Coffein-benzoate sodium
Coffein-benzoate sodium Uses, Dosage, Side Effects, Food Interaction and all others data.
Coffein-benzoate sodium is a drug of the methylxanthine class used for a variety of purposes, including certain respiratory conditions of the premature newborn, pain relief, and to combat drowsiness. Coffein-benzoate sodium is similar in chemical structure to Theophylline and Theobromine. It can be sourced from coffee beans, but also occurs naturally in various teas and cacao beans, which are different than coffee beans. Coffein-benzoate sodium is also used in a variety of cosmetic products and can be administered topically, orally, by inhalation, or by injection.
The caffeine citrate injection, used for apnea of the premature newborn, was initially approved by the FDA in 1999. According to an article from 2017, more than 15 million babies are born prematurely worldwide. This correlates to about 1 in 10 births. Premature birth can lead to apnea and bronchopulmonary dysplasia, a condition that interferes with lung development and may eventually cause asthma or early onset emphysema in those born prematurely. Coffein-benzoate sodium is beneficial in preventing and treating apnea and bronchopulmonary dysplasia in newborns, improving the quality of life of premature infants.
Coffein-benzoate sodium stimulates the central nervous system (CNS), heightening alertness, and sometimes causing restlessness and agitation. It relaxes smooth muscle, stimulates the contraction of cardiac muscle, and enhances athletic performance. Coffein-benzoate sodium promotes gastric acid secretion and increases gastrointestinal motility. It is often combined in products with analgesics and ergot alkaloids, relieving the symptoms of migraine and other types of headaches. Finally, caffeine acts as a mild diuretic.
| Trade Name | Coffein-benzoate sodium |
| Availability | Rx and/or OTC |
| Generic | Caffeine |
| Caffeine Other Names | 1-methyltheobromine, 7-methyltheophylline, Cafeína, Caféine, Caffeine, Caffeinum, Coffein, Coffeinum, Guaranine, Koffein, Mateína, Methyltheobromine, Teína, Thein, Theine |
| Related Drugs | theophylline, aminophylline, Alert, Theo-Dur, Theo-24, Vivarin, Quibron-T/SR, Uniphyl, Cafcit |
| Type | |
| Formula | C8H10N4O2 |
| Weight | Average: 194.1906 Monoisotopic: 194.080375584 |
| Protein binding | Plasma protein binding of caffeine has not been determined for neonates or infants. In vitro studies indicate a protein binding of about 10%-36%. Caffeine is reversibly bound to plasma proteins. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Coffein-benzoate sodium is a stimulant present in tea, coffee, cola beverages, analgesic drugs, and agents used to increase alertness. It is also used in to prevent and treat pulmonary complications of premature birth.
Coffein-benzoate sodium is indicated for the short term treatment of apnea of prematurity in infants and off label for the prevention and treatment of bronchopulmonary dysplasia caused by premature birth. In addition, it is indicated in combination with sodium benzoate to treat respiratory depression resulting from an overdose with CNS depressant drugs. Coffein-benzoate sodium has a broad range of over the counter uses, and is found in energy supplements, athletic enhancement products, pain relief products, as well as cosmetic products.
Coffein-benzoate sodium is also used to associated treatment for these conditions: Bronchopulmonary Dysplasia (BPD), Common Cold, Dark circles under eyes, Dyspepsia, Fatigue, Fever, Flu caused by Influenza, Headache, Migraine, Pain, Pain, Acute, Pain, Menstrual, Primary apnea of premature newborns, Respiratory Depression, Rheumatic Pain, Somnolence, Soreness, Muscle, Tension Headache, Toothache, Moderate Pain, Analgesia, Antacid therapy, Athletic Performance
How Coffein-benzoate sodium works
The mechanism of action of caffeine is complex, as it impacts several body systems, which are listed below. The effects as they relate to various body systems are described as follows:
General and cellular actions
Coffein-benzoate sodium exerts several actions on cells, but the clinical relevance is poorly understood. One probable mechanism is the inhibition of nucleotide phosphodiesterase enzymes, adenosine receptors, regulation of calcium handling in cells, and participates in adenosine receptor antagonism. Phosphodiesterase enzymes regulate cell function via actions on second messengers cAMP and cGMP. This causes lipolysis through activation of hormone-sensitive lipases, releasing fatty acids and glycerol.
Respiratory
The exact mechanism of action of caffeine in treating apnea related to prematurity is unknown, however, there are several proposed mechanisms, including respiratory center stimulation in the central nervous system, a reduced threshold to hypercapnia with increased response, and increased consumption of oxygen, among others. The blocking of the adenosine receptors enhances respiratory drive via an increase in brain medullary response to carbon dioxide, stimulating ventilation and respiratory drive, while increasing contractility of the diaphragm.
Central nervous system
Coffein-benzoate sodium demonstrates antagonism of all 4 adenosine receptor subtypes (A1, A2a, A2b, A3) in the central nervous system. Coffein-benzoate sodium's effects on alertness and combatting drowsiness are specifically related to the antagonism of the A2a receptor.
Renal system
Coffein-benzoate sodium has diuretic effects due to is stimulatory effects on renal blood flow, increase in glomerular filtration, and increase in sodium excretion.
Cardiovascular system
Adenosine receptor antagonism at the A1 receptor by caffeine stimulates inotropic effects in the heart. Blocking of adenosine receptors promotes catecholamine release, leading to stimulatory effects occurring in the heart and the rest of the body. In the blood vessels, caffeine exerts direct antagonism of adenosine receptors, causing vasodilation. It stimulates the endothelial cells in the blood vessel wall to release nitric oxide, potentiating blood vessel relaxation. Catecholamine release, however, antagonizes this and exerts inotropic and chronotropic effects on the heart, ultimately leading to vasoconstriction. Finally, caffeine is shown to raise systolic blood pressure measurements by 5 to 10 mmHg when it is not taken regularly, versus no effect in those who consume it regularly. The vasoconstricting effects of caffeine are beneficial in migraines and other types of headache, which are normally caused by vasodilation in the brain.
Toxicity
The oral LD50 of caffeine in rats is 192 mg/kg. An acute fatal overdose of caffeine in humans is about 10–14 grams (equivalent to 150–200 mg/kg of body weight).
Coffein-benzoate sodium overdose
In the case of caffeine overdose, seizures may occur, as caffeine is a central nervous system stimulant. It should be used with extreme caution in those with epilepsy or other seizure disorders. Symptoms of overdose may include nausea, vomiting, diarrhea, and gastrointestinal upset. Intoxication with caffeine is included in the World Health Organization’s International Classification of Diseases (ICD-10). Agitation, anxiety, restlessness, insomnia, tachycardia, tremors, tachycardia, psychomotor agitation, and, in some cases, death can occur, depending on the amount of caffeine consumed. Overdose is more likely to occur in individuals who do not consume caffeine regularly but consume energy drinks.
Overdose management
For a mild caffeine overdose, offer symptomatic treatment. In the case of a severe overdose, intubation for airway protection from changes in mental status or vomiting may be needed. Activated charcoal and hemodialysis can prevent further complications of an overdose and prevent absorption and metabolism. Benzodiazepine drugs can be administered to prevent or treat seizures. IV fluids and vasopressors may be necessary to combat hypotension associated with caffeine overdose. In addition, magnesium and beta blocking drugs can be used to treat arrhythmias that may occur, with defibrillation and resuscitation if the arrhythmias are lethal. Follow local ACLS protocols.
Food Interaction
No interactions found.[Minor] The effect of grapefruit juice on the pharmacologic activity of caffeine is controversial.
One report suggests that grapefruit juice increases the effect of caffeine.
The proposed mechanism is inhibition of cytochrome P-450 metabolism of caffeine.
However, a well-conducted pharmacokinetic The clinical significance of this potential interaction is unknown.
Coffein-benzoate sodium Hypertension interaction
[Major] The use of CNS stimulants is contraindicated in patients with significant cardiovascular impairment such as uncompensated heart failure, severe coronary disease, severe hypertension (including that associated with hyperthyroidism or pheochromocytoma), cardiac structural abnormalities, serious arrhythmias, etc.
Sudden death has been reported in adults and children taking CNS stimulant treatment.
Additionally, stroke, myocardial infarction, chest pain, syncope, arrhythmias and other symptoms have been reported in adults under treatment.
A careful assessment of the cardiovascular status should be done in patients being considered for treatment.
This includes family history, physical exam and further cardiac evaluation (EKG and echocardiogram).
Patients who develop symptoms should have a detailed cardiac evaluation and if needed, treatment should be suspended.
Hypertension interaction[Major] CNS stimulant medications have shown to increase blood pressure, and their use might be contraindicated in patients with severe hypertension.
Caution should be used when administering to patients with preexisting high blood pressure and other cardiovascular conditions.
All patients under treatment should be regularly monitored for changes in blood pressure and heart rate.
Hypertension interaction[Moderate] Like other methylxanthines, caffeine at high dosages may be associated with positive inotropic and chronotropic effects on the heart.
Coffein-benzoate sodium may also produce an increase in systemic vascular resistance, resulting in elevation of blood pressure.
Therapy with products containing caffeine should be administered cautiously in patients with severe cardiac disease, hypertension, hyperthyroidism, or acute myocardial injury.
Some clinicians recommend avoiding caffeine in patients with symptomatic cardiac arrhythmias and
Coffein-benzoate sodium Drug Interaction
Unknown: amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, contained in alcoholic beverages , contained in alcoholic beverages , diphenhydramine, diphenhydramine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, alprazolam, alprazolam, cetirizine, cetirizine
Coffein-benzoate sodium Disease Interaction
Major: cardiac disease, hypertension, liver disease, psychiatric disorders, PUDModerate: cardiotoxicity, bipolar disorders, psychotic disorders, renal dysfunction, seizure disorders, GERD
Volume of Distribution
Coffein-benzoate sodium has the ability to rapidly cross the blood-brain barrier. It is water and fat soluble and distributes throughout the body. Coffein-benzoate sodium concentrations in the cerebrospinal fluid of preterm newborns are similar to the concentrations found in the plasma. The mean volume of distribution of caffeine in infants is 0.8-0.9 L/kg and 0.6 L/kg in the adult population.
Elimination Route
Coffein-benzoate sodium is rapidly absorbed after oral or parenteral administration, reaching peak plasma concentration within 30 minutes to 2 hours after administration. After oral administration, onset of action takes place within 45 to 1 hour. Food may delay caffeine absorption. The peak plasma level for caffeine ranges from 6-10mg/L. The absolute bioavailability is unavailable in neonates, but reaches about 100% in adults.
Half Life
In an average-sized adult or child above the age of 9, the half-life of caffeine is approximately 5 hours. Various characteristics and conditions can alter caffeine half-life. It can be reduced by up to 50% in smokers. Pregnant women show an increased half-life of 15 hours or higher, especially in the third trimester. The half-life in newborns is prolonged to about 8 hours at full-term and 100 hours in premature infants, likely due to reduced ability to metabolize it. Liver disease or drugs that inhibit CYP1A2 can increase caffeine half-life.
Clearance
The clearance of caffeine varies, but on average, is about 0.078 L/kg/h (1.3 mL/min/kg).
Elimination Route
The major metabolites of caffeine can be found excreted in the urine. About 0.5% to 2% of a caffeine dose is found excreted in urine, as it because it is heavily absorbed in the renal tubules.
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