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PROPOFOL

Propofol is an intravenous sedative-hypnotic agent introduced in 1977. It is an alkylphenol formulated as an oil-in-water emulsion containing soybean oil, glycerol, and egg phosphatide. Propofol causes rapid induction of and recovery from anesthesia by increasing the action of the inhibitory neurotransmitter GABA at its receptor. It has a short context-sensitive half-life and is metabolized and cleared primarily by the liver. Propofol is well-suited for induction of anesthesia and conscious sedation due to its rapid onset and offset of effects. Its use is associated with dose-dependent decreases in blood pressure, respiratory drive, and intraocular pressure. High doses or

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Anusha Pradeep
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Topics covered

  • Anti-convulsant,
  • Malignant hyperthermia,
  • Pruritis treatment,
  • Baroreflex response,
  • Electrocorticographic recordin…,
  • Conscious sedation,
  • Platelet aggregation,
  • Elderly patients,
  • Hypoxic pulmonary vasoconstric…,
  • Respiratory effects
394 views22 pages

PROPOFOL

Propofol is an intravenous sedative-hypnotic agent introduced in 1977. It is an alkylphenol formulated as an oil-in-water emulsion containing soybean oil, glycerol, and egg phosphatide. Propofol causes rapid induction of and recovery from anesthesia by increasing the action of the inhibitory neurotransmitter GABA at its receptor. It has a short context-sensitive half-life and is metabolized and cleared primarily by the liver. Propofol is well-suited for induction of anesthesia and conscious sedation due to its rapid onset and offset of effects. Its use is associated with dose-dependent decreases in blood pressure, respiratory drive, and intraocular pressure. High doses or

Uploaded by

Anusha Pradeep
Copyright
© Attribution Non-Commercial (BY-NC)
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPT, PDF, TXT or read online on Scribd

Topics covered

  • Anti-convulsant,
  • Malignant hyperthermia,
  • Pruritis treatment,
  • Baroreflex response,
  • Electrocorticographic recordin…,
  • Conscious sedation,
  • Platelet aggregation,
  • Elderly patients,
  • Hypoxic pulmonary vasoconstric…,
  • Respiratory effects

PROPOFOL

-DR. K. ANUSHA

IV sedative hypnotic , reported by KAY


& ROLLY in 1977,

alkylphenol. 2,6 diisopropyl


phenol.C12H18O. ph7. unionised.

1% aqueous solution for IV


administration as oil in water emulsion containing 10% soya bean oil, 2.25% glycerol & 1.2% purified egg phosphatide

Can cause pain on injection - large vein


/ 1% lignocaine / short acting opioid

Can support growth of bacteria preservative - disodium edenate with NaOH / sodium metabisulphite

Preparations
Propofol DIPRIVAN Ampofol Aquavan

Mechanism of Action
Modulator of GABA receptor Decrease rate of dissociation of GABA
A

from receptor Increase duration of GABA activated opening chloride channel hyperpolarisation of the post synaptic membrane Functional inhibition

Pharmacokinetics
Absorption - only IV Distribution - the high lipid solubility
results in rapid onset of action

Awakening from a single bolus dose is


also rapid due to very short distribution half life of 2-8 min.

Clearance of propofol - hepatic


metabolism - sulfate & glucuronic acid derivatives - excreted by kidney

Elimination half life - 0.5 to 1.5 hrs Context sensitivity half life for infusion
upto 8 hrs is only 40 mins

Short effect site equilibration time Elimination - not impaired in cirrhosis /


renal dysfunction

Crosses placenta but rapidly cleared


from neonatal circulation

Clinical Uses
Drug of choice for induction - 1.5 to 2.5
mg / kg IV

Conscious sedation - 25 to 100 mcg /


kg / min IV minimal analgesic n amnestic effect.

Maintenance of anesthesia - 100 to 300


mcg / kg / min along with short acting opioid

Non Hypnotic Therapeutic 10 to 15Applicationto treat mg IV used in PACU nausea & vomiting post op &
chemotherapy induced.

10 mg IV - effective in treatment of pruritis associated with neuraxial opioids / cholestasis Anti convulsant - dose >1 mg / kg IV decreases seizure duration.
attenuation of bronchoconstriction.

Effect on Organ System

CNS
Decreases CMRO2; decreases CBF;
decreases ICP; decreases CPP

Cerebrovascular auto regulation not


affected

Tolerance does not develop Neuroprotective.

Cerebral protection during focal


ischemia

Does not interfere with adequacy of


electrocorticographic recording during awake craniotomy

duration of motor & EEG seizure activity


after ECT is significantly short compared to other iv anesthetics.

CVS
Decreases systemic blood pressure
accompanied by decreased cardiac output & systemic vascular resistance

Relaxation of vascular smooth muscle


is due to inhibition of sympathetic vasoconstrictor nerve activity

Laryngoscopy & intubation usually


reverses the hypotension

Negative ionotropic effect results from


decreased intracellular calcium availability secondary to inhibition of trans sarcolemmal calcium influx

Does not alter SA node or AV node


function

Blunts hypertensive response to


placement of LMA

Impairs normal arterial baroreflex


response to hypotension

Rarely, marked drop in preload may


lead to vagally mediated bradycardia

Blood pressure effects exaggerated in


hypovolemic patients, elderly patients & patients with compromised left ventricular function

RS
Profound respiratory depression usually
causes apnea after induction

Inhibits hypoxic ventilatory drive &


depress normal response to hypercarbia

Depresses upper airway reflexes

Maintanence dose - decreases tidal


volume & frequency of breathing

Hypoxic pulmonary vasoconstriction


remains intact

Renal & Hepatic


Prolonged infusion
- hepatocellular injury - lactic acidosis, bradydysrhythmia, rhabdomyolysis
phenol in urine

Prolonged infusion - green urine Uric acid excretion is increased in urine

Miscellaneous Effects
Decreases intraocular pressure Inhibits platelet aggregation Does not trigger malignant
hyperthermia

Secretion of cortisol is not influenced


even when administered for long periods in ICU

Side Effects

Allergic reaction Lactic acidosis / propofol infusion syndrome - in pediatric & adult patient receiving high dose infusion > 75 mcg / kg / min for longer than 24 hrs Abuse Bacterial growth Proconvulsant activity

THANK YOU

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