Aquavan
Aquavan Uses, Dosage, Side Effects, Food Interaction and all others data.
Aquavan is a water soluble prodrug and is converted to propofol in the liver. Aquavan is a short acting hypnotic/sedative/anesthetic agent. Unlike propofol, does not cause injection-site pain as it is unable to activate TRPA1. FDA approved in December 2008.Aquavan is a Schedule IV controlled substance in the United States under the Controlled Substances Act.
Aquavan is a prodrug of propofol, a sedative hypnotic drug. Unlike propofol, fospropofol is water soluble and can be administered in an aqueous solution. 1.86 mg of fospropofol is the molar equivalent for 1mg of propofol.
| Trade Name | Aquavan |
| Availability | Discontinued |
| Generic | Fospropofol |
| Fospropofol Other Names | Fospropofol |
| Related Drugs | trazodone, hydroxyzine, lorazepam, promethazine, fentanyl, Ativan, lidocaine, ketamine, hyoscyamine, propofol |
| Type | |
| Formula | C13H21O5P |
| Weight | Average: 288.2766 Monoisotopic: 288.112660294 |
| Protein binding | Both fospropofol and its active metabolite propofol are highly protein bound (approximately 98%), primarily to albumin. Fospropofol does not affect the binding of propofol to albumin. |
| Groups | Approved, Illicit, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Aquavan is a sedative-hypnotic agent indicated for monitored anesthesia care (MAC) sedation in adult patients undergoing diagnostic or therapeutic procedures.
For monitored anaesthesia care sedation in patients undergoing diagnostic procedures like bronchoscopy and colonscopy or minor surgical procedures like arthroscopy and bunionectomy.
Aquavan is also used to associated treatment for these conditions: Monitored anesthesia care sedation
How Aquavan works
After in-vivo conversion of fospropofol into propofol by endothelial alkaline phosphatase, propofol crosses the blood-brain barrier, binds to GABA-A receptors and acts as an agonist. By binding to GABA-A receptor, it will cause an increase in chloride conductance, thus inhibiting the firing of new action potentials in the post-synaptic neuron.
Toxicity
Overdosage may lead to cardiorespiratory depression, formic acid toxicity (methanol toxicity-like effects), and/or phosphate-induced hypocalemia. Most common adverse reactions (> 20%) are paresthesia and pruritus.
Aquavan Drug Interaction
Moderate: alfentanil, etomidate, methohexital, fentanyl, clonazepam, chlordiazepoxideUnknown: lubiprostone, coagulation factor Xa, insulin glulisine, darbepoetin alfa, fondaparinux, amoxicillin / clavulanate, propofol, apixaban, anti-inhibitor coagulant complex, acetaminophen / butalbital / caffeine, levofloxacin, enoxaparin, dronabinol, insulin isophane
Volume of Distribution
Aquavan = 0.33±0.069 L/kg; Propofol metabolite = 5.8 L/kg.
Elimination Route
Adequate sedation achieved after 7 minutes with a IV bolus dose of 10mg/kg. It takes 21-45 minutes for patients to recover for fospropopol-induced sedation. Following an intravenous bolus administration of 6 mg/kg in a healthy subject, the pharmacokinetic parameters of fospropofol are as follows: Cmax = 78.7 μg/mL; Tmax = 4 minutes; AUC(0-∞) = 19.0 μg ⋅ h/mL;
Half Life
When given to a patient, the half-lives are as follows: Aquavan = 0.81 hours; Propofol metabolite = 1.13 hours
Clearance
Total body clearance (CLp), Aquavan, healthy subject = 0.28 L/h/kg; CLp, fospropofol, patients = 0.31 L/h/kg; CLp/F, propofol, healthy subjects or patients = 2.74 L/h/kg.
Elimination Route
Chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney. There is negligible renal elimination of unchanged fospropofol (<0.02%).
Innovators Monograph
You find simplified version here Aquavan
