Emergency drug in

anesthesia
Neostigmine

• Mechanism of action: Acetylcholinesterase inhibitor.

• Dosage: Up to 0.08 mg/kg in children; 5 mg in adults.
• Onset: Effects apparent in 5 to 10 minutes; peak at 10 minutes and last more than 1 hour.
• Clinical note: Typically administered with glycopyrrolate to prevent bradycardia.
• Structure: Carbamate moiety (binds to acetylcholinesterase) and quaternary ammonium group (prevents
passage across the BBB).
Sugammadex

• Mechanism of action: Hydrophobic structural interactions trap aminosteroid neuromuscular blocking agents
(rocuronium, vecuronium) within cyclodextrin cavity, terminating neuromuscular block.
• Dosage: 4 to 8 mg/kg.
• Onset: Can reverse shallow and deep neuromuscular blockade within 2 minutes.
• Clinical note: Because of concerns about hypersensitivity and allergic reactions, not yet approved by the U.S.
Food and Drug Administration. Currently is available and used in Europe.
• Structure: Modified cyclodextrin.
Cholinergic Pharmacology
Side effects of acetylcholinesterase inhibitors: In addition to increasing the availability of acetylcholine at the
neuromuscular junction, inhibition of acetylcholinesterase can increase cholinergic receptor activity elsewhere,
leading to side effects.
• Cardiovascular system: The predominant muscarinic effect on the heart is a vagal-like bradycardia that can
progress to sinus arrest.
• Pulmonary receptors: Muscarinic stimulation can result in bronchospasm and increased respiratory
secretions.
• Cerebral receptors: Physostigmine is a cholinesterase inhibitor that can cross the blood–brain barrier (BBB).
It can cause diffuse activation of the electroencephalogram by stimulating muscarinic and nicotinic receptors
within the central nervous system (CNS).
• Gastrointestinal receptors: Muscarinic stimulation increases peristaltic activity (esophageal, gastric, and
intestinal) and glandular secretions (e.g., salivary, parietal). Perioperative bowel anastomotic leakage, nausea
and vomiting, and fecal incontinence have been attributed to the use of cholinesterase inhibitors.
Atropine

• Dosage
• Premedication (antisialagogue effect): intravenous (IV) or intramuscular (IM) 0.01 to 0.02 mg/kg up to the usual
adult dose of 0.4 to 0.6 mg
• Severe bradycardia: Larger IV doses up to 2 mg may be required
• Clinical Considerations
• Most efficacious anticholinergic for bradyarrhythmias
• Patients with coronary artery disease may not tolerate the increased myocardial oxygen demand or decreased oxygen
supply associated with atropine-induced tachycardia
• Ipratropium bromide solution (0.5 mg in 2.5 mL) is a derivative of atropine; metered-dose inhibitor treatment of
bronchospasm; particularly effective in acute COPD when combined with a β-agonist (i.e., albuterol)
• Rapidly crosses the BBB; central nervous system (CNS) effects are minimal at usual doses, although toxic doses are
typically associated with excitatory reactions
• Associated with mild postoperative memory deficits
• Cautious use in narrow-angle glaucoma, prostatic hypertrophy, and bladder-neck obstruction
Adrenergic Agonists & Antagonists

• Adrenergic agonists can be categorized as direct or indirect. Direct agonists bind to the receptor, whereas
indirect agonists increase endogenous neurotransmitter activity.
• primary effect of phenylephrine is peripheral vasoconstriction with a concomitant rise in systemic vascular
resistance and arterial blood pressure
• Clonidine decreases anesthetic and analgesic requirements and provides sedation and anxiolysis.
• Dexmedetomidine has a greater affinity for α2-receptors than clonidine. It has sedative, analgesic, and
sympatholytic effects that blunt many of the cardiovascular responses seen during the perioperative period
• Ephedrine is commonly used as a vasopressor during anesthesia. As such, its administration should be viewed
as a temporizing measure while the cause of hypotension is determined and remedied
• At low doses (0.5–3 mcg/kg/min), dopamine (DA) primarily activates dopaminergic receptors. Stimulation of
these receptors (specifically, DA1 receptors) vasodilates the renal vasculature and promotes diuresis.
• Labetalol lowers blood pressure without reflex tachycardia because of its combination of α and β effects.
• Esmolol is an ultrashort-acting selective β1-antagonist that reduces heart rate and, to a lesser extent, blood
pressure.
PHENYLEPHRINE

• noncatecholamine with selective α1-agonist activity

• peripheral vasoconstriction with a concomitant rise in systemic vascular resistance and arterial blood pressure
• Reflex bradycardia mediated by the vagus nerve can reduce cardiac output
• also used topically as a decongestant and a mydriatic agent.
• Small intravenous boluses of 50 to 100 mcg (0.5 to 1 mcg/kg) of phenylephrine rapidly reverse reductions in
blood pressure caused by peripheral vasodilation (eg, spinal anesthesia) in adults
• duration of action is short, lasting approximately 15min
• Tachyphylaxis may occur with phenylephrine infusions and require upward titration of the infusion.
• Phenylephrine must be diluted from a 1% solution (10 mg/1-mL ampule), usually to a 100 mcg/mL solution
and titrated to effect.
16
 Flumazenil
– A competitive antagonist at the
benzodiazepine binding site of
GABAA receptors in the CNS.
– Reversal of sedative effects occurs within 2 min; peak
effects at 10 min.
– Half-life is shorter than the benzodiazepine
– Metabolized to inactive metabolites in the liver.
– Dose. 0.3 mg IV every 30 to 60 seconds (to a maximum
dose of 5 mg).
– Initial dose in pediatric: 0.01 mg/kg IV over 15 seconds
– Contraindicated in patients receiving benzodiazepines
for the control of seizures or elevated ICP.
17
Dextrose
• Use in hypoglycemia patient
• < 80 mg/dL with symptom
• <60 mg/dl without symptom
• neonate?
• Available at ampule 1mg/ml
• In cpr give 1 mg every 3-5 minute rapid bolus