Drug information of کافئین

کافئین

Drug group:

Caffeine is a central nervous system stimulant. It works by stimulating the brain. Caffeine is found naturally in foods and beverages such as coffee, tea, colas, energy and chocolate. Botanical sources of caffeine include kola nuts, guarana, and yerba mate. Caffeine is also available in prescription and non-prescription medications.
Caffeine is used to restore mental alertness or wakefulness during fatigue or drowsiness. Caffeine is also found in some headache and migraine medications, in certain dietary supplements used for weight loss, and in many popular energy drinks.
Caffeine citrate (Cafcit) is available by prescription only. It is used for short-term treatment of neonatal apnea (breathing problems).
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Mechanism of effect

Increases levels of 3'5' cyclic AMP by inhibiting phosphodiesterase; CNS stimulant which increases medullary respiratory center sensitivity to carbon dioxide, stimulates central inspiratory drive, and improves skeletal muscle contraction (diaphragmatic contractility); prevention of apnea may occur by competitive inhibition of adenosine

Pharmacodynamic

  • Central Nervous System Stimulant
  • Phosphodiesterase Enzyme Inhibitor, Nonselective

Pharmacokinetics

Distribution
Vd: Neonates: 0.8 to 0.9 L/kg;
Adults: 0.6 L/kg.
Metabolism
Hepatic, via demethylation by CYP1A2.
Note: In neonates, interconversion between caffeine and theophylline has been reported (caffeine levels are ~25% of measured theophylline after theophylline administration and ~3% to 8% of caffeine would be expected to be converted to theophylline)
Excretion
Neonates: Urine (86% unchanged).
Infants ≥9 months, Children, Adolescents, and Adults: Urine (1% unchanged).
Time to Peak
Serum: Preterm neonates: Oral: 30 minutes to 2 hours.
Half-Life Elimination
Neonates: 72 to 96 hours.
Infants ≥9 months, Children, Adolescents, and Adults: 5 hours.
Protein Binding
36%.

Drug indications

Use: Labeled Indications
Caffeine citrate: Treatment of idiopathic apnea of prematurity
Caffeine and sodium benzoate: See Off-Label uses.
Caffeine [OTC labeling]: Restore mental alertness or wakefulness when experiencing fatigue

Dosage

Usual Pediatric Dose for Apnea of Prematurity
Caffeine Citrate:
28 Weeks to Less Than 33 Weeks Gestational Age:
-Loading Dose: 20 mg/kg IV over 30 minutes one time.
-Maintenance Dose: 5 mg/kg orally or IV over 10 minutes every 24 hours.
-Treatment Duration: Safety and efficacy of this drug for treatment of apnea of prematurity have not been established beyond 12 days.
Use: Short-term treatment of apnea of prematurity in infants.
Renal Dose Adjustments
Caffeine Citrate: Use with caution in infants with impaired renal function; monitor serum drug concentrations and adjust dose accordingly to avoid toxicity.
Liver Dose Adjustments
Caffeine Citrate: Use with caution in infants with impaired hepatic function; monitor serum drug concentrations and adjust dose accordingly to avoid toxicity.
Precautions
Safety and efficacy of caffeine citrate for treatment of apnea of prematurity have only been established in pediatric patients 28 weeks to less than 33 weeks gestational age.
Consult WARNINGS section for additional precautions.
Dialysis
Caffeine Citrate: Data not available.

Drug contraindications

Hypersensitivity to caffeine or any component of the formulation; sodium benzoate is not for use in neonates

Side effects

Side effects requiring immediate medical attention
Along with its needed effects, caffeine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur while taking caffeine:
More common
Feeding intolerance
Less common
Agitation
black, tarry stools
blood in the stools or urine
bruising
burning feeling or tenderness in the stomach
chills
coma
confusion
coughing or vomiting blood
decreased urine output
depression
dizziness
fainting
fast heartbeat
fever
headache
hostility
indigestion
irritability
lethargy
lightheadedness
muscle twitching
nausea
persistent bleeding
rapid, shallow breathing
rapid weight gain
rash
seizures
severe stomach pain
stomach upset
stupor
swelling of the face, ankles, or hands
trouble breathing
unusual tiredness or weakness
vomiting
vomiting of blood or material that looks like coffee grounds
Get emergency help immediately if any of the following symptoms of overdose occur while taking caffeine:
Symptoms of overdose
Irritability
nervousness
rapid heartbeat
trouble sleeping

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Alerts

Warnings/Precautions
Disease-related concerns:
• Anxiety: Avoid use in patients with anxiety, agitation, or tremor.
• Cardiovascular disease: Use with caution in patients with cardiovascular disease; avoid use in patients with symptomatic cardiac arrhythmias.
• Gastrointestinal disease: Use with caution in patients with a history of peptic ulcer and/or gastroesophageal reflux.
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• Renal impairment: Use with caution in patients with renal impairment.
• Seizure disorder: Use with caution in patients with a history of seizure disorder; may lower seizure threshold leading to new onset or breakthrough seizure activity.
Dosage form specific issues:
• OTC products: OTC products contain 200 mg of caffeine per tablet approximately the amount of caffeine similar to one cup of coffee; limit the use of other caffeine-containing beverages or foods.
• Product interchangeability: Caffeine citrate should not be interchanged with caffeine and sodium benzoate.
Other warnings and precautions:
• Transcutaneous electrical nerve stimulation: Analgesia from transcutaneous electrical nerve stimulation may be lessened with concomitant caffeine use (Marchand 1995).

Points of recommendation

May be administered without regard to feedings or meals. May administer injectable formulation (caffeine citrate) orally.

Pregnancy level

AU TGA pregnancy category: A
US FDA pregnancy category: C

Breast feeding warning

Caffeine appears in breastmilk rapidly after maternal ingestion as it readily crosses the placenta into the fetal circulation. Fussiness, jitteriness and poor sleep patterns have been reported in the infants of mothers with very high caffeine intakes (equivalent to about 10 or more cups of coffee per day). Studies in mothers taking 5 cups of coffee per day found no stimulatory effects in infants 3 weeks of age or older. Preterm and younger newborn infants metabolize caffeine very slowly and therefore a lower maternal intake is preferable. Coffee intake of more than 450 mL daily may decrease breastmilk iron concentrations and result in mild iron deficiency anemia in some breastfed infants.
Caution is recommended
Excreted into human milk: Yes

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