Аген 10
Аген 10 Uses, Dosage, Side Effects, Food Interaction and all others data.
Аген 10 is a Dihydropyridine Calcium antagonist that inhibits the transmembrane influx of Calcium ions into cardiac and vascular smooth muscle. It has greater affinity towards vascular smooth muscle than on cardiac muscle. Аген 10 is peripheral vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and thereby reduces blood pressure. Аген 10 reduces tone, decreases coronary vasoreactivity and lowers cardiac oxygen demand by reducing after load.
General pharmacodynamic effects
Аген 10 has a strong affinity for cell membranes, modulating calcium influx by inhibiting selected membrane calcium channels. This drug's unique binding properties allow for its long-acting action and less frequent dosing regimen , .
Hemodynamic effects
Trade Name | Аген 10 |
Availability | Prescription only |
Generic | Amlodipine |
Amlodipine Other Names | Amlodipine, Amlodipino, Amlodipinum |
Related Drugs | aspirin, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, propranolol, Xarelto, spironolactone |
Type | |
Formula | C20H25ClN2O5 |
Weight | Average: 408.876 Monoisotopic: 408.145199627 |
Protein binding | About 98% , . |
Groups | Approved |
Therapeutic Class | Calcium-channel blockers |
Manufacturer | |
Available Country | Ukraine |
Last Updated: | September 19, 2023 at 7:00 am |
![Аген 10 Аген 10](https://www.medicinesfaq.com/media/png/ru-agen-10.png)
Uses
Patients with mild to moderate hypertension (alone or in combination with other antihypertensives).
The treatment of chronic stable and vasospastic angina.
Raynaud\'s disease.
Аген 10 is also used to associated treatment for these conditions: Anginal Pain, Cardiovascular Events, Chronic Stable Angina Pectoris, Coronary Artery Disease (CAD), High Blood Pressure (Hypertension), Homozygous Familial Hypercholesterolemia, Hypertension,Essential, Mixed Dyslipidemias, Primary Hypercholesterolemia, Vasospastic Angina
How Аген 10 works
Mechanism of action on blood pressure
Аген 10 is considered a peripheral arterial vasodilator that exerts its action directly on vascular smooth muscle to lead to a reduction in peripheral vascular resistance, causing a decrease in blood pressure. Аген 10 is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the influx of calcium ions into both vascular smooth muscle and cardiac muscle. Experimental studies imply that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites, located on cell membranes. The contraction of cardiac muscle and vascular smooth muscle are dependent on the movement of extracellular calcium ions into these cells by specific ion channels. Аген 10 blocks calcium ion influx across cell membranes with selectivity. A stronger effect of amlodipine is exerted on vascular smooth muscle cells than on cardiac muscle cells . Direct actions of amlodipine on vascular smooth muscle result in reduced blood pressure .
Mechanism of action in angina
The exact mechanism by which amlodipine relieves the symptoms of angina have not been fully elucidated to this date, however, the mechanism of action is likely twofold:
Аген 10 has a dilating effect on peripheral arterioles, reducing the total peripheral resistance (afterload) against which the cardiac muscle functions. Since the heart rate remains stable during amlodipine administration, the reduced work of the heart reduces both myocardial energy use and oxygen requirements .
Dilatation of the main coronary arteries and coronary arterioles, both in healthy and ischemic areas, is another possible mechanism of amlodipine reduction of blood pressure. The dilatation causes an increase in myocardial oxygen delivery in patients experiencing coronary artery spasm (Prinzmetal's or variant angina) and reduces coronary vasoconstriction caused by smoking .
Dosage
Аген 10 dosage
For treatment of both hypertension and angina pectoris, the usual initial dose is 5 mg once daily. If the desired therapeutic effect cannot be achieved within 2-4 weeks, the dose may be increased to a maximum dose of 10 mg once daily. Аген 10 10 mg once daily provides symptomatic improvement in patients with Raynaud's disease.
Use in children: Use of Аген 10 in children (under 12 years of age) is not recommended.
Side Effects
Аген 10 is generally well tolerated. The most commonly observed side effects are headache, peripheral oedema, palpitations, flushing, dizziness, nausea, abdominal pain.
Toxicity
Acute oral toxicity (LD50): 37 mg/kg (mouse) .
Overdose
An overdose of amlodipine could result in a high degree of peripheral vasodilatation with a possibility of reflex tachycardia. Significant and prolonged hypotension leading to shock and fatal outcomes have been reported .
Carcinogenesis, mutagenesis, impairment of fertility
Rats and mice treated with amlodipine maleate in the diet on a long-term basis for up to 2 years demonstrated no evidence of a carcinogenic effect of the drug. For the mouse, the highest dose was comparable to the maximum recommended human dose of 10 mg amlodipine per day. For the rat, the highest dose was measured to be about twice the maximum recommended human dose .
Mutagenicity studies using amlodipine maleate showed no drug-related gene or chromosomal effects .
There was no impact on the fertility of rats given oral amlodipine maleate (males for 64 days and females for 14 days before mating) at doses up to 10 mg amlodipine/kg/day (8 times the maximum recommended human dose) .
Use in pregnancy
The safety of amlodipine in human pregnancy or lactation has not been proven. Аген 10 is therefore considered a pregnancy category C drug . Use amlodipine only if the potential benefit justifies the potential risk .
Use in nursing
Discontinue when administering amlodipine .
Precaution
Hypotension: Since the vasodilUse in renal failure
Although Аген 10 is excreted primarily via kidney, mild renal impairment does not appear to have an effect on the plasma concentrations. Severe renal impairment may however require a dosage reduction. Аген 10 is not dialyzable.
Use in patients with impaired hepatic function
Аген 10 half-life is prolonged in patient with impaired hepatic function. Аген 10 should therefore be administered at lower (5mg) initial dose in these patients.
Use in heart failure
An increased number of pulmonary oedema has been reported.atation induced by Аген 10 is gradual in onset, acute hypotension has rarely been reported after oral administration of Аген 10. Nonetheless, caution should be exercised when administering the drug with any other peripheral vasodilator particularly in patients with severe aortic stenosis.
Cardiac failure: Patients with heart failure should be treated with caution. Calcium channel blockers, including Аген 10, should be usedwith caution in patients with congestive heart failure, as they may increase the risk of future cardiovascular events and mortality.
Beta blocker withdrawal: Аген 10 gives no protection against the danger of abrupt beta blocker withdrawal; any such withdrawal should be gradualreduction of the dose of beta blocker.
Hepatic failure: The half-life of amlodipine is prolonged and AUC values are higher in patients with impaired liver function. Аген 10 should therefore be initiated at the lower end of the dosing range and caution should be used, both on initial treatment and when increasing the dose. Slow dose titration and careful monitoring may be required in patients with severe hepatic impairment.
Interaction
Use of Аген 10 together with thiazide diuretics or angiotensin-converting-enzyme inhibitors in the treatment of hypertension is additive. There are no hazardous interaction of Аген 10 with Digoxin, Cimetidine, Warfarin and food.
Food Interaction
- Avoid grapefruit products.
- Avoid natural licorice.
- Take with or without food. The absorption is unaffected by food.
[Minor] The consumption of grapefruit juice may slightly increase plasma concentrations of amlodipine.
The mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits.
Data have been conflicting and the clinical significance is unknown.
Monitoring for calcium channel blocker adverse effects (e.g., headache, hypotension, syncope, tachycardia, edema) is recommended.
Аген 10 multivitamins interaction
[Moderate] Calcium-containing products may decrease the effectiveness of calcium channel blockers by saturating calcium channels with calcium.
Calcium chloride has been used to manage acute severe verapamil toxicity.
Management consists of monitoring the effectiveness of calcium channel blocker therapy during coadministration with calcium products.
Аген 10 Drug Interaction
Moderate: aspirin, aspirin, aspirin, aspirin, atorvastatin, atorvastatin, metoprolol, metoprolol, metoprolol, metoprololUnknown: rosuvastatin, rosuvastatin, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Аген 10 Disease Interaction
Major: cardiogenic shock/hypotension, coronary artery disease, liver diseaseModerate: CHF/AMI
Volume of Distribution
21 L/kg , .
Elimination Route
Аген 10 absorbed slowly and almost completely from the gastrointestinal tract. Peak plasma concentrations are achieved 6-12 hours after oral administration. The estimated bioavailability of amlodipine is 64-90%. Steady-state plasma amlodipine levels are achieved after 7-8 days of consecutive daily dosing. Absorption is not affected by food .
Half Life
The terminal elimination half-life of about 30–50 hours .
Plasma elimination half-life is 56 hours in patients with impaired hepatic function, titrate slowly when administering this drug to patients with severe hepatic impairment .
Clearance
Total body clearance (CL) has been calculated as 7 ± 1.3 ml/min/kg (0.42 ± 0.078 L/ h/kg) in healthy volunteers , .
Elderly patients show a reduced clearance of amlodipine with an AUC (area under the curve) increase of about 40–60%, and a lower initial dose may be required .
Elimination Route
Elimination from the plasma occurs in a biphasic with a terminal elimination half-life of about 30–50 hours. Steady-state plasma levels of amlodipine are reached after 7-8 days of consecutive daily dosing . Аген 10 is 10% excreted as unchanged drug in the urine. Аген 10 can be initiated at normal doses in patients diagnosed with renal failure , .
Pregnancy & Breastfeeding use
Pregnancy: Safety in pregnancy has not been established.
Lactation: It is not known whether Аген 10 is excreted in breast milk. It is advised to stop breastfeeding during treatment with Аген 10.
Contraindication
Аген 10 is contraindicated in patients with-
- Hypersensitivity to amlodipine, dihydropyridine derivatives or any of the excipients
- Shock (including cardiogenic shock)
- Obstruction of the outflow-tract of the left ventricle (e.g. high grade aortic stenosis)
- Unstable angina
- Hemodynamically unstable heart failure after acute myocardial infarction (during the first 28 days)
- Severe hypotension
Special Warning
Children with hypertension from 6 years to 17 years of age: 2.5 mg once daily as a starting dose, up-titrated to 5 mg once daily if blood pressure goal is not achieved after 4 weeks. Doses in excess of 5 mg daily have not been studied in pediatric patients.
Children under 6 years old: The effect of amlodipine on blood pressure in patients less than 6 years of age is not known.
Elderly: Аген 10 used at similar doses in elderly or younger patients is equally well tolerated. Normal dosage regimens are recommended in the elderly, but increase of the dosage should take place with care.
Renal impairment: Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment, therefore the normal dosage is recommended. Аген 10 is not dialysable.
Hepatic impairment: Dosage recommendations have not been established in patients with mild to moderate hepatic impairment; therefore dose selection should be cautions and should start at the lower end of the dosing range. The pharmacokinetics of Аген 10 have not been studied in severe hepatic impairment. Аген 10 should be initiated at the lowest dose (2.5 mg once daily) and titrated slowly in patients with severe hepatic impairment.
Acute Overdose
There is no well documented experience with Аген 10 overdosage. In case of clinically significant hypotension due to Аген 10 over dosage, calls for active cardiovascular support including monitoring of cardiac and respiratory function, elevation of extremities and attention to circulating fluid volume and urine output. Since Аген 10 is highly protein-bound, dialysis is unlikely to be of benefit.
Storage Condition
Keep out of the reach of children. Store below 30° C. Keep in the original package in a cool & dry place in order to protect from light and moisture.
Innovators Monograph
You find simplified version here Аген 10
Аген 10 contains Amlodipine see full prescribing information from innovator Аген 10 Monograph, Аген 10 MSDS, Аген 10 FDA label
FAQ
What is Аген 10 used for?
Аген 10 is a medicine used to treat high blood pressure (hypertension).Аген 10 is also used to prevent chest pain caused by heart disease.
How safe is Аген 10?
Аген 10 is generally a safe and effective drug, but it may cause side effects in some people.
How does Аген 10 work?
Аген 10 works in high blood pressure by relaxing and widening blood vessels.
What are the common side effects of Аген 10?
The most common side effects include headache, flushing, feeling tired and swollen ankles.
Is Аген 10 safe during pregnancy?
early pregnancy does not appear to be associated with an increased rate of fetal malformations compared with other antihypertensive medications or maternal hypertension without treatment.
Is Аген 10 safe during breastfeeding?
Аген 10 use of Аген 10 during breastfeeding has not caused any adverse effects in breastfed infants. If Аген 10 is required by the mother, it is not a reason to discontinue breastfeeding.
Can I drink alcohol with Аген 10?
Yes, you can drink alcohol with Аген 10.But drinking alcohol can increase the blood pressure-lowering effect of Аген 10, which can make you feel sleepy, dizzy or bring on a headache. If this happens to you, it's best to stop drinking alcohol while you're taking Аген 10.
Can I drive after taking Аген 10 ?
If the tablets make you feel sick, dizzy or tired, or give you a headache, do not drive or use machines and contact your doctor immediately.
When is the best time to take Аген 10?
It does not matter what time of day you take Аген 10 morning or evening, but it is best to take it at the same time every day,
How long does Аген 10 take to work?
Аген 10 starts to work on the day you start taking it, but it may take a couple of weeks for full effect. If you're taking Аген 10 for high blood pressure, you may not have any symptoms.
How long does Аген 10 stay in my system?
Аген 10 will stay in your system for about 10 days after your last dose.
Can I take Аген 10 for a long time?
Аген 10 is generally safe to take for a long time. In fact, it works best when you take it for a long time.
Can Аген 10 cause kidney damage?
Аген 10 should not cause kidney damage and in fact are used to treat high blood pressure and slow the progression of chronic kidney disease.
When should I stop taking Аген 10?
If you have been using Аген 10 regularly for several weeks, do not suddenly stop using it.
Is Аген 10 bad for my liver?
Liver injury due to Аген 10 have not been reported.
Does Аген 10 affect heart rate?
Аген 10 has little or no effect on your heart rate.
Can Аген 10 cause depression?
Mood changes such as depression or anxiety may occurs.
Can Аген 10 cause a cough?
No, you probably won't have a cough when taking Аген 10.
What happens if I overdose of Аген 10?
If you take too much Аген 10 by accident, contact your doctor or go to your nearest hospital straight away. An overdose of Аген 10 can cause dizziness and sleepiness.
What happens if I miss a dose of Аген 10?
If you forget to take a dose of Аген 10, take it as soon as you remember that day and then carry on as normal. If you forget to take the dose for the whole day, skip the missed dose and carry on as normal the next day. Do not take a double dose to make up for a forgotten one.