Caldolor

Name: Caldolor

Indications

CALDOLOR is indicated in adults and pediatric patients six months and older for the:

  • management of mild to moderate pain and the management of moderate to severe pain as an adjunct to opioid analgesics
  • reduction of fever

Overdose

Symptoms following acute NSAID overdosages have been typically limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which have been generally reversible with supportive care. Gastrointestinal bleeding has occurred. Hypertension, acute renal failure, respiratory depression, and coma have occurred, but were rare [see WARNINGS AND PRECAUTIONS].

Manage patients with symptomatic and supportive care following an NSAID overdosage. There are no specific antidotes. Forced diuresis, alkalinization of urine, hemodialysis, or hemoperfusion may not be useful due to high protein binding.

For additional information about overdosage treatment contact a poison control center at 1-800-222-1222.

Caldolor Drug Class

Caldolor is part of the drug class:

  • Antiinflammatory preparations, non steroids for topical use

Side Effects of Caldolor

Serious side effects have been reported with ibuprofen. See “Drug Precautions” section.

Common side effects of ibuprofen include:

  • stomach effects:  nausea, heartburn, diarrhea, stomach irritation, bloating or flatulence, constipation
  • others: headache, dizziness, ringing in the ears, swelling of arms or legs, rash

This is not a complete list of ibuprofen side effects. Ask your doctor or pharmacist for more information.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Inform MD

Before taking ibuprofen, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

  • have kidney problems
  • have liver problems
  • have heart problems
  • have had a stomach bleed or ulcer (hole in the lining of the stomach) in the past
  • have asthma
  • are pregnant or breastfeeding

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Caldolor FDA Warning

Cardiovascular Risk:

  • NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk.
  • These drugs are contraindicated for treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.

Gastrointestinal Risk:

  • NSAIDs cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients are at greater risk for serious gastrointestinal events.

Where can i get more information?

Your doctor or pharmacist can provide more information about ibuprofen.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

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What should I avoid while receiving ibuprofen?

Avoid taking aspirin while you are receiving ibuprofen.

Ask a doctor or pharmacist before using any cold, allergy, or pain medication. Many medicines available over the counter contain aspirin or other medicines similar to ibuprofen. Taking certain products together can cause you to get too much of this type of medication. Check the label to see if a medicine contains aspirin, ibuprofen, ketoprofen, or naproxen.

Uses For Caldolor

Ibuprofen injection is a nonsteroidal antiinflammatory drug (NSAID) that is used alone or together with other medicines (eg, opioid analgesics) to relieve mild to severe pain. It is also used to treat fever.

This medicine is to be given only by or under the supervision of your doctor.

How is this medicine (Caldolor) best taken?

Use Caldolor as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • It is given as an infusion into a vein over a period of time.
  • Drink lots of noncaffeine liquids unless told to drink less liquid by your doctor.
  • Do not take more than what your doctor told you to take. Taking more than you are told may raise your chance of very bad side effects.
  • Do not take this medicine for longer than you were told by your doctor.

What do I do if I miss a dose?

  • Call your doctor to find out what to do.

What are some other side effects of Caldolor?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Belly pain or heartburn.
  • Upset stomach or throwing up.
  • Hard stools (constipation).
  • Loose stools (diarrhea).
  • Gas.
  • Dizziness.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

Caldolor - Clinical Pharmacology

Mechanism of Action

Ibuprofen has analgesic, anti-inflammatory, and antipyretic properties.

The mechanism of action of Caldolor, like that of other NSAIDs, is not completely understood but involves inhibition of cyclooxygenase (COX-1 and COX-2).

Ibuprofen is a potent inhibitor of prostaglandin synthesis in vitro. Ibuprofen concentrations reached during therapy have produced in vivo effects. Prostaglandins sensitize afferent nerves and potentiate the action of bradykinin in inducing pain in animal models. Prostaglandins are mediators of inflammation. Because ibuprofen is an inhibitor of prostaglandin synthesis, its mode of action may be due to a decrease of prostaglandins in peripheral tissues.

Pharmacokinetics

Ibuprofen is a racemic mixture of [-]R- and [+]S-isomers. In vivo and in vitro studies indicate that the [+]S-isomer is responsible for clinical activity. The [-]R-form, while thought to be pharmacologically inactive, is slowly and incompletely (~60%) interconverted into the active [+]S species in adults. The [-]R-isomer serves as a circulating reservoir to maintain levels of active drug. The pharmacokinetic parameters of Caldolor determined in a study with volunteers are presented below.

Table 4: Pharmacokinetic Parameters of Intravenous Ibuprofen

AUC = Area-under-the-curve

Cmax = Peak plasma concentration

CV = Coefficient of Variation

KEL = First-order elimination rate constant

T1/2 = Elimination half-life

* = 60 minute infusion time

400 mg* Caldolor
Mean (CV%)
800 mg* Caldolor
Mean (CV%)
Number of Patients 12 12
AUC (mcg·h/mL) 109.3 (26.4) 192.8 (18.5)
Cmax (mcg/mL) 39.2 (15.5) 72.6 (13.2)
KEL (1/h) 0.32 (17.9) 0.29 (12.8)
T1/2 (h) 2.22 (20.1) 2.44 (12.9)

The pharmacokinetic parameters of Caldolor determined in a study with febrile pediatric patients are presented in Table 5. It was observed that the median Tmax was at the end of the infusion and that Caldolor had a shorter elimination half-life in pediatric patients compared to adults. The volume of distribution and clearance increased with age.

Table 5: Pharmacokinetic Parameters of 10 mg/kg Intravenous Ibuprofen, Pediatric Patients, by Age Group

*Median (minimum-maximum)

#WT: body weight (kg)

6 months to
<2 years
Mean (CV%)
2 years to
<6 years
Mean (CV%)
6 years to
16 years
Mean (CV%)
Number of Patients 5 12 25
AUC (mcg·h/mL) 71.1 (37.1) 79.2 (37.0) 80.7 (36.9)
Cmax (mcg/mL) 59.2 (34.8) 64.2 (34.3) 61.9 (26.6)
Tmax (min)* 10 (10-30) 12 (10-46) 10 (10-40)
T1/2 (h) 1.8 (29.9) 1.5 (41.8) 1.55 (26.4)
Cl (mL/h) 1172.5 (38.9) 1967.3 (56.0) 4878.5 (71.0)
Vz (mL) 2805.7 (20.1) 3695.8 (30.0) 10314.2 (67.4)
Cl/WT# (mL/hr/kg) 133.7 (58.6) 130.1 (82.4) 109.2 (41.6)
Vz/WT# (mL/kg) 311.2 (35.4) 227.2 (41.7) 226.8 (30.4)

Ibuprofen, like most NSAIDs, is highly protein bound (>99% bound at 20 mcg/mL). Protein binding is saturable, and at concentrations >20 mcg/mL binding is nonlinear. Based on oral dosing data, there is an age- or fever-related change in volume of distribution for ibuprofen.

Drug Interaction Studies

Aspirin: When NSAIDs were administered with aspirin, the protein binding of NSAIDs were reduced, although the clearance of free NSAID was not altered. The clinical significance of this interaction is not known. See Table 3 for clinically significant drug interactions of NSAIDs with aspirin [see Drug Interactions (7)].

Important information

You should not receive Caldolor just before or after heart bypass surgery (coronary artery bypass graft, or CABG).

Caldolor can increase your risk of fatal heart attack or stroke, especially if you use it long term or use high doses, or if you have heart disease.

In Summary

Common side effects of Caldolor include: hemorrhage, vomiting, anemia, eosinophilia, and hypertension. Other side effects include: upper gastrointestinal hemorrhage, upper gastrointestinal tract ulcer, dizziness, and dyspepsia. See below for a comprehensive list of adverse effects.

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