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Minocycline (systemic): Drug information

Minocycline (systemic): Drug information
(For additional information see "Minocycline (systemic): Patient drug information" and see "Minocycline (systemic): Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • CoreMino;
  • Minocin;
  • Minolira;
  • Solodyn;
  • Ximino
Brand Names: Canada
  • CO Minocycline;
  • DOM-Minocycline [DSC];
  • Minocycline-100 [DSC];
  • Minocycline-50 [DSC];
  • MYLAN-Minocycline [DSC];
  • PMS-Minocycline [DSC];
  • SANDOZ MInocycline [DSC];
  • SANDOZ Minocycline [DSC];
  • TEVA-Minocycline [DSC]
Pharmacologic Category
  • Antibiotic, Tetracycline Derivative
Dosing: Adult

Usual dosage range:

IV: Initial: 200 mg for 1 dose; Maintenance: 100 mg every 12 hours (maximum: 400 mg daily)

Oral: Initial: 200 mg for 1 dose; Maintenance: 100 mg every 12 hours; more frequent dosing intervals may be used (100 to 200 mg initially, followed by 50 mg 4 times daily)

Acne: Oral: Capsule or immediate-release tablet: 50 to 100 mg twice daily. Note: The shortest possible duration should be used to minimize development of bacterial resistance; re-evaluate at 3 to 4 months (AAD [Zaenglein 2016])

Acne (inflammatory, non-nodular, moderate to severe): Note: Therapy should be continued for 12 weeks. Safety of use beyond 12 weeks has not been established.

Extended-release capsule (Ximino): Oral: 1 mg/kg (rounded to the nearest capsule) once daily

Extended-release tablet: Oral:

Minolira:

45 to 59 kg: 52.5 mg (one-half of the 105 mg tablet) once daily

60 to 89 kg: 67.5 mg (one-half of the 135 mg tablet) once daily

90 to 125 kg: 105 mg once daily

126 to 136 kg: 135 mg once daily

CoreMino, Solodyn:

45 to 49 kg: 45 mg once daily

50 to 59 kg: 55 mg once daily

60 to 71 kg: 65 mg once daily

72 to 84 kg: 80 mg once daily

85 to 96 kg: 90 mg once daily

97 to 110 kg: 105 mg once daily

111 to 125 kg: 115 mg once daily

126 to 136 kg: 135 mg once daily

Chlamydial or Ureaplasma urealyticum infection, uncomplicated: Oral, IV: Urethral, endocervical, or rectal: 100 mg every 12 hours for at least 7 days

Gonococcal infection, uncomplicated (males): Oral, IV:

Without urethritis or anorectal infection: Initial: 200 mg for 1 dose; Maintenance: 100 mg every 12 hours for at least 4 days (cultures 2 to 3 days post-therapy)

Urethritis: 100 mg every 12 hours for 5 days

Leprosy (alternative agent) (off-label use): Oral:

Lepromatous (multibacillary): 100 mg once daily for 24 months in combination with clofazimine and rifampin (NHDP [HRSA 2016])

Tuberculoid (paucibacillary): 100 mg once daily for 12 months in combination with rifampin (NHDP [HRSA 2016])

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 to 8 weeks

Nocardiosis (off-label use): Oral: 100 to 200 mg every 12 hours, with or without other concomitant antimicrobials (Lerner 1996). Additional data may be necessary to further define the role of minocycline in this condition.

Prosthetic joint infection:

Staphylococci (oxacillin-sensitive or -resistant) oral phase treatment (after completion of pathogen-specific IV therapy) following 1-stage exchange:

Total ankle, elbow, hip, or shoulder arthroplasty: 100 mg twice daily for 3 months; Note: Must be used in combination with rifampin (Osmon 2013)

Total knee arthroplasty: 100 mg twice daily for 6 months; Note: Must be used in combination with rifampin (Osmon 2013)

Chronic oral antimicrobial suppression (off-label use): Oral:

Cutibacterium spp (alternative to penicillin or amoxicillin): 100 mg twice daily (Osmon 2013)

Staphylococci (oxacillin-resistant): 100 mg twice daily (Osmon 2013)

Rheumatoid arthritis (off-label use): Oral: 100 mg twice daily (Kloppenburg 1994; O’Dell 1997; O’Dell 2001; Stone 2003; Tilley 1995)

Skin and soft tissue infection:

Cellulitis, nonpurulent with risk for methicillin-resistant S. aureus: Oral: 100 mg twice daily in combination with an additional agent (eg, amoxicillin, cephalexin) for coverage of beta-hemolytic streptococci (IDSA [Stevens 2014]; Spelman 2021). Some experts give an initial 200 mg loading dose (Spelman 2021).

Cellulitis, purulent or abscess: Oral: 100 mg twice daily (IDSA [Stevens 2014]). Some experts give an initial 200 mg loading dose (Spelman 2021). Note: Systemic antibiotics only indicated for abscess in certain instances (eg, immunocompromised patients, signs of systemic infection, large or multiple abscesses, indwelling device, high risk for adverse outcome with endocarditis). If at risk for gram-negative bacilli, use in combination with an appropriate agent (IDSA [Stevens 2014]; Spelman 2021).

Duration: Treat for ≥5 days but may extend up to 14 days depending on severity and clinical response (IDSA [Stevens 2014]; Spelman 2021).

Syphilis: Oral, IV: Initial: 200 mg for 1 dose; Maintenance: 100 mg every 12 hours for 10 to 15 days

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

IV:

CrCl ≥80 mL/minute: No dosage adjustment necessary.

CrCl <80 mL/minute: Do not exceed 200 mg/day.

Oral:

Immediate release:

CrCl ≥80 mL/minute: No dosage adjustment necessary.

CrCl <80 mL/minute: Do not exceed 200 mg/day.

Extended release: There are no specific dosage adjustments provided in the manufacturer's labeling. Consider decreasing dose or increasing dosing interval.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling; however, hepatotoxicity has been reported. Use with caution.

Dosing: Pediatric

(For additional information see "Minocycline (systemic): Pediatric drug information")

General dosing, susceptible infection: Children >8 years and Adolescents:

Oral: Immediate-release formulations: Initial: 4 mg/kg once (maximum dose: 200 mg), then 2 mg/kg/dose every 12 hours (maximum dose: 100 mg/dose).

IV: Initial: 4 mg/kg once (maximum dose: 200 mg), then 2 mg/kg/dose (maximum dose: 100 mg/dose) every 12 hours; maximum daily dose: 400 mg/day.

Acne, inflammatory, non-nodular, moderate to severe: Note: Higher doses do not confer greater efficacy and may be associated with more acute vestibular side effects. Due to emerging resistance patterns, should not typically be used as monotherapy for the management of acne vulgaris (AAD [Zaenglein 2016]; Eichenfield 2013).

Immediate-release formulations: Children ≥8 years and Adolescents: Oral: 50 to 100 mg 1 to 2 times daily in conjunction with topical therapy (eg, benzoyl peroxide); duration of 4 to 8 weeks of therapy usually necessary to evaluate initial clinical response with a longer duration for a maximum effect (3 to 6 months) (Eichenfield 2013).

Extended-release formulations: Children ≥12 years and Adolescents: Oral: ~1 mg/kg/dose once daily for 12 weeks.

Product-specific dosing:

Extended-release capsule: Ximino: Oral:

45 to 59 kg: 45 mg once daily.

60 to 90 kg: 90 mg once daily.

91 to 136 kg: 135 mg once daily.

Extended-release tablet:

Minolira: Oral:

45 to 59 kg: 52.5 mg (one-half of the 105 mg tablet) once daily.

60 to 89 kg: 67.5 mg (one-half of the 135 mg tablet) once daily.

90 to 125 kg: 105 mg once daily.

126 to 136 kg: 135 mg once daily.

CoreMino, Solodyn: Oral:

45 to 49 kg: 45 mg once daily.

50 to 59 kg: 55 mg once daily.

60 to 71 kg: 65 mg once daily.

72 to 84 kg: 80 mg once daily.

85 to 96 kg: 90 mg once daily.

97 to 110 kg: 105 mg once daily.

111 to 125 kg: 115 mg once daily.

126 to 136 kg: 135 mg once daily.

Skin and soft tissue infection (ie, purulent cellulitis), community-acquired MRSA: Note: Treatment duration based on clinical response; usual duration is 5 to 10 days for outpatient cellulitis (IDSA [Liu 2011]).

Children >8 years and Adolescents: Immediate-release formulations: Oral: Initial: 4 mg/kg (maximum dose: 200 mg), then 2 mg/kg/dose (maximum dose: 100 mg/dose) every 12 hours (IDSA [Liu 2011]; IDSA [Stevens 2014])

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

Immediate release: IV, Oral: There are no pediatric-specific recommendations; based on experience in adult patients; dosing adjustment suggested. Hemodialysis: Not dialyzable (Brogden 1975).

Extended-release formulations: Children ≥12 years and Adolescents: There are no specific dosage adjustments provided in the manufacturer's labeling. Consider decreasing dose or increasing dosing interval.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; however, hepatotoxicity has been reported. Use with caution.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule, Oral:

Minocin: 50 mg [DSC], 100 mg [DSC] [contains brilliant blue fcf (fd&c blue #1), fd&c yellow #10 (quinoline yellow)]

Generic: 50 mg, 75 mg, 100 mg

Capsule Extended Release 24 Hour, Oral:

Ximino: 90 mg [contains brilliant blue fcf (fd&c blue #1)]

Ximino: 45 mg [contains brilliant blue fcf (fd&c blue #1), fd&c yellow #10 (quinoline yellow), fd&c yellow #6 (sunset yellow)]

Ximino: 135 mg [contains brilliant blue fcf (fd&c blue #1), fd&c yellow #6 (sunset yellow)]

Generic: 135 mg, 45 mg, 90 mg

Solution Reconstituted, Intravenous [preservative free]:

Minocin: 100 mg (1 ea)

Tablet, Oral:

Generic: 50 mg, 75 mg, 100 mg

Tablet Extended Release 24 Hour, Oral:

CoreMino: 45 mg, 90 mg, 135 mg

Minolira: 105 mg, 135 mg [scored]

Solodyn: 55 mg [contains fd&c red #40]

Solodyn: 65 mg [contains brilliant blue fcf (fd&c blue #1), fd&c blue #2 (indigotine), fd&c yellow #10 (quinoline yellow)]

Solodyn: 80 mg [contains fd&c blue #2 (indigotine), fd&c red #40, fd&c yellow #6 (sunset yellow)]

Solodyn: 105 mg [contains brilliant blue fcf (fd&c blue #1)]

Solodyn: 115 mg [contains brilliant blue fcf (fd&c blue #1), fd&c blue #2 (indigotine), fd&c yellow #10 (quinoline yellow)]

Generic: 45 mg, 55 mg, 65 mg, 80 mg, 90 mg, 105 mg, 115 mg, 135 mg

Generic Equivalent Available: US

May be product dependent

Dosage Forms Considerations

Minocin Kit contains minocycline oral capsules packaged with T3 Calming Wipes

Minocin for injection contains magnesium 2.2 mEq per vial

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Generic: 50 mg, 100 mg

Administration: Adult

IV: Infuse over 60 minutes; avoid rapid administration. The injectable route should be used only if the oral route is not feasible or adequate. Prolonged intravenous therapy may be associated with thrombophlebitis.

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 ER tablet or capsule whole; do not chew, crush, or split. Minolira 105 mg and 135 mg ER tablets may be split on the score line.

Bariatric surgery: Capsule and tablet, extended release: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. ER capsule (Ximino) and tablet (CoreMino, Solodyn) should be swallowed whole. Do not chew, crush, or split. ER tablet (Minolira) may be split on the score line. IR tablet, capsule, and injectable formulations are available. If safety and efficacy can be effectively monitored, no change in formulation or administration is required after bariatric surgery; however, consideration should be given to conversion to IR formulations for high-risk labeled and off-label indications.

Administration: Pediatric

IV: Infuse over 60 minutes; avoid rapid administration; the injectable route should be used only if the oral route is not feasible or adequate; prolonged intravenous therapy may be associated with thrombophlebitis.

Oral: Administer with plenty of fluids with or without food. Ingestion of adequate amounts of fluid and food may reduce the risk of esophageal irritation and ulceration. Swallow pellet-filled capsule and extended-release tablet whole; do not chew, crush, or split. Minolira 105 mg and 135 mg extended-release tablets may be split on the score line. Administer antacids, calcium supplements, iron supplements, magnesium-containing laxatives, and cholestyramine 2 hours before or after minocycline.

Use: Labeled Indications

Acute intestinal amebiasis: Adjunctive therapy to amebicides in the treatment of acute intestinal amebiasis.

Acne:

Oral (immediate release) and IV: Adjunctive therapy for the treatment of severe acne.

Oral (extended-release): Treatment of only inflammatory lesions of non-nodular moderate to severe acne vulgaris in patients 12 years and older.

Actinomycosis: Treatment of actinomycosis caused by Actinomyces israelii when penicillin is contraindicated.

Anthrax: Treatment of anthrax caused by Bacillus anthracis when penicillin is contraindicated.

Asymptomatic carriers of Neisseria meningitidis: Oral (immediate-release): To eliminate the meningococci from the nasopharynx of asymptomatic carriers of N. meningitidis.

Campylobacter: Treatment of infections caused by Campylobacter fetus.

Cholera: Treatment of cholera caused by Vibrio cholerae.

Clostridium: Treatment of infections caused by Clostridium spp when penicillin is contraindicated.

Gram-negative infections: Treatment of infections caused by Acinetobacter spp, Escherichia coli, Klebsiella aerogenes (formerly Enterobacter. aerogenes), Shigella spp

Listeriosis: Treatment of listeriosis due to Listeria monocytogenes when penicillin is contraindicated.

Meningitis: Treatment of meningitis due to Neisseria meningitidis when penicillin is contraindicated.

Ophthalmic infections: Treatment of inclusion conjunctivitis or trachoma caused by Chlamydia trachomatis.

Relapsing fever: Treatment of relapsing fever caused by Borrelia recurrentis.

Respiratory tract infections: Treatment of respiratory tract infections caused by Haemophilus influenzae, Klebsiella spp, or Mycoplasma pneumonia. For the treatment of upper respiratory tract infections caused by Streptococcus pneumoniae.

Rickettsial infections: Treatment of Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsialpox, and tick fevers caused by Rickettsiae.

Sexually transmitted infections: Treatment of lymphogranuloma venereum caused by C. trachomatis; nongonococcal urethritis, endocervical, or rectal infections in adults caused by Ureaplasma urealyticum or C. trachomatis; donovanosis (granuloma inguinale) caused by Klebsiella granulomatis; syphilis caused by Treponema pallidum subspecies pallidum, when penicillin is contraindicated.

Skin and soft tissue infections: Treatment of skin and soft tissue infections caused by Staphylococcus aureus (not considered a first-line agent for any staphylococcal infection).

Urinary tract infections: Treatment of urinary tract infections caused by Klebsiella species.

Vincent infection: Treatment of Vincent infection caused by Fusobacterium fusiforme when penicillin is contraindicated.

Yaws: Treatment of yaws caused by T. pallidum subspecies pertenue when penicillin is contraindicated.

Zoonotic infections: Treatment of psittacosis (ornithosis) due to Chlamydia psittaci; plague due to Yersinia pestis; tularemia due to Francisella tularensis; brucellosis due to Brucella spp (in conjunction with streptomycin); bartonellosis due to Bartonella bacilliformis.

Use: Off-Label: Adult

Leprosy; Nocardiosis; Prosthetic Joint Infection; Rheumatoid arthritis

Medication Safety Issues
Sound-alike/look-alike issues:

Dynacin may be confused with Dyazide, Dynapen

Minocin may be confused with Indocin, Lincocin, Minizide, niacin

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%:

Dermatologic: Pruritus (5%), urticaria (2%)

Nervous system: Dizziness (9%), fatigue (9%), malaise (4%), drowsiness (2%)

Neuromuscular & skeletal: Arthralgia (1%)

Otic: Tinnitus (2%)

Frequency not defined:

Cardiovascular: Myocarditis, vasculitis

Dermatologic: Skin photosensitivity, skin rash

Gastrointestinal: Diarrhea, discoloration of permanent tooth, enamel hypoplasia

Hematologic & oncologic: Lymphadenopathy

Nervous system: Intracranial hypertension, vertigo

Renal: Nephritis

Miscellaneous: Fever

Postmarketing: Abnormal thyroid function test, acute renal failure, anaphylaxis, angioedema, autoimmune hepatitis, balanitis, bulging fontanel, Clostridioides difficile associated diarrhea, Clostridioides difficile colitis, drug reaction with eosinophilia and systemic symptoms, dysphagia, enterocolitis, eosinophilia, erythema multiforme, exacerbation of systemic lupus erythematosus, exfoliative dermatitis, fixed drug eruption, glossitis, hearing loss, hemolytic anemia, Henoch-Schonlein purpura, hepatic failure, hepatitis, hepatotoxicity (idiosyncratic) (Chalasani 2014), hypersensitivity reaction, intracranial hypertension (Tan 2019), lupus-like syndrome, malignant neoplasm of thyroid, microscopic thyroid discoloration (brown-black), mucous membrane hyperpigmentation, pancreatitis, pericarditis, pneumonitis, polyarthralgia, pseudotumor cerebri, pulmonary infiltrates (with eosinophilia), serum sickness, skin pigmentation, staining of tooth, Stevens-Johnson syndrome, thrombocytopenia

Contraindications

Hypersensitivity to minocycline, other tetracyclines, or any component of the formulation

Canadian labeling: Additional contraindications (not in the US labeling): Severe liver disease; complete renal failure; myasthenia gravis; use in children <13 years of age; pregnancy; breastfeeding

Warnings/Precautions

Concerns related to adverse effects:

• Autoimmune syndromes: Lupus-like, hepatitis, and vasculitis autoimmune syndromes (including serum sickness [eg fever, arthralgia, and malaise]) have been reported; discontinue if symptoms occur and assess liver function tests, ANA, and CBC.

• Benign intracranial hypertension (eg, pseudotumor cerebri [PTC]): Benign intracranial hypertension (headache, blurred vision, diplopia, vision loss, and/or papilledema) has been associated with use. Women of childbearing age who are overweight or have a history of intracranial hypertension are at greater risk. Concomitant use of isotretinoin (known to cause PTC) and minocycline should be avoided. Intracranial hypertension typically resolves after discontinuation of treatment; however, permanent visual loss is possible. If visual symptoms develop during treatment, prompt ophthalmologic evaluation is warranted. Intracranial pressure can remain elevated for weeks after drug discontinuation; monitor patients until they stabilize.

• CNS effects: Lightheadedness, dizziness, and vertigo may occur; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Symptoms usually disappear with continued therapy and when the drug is discontinued.

• Hepatotoxicity: Serious liver injury, including irreversible drug induced hepatitis and fulminant hepatic failure (sometimes fatal) have been reported with use for acne treatment.

• Hyperpigmentation: Hyperpigmentation may occur in nails, bone, skin (including scar and injury sites), eyes, sclerae, thyroid, oral cavity, visceral tissue, and heart valves; skin and oral hyperpigmentation are independent of dose or administration duration.

• Hypersensitivity: Anaphylaxis has been reported; discontinue drug immediately and institute supportive measures.

• Increased BUN: May be associated with increases in BUN secondary to antianabolic effects; use caution in patients with renal impairment as this may lead to azotemia, hyperphosphatemia, acidosis, and possibly to drug accumulation and potential hepatotoxicity.

• Photosensitivity: May cause photosensitivity; discontinue if skin erythema occurs. Use skin protection and avoid prolonged exposure to sunlight; avoid use of use tanning equipment or UVA/B treatment.

• Skin rash: Rash, erythema multiforme, Stevens Johnson syndrome or 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 or in conjunction with other hepatotoxic drugs.

• Renal impairment: Use with caution in patients with renal impairment (CrCl <80 mL/minute); dosage adjustment recommended.

Special populations:

• Pediatric: May cause tissue hyperpigmentation, tooth enamel hypoplasia, or permanent tooth discoloration; more common with long-term use, but observed with repeated, short courses; use of tetracyclines should be avoided during tooth development (infancy and children ≤8 years of age) unless other drugs are not likely to be effective or are contraindicated.

Dosage form specific issues:

• Magnesium content: Parenteral (IV) formulation contains magnesium; monitor serum magnesium in patients with renal impairment and signs of magnesium intoxication (eg, flushing, sweating, hypotension, depressed reflexes, flaccid paralysis, hypothermia, circulatory collapse, cardiac and CNS depression leading to respiratory paralysis). Also use with caution and closely monitor patients with heart block or myocardial damage.

Other warnings/precautions:

• Appropriate use: Acne: The American Academy of Dermatology acne guidelines recommends minocycline be used as adjunctive treatment for moderate and severe acne and forms of inflammatory acne that are resistant to topical treatments. Concomitant topical therapy with benzoyl peroxide or a retinoid is recommended should be administered with systemic antibiotic therapy (eg, minocycline) and continued for maintenance after the antibiotic course is completed (AAD [Zaenglein 2016]).

Warnings: Additional Pediatric Considerations

Pseudotumor cerebri has been reported rarely in infants and adolescents; use with isotretinoin has been associated with cases of pseudotumor cerebri; avoid concomitant treatment with isotretinoin.

Metabolism/Transport Effects

None known.

Drug Interactions

Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic). Risk X: Avoid combination

Aminolevulinic Acid (Topical): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical). Risk C: Monitor therapy

Antacids: May decrease the absorption of Tetracyclines. Management: Separate administration of antacids and oral tetracycline derivatives by several hours when possible to minimize the extent of this potential interaction. Monitor for decreased therapeutic effects of tetracyclines. Risk D: Consider therapy modification

Atazanavir: Minocycline (Systemic) may decrease the serum concentration of Atazanavir. Risk C: Monitor therapy

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Risk X: Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Risk C: Monitor therapy

Bile Acid Sequestrants: May decrease the absorption of Tetracyclines. Risk C: Monitor therapy

Bismuth Subcitrate: May decrease the serum concentration of Tetracyclines. Management: Avoid administration of oral tetracyclines within 30 minutes of bismuth subcitrate administration. This is of questionable significance for at least some regimens intended to treat H. pylori infections. Risk D: Consider therapy modification

Bismuth Subsalicylate: May decrease the serum concentration of Tetracyclines. 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

Calcium Salts: May decrease the serum concentration of Tetracyclines. Management: If coadministration of oral calcium with oral tetracyclines cannot be avoided, consider separating administration of each agent by several hours. Risk D: Consider therapy modification

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and within 14 days following the use of oral or parenteral antibiotics. Risk X: Avoid combination

CNS Depressants: Minocycline (Systemic) may enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Immune Checkpoint Inhibitors: Antibiotics may diminish the therapeutic effect of Immune Checkpoint Inhibitors. Risk C: Monitor therapy

Iron Preparations: Tetracyclines may decrease the absorption of Iron Preparations. Iron Preparations may decrease the serum concentration of Tetracyclines. Management: Avoid this combination if possible. Administer oral iron preparations at least 2 hours before, or 4 hours after, the dose of the oral tetracycline derivative. Monitor for decreased therapeutic effect of oral tetracycline derivatives. Risk D: Consider therapy modification

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Risk C: Monitor therapy

Lanthanum: May decrease the serum concentration of Tetracyclines. Management: Administer oral tetracycline antibiotics at least two hours before or after lanthanum. Risk D: Consider therapy modification

Lithium: Tetracyclines may increase the serum concentration of Lithium. Risk C: Monitor therapy

Magnesium Dimecrotate: May interact via an unknown mechanism with Tetracyclines. Risk C: Monitor therapy

Magnesium Salts: May decrease the absorption of Tetracyclines. Only applicable to oral preparations of each agent. Management: Avoid coadministration of oral magnesium salts and oral tetracyclines. If coadministration cannot be avoided, administer oral magnesium at least 2 hours before, or 4 hours after, oral tetracyclines. Monitor for decreased tetracycline therapeutic effects. Risk D: Consider therapy modification

Mecamylamine: Tetracyclines may enhance the neuromuscular-blocking effect of Mecamylamine. Risk X: Avoid combination

Methoxsalen (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Methoxsalen (Systemic). Risk C: Monitor therapy

Methoxyflurane: Tetracyclines may enhance the nephrotoxic effect of Methoxyflurane. Risk X: Avoid combination

Mipomersen: Tetracyclines may enhance the hepatotoxic effect of Mipomersen. Risk C: Monitor therapy

Multivitamins/Minerals (with ADEK, Folate, Iron): May decrease the serum concentration of Tetracyclines. Management: Avoid this combination if possible. If coadministration cannot be avoided, administer the polyvalent cation-containing multivitamin at least 2 hours before or 4 hours after the tetracycline derivative. Monitor for decreased tetracycline effects. Risk D: Consider therapy modification

Multivitamins/Minerals (with AE, No Iron): May decrease the serum concentration of Tetracyclines. Management: If coadministration of a polyvalent cation-containing multivitamin with oral tetracyclines cannot be avoided, administer the polyvalent cation-containing multivitamin either 2 hours before or 4 hours after the tetracycline product. Risk D: Consider therapy modification

Neuromuscular-Blocking Agents: Minocycline (Systemic) may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Risk C: Monitor therapy

Penicillins: Tetracyclines may diminish the therapeutic effect of Penicillins. Risk C: Monitor therapy

Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Risk C: Monitor therapy

Quinapril: May decrease the serum concentration of Tetracyclines. Risk C: Monitor therapy

Retinoic Acid Derivatives: Tetracyclines may enhance the adverse/toxic effect of Retinoic Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Risk X: Avoid combination

Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Risk D: Consider therapy modification

Strontium Ranelate: May decrease the serum concentration of Tetracyclines. Management: In order to minimize any potential impact of strontium ranelate on tetracycline antibiotic concentrations, it is recommended that strontium ranelate treatment be interrupted during tetracycline therapy. Risk X: Avoid combination

Sucralfate: May decrease the absorption of Tetracyclines. Management: Administer most tetracycline derivatives at least 2 hours prior to sucralfate in order to minimize the impact of this interaction. Administer oral omadacycline 4 hours prior to sucralfate. Risk D: Consider therapy modification

Sucroferric Oxyhydroxide: May decrease the serum concentration of Tetracyclines. Management: Administer oral/enteral doxycycline at least 1 hour before sucroferric oxyhydroxide. Specific dose separation guidelines for other tetracyclines are not presently available. No interaction is anticipated with parenteral administration of tetracyclines. Risk D: Consider therapy modification

Sulfonylureas: Tetracyclines may enhance the hypoglycemic effect of Sulfonylureas. Risk C: Monitor therapy

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Avoid use of live attenuated typhoid vaccine (Ty21a) in patients being treated with systemic antibacterial agents. Postpone vaccination until 3 days after cessation of antibiotics and avoid starting antibiotics within 3 days of last vaccine dose. Risk D: Consider therapy modification

Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Risk C: Monitor therapy

Vitamin K Antagonists (eg, warfarin): Tetracyclines may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy

Zinc Salts: May decrease the absorption of Tetracyclines. Only a concern when both products are administered orally. Management: Separate administration of oral tetracycline derivatives and oral zinc salts by at least 2 hours to minimize this interaction. Risk D: Consider therapy modification

Food Interactions

Minocycline serum concentrations are not significantly altered if taken with food or dairy products. Management: Administer without regard to food.

Reproductive Considerations

Minocycline is excreted in seminal fluid (Saivin 1988). Minocycline is not recommended for the treatment of acne in males or females attempting to conceive a child.

Pregnancy Considerations

Minocycline crosses the placenta.

Tetracycline-class antibiotics may cause fetal harm following maternal use in pregnancy. Rare spontaneous reports of congenital anomalies, including limb reduction, have been reported following maternal minocycline use. Due to limited information, a causal association cannot be established. Tetracyclines accumulate in developing teeth and long tubular bones (Mylonas 2011). Permanent discoloration of teeth (yellow, gray, brown) can occur following in utero exposure and is more likely to occur following long-term or repeated exposure.

As a class, tetracyclines are generally considered second-line antibiotics in pregnant women and their use should be avoided (Mylonas 2011). Minocycline is not recommended for the treatment of Rocky Mountain Spotted Fever (Biggs 2016), Q fever (Anderson 2012), or anthrax infection (Meaney-Delman 2014) in pregnant women. Agents other than minocycline are recommended when systemic antibiotics are needed to treat acne during pregnancy (AAD [Zaenglein 2016]).

Breastfeeding Considerations

Minocycline is present in breast milk (Brogden 1975).

Oral absorption is not affected by dairy products; therefore, oral absorption of minocycline by the breastfed infant would not be expected to be diminished by the calcium in the maternal milk. There have been case reports of black discoloration of breast milk in women taking minocycline (Basler 1985; Hunt 1996).

According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should consider the risk of exposure to the infant and the benefits of treatment to the mother. As a class, tetracyclines have generally been avoided in breastfeeding women due to theoretical concerns that they may permanently stain the teeth of the breastfeeding infant (Chung 2002). Some sources note that breastfeeding can continue during tetracycline therapy (Chung 2002; WHO 2002) but recommend use of alternative medications when possible (WHO 2002). In general, antibiotics that are present in breast milk may cause nondose-related modification of bowel flora. Monitor infants for GI disturbances (Chung 2002; WHO 2002). Long-term use of tetracyclines (eg for the treatment of acne) is not recommended in breastfeeding women (AAD [Zaenglein 2016]).

Monitoring Parameters

LFTs, BUN, renal function with long-term treatment, serum magnesium in patients with renal impairment; if symptomatic for autoimmune disorder, include ANA, CBC; ophthalmologic evaluation if visual disturbances occur. If used for syphilis, obtain follow up serologic tests 3 months after treatment.

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.

Pharmacokinetics

Absorption: Oral: Well absorbed

Distribution: Widely distributed to most body fluids, bile, and tissues; poor CNS penetration; deposits in fat for extended periods; Vd: 0.14 to 0.7 L/kg (Zhanel 2004)

Protein binding: 55% to 96% (Zhanel 2004)

Metabolism: Hepatic to inactive metabolites

Bioavailability: 90% to 100% (Zhanel 2004)

Half-life elimination: IV: 15 to 23 hours; 11 to 16 hours (hepatic impairment); 18 to 69 hours (renal impairment); Oral: 16 hours (range: 11 to 17 hours)

Time to peak: Capsule, pellet filled: 1 to 4 hours; Tablet: 1 to 3 hours; Extended release tablet: 3.5 to 4 hours

Excretion: Urine (5% to 12% excreted unchanged) (Brogden 1975; Zhanel 2004); feces (20% to 34%) (Brogden 1975)

Pharmacokinetics: Additional Considerations

Anti-infective considerations:

Parameters associated with efficacy: Time and concentration dependent, associated with free 24-hour area under the curve (fAUC24)/minimum inhibitory concentration (MIC) (Agwuh 2006; Ambrose 2007; Cunha 2000; Lashinsky 2017).

Acinetobacter baumannii: fAUC24/MIC goal: ≥20 to 25 (1-log kill) (Alfouzan 2017; Tarazi 2019).

Expected drug exposure in normal renal function:

AUC:

Adults:

Oral:

100 mg single dose: AUC0-11: 9.64 ± 3.73 mg•hour/L (range: 3.8 to 19 mg•hour/L) (Maesen 1989).

200 mg, single dose: AUC0-24: ~47 mg•hour/L (Cartwright 1975).

IV:

200 mg, single dose: AUC0-7: 67 mg•hour/L (Agwuh 2006).

Postantibiotic effect: ~2 to 3 hours (B. anthracis) (Athamna 2004).

Pricing: US

Capsule ER 24 Hour Therapy Pack (Minocycline HCl ER Oral)

45 mg (per each): $21.00

90 mg (per each): $21.00

135 mg (per each): $21.00

Capsule ER 24 Hour Therapy Pack (Ximino Oral)

45 mg (per each): $30.48

90 mg (per each): $30.48

135 mg (per each): $30.48

Capsules (Minocycline HCl Oral)

50 mg (per each): $1.70

75 mg (per each): $1.98

100 mg (per each): $1.38 - $3.40

Solution (reconstituted) (Minocin Intravenous)

100 mg (per each): $273.12

Tablet, 24-hour (CoreMino Oral)

45 mg (per each): $16.00

90 mg (per each): $16.00

135 mg (per each): $16.00

Tablet, 24-hour (Minocycline HCl ER Oral)

45 mg (per each): $20.17 - $24.16

55 mg (per each): $39.01 - $43.89

65 mg (per each): $39.01 - $43.88

80 mg (per each): $39.01 - $43.89

90 mg (per each): $20.17 - $24.16

105 mg (per each): $39.01 - $43.89

115 mg (per each): $39.01 - $43.88

135 mg (per each): $20.17 - $24.16

Tablet, 24-hour (Minolira Oral)

105 mg (per each): $29.58

135 mg (per each): $29.58

Tablet, 24-hour (Solodyn Oral)

55 mg (per each): $2.50

65 mg (per each): $2.50

80 mg (per each): $2.50

105 mg (per each): $2.50

115 mg (per each): $2.50

Tablets (Minocycline HCl Oral)

50 mg (per each): $3.43 - $4.35

75 mg (per each): $5.04 - $6.39

100 mg (per each): $6.02

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Acneclin (AR, EC);
  • Akamin (AU);
  • Aknosan (DE);
  • Antinocil (CR, DO, GT, HN, NI, PA, SV);
  • Bagomicina (CL, EC);
  • Borymycin (MY, SG, TW);
  • Cyclimycin (ZA);
  • Cynomycin (IN);
  • Delnil (CL);
  • Dentomycin (GB, IE);
  • Haicin (PH);
  • Kang Ni (CN);
  • Klinomycin (LU);
  • Klinotab (BE);
  • Lederderm (DE);
  • Melicin (TW);
  • Micromycin (CR, DO, GT, HN, MX, NI, PA, SV);
  • Minaxen (MT, TR);
  • Mino-50 (LU);
  • Minocin (AE, BB, BO, BR, CH, CN, EC, ES, GB, GR, HK, ID, IE, IT, KR, KW, LU, MX, NL, PE, PH, PK, PR, PT, PY, SA, SG, UY, VE);
  • Minocin Akne (SI);
  • Minocin MR (MT);
  • Minoclin (IL);
  • Minocyclin (CZ);
  • Minogran (CO);
  • Minolexin (RU);
  • Minoline (HK, TW);
  • Minolox (IN);
  • Minomycin (AU, NZ);
  • Minosil (IE);
  • Minostad (AT);
  • Minot (CO, DO, PE, SV);
  • Minotab (LU);
  • Minotab 50 (BE, ZA);
  • Minotek (NL);
  • Minox (IE);
  • Minoz (IN);
  • Mirosin (TW);
  • Mynocine (FR);
  • Parocline (FR);
  • Periocline (JP);
  • Sebomin (GB);
  • Ximino (BM)


For country abbreviations used in Lexicomp (show table)

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