Peringatan Keamanan

There have been no recorded cases of lacidipine tablets overdosage. Some of the symptoms of overdose include prolonged peripheral vasodilation associated with hypotension and
tachycardia. Bradycardia or prolonged AV conduction could theoretically occur. As there is no known antidote for lacidipine, the use of standard general measures for monitoring cardiac function and appropriate supportive and therapeutic measures is recommended L1126.

Oral LD50 in mouse, rabbit and rat are 300mg/kg, 3200mg/kg and 980mg/kg, respectively MSDS.

Lacidipine

DB09236

small molecule approved investigational

Deskripsi

Lacidipine is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. Due to its long duration of action, lacidipine does not lead to reflex tachycardia A31536. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure. Compared to other dihydropyridine calcium antagonists, lacidipine exhibits a greater antioxidant activity which may confer potentially beneficial antiatherosclerotic effects A31540. Lacidipine is a highly lipophilic molecule that interacts with the biological membranes. Through radiotracer analysis, it was determined that lacidipine displays a high membrane partition coefficient leading to accumulation of the drug in the membrane and slow rate of membrane washout A31539. When visualized by small-angle X-ray diffraction with angstrom resolution to examine its location within the membranes, lacidipine was found deep within the membrane's hydrocarbon core A31539. These results may explain the long clinical half-life of lacidipine A31539.

In randomised, well-controlled trials, administration of daily single-dose lacidipine ranging from 2-6 mg demonstrated comparable antihypertensive efficacy similar to that of other long-acting dihydropyridine calcium antagonists, thiazide diuretics, atenolol (a beta-blocker) and enalapril (an ACE inhibitor) A31536. It is available as once-daily oral tablets containing 2 or 4 mg of the active compound commonly marketed as Lacipil or Motens. It is not currently FDA-approved.

Struktur Molekul 2D

Berat 455.551
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average terminal half-life of lacidipine ranges from between 13 and 19 hours at steady state [L1126].
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Since it is a highly lipophilic compound, lacidpine is rapidly absorbed from the gastrointestinal tract following oral administration with the peak plasma concentrations reached between 30 and 150 minutes of dosing L1126. The peak plasma concentrations display large interindividual variability, with the values ranging from 1.6 to 5.7 ?g/L following single-dose oral administration of lacidipine 4mg in healthy young volunteers A31537. Absolute bioavailability is less than 10% due to extensive first-pass metabolism in the liver L1126.

Metabolisme

Lacidipine undergoes complete CYP3A4-mediated hepatic metabolism, with no parent drug detected in the urine or faeces. The 2 main metabolites have no pharmacological activity A31537.

Rute Eliminasi

Approximately 70% of the administered dose is eliminated as metabolites in the faeces and the remainder as metabolites in the urine L1126.

Interaksi Obat

1294 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Lacidipine is combined with Duloxetine.
Risperidone Lacidipine may increase the hypotensive activities of Risperidone.
Ceritinib Lacidipine may increase the bradycardic activities of Ceritinib.
Ivabradine Lacidipine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Lacidipine.
Alfuzosin Alfuzosin may increase the hypotensive activities of Lacidipine.
Amifostine Lacidipine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Lacidipine.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Lacidipine.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Lacidipine.
Obinutuzumab Lacidipine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Lacidipine.
Rituximab Lacidipine may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Lacidipine.
Isoetharine Isoetharine may decrease the antihypertensive activities of Lacidipine.
Etomidate Etomidate may decrease the antihypertensive activities of Lacidipine.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Lacidipine.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Lacidipine.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Lacidipine.
Doxapram Doxapram may decrease the antihypertensive activities of Lacidipine.
Metaraminol Metaraminol may decrease the antihypertensive activities of Lacidipine.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Lacidipine.
Methoxamine Methoxamine may decrease the antihypertensive activities of Lacidipine.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Lacidipine.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Lacidipine.
Dobutamine Dobutamine may decrease the antihypertensive activities of Lacidipine.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Lacidipine.
Ritodrine Ritodrine may decrease the antihypertensive activities of Lacidipine.
Bitolterol Bitolterol may decrease the antihypertensive activities of Lacidipine.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Lacidipine.
Naratriptan Naratriptan may decrease the antihypertensive activities of Lacidipine.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Lacidipine.
Dopamine Dopamine may decrease the antihypertensive activities of Lacidipine.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Lacidipine.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Lacidipine.
Arbutamine Arbutamine may decrease the antihypertensive activities of Lacidipine.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Lacidipine.
Fenoterol Fenoterol may decrease the antihypertensive activities of Lacidipine.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Lacidipine.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Lacidipine.
Ephedrine Ephedrine may decrease the antihypertensive activities of Lacidipine.
Mephentermine Mephentermine may decrease the antihypertensive activities of Lacidipine.
Procaterol Procaterol may decrease the antihypertensive activities of Lacidipine.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Lacidipine.
Bambuterol Bambuterol may decrease the antihypertensive activities of Lacidipine.
MMDA MMDA may decrease the antihypertensive activities of Lacidipine.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Lacidipine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Lacidipine.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Lacidipine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Lacidipine.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Lacidipine.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Lacidipine.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Lacidipine.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Lacidipine.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Lacidipine.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Lacidipine.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Lacidipine.
Amineptine Amineptine may decrease the antihypertensive activities of Lacidipine.
Amibegron Amibegron may decrease the antihypertensive activities of Lacidipine.
Naluzotan Naluzotan may decrease the antihypertensive activities of Lacidipine.
Solabegron Solabegron may decrease the antihypertensive activities of Lacidipine.
Droxidopa Droxidopa may decrease the antihypertensive activities of Lacidipine.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Lacidipine.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Lacidipine.
Isometheptene Isometheptene may decrease the antihypertensive activities of Lacidipine.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Lacidipine.
Naphazoline Naphazoline may decrease the antihypertensive activities of Lacidipine.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Lacidipine.
Cinitapride Cinitapride may decrease the antihypertensive activities of Lacidipine.
Tyramine Tyramine may decrease the antihypertensive activities of Lacidipine.
Adrafinil Adrafinil may decrease the antihypertensive activities of Lacidipine.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Lacidipine.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Lacidipine.
Etilefrine Etilefrine may decrease the antihypertensive activities of Lacidipine.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Lacidipine.
Cirazoline Cirazoline may decrease the antihypertensive activities of Lacidipine.
Synephrine Synephrine may decrease the antihypertensive activities of Lacidipine.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Lacidipine.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Lacidipine.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Lacidipine.
Racepinephrine Racepinephrine may decrease the antihypertensive activities of Lacidipine.
DL-Methylephedrine DL-Methylephedrine may decrease the antihypertensive activities of Lacidipine.
Amitraz Amitraz may decrease the antihypertensive activities of Lacidipine.
Medetomidine Medetomidine may decrease the antihypertensive activities of Lacidipine.
Xylazine Xylazine may decrease the antihypertensive activities of Lacidipine.
Atipamezole Atipamezole may decrease the antihypertensive activities of Lacidipine.
Ractopamine Ractopamine may decrease the antihypertensive activities of Lacidipine.
Romifidine Romifidine may decrease the antihypertensive activities of Lacidipine.
Detomidine Detomidine may decrease the antihypertensive activities of Lacidipine.
Etafedrine Etafedrine may decrease the antihypertensive activities of Lacidipine.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Lacidipine.
PF-00610355 PF-00610355 may decrease the antihypertensive activities of Lacidipine.
Ritobegron Ritobegron may decrease the antihypertensive activities of Lacidipine.
Abediterol Abediterol may decrease the antihypertensive activities of Lacidipine.
Tulobuterol Tulobuterol may decrease the antihypertensive activities of Lacidipine.
Dopexamine Dopexamine may decrease the antihypertensive activities of Lacidipine.
Piclozotan Piclozotan may decrease the antihypertensive activities of Lacidipine.
Idazoxan Idazoxan may decrease the antihypertensive activities of Lacidipine.
Higenamine Higenamine may decrease the antihypertensive activities of Lacidipine.
Reproterol Reproterol may decrease the antihypertensive activities of Lacidipine.

Target Protein

Voltage-dependent L-type calcium channel CACNA1C

Referensi & Sumber

Synthesis reference: Lacidipine synthesis: C. Semeraro et al., DE 3529997; eidem, U.S. Patent 4,801,599 (1986, 1989 both to Glaxo).
Artikel (PubMed)
  • PMID: 14524737
    McCormack PL, Wagstaff AJ: Lacidipine: a review of its use in the management of hypertension. Drugs. 2003;63(21):2327-56.
  • PMID: 7527328
    Lee CR, Bryson HM: Lacidipine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the treatment of hypertension. Drugs. 1994 Aug;48(2):274-96.
  • PMID: 8387105
    Herbette LG, Gaviraghi G, Tulenko T, Mason RP: Molecular interaction between lacidipine and biological membranes. J Hypertens Suppl. 1993 Mar;11(1):S13-9.
  • PMID: 22653165
    Ishii N, Matsumura T, Shimoda S, Araki E: Anti-atherosclerotic potential of dihydropyridine calcium channel blockers. J Atheroscler Thromb. 2012;19(8):693-704. Epub 2012 May 17.
  • PMID: 9051306
    Cerbai E, Giotti A, Mugelli A: Characteristics of L-type calcium channel blockade by lacidipine in guinea-pig ventricular myocytes. Br J Pharmacol. 1997 Feb;120(4):667-75. doi: 10.1038/sj.bjp.0700951.

Contoh Produk & Brand

Produk: 0 • International brands: 4
International Brands
  • Caldine — Boehringer Ingelheim
  • Lacimen — GlaxoSmithKline
  • Lacipil — GSK
  • Motens — Boehringer Ingelheim

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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