Tetracycline (Sumycin)

Tetracycline (Sumycin) is an antibiotic that acts by inhibiting bacterial protein synthesis. It is used to treat patients with the following conditions:

  • Acute intestinal amebiasis:

    • It is used as adjunctive therapy in acute intestinal amebiasis caused by Entamoeba histolytica.
  • Acne:

    • It is used in conjunction with other therapies to treat severe acne.
  • Actinomycosis:

    • When penicillin is not an option, it is used to treat actinomycosis caused by Actinomyces species.
  • Anthrax:

    • When penicillin is not an option, it is used to treat anthrax caused by Bacillus anthracis.
  • Campylobacter:

    • It is employed to treat infections brought on by Campylobacter foetus.
  • Cholera:

    • It is used to treat cholera that is brought on by Vibrio cholera.
  • Clostridium:

    • When penicillin is not advised, it is used to treat infections brought on by Clostridium spp.
  • Gram-negative infections:

    • Escherichia coli, Enterobacter aerogenes, Shigella spp., Acinetobacter spp., Klebsiella spp., and Bacteroides spp. infections are treated with it.
  • Listeriosis:

    • It is used in the treatment of listeriosis due to Listeria monocytogenes when penicillin is contraindicated.
  • Ophthalmic infections:

    • It is used in the treatment of inclusion conjunctivitis or trachoma caused by Chlamydia trachomatis.
  • Relapsing fever:

    • It is used in the treatment of relapsing fever due to Borrelia spp.
  • Respiratory tract infection:

    • It is used for respiratory tract infections due to Haemophilus influenzae (upper respiratory tract only), Klebsiella spp. (lower respiratory tract only), Mycoplasma pneumoniae (lower respiratory tract only), Streptococcus pneumoniae, or Streptococcus pyogenes.
  • Rickettsial infections:

    • It is used to treat typhus group infections, Q fever, Rocky Mountain spotted fever, and rickettsialpox brought on by Rickettsiae.
  • Sexually transmitted diseases:

    • When penicillin is contraindicated, it is used to treat conditions like lymphogranuloma venereum, uncomplicated urethral, endocervical, or rectal infections caused by C. trachomatis, granuloma inguinale (donovanosis), chancroid caused by Haemophilus ducreyi, and syphilis caused by Treponema pallidum.
  • Skin and skin structure infections:

    • Staphylococcus aureus or S. pyogenes-related skin and skin structure infections are treated with it.
  • Urinary tract infections:

    • It is used to treat urinary tract infections brought on by gram-negative bacteria that are susceptible to it (eg, E. coli, Klebsiella spp.).
  • Vincent infection:

    • It is used in Treatment of Vincent infection caused by Fusobacterium fusiforme when penicillin is contraindicated.
  • Yaws:

    • When penicillin is not recommended, it is used to treat yaws brought on by Treponema pertenue.
  • Zoonotic infections:

    • It is used in the treatment of psittacosis also called ornithosis) due to Chlamydophila psittaci; brucellosis due to Brucella spp. (in conjunction with an aminoglycoside); and bartonellosis due to Bartonella bacilliformis.
  • Off Label Use of Tetracycline in Adults:

    • Helicobacter pylori eradication;
    • Malaria;
    • Periodontitis associated with the presence of Actinobacillus actinomycetem comitans

Tetracycline Dose in Adults

Tetracycline usual dosage range:

    • 250 to 500 mg given every 6 to 12 hours

Dose in the treatment of Acne:

  • Once an improvement is seen, gradually reduce the dose from 1 g administered daily in divided doses to 125 to 500 mg/day (alternate day or intermittent therapy may be adequate in some patients).

Dose in the treatment of Helicobacter pylori eradication (off-label): 

  • American College of Gastroenterology guidelines
    • Bismuth quadruple regimen :

      • 500 mg administered four times day, along with:
        • standard-dose proton pump inhibitor two times a day,
        • metronidazole 250 mg 4 times a day or 500 mg 3 or 4 times a day, and
        • either bismuth sub-citrate 120 - 300 mg 4 times a day or bismuth sub-salicylate 300 mg 4 times 
      • keep up the routine for 10 to 14 days.

Dose in the treatment of severe Malaria (off-label):

  • For one week, 250 mg of quinidine gluconate were administered four times daily.

Dose in the treatment of uncomplicated Malaria (off-label):

  • Given with quinine sulphate, 250 mg four times day for one week.

Dose in the treatment of Periodontitis (off-label):

  • every six hours till improvement, 250 mg (usually 10 days)

Dose in the treatment of Syphilis, penicillin-allergic patients:

  • Early syphilis (primary or secondary infection):

    • Given four times daily for 14 days, 500 mg.
  • Latent syphilis (late or of unknown duration):

    • For 28 days, 500 mg were administered four times daily.
  • Tularemia (mild to moderate):

    • Taking 500 mg four times every day for at least 14 days
  • Vibrio cholerae:

    • administered four times daily for three days, 500 mg

Tetracycline Dose in Children

General dosing, susceptible infection:

  • Children ≥8 years and Adolescents:
    • Split doses of 25 to 50 mg/kg/day administered every six hours

Dose in the treatment of Acne:

  • Children ≥8 years and Adolescents:
    • Split doses of 25 to 50 mg/kg/day administered every six hours

Tetracycline dose in the treatment of Malaria:

  • It is used in combination with other antimalarial agents in uncomplicated chloroquine-resistant infections caused by:
    • P. falciparum,
    • P. vivax or
    • unknown species
    • Children ≥8 years and Adolescents:

      • Non-HIV-exposed/-positive: Oral:

        • 500 mg administered twice daily
      • HIV-exposed/-positive: Oral:

        • every six hours for seven days at a dose of 6.25 mg/kg.
        • 250 mg/dose is the maximum dosage.
    • Severe infection :

      • Note:

        • Children ≥8 years and Adolescents: Every six hours for seven days, 6 to 12.5 mg/kg/dose is administered.
        • 500 mg/dose is the maximum dosage.
      • Non-HIV-exposed/-positive: Oral:

        • Combined use with additional antimalarial medications
      • HIV-exposed/-positive: Oral:

        • every six hours for seven days at a dose of 6.25 mg/kg.
        • 250 mg/dose is the maximum dosage.

Dose in the treatment of Syphilis in penicillin-allergic patients:

  • Adolescents: Oral: Every six hours for seven days, 6 to 12.5 mg/kg/dose is administered.

  • 500 mg/dose is the maximum dosage.

    • Early syphilis (primary or secondary infection):

      • Four doses of 500 mg every day for fourteen days.
    • Latent syphilis (late or of unknown duration):

      • Four doses of 500 mg every day for 28 days.

Pregnancy Risk Factor D

  • The placenta is crossed by tetracycline.
  • In utero exposure can cause permanent yellowing, graying, or browning of teeth. This is more common after repeated or long-term exposure.
  • It has been reported that tetracycline can cause liver damage during pregnancy.
  • Women with renal disease may be at greater risk of developing hepatic impairment from tetracycline.
  • Tetracyclines, as a class, are generally second-line antibiotics for pregnant women. They should be avoided.
  • Many guidelines consider tetracycline contraindicated in pregnancy. However, it is considered a relative contraindication for pregnant women.
  • Other agents are often preferred when systemic antibiotics are required for dermatologic conditions in pregnant ladies.

Tetracycline use during breastfeeding:

  • Breast milk contains Tetracycline.
  • According to the manufacturer of the product, when deciding whether to breastfeed during therapy or not, it should consider the risks to the infant as well as the benefits to the mother.
  • Tetracyclines as a class are not recommended for nursing mothers because they can permanently stain breast-feeding infants' teeth.
  • Sources note that breastfeeding can be continued during tetracycline therapy, but they recommend using alternative medications whenever possible.
  • Others note that some short-term exposure is acceptable. However, breast-feeding mothers should avoid long-term use (e.g., to treat acne).
  • Breast milk antibiotics can cause non-dose-related changes in the bowel flora.
  • Monitor infants for GI disorders.

Tetracycline dose in Kidney disease:

  • Manufacturer’s labeling:

    • The manufacturer has not recommended any dose adjustment in patients with kidney disease.
  • Alternative dosing 

    • GFR greater than 50 mL/minute:

      • The recommended dose based on indication should be given every 8 to 12 hours.
    • GFR 10 - 50 mL/minute:

      • The recommended dose based on the indication should be given every 12 - 24 hours.
    • GFR less than 10 mL/minute:

      • The recommended dose based on the indication should be given as once daily.

Tetracycline Dose in Liver Disease:

  • The manufacturer has not recommended any dose adjustment in patients with liver disease.

Side effects of Tetracycline (Sumycin):

  • Cardiovascular:

    • Pericarditis
    • Thrombophlebitis
  • Central Nervous System:

    • Bulging Fontanel (Infants)
    • Increased Intracranial Pressure
    • Paresthesia
    • Pseudotumor Cerebri
  • Dermatologic:

    • Exfoliative Dermatitis
    • Nail Discoloration
    • Pruritus
    • Skin Photosensitivity
  • Gastrointestinal:

    • Abdominal Cramps
    • Anorexia
    • Dental Discoloration (Young Children)
    • Diarrhea
    • Enamel Hypoplasia (Young Children)
    • Esophagitis
    • Nausea
    • Pancreatitis
    • Pseudomembranous Colitis (Antibiotic-Associated)
    • Staphylococcal Enterocolitis
    • Vomiting
  • Genitourinary:

    • Azotemia
  • Hepatic:

    • Hepatotoxicity
  • Hypersensitivity:

    • Anaphylaxis
    • Hypersensitivity Reaction
  • Infection:

    • Fungal Superinfection (Candida)
    • Superinfection
  • Renal:

    • Acute Renal Failure
    • Renal Insufficiency

Contraindication to Tetracycline (Sumycin) Include:

  • Severe allergic reactions to any tetracyclines, or any part of the formulation.

Warnings and precautions

  • BUN Increased

    • Patients with impaired renal function should be cautious when using it as it can raise serum BUN levels due to its antianabolic properties.
  • Intracranial hypertension (pseudotumor Cerebri):

    • It may cause headaches, diplopias, blurred vision, vision loss, blurred vision, vision impairment, and/or even papilledema.
    • Patients on oral contraceptives, obese women, pregnant women and people with a history or intracranial hypertension are at highest risk for pseudotumor cerebri.
    • Concomitant use of isotretinoin (known to cause pseudotumor cerebri [PTC]) and tetracycline is avoided.
    • If the drug is not stopped promptly, permanent vision loss is possible.
    • It is important to seek prompt medical attention if you experience visual symptoms.
    • Patients should be monitored until intracranial pressure stabilizes.
  • Photosensitivity

    • Photosensitivity patients who experience skin erythema or photosensitivity should stop using it.
    • Avoid using tanning equipment.
    • Patients should avoid prolonged sun exposure and should be encouraged to use sunscreens.
  • Superinfection

    • Long-term use of the drug can lead to superinfections, especially fungal or bacterial.
    • Pseudomembranous collitis and bacterial superinfection, such as clostridioides difficile-associated diarrhoea (CDAD), are potential side effects.
    • Clostridioides difficile -associated diarrhea (CDAD), can occur up to 2 months after the end of antibiotics.
  • Hepatic impairment

    • Patients with preexisting liver or renal disease are at risk of developing hepatic impairment.
  • Renal impairment

    • Patients with impaired renal function need to use it with caution.
    •  Recommendations for adjustment of the dos

Tetracycline: Drug Interaction

Risk Factor C (Monitor therapy)

Aminolevulinic Acid (Topical)

Aminolevulinic Acid's photosensitizing impact may be enhanced by photosensitizing agents (Topical).

Atovaquone

Tetracycline (Systemic) may lower atovaquone's serum levels.

BCG Vaccine (Immunization)

Antibiotics may reduce the BCG vaccine's therapeutic effect (Immunization).

Bosentan

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

CYP3A4 Inducers (Moderate)

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Deferasirox

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Erdafitinib

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Ivosidenib

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Lactobacillus and Estriol

The therapeutic effects of Lactobacillus and Estriol may be reduced by antibiotics.

Magnesium Dimecrotate

May interact with tetracyclines through an unknown method.

Mipomersen

Tetracyclines may intensify Mipomersen's hepatotoxic effects.

Neuromuscular-Blocking Agents

Tetracyclines might make neuromuscular-blocking agents more effective at blocking neuromuscular activity.

Porfimer

The photosensitizing effect of Porfimer may be strengthened by photosensitizing agents.

QuiNINE

The blood levels of QuiNINE may rise when taken systemically with tetracycline.

Sarilumab

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Siltuximab

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Tocilizumab

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Verteporfin

Verteporfin's photosensitizing effect may be strengthened by photosensitizing agents.

Vitamin K Antagonists (eg, warfarin)

Tetracyclines might make Vitamin K antagonists' anticoagulant effects even more potent.

Risk Factor D (Consider therapy modification)

Antacids

Tetracyclines' absorption might be reduced. When possible, administer antacids and oral tetracycline derivatives at different times to reduce the severity of this potential interaction.

Bile Acid Sequestrants

Tetracyclines' absorption might be reduced.

Bismuth Subcitrate

Tetracyclines' serum concentration can drop. Treatment: After taking bismuth subcitrate, avoid taking oral tetracyclines for 30 minutes. This has dubious significance for at least certain H. pylori infection treatment strategies.

Bismuth Subsalicylate

Tetracyclines' serum concentration can drop. Tetracyclines may be dosed 2 hours before or 6 hours after bismuth. It's debatable if Helicobacter pylori eradication strategies require separating dosages.

Calcium Salts

Tetracyclines' serum concentration can drop. Management: If oral calcium and oral tetracyclines must be administered simultaneously, think about giving each medication several hours apart.

CYP3A4 Inducers (Strong)

May speed up CYP3A4 substrate metabolism (High risk with Inducers). Management: Take into account a substitute for one of the interfering medications. Specific contraindications may apply to some combinations. the relevant manufacturer's label.

Dabrafenib

May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: When possible, look for substitutes for the CYP3A4 substrate. If concurrent therapy cannot be avoided, pay special attention to the substrate's clinical consequences (particularly therapeutic effects).

Enzalutamide

May lower the serum level of CYP3A4 substrates (High risk with Inducers). Treatment: Enzalutamide should not be used concurrently with CYP3A4 substrates that have a limited therapeutic index. Enzalutamide use, like with the use of any other CYP3A4 substrate, should be done cautiously and under close observation.

Iron Salts

Tetracyclines may make it harder for iron salts to be absorbed. Tetracyclines' serum levels may drop if you take iron salts. Iron Carboxymaltose, Iron Gluconate, Iron Hydroxide Polymaltose Complex, Iron Pyrophosphate Citrate, Ferumoxytol, Iron Dextran Complex, Iron Isomaltoside, and Iron Sucrose are exceptions.

Lanthanum

Tetracyclines' serum concentration can drop. Treatment: Give oral antibiotics containing tetracycline at least two hours before or after lanthanum.

Lorlatinib

May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Avoid taking lorlatinib at the same time as any CYP3A4 substrates for which even a small drop in serum levels of the substrate could result in therapeutic failure and negative clinical outcomes.

Magnesium Salts

Tetracyclines' absorption might be reduced. applies only to oral forms of each drug.

Mitotane

May lower the serum level of CYP3A4 substrates (High risk with Inducers). Treatment: When administered in individuals receiving mitotane, doses of CYP3A4 substrates may need to be significantly modified.

Multivitamins/Minerals (with ADEK, Folate, Iron)

Tetracyclines' serum concentration can drop. Treatment: Separate the delivery of each medication by several hours if coadministration of an oral tetracycline and a multivitamin containing polyvalent cations cannot be avoided.

Multivitamins/Minerals (with AE, No Iron)

Tetracyclines' serum concentration can drop. Treatment: Separate the delivery of each medication by several hours if coadministration of an oral tetracycline and a multivitamin containing polyvalent cations cannot be avoided.

Penicillins

Tetracyclines may lessen penicillins' capacity for healing.

Quinapril

Tetracyclines' serum concentration can drop. To lessen the possibility of an interaction, quinapril and oral tetracycline derivative dosages should be separated by at least two hours. If these products are administered concurrently, keep an eye out for any tetracycline efficacy reduction.

Sodium Picosulfate

Antibiotics may reduce Sodium Picosulfate's therapeutic impact. Management: If a patient previously used or is currently using an antibiotic, think about utilising an alternative product for bowel cleansing prior to a colonoscopy.

St John's Wort

May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Take into account a substitute for one of the interfering medications. Specific contraindications may apply to some combinations. the relevant manufacturer's label.

Sucralfate

Tetracyclines' absorption might be reduced. To lessen the effects of this interaction, administer the tetracycline derivative at least two hours before sucralfate.

Sucroferric Oxyhydroxide

Tetracyclines' serum concentration can drop. Treatment: Give doxycycline orally or intravenously at least an hour before taking sucroferric oxyhydroxide. There are currently no specific dose separation recommendations for additional tetracyclines. Parenteral tetracycline treatment is not predicted to cause any interactions.

Typhoid Vaccine

The Typhoid Vaccine's therapeutic benefits may be reduced by antibiotics. The only strain impacted is the live attenuated Ty21a strain. Treatment: Patients receiving systemic antibacterial drugs should refrain from receiving the live attenuated typhoid vaccination (Ty21a). It is recommended to wait at least 3 days following the last dose of antibacterial medication before administering this vaccine.

Zinc Salts

Tetracyclines' absorption might be reduced. Only a problem if both medications are taken orally. Management: Take doxycycline into account as a tetracycline derivative that does not interact. To reduce interaction, administer oral zinc salts and tetracycline derivatives at least two hours apart. Exceptions: chloride of zinc.

Risk Factor X (Avoid combination)

Aminolevulinic Acid (Systemic)

Aminolevulinic Acid's photosensitizing impact may be enhanced by photosensitizing agents (Systemic).

BCG (Intravesical)

Antibiotics may lessen BCG's therapeutic effects (Intravesical).

Cholera Vaccine

The therapeutic benefit of the cholera vaccine may be reduced by antibiotic use. Management: Cholera vaccine should not be administered to individuals taking systemic antibiotics or within 14 days after taking oral or parenteral antibiotics.

Mecamylamine

Sulfa drugs might strengthen Mecamylamine's ability to suppress neuromuscular activity.

Methoxyflurane

Tetracyclines might make Methoxyflurane's nephrotoxic effects worse.

Retinoic Acid Derivatives

Tetracyclines might make retinoic acid derivatives more harmful or poisonous. It is especially concerning when pseudotumor cerebri develops. Exceptions: Tretinoin, Adapalene, and Bexarotene (Topical) (Topical).

Strontium Ranelate

Tetracyclines' serum concentration can drop. Management: It is advised that strontium ranelate therapy be stopped during tetracycline therapy in order to reduce any potential impact of strontium ranelate on tetracycline antibiotic concentrations.

Monitor:

  • Renal, hepatic, and hematologic function test
  • temperature
  • WBC, cultures and sensitivity
  • appetite
  • mental status

How to administer Tetracycline (Sumycin)?

  • Administer with enough liquids to lower the risk of esophageal irritation and ulcers and on an empty stomach (i.e., 1 hour before or 2 hours after meals) to increase overall absorption.
  • Give at least 1 to 2 hours prior to, or 4 hours after antacid because aluminum and magnesium cations may chelate with tetracycline and reduce its total absorption.

Mechanism of action of Tetracycline (Sumycin):

  • By attaching to the 30S or 50S ribosomal (subunits) of the sensitive bacteria, it prevents the synthesis of bacterial proteins.
  • It can also alter the cytoplasmic layer.

Absorption:

  • Oral: 77% to 88%
  • Intramuscular absorption is poor, with less than 60% of dose absorbed

Distribution:

  • It is well dispersed to most human tissues and fluids, including pleural, synovial, and ascitic fluids. It also has weak penetration into cerebral spinal fluid (CSF).

Protein binding:

  • 55% to 64%

Half-life elimination:

  • 6 to 11 hours

Time to peak, serum:

  • Oral: 2 to 4 hours

Excretion:

  • Via Urine (30%) & feces (20% to 60%) (Agwuh 2006 

International Brands of Tetracycline:

  • A tetra
  • Achromycin
  • Achromycin V
  • Aclocin
  • Acromicina
  • Alexcyclin
  • Ambramicina
  • Apocyclin
  • Atron
  • Beatacycline
  • Berciclina
  • Biotine
  • Bocycline
  • Cadicycline
  • Ciclotetryl
  • Cinatrex
  • Clincor
  • Cyclabid
  • Dhatracin
  • Dicyclin Forte
  • Dumocycline
  • Eapatet
  • Emcycline
  • Erifor
  • Florocycline
  • Hexacycline
  • Hostacyclin
  • Hostacycline
  • Hostacycline-P
  • Hydromycin
  • Ibicyn
  • Imex
  • Latycin
  • Lenocin
  • Medocycline
  • Mephicycline
  • Metacycline
  • Ophth-tetracil
  • Opticyclin
  • Oricyclin
  • Panmycin
  • Pantocycline
  • Quemiciclina-S
  • Recycline
  • Resteclin
  • Rimatet
  • Servitet
  • Steclin V
  • Subamycin
  • Tc
  • Tefilin
  • Teracin
  • Tetrabiotico
  • Tetrachem
  • Tetracid
  • Tetraciklins
  • Tetracilin
  • Tetracin
  • Tetracyclinum
  • Tetracyklin
  • Tetradar
  • Tetralan
  • Tetramed
  • Tetramig
  • Tetramin
  • Tetran
  • Tetrana
  • Tetrarco
  • Tetras
  • Tetraseptin
  • Tetrasuiss
  • Tetrecu
  • Tetret-250
  • Tetrex
  • Tetrm
  • Tetrop
  • Tevacycline
  • Traxetrine
  • Ttmycin
  • Wintel
  • Xepacycline

Tetracycline Brands in Pakistan:

Tetracycline (HCl) [Eye Oint 1 %w/w]

Ophth-Tetracyl Ophth-Pharma (Pvt) Ltd.

 

Tetracycline (HCl) [Tabs 250 mg]

Rekomycin Reko Pharmacal (Pvt) Ltd.
Tetracycline Unexo Labs (Pvt) Ltd.

 

Tetracycline (HCl) [Tabs 500 mg]

Rekomycin Reko Pharmacal (Pvt) Ltd.

 

Tetracycline (HCl) [Caps 250 mg]

Dosamycin Dosaco Laboratories
Pexocycline Karachi Pharmaceutical Laboratory
Tetracycline Lisko Pakistan (Pvt) Ltd
Tetracycline Unexo Labs (Pvt) Ltd.