Drugs

Published on 24/02/2015 by admin

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Last modified 24/02/2015

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Drugs

Acetaminophen (ofirmev)

Classification: Nonnarcotic analgesic; nonsteroidal anti-inflammatory drug

Indications: Mild to moderate analgesia for pain, antipyretic

Dose: The recommended dose of Ofirmev for patients 13 years old or older weighing 50 kg or more is 1000 mg every 6 hours or 650 mg every 4 hours intravenously; the maximum daily dose of acetaminophen by any route is 4000 mg. For patients older than 2 years old weighing less than 50 kg, the recommended dose is 15 mg/kg every 6 hours or 12.5 mg/kg every 4 hours intravenously.

Onset and duration: Onset: 5 to 15 minutes. Duration: 4 to 6 hours

Ofirmev can be given directly from the 100-mL vial (10 mg/mL) without further dilution and should be infused over 15 minutes.

Adverse effects: The antipyretic effect of acetaminophen may mask fever. In clinical trials of intravenous acetaminophen, adverse effects were minor and similar to those with placebo.

Precautions and contraindications: Avoid use in patients with liver disease. Overdose can cause serious or fatal hepatic injury, particularly in patients who are fasting. Hepatic toxicity after acetaminophen overdose can be treated with N-acetylcysteine.

Anesthetic considerations: Intravenous acetaminophen decreases pain and reduces fever in adults and children. It has an opioid-sparing effect. It is effective for mild to moderate pain.

Adenosine (adenocard)

Classification: Antiarrhythmic

Indications: Supraventricular tachycardia

Dose: 6-mg bolus administered over 1 to 2 seconds followed by normal saline line flush; may increase to 12-mg bolus if arrhythmia persists past 2 minutes. May repeat 12-mg bolus once.

Dosage forms: 3 mg/mL; 2- and 5-mL vials

Onset and duration: Onset: 10 to 20 seconds; duration: 1 minute

Adverse effects: Flushing, dyspnea, chest pain, headache, nausea, cough, malaise

Precautions and contraindications: Adenosine should not be used in patients receiving methylxanthine therapy (i.e., aminophylline, theophylline). Dipyridamole (Persantine) inhibits cellular uptake of adenosine. Use it with caution in patients with asthma. It is contraindicated in patients with second- or third-degree heart block.

Anesthetic considerations: This is an agent for use preoperatively and postoperatively. It is not used under anesthesia because it produces sinus arrest. It may be administered in lieu of or preceding administration of calcium channel blockers for long-term suppression.

Albuterol sulfate (proventil, ventolin)

Classification: β₂-adrenergic agonist, sympathomimetic, bronchodilator

Indications: Treatment of asthma and other forms of bronchospasm

Dose: Inhaler (metered dose): two deep inhalations 1 to 5 minutes apart; may be repeated every 4 to 6 hours (daily dose should not exceed 16 to 20 inhalations; each metered aerosol actuation delivers approximately 90 mcg/puff). Oral: 2 to 4 mg three to four times daily (total dose not to exceed 16 mg). Syrup: 2 mg/5 mL is available.

Onset and duration: Onset: inhalation: 5 to 15 minutes; oral: 15 to 30 minutes. Peak effect: inhalation: 0.5 to 2 hours; oral: 2 to 3 hours. Duration: inhalation: 3 to 6 hours; oral: 4 to 8 hours.

Adverse effects: Tachycardia, arrhythmias, hypertension, tremors, anxiety, headache, nausea, vomiting, hypokalemia

Precautions and contraindications: Safe use is not established during pregnancy. Use albuterol cautiously in patients with cardiovascular disease, hypertension, and hyperthyroidism. Monitor glucose and electrolyte levels.

Anesthetic considerations: Tolerance or tachyphylaxis can develop with long-term use. It has additive effects with epinephrine and other sympathomimetics. It is antagonized by β-receptor antagonists.

Alfentanil HCL (alfenta)

Classification: Opioid agonist; produces analgesia and anesthesia

Indications: Perioperative analgesia

Dose: Induction: intravenous: 50 to 150 mcg/kg; infusion: 0.1 to 3 mcg/kg/min.

Onset and duration: Onset: intravenous: 1 to 2 minutes; intramuscular: less than 5 minutes; epidural: 5 to 15 minutes. Duration: intravenous: 1 to 15 minutes; intramuscular: 10 to 60 minutes; epidural: 30 minutes.

Adverse effects: Bradycardia, hypotension, arrhythmias, respiratory depression; euphoria, dysphoria, convulsions, nausea and vomiting, biliary tract spasm, delayed gastric emptying, muscle rigidity, pruritus

Precautions and contraindications: Reduce the alfentanil dose in elderly, hypovolemic, or high-risk surgical patients and with the concomitant use of sedatives and other narcotics.

It crosses the placental barrier, and use in labor may produce respiratory depression in neonates. Resuscitation may be required; have naloxone available.

Anesthetic considerations: Circulatory and ventilatory depressant effects are potentiated by narcotics, sedatives, volatile anesthetics, and nitrous oxide. Analgesia is enhanced by α₂-agonists. Muscle rigidity in the higher dose range can be sufficient to interfere with ventilation.

Alprostadil, PGE₁ (prostin VR)

Classification: Prostaglandin E

Indications: Neonates: to maintain temporary patency of the ductus arteriosus until corrective or palliative surgery can be performed

Dose: Children: continuous infusion into large vein: 0.05 to 0.1 mcg/kg/min initially; when a therapeutic response occurs, decrease to lowest possible dose to maintain response (maximum dose: 0.4 mcg/kg/min).

Dosage forms: 500 mcg/mL, 1-mL ampules (refrigerate at 2° to 8° C). Must be diluted in 5% dextrose in water (D₅W) or normal saline for continuous infusion to a final concentration of 5 to 20 mcg/mL.

Onset and duration: Onset: 30 minutes; elimination half-life: 5 to 10 minutes; duration: 30 minutes to 2 hours

Adverse effects: Apnea (10%-12%), fever (14%), flushing (10%), bradycardia and seizures (4%), thrombocytopenia (less than 1%), disseminated intravascular coagulation (1%), anemia, tachycardia, hypotension (4%), diarrhea (2%), gastric outlet obstruction secondary to antral hyperplasia (related to cumulative dose)

Precautions and contraindications: Apnea is most frequent in infants weighing less than 2 kg within the first hour of alprostadil administration; ventilatory assistance may be required. It is contraindicated in neonates with respiratory distress syndrome. Use it with caution in patients with bleeding tendencies because of alprostadil’s ability to inhibit platelet aggregation. In all neonates, monitor arterial pressure; if arterial pressure falls significantly, decrease the rate of infusion.

Anesthetic considerations: Alprostadil is used to maintain a patent ductus arteriosus in newborns.

Aminocaproic acid (amicar)

Classification: Hemostatic agent; prevents the conversion of plasminogen to plasmin

Indications: Control of clinical bleeding in which hyperfibrinolysis is a contributing factor (hyperfibrinolysis should be confirmed by laboratory values such as prolonged thrombin time, prolonged prothrombin time, hypofibrinogenemia, or decreased plasminogen levels); also: open heart surgery; postoperative hematuria after transurethral prostatic resection, suprapubic prostatectomy, and nephrectomy; hematologic disorders such as aplastic anemia, abruptio placentae, cirrhosis, neoplastic diseases, and prophylaxis in patients with hemophilia before and after tooth extraction and other bleeding in the mouth and nasopharynx; reduction of blood loss in trauma and shock; possible prevention of ocular hemorrhaging and bleeding in subarachnoid hemorrhage

Dose: Acute bleeding: 5 g infused during the first hour followed by a continuous infusion of 1 g/hr for 8 hours or until bleeding is controlled

Chronic bleeding: 5 g preoperatively by intravenous piggyback over 1 hour; then 5 g by intravenous piggyback every 6 hours. Do not exceed 30 g in 24 hours. Decrease dose by 15% to 25% in patients with renal disease.

Children: 100 mg/kg intravenous piggyback over 1 hour; then 30 mg/kg/hr until bleeding is controlled (maximum dose: 18 g/m²/day).

Dosage forms: 250 mg/mL, 20 mL parenteral vial (5 g)

Administration: Dilute each dose in a proper volume of D₅W normal saline or lactated Ringer’s solution.

Onset and duration: Onset: 1 to 72 hours; half-life 1 to 2 hours in patients with normal renal function. No single concentration fits all. It must be diluted. Consult the package insert, an intravenous reference, or the pharmacy. Duration: 8 to 12 hours.

Adverse effects: Convulsions; myopathy; rarely muscle necrosis, nausea, vomiting; rapid infusion associated with hypotension, bradycardia, arrhythmias

Precautions and contraindications: A definitive diagnosis of hyperfibrinolysis must be made before aminocaproic acid administration. Use caution in patients with cardiac, renal, or hepatic disease. Administration in the presence of renal or ureteral bleeding is not recommended because of ureteral clot formation and the possible risk of obstruction. Owing to the substantial risk of serious or fatal thrombus formation, aminocaproic acid is contraindicated in patients with disseminated intravascular coagulation unless heparin is administered concurrently.

Anesthetic considerations: Do not administer without a definite diagnosis of laboratory findings indicative of hyperfibrinolysis.

Aminophylline (theodur, others)

Classification: Bronchodilator

Indications: Long-term therapy for bronchial asthma; reversal of bronchospasm associated with chronic obstructive pulmonary disease

Dose: Loading dose: for patients not already receiving a theophylline preparation, intravenous: 5 to 6 mg/kg (administered over 20-30 minutes). Oral or rectal: 6 mg/kg. Maintenance: intravenous: 0.5 mg/kg/hr; oral: 2 to 4 mg/kg every 6 to 12 hours. Therapeutic range: 10 to 20 mcg/mL.

Dilution for infusion loading dose: dilute 500 mg in 500 mL D₅W or normal saline (1 mg/mL)

Children 9 to 16 years: 1 mg/kg/hr for 12 hours; then 0.8 mg/kg/hr; children 6 months to 9 years: 1.2 mg/kg/hr for 12 hours; then 1 mg/kg/hr

Dosage forms: injection: 25 mg/mL; tablets: 100, 200 mg; tablets (sustained release): 225 mg; oral solution: 105 mg/5 mL; rectal solution: 60 mg/mL (rectal solution not marketed in the United States); rectal suppositories: 250, 500 mg

Onset and duration: Onset: intravenous: 2 to 5 minutes; oral: within 30 minutes. Duration: oral: 4 to 8 hours

Adverse effects: Palpitations, sinus tachycardia, supraventricular and ventricular tachycardia, flushing, tachypnea, seizures, headache, irritability, nausea, vomiting, hyperglycemia

Elevated serum levels are noted in patients receiving cimetidine, quinolone antibiotics, and macrolide antibiotics and in patients with cardiac failure or liver insufficiency. Decreased serum levels are seen with phenobarbital, phenytoin, rifampin, and smokers. Toxicity occurs with plasma levels greater than 20 mcg/mL. Avoid rapid infusions, which may cause hypotension, arrhythmias, and possibly death.

Precautions and considerations: Caution when used in patients with seizure disorders, hypertension, or ischemic heart disease.

Anesthetic considerations: Aminophylline potentiates the pressor effects of sympathomimetics and may produce seizures, cardiac arrhythmias, cardiorespiratory arrest, and ventricular arrhythmias with excessive plasma levels or in patients receiving volatile anesthetics. Use isoflurane or sevoflurane in patients who must be administered aminophylline or other exogenous sympathomimetic drugs before or during surgery. Use of halothane may potentiate cardiac dysrhythmia.

Amiodarone (cordarone)

Classification: Class III antiarrhythmic

Indications: Treatment of life-threatening ventricular arrhythmias that do not respond to other antiarrhythmics (i.e., recurrent ventricular fibrillation and hemodynamically unstable ventricular tachycardia); selective treatment of supraventricular arrhythmias

Dose: Loading: oral: 800 to 1600 mg/day for 1 to 3 weeks; maintenance: oral: 200 to 600 mg/day; therapeutic level: 1 to 2.5 mcg/mL

Dosage forms: tablets: 200 mg; intravenous: 100 to 300 mg

The recommended starting dose of intravenous amiodarone HCl is about 1000 mg over the first 24 hours of therapy delivered by the following infusion:

• Loading infusions: first rapid: 150 mg over the first 10 minutes (15 mg/min). Add 3 mL of amiodarone HCl intravenously (150 mg) to 100 mL D₅W (concentration = 1.5 mg/mL). Infuse 100 mL over 10 minutes.

• Followed by slow infusion: 360 mg over the next 6 hours (1 mg/min). Add 18 mL of amiodarone HCl intravenously (900 mg) to 500 mL D₅W (concentration = 1.8 mg/mL).

• Maintenance infusion: 540 mg over the remaining 18 hours (0.5 mg/min). Decrease the rate of the slow loading infusion to 0.5 mg/min.

Onset and duration: Onset: 2 to 4 days. Half-life: between 2 weeks and 2 months (including active metabolites). Duration: 45 days

Adverse effects: Arrhythmias, pulmonary fibrosis or inflammation, hepatitis or cirrhosis, corneal deposits, hyperthyroidism, hypothyroidism, peripheral neuropathy, cutaneous photosensitivity

Precautions and contraindications: Amiodarone increases serum levels of digoxin, warfarin, quinidine, procainamide, phenytoin, and diltiazem. The likelihood of bradycardia, sinus arrest, and atrioventricular block increases with concurrent β-adrenergic antagonist and calcium channel blocker therapy.

Anesthetic considerations: Antiadrenergic effects are enhanced in the presence of general anesthetics and manifest as sinus arrest, atrioventricular block, low cardiac output, or hypotension. Drugs that inhibit the automaticity of the sinus node such as halothane and lidocaine could accentuate the effects of amiodarone and increase the likelihood of sinus arrest. The potential need for a temporary artificial cardiac (ventricular) pacemaker and administration of sympathomimetics such as isoproterenol should be considered in patients receiving this drug.

Amrinone lactate (inocor)

Classification: Positive inotrope (phosphodiesterase inhibitor)

Indication: Short-term management of congestive heart failure

Dose: Loading dose: 0.75 mg/kg over 2 to 3 minutes. A second bolus may follow after 30 minutes. Maintenance is by continuous infusion of 5 to 10 mcg/kg/min (maximum dose: 10 mg/kg/day).

Dosage forms: injection: 5 mg/mL; dilution for infusion: 500 mg in 500 mL normal saline solution

Onset and duration: Onset: within 5 minutes; duration: 30 minutes to 2 hours

Adverse effects: Hypotension, arrhythmia, thrombocytopenia, abdominal pain, hepatic dysfunction

Precautions and contraindications: Use amrinone with caution in hypotensive patients. Avoid exposure of the ampule to light. Do not mix in solutions containing dextrose or furosemide. Use it with caution in patients with allergies to bisulfites. Fluid balance, electrolyte concentrations, and renal function should be monitored carefully during treatment. Monitor platelet counts on a long-term basis. Amrinone contains sodium metabisulfite, a sulfite that may cause allergic-type reactions, including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in susceptible patients. Sulfite sensitivity is seen more frequently in patients with asthma than in patients without asthma.

Anesthetic considerations: This drug is an alternative to conventional inotropes. It is useful when both inotropic and vasodilating properties are desired or to lower pulmonary vascular resistance. Milrinone, another phosphodiesterase-3 inhibitor, is more commonly used.

Aprepitant (emend)

Classification: Antiemetic; neurokinin 1 (NK1) receptor antagonist

Indication: Postoperative nausea and vomiting

Dose: Oral 40-mg dose administered within 3 hours before the induction of anesthesia

Onset and duration: Onset: 1 to 3 hours. Duration: up to 24 hours when used in multimodal therapy

Adverse effects: The most frequent adverse events reported in clinical trials of aprepitant for postoperative nausea and vomiting were constipation, nausea, pruritus, pyrexia, hypotension, headache, and bradycardia.

Precautions and contraindications: Aprepitant produces a dose-dependent inhibition of CYP3A4 and should be used with caution in patients receiving drugs that are primarily metabolized through CYP3A4. Weak inhibition of CYP3A4 by a single 40-mg dose is not expected to alter the plasma concentrations of these products to a clinically significant degree.

The efficacy of hormonal contraceptives may be reduced during coadministration with aprepitant for up to 28 days after the last dose.

Anesthetic considerations: Aprepitant is most effective when used as a component of multimodal prophylaxis with a serotonin receptor blocker.

Atracurium (tracrium)

Classification: Nondepolarizing skeletal muscle relaxant

Indications: Relaxation of skeletal muscles during surgery; adjunct to general anesthesia or mechanical ventilation; facilitation of endotracheal intubation

Dose: Initially for paralyzing: intravenous: 0.3 to 0.5 mg/kg; maintenance: intravenous: 0.08 to 0.1 mg/kg

Dosage forms: injection: 10 mg/mL

Onset and duration: Onset: less than 3 minutes. Duration: 30 to 45 minutes. Elimination: plasma (Hofmann elimination, ester hydrolysis). The primary metabolite is laudanosine (a cerebral stimulant) produced in low doses, excreted primarily in the urine.

Adverse effects: Primarily resulting from histamine release: vasodilation, hypotension, sinus tachycardia, sinus bradycardia, hypoventilation, apnea, bronchospasm, laryngospasm, dyspnea, inadequate block, prolonged block, rash, and urticaria

Precautions and contraindications: Use atracurium with caution in patients with conditions in which histamine release may prove hazardous, in patients with myasthenia gravis or other muscle disorders, and in patients with electrolyte disturbances.

Anesthetic considerations: Monitor the patient’s response with a peripheral nerve stimulator. Reverse the effects with anticholinesterase. Pretreatment doses may induce sufficient neuromuscular blockade to cause hypoventilation in some patients.

Atropine sulfate

Classification: Competitive acetylcholine antagonist at muscarinic receptor

Indications: Symptomatic bradycardia, asystole, cardiopulmonary resuscitation (CPR); antisialagogue; for vagolytic effects to block bradycardia during surgery from stimulation of the carotid sinus, traction on abdominal viscera, or extraocular muscles; blockade of muscarinic effects of anticholinesterases; adjunctive therapy in the treatment of bronchospasm, peptic ulcer disease

Dose: Adults: sinus bradycardia. CPR: intravenous, intramuscular, subcutaneous, via endotracheal tube (diluted in 10 mL of sterile water or normal saline): 0.5 to 1 mg every 3 to 5 minutes as indicated (maximum dose: 40 mcg/kg/event). Preoperative: 0.4 mg intramuscular, subcutaneous, or oral: 30 to 60 minutes preinduction.

Blockade of muscarinic effects of anticholinesterases: 7 to 10 mcg/kg with edrophonium, 15 to 30 mcg/kg with neostigmine, 15 to 20 mcg/kg with pyridostigmine

Bronchodilation: inhalation: 0.025 mg/kg every 4 to 6 hours. Dilute to 2 to 3 mL in normal saline and deliver by compressed air nebulizer (maximum dose: 2.5 mg/dose). Pediatric bronchodilatory dose: 0.05 mg/kg diluted in normal saline three or four times daily.

Children: sinus bradycardia, CPR: intravenous, intramuscular, subcutaneous, or via endotracheal tube: 0.02 mg/kg every 5 minutes up to a maximum of 1 mg in children and 2 mg in adolescents (minimum dose, 0.1 mg).Preoperative: oral, intramuscular, subcutaneous: 0.02 mg/kg for neonates, 0.1 mg for children weighing 3 kg, 0.2 mg for those weighing 7 to 9 kg, and 0.3 mg for those weighing 12 to 16 kg.

Dosage forms: injection: 0.05, 0.1, 0.3, 0.4, 0.5, 0.8, and 1 mg/mL; inhalation solution: 0.2%, 0.5%; tablets: 0.4 mg, 0.6 mg

Onset and duration: Inhibition of salivation occurs within 30 minutes to 1 hour and peaks in 1 to 2 hours after oral or intramuscular atropine administration. Increase in heart rate occurs within 3 to 10 minutes after intravenous or intramuscular administration. Duration: 15 to 45 minutes after intravenous administration and 2 to 4 hours after intramuscular administration.

Adverse effects: Transient bradycardia resulting from a weak peripheral muscarinic cholinergic agonist effect in small doses (less than 0.5 mg in adults), tachycardia (high doses), urinary hesitancy, retention, mydriasis, blurred vision, increased intraocular pressure, decreased sweating, excitement, agitation, drowsiness, confusion, hallucinations, dry nose and mouth, allergic reactions, constipation.

Children and elderly patients are more susceptible to these adverse effects.

Precautions and contraindications: Avoid atropine in situations in which tachycardia would be harmful (i.e., thyrotoxicosis, pheochromocytoma, coronary artery disease). Avoid in hyperpyrexial states because it inhibits sweating. It is contraindicated in acute-angle glaucoma, obstructive disease of the gastrointestinal tract, obstructive uropathy, paralytic ileus or intestinal atony, and acute hemorrhage in patients with unstable cardiovascular status. Use it with caution in patients with tachyarrhythmias, hepatic or renal disease, congestive heart failure, chronic pulmonary disease (because a reduction in bronchial secretions may lead to formation of bronchial plugs), autonomic neuropathy, hiatal hernia, gastroesophageal reflux, gastric ulcers, gastrointestinal infections, and ulcerative colitis.

Anesthetic considerations: Additive anticholinergic effects may occur when atropine is administered concomitantly with meperidine, some antihistamines, phenothiazines, tricyclic antidepressants, and antiarrhythmic drugs that possess anticholinergic activity (e.g., quinidine, disopyramide, procainamide).

Bumetanide

Classification: Loop diuretic

Indications: Treatment of edema of cardiac, hepatic, or renal origin; hypertension, pulmonary edema; usually reserved for patients who do not respond to thiazide diuretics or in whom a rapid onset of diuresis is desired.

Dose: Initial dose: 0.5 to 1 mg intravenously over 1 to 2 minutes. If response is not adequate after the initial dose, a second or third dose may be administered at intervals of up to 2 to 3 hours, up to a maximum of 10 mg/day.

Children: intravenous, intramuscular, oral: 0.015 to 0.1 mg/kg. maximum, 2 mg/day

Onset and duration: Onset: intravenous: few minutes. Peak effect: 15 to 30 minutes. Duration: 4 hours with normal doses of 1 to 2 mg and up to 6 hours with higher doses. Elimination half-life: 1 to 1.5 hours

Adverse effects: Transient leukopenia, granulocytopenia, thrombocytopenia, hypotension, chest pain, dizziness; electrolyte abnormalities such as hyperuricemia, hypomagnesemia, hypokalemia, hypochloremia, azotemia, hyponatremia, or metabolic alkalosis; hyperglycemia; diarrhea; pancreatitis; nephrotoxicity; muscle cramps; arthritic pain; ototoxicity (less frequent than with furosemide)

Precautions and contraindications: Patients may have anuria, hypersensitivity to bumetanide, severe fluid and electrolyte imbalances, and hepatic coma if an increase in blood urea nitrogen or creatinine occurs. Patients who are allergic to sulfonamides may have hypersensitivity to bumetanide.

Anesthetic considerations: Loop diuretics may increase the neuromuscular blocking effect of nondepolarizing relaxants.

Bupivacaine HCL (marcaine, sensorcaine)

Classification: Amide-type local anesthetic

Indication: Regional anesthesia

Dose: Infiltration or peripheral nerve block: less than 150 mg (0.25%-0.5% solution). Epidural: 50 to 100 mg (0.25%-0.75% solution); children: 1.5 to 2.5 mg/kg (0.25%-0.5% solution). Caudal: 37.5 to 150 mg (15-30 mL of 0.25% or 0.5% solution); children: 0.4 to 0.7 mL/kg. Spinal bolus/infusion: 7 to 17 mg (0.75% solution); children: 0.5 mg/kg with minimum of 1 mg. Do not exceed 400 mg in 24 hours (maximum single dose, 175 mg).

Onset and duration: Onset: infiltration: 2 to 10 minutes. Epidural: 4 to 7 minutes. Spinal: less than 1 minute. Peak effect: infiltration and epidural: 30 to 45 minutes. Spinal: 15 minutes. Duration: infiltration, spinal, epidural: 200 to 400 minutes (prolonged with epinephrine).

Adverse effects: Hypotension, arrhythmias, cardiac arrest, respiratory impairment or arrest, seizures, tinnitus, blurred vision, urticaria, anaphylactoid symptoms; high spinal: urinary retention, lower extremity weakness and paralysis, loss of sphincter control, backache, palsies, slowing of labor

Precautions and contraindications: Use bupivacaine with caution in patients with hypovolemia, severe congestive heart failure, shock, and all forms of heart block. It is not recommended for obstetric paracervical block or in concentrations higher than 0.5% because of the incidence of intractable cardiac arrest. It is contraindicated in patients with hypersensitivity to amide-type local anesthetics.

Anesthetic considerations: Intravenous access is essential during major regional block. Toxic plasma levels of bupivacaine may cause cardiopulmonary collapse and seizures.

Chloroprocaine HCL (nesacaine)

Classification: Ester-type local anesthetic

Indications: Regional anesthesia; local anesthesia, including infiltration, epidural (including caudal), peripheral nerve block, sympathetic nerve block

Dose: Infiltration and peripheral nerve block: less than 40 mL (1%-2% solution). Epidural: bolus 10 to 25 mL (2%-3% solution), approximately 1.5 to 2 mL for each segment to be anesthetized. Repeat doses at 40- to 60-minute intervals. Infusion: 30 mL/hr (0.5% solution). Caudal: 10 to 25 mL (2%-3% solution); children: 0.4 to 0.7 mL/kg (L2-T10 level of anesthesia). Repeat doses at 40- to 60-minute intervals.

Onset and duration: Rate of onset and potency of local anesthetic action may be enhanced by carbonation. Onset: infiltration or epidural: 6 to 12 minutes. Peak effect: infiltration or epidural: 10 to 20 minutes. Duration: infiltration or epidural: 30 to 60 minutes (prolonged with epinephrine).

Adverse effects: Hypotension, arrhythmias, bradycardia, respiratory depression or arrest, seizures, tinnitus, tremors, urticaria, pruritus, angioneurotic edema; high spinal: backache; loss of perianal sensation and sexual function; permanent motor, sensory, autonomic (sphincter control) deficit in lower segments; slowing of labor

Precautions and contraindications: Use with caution in patients with severe disturbances of cardiac rhythm, shock, heart block, or impaired hepatic function. Inflammation or infection may occur at the injection site. Elderly and pregnant patients are most at risk. It is contraindicated in patients with hypersensitivity to ester-type local anesthetics and to para-aminobenzoic acid or parabens. Do not use for spinal anesthesia.

Anesthetic considerations: Reduce doses in obstetric, elderly, hypovolemic, and high-risk surgical patients and in those with increased intraabdominal pressure.

Cimetidine (tagamet)

Classification: Histamine (H₂) antagonist

Indications: Treatment of duodenal or gastric ulcers, gastroesophageal reflux disease; prophylaxis of aspiration pneumonitis in patients at high risk during surgery

Dose: Prophylaxis of aspiration pneumonitis: adults: 300 to 400 mg orally 1.5 to 2 hours before induction of anesthesia with or without a similar dose the preceding evening. When a more rapid onset of effect is needed, intravenous: dilute 300 to 400 mg in D₅W or normal saline to a volume of at least 20 mL and inject over a period not less than 5 minutes. A slower infusion, over 15 to 30 minutes, may be preferable owing to association of occasional severe bradycardia and hypotension with rapid infusion. Children younger than 12 years: use not indicated.

Dosage forms: tablets: 300, 400 mg; parenteral injection: 150 mg/mL

Onset and duration: Onset: 15 to 45 minutes. Peak effect: 1 to 2 hours orally. Duration: 2 to 4 hours. Elimination half-life: 2 hours. Plasma cimetidine levels that suppress gastric acid secretion by 50% were maintained 4 to 5 hours after intravenous injection.

Adverse effects: Mental status changes such as delirium, confusion, depression, primarily in elderly patients or those with hepatic or renal impairment; leukopenia, thrombocytopenia, and gynecomastia rarely (1%)

Hypotension and severe bradycardia are associated with rapid intravenous infusion. Serum creatinine and liver enzymes may rise during treatment, although hepatotoxicity and renal dysfunction are usually reversible.

Precautions and contraindications: Caution is suggested in renal or hepatic insufficiency. Microsomal metabolism of many drugs may be inhibited. It is contraindicated in patients allergic to cimetidine or other H₂ antagonists.

Anesthetic considerations: Cimetidine inhibits the hepatic mixed-function oxidase system; therefore, it may prolong the half-life of many drugs, including diazepam, midazolam, metoprolol, propranolol, theophylline, lidocaine, and other amide local anesthetics. Ranitidine may be the drug of choice in patients receiving lidocaine local or regional anesthesia.

Cleviprex (clevidipine)

Classification: Intravenous calcium channel blocker; antihypertensive

Indication: Antihypertensive, when oral drugs are not feasible

Dose: Clevidipine is a milky white lipid emulsion. Titrate to achieve desired blood pressure reduction. Initial dose is 1 to 2 mg/hr. Double the dose every few minutes until blood pressure goals are met. Maintenance doses usually range from 4 to 6 mg/hr. Maximum doses are usually less than 16 mg/hr.

Onset and duration: Onset: 2 to 4 minutes. Duration: 5 to 15 minutes after the infusion is stopped

Adverse effects: Hypotension, tachycardia, negative inotropic effects in heart failure patients

Precautions and contraindications: Contraindicated in patients with allergies to soybeans, soy products, eggs or egg products, defects in lipid metabolism such as pathologic hyperlipemia, lipoid nephrosis, or acute pancreatitis, and patients with severe aortic stenosis

Caution handling the lipid emulsion. Use aseptic technique and discard if not used in 12 hours. Caution in patients on beta-blocker therapy.

Anesthetic considerations: Useful for titration to control blood pressure. Insertion of an arterial line advised to closely monitor pressures. Monitor for rebound hypertension for 8 hours after the infusion is discontinued.

Clonidine (catapres, dixarit); epidural clonidine (catapres, duraclon)

Classification: Central-acting α₂-adrenergic agonist; reduces sympathetic outflow by directly stimulating α₂-receptors in the medulla vasomotor center

Epidural action produces dose-dependent analgesia by preventing pain signal transmission at presynaptic and postjunctional α₂-adrenoreceptors in the spinal cord.

Indications: Hypertension; epidural and spinal anesthesia; symptomatic control of alcohol, opiate, nicotine, and benzodiazepine withdrawal; diagnosis of pheochromocytoma; growth hormone stimulation test; cancer-related pain; Tourette syndrome; attention deficit disorder; migraines.

The use of epidural clonidine in combination with epidural opiate agonists results in a decreased opiate requirement that treats neuropathic pain more effectively than visceral pain.

Dose: Maintenance: 0.2 to 0.6 mg/day orally in two divided doses. Hypertensive emergencies: 0.15 mg intravenously over 5 minutes. Transdermal patch: every 7 days (maximum dose: 0.6 mg/day). The same doses are used in renal impairment.

Epidural: must be preservative free. Postoperative pain: epidural clonidine combined with an opiate analgesic: 30 mcg/hr if added to fentanyl. Neuropathic pain: continuous epidural infusion combined with an opiate analgesic is 30 mcg/hr.

All dosages must be titrated to pain relief and the incidence of side effects.

The recommended starting dose of epidural clonidine HCl for continuous epidural infusion is 30 mcg/hr. Although dosage may be titrated up or down, depending on pain relief and occurrence of adverse events, experience with dosage rates above 40 mcg/hr is limited.

Familiarization with the continuous epidural infusion device is essential. Patients receiving epidural clonidine from a continuous infusion device should be closely monitored for the first few days to assess their response.

The 500 mcg/mL (0.5 mg/mL) strength product must be diluted before use in 0.9% sodium chloride for injection to a final concentration of 100 mcg/mL.

Onset and duration: Onset: intravenous or oral: 30 to 60 minutes. Peak effect: 2 to 4 hours. May take too long for a true hypertensive crisis. Duration: antihypertensive: 6 to 10 hours, dose dependent.

Adverse effects: Rebound hypertension, atrioventricular block, bradycardia, congestive heart failure, orthostatic hypotension, sedation, nightmares, constipation, dry mouth, pruritus, urinary retention, contact dermatitis

The most common noncardiovascular adverse reactions to epidural clonidine include anxiety, asthenia, chest pain, confusion, diaphoresis, dizziness, drowsiness, dyspnea, fever, nausea or vomiting, and xerostomia.

Precautions and contraindications:

• Avoid in conduction or sinoatrial disorders, hypersensitivity to clonidine, pregnancy, severe renal or hepatic disease. Concomitant administration of tricyclic antidepressants may increase the serum level.

• If the dose is held or when changing to transdermal application, watch for a rapid increase in blood pressure from unopposed α stimulation.

• It crosses the placenta easily and should be discontinued 8 to 12 hours before delivery.

• Epidural clonidine is not recommended for intrathecal administration or as an analgesic during labor and delivery or for postpartum or perioperative analgesia because of the risks of hemodynamic instability.

Anesthetic considerations:

• Severe rebound hypertension may result from abrupt withdrawal, with neurologic sequelae and myocardial infarction. Labetalol has been successfully used in treatment of hypertensive crisis. Continue on the day of surgery.

• Hepatic elimination is 50%.

• Clonidine reduces perioperative requirements of narcotics and volatile agents.

• Female patients and lower weight patients have an increased risk of the hypotensive effects of epidural clonidine (use cautiously in patients with severe cardiac disease or hemodynamic instability). More profound decreases in blood pressure may be seen if the drug is administered into the upper thoracic spinal segments.

Cocaine HCL (cocaine)

Classification: Topical anesthetic and vasoconstrictor, ester-type local anesthetic

Indications: Topical anesthesia and vasoconstriction of mucous membranes (oral, laryngeal, and nasal)

Dose: Topical: 1.5 mg/kg (1%-4% solution). Nasal: 1 to 2 mL each nostril (1%-10% solution). Concentrations greater than 4% increase potential for systemic toxic reactions. Maximum dose: 1.5 mg/kg.

Onset and duration: Onset: less than 1 minute. Peak effect: 2 to 5 minutes. Duration: 30 to 120 minutes. It is rapidly absorbed from all areas of application.

Adverse effects: Seizures, sloughing of nasal mucosa, arrhythmias, tachycardia, hypertension

Precautions and contraindications: Cocaine is for topical use only, not for intraocular or intravenous use. It potentiates other sympathomimetics; therefore, use reduced doses (if any at all) in patients receiving pressors or ketamine. Use it with caution in patients with nasal trauma.

Anesthetic considerations: Hypertension, bradyarrhythmias, tachyarrhythmias, ventricular fibrillation, tachypnea, respiratory failure, euphoria, excitement, seizures, and sloughing of corneal epithelium may occur. Use it with caution in patients with a history of drug sensitivities or drug abuse (high addiction potential) and pregnancy. Prolonged use can cause ischemic damage to nasal mucosa. Cocaine is contraindicated for intraocular or intravenous use. It sensitizes the heart to catecholamines (epinephrine and monoamine oxidase inhibitors may increase cardiac arrhythmias, ventricular fibrillation, hypertensive episodes). It potentiates arrhythmogenic effects of sympathomimetics, and it has a high addiction potential.

Codeine

Classification: Opioid agonist

Indications: Preoperative and postoperative analgesia

Dose: Oral: 15 to 60 mg every 4 hours; intramuscular or subcutaneous: 15 to 60 mg every 4 hours.

Onset and duration: Onset: oral: 30 to 60 minutes; intramuscular or subcutaneous: 20 to 60 minutes. Duration: oral: 2 to 4 hours; intramuscular or subcutaneous: 2 to 3 hours.

Adverse effects: Sedation, clouded sensorium, euphoria, dizziness, seizures with large doses, hypotension, bradycardia, nausea, vomiting, constipation, dry mouth, ileus, urinary retention, pruritus, flushing

Precautions and contraindications: Use codeine with caution in patients with head injury, owing to respiratory depression and resulting increased intracranial pressure; in hepatic or renal disease; hypothyroidism; Addison disease; acute alcoholism; seizures; severe central nervous system depression; bronchial asthma; chronic obstructive pulmonary disease; respiratory depression; and shock. Use it with caution in patients with known hypersensitivity to the drug and in elderly patients. It may produce histamine release.

Anesthetic considerations: General anesthetics, other narcotic analgesics, tranquilizers, sedatives, hypnotics, alcohol, tricyclic antidepressants, or monoamine oxidase inhibitors increase central nervous system depression.

Cyclosporine (sandimmune, others)

Classification: Immunosuppressant

Indications: Prevention of rejection of organ or tissue (kidney, liver, heart) allograft in combination with steroid therapy

Dose: Initial: oral: 15 mg/kg as a single dose 4 to 24 hours before transplantation; continue for 1 to 2 weeks. Taper to maintenance dose: 5 to 10 mg/kg/day. Intravenous: 5 to 6 mg/kg/day as a single dose 4 to 12 hours before transplantation; continue until the patient is able to take oral medication.

Coadministration of a corticosteroid is recommended, as well as possibly azathioprine.

Onset and duration: Onset: 1 to 6 hours (variable). Duration: 1 to 4 days. After oral administration, onset is variable. Elimination half-life: 10 to 27 hours.

Adverse effects: Hypertension, hirsutism, tremor, acne, gum hyperplasia, headache, blurred vision, diarrhea, nausea, paresthesia, mild nephrotoxicity or hepatotoxicity

Precautions and contraindications: History of hypersensitivity to cyclosporine or polyoxyethylated castor oil. Use it with caution in patients with impaired hepatic, renal, cardiac function, or malabsorption syndrome and in those who are pregnant.

Anesthetic considerations: Altered laboratory values may occur. Cyclosporine may elevate blood urea nitrogen, serum creatinine, serum bilirubin, serum glutamic-oxaloacetic transaminase (aspartate aminotransferase), serum glutamic-pyruvic transaminase (alanine aminotransferase), and lactate dehydrogenase. It may prolong the duration of neuromuscular blockade by nondepolarizing muscle relaxants.

Dantrolene sodium (dantrium)

Classification: Skeletal muscle relaxant

Indications: Treatment of malignant hyperthermia (MHT); prophylaxis of MHT in patients with a family history; control of spasticity secondary to multiple sclerosis, spinal cord injury, cerebral palsy, or stroke

Dose: Adults: MHT: 1 mg/kg rapid intravenous bolus; repeat every 5 to 10 minutes until symptoms are controlled; the dose may be repeated to a cumulative dose of 10 mg/kg; oral doses of 4 to 8 mg/kg/day for 1 to 3 days may be administered in three or four divided doses to prevent recurrence of the manifestations. Prophylaxis of MHT: 2.5 mg/kg intravenous bolus 10 to 30 minutes preinduction; then 1.25 mg/kg intravenous bolus 6 hours later.

Dosage forms: capsules: 25, 50, 100 mg; parenteral injection: 20 mg. Administration: reconstitute by adding 60 mL of preservative-free sterile water for injection to each 20-mg vial and shake the vial until clear. Avoid diluent that contains a bacteriostatic agent. Protect from light and use within 6 hours. For direct intravenous injection. Avoid extravasation.

Onset and duration: Effective blood concentrations: 100 to 600 ng/mL. Intravenous blood concentrations of the drug remain at approximately steady-state levels for 3 or more hours after infusion is completed. Mean half-life: 5 to 9 hours. Onset: oral: 1 to 2 hours; intravenous: less than 5 minutes. Duration: 8 to 12 hours.

Adverse effects:

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Handbook of Anesthesia 5e