Therapeutic

Class Medication

Mechanism of

Action Metabolism

Route of

Administration

(neonates) Dose and Frequency Reversal

Agent Comments

α-adrenergic agonist analgesics Clonidine Stimulates alpha-2- adrenoreceptors

in locus ceruleus, ↓s presynaptic calcium,

inhibits NE

release from

sympathetic

nerve endings

reducing sympathetic outflow.

(Useful in managing opioid

withdrawal—

activates K+

channel via G

inhibitory protein as opioids.)

Hepatic: Primarily

hydroxylation, via

CYP2D6.

Onset of action:

Oral: 30–60 min

IV

Oral,

IV

Oral:

1 mcg/kg/dose

q4–6h

Maximum:

6 mcg/kg/dose

IV infusion:

0.5 mcg/kg/h increasing to

maximum:

3 mcg/kg/h

None:

Discontinue

Infusion/dose,

Support respiration, cardiac

function,

Correct BP

Attenuates adrenergic hyperactivity;

somatic and autonomic signs of

withdrawal.

Consider as adjunct for infants with persistent and severe signs of withdrawal

(i.e., long-term continuous opioid/

benzodiazepine IV infusions).

Hold doses for SBP <50 mm Hg or HR

<100 bpm.

Do not confuse with clonazepam

(Klonopin).

Has been used for treating opioid

induced myoclonus in

neonates.

Dexmedetomidine Hypnotic, analgesic, sympatholytic.

↓ sympathetic

response to pain;

Selectively stimulates dorsal horn

of spinal cord α2-

adrenergic receptors; produces

sedation via α1-

effects in locus

ceruleus, preserving spontaneous

ventilation.

↑ intraoperative

hemodynamic

stability.

Hepatic:

Primarily by

CYP2A6 then

N-glucuronidation

and N-methylation.

Clearance in newborn

≈30% of adult, ↑ to

adults rates by

12 months of age.l

IV, IM

(preservativefree solution)

100 mcg/mL

(2 mL)

IV: 1 mcg/kg initial then

0.5 mcg/kgl

Most adverse effects

respond to:

DC infusion or

↓ rate.

Treat bradycardia:

atropine; hypotension; ↑ IVF or

start vasopressor,

Hypertension

during load dose:

↓ rate.

Additive analgesic effect with ketamine,

fentanyl.

Sevoflurane for surgical procedures.

Control of withdrawal with prolonged

opioid use.

Sedation during mechanical ventilation.

Monitor pain scores; may cause significant ↓ body temperaturel

Avoid abrupt discontinuation—rapid

awakening, anxiety, “fighting” ventilator, and withdrawal.

↓ dose in hepatic insufficiency

Not labeled for use for <18 y

General

anesthetics

Ketamine Direct action on

cortex and limbic system to

produce dissociative anaesthesia.

Blocks D-2 dopamine receptor.

Noncompetitive

agonist of

NMDA.

No effect on pharyngeal or laryngeal reflexes.m

Hepatic:

N-dealkylation

hydroxylation, glucuronide conjugation,

dehydration of hydroxylated metabolites

IV IV: 0.5–2 mg/kg

Induction dose:

1–2 mg/kg

Continuous IV infusion

(sedation):

5–20 mcg/kg/min

Titrate to desired level.m

None

Discontinue infusion,

Support respiration, cardiac

function,

Emergence

reactions (pediatrics < adults)m

Provides sedation, analgesia, amnesia.

Caution in GERD: ↑ vomiting, will

↑ ICP, not adequate as sole anesthetic

for surgical procedures of pharynx,

larynx, bronchial tree or visceral pain

pathways.

Premedicate with IV atropine dose

secondary to increased production

of upper respiratory and salivary

secretions.

Limited neonatal use due to potential

↑ ICP and neurotoxicity.m

Long-term effects are unknown

Potential neuroprotective effects in

animal models.

Sedation in mechanically ventilated neonates, especially during suctioning.

(continued )