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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Caffeine Citrate
Generic Name
Caffeine Citrate
Active Ingredient
CaffeineCategory
Barbiturate [EPC]
Variants
14
Different strengths and dosage forms
| Strength | Form | Route | NDC |
|---|---|---|---|
| 20 mg/mL | SOLUTION | INTRAVENOUS | 25021-601 |
| 20 mg/mL | INJECTION | INTRAVENOUS | 47335-289 |
| 20 mg/mL | INJECTION | INTRAVENOUS | 51754-0500 |
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Caffeine Citrate, you must consult a qualified healthcare professional.
| 20 mg/mL | SOLUTION | ORAL | 51754-0501 |
| 60 mg/3mL | INJECTION | INTRAVENOUS | 72485-104 |
| 20 mg/mL | INJECTION, SOLUTION | INTRAVENOUS | 63323-407 |
| 60 mg/3mL | SOLUTION | ORAL | 42571-346 |
| 20 mg/mL | INJECTION | INTRAVENOUS | 0641-6267 |
| 20 mg/mL | SOLUTION | ORAL | 63323-406 |
| 60 mg/3mL | INJECTION, SOLUTION | INTRAMUSCULAR, INTRAVENOUS | 42571-244 |
| 20 mg/mL | INJECTION, SOLUTION | INTRAVENOUS | 55150-187 |
| 20 mg/mL | SOLUTION | ORAL | 25021-602 |
+ 1 more variants
Detailed information about Caffeine Citrate
Caffeine is a methylxanthine central nervous system (CNS) stimulant primarily used to treat neonatal apnea and as an adjunct in pain management. It belongs to the methylxanthine class and works by antagonizing adenosine receptors to increase alertness and respiratory drive.
For the treatment of fatigue or drowsiness, OTC doses typically range from 100 mg to 200 mg every 3 to 4 hours as needed. When used as an adjunct for headaches, Caffeine is often administered in doses of 65 mg to 130 mg in combination with other analgesics. For respiratory depression, Caffeine and Sodium Benzoate may be administered intramuscularly or intravenously in doses of 250 mg to 500 mg.
In neonates (apnea of prematurity), the standard loading dose of Caffeine Citrate is 20 mg/kg (equivalent to 10 mg/kg of Caffeine base) administered intravenously or orally. This is followed by a maintenance dose of 5 mg/kg to 10 mg/kg once daily. Use in children for other indications must be strictly supervised by a pediatrician.
While Caffeine is primarily metabolized by the liver, its metabolites are excreted renally. In patients with severe renal impairment, there is a risk of metabolite accumulation; however, specific dose adjustment guidelines are not standardized. Monitoring for toxicity is recommended.
Since CYP1A2 is the primary metabolic pathway, patients with hepatic cirrhosis or severe liver dysfunction may experience a significantly prolonged Caffeine half-life. Dose reductions or extended intervals may be necessary.
Elderly patients may be more sensitive to the stimulant effects of Caffeine. Lower initial doses and careful monitoring for cardiovascular side effects (such as arrhythmias) are advised.
Oral Caffeine can be taken with or without food. If gastrointestinal upset occurs, taking it with a meal or milk may help. For neonatal use, the oral solution should be measured carefully with a calibrated syringe. Store all forms at room temperature away from moisture and heat. Do not use Caffeine products late in the evening if you experience insomnia.
If a dose is missed, it should be taken as soon as remembered. If it is almost time for the next scheduled dose, skip the missed dose. Do not double the dose to catch up.
Signs of acute Caffeine overdose include tremors, agitation, palpitations, rapid breathing, vomiting, and in severe cases, seizures or cardiac arrhythmias. In the event of a suspected overdose, contact a poison control center or seek emergency medical attention immediately.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose without medical guidance.
Commonly reported side effects include insomnia (difficulty falling or staying asleep), restlessness, nervousness, and irritability. Patients may also experience gastrointestinal symptoms such as nausea, epigastric pain, or increased gastric acid secretion, which can feel like a burning sensation in the chest or stomach.
Less frequent reactions include tachycardia (rapid heart rate), palpitations, diuresis (increased urination), and fine muscle tremors (particularly in the hands). Some patients may report flushing or lightheadedness shortly after administration.
Rare but documented effects include tinnitus (ringing in the ears), visual disturbances (scotomas), and hyperesthesia (increased sensitivity to touch or sound).
Caffeine should be used with caution in individuals with a history of peptic ulcers, as it stimulates gastric acid secretion. It is also a potent cardiovascular stimulant and should be monitored in patients with hypertension or pre-existing cardiac conditions. Patients should be aware that many over-the-counter products and beverages contain caffeine, which can lead to cumulative toxicity.
No FDA black box warnings for Caffeine.
There are few absolute contraindications; however, Caffeine should not be used with highly potent sympathomimetic amines (like certain high-dose stimulants) where the combination could lead to hypertensive crisis or fatal arrhythmias.
Caffeine is classified as FDA Pregnancy Category C. It readily crosses the placenta. While moderate consumption (less than 200 mg/day) is generally considered safe by the American College of Obstetricians and Gynecologists (ACOG, 2020), high doses have been associated with an increased risk of low birth weight and potentially miscarriage. Clinical use during pregnancy should only occur if the benefits clearly outweigh the risks.
Caffeine is excreted into breast milk in small amounts (typically less than 1% of the maternal dose). While generally compatible with breastfeeding, excessive maternal intake can cause irritability and poor sleeping patterns in the nursing infant. The American Academy of Pediatrics (AAP) suggests monitoring the infant for jitteriness.
Caffeine Citrate is specifically FDA-approved for the treatment of apnea of prematurity in neonates. It is not generally recommended for use as a stimulant in children under 12 years of age due to the risk of affecting developing nervous systems and sleep patterns.
Caffeine's primary mechanism is the competitive antagonism of adenosine receptors, particularly the A1 and A2A subtypes. Adenosine normally acts as a CNS depressant; by blocking these receptors, Caffeine increases the release of excitatory neurotransmitters like dopamine and glutamate. Furthermore, Caffeine acts as a competitive inhibitor of the enzyme phosphodiesterase (PDE). By inhibiting PDE, Caffeine prevents the breakdown of cyclic AMP (cAMP), leading to prolonged effects of catecholamines and relaxation of bronchial smooth muscle.
The onset of action for oral Caffeine is approximately 15 to 45 minutes, with peak effects occurring around 1 hour. The duration of effect typically lasts 3 to 5 hours in adults. In the respiratory system, Caffeine stimulates the respiratory center in the medulla, increases minute ventilation, and improves diaphragmatic contractility.
| Parameter | Value |
|---|---|
| Bioavailability | 99% |
Common questions about Caffeine Citrate
In a clinical setting, Caffeine is primarily used to treat apnea of prematurity, a condition where newborn babies stop breathing for short periods. It is also frequently added to pain relievers like acetaminophen or aspirin to increase their effectiveness in treating migraines and tension headaches. Additionally, healthcare providers may use it to treat respiratory depression in adults caused by certain drug overdoses. Beyond these uses, it is widely used over-the-counter to temporarily restore mental alertness or wakefulness when experiencing fatigue. Always consult your doctor before using medical-grade Caffeine for any condition.
The most frequently reported side effects of Caffeine include insomnia, nervousness, restlessness, and irritability. Many people also experience gastrointestinal issues such as nausea, stomach pain, or an increase in stomach acid. Physical symptoms like a rapid heart rate, palpitations, and muscle tremors, especially in the hands, are also quite common. These effects are usually dose-dependent, meaning they become more pronounced as the amount of Caffeine increases. If these symptoms become severe or persistent, you should contact your healthcare provider for guidance.
It is generally advised to avoid or strictly limit alcohol consumption while taking medicinal Caffeine. Alcohol can interfere with the way your liver processes Caffeine, which may lead to higher levels in your bloodstream and increased side effects like jitteriness and a racing heart. Furthermore, Caffeine can mask the sedative effects of alcohol, making you feel more alert than you actually are, which can lead to dangerous situations like impaired driving. This combination can also put additional strain on your cardiovascular system. Discuss your alcohol consumption habits with your doctor to ensure your safety.
According to the American College of Obstetricians and Gynecologists (ACOG), moderate caffeine consumption of less than 200 mg per day does not appear to be a major contributing factor in miscarriage or preterm birth. However, high doses of Caffeine readily cross the placenta and have been linked to lower birth weights in some studies. Because Caffeine can increase your heart rate and metabolism, it may also affect the developing fetus. Most healthcare providers recommend limiting intake as much as possible during pregnancy to minimize any potential risks. Always follow the specific advice provided by your obstetrician regarding Caffeine use.
When taken orally, Caffeine is absorbed very quickly by the body, with effects typically beginning within 15 to 45 minutes. The peak concentration in the bloodstream is usually reached between 30 minutes and two hours after ingestion. The speed of onset can be affected by whether you have recently eaten, as food in the stomach can slightly delay absorption. For intravenous forms used in hospitals, the onset of action is almost immediate. The effects generally last for about three to five hours in most healthy adults.
If you have been taking high doses of Caffeine regularly, stopping suddenly can lead to withdrawal symptoms. These symptoms often include severe headaches, significant fatigue, drowsiness, irritability, and sometimes even nausea or flu-like symptoms. Withdrawal usually begins 12 to 24 hours after the last dose and can last for several days. To avoid these unpleasant effects, healthcare providers typically recommend gradually reducing your intake over a week or two. If you are using Caffeine for a medical condition, do not stop taking it without first consulting your doctor.
If you miss a dose of Caffeine, you should take it as soon as you remember, provided it is not too close to your next scheduled dose. If it is almost time for your next dose, it is better to skip the missed one and continue with your regular schedule. You should never take two doses at once to make up for a missed one, as this increases the risk of side effects like tremors and palpitations. For parents administering Caffeine to infants, it is particularly important to stay on schedule and consult a pediatrician if multiple doses are missed. Consistency is key to maintaining therapeutic levels in the body.
Caffeine itself does not cause weight gain and is actually often included in weight loss supplements because it can slightly increase metabolism and fat burning. However, the way Caffeine is consumed can lead to weight gain if it comes from high-calorie sources like sugary sodas, energy drinks, or specialty coffee beverages with cream and sugar. Additionally, excessive Caffeine can disrupt sleep, and poor sleep is a known risk factor for weight gain and increased appetite. Some people may also experience increased cortisol levels with high Caffeine intake, which can theoretically influence fat storage. Focus on the source of your Caffeine and its impact on your overall lifestyle.
Caffeine can interact with a wide variety of medications, sometimes with serious consequences. For example, certain antibiotics like ciprofloxacin can slow down the removal of Caffeine from your body, leading to toxic levels. It can also interfere with medications for asthma, heart rhythm disorders, and depression. Because Caffeine is a stimulant, taking it with other stimulant drugs can dangerously increase your heart rate and blood pressure. It is essential to provide your doctor or pharmacist with a full list of all medications, including over-the-counter drugs and herbal supplements, before starting a Caffeine regimen.
Yes, Caffeine is widely available in various generic forms, which are typically much less expensive than brand-name products. Generic Caffeine Citrate is commonly used in hospitals for neonatal care, and generic Caffeine tablets are available over-the-counter for alertness. Generic versions are required by the FDA to have the same active ingredient, strength, and effectiveness as the brand-name versions. When buying over-the-counter, look for the 'Drug Facts' label to ensure you are getting the correct dosage. Your pharmacist can help you identify the most cost-effective generic option for your needs.
Other drugs with the same active ingredient (Caffeine)
> Warning: Stop taking Caffeine and call your doctor immediately if you experience any of these.
Prolonged use of high-dose Caffeine can lead to physical dependence and tolerance. Withdrawal symptoms, including severe headaches, fatigue, and depressed mood, typically occur within 12 to 24 hours after cessation. Long-term excessive intake may also exacerbate bone density loss in populations with low calcium intake.
There are currently no FDA black box warnings for Caffeine or Caffeine Citrate. However, clinicians are cautioned regarding its use in patients with underlying cardiovascular disease or seizure disorders.
Report any unusual symptoms to your healthcare provider.
For neonates treated for apnea of prematurity, serum Caffeine levels should be monitored to ensure they remain within the therapeutic range (typically 5–25 mcg/mL). In adults, routine lab tests are generally not required unless toxicity is suspected, in which case serum electrolytes and ECG monitoring may be indicated.
While Caffeine is intended to increase alertness, excessive doses can cause tremors or anxiety that may impair fine motor skills. Use caution until you know how the medication affects you.
Alcohol can slow the clearance of Caffeine from the body, potentially increasing its stimulant effects and side-profile. Conversely, Caffeine may mask the sedative effects of alcohol, leading to "wide-awake drunkenness," which increases the risk of injury.
Abrupt discontinuation after chronic use can result in a withdrawal syndrome characterized by headache, fatigue, and irritability. A gradual reduction in intake (tapering) is recommended for those consuming high daily amounts.
> Important: Discuss all your medical conditions with your healthcare provider before starting Caffeine.
Caffeine may cause falsely elevated results in tests for urinary catecholamines (VMA) and may interfere with pharmacological stress tests using dipyridamole or adenosine. Patients should avoid Caffeine for 24 hours prior to a cardiac stress test.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking.
Patients who are sensitive to other methylxanthines, such as theophylline or theobromine, may also exhibit sensitivity to Caffeine. There is no known cross-sensitivity with barbiturates or NSAIDs, though they are often co-formulated.
> Important: Your healthcare provider will evaluate your complete medical history before prescribing Caffeine.
Older adults may experience a slower clearance of Caffeine. There is an increased risk of sleep disturbances and cardiovascular sensitivity (e.g., palpitations) in this population. Monitoring for CNS and cardiac effects is essential.
In patients with end-stage renal disease (ESRD), the half-life of Caffeine may be altered, and the accumulation of metabolites is possible. No specific dose adjustments are provided in labeling, but clinical monitoring is advised.
Caffeine clearance is significantly reduced in patients with hepatic impairment, such as cirrhosis or hepatitis. According to studies published in the Journal of Hepatology, the half-life can exceed 60 hours in patients with severe liver disease, necessitating significant dose reductions.
> Important: Special populations require individualized medical assessment.
| Half-life | 3 - 7 hours (Adults); 65 - 100 hours (Neonates) |
| Tmax | 0.5 - 2 hours |
| Metabolism | Hepatic (CYP1A2) |
| Excretion | Renal (1% - 5% unchanged) |
Caffeine is a methylxanthine derivative. It is classified as a Central Nervous System Stimulant [EPC] and a Respiratory Stimulant. It is chemically related to theophylline and theobromine.