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Pronunciation
(mi noe SYE kleen)
Generic Available (U.S.)
Yes: Excludes injection, pellet-filled capsule
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment of susceptible bacterial infections of both gram-negative and gram-positive organisms; treatment of anthrax (inhalational, cutaneous, and gastrointestinal); moderate-to-severe acne; meningococcal (asymptomatic) carrier state; Rickettsial diseases (including Rocky Mountain spotted fever, Q fever); nongonococcal urethritis, gonorrhea; acute intestinal amebiasis; respiratory tract infection; skin/soft tissue infections; chlamydial infections
Extended release (Solodyn®): Only indicated for treatment of inflammatory lesions of non-nodular moderate-to-severe acne
Use: Unlabeled
Rheumatoid arthritis (patients with low disease activity of short duration); nocardiosis; alternative treatment for community-acquired MRSA infection
Pregnancy Risk Factor
D
Pregnancy Considerations
Tetracyclines, including minocycline, cross the placenta, enter fetal circulation, and may cause permanent discoloration of teeth if used during the second or third trimester. Congenital anomalies after minocycline use have been reported postmarketing. Because use during pregnancy may cause fetal harm, minocycline is classified as pregnancy category D.
Lactation
Enters breast milk/not recommended
Breast-Feeding Considerations
Small amounts of minocycline are excreted in breast milk and therefore, breast-feeding is not recommended by the manufacturer. Minocycline absorption is not affected by dairy products. This may lead to increased absorption from maternal milk when compared to other tetracyclines which are bound by the calcium in the maternal milk. Nondose-related effects could include modification of bowel flora. There have been case reports of black discoloration of breast milk in women taking minocycline.
Contraindications
Hypersensitivity to minocycline, other tetracyclines, or any component of the formulation; children <8 years of age
Warnings/Precautions
Concerns related to adverse effects:
• Autoimmune syndromes: Lupus-like, hepatitis, and vasculitis autoimmune syndromes have been reported; discontinue if symptoms occur.
• CNS effects: Lightheadedness and vertigo may occur; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Increased BUN: May be associated with increases in BUN secondary to antianabolic effects; use caution in patients with renal impairment.
• Photosensitivity: May cause photosensitivity; discontinue if skin erythema occurs. Use skin protection and avoid prolonged exposure to sunlight; avoid use of use tanning equipment.
• Pseudotumor cerebri: Has been (rarely) reported with tetracycline use; usually resolves with discontinuation.
• Skin rash: Rash, along with eosinophilia, fever, and organ failure (Drug Rash with Eosinophilia and Systemic Symptoms [DRESS] syndrome), may occur; onset of symptoms may be delayed up to several weeks; fatal in up to 10% of cases; discontinue treatment immediately if DRESS syndrome is suspected
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.
Disease-related concerns:
• Hepatic impairment: Hepatotoxicity has been reported; use with caution in patients with hepatic impairment.
• Renal impairment: Use with caution in patients with renal impairment (Clcr <80 mL/minute).
Special populations:
• Pediatrics: May cause tissue hyperpigmentation, enamel hypoplasia, or permanent tooth discoloration; use of tetracyclines should be avoided during tooth development (children <8 years of age) unless other drugs are not likely to be effective or are contraindicated.
• Pregnancy: Do not use during pregnancy. In addition to affecting tooth development, tetracycline use has been associated with retardation of skeletal development and reduced bone growth.
• Rheumatoid arthritis (unlabeled/investigational): Contraindicated in pregnancy and breast-feeding; Child-Pugh Class C and acute hepatitis B and C. (Saag KG, 2008)
Adverse Reactions
Frequency not defined.
Cardiovascular: Myocarditis, pericarditis, vasculitis
Central nervous system: Bulging fontanels, dizziness, fatigue, fever, headache, hypoesthesia, malaise, mood changes, paresthesia, pseudotumor cerebri, sedation, seizure, somnolence, vertigo
Dermatologic: Alopecia, angioedema, drug rash with eosinophilia and systemic symptoms (DRESS), erythema multiforme, erythema nodosum, erythematous rash, exfoliative dermatitis, hyperpigmentation of nails, maculopapular rash, photosensitivity, pigmentation of the skin and mucous membranes, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Endocrine & metabolic: Thyroid cancer, thyroid discoloration, thyroid dysfunction
Gastrointestinal: Anorexia, diarrhea, dyspepsia, dysphagia, enamel hypoplasia, enterocolitis, esophageal ulcerations, esophagitis, glossitis, inflammatory lesions (oral/anogenital), moniliasis, nausea, oral cavity discoloration, pancreatitis, pseudomembranous colitis, stomatitis, tooth discoloration, vomiting, xerostomia
Genitourinary: Balanitis, vulvovaginitis
Hematologic: Agranulocytosis, eosinophilia, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
Hepatic: Autoimmune hepatitis, hepatic cholestasis, hepatic failure, hepatitis, hyperbilirubinemia, jaundice, liver enzyme increases
Local: Injection site reaction (I.V. administration)
Neuromuscular & skeletal: Arthralgia, arthritis, bone discoloration, joint stiffness, joint swelling, myalgia
Otic: Hearing loss, tinnitus
Renal: Acute renal failure, BUN increased, interstitial nephritis
Respiratory: Asthma, bronchospasm, cough, dyspnea, pneumonitis, pulmonary infiltrate (with eosinophilia)
Miscellaneous: Anaphylaxis, hypersensitivity, lupus erythematosus, lupus-like syndrome, serum sickness
Metabolism/Transport Effects
None known.
Drug Interactions
Antacids: May decrease the absorption of Tetracycline Derivatives. Risk D: Consider therapy modification
Atazanavir: Minocycline may decrease the serum concentration of Atazanavir. Risk C: Monitor therapy
BCG: Antibiotics may diminish the therapeutic effect of BCG. Risk X: Avoid combination
Bile Acid Sequestrants: May decrease the absorption of Tetracycline Derivatives. Risk D: Consider therapy modification
Bismuth: May decrease the serum concentration of Tetracycline Derivatives. Management: Consider dosing tetracyclines 2 hours before, or 6 hours after, bismuth. The need to separate doses during Helicobacter pylori eradication regimens is questionable. Risk D: Consider therapy modification
Bismuth Subsalicylate: May decrease the serum concentration of Tetracycline Derivatives. Management: Consider dosing tetracyclines 2 hours before, or 6 hours after, bismuth subsalicylate. The need to separate doses during Helicobacter pylori eradication regimens is questionable. Risk D: Consider therapy modification
Calcium Salts: May decrease the serum concentration of Tetracycline Derivatives. Management: If coadministration of oral calcium with oral tetracyclines can not be avoided, consider separating administration of each agent by several hours. Risk D: Consider therapy modification
Iron Salts: May decrease the absorption of Tetracycline Derivatives. Only a concern with orally administered products. Exceptions: Ferric Gluconate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Risk D: Consider therapy modification
Lanthanum: May decrease the serum concentration of Tetracycline Derivatives. Management: Administer oral tetracycline antibiotics at least two hours before or after lanthanum. Risk D: Consider therapy modification
Magnesium Salts: May decrease the absorption of Tetracycline Derivatives. Only applicable to oral preparations of each agent. Risk D: Consider therapy modification
Neuromuscular-Blocking Agents: Tetracycline Derivatives may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Risk C: Monitor therapy
Penicillins: Tetracycline Derivatives may diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification
Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Risk C: Monitor therapy
Quinapril: May decrease the serum concentration of Tetracycline Derivatives. Management: Separate doses of quinapril and oral tetracycline derivatives by at least 2 hours in order to reduce the risk of interaction. Monitor for reduced efficacy of the tetracycline if these products are used concomitantly. Risk D: Consider therapy modification
Retinoic Acid Derivatives: Tetracycline Derivatives may enhance the adverse/toxic effect of Retinoic Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Exceptions: Adapalene; Alitretinoin; Tretinoin (Topical). Risk X: Avoid combination
Sucralfate: May decrease the absorption of Tetracycline Derivatives. Management: Administer the tetracycline derivative at least 2 hours prior to sucralfate in order to minimize the impact of this interaction. Risk D: Consider therapy modification
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 24 hours after cessation of antibacterial agents. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Tetracycline Derivatives may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Zinc Salts: May decrease the absorption of Tetracycline Derivatives. Only a concern when both products are administered orally. Exceptions: Zinc Chloride. Risk D: Consider therapy modification
Ethanol/Nutrition/Herb Interactions
Food: Minocycline serum concentrations are not significantly altered if taken with food or dairy products.
Herb/Nutraceutical: Avoid dong quai, St John's wort (may also cause photosensitization).
Storage
Capsule (including pellet-filled), tablet: Store at 20°C to 25°C (68°F to 77°F); protect from heat. Protect from light and moisture.
Extended release tablet: Store at 15°C to 30°C (59°F to 86°F); protect from heat. Protect from light and moisture.
Injection: Store vials at 20°C to 25°C (68°F to 77°F) prior to reconstitution. Reconstituted solution is stable at room temperature for 24 hours. Final dilutions should be administered immediately.
Reconstitution
Injection: Reconstitute with 5 mL of sterile water for injection, and further dilute in 500-1000 mL of NS, D5W, D5NS, Ringer's injection, or LR.
Compatibility
Stable in NS, D5LR, D5W, D10W, D51/4NS, D51/2NS, D5NS, Ringer's injection, LR.
Incompatible with calcium-containing solutions (except LR)
Y-site administration: Compatible: Aztreonam, cisatracurium, cyclosporine, docetaxel, etoposide phosphate, filgrastim, fludarabine, gemcitabine, granisetron, heparin, hydrocortisone sodium succinate, linezolid, magnesium sulfate, melphalan, oxytocin, potassium chloride, remifentanil, sargramostim, teniposide, vitamin B complex with C. Incompatible: Allopurinol, amifostine, hydromorphone, meperidine, morphine, pemetrexed, propofol, thiotepa.
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
Rheumatoid arthritis: The mechanism of action of minocycline in rheumatoid arthritis is not completely understood. It is thought to have antimicrobial, anti-inflammatory, immunomodulatory, and chondroprotective effects. More specifically, it is thought to be a potent inhibitor of metalloproteinases, which are active in rheumatoid arthritis joint destruction.
Pharmacodynamics/Kinetics
Absorption: Oral: Well absorbed
Protein binding: 70% to 75%
Metabolism: Hepatic to inactive metabolites
Half-life elimination: I.V.: 15-23 hours; Oral: 16 hours (range: 11-22 hours)
Time to peak: Capsule, pellet filled: 1-4 hours; Extended release tablet: 3.5-4 hours
Excretion: Urine, feces
Dosage
Usual dosage range:
I.V.:
Children >8 years: Initial: 4 mg/kg, followed by 2 mg/kg/dose every 12 hours (maximum: 400 mg/day)
Adults: Initial: 200 mg, followed by 100 mg every 12 hours (maximum: 400 mg/day)
Oral:
Capsule or immediate release tablet:
Children >8 years: Oral: Initial: 4 mg/kg, followed by 2 mg/kg/dose every 12 hours
Adults: Oral: Initial: 200 mg, followed by 100 mg every 12 hours; more frequent dosing intervals may be used (100-200 mg initially, followed by 50 mg 4 times daily)
Extended release tablet (Solodyn®): Children ≥12 years and Adults (≥45 kg): Oral: 45-135 mg once daily (weight based)
Indication-specific dosing:
Children:
Acne (inflammatory, non-nodular, moderate-to-severe) (Solodyn®): Oral: Children ≥12 years:
45-54 kg: 45 mg once daily
55-77 kg: 65 mg once daily
78-102 kg: 90 mg once daily
103-125 kg: 115 mg once daily
126-136 kg: 135 mg once daily
Note: Therapy should be continued for 12 weeks. Higher doses do not confer greater efficacy and may be associated with more acute vestibular side effects. Safety of use beyond 12 weeks has not been established.
Cellulitis (purulent) infection due to community-acquired MRSA (unlabeled use): Oral: Children >8 years: Initial: 4 mg/kg (maximum: 200 mg); Maintenance: 2 mg/kg/dose (maximum: 100 mg) every 12 hours for 5-10 days (Liu, 2011)
Adults:
Acne: Oral: Capsule or immediate-release tablet: 50-100 mg twice daily
Inflammatory, non-nodular, moderate-to-severe (Solodyn®):
45-54 kg: 45 mg once daily
55-77 kg: 65 mg once daily
78-102 kg: 90 mg once daily
103-125 kg: 115 mg once daily
126-136 kg: 135 mg once daily
Note: Therapy should be continued for 12 weeks. Higher doses do not confer greater efficacy and may be associated with more acute vestibular side effects. Safety of use beyond 12 weeks has not been established.
Cellulitis (purulent) due to community-acquired MRSA (unlabeled use): Oral: Initial: 200 mg; Maintenance: 100 mg twice daily for 5-10 days (Liu, 2011)
Chlamydial or
Ureaplasma urealyticum
infection, uncomplicated: Oral, I.V.: Urethral, endocervical, or rectal: 100 mg every 12 hours for at least 7 days
Gonococcal infection, uncomplicated (males): Oral, I.V.:
Without urethritis or anorectal infection: Initial: 200 mg, followed by 100 mg every 12 hours for at least 4 days (cultures 2-3 days post-therapy)
Urethritis: 100 mg every 12 hours for 5 days
Meningococcal carrier state (manufacturer's labeling): Oral: 100 mg every 12 hours for 5 days. Note: CDC recommendations do not mention use of minocycline for eradicating nasopharyngeal carriage of meningococcal
Mycobacterium marinum
: Oral: 100 mg every 12 hours for 6-8 weeks
Nocardiosis, cutaneous (non-CNS) (unlabeled use): Oral: 100-200 mg every 12 hours
Rheumatoid arthritis (unlabeled use): Oral: 100 mg twice daily (O'Dell, 2001)
Syphilis: Oral, I.V.: Initial: 200 mg, followed by 100 mg every 12 hours for 10-15 days
Elderly: Refer to adult dosing.
Dosage adjustment in renal impairment: Use with caution; monitor BUN and creatinine clearance. Consider decreasing dose or increasing dosing interval (extended release).
Clcr <80 mL/minute: Do not exceed 200 mg/day
Administration: Oral
May be administered with or without food. Administer with adequate fluid to decrease the risk of esophageal irritation and ulceration. Swallow pellet-filled capsule and extended release tablet whole; do not chew, crush, or split.
Administration: I.V.
I.V.: Infuse slowly; avoid rapid administration. The manufacturer's labeling does not provide a recommended administration rate. The injectable route should be used only if the oral route is not feasible or adequate. Prolonged intravenous therapy may be associated with thrombophlebitis.
Monitoring Parameters
LFTs, BUN, renal function with long-term treatment; if symptomatic for autoimmune disorder, include ANA, CBC
Test Interactions
May cause interference with fluorescence test for urinary catecholamines (false elevations)
Dietary Considerations
May be taken with or without food.
Patient Education
May cause photosensitivity reaction, nausea, fatigue, headache, dizziness, sedation, or diarrhea. Report rash or itching, unresolved nausea or diarrhea, change in urinary output (excess), and opportunistic infection (eg, fever, chills, sore throat, burning urination, fatigue).
I.V.: Report immediately any pain, burning, or swelling at infusion site or any signs of allergic reaction (eg, respiratory difficulty or swallowing, back pain, chest tightness, rash, hives, swelling of lips or mouth).
Oral: May be taken with or without food.
Geriatric Considerations
Minocycline has not been studied in the elderly but its CNS effects may limit its use. Dose reduction for renal function not necessary.
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. No data documenting these effects with minocycline; use caution.
Nursing: Physical Assessment/Monitoring
Assess results of culture and sensitivity tests and allergy history before beginning therapy. Teach patient importance of adequate hydration.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, oral: 50 mg, 75 mg, 100 mg
Capsule, pellet filled, oral:
Minocin®: 50 mg, 100 mg
Minocin® PAC: 50 mg, 100 mg
Injection, powder for reconstitution:
Minocin®: 100 mg
Tablet, oral: 50 mg, 75 mg, 100 mg
Dynacin®: 50 mg, 75 mg, 100 mg
Tablet, extended release, oral: 45 mg, 90 mg, 135 mg
Solodyn®: 45 mg, 65 mg, 90 mg, 115 mg, 135 mg
Pricing: U.S. (www.drugstore.com)
Capsules (Minocin)
50 mg (30): $139.99
100 mg (30): $308.36
Capsules (Minocycline HCl)
50 mg (30): $15.99
75 mg (30): $48.99
100 mg (30): $22.99
Tablet, 24-hour (Solodyn)
45 mg (30): $799.24
65 mg (30): $848.03
90 mg (100): $2698.59
135 mg (30): $799.24
Tablets (Dynacin)
50 mg (30): $249.99
75 mg (30): $365.98
100 mg (30): $440.01
Tablets (Minocycline HCl)
75 mg (30): $146.00
100 mg (50): $199.98
References
Ghislain PD and Roujeau JC, "Treatment of Severe Drug Reactions: Stevens-Johnson Syndrome, Toxic Epidermal Necrolysis and Hypersensitivity Syndrome," Dermatol Online J, 2002, 8(1):5. Available at http://dermatology.cdlib.org/DOJvol8num1/reviews/drugrxn/ghislain.html
Goulden V, “Guidelines for the Management of Acne Vulgaris in Adolescents,” Paediatr Drugs, 2003, 5(5):301-13.
Liu C, Bayer A, Cosgrove SE, et al, “Clinical Practice Guidelines by the Infectious Diseases Society of America for the Treatment of Methicillin-Resistant Staphylococcus Aureus Infections in Adults and Children: Executive Summary,” Clin Infect Dis, 2011, 52(3):285-92.
O'Dell JR, Haire CE, Palmer W, et al, “Treatment of Early Rheumatoid Arthritis With Minocycline or Placebo: Results of a Randomized, Double-Blind, Placebo-Controlled Trial,” Arthritis Rheum, 1997, 40(5):842-8.
O'Dell JR, Blakely KW, Mallek JA, et al, “Treatment of Early Seropositive Rheumatoid Arthritis: A Two-Year, Double-Blind Comparison of Minocycline and Hydroxychloroquine,” Arthritis Rheum, 2001, 44(10):2235-41.
Saag, KG, Teng GG, Patkar NM, et al, “American College of Rheumatology 2008 Recommendations for the Use of Nonbiologic and Biologic Disease-Modifying Antirheumatic Drugs in Rheumatoid Arthritis,” Arthritis Rheum, 2008, 59(6):762-84.
Smilack JD, Wilson WR, and Cockerill FR 3d, “Tetracyclines, Chloramphenicol, Erythromycin, Clindamycin, and Metronidazole,” Mayo Clin Proc, 1991, 66(12):1270-80.
International Brand Names
Lexi-Comp.com
Last full review/revision March 2012
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