- Accession Number
- Small Molecule
Allantoin is a substance that is endogenous to the human body and also found as a normal component of human diets [Label]. In healthy human volunteers, the mean plasma concentration of allantoin is about 2-3 mg/l. During exercise, the plasma allantoin concentration rapidly increases about two fold and remains elevated [Label]. In human muscle, urate is oxidized to allantoin during such exercise [Label]. The concentration of allantoin in muscles increases from a resting value of about 5000 ug/kg to about 16000 ug/kg immediately after short-term exhaustive cycling exercise [Label].
More specifically, allantoin is a diureide of glyoxylic acid that is produced from uric acid. It is a major metabolic intermediate in most organisms. Allantoin is found in OTC cosmetic products and other commercial products such as oral hygiene products, in shampoos, lipsticks, anti-acne products, sun care products, and clarifying lotions . Allantoin has also demonstrated to ameliorate the wound healing process in some studies .
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Elta Dermal Gel for Wound Dressing Gel 2 % Topical Swiss American Products Not applicable Not applicable
- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End 12 Hour Healing Ointment 0.5 g/100g Topical Canadian Custom Packaging Company 2017-05-02 2017-11-17 12 Hour Healing Ointment 0.5 g/100g Topical Skinfix, Inc. 2017-05-02 Not applicable 12 Hour Miracle Ointment 0.5 g/100g Topical Skinfix, Inc. 2015-05-23 Not applicable 28 Remedy Aqua Brightening Peeling Gel 0.05 g/100mL Topical NoTS Co.,Ltd 2016-01-02 Not applicable 3ce Fixer and Mascara Black Liquid 0.006 g/6.6g Topical Nanda Co., Ltd. 2016-08-20 Not applicable 3ce Fixer and Mascara Brown Liquid 0.006 g/6.6g Topical Nanda Co., Ltd. 2016-08-20 Not applicable 911 Balm-C Ointment 1 g/100g Topical Skinfix, Inc. 2017-02-27 Not applicable AAFX Hair Solution 0.02 mg/71 Topical Prostemics Co., Ltd. 2014-12-01 Not applicable AAFX Skin Solution 0.02 mg/71 Topical Prostemics Co., Ltd. 2014-12-01 Not applicable AAPE Hair Ampoule Solution 0.03 mg/61 Topical Prostemics Co., Ltd. 2014-08-01 Not applicable
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End 3M Nexcare Cold Sore Treatment Allantoin (10 mg/1g) + Benzocaine (50 mg/1g) Ointment Topical 3M Company 2008-02-20 Not applicable 4Jointz Allantoin (0.025 g/100g) + Eucalyptus oil (4 g/100g) + Tannic acid (5 g/100g) Cream Topical Arp(usa) Pty Ltd 2017-01-31 2018-04-05 A.H.c Cotton 100 Mask Multi Peptide Allantoin (0.025 g/25mL) + Adenosine (0.01 g/25mL) + Nicotinamide (0.05 g/25mL) Patch Topical Carver Korea Co.,Ltd. 2017-09-20 Not applicable A.H.c Cotton 100 Mask Skin Ceramide Allantoin (0.025 g/25mL) + Adenosine (0.01 g/25mL) + Nicotinamide (0.05 g/25mL) Patch Topical Carver Korea Co.,Ltd. 2017-09-05 Not applicable A.H.c Cotton 100 Mask Soy Isoflavone Allantoin (0.025 g/25mL) + Adenosine (0.01 g/25mL) + Nicotinamide (0.05 g/25mL) Patch Topical Carver Korea Co.,Ltd. 2017-09-14 Not applicable A.H.c Cotton 100 Mask Triple Hyaluronic Allantoin (0.025 g/25mL) + Adenosine (0.01 g/25mL) + Nicotinamide (0.05 g/25mL) Patch Topical Carver Korea Co.,Ltd. 2017-09-20 Not applicable A.H.c Cotton 100 Mask Triple Hyaluronic Allantoin (0.025 g/25mL) + Adenosine (0.01 g/25mL) + Nicotinamide (0.05 g/25mL) Patch Topical Carver Korea Co.,Ltd. 2017-09-20 2017-09-21 Actinac Pwr Allantoin (24 mg) + Chloramphenicol (40 mg) + Hydrocortisone acetate (40 mg) + Nicoboxil (24 mg) + Octasulfur (320 mg) Powder Topical Roussel Canada Inc. 1978-12-31 1996-09-09 Actinac Pws Allantoin (24 mg) + Chloramphenicol (40 mg) + Hydrocortisone acetate (40 mg) + Nicoboxil (24 mg) + Octasulfur (320 mg) Powder, for solution Topical Hoechst Roussel Canada Inc. 1994-12-31 2001-07-20 Ahc Radiance Gommage Peeling Allantoin (1 g/100mL) + Panthenol (1 g/100mL) Gel Topical Carver Korea Co.,Ltd. 2017-05-10 Not applicable
- Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Antiscar Allantoin (2 g/100g) + 13-cis-12-(3'-Carboxyphenyl)retinoic acid (2 g/100g) + Epigallocatechin gallate (.3 g/100g) + Onion (.5 g/100g) + Petrolatum (3 g/100g) Patch Topical Basiem 2015-04-01 2015-04-20 Elite Allantoin (2 g/100g) + Lidocaine (4 g/100g) + Petrolatum (30 g/100g) Patch Topical Meds Direct Rx Of Ny Llc 2015-01-31 2015-06-08 Preginot Allantoin (2 g/100g) + Lidocaine (4 g/100g) + Petrolatum (30 g/100g) Patch Topical Pharmaco Technology Llc 2015-04-01 2015-04-01 Premium Scar Patch Allantoin (2 g/100g) + Lidocaine (5 g/100g) + Petrolatum (30 g/100g) Patch Topical Alivio Medical Products, Llc 2015-03-15 Not applicable Renuu NL Allantoin (2 g/100g) + Petrolatum (30 g/100g) Patch Topical Patchwerx Labs 2014-04-15 Not applicable Renuu Patch Allantoin (2 g/100g) + Lidocaine (5 g/100g) + Petrolatum (30 g/100g) Patch Topical Patchwerx Labs 2014-04-15 Not applicable Scar Patch Allantoin (2 g/100g) + Lidocaine hydrochloride (4 g/100g) + Petrolatum (30 g/100g) Patch Topical Binger Consulting Corporation 2014-12-01 2015-11-30 Scar Patch Allantoin (2 g/100g) + Lidocaine (5 g/100g) + Petrolatum (30 g/100g) Patch Topical Binger Consulting Corporation 2014-12-01 2016-07-31 Vexa Allantoin (2 g/100g) + Lidocaine (4 g/100g) + Petrolatum (30 g/100g) Patch Topical N.O.R.T.H., Inc. 2014-06-20 2014-07-30 Vexa Allantoin (2 mg/1) + Lidocaine (4 mg/1) + Petrolatum (30 mg/1) Patch Topical Pharmaceutics Corporation 2015-03-19 Not applicable
- CAS number
- Average: 158.1154
- Chemical Formula
- InChI Key
- IUPAC Name
Allantoin is commonly applied in a variety of topical vehicles or applications such as cosmetic creams, toothpastes, mouthwashes, shampoos, lipsticks, anti-acne products, and lotions  for the purpose of moisturizing skin, enhancing the smoothness of skin, stimulating the healing of wounds, and soothing irritated skin .
There is no well controlled and appropriate data that can formally substantiate the pharmacodynamic properties of allantoin [Label]. Nevertheless, ongoing studies suggest that allantoin possesses moisturizing and keratolytic effects, as well as abilities to increase the water content of the extracellular matrix and enhance the desquamation of upper layers of dead skin cells, all of which are activities that can promote cell proliferation and facilitate wound healing .
- Mechanism of action
There is no well controlled data that can formally substantiate the method of action [Label]. However, ongoing studies suggest that there may exist a histological wound healing profile induced by allantoin in rats that leads to the amelioration and fastening of the reestablishment of normal skin . This facilitation of wound healing is supported by observations that wounds inflicted to rat subjects to which topical allantoin preparations were applied histologically demonstrated increased vasodilation, presence of inflammatory exudates, number of inflammatory cells, angiogenesis, fibroblast proliferation, and increased collagen deposition when compared to rat subjects with wounds that did not receive any allantoin administration .
In studies on human subjects, a recovery of 19% and 34% of allantoin in the urine was observed but only in two individuals and only after the administration of massive doses of allantoin . After intravenous administration, recovery in the urine was practically quantitative with doses of 75 to 600 mgm in the human model . After 240 mgm, excretion continued for 72 hours in human subjects and the results were similar in regards to subcutaneous injection .
- Volume of distribution
- Not Available
- Protein binding
- Not Available
Uricase is the enzyme that possesses the functionality to convert uric acid to allantoin. Considering humans do not possess any endogenous uricase, uric acid is the only final breakdown product in the purine degradation of unwanted waste product purine nucleotides . The presence of allantoin in human urine is subsequently the result of non-enzymatic processes on uric acid with reactive oxygen species . Such non-enzymatic processes are consequently potentially suitable biomarkers for measuring oxidative stress in chronic illnesses and aging . Furthermore, as allantoin is found endogenously and is part of basic, natural metabolic pathways, no accumulation is expected of it [Label]. Additionally, allantoin is not believed to be metabolized to a measurable extent in humans and animals [Label].
- Route of elimination
Urinary clearance is the predominant excretion route [Label].
- Half life
When studied in cattle, sheep, and horses, the half-life of allantoin is in the range of 1 to 2.5 hours [Label].
Some studies suggest that the average renal clearance of allantoin in normal, healthy human subjects is approximately 123 cc per minute . It is generally agreed upon that exogenously administered allantoin is rapidly excreted [Label].
No studies on repeated dose toxicity and reproductive toxicity have been submitted. Moreover, studies show that the tumor incidence in allantoin treated animals did not differ largely from that found in untreated controls. As a result, further or additional toxicity, mutagenicity, or carcinogenicity tests are not required in view of the endogenous nature of allantoin and the general lack of overall toxicity [Label].
Finally, as allantoin is a normal component of the diet in humans and is a substance of endogenous origin present in the body of humans, it is generally recognized as being a safe substance for humans [Label].
- Affected organisms
- Humans and other mammals
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
- General References
- Araujo LU, Grabe-Guimaraes A, Mosqueira VC, Carneiro CM, Silva-Barcellos NM: Profile of wound healing process induced by allantoin. Acta Cir Bras. 2010 Oct;25(5):460-6. [PubMed:20877959]
- FRIEDMAN M, MYERS SO, ABRAHM PM: Allantoin clearance as a measure of glomerular filtration rate in man. Proc Soc Exp Biol Med. 1947 Dec;66(3):522. [PubMed:18900011]
- Kand'ar R, Zakova P: Allantoin as a marker of oxidative stress in human erythrocytes. Clin Chem Lab Med. 2008;46(9):1270-4. doi: 10.1515/CCLM.2008.244. [PubMed:18636793]
- Thornfeldt C: Cosmeceuticals containing herbs: fact, fiction, and future. Dermatol Surg. 2005 Jul;31(7 Pt 2):873-80; discussion 880. [PubMed:16029681]
- Toxnet Toxicology Data Network: Allantoin [Link]
- External Links
- AHFS Codes
- 84:24.12 — Basic Ointments and Protectants
- 92:01.00* — Herbs and Natural Products
- FDA label
- Download (115 KB)
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Treatment Epidermolysis Bullosa 1 4 Recruiting Treatment Sickle Cell Anemia Crisis 1
- Not Available
- Not Available
- Dosage forms
Form Route Strength Ointment Topical 0.5 g/100g Liquid Topical 0.006 g/6.6g Ointment Topical 1 g/100g Solution Topical 0.02 mg/71 Solution Topical 0.03 mg/61 Cream Topical 0.1 g/50mL Cream Cutaneous 0.2 mg/20mL Powder Topical Powder, for solution Topical Paste, dentifrice Topical Aerosol, spray Topical 0.425 g/85g Spray Topical 0.425 g/85g Gel Topical 0.5 g/100mL Gel Topical 0.15 g/30mL Lotion Topical Cream Topical 0.0005 g/1mL Cream Topical 0.8 mg/160mL Lotion Topical 0.8 mg/160mL Gel Topical 0.8 mg/160mL Shampoo Topical 1.5 mg/300mL Lotion Topical 1.5 g/300mL Shampoo Topical 1.5 g/300mL Liquid Topical 0.1 g/20mL Soap Topical 0.5 g/100g Liquid Topical 1.0 g/200mL Solution Topical 0.005 mg/181 Spray Topical Lotion Topical 0.4 mL/200mL Liquid Topical 0.004 mL/2mL Patch Topical 0.12 g/60g Elixir Topical Emulsion Topical 0.6 % Lotion Topical 0.25 g/250g Cream Cutaneous 0.2 g/40g Patch Topical 0.15 g/31 Gel Topical 0.15 g/31 Patch Topical 0.004 g/2.4g Emulsion Topical 0.1 g/100mL Patch Topical 0.2 g/40g Stick Topical 0.5 g/100g Salve Topical 5 mg/1g Liquid Topical 0.15 g/100mL Gel Topical 0.75 g/75g Cream Topical 0.225 mg/45mL Cream Topical 0.65 mg/130mL Spray Topical 0.6 mg/120mL Cream Topical 0.22 mg/45mL Cream Topical 2 g/100g Patch Topical 0.5 1/25g Patch Topical 0.06 g/51 Liquid Topical 0.05 g/100mL Cream Topical 0.5 mg/100g Cream Topical 5 mg/1g Jelly Topical 0.5 g/100mL Lotion Topical 0.5 g/100mL Cream Topical 50 mg/5g Lipstick Topical Cream Topical 0.5 mL/100mL Cream Topical 0.5 g/100mL Powder Topical 0.02 g/50g Disc Topical Paste, dentifrice Dental Emulsion Topical Cream Topical 3.6 mL/60mL Lotion Topical 0.5 1/50mL Cream Topical 0.5 mg/100mL Gel Topical 0.05 g/100g Cream Topical 0.1 g/100g Cream Cutaneous Patch Topical 0.1 g/49g Shampoo Topical 6.0 g/300mL Lotion Topical 0.75 mg/150mL Gel Topical 2 % Lotion Topical 2 % Gel Topical 0.1 g/100mL Liquid Topical 0.1 g/100mL Cream Topical 1 g/50g Spray Topical 0.3 g/60g Spray Topical 1.2 g/100g Tablet, soluble Topical 0.5 mg/100mg Liquid Topical 0.02 g/4mL Liquid Topical 0.19 g/100g Cream Topical 0.1 g/100mL Powder Topical 0.44 mg/80mL Powder Topical 0.055 g/10g Gel Topical 0.8 g/100g Soap Topical 2.0 g/100g Liquid Topical 0.54 mg/90mL Solution Topical 0.96 g/120mL Solution Topical 0.96 mg/120mL Solution Topical Liquid Topical 0.1 g/10g Gel Topical 0.5 g/100g Ointment Topical .02 g/1g Cream Topical 0.75 mg/150mL Cream Topical 10 mg/1g Solution Topical 0.04 g/5g Lotion Topical 3 g/600g Lotion Cutaneous 0.1 mL/20mL Soap Cutaneous; Topical 5 mg/1g Powder Topical 0.002 g/1g Solution Topical 0.25 g/205g Tablet Vaginal 0.2 1/1 Tablet Vaginal 0.11 1/600mg Tablet Vaginal 66 mg/600mg Gel Topical 51.0 mg/10mL Gel Topical 50 mg/10mL Cream Topical 0.67 mg/135mL Cream Topical 0.25 mg/50mL Patch Topical 0.2 g/100g Cream Topical 1 g/100mL Gel Topical 10 mg/1mL Gel Topical 0.1 mg/1mL Stick Topical Lotion Topical 0.55 % Patch Topical 0.17 mg/35mL Soap Topical 0.6 g/100g Liquid Topical 0.01 g/100mL Ointment Topical 1 % Cream Topical 0.075 g/15mL Liquid Topical 1 mg/30mL Liquid Topical 0.08 g/100mL Liquid Topical 0.75 mg/150mL Patch Topical 0.028 g/28g Spray Topical 0.3 mg/60mL Cream Topical 0.5 g/100g Liquid Topical 0.6 mg/30mL Liquid Topical 0.54 mg/30mL Soap Topical 0.55 g/110g Gel Topical 3 mg/1mL Liquid Topical 0.05 g/10mL Shampoo Topical 0.75 g/150mL Solution Topical 0.30 g/60mL Liquid Topical 0.025 g/5mL Liquid Topical 0.0005 g/1mL Ointment Topical Soap Topical 1.30 g/100g Aerosol, foam Topical 1.25 mg/250mL Oil Topical 0.75 mg/150mL Gel Topical 5 mg/1g Solution Topical 0.1 g/100mL Liquid Topical 0.002 g/1mL Emulsion Topical 0.002 g/1mL Liquid Topical 2 g/100mL Aerosol, foam Topical 0.5 g/100mL Lotion Topical 0.1 mL/50mL Liquid Topical 0.2 g/100mL Lotion Topical 0.4 g/20mL Liquid Topical 0.02 mg/1mL Liquid Topical 0.1 g/100g Powder Topical 0.007 g/0.7g Cloth Topical 0.75 mL/1mL Liquid Topical 1 g/100mL Gel Topical 0.05 g/100mL Cream Topical 0.25 g/50g Shampoo Topical 0.75 mg/150mL Solution Topical 0.3 mg/60mL Liquid Topical 0.025 mg/5mL Liquid Topical 0.3 g/100mL Solution Topical 0.175 mg/51 Patch Topical 0.16 g/32g Lotion Topical 0.1 g/100mL Patch Topical 0.015 mg/101 Spray Topical 0.36 mg/60mL Spray Topical 0.1 g/100mL Cream Topical 0.0125 mg/25g Cream Topical 0.004 mg/20mL Cream Topical 0.0042 mg/21mL Soap Topical 0.05 g/100g Stick Topical 5 mg/1g Lotion Topical 0.5 mL/100 mL Cream Topical 5 mg/100mL Cream Topical Cream Topical 5 mg/1mL Lotion Topical 0.5 mL/100mL Cream Topical 0.005 mg/1g Gel Topical 10 mg/1g Cream Topical 1.5 g/300g Liquid Topical 0.48 mg/80mL Solution Topical 0.48 mg/80mL Cream Topical 0.2 g/100mL Emulsion Topical 0.02 g/100mL Cream Topical 0.02 g/100mL Liquid Topical 0.02 g/100mL Soap Cutaneous 5 mg/1g Liquid Topical Lotion Topical 0.1 g/100g Cream Topical 7.5 mg/1mL Lotion / shampoo Topical 5.5 mg/1mL Emulsion Topical 0.55 % Cream Topical 0.28 mg/40mL Kit Topical Cream Topical 1 % Concentrate Topical 0.22 g/45mL Liquid Topical 0.075 g/15mL Liquid Topical 0.002 mg/1mL Cream Topical 0.000003 g/30mL Gel Topical Kit Cream Topical 0.002 g/1g Liquid Topical 5 mg/1mL Liquid Topical 0.5 g/100g Solution Topical 1.9 mg/380mL Emulsion Topical 0.65 mg/130mL Cream Topical 0.1 mL/100mL Liquid Topical 0.5 g/100mL Cream Topical 0.0075 g/25g Liquid Topical 0.625 mg/125mL Liquid Topical 0.57 g/113g Liquid Topical 0.75 g/150g Patch Topical Cream Topical 0.51 % Powder Topical 0.3 mg/3g Powder Topical 0.003 g/3g Powder Topical 0.2 mg/2g Cream Topical 0.15 mg/30mL Liquid Topical 0.001 g/1mL Liquid Topical 0.1 mg/1mL Mouthwash Dental Gel, dentifrice Dental Cream Topical 0.0005 g/1g Powder Topical 0.0001 g/1g Cream Topical 0.425 g/85mL Cream Topical 0.02 mg/1mL Gel Topical 5.5 g/1L
- Not Available
- Not Available
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 4.73 mg/mL ALOGPS logP -2 ALOGPS logP -2.4 ChemAxon logS -1.5 ALOGPS pKa (Strongest Acidic) 7.95 ChemAxon pKa (Strongest Basic) -3.4 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 4 ChemAxon Polar Surface Area 113.32 Å2 ChemAxon Rotatable Bond Count 1 ChemAxon Refractivity 32.02 m3·mol-1 ChemAxon Polarizability 12.89 Å3 ChemAxon Number of Rings 1 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon
- Predicted ADMET features
- Not Available
- Mass Spec (NIST)
- Not Available
- Not classified
Drug created on December 03, 2015 09:51 / Updated on December 14, 2018 16:53