Levamlodipine Besylate Tablets

Levamlodipine Besylate Tablet

Generic name: Levamlodipine Besylate Tablets
Brand name:XinTa
Chemical Name: (S) - (-) - 3-Ethyl-5- methyl-2- (2-aminoethoxymethyl) -4- Methyl- 3,5- pyridinedicarboxylate
besylate
Chemical Structure:

 

Molecular formula: C20H25 Cl N2O5·C6H6O3S
Molecular weight: 567.05
Description: White round Tablet.
Strength: 2.5mg
Indications: (1) hypertension; (2)Angina.
Dosage and Administration:
 (1) The initial dose for the treatment of hypertension and angina pectoris is 2.5 mg once a day. Depending
on the patient's clinical response, the dose may be increased up to 5 mg once daily. 
(2) This product and thiazide diuretics, β-blockers and angiotensin converting enzyme inhibitors do not need
to adjust the dose when combined.Adverse ReactionsAdverse reactions to patients with this product can be
well tolerated.
(1) The less common side effects : headache, edema, fatigue, insomnia, nausea, abdominal pain, redness,
heart palpitations and dizziness;
(2) rare side effects: itching, rash, difficulty breathing, weakness, muscle spasms and indigestion;
(3) similar to other calcium antagonists, with minimal adverse reactions to myocardial infarction and chest
pain, and these adverse reactions can not be clearly distinguished from the patient's underlying disease;
(4) Have not found the laboratory-related parameters of this product abnormalities.
ContraindicationsDisable dihydropyridine calcium antagonist patients.
Precautions:
 (1) the use of impaired liver function, and all other calcium antagonists the same, the use of this product
should be very careful when impaired liver function.
 (2) the use of renal failure patients, patients with impaired renal function can use the normal dose.
 (3) This product is not dialysis.
Pharmacology and toxicology:
(1) This product is calcium influx blockers (calcium channel blockers or calcium antagonists), block
myocardial and vascular smooth muscle extracellular calcium ion through the cell membrane calcium channel
(slow Channel) into the cell. 
(2) This product directly vasodilator smooth muscle, with anti-hypertensive effect. 
(3) The mechanism of relieving angina pectoris has not yet been fully determined, but it can reduce
myocardial ischemia by a) expanding the peripheral arterioles and reducing the peripheral resistance
(afterload), thereby reducing the myocardial energy expenditure and oxygen demand; b) Dilatation of
coronary arteries and coronary arteries in both normal and ischemic areas increases myocardial oxygen
supply to patients with coronary artery spasm (variant angina).
(4) This product is metabolized for a long time in liver, and is the same with all other calcium antagonists.
It is very careful to use this product when liver function is damaged.
Pharmacokinetics:
 (1) According to the literature, oral administration of amlodipine besylate tablets, 6-12 hours plasma
concentration reached its peak, the absolute bioavailability of about 64-80%, the apparent volume of
distribution of about 21L / kg, terminal elimination half-life of about 35-50 hours.  Once a day, continuous
administration of blood plasma concentration 7-8 days steady state, amlodipine besylate widely metabolized
by the liver as inactive metabolites to 10% of the prototype drug and 60% of the metabolites by the urine
Excretion, plasma protein binding rate of 97.5%. 
(2) According to the literature, 18 healthy volunteers once oral administration of 20mg racemic amlodipine,
pharmacologically active levamlodipine and inactive dexamtrodipine average peak plasma concentration
ratio of 47: 53, the average AUC ratio of 41:49.  The average terminal elimination half-life of levamlodipine
was 49.6 hours, and dexamlodipine was 34.9 hours. The half-life of elimination of amlodipine was
significantly correlated with the half-life of levamlodipine.
Storage: Shading, sealed, cool place (no more than 20 ºC preservation.
Packing :Double aluminum blister packaging.  7Tablets/ Blister,14Tablet/box, 21Tablet/box.
Shelf-life: 24 months