Pronunciation: min-oh-SIGH-kleen
Class: Tetracycline, GI agent

Trade Names

Arestin
- Microspheres, sustained-release 1 mg (as hydrochloride)

Dynacin
- Tablets 50 mg (as hydrochloride)
- Tablets 75 mg (as hydrochloride)
- Tablets 100 mg (as hydrochloride)
- Capsules 50 mg (as hydrochloride)
- Capsules 100 mg (as hydrochloride)

Minocin
- Capsules, pellet-filled 50 mg (as hydrochloride)
- Capsules, pellet-filled 100 mg (as hydrochloride)
- Injection, lyophilized powder for solution 100 mg (as hydrochloride)

Minocycline HCl
- Tablets, extended-release 45 mg
- Tablets, extended-release 90 mg
- Tablets, extended-release 135 mg

Apo-Minocycline (Canada)
Enca (Canada)
Gen-Minocycline (Canada)
ratio-Minocycline (Canada)
Sandoz Minocycline (Canada)

Pharmacology

Inhibits bacterial protein synthesis.

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Pharmacokinetics

Absorption

T _max is 1 to 4 h after a single dose. Food does not affect extent of absorption, but C _max is slightly decreased and delayed by 1 h.

Distribution

Minocycline has a very high lipid solubility, readily penetrates the CSF, and displays a good penetration of saliva, brain, eye, and prostate. 70% to 80% is protein bound.

Metabolism

Metabolism is concentrated by the liver in the bile.

Elimination

1% to 12% is excreted unchanged in urine. Serum t _½ is approximately 11 to 23 h in healthy volunteers. Hemodialysis and peritoneal dialysis have little effect.

Special Populations

Renal Function Impairment

Serum t _½ is 18 to 69 h.

Hepatic Function Impairment

Serum t _½ is 11 to 16 h.

Indications and Usage

Treatment of periodontitis as an adjunct to scaling and root planing. Treatment of infections caused by susceptible strains of gram-positive and gram-negative bacteria, Rickettsia and Mycoplasma pneumonia, and trachoma; treatment for susceptible infections when penicillins are contraindicated; adjunctive treatment of acute intestinal amebiasis; treatment of asymptomatic carriers of Neisseria meningitidis to eliminate meningococci from nasopharynx, chlamydia, inflammatory acne, syphilis, gonorrhea.

Contraindications

Standard considerations.

Dosage and Administration

Inflammatory Acne
Adults

PO 50 mg 1 to 3 times per day.

Meningococcal Carrier State
Adults

PO 100 mg every 12 h for 5 days.

Mycobacterium Marinum Infections
Adults

PO 100 mg every 12 h for 6 to 8 wk, although optimal doses have not been established.

Periodontitis
Adults

Subgingival 1 mg microspheres are to be inserted by an oral health care professional.

Primary/Secondary Syphilis
Adults

PO 200 mg initially then 100 mg every 12 h for 10 to 15 days.

Renal Function Impairment

Do not exceed 200 mg per 24 h.

Susceptible Infections
Adults

PO/IV 200 mg initially, then PO/IV 100 mg every 12 h or PO 50 mg 4 times daily (max, parenteral 400 mg per 24 h).

Children older than 8 yr of age

PO/IV 4 mg/kg initially, then 2 mg/kg every 12 h (max, usual adult dose).

Uncomplicated Gonococcal Infections Except Urethritis and Anorectal Infections in Men
Adults

PO 200 mg initially followed with 100 mg every 12 h for at least 4 days, with posttherapy cultures within 2 to 3 days.

Uncomplicated Gonococcal Urethritis in Men
Adults

PO 100 mg every 12 h for 5 days.

Uncomplicated Urethral, Endocervical, or Rectal Infections in Adults Caused by C. Trachomatis or Ureaplasma Urealyticum
Adults

PO 100 mg every 12 h for at least 7 days.

General Advice

Injection

• For IV infusion only, avoid rapid infusion. Not for intradermal, subcutaneous, IM, intra-arterial, or IV bolus administration.
• Because of the risk of thrombophlebitis, use parenteral therapy only when oral therapy is not indicated. Institute oral therapy as soon as possible.
• Follow manufacturer's guidelines for reconstituting and further diluting the powder for injection.
• Do not administer if particulate matter, cloudiness, or discoloration is noted.

Storage/Stability

Store capsules at controlled room temperature (68° to 77°F). Protect from light, moisture, and excessive heat. Diluted solution should be administered immediately, but can be stored at room temperature (68° to 77°F) for up to 24 h. Discard any unused solution after 24 h. Store powder for injection at controlled room temperature (68° to 77°F). Protect from light moisture and excessive heat. Store at controlled room temperature (59° to 86°F). Avoid exposure to excessive heat.

Drug Interactions

Antacids (containing aluminum, calcium, magnesium, zinc), bismuth salts, divalent or trivalent cations

May decrease oral absorption of minocycline.

Anticoagulants, oral

Increased anticoagulant activity.

Contraceptives, oral

May reduce effect of oral contraceptives.

Digoxin

May increase digoxin serum levels.

Insulin

Increases hypoglycemic potential.

Iron salts

May decrease absorption of minocycline.

Isotretinoin

Because the risk of pseudotumor cerebri may be increased, avoid isotretinoin administration shortly before, during, or after minocycline therapy.

Methoxyflurane

Increased potential for nephrotoxicity exists; do not coadminister.

Milk and dairy products

Although the effects of milk and dairy products on minocycline absorption are less than observed with other tetracycline derivatives, it would be prudent to avoid the administration of milk or dairy products with all tetracycline derivatives.

Penicillins

May interfere with bactericidal action of penicillins.

Urinary alkalinizers, zinc salts

May decrease serum minocycline levels.

Incompatibility

Do not mix before or during administration with adrenocorticotropic hormone, 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, polymyxins, prochlorperazine, sodium ascorbate, sulfadiazine, sulfisoxazole, thiopental sodium, vitamin K (sodium bisulfate or sodium salt), whole blood.

Laboratory Test Interactions

False increase in urinary catecholamines with fluorometric method.

Adverse Reactions

CNS

Convulsions; dizziness; hypoesthesia; paresthesia; sedation; vertigo; bulging fontanels in infants; benign intracranial hypertension (pseudotumor cerebri) in adults; headache.

Dermatologic

Alopecia; erythema nodosum; hyperpigmentation of nails; pruritus; toxic epidermal necrolysis; vasculitis; maculopapular and erythematous rashes; exfoliative dermatitis; fixed drug eruptions; balanitis due to lesions on the penis; erythema multiforme; Stevens-Johnson syndrome; photosensitivity.

EENT

Tinnitus; decreased hearing.

GI

Anorexia; nausea; vomiting; diarrhea; dyspepsia; stomatitis; glossitis; dysphagia; enamel hypoplasia; enterocolitis; pseudomembranous colitis; pancreatitis; inflammatory lesions (with monilial overgrowth) in oral and anogenital regions; esophagitis; esophageal ulceration; tooth discoloration; oral cavity discoloration (including tongue, lips, and gums).

Genitourinary

Vulvovaginitis.

Hepatic

Hyperbilirubinemia; hepatic cholestasis; increased liver enzymes, fatal hepatic failure; jaundice; hepatitis (including autoimmune hepatitis); liver failure.

Hematologic-Lymphatic

Agranulocytosis; hemolytic anemia; thrombocytopenia; leukopenia; neutropenia; pancytopenia; eosinophilia.

Hypersensitivity

Urticaria; angioneurotic edema; polyarthralgia; anaphylaxis/anaphylactoid reaction (including shock and death); anaphylactoid purpura; myocarditis; pericarditis; exacerbation of SLE; pulmonary infiltrates with eosinophilia; transient lupus-like syndrome; serum sickness-like reactions; hypersensitivity syndrome (including rash, exfoliative dermatitis, eosinophilia, fever, lymphadenopathy and one or more of the following hepatitis, pneumonitis, nephritis, myocarditis, pericarditis).

Musculoskeletal

Arthralgia; arthritis; bone discoloration; myalgia; joint stiffness; joint swelling.

Renal

Interstitial nephritis; elevations in BUN; reversible renal failure.

Respiratory

Cough; dyspnea; bronchospasm; exacerbation of asthma; pneumonitis.

Miscellaneous

Fever, discoloration of secretions; brown-black microscopic discoloration of the thyroid gland.

Precautions

Pregnancy

Category D .

Lactation

Excreted in breast milk. Advise against breast-feeding.

Children

Avoid in children younger than 8 yr of age unless other appropriate drugs are ineffective or contraindicated because abnormal bone formation and discoloration of teeth may occur.

Renal Function

May increase BUN, may lead to azotemia, hyperphosphatemia, and acidosis.

Superinfection

Prolonged use may result in bacterial or fungal overgrowth.

Photosensitivity

May cause exaggerated sunburn reactions.

Expiration

Do not use outdated product; degraded product is highly nephrotoxic.

Hepatotoxicity

Has been reported. Use with caution in patients with hepatic function impairment and in conjunction with hepatotoxic drugs.

Parenteral therapy

Prolonged periods of parenteral use may result in thrombophlebitis.

Pseudotumor cerebri (benign intracranial hypertension)

Has been reported in adults. Usual manifestations are headache and blurred vision.

Tooth discoloration

May cause permanent discoloration of the teeth.

Overdosage

Symptoms

Dizziness, nausea, vomiting.

Patient Information

• Review dosing schedule and prescribed length of therapy with patient. Advise patient that dose and duration of therapy are dependent on site and cause of infection.
• Instruct patient using capsules to take prescribed dose with a full glass of water.
• Instruct patient or caregiver using oral suspension to measure and administer prescribed dose using dosing spoon, dosing syringe, or medicine cup.
• Advise patient to take without regard to meals, but to take with food if GI upset occurs.
• Advise patient to take 1 h before or 2 h after antacids containing aluminum, calcium, or magnesium, or preparations containing iron or zinc.
• Instruct patient to complete entire course of therapy, even if symptoms of infection have disappeared.
• Advise patient to discontinue therapy and contact health care provider immediately if skin rash, hives, itching, shortness of breath, headache, or blurred vision occur.
• Advise patient that medication may cause photosensitivity (sensitivity to sunlight) and to avoid unnecessary exposure to sunlight or tanning lamps and to use sunscreens and wear protective clothing to avoid photosensitivity reactions.
• Caution women taking oral contraceptives that minocycline may make birth control pills less effective and to use nonhormonal forms of contraception during treatment.
• Caution patient that drug may cause dizziness, light-headedness, or blurred vision and to use caution while driving or performing other hazardous tasks until tolerance is determined.
• Advise patient to report signs of superinfection to health care provider: black furry tongue, white patches in mouth, foul-smelling stools, vaginal itching, or discharge.
• Warn patient that diarrhea containing blood or pus may be a sign of a serious disorder and to seek medical care if noted and not treat at home.
• Advise patient to discard any unused minocycline by the expiration date noted on the label.

• Subgingival Microspheres
• Caution patient to avoid touching treated areas and to avoid brushing for 12 h following treatment. Advise patient to avoid eating hard, crunchy, or sticky foods for 1 wk following treatment and postpone use of interproximal cleaning devices for 10 days.
• Advise patient that mild to moderate sensitivity is expected after treatment, but to notify dental professional immediately if pain, swelling, or other problems occur.

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