Ticoplan400 mg/vial

Ticoplan is a glycopeptide antibiotic indicated for the treatment of serious infections caused by susceptible Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), particularly when penicillins or cephalosporins are inappropriate, ineffective, or not tolerated.

Established / guideline-supported uses

• Complicated skin and soft tissue infections
• Bone and joint infections (e.g., osteomyelitis, septic arthritis)
• Hospital-acquired and community-acquired pneumonia caused by susceptible Gram-positive organisms
• Infective endocarditis caused by susceptible Gram-positive organisms (often as part of combination therapy)
• Complicated urinary tract infections
• Peritonitis associated with continuous ambulatory peritoneal dialysis (CAPD)

Adjunct / combination uses

• Empirical therapy of febrile neutropenia, used in combination with other antibacterial agents when Gram-positive infection is suspected
• Antibiotic prophylaxis during major surgery (e.g., orthopaedic surgery) in patients at high risk of Gram-positive infection, especially when beta-lactam allergy is present

Off-label use

Clostridioides difficile-associated diarrhoea/colitis (oral Ticoplan) has been used off-label as an alternative to oral vancomycin in some settings, though this is not a primary approved indication everywhere.

Ticoplan should only be used for infections confirmed or strongly suspected to be caused by susceptible Gram-positive organisms; it is not effective against Gram-negative bacteria.

Each vial of Teicoplanin for injection contains Teicoplanin (as a lyophilized powder) equivalent to 200 mg or 400 mg of Teicoplanin base, along with sodium hydroxide/hydrochloric acid for pH adjustment. The product is supplied with or without a separate solvent (water for injection) for reconstitution. Strength and exact excipients may vary by manufacturer/brand; refer to the specific product label for details.

Ticoplan is a semi-synthetic glycopeptide antibiotic derived from fermentation of Actinoplanes teichomyceticus. It is structurally and mechanistically related to vancomycin and is active against a broad range of aerobic and anaerobic Gram-positive bacteria, including staphylococci (including MRSA), streptococci, and enterococci.

A notable feature of Ticoplan is its long elimination half-life, which allows once-daily maintenance dosing after an initial loading-dose phase, and its suitability for both intravenous and intramuscular administration, unlike some other glycopeptides. It is used in hospital settings for serious, often multidrug-resistant, Gram-positive infections.

Glycopeptide antibiotic (anti-infective agent for systemic use)

Teicoplanin is a bactericidal glycopeptide antibiotic. It inhibits bacterial cell wall biosynthesis by binding with high affinity to the D-alanyl-D-alanine terminus of the pentapeptide side chains of peptidoglycan precursor units. This binding sterically blocks the transglycosylation and transpeptidation reactions required to build and cross-link the peptidoglycan layer, weakening the cell wall and leading to bacterial cell lysis and death.

Because its mechanism targets the bacterial cell wall precursor rather than a specific enzyme, cross-resistance with beta-lactam antibiotics is not expected, making Teicoplanin useful against beta-lactam-resistant organisms such as MRSA. Teicoplanin has a long plasma half-life (often 40-70 hours or longer at steady state) and high protein binding, allowing once-daily dosing after loading doses; it is primarily eliminated renally in unchanged form.

Ticoplan is given only by injection - either as a slow intravenous bolus (3-5 minutes), a short intravenous infusion (about 30 minutes, diluted in a compatible solution), or by intramuscular injection - and must be administered by a qualified healthcare professional in a hospital or clinical setting. It is not given orally for systemic infections (an oral formulation, when used, is reserved for local gut infections such as C. difficile-associated diarrhoea, where the drug acts locally in the bowel). Do not attempt to self-administer Ticoplan.

Ticoplan should be used with caution when co-administered with other drugs that share nephrotoxic and/or ototoxic potential, because the risk of kidney injury and hearing/balance disturbance may be additive. Clinically significant interactions include:

• Aminoglycosides (e.g., gentamicin, amikacin) - increased risk of nephrotoxicity and ototoxicity; renal function and, where possible, drug levels should be monitored closely if combined therapy is necessary.
• Amphotericin B - additive nephrotoxicity risk.
• Ciclosporin - additive nephrotoxicity risk; renal function monitoring advised.
• Loop diuretics (e.g., furosemide) - may increase the risk of ototoxicity, particularly with high-dose or prolonged therapy.
• Other potentially nephrotoxic or ototoxic agents (e.g., cisplatin, colistin) - increased risk of cumulative toxicity; use only if clearly necessary, with close monitoring.

There is no clinically significant evidence that Ticoplan itself induces or inhibits hepatic drug-metabolising enzymes. Always inform your physician of all medicines, including over-the-counter drugs and supplements, being taken before starting Ticoplan.

Most patients tolerate Ticoplan well, but as with any antibiotic, side effects can occur.

Common

• Injection-site reactions: pain, redness (erythema), local swelling, or abscess formation
• Rash, pruritus (itching)
• Fever
• Nausea, vomiting, diarrhoea
• Headache, dizziness

Less common / serious

• Nephrotoxicity - impaired kidney function, more likely with high doses, prolonged use, pre-existing renal impairment, or concurrent nephrotoxic drugs
• Ototoxicity - tinnitus (ringing in ears), hearing disturbance, or balance problems, particularly with prolonged high-dose therapy
• Thrombocytopenia - low platelet count, generally reversible on stopping treatment
• Transient elevation of liver enzymes
• Infusion-related reactions (flushing, itching during rapid administration) - less frequently associated with the "red man syndrome" seen with vancomycin, but still possible
• Hypersensitivity reactions, including rare anaphylaxis
• Leukopenia, eosinophilia (rare)

Seek prompt medical attention for signs of a serious allergic reaction (swelling of the face/throat, difficulty breathing, severe rash), unusual bleeding or bruising, significant reduction in urine output, or new hearing/balance problems while receiving Ticoplan.

Pregnancy: There are limited controlled data on the use of Ticoplan in pregnant women. It should be used during pregnancy only if clearly needed and if the potential benefit to the mother justifies the potential risk to the fetus. Consult a physician before use in pregnancy.

Lactation: It is not well established whether Ticoplan passes into human breast milk in clinically significant amounts. Caution is advised, and a physician should be consulted to weigh the benefits of treatment against any potential risk to the breastfeeding infant.

Nephrotoxicity and ototoxicity: As with other glycopeptide antibiotics, Ticoplan carries a risk of kidney and inner-ear (hearing/balance) toxicity, particularly with high doses, prolonged therapy, pre-existing renal impairment, or concurrent use of other nephrotoxic/ototoxic drugs (e.g., aminoglycosides - see Interactions). Renal function should be assessed before and periodically during therapy, and auditory function should be monitored during prolonged treatment, especially in patients with renal impairment or pre-existing hearing loss.

Hypersensitivity: Use with caution in patients with known vancomycin allergy due to possible cross-sensitivity (see Contraindications). Discontinue immediately if signs of a serious allergic reaction occur.

Thrombocytopenia: Blood counts, including platelets, should be monitored periodically, particularly with higher doses or prolonged courses.

Hepatic impairment: Use with caution; monitor liver function periodically, especially during prolonged therapy.

Infusion-related reactions: Administer by slow injection/infusion as directed; monitor patients during administration for flushing, itching, or other infusion-related reactions.

Superinfection: Prolonged use may result in overgrowth of non-susceptible organisms, including Clostridioides difficile; monitor for new or worsening diarrhoea.

Antibiotic stewardship: Ticoplan should be reserved for serious or resistant Gram-positive infections and used only under medical supervision. Take exactly as prescribed by your physician; do not stop, extend, skip doses, or share this medicine with others without medical advice, to reduce the risk of treatment failure and antimicrobial resistance.

There is limited clinical experience with overdose of Ticoplan. Because it is given only under medical supervision, accidental overdose is uncommon, but excessive doses may increase the risk of nephrotoxicity, ototoxicity, and other adverse effects described above.

There is no specific antidote for Ticoplan overdose. If overdose is suspected, seek immediate medical attention or contact a poison control center; management is supportive and symptomatic, with close monitoring of renal and auditory function. Ticoplan is not significantly removed by conventional haemodialysis due to its high protein binding.

Store at room temperature (below 30°C), away from light and moisture, in a dry place. Once reconstituted, use the solution immediately; if not used immediately, it may be stored under refrigeration (2-8°C) for a maximum of 24 hours. Keep out of reach of children. Do not use if the solution is discoloured or contains particulate matter.

Renal impairment: No dose adjustment is generally required in the first 3-4 days of therapy; thereafter, the maintenance dose of Ticoplan must be reduced according to creatinine clearance (see Dosage and Administration). Close monitoring of renal function is advised throughout treatment.

Hepatic impairment: Limited data are available; use with caution and monitor liver function, though formal dose adjustment guidelines are not well established.

Elderly: Dosing is generally the same as in younger adults with normal renal function, but age-related decline in renal function should be assessed and doses adjusted accordingly.

Pediatric patients: See Pediatric Uses for detailed weight-based dosing; safety and efficacy in infants under 2 months (other than defined neonatal dosing) are less well established.

Pregnancy and lactation: See Pregnancy and Lactation section for detailed guidance.

The duration of treatment with Ticoplan depends on the type and severity of infection and the patient's clinical and microbiological response, and should be determined by the treating physician. As a general guide: skin/soft tissue infections and uncomplicated urinary tract infections are typically treated for about 7-14 days; bone/joint infections, endocarditis, and other deep-seated or complicated infections often require several weeks of therapy. Surgical prophylaxis typically involves a single perioperative dose. Treatment should not be stopped early, extended, or interrupted without the prescribing physician's advice, even if symptoms improve, to ensure complete eradication of infection and reduce the risk of resistance.

Ticoplan for injection is supplied as a lyophilized (freeze-dried) powder that must be reconstituted before use, typically with the water for injection provided with the vial (or as directed by the manufacturer). To reconstitute: slowly inject the diluent down the inside wall of the vial, then gently roll the vial between the palms until the powder is fully dissolved - avoid shaking vigorously, as this can cause excessive foaming. Allow any foam to settle before withdrawing the dose. The reconstituted solution may be given directly by slow IV/IM injection or further diluted in a compatible IV fluid (e.g., 0.9% sodium chloride or 5% dextrose) for infusion. Use the reconstituted/diluted solution immediately where possible; if storage is necessary, refrigerate (2-8°C) and use within 24 hours. Discard any unused portion.

Glycopeptide antibiotics; Antibacterial agents active against Gram-positive organisms (including MRSA)

Teicoplanin exerts its bactericidal effect by binding tightly to the D-alanyl-D-alanine terminal residues of peptidoglycan precursor units in the bacterial cell wall. This binding sterically hinders the transglycosylase and transpeptidase enzymes needed for peptidoglycan chain elongation and cross-linking, preventing proper cell wall assembly. The resulting defective cell wall makes the bacterium osmotically unstable, leading to cell lysis and death. Because this mechanism does not involve penicillin-binding proteins, Teicoplanin remains active against many beta-lactam-resistant Gram-positive organisms, including MRSA.

B3

Ticoplan may be used in children from 2 months of age and in neonates for serious Gram-positive infections, using weight-based dosing regimens distinct from adult dosing (see Dosage and Administration).

• Children 2 months-12 years: 10 mg/kg every 12 hours for 3 doses (loading), then 6-10 mg/kg once daily (maintenance), depending on infection severity.
• Neonates: 16 mg/kg as a single loading dose, then 8 mg/kg once daily.

Renal function, and where relevant auditory function, should be monitored in pediatric patients, particularly neonates and those with renal impairment, given the immaturity of renal clearance mechanisms in this age group. Safety and efficacy of Ticoplan in infants younger than 2 months, other than the defined neonatal regimen, have not been well established; use in this population should be under specialist paediatric/neonatal guidance only.