Peringatan Keamanan

The reported LD50 after oral administration of phentermine in rats is reported to be of 151 mg/kg.L5239 Reports of acute overdose include restlessness, tremors, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations and panic state followed by fatigue, and depression. In the cardiovascular system, there are reports of tachycardia, arrhythmia, hypertension, hypotension, circulatory collapse. In the GI tract, there are symptoms of nausea, vomiting, diarrhea and abdominal cramps. The management of acute overdosage includes symptomatic treatment as well as lavage and sedation with barbiturates.FDA label

On the other hand, chronic overdosage is marked by dermatoses, insomnia, irritability, hyperactivity and personality changes. In severe cases, it can derive into a schizophrenia-like psychosis.FDA label

Studies regarding the carcinogenic potential have not been performed. On the case of mutagenic assays, phentermine was shown to not be mutagenic nor clastogenic.FDA label

Phentermine

DB00191

small molecule approved illicit

Deskripsi

Phentermine is a sympathomimetic amine anorectic agent and it was introduced in 1959 as part of an anti-obesity combination drug.A174361, A174364 It is chemically related to amphetamine and it is commonly referred to as an atypical amphetamine.A174370 Phentermine has not been reported an addictive potential which allows this agent to be classified under the Schedule IV drugs (low abuse potential).A174367

Phentermine was FDA approved for short-term weight management in 1959 and it became widely used in 1960. This initial product, formed by the combination of phentermine with fenfluramine and dexfenfluramine was discontinued after finding several reports of abnormal valves in nearly 30% of the consumers.A174376, T403 Later on, phentermine was approved alone and in combination with topiramate in 2012 as a new alternative that required lower doses of phentermine to obtain the desired effect.A174373

Struktur Molekul 2D

Berat 149.2328
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal half-life of phentermine is reported to be of approximately 20 hours.[A174370] In conditions where there is acidic urine (pH <5), the elimination half-life is of 7-8 hours.[T49]
Volume Distribusi The reported volume of distribution for phentermine is reported to be of 5 L/kg.[L5236]
Klirens (Clearance) The reported clearance when administered orally is 8.79 L/h as observed in pharmacokinetic population studies.[F3283]

Absorpsi

Phentermine shows a dose-dependent pharmacokinetic profile. After oral administration of a dose of 15 mg, the maximal concentration was achieved after 6 hours and its bioavailability was not affected by the consumption of high-fat meals.A174370 The reported plasma concentration at steady-state is of around 200 ng/ml as observed in clinical trials.T49

Metabolisme

Phentermine undergoes minimal p-hydroxylation, N-oxidation and N-hydroxylation followed by conjugation. The total proportion of the drug that goes under metabolism only represents about 6% of the administered dose where about 5% is represented by the N-oxidized and N-Hydroxylated metabolites.T49

Rute Eliminasi

Phentermine is excreted mainly in the urine from which about 70-80% of the administered dose can be found as the unchanged drug.A174370

Interaksi Makanan

2 Data
  • 1. Limit caffeine intake.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1186 Data
Valsartan Phentermine may decrease the antihypertensive activities of Valsartan.
Ramipril Phentermine may decrease the antihypertensive activities of Ramipril.
Remikiren Phentermine may decrease the antihypertensive activities of Remikiren.
Torasemide Phentermine may decrease the antihypertensive activities of Torasemide.
Olmesartan Phentermine may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Phentermine may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Phentermine may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Phentermine may decrease the antihypertensive activities of Minoxidil.
Treprostinil Phentermine may decrease the antihypertensive activities of Treprostinil.
Bendroflumethiazide Phentermine may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Phentermine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Phentermine may decrease the antihypertensive activities of Trandolapril.
Metolazone Phentermine may decrease the antihypertensive activities of Metolazone.
Benazepril Phentermine may decrease the antihypertensive activities of Benazepril.
Enalapril Phentermine may decrease the antihypertensive activities of Enalapril.
Cyclothiazide Phentermine may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Phentermine may decrease the antihypertensive activities of Candoxatril.
Guanabenz Phentermine may decrease the antihypertensive activities of Guanabenz.
Mecamylamine Phentermine may decrease the antihypertensive activities of Mecamylamine.
Moexipril Phentermine may decrease the antihypertensive activities of Moexipril.
Lisinopril Phentermine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Phentermine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Phentermine may decrease the antihypertensive activities of Metyrosine.
Hydroflumethiazide Phentermine may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Phentermine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Phentermine may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Phentermine may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Phentermine may decrease the antihypertensive activities of Fenoldopam.
Eprosartan Phentermine may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Phentermine may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Phentermine may decrease the antihypertensive activities of Quinapril.
Telmisartan Phentermine may decrease the antihypertensive activities of Telmisartan.
Methyldopa Phentermine may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Phentermine may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Phentermine may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Phentermine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Phentermine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Phentermine may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Phentermine may decrease the antihypertensive activities of Diazoxide.
Captopril Phentermine may decrease the antihypertensive activities of Captopril.
Epoprostenol Phentermine may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Phentermine may decrease the antihypertensive activities of Polythiazide.
Cilazapril Phentermine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Phentermine may decrease the antihypertensive activities of Saprisartan.
Spirapril Phentermine may decrease the antihypertensive activities of Spirapril.
Tienilic acid Phentermine may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Phentermine may decrease the antihypertensive activities of Debrisoquine.
Diethylnorspermine Phentermine may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Phentermine may decrease the antihypertensive activities of Temocapril.
Hexamethonium Phentermine may decrease the antihypertensive activities of Hexamethonium.
Nicorandil Phentermine may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Phentermine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Phentermine may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Phentermine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Phentermine may decrease the antihypertensive activities of Imidapril.
BQ-123 Phentermine may decrease the antihypertensive activities of BQ-123.
Cicletanine Phentermine may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Phentermine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Phentermine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Phentermine may decrease the antihypertensive activities of Guanoxan.
Delapril Phentermine may decrease the antihypertensive activities of Delapril.
Vincamine Phentermine may decrease the antihypertensive activities of Vincamine.
Linsidomine Phentermine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Phentermine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Phentermine may decrease the antihypertensive activities of Tolonidine.
Endralazine Phentermine may decrease the antihypertensive activities of Endralazine.
Cadralazine Phentermine may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Phentermine may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Phentermine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Phentermine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Phentermine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Phentermine may decrease the antihypertensive activities of Guanoclor.
Muzolimine Phentermine may decrease the antihypertensive activities of Muzolimine.
Xipamide Phentermine may decrease the antihypertensive activities of Xipamide.
Candesartan Phentermine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Phentermine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Phentermine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Phentermine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Phentermine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Phentermine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Phentermine may decrease the antihypertensive activities of Quinaprilat.
Furosemide Phentermine may decrease the antihypertensive activities of Furosemide.
Amlodipine Phentermine may decrease the antihypertensive activities of Amlodipine.
Nimodipine Phentermine may decrease the antihypertensive activities of Nimodipine.
Lercanidipine Phentermine may decrease the antihypertensive activities of Lercanidipine.
Indapamide Phentermine may decrease the antihypertensive activities of Indapamide.
Guanfacine Phentermine may decrease the antihypertensive activities of Guanfacine.
Nitrendipine Phentermine may decrease the antihypertensive activities of Nitrendipine.
Bepridil Phentermine may decrease the antihypertensive activities of Bepridil.
Ambrisentan Phentermine may decrease the antihypertensive activities of Ambrisentan.
Pinacidil Phentermine may decrease the antihypertensive activities of Pinacidil.
Riociguat Phentermine may decrease the antihypertensive activities of Riociguat.
Macitentan Phentermine may decrease the antihypertensive activities of Macitentan.
Aliskiren Phentermine may decrease the antihypertensive activities of Aliskiren.
Lacidipine Phentermine may decrease the antihypertensive activities of Lacidipine.
Selexipag Phentermine may decrease the antihypertensive activities of Selexipag.
Dexniguldipine Phentermine may decrease the antihypertensive activities of Dexniguldipine.
Tadalafil Phentermine may decrease the antihypertensive activities of Tadalafil.
Nisoldipine Phentermine may decrease the antihypertensive activities of Nisoldipine.
Eplerenone Phentermine may decrease the antihypertensive activities of Eplerenone.

Target Protein

Sodium-dependent noradrenaline transporter SLC6A2
Sodium-dependent serotonin transporter SLC6A4
Sodium-dependent dopamine transporter SLC6A3
Amine oxidase [flavin-containing] A MAOA
Amine oxidase [flavin-containing] B MAOB
Pro-neuropeptide Y NPY

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29489234
    Johnson DB, Quick J: Topiramate And Phentermine .
  • PMID: 27773937
    Ryder JR, Kaizer A, Rudser KD, Gross A, Kelly AS, Fox CK: Effect of phentermine on weight reduction in a pediatric weight management clinic. Int J Obes (Lond). 2017 Jan;41(1):90-93. doi: 10.1038/ijo.2016.185. Epub 2016 Oct 24.
  • PMID: 24457398
    Kiortsis DN: A review of the metabolic effects of controlled-release Phentermine/Topiramate. Hormones (Athens). 2013 Oct-Dec;12(4):507-16.
  • PMID: 23738843
    Garvey WT: Phentermine and topiramate extended-release: a new treatment for obesity and its role in a complications-centric approach to obesity medical management. Expert Opin Drug Saf. 2013 Sep;12(5):741-56. doi: 10.1517/14740338.2013.806481. Epub 2013 Jun 6.
  • PMID: 29244650
    Bersoux S, Byun TH, Chaliki SS, Poole KG: Pharmacotherapy for obesity: What you need to know. Cleve Clin J Med. 2017 Dec;84(12):951-958. doi: 10.3949/ccjm.84a.16094.
  • PMID: 12788841
    Weigle DS: Pharmacological therapy of obesity: past, present, and future. J Clin Endocrinol Metab. 2003 Jun;88(6):2462-9. doi: 10.1210/jc.2003-030151.
  • PMID: 4415200
    Adebonojo FO: Primary exogenous obesity. A conceptual classification. Clin Pediatr (Phila). 1974 Sep;13(9):715-8. doi: 10.1177/000992287401300901.
Textbook
  • ISBN: 978-1-60413-204-5
    May S. (2009). Weight-Loss Drugs. Chelsea House Publishers.
  • Barceloux D.G. (2012). Medical toxicology of drug abuse: Synthesized chemicals and psychoactive plants.. Wiley.

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  • Umi-Pex — Fernidale Labs

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