|Other names||Demeclocycline hydrochloride, RP-10192|
|Drug class||Tetracycline antibiotic|
|Main uses||Bacterial infections, SIADH|
|Side effects||Nausea, rash, kidney problems, allergic reactions|
|Elimination half-life||10–17 hours|
|Chemical and physical data|
|Molar mass||464.86 g·mol−1|
|3D model (JSmol)|
Demeclocycline, sold under the brand names Declomycin among others, is a tetracycline antibiotic used to treat a number of bacterial infections as well as low sodium due to syndrome of inappropriate ADH (SIADH). These infections include pneumonia, acne, chlamydia, gonorrhea, and syphilis. It is taken by my mouth.
Common side effects include nausea, rash, kidney problems, and allergic reactions. Other side effects may include diabetes insipidus and a feeling of the world spinning. Use in pregnancy may harm the baby and use in children under 8 not generally recommended. Other side effects may include sunburns.
Demeclocycline has been approved for medical use in the United States since at least 1960. It is available as a generic medication. In the United Kingdom 28 tablets of 150 mg costs the NHS about £220 as of 2021. In the United States this amount is about 70 USD. It is made from Streptomyces aureofaciens.
Demeclocycline is used to treat various types of bacterial infections. It is used as an antibiotic in the treatment of Lyme disease, acne, and bronchitis. Resistance, though, is gradually becoming more common, and demeclocycline is now rarely used for treatment of infections.
It is used (though off-label in many countries including the United States) in the treatment of hyponatremia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) when fluid restriction alone has been ineffective. Physiologically, this works by reducing the responsiveness of the collecting tubule cells to ADH.
The use of demeclocycline in SIADH was first reported in 1975, and, in 1978, a larger study found it to be more effective and better tolerated than lithium carbonate, the only available treatment at the time. Demeclocycline used to be the drug of choice for treating SIADH. Meanwhile it might be superseded, now that vasopressin receptor antagonists, such as tolvaptan, became available.
For infections it may be used at 300 mg twice per day while for SIADH it may be used at doses of 300 mg three times per day.
These are similar to those of other tetracyclines. Skin reactions with sunlight have been reported. Like only few other known tetracycline derivatives, demeclocycline causes nephrogenic diabetes insipidus. Furthermore demeclocycline might have psychotropic side effects similar to lithium.
Tetracyclines bind to cations, such as calcium, iron (when given orally), and magnesium, rendering them insoluble and inadsorbable for the gastrointestinal tract. Demeclocycline should not be taken with food (particularly milk and other dairy products) or antacids.
Mechanism of action
As with related tetracycline antibiotics, demeclocycline acts by binding to the 30S ribosomal subunit to inhibit binding of aminoacyl tRNA which impairs protein synthesis by bacteria. It is bacteriostatic (it impairs bacterial growth, but does not kill bacteria directly).
Demeclocycline inhibits the renal action of antidiuretic hormone by interfering with the intracellular second messenger cascade (specifically, inhibiting adenylyl cyclase activation) after the hormone binds to vasopressin V2 receptors in the kidney. Exactly how demeclocycline does this has yet to be elucidated, however.
Society and culture
Declomycin, Declostatin, Ledermycin, Bioterciclin, Deganol, Deteclo, Detravis, Meciclin, Mexocine, and Clortetrin.
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