Lacidipine

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Lacidipine.jpg

[edit] MECHANISM OF ACTION

Lacidipine is a potent dihydropyridine calcium channel blocker with predominant selectivity on calcium channels in vascular smooth muscle than on cardiac smooth muscle. Lacidipine inhibits the influx of extra cellular calcium across the peripheral arterial smooth muscle cell membranes by binding directly to inactive L-type calcium channels, stabilizing their inactive conformation.

The decrease in intracellular calcium inhibits the contractile processes of the systemic arteries smooth muscle cells, and thus, decreases total peripheral resistance and systemic blood pressure.

Lacidipine is characterized by long duration of action. Plasma elimination half-life ranges from 13 to 19 hours at steady state.

After administration oral lacidipine is poorly absorbed from the gastrointestinal tract. The drug also undergoes extensive first-pass metabolism in the liver. Absolute bioavailability averages about 10 %. Peak plasma concentrations are reached between 30 and 150 minutes. The drug is eliminated primarily by hepatic metabolism (involving P450 CYP3A4 isoform ). There is no evidence that lacidipine causes either induction or inhibition of hepatic enzymes. The metabolites of the drug has such a low key pharmacodynamic activity. Approximately 70 % of the administered dose is eliminated as metabolites in the feces and the remainder as metabolites in the urine.

[edit] INDICATIONS

[edit] DOSAGE

The recommended starting dose is 2 mg once a day, preferably in the morning, with or without food.

The dose may be increased to 4 mg and even 6 mg once a day in the morning after about 3-4 weeks unless the condition of the case requires a rapid titration to raise the dose.

No dose adjustment is required in elderly patients

[edit] CONTRAINDICATIONS

  • Known sensitivity to Lacidipine
  • Patients with advanced aortic stenosis
  • Pregnancy and lactation

[edit] WARNINGS AND PRECAUTIONS

  • Lacidipine may lead to reflex tachycardia which, particularly in patients with severe obstructive coronary artery disease, may precipitate angina pectoris
  • Lacidipine should be used with caution in patients with impaired liver function because antihypertensive effect may be increased

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy: Lacidipine should only be used in pregnancy when the potential benefits for the mother outweigh the possibility of adverse effects in the fetus or neonate. The possibility that Lacidipine can cause relaxation of the uterine muscle at term should be considered.
  • Lactation: Milk transfer studies in animals have shown that lacidipine (or its metabolites) are likely to be excreted into breast milk. Lacidipine should only be used during lactation when the potential benefits for the mother outweigh the possibility of adverse effects in the fetus or neonate.

[edit] SIDE EFFECTS

Most common: dizziness, headache, flushing, tachycardia, Skin rash or itching, palpitations and localised peripheral edema of non-cardiac origin (local arterial dilatation seems to be involved rather than fluid retention). These tend to disappear or to decrease as treatment continues.

  • Anaphylactic reactions (rare)

[edit] RELATED LINKS

Calcium Channel Blockers Pharmacology

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)