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standards of non-Merck sources.
Medication Safety Issues
Sound-alike/look-alike issues:
Dynacin® may be confused with Dyazide®, Dynabac®, DynaCirc®, Dynapen®
Minocin® may be confused with Indocin®, Lincocin®, Minizide®, Mithracin®, niacin
Pronunciation
(mi noe SYE kleen)
U.S. Brand Names
Index Terms
Generic Available
Yes: Excludes extended release tablet
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use
Treatment of susceptible bacterial infections of both gram-negative and gram-positive organisms; treatment of anthrax (inhalational, cutaneous, and gastrointestinal); acne; meningococcal (asymptomatic) carrier state; Rickettsial diseases (including Rocky Mountain spotted fever, Q fever); nongonococcal urethritis, gonorrhea; acute intestinal amebiasis
Pregnancy Risk Factor
D
Pregnancy Implications
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; pregnancy
Warnings/Precautions
Concerns related to adverse effects:
• Autoimmune syndromes: Lupus-like, hepatitis, and vasculitis autoimmune syndromes have been reported; discontinue if symptoms.
• CNS effects: Lightheadedness and vertigo may occur; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Hepatotoxicity: Has been reported; use caution in patients with hepatic impairment.
• 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; do not use tanning equipment.
• Pseudotumor cerebri: Has been (rarely) reported with tetracycline use; usually resolves with discontinuation.
• 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.
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. However, recommended in treatment of anthrax exposure.
• 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.
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, 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 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: Hepatic cholestasis, hepatic failure, hepatitis, hyperbilirubinemia, jaundice, liver enzyme increases
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
Drug Interactions
Calcium-, magnesium-, or aluminum-containing antacids, bile acid sequestrants, bismuth, oral contraceptives, iron, zinc, sodium bicarbonate, penicillins, quinapril: May decrease absorption of tetracyclines.
Methoxyflurane anesthesia, when concurrent with tetracyclines, may cause fatal nephrotoxicity.
Penicillins: Tetracyclines may reduce bactericidal efficacy of penicillins and cephalosporins.
Retinoic acid derivatives: May increase risk of pseudotumor cerebri.
Typhoid vaccine: Antibacterial agents may decrease the therapeutic efficacy of the live, attenuated typhoid (Ty21a strain) vaccine
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 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 light and moisture.
Extended release tablet: Store at 15°C to 30°C (59°F to 86°F). Protect from light, moisture, and heat.
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
Protein binding: 70% to 75%
Metabolism: Hepatic to inactive metabolites
Half-life elimination: 16 hours (range: 11-23 hours)
Time to peak: Capsule, pellet filled: 1-4 hours; Extended release tablet: 3.5-4 hours
Excretion: Urine, feces
Dosage
Usual dosage range:
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 (maximum: 400 mg/day)
Indication-specific dosing:
Children ?12 years: Acne (inflammatory, non-nodular, moderate-to-severe) (Solodyn™): Oral:
45-59 kg: 45 mg once daily
60-90 kg: 90 mg once daily
91-136 kg: 135 mg once daily
Note: Therapy should be continued for 12 weeks. Higher doses do not confer greater efficacy, and safety of use beyond 12 weeks has not been established.
Adults: Oral:
Acne: Capsule or immediate-release tablet: 50-100 mg daily
Inflammatory, non-nodular, moderate-to-severe (Solodyn™):
45-59 kg: 45 mg once daily
60-90 kg: 90 mg once daily
91-136 kg: 135 mg once daily
Note: Therapy should be continued for 12 weeks. Higher doses do not confer greater efficacy, and safety of use beyond 12 weeks has not been established.
Chlamydial or
Ureaplasma urealyticum
infection, uncomplicated: Urethral, endocervical, or rectal: 100 mg every 12 hours for at least 7 days
Gonococcal infection, uncomplicated (males):
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: 100 mg every 12 hours for 5 days
Mycobacterium marinum
: 100 mg every 12 hours for 6-8 weeks
Nocardiosis, cutaneous (non-CNS): 100 mg every 12 hours
Syphilis: Initial: 200 mg, followed by 100 mg every 12 hours for 10-15 days
Dosage adjustment in renal impairment: Consider decreasing dose or increasing dosing interval; total daily dose should not exceed 200 mg
Administration: Oral
May be taken with food or milk. Administer with adequate fluid to decrease the risk of esophageal irritation and ulceration.
Monitoring Parameters
Culture and sensitivity testing prior to initiating therapy; 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 food or milk.
Patient Education
Do not take any new medication during therapy unless approved by prescriber. Take exactly as directed; may be taken with food. Do not chew, break, or dissolve extended release tablet. Complete full course of therapy; do not discontinue even if condition is resolved. May cause photosensitivity reaction (avoid sun, use sunscreen, 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 or persistent 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.
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. Assess potential for interactions with other pharmacological agents or herbal products patient may be taking (eg, warfarin, antacids, hydantoins, carbamazepine). Assess therapeutic effectiveness (resolution of infection) and adverse reactions on a regular basis during therapy. Teach patient proper use, possible side effects/appropriate interventions (eg, importance of adequate hydration), and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: 50 mg, 75 mg, 100 mg
Dynacin®: 75 mg [DSC], 100 mg [DSC]
Capsule, pellet filled: 50 mg, 100 mg
Minocin® PAC: 50 mg, 100 mg [packaged with wipes, serum, and masque]
Tablet: 50 mg, 75 mg, 100 mg
Dynacin®, myrac™: 50 mg, 75 mg, 100 mg
Tablet, extended release:
Solodyn™: 45 mg, 90 mg, 135 mg
Pricing: U.S. (www.drugstore.com)
Capsules (Dynacin)
50 mg (30): $97.30
75 mg (30): $195.99
Capsules (Minocin)
50 mg (30): $136.03
Capsules (Minocycline HCl)
50 mg (30): $15.99
75 mg (30): $48.99
100 mg (30): $23.00
Tablet, 24-hour (Solodyn)
90 mg (100): $1641.55
Tablets (Dynacin)
75 mg (30): $252.24
100 mg (30): $305.75
Tablets (Minocycline HCl)
75 mg (30): $143.99
Tablets (Myrac)
100 mg (50): $222.00
References
Goulden V, “Guidelines for the Management of Acne Vulgaris in Adolescents,” Paediatr Drugs, 2003, 5(5):301-13.
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 May 2008
Content last modified May 2008
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