CAFFEINE

CAFFEINE (kaf-een') Caffedrine, Dexitac, NoDoz, Quick Pep, S-250, Tirend, Vivarin CAFFEINE AND SODIUM BENZOATE CITRATED CAFFEINE Cafcit Classifications: respiratory and cerebral stimulant; xanthine; Therapeutic: respiratory and cerebral stimulant Pregnancy Category: C

Availability

100 mg, 150 mg, 200 mg tablets; 200 mg capsules; 10 mg/mL caffeine citrate oral solution; 10 mg/mL caffeine citrate injection

Action

Chief action is thought to be related to inhibition of the enzyme phosphodiesterase, which results in higher concentrations of cyclic AMP. Releases epinephrine and norepinephrine from adrenal medulla, producing CNS stimulation. Small doses improve psychic and sensory awareness and reduce drowsiness and fatigue by stimulating cerebral cortex. Higher doses stimulate medullary, respiratory, vasomotor, and vagal centers. Produces smooth muscle relaxation by direct action on vascular musculature. Mild diuretic action may result from increase in renal blood flow and glomerular filtration rate and decrease in renal tubular reabsorption of sodium and water.

Therapeutic Effect

Effective in managing neonatal apnea, and as an adjuvant for pain control in headaches and following dural puncture. Relief of headache is perhaps due to mild cerebral vasoconstriction action and increased vascular tone. It acts as a bronchodilator in asthma.

Uses

Orally as a mild CNS stimulant to aid in staying awake and restoring mental alertness, and as an adjunct in narcotic and nonnarcotic analgesia. Used parenterally as an emergency stimulant in acute circulatory failure, as a diuretic, and for neonatal apnea.

Unlabeled Uses

Topical treatment of atopic dermatitis; to releave spinal puncture headache.

Contraindications

Acute MI, symptomatic cardiac arrhythmias, palpitations; peptic ulcer; pulmonary disease; insomnia, panic attacks; pregnancy (category C). Safe use in children not established.

Cautious Use

Diabetes mellitus; hiatal hernia; psychotic disorders; dementia; depressive disorders; hepatic disease; hypertension with heart disease.

Route & Dosage

Mental Stimulant Adult: PO 100–200 mg q3–4h prn Circulatory Stimulant Adult: IM 200–500 mg prn Apnea of Prematurity (Caffeine Citrate Only) Neonate (28–33 wk gestation): PO/IV 20 mg/kg (loading dose); then, after 24 h, 5 mg/kg/d

Administration

Oral

• Give sustained-release oral preparations not less than 6 h before bedtime.
• Ensure that timed-release form of drug is not chewed or crushed. It must be swallowed whole.

Intramuscular

• Give deep IM into a large muscle.

Intravenous Note: IV route reserved for emergency situations only. PREPARE: IV Infusion: May be diluted for infusion in D5W.   ADMINISTER: IV Infusion: A syringe infusion pump is recommended. Give loading dose over 30 min and maintenance dose over at least 10 min.   INCOMPATIBILITIES Y-site: Acyclovir, furosemide, lorazepam, nitroglycerin, oxacillin, pantoprazole.

Adverse Effects (≥1%)

CV: Tingling of face, flushing, palpitation, tachycardia, arrhythmia, angina, ventricular ectopic beats. GI: Nausea, vomiting; epigastric discomfort, gastric irritation (oral form), diarrhea, hematemesis, kernicterus (neonates). CNS: Nervousness, insomnia, restlessness, irritability, confusion, agitation, fasciculations, delirium, twitching, tremors, clonic convulsions. Respiratory: Tachypnea. Special Senses: Scintillating scotomas, tinnitus. Urogenital: Increased urination, diuresis.

Diagnostic Test Interference

Caffeine reportedly may interfere with diagnosis of pheochromocytoma or neuroblastoma by increasing urinary excretion of catecholamines, VMA, and 5-HIAA and may cause false positive increases in serum urate (by Bittner method).

Interactions

Drug: Increases effects of cimetidine; increases cardiovascular stimulating effects of beta-adrenergic agonists; possibly increases theophylline toxicity.

Pharmacokinetics

Absorption: Rapid. Peak: 15–45 min. Distribution: Widely throughout body; crosses blood-brain barrier and placenta. Metabolism: In liver. Elimination: In urine as metabolites; excreted in breast milk in small amounts. Half-Life: 3–5 h in adults, 36–144 h in neonates.

Nursing Implications

Assessment & Drug Effects

• Monitor vital signs closely as large doses may cause intensification rather than reversal of severe drug-induced depressions.
• Observe children closely following administration as they are more susceptible than adults to the CNS effects of caffeine.
• Lab tests: Monitor blood glucose and HbA_1c levels in diabetics.

Patient & Family Education

• Caffeine in large amounts may impair glucose tolerance in diabetics.
• Do not consume large amounts of caffeine as headache, dizziness, anxiety, irritability, nervousness, and muscle tension may result from excessive use, as well as from abrupt withdrawal of coffee (or oral caffeine). Withdrawal symptoms usually occur 12–18 h following last coffee intake.

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Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug