Abstract

Background
Ever since the days of Hippocrates, medications have been administered through the rectum. This Fast Fact introduces the use of rectal medications for patients in palliative care settings.
Indications and Benefits
Contraindications and Cautions
The rectal route should be avoided in patients with neutropenia, thrombocytopenia, diarrhea, anorectal disease (e.g., perianal abscess and fistulas), and prior abdominoperineal resection. Giving drugs rectally may cause local irritation, producing an inconvenient and uncomfortable sensation of the need to defecate. Serious complications, usually associated with prolonged use of ergotamine, acetylsalicylic acid, and acetaminophen, are rectal ulceration, necrosis, and stenosis. Suppositories are radiopaque and may be mistaken for contrast material or bladder or kidney stones. Some patients and caregivers find rectal administration objectionable.
Drug Considerations
1. The bioavailability of drugs given rectally is influenced by the site of insertion. First-pass metabolism is avoided in the lower part of the rectum drained by the middle and inferior rectal veins which return to the inferior vena cava. The upper rectum, on the other hand, is drained by the superior rectal vein which empties into the portal system and subsequently into the liver. It is, however, difficult to predict how much of the drug will enter the portal circulation due to extensive anastomoses between the rectal veins. Therefore, drugs administered through the rectum, especially opioids, are dosed as when given orally.
2. Any pill can be given rectally. A specially formulated suppository merely assists in its retention and is not required for efficacy. There are a limited number of commercially available drugs specifically manufactured for rectal administration. If consistent use is necessary, almost any medication can be compounded into custom-made suppositories, gelatin-capsule-encased oral medications, or microenemas of oral elixirs. Pertinent drugs that have acceptable rectal bioavailabilities are listed in Table 1; those marked with an asterisk (*) are commercially available as a suppository or enema in the United States.
Guides to Using the Rectal Route
1. Rectum should be emptied prior to insertion, as stool interferes with drug absorption.
2. Insert the drug about a finger's length into the rectum and place against the rectal wall.
3. Tolerance is the same whether the suppository's apex or base is inserted first, but retention is superior when the base (blunt end) is inserted first. The lower edge of the external sphincter contracts along the edge of the apex and forces the suppository upwards, facilitating retention.
4. 10 ml warm water can be inserted via syringe to assist dissolution of the suppository or suspension.
5. Keep volume of drug preparation less than 60 ml to avoid spontaneous expulsion before absorption.
Bottom Line
The rectal route is an efficient and practical alternative in administering a broad array of palliative care medications to patients with a compromised oral route.
