ATRACURIUM BESYLATE PRESERVATIVE FREE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ATRACURIUM BESYLATE PRESERVATIVE FREE (ATRACURIUM BESYLATE PRESERVATIVE FREE).
Nondepolarizing neuromuscular blocking agent that competitively antagonizes acetylcholine at nicotinic cholinergic receptors at the neuromuscular junction, preventing depolarization and muscle contraction. Degraded via Hofmann elimination (non-enzymatic) and ester hydrolysis.
| Metabolism | Hofmann elimination (non-enzymatic, pH- and temperature-dependent) and ester hydrolysis (by nonspecific plasma esterases); major metabolite: laudanosine. |
| Excretion | Primarily via Hofmann elimination (non-enzymatic degradation) and ester hydrolysis; renal excretion accounts for less than 10% unchanged, with biliary/fecal elimination minimal. Approximately 40% as laudanosine and other metabolites via urine, with laudanosine further metabolized and renally excreted. |
| Half-life | Terminal elimination half-life of atracurium is approximately 20 minutes (range 15-35 min) in healthy adults; clinically, this short half-life correlates with rapid spontaneous recovery without the need for reversal agents, though prolonged in hypothermia or acidosis. |
| Protein binding | Approximately 82% bound to plasma proteins (mainly albumin). |
| Volume of Distribution | Vd: 0.16-0.2 L/kg, approximating extracellular fluid volume; reflects limited tissue distribution due to polarity. |
| Bioavailability | IV: 100%; not administered orally due to negligible oral bioavailability (first-pass metabolism and degradation). |
| Onset of Action | IV: 2-3 minutes for intubating dose (0.4-0.5 mg/kg); maximal effect within 3-5 minutes. |
| Duration of Action | Clinical duration (time to 25% recovery of twitch) is 25-40 minutes after intubating dose; recovery is predictable due to organ-independent elimination, with full recovery in 60-90 minutes. Prolonged with hypothermia or acidosis. |
0.4-0.5 mg/kg IV bolus for intubation; maintenance: 0.08-0.1 mg/kg IV every 15-25 min or continuous infusion 5-10 mcg/kg/min
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR ≥5 mL/min; patients with renal failure may have prolonged duration but no specific dose reduction recommended |
| Liver impairment | Child-Pugh A/B: no adjustment; Child-Pugh C: consider reduced dose (e.g., 0.3 mg/kg) due to prolonged elimination half-life and increased volume of distribution |
| Pediatric use | 1 month-2 years: 0.3-0.5 mg/kg IV bolus; 2-12 years: 0.5-0.6 mg/kg IV bolus; maintenance infusion: 5-10 mcg/kg/min for all ages |
| Geriatric use | Start at lower end of dosing range (0.3-0.4 mg/kg bolus); infusion rate may need reduction due to decreased clearance and prolonged duration of action |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ATRACURIUM BESYLATE PRESERVATIVE FREE (ATRACURIUM BESYLATE PRESERVATIVE FREE).
| Breastfeeding | It is not known whether atracurium is excreted in human milk. However, due to its quaternary ammonium structure and high molecular weight, minimal excretion into breast milk is expected. The M/P ratio is unknown. Caution should be exercised when administered to a nursing woman. |
| Teratogenic Risk | Atracurium is a nondepolarizing neuromuscular blocker. Animal studies have not revealed evidence of teratogenicity. There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, atracurium should be used during pregnancy only if clearly needed. However, it is used in cesarean section and has not been associated with fetal harm when used as part of general anesthesia. |
■ FDA Black Box Warning
Should be administered only by experienced clinicians familiar with neuromuscular blocking agents. Resuscitative equipment and drugs (e.g., atropine, neostigmine) must be immediately available.
| Serious Effects |
Hypersensitivity to atracurium or cisatracurium; history of severe anaphylactic reaction to neuromuscular blocking agents.
| Precautions | Risk of histamine release causing hypotension, flushing, and bronchospasm; prolonged neuromuscular blockade in patients with electrolyte disturbances, acidosis, or neuromuscular diseases; higher dose requirements in burn patients; caution in renal or hepatic impairment as metabolite laudanosine may accumulate (potential CNS excitatory effects); anaphylaxis risk. |
| Food/Dietary | No known food interactions. Avoid grapefruit juice due to potential interference with clearance, though not well-studied. |
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| Fetal Monitoring | Monitor maternal vital signs, oxygen saturation, and neuromuscular function (e.g., train-of-four monitoring). Fetal heart rate should be monitored if used during cesarean section. Be prepared for possible neonatal respiratory depression, although this is rare due to minimal placental transfer. |
| Fertility Effects | No studies have been conducted on the effect of atracurium on fertility. It is unlikely to have a significant impact on male or female fertility due to its short-term use as an anesthetic adjunct. |
| Clinical Pearls | Atracurium undergoes Hofmann elimination, making it safe in renal and hepatic impairment. Avoid mixing with alkaline solutions (e.g., thiopental) in same IV line. Reversal with neostigmine requires glycopyrrolate to avoid bradycardia. Use with caution in burns, hypermagnesemia, and neuromuscular diseases. |
| Patient Advice | You will receive this medication only by a healthcare professional to relax muscles during surgery or mechanical ventilation. · You will be monitored closely for breathing and heart rate throughout treatment. · Tell your doctor if you have kidney or liver problems, heart disease, or electrolyte imbalances. · Report any history of allergic reactions to this drug or similar medications. |