Lacidipine; Uses, Dosage, Side Effects, Interactions

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. 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.

Mechanism of Action of Lacidipine

By blocking the voltage-dependent L-type calcium channels, it prevents the transmembrane calcium influx. Normally, calcium ions serve as intracellular messengers or activators in excitable cells including vascular smooth muscles. The influx of calcium ultimately causes the excitation and depolarization of the tissues. Lacidipine inhibits the contractile function in the vascular smooth muscle and reduce blood pressure. Due to its high membrane partition coefficient, some studies suggest that lacidipine may reach the receptor via a two-step process; it first binds and accumulates in the membrane lipid bilayer and then diffuses within the membrane to the calcium channel receptor. It is proposed that lacidipine preferentially blocks the inactivated state of the calcium channel. Through its antioxidant properties shared amongst other dihydropyridine calcium channel blockers, lacidipine demonstrates an additional clinical benefit. Its antiatherosclerotic effects are mediated by suppressing the formation of reactive oxygen species (ROS) and subsequent inflammatory actions by chemokines, cytokines and adhesion molecules, thus reducing atherosclerotic lesion formation. Lacidipine may also suppress cell proliferation and migration in smooth muscle cells and suppress the expression of matrix metalloproteinases, which affects the stability of atheromatous plaques

Indications of Lacidipine

• High blood pressure (Hypertension)
• Angina pectoris prophylaxis
• Raynaud’s Syndrome
• Heart failure
• Angina pectoris prophylaxis
• Also for the treatment of hypertension either alone or in combination with other antihypertensive agents, including β-adrenoceptor antagonists, diuretics, and ACE-inhibitors

Contra-Indications of Lacidipine

• The acute syndrome of the heart
• Severe narrowing of the aortic heart valve
• Severe heart failure
• Abnormally low blood pressure
• Kidney disease with the reduction in kidney function
• Fluid Retention in the Legs, arms or hands
• Blood Circulation Failure due to Serious Heart Condition
• Chronic idiopathic constipation
• Stomach or intestine blockage
• Narrowing of the intestines
• Decreased motility function of the stomach or intestines

Dosage of Lacidipine

Strengths: 2 mg, 4 mg, 6 mg

Hypertension

• The recommended initial dose is 2 mg once daily.
• The dose may be increased to 4 mg (and then, if necessary, to 6 mg) after adequate time has been allowed for the full pharmacological effect to occur. In practice, this should not be less than 3 to 4 weeks.
• Daily doses above 6 mg have not been shown to be significantly more effective.

Side Effects of Lacidipine

The most common 

• a severe headache, rapid heartbeat, stiffness in your neck,  
• chest pain, fast or slow heart rate;
• swelling, rapid weight gain;
• Xerostomia (dry mouth)
• A headache 
• Fatigue
• Skin reactions 
• Hypotension
• Anxiety
• Constipation
• Nausea/vomiting
• Weight gain/loss
• Erectile dysfunction

More common

• Abdominal or stomach pain, discomfort, or tenderness
• chills or fever
• difficulty with moving
• a headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in the chest
• discomfort in arms, shoulders, neck or upper back
• excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• sudden slow or difficult speech
• sudden drowsiness or need to sleep
• fast breathing
• sharp pain when taking a deep breath
• fast or slow heartbeat
• coughing up blood
• rust colored urine
• decreased amount of urine

Rare

• Anxiety
• change in vision
• chest pain or tightness
• confusion
• a cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• fainting
• hallucinations
• a headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps
• muscle spasm or jerking of all extremities
• nervousness

Drug Interactions of Lacidipine

Lacidipine may interact with the following drugs, supplements, & may change the efficacy of the drug

• alpha blockers (e.g., alfuzosin, doxazosin, tamsulosin)
• alpha agonists (e.g., clonidine, methyldopa)
• angiotensin II receptor blockers (ARBs; e.g., candesartan, losartan)
• antidiabetes medications (e.g., insulin, metformin, glyburide)
• atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
• azathioprine
• barbiturates (e.g., butalbital, pentobarbital phenobarbital)
• beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
• “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
• calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
• canagliflozin
• ciprofloxacin
• calcium supplements (e.g., calcium carbonate, calcium citrate)
• carbamazepine
• clopidogrel
• cyclosporine
• diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
• duloxetine
• “gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
• guanfacine
• heparin
• levodopa
• medications that increase potassium levels (e.g., potassium supplements, spironolactone, amiloride, and salt substitutes containing potassium)
• metformin
• nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., ibuprofen, indomethacin, naproxen)
• other angiotensin-converting-enzyme inhibitors (ACEIs; e.g., captopril,  ramipril)
• pentoxifylline
• macrolide antibiotics (e.g., clarithromycin, erythromycin)
• methylphenidate
• monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline,selegiline, tranylcypromine)
• phosphodiesterase-5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)
• pregabalin
• sodium phosphates
• tizanidine
• trimethoprim
• valproic acid
• warfarin

Pregnancy Category

FDA Pregnancy Category C

Pregnancy

This medication should not be taken by women who are or may become pregnant, as may lacidipine cause harm to the developing baby if it is taken by the mother during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

This medication should not be taken by women who are breastfeeding. 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. The safety and effectiveness of using this medication have not been established for children.

References

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