What Is Lacidipine?

Laxidipine can be used to treat high blood pressure. This product is a specific, strong and durable dihydropyridine calcium channel blocker, which mainly selectively blocks the calcium channels of vascular smooth muscle, expands peripheral arteries, reduces peripheral vascular resistance, reduces cardiac afterload, and reduces blood pressure.

Drug Name: Laxidipine
Foreign name: Lacidipine, Lacipil
Main indications: Treating hypertension

Function use: Dilatation of peripheral arteries
CAS: 103890-78-4
Molecular formula: C26H33NO6
Molecular weight: 455.54300

Laxidipine Basic Information

Chinese name

Chinese alias: (E) -4- [2- [3- (1,1-dimethylethoxy) -3-oxo-1-propenyl] phenyl] -1,4-dihydro-2 , 6-dimethyl-3,5-pyridine dicarboxylic acid diethyl ester

English name: diethyl 2,6-dimethyl-4- [2-[(E) -3-[(2-methylpropan-2-yl) oxy] -3-oxoprop-1-enyl] phenyl] -1,4- dihydropyridine-3,5-dicarboxylate

English alias: Motens; Lacipil; Lacidipine;

Drug classification: Chemical drug circulation (cardiovascular) system drugs

CAS number: 103890-78-4

Molecular formula: C ₂₆ H ₃₃ NO ₆

Molecular weight: 455.54300

Exact mass: 455.23100

PSA: 90.93000

LogP: 4.73130

Lasidipine physical and chemical properties

Appearance and properties: white to off-white crystalline solid

Density: 1.127 g / cm ³

Melting point: 174-175 ° C

Boiling point: 558.4ºC at 760 mmHg

Flash point: 291.5ºC

Refractive index: 1.54

Storage conditions: Store in original container in a cool dark place.

Vapor pressure: 1.67E-12mmHg at 25 ° C ^[1]

Laxidipine production method

Orthophthalaldehyde and tert-butyl triphenylphosphine acetate were reacted in dichloromethane at 0 ° C for 15 minutes to obtain tert-butyl 3- (2-formylphenyl) acrylate. Then, it was obtained by reacting with ethyl 2-amino-2-butenoate in acetic acid at room temperature for 5h. ^[2]

Lasilidipine Lasilidipine related drug label information

Laxidipine pharmacological action

It is a specific, strong and durable dihydropyridine calcium channel blocker, which mainly selectively blocks the calcium channels of vascular smooth muscle, expands peripheral arteries, reduces peripheral vascular resistance, reduces cardiac postload, and reduces blood pressure. The selectivity ratio to blood vessels and heart is nearly 100. In normal volunteers, 3 to 5 mg, the peripheral vascular resistance decreased in a dose-dependent manner. Does not affect sinoatrial or atrioventricular conduction, nor does it affect autonomic tissue.

Lacidipine pharmacokinetics

Oral intestinal absorption is rapid but incomplete, with absolute bioavailability of 30% to 52%. The peak time of plasma concentration is 30 ~ 150min. Plasma protein binding rate was 95%. Elimination half-life is about 8h. Metabolized only in the liver, there are 4 metabolites with lower pharmacological activity. 70% of the drug is excreted in the feces as metabolites, and the remaining metabolites are excreted in urine.

Laxidipine Elixir Type

Tablet: 2mg, 4mg.

Laxidipine contraindications

1. Severe aortic stenosis. 2. Allergic to this medicine or other calcium channel blockers.

Laxidipine dosage

Laxidipine is administered once daily, 2 mg orally after breakfast, and if the blood pressure drops to a significant level after 1 week, it is maintained at the original dose. If the significant level is not reached, it should be increased by 2 mg per week, and the maximum dose is 8 mg per day. The control group took felodipine, 2.5 mg daily, and gradually increased to 10 mg. The maximum dose was 20 mg daily.

Lacidipine drug interactions

1. Amiodarone combined with calcium channel blockers can further slow sinus rhythm and aggravate atrioventricular block. Therefore, patients with sinus bradycardia or atrioventricular block should avoid using this drug in combination with amiodarone. 2. It is well tolerated in combination with -blockers, which is beneficial for the treatment of angina pectoris and hypertension. However, in patients with left ventricular dysfunction, arrhythmia, or aortic stenosis, the combination of -blockers and dihydropyridine calcium channel blockers can easily cause significant hypotension and cardiac depression. If this drug is used in combination with -blockers, cardiac function should be carefully monitored, especially in patients with potential heart failure. 3. Cimetidine can increase the blood concentration of this drug. 4. Delafadine can inhibit the metabolism of this drug mediated by cytochrome P4503A4, increase the blood concentration of this drug, and increase its toxicity. 5. When using fentanyl anesthesia, the combination of calcium channel blockers (such as this drug) and -blockers can cause severe hypotension. When interactions are estimated to occur, fluids should be replenished. 6. Quinopeptin / dafoputin is a cytochrome P4503A4 enzyme inhibitor, which can increase the blood concentration of this drug. If combined, monitor for adverse reactions and reduce the dosage if necessary. 7. Although no interaction between this drug and saquinavir has been reported, saquinavir has an inhibitory effect on the liver cytochrome P4503A4 enzyme family, so it may reduce the metabolism of this drug and increase the blood concentration of this drug , Increased toxicity. 8. Calcium channel blockers can increase the possibility of gastrointestinal bleeding caused by non-steroidal anti-inflammatory drugs or oral anticoagulants, and should be closely monitored for signs of gastrointestinal bleeding when combined. 9. Although no interaction with rifampicin has been reported, rifampicin can induce the liver cytochrome P450 enzyme system, so it may reduce the blood concentration of this drug and reduce the efficacy. 10. Ephedra is a natural medicine containing ephedrine and pseudoephedrine, which has an uncertain effect on the blood pressure of normal individuals and can reduce the efficacy of antihypertensive drugs. Patients with hypertension treated with this drug should avoid taking ephedra-containing preparations.

Laxipine indication

Angina pectoris due to hypertension, coronary atherosclerotic heart disease.

Laxidipine precautions

Use with caution: (1) Patients with angina pectoris may experience increased angina pectoris when calcium channel blockers are started or the dosage is increased. Caution should be used. (2) Chronic renal insufficiency. (3) Caution should be exercised in patients with left ventricular dysfunction using beta blockers. (4) Congestive heart failure. (5) It is recommended to stop lacidipine 36 hours before fentanyl anesthesia. (6) Sustained-release preparations should be used with caution when gastrointestinal motility is enhanced or gastrointestinal obstruction. (7) Patients with hypotension should be cautious when starting treatment and in combination with -blockers. (8) Use with caution in pregnant and lactating women. 2. Dosage adjustment should be 3 to 4 weeks apart. 3. Patients with hepatic insufficiency or elderly need to be halved at the beginning. 4. Overdose can cause hypotension and tachycardia. At this time, fluid replacement and booster drugs are needed.

Laxidipine adverse reactions

It is mostly related to its vasodilator effect, such as headache, skin flushing, edema, dizziness, fatigue, and palpitations, which are usually transient and gradually disappear or weaken with continued use. Rarely, rash, erythema, itching, lack of appetite, nausea, polyuria, rare chest pain, hyperplasia of the gums, transient elevated alkaline phosphatase. It usually disappears or returns to normal after stopping the medicine.

Efficacy Evaluation Standards of Laxipine

Significant effect: blood pressure decreased to normal range, systolic blood pressure 140mmHg, diastolic blood pressure 90mmHg; Effective: Diastolic blood pressure decreased by 20mmHg, but did not reach normal range; Invalid: Antihypertensive effect did not reach effective level. Significant effect plus effective is the total effective rate. ^[3]