Propofol

Propofol can cause severe drowsiness or dizziness, which may last for several hours. You will need someone to drive you home after your surgery or procedure. Do not drive yourself or do anything that requires you to be awake and alert for at least 24 hours after you have been treated with propofol.

Propofol may be found in some form under the following brand names:

• Diprivan

• Propoflo

• Propoven

Serious side effects have been reported with propofol. See the "Drug Precautions" section.

Common side effects of propofol include the following:

• low blood pressure
• low heart rate
• difficulty breathing
• local irritation at the injection site
• rash

This is not a complete list of propofol side effects. Ask your doctor or pharmacist for more information. 

Tell your doctor if you have any side effect that bothers you or that does not go away. Call your doctor for medical advice about side effects. 

You may report side effects to the FDA at 1-800-FDA-1088.

Propofol is injected into a vein through an IV. A healthcare provider will give you this injection.

You will relax and fall asleep very quickly after propofol is injected.

Your breathing, blood pressure, oxygen levels, kidney function, and other vital signs will be watched closely while you are under the effects of propofol.

Propofol can cause severe drowsiness or dizziness, which may last for several hours. You will need someone to drive you home after your surgery or procedure. Do not drive yourself or do anything that requires you to be awake and alert for at least 24 hours after you have been treated with propofol.

• Effects appear to be related, at least partially, to propofol’s ability to enhance the activity of GABA6 116 145 by interacting with the GABAA receptor complex at spinal and supraspinal synapses.6 17 116 145 181 192 Also may interact with other neurotransmitter sites (e.g., glycine, nicotinic, glutamate, G-protein coupled receptors) and inhibit sodium channels.6 145

• Capable of producing all levels of CNS depressionfrom light sleep to deep comadepending on the dosage.5 117

• Associated with both anticonvulsant activity and excitatory effects on the nervous system.5 6 17 117 118 210

• Anesthetic doses may increase cerebral vascular resistance and decrease cerebral blood flow and cerebral metabolic rate for oxygen and glucose.1 2 5 6 7 8 10 117 118 May slightly decrease intracranial pressure in patients undergoing intracranial surgery6 8 10 or in those undergoing sedation in a critical care setting.5

• Hypnotic doses may be associated with analgesic effects; responses to subhypnotic doses vary from analgesia to hyperalgesia.5 6 10 18 Subhypnotic doses may have anxiolytic effects comparable to those of midazolam or methohexital.17 192 Amnesic effects are less than those of the benzodiazepines.5 6 7 9 36 43 136

• Propofol anesthesia associated with substantial (30–60%) reductions in intraocular pressure in patients undergoing ophthalmic surgery.1 2 6 9 10 118

• May have direct antiemetic properties; however, mechanism not established.17

Use propofol as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• It is given as a shot into a vein.
• It is given as an infusion into a vein over a period of time.

What do I do if I miss a dose?

• This medicine is given on an as needed basis.

Strict aseptic technique must always be maintained during handling. Propofol injectable emulsion is a single-use parenteral product which contains benzyl alcohol 1.5 mg/mL and sodium benzoate 0.7 mg/mL to inhibit the rate of growth of microorganisms, for up to 12 hours, in the event of accidental extrinsic contamination. However, Propofol injectable emulsion can still support the growth of microorganisms as it is not an antimicrobially preserved product under USP standards. Accordingly, strict aseptic technique must still be adhered to. Do not use if contamination is suspected. Discard unused portions as directed within the required time limits (see DOSAGE AND ADMINISTRATION - Handling Procedures). There have been reports in which failure to use aseptic technique when handling Propofol injectable emulsion was associated with microbial contamination of the product and with fever, infection/sepsis, other life-threatening illness, and/or death.

Propofol injectable emulsion is a sterile, nonpyrogenic emulsion containing 10 mg/mLof Propofol suitable for intravenous administration. Propofol is chemicallly described as 2,6-diisopropylphenol and has a molecular weight of 178.27. The structural and molecular formulas are:

Propofol is slightly soluble in water and, thus, is formulated in a white, oil-in-water emulsion. The pKa is 11. The octanol/water partition coefficient for Propofol is 6761:1 at a pH of 6 to 8.5. In addition to the active component, Propofol, the formulation also contains soybean oil (100 mg/mL), glycerol (22.5 mg/mL), egg lecithin (12 mg/mL), benzyl alcohol (1.5 mg/mL) and sodium benzoate (0.7 mg/mL) added. The pH is adjusted with sodium hydroxide. The Propofol injectable emulsion is isotonic and has a pH of 7 to 8.5.

Propofol injectable emulsion is an I.V. sedative-hypnotic agent that can be used as described in the table below.

Safety, effectivness and dosing guidelines for Propofol injectable emulsion have not been established for MAC Sedation in the pediatric population; therefore, it is not recommended for this use. (See PRECAUTIONS - Pediatric Use.)

Propofol injectable emulsion is not recommended for induction of anesthesia below the age of 3 years or for maintenance of anesthesia below the age of 2 months because its safety and effectiveness have not been established in those populations.

In the Intensive Care Unit (ICU), Propofol injectable emulsion can be administered to intubated, mechanically ventilated adult patients to provide continuous sedation and control of stress responses only by persons skilled in the medical management of critically ill patients and trained in cardiovascular resuscitation and airway management.

Propofol injectable emulsion is not indicated for use in Pediatric ICU sedation since the safety of this regimen has not been estabished. (See PRECAUTIONS - Pediatric Use.)

Propofol injectable emulsion is not recommended for obstetrics, including Cesarean section deliveries. Propofol injectable emulsion crosses the placenta, and as with other general anesthetic agents, the administration of Propofol injectable emulsion may be associated with neonatal depression. (See PRECAUTIONS).

Use of Propofol injectable emulsion has been associated with both fatal and life-threatening anaphylactic and anaphylactoid reactions.

For general anesthesia or monitored anesthesia care (MAC) sedation, Propofol injectable emulsion should be administered only by persons trained in the administration of general anesthesia and not involved in the conduct of the surgical/diagnostic procedure. Sedated patients should be continuously monitored, and facilities for amintenance of a patent airway, providing artificial ventilation, administering supplemental oxygen, and instituting cardiovascular resuscitation must be immediately available. Patients should be continuously monitored for early signs of hypotension, apnea, airway, obstruction, and/or oxygen desaturation. These cardiorespiratory effects are more likely to occur following rapid bolus administration, especially in the elderly, debilitated, or ASA-PS III or IV patients.

For sedation of intubated, mechanically ventilated patients in the Intensive Care Unit (ICU), Propofol injectable emulsion should be administered only by persons skilled in the management of critically ill patients and trained in cardiovascular resuscitation and airway management.

Use of Propofol injectable emulsion for both adult and pediatric ICU sedation has been associated with a constellation of metabolic derangements and organ system failures, referred to as Propofol Infusion Syndrome, that have resulted in death. The syndrome in characterized by severe metabolic acidosis, hyperkalemia, lipemia, rhabdomyolysis, hepatomegaly, cardiac and renal failure. The syndrome is most often associated with prolonged, high-dose infusions (>5 mg/kg/h for > 48h) but has also been reported following large-dose, short-term infusions during surgical anesthesia. In the setting of prolonged need for sedation, increasing Propofol dose requirements to maintain a constant level of sedation, or onset of metabolic acidosis during administration of a Propofol infusion, consideration should be given to using alternative means of sedation.

Abrupt discontinuation of Propofol injectable emulsion prior to weaning or for daily evaluation of sedation levels should be avoided. This may result in rapid awakening with associated anxiety, agitation, and resistance to mechanical ventilation. Infusions of Propofol injectable emulsion should be adjusted to maintain a light level of sedation through the weaning process or evaluation of sedation level. (See PRECAUTIONS.)

Propofol injectable emulsion should not be coadministered through the same I.V. catheter with blood or plasma because compatibility has not been established. In vitro tests have shown that aggregates of the globular component of the emulsion vehicle have occurred with blood/plasma/serum from humans and animals. The clincal significance of these findings is not known.

There have been reports in which failure to use aseptic technique when handling Propofol injectable emulsion was associated with microbial contamination of the product and with fever, infection, sepsis, other life-threatening illness, and death. Do not u se if contamination is suspected. Discard unused portions as directed within the required time limits (see DOSAGE AND ADMINISTRATION - Handling Procedures).

Propofol injectable emulsion is supplied in ready-to-use vials containing 10 mg/mL of Propofol as follows:

Propofol undergoes oxidative degradation in the presence of oxygen and is therefore packaged under nitrogen to eliminate this degradation path. Store at 20 to 25C (68 to 77F). [See USP Controlled Room Temperature.] Do not freeze. Shake well before use. Do not use if there is evidence of excessive creaming or aggregation, if large droplets are visible, or if there are other forms of phase separation indicating that the stability of the product has been compromised. Slight creaming, which should disappear after shaking, may be visible upon prolonged standing.

Revised 3/2016

Made in India

Mfd. for: Hospira, Inc., Lake Forest, IL 60045 USA

Consult local regulations and individual institutional policies and procedures. Dosage must be individualized based on total body weight and titrated to the desired clinical effect. Wait at least 3 to 5 minutes between dosage adjustments to clinically assess drug effects. Smaller doses are required when used with opioids; the following are general dosing guidelines (see “Abbreviations, Acronyms, and Symbols” for explanation of ASA-PS classes):

General anesthesia:

Induction of general anesthesia: IV: Healthy children 3 to 16 years, ASA-PS 1 or 2: 2.5 to 3.5 mg/kg over 20 to 30 seconds; use a lower dose for children ASA-PS 3 or 4

Maintenance of general anesthesia: IV infusion: Healthy children 2 months to 16 years, ASA-PS 1 or 2: 125 to 300 mcg/kg/minute (or 7.5 to 18 mg/kg/hour); after 30 minutes, if clinical signs of light anesthesia are absent, decrease the infusion rate. Children ≤5 years may require larger infusion rates compared to older children.

Status epilepticus, refractory (off-label use): IV: Note: Mechanical ventilation and cardiovascular monitoring required; titrate dose to cessation of electrographic seizures or burst suppression (NCS [Brophy 2012]).

Neurocritical Care Society recommendations (NCS [Brophy 2012]):

Loading dose: 1 to 2 mg/kg with initiation of a continuous infusion.

Continuous infusion: Initial: 20 mcg/kg/minute (1.2 mg/kg/hour). If the patient experiences breakthrough status epilepticus while on continuous infusion, increase infusion rate by 5 to 10 mcg/kg/minute (0.3 to 0.6 mg/kg/hour) every 5 minutes (may also administer a 1 mg/kg bolus dose with continuous infusion titration); dosage range: 30 to 200 mcg/kg/minute (1.8 to 12 mg/kg/hour). Note: Use caution with doses >80 mcg/kg/minute (>4.8 mg/kg/hour) for >48 hours. Prior to withdrawal, a period of at least 24 to 48 hours of electrographic control is recommended; withdraw gradually to prevent recurrent status epilepticus.

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience fatigue. Have patient report immediately to prescriber signs of pancreatitis (severe abdominal pain, severe back pain, severe nausea, or vomiting), severe dizziness; passing out; severe headache; difficulty breathing; slow breathing; shallow breathing; bradycardia; angina; abnormal movements; twitching; change in balance; difficulty swallowing; difficulty speaking; seizures; vision changes; severe injection site pain, redness, burning, edema, blistering, or irritation; muscle rigidity; or signs of propofol infusion syndrome (dark urine or urinary retention; fast breathing; tachycardia or abnormal heartbeat; severe fatigue; nausea or vomiting; severe muscle pain or weakness; or shortness of breath, excessive weight gain, or swelling of the arms or legs) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.