Peringatan Keamanan

The oral LD50 of orlistat is >5000 mg/kg in rats.L32078 Single orlistat doses of 800 mg and multiple doses of up to 400 mg three times a day for 15 days have been administered to healthy weight and obese subjects without clinically significant adverse findings. In addition, doses of 240 mg three times a day have been given to obese patients for 6 months without a significant adverse effects. Post-marketing reports of overdoses cases indicate no adverse events or adverse events that are similar to those reported with the recommended dose. If a significant overdose with orlistat occurs, the patient should be observed for at least 24 hours. Based on the results of clinical studies, systemic effects caused by orlistat are likely to be rapidly reversible.L32068

Orlistat

DB01083

small molecule approved investigational

Deskripsi

The global prevalence of obesity is increasing rapidly. Obesity-related complications lead to significant personal and economic burden by reducing quality of life and increasing the cost of healthcare. In some individuals, diet and exercise are insufficient to maintain weight loss, and pharmacological or surgical intervention is required.A229928

Orlistat is a lipase inhibitor used in the treatment of obesity that works by inhibiting fat-metabolizing enzymes. It was approved by the FDA for use in combination with a reduced-calorie diet in 1999.L11130 This drug is a generally well-tolerated and effective weight-loss aid and is now available in both over-the-counterL31963 and prescription preparations, depending on the dosage quantity.L11130

Struktur Molekul 2D

Berat 495.7348
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 orlistat of the small amount of absorbed orlistat ranges between 1-2 hours.[A229918,L11130]
Volume Distribusi Volume of distribution cannot be obtained because the absorption of orlistat is minimal. Orlistat is minimally distributed to erythrocytes and is primarily bound to proteins.[L11130]
Klirens (Clearance) -

Absorpsi

The systemic absorption and exposure of orlistat is low, however, systemic absorption of the drug is not required for orlistat activity.L31993 After an oral dose with 360 mg of radiolabeled orlistat, plasma radioactivity achieved a peak at about 8 hours. Plasma concentrations of unchanged parent drug were close to the lower end of detection limits (<5 ng/mL). In plasma samples of patients taking orlistat, the detection of unchanged drug was sporadic and very low concentrations were detected (<10 ng/mL or 0.02 ?M) with no evidence suggesting drug accumulation.L11130

Metabolisme

Orlistat is hydrolyzed in the intestinal wall.L31988 In a radiolabeled orlistat mass balance study in obese patients, two metabolites were identified. The first metabolite, M1, was the hydrolyzed ?-lactone ring product of orlistat. The second metabolite, M3, was produced from M1’s cleavage of the N-formyl leucine side-chain. Both metabolites accounted for about 42% of total plasma radioactivity. Both M1 and M3 are considered pharmacologically inactive.A229918,L11130

Rute Eliminasi

After single oral dose of radiolabled orlistat in both normal weight and obese volunteers fecal excretion of the unabsorbed drug was found to be the major route of elimination with <2% urinary excretion.A229743,L32068 Fecal elimination of orlistat is estimated between 95-97%.L11130 Complete excretion by both routes occurs within in 3 to 5 days.L32068

Interaksi Makanan

1 Data
  • 1. Take with food. Take with meals or up to 1 hour after a meal. Doses may be skipped for missed meals or fat-free meals.

Interaksi Obat

139 Data
Cyclosporine Orlistat can cause a decrease in the absorption of Cyclosporine resulting in a reduced serum concentration and potentially a decrease in efficacy.
1alpha,24S-Dihydroxyvitamin D2 Orlistat can cause a decrease in the absorption of 1alpha,24S-Dihydroxyvitamin D2 resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcitriol Orlistat can cause a decrease in the absorption of Calcitriol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcifediol Orlistat can cause a decrease in the absorption of Calcifediol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ergocalciferol Orlistat can cause a decrease in the absorption of Ergocalciferol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vitamin A Orlistat can cause a decrease in the absorption of Vitamin A resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vitamin E Orlistat can cause a decrease in the absorption of Vitamin E resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholecalciferol Orlistat can cause a decrease in the absorption of Cholecalciferol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Menadione Orlistat can cause a decrease in the absorption of Menadione resulting in a reduced serum concentration and potentially a decrease in efficacy.
Alitretinoin Orlistat can cause a decrease in the absorption of Alitretinoin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tretinoin Orlistat can cause a decrease in the absorption of Tretinoin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Phylloquinone Orlistat can cause a decrease in the absorption of Phylloquinone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dihydrotachysterol Orlistat can cause a decrease in the absorption of Dihydrotachysterol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Alfacalcidol Orlistat can cause a decrease in the absorption of Alfacalcidol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Seocalcitol Orlistat can cause a decrease in the absorption of Seocalcitol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Inecalcitol Orlistat can cause a decrease in the absorption of Inecalcitol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Becocalcidiol Orlistat can cause a decrease in the absorption of Becocalcidiol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Eldecalcitol Orlistat can cause a decrease in the absorption of Eldecalcitol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Elocalcitol Orlistat can cause a decrease in the absorption of Elocalcitol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Maxacalcitol Orlistat can cause a decrease in the absorption of Maxacalcitol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Doxercalciferol Orlistat can cause a decrease in the absorption of Doxercalciferol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Beta carotene Orlistat can cause a decrease in the absorption of Beta carotene resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vitamin D Orlistat can cause a decrease in the absorption of Vitamin D resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tocopherol Orlistat can cause a decrease in the absorption of Tocopherol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tocofersolan Orlistat can cause a decrease in the absorption of Tocofersolan resulting in a reduced serum concentration and potentially a decrease in efficacy.
Menatetrenone Orlistat can cause a decrease in the absorption of Menatetrenone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tocotrienol Orlistat can cause a decrease in the absorption of Tocotrienol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Menaquinone 7 Orlistat can cause a decrease in the absorption of Menaquinone 7 resulting in a reduced serum concentration and potentially a decrease in efficacy.
1alpha-Hydroxyvitamin D5 Orlistat can cause a decrease in the absorption of 1alpha-Hydroxyvitamin D5 resulting in a reduced serum concentration and potentially a decrease in efficacy.
Motretinide Orlistat can cause a decrease in the absorption of Motretinide resulting in a reduced serum concentration and potentially a decrease in efficacy.
alpha-Tocopherol succinate Orlistat can cause a decrease in the absorption of alpha-Tocopherol succinate resulting in a reduced serum concentration and potentially a decrease in efficacy.
D-alpha-Tocopherol acetate Orlistat can cause a decrease in the absorption of D-alpha-Tocopherol acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
alpha-Tocopherol acetate Orlistat can cause a decrease in the absorption of alpha-Tocopherol acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
DL-alpha-Tocopherol Orlistat can cause a decrease in the absorption of DL-alpha-Tocopherol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Menaquinone 6 Orlistat can cause a decrease in the absorption of Menaquinone 6 resulting in a reduced serum concentration and potentially a decrease in efficacy.
gamma-Tocopherol Orlistat can cause a decrease in the absorption of gamma-Tocopherol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Previtamin D(3) Orlistat can cause a decrease in the absorption of Previtamin D(3) resulting in a reduced serum concentration and potentially a decrease in efficacy.
Menadione bisulfite Orlistat can cause a decrease in the absorption of Menadione bisulfite resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lorazepam Orlistat can cause a decrease in the absorption of Lorazepam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pregabalin Orlistat can cause a decrease in the absorption of Pregabalin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Butalbital Orlistat can cause a decrease in the absorption of Butalbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Phenytoin Orlistat can cause a decrease in the absorption of Phenytoin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topiramate Orlistat can cause a decrease in the absorption of Topiramate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pentobarbital Orlistat can cause a decrease in the absorption of Pentobarbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Valproic acid Orlistat can cause a decrease in the absorption of Valproic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Trimethadione Orlistat can cause a decrease in the absorption of Trimethadione resulting in a reduced serum concentration and potentially a decrease in efficacy.
Clobazam Orlistat can cause a decrease in the absorption of Clobazam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Secobarbital Orlistat can cause a decrease in the absorption of Secobarbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Metharbital Orlistat can cause a decrease in the absorption of Metharbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methohexital Orlistat can cause a decrease in the absorption of Methohexital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Mephenytoin Orlistat can cause a decrease in the absorption of Mephenytoin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lamotrigine Orlistat can cause a decrease in the absorption of Lamotrigine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Carbamazepine Orlistat can cause a decrease in the absorption of Carbamazepine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ethosuximide Orlistat can cause a decrease in the absorption of Ethosuximide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Thiopental Orlistat can cause a decrease in the absorption of Thiopental resulting in a reduced serum concentration and potentially a decrease in efficacy.
Paramethadione Orlistat can cause a decrease in the absorption of Paramethadione resulting in a reduced serum concentration and potentially a decrease in efficacy.
Clorazepic acid Orlistat can cause a decrease in the absorption of Clorazepic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium sulfate Orlistat can cause a decrease in the absorption of Magnesium sulfate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tizanidine Orlistat can cause a decrease in the absorption of Tizanidine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Riluzole Orlistat can cause a decrease in the absorption of Riluzole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ethotoin Orlistat can cause a decrease in the absorption of Ethotoin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Oxcarbazepine Orlistat can cause a decrease in the absorption of Oxcarbazepine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Primidone Orlistat can cause a decrease in the absorption of Primidone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetazolamide Orlistat can cause a decrease in the absorption of Acetazolamide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Diazepam Orlistat can cause a decrease in the absorption of Diazepam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Phensuximide Orlistat can cause a decrease in the absorption of Phensuximide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Progabide Orlistat can cause a decrease in the absorption of Progabide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methylphenobarbital Orlistat can cause a decrease in the absorption of Methylphenobarbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tiagabine Orlistat can cause a decrease in the absorption of Tiagabine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zonisamide Orlistat can cause a decrease in the absorption of Zonisamide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Felbamate Orlistat can cause a decrease in the absorption of Felbamate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zaleplon Orlistat can cause a decrease in the absorption of Zaleplon resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gabapentin Orlistat can cause a decrease in the absorption of Gabapentin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Clonazepam Orlistat can cause a decrease in the absorption of Clonazepam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vigabatrin Orlistat can cause a decrease in the absorption of Vigabatrin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Phenacemide Orlistat can cause a decrease in the absorption of Phenacemide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Thiamylal Orlistat can cause a decrease in the absorption of Thiamylal resulting in a reduced serum concentration and potentially a decrease in efficacy.
Phenobarbital Orlistat can cause a decrease in the absorption of Phenobarbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Levetiracetam Orlistat can cause a decrease in the absorption of Levetiracetam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Estazolam Orlistat can cause a decrease in the absorption of Estazolam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Fosphenytoin Orlistat can cause a decrease in the absorption of Fosphenytoin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Amobarbital Orlistat can cause a decrease in the absorption of Amobarbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hexobarbital Orlistat can cause a decrease in the absorption of Hexobarbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Barbital Orlistat can cause a decrease in the absorption of Barbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Delorazepam Orlistat can cause a decrease in the absorption of Delorazepam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nitrazepam Orlistat can cause a decrease in the absorption of Nitrazepam resulting in a reduced serum concentration and potentially a decrease in efficacy.
7-Nitroindazole Orlistat can cause a decrease in the absorption of 7-Nitroindazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Valpromide Orlistat can cause a decrease in the absorption of Valpromide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Flunarizine Orlistat can cause a decrease in the absorption of Flunarizine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ezogabine Orlistat can cause a decrease in the absorption of Ezogabine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methsuximide Orlistat can cause a decrease in the absorption of Methsuximide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Brivaracetam Orlistat can cause a decrease in the absorption of Brivaracetam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rufinamide Orlistat can cause a decrease in the absorption of Rufinamide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lacosamide Orlistat can cause a decrease in the absorption of Lacosamide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Remacemide Orlistat can cause a decrease in the absorption of Remacemide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Clomethiazole Orlistat can cause a decrease in the absorption of Clomethiazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Deramciclane Orlistat can cause a decrease in the absorption of Deramciclane resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tramiprosate Orlistat can cause a decrease in the absorption of Tramiprosate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gaboxadol Orlistat can cause a decrease in the absorption of Gaboxadol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sulthiame Orlistat can cause a decrease in the absorption of Sulthiame resulting in a reduced serum concentration and potentially a decrease in efficacy.

Target Protein

Pancreatic triacylglycerol lipase PNLIP
Cannabinoid receptor 1 CNR1
Gastric triacylglycerol lipase LIPF
Fatty acid synthase FASN

Referensi & Sumber

Synthesis reference: Vilmos Keri, "Preparation of orlistat and orlistat crystalline forms." U.S. Patent US20030149095, issued August 07, 2003.
Artikel (PubMed)
  • PMID: 14693982
    Torgerson JS, Hauptman J, Boldrin MN, Sjostrom L: XENical in the prevention of diabetes in obese subjects (XENDOS) study: a randomized study of orlistat as an adjunct to lifestyle changes for the prevention of type 2 diabetes in obese patients. Diabetes Care. 2004 Jan;27(1):155-61.
  • PMID: 16767304
    Mancini MC, Halpern A: Pharmacological treatment of obesity. Arq Bras Endocrinol Metabol. 2006 Apr;50(2):377-89. Epub 2006 May 23.
  • PMID: 15870086
    Menendez JA, Vellon L, Lupu R: Antitumoral actions of the anti-obesity drug orlistat (XenicalTM) in breast cancer cells: blockade of cell cycle progression, promotion of apoptotic cell death and PEA3-mediated transcriptional repression of Her2/neu (erbB-2) oncogene. Ann Oncol. 2005 Aug;16(8):1253-67. Epub 2005 May 3.
  • PMID: 16377080
    Garcia SB, Barros LT, Turatti A, Martinello F, Modiano P, Ribeiro-Silva A, Vespucio MV, Uyemura SA: The anti-obesity agent Orlistat is associated to increase in colonic preneoplastic markers in rats treated with a chemical carcinogen. Cancer Lett. 2006 Aug 28;240(2):221-4. Epub 2005 Dec 27.
  • PMID: 18200802
    Drew BS, Dixon AF, Dixon JB: Obesity management: update on orlistat. Vasc Health Risk Manag. 2007;3(6):817-21.
  • PMID: 11728255
    Wong NN, Cheng-Lai A: Orlistat. Heart Dis. 2000 Mar-Apr;2(2):174-81.
  • PMID: 10551441
    Hvizdos KM, Markham A: Orlistat: a review of its use in the management of obesity. Drugs. 1999 Oct;58(4):743-60.
  • PMID: 11261530
    Lucas KH, Kaplan-Machlis B: Orlistat--a novel weight loss therapy. Ann Pharmacother. 2001 Mar;35(3):314-28.
Menampilkan 8 dari 14 artikel.

Contoh Produk & Brand

Produk: 25 • International brands: 0
Produk
  • Alli
    Capsule • 60 mg/1 • Oral • US • OTC • Approved
  • Alli
    Capsule • 60 mg/1 • Oral • US • OTC • Approved
  • Alli
    Capsule • 60 mg • Oral • EU • Approved
  • Alli
    Capsule • 60 mg • Oral • EU • Approved
  • Alli
    Capsule • 60 mg • Oral • EU • Approved
  • Alli
    Capsule • 60 mg • Oral • EU • Approved
  • Alli
    Capsule • 60 mg • Oral • EU • Approved
  • Alli
    Tablet, chewable • 27 mg • Oral • EU • Approved
Menampilkan 8 dari 25 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul