Targocid

What Is Targocid and What Is It Used For?

Targocid is the originator brand of teicoplanin, a glycopeptide antibiotic derived from fermentation products of the soil microorganism Actinoplanes teichomyceticus. First approved in Europe in the late 1980s, it has been a mainstay of hospital antimicrobial therapy for decades and remains listed on the World Health Organization's Model List of Essential Medicines as a reserve antibiotic for serious Gram-positive infections. The 200 mg vial is the most frequently used strength for routine parenteral dosing in adults, with higher doses typically built up by combining multiple vials.

Teicoplanin, the active ingredient in Targocid, exerts its bactericidal effect by binding to the D-alanyl-D-alanine terminus of peptidoglycan precursor units in the bacterial cell wall. This binding physically blocks the transglycosylation and transpeptidation reactions that cross-link peptidoglycan strands. Without a stable cell wall, susceptible Gram-positive bacteria lyse under osmotic pressure and die. The mechanism is very similar to that of vancomycin but operates at a different step of wall assembly, and teicoplanin's more lipophilic side chain also gives it a strong affinity for the bacterial membrane, contributing to its prolonged tissue presence.

Targocid is active against a broad range of Gram-positive organisms, including methicillin-sensitive and methicillin-resistant Staphylococcus aureus (MSSA and MRSA), coagulase-negative staphylococci, streptococci (including S. pneumoniae, S. pyogenes and viridans group streptococci), Enterococcus faecalis, Listeria monocytogenes, corynebacteria and Clostridioides difficile. It has no activity against Gram-negative organisms, mycobacteria or fungi, and should not be used as monotherapy when these pathogens are suspected.

The approved clinical indications for Targocid include treatment of the following infections in adults and children, including neonates, when caused by susceptible Gram-positive pathogens:

• Complicated skin and soft tissue infections – including cellulitis, surgical site infections, infected diabetic foot ulcers and deep wound infections.
• Bone and joint infections – acute and chronic osteomyelitis, septic arthritis and prosthetic joint infections, where prolonged antibiotic courses are frequently required.
• Hospital-acquired and ventilator-associated pneumonia – when Gram-positive pathogens are identified or suspected.
• Complicated urinary tract infections – involving Gram-positive organisms such as enterococci.
• Infective endocarditis – infection of the native or prosthetic heart valves, a life-threatening condition requiring intensive, prolonged antibiotic therapy with therapeutic drug monitoring.
• Peritonitis – including bacterial peritonitis in patients on continuous ambulatory peritoneal dialysis (CAPD).
• Bacteremia (bloodstream infection) – occurring in association with any of the above conditions.
• Clostridioides difficile colitis (CDI) – given orally as a reconstituted solution, Targocid is effective against moderate-to-severe CDI, a major cause of hospital-acquired diarrhea.

A key pharmacological advantage of Targocid over vancomycin is its very long elimination half-life, approximately 70 to 100 hours in patients with normal renal function, which allows once-daily maintenance dosing after an initial loading phase. This simplifies treatment schedules, reduces infusion-related nursing workload and facilitates outpatient parenteral antibiotic therapy (OPAT) in appropriately selected patients. Targocid is also compatible with intramuscular administration, which is useful when intravenous access is limited — something not possible with vancomycin because of the severe local tissue irritation it causes.

Because resistance to teicoplanin remains uncommon in most regions, Targocid continues to play an important role in antimicrobial stewardship programs for serious Gram-positive infections. Its use should always be guided by susceptibility testing and local microbiology data, and reserved for situations where first-line narrower-spectrum agents are not suitable.

What Should You Know Before Taking Targocid?

Contraindications

Targocid must not be used in patients with a known hypersensitivity to teicoplanin or to any of the other ingredients of the medicine. The excipient profile typically includes sodium chloride and sodium hydroxide for pH adjustment, with water for injections as the diluent. Patients who have previously experienced an allergic reaction to teicoplanin — for example rash, urticaria, angio-oedema, bronchospasm or anaphylaxis — must not receive this medicine again, as re-exposure can trigger a more severe reaction.

Warnings and Precautions

Before you are given Targocid, inform your doctor, pharmacist or nurse about any of the following conditions, as they may affect how the medicine is used or require additional monitoring:

• Vancomycin allergy: Patients with known hypersensitivity to vancomycin may be at increased risk of cross-reactivity with teicoplanin. Although the two molecules have distinct structures, both belong to the glycopeptide class. Treatment should be initiated cautiously and, where possible, under close clinical observation.
• Red man (red neck) syndrome: This infusion-related reaction, characterised by flushing and erythema of the upper body, is less common with teicoplanin than with vancomycin but has been described. Slowing the rate of infusion to at least 30 minutes reduces the risk.
• Thrombocytopenia: A reversible decrease in platelet count has been reported, particularly at doses > 12 mg/kg twice daily. Regular monitoring of complete blood counts is recommended during prolonged treatment.
• Renal impairment: Teicoplanin is eliminated almost entirely by the kidneys. Patients with reduced creatinine clearance need dose reduction from the fourth day of therapy and closer monitoring of serum levels to avoid accumulation.
• Hepatic impairment: Mild to moderate hepatic impairment does not normally require dose adjustment, but transient elevations in liver enzymes have been reported during therapy and should be monitored.
• Concurrent ototoxic or nephrotoxic medicines: If you are taking other medications that can affect the kidneys or hearing (see Drug Interactions), your doctor will monitor you more closely with blood tests, serum creatinine and audiometry where appropriate.
• Risk of superinfection: Prolonged use of any antibiotic, including Targocid, may allow overgrowth of non-susceptible organisms such as Gram-negative bacteria or fungi, requiring additional treatment.

During treatment, your medical team may order regular blood tests to check kidney function (serum creatinine), liver enzymes and complete blood counts. Hearing tests (audiometry) may be considered in high-risk patients. Closer monitoring is especially recommended when:

• Treatment is expected to continue for more than 7–10 days
• High loading or maintenance doses (12 mg/kg twice daily or 12 mg/kg once daily) are required, as in endocarditis or osteomyelitis
• You have pre-existing kidney impairment or are elderly
• You are receiving concurrent nephrotoxic or ototoxic medications
• You are critically ill, on extracorporeal circuits or receiving renal replacement therapy

Therapeutic drug monitoring (TDM) of teicoplanin trough serum concentrations is strongly recommended in routine practice, particularly for deep-seated infections such as endocarditis, osteomyelitis, prosthetic joint infections and staphylococcal bacteremia. Target trough levels of at least 10 mg/L are appropriate for most infections, while targets of 15–30 mg/L or even higher (up to 30–60 mg/L) are recommended for endocarditis, osteomyelitis and serious staphylococcal infections, according to international guidance. TDM reduces both the risk of under-dosing (which can lead to treatment failure and emergence of resistance) and over-dosing (which can lead to nephrotoxicity or thrombocytopenia).

Pregnancy and Breastfeeding

If you are pregnant, think you may be pregnant or are planning to have a baby, speak to your doctor before receiving Targocid. There is limited human data on the safety of teicoplanin in pregnancy, and the medicine should only be used when the potential benefit justifies the potential risk to the fetus. The theoretical concerns relate mainly to possible damage to the developing inner ear (ototoxicity) and kidneys (nephrotoxicity) based on the known pharmacology of glycopeptide antibiotics, particularly in the second and third trimesters.

Information about excretion of teicoplanin into human breast milk is limited. If you are breastfeeding, discuss the risks and benefits with your doctor. A decision should be made either to discontinue breastfeeding or to discontinue or avoid Targocid therapy, taking into account the benefit of breastfeeding for the child and the benefit of treatment for the mother.

Animal reproductive studies have not shown evidence of impaired fertility or teratogenic effects at therapeutic doses. However, animal data are not always predictive of the human response, and specialist advice should be sought where possible.

Driving and Using Machines

Targocid may cause headache, dizziness or, uncommonly, hearing changes. If you experience any of these effects, you should not drive or operate machinery until you feel well enough to do so safely. Most hospitalised patients receiving Targocid are not driving during acute therapy, but this becomes relevant for those receiving outpatient parenteral antibiotic therapy.

How Does Targocid Interact with Other Drugs?

Drug interactions are an important consideration when using Targocid. Although teicoplanin has relatively few pharmacokinetic interactions — it is not metabolised by the cytochrome P450 system and does not significantly induce or inhibit these enzymes — its pharmacodynamic interactions with nephrotoxic and ototoxic medications are clinically important. Always tell your doctor or pharmacist about all medicines you are currently taking, have recently taken or may take, including over-the-counter products and supplements.

The following drug interactions are of particular clinical importance during Targocid therapy:

Major Interactions

Additional Considerations

Other potentially nephrotoxic agents, including non-steroidal anti-inflammatory drugs (NSAIDs), angiotensin-converting enzyme inhibitors, angiotensin receptor blockers and iodinated contrast media, should be used with caution during Targocid therapy. While formal interaction studies are limited, the theoretical risk of additive renal injury warrants careful fluid management and renal function monitoring when these agents are combined, especially in elderly or critically ill patients.

Targocid does not appear to interact significantly with warfarin, digoxin or most common oral hypoglycaemic agents, and there are no clinically important interactions with oral contraceptives. However, as with any hospitalised patient receiving multiple medications, a thorough medication review should be performed by the clinical pharmacist or attending physician, and therapeutic drug monitoring should be used to individualise teicoplanin exposure.

It is also worth noting that Targocid is physically incompatible with some intravenous solutions containing heavy metal ions and with certain injectable diazepam preparations. For this reason, it should be administered through a dedicated line or flushed adequately if a shared line must be used.

What Is the Correct Dosage of Targocid?

Targocid is always administered by a healthcare professional in a hospital or clinical setting. The dose is individualised based on the type of infection, its severity, the patient's age, body weight, renal function and, where relevant, therapeutic drug monitoring levels. Targocid can be given as a bolus intravenous injection over 3–5 minutes, as an intravenous infusion over 30 minutes, as an intramuscular injection, or orally (for C. difficile colitis). For neonates up to 2 months of age, only intravenous infusion should be used.

Adults and Adolescents (12 Years and Older) with Normal Kidney Function

For most routine infections in adults of average weight, a single 400 mg dose (or two 200 mg vials) given once daily after the loading phase is a convenient practical regimen. For endocarditis, osteomyelitis and other deep-seated infections, higher weight-based dosing guided by trough serum levels is the standard of care.

Children (2 Months to 12 Years)

Neonates (Birth to 2 Months)

Elderly

No specific dose adjustment is required in older adults with normal renal function. However, because renal function declines with age (often to a greater extent than suggested by serum creatinine alone), creatinine clearance should be estimated and maintenance doses adjusted accordingly. In elderly patients with multiple comorbidities and polypharmacy, more frequent monitoring is appropriate.

Dose Adjustment for Kidney Impairment

Patients with impaired kidney function require dose adjustments starting from the fourth day of treatment. Loading doses in the first 3 days remain the same as in patients with normal renal function. Maintenance doses are then modified as follows:

Teicoplanin is not significantly removed by conventional haemodialysis due to its high protein binding (approximately 90%), so no supplemental dose is required after dialysis. Continuous renal replacement therapy (CRRT) removes teicoplanin more effectively, and dosing should be individualised in the intensive care setting using therapeutic drug monitoring.

Peritonitis in Peritoneal Dialysis Patients

For patients undergoing continuous ambulatory peritoneal dialysis (CAPD) who develop peritonitis, a specific intraperitoneal regimen is used:

• Loading dose: 6 mg/kg as a single intravenous injection
• Week 1: 20 mg/L added to every dialysis bag
• Week 2: 20 mg/L added to every other dialysis bag
• Week 3: 20 mg/L added to the overnight dialysis bag only

Missed Dose

Because Targocid is administered by healthcare professionals in a hospital setting, it is unlikely that a dose will be missed. Your clinical team follows a strict dosing schedule recorded in the drug chart or electronic prescribing system. If you have concerns about whether you have received all your scheduled doses, speak with your nurse or doctor. For patients on outpatient parenteral antibiotic therapy (OPAT) who receive Targocid at home or in an ambulatory clinic, missed doses should be reported to the OPAT team as soon as possible so they can arrange a replacement dose.

Overdose

Overdose with teicoplanin is unlikely in a hospital setting, as doses are calculated by weight and verified by healthcare professionals. Cases of accidental overdose in neonates and young children have been reported, presenting with agitation but usually without serious sequelae. In the event of an overdose, treatment is supportive and symptomatic. There is no specific antidote. Because of its high protein binding, teicoplanin is not significantly removed by haemodialysis or peritoneal dialysis. If an overdose is suspected, contact your medical team immediately.

What Are the Side Effects of Targocid?

Like all medicines, Targocid can cause side effects, although not everybody gets them. Most side effects are mild to moderate in severity and resolve after treatment is completed. However, some side effects can be serious and require immediate medical attention. The frequency categories used below follow the standard MedDRA convention applied in the Summary of Product Characteristics (SmPC).

Serious Side Effects – Seek Immediate Medical Help

Stop treatment and tell your doctor or nurse immediately if you experience any of the following serious side effects:

Other Side Effects

The severity and frequency of kidney-related side effects tend to increase with higher doses of Targocid and with duration of therapy. Ototoxicity (hearing impairment and tinnitus) is uncommon but is more likely when Targocid is combined with aminoglycosides, loop diuretics or other ototoxic medicines. Your medical team will monitor your kidney function and, where appropriate, your hearing throughout treatment and adjust the dose if necessary.

If you notice any side effects not listed here, or if any of the listed side effects become severe, tell your doctor, pharmacist or nurse. You can also report suspected side effects directly to your national pharmacovigilance authority — for example the MHRA Yellow Card scheme in the UK, the FDA MedWatch programme in the United States, or the EMA EudraVigilance system in the EU. Patient reporting helps ensure ongoing monitoring of the benefit-risk balance of Targocid.

How Should You Store Targocid?

Keep this medicine out of the sight and reach of children at all times. Do not use Targocid after the expiry date printed on the carton and vials after “EXP”. The expiry date refers to the last day of the stated month. Medicines stored beyond their expiry date may be less effective or potentially unsafe.

The unopened powder and solvent packaged for sale do not require any special storage conditions. They can be kept at ambient room temperature (below 25°C) in their original packaging to protect from light and moisture.

Reconstituted Solution

Targocid is intended for single use only. Any unused solution in an opened vial must be discarded and never saved for later use. The chemical and physical stability of the reconstituted solution has been demonstrated as follows:

• Reconstituted solution: Stable for up to 24 hours when stored at 2–8°C (in a domestic refrigerator or controlled pharmacy refrigerator).
• Further diluted solution (4–20 mg/mL): Stable for an additional 24 hours at 2–8°C after the initial 24-hour reconstitution period.

From a microbiological standpoint, the reconstituted product should ideally be used immediately unless the reconstitution has been performed under validated aseptic conditions (for example in a hospital pharmacy's laminar flow cabinet). If not used immediately, in-use storage times and conditions prior to administration are the responsibility of the healthcare professional preparing the medicine.

Disposal

Do not dispose of medicines via wastewater or household waste. Ask your pharmacist how to dispose of medicines you no longer use. These measures help to protect the environment from contamination with active pharmaceutical ingredients. In the hospital setting, unused Targocid should be discarded through pharmaceutical waste streams in line with local biosafety and environmental protection policies.

What Does Targocid Contain?

Targocid is supplied as a sterile, white to pale yellow powder in a clear glass vial, together with a clear, colourless solvent (water for injections) in a separate ampoule or vial. The powder vial is sealed with a rubber stopper and an aluminium cap with a plastic flip-off top, and the solvent ampoule has a twist-off cap. The appearance of the reconstituted solution should be clear and pale yellow; any solution that appears cloudy or discoloured must not be used.

Composition

• Active substance: Teicoplanin – 200 mg per vial (this article's reference strength; the 400 mg vial contains 400 mg teicoplanin)
• Excipients (powder): Sodium chloride, sodium hydroxide (for pH adjustment)
• Solvent: Water for injections (typically 3 mL ampoule for the 200 mg vial)

Pack Sizes

Pack sizes vary by country but typically include:

• 1 vial × 200 mg + 1 ampoule × 3 mL solvent
• 10 vials × 200 mg + 10 ampoules × 3 mL solvent
• 1 vial × 400 mg + 1 ampoule × 3 mL solvent (where marketed)
• 10 vials × 400 mg + 10 ampoules × 3 mL solvent (where marketed)

Not all pack sizes may be marketed in your country.

Reconstitution and Dilution (Healthcare Professionals)

For healthcare professionals preparing Targocid: inject 3 mL of the supplied diluent (water for injections) slowly into the vial containing the powder, directing the stream onto the vial wall to minimise foaming. Roll the vial gently between your hands until the powder is completely dissolved; do not shake vigorously. If foam forms, allow the solution to stand for approximately 15 minutes until the foam settles. Only a clear, pale yellow solution should be used. The reconstituted solution is essentially isotonic and does not require further dilution for intramuscular or slow intravenous injection.

For intravenous infusion, the reconstituted solution may be further diluted to concentrations between 4 mg/mL and 20 mg/mL using the following compatible solutions:

• Sodium chloride 0.9%
• Glucose 5%
• Ringer-lactate solution
• Sodium chloride 0.18% / Glucose 4%
• Peritoneal dialysis solutions (glucose 1.36% or 3.86%)
• Ringer's solution
• Glucose 10%
• Sodium chloride 0.45% / Glucose 5%

The reconstituted solution has an osmolality of approximately 264–275 mOsm/kg (200 mg vial) and 285–305 mOsm/kg (400 mg vial), with a pH of 7.2–7.8, making it suitable for peripheral or central venous administration. For C. difficile colitis, the reconstituted solution is administered orally at the prescribed dose and does not require further dilution.