Peringatan Keamanan

The oral LD50 in rats is 98 mg/kg.L11470 Signs and symptoms of overdose with meloxicam may include shallow breathing, seizure, decreased urine output, gastrointestinal irritation, nausea, vomiting, gastrointestinal bleeding, and black tarry stools.L11473 In the case of an overdose, offer supportive treatment and attempt to remove gastrointestinal contents. Cholestyramine has been shown to enhance the elimination of meloxicam.L11470

Meloxicam

DB00814

small molecule approved vet_approved

Deskripsi

Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) used to relieve various types of pain, including pain caused by musculoskeletal conditions, osteoarthritis, and rheumatoid arthritis.A190189 With a longer half-life than most other NSAIDS, it is a favorable option for those who require once-daily dosing. Meloxicam is available in oral, transdermal, and intravenous formulations. It is a preferential COX-2 inhibitor, purportedly reducing the risk of adverse gastrointestinal tract effects, however, this is a topic of controversy.A190198,A190201

Struktur Molekul 2D

Berat 351.401
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of meloxicam is approximately 20 hours[A190195], which is considerably longer than most other NSAIDS. It can therefore be dosed without the need for slow-release formulations.[A190189] Meloxicam applied together with [bupivacaine] for postsurgical analgesia had a median half-life of 33-42 hours, depending on dose and application site.[L34100]
Volume Distribusi The volume of distribution of meloxicam is 10-15L. Because of its high binding to albumin, it is likely to be distributed in highly perfused tissues, such as the liver and kidney.[A190189] Meloxicam concentrations in synovial fluid, measured after an oral dose, is estimated at 40% to 50% of the concentrations measured in the plasma.[L11398] This drug is known to cross the placenta in humans.[T757]
Klirens (Clearance) After an oral dose, the total clearance of meloxicam is 0.42–0.48 L/h.[A190189,A190195] The FDA label indicates a plasma clearance from 7 to 9 mL/min. No dose changes are required in mild to moderate renal or hepatic impairment. The use of meloxicam in patients with severe renal or hepatic impairment has not been studied. FDA prescribing information advises against it.[L11398]

Absorpsi

The absolute bioavailability oral capsules after a dose was 89% in one pharmacokinetic study. Cmax was reached 5–6 hours after administration of a single dose given after the first meal of the day. The Cmax doubled when the drug was administered in the fasting state. Despite this, meloxicam can be taken without regard to food, unlike many other NSAIDS.A190189,L11398 Meloxicam formulated for instillation with bupivacaine produced varied systemic measures following a single dose of varying strength. In patients undergoing bunionectomy, 1.8 mg of meloxicam produced a Cmax of 26 ± 14 ng/mL, a median Tmax of 18 h, and an AUC? of 2079 ± 1631 ng\*h/mL. For a 9 mg dose used in herniorrhaphy, the corresponding values were 225 ± 96 ng/mL, 54 h, and the AUC? was not reported. Lastly, a 12 mg dose used in total knee arthroplasty produced values of 275 ± 134 ng/mL, 36 h, and 25,673 ± 17,666 ng\*h/mL.L34100

Metabolisme

Meloxicam is almost completely metabolized. CYP2C9 is the main enzyme responsible for the metabolism of meloxicamA190189,A14902 with minor contributions from CYP3A4.L11398 Meloxicam has 4 major metabolites with no activity determined. About 60% of the ingested dose is metabolized to 5'-carboxy meloxicam from hepatic cytochrome enzyme oxidation of an intermediate metabolite, 5’-hydroxymethylmeloxicam.A14902,A39443 Two other metabolites are likely produced via peroxidation.A14902,L11398

Rute Eliminasi

Meloxicam is mainly eliminated through metabolism. Its metabolites are cleared through renal and fecal elimination.A190195 Less than <0.25% of a dose is eliminated in the urine as unchanged drug.L11398 About 1.6% of the parent drug is excreted in the feces.A190189

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. The risk of gastrointestinal bleeding may be increased.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

2363 Data
Amlodipine The metabolism of Meloxicam can be decreased when combined with Amlodipine.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Meloxicam.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Meloxicam.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Meloxicam.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Meloxicam.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Meloxicam.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Meloxicam.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Meloxicam.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Meloxicam.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Meloxicam.
Linezolid The risk or severity of methemoglobinemia can be increased when Linezolid is combined with Meloxicam.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Meloxicam.
Furazolidone The risk or severity of hypertension can be increased when Furazolidone is combined with Meloxicam.
Nicergoline The risk or severity of hypertension can be increased when Nicergoline is combined with Meloxicam.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Meloxicam.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with Meloxicam.
Propiomazine The risk or severity of hypertension can be increased when Propiomazine is combined with Meloxicam.
Minaprine The risk or severity of hypertension can be increased when Minaprine is combined with Meloxicam.
Orciprenaline The risk or severity of hypertension can be increased when Meloxicam is combined with Orciprenaline.
Phenmetrazine The risk or severity of hypertension can be increased when Meloxicam is combined with Phenmetrazine.
Trifluoperazine The risk or severity of hypertension can be increased when Meloxicam is combined with Trifluoperazine.
Pseudoephedrine The risk or severity of hypertension can be increased when Meloxicam is combined with Pseudoephedrine.
Ritodrine The risk or severity of hypertension can be increased when Meloxicam is combined with Ritodrine.
Flupentixol The risk or severity of hypertension can be increased when Meloxicam is combined with Flupentixol.
Remifentanil The risk or severity of hypertension can be increased when Meloxicam is combined with Remifentanil.
Bitolterol The risk or severity of hypertension can be increased when Meloxicam is combined with Bitolterol.
Oxymetazoline The risk or severity of hypertension can be increased when Meloxicam is combined with Oxymetazoline.
Diethylpropion The risk or severity of hypertension can be increased when Meloxicam is combined with Diethylpropion.
Naratriptan The risk or severity of hypertension can be increased when Meloxicam is combined with Naratriptan.
Frovatriptan The risk or severity of hypertension can be increased when Meloxicam is combined with Frovatriptan.
Isoprenaline The risk or severity of hypertension can be increased when Meloxicam is combined with Isoprenaline.
Arbutamine The risk or severity of hypertension can be increased when Meloxicam is combined with Arbutamine.
Desflurane The risk or severity of hypertension can be increased when Meloxicam is combined with Desflurane.
Isocarboxazid The risk or severity of hypertension can be increased when Meloxicam is combined with Isocarboxazid.
Lisdexamfetamine The risk or severity of hypertension can be increased when Meloxicam is combined with Lisdexamfetamine.
Fenoterol The risk or severity of hypertension can be increased when Meloxicam is combined with Fenoterol.
Pirbuterol The risk or severity of hypertension can be increased when Meloxicam is combined with Pirbuterol.
Ephedra sinica root The risk or severity of hypertension can be increased when Meloxicam is combined with Ephedra sinica root.
Ephedrine The risk or severity of hypertension can be increased when Meloxicam is combined with Ephedrine.
Mephentermine The risk or severity of hypertension can be increased when Meloxicam is combined with Mephentermine.
Procaterol The risk or severity of hypertension can be increased when Meloxicam is combined with Procaterol.
Methotrimeprazine The risk or severity of hypertension can be increased when Meloxicam is combined with Methotrimeprazine.
Clenbuterol The risk or severity of hypertension can be increased when Meloxicam is combined with Clenbuterol.
Bambuterol The risk or severity of hypertension can be increased when Meloxicam is combined with Bambuterol.
MMDA The risk or severity of hypertension can be increased when Meloxicam is combined with MMDA.
Midomafetamine The risk or severity of hypertension can be increased when Meloxicam is combined with Midomafetamine.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when Meloxicam is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when Meloxicam is combined with 4-Methoxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when Meloxicam is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The risk or severity of hypertension can be increased when Meloxicam is combined with Tenamfetamine.
Chlorphentermine The risk or severity of hypertension can be increased when Meloxicam is combined with Chlorphentermine.
Dextroamphetamine The risk or severity of hypertension can be increased when Meloxicam is combined with Dextroamphetamine.
Phendimetrazine The risk or severity of hypertension can be increased when Meloxicam is combined with Phendimetrazine.
Periciazine The risk or severity of hypertension can be increased when Meloxicam is combined with Periciazine.
Acepromazine The risk or severity of hypertension can be increased when Meloxicam is combined with Acepromazine.
Thioproperazine The risk or severity of hypertension can be increased when Meloxicam is combined with Thioproperazine.
Epicaptopril The risk or severity of hypertension can be increased when Meloxicam is combined with Epicaptopril.
Clorgiline The risk or severity of hypertension can be increased when Meloxicam is combined with Clorgiline.
1-benzylimidazole The risk or severity of hypertension can be increased when Meloxicam is combined with 1-benzylimidazole.
Nialamide The risk or severity of hypertension can be increased when Meloxicam is combined with Nialamide.
Amibegron The risk or severity of hypertension can be increased when Meloxicam is combined with Amibegron.
Naluzotan The risk or severity of hypertension can be increased when Meloxicam is combined with Naluzotan.
Pizotifen The risk or severity of hypertension can be increased when Meloxicam is combined with Pizotifen.
Solabegron The risk or severity of hypertension can be increased when Meloxicam is combined with Solabegron.
Esmirtazapine The risk or severity of hypertension can be increased when Meloxicam is combined with Esmirtazapine.
Nitrous oxide The risk or severity of hypertension can be increased when Meloxicam is combined with Nitrous oxide.
Xylometazoline The risk or severity of hypertension can be increased when Meloxicam is combined with Xylometazoline.
Dexmethylphenidate The risk or severity of hypertension can be increased when Meloxicam is combined with Dexmethylphenidate.
Isometheptene The risk or severity of hypertension can be increased when Meloxicam is combined with Isometheptene.
Levonordefrin The risk or severity of hypertension can be increased when Meloxicam is combined with Levonordefrin.
Naphazoline The risk or severity of hypertension can be increased when Meloxicam is combined with Naphazoline.
Tetryzoline The risk or severity of hypertension can be increased when Meloxicam is combined with Tetryzoline.
Cinitapride The risk or severity of hypertension can be increased when Meloxicam is combined with Cinitapride.
Tyramine The risk or severity of hypertension can be increased when Meloxicam is combined with Tyramine.
Adrafinil The risk or severity of hypertension can be increased when Meloxicam is combined with Adrafinil.
Isoxsuprine The risk or severity of hypertension can be increased when Meloxicam is combined with Isoxsuprine.
Ifenprodil The risk or severity of methemoglobinemia can be increased when Ifenprodil is combined with Meloxicam.
Hexoprenaline The risk or severity of hypertension can be increased when Meloxicam is combined with Hexoprenaline.
Etilefrine The risk or severity of hypertension can be increased when Meloxicam is combined with Etilefrine.
Cirazoline The risk or severity of hypertension can be increased when Meloxicam is combined with Cirazoline.
Synephrine The risk or severity of hypertension can be increased when Meloxicam is combined with Synephrine.
Hydracarbazine The risk or severity of hypertension can be increased when Meloxicam is combined with Hydracarbazine.
Benmoxin The risk or severity of hypertension can be increased when Meloxicam is combined with Benmoxin.
Mebanazine The risk or severity of hypertension can be increased when Meloxicam is combined with Mebanazine.
Octamoxin The risk or severity of hypertension can be increased when Meloxicam is combined with Octamoxin.
Pheniprazine The risk or severity of hypertension can be increased when Meloxicam is combined with Pheniprazine.
Phenoxypropazine The risk or severity of hypertension can be increased when Meloxicam is combined with Phenoxypropazine.
Pivhydrazine The risk or severity of hypertension can be increased when Meloxicam is combined with Pivhydrazine.
Safrazine The risk or severity of hypertension can be increased when Meloxicam is combined with Safrazine.
Caroxazone The risk or severity of hypertension can be increased when Meloxicam is combined with Caroxazone.
Doxofylline The risk or severity of hypertension can be increased when Meloxicam is combined with Doxofylline.
Iofetamine I-123 The risk or severity of hypertension can be increased when Meloxicam is combined with Iofetamine I-123.
Racepinephrine The risk or severity of hypertension can be increased when Meloxicam is combined with Racepinephrine.
Amitraz The risk or severity of hypertension can be increased when Meloxicam is combined with Amitraz.
Medetomidine The risk or severity of hypertension can be increased when Meloxicam is combined with Medetomidine.
Xylazine The risk or severity of hypertension can be increased when Meloxicam is combined with Xylazine.
Atipamezole The risk or severity of hypertension can be increased when Meloxicam is combined with Atipamezole.
Ractopamine The risk or severity of hypertension can be increased when Meloxicam is combined with Ractopamine.
Romifidine The risk or severity of hypertension can be increased when Meloxicam is combined with Romifidine.
Detomidine The risk or severity of hypertension can be increased when Meloxicam is combined with Detomidine.

Target Protein

Prostaglandin G/H synthase 2 PTGS2
Prostaglandin G/H synthase 1 PTGS1

Referensi & Sumber

Synthesis reference: Laura Coppi, "Crystalline forms of meloxicam and processes for their preparation and interconversion." U.S. Patent US20030109701, issued June 12, 2003.
Artikel (PubMed)
  • PMID: 30774225
    Bekker A, Kloepping C, Collingwood S: Meloxicam in the management of post-operative pain: Narrative review. J Anaesthesiol Clin Pharmacol. 2018 Oct-Dec;34(4):450-457. doi: 10.4103/joacp.JOACP13318.
  • PMID: 19821429
    Moore RA, Derry S, McQuay HJ: Single dose oral meloxicam for acute postoperative pain in adults. Cochrane Database Syst Rev. 2009 Oct 7;(4):CD007552. doi: 10.1002/14651858.CD007552.pub2.
  • PMID: 8630630
    Turck D, Roth W, Busch U: A review of the clinical pharmacokinetics of meloxicam. Br J Rheumatol. 1996 Apr;35 Suppl 1:13-6. doi: 10.1093/rheumatology/35.suppl_1.13.
  • PMID: 24373107
    Katz JA: COX-2 inhibition: what we learned--a controversial update on safety data. Pain Med. 2013 Dec;14 Suppl 1:S29-34. doi: 10.1111/pme.12252.
  • PMID: 23537413
    Seddik H, Rabhi M: Meloxicam-induced colitis revealed by acute abdominal pain. Ann Pharm Fr. 2013 Mar;71(2):119-22. doi: 10.1016/j.pharma.2012.12.003. Epub 2013 Mar 8.
  • PMID: 9493314
    Chesne C, Guyomard C, Guillouzo A, Schmid J, Ludwig E, Sauter T: Metabolism of Meloxicam in human liver involves cytochromes P4502C9 and 3A4. Xenobiotica. 1998 Jan;28(1):1-13. doi: 10.1080/004982598239704.
  • PMID: 21508345
    Ricciotti E, FitzGerald GA: Prostaglandins and inflammation. Arterioscler Thromb Vasc Biol. 2011 May;31(5):986-1000. doi: 10.1161/ATVBAHA.110.207449.
  • PMID: 27026863
    Prasad GS, Srisailam K, Sashidhar RB: Metabolic inhibition of meloxicam by specific CYP2C9 inhibitors in Cunninghamella blakesleeana NCIM 687: in silico and in vitro studies. Springerplus. 2016 Feb 24;5:166. doi: 10.1186/s40064-016-1794-4. eCollection 2016.
Textbook
  • Carl P. Weiner MD, MBA, FACOG, Clifford Mason PhD (2019). Drugs for Pregnant and Lactating Women (3rd ed.). Elsevier.

Contoh Produk & Brand

Produk: 353 • International brands: 35
Produk
  • Act Meloxicam
    Tablet • 7.5 mg • Oral • Canada • Approved
  • Act Meloxicam
    Tablet • 15 mg • Oral • Canada • Approved
  • Anjeso
    Injection • 30 mg/1mL • Intravenous • US • Approved
  • Apo-meloxicam
    Tablet • 7.5 mg • Oral • Canada • Generic • Approved
  • Apo-meloxicam
    Tablet • 15 mg • Oral • Canada • Generic • Approved
  • Auro-meloxicam
    Tablet • 7.5 mg • Oral • Canada • Generic • Approved
  • Auro-meloxicam
    Tablet • 15 mg • Oral • Canada • Generic • Approved
  • Ava-meloxicam
    Tablet • 7.5 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 353 produk.
International Brands
  • Achefree — Achefree
  • Acticam — Acromax Dominicana
  • Aflamid — Anchor
  • Afloxx — Lusa
  • Aglan — Zentiva
  • Ainecox — Cheminter
  • Aldoron — Ivax
  • Alentum — Lafrancol
  • Algiflex — Biogen
  • Aliviodol — Centrum

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