minocycline (systemic)

Inhibit bacterial protein synthesis at the level of the 30S bacterial ribosome.

Therapeutic effects:

Bacteriostatic action against susceptible bacteria.

Spectrum:

Include activity against some gram-positive pathogens:
- Bacillus anthracis,
- Listeria monocytogenes,
- Staphylococcus aureus,
- Streptococcus pneumoniae.
Active against some gram-negative pathogens:
- Acinetobacter spp.,
- Bartonella bacilliformis,
- Brucella spp.,
- Campylobacter fetus,
- Escherichia coli,
- Francisella tularensis,
- Haemophilus ducreyi,
- Haemophilus influenzae,
- Klebsiella aerogenes,
- Klebsiella granulomatis,
- Neisseria gonorrhoeae,
- Neisseria meningitidis,
- Shigella spp.,
- Vibrio cholerae,
- Yersinia pestis.
Also active against several other pathogens, including:
- Actinomyces spp.,
- Borrelia recurrentis,
- Chlamydophila psittaci,
- Chlamydia trachomatus,
- Clostridium spp.,
- Entamoeba spp.,
- Fusobacterium nucleatum,
- Mycobacterium marinum,
- Mycoplasma pneumoniae,
- Proprionibacterium acnes,
- Rickettsiae,
- Treponema pallidum,
- Ureaplasma urealyticum.

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed from the GI tract. IV administration results in complete bioavailability.

Distribution: Widely distributed, some CSF and good bone penetration.

Metabolism/Excretion: 5–20% excreted unchanged by the urine; some metabolism by the liver with enterohepatic circulation and excretion in bile and feces.

Half-Life: 11–26 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	2–3 hr	6–12 hr
PO—ER	unknown	3.5–4 hr	24 hr
IV	unknown	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to any of the tetracyclines;
Some products contain alcohol or bisulfites and should be avoided in patients with known hypersensitivity or intolerance;
OB: Risk of permanent staining of teeth in infant if used during last half of pregnancy;
Lactation: Lactation;
Pedi: Children 8 yr (permanent staining of teeth).

Use Cautiously in:

Cachectic or debilitated patients;
Renal impairment;
Hepatic impairment;
Nephrogenic diabetes insipidus;
Rep: Women of reproductive potential ( risk of intracranial hypertension if overweight or have a previous history of intracranial hypertension).

Adv. Reactions/Side Effects ⬆ ⬇

Derm: hyperpigmentation of skin and mucous membranes, photosensitivity, DRUG RASH WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS SYNDROME (DRESS), ERYTHEMA MULTIFORME (EM), rash, STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN)

EENT: vestibular reactions

Endo: thyroid disorders

GI: diarrhea, nausea, vomiting, CLOSTRIDIODES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), esophagitis, HEPATOTOXICITY, pancreatitis

Hemat: blood dyscrasias

Neuro: dizziness, headache, intracranial hypertension

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), lupus-like syndrome, superinfection

Interactions ⬆ ⬇

Drug-drug:

May ↑ the risk of bleeding with warfarin.
May ↓ the effectiveness of estrogen-containing oral contraceptives.
Antacids,calcium, iron supplements, and magnesium salts form insoluble compounds (chelates) and ↓ absorption of tetracyclines.
Sucralfate, cholestyramine, colestipol, or adsorbentantidiarrheals may bind to minocycline and prevent its absorption from the GI tract.
Isotretinoin may ↑ risk of intracranial hypertension; avoid concurrent use.

Calcium in foods or dairy products↓ absorption by forming insoluble compounds (chelates).

Route/Dosage ⬆ ⬇

PO (Adults ): 100–200 mg initially, then 100 mg every 12 hr or 50 mg every 6 hr.
PO IV (Children ≥8 yr): 4 mg/kg initially, then 2 mg/kg every 12 hr.
PO (Adults and Children ≥12 yr and 126–136 kg): Extended-release tablets: 135 mg once daily for 12 wk.
PO (Adults and Children ≥12 yr and 111–125 kg): Extended-release tablets:115 mg once daily for 12 wk.
PO (Adults and Children ≥12 yr and 97–110 kg): Extended-release tablets:105 mg once daily for 12 wk;
PO (Adults and Children ≥12 yr and 85–96 kg): Extended-release tablets:90 mg once daily for 12 wk;
PO (Adults and Children ≥12 yr and 72–84 kg): Extended-release tablets:80 mg once daily for 12 wk;
PO (Adults and Children ≥12 yr and 60–71 kg): Extended-release tablets:65 mg once daily for 12 wk;
PO (Adults and Children ≥12 yr and 50–59 kg): Extended-release tablets:55 mg once daily for 12 wk;
PO (Adults and Children ≥12 yr and 45–49 kg): Extended-release tablets:45 mg once daily for 12 wk.
PO (Adults and Children ≥12 yr and 126–136 kg): Extended-release tablets: 135 mg once daily for 12 wk.
PO (Adults and Children ≥12 yr and 90–125 kg): Extended-release tablets: 105 mg once daily for 12 wk.
PO (Adults and Children ≥12 yr and 60–89 kg): Extended-release tablets: 67.5 mg once daily for 12 wk.
PO (Adults and Children ≥12 yr and 45–59 kg): Extended-release tablets: 52.5 mg once daily for 12 wk.
IV (Adults ): 200 mg initially, then 100 mg every 12 hr (not to exceed 400 mg/day).

Availability ⬆ ⬇

(Generic available)

Immediate-release capsules: 50 mg; 75 mg; 100 mg
Immediate-release tablets: 50 mg; 75 mg; 100 mg
Extended-release tablets: 45 mg; 55 mg; 65 mg; 80 mg; 90 mg; 105 mg; 115 mg; 135 mg
Lyophilized powder for injection: 100 mg/vial

Assessment ⬆ ⬇

Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of CDAD. May begin up to several wk following cessation of therapy.
Assess for rash periodically during therapy. May cause SJS, TEN, or EM. Discontinue therapy if severe or if accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.
Monitor for signs and symptoms of DRESS (fever, rash, lymphadenopathy, facial swelling), associated with involvement of other organ systems (hepatitis, nephritis, hematologic abnormalities, myocarditis, myositis) during therapy. May resemble an acute viral infection. Eosinophilia is often present. Discontinue therapy if signs occur.
Infection: Assess patient for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and throughout therapy.
- Obtain specimens for culture and sensitivity before initiating therapy. First dose may be given before receiving results.

Lab Test Considerations:

Monitor renal and hepatic function and CBC periodically during long-term therapy.
- May cause ↑ AST, ALT, serum alkaline phosphatase, bilirubin, and amylase concentrations. May cause ↑ BUN.
- May cause false ↑ in urinary catecholamine levels.

Implementation ⬆ ⬇

May cause yellow-brown discoloration and softening of teeth and bones if administered prenatally or during early childhood. Not recommended for children <8 yr of age or during pregnancy or lactation.
PO: Administer around the clock. May be taken with food or milk if GI irritation occurs. Administer with a full glass of liquid ≥1 hr before going to bed to avoid esophageal ulceration.DNC: Swallow extended-release tablets and capsules whole; do not open, crush, break, or chew. Do not administer within 1–3 hr of other medications.
- Avoid administration of calcium, antacids, magnesium-containing medications, sodium bicarbonate, or iron supplements within 1–3 hr of minocycline.

IV Administration:

IV doses are indicated only when oral therapy is not adequate or tolerated. Resume oral doses as soon as possible.
Intermittent Infusion: Reconstitute vial with 5 mL of sterile water for injection. Diluent: 100 mL to 1,000 mL 0.9% NaCl, D5W, or D5/0.9% NaCl, or in 250 mL to 1000 mL LR, but not with other solutions containing calcium; precipitate may form especially in neutral and alkaline solutions.Solutions are stable for 4 hr at room temperature or 24 hr if refrigerated.
Rate: Infuse over 60 min. Do not infuse rapidly.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take medication around the clock and to finish the drug completely as directed, even if feeling better. Take missed doses as soon as possible unless almost time for next dose; do not double doses. Advise patient that sharing of this medication may be dangerous.
- Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
- Advise patient to avoid taking antacids, calcium, magnesium-containing medications, sodium bicarbonate, and iron supplements within 1–3 hr of oral tetracyclines.
- Commonly causes dizziness or unsteadiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known. Notify health care professional if these symptoms occur.
- Instruct patient to notify health care professional immediately if rash, diarrhea, abdominal cramping, fever, or bloody stools occur and not to treat with antidiarrheals without consulting health care professionals.
- Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions. Advise patient to discontinue medication and notify health care professional at the first sign of skin erythema.
- Advise patient to report the signs of superinfection (black, furry overgrowth on the tongue; vaginal itching or discharge; loose or foul-smelling stools) or intracranial hypertension (headache, blurred vision, diplopia, vision loss). Women who are overweight, are of reproductive potential, or have a history of intracranial hypertension are at greater risk for developing minocycline-associated intracranial hypertension. Skin rash, pruritus, and urticaria should also be reported.
- Instruct patient to notify health care professional of medication regimen before treatment or surgery.
- Caution patient to discard outdated or decomposed minocycline; may be toxic.
- May cause fetal harm. Advise females of reproductive potential to use a nonhormonal method of contraception while taking minocycline and until next menstrual period and to avoid breastfeeding during therapy. May impair male fertility. Advise females of reproductive potential to notify health care professional promptly if pregnancy is planned or suspected.
- Instruct patient to notify health care professional if symptoms do not improve within a few days for systemic preparations.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇