Caffeine

Pronunciation

Pronunciation: KAF-een
Class: Analeptic

Trade Names

Caffedrine
- Tablets 200 mg

Maximum Strength NoDoz
- Tablets 200 mg

Stay Awake
- Tablets 200 mg

Vivarin
- Tablets 200 mg

Keep Alert
- Tablets 200 mg

357 HR Magnum
- Tablets 200 mg

Overtime
- Tablets 200 mg

20–20
- Tablets 200 mg

Valentine
- Tablets 200 mg

Keep Going
- Tablets 200 mg

Molie
- Capsules 200 mg

Fastlene
- Capsules 200 mg

Enerjets
- Lozenges 75 mg

Cafcit
- Oral solution 20 mg/mL (caffeine citrate; 2 mg caffeine citrate is equivalent to 1 mg caffeine base)
- Injection 20 mg/mL (caffeine citrate; 2 mg caffeine citrate is equivalent to 1 mg caffeine base)

Wake Ups (Canada)

Pharmacology

Increases calcium permeability in sarcoplasmic reticulum, inhibiting phosphodiesterase-promoting accumulation of cyclic AMP.

Slideshow: OTC Medication Use In Pregnancy: Wise or Worrisome?

Pharmacokinetics

Absorption

99% absorbed orally. C max is 5 to 25 mcg/mL; T max is 15 to 120 min.

Distribution

Rapidly distributed throughout tissues; crosses the blood-brain barrier and placenta; excreted in breast milk. 17% to 36% protein bound. Vd is 0.64 kg.

Metabolism

Rapidly metabolized in the liver to 1-methyluric acid, 1-methylxanthine, and 7-methylxanthine; CYP1A2 is involved in the biotransformation.

Elimination

The t ½ is 3 to 5 h. Approximately 1% is excreted in the urine as unchanged drug.

Special Populations

Pregnancy, smoking, and cirrhosis

The t ½ is increased.

Indications and Usage

Fatigue and drowsiness; analgesia; apnea of prematurity; respiratory depression.

Contraindications

Caffeine and sodium benzoate solution in pediatrics.

Dosage and Administration

Fatigue/Drowsiness
Adults and children (older than 12 yr of age)

PO 100 to 200 mg every 3 to 4 h as needed.

Apnea of Prematurity
Preterm infants Loading dose (caffeine citrate)

IV 20 mg/kg (1 mL/kg) over 30 min once.

Maintenance dose (caffeine citrate)

IV (over 10 min) or PO 5 mg/kg (0.25 mL/kg) every 24 h.

General Advice

  • Do not administer tablets, capsules, or lozenges late in the day to avoid insomnia.

Storage/Stability

Store capsules, tablets, lozenges, and oral solution at controlled room temperature (59° to 86°F). Keep oral solution tightly capped. Citrated caffeine parenteral solution may be stored for up to 24 h at room temperature following dilution.

Drug Interactions

Aspirin, clozapine, theophylline

Plasma levels of these agents may be elevated by caffeine, increasing their pharmacologic effects and adverse reactions.

Cimetidine, disulfiram, fluoroquinolones, mexiletine, oral contraceptives

May increase caffeine levels, enhancing the effects.

Lithium

Plasma levels may be reduced by caffeine, decreasing the pharmacologic effect.

Phenytoin, smoking

May decrease caffeine levels.

Laboratory Test Interactions

False-positive elevations in serum urate measured by Bittner method; may increase urine levels of vanillymandelic acid, catecholamines, and 5-hydroxyindoleacetic acid, resulting in false-positive diagnosis of pheochromocytoma and neuroblastoma.

Adverse Reactions

Cardiovascular

Tachycardia; extrasystoles; palpitations; other cardiac arrhythmias.

CNS

Insomnia; restlessness; excitement; nervousness; tinnitus; scintillating scotoma; muscular tremor; headache; lightheadedness.

Dermatologic

Urticaria; rash, dry skin, skin breakdown (caffeine citrate).

EENT

Retinopathy of prematurity (caffeine citrate).

GI

Vomiting; nausea; diarrhea; stomach pain; necrotizing enterocolitis, gastritis, GI hemorrhage (caffeine citrate).

Genitourinary

Diuresis; kidney failure (caffeine citrate).

Hematologic

Disseminated intravascular coagulation (caffeine citrate).

Metabolic

Hyperglycemia; acidosis (caffeine citrate).

Respiratory

Dyspnea, lung edema (caffeine citrate).

Miscellaneous

Hypersensitivity (eg, dermatitis, rhinitis, bronchial asthma); feeding intolerance, sepsis, accidental injury, hemorrhage, cerebral hemorrhage (caffeine citrate).

Precautions

Monitor

Apnea

Monitor neonates for apnea events and notify health care provider if noted.

Caffeine intake

Note concurrent use of caffeine-containing beverages, foods, dietary supplements, or OTC products.

Neonate caffeine serum levels

Ensure that caffeine serum levels have been determined in neonates who have been treated with theophylline before starting caffeine citrate therapy for apnea.


Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Caffeine and sodium benzoate injection is contraindicated in children.

Necrotizing enterocolitis

Other methylxanthines have been associated with development of necrotizing enterocolitis.

Depression

Too-vigorous treatment with parenteral caffeine can worsen depression.

GI effects

Caffeine may aggravate diarrhea in patients with irritable colon or exacerbate duodenal ulcers.

Seizure disorder

Seizures have been reported with caffeine overdose; use caffeine citrate with caution in infants with seizure disorders.

CV disease

Caffeine can increase heart rate, left ventricular output, and stroke volume; use caffeine citrate with caution in infants with CV disease.

Metabolic effects

Caffeine stimulates glycogenolysis and lipolysis, which increases free fatty acids and produces hyperglycemia.

Bone mineral density

Caffeine is associated with decreased bone density.

Withdrawal

Symptoms may occur within 12 h after cessation of chronic caffeine ingestion and persist up to 7 days.

Overdosage

Symptoms

Vomiting, myoclonus, agitation, myocardial irritability, cardiac arrhythmia, seizures, hematemesis, opisthotonus, decerebrate posturing, generalized muscular hypertonicity, rhabdomyolysis with renal failure, pulmonary edema, hyperglycemia; hypokalemia, leukocytosis, ketosis, metabolic acidosis, death.

Patient Information

  • Caution patient to not exceed recommended dose.
  • Inform patient that caffeine is not a substitute for normal sleep.
  • Advise pregnant women to limit intake of caffeine and caffeine-containing beverages to a minimum.
  • Warn patient that withdrawal symptoms may occur within 12 to 24 h following cessation of chronic caffeine ingestion. Symptoms consist of headache, fatigue, depression, anxiety or insomnia and may last for up to 7 days.
  • Advise patient to discontinue use if increased or abnormal heart rate, palpitations, dizziness, agitation, nervousness, or insomnia occur.
  • Caffeine citrate
  • Instruct parents or caregiver in proper measurement of dose.
  • Caution parents or caregiver that if baby continues to have apnea events to contact the baby's health care provider and to not increase the dose of caffeine citrate unless advised to do so by health care provider.
  • Advise parents or caregivers to contact the baby's health care provider if the baby seems lethargic or develops abdominal distention, vomiting, or bloody stools.

Copyright © 2009 Wolters Kluwer Health.

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