Amlodipine 5mg Tablets (Amlor) Uses, Dosage, Side Effects,&Warnings

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Amlor  generic name : Amlodipine

Amlodipine generic drug of the therapeutic class: Cardiology and angiology
active principles: Amlodipine

What is Amlor 5mg?

AMLOR is used to treat high blood pressure (hypertension), or a certain type of chest pain called angina, a rare form of which is Prinzmetal’s angina.

In patients with high blood pressure values, your medication works by relaxing the blood vessels, so that the blood passes through them more easily. In patients with angina, AMLOR works by improving the blood supply to the heart muscle, which thus receives more oxygen, which prevents the development of chest pain. Your medication does not provide immediate relief for angina chest pain.

Amlor indication and Uses

• Hypertension.
• Chronic stable angina.
• Vasospastic angina (Prinzmetal syndrome).

amlodipine dosage

Dosage:

adults:

• For hypertension and langor, the usual starting dose is 5 mg AMLOR once daily, which can be increased to a maximum dose of 10 mg depending on the patient’s individual response.
• In hypertensive patients, AMLOR has been used in combination with a thiazide diuretic, an alphablocker, a beta-blocker or a langiotensin converting enzyme inhibitor. In langor, AMLOR can be used alone or in combination with other anti-anginal drugs in patients with nitrate-refractory angina and / or adequate doses of beta-blockers.
• No dose adjustment of AMLOR is necessary when coadministered with thiazide diuretics, beta-blockers and langiotensin converting enzyme inhibitors.

Special populations

Elderly patients

• AMLOR used at similar doses shows good equivalent tolerance in elderly patients and younger patients. Normal dosing regimens are recommended in elderly patients, but an increase in dosage should be made with caution .

Patients with hepatic insufficiency

• Dose recommendations have not been established in patients with mild to moderate hepatic impairment therefore the dose should be selected with caution and started at the lowest effective dose.
•  The pharmacokinetic properties of lamlodipine have not been studied in patients with severe hepatic impairment. Lamlodipine should be started at the lowest dose and slowly increased in patients with severe hepatic insufficiency.

Patients with renal insufficiency

• Changes in damlodipine plasma concentrations are not correlated with the degree of renal insufficiency, so a usual dose is recommended. Lamlodipine is not dialysable.

Pediatric population

Hypertensive children and adolescents aged 6 to 17

• The recommended oral antihypertensive dosage in children aged 6 to 17 years is 2.5 mg once daily as an initial dose, which can be increased to 5 mg once daily if the desired blood pressure is not reached after four weeks. . Doses greater than 5 mg once daily have not been studied in pediatric patients.
• A dosage of 2.5 mg damlodipine is not possible with this drug.

Children under 6 years

There is no data available.

Administration mode

Capsule for oral administration.

amlodipine mechanism of action

Pharmacotherapeutic group: Selective calcium antagonist with predominantly vascular effect

ATC Code: C08 CA01.

Amlodipine is an inhibitor of calcium influx from the dihydropyridine group (slow channel inhibitor or calcium ion antagonist) and transmembrane influx of calcium ions into vascular smooth muscle and vascular smooth muscle.

The mechanism of the antihypertensive effect of amlodipine is related to a direct relaxant effect on vascular smooth muscle. The precise mechanism by which amlodipine relieves angina has not been fully determined, but amlodipine reduces the total ischemic load by the following two actions:

1. Amlodipine dilates the peripheral arterioles and therefore reduces the total peripheral resistance (afterload) against which the heart acts. Since the heart rate remains stable, this reduction in heart work decreases myocardial energy consumption and oxygen requirements.
2. The mechanism of action of amlodipine probably also involves the dilation of the main coronary arteries and coronary arteries, in the normal and ischemic regions. This dilation increases oxygen delivery to the myocardium in patients with coronary artery spasm (Prinzmetal’s angina).

In hypertensive patients, once-daily dosing provides clinically significant reductions in both supine and upright blood pressure over a 24-hour interval. Due to the slow onset of action, acute hypotension is not associated with amlopidine administration.

In patients with angina, once-daily administration of amlopidine increases total exercise time, onset of angina, and 1 mm ST segment depression and it decreases both the frequency of angina attacks and the consumption of glyceryl trinitrate tablets.

Amlopidine has not been associated with adverse metabolic effects or changes in plasma lipids, and is suitable for patients with asthma, diabetes and gout.

Use in patients with coronary artery disease

The efficacy of amlopidine for the prevention of clinical events in patients with coronary artery disease was evaluated in an independent, multicenter, randomized, double-blind, controlled versusplacebo in 1,997 patients: the CAMELOT study (Comparison of Amlodipine vs Enalapril to Limit Occurrences of Thrombosis, comparison of amlopidine and enalapril in the limitation of episodes of thrombosis).

Of these patients, 663 were treated with amlopidine 5-10 mg, 673 were treated with enalapril 10-20 mg, and 655 with placebo, in addition to standard statin therapy, betablockers. , diuretics and aspirin for two years. The main efficacy results are shown in Table 1. The results indicate that amlopidine treatment was associated with fewer angina hospitalizations and revascularization procedures in patients with coronary artery disease.

Table  1 . Impact of significant clinical endpoints of the CAMELOT study
	Cardiovascular event rate, number (%)			Amlopidine versus placebo
Evaluation criteria	amlodipine	Placebo	Enalapril	Relative risk (95% CI)	P value
Main criterion
Cardiovascular adverse events	110 (16.6)	151 (23.1)	136 (20.2)	0.69 (0.54-0.88)	0,003
Individual components
Coronary revascularization	78 (11.8)	103 (15.7)	95 (14,1)	0.73 (0.54-0.98)	0.03
Hospitalization for angor	51 (7.7)	84 (12.8)	86 (12.8)	0.58 (0.41-0.82)	0,002
Non-fatal IDM	14 (2.1)	19 (2.9)	11 (1,6)	0.73 (0.37-1.46)	0.37
Stroke or AIT	6 (0.9)	12 (1,8)	8 (1,2)	0.50 (0.19-1.32)	0.15
Cardiovascular mortality	5 (0.8)	2 (0.3)	5 (0.7)	2.46 (0.48-12.7)	0.27
Hospitalization for ICC	3 (0.5)	5 (0.8)	4 (0.6)	0.59 (0.14-2.47)	0.46
Resuscitation after cardiac arrest	0	4 (0.6)	1 (0,1)	N / A	0.04
Appearance of peripheral vascular disease	5 (0.8)	2 (0.3)	8 (1,2)	2.6 (0.50-13.4)	0.24
Abbreviations: CHF, congestive heart failure; IC, confidence interval; MI, myocardial infarction; TIA, transient ischemic attacks; Stroke, stroke.

Use in patients with heart failure  :

• Hemodynamic studies and controlled studies based on exercise tests conducted in patients with heart failure NYHA II-IV classes showed that AMLOR did not cause any clinical deterioration in exercise tolerance, of left ventricular ejection fraction and clinical symptomatology.
• A controlled study versus placebo (PRAISE) designed to evaluate patients with heart failure NYHA class III-IV receiving digoxin, diuretics and ACE inhibitors has shown that AMLOR did not lead to increased risk of death or death and morbidity combined with heart failure.
• In controlled long-term follow-up study versus placebo (PRAISE-2) AMLOR in patients with heart failure NYHA class III and IV without clinical symptoms or objective findings suggestive or underlying ischemic disease, treated stable doses of ACE inhibitors, digitalis and diuretics, AMLOR had no effect on total cardiovascular mortality. In this same population, AMLOR has been associated with an increase in pulmonary edema notifications.

Study on the Preventive Treatment of Heart Failure (Treatment to Prevent Attack Heart Attack, ALLHAT)

The ALLHAT (Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trials) study, a randomized, double-blind study on morbidity and mortality was conducted to compare treatments. recent studies: amlodipine 2.5 to 10 mg / day (calcium channel blocker) or lisinopril 10 to 40 mg / day (ACE inhibitor) as a first-line treatment compared to a thiazide diuretic, chlortalidone at a dose of 12, 5 to 25 mg / day in mild to moderate hypertension.

A total of 33,357 hypertensive patients aged 55 years or older were randomized and followed for an average of 4.9 years. Patients had at least one risk factor for additional coronary heart disease, including: history of myocardial infarction or stroke (more than six months prior to inclusion) or documentation of other atherosclerotic cardiovascular disease (in total 51.5%), type 2 diabetes (36.1%), HDL cholesterol <35 mg / dl (11.6%), left ventricular hypertrophy diagnosed by electrocardiography or echocardiography (20.9%), current smoking (21%). , 9%).

The composite primary endpoint was fatal coronary artery disease or nonfatal myocardial infarction. There was no significant difference in the primary end point between amlopidine treatment and chlortalidone treatment: RR 0.98; 95% CI (0.90 to 1.07); p = 0.65. Among the secondary endpoints, the incidence of heart failure (component of a composite cardiovascular endpoint) was significantly higher in the amlodipine group compared to the chlortalidone group (10.2% versus7.7%; RR: 1.38; 95% CI [1.25 to 1.52]; p <0.001). However, there was no significant difference in all-cause mortality between amlopidine-based treatment and chlortalidone treatment: RR 0.96; 95% CI [0.89 to 1.02]; p = 0.20.

Use in children (at least six years old)

• In a study of 268 children aged 6 to 17 years with predominant secondary hypertension, a 2.5 mg dose and a 5.0 mg dose of amlodipine were compared to placebo. It was found that both doses reduced systolic blood pressure significantly more significantly than placebo. The difference between the two doses was not statistically significant.
• The long-term effects of amlodipine on growth, puberty and general development have not been studied. The long-term efficacy of amlopidine in a child’s treatment aimed at reducing morbidity and cardiovascular mortality in adulthood has not been established.

How it works Amlor

What are side effects of amlodipine?

Summary of the security profile

• The most common side effects reported during treatment are drowsiness, dizziness, headache, palpitations, flushing, abdominal pain, nausea, swollen ants, edema, and fatigue.

List of undesirable effects

The following side effects have been observed and reported during treatment with amlopidine at the following frequencies: very common (≥ 1/10); frequent (≥ 1/100 to <1/10); uncommon (≥ 1/1000 to ≤ 1/100); rare (≥ 1/10 000 to ≤ 1/1 000); very rare (≤1 / 10,000).

In each frequency group, the adverse effects are presented in order of decreasing severity.

Class of organ systems	Frequency	Side effects
Blood and lymphatic system disorders	Very rare	Leukocytopenia, thrombocytopenia,
Immune system disorders	Very rare	Allergic reaction
Metabolism and nutrition disorders	Very rare	hyperglycemia
Psychiatric disorders	Rare	Insomnia, change of mood (including anxiety), depression
	Rare	Confusion
Nervous system disorders	Frequent	Drowsiness, dizziness, headache (especially at the beginning of treatment)
	Rare	Tremor, dysgeusia, syncope, hypoaesthesia, paresthesia
	Very rare	Hypertonia, peripheral neuropathy
Eye disorders	Rare	Visual disorder (including, diplopia)
Affections of the ear and labyrinth	Rare	tinnitus
Heart conditions	Frequent	palpitations
	Very rare	Myocardial infarction, arrhythmia (including bradycardia, ventricular tachycardia, and atrial fibrillation)
Vascular disorders	Frequent	Flushing
	Rare	hypotension
	Very rare	vasculitis
Respiratory, thoracic and mediastinal disorders	Rare	Dyspnea, rhinitis
	Very rare	Cough
Gastrointestinal disorders	Frequent	Abdominal pain, nausea
	Rare	Vomiting, dyspepsia, transit disorders (including diarrhea and constipation), dry mouth
	Very rare	Pancreatitis, gastritis, gingival hyperplasia
Hepatobiliary disorders	Very rare	Hepatitis, jaundice, elevated liver enzymes *
Skin and subcutaneous tissue disorders	Rare	Alopecia, purpura, change of skin color, hyperhidrosis, pruritus, rash, exanthema
	Very rare	Angioedema, erythema multiforme, urticaria, exfoliating dermatitis, Stevens-Johnson syndrome, angioedema, photosensitivity
Musculoskeletal, Connective Tissue and Bone Disorders	Frequent	Edema of the ankles
	Rare	Arthralgia, myalgia, muscle cramp, back pain
Renal and urinary disorders	Rare	Micturition disorder, nocturia, increased urinary frequency
Disorders of reproductive organs and breast	Rare	Impotence, gynecomastia
General disorders and administration site conditions	Frequent	Edema, tiredness
	Rare	Chest pain, asthenia, pain, discomfort
investigations	Rare	Increased weight, decreased weight

* Generally suggestive of cholestasis

Exceptional cases of extrapyramidal syndrome have been reported.

amlodipine interactions

Effects of other drugs on amlopidine

CYP3A4 inhibitors

• Concomitant use of amlodipine with strong or moderate CYP3A4 inhibitors (protease inhibitors, azole antifungals, macrolides such as erythromycin or clarithromycin, verapamil or diltiazem) may result in a significant increase in the concentration of amlodipine. plasma level of amlodipine resulting in an increased risk of hypotension.
• The clinical translation of these pharmacokinetic variations may be more pronounced in the elderly. Therefore, clinical monitoring and dose adjustment may be necessary.

CYP3A4 inducers

• No data are available on the effect of CYP3A4 inducers on amlodipine. Concomitant use of inducers of CYP3A4 (eg, rifampicin, St. John’s Wort [Hypericum perforatum]) may result in decreased plasma amlopidine concentration. Amlopidine should be used with caution with inducers of CYP3A4 isoenzyme.
• Administration of amlopidine with grapefruit or grapefruit juice is not recommended as bioavailability may be increased in some patients, which may result in increased hypotensive effects.

Dantrolene (infusion)

• In animals, ventricular fibrillation and lethal cardiovascular collapse have been observed in association with hyperkalemia following administration of verapamil and dantrolene IV. Given the risk of hyperkalemia, it is recommended to avoid the concomitant administration of calcium channel blockers such as amlodipine in patients who may have malignant hyperthermia and in the management of malignant hyperthermia.

Effects of amlodipine on other drugs

• The hypotensive effects of amlodipine add to those of other drugs with antihypertensive properties.

tacrolimus

• There is a risk of increased plasma concentrations of tacrolimus when co-administered with amlodipine, but the pharmacokinetic mechanism of this interaction is not fully understood. In order to avoid tacrolimus toxicity, administration of amlodipine to a tacrolimus-treated patient requires monitoring of tacrolimus plasma concentrations and dosage adjustment of tacrolimus where appropriate.

cyclosporin

• No interaction studies have been conducted with ciclosporin and amlodipine in healthy volunteers or other populations, with the exception of renal transplant patients; a variable increase in the minimum concentration of ciclosporin was observed (from 0% to 40% on average). The ciclosporin level should be monitored in renal transplant patients treated with amlodipine and a reduction in ciclosporin dosage should be considered if necessary.

simvastatin

• Co-administration of repeated doses of 10 mg amlodipine with 80 mg simvastatin resulted in a 77% increase in simvastatin exposure compared with simvastatin alone. The daily dose of simvastatin should be limited to 20 mg in patients treated with amlodipine.
• In clinical interaction studies, amlodipine did not affect the pharmacokinetics of atorvastatin, digoxin or warfarin.

Amlor Warnings and Precautions

The safety and efficacy of lamlodipine during a hypertensive crisis have not been established.

Patients with heart failure

• Patients with heart failure should be treated with caution. In controlled long-term study versus placebo conducted in patients with severe heart dinsuffisance (class NYHA III and IV), the incidence reported pulmonary edema was higher in the group treated lamlodipine compared to placebo (see section 5.1). The calcium channel blockers including lamlodipine should be used with caution in patients with congestive heart failure because they may increase the risk of cardiovascular events and mortality.

Patients with hepatic insufficiency

• The half-life of lamlodipine is increased and its AUC (Greater Curve) is greater in patients with hepatic insufficiency; dosage recommendations have not been established. Therefore, lamlodipine should be initiated at the lowest effective dose and with caution, both during initiation of treatment and when the dose is increased. A slow dose increase and careful monitoring may be necessary in patients with severe hepatic impairment.

Elderly patients

• In elderly patients, an increase in dosage should be made with caution.

Patients with renal insufficiency

• Lamlodipine can be used in these patients at normal doses. Changes in plasma concentrations of damlodipine do not correlate with the degree of renal insufficiency. Lamlodipine is not dialysable.

Drive and use machines

Lamlodipine may have a minor or moderate influence on the ability to drive vehicles and use machines. If patients treated with lamlodipine experience dizziness, headache, fatigue or nausea, their ability to respond may be impaired. Precautions are recommended especially at the beginning of treatment.

Amlor and PREGNANCY / BREAST FEEDING / FERTILITY

Pregnancy:

1. In women, the safety of amlodipine during pregnancy has not been established.
2. In animal studies, reproductive toxicity has been observed at high doses (see section 5.3 ).
3. Use during pregnancy is recommended only if no safer alternatives are available and when the disease itself poses greater risks to the mother and fetus.

feeding:

• It has not been established whether amlopidine is excreted in breast milk. The decision to continue or discontinue breastfeeding or to continue or discontinue amlodipine therapy should be considered in consideration of the benefit of breastfeeding for the child and the benefit of amlopidine treatment for the mother.

Fertility:

• Reversible biochemical changes in the spermatozoa head have been reported in some patients treated with calcium channel blockers. There is insufficient clinical data regarding the potential effect of amlopidine on fertility. In a rat study, adverse effects were detected on male fertility (see section 5.3 ).

What should I do if I miss a dose?

If you forget to take AMLOR 10 mg, capsule:

• Do not worry. If you forget to take one capsule, skip the dose completely. Take the next dose according to the normal rhythm. Do not take a double dose to make up for the dose you forgot to take.

What happens if I overdose from Amlor ?

If you take more AMLOR 10 mg capsule than you should:

• Taking too many capsules can lead to a sometimes dangerous drop in your blood pressure. You may feel dizzy, dizzy, faint or weak. If the blood pressure falls too much, a shock may occur. Your skin may become cold and clammy and you may lose consciousness. Consult a doctor if you have taken too many AMLOR capsules.

What is  Forms and Composition Amlor?

COMPOSITION

What does AMLOR 10 mg capsule contain?

Active substance

• Amlodipine besylate: 13.889 mg
• Amlodipine equivalent quantity: 10,000 mg

For one capsule

Other components

• The capsule shell contains: gelatin, black iron oxide, yellow iron oxide, titanium dioxide.
• The printing ink on the capsule shell contains: shellac, black iron oxide.

NOT’s

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general information:

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Additional information:

• General explanation about dealing with the medicine: how to take the medicine, the doses and times of it, the start and duration of its effectiveness, the recommended diet during the period of taking the medicine, the method of storage and storage, recommendations in cases for forgetting the dose and instructions to stop taking the drug and take additional doses.

Special warnings:

• For pregnant and breastfeeding women, the elderly, boys and drivers, and use before surgery.

Side effects:

• It treats possible side effects and drug interactions that require attention and its effect on continuous use.
• The information contained in this medicine is based on medical literature, but it is not a substitute for consulting a doctor.

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