creatine

Action and Spectrum

Actions and spectrum: 

creatine is a naturally occurring nitrogen-containing compound synthesized in the liver, pancreas, and kidneys from three amino acids: arginine, glycine, and methionine. It plays a vital role in metabolism of energy, particularly in producing ATP (adenosine triphosphate), the primary energy source for muscle contraction. 

As a dietary supplement, creatine is commonly used by athletes and bodybuilders to increase strength, muscle mass and exercise performance. It is believed to work by increasing the availability of ATP for muscle contractions, reducing fatigue, and improving recovery time. 

In addition to its effects on muscle performance, creatine has also been studied for its potential therapeutic benefits in various conditions, including neurodegenerative diseases, cardiovascular disease, and diabetes. 

Drug Interaction

Adverse Reaction

Frequency defined 

arrhythmias, cardiomyopathy, diarrhea, ischemic stroke, nausea, rhabdomyolysis, weight gain, Abdominal pain, cardiac arrest, dehydration, hypertension, muscle cramping, renal dysfunction, seizures 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Kidney disease: Individuals with kidney disease or a history of kidney disease should not take creatine supplements without consulting their healthcare provider. 
• Liver disease: creatine can increase liver enzymes, so individuals with liver disease should use it with caution and only under medical supervision. 
• Diabetes: creatine can affect blood sugar levels and insulin sensitivity, so individuals with diabetes should use it with caution and only under medical supervision. 
• High blood pressure: creatine can increase blood pressure, so individuals with high blood pressure should use it with caution and only under medical supervision. 
• Pregnancy and breastfeeding: There is insufficient evidence regarding the safety of creatine supplements during pregnancy and breastfeeding, so it is not recommended. 
• Allergies: Individuals with allergies to creatine should avoid creatine supplements.

Caution: 

• Kidney problems: creatine can put a strain on the kidneys, particularly if taken in high doses or used for a long time. People with kidney problems should talk to their doctor before taking creatine. 
• Dehydration: creatine can retain water from the body, so it’s important to stay well hydrated when taking it. 
• Diabetes: creatine can affect blood sugar levels, people with diabetes should monitor blood sugar closely when taking creatine. 
• Breastfeeding and Pregnancy: There is not enough research to know whether creatine is safe during pregnancy or breastfeeding, so it’s best to avoid it during these times. 
• Children: creatine supplements are not recommended for children under 18, as not enough research has been done to confirm their safety.

Comorbidities: 

• • Kidney disease: creatine supplementation may increase the risk of kidney damage or exacerbate pre-existing kidney disease. 
  • Liver disease: creatine supplementation may increase liver enzymes in some individuals with liver disease. 
  • Diabetes: creatine may affect blood sugar levels, so caution is recommended in individuals with diabetes. 
  • Neurological conditions: creatine may worsen symptoms of Parkinson’s disease and Huntington’s disease. 
  • Pregnancy and breast-feeding: There is not enough information available on the safety of creatine supplementation during pregnancy or breastfeeding.

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

creatine gets synthesized in the liver, pancreas, and kidneys from the amino acids glycine, arginine, and methionine. It is primarily involved in the phosphagen energy system, which provides short bursts of energy for high-intensity activities such as weightlifting and sprinting. 

creatine is stored in the form of phosphocreatine in skeletal muscles, which can be quickly converted to ATP (adenosine triphosphate) to provide energy for muscle contractions. creatine along with supplementation has been shown to increase muscle strength and size, improve exercise performance, and enhance recovery from high-intensity exercise. It may also have potential therapeutic uses in neurodegenerative diseases, such as Parkinson’s and Huntington’s disease.  

Pharmacodynamics: 

creatine acts by replenishing the high-energy molecule ATP (adenosine triphosphate) in muscles during exercise, allowing for increased energy production and improved muscle performance. creatine shown to have neuroprotective and cardioprotective effects. It may also help increase muscle mass and improve recovery time after exercise. Some research also suggests that creatine supplementation may have potential benefits for neurological and cognitive function, as well as various medical conditions such as congestive heart failure and muscular dystrophy. 

The precise mechanism of action of creatine is not well known, but it is thought to involve increasing the availability of phosphocreatine, a key source of ATP, in muscle cells. This can help improve muscle function and delay fatigue during exercise. creatine may also have anti-inflammatory effects and promote muscle protein synthesis.  

Pharmacokinetics: 

Absorption 

creatine is an orally administered supplement that is rapidly absorbed from the small intestine. It is transported to the muscles via the bloodstream where it is taken up by the cells. 

Distribution 

creatine is distributed to various tissues, including skeletal muscle, heart, brain, and testes. The highest concentration of creatine is found in skeletal muscle, where it is stored as phosphocreatine. 

Metabolism 

creatine is metabolized in the body via several pathways. Approximately 1-2% of creatine is metabolized to creatinine per day and excreted in the urine. Another pathway involves the conversion of creatine-to-creatine phosphate, which can be used as an energy source by the body’s cells. creatine can also be converted to creatine kinase, which is involved in muscle contraction. 

Elimination and excretion 

creatine is mainly excreted by the kidneys in the form of creatinine. It is filtered by kidneys through blood and eliminated from the body in the urine. A small amount of creatine is excreted in the bile and feces. 

Adminstartion

Administration: 

creatine is commonly available as a dietary supplement in various forms such as powder, capsules, tablets, energy bars, and drink mixes. It is often taken orally by dissolving the powder in water or juice and drinking it.

The dosage and administration of creatine supplements may vary depending on the form, brand, and individual factors such as age, sex, weight, and physical activity level. creatine can also be obtained naturally from dietary sources such as meat, fish, and poultry. The average daily intake of creatine from food sources is about 1-2 grams. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: creatine 

Pronounced: [ KREE-a-teen]  

Why do we use creatine? 

• Neurological conditions: Some research suggests that creatine may have neuroprotective properties and could be beneficial for conditions such as Huntington’s disease, Parkinson’s disease, and traumatic brain injury. 
• Muscle wasting conditions: creatine may help to prevent muscle wasting in conditions such as cancer, HIV/AIDS, and muscular dystrophy. 
• Cardiovascular health: Creatine supplementation may help to reduce blood pressure and improve vascular health. 
• Diabetes: Some studies have shown that creatine supplementation may increase glucose tolerance and insulin sensitivity in people with type 2 diabetes.