Indications
PO, IV: Treatment of: Mild to moderate pain, Fever.
PO: Treatment of: Inflammatory disorders including
rheumatoid arthritis (including juvenile) and osteoarthritis,
Dysmenorrhea. IV: Moderate to severe pain with
opioid analgesics. Closure of a clinically significant PDA
in neonates weighing 500–1500 g and 32 wk gestational
age (ibuprofen lysine only)
Action
Inhibits prostaglandin synthesis. Therapeutic Effects:
Decreased pain and inflammation. Reduction of fever.
Pharmacokinetics
Absorption: Oral formulation is well absorbed
(80%) from the GI tract; IV administration results in
complete bioavailability.
Distribution: Does not enter breast milk in significant
amounts.
Protein Binding: 99%.
Metabolism and Excretion: Mostly metabolized
by the liver; small amounts (1%) excreted unchanged
by the kidneys.
Half-life: Neonates: 26–43 hr; Children: 1–2 hr;
Adults: 2–4 hr.
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
PO (antipyretic) 0.5–2.5 hr 2–4 hr 6–8 hr
PO (analgesic) 30 min 1–2 hr 4–6 hr
PO (anti-inflammatory)
7 days 1–2 wk unknown
IV (analgesic) unknown unknown 6 hr
IV (antipyretic) within 2 hr 10–12 hr† 4–6 hr
† With repeated dosing.
Contraindications/Precautions
Contraindicated in: Hypersensitivity (cross-sensitivity
may exist with other NSAIDs, including aspirin);
Active GI bleeding or ulcer disease; Chewable tablets
contain aspartame and should not be used in patients
with phenylketonuria; Coronary artery bypass graft
(CABG) surgery; History of recent MI; Severe HF; OB:
Avoid after 30 wk gestation (may cause premature closure
of fetal ductus arteriosus); Pedi: Ibuprofen lysine:
Preterm neonates with untreated infection, congenital
heart disease where patency of PDA is necessary for
pulmonary or systemic blood flow, bleeding, thrombocytopenia,
coagulation defects, necrotizing enterocolitis,
significant renal dysfunction.
Use Cautiously in: Cardiovascular disease or risk
factors for cardiovascular disease (mayqrisk of serious
cardiovascular thrombotic events, MI, and stroke,
especially with prolonged use or use of higher doses);
avoid use in patients with recent MI or HF; Renal or hepatic
disease, dehydration, or patients on nephrotoxic
drugs (mayqrisk of renal toxicity); Aspirin triad patients
(asthma, nasal polyps, and aspirin intolerance);
can cause fatal anaphylactoid reactions; Chronic alcohol
use/abuse; Geri:qrisk of adverse reactions secondary
to age-relatedpin renal and hepatic function, concurrent
illnesses, and medications; Coagulation
disorders; OB: Use cautiously up to 30 wk gestation;
avoid after that; Lactation: Use cautiously; Pedi: Safety
not established for infants 6 mo (oral and IV Caldolor);
Hyperbilirubinemia in neonates (may displace bilirubin
from albumin-binding sites).
Exercise Extreme Caution in: History of GI
bleeding or GI ulcer disease.
Adverse Reactions/Side Effects
CNS: headache, dizziness, drowsiness, intraventricular
hemorrhage (ibuprofen lysine), psychic disturbances.
EENT: amblyopia, blurred vision, tinnitus. CV: HF,
MYOCARDIAL INFARCTION, STROKE, arrhythmias, edema,
hypertension. F and E: hyperkalemia. GI: GI BLEEDING,
HEPATITIS, constipation, dyspepsia, nausea, necrotizing
enterocolitis (ibuprofen lysine), vomiting, abdominal
discomfort. GU: cystitis, hematuria, renal
failure. Derm: EXFOLIATIVE DERMATITIS, STEVENS-JOHNSON
SYNDROME, TOXIC EPIDERMAL NECROLYSIS, rash, injection
site reaction. Hemat: anemia, blood dyscrasias,
prolonged bleeding time. Misc: allergic reactions
including ANAPHYLAXIS.
Interactions
Drug-Drug: May limit the cardioprotective effects of
low-dose aspirin. Concurrent use with aspirin mayp
effectiveness of ibuprofen. Additive adverse GI side effects
with aspirin, oral potassium, other NSAIDs,
corticosteroids, or alcohol. Chronic use with acetaminophen
mayqrisk of adverse renal reactions. May
peffectiveness of diuretics, ACE inhibitors, or other
antihypertensives. Mayqhypoglycemic effects of insulin
or oral hypoglycemic agents. Mayqserum
lithium levels and risk of toxicity.qrisk of toxicity
from methotrexate. Probenecidqrisk of toxicity
from ibuprofen.qrisk of bleeding with cefotetan,
corticosteroids, valproic acid, thrombolytics,
warfarin, and drugs affecting platelet function including
clopidogrel, abciximab, eptifibatide, or tirofiban.
qrisk of adverse hematologic reactions with
antineoplastics or radiation therapy.qrisk of
nephrotoxicity with cyclosporine.
Drug-Natural Products:qbleeding risk with, arnica,
chamomile, feverfew, garlic, ginger, ginkgo,
Panax ginseng, and others.
Route/Dosage
Analgesia
PO (Adults): Anti-inflammatory—400–800 mg 3–
4 times daily (not to exceed 3200 mg/day). Analgesic/
antidysmenorrheal/antipyretic—200–400 mg every
4–6 hr (not to exceed 1200 mg/day).
PO (Children 6 mo–12 yr): Anti-inflammatory—
30–50 mg/kg/day in 3–4 divided doses (maximum
dose: 2.4 g/day). Antipyretic—5 mg/kg for temperature
102.5F (39.17C) or 10 mg/kg for higher temperatures
(not to exceed 40 mg/kg/day); may be repeated
every 4–6 hr. Cystic fibrosis (unlabeled)—
20–30 mg/kg/day divided twice daily.
PO (Infants and Children): Analgesic—4–10 mg/
kg/dose every 6–8 hr.
IV (Adults): Analgesic—400–800 mg every 6 hr as
needed (not to exceed 3200 mg/day); Antipyretic—
400 mg initially, then 400 mg every 4–6 hr or 100–
200 mg every 4 hr as needed (not to exceed 3200 mg/
day).
IV (Children 12–17 yr): Analgesic and antipyretic—
400 mg every 4–6 hr as needed (not to exceed
2400 mg/day).
IV (Children 6 mo–12 yr): Analgesic and antipyretic—
10 mg/kg (not to exceed 400 mg) every 4–6
hr as needed (not to exceed 40 mg/kg/day or 2400 mg/
day whichever is less).
Pediatric OTC Dosing
PO (Children 11 yr/72–95 lb): 300 mg every 6–8
hr.
PO (Children 9–10 yr/60–71 lb): 250 mg every 6–
8 hr.
PO (Children 6–8 yr/48–59 lb): 200 mg every 6–
8 hr.
PO (Children 4–5 yr/36–47 lb): 150 mg every 6–
8 hr.
PO (Children 2–3 yr/24–35 lb): 100 mg every 6–
8 hr.
PO (Children 12–23 mo/18–23 lb): 75 mg every
6–8 hr.
PO (Infants 6–11 mo/12–17 lb): 50 mg every 6–8
hr.
PDA Closure
IV (Neonates Gestational age 32 weeks, 500–
1500 g): 10 mg/kg followed by two doses of 5 mg/kg
at 24 and 48 hr after initial dose.
Availability (generic available)
Tablets: 100 mgOTC, 200 mgOTC, 300 mg, 400 mg, 600
mg, 800 mg. Capsules (liquigels): 200 mgOTC. Chewable
tablets (fruit, grape, orange, and citrus flavor
): 50 mgOTC, 100 mgOTC. Oral suspension (fruit,
berry, grape flavor): 100 mg/5 mLOTC. Pediatric
drops (berry flavor): 50 mg/1.25 mLOTC. Solution
for injection: 100 mg/mL (Caldolor), 17.1 mg/mL as
lysine, 10 mg/mL as ibuprofen base (Neoprofen). In
combination with: decongestantsOTC, hydrocodone
(Reprexain), famotidine (Duexis). See Appendix B.
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