Aspartato de arginina

Otros Nombres

(2S)-2-Amino-5-carbamimidamidopentanoic acid(2S)-2-Amino-5-guanidinopentanoic acid (2S)-2-aminobutanedioate(2S)-2-aminobutanedioic acid and (2S)-2-amino-5-(diaminomethylideneamino)pentanoic acid(2S)-2-aminobutanedioic acid compound with (2S)-2-amino-5-{[amino(imino)methyl]amino}pentanoic acid (1:1)(2S)-2-aminobutanedioic acid; (2S)-2-amino-5-(diaminomethylideneamino)pentanoic acid2-AMINO-5-CARBAMIMIDAMIDOPENTANOIC ACID; 2-AMINOBUTANEDIOIC ACIDArginine Aspartate EPArginine, L-, L-aspartate (1:1)Arginyl aspartateAspartic acid, compd. with ornithine, N5-(diaminomethylene)- (1:1)Aspartic acid, L-, compd. with L-arginine (1:1)L-ARG L-ASPL-Arginin--L-asparaginsäure (1:1)L-Arginine - acide L-aspartique (1:1)L-Arginine - L-aspartic acid (1:1)L-Arginine compound with L-aspartic acidL-Arginine L-aspartateL-Arginine L-aspartate saltL-Arginine, compd. with L-aspartic acid (1:1)L-Arginyl aspartateL-Aspartic acid, compd. with L-arginine (1:1)N5-(Diaminomethylen)ornithin-asparaginsäure (1:1)N5-(Diaminométhylène)ornithine - acide aspartique (1:1)N5-(Diaminomethylene)ornithine - aspartic acid (1:1)S(+)-2-Amino-5-[(aminoiminomethyl)amino]pentanoic acid

Sinopsis

Arginine Aspartate

1. Identity and Chemical Nature

Arginine aspartate (also referred to as L-arginine L-aspartate, arginyl-aspartate, or the arginine–aspartate salt) is a molecular compound formed by the ionic pairing of the amino acid L-arginine (a semi-essential, basic amino acid) with L-aspartic acid (an acidic, dicarboxylic amino acid). Its molecular formula is C₁₀H₂₁N₅O₆, and it is assigned PubChem CID 24325. The compound is also registered separately as PubChem CID 11500504 under the name "arginine aspartate."

L-arginine is the most nitrogen-rich amino acid, acting as a key precursor for the synthesis of nitrogen-containing metabolites and an essential intermediate in the clearance of excess nitrogen. Its side chain possesses a guanidino group with unique biochemical properties, playing a primary role in nitrogen excretion (urea), cellular signaling (nitric oxide), and energy buffering (phosphocreatine). In the salt form, aspartate acts as the anionic countercharge, solving the solubility limitations of free-base arginine. L-arginine is an alkaline amino acid that is not very water-soluble, unless in ionic forms with anionic countercharge; aspartate fulfils this purpose in arginine aspartate preparations.

In one gram of arginine aspartate the true quantity of arginine is only 560 mg (not 1000 mg), so to attain a quantity of one gram of arginine, it is necessary almost to double the dose of the administered salt. This stoichiometry is important when comparing study dosages to free-arginine equivalents.

The compound is classified as a dietary supplement in most jurisdictions. Aspartate and arginine are favorably administered together as dipeptides or in mixtures to provide higher bioavailability for both amino acids and thereby increase their effectiveness at lower doses. The combination is sometimes described as a dipeptide form (arginyl-aspartate) and sometimes as a simple ionic salt, depending on the preparation and the source.

Natural Sources

Most human cells do not synthesize sufficient arginine to meet demand and are dependent on exogenous arginine. Both constituent amino acids are present in protein-rich foods: L-arginine is abundant in nuts, seeds, legumes, red meat, poultry, and dairy, while L-aspartate is found widely in plant and animal protein sources. The combined salt form, however, does not occur naturally in significant quantities and is produced synthetically for pharmaceutical and supplement purposes.

Common Preparations and Tradenames

Drinkable formulations are available based on arginine aspartate in Europe under the names Sargenor® (L-arginine aspartate) and Pargine® (L-arginine aspartate), presented in drinkable vials to dilute in water, with respective doses of 1 or 1.5 grams (Sargenor®) and 5 grams (Pargine®) per unit. Effervescent tablets containing 1 gram and 1.5 grams (Sargenor®) of arginine salt to dissolve in water are also available. The compound is also a key ingredient in the proprietary combination product Prelox®, which pairs L-arginine aspartate with Pycnogenol® (French maritime pine bark extract). Prelox® is a trademarked proprietary blend of French maritime pine bark extract (Pycnogenol®) and L-arginine aspartate.

In addition to oral solutions and effervescent tablets, arginine aspartate is available in powder and capsule/tablet forms as a dietary supplement in various markets. Oral products available in the US are often marketed as dietary supplements.

2. Traditional and Historical Use

Unlike many botanical or herbal ingredients, arginine aspartate is a relatively modern nutritional-pharmaceutical compound; it does not feature in ancient traditional medicinal systems such as Ayurveda, Traditional Chinese Medicine, or Western herbalism. Its history begins in mid-twentieth-century European, particularly French, pharmacology.

Arginine-aspartate was tested clinically in 1965 for the first time against physical and psychic asthenia (Duruy, A. and Baujat, J. P., Vie. Med. Int. 9:1589 (1965)), and the positive effect was later confirmed (Duruy, A., Med. Int. 1:203 (1966)). This early work established the use of the compound for combating fatigue—both physical and psychological—in European clinical settings.

Other studies showed that long-term administration of arginine-aspartate improves aerobic energy metabolism and performance (Sellier, J., Rev. Med. Toulouse 5:879 (1979); Schmid, P. et al., Leistungssport 10:486-495 (1980)). These publications from the late 1970s and early 1980s established the compound's reputation in European sports medicine and athletic performance contexts.

L-Arginine-L-Aspartate (Sargenor®) is widely used by athletes and patients to increase training effects as well as exercise tolerance. The brand Sargenor® was developed and commercialized predominantly in France, where it has been used as a licensed pharmaceutical product for transient fatigue, and its use spread to other European countries including Italy, Portugal, and several others. Its traditional pharmaceutical indications in Europe center on the treatment of transient physical and mental fatigue and states of asthenia (general debility).

3. Key Constituents and Mechanisms of Action

Arginine aspartate delivers two pharmacologically active amino acids simultaneously. Both components have distinct and complementary biochemical roles.

L-Arginine: Active Constituent and Mechanisms

Nitric Oxide (NO) Production: In the nitric oxide/citrulline cycle, arginine is converted to citrulline by nitric oxide synthases (NOS), producing NO. NO is an important regulator of vascular tone. Arginine up-regulates the activity of GTP cyclohydrolase-I, freeing tetrahydrobiopterin (THB) for NO synthesis and the hydroxylation of aromatic amino acids by aromatic amino acid hydroxylase. This vasodilatory pathway underpins much of arginine's proposed cardiovascular and erectile physiology applications.

Urea Cycle and Ammonia Clearance: Arginine is a constituent of body proteins and an intermediate in the urea cycle in the liver. The urea cycle is a series of five reactions in which urea synthesis is the final step in the detoxification of ammonia. Arginine is not only a substrate for ureagenesis, but also an activator of N-acetylglutamate synthetase, which is a key ureagenic enzyme. Arginine is an allosteric activator of N-acetylglutamate synthase, an enzyme which converts glutamate and acetyl-CoA into N-acetylglutamate in the mitochondria, pushing the hepatic urea cycle towards the active state, useful for ammonia detoxification.

Growth Hormone and IGF-1 Axis: In addition to the alleged effect of increased NO synthase, L-arginine has been studied as a possible stimulator of GH secretion. GH stimulates the production of insulin-like growth factor 1 (IGF-1), which acts as an anabolic hormone by increasing protein synthesis. The proposed mechanism is inhibition of hypothalamic somatostatin (the GH-inhibiting hormone), though evidence from human studies is inconsistent (discussed under clinical evidence).

Collagen Synthesis and Wound Healing: Arginine is also a key substrate for the synthesis of collagen. This has been documented in wound-healing models.

Neurotransmitter Precursor Activity: Delivery of high levels of arginine to raise cellular levels of THB directly stimulates the biosynthesis of many neurotransmitters in CNS capillary endothelial cells. Aromatic amino acids serve as precursors for biosynthesis of monoamine neurotransmitters, including melatonin, dopamine, norepinephrine, and epinephrine.

Creatine Synthesis: Depending on cellular conditions and/or cell type, arginine can be used to support protein production; to clear excess NH₄⁺ through the production of urea; as a precursor in the production of the energy-buffering phosphagen creatine; or to synthesize agmatine and polyamines.

L-Aspartate: Active Constituent and Mechanisms

Tricarboxylic Acid (TCA) Cycle Entry and Fat Oxidation: L-aspartate, a precursor of oxaloacetate, was proposed to increase the utilization of free fatty acids (FFA) and to spare muscle glycogen. L-aspartate, as a precursor of oxaloacetate, was suggested to improve the biochemical capacity of muscle for oxidation of fatty acids through the Krebs cycle.

Ammonia Clearance: L-aspartate increased the peripheral clearance of ammonia, with the consequence of delayed muscle fatigue. This occurs because aspartate participates directly in the urea cycle as the nitrogen donor for argininosuccinate formation. In a cytosolic reaction catalyzed by argininosuccinate synthetase, citrulline and aspartate are condensed to form argininosuccinate, which is a critical step for incorporating nitrogen into urea for excretion.

Inhibition of Glycolysis: This would be in line with the observation of enhanced fat oxidation and improved aerobic performance after L-arginine-L-aspartate intake. Thus, when glycolysis is inhibited by L-arginine, L-aspartate may be an important contributor to energy production via the Krebs cycle.

Synergistic Effects of the Combined Salt

The effects of orally administered arginine aspartate (250 mg per kg) on the secretion of insulin, glucagon, and growth hormone in the rat were compared with those of equimolar doses of arginine (142 mg per kg) and aspartic acid (108 mg per kg) alone. There were no significant changes in blood levels of insulin and glucagon. Arginine aspartate increased growth hormone levels, whereas its two components administered individually failed to induce any significant changes. This animal study suggests a possible synergistic effect of the combined salt on GH secretion that is not seen with either component given separately, though the clinical relevance in humans is debated.

Within the Prelox® combination, Prelox® (a combination of French maritime pine bark extract with L-arginine aspartate) enhanced activity of endothelial nitric oxide synthase (e-NOS) and reduced plasma concentrations of the e-NOS inhibitor ADMA (asymmetric dimethylarginine), thus enhancing bioavailability of nitric oxide.

4. Scientific Evidence by Area of Use

4.1 Exercise Performance and Ergogenics

L-arginine-L-aspartate is widely used by athletes for its potentially ergogenic properties; however, only little information on its real efficacy is available from controlled studies.

Blood Lactate and Oxygen Consumption: A key controlled clinical study evaluated the compound prospectively. A double-blind placebo-controlled trial evaluated the effects of prolonged supplementation with L-arginine-L-aspartate on metabolic and cardiorespiratory responses to submaximal exercise. Sixteen healthy male volunteers (22 ± 3 years) performed incremental cycle spiroergometry up to 150 watts before and after intake of L-arginine-L-aspartate (3 grams per day) or placebo for a period of 3 weeks. Results demonstrated reductions in blood lactate accumulation and oxygen consumption during submaximal exercise. The authors noted that whereas L-arginine can increase exercise tolerance and performance in patients with cardiovascular diseases, no satisfactory clinical studies found any beneficial effects of L-arginine on endurance performance in healthy subjects, suggesting that L-aspartate made a noteworthy contribution to the beneficial effects observed.

Earlier Ergogenic Reports (Non-standardized Studies): Impressive effects on endurance performance have been reported after prolonged intake of L-Arginine-L-Aspartate, causing decreased blood lactate concentrations and heart rates during submaximal exercise and increased oxygen uptake with workload increments, though these early studies did not use standardized test procedures.

Ammonia Reduction: To investigate the effect of the ingestion of arginine aspartate (AA) in the decrease of exercise-induced accumulation of ammonia in plasma, 11 voluntary subjects took part in a cross-over study where AA effect was tested against placebo, administered in a double-blind procedure. Both concentrations were unchanged between AA and placebo at rest, but a significant lesser delta plasma ammonia was found under AA at the 15th minute of exercise only (P < 0.05). It was concluded that the AA effect was minor with regard to the training effect. This study's small sample (11 subjects) and the modest magnitude of effect limit its conclusions.

Contradictory Evidence (Short-Term Use): A study on well-trained judo athletes found that short-term arginine supplementation had no effect on nitric oxide production, lactate and ammonia metabolism, and performance in intermittent anaerobic exercise. This underscores the variability in findings between different exercise modalities, training status, and supplementation duration.

Overall strength of evidence for ergogenic use: Preliminary to mixed. The most methodologically rigorous controlled studies use small samples, and results differ across exercise type, supplementation duration, and athlete training level. No large-scale randomized controlled trials have established a clear, consistent ergogenic benefit for healthy, well-trained athletes.

4.2 Exercise-Induced Hyperammonemia

The theoretical basis for arginine aspartate's anti-hyperammonemic effect is well-established biochemically: both arginine and aspartate participate in the urea cycle, promoting ammonia clearance. In a separate intravenous arginine study, peak plasma ammonia and lactate were significantly decreased after L-arginine load (60.6 ± 8.2 vs. 73.1 ± 9.1 µmol/L, p < 0.01, and 7.1 ± 0.7 vs. 8.2 ± 1.1 mmol/L, p < 0.01, for ammonia and lactate respectively). However, this used intravenous delivery in a controlled laboratory setting. The translation to oral supplementation in free-living athletes is less certain, and as noted above, the cross-over trial by Denis et al. found only a minor effect with oral arginine aspartate that was overshadowed by training adaptation.

4.3 Wound Healing and Collagen Synthesis

A well-designed human study examined arginine aspartate in an established wound-healing model. In this study, 36 young, healthy human volunteers (ages 25 to 35) were randomized into one of three groups: (1) 30 g arginine hydrochloride daily supplements (24.8 g free arginine), (2) 30 g arginine aspartate (17 g free arginine), or (3) placebo. The supplements were given for 2 weeks, after which PTFE catheters were removed and hydroxyproline content (an index of reparative collagen synthesis) was evaluated. Arginine supplementation at both doses significantly increased the amount of hydroxyproline and total protein deposition at the wound site.

Dietary supplementation with 30 g/d arginine aspartate for 2 weeks to healthy elderly human volunteers enhanced wound collagen accumulation significantly. These findings support a physiologically coherent role for arginine (delivered as the aspartate salt) in wound repair and collagen deposition, particularly in older individuals and surgical contexts.

Evidence strength: Moderate, based on controlled human studies using validated collagen deposition models. The sample sizes are small, and doses used (17–30 g free arginine equivalent) are much higher than typical supplement doses.

4.4 Erectile Dysfunction (ED)

Arginine aspartate, primarily in combination with Pycnogenol® (as Prelox®), has been tested in several clinical trials for mild to moderate ED.

Combination with Pycnogenol (Prelox®): In a randomly allocated, double-blind, placebo-controlled, crossover design, 50 patients with mild to moderate erectile dysfunction were treated for 1 month with placebo or a combination of L-arginine aspartate and Pycnogenol (Prelox). Patients reported sexual function from diaries. Testosterone levels and endothelial NO synthase (e-NOS) were monitored. Intake of Pycnogenol for 1 month restored erectile function to normal. Intercourse frequency doubled. e-NOS in spermatozoa and testosterone levels in blood increased significantly. Cholesterol levels and blood pressure were lowered. No unwanted effects were reported.

L-arginine aspartate alone: A first experimental study tested L-arginine aspartate (dosage 3 g/day) both alone and in combination with Pycnogenol® for recovery of ED in 40 men. Application of L-arginine aspartate alone for 1 month was effective in only 5% of men, while the addition of Pycnogenol® (80 mg/day) to the L-arginine aspartate regimen was effective during a second month's treatment in recovering erectile function in 80% of the cases (P < 0.01). A subsequent increase in the Pycnogenol® dose further raised responder rates. Throughout the 3-month trial period, patients received 3 ampoules Sargenor a day, a drinkable solution of the dipeptide arginyl-aspartate (equivalent to 1.7 g L-arginine per day). Remarkably, after the third month of treatment, 92.5% of the men experienced a normal erection.

Arginine aspartate + Adenosine Monophosphate (AMP): A separate pilot trial tested arginine aspartate alone (without Pycnogenol). A double-blind, placebo-controlled, two-way crossover randomized clinical trial with 26 patients compared the efficacy and safety of L-arginine aspartate 8 g combined with 200 mg of adenosine monophosphate (AA) with placebo alone for intermittent treatment of mild-to-moderate erectile dysfunction. Efficacy was assessed by International Index of Erectile Function (IIEF) and two additional validated questionnaires. Investigators' and patients' assessment of efficacy was significantly improved by the combination vs. placebo (p = 0.01 and p = 0.04 respectively). EHS and EDITS questionnaires were both improved (p = 0.015 and p = 0.017 respectively). ED patients demonstrated significant improvements in all IIEF domains with the exception of the Sexual Desire and Orgasmic Domains. This pilot phase II study showed that on-demand oral administration at a high dosage of L-arginine aspartate–adenosine monophosphate combination may be effective in patients with mild-to-moderate ED, is very well tolerated, and could be tested as a safe first-line therapy in a larger phase III study.

The improvement of ED with Prelox® was not persistent; ED deteriorated again at the end of the supplementation period. This indicates that the effect requires ongoing supplementation.

Evidence strength for ED: Moderate, based on multiple small-to-medium randomized controlled trials. However, most positive results are for the combination Prelox® and not for arginine aspartate as a sole agent. The most studied scenario involves 3 g/day arginine aspartate plus 80–120 mg/day Pycnogenol®. Larger, independent trials are needed.

4.5 Male Fertility and Semen Parameters

In a randomly allocated, double-blind, placebo-controlled, cross-over design, 50 infertile patients were treated for 1 month with placebo or a combination of L-arginine aspartate and Pycnogenol® (Prelox®). Semen samples were examined at 4-week intervals according to WHO criteria. Treatment with Prelox® increased significantly the semen volume, concentration of spermatozoa, percentage of motile spermatozoa, and percentage of spermatozoa with normal morphology compared with placebo. The placebo had no influence on the parameters of seminological analysis. Intake of Pycnogenol for 1 month improved the fertility index to normal values. After treatment, the fertility index decreased again to infertile status. No unwanted effects were reported.

Prelox® was also effective in improving quantity and quality of spermatozoa in men with ED. Concentration, morphology, and viability of spermatozoa were highly significantly improved (p < 0.001) versus placebo.

An older study using arginine supplementation in a broader sense found that 74% of 178 men with low sperm counts had significant improvements in sperm counts and motility after arginine therapy. However, this precedes the specific combination product trials and used various arginine forms.

Evidence strength for fertility: Preliminary to moderate. Results are promising but confined to small trials (typically 40–50 subjects), most by a single research group, using the arginine aspartate plus Pycnogenol® combination rather than arginine aspartate alone.

4.6 Growth Hormone Secretion

The GH-stimulating potential of arginine (and the aspartate salt specifically) has produced inconsistent findings across human studies.

When 250 mg/kg/day of oral arginine aspartate were administered to five healthy subjects aged 20 to 35 for seven days, a 60% rise in GH occurred during slow wave sleep. This early finding from Besset et al. stimulated interest in arginine aspartate as a sleep-related GH secretagogue.

Colombani et al. supplemented fourteen trained males with 15 g/day arginine aspartate, or placebo for 14 days before a marathon. On the day of the marathon, blood samples were collected before and after the 31 km race, and 2 h post marathon race. The authors observed a significant increase in plasma GH only in the group supplemented with L-arginine.

However, contradictory human data also exist. Abel et al. found no difference in plasma GH concentration after supplementation with arginine aspartate in eight volunteers for 4 weeks with a low dose (5 g total — 2.8 g of L-arginine and 2.2 g of aspartate) and high dose (14.4 g total — 5.7 g of L-arginine and 8.7 g of aspartate).

Paradoxically, chronic very high-dose oral arginine aspartate may suppress the GH axis. A study investigating the effect of chronic oral arginine aspartate on growth hormone (GH), GHRH, IGF-1, and IGF-binding protein-3 secretions administered arginine aspartate (30 g) orally once daily at 21:00 h for 21 consecutive days to 23 healthy non-athlete volunteer males. Over the course of the study, GH changes were accompanied by a general decrease in IGF-1 and IGFBP-3. In healthy volunteers, a chronic oral treatment with 30 g/day arginine aspartate is followed by a decrease in IGF-1 and IGFBP-3 secretions.

Evidence strength for GH stimulation: Weak and contradictory. Studies show divergent results depending on dose, duration, subject training status, and timing of measurement. Chronic high-dose supplementation may paradoxically reduce IGF-1 levels.

4.7 Lipid Profile

Patients taking 30 g arginine aspartate (17 g free arginine) or placebo dissolved in syrup for 2 weeks experienced arginine-related significant increases in serum IGF-1 levels, improved nitrogen balance, lower total cholesterol and LDL-cholesterol levels, with no effect on HDL-cholesterol levels. Despite the high dose, no adverse effects were observed. However, there have been few studies testing the regulatory potential of supplementary L-arginine on blood lipid profile in humans, and the results are inconsistent or controversial.

Evidence strength for lipid effects: Weak and inconsistent. A positive finding exists at very high doses (30 g/day arginine aspartate), but conflicting data from other studies prevent any firm conclusions.

4.8 Physical and Mental Fatigue (Asthenia)

The first clinical indication established for arginine aspartate, dating to 1965, was the treatment of physical and psychic asthenia. L-arginine-L-aspartate is widely used by athletes for its potentially ergogenic properties. In Europe, Sargenor® and related preparations are indicated and licensed for transient fatigue states in adults and, in some countries, in children over a certain age threshold.

The mechanistic rationale combines ammonia clearance (reducing the accumulation that contributes to central and peripheral fatigue) with improved energy substrate utilization via the TCA cycle entry point provided by aspartate-derived oxaloacetate. However, only little information on its real efficacy for fatigue is available from controlled studies. Rigorous, placebo-controlled trials specifically focused on fatigue as a primary endpoint in non-athletic populations are limited.

5. Body Systems and Health Areas

Musculoskeletal / Exercise Physiology: Reduction of exercise-induced lactate and ammonia accumulation; potential improvement of submaximal aerobic performance; muscle energy metabolism via TCA cycle substrate provision.
Cardiovascular / Vascular: NO-mediated vasodilation; potential blood pressure reduction; improved endothelial function via e-NOS enhancement. L-arginine undoubtedly can increase exercise tolerance and performance in patients with cardiovascular diseases through endothelial NO production.
Endocrine: Modulation of GH, IGF-1, and insulin secretion; evidence is inconsistent and dose-dependent.
Reproductive (Male): Improvement of erectile function and semen parameters, primarily when combined with Pycnogenol®.
Wound Healing / Immune: Arginine-aspartate supplementation enhanced wound healing and the immune functions of T-cells.
Hepatic / Nitrogen Metabolism: Activation of the urea cycle for ammonia detoxification; potential utility in hyperammonemic states.
Central Nervous System: As a precursor to neurotransmitter synthesis pathways via THB upregulation; cognitive and mood effects are plausible but not well-studied specifically for the aspartate salt form.

6. Dosage Forms and Reported Study Dosages

The following dosages are drawn directly from human clinical sources:

3 g/day arginine aspartate (equivalent to ~1.7 g free arginine) for 3 weeks in healthy male athletes (ergogenic/lactate study).
3 g/day arginine aspartate alone for 1 month in ED patients, subsequently combined with Pycnogenol® 80 mg/day (Prelox®).
3 ampoules Sargenor/day (equivalent to 1.7 g L-arginine per day) for 3 months in men with erectile dysfunction.
30 g/day arginine aspartate (equivalent to 17 g free arginine) for 2 weeks in wound-healing studies in young healthy volunteers.
30 g/day arginine aspartate (17 g free arginine) for 2 weeks in elderly patients examining lipid and IGF-1 effects.
30 g/day arginine aspartate orally once daily at 21:00 h for 21 consecutive days in 23 healthy non-athlete males (GH/IGF-1 study).
15 g/day arginine aspartate for 14 days before a marathon in fourteen trained males (GH study).
5 g total arginine aspartate (low dose, 2.8 g L-arginine + 2.2 g aspartate) and 14.4 g total arginine aspartate (high dose, 5.7 g L-arginine + 8.7 g aspartate) for 4 weeks in eight volunteers (GH study).
8 g L-arginine aspartate combined with 200 mg adenosine monophosphate (AA), administered on-demand, in 26 patients with mild-to-moderate ED (crossover RCT).
250 mg/kg/day oral arginine aspartate for 7 days in five healthy subjects aged 20–35 (GH/sleep study).
Prelox® (L-arginine aspartate + Pycnogenol®) for 1 month in 50 infertile patients (semen parameters study).

Regarding standard commercial formulations: The recommended adult dose for Sargenor® supplementation products is 3 vials for oral use within 24 hours, preferably before meals, with each vial containing 1.0 g arginine aspartate (equivalent to 0.57 g arginine), giving a daily arginine equivalent of approximately 1.7 g.

7. Safety Considerations and Drug Interactions

General Tolerability

Significant adverse effects have not been observed with arginine supplementation; however, long-term studies are needed to confirm its apparent safety. The clinical data cover a wide span of arginine intakes from 3 g/d to more than 100 g/d. Single doses of 3–6 g rarely provoked side effects, and healthy athletes appeared to be more susceptible than diabetic patients to gastrointestinal symptoms at individual doses above 9 g. Most side effects of arginine occurred at single doses of more than 9 g in adults (more than 140 mg/kg), often when part of a daily regimen of approximately more than 30 g/d.

Across medical sources, the most common adverse effects are gastrointestinal (nausea, cramps, diarrhea), allergic reactions, and rare reports of esophagitis from pills; doses above ~10 g at once are associated with GI distress in some analyses.

Regarding which salt form is best tolerated: there is insufficient data to show which form of arginine (free base, chloride, or aspartate salt) is best tolerated.

Observed Safety Level

Through a quantitative risk assessment based on published human clinical trial data, the observed safety level for arginine is up to 20 g per day. Although some studies have exceeded 20 g a day for a short time period, there is insufficient data to make a confident conclusion about the potential adverse effects.

Renal and Hepatic Disease

People with renal failure or hepatic disease may be unable to appropriately metabolize and excrete supplemental arginine and should be closely monitored when taking arginine supplements.

Herpes Virus Infections

It has been postulated, on the basis of older in vitro data and anecdotal reporting, that arginine supplementation is contraindicated in persons with herpes infections (i.e., cold sores, genital herpes). The assumption is that arginine might stimulate replication of the virus and/or provoke an outbreak; however, this caution has not been validated by controlled clinical trials. L-arginine also serves an essential role in viral replication, and case reports describe recurrence of herpes zoster following high-dose L-arginine supplementation. The established pharmaceutical practice in some jurisdictions, such as the French Sargenor® prescribing information, may reflect this unconfirmed but plausible risk.

Cardiovascular Interactions

L-arginine can lower blood pressure; combining it with antihypertensive drugs or PDE5 inhibitors may cause blood pressure to drop too far. Several clinical resources warn against use after a recent heart attack because some data link post-MI supplementation with increased risk, and they advise caution in asthma, allergies, bleeding disorders, kidney or liver disease, and with latent herpes infections.

Drug Interactions

L-arginine supplements and medications may interact with drugs that lower blood pressure, including sildenafil (Viagra). The combination with PDE5 inhibitors is particularly notable because arginine aspartate itself is used for ED, and any co-administration with pharmaceutical ED agents would carry additive vasodilatory risk. Arginine can increase the toxicity of nitrate drugs by pharmacodynamic synergism, and both drugs can cause metabolic acidosis.

Argininemia (Absolute Contraindication)

Supplemental L-arginine is contraindicated in those with the rare genetic disorder argininemia. Argininemia is a urea cycle defect in which arginase deficiency leads to toxic arginine accumulation; exogenous arginine supplementation would exacerbate this condition.

Duration of Use

The duration of treatment for standard Sargenor® formulations is limited to 15 days in licensed pharmaceutical use. For the Prelox® formulation studied in ED and fertility trials, study durations ranged from 1 to 6 months with no observed adverse events reported in those trials, though systematic long-term safety data remain limited.

References

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Arginine aspartate is a salt of L-arginine and aspartic acid; aspartate participates directly in the argininosuccinate synthase reaction regenerating arginine for eNOS-mediated NO synthesis. Preclinical data show aspartate combined with malate elevates L-arginine and NO production in hypertension models, complementing the established arginine-to-NO mechanism.

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