Demeclocycline Hydrochloride
Indications
Demeclocycline Hydrochloride is used for:
Atypical pneumonia, Hyponatraemia
Adult Dose
Oral
Oral
Susceptible infections (e.g. chlamydia, rickettsia and
mycoplasma)
Adult: 600 mg daily in 2 or 4 divided doses.
Atypical pneumonia
Adult: 900 mg daily in 3 divided doses for 6 days.
Chronic hyponatraemia associated with syndrome of inappropriate antidiuretic hormone secretion (SIADH)
Adult: Initially, 900-1,200 mg daily in divided doses.
Maintenance: 600-900 mg daily in divided doses.
Child Dose
Child: Not recommended for childn <12 yr.
Renal Dose
RENAL IMPAIRMENT
May exacerbate renal failure and should not be given to patients with renal impairment.
Administration
Should be taken on an empty stomach. Take w/ a full glass of water on an empty stomach at least 1 hr before or 2 hr after meals.
Contra Indications
Hypersensitivity. Pregnancy and lactation.
Precautions
All tetracyclines form a stable calcium complex in any bone-forming tissue; a decrease in fibula growth rate has been observed in premature human infants given in doses of 25 mg/kg/ every six hr; this reaction was shown to be reversible when the drug was discontinued
Results of animal studies indicate that tetracyclines cross the placenta, are found in fetal tissues, and can have toxic effects on the developing fetus (often related to retardation of skeletal development); evidence of embryotoxicity has been noted in animals treated early in pregnancy
The anti-anabolic action of the tetracyclines may cause an increase in BUN; while this is not a problem in those with normal renal function, in patients with significantly impaired function, higher serum levels of tetracycline may lead to azotemia, hyperphosphatemia, and acidosis; if renal impairment exists, even usual oral or parenteral doses may lead to excessive systemic accumulation of the drug and possible liver toxicity; under such conditions, lower than usual total doses are indicated and, if therapy is prolonged, serum level determinations of the drug may be advisable
Photosensitivity manifested by exaggerated sunburn reaction has been observed in some individuals taking tetracyclines; phototoxic reactions can occur in individuals taking demeclocycline, and are characterized by severe burns or exposed surfaces resulting from direct exposure of patients to sunlight during therapy with moderate or large doses of demeclocycline; patients that may be exposed to direct sunlight or ultraviolet light should be advised that this reaction can occur and treatment should be discontinued at first evidence of erythema of skin
Administration of demeclocycline hydrochloride has resulted in appearance of the diabetes insipidus syndrome (polyuria, polydipsia, and weakness) in some patients on long-term therapy; the syndrome has been shown to be nephrogenic, dose-dependent, and reversible on discontinuance of therapy; patients, who are experiencing central nervous system symptoms associated with this therapy, should be cautioned about driving vehicles or using hazardous machinery while on demeclocycline therapy
Pseudotumor cerebri (benign intracranial hypertension) in adults has been associated with use of this medication; the usual clinical manifestations are headache and blurred vision; bulging fontanels have been associated with use of tetracyclines in infants; while both of these conditions and related symptoms usually resolve soon after discontinuation of tetracycline, the possibility for permanent sequelae exists
As with other antibiotic preparations, use of this drug may result in overgrowth of nonsusceptible organisms, including fungi; if superinfection occurs, the antibiotic should be discontinued and appropriate therapy should be instituted; incision and drainage or other surgical procedures should be performed in conjunction with antibiotic therapy, when indicated; prescribing therapy in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to patient and increases risk of development of drug-resistant bacteria
Clostridioides difficile diarrhea
Clostridioides difficile associated with diarrhea (CDAD) reported with use; may range in severity from mild diarrhea to fatal colitis; treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile; C. difficile produces toxins A and B which contribute to development of CDAD
Pregnancy-Lactation
Pregnancy
Avoid during pregnancy; use alternant antibiotics
Tetracycline use during tooth development (last one-half of pregnancy through age 8 y) can cause permanent discoloration of teeth
Lactation
Tetracyclines are excreted in breastmilk
Avoided in breastfeeding women due to theoretical concerns that they may permanently stain the teeth of the breastfed infants
Interactions
Reduced absorption with antacids containing Al, Mg, or Ca, Fe-containing preparations, zinc, kaolin, quinapril, strontium ranelate, sucralfate, tripotassium dicitratobismuthate.
May reduce the efficacy of oral contraceptives and penicillins.
Increased risk of benign intracranial HTN with retinoids (e.g. acitretin, isotretinoin, tretinoin).
Increased risk of ergotism with ergotamine and methysergide.
May inactivate oral typhoid vaccine.
May potentiate the effect of anticoagulants.
Potentially Fatal: Concurrent use with methoxyflurane may result to fatal renal toxicity.
Contraindicated (1)
acitretin
Adverse Effects
Side effects of Demeclocycline Hydrochloride :
Frequency Not Defined
Photosensitivity rxn (more frequent & severe than other tetracyclines), reversible
Dose-related diabetes insipidus (does not occur with other tetracyclines)
Discoloration of teeth
Superinfection, monilial
Dysphagia
Glossitis
Nausea
Vomiting
Diarrhea
Hepatotoxicity
Potentially Fatal: Anaphylaxis (rare).
Mechanism of Action
Demeclocycline inhibits protein synthesis by binding w/ the 30S and possibly the 50S ribosomal subunits of susceptible bacteria. It may also cause alterations in the cytoplasmic membrane. It inhibits the action of antidiuretic hormone (ADH) in patients w/ chronic syndrome of inappropriate antidiuretic hormone secretion (SIADH).