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minocycline (Dynacin, Minocin, Minocin Kit, Solodyn, Ximino)

 

Classes: Tetracyclines

Dosing and uses of Dynacin, Minocin (minocycline)

 

Adult dosage forms and strengths

tablet/capsule

  • 50mg
  • 75mg
  • 100mg

tablet, extended-release (Solodyn)

  • 45mg
  • 55mg
  • 65mg
  • 80mg
  • 90mg
  • 105mg
  • 115mg
  • 135mg

injection, intravenous

  • 100mg/vial

 

Acne Vulgaris

50-100 mg PO twice daily

Solodyn (extended-release tablet): 1 mg/kg PO qDay

Administer therapy for 12 weeks

Extended-release tablets

  • 45-49 kg: 45 mg qDay (1-0.92 mg/kg)
  • 50-59 kg: 55 mg qDay (1.1-0.93 mg/kg)
  • 60-71 kg: 65 mg qDay (1.08-0.92 mg/kg)
  • 72-84 kg: 80 mg qDay (1.11-0.95 mg/kg)
  • 85-96 kg: 90 mg qDay (1.06-0.94 mg/kg)
  • 97-110 kg: 105 mg qDay (1.08-0.95 mg/kg)
  • 111-125 kg: 115 mg qDay (1.04-0.92 mg/kg)
  • 126-136 kg: 135 mg qDay (1.07-0.99 mg/kg)

 

Purulent Cellulitis (Off-label)

Community acquired MRSA: 200 mg PO initially

Maintenance: 100 mg PO twice daily for 5-10 days

 

Chlamydial or Ureaplasma Urealyticum

Uncomplicated infection: 100 mg PO q12hr for at least 7 days

 

Gonococcal Infection

Uncomplicated infection in males (no anorectal infections or presence of urethritis: 200 mg PO initially)

Maintenance: 100 mg PO twice daily for at least 4 days

Uncomplicated gonococcal urethritis in men: 100 mg PO q12hr for 5 days

 

Meningococcal Carrier State

100 mg PO q12hr for 5 days

 

Urethral, Endocervical, or Rectal Infections

Caused by C. trachomatis or U. urealyticum (uncomplicated infection): 100 mg PO q12hr for 7 days

 

Mycobacterium marinum

100 mg PO q12hr for 6-8 weeks

 

Syphilis

200 mg PO initially, followed by 100 mg q12hr for 10-15 days

 

Rheumatoid Arthritis (Off-label)

100 mg PO twice daily

 

Infective Endocarditis

100 mg IV twice daily for at least 5 weeks

 

Infections, General Dosing

200 mg PO/IV initially, THEN 100 mg PO/IV q12hr; not to exceed 400 mg/day, Or

Alternatively, 200 mg PO initially, THEN 100 mg PO q12hr; OR 100-200 mg initially; THEN 50 mg PO q6hr

 

Sarcoidosis (Orphan)

Orphan indication sponsor

  • Autoimmunity Research Foundation; Autoimmunity Research, Inc; Thousand Oaks, CA 91360

 

Dosing Considerations

Susceptible organisms

  • Acinetobacter baumannii, Actinomyces spp, Afipia felis, Bacteroides spp, Bartonella bacilliformis, Borrelia recurrentis, Brucella spp, Burkholderia cepacia, Klebsiella granulomatis, Campylobacter jejuni, Chlamydia spp, Clostridium spp, Coxiella burnetii, Eikenella corrodens, Escherichia coli, Entamoeba spp, Francisella tularensis, Haemophilus ducreyi, Legionella pneumophila, Leptospira interrogans, Listeria monocytogenes, Mycoplasma hominis, Mycoplasma pneumoniae, Neisseria meningitidis, Neisseria gonorrhoeae, Nocardia asteroides, Prevotella melaninogenica, Propionibacterium acnes, Rickettsiae, Shigella spp, MRSA, Streptococcus pneumoniae, Streptococcus pyogenes, Treponema pallidum, Ureaplasma urealyticum, Vibrio cholerae, Yersinia pestis, Yersinia enterocolitica, Yersinia pseudotuberculosis, mycobacteria other than tuberculosis

 

Dosing Modifications

Renal impairment: Reduce dose and/or frequency

 

Pediatric dosage forms and strengths

tablet/capsule

  • 50mg
  • 75mg
  • 100mg

tablet, extended-release

  • 45mg
  • 55mg
  • 65mg
  • 80mg
  • 90mg
  • 105mg
  • 135mg

injection, intravenous

  • 100mg/vial

 

Acne Vulgaris

<12 years: Safety and efficacy not established

Immediate-release products: 4 mg/kg PO initially (not to exceed 200 mg), THEN 2 mg/kg/day PO q12hr; not to exceed 400 mg/day

Solodyn (extended-release tablet): 1 mg/kg PO qDay

Administer therapy for 12 weeks

Extended-release tablets

  • 45-49 kg: 45 mg qDay (1-0.92 mg/kg)
  • 50-59 kg: 55 mg qDay (1.1-0.93 mg/kg)
  • 60-71 kg: 65 mg qDay (1.08-0.92 mg/kg)
  • 72-84 kg: 80 mg qDay (1.11-0.95 mg/kg)
  • 85-96 kg: 90 mg qDay (1.06-0.94 mg/kg)
  • 97-110 kg: 105 mg qDay (1.08-0.95 mg/kg)
  • 111-125 kg: 115 mg qDay (1.04-0.92 mg/kg)
  • 126-136 kg: 135 mg qDay (1.07-0.99 mg/kg)

 

C. trachomatis or U. urealyticum

100 mg PO q12hr for 7 days

 

Infections, General Dosing

≤8 years: Not recommended, unless unable to take other, alternate antibiotics

>8 years: 4 mg/kg PO/IV initially; not to exceed 200 mg; THEN 2 mg/kg PO/IV q12hr; not to exceed adult dose; not to exceed 100 mg PO/IV q12hr for 5-10 days

 

Dosing Considerations

Susceptible organisms

  • Acinetobacter baumannii, Actinomyces spp, Afipia felis, Bacteroides spp, Bartonella bacilliformis, Borrelia recurrentis, Brucella spp, Burkholderia cepacia, Klebsiella granulomatis, Campylobacter jejuni, Chlamydia spp, Clostridium spp, Coxiella burnetii, Eikenella corrodens, Escherichia coli, Entamoeba spp, Francisella tularensis, Haemophilus ducreyi, Legionella pneumophila, Leptospira interrogans, Listeria monocytogenes, Mycoplasma hominis, Mycoplasma pneumoniae, Neisseria meningitidis, Neisseria gonorrhoeae, Nocardia asteroides, Prevotella melaninogenica, Propionibacterium acnes, Rickettsiae, Shigella spp, MRSA, Streptococcus pneumoniae, Streptococcus pyogenes, Treponema pallidum, Ureaplasma urealyticum, Vibrio cholerae, Yersinia pestis, Yersinia enterocolitica, Yersinia pseudotuberculosis, mycobacteria other than tuberculosis

 

Dynacin, Minocin (minocycline) adverse (side) effects

Frequency not defined

Discoloration of teeth (in children)

Vestibular symptoms (>30%)

Pericarditis

Myocarditis

Vasculitis

Angioedema

Alopecia

Erythema nodosum

Erythematous rash

Exfoliative dermatitis

Pruritus

Toxic epidermal necrolysis

Urticaria

Dizziness

Fever

Fatigue

Somnolence

Angioedema

Hyperpigmentation of nails

Pigmentation of skin and mucous membranes

Thyroid dysfunction

Thyroid discoloration

Thyroid cancer

Vulvovaginitis

Hemolytic anemia

Neutropenia

Thrombocytopenia

Agrunolocytosis

Pancytopenia

Hepatic cholestasis

Hepatitis

Hyperbilirubinemia

Jaundice

CNS effects

Clostridium difficile diarrhea

 

Warnings

Contraindications

Documented hypersensitivity

 

Cautions

Caution in significant renal impairment (may lead to azotemia, hyperphosphatemia, and acidosis; monitor BUN)

Adjust dose if renal impairment occurs

Anaphylaxis reported; discontinue use and institute supportive therapy

Prolonged use may result in fungal or bacterial superinfection

Lupus, hepatitis, and vasculitis autoimmune syndromes reported with use; discontinue if lupus symptoms occur and assess liver function tests; ANA and CBC

Discontinue therapy if pseudomembranous colitis occurs

Risk of vestibular reactions

Caution in hepatic impairment; discontinue if liver injury occurs

Photosensitivity may occur with prolonged exposure to sunlight or tanning equipment; use skin protection and avoid prolonged exposure to sunlight

Reduce dose in renal impairment; consider drug serum level determinations in prolonged therapy

Tetracycline use during tooth development (last half of pregnancy through age 8 years) can cause tooth enamel hypoplasia or permanent teeth discoloration; more common with long-term use and with repeated, short courses; during pregnancy, may retard skeletal development and reduce bone growth

Fanconi-like syndrome may occur with outdated tetracyclines

Lightheadedness and vertigo may occur; use caution when performing tasks that require mental alertness or operating heavy machinery

May increase BUN secondary to antianabolic effects

Cases of drug rash with eosinophilia and systemic symptoms (DRESS) reported, some fatal; discontinue immediately

Intracranial hypertension (pseudotumor cerebri) has been associated with use of tetracyclines including minocycline; avoid concomitant use of isotretinoin and minocycline; isotretinoin is also known to cause pseudotumor cerebri; although intracranial hypertension typically resolves after discontinuation of treatment, risk of permanent visual loss exists; seek ophthalmologic evaluation if visual disturbance occurs during treatment; since intracranial pressure can remain elevated for weeks after drug cessation, monitor until patient stabilizes

A decrease in fibula growth rate observed in premature human infants given oral tetracycline in doses of 25 mg/kg q6hr

Hyperpigmentation may occur in nails, bone, skin (including scars), eyes, sclerae, thyroid, oral cavity, visceral tissue, and heart valves

Increased risk of ergotism when coadministered with ergot alkaloids

 

Pregnancy and lactation

Pregnancy category: d

Lactation: Enters breast milk, some manufacturers say do not nurse; however AAP considers nursing compatible due to calcium chelation of drug and prevention of its absorption; long-term safety of prolonged exposure unknown

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Dynacin, Minocin (minocycline)

Mechanism of action

Infection: Inhibits protein synthesis and thus bacterial growth by binding to 30S and possibly 50S ribosomal subunits of susceptible bacteria

Rheumatoid arthritis: Mechanism not fully understood; may play immunomodulatory, anti-inflammatory, or chondroprotective effects; thought to be a potent inhibitor of metalloproteinases, which are active in rheumatoid arthritis joint destruction

 

Absorption

Absorption: 90-100%

Peak plasma time: 1-4 hr (immediate release); 3.5-4 hr (extended release tablet)

Peak plasma concentration (200 mg dose): 2-3.5 mcg/mL

 

Distribution

Majority deposits for extended periods in fat; crosses placenta; enters breast milk

Protein bound: 70-75%

 

Metabolism

Liver (partially)

 

Elimination

Half-life, elimination: 15-23 hr (PO/IV)

Excretion: Feces and urine

 

Administration

Incompatibilities

IV solutions: Calcium containing solutions (precipitant may form, particularly with alkaline solutions)

Y-site: Adrenocorticotropic hormone (ACTH), aminophylline, amobarbital sodium, amphotericin B, bicarbonate infusion mixtures, calcium gluconate or chloride, carbenicillin, cephalothin sodium, cefazolin sodium, chloramphenicol succinate, colistin sulfate, heparin sodium, hydrocortisone sodium succinate, iodine sodium, methicillin sodium, novobiocin, penicillin, pentobarbital, phenytoin sodium, polymyxin, prochlorperazine, sodium ascorbate, sulfadiazine, sulfisoxazole, thiopental sodium, vitamin K (sodium bisulfate or sodium salt), whole blood

 

Compatibilities

IV solutions: 0.9% NaCl, dextrose solutions, dextrose and NaCl solutions, Ringer Injection, or Lactated Ringer

 

IV Preparation

Reconstitute cryodessicated powder with 5 mL sterile water for injection

Immediately dilute further with 500-1000 mL of 0.9% NaCl, dextrose solutions, dextrose and NaCl solutions, Ringer Injection, or Lactated Ringer

Reformulated Minocin IV

  • Allows for dilution with lower fluid volume
  • After vial reconstitution, dilute further with 100-1000 mL of 0.9% NaCl, dextrose solutions, dextrose and NaCl solutions, or 250-1000 mL of Ringer or Lactated Ringer injections

 

IV Administration

Avoid rapid IV infusion

Infuse over one hour

Not to exceed 400mg in 24 hours

 

Oral Administration

May take with or without food

Ingestion of food along with may help reduce the risk of esophageal irritation and ulceration

Extended-release tablets or capsules: Swallow whole without chewing, crushing, or splitting

 

Storage

Unreconstituted vial: Store at controlled room temperature 20-25 degrees C (68-77 degrees F)

Final dilutions: Store at controlled room temperature or refrigerated for up to 24 hr

May be stored at room temperature for up to 4 hours