Version July 2025
Dosage guidance:
Dosage form information: Doses presented are for immediate release unless otherwise specified; IR and ER products are not interchangeable.
Usual dosage range:
IV, Oral: 200 mg once, followed by 100 mg every 12 hours (maximum: 400 mg daily). For multidrug-resistant, gram-negative infections (eg, carbapenem-resistant Acinetobacter sp., S. maltophilia) and nocardiosis, some experts recommend 200 mg every 12 hours (Ref).
Acinetobacter baumannii infection, multidrug resistant (alternative agent):
Note: Not recommended for urinary tract infections because of inadequate concentrations (Ref).
IV, Oral: 200 mg every 12 hours as part of an appropriate combination regimen (Ref). For mild skin and soft tissue and respiratory infections with adequate source control some experts use as monotherapy (Ref).
Acne vulgaris, inflammatory, moderate to severe:
Note: Use in combination with topical acne therapy. Some experts prefer other tetracyclines because of adverse effect profiles (Ref). Treatment should ideally be limited to 3 to 4 months to minimize the risk of resistance (Ref).
IR capsule or tablet: Oral: 50 to 100 mg once or twice daily; usual dose: 100 mg twice daily (Ref).
ER capsule (Ximino only) or tablet: Oral: 1 mg/kg once daily, rounded to the nearest dosage form available; maximum dose: 135 mg/day.
ER capsule:
Ximino:
45 to 59 kg: Oral: 45 mg once daily.
60 to 90 kg: Oral: 90 mg once daily.
91 to 136 kg: Oral: 135 mg once daily.
ER tablet:
Minolira:
45 to 59 kg: Oral: 52.5 mg (one-half of the 105 mg tablet) once daily.
60 to 89 kg: Oral: 67.5 mg (one-half of the 135 mg tablet) once daily.
90 to 125 kg: Oral: 105 mg once daily.
126 to 136 kg: Oral: 135 mg once daily.
CoreMino, Solodyn:
45 to 49 kg: Oral: 45 mg once daily.
50 to 59 kg: Oral: 55 mg once daily.
60 to 71 kg: Oral: 65 mg once daily.
72 to 84 kg: Oral: 80 mg once daily.
85 to 96 kg: Oral: 90 mg once daily.
97 to 110 kg: Oral: 105 mg once daily.
111 to 125 kg: Oral: 115 mg once daily.
126 to 136 kg: Oral: 135 mg once daily.
Anthrax:
Note: Consult public health officials for event-specific recommendations.
Postexposure prophylaxis after aerosol exposure: Oral: 200 mg once, followed by 100 mg every 12 hours; duration depends on anthrax vaccine status and series completion, age, immune status, and pregnancy/breastfeeding status. For those who have not previously received an anthrax vaccine, duration ranges from 42 to 60 days (Ref). Some experts favor longer durations of prophylaxis (eg, total of 3 to 4 months) for patients who are immunocompromised or remain unvaccinated (Ref).
Note: Administer anthrax vaccine to exposed individuals (Ref).
Cutaneous, without meningitis, treatment: Oral: 200 mg once, followed by 100 mg every 12 hours for 7 to 10 days after naturally acquired infection. For patients with aerosol exposure, continue for postexposure prophylaxis for a total duration of at least 42 to 60 days, depending on vaccine status, age, pregnancy/breastfeeding status, and immunocompetence (Ref).
Systemic, including meningitis, treatment: IV: 200 mg once, followed by 100 mg every 12 hours, in combination with bactericidal agents; treat for ≥2 weeks; duration may be shortened, and patient transitioned to oral therapy based on response and clinical judgement (Ref). Some experts suggest ≥3 weeks of IV combination therapy for patients with meningitis (Ref). For patients who are immunocompromised and had aerosol exposure, transition to oral postexposure prophylaxis for a total duration of at least 60 days. Administer antitoxin in addition to antibiotics for systemic anthrax (Ref).
Hidradenitis suppurativa (alternative agent) (off-label use): Oral: 100 mg once or twice daily for ≥3 months (Ref).
Leprosy, treatment (alternative agent) (off-label use):
Note: For patients who cannot tolerate first-line therapies due to intolerance, drug interactions, or resistance (Ref).
Drug-susceptible: Oral: 100 mg once daily as part of an appropriate combination regimen for 12 months for tuberculoid (paucibacillary) disease and 24 months for lepromatous (multibacillary) disease (Ref). For resource-limited settings, the World Health Organization recommends 100 mg once daily as part of an appropriate combination regimen for 6 months (paucibacillary) or 12 months (multibacillary) (Ref).
Drug- resistant (eg, rifampin and/or ofloxacin resistant): Oral: 100 mg once daily for 24 months as part of an appropriate combination regimen (Ref).
Nocardiosis (alternative agent) (off-label use):
Note: Confirm susceptibility because of concern for resistance (Ref).
IV, Oral: 100 to 200 mg every 12 hours; for severe or CNS infection, use as part of an appropriate combination regimen (Ref). Total duration including IV and oral therapy ranges from 3 months to ≥1 year depending on extent of infection and patient immune status (Ref).
Perioral (periorificial) dermatitis, moderate to severe (off-label use): Oral: 50 to 100 mg twice daily or 100 mg once daily for 8 weeks (Ref).
Pleurodesis, chemical (sclerosing agent for prevention of recurrent pleural effusion/pneumothorax) (off-label use): Intrapleural: 150 to 400 mg (usual dose: 300 mg) as a single dose in 20 to 100 mL NS or D5W (Ref); may be combined with or administered following instillation of a local anesthetic (Ref).
Prosthetic joint infection (alternative agent) (off-label use):
Note: For use after pathogen-specific IV therapy in patients undergoing 1-stage exchange or debridement with retention of prosthesis (Ref).
Oral: 100 mg twice daily for ≥3 months, depending on patient-specific factors; for staphylococcus, use in combination with rifampin (Ref).
Pyoderma gangrenosum (alternative agent) (off-label use): Oral: 100 mg twice daily for 6 to 8 weeks (Ref).
Rosacea: Note: For severe, papulopustular lesions, or cases unresponsive to topical therapy (Ref).
ER capsule (Emrosi only): Oral: 40 mg once daily.
IR capsule or tablet (off-label use): Oral: 50 to 100 mg twice daily for 4 to 12 weeks; may follow with a topical agent and/or subantimicrobial doxycycline dosing for long-term management (Ref).
Skin and soft tissue infection:
Abscess:
Note: Systemic antibiotics may be reasonably withheld in patients who are healthy and immunocompetent with a single, small abscess that has been drained if they are clinically well and have no indwelling device, risk factors for endocarditis, or risk for MRSA transmission (Ref).
Oral: 200 mg once followed by 100 mg twice daily (Ref). Treat for ≥5 days but may extend up to 14 days depending on severity and clinical response (Ref).
Cellulitis, purulent or with risk for methicillin-resistant S. aureus (alternative agent): Oral: 200 mg once followed by 100 mg twice daily in combination with an additional agent (eg, amoxicillin, cephalexin) for coverage of beta-hemolytic streptococci. Treat for ≥5 days but may extend up to 14 days depending on severity and clinical response (Ref).
Stenotrophomonas maltophilia infection (off-label use):
Note: Not recommended for urinary tract infections because of inadequate concentrations (Ref).
IV, Oral: 200 mg every 12 hours as part of an appropriate combination regimen (Ref); for mild infections in patients who are immunocompetent, some experts use as monotherapy (Ref).
Vibrio vulnificus infection (off-label use):
Bloodstream or severe wound infection: IV, Oral: 100 mg every 12 hours as part of an appropriate combination regimen for ~7 to 14 days; may consider transition to oral monotherapy after clinical improvement (Ref).
Mild wound infection: Note: For patients with risk factors for severe disease (eg, chronic liver disease, immunocompromising condition), treat as severe wound infection (Ref).
Oral: 100 mg every 12 hours for 5 to 7 days depending on clinical response (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Altered kidney function:
Oral, IV: No dosage adjustment necessary for any degree of kidney dysfunction (Ref). Note: Theoretically, minocycline doses >200 mg/day may increase plasma urea concentrations due to antianabolic effects. Therefore, patients with kidney impairment requiring doses >200 mg/day should be frequently monitored for increased BUN, serum creatinine, and/or signs and symptoms of uremia (Ref).
Augmented renal clearance (measured urinary CrCl ≥130 mL/minute/1.73 m2):
Note: Augmented renal clearance (ARC) is a condition that occurs in certain critically ill patients without organ dysfunction and with normal serum creatinine concentrations. Younger patients (<55 years of age) admitted post trauma or major surgery are at highest risk for ARC, as well as those with sepsis, burns, or hematologic malignancies. An 8- to 24-hour measured urinary CrCl is necessary to identify these patients (Ref).
Oral, IV: No dosage adjustment necessary (Ref).
Hemodialysis, intermittent (thrice weekly): Not dialyzable (Ref):
Oral, IV: No dosage adjustment necessary (Ref).
Peritoneal dialysis: Not dialyzable (Ref):
Oral, IV: No dosage adjustment necessary (Ref).
CRRT: Oral, IV: No dosage adjustment necessary (Ref).
PIRRT (eg, sustained, low-efficiency diafiltration): Oral, IV: No dosage adjustment necessary (Ref).
There are no dosage adjustments provided in the manufacturer's labeling; however, hepatotoxicity has been reported. Use with caution.
Refer to adult dosing.
(For additional information see "Minocycline (systemic): Pediatric drug information")
General dosing:
Children >8 years and Adolescents:
Oral: Immediate-release formulations: 4 mg/kg once (maximum dose: 200 mg), then 2 mg/kg/dose every 12 hours (maximum dose: 100 mg/dose).
IV: 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 vulgaris, inflammatory, moderate to severe: Note: Limit use when possible to avoid the development of antibiotic resistance and other complications. Should not be used as monotherapy for the management of acne vulgaris (Ref).
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, topical retinoids) (Ref). Duration of 4 to 8 weeks of therapy usually necessary to evaluate initial clinical response. Limit to shortest duration possible, typically no more than 3 to 4 months, although patients with inadequate response or who cannot use other therapies may need longer courses (Ref).
Extended-release formulations: Children ≥12 years and Adolescents:
Weight-directed dosing: Oral: ~1 mg/kg/dose once daily for 12 weeks (maximum dose: 135 mg/dose).
Fixed dosing (product-specific):
Extended-release capsule:
Ximino:
45 to 59 kg: Oral: 45 mg once daily.
60 to 90 kg: Oral: 90 mg once daily.
91 to 136 kg: Oral: 135 mg once daily.
Extended-release tablet:
Minolira:
45 to 59 kg: Oral: 52.5 mg (one-half of the 105 mg tablet) once daily.
60 to 89 kg: Oral: 67.5 mg (one-half of the 135 mg tablet) once daily.
90 to 125 kg: Oral: 105 mg once daily.
126 to 136 kg: Oral: 135 mg once daily.
CoreMino, Solodyn:
45 to 49 kg: Oral: 45 mg once daily.
50 to 59 kg: Oral: 55 mg once daily.
60 to 71 kg: Oral: 65 mg once daily.
72 to 84 kg: Oral: 80 mg once daily.
85 to 96 kg: Oral: 90 mg once daily.
97 to 110 kg: Oral: 105 mg once daily.
111 to 125 kg: Oral: 115 mg once daily.
126 to 136 kg: Oral: 135 mg once daily.
Anthrax:
Note: Consult public health officials for event-specific recommendations; do not delay therapy. When a tetracycline is used in patients <8 years of age, doxycycline is generally preferred, as tooth discoloration may occur less often (with short durations of therapy) compared to other tetracyclines (Ref).
Postexposure prophylaxis (alternative agent): Limited data available: Infants, Children, and Adolescents. Oral: 4 mg/kg once (maximum dose: 200 mg), then 2 mg/kg/dose (maximum dose: 100 mg/dose) every 12 hours. Continue for 60 days after an aerosol exposure or 7 days after a nonaerosol exposure (ie, cutaneous or ingestion) (Ref).
Cutaneous, without meningitis, treatment: Infants, Children, and Adolescents (limited data available in ages ≤8 years): Oral: 4 mg/kg once (maximum dose: 200 mg), then 2 mg/kg/dose (maximum dose: 100 mg/dose) every 12 hours for 7 to 10 days or patient is clinically stable. For patients who had an aerosol exposure, continue for postexposure prophylaxis for a total of 60 days from exposure (Ref).
Systemic, including meningitis, treatment: Infants, Children, and Adolescents (limited data available in ages ≤8 years): IV: 4 mg/kg once (maximum dose: 200 mg), then 2 mg/kg/dose (maximum dose: 100 mg/dose) every 12 hours as part of an appropriate combination regimen for ≥2 weeks; duration may be shortened and patient transitioned to oral therapy (at same dose) based on clinical response. Following completion of initial therapy, patients who had an aerosol exposure who are immunocompromised should continue oral therapy for postexposure prophylaxis for a total of 60 days from onset of illness (Ref).
Plague (Yersinia pestis) (alternative agent):
Note: Consult public health officials for event-specific recommendations; do not delay therapy. Minocycline should only be used in patients <8 years of age when other treatment options are not available (Ref).
Prophylaxis, postexposure: Limited data available: Infants, Children, and Adolescents: Oral: 2 mg/kg/dose every 12 hours for 7 days; maximum dose: 100 mg/dose (Ref).
Treatment, bubonic or pharyngeal: Infants, Children, and Adolescents (limited data available in ages ≤8 years): Oral, IV: 4 mg/kg once as a single dose (maximum dose: 200 mg/dose), then 2 mg/kg/dose (maximum dose: 100 mg/dose) every 12 hours for 10 to 14 days (Ref).
Pneumonia, community acquired (Mycoplasma pneumoniae) (alternative agent):
Children >8 years and Adolescents: Oral, IV: 4 mg/kg once as a single dose (maximum dose: 200 mg/dose), followed by 2 mg/kg/dose (maximum dose: 100 mg/dose) every 12 hours (Ref). Typical duration is 5 to 14 days, although reported duration varies (Ref).
Skin and soft tissue infection (ie, purulent cellulitis), community-acquired methicillin-resistant Staphylococcus aureus: Note: Treatment duration based on clinical response; usual duration is 5 to 10 days for outpatient cellulitis (Ref).
Children >8 years and Adolescents: Immediate-release formulations: Oral: 4 mg/kg once (maximum dose: 200 mg), then 2 mg/kg/dose (maximum dose: 100 mg/dose) every 12 hours (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Altered kidney function:
IV, Oral: There are no pediatric-specific dosage adjustments provided by the manufacturer; based on experience in adult patients, no dosage adjustment necessary for any degree of kidney dysfunction. Note: In adults, minocycline doses >200 mg/day may theoretically increase plasma urea concentrations due to antianabolic effects. Therefore, patients with kidney impairment requiring higher doses (eg. doses >200 mg/day) should be frequently monitored for increased BUN, serum creatinine, and/or signs and symptoms of uremia (Ref).
Hemodialysis: Not dialyzable (Ref).
There are no dosage adjustments provided in the manufacturer's labeling; however, hepatotoxicity has been reported. Use with caution.
Bone growth suppression, as evidenced by growth retardation (fibula), has been reported in premature infants treated with tetracycline; growth restriction up to 40% has been associated with oral tetracycline therapy but is reversible when short-term treatment is discontinued. Upon discontinuation of tetracycline, rapid compensatory bone growth is observed (Ref). There are limited/no data with minocycline; therefore, the risk for bone growth suppression is extrapolated from data with tetracycline.
Mechanism: Dose-related; tetracycline binds to calcium in growing bones and negatively affects calcium orthophosphate metabolism (Ref).
Onset: Intermediate; deposition of tetracycline in bone has been shown after one dose and treatment with tetracycline for 9 to 12 days has resulted in restricted bone growth (Ref).
Risk factors:
• Dose; tetracycline 25 mg/kg/dose every 6 hours in premature infants (Ref)
• Age: Premature infants (Ref)
Minocycline is associated with dizziness, tinnitus, and vertigo, which are often mild and reversible within 48 hours after discontinuation (Ref).
Mechanism: Unknown; readily crosses the blood-brain barrier, impacts microglia activation and cytokine expression (Ref). Peak minocycline serum concentrations correlate with the peak onset of adverse reactions; however, lower doses do not appear to improve adverse reaction profile with short treatment courses (Ref).
Onset: Rapid; usually within 2 to 3 days of initiation (Ref).
Idiopathic intracranial hypertension (ie, pseudotumor cerebri) has been associated with minocycline (Ref). Symptoms include headache (predominant symptom), blurred vision, diplopia, vision loss, and/or papilledema. Intracranial hypertension is typically benign and resolves with discontinuation; however, permanent vision loss is possible (Ref). Intracranial pressure may remain elevated for 2 to 5 weeks after discontinuation (Ref). Idiopathic intracranial hypertension has been reported in infants following tetracycline exposure, manifested by bulging fontanel (Ref).
Mechanism: Unknown; proposed that minocycline reduces cerebrospinal fluid absorption at the arachnoid villi, leading to increased intracranial pressure (Ref).
Onset: Varied; generally within 8 weeks of initiation (range <1 week to 1 year) (Ref).
Risk factors:
• Concurrent isotretinoin (Ref)
• Females of childbearing age (especially those who are overweight, obese, have experienced recent weight gain, or have a history of intracranial hypertension) (Ref)
Minocycline may cause hepatotoxicity (ranging from mild elevations in serum aminotransferase levels to hepatic failure [including fatal cases]) (Ref). Liver injury may present as an acute hepatitis-like syndrome, or a chronic autoimmune hepatitis, usually with hepatocellular pattern of enzyme elevation (Ref). Autoantibodies are usually present with autoimmune hepatitis, typically antinuclear antibody (ANA) at titers of >1:160 (Ref). Most cases of hepatotoxicity resolve within 3 months after discontinuation of therapy (Ref). Some cases may require treatment; persistent and severe injury has been reported (Ref). Hepatic failure is rare (Ref).
Mechanism: Non–dose-related; not clearly established, immunologic (Ref).
Onset: Varied; acute hepatitis: 3 to 4 weeks after initiation (Ref). Autoimmune hepatitis: generally occurs with prolonged therapy (average within 2 years but may occur within a few months after initiation) (Ref).
Risk factors:
• First month of use (Ref)
Hypersensitivity reactions include immediate (eg, anaphylaxis) (Ref) and delayed reactions. Drug reaction with eosinophilia and systemic symptoms (DRESS) has been reported (Ref). Although the liver is the main organ affected, meningitis, myocarditis, and pneumonitis may also occur (Ref). DRESS may have a prolonged course with development of autoimmune syndromes, including diabetes mellitus, hepatitis, thyroiditis, and vasculitis (Ref). Other cutaneous reactions that have been associated with minocycline include serum sickness-like reaction (Ref), Stevens-Johnson syndrome/toxic epidermal necrolysis (SJS/TEN) (Ref), Sweet syndrome (Ref), fixed drug eruption (Ref) and lupus-like syndrome, usually with positive ANA antibodies (Ref).
Mechanism: Non–dose-related; immunologic (Ref). Immediate hypersensitivity reactions (eg, anaphylaxis, urticaria) are IgE-mediated. Delayed hypersensitivity reactions are T-cell mediated (Ref), triggered by minocycline or a reactive metabolite (Ref). Prolonged courses of DRESS may be the result of accumulation of melanin-minocycline complex in patients with pigmented skin (Ref).
Onset: Immediate hypersensitivity reactions: Rapid; occur within 1 hour of administration but may occur up to 6 hours after exposure (Ref). Delayed hypersensitivity reactions: Varied; DRESS has been reported 16 to 60 days after initiation (mean 23.7 days) (Ref), and serum sickness-like reactions approximately 16 days (Ref). Lupus-like syndrome occurs from 3 months to 6 years (median 22.5 months) (Ref).
Risk factors:
• Longer duration of use (for autoimmune syndromes) (Ref)
• African or West Indian origin (Ref)
• Females (for lupus-like syndrome) (Ref)
• Cross-reactivity between minocycline and other tetracyclines is unknown (Ref)
• Viral reactivation, in particular human herpesvirus 6 (HHV-6) has been associated with DRESS (Ref)
• Increased risk with minocycline for DRESS and autoimmune syndromes compared to other tetracyclines (Ref)
• Genetic variants (for lupus-like syndrome) (Ref)
Minocycline may cause skin photosensitivity reactions ranging from mild sunburn-like reactions to photodermatitis. However, minocycline is less phototoxic than other tetracyclines (eg, doxycycline) (Ref). Reactions have not been reported with topical minocycline (Ref). Phototoxic reactions are restricted to exposed skin, usually develop shortly after sun exposure, and appear to be dose-related (Ref). Photo-onycholysis has also been reported, which may take up to 6 months to resolve after discontinuation (Ref).
Mechanism: Dose-related; minocycline absorbs light energy resulting in subsequent photochemical reactions in living tissues (Ref).
Onset: Varied; photosensitivity occurs <24 hours after sun exposure (Ref). Photo-onycholysis may occur weeks after sun exposure (Ref).
Minocycline may induce diffuse skin hyperpigmentation (brown, bluish-grey, and/or black discoloration) including nails, skin of face, arms, legs, or around scars and dental discoloration (staining of tooth) (Ref). Hyperpigmentation may be more prevalent with minocycline than doxycycline and associated with a greater variety of tissues (eg, bone, conjunctiva and sclera, ear tympanic membrane, internal organs, nails, subcutaneous fat, teeth and oral mucosa, and thyroid) (Ref). Minocycline hyperpigmentation and dental discoloration may be partially reversible, but permanent in some cases (Ref). Discoloration may be amenable to vital bleaching (Ref). Minocycline may affect fully erupted teeth compared to tetracycline, which may cause dental staining and enamel hypoplasia in unerupted, uncalcified teeth. Furthermore, the gingival third of the crown tends to be spared in minocycline staining compared with tetracycline (Ref).
Mechanism: Dose- and time-related; minocycline may mineralize tissue as it binds to calcium/iron to form a tetracycline-calcium/iron orthophosphate complex and/or activate melanocytes in the upper dermis (Ref).
Onset: Delayed; months to years (Ref).
Risk factors:
• Higher doses (≥100 mg daily) (Ref)
• Long-term use (>1 to 2 months) (Ref)
• Sun-exposed areas of skin with higher density of melanocytes (Ref)
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Dermatologic: Pruritus (5%), urticaria (2%)
Gastrointestinal: Dyspepsia (2%)
Nervous system: Dizziness (9%) (table 1), drowsiness (2%), fatigue (9%), malaise (4%)
|
Drug (Minocycline [Systemic]) |
Placebo |
Dose |
Dosage Form |
Number of Patients (Minocycline [Systemic]) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|
|
9% |
5% |
1 mg/kg |
Extended-release tablets |
674 |
364 |
Neuromuscular & skeletal: Arthralgia (1%)
Otic: Tinnitus (2%) (table 2)
|
Drug (Minocycline [Systemic]) |
Placebo |
Dose |
Dosage Form |
Number of Patients (Minocycline [Systemic]) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|
|
2% |
1% |
1 mg/kg |
Extended-release tablets |
674 |
364 |
Postmarketing:
Cardiovascular: Myocarditis (Ref), pericarditis (Ref), vasculitis (including polyarteritis nodosa) (Ref)
Dermatologic: Erythema multiforme (Ref), exfoliative dermatitis (Ref), fixed drug eruption (Ref), onycholysis (Ref), skin hyperpigmentation (Ref), skin photosensitivity (Ref), skin pigmentation (Ref), skin rash, Stevens-Johnson syndrome (Ref), Sweet syndrome (Ref), toxic epidermal necrolysis (Ref)
Endocrine & metabolic: Abnormal thyroid function test (Ref), diabetes mellitus (Ref), malignant neoplasm of thyroid (Ref), microscopic thyroid discoloration (Ref), thyroiditis (Ref)
Gastrointestinal: Clostridioides difficile colitis, Clostridioides difficile-associated diarrhea, diarrhea, dysphagia, enamel hypoplasia, enterocolitis, glossitis, mucous membrane hyperpigmentation (Ref), pancreatitis (Ref), parotitis (bilateral) (Ref), staining of tooth (Ref)
Genitourinary: Balanitis
Hematologic & oncologic: Eosinophilia, hemolytic anemia (Ref), Henoch-Schonlein purpura, lymphadenopathy (Ref), thrombocytopenia (Ref)
Hepatic: Autoimmune hepatitis (Ref), hepatic failure (Ref), hepatitis, hepatotoxicity (Ref)
Hypersensitivity: Anaphylaxis (Ref), angioedema (Ref), drug reaction with eosinophilia and systemic symptoms (Ref), nonimmune anaphylaxis (Ref), serum sickness (Ref), serum sickness-like reaction (Ref)
Nervous system: Bulging fontanel (Ref), intracranial hypertension (Ref), meningitis (Ref), vertigo
Neuromuscular & skeletal: Arthritis, exacerbation of systemic lupus erythematosus (Ref), joint stiffness, joint swelling, lupus-like syndrome (Ref), myalgia, polyarthralgia
Otic: Hearing loss, vestibular ototoxicity (Ref)
Renal: Acute kidney injury (Ref), nephritis (including acute intestinal nephritis) (Ref)
Respiratory: Pneumonitis (including eosinophilic pneumonitis) (Ref), pulmonary infiltrates (Ref), respiratory failure (Ref)
Miscellaneous: Fever
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
Concerns related to adverse effects:
• 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: Use with caution in patients with hepatic impairment or in conjunction with other hepatotoxic drugs.
• Renal impairment: Use with caution in patients with kidney impairment. see "Dosing: Altered Kidney Function" for additional information.
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; avoid use of minocycline 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. Also use with caution and closely monitor patients with heart block or myocardial damage.
Minocin for injection contains magnesium 2.2 mEq per vial.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule, Oral:
Generic: 50 mg, 75 mg, 100 mg
Capsule Extended Release 24 Hour, Oral, as hydrochloride:
Emrosi: 40 mg
Capsule Extended Release 24 Hour, Oral, as hydrochloride [strength expressed as base]:
Ximino: 90 mg [DSC] [contains fd&c blue #1 (brilliant blue)]
Ximino: 135 mg [DSC] [contains fd&c blue #1 (brilliant blue), fd&c yellow #6 (sunset yellow)]
Ximino: 45 mg [DSC] [contains fd&c blue #1 (brilliant blue), fd&c yellow #6 (sunset yellow), quinoline yellow (d&c yellow #10)]
Generic: 135 mg [DSC], 45 mg [DSC], 90 mg [DSC]
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 [DSC], 90 mg [DSC], 135 mg [DSC]
Minolira: 105 mg [DSC], 135 mg [DSC] [scored]
Solodyn: 55 mg [DSC] [contains fd&c red #40 (allura red ac dye)]
Solodyn: 65 mg [DSC] [contains fd&c blue #1 (brilliant blue), fd&c blue #2 (indigotine,indigo carmine), quinoline yellow (d&c yellow #10)]
Solodyn: 80 mg [DSC] [contains fd&c blue #2 (indigotine,indigo carmine), fd&c red #40 (allura red ac dye), fd&c yellow #6 (sunset yellow)]
Solodyn: 105 mg [DSC] [contains fd&c blue #1 (brilliant blue)]
Solodyn: 115 mg [DSC] [contains fd&c blue #1 (brilliant blue), fd&c blue #2 (indigotine,indigo carmine), quinoline yellow (d&c yellow #10)]
Generic: 45 mg, 55 mg, 65 mg, 80 mg, 90 mg, 105 mg, 115 mg, 135 mg
May be product dependent
Capsule ER 24 Hour Therapy Pack (Emrosi Oral)
40 mg (per each): $51.92
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): $310.20
Tablet, 24-hour (Minocycline HCl ER Oral)
45 mg (per each): $24.08
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): $24.08
105 mg (per each): $39.01 - $43.89
115 mg (per each): $39.01 - $43.88
135 mg (per each): $24.08
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
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Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Generic: 50 mg, 100 mg
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 ER tablets or capsules. 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.
Parenteral: IV: Infuse over 60 minutes; avoid rapid administration. Prolonged IV therapy may be associated with thrombophlebitis; the injectable route should be used only if the oral route is not feasible or adequate.
Oral: Administer with plenty of fluids with or without food; administration with adequate amounts of fluid may reduce the risk of esophageal irritation and ulceration.
Immediate-release formulations: Swallow capsules whole.
Extended-release formulations:
Capsules: Ximino: Swallow whole; do not chew, crush, or split.
Tablets:
CoreMino, Solodyn: Swallow whole; do not chew, crush, or split.
Minolira: Do not crush or chew. Minolira 105 mg and 135 mg extended-release tablets may be split on the score line.
Acute intestinal amebiasis: Adjunctive therapy to amebicides in the treatment of acute intestinal amebiasis.
Acne vulgaris, inflammatory, moderate to severe:
Oral (immediate release) and IV: Adjunctive therapy for the treatment of severe acne.
Oral (ER capsule [Ximino only] or tablet): 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.
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.
Meningococcal disease, chemoprophylaxis after close contact with a patient with invasive disease : Oral (immediate-release): To prevent meningococcal disease after exposure to a close contact with N. meningitidis infection. Note: CDC recommendations do not mention minocycline for eradicating nasopharyngeal carriage of meningococcus (CDC [McNamara 2022]).
Mycobacterial infection: Treatment of infection caused by Mycobacterium marinum.
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.
Rosacea (ER capsule [Emrosi only]): Treatment of inflammatory lesions (papules and pustules) of rosacea in adults.
Limitations of use: Emrosi has not been evaluated for the treatment or prevention of infections; use only as indicated.
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. Treatment of uncomplicated urethritis in males due to Neisseria gonorrhoeae and other gonococcal infections are FDA-approved uses in the manufacturer’s prescribing information, but clinical practice guidelines do not recommend tetracyclines for the treatment of gonorrhea because of increased resistance (CDC [Workowski 2021]).
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.
Hidradenitis suppurativa; Leprosy; Nocardiosis; Perioral dermatitis, moderate to severe; Pleurodesis, chemical (sclerosing agent for prevention of recurrent pleural effusion/pneumothorax); Prosthetic joint infection; Pyoderma gangrenosum; Stenotrophomonas maltophilia infection; Vibrio vulnificus infection
Dynacin may be confused with Dyazide, Dynapen
Minocin may be confused with Indocin, Lincocin, Minizide, niacin
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Aminolevulinic Acid (Systemic): Photosensitizing Agents may increase photosensitizing effects of Aminolevulinic Acid (Systemic). Risk X: Avoid
Aminolevulinic Acid (Topical): Photosensitizing Agents may increase photosensitizing effects of Aminolevulinic Acid (Topical). Risk C: Monitor
Antacids: May decrease 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 serum concentration of Atazanavir. Risk C: Monitor
Bacillus clausii: Antibiotics may decrease therapeutic effects of Bacillus clausii. Management: Bacillus clausii should be taken in between antibiotic doses during concomitant therapy. Risk D: Consider Therapy Modification
BCG (Intravesical): Antibiotics may decrease therapeutic effects of BCG (Intravesical). Risk X: Avoid
BCG Vaccine (Immunization): Antibiotics may decrease therapeutic effects of BCG Vaccine (Immunization). Risk C: Monitor
Bile Acid Sequestrants: May decrease absorption of Tetracyclines. Risk C: Monitor
Bismuth Subcitrate: May decrease 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 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 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 decrease therapeutic effects 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
CNS Depressants: Minocycline (Systemic) may increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Fecal Microbiota (Live) (Oral): May decrease therapeutic effects of Antibiotics. Risk X: Avoid
Fecal Microbiota (Live) (Rectal): Antibiotics may decrease therapeutic effects of Fecal Microbiota (Live) (Rectal). Risk X: Avoid
Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies): Antibiotics may decrease therapeutic effects of Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies). Risk C: Monitor
Iron Preparations: Tetracyclines may decrease absorption of Iron Preparations. Iron Preparations may decrease 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 decrease therapeutic effects of Lactobacillus and Estriol. Risk C: Monitor
Lanthanum: May decrease serum concentration of Tetracyclines. Management: Administer oral tetracycline antibiotics at least 2 hours before or after lanthanum. Risk D: Consider Therapy Modification
Lithium: Tetracyclines may increase serum concentration of Lithium. Risk C: Monitor
Magnesium Dimecrotate: And Tetracyclines may interact via an unclear mechanism. Risk C: Monitor
Magnesium Salts: May decrease 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 increase neuromuscular-blocking effects of Mecamylamine. Risk X: Avoid
Methotrexate: Tetracyclines may increase serum concentration of Methotrexate. Risk C: Monitor
Methoxsalen (Systemic): Photosensitizing Agents may increase photosensitizing effects of Methoxsalen (Systemic). Risk C: Monitor
Methoxyflurane: Tetracyclines may increase nephrotoxic effects of Methoxyflurane. Risk X: Avoid
Multivitamins/Minerals (with ADEK, Folate, Iron): May decrease 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 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
Mycophenolate: Antibiotics may decrease active metabolite exposure of Mycophenolate. Specifically, concentrations of mycophenolic acid (MPA) may be reduced. Risk C: Monitor
Neuromuscular-Blocking Agents: Minocycline (Systemic) may increase neuromuscular-blocking effects of Neuromuscular-Blocking Agents. Risk C: Monitor
Penicillins: Tetracyclines may decrease therapeutic effects of Penicillins. Risk C: Monitor
Polyethylene Glycol-Electrolyte Solution: May decrease absorption of Tetracyclines. Management: Give oral tetracyclines at least 2 hours before or at least 6 hours after polyethylene glycol-electrolyte solutions that contain magnesium sulfate (Suflave brand). Other products without magnesium do not require dose separation. Risk D: Consider Therapy Modification
Porfimer: Photosensitizing Agents may increase photosensitizing effects of Porfimer. Risk X: Avoid
Quinapril: May decrease serum concentration of Tetracyclines. Risk C: Monitor
Retinoic Acid Derivatives: Tetracyclines may increase adverse/toxic effects of Retinoic Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Risk X: Avoid
Sodium Bicarbonate (Systemic): May decrease serum concentration of Tetracyclines. Risk C: Monitor
Sodium Picosulfate: Antibiotics may decrease therapeutic effects 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 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
Sucralfate: May decrease 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 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 increase hypoglycemic effects of Sulfonylureas. Risk C: Monitor
Typhoid Vaccine: Antibiotics may decrease therapeutic effects 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 increase photosensitizing effects of Verteporfin. Risk C: Monitor
Vitamin K Antagonists: Tetracyclines may increase anticoagulant effects of Vitamin K Antagonists. Risk C: Monitor
Zinc Salts: May decrease 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
Minocycline serum concentrations are not significantly altered if taken with food or dairy products. Management: Administer without regard to food.
ER capsule (Emrosi): Administration with a high fat meal delayed Tmax 3 hours and increased AUC by ~15%; Cmax was not affected. Management: Administer without regard to food.
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.
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 patients and their use should be avoided (Mylonas 2011).
Untreated plague (Yersinia pestis) infection in pregnant patients may result in hemorrhage (including postpartum hemorrhage), maternal and fetal death, preterm birth, and stillbirth. Limited data suggest maternal-fetal transmission of Y. pestis can occur if not treated. Pregnant patients should be treated for Y. pestis; parenteral antibiotics are preferred for initial treatment when otherwise appropriate. Minocycline may be used as an alternative antibiotic for pre- and postexposure prophylaxis in pregnant patients exposed to Y. pestis (CDC [Nelson 2021]).
Minocycline is not recommended for the treatment of Rocky Mountain Spotted Fever (Biggs 2016), Q fever (Anderson 2012), or anthrax infection (CDC [Bower 2023]) in pregnant patients. Agents other than minocycline are recommended when systemic antibiotics are needed to treat acne during pregnancy (AAD [Zaenglein 2016]).
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 patients 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 patients (AAD [Zaenglein 2016]).
Mental alertness; LFTs, BUN, renal function with long-term treatment, 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); if symptomatic for autoimmune disorder, include ANA, CBC; ophthalmologic evaluation if visual disturbances occur; intracranial pressure until stabilization in patients with idiopathic intracranial hypertension. If used for syphilis, obtain follow up serologic tests 3 months after treatment.
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.
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; ER tablet: 3.5 to 4 hours; ER capsule (Emrosi): 1.5 hours (administration with food delays Tmax ~3 hours).
Excretion: Urine (5% to 12% excreted unchanged) (Brogden 1975; Zhanel 2004); feces (20% to 34%) (Brogden 1975).
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).
