Actions of Amlodipino Chemopharma in details
Calcium-channel blocker.
Pharmacology: Pharmacodynamics: S(-) Amlodipino Chemopharma, the chirally pure form of Amlodipino Chemopharma, is a calcium channel antagonist belonging to the dihydropyridine class. The S(-) isomer of Amlodipino Chemopharma is found to possess greater pharmacological effects than R(+) Amlodipino Chemopharma. S(-) Amlodipino Chemopharma is 1000 times more potent than the R(+) isomer in binding to the dihydropyridine receptor. In humans, the dominant effects of Amlodipino Chemopharma are consequent to vasodilation. S(-) Amlodipino Chemopharma lowers peripheral vascular resistance without causing a reflex tachycardia. It is effective as a once-daily dosing in the control of hypertension.
Pharmacokinetics: Administration of S(-) Amlodipino Chemopharma 2.5 mg as a single dose in the fasting state produced maximum plasma concentration (Cmax) of 8.3 ± 1.071 ng/mL in 2.73 ± 0.88 hrs (Tmax). Amlodipino Chemopharma is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine. Ex vivo studies have shown that approximately 93% of the circulating drug is bound to plasma proteins in hypertensive patients. The mean AUC0-t value (t=48 hrs) of Amlodipino Chemopharma 2.5 mg is 95.33 ± 14.45 ng·hr/mL. The AUC0-∞ value is recorded to be 140.91 ± 28.06 ng·hr/mL. The plasma elimination half-life of S(-) Amlodipino Chemopharma has been found to be in the range of 14.62-68.88 hrs.
How should I take Amlodipino Chemopharma?
Take Amlodipino Chemopharma exactly as prescribed by your doctor. Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use this medicine in larger or smaller amounts or for longer than recommended.
You may take Amlodipino Chemopharma with or without food. Take the medicine at the same time each day.
Your blood pressure will need to be checked often.
Your chest pain may become worse when you first start taking Amlodipino Chemopharma or when your dose is increased. Call your doctor if your chest pain is severe or ongoing.
If you are being treated for high blood pressure, keep using Amlodipino Chemopharma even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medicine for the rest of your life.
Your hypertension or heart condition may be treated with a combination of drugs. Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication. Do not change your doses or stop taking any of your medications without your doctor's advice. This is especially important if you also take nitroglycerin.
Amlodipino Chemopharma is only part of a complete program of treatment that may also include diet, exercise, weight control, and other medications. Follow your diet, medication, and exercise routines very closely.
Store at room temperature away from moisture, heat, and light.
Amlodipino Chemopharma administration
Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Amlodipino Chemopharma is usually taken once daily. Your doctor may occasionally change your dose to make sure you get the best results.
Your chest pain may become worse when you first start taking Amlodipino Chemopharma or when your dose is increased. Call your doctor if your chest pain is severe or ongoing.
Amlodipino Chemopharma is only part of a complete program of treatment that may also include diet, exercise, weight control, and other medications. Follow your diet, medication, and exercise routines very closely.
If you are being treated for high blood pressure, keep using this medication even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.
Store at room temperature away from moisture, heat, and light.
Amlodipino Chemopharma pharmacology
Mechanism of Action
Amlodipino Chemopharma is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that Amlodipino Chemopharma binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipino Chemopharma inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects can be detected in vitro but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by Amlodipino Chemopharma. Within the physiologic pH range, Amlodipino Chemopharma is an ionized compound (pKa=8.6), and its kinetic interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect.
Amlodipino Chemopharma is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.
The precise mechanisms by which Amlodipino Chemopharma relieves angina have not been fully delineated, but are thought to include the following:
Exertional Angina: In patients with exertional angina, Amlodipino Chemopharma reduces the total peripheral resistance (afterload) against which the heart works and reduces the rate pressure product, and thus myocardial oxygen demand, at any given level of exercise.
Vasospastic Angina: Amlodipino Chemopharma has been demonstrated to block constriction and restore blood flow in coronary arteries and arterioles in response to calcium, potassium epinephrine, serotonin, and thromboxane A2 analog in experimental animal models and in human coronary vessels in vitro. This inhibition of coronary spasm is responsible for the effectiveness of Amlodipino Chemopharma in vasospastic (Prinzmetal's or variant) angina.
Pharmacodynamics
Hemodynamics: Following administration of therapeutic doses to patients with hypertension, Amlodipino Chemopharma produces vasodilation resulting in a reduction of supine and standing blood pressures. These decreases in blood pressure are not accompanied by a significant change in heart rate or plasma catecholamine levels with chronic dosing. Although the acute intravenous administration of Amlodipino Chemopharma decreases arterial blood pressure and increases heart rate in hemodynamic studies of patients with chronic stable angina, chronic oral administration of Amlodipino Chemopharma in clinical trials did not lead to clinically significant changes in heart rate or blood pressures in normotensive patients with angina.
With chronic once daily oral administration, antihypertensive effectiveness is maintained for at least 24 hours. Plasma concentrations correlate with effect in both young and elderly patients. The magnitude of reduction in blood pressure with Amlodipino Chemopharma is also correlated with the height of pretreatment elevation; thus, individuals with moderate hypertension (diastolic pressure 105–114 mmHg) had about a 50% greater response than patients with mild hypertension (diastolic pressure 90–104 mmHg). Normotensive subjects experienced no clinically significant change in blood pressures (+1/–2 mmHg).
In hypertensive patients with normal renal function, therapeutic doses of Amlodipino Chemopharma resulted in a decrease in renal vascular resistance and an increase in glomerular filtration rate and effective renal plasma flow without change in filtration fraction or proteinuria.
As with other calcium channel blockers, hemodynamic measurements of cardiac function at rest and during exercise (or pacing) in patients with normal ventricular function treated with Amlodipino Chemopharma have generally demonstrated a small increase in cardiac index without significant influence on dP/dt or on left ventricular end diastolic pressure or volume. In hemodynamic studies, Amlodipino Chemopharma has not been associated with a negative inotropic effect when administered in the therapeutic dose range to intact animals and man, even when co-administered with beta-blockers to man. Similar findings, however, have been observed in normal or well-compensated patients with heart failure with agents possessing significant negative inotropic effects.
Electrophysiologic Effects: Amlodipino Chemopharma does not change sinoatrial nodal function or atrioventricular conduction in intact animals or man. In patients with chronic stable angina, intravenous administration of 10 mg did not significantly alter A-H and H-V conduction and sinus node recovery time after pacing. Similar results were obtained in patients receiving Amlodipino Chemopharma and concomitant beta-blockers. In clinical studies in which Amlodipino Chemopharma was administered in combination with beta-blockers to patients with either hypertension or angina, no adverse effects on electrocardiographic parameters were observed. In clinical trials with angina patients alone, Amlodipino Chemopharma therapy did not alter electrocardiographic intervals or produce higher degrees of AV blocks.
Drug interactions
Sildenafil: When Amlodipino Chemopharma and sildenafil were used in combination, each agent independently exerted its own blood pressure lowering effect.
Pharmacokinetics
After oral administration of therapeutic doses of Amlodipino Chemopharma, absorption produces peak plasma concentrations between 6 and 12 hours. Absolute bioavailability has been estimated to be between 64 and 90%. The bioavailability of Amlodipino Chemopharma is not altered by the presence of food.
Amlodipino Chemopharma is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine. Ex vivo studies have shown that approximately 93% of the circulating drug is bound to plasma proteins in hypertensive patients. Elimination from the plasma is biphasic with a terminal elimination half-life of about 30–50 hours. Steady-state plasma levels of Amlodipino Chemopharma are reached after 7 to 8 days of consecutive daily dosing.
The pharmacokinetics of Amlodipino Chemopharma are not significantly influenced by renal impairment. Patients with renal failure may therefore receive the usual initial dose.
Elderly patients and patients with hepatic insufficiency have decreased clearance of Amlodipino Chemopharma with a resulting increase in AUC of approximately 40–60%, and a lower initial dose may be required. A similar increase in AUC was observed in patients with moderate to severe heart failure.
Drug interactions
In vitro data indicate that Amlodipino Chemopharma has no effect on the human plasma protein binding of digoxin, phenytoin, warfarin, and indomethacin.
Impact of other drugs on Amlodipino Chemopharma
Co-administered cimetidine, magnesium-and aluminum hydroxide antacids, sildenafil, and grapefruit juice have no impact on the exposure to Amlodipino Chemopharma.
CYP3A inhibitors: Co-administration of a 180 mg daily dose of diltiazem with 5 mg Amlodipino Chemopharma in elderly hypertensive patients resulted in a 60% increase in Amlodipino Chemopharma systemic exposure. Erythromycin co-administration in healthy volunteers did not significantly change Amlodipino Chemopharma systemic exposure. However, strong inhibitors of CYP3A (e.g., itraconazole, clarithromycin) may increase the plasma concentrations of Amlodipino Chemopharma to a greater extent.
Impact of Amlodipino Chemopharma on other drugs
Co-administered Amlodipino Chemopharma does not affect the exposure to atorvastatin, digoxin, ethanol and the warfarin prothrombin response time.
Simvastatin: Co-administration of multiple doses of 10 mg of Amlodipino Chemopharma with 80 mg simvastatin resulted in a 77% increase in exposure to simvastatin compared to simvastatin alone.
Cyclosporine: A prospective study in renal transplant patients (N=11) showed on an average of 40% increase in trough cyclosporine levels when concomitantly treated with Amlodipino Chemopharma.
Tacrolimus: A prospective study in healthy Chinese volunteers (N=9) with CYP3A5 expressers showed a 2.5- to 4-fold increase in tacrolimus exposure when concomitantly administered with Amlodipino Chemopharma compared to tacrolimus alone. This finding was not observed in CYP3A5 non-expressers (N= 6). However, a 3-fold increase in plasma exposure to tacrolimus in a renal transplant patient (CYP3A5 non-expresser) upon initiation of Amlodipino Chemopharma for the treatment of post-transplant hypertension resulting in reduction of tacrolimus dose has been reported. Irrespective of the CYP3A5 genotype status, the possibility of an interaction cannot be excluded with these drugs.
Pediatric Patients
Sixty-two hypertensive patients aged 6 to 17 years received doses of Amlodipino Chemopharma between 1.25 mg and 20 mg. Weight-adjusted clearance and volume of distribution were similar to values in adults.
References
- NCIt. "Amlodipine: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Amlodipine: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
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Information checked by Dr. Sachin Kumar, MD Pharmacology
