Oxytetracycline

Oxytetracycline is an Antibiotic agent belonging to the pharmacology class of Tetracycline

Oxytetracycline is used in the treatment of Acne Vulgaris, Rosacea, Brucellosis, Epididymo-orchitis, Rectal infection due to Chlamydia trachomatis, Nongonococcal urethritis, Primary syphilis, Secondary syphilis, Streptococcal infectious disease.

Oxytetracycline is Incompletely and irregularly absorbed from the gastrointestinal tract. Time to peak plasma concentration of approx 1-4 hours and widely distributed throughout the body tissues and fluids and crosses the placenta and enters breast milk. Plasma protein binding: Approx 20-40% and get excreted via urine (40-70%); faeces with elimination half-life of Approx 6-12 hours.

Oxytetracycline is available in the form of dosage forms as ointment, injection, solution, capsule, suspension, tablet

Oxytetracycline is available in India, France, Japan, and the USA.

Oxytetracycline inhibits cell growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. The binding is reversible in nature. Oxytetracycline is lipophilic and can easily pass through the cell membrane or passively diffuses through porin channels in the bacterial membrane.

Oxytetracycline is available in the form of ointment, injection, solution, capsule, suspension, tablet.

Oxytetracycline is used in the treatment of Acne Vulgaris, Rosacea, Brucellosis, Epididymo-orchitis, Rectal infection due to Chlamydia trachomatis, Nongonococcal urethritis, Primary syphilis, Secondary syphilis, Streptococcal infectious disease.

Oxytetracycline, is a broad spectrum tetracycline derivative that exhibits its bacteriostatic action against a wide range of gram-positive and gram-negative organisms by inhibiting bacterial protein synthesis.

Oxytetracycline is approved for use in the following clinical indications:

Treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae.

Oral

Acne vulgaris

Adult: 250-500 mg in single or divided doses for at least 3 months. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Child: ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Renal impairment: Contraindicated.

Hepatic impairment: Contraindicated.

Oral

Rosacea

Adult: For the treatment of severe cases: 250-500 mg in single or divided doses for at least 3 months. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Renal impairment: Contraindicated.

Hepatic impairment: Contraindicated.

Oral

Brucellosis

Adult: In combination with streptomycin: 500 mg 4 times daily. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Child: ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Renal impairment: Contraindicated.

Hepatic impairment: Contraindicated.

Oral

Epididymo-orchitis

Adult: For the treatment of acute cases associated with Chlamydia trachomatis or Neisseria gonorrhoeae: 500 mg 4 times daily for 10 days. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Child: ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Renal impairment: Contraindicated.

Hepatic impairment: Contraindicated.

Oral

Rectal infection due to Chlamydia trachomatis

Adult: 500 mg 4 times daily for 7 days. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Child: ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Oral

Uncomplicated genital infections due to Chlamydia trachomatis

Adult: 500 mg 4 times daily for 7 days. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Child: ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Oral

Nongonococcal urethritis

Adult: For cases associated with Ureaplasma urealyticum: 500 mg 4 times daily for 7 days. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Child: ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Renal impairment: Contraindicated.

Hepatic impairment: Contraindicated.

Oral

Primary syphilis

Adult: As an alternative treatment: Early syphilis: 500 mg 4 times daily for 15 days. Latent syphilis of >1 year or of unknown duration, CV syphilis, or late benign syphilis (except neurosyphilis): 500 mg 4 times daily for 30 days. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Child: ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Renal impairment: Contraindicated.

Hepatic impairment: Contraindicated.

Oral

Secondary syphilis

Adult: As an alternative treatment: Early syphilis: 500 mg 4 times daily for 15 days. Latent syphilis of >1 year or of unknown duration, CV syphilis, or late benign syphilis (except neurosyphilis): 500 mg 4 times daily for 30 days. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Child: ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Renal impairment: Contraindicated.

Hepatic impairment: Contraindicated.

Oral

Streptococcal infectious disease

Adult: Usual dosage range: 250-500 mg 6 hourly. Max treatment duration: 10 days. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Child: ≥12 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Renal impairment: Contraindicated.

Hepatic impairment: Contraindicated.

Oxytetracycline is available in the form of ointment, injection, solution, capsule, suspension, tablet.

Oxytetracycline may be contraindicated in the following:

Hypersensitivity to oxytetracycline or to other tetracycline antibiotics. Porphyria, SLE. Hepatic and renal impairment. Children <12 years. Pregnancy and lactation. Patients receiving vitamin A or retinoid therapy.

Photosensitivity manifested by an exaggerated sunburn reaction has been observed in some individuals taking tetracyclines. Patients apt to be exposed to direct sunlight or ultraviolet light should be advised that this reaction can occur with tetracycline drugs, and treatment should be discontinued at the first evidence of skin erythema.

The antianabolic 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.

Precautions

As with other antibiotic preparations, use of this drug may result in overgrowth of non-susceptible organisms, including fungi. If superinfection occurs, the antibiotic should be discontinued and appropriate therapy instituted.

In venereal diseases when coexistent syphilis is suspected, a dark field examination should be done before treatment is started and the blood serology repeated monthly for at least 4 months.

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

In long term therapy, periodic laboratory evaluation of organ systems, including hematopoietic, renal and hepatic studies should be performed.

All infections due to Group A beta-hemolytic streptococci should be treated for at least 10 days.

Since bacteriostatic drugs may interfere with the bactericidal action of penicillin, it is advisable to avoid giving tetracycline in conjunction with penicillin.

Oxytetracycline use in breast feeding patients is not known.

The adverse reactions related to molecule Oxytetracycline can be categorized as

• Common Adverse effects:

Hematologic disorders (e.g. hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia), increased BUN, intracranial hypertension, photosensitivity, overgrowth of non-susceptible organisms, permanent yellow-grey-brown tooth discoloration.

• Less Common adverse effect:

Gastrointestinal irritation, nausea, abdominal discomfort, vomiting, diarrhea, anorexia, dysphagia, pseudomembranous colitis, glossitis

• Rare adverse effects:

Skin and subcutaneous tissue disorders: Macropapular and erythematous rash, urticaria, angioneurotic oedema, anaphylaxis, anaphylactoid purpura, exfoliative dermatitis, exacerbation of SLE.

The clinically relevant drug interactions of Oxytetracycline are briefly summarized here:

• Impaired absorption with antacids, Fe, Al, Ca, Mg, Zn, and anti-diarrheal preparations (e.g. kaolin-pectin, bismuth subsalicylate).
• May impair renal function with diuretics.
• May depress plasma prothrombin activity; dosage reduction of anticoagulants may be needed.
• May prolong the therapeutic activity of coumarin anticoagulants. May increase the hypoglycemic effects of insulin and sulfonylureas.
• May diminish the therapeutic effect of penicillin.
• May cause breakthrough bleeding with oral contraceptives.

The common side of Oxytetracycline include the following

Hematologic disorders (e.g. hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia), increased BUN, intracranial hypertension, photosensitivity, overgrowth of non-susceptible organisms, permanent yellow-grey-brown tooth discoloration.

The use of Oxytetracycline should be prudent in the following group of special populations:

Pregnancy Category D

Nursing Mothers

NA

Pediatric Use

All tetracyclines form a stable calcium complex in any bone forming tissue. A decrease in the fibula growth rate has been observed in prematures given oral tetracycline in doses of 25 mg/kg every 6 hours. This reaction was shown to be reversible when the drug was discontinued.

The use of drugs of the tetracycline class during tooth development ( infancy, and childhood to the age of 8 years) may cause permanent discoloration of the teeth (yellow-gray-brown). This adverse reaction is more common during long term use of the drugs but has been observed following repeated short term courses. :enamel hypoplasia has also been reported. Tetracycline drugs, therefore, should not be used in this age group unless other drugs are not likely to be effective or are contraindicated

Geriatric Use

There is no FDA guidance on the use of Oxytetracycline in geriatric settings.

Pharmacodynamics:

Oxytetracycline is known as a broad-spectrum antibiotic due to its activity against such a wide range of infections. It was the second of the tetracyclines to be discovered. Oxytetracycline, like other tetracyclines, is used to treat many infections common and rare. Its better absorption profile makes it preferable to tetracycline for moderately severe acne, but alternatives should be sought if no improvement occurs by 3 months.

Pharmacokinetics:

Absorption: Incompletely and irregularly absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 1-4 hours.

Distribution: Widely distributed throughout the body tissues and fluids. Crosses the placenta and enters breast milk. Plasma protein binding: Approx 20-40%.

Excretion: Via urine (40-70%); faeces. Elimination half-life: Approx 6-12 hours.

• https://www.pfizer.com/products/product-detail/altace
• https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022021s008lbl.pdf
• https://go.drugbank.com/drugs/DB00178