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Minocycline


General


Pronunciation

(mi noe SYE kleen)


Brand Names: U.S.

  • Dynacin [DSC]
  • Minocin
  • Solodyn

Indications


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 meningitides: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 susceptible Acinetobacter spp, Escherichia coli, Enterobacter aerogenes, Shigella spp

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

Meningitis: Treatment of meningitis due to Neisseria meningitidis

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 skin structure infections: Treatment of skin and skin structure infections caused by Staphylococcus aureus

Limitations of use: 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


Contraindications


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

Documentation of allergenic cross-reactivity for tetracyclines is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.


Dosing and Administration


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

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 (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

Cellulitis (purulent) due to community-acquired MRSA (off-label use): Oral: Initial: 200 mg; Maintenance: 100 mg twice daily for 5-10 days (Liu, 2011)

Chlamydial orUreaplasma urealyticuminfection, 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

Meningococcal carrier state (manufacturers 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, cutaneous (non-CNS) (off-label use): Oral: 100 to 200 mg every 12 hours

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:

Propionibacterium 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 (O 'Dell, 2001)

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


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

Usual dosage range: Children >8 years and Adolescents: Oral, IV: Initial: 4 mg/kg/dose for 1 dose; Maintenance: 2 mg/kg/dose every 12 hours (maximum: 400 mg daily)

Acne (inflammatory, non-nodular, moderate to severe: Children ≥12 years and Adolescents: Oral: Refer to adult dosing.

Cellulitis (purulent) infection due to community-acquired MRSA (off-label use): Oral: Children >8 years: Initial: 4 mg/kg (maximum: 200 mg); Maintenance: 2 mg/kg/dose (maximum: 100 mg) every 12 hours for 5 to 10 days (Liu, 2011)


Dosing: Renal Impairment

Use with caution. Consider decreasing dose or increasing dosing interval (extended release).

CrCl ≥80 mL/minute: No dosage adjustment necessary

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


Dosing: Hepatic Impairment

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


Reconstitution

Injection: Reconstitute with 5 mL of sterile water for injection and immediately further dilute in 100 to 1,000 mL of NS, D5W, D5NS, or 250 mL to 1,000 mL of LR. Note: Preparation instructions are for the reformulated product (containing magnesium) available as of July 2015.


Administration

Note: IV administration instructions are for the reformulated product (containing magnesium) available as of July 2015. Refer to the following for additional information: http://links.mkt1283.com/servlet/MailView?ms=MjMwNTcwMzIS1&r=MTI2NjgzODE5NjE3S0&j=NjAxNDY4MzkzS0&mt=1&rt=0

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 extended-release tablet or capsule whole; do not chew, crush, or split.


Storage

Capsule (including pellet-filled), tablet: Store at 20 ‚ °C to 25 ‚ °C (68 ‚ °F to 77 ‚ °F); protect from heat. Protect from light and moisture.

Extended-release capsule: Store at 20 ‚ °C to 25 ‚ °C (68 ‚ °F to 77 ‚ °F); excursions are permitted to 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F). Protect from light, moisture, and excessive heat.

Extended-release tablet: Store at 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F); protect from heat. Protect from light and moisture.

Injection: Store intact vials at 20 ‚ °C to 25 ‚ °C (68 ‚ °F to 77 ‚ °F). Diluted solution in NS, D5W, D5NS, or LR is stable at room temperature for up to 4 hours or at 2 ‚ °C to 8 ‚ °C (36 ‚ °F to 46 ‚ °F) for up to 24 hours.


Dosage Forms/Strengths


Dosage Forms

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

Capsule, Oral:

Minocin: 50 mg, 75 mg, 100 mg [contains brilliant blue fcf (fd&c blue #1), fd&c yellow #10 (quinoline yellow)]

Generic: 50 mg, 75 mg, 100 mg

Kit, Combination:

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

Solution Reconstituted, Intravenous:

Minocin: 100 mg (1 ea)

Tablet, Oral:

Dynacin: 50 mg [DSC], 75 mg [DSC], 100 mg [DSC]

Generic: 50 mg, 75 mg, 100 mg

Tablet Extended Release 24 Hour, Oral:

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, 90 mg, 135 mg


Compatibility

Stable in NS, D5W, D51/4NS, D51/2NS, D5NS, LR.

Incompatible with calcium-containing solutions (except LR)


Drug Interactions

Aminolevulinic Acid: Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid. Monitor therapy

Antacids: May decrease the absorption of Tetracycline Derivatives. Consider therapy modification

Atazanavir: Minocycline may decrease the serum concentration of Atazanavir. Monitor therapy

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

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

Bile Acid Sequestrants: May decrease the absorption of Tetracycline Derivatives. Consider therapy modification

Bismuth Subcitrate: May decrease the serum concentration of Tetracycline Derivatives. 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. Consider therapy modification

Bismuth Subsalicylate: May decrease the serum concentration of Tetracycline Derivatives. Management: Consider dosing tetracyclines 2 hours before or 6 hours after bismuth. The need to separate doses during Helicobacter pylori eradication regimens is questionable. Consider therapy modification

Calcium Salts: May decrease the serum concentration of Tetracycline Derivatives. Management: If coadministration of oral calcium with oral tetracyclines can not be avoided, consider separating administration of each agent by several hours. Consider therapy modification

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Avoid combination

CNS Depressants: Minocycline may enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Iron Salts: Tetracycline Derivatives may decrease the absorption of Iron Salts. Iron Salts may decrease the serum concentration of Tetracycline Derivatives. Exceptions: Ferric Carboxymaltose; Ferric Gluconate; Ferric Hydroxide Polymaltose Complex; Ferric Pyrophosphate Citrate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Consider therapy modification

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

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

Magnesium Dimecrotate: May interact via an unknown mechanism with Tetracycline Derivatives. Monitor therapy

Magnesium Salts: May decrease the absorption of Tetracycline Derivatives. Only applicable to oral preparations of each agent. Consider therapy modification

Mecamylamine: Tetracycline Derivatives may enhance the neuromuscular-blocking effect of Mecamylamine. Avoid combination

Mipomersen: Tetracycline Derivatives may enhance the hepatotoxic effect of Mipomersen. Monitor therapy

Multivitamins/Minerals (with ADEK, Folate, Iron): May decrease the serum concentration of Tetracycline Derivatives. Management: If coadministration of a polyvalent cation-containing multivitamin with oral tetracyclines can not be avoided, separate administration of each agent by several hours. Consider therapy modification

Multivitamins/Minerals (with AE, No Iron): May decrease the serum concentration of Tetracycline Derivatives. Management: If coadministration of a polyvalent cation-containing multivitamin with oral tetracyclines can not be avoided, separate administration of each agent by several hours. Consider therapy modification

Neuromuscular-Blocking Agents: Minocycline may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Monitor therapy

Penicillins: Tetracycline Derivatives may diminish the therapeutic effect of Penicillins. Consider therapy modification

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

Quinapril: May decrease the serum concentration of Tetracycline Derivatives. Management: Separate doses of quinapril and oral tetracycline derivatives by at least 2 hours in order to reduce the risk of interaction. Monitor for reduced efficacy of the tetracycline if these products are used concomitantly. Consider therapy modification

Retinoic Acid Derivatives: Tetracycline Derivatives may enhance the adverse/toxic effect of Retinoic Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Exceptions: Adapalene; Bexarotene (Topical); Tretinoin (Topical). 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. Consider therapy modification

Strontium Ranelate: May decrease the serum concentration of Tetracycline Derivatives. 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. Avoid combination

Sucralfate: May decrease the absorption of Tetracycline Derivatives. Management: Administer the tetracycline derivative at least 2 hours prior to sucralfate in order to minimize the impact of this interaction. Consider therapy modification

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

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 3 days after cessation of antibacterial agents. Consider therapy modification

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

Vitamin K Antagonists (eg, warfarin): Tetracycline Derivatives may enhance the anticoagulant effect of Vitamin K Antagonists. Monitor therapy

Zinc Salts: May decrease the absorption of Tetracycline Derivatives. Only a concern when both products are administered orally. Management: Consider doxycycline as a noninteracting tetracycline derivative. Separate dose administration of oral tetracycline derivative and oral zinc salts by at least 2 hours to minimize interaction. Exceptions: Zinc Chloride. Consider therapy modification


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.


Lab Test Interferences


Test Interactions

May cause interference with fluorescence test for urinary catecholamines (false elevations)


Adverse Reactions


1% to 10%:

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

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

Neuromuscular & skeletal: Arthralgia (1%)

Otic: Tinnitus (2%)

Postmarketing and/or case reports (Limited to important or life-threatening): Acute renal failure (reversible), autoimmune hepatitis, balanitis, bulging fontanel, Clostridium dificile associated diarrhea, DRESS syndrome, enterocolitis, eosinophilia, erythema multiforme, exacerbation of systemic lupus erythematosus, exfoliative dermatitis, fixed drug eruption, glossitis, hearing loss, hemolytic anemia, hepatic failure, hepatitis, hepatotoxicity (idiosyncratic) (Chalasani 2014), hypersensitivity, IgA vasculitis, lupus-like syndrome, malignant neoplasm of thyroid, microscopic thyroid discoloration (brown-black), mucous membrane pigmentation, myocarditis, pancreatitis, pericarditis, pneumonitis, polyarthralgia, pseudomembranous colitis, pseudotumor cerebri, pulmonary infiltrates (with eosinophilia), serum sickness, skin photosensitivity, skin pigmentation, Stevens-Johnson syndrome, thrombocytopenia, thyroid dysfunction, tooth discoloration, vasculitis


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]): 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).

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed 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; 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.

- Pregnancy: Do not use during pregnancy. In addition to affecting tooth development, tetracycline use has been associated with retardation of skeletal development and reduced bone growth.

- Rheumatoid arthritis (off-label/investigational): Contraindicated in pregnancy and breast-feeding; Child-Pugh Class C and acute hepatitis B and C (Saag KG, 2008).

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.


Pregnancy Risk Factor

D


Pregnancy Considerations

Tetracyclines cross the placenta and accumulate in developing teeth and long tubular bones. 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 may discolor fetal teeth following maternal use during pregnancy; the specific teeth involved and the portion of the tooth affected depends on the timing and duration of exposure relative to tooth calcification. As a class, tetracyclines are generally considered second-line antibiotics in pregnant women and their use should be avoided (Mylonas, 2011). Minocycline should not be used for the treatment of acne in pregnant women, or in males or females attempting to conceive a child.


Actions


Pharmacology

Inhibits bacterial protein synthesis by binding with the 30S and possibly the 50S ribosomal subunit(s) of susceptible bacteria; cell wall synthesis is not affected

Rheumatoid arthritis: The mechanism of action of minocycline in rheumatoid arthritis is not completely understood. It is thought to have antimicrobial, anti-inflammatory, immunomodulatory, and chondroprotective effects. More specifically, it is thought to be a potent inhibitor of metalloproteinases, which are active in rheumatoid arthritis joint destruction.


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)


Metabolism

Hepatic to inactive metabolites


Excretion

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


Time to Peak

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


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)


Protein Binding

55% to 96% (Zhanel 2004)


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience diarrhea, dizziness, fatigue, nausea, vomiting, lack of appetite, or injection site irritation. Have patient report immediately to prescriber signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes), signs of pancreatitis (severe abdominal pain, severe back pain, severe nausea, or vomiting), vision changes, blurred vision, urinary retention, change in amount of urine passed, chills, pharyngitis, hearing impairment, joint pain, joint edema, muscle pain, muscle weakness, tinnitus, seizures, shortness of breath, dysphagia, hematuria, angina, arrhythmia, edema, skin discoloration, eye discoloration, nail discoloration, tooth discoloration, gingival changes, bruising, bleeding, severe loss of strength and energy, stomatitis, redness or white patches in mouth or throat, rectal irritation, genital irritation, vaginitis, headache, diplopia, blindness, enlarged lymph nodes, signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (red, swollen, blistered, or peeling skin [with or without fever]; red or irritated eyes; or sores in mouth, throat, nose, or eyes), or signs of Clostridium difficile (C. diff)-associated diarrhea (stomach pain or cramps, very loose or watery stools, or bloody stools) (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating, and advising patients.

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