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The caffeine citrate injection, used for apnea of the premature newborn, was initially approved by the FDA in . 19 According to an article from , 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. 5 Caffeine is beneficial in preventing and treating apnea and bronchopulmonary dysplasia in newborns, improving the quality of life of premature infants. 12
Caffeine 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. Caffeine is similar in chemical structure to Theophylline and Theobromine . 4 , 16 It can be sourced from coffee beans, but also occurs naturally in various teas and cacao beans, which are different than coffee beans. 12 Caffeine is also used in a variety of cosmetic products and can be administered topically, orally, by inhalation, or by injection. 12
Caffeine 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.
- Indication
- Associated Conditions
- Associated Therapies
- Contraindications & Blackbox Warnings
- Pharmacodynamics
Caffeine 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.1,12,18 Caffeine 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.12
- Mechanism of action
- Absorption
Caffeine is rapidly absorbed after oral or parenteral administration, reaching peak plasma concentration within 30 minutes to 2 hours after administration.10 After oral administration, onset of action takes place within 45 to 1 hour.15 Food may delay caffeine absorption. The peak plasma level for caffeine ranges from 6-10mg/L.16 The absolute bioavailability is unavailable in neonates16, but reaches about 100% in adults.12
- Volume of distribution
Caffeine has the ability to rapidly cross the blood-brain barrier. It is water and fat soluble and distributes throughout the body.12,14,16 Caffeine 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.16
- 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.14,16
- Metabolism
Caffeine metabolism occurs mainly in the liver via the cytochrome CYP1A2 enzyme.10 The products of caffeine metabolism include paraxanthine, theobromine, and theophylline. The first step of caffeine metabolism is demethylation, yielding paraxanthine (a major metabolite), followed by theobromine, and theophylline, which are both minor metabolites. They are then excreted in urine as urates after additional metabolism.10,12,16 The enzymes xanthine oxidase and N-acetyltransferase 2 (NAT2) also participate in the metabolism of caffeine.10
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- Route of elimination
The major metabolites of caffeine can be found excreted in the urine.12 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.14,10
- 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.12,14
- Clearance
The clearance of caffeine varies, but on average, is about 0.078&#;L/kg/h (1.3&#;mL/min/kg).10,14
- Adverse Effects
- Toxicity
The oral LD50 of caffeine in rats is 192 mg/kg.MSDS An acute fatal overdose of caffeine in humans is about 10&#;14 grams (equivalent to 150&#;200 mg/kg of body weight).14
Caffeine 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.16 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.8
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.12
- Pathways
- PathwayCategoryCaffeine MetabolismMetabolic
- Pharmacogenomic Effects/ADRs
- Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetailsCytochrome P450 1A2
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(C;C)
/
(A;C)
C alleleADR
Directly Studied
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Patients with this genotype have increased risk of a non-fatal myocardial infarction with caffeineDetails
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