NAV

Felypressin

Identification

Generic Name
Felypressin
DrugBank Accession Number
DB00093
Background

A synthetic nonapeptide comprising cysteinyl, phenylalanyl, phenylalanyl, glutaminyl, asparaginyl, cysteinyl, prolyl, lysyl, and glycinamide residues in sequence, with a disulfide bridge joining the two cysteine residues. Its antidiuretic effects are less than those of vasopressin. It is a non-catecholamine vasoconstrictor used in local anaesthetic injections for dental use, and is an ingredient of preparations that have been used for treatment of pain and inflammation of the mouth.

Type
Biotech
Groups
Experimental
Biologic Classification
Protein Based Therapies
Peptides
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • 2-(L-phenylalanine)-8-L-lysinevasopressin
  • Felipresina
  • Felypressin
  • Felypressine
  • Felypressinum
  • PLV-2

Pharmacology

Indication

For use as an alternative to adrenaline as a localising agent, provided that local ischaemia is not essential.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Felypressin is a synthetic analog of lypressin or vasopressin with a greater vasoconstrictor activity than antidiuretic action. It is used primarily as a hemostatic.

Mechanism of action

Felypressin binds to the vasopressin receptor V1a. This causes contraction of the smooth muscle in the vascular bed, especially capillaries, small arterioles and venules.

TargetActionsOrganism
AVasopressin V1a receptor
agonist
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
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interactions in your software
ChloroprocaineThe risk or severity of adverse effects can be increased when Felypressin is combined with Chloroprocaine.
LevothyroxineLevothyroxine may increase the vasoconstricting activities of Felypressin.
LidocaineThe risk or severity of hypertension can be increased when Felypressin is combined with Lidocaine.
LiothyronineLiothyronine may increase the vasoconstricting activities of Felypressin.
LiotrixLiotrix may increase the vasoconstricting activities of Felypressin.
OxytocinThe risk or severity of hypertension can be increased when Felypressin is combined with Oxytocin.
Patent BlueThe risk or severity of hypotension can be increased when Patent Blue is combined with Felypressin.
Thyroid, porcineThyroid, porcine may increase the vasoconstricting activities of Felypressin.
Thyrotropin alfaThyrotropin alfa may increase the vasoconstricting activities of Felypressin.
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Food Interactions
Not Available

Products

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International/Other Brands
Colupressine (Joullie) / Octapressin (Sandoz)
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
CITANEST OCTAPRESSIN INJECTIONFelypressin (0.066 iu/2.2ml) + Prilocaine hydrochloride (66 mg/2.2ml)InjectionBuccalDENTSPLY (SINGAPORE) PTE. LTD.1991-03-05Not applicable

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
17N2918V6G
CAS number
56-59-7

References

Synthesis Reference

Boissonnas, R.and Guttmann, S.; U.S. Patent 3,232,923; February 1, 1966: assigned to Sandoz AG, Switzerland.

General References
  1. Cecanho R, De Luca LA Jr, Ranali J: Cardiovascular effects of felypressin. Anesth Prog. 2006 Winter;53(4):119-25. [Article]
PubChem Compound
14257662
PubChem Substance
46507522
ChemSpider
16736539
RxNav
4319
ChEBI
60564
ChEMBL
CHEMBL3185126
Therapeutic Targets Database
DAP000217
PharmGKB
PA164744374
Wikipedia
Felypressin

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentDental Extraction / Maxillary Teeth / Overcoming the Failure of Anaesthesia1

Pharmacoeconomics

Manufacturers
  • Novartis pharmaceuticals corp
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionBuccal
SolutionSubcutaneous
SolutionParenteral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)222Boissonnas, R.and Guttmann, S.; U.S. Patent 3,232,923; February 1, 1966: assigned to Sandoz AG, Switzerland.
hydrophobicity-3.6Not Available

Targets

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Details1. Vasopressin V1a receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Vasopressin receptor activity
Specific Function
Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl-inositol-calcium second messenger system. Has been involved in social behavi...
Gene Name
AVPR1A
Uniprot ID
P37288
Uniprot Name
Vasopressin V1a receptor
Molecular Weight
46799.105 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Manning M, Stoev S, Chini B, Durroux T, Mouillac B, Guillon G: Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. Prog Brain Res. 2008;170:473-512. doi: 10.1016/S0079-6123(08)00437-8. [Article]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Drug created at June 13, 2005 13:24 / Updated at April 07, 2023 13:18