Minocycline

457.48

457.48

237-099-7

FYY3R43WGO

DTXSID1045033

BRIGHT YELLOW-ORANGE AMORPHOUS SOLID

A - Alimentary tract and metabolism|D - Dermatologicals|J - Antiinfectives for systemic use

165

-0.6

Bright yellow-orange amorphous solid.

1.3283 (rough estimate)

563.31°C (rough estimate)

439.6±34.3 °C

1.6500 (estimate)

In water, 52,000 mg/l at 25 deg C.

Keep in a cool, dry, dark location in a tightly sealed container or cylinder. Keep away from incompatible materials, ignition sources and untrained individuals. Secure and label area. Protect containers/cylinders from physical damage.

D25 -166° (c = 0.524)

ODORLESS; SLIGHTLY BITTER TASTE; SLIGHTLY HYGROSCOPIC; PH OF 1% SOLN BETWEEN 3.5 & 4.5;/HYDROCHLORIDE/ PKA1= 2.8; PKA2= 5.0; PKA3= 7.8; PKA4= 9.3 /HYDROCHLORIDE/|Slightly hygroscopic; sensitive to light and to surface oxidation /Hydrochloride/

Ⅲ

2811

6.1

POTENCY IN SOLN AFFECTED PRIMARILY DUE TO EPIMERIZATION /HYDROCHLORIDE/

P201, P202, P260, P263, P264, P270, P280, P281, P305+P351+P338, P308+P313, P337+P313, P405, P501

H319

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

The oral LD50 in rats is 2380mg/kg and in mice is 3600mg/kg. The intraperitoneal LD50 in rats is 331mg/kg and in mice is 299mg/kg. The subcutaneous LD50 in rats is 1700mg/kg and in mice is 2290mg/kg. Patients experiencing an overdose may present with dizziness, nausea, and vomiting. In the event of an overdose, discontinue minocycline and treat patients with symptomatic and supportive measures.

Minocycline therapy is associated with two forms of clinically apparent liver injury, an acute hepatitis-like syndrome that arises within 1 to 3 months of starting therapy and a chronic hepatitis-like syndrome typically with autoimmune features that occurs with long term therapy, sometimes after several years of use. There is some overlap between these two presentations of minocycline hepatotoxicity, both are associated with a hepatocellular pattern of serum enzyme elevations and both can be associated with autoantibodies and immunological features.

BECAUSE METHOTREXATE BINDS TO PLASMA PROTEINS, IT CAN BE DISPLACED FROM ITS BONDING SITES & MADE AVAILABLE TO REACT WITH DIHYDROFOLATE REDUCTASE. ...COMPD THAT...DISPLACE...INCL...TETRACYCLINES. /TETRACYCLINES/|STRIKING ANTAGONISM BETWEEN PENICILLIN & TETRACYCLINES HAS BEEN OBSERVED CLINICALLY IN PNEUMOCOCCAL MENINGITIS... /TETRACYCLINES/|NEOMYCIN & RELATED ANTIBIOTICS PRODUCE PROFOUND NEUROMUSCULAR BLOCKADE IN HUMANS. USE OF THESE ANTIBIOTICS WITH NEUROMUSCULAR BLOCKING AGENTS COULD LEAD TO...RESP FAILURE. /NEOMYCIN/|...POSSIBILITY OF...SEVERE RENAL FAILURE IN PT WHO RECEIVE TETRACYCLINE AFTER BEING ANESTHETIZED WITH METHOXYFLURANE; IN THOSE WHO DIED, KIDNEYS CONTAINED NUMEROUS CALCIUM OXALATE CRYSTALS. /TETRACYCLINES/|For more Interactions (Complete) data for MINOCYCLINE (11 total), please visit the HSDB record page.

Minocycline is 76% protein bound in serum.

Oral and topical minocycline are indicated to treat inflammatory lesions of acne vulgaris. Subgingival microspheres are indicated as an adjunct treatment in the reduction of pocket depth in adults with periodontitis. Oral and intravenous formulations are indicated to treat infections of susceptible microorganisms. These include rickettsiae, _Mycoplasma pneumoniae_, _Chlamydia trachomatis_, _Chlamydophila psittaci_, _Chlamydia trachomatis_, _Ureaplasma urealyticum_, _Borrelia recurrentis_, _Haemophilus ducreyi_, _Yersinia pestis_, _Francisella tularensis_, _Vibrio cholerae_, _Campylobacter fetus_, _Brucella_ species, _Bartonella bacilliformis_, _Klebsiella granulomatis_, _Escherichia coli_, _Enterobacter aerogenes_, _Shigella_ species, _Acinetobacter_ species, _Haemophilus influenzae_, and _Kelbsiella_ species.|FDA Label

Minocycline is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long term treatment.

Antiinfective Agents

Antibiotics, Tetracycline|Minocycline is indicated in the treatment of uncomplicated genitourinary tract infections (including endocervical infections) caused by Ureaplasma urealyticum. /Included in US product labeling/|Oral minocycline is indicated in the treatment of asymptomatic meningococcal carriers to eliminate Neisseria meningitidis from the nasopharynx. /Included in US product labeling/|Systemic minocycline is used in the treatment of atypical mycobacterial infections. /NOT included in US product labeling/|For more Therapeutic Uses (Complete) data for MINOCYCLINE (33 total), please visit the HSDB record page.

UNTOWARD EFFECTS CAUSED BY MINOCYCLINE ARE ESSENTIALLY THOSE OF TETRACYCLINES IN GENERAL. HOWEVER, PHOTOTOXICITY SEEMS TO BE MUCH LESS THAN WITH OTHER TETRACYCLINES. MORE CLINICAL OBSERVATIONS ARE NEEDED TO ESTABLISH EXACT TOXIC POTENTIAL...|CROSS-SENSITIZATION AMONG VARIOUS TETRACYCLINES IS COMMON. /TETRACYCLINES/|VESTIBULAR DISTURBANCE MAY POSE HAZARD FOR PT ENGAGED IN ACTIVITIES REQUIRING UNIMPAIRED MOTOR COORDINATION.|...TETRACYCLINES ADMIN ORALLY OR PARENTERALLY MAY LEAD TO DEVELOPMENT OF SUPRAINFECTIONS THAT ARE USUALLY DUE TO STRAINS OF BACTERIA OR YEASTS RESISTANT TO THESE AGENTS. ... INCIDENCE OF SUPRAINFECTIONS IS MUCH HIGHER WITH TETRACYCLINES THAN WITH PENICILLIN OR STREPTOMYCIN. /TETRACYCLINES/|For more Drug Warnings (Complete) data for MINOCYCLINE (25 total), please visit the HSDB record page.

2 OR 3. 2= SLIGHTLY TOXIC: PROBABLE ORAL LETHAL DOSE (HUMAN) 5-15 G/KG; BETWEEN 1 PINT & QT FOR 70 KG PERSON (150 LB). 3= MODERATELY TOXIC: PROBABLE ORAL LETHAL DOSE (HUMAN) 0.5-5 G/KG; BETWEEN 1 OZ & 1 PINT (OR 1 LB) FOR 70 KG PERSON (150 LB). /TETRACYCLINES/

Minocycline is a tetracycline antibiotic that binds to the bacterial 30S ribosomal subunit and interferes with protein synthesis. It is generally given 2-4 times daily, so the duration of action is short. Intravenous minocycline should not exceed 400mg in 24 hours. Patients should be counselled regarding the risks related to tooth and bone development, pseudomembranous colitis, central nervous system side effects, and pseudotumor cerebri.

Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)

100mg of oral minocycline reaches a C_max of 1.6mg/L, with a T_max of 1.9h, and an AUC of 31.6mg/L\*h. 200mg of oral minocycline reaches a C_max of 3.1mg/L, with a T_max of 2.5h, and an AUC of 48.3mg/L\*h.|Minocycline is predominantly eliminated through the biliary route. 4.5-9% of an intravenous minocycline dose is recovered in the urine. 10-19.5% of an oral dose is recovered in the urine and 20-34% is recovered in the feces.|The volume of distribution of minocycline has been reported as 67.5-115L.|Intravenous minocycline has a clearance of 3.36-5.7L/h, while oral minocycline has a clearance of 3.42-4.4L/h.|ALL TETRACYCLINES ARE ADEQUATELY BUT INCOMPLETELY ABSORBED FROM GI TRACT. MOST ABSORPTION TAKES PLACE FROM STOMACH & UPPER SMALL INTESTINE & IS GREATEST IN FASTING STATE. /TETRACYCLINES/|The percentage of an oral dose that is absorbed is 100%.|ALL TETRACYCLINES ARE REMOVED FROM BLOOD BY LIVER, WHERE THEY ARE CONCENTRATED & THEN EXCRETED, BY...BILE, INTO INTESTINE, FROM WHICH THEY ARE PARTIALLY REABSORBED. BILIARY CONCN OF THESE AGENTS AVG AT LEAST 5-10 TIMES HIGHER THAN SIMULTANEOUS VALUES IN PLASMA. /TETRACYCLINES/|FOOD DOES NOT INTERFERE WITH ABSORPTION OF...MINOCYCLINE.|For more Absorption, Distribution and Excretion (Complete) data for MINOCYCLINE (14 total), please visit the HSDB record page.

Minocycline is primarily metabolized to 9-hydroxyminocycline. It is also metabolized to 2 different N-demethylated metabolites.|MINOCYCLINE IS PARTIALLY METABOLIZED...

The half life of minocycline pellet filled capsules is 11.1-22.1 hours. Minocycline intravenous injections have a half live of 15-23 hours.|.../MINOCYCLINE HALF-LIFE IS/ LONG (16-18 HR)...|IN MAN MINOCYCLINE, A NEW TETRACYCLINE, HAS BIOLOGICAL HALF-LIFE APPROX THAT OF DOXYCYCLINE BUT APPRECIABLY LONGER THAN THAT OF OTHER TETRACYCLINES.

Tetracyclines enter bacterial cells through OmpF and OmpC porins by coordinating with cations like magnesium. This allows tetracyclines into the periplasm where they dissociate, allowing the lipophilic tetracycline to diffuse into the bacterial cytoplasm. Tetracyclines prevent aminoacyl-tRNA from binding to the 30S ribosome, inhibiting protein synthesis.|TETRACYCLINES ARE THOUGHT TO INHIBIT PROTEIN SYNTHESIS BY BINDING TO 30 S RIBOSOMES. THEY APPEAR TO PREVENT ACCESS OF AMINOACYL TRNA TO MRNA-RIBOSOME COMPLEX. ONLY SMALL PORTION OF DRUG IS IRREVERSIBLY BOUND, & INHIBITORY EFFECTS OF TETRACYCLINES CAN BE REVERSED BY WASHING. /TETRACYCLINES/|...IT IS POSSIBLE THAT REVERSIBLY BOUND ANTIBIOTIC IS RESPONSIBLE FOR ANTIBACTERIAL ACTION. /TETRACYCLINES/|PHOTOALLERGIC REACTIONS ARE BELIEVED TO RESULT FROM LIGHT ENERGY ACTING ON OR ALTERING DRUG & SKIN PROTEINS IN SUCH MANNER AS TO FORM AN ANTIGEN. THESE ERUPTIONS REQUIRE PREVIOUS CONTACT WITH OFFENDING SUBSTANCE, ARE NOT DOSE-RELATED, & EXHIBIT CROSS-SENSITIVITY WITH CHEM RELATED COMPD. /TETRACYCLINES/

LONG-TERM THERAPY WITH TETRACYCLINES MAY PRODUCE CHANGES IN PERIPHERAL BLOOD. LEUKOCYTOSIS, ATYPICAL LYMPHOCYTES, TOXIC GRANULATION OF GRANULOCYTES & THROMBOPENIC PURPURA HAVE BEEN OBSERVED. /TETRACYCLINES/|CHILDREN RECEIVING LONG OR SHORT TERM THERAPY WITH A TETRACYCLINE MAY DEVELOP BROWN DISCOLORATIONS OF TEETH. LARGER THE DOSE...RELATIVE TO BODY WT, MORE INTENSE DISCOLORATION OF ENAMEL. DURATION OF THERAPY APPEARS TO BE LESS IMPORTANT THAN TOTAL.../AMT/ ANTIBIOTIC ADMIN. /TETRACYCLINES/|Benign intracranial hypertension, with 6th nerve palsy and papilledema, has been reported in a girl taking minocycline...

Akamin

...MINOCYCLINE HYDROCHLORIDE, USP (MINOCIN, VECTRIN).../IS/ AVAIL IN WIDE VARIETY OF FORMS FOR ORAL, TOPICAL & PARENTERAL ADMIN.|SOME OF THE TETRACYCLINES ARE...MARKETED AS FLAVORED POWDERS, OPHTHALMIC SOLN & OINTMENTS, SOLN FOR INJECTION, SOL SALTS FOR PREPN OF ORAL SUSPENSIONS & DROPS, & SYRUPS & ELIXIRS FOR PEDIATRIC USE. /TETRACYCLINES/

PATENT: US 4,483,251. /HYDROCHLORIDE/

COMPARISON OF RAPID FLUOROMETRIC ASSAY OF MINOCYCLINE IN PLASMA OR SERUM WITH MICROBIOLOGICAL ASSAY.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Polyketides [PK] -> Linear tetracyclines [PK07]|Pharmaceuticals -> Animal Drugs -> Approved in Taiwan