minocycline (systemic)

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.

Drug-Food:

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

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

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).

US Brand Names ⬆ ⬇

Minocin, ~~Minolira,~~ ~~Solodyn~~

Action ⬆ ⬇

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.

Classifications ⬆ ⬇

Therapeutic Classification: anti-infectives

Pharmacologic Classification: tetracyclines

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

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.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇