محاضرة 7

1-سلسلة ادوية

خلصنا البيتا بلوكز وهنبدأ انهاردة الكالسيوم تشانيل بلوكرز

Calcium channel blockers

What are calcium channel blockers (CCBs) and how do they work?

In order to pump blood, the heart needs oxygen.

The harder the heart works, the more oxygen it requires.

Anginaالذبحة الصدرية (heart pain) occurs when the supply of oxygen to the heart is inadequateغير كاف for the amount of work the heart must do.

CCBs also are used for treating high blood pressure because of their blood pressure-lowering effects.

CCBs also slow the rate at which the heart beats and are therefore used for treating certain types of abnormally rapid heart rhythms.ايقاع القلب السريع والغير طبيعى

What calcium channel blockers are available?

طيب هيا المواد الفعالة بالنسبة للكلاس دى والمتوفرة فى مصر

For what conditions are calcium channel blockers used?

الكلاس دى بنستخدمها فى الاتى

CCBs are used for treating

high blood pressureالضغط العالى

anginaالذبحة الصدرية

abnormal heart rhythms (for example, atrial fibrillation, paroxysmal supraventricular tachycardia).

They also may be used after a heart attack نوبة قلبية , particularly among patients who cannot tolerate تحمل beta-blocking drugs, have atrial fibrillation, or require treatment for their angina.

يستخدم بعد النوبات القلبية خصوصا عند المرضى الذين لا يتحملون ادوية البيتا بلوكز اللى درسناها قبل كده

Unlike beta blockers, CCBs have not been shown to reduce mortality نسبة الموت or additional heart attacks after a heart attack.

على عكس البيتا بلوكز مش بيقلل النوبات القلبية التالية بعد اول نوبة

CCBs are as effective as ACE inhibitors in reducing blood pressure, but they may not be as effective as ACE inhibitors in preventing the kidney failureالفشل الكلوى caused by high blood pressure الضغط العالى or diabetesمرض السكر.

They also are used for treating:

pulmonary hypertension, ارتفاع ضغط الدم الرئوى

Raynaud's syndrome,

cardiomyopathy, and
subarachnoid hemorrhage.

CCBs are also used in the prevention of migraine headachesالصداع النصفى .

Are there any differences among calcium channel blockers?

CCBs differ in their duration of action,

the process by which they are eliminated from the body,

and, most importantly, in their ability to affect heart rate and contraction.

Some CCBs [for example, amlodipine have very little effect on heart rate and contraction so they are safer to use in individuals who have heart failure or bradycardia (a slow heart rate).

diltiazem have the greatest effects on the heart and reduce the strength and rate of contraction. Therefore, they are used in reducing heart rate when the heart is beating too fast.

هندرس اول مادة النيكارديبين

nicardipine

Indications

Prophylaxis of angina

الوقاية من الذبحة الصدرية

ولا يستخدم فى علاج الذبحة

mild to moderate hypertension

Dose

. Initially 20mg 3 times daily,increased ,after at least

Three days, to 30 mg 3 times daily (usual range 60–

120mg daily)

How should I take nicardipine?

Take each dose with a full glass of water. Do not crush, break, or chew the extended-release (SR) capsules. Swallow them whole. They are specially formulated to release the medication slowly in the body.

Do not stop taking nicardipine without first talking to your doctor, even if you begin to feel better.

If you stop taking the medication, your condition could become worse.

Grapefruit and grapefruit juice may interact with nicardipine. The interaction could have potentially dangerous effects

What happens if I miss a dose?

Take the missed dose as soon as you remember. However, if it is almost time for the next dose, skip the missed dose and take only the next regularly scheduled dose. Do not take a double dose of this medication.

What happens if I overdose?

Seek emergency medical attention.

Symptoms of a nicardipine overdose include

dizziness,

weakness,

الضعف

chest painالم فى الصدر,

shortness of breathقصر التنفس

, fainting,اغماء

an unusually fast or slow heartbeat, comaغيبوبة, slurred speechكلام متداخل وملخبط , and confusionتشويش .

What should I avoid while taking nicardipine?

Grapefruit and grapefruit juice may interact with nicardipine.

The interaction could have potentially dangerous effects.

Use caution when you stand or sit up from a lying position, especially if you wake up during the night.

You may become dizzy when changing positions. Use alcohol cautiously. Alcohol may further lower blood pressure and increase drowsiness or dizziness while taking nicardipine.

Nicardipine Disease Interactions

Aortic Stenosis•
تضيق الأورطي

Cardiogenic Shock صدمة قلبية /Hypotension

Coronary Artery Diseaseمرض الشريان التاجي

Liver Diseaseامراض الكبد
Renal Dysfunctionقصور الكلى
Chf/Ami فشل القلب الاحتقاني

Nicardipine Alcohol & Food Interactions

Nicardipine and multivitamins with minerals

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.

Moderate Food Interaction

The consumption of grapefruit juice may be associated with significantly increased plasma concentrations of some calcium channel blockers (CCBs) when they are administered orally.

Drug Interactions

Beta Blockers

ادوية ضغط

درسناهم فى المحاضرات السابقة

In controlled clinical studies, adrenergic beta-receptor blockers have been frequently administered concomitantly بشكل مصاحب with Nicardipine. The combination is well tolerated.

Cimetidine

دواء حموضة

Cimetidine increases Nicardipine plasma levels. Patients receiving the two drugs concomitantly should be carefully monitored.

Digoxin

دواء قلب

Some calcium blockers may increase the concentration of digitalis preparations in the blood. Nicardipine usually does not alter the plasma levels of digoxin, however, serum digoxin levels should be evaluated after concomitant therapy with Nicardipine is initiated.

Aluminum and Magnesium Hydroxides

دواء حموضة

Co-administration of an antacid containing 600 mg aluminum hydroxide and 300 mg magnesium hydroxide had no effect on Nicardipine absorption.

Fentanyl Anesthesia

دواء تخدير

Severe hypotension has been reported during fentanyl anesthesia with concomitant use of a beta-blocker and a calcium channel blocker. Even though such interactions were not seen during clinical studies with Nicardipine, an increased volume of circulating fluids might be required if such an interaction were to occur.

Cyclosporine

دواء مناعة

Concomitant administration of Nicardipine and cyclosporine results in elevated plasma cyclosporine levels. Plasma concentrations of cyclosporine should therefore be closely monitored, and its dosage reduced accordingly, in patients treated with Nicardipine.

When therapeutic concentrations of furosemide, propranolol, dipyridamole, warfarin, quinidine, or naproxen were added to human plasma (in vitro), the plasma protein binding of Nicardipine was not altered.

Do NOT use Nicardipine if:

you are allergic to any ingredient in Nicardipine
you are breast-feeding
you have advanced narrowing of your aorta (stenosis)

Contraindications

Warnings

Increased Angina

About 7% of patients in short term placebo-controlled angina trials have developed increased frequency, duration or severity of angina on starting Nicardipine or at the time of dosage increases, compared with 4% of patients on placebo. Comparisons with beta-blockers also show a greater frequency of increased angina, 4% vs 1%. The mechanism of this effect has not been established. (See ADVERSE REACTIONS.)

Use in Patients with Congestive Heart Failure

Although preliminary hemodynamic studies in patients with congestive heart failure have shown that Nicardipine reduced afterload without impairing myocardial contractility, it has a negative inotropic effect in vitro and in some patients. Caution should be exercised when using the drug in congestive heart failure patients, particularly in combination with a beta-blocker.

Beta-Blocker Withdrawal

Nicardipine is not a beta-blocker and therefore gives no protection against the dangers of abrupt beta-blocker withdrawal; any such withdrawal should be by gradual reduction of the dose of beta-blocker, preferably over 8 to 10 days.

Pregnancy

Pregnancy Category C

Nursing mothers

it is recommended that women who wish to breast-feed should not take this drug.

Pediatric use

Safety and efficacy in patients under the age of 18 have not been established.

لا يستخدم للحوامل و المرضعات والاطفال تحت 18 الا تحت ارشاد الطبيب

Before using Nicardipine:

if you are pregnant, planning to become pregnant, or are breast-feeding

if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement

if you have allergies to medicines, foods, or other substances

if you have angina (chest pain), congestive heart failure (CHF) or other heart problems, adrenal gland problems (eg, pheochromocytoma), liver or kidney problems, low blood pressure, or lung congestion associated with heart attack, or you have had a stroke
you have CHF and you are taking a beta-blocker, or you are having beta-blocker withdrawal

Important safety information:

Nicardipine may cause dizziness or fainting. These effects may be worse if you take it with alcohol or certain medicines. Use Nicardipine with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.

Patients who take medicine for high blood pressure often feel tired or run down for a few weeks after starting treatment. Be sure to take your medicine even if you may not feel "normal." Tell your doctor if you develop any new symptoms

Maximum lowering of blood pressure occurs approximately 1 to 2 hours after taking the medicine. Blood pressure should be taken 1 to 2 hours after the medicine has been taken.

Tell your doctor or dentist that you take Nicardipine before you receive any medical or dental care, emergency care, or surgery.

Additional monitoring of your dose or condition may be necessary if you are using intravenous (IV) calcium.

Lab tests, including blood pressure, electrocardiogram (ECG) readings, and monitoring of heart rate, may be performed while you use Nicardipine. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments

Nicardipine should be used with extreme caution in CHILDREN younger than 18 years old; safety and effectiveness in these children have not been confirmed

PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Nicardipine while you are pregnant. Nicardipine is found in breast milk. Do not breast-feed while taking Nicardipine.

If you stop taking Nicardipine suddenly, you may have WITHDRAWAL symptomsاعراض الانسحاب . These may include increased chest pain (angina) and more frequent chest pain.

Nicardipine side effects

If you experience any of the following serious side effects, stop taking nicardipine and contact your doctor immediately or seek emergency medical treatment:

· an allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives);

· unusually fast or slow heartbeats;

· fainting or severe dizziness;

· abnormal behavior or psychosis;

· chest pain or worsening angina;

· jaundice (yellowing of the skin or eyes); or

· swelling of the legs or ankles.

Other, less serious side effects may be more likely to occur. Continue to take nicardipine and talk to your doctor if you experience

· unusual headache, fatigue, or tiredness;

· dizziness;دوخة

· flushing;احمرار

· rash;هرش

· insomnia;ارق

· vivid or abnormal dreams;

· increased urination;

· dry mouth;فم جاف

· nauseaقئ or constipation;امساك or

· nervousness or tremor.رعاش

This is not a complete list of side effects and others may occur

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لينك 1

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Reference

1-drugs.com

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nicardipine محاضرة 7