Propofol-Lipuro

Quick links

Choose a section

Quick links to important sections

Advertisements

Propofol-Lipuro

Advertisements
Advertisements
Advertisements

Overview of Propofol-Lipuro

Property Description
Active ingredient Propofol (2,6-diisopropylphenol)
Form White milky oil-in-water emulsion
Pharmacological class General Anaesthetic (N01AX10)
Common use Induction and maintenance of general anaesthesia
Origin Synthetic compound (phenol derivative)

Understanding the Anaesthetic Agent

Propofol-Lipuro is a widely clinically recognized short-acting intravenous general anaesthetic agent used by medical professionals to quickly and reliably induce a controlled state of unconsciousness and profound sedation. It functions as a potent sedative-hypnotic drug, and its primary purpose is to produce hypnosis—a temporary, controlled loss of awareness.

This medication is a synthetic compound derived from the phenol chemical class, with the active substance chemically known as propofol (2,6-diisopropylphenol). Propofol-Lipuro belongs to the pharmacological class of general anaesthetics, and its general effect is to rapidly suppress the central nervous system (CNS). This agent's utility is characterized by its rapid distribution and clearance profile, leading to a quick and controlled emergence from the anaesthetic state.


The Composition: Propofol and the Lipuro Emulsion

Propofol-Lipuro is formulated as a sterile, white milky oil-in-water emulsion for injection or infusion, which is the necessary physical dosage form for its delivery. The core active ingredient, propofol, is a highly lipophilic molecule and requires this specialized lipid vehicle for safe and effective intravenous administration.

The designation Lipuro is a key differentiating feature, referring to the unique base/vehicle composition of the emulsion. This specific vehicle utilizes a blend of both Medium-chain Triglycerides (MCT) and Long-chain Triglycerides (LCT), stabilized by excipients such as refined soya-bean oil and egg lecithin. This balanced lipid mixture is a composition feature designed to enhance the stability of the formulation.


General Therapeutic Use and Rapid Action

Propofol-Lipuro is primarily applied to provide reversible general anaesthesia during surgical operations. It is also essential for delivering controlled deep sedation to patients, such as those undergoing mechanical ventilation in an intensive care setting. The medication’s characteristic rapid action and efficient clearance from the body are central to its utility, allowing medical teams precise control over the depth of the patient’s consciousness throughout the procedure.

Regulatory References

  1. Propofol 1% (10 mg/ml) SmPC (electronic Medicines Compendium)
  2. Propofol - StatPearls (NIH National Library of Medicine)
Advertisements

What side effects are possible with Propofol-Lipuro?

Propofol-Lipuro's safety profile is formally documented by regulatory authorities, classifying possible effects by frequency and the body system affected. These classifications reflect the official understanding of its risk characteristics.

Adverse Reaction Classifications

Adverse reactions are grouped according to the physiological system affected and their likelihood of occurrence:

  • Very Common (Affecting ge 1/10): Reactions at the administration site, primarily pain on injection, are highly frequent.
  • Common (Affecting ge 1/100): These include transient cardiovascular and respiratory changes such as Hypotension (low blood pressure) and Bradycardia (slow heart rate), as well as transient Apnoea (temporary cessation of breathing) during the initial administration phase. Nausea and Vomiting may also be observed upon waking.
  • Uncommon to Rare: Less frequent reactions involve Thrombosis or Phlebitis at the injection site, Convulsions, or Sexual Disinhibition.

Serious Adverse Reactions and Safety Constraints

The regulatory profile highlights specific serious, rare risks, notably Propofol Infusion Syndrome (PRIS). This is a potentially fatal complication associated with prolonged, high-dose continuous infusion, characterized by severe events like metabolic acidosis, rhabdomyolysis, and cardiac and renal failure. Anaphylaxis (severe allergic reaction) is documented as a very rare event.

Safety constraints require caution in specific patient groups. For older adults, increased sensitivity to haemodynamic effects necessitates careful use. Furthermore, the official label does not recommend the use of Propofol-Lipuro for ICU sedation in pediatric patients aged 16 years or younger. Contraindications include known hypersensitivity to the active substance or excipients, such as egg or soy products.

Advertisements

Overdose and Emergency Response

Propofol overdose is formally documented to result in severe, dose-dependent cardiorespiratory depression and arterial hypotension due to high blood concentrations. Acute intoxication can manifest as profound apnea (cessation of breathing) and oxyhemoglobin desaturation, with life-threatening outcomes including cardiac arrest and respiratory arrest.

Immediate medical attention must be sought for any sign of severe respiratory or cardiovascular compromise. Emergency actions mandated by regulatory authorities require immediate discontinuation of the Propofol infusion, establishment of a patent airway, provision of artificial ventilation with supplemental oxygen, and cardiovascular resuscitation if needed. No specific antidote is known, meaning management is exclusively symptomatic and supportive, utilizing measures such as vasoconstrictors for severe circulatory depression.

A distinct, severe toxicity known as Propofol Infusion Syndrome (PRIS) is associated with high-dose or prolonged exposure. This potentially fatal condition is characterized by findings such as severe metabolic acidosis, rhabdomyolysis, acute renal failure, and cardiac failure. Continuous monitoring is mandatory, and regulatory information notes that elderly, debilitated, or severely ill patients are more susceptible to these cardiorespiratory effects.

Advertisements

Therapeutic Uses of Propofol-Lipuro

This medication is generally used as an intravenous general anesthetic and sedation agent. Its therapeutic role is applied across three key clinical contexts, relevant for easing states of profound lack of awareness and physical response.

The medication is applied across therapeutic domains, including:

  • Induction and Maintenance of General Anaesthesia for all surgical operations.
  • Supportive, Profound Sedation for critically ill, mechanically ventilated adult patients in the intensive care setting.
  • Deep Sedation during short, non-surgical procedures, such as Monitored Anaesthesia Care (MAC) sedation.

Its functional role includes providing support in easing symptoms related to heightened physiological activity during surgical operations and procedures. It is applied across domains where additional symptomatic support is needed, supporting the achievement of symptom control in high-acuity scenarios like refractory status epilepticus.

“The medication supports the patient by contributing to a sense of stability and comfort, and assists with easing sensation or memory of the procedure.”


Quick Fact: Relief for Unconsciousness and Agitation

Quick Fact: Relief for Unconsciousness and Agitation This agent is relevant for easing symptoms related to heightened physiological activity (e.g., severe agitation) and symptoms that interfere with daily functioning (e.g., loss of awareness). It provides support that helps ease the overall symptom load and contributes to improved comfort during periods of heightened symptoms.

Advertisements

Eligibility and Restrictions for Use

Contraindications and Absolute Restrictions

Propofol-Lipuro is contraindicated (must not be used) in patients with a known hypersensitivity to the active substance, propofol, or to the excipients, which include refined soya-bean oil. Therefore, patients with known soya or peanut allergies are ineligible. Regulators also impose an absolute ban on using this medicine for sedation in the intensive care unit (ICU) in any patient 16 years of age or younger.


Age and Conditional Eligibility

Eligibility for use is tied to specific age groups and clinical status. For general anaesthesia and procedural sedation, the medicine is allowed for use in adults and children greater than one month of age. Use in newborn infants (under one month) is not recommended due to insufficient investigation and reduced clearance. Older adult patients and those with impaired cardiac, respiratory, renal, or hepatic function are generally eligible but require conditional use with special caution and potentially lower doses.


Reproductive Status

Propofol-Lipuro is not recommended for use in pregnant or breastfeeding women as safety has not been fully established in these populations by regulatory authorities.

Advertisements

What should I know about interactions with other medicines?

Interactions with other medicines and products

The official interaction profile for Propofol-Lipuro is defined by documented pharmacodynamic augmentation and exposure modification, as stated in authoritative regulatory labels. These interaction patterns necessitate specific professional management and observation.

1. Pharmacodynamic Augmentation

Co-administration with other Central Nervous System (CNS) Depressants, including Opioids, Sedatives, Inhalational Agents, and certain Analgesic Agents, may intensify the anesthetic, sedative, and cardiorespiratory depressant effects. This interaction is officially documented to result in more pronounced decreases in systolic, diastolic, and mean arterial pressures.

2. Exposure Modification and Specific Agents

The simultaneous administration of Valproate is officially documented to increase the blood concentration of propofol, a pharmacokinetic interaction that requires a corresponding reduction in the propofol dose. Cases of profound hypotension have been reported when propofol is used following treatment with Rifampicin. Furthermore, the concurrent use of Fentanyl in pediatric patients is associated with an increased risk of serious bradycardia, a specific population-dependent interaction note. The medication’s lipid vehicle, when co-administered with Ciclosporin, has been associated with the occurrence of leucoencephalopathy.

3. Procedural and Substance Constraints

Propofol-Lipuro must not be mixed in the same syringe or infusion line with any medicinal products or fluids not officially specified, due to administration requirements and physical compatibility constraints. Following administration, the consumption of alcohol is officially cautioned against, as it may increase the sedative effects.

Advertisements

Mechanism of Action

Mechanism of Action: Central Nervous System Modulation

The primary mechanism of Propofol involves positive allosteric modulation of GABA-A receptors, the main targets for the inhibitory neurotransmitter GABA. This interaction significantly increases the receptor's sensitivity to GABA, resulting in greater influx of chloride ions into the neuron. This mechanistic cascade drives neuronal hyperpolarization, leading to widespread suppression of electrical signaling across the central nervous system ( CNS).

In addition to enhancing inhibition, Propofol exerts secondary actions, including non-competitive antagonism of NMDA receptors (which mediate excitation) and inhibition of voltage-gated sodium channels. The collective CNS suppression extends to regulatory centers in the brainstem, leading to the dampening of autonomic control. This physiological modulation causes systemic vasodilation and a subsequent reduction in blood pressure, alongside a decrease in respiratory drive. The drug's high lipophilicity and its Lipuro lipid formulation facilitate its rapid transport across the blood-brain barrier, contributing to a rapid onset of effect and short duration of action due to quick redistribution.

Advertisements

Dosage and Administration Information

Propofol-Lipuro is administered exclusively via the intravenous (IV) route as an emulsion for injection (bolus) or continuous infusion. Due to the need for continuous titration, administration is restricted to physicians trained in anaesthesia or intensive care and must take place in an appropriately equipped facility.

Dosing is highly individualized and is continuously titrated based on the patient's body weight and the required depth of effect (anaesthesia or sedation). For induction of general anaesthesia in adults, the dose is typically 1.5 mg/kg to 2.5 mg/kg given over 1 to 3 minutes. Maintenance is achieved via continuous infusion, generally ranging from 4 mg/kg/hour to 12 mg/kg/hour. For ICU sedation, the infusion rate is adjusted, with a maximum dose of 4.0 mg/kg/hour.

Older adults generally require a reduced induction dose and a slower rate of administration. The 10 mg/mL formulation may be diluted with 5% glucose solution or 0.9% sodium chloride solution, provided the final concentration is not less than 2 mg/mL. For prolonged use in ICU sedation, administration must not exceed seven days. The container must be shaken before use, and the product is not authorized for prolonged ICU sedation in children under 16 years of age.

Advertisements

Recent Clinical Evidence

Propofol-Lipuro: Recent Clinical Evidence


Evidence for Use in General Anaesthesia

Research for inducing and maintaining a state of general anaesthesia during surgical operations was conducted in clinical trials, with a focus on Randomized Controlled Trials (RCTs) and Systematic Reviews. These studies included the general adult surgical population, as well as patients undergoing specific procedures. Researchers monitored specific time-related outcomes such as the time it took to achieve the desired anaesthetic depth and the time to patient awakening after the medication was stopped. Evidence suggests that while patterns related to emergence were often described consistently, findings related to the exact time intervals of anaesthetic onset showed some variability across different reported studies.


Evidence for Use in Intensive Care Sedation

Propofol-Lipuro was evaluated in studies involving supportive, profound sedation of critically ill adult patients who require mechanical ventilation in the Intensive Care Unit (ICU). These studies explored how the use of the medication was associated with various outcomes related to systemic or functional imbalance during critical care. The trials monitored outcomes such as the duration of time patients remained on mechanical ventilation and the total duration of their stay in the ICU. Findings indicate that this evidence contributes to understanding symptom patterns and recovery profiles in this critically ill group.


What is Still Uncertain About Propofol-Lipuro Research

Despite the breadth of research, the evidence base still contains important gaps and areas of uncertainty. One major limitation is that long-term effects are not fully established because follow-up durations were typically limited to the time around the procedure or the ICU stay. For instance, the evidence base for continuous ICU sedation does not include the pediatric population. Furthermore, for specialized indications, such as in acute neurological conditions, comparative evidence is lacking for comparison with other treatment options.

Advertisements

Frequently Asked Questions (FAQ)

Common questions about Propofol-Lipuro (FAQ)

Q: What is the main difference between general anesthesia and sedation using Propofol-Lipuro?

Official product information describes Propofol-Lipuro as being used for both sedation and general anesthesia. Both states involve controlled central nervous system (CNS) depression, but sedation is maintained at a lesser depth of CNS effect. General anesthesia is defined as the deeper, controlled state of unconsciousness and temporary loss of awareness (hypnosis).

Q: Why did some versions of Propofol-Lipuro require an Emergency Use Authorization (EUA) in the US?

Regulatory documents indicate that the Emergency Use Authorization (EUA) was issued to permit the use of the drug in the United States for ICU sedation. This action was taken to help address a national shortage of the medication during the COVID-19 pandemic.

Q: Why does the packaging mention a risk of abnormal urine color as a side effect?

Official adverse reaction documentation states that a change in the color of urine has been reported, sometimes appearing green. This occurs due to the body excreting inactive byproducts of the drug, particularly with prolonged intravenous administration. This is generally described in official sources as a change due to the body excreting inactive byproducts.

Q: Does Propofol-Lipuro have any known interactions with herbal products?

Official patient leaflets advise individuals to inform their healthcare providers about all medicines, including herbal products and supplements, prior to administration. This is a standard safety measure described in official patient information to help manage the potential for unlisted interactions.

Q: What are the concerns about using Propofol-Lipuro in patients who are very overweight?

The official product warnings advise caution in patients who have disorders of fat metabolism (such as high levels of fat in the blood). Because the drug is formulated as a lipid emulsion, official information notes that monitoring blood lipid levels may be required for these patients.

Q: Is there research on minimizing the pain felt at the injection site of Propofol-Lipuro?

Regulatory documents acknowledge that pain on injection is a very common side effect. Official instructions state that Propofol-Lipuro may be mixed with preservative-free lidocaine to reduce the pain felt upon initial injection.

Q: How is the depth of sedation measured when a patient is receiving a Propofol-Lipuro infusion?

The official labeling states that the dose is titrated (adjusted) based on the patient's desired level of effect. The dose is adjusted against the patient’s clinical signs and response until the necessary level of effect is achieved, according to official labeling.

Q: What are the general rules regarding eating or drinking before receiving Propofol-Lipuro?

Fasting rules regarding eating and drinking before sedation are standard care requirements, consistent with guidance from authoritative bodies. These rules are in place to manage the potential risks associated with receiving anesthesia.

Q: Is the recovery time from Propofol-Lipuro generally faster or slower than with other types of anesthesia?

Official product information characterizes Propofol-Lipuro as a short-acting agent. It is associated with a rapid recovery profile, which is a characteristic of the medication's rapid action profile. This fast clearance from the body allows for quick and controlled emergence from the sedative state.

Q: What sensation do patients typically describe when the medication is first given?

According to regulatory documents, the most common sensation reported at the time of administration is pain at the injection site. This is officially listed as a 'Very Common' adverse reaction.

Q: What are the general signs of a severe allergic reaction to Propofol-Lipuro?

Severe allergic reactions, known as anaphylaxis, are very rare but officially documented. They can be characterized by difficulty breathing or wheezing, swelling of the face, tongue, or throat, and a sudden reduction in blood pressure.

Q: Is it possible for Propofol-Lipuro to interact with common pain relievers or supplements?

Regulatory labels document that co-administration with other central nervous system depressants, which can include certain pain relievers, may intensify the sedative effects. Patients are generally advised in official patient materials to report all supplements to their provider to manage potential effects.

Q: Can a patient with an existing heart condition receive Propofol-Lipuro safely?

Patients with impaired cardiac (heart) function are generally eligible for the drug, but the official warnings note that special caution is required. This is because the medication has the potential to cause a reduction in blood pressure and a slowing of the heart rate.

Q: Does having a history of epilepsy affect eligibility for Propofol-Lipuro?

Official documents advise caution for patients with epilepsy. The medication is associated with the potential for neuroexcitatory symptoms, such as seizures or seizure-like movements, that may occur during the process of going to sleep or waking up.

Q: How long after receiving Propofol-Lipuro is it safe to breastfeed?

Official patient information provides guidance for breastfeeding mothers. It indicates that nursing should typically be stopped and breast milk discarded for 24 hours after receiving the medication.

Q: Is it common for Propofol-Lipuro to cause hallucinations or unusual dreams upon waking?

Adverse effects that relate to psychological state during recovery are documented, although specific mentions of hallucinations are not in the main frequency tables. These may include mood changes or loss of sexual control (sexual disinhibition).

Advertisements

How should Propofol-Lipuro be stored and disposed of?

Storage and Disposal of Propofol-Lipuro

Propofol-Lipuro must be stored and handled according to strict regulatory conditions to ensure the stability of the emulsion and maintain patient safety.


Required Storage Conditions

  • Temperature: Store the medicinal product below 25 C.
  • Freezing: It is mandatory to not freeze the product.
  • Protection: Unopened containers must be kept in the original outer carton to protect the contents from light.
  • Safety: The product must be stored out of the reach and sight of children.

In-Use Handling and Disposal

  • Propofol-Lipuro is for single use only. Any unused product or portion remaining after the first use must be discarded.
  • Due to the lack of preservatives, strict aseptic technique is required during handling.
  • Administration must commence immediately after opening or dilution.
  • Disposal of all waste material and unused contents must be performed in accordance with local requirements and regulations.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

Available in countries:

Equivalent of Propofol-Lipuro found in:

A-Z Index: