chapter 8 
Rectal Sedation
CHAPTER OUTLINE
ADVANTAGES
DISADVANTAGES
DRUGS
Hydromorphone
Oxymorphone
Promethazine
Chloral Hydrate
I nterest in the rectal route of drug administration has
increased in anesthesiology and, to a lesser extent, in
dentistry in recent years.1–3 Historically the rectal route
of drug administration was used for the administration of
smoke (“fumigation”) for resuscitation4 and the administration
of anesthetics. An ether boiler for rectal application was
developed in 1847 by Pirogoff.1,5 With the advent of more
reliable routes of drug administration (e.g., intravenous [IV]
and inhalation), use of the rectal route decreased.
Certain situations remain in which rectal drug administration
may be valuable. These include the administration of a drug
to a patient who is unwilling or unable to take drugs orally.
In most instances, this is a child or an adult with a disability
requiring sedation either to permit treatment to proceed6–8 or
as a preliminary to the induction of general anesthesia.9–11
Another situation in which rectal drugs are warranted is the
administration of antiemetics to patients with nausea and
vomiting.12 Although parenteral administration is preferred (if
the patient is present in the office where the drug may be
injected), rectal administration can be used if the patient objects
to injection or if the patient is at home. Another indication
for rectal administration of drugs is analgesics for postoperative
control of pain.13
ADVANTAGES
Advantages of the rectal route include a relatively rapid onset
of clinical activity; a decreased incidence and intensity of
drug-related side effects; the lack of a needle, syringe, or other
120
Diazepam
Midazolam
Ketamine
Lytic Cocktail
COMPLICATIONS OF RECTAL
ADMINISTRATION
potentially threatening equipment; the avoidance of an injection;
ease of administration (many children who vehemently object
to the oral route will not object to this route); and its low cost.
In the past, it was thought that rectally administered drugs
were absorbed directly into the systemic circulation via the
vena cava, bypassing the enterohepatic circulation and thereby
eliminating the hepatic first-pass effect that influences the
clinical activity of most drugs administered enterally.14 The
superior rectal vein empties into the inferior mesenteric vein
and then into the portal system. The middle and inferior rectal
veins empty into the internal iliac vein and the inferior vena
cava.15,16 However, it has been demonstrated that hepatic
clearance is the main factor affecting bioavailability of rectally
administered drugs.1 This may be because blood flow occurs
through anastomoses that interconnect the superior, middle,
and inferior rectal venous systems, thereby producing a hepatic
first-pass effect with rectally administered drugs. Other potential
factors, such as adsorption by feces, intraluminal degradation
by microorganisms, metabolism within the mucosal cell, and
lymphatic drainage, do not significantly affect the fate of rectally
administered drugs.
Comparing the oral, nasal, and rectal administration of the
water-soluble benzodiazepine midazolam, Tolksdorf9 found
that children aged 1 to 6 years accepted the oral drug better
than rectal or nasal, but that the rectally administered midazolam
had the most rapid onset of action and fewest side effects in
the postoperative period. In several studies, peak levels of
clinical action were noted rapidly after rectal administration.
Roelofse et al6 noted good anxiolysis, sedation, and cooperation