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propofol (Diprivan)

 

Classes: General Anesthetics, Systemic

Dosing and uses of Diprivan (propofol)

 

Adult dosage forms and strengths

injectable solution

  • 10mg/mL

 

Anesthesia

Induction

  • <55 years: 40 mg IVP q10sec until onset (2-2.5 mg/kg)
  • >55 years or debilitated or ASA III/IV: 20 mg IVP q10sec until onset (1-1.5 mg/kg)

Maintenance

  • <55 years old: 0.1-0.2 mg/kg/min IV
  • >55 years old or debilitated or ASA III/IV: 0.05-0.1 mg/kg/min IV

 

MAC Sedation

Initiation

  • 0.1-0.15 mg/kg/min IV

Maintenance

  • 0.025-0.075 mg/kg/min IV
  • Geriatric: 0.02-0.06 mg/kg/min IV

 

Postoperative Nausea/Vomiting

20 mg IV; may repeat

 

ICU Patient

Initiation: 0.005 mg/kg/min IV

Maintenance: 0.005-0.05 mg/kg/min IV (0.005 mg/kg/min increment increase q5min)

 

Pediatric dosage forms and strengths

injectable solution

  • 10mg/mL

 

Anesthesia

Induction

  • 3-16 years: 2.5-3.5 mg/kg IVP over 20-30 sec

Maintenance

  • 2 months to 16 years: 0.125-0.3 mg/kg/min IV

 

Diprivan (propofol) adverse (side) effects

>10%

Hypotension (peds 17%; adults 3-26%)

Apnea lasting 30-60 sec (peds 10%; adults 24%)

Apnea lasting >60 sec (peds 5%; adults 12%)

Movement (peds 17%; adults 3-10%)

Injection site burning/stinging/pain (peds 10%; adults 18%)

 

1-10%

Respiratory acidosis during weaning (3-10%)

Hypertriglyceridemia (3-10%)

Hypertension (peds 8%)

Rash (peds 5%; adults 1-3%)

Pruritus (1-3%)

Arrhythmia (1-3%)

Bradycardia (1-3%)

Cardiac output decreased (1-3%; concurrent opioid use increases incidence)

Tachycardia (1-3%)

 

<1%

Arterial hypotension

Anaphylaxis

Asystole

Bronchospasm

Cardiac arrest

Seizures

Opisthotic rxn

Pancreatitis

Pulmonary edema

Phlebitis

Thrombosis

Renal tubular toxicity

 

Warnings

Contraindications

Lack of ventilatory support

Severe cardiac dysfunction

Documented hypersensitivity, egg allergy, soybean/soy allergy

Sedation in pediatric ICU patients

Use in labor and delivery (including cesarean section) may cause neonatal depression

 

Cautions

Drug vehicle (emulsion) is capable of supporting rapid growth of microorganisms; proper aseptic technique is imperative

Closely monitor patients with anemia, hepatic impairment, myxedema, or renal impairment

Risk of potentially fatal propofol infusion syndrome in ICU patients

Do not give bolus to ASA III/IV patients; rapid bolus doses will increase cardiorespiratory effects (ie, hypotension, apnea, airway obstruction)

Significant hypertriglyceridemia may be observed during infusion of propofol; 0.1 g lipid (1.1 kcal) per 1 mL propofoL

Accidental extravasation may result in tissue necrosis

Risk of chills, fever, body aches

Propofol infusion syndrome may occur; this is characterized by severe metabolic acidosis, hyperkalemia, lipemia, rhabdomyolysis, hepatomegaly, and cardiac and renal failure (esp with prolonged, high-dose infusions >5 mg/kg/hr for >48 hr)

Anxiety, agitation, and resistance to mechanical ventilation may occur with abrupt withdrawaL

 

Pregnancy and lactation

Pregnancy category: B

Lactation: Excreted in breast milk; effect on nursing infant not known

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Diprivan (propofol)

Mechanism of action

Short-acting, lipophilic sedative/hypnotic; causes global CNS depression, presumably through agonist actions on GABAa receptors

 

Absorption

Onset: 30-45 sec

Duration: 3-10 min (dose-dependent duration; dissipation is function of drug redistribution from CNS)

 

Distribution

Protein bound: 97-99%

 

Metabolism

Metabolized by hepatic conjugation to inactive compound

 

Elimination

Half-life: 40 min (initial); 24-72 hr (after 10-day infusion)

Excretion: Urine, feces

 

Administration

IV Incompatibilities

Y-site: Amikacin, amphotericin B, atracurium, bretylium, calcium chloride, ceftazidime (?), ciprofloxacin, cisatracurium, diazepam, digoxin, doxorubicin, gentamicin, levofloxacin, methotrexate, methylprednisolone sodium succinate, metoclopramide, minocycline, mitoxantrone, morphine sulfate (at high conc of morphine, compatible at 1 mg/mL), netilmicin, phenytoin, tobramycin, verapamiL

Do not mix with other drugs prior to administration

 

IV Compatibilities

Solution: D5W, LR, D5/LR, D5/0.45% NaCl, D5/0.2% NaCL

Syringe: ondansetron, thiopentaL

Y-site (partial list): Acyclovir, buprenorphine, dopamine, dobutamine, epinephrine, fentanyl, furosemide, hydromorphone, ketamine, lidocaine, meperidine, midazolam (?), nitroglycerin, KCl, MgSO4, vecuronium

 

IV Preparation

Does not need to be diluted (available form: 10 mg/mL); however, may be further diluted in D5W to 2 mg/mL

 

IV Administration

To reduce pain associated with injection, use larger veins of forearm or antecubital fossa; lidocaine IV (1 mL of a 1% solution) may also be used prior to administration

Do not use filter with <5 micron for administration

Soybean fat emulsion is used as a vehicle for propofoL

Strict aseptic technique must be maintained in handling, although a preservative has been added

Do not administer through the same IV catheter with blood or plasma

American College of Critical Care Medicine recommends use of a central vein for administration in an ICU setting

 

Storage

Store at room temp; refrigeration is not recommended

Protect from light

Do not use if there is evidence of separation of phases of emulsion