Peringatan Keamanan

There are no available human data on aminolevulinic acid (ALA) in pregnant women to inform a drug-associated risk of adverse developmental outcomes. In animal reproduction studies, no adverse developmental effects were observed with oral ALA HCl administration to pregnant rabbits during organogenesis at doses 3 times the maximum recommended human oral dose.L40353

No carcinogenicity testing has been carried out using ALA. No evidence of mutagenic effects was seen in four studies conducted with ALA to evaluate this potential. In the Salmonella-Escherichia coli/mammalian microsome reverse mutation assay (Ames mutagenicity assay), no increases in the number of revertants were observed with any of the tester strains. In the Salmonella-Escherichia coli/mammalian microsome reverse mutation assay in the presence of solar light radiation (Ames mutagenicity assay with light), ALA did not cause an increase in the number of revertants per plate of any of the tester strains in the presence or absence of simulated solar light. In the L5178Y TK± mouse lymphoma forward mutation assay, ALA was evaluated as negative with and without metabolic activation under the study conditions. PpIX formation was not demonstrated in any of these in vitro studies. In the in vivo mouse micronucleus assay, ALA was considered negative under the study exposure conditions. In contrast, at least one report in the literature has noted genotoxic effects in cultured rat hepatocytes after ALA exposure with PpIX formation. Other studies have documented oxidative DNA damage in vivo and in vitro as a result of ALA exposure.L40348

No assessment of effects of ALA HCl on fertility has been performed in laboratory animals. It is unknown what effects systemic exposure to ALA HCl might have on fertility or reproductive function.L40348

Aminolevulinic acid

DB00855

small molecule approved

Deskripsi

A compound produced from succinyl-CoA and glycine as an intermediate in heme synthesis. It is used as a photochemotherapy for actinic keratosis. PubChem

Struktur Molekul 2D

Berat 131.1299
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 ± SD elimination half-life (t<sub>1/2</sub>) of aminolevulinic acid was 5.7 ± 3.9 hours for the topical solution formulation and the mean half-life was 0.9 ± 1.2 hours for the oral solution formulation.[L40348,L40353] In another pharmacokinetic studies with 6 healthy volunteers using a 128 mg dose, the mean half-life was 0.70 ± 0.18 h after the oral dose and 0.83 ± 0.05 h after the intravenous dose.[L48491]
Volume Distribusi In healthy volunteers, the administration of aminolevulinic acid resulted in a volume of distribution of 9.3 ± 2.8 L intravenously and 14.5 ± 2.5 orally.[11961050]
Klirens (Clearance) -

Absorpsi

Oral bioavailability is 50-60%. ### Topical gel Pharmacokinetics (PK) of aminolevulinic acid (ALA) and PpIX was evaluated in a trial of 12 adult subjects with mild to moderate AK with at least 10 AK lesions on the face or forehead. A single dose of one entire tube of ALA (2 grams) was applied under occlusion for 3 hours followed by photodynamic therapy (PDT) to a total area of 20 cm2. The mean ± SD baseline plasma ALA and PpIX concentrations were 20.16 ± 16.53 ng/mL and 3.27 ± 2.40 ng/mL, respectively. In most subjects, an up to 2.5-fold increase of ALA plasma concentrations was observed during the first 3 hours after ALA application. The mean ± SD area under the concentration time curve (AUC0-t) and maximum concentration (Cmax) for baseline corrected ALA (n=12) were 142.83 ± 75.50 ng.h/mL and 27.19 ± 20.02 ng/mL, respectively. The median Tmax (time at which Cmax occurred) was 3 hours. ### Topical solution Two human pharmacokinetic (PK) studies were conducted in subjects with minimally to moderately thick actinic keratoses on the upper extremities, having at least 6 lesions on one upper extremity and at least 12 lesions on the other upper extremity. A single dose comprising of two topical applications of ALA topical solution (each containing 354 mg ALA HCl) were directly applied to the lesions and occluded for 3 hours prior to light treatment. The first PK study was conducted in 29 subjects and PK parameters of ALA were assessed. The baseline corrected mean ± SD of the maximum concentration (Cmax) of ALA was 249.9 ± 694.5 ng/mL and the median Tmax was 2 hours post dose. The mean ± SD exposure to ALA, as expressed by area under the concentration time curve (AUCt) was 669.9 ± 1610 ng·hr/mL. The mean ± SD elimination half-life (t1/2) of ALA was 5.7 ± 3.9 hours. A second PK study was conducted in 14 subjects and PK parameters of ALA and PpIX were measured. The baseline corrected PpIX concentrations were negative in at least 50% of samples in 50% (7/14) subjects and AUC could not be estimated reliably. The baseline-corrected mean ± SD of Cmax for ALA and PpIX was 95.6 ± 120.6 ng/mL and 0.95 ± 0.71 ng/mL, respectively. The median Tmax of ALA and PpIX was 2 hours post dose and 12 hours post dose, respectively. The mean AUCt of ALA was 261.1 ± 229.3 ng·hr/mL. The mean ± SD t1/2 of ALA was 8.5 ± 6.7 hours. ### Oral solution In 12 healthy subjects, the absolute bioavailability of ALA following the recommended dose of ALA solution was 100.0% + 1.1 with a range of 78.5% to 131.2%. Maximum ALA plasma concentrations were reached with a median of 0.8 hour (range 0.5 – 1.0 hour).

Metabolisme

Exogenous aminolevulinic acid (ALA) is metabolized to PpIX, but the fraction of administered ALA that is metabolized to PpIX is unknown. The average plasma AUC of PpIX is less than 6% of that of ALA.L40353

Rute Eliminasi

In 12 healthy subjects, excretion of parent aminolevulinic acid (ALA) in urine in the 12 hours following administration of the recommended dose of ALA solution was 34 + 8% (mean + std dev) with a range of 27% to 57%.L40353

Interaksi Obat

42 Data
Porfimer sodium Aminolevulinic acid may increase the photosensitizing activities of Porfimer sodium.
Verteporfin Aminolevulinic acid may increase the photosensitizing activities of Verteporfin.
Tretinoin The risk or severity of adverse effects can be increased when Tretinoin is combined with Aminolevulinic acid.
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Aminolevulinic acid.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Aminolevulinic acid.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Aminolevulinic acid.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Aminolevulinic acid.
Padeliporfin Aminolevulinic acid may increase the photosensitizing activities of Padeliporfin.
Lidocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Quinisocaine.
Ambroxol The risk or severity of methemoglobinemia can be increased when Aminolevulinic acid is combined with Ambroxol.
Etrasimod The risk or severity of immunosuppression can be increased when Aminolevulinic acid is combined with Etrasimod.

Target Protein

Protoporphyrinogen oxidase PPOX
Delta-aminolevulinic acid dehydratase ALAD

Referensi & Sumber

Synthesis reference: Takashi Ebata, Hiroshi Kawakami, Katsuya Matsumoto, Koshi Koseki, Hajime Matsushita, "Method of preparing an acid additional salt of delta-aminolevulinic acid." U.S. Patent US5284973, issued July, 1974.
Artikel (PubMed)
  • PMID: 16648043
    Stummer W, Pichlmeier U, Meinel T, Wiestler OD, Zanella F, Reulen HJ: Fluorescence-guided surgery with 5-aminolevulinic acid for resection of malignant glioma: a randomised controlled multicentre phase III trial. Lancet Oncol. 2006 May;7(5):392-401.
  • PMID: 9612195
    Kennedy JC, Marcus SL, Pottier RH: Photodynamic therapy (PDT) and photodiagnosis (PD) using endogenous photosensitization induced by 5-aminolevulinic acid (ALA): mechanisms and clinical results. J Clin Laser Med Surg. 1996 Oct;14(5):289-304.
  • PMID: 11961050
    Dalton JT, Yates CR, Yin D, Straughn A, Marcus SL, Golub AL, Meyer MC: Clinical pharmacokinetics of 5-aminolevulinic acid in healthy volunteers and patients at high risk for recurrent bladder cancer. J Pharmacol Exp Ther. 2002 May;301(2):507-12. doi: 10.1124/jpet.301.2.507.

Contoh Produk & Brand

Produk: 10 • International brands: 1
Produk
  • Ameluz
    Gel • 100 mg/1g • Topical • US • Approved
  • Ameluz
    Gel • 78 mg/g • Cutaneous • EU • Approved
  • Gleolan
    Powder, for solution • 1500 mg/1 • Oral • US • Approved
  • Gleolan
    Powder, for solution • 1.5 g / vial • Oral • Canada • Approved
  • Gleolan
    Powder, for solution • 1500 mg/1 • Oral • US • Approved
  • Gliolan
    Powder, for solution • 30 mg/ml • Oral • EU • Approved
  • Gliolan
    Powder, for solution • 30 mg/ml • Oral • EU • Approved
  • Gliolan
    Powder, for solution • 30 mg/ml • Oral • EU • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Levulan — DUSA Pharmaceuticals, Inc.

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