Ledermycin hydrochloride: Full Drug Profile

Ledermycin hydrochloride - General Information

A tetracycline analog having a 7-chloro and a 6-methyl. Because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time. [PubChem]

Pharmacology of Ledermycin hydrochloride

Ledermycin hydrochloride is a tetracycline antibiotic active against the following microorganisms: Rickettsiae (Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsial pox, tick fevers), Mycoplasma pneumoniae (PPLO, Eaton agent), agents of psittacosis and ornithosis, agents of lymphogranulomavenereum and granuloma inguinale, the spirochetal agent of relapsing fever (Borrelia recurrentis), Haemophilus ducreyi (chancroid), Yersinia pestis, Pasteurella pestis and Pasteurella tularensis, Bartonella bacilliformis, Bacteroides species, Vibrio comma and Vibrio fetus, and Brucella species (in conjunction with streptomycin). Ledermycin hydrochloride inhibits cell growth by inhibiting translation. Ledermycin hydrochloride is lipophilic and can easily pass through the cell membrane or passively diffuses through porin channels in the bacterial membrane. Ledermycin hydrochloride is bacteriostatic (it impairs bacterial growth but does not kill bacteria directly). Because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time.

Ledermycin hydrochloride for patients

Demeclocycline hydrochloride is a pill given by mouth, usually 2 to 4 times a day. Take the pill on an empty stomach with a full glass of water, 1 hour before or 2 hours after eating a meal or dairy products like milk, yogurt, and ice cream. If you have nausea when taking the medicine, take it with a cracker but no dairy products. If you are also taking iron pills, take the iron pills 2 hours before or 3 hours after the demeclocycline hydrochloride pill. Keep the medicine in a tightly closed container away from heat and moisture and out of the reach of children and pets. Do not drive a car or operate heavy machinery until you know the effect that demeclocycline hydrochloride has on you. If you are dizzy, lightheaded, or feel tired, you should not drive or operate heavy machinery. Stop the drug and call your doctor or nurse right away if you develop a rash, fever, muscle aches, diarrhea with abdominal cramping, or blood or pus in your stool. This can be a serious reaction and needs to be treated right away.

Ledermycin hydrochloride Interactions

Because the tetracyclines have been shown to depress plasma prothrombin activity, patients who are on anticoagulant therapy may require downward adjustment of their anticoagulant dosage.

Since bacteriostatic drugs, such as the tetracycline class of antibiotics, may interfere with the bactericidal action of penicillins, it is not advisable to administer these drugs concomitantly.

Concurrent use of tetracyclines with oral contraceptives may render oral contraceptives less effective. Breakthrough bleeding has been reported

Ledermycin hydrochloride Contraindications

This drug is contraindicated in persons who have shown hypersensitivity to any of the tetracyclines.

Additional information about Ledermycin hydrochloride

Ledermycin hydrochloride Indication

Used primarily to treat Lyme disease, acne, and bronchitis. Also indicated (but rarely used) to treat urinary tract infections, gum disease, malaria, and other bacterial infections such as gonorrhea and chlamydia. One of its other registered uses is the treatment of hyponatremia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective.

Mechanism Of Action

Ledermycin hydrochloride inhibits cell growth by inhibiting translation. It binds (reversibly) to the 30S and 50S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome, which impairs protein synthesis by bacteria. The binding is reversible in nature. The use in SIADH actually relies on a side-effect of tetracycline antibiotics; many may cause diabetes insipidus (dehydration due to the inability to concentrate urine). It is not completely understood why demeclocycline impairs the action of antidiuretic hormone, but it is thought that it blocks the binding of the hormone to its receptor.

Drug Interactions

Acitretin Increased risk of intracranial hypertension

Food Interactions

Take on an empty stomach.

Generic Name

Demeclocycline

Drug Category

Anti-Bacterial Agents; Tetracyclines

Drug Type

Small Molecule; Approved

Other Brand Names containing Demeclocycline

6-Demethyl-7-chlorotetracycline; 6-Demethylchlorotetracycline; 7-Chloro-6-demethyltetracycline; Bioterciclin; Clortetrin; DMCT; DMCT (antibiotic); Declomycin; Deganol; Demeclociclina [INN-Spanish]; Demeclocycline HCL; Demeclocycline [USAN:BAN]; Demeclocycline hydrochloride; Demeclocyclinum [INN-Latin]; Demeclor; Demethylchlorotetracycline; Demethylchlortetracyclin; Demethylchlortetracycline; Demethylchlortetracycline hydrochloride; Demethylchlortetracyclinum; Demetraclin; Diuciclin; Elkamicina; Ledermycin; Ledermycin hydrochloride; Methylchlorotetracycline; Mexocine; Novotriclina; Perciclina; Sumaclina; Tri-demethylchlortetracycline;

Absorption

Tetracyclines are readily absorbed.

Toxicity (Overdose)

Oral, rat: LD₅₀ = 2372 mg/kg

Protein Binding

41-50%

Biotransformation

Hepatic

Half Life

10-17 hours

Dosage Forms of Ledermycin hydrochloride

Tablet Oral

Chemical IUPAC Name

(2E,4S,4aS,5aS,6S,12aS)-2-(amino-hydroxymethylidene)-7-chloro-4-dimethylamino-6,10,11,12a-tetrahydroxy-4a,5,5a,6-tetrahydro-4H-tetracene-1,3,12-trione

Chemical Formula

C21H21ClN2O8

Demeclocycline on Wikipedia

https://en.wikipedia.org/wiki/Demeclocycline

Organisms Affected

Enteric bacteria and other eubacteria