Drug reference

Tigecycline

Glycylcycline antibacterial (tetracycline derivative) · Antibiotic

Also known as Tygacil

START

Reserve for MDR organisms or when other options unsuitable (FDA mortality warning). Check baseline LFTs, amylase/lipase. Anti-emetic prophylaxis often needed.

TYPICAL MAX

100mg load, 50mg q12h. Do NOT increase dose for severe infections—no additional efficacy and more toxicity.

STOP IF

Severe vomiting, pancreatitis (rising amylase/lipase with abdominal pain), severe hepatic dysfunction, anaphylaxis, C. difficile colitis.

WATCH

FDA BLACK BOX WARNING: increased all-cause mortality in pooled clinical trials compared to other antibiotics. Reserve for situations where alternatives are not suitable. Nausea/vomiting is very common (~30%)—pre-treat with anti-emetics. NOT for pneumonia with bacteremia (poor lung penetration in some studies). NOT for uncomplicated infections.

CDSCO approvedHATC J01AA12

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 30min · Onset ~30 min
PEAK: 1h · Cmax at end of infusion
t½: 1.8d · t½ ~42 hours (long terminal)
DURATION: 12h · 12 hours (q12h)

EXCRETION

Fecal unchanged and metabolites (~59%)

route + CYP

INTERACTIONS

2 major

SEVERE in our sources

PREGNANCY

Avoid in pregnancy—crosses placenta; risk of fetal bone growth inhibition and tooth discoloration (tetracycline class effect).

FDA category + note

Top interactionssee all 6 →

Aminolevulinic AcidSevereDatabaseDDInter
BexaroteneSevereDatabaseDDInter

Available in India

79 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Binds to 30S ribosomal subunit, blocking aminoacyl-tRNA entry into the A site of the ribosome, inhibiting protein synthesis. Structural modifications (glycylcycline side chain) overcome tetracycline resistance mechanisms (efflux pumps and ribosomal protection proteins). Bacteriostatic.

Indications

Complicated intra-abdominal infectionsComplicated skin and skin structure infections (including diabetic foot, MRSA)Community-acquired bacterial pneumoniaMDR Acinetobacter baumannii infections (off-label but widely used)Carbapenem-resistant Enterobacteriaceae (CRE) infections (off-label, salvage therapy)

Dosing

Adult: 100mg IV loading dose, then 50mg IV q12h over 30-60 minutes. Treat 5-14 days depending on indication and response.
Pediatric: ≥8 years: 1.2mg/kg IV (max 50mg) q12h after 2.4mg/kg (max 100mg) loading.
Renal adjustment: No adjustment needed (not renally excreted).
Hepatic adjustment: Mild-moderate (Child-Pugh A/B): no adjustment. Severe (Child-Pugh C): 100mg load, then 25mg q12h.
Geriatric: No specific adjustment; increased mortality signal in some analyses—use only when alternatives are unsuitable.
Max dose: 100mg loading; 50mg q12h maintenance

Pharmacokinetics

Onset

Bacteriostatic effect; clinical improvement 48-72 hours

Peak effect

Cmax at end of infusion; Tmax ~1 hour

Duration

12 hours (q12h dosing)

Half-life

~42 hours (long terminal half-life; tissue redistribution)

Bioavailability

N/A (IV only)

Protein binding

~71-89%

Metabolism

Not extensively metabolized; minor glucuronidation and epimerization

Excretion

~59% fecal (unchanged + metabolites); ~33% renal (mostly unchanged); biliary excretion significant

Contraindications

Hypersensitivity to tigecycline or tetracyclines
Pregnancy (fetal bone and tooth effects)
Children <8 years (tooth discoloration)
Severe hepatic impairment (Child-Pugh C) without dose adjustment

Side effects

Common

Nausea and vomiting (~30%—most common)DiarrheaHeadacheElevated transaminasesPhlebitis at infusion siteHypoproteinemia

Serious

Severe nausea/vomiting (dose-limiting)
Clostridioides difficile colitis
Hepatotoxicity
Pancreatitis
Increased all-cause mortality (FDA black box warning—higher mortality vs comparators in pooled analysis)
Anaphylaxis
Photosensitivity

Pregnancy & lactation

Pregnancy

Avoid in pregnancy—crosses placenta; risk of fetal bone growth inhibition and tooth discoloration (tetracycline class effect).

Lactation

Excreted in breast milk; avoid during breastfeeding (tetracycline class effect on infant bone and teeth).

Drug interactions

Aminolevulinic Acid

Severe

Database

Clinical effect not specified

Source: DDInter

Bexarotene

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Cyclosporine

Moderate

Database

Potentially increased cyclosporine levels, leading to increased risk of cyclosporine-related toxicities (e.g., nephrotoxicity, neurotoxicity).

Monitor cyclosporine levels if co-administered with tigecycline, especially in patients with pre-existing renal impairment. Adjust cyclosporine dose as necessary.

Source: DDInter

Methotrexate

Moderate

Database

Tetracyclines may displace methotrexate from protein binding or reduce renal clearance.

Monitor methotrexate levels and for toxicity.

Source: Kimi deep-research + Cla

Live Vaccines

Moderate

Database

Bacteriostatic antibiotics may reduce efficacy of live bacterial vaccines.

Defer live bacterial vaccines until 24-48 hours after completing tigecycline.