Peri-Workout Supplements The Complete Pre-, Intra- & Post-Workout Guide Part 2
Caffeine (1,3,7-trimethylxanthine)
Caffeine is the most commonly used over-the-counter stimulant drug in the world - and for good reason (9). Caffeine is an organic, alkaline substance and a derivative of xanthine. It is primarily found in tea leaves, coffee beans, guarana, various fruits and other sources. Its sister compounds -- theobromine (aka 3,7-dimethylxanthine) and theophylline (aka 1,3-dimethylxanthine) - are primarily found in kola nuts and the cocoa plant. Caffeine is readily available, cheap, relatively safe (when used correctly) and an exceptional performance-enhancing compound.
How does caffeine work?
Caffeine acts as a central nervous system and cardiac stimulant and is often used therapeutically to relieve conditions such as COPD and asthma due to its bronchodilator properties.
It acts as an acetylcholinesterase and phosphodiesterase (PDE) inhibitor, although we are more interested in the latter from a performance enhancement perspective. PDE enzymes are used to break down phosphodiester bonds such as those in cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP).
cAMP and cGMP transmit signals from different hormones and other substrates from cell membrane receptors to intracellular target molecules. When these signals are amplified by cAMP and cGMP, metabolic processes are accelerated and this can have dramatic effects on physical and psychological performance.
Primary benefits (10, 11, 12)
- Stimulates carbohydrate metabolism
- Can support fat loss by increasing fat oxidation
- Provides mental stimulation by increasing epinephrine (adrenaline) levels
- Increases oxygen uptake by dilating the bronchi
- Reduces muscle interstitial potassium levels
Possible side effects (usually dose-dependent)
Keeping caffeine intake within the recommended dosage range and using caffeine cyclically should reduce most of these side effects:
- Dehydration, cramping, digestive discomfort
- Headaches, nausea, dizziness
- Frequent urination (caffeine is a diuretic)
- Palpitations
- Increased blood pressure
- Mental problems such as irritability, anxiety, nervousness, depression, etc.
- Reduced fine motor skills
Note: Caffeine is toxic in exceptionally high doses (>5 grams per day) and may even be fatal. For this reason, caffeine should be used like any other drug and not abused.
Who should use caffeine and who should avoid it?
- Bodybuilders
- powerlifters
- Endurance athletes
- Those who are looking for a mental boost
- People suffering from a medical condition (especially heart disease) should avoid caffeine without first consulting their doctor
Recommended time of intake
Caffeine is a relatively fast-acting substance with a short half-life (about 4 to 6 hours assuming your liver is functioning properly), which is why it is recommended to take caffeine about 30 to 60 minutes before training or competition.
If you take caffeine on an empty stomach, it can also be taken 10 to 15 minutes before training, as food slows absorption somewhat. If you prefer to have a pre-workout meal, then I would aim to take the caffeine about one to two hours after said meal (this should help minimize any potential digestive discomfort).
If you train late in the evening, it is advisable to avoid caffeine or limit your caffeine intake, otherwise you may experience sleep disturbances.
Recommended dosage
The general recommended dose to increase performance is 1 to 3 mg of caffeine per kilogram of body weight (13).
Example: If you are an 81 kilogram athlete, your recommended dosage range is between 80 and 240 mg. Within this range, the optimal dosage should be determined by trial and error based on individual goals and individual tolerance.
Cyclical use of caffeine to avoid desensitization
Caffeine can be addictive and the dosage required to enhance performance increases gradually as a habituation effect occurs. This is the reason why most coffee drinkers can drink a triple espresso without feeling anything or only experience a short-lived boost followed by a slump 20 minutes later. When you reach such a point, it is highly recommended to gradually reduce your caffeine intake or to give up caffeine completely from one day to the next (if you can live with the possible withdrawal symptoms for a few days).
The time it takes for your body to wean itself off is not exactly known as there are too many variables at play. A general recommendation is that every 8 to 12 weeks of caffeine use should be followed by 1 to 2 weeks without caffeine (and without other stimulants).
Again, this is a matter of trial and error. If you feel you tolerate caffeine well and are still experiencing positive effects after 4 or 5 months, then listen to your body and continue to use caffeine. If, on the other hand, you feel terrible after just three weeks of caffeine supplementation (with or without your daily dose), then it's time to rethink your approach and reduce or eliminate your caffeine intake for a while.
Caffeine FAQs:
Q: Since caffeine is a diuretic and creatine promotes water retention, I wonder if you can only use one of the two at a time.
A: No. In fact, caffeine has been shown to promote creatine absorption (14). Of course, you need to make sure you stay hydrated.
Q: Does it matter which source of caffeine (coffee, capsules or powder, tea, etc.) I use?
A: No, caffeine is a chemical and synthetic and organic versions work completely identically.
Q: Should I use several servings of caffeine throughout the day or should I only take one large dose per day?
A: This is entirely up to you. It also depends on how much caffeine you plan to take, as large doses of caffeine at once can cause many of the side effects mentioned earlier.
Q: I drink quite a lot of caffeine every day. How do I know if I'm addicted to caffeine?
A: Simply abstain from coffee for a few days and see if you experience a significant decrease in your cognitive and physical performance. If this is the case, then it's time to give up caffeine for a period of time.
Beta-alanine
Structurally speaking, the amino acid alanine exists in the form of two different isomers. Alpha-alanine is one of the 20 amino acids found in many body proteins, while beta-alanine is not used in enzymes or in any protein biosynthesis pathways. Instead, beta-alanine is primarily found in naturally occurring peptides such as anserine and carnosine. The latter is an important dipeptide (consisting of histidine and beta-alanine) in muscle cells, the amount of which is limited by the availability of beta-alanine. Therefore, beta-alanine provides benefits for athletes who are looking to increase their anaerobic and aerobic performance by increasing the concentration of carnosine in their muscles. In addition, beta-alanine is inexpensive and well tolerated.
How does beta-alanine work?
The majority of studies that have concluded that beta-alanine has benefits for athletic performance have shown that this effect is the result of an increase in carnosine levels in muscle tissue (15). The mechanism by which carnosine enhances athletic performance is through the increased buffering capacity in working muscles, which delays the onset of muscle fatigue (16).
Primary benefits
- Increases intracellular carnosine levels
- Delays the onset of muscle fatigue (15)
- Increases the capacity of muscles to perform work, which subsequently supports muscle anabolism (16)
- Promotes vasodilation/pump as carnosine stimulates NO synthase production
Possible side effects
- The primary side effect of beta-alanine is paresthesia, also known as "beta-alanine tingling". This is variable among users and seems to subside by finding the right dosage.
Who should use beta-alanine and who should avoid it?
- Mainly those who perform anaerobically demanding sports such as sprinting or purely training with weights
- bodybuilders
- Powerlifters
- Possibly also those who perform aerobically demanding sports such as long distance running, but there is limited data to support this aspect
Recommended time of intake
Beta-alanine is similar to creatine in that its effects only occur when muscle carnosine levels are significantly elevated, which can take days or weeks. For this reason, it makes sense to consume beta-alanine at times other than around your workout, but for convenience it is usually easier to simply combine it with your other training supplements.
Recommended dosage
- A base dosage of 10 mg per kilogram of body weight should be used to assess individual tolerance. From this dosage, the daily dosage can be gradually increased to 3 to 6 grams per day.
Note: The daily dose should be divided into several single doses so that you do not take too much at once. Large doses can cause paresthesia as a side effect.
Beta-Alanine FAQs:
Q: Why not just use a carnosine supplement instead of beta-alanine?
A: Carnosine is generally less effective than beta-alanine - both in terms of cost and effect (i.e. you would need to use a much higher dose of carnosine to increase intramuscular carnosine levels as much as you would by taking beta-alanine).
Q: I have been taking beta-alanine for a week with no noticeable effect. Should I stop taking it?
A: It can take several weeks for the full effects of beta-alanine to kick in. Therefore, you should give beta-alanine a month or two before making a decision about whether or not to continue using it.
Q: Will this beta-alanine tingling ever go away?
A: The paresthesia caused by bata-alanine can occur every time you take it. However, this side effect usually diminishes over time and can also be reduced with smaller single doses.
L-citrulline (malate)
Citrulline is an alpha amino acid that does not occur in muscle protein but is found in certain proteins. Citrulline can be produced as a by-product of arginine oxidation and the uric acid cycle. It is found in small amounts in the rind of the watermelon and is a popular supplement.
Citrulline has been shown to work synergistically with a number of other supplements, making it the perfect component of a training supplement stack. It is also very safe and not expensive.
How does citrulline work?
The primary mechanism of action of citrulline is an enhancement of nitric oxide-dependent signaling (22). Oral citrulline supplementation has been shown to increase plasma arginine concentrations, thereby increasing the production of arginine metabolites (i.e. nitric oxide, nitrites, ornithine, creatinine, etc.) (22). It provides further benefits by increasing the utilization of other amino acids, particularly BCAAs.
Primary benefits
- Increases intracellular nitric oxide production, which acts as a positive regulator of blood flow and perfusion (23)
- Increases the utilization of essential amino acids during exercise (22)
- Increases the elimination of endotoxins (22)
- Increases growth hormone levels after resistance training more than a placebo (22)
- Reduces/inhibits the increase in plasma insulin levels that usually occurs after high-intensity exercise (24)
Possible side effects
- In some cases citrulline may cause stomach discomfort
Who should use citrulline and who should avoid it?
- Bodybuilders
- Athletes who do aerobic and/or anaerobic sports
- Powerlifters
- All those looking for increased blood flow and pump during training
Recommended time of intake?
- Ideally, citrulline should be taken around 15 to 30 minutes before training
- It can also be taken during and after training if desired
Recommended dosage
- Start with a dose of 6 to 7 grams per day
- If necessary, the dosage can be increased to 15 to 20 grams divided into several individual doses
Citrulline Malate FAQs:
Q: I have heard that citrulline can be taken on an empty stomach. Is this true?
A: In rare cases, taking citrulline with meals can cause digestive discomfort. It is perfectly fine to take citrulline with meals if you can tolerate it.
Q: How long does it usually take to feel the effects of citrulline?
A: This varies from person to person, but acute effects such as the removal of toxins will come about after the first dose. More latent benefits such as strength gains may take a few weeks.
Summary
This is by no means an exhaustive list of supplements you can consider using around your training, but more of a solid foundation that most active people can benefit from. Supplements are constantly evolving and it is certainly wise to try new products if you feel they may have potential benefits for you. Hopefully, these basic supplements can serve as a platform for you to perform better in the gym and achieve your health and fitness goals.
References:
- https://pubmed.ncbi.nlm.nih.gov/9458525/
- https://pubmed.ncbi.nlm.nih.gov/9368278/
- https://www.jbc.org/article/S0021-9258(18)99874-1/fulltext
- https://pubmed.ncbi.nlm.nih.gov/6031321/
- Buford TW, et al. International Society of Sports Nutrition position stand: creatine supplementation and exercise. J Int Soc Sports Nutr (2007).
- https://pubmed.ncbi.nlm.nih.gov/16365096/.
- https://pubmed.ncbi.nlm.nih.gov/22391631/
- https://jissn.biomedcentral.com/articles/10.1186/1550-2783-9-20
- https://www.newscientist.com/article/mg18725181-700-coffee-the-demon-drink/
- https://pubmed.ncbi.nlm.nih.gov/18714218/
- https://pubmed.ncbi.nlm.nih.gov/18708685/
- https://pubmed.ncbi.nlm.nih.gov/14634198/#:~:text=The%20present%20data%20demonstrated%20that,(%2B)%2DATPase%20pumps.
- https://pubmed.ncbi.nlm.nih.gov/22569090/
- https://pubmed.ncbi.nlm.nih.gov/9629989/
- https://pubmed.ncbi.nlm.nih.gov/20479615/
- https://pubmed.ncbi.nlm.nih.gov/20671038/
- https://pubmed.ncbi.nlm.nih.gov/19841932/
- https://pubmed.ncbi.nlm.nih.gov/17927294/
- https://www.researchgate.net/publication/24414844_Activation_of_I2-imidazoline_receptors_by_agmatine_improved_insulin_sensitivity_through_two_mechanisms_in_type-2_diabetic_rats
- https://pubmed.ncbi.nlm.nih.gov/19913596/
- http://www.sciencedirect.com/science/article/pii/S0014299999000606
- https://pubmed.ncbi.nlm.nih.gov/20499249
- https://www.researchgate.net/publication/225187246_Citrulline_a_More_Suitable_Substrate_than_Arginine_to_Restore_NO_Production_and_the_Microcirculation_during_Endotoxemia
- https://www.researchgate.net/publication/7101095_L-Citrulline_Reduces_Time_to_Exhaustion_and_Insulin_Response_to_a_Graded_Exercise_Test
Source: https://www.muscleandstrength.com/expert-guides/peri