propofol

Absorption: IV administration results in complete bioavailability.

Distribution: Rapidly and widely distributed. Crosses the blood-brain barrier well; rapidly redistributed to other tissues.

Protein Binding: 95–99%.

Metabolism/Excretion: Rapidly metabolized by the liver. Primarily excreted in urine as metabolites.

Half-Life: 3–12 hr (blood-brain equilibration half-life 2.9 min).

Time/Action Profile ⬆ ⬇

(loss of consciousness)

ROUTE	ONSET	PEAK	DURATION‡
IV	40 sec	unknown	3–5 min

‡Time to recovery is 8 min (up to 19 min if opioid analgesics have been used).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to propofol, soybean oil, egg lecithin, or glycerol;
OB: Crosses placenta; may cause neonatal depression; may affect child's brain development when used during 3rd trimester.

Use Cautiously in:

Cardiovascular disease;
Lipid disorders (emulsion may have detrimental effect);
↑intracranial pressure;
Cerebrovascular disorders;
Hypovolemic patients (lower induction and maintenance dosage ↓ recommended);
Lactation: Safety not established in breastfeeding;
Pedi: Not recommended for induction of anesthesia in children 3 yr, or for maintenance of anesthesia in infants 2 mo; not for ICU or pre-procedure sedation; may affect brain development in children 3 yr;
Geri: Lower induction and maintenance dose recommended in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: bradycardia, hypotension, hypertension

Derm: flushing

GI: abdominal cramping, hiccups, nausea, vomiting

GU: discoloration of urine (green)

Local: burning, pain, stinging, coldness, numbness, tingling at IV site

MS: involuntary muscle movements, perioperative myoclonia

Neuro: dizziness, headache

Resp: apnea, cough

Misc: fever, PROPOFOL INFUSION SYNDROME

Interactions ⬆ ⬇

Drug-drug:

Additive CNS and respiratory depression with alcohol, antihistamines, opioid analgesics, and sedative/hypnotics (dose ↓ may be required).
Theophylline may antagonize the CNS effects of propofol.
Cardiorespiratory instability can occur when used with acetazolamide.
Serious bradycardia can occur with concurrent use of fentanyl in children.
↑risk of hypertriglyceridemia with intravenous fat emulsion.

Route/Dosage ⬆ ⬇

General Anesthesia

IV (Adults <55 yr): Induction: 40 mg every 10 sec until induction achieved (2–2.5 mg/kg total). Maintenance: 100–200 mcg/kg/min. Rates of 150–200 mcg/kg/min are usually required during first 10–15 min after induction, then ↓ by 30–50% during first 30 min of maintenance. Rates of 50–100 mcg/kg/min are associated with optimal recovery time. May also be given intermittently in increments of 25–50 mg.
IV Geriatric Patients , Cardiac Patients, Debilitated Patients, or Hypovolemic Patients): Induction: 20 mg every 10 sec until induction achieved (1–1.5 mg/kg total). Maintenance: 50–100 mcg/kg/min (dose in cardiac anesthesia ranges from 50–150 mcg/kg/min depending on concurrent use of opioid).
IV (Adults Undergoing Neurosurgical Procedures): Induction: 20 mg every 10 sec until induction achieved (1–2 mg/kg total). Maintenance: 100–200 mcg/kg/min.
IV (Children ≥3 yr–16 yr): Induction: 2.5–3.5 mg/kg, use lower dose for children ASA III or IV.
IV (Children 2 mo–16 yr): Maintenance: 125–300 mcg/kg/min (following first 30 min of maintenance, rate should be ↓ if possible), younger children may require larger infusion rates compared to older children.

Monitored Anesthesia Care Sedation

IV (Adults <55 yr): Initiation: 100–150 mcg/kg/min infusion or 0.5 mg/kg as slow injection. Maintenance: 25–75 mcg/kg/min infusion or incremental boluses of 10–20 mg.
IV Geriatric Patients , Debilitated Patients, or ASA III/IV Patients): Initiation: Use slower infusion or injection rates. Maintenance: 20% less than the usual adult infusion dose; rapid/repeated bolus dosing should be avoided.

ICU Sedation

IV (Adults ): 5 mcg/kg/min for a minimum of 5 min. Additional increments of 5–10 mcg/kg/min over 5–10 min may be given until desired response is obtained. (Range 5–50 mcg/kg/min.) Dose should be reassessed every 24 hr.

Availability ⬆ ⬇

(Generic available)

Lipid emulsion for injection: 10 mg/mL

Assessment ⬆ ⬇

Assess respiratory status, pulse, and BP continuously throughout propofol therapy. Frequently causes apnea lasting ≥60 sec. Maintain patent airway and adequate ventilation. Propofol should be used only by individuals experienced in endotracheal intubation, and equipment for this procedure should be readily available.
Assess level of sedation and level of consciousness throughout and following administration.
When using for ICU sedation, wake-up and assessment of CNS function should be done daily during maintenance to determine minimum dose required for sedation. Maintain a light level of sedation during these assessments; do not discontinue. Abrupt discontinuation may cause rapid awakening with anxiety, agitation, and resistance to mechanical ventilation.
Assess injection site for pain; may be minimized if larger veins of the forearm or antecubital fossa are used, especially in pediatric patients. Pain may be reduced by a prior injection of intravenous lidocaine (1 mL of a 1% solution). Monitor for extravasation.
Monitor for propofol infusion syndrome (severe metabolic acidosis, hyperkalemia, lipemia, rhabdomyolysis, hepatomegaly, cardiac and renal failure). Most frequent with prolonged, high-dose infusions (>5 mg/kg/hr for >48 hr) but has also been reported following large-dose, short-term infusions during surgical anesthesia. If prolonged sedation or increasing dose is required, or metabolic acidosis occurs, consider alternative means of sedation.

Toxicity and Overdose:

If overdose occurs, monitor pulse, respiration, and BP continuously. Maintain patent airway and assist ventilation as needed. If hypotension occurs, treatment includes IV fluids, repositioning, and vasopressors.

Implementation ⬆ ⬇

Do not confuse Diprivan with Diflucan.
- Dose is titrated to patient response.
- Propofol has no effect on the pain threshold. Adequate analgesia should always be used when propofol is used as an adjunct to surgical procedures.

IV Administration:

Diluent: Usually administered undiluted. If dilution is necessary, use only D5W. Shake well before use. Solution is opaque, making detection of contaminants difficult. Do not use if separation of the emulsion is evident. Contains no preservatives; maintain sterile technique and administer immediately after preparation.Concentration: Undiluted: 10 mg/mL. If dilution is necessary, dilute to concentration 2 mg/mL.
- Discard unused portions and IV lines at the end of anesthetic procedure or within 6 hr. For ICU sedation, discard after 12 hr if administered directly from vial or after 6 hr if transferred to a syringe or other container. Do not administer via filter <5–micron pore size.
- Aseptic technique is essential. Solution is capable of rapid growth of bacterial contaminants. Infections and subsequent deaths have been reported.
Rate: Administer over 3–5 min. Titrate to desired level of sedation. Frequently causes pain, burning, and stinging at injection site; use larger veins of the forearm, antecubital fossa, or a dedicated IV catheter. Lidocaine 10–20 mg IV may be administered prior to injection to minimize pain. Pedi: Induction doses may be administered over 20–30 sec.
Intermittent/Continuous Infusion: Diluent: Administer undiluted. Allow 3 to 5 min between dose adjustments to allow for and assess the clinical effects.Concentration: 10 mg/mL.
Rate: Based on patient's weight (see Route/Dosage section).

Patient/Family Teaching ⬆ ⬇

Inform patient that this medication will decrease mental recall of the procedure.
May cause drowsiness or dizziness. Advise patient to request assistance prior to ambulation and transfer and to avoid driving or other activities requiring alertness for 24 hr following administration.
Advise patient to avoid alcohol or other CNS depressants, including opioids, without the advice of a health care professional for 24 hr following administration.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Monitor neonates for hypotonia and sedation following maternal exposure to propofol.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇