TIGLUTIK KIT
Clinical safety rating
cautionComprehensive clinical and safety monograph for TIGLUTIK KIT (TIGLUTIK KIT).
Glutamate antagonist that inhibits presynaptic glutamate release via sodium channel blockade and modulation of excitatory amino acid transport.
| Metabolism | Hepatic metabolism primarily via CYP1A2, with minor contributions from CYP3A4 and glucuronidation. |
| Excretion | Riluzole is primarily eliminated via hepatic metabolism, with <10% excreted unchanged in urine. Metabolites are eliminated renally (~85%) and fecally (~5%). |
| Half-life | Terminal elimination half-life is approximately 9-15 hours, with a mean of 12 hours. Steady-state is reached within 5-7 days. Clinically, this supports twice-daily dosing. |
| Protein binding | 97% bound primarily to plasma proteins, including albumin and lipoproteins. |
| Volume of Distribution | Approximately 3.4 L/kg, indicating extensive tissue distribution, particularly into the CNS. |
| Bioavailability | Oral bioavailability is approximately 60% (range 36-76%) due to extensive first-pass metabolism. High-fat meals reduce AUC by 20% and Cmax by 45%. |
| Onset of Action | The onset of clinical effect (neuroprotective) is not immediate; therapeutic benefit is observed after weeks to months of continuous dosing. No acute effect. |
| Duration of Action | Duration of action is approximately 12 hours due to twice-daily dosing. Consistent plasma levels are required for sustained neuroprotection. |
| Molecular Weight | 178.16 |
50 mg orally every 12 hours, administered via enteral tube (e.g., nasogastric tube) as a suspension after mixing contents of the 5 mg/mL oral suspension packet with 10 mL of water.
| Dosage form | SUSPENSION |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl 30-89 mL/min). Not recommended in severe renal impairment (CrCl <30 mL/min) due to lack of data. |
| Liver impairment | Contraindicated in patients with severe hepatic impairment (Child-Pugh Class C). No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh Class A or B), but use with caution. |
| Pediatric use | Not approved for pediatric patients under 18 years of age. Safety and efficacy have not been established. |
| Geriatric use | No specific dose adjustment recommended based on age alone; consider renal function and overall frailty. Monitor for adverse effects, particularly falls and dysphagia. |
| 1st trimester | Use only if benefit outweighs risk; no adequate studies in pregnant women. Animal studies suggest potential risk. |
| 2nd trimester | Use only if benefit outweighs risk; limited human data. Monitor for maternal adverse effects. |
| 3rd trimester | Use only if benefit outweighs risk; potential for neonatal adverse effects (e.g., respiratory depression). |
Clinical note
Comprehensive clinical and safety monograph for TIGLUTIK KIT (TIGLUTIK KIT).
| Placental transfer | Likely crosses placenta based on molecular weight (178.16 Da) and lipophilicity; no specific human data. |
| Breastfeeding | Excretion into human milk unknown; due to potential for serious adverse reactions in nursing infants, consider discontinuing breastfeeding or drug, weighing importance of drug to mother. |
| Lactation Rating | L3 (Moderately Safe) - No controlled studies in breastfeeding women, but potential benefits may outweigh risks. |
| Teratogenic Risk | FDA Pregnancy Category C. Animal studies show fetal harm at 0.6 times human dose; no adequate human studies. First trimester: potential organogenesis disruption; use only if benefit justifies risk. Second/third trimesters: possible fetal growth restriction; avoid if possible. |
| Fetal Monitoring | Monitor maternal liver function (ALT, AST) monthly; fetal ultrasound for growth restriction and anomalies; respiratory status for aspiration risk. |
| Fertility Effects | In animal studies, no adverse effects on fertility at therapeutic doses; human data lacking. |
■ FDA Black Box Warning
None
| Serious Effects |
Severe hypersensitivity to riluzole or any componentSevere hepatic impairment (Child-Pugh class C)Concurrent use of strong CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin)
| Precautions | Hepatic injury (elevated transaminases, bilirubin), Neutropenia, Interstitial lung disease, Dizziness and somnolence |
| Food/Dietary | Avoid high-fat meals (e.g., fried foods, cheese, creamy sauces) within 1 hour before or 2 hours after dosing, as they increase absorption and may increase risk of side effects. Grapefruit juice may increase riluzole levels; avoid concurrent consumption. |
| Clinical Pearls | Tiglutik (riluzole) is the first liquid formulation of riluzole, approved for ALS. It can be administered via feeding tube. Monitor liver function tests (ALT, AST) monthly for 3 months, then quarterly. Avoid use in patients with baseline transaminase elevations >3x ULN. Concomitant use with hepatotoxic drugs (e.g., NSAIDs, acetaminophen >3 g/day) requires caution. Has a high fat emulsion suspension; do not dilute. |
| Patient Advice | Take each dose at least 1 hour before or 2 hours after a meal to avoid food interactions. · Shake the bottle well for at least 30 seconds before each use. · Use the provided dosing syringe to measure the correct dose; do not use household spoons. · If you miss a dose, take it as soon as you remember unless it is close to the next dose; do not double-dose. · Report any yellowing of skin or eyes, dark urine, or abdominal pain immediately as signs of liver toxicity. · You may feel dizzy or lightheaded; avoid driving until you know how the drug affects you. |
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