propofol

propofol

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Product Description

 propofol 

COMPOSITION

Propofol Injection 20 ml: Each ml contains Propofol BP 10 mg.

DESCRIPTION

Propofol® Injectable Emulsion is a sterile, nonpyrogenic emulsion containing 10 mg/ml of propofol suitable for intravenous administration. Propofol® is slightly soluble in water and, thus, is formulated in a white to light yellow, oil-in-water emulsion. In addition to the active component, Propofol®, the formulation also contains soybean oil (100 mg/m1), glycerol (22.5 mg/ml), egg lecithin (12 mg/ml) and disodium edentate (0.005%) with sodium hydroxide to adjust pH.

PHARMACOLOGY

Propofol® Injectable Emulsion is an intravenous sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol induces hypnosis, with minimal excitation, usually within 40 seconds from the start of injection ‘the time for one arm-brain circulation). As with other rapidly acting intravenous anesthetic agents, the half-time of the blood-brain equilibration is approximately 1 to 3 minutes, accounting for the rate of induction of anesthesia.

Mechanism of action: Ultra short-acting anesthetics depress the central nervous system (CNS) to produce hypnosis and anesthesia without analgesia: 1. Binding of propofol to GABA A (BZD: Chloride) receptor in CNS causes prolongation of action of GABA and increased duration of opening of chloride channel resulting in hyperpolarisation of postsynaptic cell membrane and functional inhibition of postsynaptic neurons. 2. It causes wide spread inhibition of NMDA (N- methyl- D Aspartate) receptor through sodium channel gating. 3. Propofol increases dopamine concentration in the nucleus acumens (phenomenon associated with drug abuse and pleasure seeking behaviour) resulting in a sense of well being in a patient. 4. It also decreases serotonin levels in the area postrema through action on GABA receptors resulting in its anti emetic effect. 5. Depresses spinal cord activity (anti pruritic effect). Duration of effect: 5- 10 minutes.

Pharmacokinetics:

  1. pKa— 11
  2. Volume of distribution at steady-state (Vd): 3.5- 4.5 L/kg
  3. Protein binding: 95%-98%
  4. Distribution: Three compartment phase linear model after intravenous injection
  5. Metabolism & Excretion: Propofol is rapidly metabolised in the liver by conjugation to glucuronide and sulphate to produce water- soluble inactive compounds, wh.cn are excreted by kidneys. Less than 1% propofol is excreted unchanged in urine and only 2% is excreted, in feces.

INDICATION

Propofol® is a short-acting intravenous anesthetic agent suitable for

-induction and maintenance of genera` anesthesia

-sedation of ventilated patients receiving intensive care

-monitored anesthesia care sedation for surgical and diagnostic procedures

DOSAGE & ADMINISTRATION

Adults:

Induction of general anesthesia: The dosage of Propofol® should be titrated individually against the response of the patient. The ordinary initial dosage in adults is 40 mg (4ml) by slow intravenous bolus injection at intervals of 10 seconds until the clinical signs show the onset of anesthesia. The ordinary induction dose in healthy patient below 55 years of age is 2.2-2.5 mg/kg. A dose of 1.0-1.5 mg/kg is often sufficient for older patient. Lower doses, roost often 20 mg 2 ml, at intervals of 10 seconds, are recommended for patient of ASA grades 3 and 4.

Maintenance of general anesthesia: Anesthesia can be maintained by administering Propofol® either by continuous infusion or by repeat bolus injections to maintain sufficient anesthesia. Continuous infusion: The required rate of infusion varies considerably between patients. At the onset of anesthesia (during roughly the first 10-20 minutes), some patient may require a slightly higher infusion rate (8-10 mg/kg/h). However, sufficient anesthesia is normally achieved by infusing 4-6 (up to 12) mg/kg/h of Propofol®. Repeat bolus injections: 25-50 mg (2.5- 5.0 ml) bolus injections, depending on response. Sedation during intensive care: A bolus injection of 1.0-2.0 mg/kg should be given first, followed by continuous infusion adjusted according to required degree of sedation. An infusion rate of 0.3-4 mg/kg/h is usually sufficient.

Sedation for surgical and diagnostic procedures: Dosages shall be adjusted individually. Sufficient sedation for surgical and diagnostic procedures can usually be achieved by administering initially 0.5-1 mg/kg during 1-5 minutes, and maintained by continuous at a rate of 1-4.5 mg/kg/h. Bolus dose of 10-20 mg can be given in addition, should deeper sedation be suddenly required. Lower doses of Propofol are often sufficient for patient of ASA grades 3 and 4, and for older patient.

Children:

Propofol® is not recommended for use in children less then 3 years of age as its safety has not been demonstrated. Induction of general anesthesia: Dosage of Propofol® in children shall be adjusted for weight and age. The mean induction dosage in children over 8 years is 2.5 mg/kg, given by slow intravenous injection until the clinical signs show the onset of anesthesia. Younger children may need slightly higher doses of propofol per kilogram of weight. Lower dosages are recommended for children of ASA grades 3 and 4.

Maintenance of general anesthesia: Anesthesia can be maintained by administering Propofol® either by continuous infusion or by repeat bolus injections. Dosage shall be adjusted individually, but an infusion rate of 9-15 mg/kg/h is usually sufficient to achieve satisfactory anesthesia.Satirpara, Narsingdi, BangladeshManufactured by:Techno Drugs Ltd.Revision No.: 00

Sedation during intensive care, surgical diagnostic procedures: Propofol® is not recommended for sedation in children as its efficacy and safety have not been demonstrated. Although no casual relationship has been established, serious adverse events (including fatalities) have been reported in cases, where Propofol® has been used against recommenda-tions. Adverse events have most commonly been seen in children with respiratory tract infections given doses in excess of those recommended for adults.

 

Special Precautions for Handling: Propofol® and any equipment needed in its administration shall be treated strictly aseptically, since Propofol® contains no antimicrobial preservatives and as a lipid emulsion it supports the growth of bacteria and other micro-organisms. When Propofol® is to be aspirated, it must be drawn aseptically into a sterile syringe immediately after opening the vial, and administered without delay. Any fluids to be given simultaneously with Propofol® shall be administered as close to the cannula site as possible. Propofol® must not be administered via a microbiological filter. Propofol® and any equipment needed in its administration are for use in an individual patient only. According to general recommendations related to the use of lipid emulsions, the infusion period of undiluted Propofol®  shall not exceed 12 hours at a time. Any unused Propofol® and the infusion line shall be discarded at the end of infusion or not later than 12 hours from the start of infusion. Infusion may be repeated, if necessary.

Method of Administration: In order to reduce pain on injection, the induction dose of Propofol® may be mixed immedi-ately before injection in the plastic syringe with lidocaine 10 mg/m1 injection, in a ratio of 1 part of lidocaine injection for 20 parts of Propofol®. Propofol® can be administered either undiluted or diluted for infusion. Before injection or dilution, each vial shall be inspected for any irregularity. Should any changes be observed, the product shall not be used. Suitable equipment shall be used to ensure correct rate of infusion. Volumetric infusion pumps and syringe pumps, for example, are suitable for this purpose. The ordinary infusion set used alone is not sufficient to prevent accidential overdosage reliably enough. Compatibility: Propofol® may be diluted only with 5% dextrose infusion. Dilution shall not exceed 1 in 5 (containing 2 mg/ ml Propofol) and shall be prepared in an infusion bag or glass infusion bottle. If an infusion bag is used, the bag should be full and the dilution be prepared by withdrawing a volume of infusion fluid and replacing it with an equal volume of Propofol® .Special attention shall be paid to preparing the dilution aseptically, immediately before adminis7ration. Any diluted solution shall be used within 6 hours of preparation. Any remaining solution shall be discarded.

CONTRAINDICATION

Absolute contraindications: Patients with a known hypersensitivity to propofol or any of its components; allergies to eggs, egg products, soybeans or soy products: disorders of fat metabolism.

Relative contraindications: Patients undergoing stereotactic neurosurgery such as pallidotomy, as it temporary abolishes tremors in patients with Parkinsonism; Known case of Epilepsy; Untreated hypertensive, hypovolemia, compromised Left ventricle function; Hepatic or Renal impairment; Pregnant and lactating mother; Paediatric patients age < 3 years.

OVERDOSAGE

Accidental overdosage is likely to cause cardio-respiratory depression. Respiratory depression should be treated by artificial ventilation with oxygen. Cardiovascular depression would require lowering of the patient s head and, if severe, use of plasma expanders and pressor agents.

PRECAUTION

Containers should be shaken well before use. Any portion of the contents remaining after use should be discarded. Do not use if there is color change, evidence of excessive creaming or aggregation, if large droplets are visible or if there are other forms of phase separation. Incompatibility: Propofol® should not be mixed prior to administration with injections or infusion fluids with the exception of Propofol® 1% which can be mixed with 5% Dextrose (Intravenous Infusion BP) in PVC bags or glass infusion bottles or lignocaine Injection or alfentanil injection in plastic syringes. The neuromuscular blocking agents, atracurium and mivacurium should not be given through the same IV line as Propofol® without prior flushing.

PREGNANCY & LACTATION FDA

FDAPregnancy Category B. Propofol® is not recommended for obstetrics, including caesarean section deliveries. Propofol crosses the placenta, and as with other general anesthetic agents, the administration of Propofol may be associated with neonatal depression. Propofol® Injectable Emulsion is not recommended for use in nursing mothers because Propofol® injectable Emulsion has been reported to be excreted in human milk.

SIDE-EFFECT

Very common: Local pain on induction. Common: Hypotension, Bradycardia, Transient apnoea during induction, Nausea and vomiting during recovery phase, Headache during recovery phase, Withdrawal symptoms in children, Flushing in children. Uncommon: Thrombosis and phlebitis.

DRUG INTERACTION

  1. The induction dose requirements of Propofol® may be reduced in patients with intramuscular or intravenous premedication, particularly with opioids and sedatives (e.g., benzodiazepines, barbiturates, chloral hydrate, droperidol, etc). These agents may increase the anesthetic or sedative effects of Propofol and may also result in more pronounced decreases in systolic, diastolic, and mean arterial pressures and cardiac output, post- operative respiratory depression.
  2. Bradycardia with fentanyl and vecuronium.

STORAGE

Store at 20° C to 25° C. Do not freeze.

 COMMERCIAL PACK

Propofol® Injection 20 ml :  Each box contains 5 glass vials of 20 ml propofol emulsion.

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