Handbook of Critical Care Drug Therapy

Editors: Susla, Gregory M.; Suffredini, Anthony F.; McAreavey, Dorothea; Solomon, Michael A.; Hoffman, William D.; Nyquist, Paul; Ognibene, Frederick P.; Shelhamer, James H.; Masur, Henry

Title: Handbook of Critical Care Drug Therapy, 3rd Edition

Copyright 2006 Lippincott Williams & Wilkins

> Table of Contents > Chapter 2 - Anesthesia: Analgesia, Sedation, and Neuromuscular Blockade

Chapter 2

Anesthesia: Analgesia, Sedation, and Neuromuscular Blockade

TABLE 2.1. Commonly Used Agents for Intravenous Sedation/Anesthesia

Drug Initial IV Dosagea Maintenance Infusiona Comments
Barbiturates
Pentobarbital 5 20 mg/kg Onset: <1 min Duration: 15 min 1 4 mg/kg/h Infuse loading dose over 2 h

Rapid administration produces hypotension and hemodynamic instability

Thiopental 3 4 mg/kg Onset: 10 20 s Duration: 5 15 min Not applicable Alkaline solution; decreases cardiac index
Benzodiazepines
Diazepam 0.1 0.2 mg/kg Onset: 1 3 min Duration: 1 2 h Not applicable Active metabolite with long half-life (desmethyldiazepam) contributes to activity
Lorazepam 0.04 mg/kg Onset: 5 15 min Duration: 1 6 h 0.02 0.1 mg/kg/h No active metabolites

Approximately 5 times more potent than diazepam

Midazolam 0.025 0.035 mg/kg Onset: 1 3 min Duration: 30 min 3 h 0.05 5 g/kg/min Elderly patients may develop apnea when midazolam is administered with narcotics

Approximately 3 4 times more potent than diazepam

Active metabolites accumulate in renal failure

Unpredictable elimination in critically ill patients (e.g., shock, liver failure)

Initial dose: 0.5 1 mg and titrate to effect in 0.5 2 mg increments

Other
Propofol 1 2 mg/kg Onset: <1 min Duration: 5 10 min 5 75 g/kg/min Generally a rapid recovery

Pain on injection is common with peripheral administration

Hypotension may occur especially with rapid bolus in hypovolemic or elderly patients

Propofol may increase serum triglyceride levels when used at high infusion rates; take caution when using in patients with pancreatitis

Doses of propofol of 5 mg/kg/h have been associated with cardiac failure and death

Safety of propofol has not been established for ICU sedation of children

Propofol contains 1.4 mmol of PO4=/100 ml

Dexmedeto- midine 1 g/kg IV over 10 min 0.2 0.7 g/kg/h for up to 24 h Alpha-2 adrenergic agonist with analgesic and sedative properties

Numerous cardiovascular effects including brady- and tachyarrhythmias, hyper- and hypotension, and atrioventricular block

Does not produce respiratory depression

Ketamine 1 2 mg/kg (or 5 10 mg/kg IM) Onset: <1 min Duration: 5 10 min 9 45 g/kg/min Usually preserves airway reflexes

Central sympathetic stimulation; hypertension; tachycardia; advantageous in hypovolemic patients

Tachyphylaxis is rare

Etomidate 0.3 0.4 mg/kg Onset: <1 min Duration: 3 5 min Not recommended

Produces adrenal suppression in continuous infusion

Minimal cardiovascular effects

Myoclonic muscle movements

Pain on IV injection

Remifentanil 0.05 g/kg Onset: <1 min Duration: <4 min 0.05 0.2 g/kg/min Ultrashort acting narcotic analgesic; used primarily as an intraoperative analgesic; elimination not dependent on liver or kidney function
CNS, central nervous system; ICU, intensive care unit; IM, intramuscular; IV, intravenous

aBolus doses and rates of infusion should be individualized to provide the desired level of sedation with consideration of potential hemodynamic compromise. Doses should generally be reduced for elderly and hypovolemic patients. It may be beneficial to wake patients daily and assess their CNS function during maintenance infusions to determine the minimal dose required for sedation.

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TABLE 2.2. Tracheal Intubation Techniques

Technique Clinical Setting Procedural Features Cautions
All listed below Indications: Upper airway obstruction

Airway protection

Tracheal toilet

Minimum required monitoring ECG, BP, pulse oximetry

Prepare patient for 100% O2

Establish IV access for rapid administration of resuscitative drugs and fluids if necessary

Equipment and drugs: Oxygen bag-mask ventilation equipment, monitors, suction laryngoscopes, ETT, stylettes, cuff, syringes, Code Blue cart

Anesthetics: Neuromuscular blocking agents, Sedative/hypnotic agents

Aspiration

Loss of airway

Dental damage

Trauma to airway

Hemodynamic compromise

Awake Anticipated difficult laryngoscopy

Full stomach

Minimize risk of airway loss as a result of sedation or neuromuscular blockade

Assessment and protection of neurologic function in cervical spine instability

Can be performed without depression of airway reflexes

Requires patient cooperation

Patient maintains airway and ventilation Vomiting from pharyngeal stimulation

Hypertension and tachycardic response to intubation is undesirable in certain clinical settings (e.g., myocardial ischemia, cerebral or aortic aneurysm)

Topical anesthesia of larynx or nerve blocks of larynx obtunds protective airway reflexes

Conscious: Oral Allows largest diameter ETT Topical anesthesia of pharynx or pharyngeal nerve blocks

Intubation with direct vision

 
Conscious: Blind nasal   Apply vasoconstrictor and topical anesthetic to nasal mucosa

Gently dilate nasal passage with soft nasal airways

Gently advance ETT from nose to trachea during inhalation

Nasal bleeding, avoid in coagulopathic patients

Sinusitis

Avoid in craniofacial trauma

Fiberoptic (oral or nasal)   Consider administering an antisialagogue (glycopyrrolate 0.2 mg IV)

Topical anesthetic and vasoconstrictor (for nasal)

Insert bronchoscope through ETT and directly into trachea

Advance ETT over bronchoscope and remove bronchoscope

 
Not Awake Uncooperative patients

Preexisting loss of consciousness (e.g., cardiac arrest, heavy sedation)

Blunts tachycardic and hypertensive response

Minimizes unpleasantness of procedure

  Risk of apnea, aspiration, airway loss
Unsedated unconscious Cardiac arrest Bag-mask ventilation until intubation equipment available

Immediate oral laryngoscopy and intubation

 
Rapid-sequence: oral (see Table 2.3) Full stomach or risk of aspiration in a patient without an anatomically difficult airway for laryngoscopy Administration of sedative and neuromuscular blocking agents

Cricoid pressure

Rapid intubation after onset of neuromuscular blockade

Check ETT placement

Remove cricoid pressure

Risk of airway loss

Hemodynamic compromise may result from sedation or positive pressure ventilation

Reintubation Nonfunctioning ETT (e.g., cuff leak)

Placement of an ETT with different features (e.g., larger diameter)

Sedate and administer neuromuscular blockade Chronically intubated patients may have swelling or traumatic changes of larynx making reintubation difficult

Patients who are dependent on high oxygen concentrations or PEEP may become hypoxemic

Direct vision extubation and reintubation Laryngoscopy possible Perform laryngoscopy with existing ETT in place

If glottis is visualized, remove existing ETT and replace with new one

Loss of airway
Styletted reintubationa Difficult laryngoscopy anticipated Insert stylette into existing ETT

Remove ETT without removing stylette

Insert new ETT over stylette

 
BP, blood pressure; ETT, endotracheal tube; ECG, electrocardiogram; IV, intravenous; PEEP, positive end-expiratory pressure

aaRefers to specific intubating stylettes and not to those routinely used to stiffen ETT during routine intubation.

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TABLE 2.3. Suggested Drugs for Rapid Sequence Intubation

Drug Dosage Comment
Sedatives/Anesthetics
Thiopental 3 4 mg/kg IV Reduce dose in elderly and hemodynamically unstable patients (0.25 1 mg/kg)

May produce hypotension and hemodynamic instability

Blunts intracranial hypertensive response to intubation and is useful in hemodynamically stable patients with elevated ICP

Ketamine 1 2 mg/kg IV

4 10 mg/kg IM

Useful in hypovolemic patients as this drug tends to support the circulation; may rarely produce myocardial depression

Produces hypertension, tachycardia, and elevates ICP; therefore, avoid in patients with myocardial ischemia, severe hypertension, or intracranial mass lesions

Etomidate 0.3 0.4 mg/kg IV Hemodynamic stability

Patients often have benign nonpurposeful muscle movements during induction which may be blunted by low doses of fentanyl (50 100 g)

Propofol 1 2.5 mg/kg IV Reduce dose in elderly and hemodynamically unstable patients (0.25 0.5 mg/kg)

May produce hypotension and hemodynamic instability

Muscle Relaxantsa
Cisatracurium 0.15 0.2 mg/kg IV Slower in onset than succinylcholine

Less histamine release than atracurium

Hemodynamic stability

Duration of action is dose-dependent (30 min 1 h)

Rocuronium 0.6 1.2 mg/kg IV Reported as most rapid onset of nondepolarizing neuromuscular blocking drugs (60 90 s)

Not recommended in Caesarean section patients

Hemodynamic stability

Duration of action is dose dependent (30 min 1 h)

Succinylcholine 1 mg/kg IV Depolarizing agent

Because of rapidity of onset, drug of choice unless specifically contraindicated (see Table 2.4)

Duration of action [congruent]10 min for patients with normal pseudocholinesterase activity

Vecuronium 0.1 0.28 mg/kg Slower onset than succinylcholine

Hemodynamic stability

Duration of action is dose dependent (30 min 1 h)

ICP, intracranial pressure; IM, intramuscular; IV, intravenous

aFor most clinical situations, cost may be the overriding consideration when choosing among the available nondepolarizing muscle relaxants.

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TABLE 2.4. Neuromuscular Blockade Bolus Dosing

Agent Dosage Onset/Duration Comments
Depolarizing Relaxant
Succinylcholinea Bolus: 1 2 mg/kg Onset: 1 min

Duration: 10 min

Prolonged effect in pseudocholinesterase deficiencies

Contraindications: family history of malignant hyperthermia, neuromuscular disease, hyperkalemia, open eye injury, major tissue injury (burns, trauma, crush); increased intracranial pressure; not indicated for routine use in children or adolescents

Side effects: bradycardia (especially in children), tachycardia, increased serum potassium

Nondepolarizing Relaxants
Atracurium Bolus: 0.5 mg/kg Onset: 2 min

Duration: 30 40 min

Rapid injection of atracurium bolus doses >0.6 mg/kg releases histamine and may precipitate asthma or hypotension

Metabolized in the plasma by Hofmann elimination and ester hydrolysis

Duration not prolonged by renal or liver failure; otherwise, see comments with vecuronium

Cisatracurium Bolus: 0.15 mg/kg Onset: 2 min

Duration: 30 40 min

Less histamine release than racemic atracurium (see above)

Metabolism and duration of action similar to atracurium

Mivacurium Bolus: 0.15 mg/kg followed in 30 s by 0.10 mg/kg Onset: 1.5 min

Duration: 25 min

Inject over 30 s

May cause histamine release

Metabolized by pseudocholinesterase

Rocuronium Bolus: 0.6 mg/kg Onset: 1 min

Duration: 30 40 min

Metabolized by liver, prolonged duration in hepatic failure

Duration not prolonged by renal failure

Used when succinylcholine is contraindicated or not preferred

Vecuronium Bolus: 0.1 mg/kg Onset: 2 min

Duration: >30 40 min

Metabolized by liver; duration not significantly prolonged by renal failure
  Bolus: 0.28 mg/kg Onset: 60 s

Duration: 100 min

Used when succinylcholine is contraindicated or not preferred

No cardiovascular effects

aThe pharmaceutical companies that manufacture succinylcholine have changed the package insert to indicate that the drug should not be used routinely in children, except for airway emergencies, risk of aspiration, and special situations. This practice is a response to reported complications including malignant hyperthermia, masseter muscle rigidity, rhabdomyolysis, and sudden cardiac arrest in children with undiagnosed myopathies.

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TABLE 2.5. Neuromuscular Blockade Maintenance Dosing

Agent Maintenance Dosage Duration Comments
Short Acting
Mivacurium 0.01 0.1 mg/kg

Infusion: 9 10 g/kg/min

15 min Metabolized by pseudocholinesterase
Intermediate Acting
Atracuriuma 0.08 0.10 mg/kg

Infusion: 5 9 g/kg/min

15 25 min Elimination independent of renal or hepatic function
Cisatracuriuma 0.01 0.02 mg/kg

Infusion: 1 2 g/kg/min

15 25 min Elimination independent of renal or hepatic function
Rocuroniuma 0.1 0.2 mg/kg

Infusion: 10 12 g/kg/min

10 25 min Metabolized primarily by the liver

Active metabolite significantly less potent than parent compound

Vecuroniuma 0.01 0.15 mg/kg

Infusion: 1 g/kg/min

15 25 min Bile is main route of elimination

Minimal dependence on renal function, although active metabolite accumulates in renal failure

Long Acting
Doxacuriuma 0.005 0.01 mg/kg

Infusion: 0.25 g/kg/min (not generally recommended)

35 45 min Cardiovascular stability

Predominantly renal elimination significant accumulation in renal failure

Pancuroniuma 0.01 0.015 mg/kg

Infusion: 1 g/kg/min (not generally recommended)

25 60 min Tachycardia (vagolytic effect)

Active metabolite accumulates in renal failure

aProlonged infusions of neuromuscular blocking drugs have been associated with undesirable prolongation of neuromuscular blockade and myopathy. When indicated, general guidelines for use of infusions include: (a) periodic monitoring of neuromuscular function (train-of-four stimulation) during administration of infusions, and (b) infusions should be stopped every 24 28 hours to allow recovery of function. Concurrent steroid administration may increase likelihood of this complication.

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TABLE 2.6. Reversal of Nondepolarizing Neuromuscular Blocking Drugs

Drug Dosage Onset/Duration Comments
Neostigmine-Glycopyrrolate 25 75 g/kg

5 15 g/kg

Onset: 3 8 min

Duration: 40 60 min

 
Pyridostigmine-Glycopyrrolate 100 300 g/kg

5 15 g/kg

Onset: 2 5 min

Duration: 90 min

Must be used to reverse long-acting neuromuscular blocking agents (i.e., doxacurium, pancuronium)
Edrophonium-Atropine 500 1000 g/kg

10 g/kg

Onset: 30 60 s

Duration: 10 min

Rapid onset; not useful for deep blockade
Use lower doses to reverse minimal blockade, maximum doses for deep blockade. The anticholinergic agent must be given to block undesired muscarinic effects of anticholinesterase drug; this applies even when the patient has a baseline tachycardia. Reversal of neuromuscular blockade is associated with a high incidence of transient arrhythmias.

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TABLE 2.7. Topical Anesthetics

Agent Concentration Use Comments
Cocaine 4% Topical to nares and nasopharynx prior to nasal intubation Vasoconstriction

Controlled substance

Lidocaine 1 4% Solution: oropharynx, tracheobronchial tree

Viscous: nasal and oral pharynx

Vasodilating, therefore must be used in conjunction with a vasoconstrictor during nasal intubation

Dilute solutions (1 2%) may be nebulized and inhaled to provide anesthesia for bronchoscopy

Total dose should be less than 400 mg

Large doses have been associated with methemoglobinemia

Eutectic Mixture Lidocaine and Prilocaine (EMLA)   Apply to skin for 1 h prior to procedures involving skin puncture Application to inflamed skin may increase absorption

Ineffective when rubbed into skin

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TABLE 2.8. Local Anesthetics for Infiltration and Nerve Blocks

Drug Concentration (Maximum Dose) Use Features
Lidocaine 0.5% (400 mg without epinephrine; 500 mg with epinephrine) Local infiltration Relatively short duration

Epinephrine prolongs block and decreases peak levels

Lidocaine 1 2% (400 mg without epinephrine; 500 mg with epinephrine) Nerve blocks Short duration

Epinephrine prolongs block and decreases peak levels

Bupivicaine 0.25 0.75% Nerve blocks

Epidural

Long duration, slow onset

Addition of epinephrine may not prolong block but may decrease systemic absorption

Avoid epinephrine-containing solutions in areas supplied by end-arteries (e.g., fingers, toes, penis). Nerve blocks should be performed by personnel trained in the procedures and in treatment of local anesthetic toxicity.

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TABLE 2.9. Comparison of Narcotic Analgesics

Drug Route/Equivalencea Onset of Action (min) Peak Analgesic Effect (min) Duration of Action (h)
Alfentanil IM: 1 mg IV: 1 2 IV: 1 2 IV: 0.25
Codeine PO: 200 mg PO: 30 45 PO: 60 120 PO: 4 6
  IM: 120 mg IM: 10 30 IM: 30 60 IM: 4
Fentanyl IM: 0.1 mg IV: <1 IV: 1 2 IV: 0.5 1
    IM: 7 5 IM: N/A IM: 1 2
Hydromor-phone PO: 7.5 mg PO: 30 PO: 90 120 PO: 4
  IM: 1.5 mg IM: 30 60 IM: 4 5  
    IV: 10 15 IV: <20 IV: 2 3
Levorphanol PO: 4 mg PO: 10 60 PO: 90 120 PO: 4 5
  IM: 2 mg IM: N/A IM: 30 60 IM: 4 5
      IV: <20 IV: 4 5
Meperidine PO: 300 mg PO: 15 PO: 60 90 PO: 2 4
  IM: 75 mg IM: 10 15 IM: 60 120 IM: 2 4
    IV: 1 IV: 15 30 IV: 2 4
Methadone PO: 20 mg PO: 30 60 PO: 90 120 PO: 4 6b
  IM: 10 mg IM: 10 20 IM: 60 120 IM: 4 5b
    IV: N/A IV: 15 30 IV: 3 4b
Morphine PO: 60 mg PO: 15 60 PO: 60 120 PO: 4 5
  IM: 10 mg IM: 10 30 IM: 30 60 IM: 4 5
    IV: <1 IV: 20 IV: 4 5
Oxycodone PO: 30 mg PO: 15 30 PO: 60 PO: 4 6
Propoxyphene Toxicc PO: 15 60 PO: 120 PO: 4 6
Remifentanild IV: 0.05 0.15 g/kg IV: <1 IV: <1 IV: 3 4 min
Sufentanil IM: 0.01 0.02 mg IV: <1 IV: 1 2 IV: 0.25 1
IM, intramuscular; IV, intravenous; PO, by mouth

aDose in mg therapeutically equivalent to morphine 10 mg IM. IM doses are used to specify equivalent doses but are not recommended when IV access is available.

bIncreases with repetitive dosing due to accumulation of drug and/or metabolites.

cDose equivalent to 10 mg of morphine would be too toxic to administer.

dRemifentanil is suitable for IV infusion only.

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TABLE 2.10. Parenteral Analgesic Agents

Drug Bolus Dosage Continuous Infusion Comments
Alfentanil 10 25 g/kg 0.5 3 g/kg/min Safe to use in renal failure because lack of active metabolites
Codeine 15 60 mg N/A Usually effective for mild to moderate pain

Recommended in renal failure

Fentanyl 25 50 g 50 100 g/h Slows heart rate

Chest wall rigidity can occur

Increased half-life with continuous infusions

Hydromor- phone 1 4 mg N/A Reserved for patients who are tolerant to and are receiving high doses of opiates

Recommended in renal failure

Ketorolac 15 60 mg IV followed by 15 30 mg IV q6h   Parenteral NSAID; lower doses in elderly patients; especially useful for orthopedic pain; reversible platelet dysfunction; associated with acute renal failure when given for more than 5 d

Advantage over opioids: no hemodynamic effects, respiratory depression, or ileus

Combined IV/IM/PO therapy limited to 5 d

Levorphanol 2 mg N/A Optimal IV dose has not been established

Avoid in patients with increased intracranial pressure, asthma, acute alcoholism

Meperidine 25 100 mg 5 35 mg/h Highly lipid soluble

Accumulation of neurotoxic (convulsant) normeperidine metabolite in renal failure and in patients receiving large cumulative doses

Avoid in patients receiving MAOI

Methadone 2.5 10 mg N/A Duration of action and half-life increases with repetitive dosing

With repetitive doses, the dose should be lowered or the interval lengthened to avoid excessive narcosis

Morphine 2 10 mg 2 5 mg/h Less lipid soluble versus fentanyl

Histamine release with bolus doses may cause hypotension or, rarely, bronchospasm

Active metabolite morphine-6-glucuronide accumulates in renal failure, producing enhanced narcosis

Remifentanil 0.05 g/kg 0.0125 0.025 g/kg/min Ultrashort action may limit its use for pain

Bolus doses are not recommended to treat postoperative pain

IV tubing must be cleared after administration to avoid inadvertent bolus dose

Sufentanil 0.2 0.6 g/kg 0.01 0.05 g/kg/min May allow for volume reduction in patients receiving large doses of continuous infusion narcotics
IV, intravenous; MAOI, monoamine oxidase inhibitor; NSAID, nonsteroidal anti-inflammatory drug

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TABLE 2.11. Patient-Controlled Analgesia (PCA) Guidelines

  Morphine Fentanyl Hydromorphone
Standard dilution 2 mg/mL 20 g/mL 0.5 mg/mL
Demand dose 1 mg 20 g 0.2 mg
Initial lockout 6 min 6 min 6 min
Initial basal rate 0 0 0
Considerations Generally, opioid of choice unless patient has renal insufficiency or is intolerant to morphine: nausea, vomiting, pruritus Less accumulation may result in less confusion in elderly patients; preferred over morphine in patients with renal insufficiency to avoid accumulation of morphine metabolites  
For patients who report pain on PCA, first assess the frequency of self-dosing. If the patient is not self-dosing at least 3 times per hour, encourage him or her to dose more often. Failing that, give the patient a bolus dose (2 5 mg of morphine or equivalent) and increase the demand dose to 1.5 or 2 mg of morphine or equivalent. Finally, consider an adjuvant drug (ketorolac) or a low basal rate (0.5 mg/h of morphine or equivalent).

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TABLE 2.12. Oral Analgesic Agents

Agent Onset/Duration Dosage Comments
Narcotic
Codeine Onset: 15 30 min

Duration: 4 6 h

30 60 mg q4h  
Codeine with acetaminophen 300 mg Onset: 15 30 min

Duration: 4 6 h

1 2 tablets q4h Available with codeine 7.5 mg, 15 mg, 30 mg, or 60 mg
Oxycodone 5 mg Onset: 15 30 min

Duration: 4 6 h

5 10 mg q4h Sustained release preparation, Oxycontin, has been associated with illegal abuse and diversion; deaths have resulted when the pills have been crushed and the powder inhaled
Oxycodone 5 mg with acetamino- phen 325 mg Onset: 15 30 min

Duration: 4 6 h

1 2 tablets q4h  
Oxycodone HCl 4.5 mg plus oxycodone terephthalate 0.38 mg with aspirin 325 mg Onset: 15 30 min

Duration: 4 6 h

1 2 tablets q4h  
Propoxyphene napsylate 50 or 100 mg with acetaminophen 325 mg Onset: 15 60 min

Duration: 4 6 h

1 2 tablets q4h  
Propoxyphene 32 or 65 mg Onset: 15 60 min

Duration: 4 6 h

32 65 mg q4h  
Non-narcotic
Acetaminophen Onset: 0.5 1 h

Duration: 3 6 h

325 650 mg q4h  
Aspirin Onset: 0.5 h

Duration: 3 6 h

325 650 mg q4h  
Choline magnesium salicylate Onset: 30 60 min

Duration: N/A

1000 2000 mg bid 500 mg = ASA 650 mg

May monitor with salicylate levels

Does not affect platelet aggregation

Available as a liquid 500 mg/5 ml

Ibuprofen Onset: 0.5 h

Duration: 3 6 h

400 800 mg tid-qid Reversible effect on platelet aggregation

Available as a liquid 100 mg/5 ml

Ketorolac Onset: 30 60 min

Duration: 4 6 h

10 mg q4 6h Reversible platelet effect

Reduce dose in elderly patients

Maximum oral dose 40 mg/day

Indicated only as continuation therapy to parenteral ketorolac up to a maximum duration of 5 d of combined IV/IM/PO administration

Tramadol Onset: 1 h

Duration: 3 6 h

50 100 mg q4 6h Reduce dose in patients with renal or liver failure
IV, intravenous; IM, intramuscular, PO, by mouth

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TABLE 2.13. Oral Sedative-Hypnotic Agents

Agent Onset Usual Dosage Half-Life Comments
Benzodiazepines
Alprazolam Intermediate Sedative: 0.25 0.5 mg PO tid 12 15 h No active metabolites
Diazepam Fast Sedative: 2 10 mg PO bid-qid Pre-op medication: 5 10 mg PO 1 h before procedure 20 200 h Active metabolites accumulate with chronic dosing and contribute to pharmacologic effect

Available in a liquid dosage form (1 mg/ml and 5 mg/ml)

Lorazepam Intermediate Sedative: 0.5 3 mg PO bid-tid 10 20 h No active metabolites

Safe to use in liver disease

    Hypnotic: 0.5 4 mg PO qhs   Available in a liquid dosage form (2 mg/ml)
    Pre-op medication: 1 4 mg PO 1 2 h before procedure   Amnesia may be produced for as long as 4 6 h without excessive sedation when lorazepam is used as a pre-op medication
Midazolam Fast Pre-op medication: 0.5 0.75 mg/kg PO 1 2 h before procedure 3 6 h Use high potency 5 mg/ml injectable form and dilute in 3 5 ml of fruit juice
Oxazepam Slow Sedative: 10 30 mg PO tid-qid

Hypnotic: 10 30 mg PO qhs

5 20 h No active metabolites
Temazepam Intermediate Sedative: N/A

Hypnotic: 7.5 30 mg PO qhs

10 17 h No active metabolites
Barbiturates
Pentobar- bital Fast Sedative: N/A

Hypnotic: 100 mg PO qhs

Pre-op medication: 100 mg PO 1 2 h before procedure

22 h Geriatric or debilitated patients may react to usual doses with excitement, confusion, or mental depression; lower doses may be required in these patients
Secobarbital Fast Sedative: N/A

Hypnotic: 100 mg PO qhs

Pre-op medication: 200 300 mg PO 1 2 h before procedure

28 h Geriatric or debilitated patients may react to usual doses with excitement, confusion, or mental depression; lower doses may be required in these patients
Other agents
Chloralhy-drate Intermediate Sedative: 250 mg PO tid after meals

Hypnotic:500 1000 mg PO qhs

Pre-op medication: 25 75 mg/kg up to 2 g PO 1 h before procedure

8 h TCE Active metabolite TCE

Available in liquid (10 mg/ml) and suppository (500 mg) dosage forms

Diphenhydramine Slow Hypnotic: 25 50 mg PO qhs 1 4 h Available in a liquid dosage form (12.5 mg/5 ml)

Half-life is prolonged in patients with liver disease

Eszopic-lone Fast Sedative: N/A

Hypnotic: 1 3 mg PO qhs

  Reduce to 1 mg in elderly patients, patients receiving CYP3A4 inhibitors and patients with severe hepatic disease
Zaleplon Fast Sedative: N/A

Hypnotic: 5 10 mg PO qhs

1 h The initial dose should be reduced to 5 mg in elderly and in patients with liver disease
Zolpidem Fast Sedative: N/A

Hypnotic: 5 10 mg PO qhs

2.5 h No active metabolites

An initial dose of 5 mg should be used in patients with liver disease

Amitripty-line Slow 25 100 mg qhs   Sedating tricyclic antidepressant

Contraindicated in acute recovery phase of myocardial infarction

Quetiapine Intermediate 25 100 mg qhs   Sedating dibenzothiazepine antiphychotic

May result in orthostatic hypotension or tachyarrhythmias

Anticholinergic effects (dry mouth, constipation)

PO, by mouth; TCE, trichloroethanol

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TABLE 2.14. Malignant Hyperthermia Therapy

Typical Presentation

Setting: Intraoperative or early postoperative.

Clinical: Tachycardia, tachypnea, ventricular arrhythmias, muscle rigidity, fever

Laboratory: Combined respiratory and metabolic acidosis, hyperkalemia, hypercalcemia, myoglobinuria, elevation in creatine phosphokinase.

Protocol for treatment

Discontinue triggering drug (succinylcholine, inhalational anesthetic).

Hyperventilate with 100% oxygen.

Dantrolene 2.5 mg/kg IV repeated every 5 10 min as dictated by the clinical situation. Although 10 mg/kg is often reported as a maximum total dose, more dantrolene may be needed.

Follow usual guidelines for treatment of metabolic acidosis, hyperkalemia (calcium has not been investigated in this setting), hyperthermia (external ice, gastric lavage), disseminated intravascular coagulation, prevention and treatment of myoglobinuric renal failure.

Procainamide as needed for arrhythmias refractory to general measures. Avoid calcium channel blockers in conjunction with dantrolene.

For health care providers having questions on patient management, the Malignant Hyperthermia Association of the United States operates a hot line: 1-800-644-9737.

IV, intravenous

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TABLE 2.15. Neuroleptic Malignant Syndrome

Typical Presentation

Setting: Most cases within 30 days of antipsychotic (neuroleptic) drug administration (incidence ~0.07 0.4%) or withdrawal of dopamine agonist (e.g., levodopa, amantadine).

Viewed as extreme extrapyramidal adverse effect versus idiosyncratic drug reaction related to antidopaminergic effects in central nervous system. Increased risk in highly agitated restrained patient.

Clinical Presentation: Hyperthermia caused by muscle rigidity, vasoconstriction, and possibly central nervous system effect. Dehydration, mental status changes (obtundation), autonomic instability (tachycardia, oscillations in blood pressure).

Laboratory: Elevated serum creatine phosphokinase, leukocytosis, metabolic acidosis.

Protocol for treatment

Discontinue antipsychotics if muscle rigidity impairs breathing or swallowing.

Control temperature (cooling blankets, ice baths, antipyretics; avoid NSAID because of renal effects), correct fluid and electrolyte disturbances.

Anticholinergics (if temperature <38.9 C): benztropine (up to 8 mg/d, PO, IM, IV), may worsen hyperthermia.

Dopamine agonists (if temperature >38.9 C): amantadine 200 300 mg/d PO, bromocriptine 7.5 75 mg/day PO, carbidopa/levodopa 300 800 mg/d PO.

Dantrolene 4 8 mg/kg/d PO/IV.

IV, intravenous; IM, intramuscular, PO, by mouth

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