Not Approved (US) Cardiovascular & Renal

Felypressin

also known as: Octapressin, PLV-2, 2-phenylalanine-8-lysine-vasopressin

⚠ Not FDA-approved. The dental-anaesthetic alternative to epinephrine — used in Europe, Japan, and Brazil as a non-catecholamine vasoconstrictor in prilocaine-based dental cartridges (Citanest® Octapressin). Useful where cardiac patients need dental work but epinephrine poses risk; unfamiliar to US dentists because of non-approval.

A synthetic nonapeptide vasopressin analog with phenylalanine at position 2 and lysine at position 8, developed by Sandoz (Novartis precursor) in the 1950s and marketed as a dental-anaesthetic vasoconstrictor — predominantly as Citanest® with Octapressin® (prilocaine 3% + felypressin 0.03 IU/mL) by DENTSPLY. Primary pharmacologic feature: selective V1a-receptor-mediated vasoconstriction without catecholamine activity, meaning it avoids epinephrine-associated cardiovascular reactions (tachycardia, arrhythmias, hypertensive episodes) in susceptible patients. Not FDA-approved in the US; standard US dental anaesthetic cartridges use lidocaine or articaine with epinephrine. Approved and widely used in the UK, Germany, Japan, Brazil, Australia, and other markets for dental local anaesthesia, particularly in cardiovascular-risk patients.

Mechanism of action

Selective V1a vasopressin receptor agonist — the phenylalanine-2 and lysine-8 substitutions of felypressin retain V1a binding and vasoconstrictor activity while minimising V2 antidiuretic activity. Local injection into oral tissues produces vasoconstriction in the submucosal microvasculature (V1a on arteriolar smooth muscle), reducing bleeding at the surgical site and prolonging the duration of the co-administered local anaesthetic by slowing its washout. Unlike epinephrine, felypressin does not engage β1 cardiac adrenergic receptors and therefore avoids direct positive-chronotropic and positive-inotropic effects — a safety advantage in patients with arrhythmia history, uncontrolled hypertension, or catecholamine-sensitive cardiovascular disease. Potential concerns include coronary artery vasoconstriction at higher doses (V1a-mediated), which makes it still relatively contraindicated in severe coronary artery disease. Uterine V1a receptors are also engaged, so felypressin is avoided in obstetric patients.

Primary uses

  • Dental local anaesthesia (vasoconstrictor component of prilocaine-felypressin cartridges) — international approvals
  • Cardiovascular-risk patients requiring dental procedures where epinephrine is contraindicated

Typical dosing

0.03 IU/mL (in local-anaesthetic cartridge) IU per dental cartridge (1.8 mL) single local injection per site (local submucosal injection (dental))

⚠ Not FDA-approved in the US. Used as a vasoconstrictor component in prilocaine-felypressin dental cartridges. Relatively contraindicated in obstetric patients (V1a uterine activity) and in severe coronary artery disease (coronary V1a vasoconstriction). Maximum of approximately 8 cartridges per appointment for adult patients.

Regulatory status

Not FDA-approved in the United States. Approved in the United Kingdom, Germany, Japan, Brazil, Australia, Scandinavia, and other markets for dental local anaesthesia as a vasoconstrictor component. Typical formulation: prilocaine 3% + felypressin 0.03 IU/mL (Citanest® Octapressin, DENTSPLY / Septodont depending on region).

References

  1. [review] Malamed SF. "Handbook of Local Anesthesia, 7th ed." Elsevier, 2019 (felypressin chapter on dental vasoconstrictors).
  2. [pubmed] Sunada K, Nakamura K, Yamashiro M, et al. "Clinically safe dosage of felypressin for patients with essential hypertension." Anesth Prog, 1996;43(4):108-115.
  3. [review] Jastak JT, Yagiela JA. "Vasoconstrictors and local anesthesia: a review and rationale for use." J Am Dent Assoc, 1983;107(4):623-630.

Related peptides

Vasopressin

Vasostrict — the endogenous antidiuretic hormone as an ICU vasopressor. FDA-approved April 2014 for adults with vasodilatory shock (post-cardiotomy, sepsis) who remain hypotensive despite fluids and catecholamines. Works through V1a receptors on vascular smooth muscle — a receptor axis pharmacologically distinct from catecholamine receptors, preserving its vasopressor effect when adrenergic receptors are desensitised.

Terlipressin

Terlivaz — the first and only FDA-approved drug for hepatorenal syndrome (HRS). FDA-approved September 2022 (Mallinckrodt) for adults with HRS with rapid reduction in kidney function, after a multi-decade regulatory history including four prior Complete Response Letters and the successful CONFIRM Phase 3 trial (NEJM 2021).

Desmopressin

DDAVP — the classic V2-selective vasopressin analog. FDA-approved February 1978 for central diabetes insipidus; decades of label expansion added primary nocturnal enuresis, nocturia (Noctiva / Nocdurna), and hemostatic use in mild hemophilia A and type 1 von Willebrand disease. WHO Essential Medicines List.
Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.