Exploring Buccal Prochlorperazine: A Targeted Review of Its Pharmacological Profile
The Clinical Value of Buccal Prochlorperazine
Prochlorperazine remains a clinically valuable agent for managing nausea, dizziness, vertigo, and vestibular migraine. (1) However, oral administration is often limited by variable absorption, significant first-pass metabolism, and poor tolerability in symptomatic patients. With such clinical needs, buccal delivery serves as a relevant treatment option with potential advantages in pharmacokinetic reliability and ease of use, particularly in ENT and neurology settings. (2)
Buccal Mucosa as a Drug Delivery Site: Physiology and Practical Use:
The buccal mucosa provides a highly vascularized, enzymatically stable surface that supports sustained drug absorption while bypassing first-pass metabolism. (4) Compared to sublingual delivery, the buccal mucosa covers a larger surface area (23% of oral mucosa) and is better suited for systemic drug delivery, allowing longer mucosal contact and more consistent plasma levels. (4) Buccal tablets are required to ideally be placed high between the upper gum and cheek, left undisturbed for 1–2 hours, with patients advised to avoid eating, drinking, or switching sides. (2)
Pharmacokinetics of Buccal vs Oral and IV Prochlorperazine
Buccal prochlorperazine demonstrates superior pharmacokinetics to oral swallowed tablet dosing, with over twice the systemic exposure (AUC₀–∞: 11.3 vs 4.5 ng·h/mL), higher peak plasma levels (0.545 vs 0.26 ng/mL), and reduced interpatient variability. Metabolite exposure, including prochlorperazine sulfoxide, is approximately 50% lower with buccal administration compared to the oral swallowed route. (5) Compared to IV administration, buccal delivery provides comparable symptom relief with fewer adverse effects. (6) A twice-daily buccal regimen offers therapeutic equivalence to oral dosing, a swallowed tablet administered three to four times daily and may serve as a non-invasive alternative to IV therapy in selected clinical settings. (4)
Clinical Applications of Buccal Prochlorperazine Across Indications
Buccal Prochlorperazine- Faster Symptom Control in Vertigo: In a randomized, double-blind trial involving 169 patients with vertigo, buccal prochlorperazine (3 mg twice daily) was compared to oral prochlorperazine (5 mg three times daily) swallowed tablet over seven days. The buccal form showed a significantly faster onset of relief within a few hours (p=0.004), with over half (56%) of patients improving within a few hours, versus 40% in the oral group. At 24–36 hours, buccal prochlorperazine significantly reduced nausea frequency (p=0.02) and vomiting severity (p = 0.05). Buccal prochlorperazine offers faster relief and better control of nausea and vomiting than oral forms, with improved tolerability, making it a preferred option for rapid symptom relief in vestibular disorders. (7)
Buccal Prochlorperazine Better Tolerability Than Oral Metoclopramide Post-Surgery Nausea & Vomiting: In a study including 50 post-cholecystectomy patients, buccal prochlorperazine (3 mg) led to faster relief (15–60 min vs 30–60 min) than oral swallowed metoclopramide, and better tolerability than oral metoclopramide. About 72% of the patients found it very easy to use, 68% had no mucosal irritation, and no patients had vomiting recurrence. (8)
Buccal Prochlorperazine in Headache: Comparison with Oral Ergotamine-Caffeine: In a randomized trial of 114 migraine episodes, 3 mg buccal prochlorperazine achieved headache relief within 2 hours in 59.5% of cases, significantly outperforming oral ergotamine-caffeine swallowed tablet and placebo (22–28%). Over 50% patients had complete relief by 60 minutes (p < 0.001), with superior control of nausea, photophobia, and phonophobia. (9)
Why Buccal Prochlorperazine Deserves Broader Use?
Buccal prochlorperazine offers practical benefits beyond pharmacokinetics. Its ease of administration and non-invasive delivery (unlike parenteral forms) improve compliance in nauseated, elderly, or motion-sensitive patients. In outpatient and acute care settings, it provides a convenient alternative where IV access is impractical or oral swallow tablet absorption may be unpredictable or less unreliable. Given its favorable tolerability profile and rapid symptom control, buccal prochlorperazine holds unique value in clinical practice. (5,6,7,8)
Key Takeaway
- Buccal prochlorperazine offers superior pharmacokinetics compared to oral formulations, with over 2× systemic exposure, higher peak plasma levels, and reduced interpatient variability, while avoiding first-pass metabolism.
- Clinical trials demonstrate its rapid, effective symptom control across vertigo, vestibular migraine, and post-operative nausea and vomiting, with good tolerability.
- Its ease of administration makes it particularly suitable for nauseated, outpatient, or elderly patients.
- Buccal prochlorperazine deserves broader clinical adoption in clinical practice settings, offering a patient-friendly, efficient solution for acute symptom management in managing nausea, vomiting, dizziness, vertigo, and vestibular migraine.
References:
1. Ilambarathi, M., A. Yeolekar, D. Roy, S. Saxena, and S. Kumar. “A Prospective, Multicenter Study to Evaluate the Effectiveness and Safety of Prochlorperazine in Patients Suffering from Vestibular Migraine”. International Journal of Otorhinolaryngology and Head and Neck Surgery, vol. 10, no. 3, Apr. 2024, pp. 258-64, doi:10.18203/issn.2454-5929.ijohns20240950.
2. Ward AE. Studies of prochlorperazine as a buccal tablet (Buccastem) and an oral tablet (Stemetil) for the treatment of dizziness, nausea or vomiting in a general practice setting. Br J Clin Pract. 1988;42(6):228-232.
3. Chapter 15 - Buccal and sublingual drug delivery systems,Editor(s): Kevin Ita,Drug Delivery,Academic Press,2025, Pages 323-359,ISBN 9780443267871,https://doi.org/10.1016/B978-0-443-26787-1.00015-1.
4. Teubl, Birgit J et al. “The oral cavity as a biological barrier system: design of an advanced buccal in vitro permeability model.” European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V vol. 84,2 (2013): 386-93. doi:10.1016/j.ejpb.2012.10.021
5. Finn A, Collins J, Voyksner R, Lindley C. Bioavailability and metabolism of prochlorperazine administered via the buccal and oral delivery route. J Clin Pharmacol. 2005;45(12):1383–1390. doi:10.1177/0091270005281044
6. Fernando, Tasha et al. “Buccally absorbed vs intravenous prochlorperazine for treatment of migraines headaches.” Acta neurologica Scandinavica vol. 140,1 (2019): 72-77. doi:10.1111/ane.13104
7. Bond CM. Comparison of Buccal and Oral Prochlorperazine in the Treatment of Dizziness Associated with Nausea and/or Vomiting. Curr Med Res Opin. 1998;14(4):203-212. DOI: 10.1185/03007999809113360
8. Singh S, Sharma DR, Chaudhary A. Evaluation of prochlorperazine buccal tablets (Bukatel) and metoclopramide oral tablets in the treatment of acute emesis. Journal of the Indian Medical Association. 1999;97(8):346–347.
9. Sharma S, Prasad A, Nehru R, Anand KS, Rishi RK, Chaturvedi S, Bapna JS, Sharma DR. Efficacy and Tolerability of Prochlorperazine Buccal Tablets in Treatment of Acute Migraine. Headache. 2002 Oct;42(9):896–902. doi:10.1046/j.1526-4610.2002.02177.x
Abbreviations: ENT – Ear, Nose, and Throat, IV – Intravenous, AUC₀–∞ – Area Under the Curve from time zero to infinity (drug exposure over time), Cmax – Maximum concentration of the drug in blood
