PROPOFOL 1%W/V (10MG/ML) INJECTABLE EMULSION

Indications

• Induction of general anesthesia
• Maintenance of general anesthesia
• Sedation for procedures

Dosage

Children: For children aged 1 month to 16 years, the usual dose for induction of anesthesia is 2.5–4 mg/kg, adjusted according to age, body weight, and response.

Adults: For induction of anesthesia, the usual adult dose is 1.5–2.5 mg/kg administered by slow intravenous injection. For maintenance, a continuous infusion of 4–12 mg/kg/hour may be used.

Mechanism of action

Propofol exerts its anesthetic effects by positively modulating the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) at GABA-A receptors, leading to increased inhibitory neurotransmission and resulting in sedation and anesthesia.

Pharmacodynamics

As a sedative-hypnotic agent, propofol rapidly induces hypnosis with minimal excitation, typically within 40 seconds after intravenous administration. This rapid action is due to its high lipid solubility, allowing for quick distribution to the central nervous system. The drug also has a favorable recovery profile, with patients often regaining consciousness shortly after cessation of the infusion.

Pharmacokinetics

Propofol is highly lipophilic, leading to rapid distribution and a short half-life. It is primarily metabolized in the liver via conjugation and oxidation, and excreted in urine, mainly as metabolites. The drug has a volume of distribution of around 4 liters per kilogram, and its clearance is approximately 1.5 liters per minute, which results in a short duration of action.

Contra-indications

• Hypersensitivity to propofol or any of its components
• Severe respiratory depression
• Acute porphyrias
• Acute circulatory failure (shock)
• Adrenal insufficiency

Adverse effects

• Apnea
• Hypotension
• Nausea
• Respiratory disorders
• Skin reactions
• Vascular pain
• Vomiting
• Arrhythmias
• Cough
• Hiccups
• Hypertension
• Muscle rigidity
• Neuromuscular dysfunction
• Nystagmus
• Procedural complications

Interactions

• Valproate may increase propofol concentration
• Active component of sacituzumab govitecan may increase exposure to propofol

Precautions

• Careful monitoring of fluids and electrolytes
• Use with caution in patients with cardiovascular disease
• Elderly patients may require dose adjustment
• Avoid in patients with fixed cardiac output, hypovolaemia, or severe hypotension

Pregnancy

Propofol should be used during pregnancy only if clearly needed and after careful consideration of risks and benefits.

Breast-feeding

Propofol is excreted in breast milk; caution should be exercised when administered to breastfeeding women.

Storage

Store at room temperature, protect from light, and do not freeze.

Formulations

• Emulsion for injection
• 0.5% or 1% injection solution

Mechanism of action

The action of propofol involves a positive modulation of the inhibitory function of the neurotransmitter gama-aminobutyric acid (GABA) through GABA-A receptors.

Pharmacodynamics

Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol produces hypnosis rapidly with minimal excitation, usually within 40 seconds from the start of an injection (the time for one arm-brain circulation).