meloxicam

Absorption: Well absorbed following oral administration. IV administration results in complete bioavailability.

Distribution: Not widely distributed to tissues.

Protein Binding: 99.4%.

Metabolism/Excretion: Mostly metabolized to inactive metabolites by the liver via the CYP2C9 isoenzyme (and to a lesser extent by the CYP3A4 isoenzyme); the CYP2C9 isoenzyme exhibits genetic polymorphism (intermediate or poor metabolizers may have significantly ↑ meloxicam concentrations and an ↑ risk of adverse reactions). Metabolites are excreted in urine and feces.

Half-Life: 20.1 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	5–6 hr	24 hr
IV	rapid	end of injection	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Cross-sensitivity may occur with other NSAIDs, including aspirin;
Severe renal impairment (CCr ≤15 mL/min) (oral);
Moderate to severe renal impairment in patients who are at risk for renal failure due to volume depletion (IV);
Concurrent use of aspirin (↑ risk of adverse reactions);
Coronary artery bypass graft surgery
;
Recent MI
;
HF
OB: Avoid use after 30 wk gestation.

Use Cautiously in:

Cardiovascular disease or risk factors for cardiovascular disease (may ↑ risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, especially with prolonged use or use of higher doses)
;
History of long duration of NSAID use, smoking, alcohol use, advanced liver disease, coagulopathy, or poor general health (↑ risk of GI bleeding)
;
History of peptic ulcer disease and/or GI bleeding
;
Bleeding tendency or concurrent anticoagulant therapy
;
Dehydration (correct deficits before initiating therapy);
Renal impairment, hepatic impairment, or concurrent ACE inhibitor or diuretic therapy (↑ risk of renal impairment);
Hypertension;
OB: Use at or after 20 wk gestation may cause fetal or neonatal renal impairment; if treatment is necessary between 20 wk and 30 wk gestation, limit use to the lowest effective dose and shortest duration possible;
Lactation: Safety not established in breastfeeding;
Pedi: Children <2 yr or <60 kg (safety and effectiveness of tablets not established); safety and effectiveness of capsules and injection not established in children;
Geri:
Appears on Beers list. ↑ risk GI bleeding or peptic ulcer disease in older adults. Avoid chronic use unless other alternatives are not effective and the patient can take a gastroprotective agent; avoid short-term use in combination with oral or parenteral corticosteroids, anticoagulants, or antiplatelet agents unless other alternatives are not effective and the patient can take a gastroprotective agent
.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, HF, hypertension, MI

Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), EXFOLIATIVE DERMATITIS, GENERALIZED BULLOUS FIXED DRUG ERUPTION, pruritus, rash, STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN)

F and E: hyperkalemia

GI: ↑liver enzymes, diarrhea, dyspepsia, GI BLEEDING, GI PERFORATION, GI ULCERATION, HEPATOTOXICITY, nausea

GU: delayed ovulation

Hemat: anemia, leukopenia, thrombocytopenia

Neuro: STROKE

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND SERIOUS SKIN REACTIONS)

Interactions ⬆ ⬇

Drug-drug:

May ↓ antihypertensive effects of ACE inhibitors.
May ↓ diuretic effects of furosemide or thiazide diuretics.
Concurrent use with aspirin↑ meloxicam blood levels and may ↑ risk of adverse reactions.
Concurrent use with cholestyramine↓ blood levels.
↑plasma lithium levels; close monitoring recommended when meloxicam is introduced or withdrawn.
↑risk of GI bleeding with anticoagulants, aspirin, clopidogrel, ticagrelor, prasugrel, corticosteroids, fibrinolytics, SNRIs, or SSRIs.
Concurrent use with sodium polystyrene sulfonate may ↑ risk of colonic necrosis; concurrent use should be avoided.

Route/Dosage ⬆ ⬇

PO (Adults ): Capsules: 5 mg once daily; may ↑ to 10 mg once daily, if needed; Tablets: 7.5 mg once daily; may ↑ to 15 mg once daily, if needed.
PO (Children 2–17 yr and ≥60 kg): Tablets: 7.5 mg once daily.
IV (Adults ): 30 mg once daily.

Availability ⬆ ⬇

(Generic available)

Tablets: 7.5 mg; 15 mg
Capsules: 5 mg; 10 mg
Oral suspension raspberry flavor: 7.5 mg/5 mL
Solution for injection: 30 mg/mL
In combination with: bupivacaine (Zynrelef Kit). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Assess pain and range of motion prior to and 2–3 hr following administration. If analgesic effect is delayed in the 1st 24 hr, consider administering a short-acting, non-NSAID analgesic.
Monitor for signs and symptoms of hypersensitivity reaction, including anaphylaxis. Patients with asthma, aspirin-induced allergy, and nasal polyps are at ↑ risk.
Assess for rash periodically during therapy. May cause SJS, TEN, or generalized bullous fixed drug eruption. At the 1st sign of rash, discontinue meloxicam.
Monitor for signs and symptoms of DRESS (fever, rash, lymphadenopathy, facial swelling) periodically during therapy. If symptoms of DRESS occur, immediately stop meloxicam and evaluate for DRESS.
Monitor BP during initiation and periodically during therapy. May cause fluid retention and edema leading to new onset hypertension.
Monitor for GI bleeding, ulceration, and perforation during extended therapy. If serious GI event is suspected, promptly evaluate and hold therapy until a serious GI event is ruled out.

Lab Test Considerations:

Monitor serum potassium and CBC periodically in patients receiving prolonged therapy. May cause hyperkalemia, anemia, thrombocytopenia, leukopenia, and eosinophilia.
- Monitor renal function (BUN, serum creatinine) in patients on extended therapy and those with renal or hepatic impairment, dehydration, or hypovolemia. If signs and symptoms of hepatotoxicity occur,immediately discontinue meloxicam.
- Bleeding time may be prolonged.

Implementation ⬆ ⬇

Correct volume status in dehydrated or hypovolemic patients prior to initiation.
Administration in higher than recommended doses does not provide ↑ effectiveness but may cause ↑ side effects. Use lowest effective dose for shortest period of time to minimize risk of cardiovascular thrombotic events.
PO: Administer without regard to food. Administer with food or milk to ↓ GI irritation.
- Shake oral suspension gently before using.

IV Administration:

IV Push: Single-dose vial; undiluted. Solution is clear to yellow. Concentration: 30 mg/mL.
Rate: Administer over 15 sec.
Y-Site Incompatibility: Do not administer other drugs through same IV line.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Advise patient to remain in an upright position for 15–30 min after administration and to take missed doses as soon as remembered but not if almost time for the next dose. Do not double doses.
Caution patient to avoid the concurrent use of alcohol, aspirin, acetaminophen, or other OTC medications without consulting health care provider.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other medications, especially the concurrent use of alcohol, aspirin, NSAIDs, or acetaminophen.
Inform patient of ↑ risk of MI and stroke. Use lowest effective dose for shortest time. Advise patient to notify health care provider immediately if signs and symptoms (shortness of breath or trouble breathing, chest pain, weakness in one part or side of body, slurred speech, swelling of the face or throat) occur.
Advise patient to notify health care provider promptly if signs or symptoms of GI toxicity (abdominal pain, black stools) occur.
Advise patient to consult health care provider if rash, itching, visual disturbances, weight gain, edema, or signs of hepatotoxicity (nausea, fatigue, lethargy, jaundice, upper right quadrant tenderness, flu-like symptoms) occur.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding. Advise patient to avoid meloxicam in 3rd trimester of pregnancy (after 29 wk); may cause premature closure of fetal ductus arteriosus. Use of meloxicam after 20 wk may cause fetal renal impairment leading to oligohydramnios. May cause reversible infertility in men and women attempting to conceive; may consider discontinuing meloxicam.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇