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Product Name
:
KETAMINE-ELSaad
Chemical Name
:
Ketamine (HCl)
Therapeutic Category
:
Analgesic & Anesthetic
Pharmacologic Category
:
General Anesthetic
Pharmaceutical Form
:
Ampoule
Composition
:
Ketamine (HCl) 250mg/5ml
Lactation
Dosing
 
Dosing: Adult
May be used in combination with anticholinergic agents to decrease hypersalivation. Note: Titrate dose for desired effect.
Sedation/analgesia (unlabeled use):
I.M.: 2-4 mg/kg (White, 1982)
I.V.: 0.2-0.75 mg/kg (White, 1982)
Continuous I.V. infusion: 2-7 mcg/kg/minute (Hocking, 2003; Remérand, 2009; Zakine, 2008)
Induction of anesthesia (unlabeled dosing):
I.M.: 4-10 mg/kg (Green, 1990; Miller, 2010; White, 1982)
I.V.: 0.5-2 mg/kg (Miller, 2010; White, 1982)
Maintenance of anesthesia: May administer supplemental doses of one-half to the full induction dose or a continuous infusion of 0.1-0.5 mg/minute (per manufacturer). Note: To maintain an adequate concentration of ketamine for maintenance of anesthesia, 1-2 mg/minute has been recommended (White, 1982); doses in the range of 15-90 mcg/kg/minute (~1-6 mg/minute in a 70-kg patient) have also been suggested (Miller, 2010). Concurrent use of nitric oxide reduces ketamine requirements.

Dosing: Pediatric

May be used in combination with anticholinergic agents to decrease hypersalivation. Note: Titrate dose for desired effect.

Sedation (unlabeled use):
Oral (unlabeled route): 5-8 mg/kg for 1 dose (mixed in 0.2-0.3 mL/kg of cola or other beverage) given 30 minutes before the procedure (Sacchetti, 1994; Rosenberg, 1991)

Sedation/analgesia (unlabeled use):

I.M.: 2-5 mg/kg/dose (Green, 2011; Krause, 2000; McGlone, 2004; White, 1982)
I.V.: 0.5-1 mg/kg/dose (Sacchetti, 1994; Tobias, 1990)
Continuous I.V. infusion: 5-20 mcg/kg/minute (White, 1982; Tobias, 1990)
Children ≥16 years: Refer to adult dosing.

Dosing: Geriatric

Refer to adult dosing.
Use
 
Induction and maintenance of general anesthesia
Use - Unlabeled/Investigational
Analgesia, sedation
Adverse Reactions
 
Frequency not always defined.
Cardiovascular: Arrhythmia, bradycardia/tachycardia, hyper-/hypotension
Central nervous system: CSF pressure increased
Dermatologic: Erythema (transient), morbilliform rash (transient)
Gastrointestinal: Anorexia, nausea, salivation increased, vomiting
Local: Pain at the injection site, exanthema at the injection site
Neuromuscular & skeletal: Skeletal muscle tone enhanced (tonic-clonic movements)
Ocular: Diplopia, intraocular pressure increased, nystagmus
Respiratory: Airway obstruction, apnea, bronchial secretions increased, respiratory depression, laryngospasm
Miscellaneous: Anaphylaxis, dependence with prolonged use, emergence reactions (~12%; includes confusion, delirium, dreamlike state, excitement, hallucinations, irrational behavior, vivid imagery)
Contraindications
 
Hypersensitivity to ketamine or any component of the formulation; conditions in which an increase in blood pressure would be hazardous
Warnings / Precautions Drug
 
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). When used for outpatient surgery, the patient should be accompanied by a responsible adult.
• Dependence: May cause dependence (withdrawal symptoms on discontinuation) and tolerance with prolonged use.
• Emergence reactions: Postanesthetic emergence reactions which can manifest as vivid dreams, hallucinations, and/or frank delirium occur; these reactions are less common in patients <15 years of age and >65 years and when given intramuscularly. Emergence reactions, confusion, or irrational behavior may occur up to 24 hours postoperatively and may be reduced by pretreatment with a benzodiazepine and the use of ketamine at the lower end of the dosing range.
• Respiratory depression: Rapid I.V. administration or overdose may cause respiratory depression or apnea. Resuscitative equipment should be available during use.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with coronary artery disease, catecholamine depletion, hypertension, and tachycardia. Cardiac function should be continuously monitored in patients with increased blood pressure or cardiac decompensation.
• Cerebrospinal fluid (CSF) pressure elevation: Use with caution in patients with CSF pressure elevation; an increase in CSF pressure may be associated with use.
• Ethanol use: Use with caution in the chronic alcoholic or acutely alcohol-intoxicated.
Other warnings/precautions:
• Experienced physician: Should be administered under the supervision of a physician experienced in administering general anesthetics.
Controlled Substance
C-III
Metabolism/Transport Effects
Substrate (major) of CYP2B6, 2C9, 3A4
Interactions
 
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Risk X: Avoid combination
CYP2B6 Inhibitors (Moderate): May decrease the metabolism of CYP2B6 Substrates. Risk C: Monitor therapy
CYP2B6 Inhibitors (Strong): May decrease the metabolism of CYP2B6 Substrates. Risk D: Consider therapy modification
CYP2C9 Inducers (Highly Effective): May increase the metabolism of CYP2C9 Substrates (High risk). Risk C: Monitor therapy
CYP2C9 Inhibitors (Moderate): May decrease the metabolism of CYP2C9 Substrates (High risk). Risk C: Monitor therapy
CYP2C9 Inhibitors (Strong): May decrease the metabolism of CYP2C9 Substrates (High risk). Risk D: Consider therapy modification
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2C9 Substrates (High risk). Risk C: Monitor therapy
Quazepam: May increase the serum concentration of CYP2B6 Substrates. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Pregnancy
 
Pregnancy Implications
Adverse events have not been observed in animal reproduction studies. Ketamine crosses the placenta and can be detected in fetal tissue. Ketamine produces dose dependent increases in uterine contractions; effects may vary by trimester. The plasma clearance of ketamine is reduced during pregnancy. Dose related neonatal depression and decreased APGAR scores have been reported with large doses administered at delivery.
Monitoring Parameters
 
Heart rate, blood pressure, respiratory rate, transcutaneous O2 saturation, emergence reactions; cardiac function should be continuously monitored in patients with increased blood pressure or cardiac decompensation
Mechanism of Action
 
Produces a cataleptic-like state in which the patient is dissociated from the surrounding environment by direct action on the cortex and limbic system. Ketamine is a noncompetitive NMDA receptor antagonist that blocks glutamate. Low (subanesthetic) doses produce analgesia, and modulate central sensitization, hyperalgesia and opioid tolerance. Reduces polysynaptic spinal reflexes.
Pharmacodynamics / Kinetics
 
Onset of action:
I.V.: Anesthetic effect: 30 seconds
I.M.: Anesthetic effect: 3-4 minutes
Duration: Anesthetic effect: I.V.: 5-10 minutes; I.M.: 12-25 minutes
Distribution: Vd: 3 L/kg
Metabolism: Hepatic via hydroxylation and N-demethylation; the metabolite norketamine is 33% as potent as parent compound; greater conversion to norketamine occurs after oral administration as compared to parenteral administration
Bioavailability: Oral: 16%; Intranasal: 50%
Half-life elimination: Alpha: 10-15 minutes; Beta: 2.5 hours
Excretion: Primarily urine
 
   
 
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