Fospropofol

Fospropofol
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Chetan Lokhande, M.B.B.S [2]

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Overview

Fospropofol is a general anesthetic that is FDA approved for the {{{indicationType}}} of monitored anesthesia care sedation.. Common adverse reactions include cardiovascular: hypoxemia (1% to 27% ), dermatologic: pruritus (16% to 28% ), neurologic: paresthesia (49% to 74%).

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

• Monitored anesthesia care sedation: healthy adults or adults with mild systemic disease (American Society of Anesthesiology physical status of P1 or P2) 18 to 65 years of age, initiation, 6.5 mg/kg IV bolus followed immediately by supplemental infusion; patients weighing less than 60 kg should be dosed at 60 kg and patients weighing greater than 90 kg should be dosed at 90 kg.
• Monitored anesthesia care sedation: healthy adults or adults with mild systemic disease (American Society of Anesthesiology physical status of P1 or P2) 18 to 65 years of age, supplemental, 1.6 mg/kg IV no more frequently than every 4 min as needed to achieve the desired level of sedation; patients weighing less than 60 kg should be dosed at 60 kg and patients weighing greater than 90 kg should be dosed at 90 kg.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information about Off-Label Guideline-Supported Use of Fospropofol in adult patients.

Non–Guideline-Supported Use

There is limited information about Off-Label Non–Guideline-Supported Use of Fospropofol in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

• Safety and effectiveness of fospropofol injection has not been established in pediatric patients

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information about Off-Label Guideline-Supported Use of Fospropofol in pediatric patients.

Non–Guideline-Supported Use

There is limited information about Off-Label Non–Guideline-Supported Use of Fospropofol in pediatric patients.

Contraindications

None.

Warnings

Monitoring

LUSEDRA should be administered only by persons trained in the administration of general anesthesia and not involved in the conduct of the diagnostic or therapeutic procedure. Sedated patients should be continuously monitored, and facilities for maintenance of a patent airway, providing artificial ventilation, administering supplemental oxygen, and instituting cardiovascular resuscitation must be immediately available. Patients should be continuously monitored during sedation and through the recovery process for early signs of hypotension, apnea, airway obstruction, and/or oxygen desaturation.

5.2 Respiratory Depression

LUSEDRA may cause loss of spontaneous respiration. Apnea was reported in 1/455 (< 1%) patients treated with LUSEDRA using the standard or modified dosing regimen [see Dosage and Administration (2.2, 2.3)]. In patients treated with greater than the recommended LUSEDRA dose, apnea was reported in 14/556 (3%).

Supplemental oxygen is recommended for all patients receiving LUSEDRA. Dosages of LUSEDRA must be individualized for each patient and titrated to effect [see Dosage and Administration (2.1) and Clinical Pharmacology (12.2)]. Use lower doses of LUSEDRA in patients who are ≥65 years of age or who have severe systemic disease [see Dosage and Administration (2.3)]. The additive cardiorespiratory effects of narcotic analgesics and sedative-hypnotic agents should be considered when administered concomitantly with LUSEDRA.

Patients should be assessed for their ability to demonstrate purposeful response while sedated with LUSEDRA as patients who are unable to do so may lose protective reflexes. Airway assistance maneuvers may be required in the management of respiratory depression (see Table 4).

5.3 Hypoxemia

LUSEDRA may cause hypoxemia detectable by pulse oximetry. Hypoxemia was reported in 20/455 (4%) patients treated with LUSEDRA using the standard or modified dosing regimen [see Dosage and Administration (2.2, 2.3)]. Hypoxemia was reported among patients who retained the ability to respond purposefully to their health care provider following administration of LUSEDRA. Therefore, retention of purposeful responsiveness did not prevent patients from becoming hypoxemic following administration of LUSEDRA. In patients treated with greater than the recommended LUSEDRA dose, hypoxemia was reported in 151/556 (27%).

The risk of hypoxemia is reduced by appropriate positioning of the patient and the use of supplemental oxygen in all patients receiving LUSEDRA. Airway assistance maneuvers may be required in the management of hypoxemia (see Table 4). The additive cardiorespiratory effects of narcotic analgesics and other sedative-hypnotic agents should be considered when administered concomitantly with LUSEDRA.

5.4 Patient Unresponsiveness to Vigorous Tactile or Painful Stimulation

LUSEDRA has not been studied for use in general anesthesia. However, administration of LUSEDRA may inadvertently cause patients to become unresponsive or minimally responsive to vigorous tactile or painful stimulation. The incidence of patients sedated for colonoscopy who became minimally responsive or unresponsive to vigorous tactile or painful stimulation was 7/183 (4%). The duration of minimal or complete unresponsiveness in colonoscopy patients ranged from 2 to 16 minutes. Among patients sedated for bronchoscopy, the incidence of patients who became minimally or completely unresponsive to vigorous tactile or painful stimulation was 24/149 (16%). The duration of minimal to complete unresponsiveness in bronchoscopy patients ranged from 2 to 20 minutes.

5.5 Hypotension

Hypotension following the use of LUSEDRA may occur. Hypotension was reported in 18/455 (4%) patients treated with LUSEDRA using the standard or modified dosing regimen [see Dosage and Administration (2.2, 2.3)]. In patients treated with greater than the recommended LUSEDRA dose, hypotension was reported in 31/556 (6%).

Patients with compromised myocardial function, reduced vascular tone, or who have reduced intravascular volume may be at an increased risk for hypotension. A secure intravenous access catheter and supplemental volume replacement fluids should be readily available during the procedure. Additional pharmacological management may be necessary.

Adverse Reactions

Clinical Trials Experience

The following serious adverse reactions are discussed elsewhere in the labeling:

   Respiratory depression [see Warnings and Precautions (5.2)]
   Hypoxemia [see Warnings and Precautions (5.3)]
   Loss of purposeful responsiveness [see Warnings and Precautions (5.4)]
   Hypotension [see Warnings and Precautions (5.5)]

The most common adverse reactions (reported in greater than 20%) are paresthesia and pruritus.

The most commonly reported reasons for discontinuation are paresthesia and cough.

6.1 Clinical Trials Experience

Adverse reactions presented in this section are derived from 332 patients in 3 controlled clinical trials in patients undergoing colonoscopy or flexible bronchoscopy and 123 patients in one open-label study in patients undergoing minor procedures. Patients enrolled in the studies who received the standard or modified dosing regimen included males and females, ≥18 years of age and ranging from healthy (359/455 [79%] ASA P1 or P2) to those with severe systemic disease (96/455 [21%] ASA P3 or P4). Of the 455 patients enrolled, 345 (76%) were ≥18 to <65 years of age and 110 (24%) were ≥65 years of age. Adverse reactions are reported for patients who received the standard or the modified dosing regimen [see Dosage and Administration (2)]. The majority of procedures were less than thirty minutes in duration. All patients in these studies received 50 mcg fentanyl citrate intravenously as premedication, and some of the patients received additional 25 mcg fentanyl citrate supplemental doses. Adverse reactions occurring in ≥2% of patients in these studies are presented in Table 3.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not accurately reflect the rates observed in practice.

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Paresthesias (including burning, tingling, stinging) and/or pruritus, usually manifested in the perineal region, were the most frequently recorded adverse reactions in clinical trials. Paresthesias and pruritus generally occurred within 5 minutes after administration of the initial dose of LUSEDRA and were generally transient and mild to moderate in intensity. The pharmacologic basis of these sensory phenomena is unknown. No pretreatments, including the use of nonsteroidal anti-inflammatory drugs, opioids, or lidocaine, are known to have an effect on or to reduce the incidence of these sensations.

Sedation-related adverse reactions were experienced at the following rates for subjects receiving the standard or modified LUSEDRA dosing regimen: 20/455 (4%) hypoxemia, 18/455 (4%) hypotension, 1/455 (< 1%) apnea. A greater rate of sedation-related adverse reactions necessitating intervention was observed in patients undergoing bronchoscopy compared with colonoscopy and minor surgical procedures. In the colonoscopy studies, 5/183 (3%) patients were ASA P3. In the minor surgical procedures study, 23/123 (19%) patients were ASA P3 or P4. In the flexible bronchoscopy study, 68/150 (46%) patients were ASA P3 or P4. The type and incidence of airway assistance interventions required for patients who experienced sedation-related adverse reactions are presented in Table 4.

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Adverse Reactions in Prolonged Exposure in Adults

The safety of LUSEDRA for continuous sedation has not been established and therefore its use is not recommended. LUSEDRA was administered to 38 intubated and mechanically ventilated patients in postoperative and intensive care settings. An occurrence of nonsustained ventricular tachycardia was observed as a serious adverse reaction in one patient in the study. Another patient with acute myeloid leukemia with renal and hepatic insufficiency experienced a further increase in plasma formate concentration from a baseline of 66 mcg/mL to a post-dose level of 212 mcg/mL after a 12-hour infusion. The clinical significance of these findings is unknown.

Postmarketing Experience

There is limited information regarding Fospropofol Postmarketing Experience in the drug label.

Drug Interactions

LUSEDRA may produce additive cardiorespiratory effects when administered with other cardiorespiratory depressants such as sedative-hypnotics and narcotic analgesics.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): B Teratogenic Effects:

Pregnancy Category B.

There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Reproduction studies have been performed in rats and rabbits at doses up to 0.6 and 1.7 times the anticipated human dose for a procedure of 16 minutes based on a comparison of doses expressed as mg/m2 and have revealed no evidence of impaired fertility or harm to the fetus due to LUSEDRA.

Pregnant rats were treated with fospropofol disodium (5, 20, or 45 mg/kg/day, IV) from gestation day 7 through 17 (the highest dose is 0.6 times the anticipated human dose for a procedure of 16 minutes based on a comparison of doses expressed as mg/m2). Doses of 20 and 45 mg/kg/day produced significant maternal toxicity. No drug-related adverse effects on embryo-fetal development were noted.

Pregnant rabbits were treated with fospropofol disodium (14, 28, 56 or 70 mg/kg/day, IV) from gestation day 6 through 18 (the highest dose is 1.7 times the anticipated human dose for a procedure of 16 minutes based on a comparison of doses expressed as mg/m2). Significant maternal toxicity was noted at all doses. No drug-related adverse effects on embryo-fetal development were noted.

Nonteratogenic Effects.

Pregnant rats were administered 0, 5, 10, or 20 mg/kg/day fospropofol disodium from gestation day 7 through lactation day 20 to evaluate perinatal and postnatal development (the highest dose is 0.2 times the anticipated human dose for a procedure of 16 minutes based on a comparison of doses expressed as mg/m2). There were no clear treatment-related effects on growth, development, behavior (passive avoidance and water maze) or fertility and mating capacity of the offspring.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Fospropofol in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Fospropofol during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Fospropofol in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Fospropofol in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Fospropofol in geriatric settings.

Gender

There is no FDA guidance on the use of Fospropofol with respect to specific gender populations.

Race

There is no FDA guidance on the use of Fospropofol with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Fospropofol in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Fospropofol in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Fospropofol in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Fospropofol in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Fospropofol Administration in the drug label.

Monitoring

There is limited information regarding Fospropofol Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Fospropofol and IV administrations.

Overdosage

There is limited information regarding Fospropofol overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

There is limited information regarding Fospropofol Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Fospropofol Mechanism of Action in the drug label.

Structure

There is limited information regarding Fospropofol Structure in the drug label.

Pharmacodynamics

There is limited information regarding Fospropofol Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Fospropofol Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Fospropofol Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Fospropofol Clinical Studies in the drug label.

How Supplied

There is limited information regarding Fospropofol How Supplied in the drug label.

Storage

There is limited information regarding Fospropofol Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Fospropofol Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Fospropofol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Fospropofol Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Fospropofol Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.