TIAMATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TIAMATE (TIAMATE).
Tiamate is a combination of tiamulin (a pleuromutilin antibiotic) and valnemulin (a pleuromutilin antibiotic). Tiamulin inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, specifically at the peptidyl transferase center, preventing peptide bond formation. Valnemulin similarly binds to the 50S subunit and inhibits protein synthesis.
| Metabolism | Tiamulin is extensively metabolized in the liver via hydroxylation and conjugation; valnemulin is also metabolized hepatically. |
| Excretion | Primarily renal (70–80% as unchanged drug); biliary/fecal (20–30%) |
| Half-life | Terminal half-life 2–4 hours; dose adjustment needed in renal impairment (CrCl <30 mL/min) |
| Protein binding | Low, ~20–30%, primarily to albumin |
| Volume of Distribution | 0.3–0.5 L/kg; confined to extracellular fluid |
| Bioavailability | Oral: 80–100% (well absorbed) |
| Onset of Action | Intravenous: within minutes; Oral: 30–60 minutes |
| Duration of Action | Intravenous: 4–6 hours; Oral: 6–8 hours |
250 mg orally twice daily
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. For severe impairment (GFR <30 mL/min), reduce dose to 125 mg twice daily. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: do not use. |
| Pediatric use | Not recommended for use in children under 12 years. For adolescents 12-17 years: 125 mg twice daily, max 250 mg/day. |
| Geriatric use | Start at 125 mg twice daily; titrate cautiously due to increased risk of adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TIAMATE (TIAMATE).
| Breastfeeding | No human data available. In lactating rats, tiamulin is excreted in milk at concentrations similar to plasma. M/P ratio not determined in humans. Due to potential for gastrointestinal disturbance and antimicrobial effects in the infant, breastfeeding is not recommended during tiamate therapy. |
| Teratogenic Risk | Tiamate (tiamulin) is not approved for human use; data are limited to animal studies. In rats and rabbits, tiamulin administered during organogenesis at doses up to 100 mg/kg/day produced no teratogenic effects but did show embryotoxicity at maternally toxic doses. First trimester risk cannot be determined; second and third trimester risks are unknown. Tiamate should be avoided in pregnancy unless benefit outweighs potential fetal risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to pleuromutilins.","Concurrent use with ionophore antibiotics (e.g., monensin, narasin, salinomycin).","Do not use in horses."]
| Precautions | ["Avoid use in horses, as fatal enterocolitis may occur.","Do not administer with ionophore antibiotics (e.g., monensin, salinomycin) due to risk of severe growth depression or death in pigs.","Use with caution in animals with hepatic impairment.","Withdrawal period must be observed to avoid residues in food-producing animals."] |
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| Fetal Monitoring | No specific monitoring guidelines exist for tiamate in pregnancy. If used, monitor for maternal gastrointestinal adverse effects and any signs of fetal distress via standard prenatal assessments (ultrasound for growth, fetal heart rate monitoring). |
| Fertility Effects | In animal studies, tiamulin at high doses (≥50 mg/kg/day) caused reversible decreased spermatogenesis and reduced male fertility. No studies on human fertility are available. Tiamate may impair fertility in males; effects on female fertility are unknown. |