Oxytetracycline Hydrochloride

(BANM, rINNM)
Synonyms: Hidrocloruro de oxitetraciclina; Oksitetraciklino hidrochloridas; Oksitetrasiklin Hidroklorür; Oksitetrasykliinihydrokloridi; Oksytetracykliny chlorowodorek; Oxitetraciklin-hidroklorid; Oxitetracyklinhydroklorid; Oxytétracycline, chlorhydrate d’; Oxytetracyclini hydrochloridum; Oxytetracyklin-hydrochlorid.
Cyrillic synonym: Окситетрациклина Гидрохлорид.

💊 Chemical information

Chemical formula: C22H24N2O9,HCl = 496.9.
CAS — 2058-46-0.
ATC — D06AA03; G01AA07; J01AA06; S01AA04. ATC Vet — QD06AA03; QG01AA07; QJ01AA06; QS01AA04.

Pharmacopoeias.

In Chin., Eur., Int., Jpn, and US.

Ph. Eur. 6.2

(Oxytetracycline Hydrochloride). A yellow, hygroscopic, crystalline powder. Freely soluble in water; sparingly soluble in alcohol. Solutions in water become turbid on standing owing to the precipitation of oxytetracycline. A 1% solution in water has a pH of 2.3 to 2.9. Store in airtight containers. Protect from light.

USP 31

(Oxytetracycline Hydrochloride). A yellow, odourless, hygroscopic, crystalline powder. It decomposes at temperatures exceeding 180°, and exposure to strong sunlight or temperatures exceeding 90° in moist air causes it to darken. Its potency is diminished in solutions having a pH below 2, and it is rapidly destroyed by alkali hydroxide solutions. Freely soluble in water, but crystals of oxytetracycline separate as a result of partial hydrolysis of the hydrochloride; sparingly soluble in alcohol and in methyl alcohol, and even less soluble in dehydrated alcohol; insoluble in chloroform and in ether. pH of a 1% solution in water is between 2.0 and 3.0. Store in airtight containers. Protect from light.

Incompatibility.

Oxytetracycline injections have an acid pH and incompatibility may reasonably be expected with alkaline preparations, or with drugs unstable at low pH. Tetracyclines can chelate metal cations to produce insoluble complexes, and incompatibility has been reported with solutions containing metallic salts. Reports of incompatibility are not always consistent, and other factors, such as the strength and composition of the vehicles used, may play a role.

💊 Adverse Effects and Precautions

As for Tetracycline. Oxytetracycline may produce less tooth discoloration than some other tetracyclines but gastrointestinal symptoms tend to be more severe.

Porphyria.

For the suggestion that oxytetracycline might be porphyrinogenic, see under Tetracycline.

💊 Interactions

As for Tetracycline.

💊 Antimicrobial Action

As for Tetracycline. Oxytetracycline is somewhat less active against many organisms.

💊 Pharmacokinetics

For the general pharmacokinetics of the tetracyclines, see Tetracycline. An oral dose of 500 mg every 6 hours is reported to produce steady-state plasma concentrations of 3 to 4 micrograms/mL. Plasma protein binding is reported to be about 20 to 40% and the half-life to be about 9 hours.

💊 Uses and Administration

Oxytetracycline is a tetracycline derivative with actions and uses similar to those of tetracycline. Oxytetracycline dihydrate or hydrochloride are usually used in tablets, capsules, and injections, and the calcium salt in aqueous oral suspensions; all three are also used in topical preparations. Doses have been expressed as anhydrous oxytetracycline, the dihydrate, or the hydrochloride but in practice this appears to make little difference. Oxytetracycline dihydrate and oxytetracycline hydrochloride 269.8 mg, and oxytetracycline calcium 260.3 mg, are each equivalent to about 250 mg of oxytetracycline. Oxytetracycline is usually given orally in adult doses of 250 to 500 mg four times daily, usually 1 hour before or 2 hours after food. Higher doses, up to 4 g daily, have occasionally been given to adults with severe infection, but increase the risk of adverse effects. Doses of oxytetracycline 250 to 500 mg daily have been used in acne, although the BNF advocates a dose of 1 g daily. Oxytetracycline is sometimes given intramuscularly, in doses of 250 mg once daily or 300 mg daily in 2 or 3 divided doses, but this route may be painful and produces lower blood concentrations than recommended oral doses. As intramuscular injections are painful, lidocaine is usually included in the solution. Oxytetracycline has also been given intravenously. For details of doses in children and adolescents, see below. Oxytetracycline and its salts have been applied topically, often with other agents, as a variety of eye and ear drops, ointments, creams, and sprays.

Administration in children.

In children, the effects on teeth should be considered and tetracyclines only used when absolutely essential. In the UK, oxytetracycline is licensed for use in children aged 12 years and over; the usual adult dose (see above) may be given orally. However, in the USA, it may be given to those over 8 years old in usual oral doses of 25 to 50 mg/kg daily in 4 divided doses or by intramuscular injection in usual doses of 15 to 25 mg/kg (to a maximum of 250 mg) daily in 2 or 3 divided doses.

Skin disorders.

For reference to the use of oxytetracycline in the treatment of various skin disorders, see under Tetracycline.

💊 Preparations

BP 2008: Oxytetracycline Capsules; Oxytetracycline Tablets; USP 31: Oxytetracycline and Nystatin Capsules; Oxytetracycline and Nystatin for Oral Suspension; Oxytetracycline Calcium Oral Suspension; Oxytetracycline for Injection; Oxytetracycline Hydrochloride and Hydrocortisone Acetate Ophthalmic Suspension; Oxytetracycline Hydrochloride and Hydrocortisone Ointment; Oxytetracycline Hydrochloride and Polymyxin B Sulfate Ointment; Oxytetracycline Hydrochloride and Polymyxin B Sulfate Ophthalmic Ointment; Oxytetracycline Hydrochloride and Polymyxin B Sulfate Topical Powder; Oxytetracycline Hydrochloride and Polymyxin B Sulfate Vaginal Tablets; Oxytetracycline Hydrochloride Capsules; Oxytetracycline Injection; Oxytetracycline Tablets.

Proprietary Preparations

Arg.: Terramicina; Braz.: Terramicina; Denm.: Oxytetral; Fr.: Posicycline; Gr.: Terramycin; Hong Kong: Oxylim; Hung.: Te tr a n; India: Terramycin; Indon.: Chemotrex; Corsamycin; Terramycin; Irl.: Clinimycin; Malaysia: Oxylim; Mex.: Metrecina; Oxitraklin; Terrados; Terramicina; Norw.: Oxytetral; Philipp.: Noxebron; Pol.: Oxyterracyna†; Port.: Geomicina†; Terricil; S.Afr.: Acu-Oxytet; Be-Oxytet; Cotet; O-4 Cycline; Oxymycin; Oxypan; Roxy; Spectratet; Tetracem†; Tetramel†; Singapore: Oxylim; Terramycin†; Spain: Terramicina; Swed.: Oxytetral; Thai.: Oxycline; Oxylim; Turk.: Neocol; UK: Oxymycin; Oxytetramix†; USA: Terramycin†; Venez.: Oxifesa†; Terramicina. Multi-ingredient: Arg.: Terra-Cortril; Terra-Cortril Nistatina†; Terramicina con Polimixina B†; Austria: Tetra-Gelomyrtol; Belg.: Eoline†; TerraCortril; Terra-Cortril + Polymyxine B; Terramycine + Polymyxine B; Braz.: Terra-Cortril; Terramicina c/Polimixina; Denm.: Hydrocortison med Terramycin; Hydrocortison med Terramycin og Polymyxin-B; Terramycin Polymyxin B; Fin.: Terra-Cortril; Terra-Cortril P; Fr.: Auricularum; Primyxine†; Ster-Dex; Ger.: Corti Biciron N; Farco-Tril†; Oxy Biciron; Terracortril†; Terramycin†; Tetra-Gelomyrtol; Gr.: Oxacycle-P; Terra-Cortril; Terramycin; Hong Kong: Terramycin with Polymyxin B; Hung.: Oxycort; Tetran-Hydrocortison; India: Terramycin SF; Indon.: Sancortmycin; Terra-Cortril; Terramycin Poly; Israel: Auricularum; Terramycin; Ital.: Cosmiciclina; Malaysia: Terramycin; Mex.: Andociclina Balsamica†; Terramicina; Neth.: Terra-Cortril Gel Steraject met polymyxine-B†; Terra-Cortril met polymyxine-B; Norw.: Terra-Cortril; Terra-Cortril Polymyxin B; Terramycin Polymyxin B; Philipp.: Terramycin; Pol.: Atecortin; Oxycort; Port.: Corticil T; Rus.: Gioxyson (Гиоксизон); Oxycort (Оксикорт); S.Afr.: Terra-Cortril; Terramycin; Singapore: Terramycin; Spain: Coliriocilina Espectro†; TerraCortril; Terramicina; Swed.: Terracortril; Terracortril med polymyxin B; Terramycin Polymyxin B; Switz.: Terracortril†; Thai.: Terramycin; Terrasil†; Turk.: Geotril; Heksa; Polimisin; Sekamisin; Terramycin; UK: Terra-Cortril†; Tr im ovate; USA: Terak; Terra-Cortril; Terramycin with Polymyxin B; Urobiotic-250; Venez.: Ofterra; Terra-Cortril†; Terramicina con Polimixina B.
Published May 08, 2019.