Rectal Drug Delivery Route

Aka: Rectal Drug Delivery Route, Rectal Medication Route, Rectal Route of Medication Delivery, Per Rectum Medication

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II. Indications

  1. Patient unable to take medication by oral or Parenteral Route

III. Contraindications

  1. Rectal lesions
  2. Significant Diarrhea
  3. Neutropenia
  4. Large stool burden or Fecal Impaction
  5. Timed release medications
  6. Enteric coated medications
  7. Medications known to cause Esophagitis (similar risk to rectal mucosa)
  8. Oral Antibiotics
    1. Altered Pharmacokinetics by rectal route

IV. Mechanism

  1. Many medications are well absorbed systemically by the rectal mucosa
  2. Distal rectal medications avoid first pass metabolism
    1. Distal middle and inferior Rectal Veins drain directly into the inferior vena cava
  3. Pitfalls
    1. Some medications have variable or erratic rectal absorption
    2. Altered bowel function may limit rectal use (profuse Diarrhea, stool impaction)
    3. Distal rectal mucosa has limited surface area for absorption

V. Medications: Locally Active Medications

  1. Laxatives
    1. Bisacodyl Suppository
    2. Glycerin Suppository
    3. Fleet Enema
  2. Inflammatory Bowel Disease
    1. Mesalamine suppository
    2. Rectal Budesonide
  3. Hemorrhoid Management
    1. Topical Corticosteroids
  4. Anal Fissures
    1. Rectal Nitroglycerin

VI. Medications: Systemically Active Medications

  1. Analgesics
    1. Acetaminophen suppository
    2. Aspirin suppository
    3. Ibuprofen suppository
    4. Diclofenac suppository
    5. Indomethacin suppository
    6. Oxycodone Suppository
    7. Morphine Suppository
  2. Antiemetics
    1. Ondansetron Suppository
    2. Prochlorperazine Suppository
    3. Promethazine Suppository
    4. Metoclopramide Suppository
  3. Benzodiazepines (e.g. Status Epilepticus)
    1. Rectal Diazepam (gel, enema)
  4. Migraine Medications
    1. Caffeine and Ergotamine Suppository
    2. Sumatriptan suppository

VII. Medications: Oral Formulations Given Rectally

  1. Some oral medications may be crushed and delivered rectally
    1. Do NOT give timed release medications rectally
    2. Do NOT give enteric coated medications rectally
    3. Do NOT give medications rectally that are known to cause Esophagitis
    4. Do NOT give oral Antibiotics rectally (altered Pharmacokinetics, exceptions may exist)
  2. Example medications
    1. Antiplatelet agents (Aspirin, Clopidogrel, Ticagrelor)
    2. Consult pharmacist on oral medications that may be given by rectal route
  3. Rectal administration
    1. Crush oral tablet and mix with 10-20 ml water
    2. Instill solution into Rectum via angiocatheter or commercial device

VIII. References

  1. Swaminathan and Fisher (2025) EM:Rap, 7/21/2025
  2. Hua (2019) Front Pharmacol 10:1196 +PMID: 31680970 [PubMed]

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