Primary Sedative - Hypnotic Drugs ("Sleepers")
Drugs used to make children sleep. Particularly effective for procedures requiring a high level of immobility.
Chloral Hydrate
Historically the most widely used hypnotic agent in children, has stood the “test of time.” Generally safe and effective.
Pharmacodynamic Features
Desired Clinical Effects
- Good sedation – hypnosis (similar to barbiturates)
Other Clinical Effects (Isolated Reports of Dealths in Dental Office)
- Respiratory: mild to moderate respiratory depressant effects
- Isolated oxygen desaturations (~5%)
- Bronchiolitis: oxygen desaturations (Pediatr Pulmonol 1988;5:96)
- Obstructive sleep apnea: upper airway obstruction (Pediatrics 1993;92:471)
- Cardiovascular: arrhythmias may occur following high doses or chronic use due to trichloroethanol (TCE) accumulation.
- Other: vomiting, agitation, tastes bad
Pharmacokinetic Features
Chloral hydrate, 2,2,2-trichloroacetaldehyde, is metabolized by the liver by alcohol dehydrogenase (AD) to trichloroethanol, the major active metabolite.
Basics
- Dose:
- 50–75 mg/kg (oral, rectal)
- >75 mg/kg (high dose) (max. 2–2.5 g)
- Repeat dose: 20–25 mg/kg @ 20–25 min
- Induction time: ~15–25 min
- Recovery time: ~60–120 min
- Effectiveness: multifactorial
Clinical Use
Effective for nonpainful procedures requiring sedation or sleep (e.g., EEG, CT, MRI), particularly in children younger than 2 years. Success rates generally >85% for CT and MRI (AJR 1993;161:639, J Pediatr 1996;128:573).
Barbiturates: Potent Sedative, Hypnotic, and Anticonvulsant Drugs
Pharmacodynamic Features
Desired Clinical Effects
- Excellent sedation – hypnosis (dose-related)
Other Clinical Effects
- Respiratory: Despite direct respiratory depressant effects, generally tolerated well in healthy children. Infants most sensitive.
- Cardiovascular: Both negative inotropic and vasodilatory properties; few clinically significant effects in healthy individuals. Hemodynamic effects most pronounced with rapid administration and in hypovolemia.
- Neurologic: ↓ CBF, and ↓ CMRO2, anticonvulsant
- Other: excitatory phenomena such as laryngospasm, agitation<
Pharmacokinetic Features
Substitutions at various positions of the barbituric acid ring confer different physical properties.
Pentobarbital: Most Frequently Used Barbiturate for Pediatric Sedation
Basics: Generally Safe and Effective
- Dose: 2–4 mg/kg (IV)
- Repeat dose: 1–2 mg/kg @ 5–10 min
- Induction time: 1–2 min
- Recovery time: 60 min
- Elimination t 1/2 b = 21–42 hrs
Clinical Use: Very Effective for Non-painful Procedures Requiring High Level of Immobility
(>95% success rate CT and MRI). Oxygen desaturations not uncommon (~5%) (Radiology 1986;161:105, AJNR 1988;9:955).