Asolmicina® (AR); Auramin® (AT); Blemix® (GB); Borymycin® (SG); Cyclimycin® (ZA); Cyclomin® (GB); Cyclops® (AU); Cynomycin® (IN); Dentomycin® (GB); Gen-Minocycline (CA); Icht-Oral® (DE); Klinoc® (AT); Klinomycin® (DE); Klinomycin® [liqu.oral] (LU); Klinotab® (BE); Lederderm® (DE); Mestacine® (FR); Minac® (CH); Minakne® (DE); Mino-50® (BE, LU); Minocin Akne® (CH); Minocin® (AR, AT, BE, CA, CL, CO, CY, EG, ES, GB, HK, ID, IE, IL, IT, JO, KW, LB, LU, MX, NL, PT, SG, TH); Minocin MR® (GB); Minoclin® (IL); Minoclir® (DE); Minocyclin beta® (DE); Minocycline BC® (BE); Minocycline® (GB, IL); Minocyclin Heumann® (DE); Minocyclin Hexal® (DE); Minocyclin Lederle® (AT); Minocyclin-ratiopharm® (DE); Minocyclin Stada® (DE); minocyclin von ct® (DE); Minolis® (FR); Minomax® (BR); Minomycin® (AU, NZ); Minoplus® (DE); Minostad® (AT); Minotab® (AR, BE, LU, NL); Minotabs® (NZ); Minotrex® (PT); Mino-Wolff® (DE); Minox 50® (IE); Mynocine® (FR); Novo-Minocycline (CA); Periocline® (JP); PMS-Minocycline (CA); Rhoxal-minocycline (CA); Rolab-Minocycline® (ZA); Skid® (DE); Skinocyclin® (DE); Triomin® (ZA); Udima® (DE); Zacnan® (FR)
References
Smilack JD, Wilson WR, and Cockerill FR 3d, "Tetracyclines, Chloramphenicol, Erythromycin, Clindamycin, and Metronidazole,"Mayo Clin Proc, 1991, 66(12):1270-80.