Nifedipine + Atenolol Pharmacology

Nifedipine + Atenolol

About Nifedipine + Atenolol
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Mechanism of Action of Nifedipine + Atenolol
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Pharmacokinets of Nifedipine + Atenolol
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Onset of Action for Nifedipine + Atenolol
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Duration of Action for Nifedipine + Atenolol
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Half Life of Nifedipine + Atenolol
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Side Effects of Nifedipine + Atenolol
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Contra-indications of Nifedipine + Atenolol
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Special Precautions while taking Nifedipine + Atenolol
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Nifedipine + Atenolol
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Interactions for Nifedipine + Atenolol
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Typical Dosage for Nifedipine + Atenolol
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Schedule of Nifedipine + Atenolol
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Storage Requirements for Nifedipine + Atenolol
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Effects of Missed Dosage of Nifedipine + Atenolol
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Effects of Overdose of Nifedipine + Atenolol
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Nifedipine

About Nifedipine
A dihydropyridine calcium channel blocker, Antianginal, antihypertensive,tocolytic.
Mechanism of Action of Nifedipine
Nifedipine is a dihydropyridine Ca channel blocker. It exerts it`s antianginal, antihypertensive actions through blocking the influx of Ca2+ ions through voltage gated L-type Ca channels to the peripheral vascular smooth muscle cells, Coronary smooth muscle cells and to the myocardial cells. Thus causes dilatation of vascular endothelium, decrease peripheral resistance, & reduce myocardial oxygen demand .It markedly relax arterioles and milder effects on veins, decrease after load and increase cardiac index. It do not compromise haemodynamics and cerebral and renal perfusion. It inhibits platelet aggregation and relaxes bronchial, uterine, and ureteric smooth muscles. It is an effective uterine relaxant agent.
Migraine: It is used in migraine by reducing intracellular Ca+2 overload due to brain hypoxia and other causes.
Pharmacokinets of Nifedipine
Absorption: Well absorbed orally, Distribution: Widely distributed in a protein bound form, Metabolism: Metabolized in liver. Excretion: Excreted through urine and faeces
Onset of Action for Nifedipine
Half to two hours
2 to 3minutes for sublingual
Duration of Action for Nifedipine
4 to 8hours,
2 to 3minutes for sublingual
Half Life of Nifedipine
2 to 5 hours
Side Effects of Nifedipine
1.Tachycardia
2.Palpitation
3.Hypotension
4.Nausea
5.Edema
6.Headache
7.Dizziness
8.Fatigue
9.Orthostatic hypotension
10.Leg cramps
11.Rashes
12.Gingival hyperplasia
13.Congestive heart failures

Contra-indications of Nifedipine
1.Acute myocardial infarction
2.Heart failure
3.Aortic stenosis
4.Hypotension
5.Cardiogenic shock
6.Hypersensitivity to the drug
7.Unstable angina
8.Coronary artery diseases
Special Precautions while taking Nifedipine
1.Congestive heart failure
2.Cardiovascular insufficiency
3.Hypotension
4.Left ventricular outflow obstruction
5.Hepatic impairment
6.Slowly withdraw the drug with caution
7.Use cautiously along with other antihypertensive drugs
8.Diabetes mellitus

Pregnancy Related Information
Contraindicated.
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Use with caution.
Children Related Information
Use with caution.
Indications for Nifedipine
1.Hypertension
2.Hypertensive emergencies
3.Prinzmetal`s angina and Stable angina
4.As Tocolytic agent
5.In mountain sickness
6.Bronchial asthma
7.Peripheral vascular disorders
8. Migraine prophylaxis
9.Oesophageal spasm

Interactions for Nifedipine
Histamine H2 antagonists: Cimetidine and ranitidine enhance the bioavailability of nifedipine.
Beta-blockers: Though advantageous in some, concomitant use results in increased adverse effects like bradycardia and conduction disturbances.
Digitalis Glycosides: Increased serum digoxin levels with pssible toxicity.
Magnesium Sulphate: With parenteral magnesium suplhate neuromuscular blockade and hypotension may occur.
Theophyllines: Increased pharmacological effects of theophylline, resulting in toxicity.
Quinidine: Hypotension, bradycardia, ventricular tachycardia, AV block and pulmonary oedema may occur. Serum quinidine levels may also be decreased by nifedipine.
Anticoagulants: Increased prothrombin time.
Fentanyl: Severe hypotension or increased fluid requirements.
Typical Dosage for Nifedipine
Prinzmetal`s angina and Stable angina: Starts with 10mg 8th hourly. Increases the dosage up to 20mg 8th hourly. Further increases the dosage based on patient`s response at weekly intervals and repeat at 8th to 6th hourly.
Maximum daily dose: 120mg
Hypertension: 20mg twice daily or 30 to 60mg once daily extended release formulations. Adjust the dosage based on patient`s response.Maximum dose: 4omg twice daily
Maximum dose for extended release formulations: 120mg/day
Emergency reduction of blood pressure: Chew 10mg tablet and at the same time swallow another 10mg tablet. Repeat at every 20 to 30minutes.
As Tocolytic: 10mg sublingually and repeat at 20minutes for 2 to 3 doses.
Maintenance dosage: 10 to 20mg orally every 4 to 6 hours
Children:
For hypertensive emergencies: 250mcg to 500mcg/kg/dose 3 to 4 times daily.

Schedule of Nifedipine
H
Storage Requirements for Nifedipine
Store at room temperature below 30 degree C. Protect from moisture and avoid freezing.
Effects of Missed Dosage of Nifedipine
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Nifedipine
Monitor & support cardiac and respiratory functions. Measure the BP. Give cardiovascular support by elevating the limbs and maintaining fluid balance. Administer vasopressers like Nor epinephrine and Calcium gluconate if required.

Atenolol

About Atenolol
Cardioselective Beta(Beta1 )-adrenergic blocking agent, Antihypertensive,anti anginal.
Mechanism of Action of Atenolol
Atenolol is a cardio selective beta-1 adrenergic antagonist. It has negative chronotropic and negative inotropic effects on heart. It decreases oxygen consumption; cardiac work and aortic pressure. It decreases nor adrenaline and renin releases. It decreases central sympathetic out flow In sympathetic over activity, it prolongs systole by retarding conduction. It increases oxygen supply and exercise tolerance in angina patients. The drug decreases BP in hypertensive individuals; both systolic and diastolic BP is reduced.
Antimigraine action: Atenolol is useful in migraine due to its beta blockade action. Through beta blockade action it inhibits vasodilation and relieves migraine.
Pharmacokinets of Atenolol
Absorption: Absorbed orally up to 60%, Distribution: Widely distributed but no CSF penetration Metabolism: A small portion is metabolized in liver. Excretion: Excreted mainly through urine. Remaining portion is excreted through faeces.
Onset of Action for Atenolol
1hour
Duration of Action for Atenolol
Below 1day
Half Life of Atenolol
6 - 7 hours
Side Effects of Atenolol
1.Heart failure
2.Gastrointestinal problems
3.Nausea
4.Tiredness
5.Sinus bradycardia
6.Depression
7.Rash
8.Dizziess
9.Fatigue
10.Vomiting
11.Diarrhoea
12.Bronchospasm
13.Fever
14.Leg pain
15.Changes in kidney function tests
16.Changes in liver function tests.
Contra-indications of Atenolol
1.Hypersensitivity to the drug
2.Second or third degree heart block
3.Heart failure
4.Cardiogenic shock
5.Sinus bradycardia
Special Precautions while taking Atenolol
1.Congestive heart failure
2.Hepatic impairment
3.Renal impairment
4.The drug should be gradually withdraw with caution
5.Bronchospastic disorders
6.Diabetes mellitus
7.Hyper thyroidism
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Atenolol
1.Hypertension
2. Angina
3.Myocardial infarction
4.Migraine prophylaxis
Interactions for Atenolol
Alcohol, Anaesthetics, Antidepressants, Anxiolytics, Hypnotics, Cimetidine, Diuretics: Enhanced hypotensive effect.
Analgesics: NSAIDs antagonise hypotensive effect.
Antibacterials (Rifampicin): Reduce plasma concentration of atenolol.
Antidiabetics: Enhanced hypoglycemic effect.
Antihypertensives: Enhanced hypotensive effect, with clonidine there is increased severity of rebound hypertension.
Calcium channel Blockers: increased risk of bradycardia and AV block with diltiazem, severe hypotension and heart failure with verapamil, nifedipine
Cardiac glycosides: Increased AV block and bradycardia.
Cholinergics: Effects antagonised by atenolol.
Corticosteroids: Antagonism of hypotensive effect.
Ergotamine: Increased peripheral vasoconstriction
Sympathomimetics: Severe hypertension with adrenaline and noradrenaline.
Lab. Tests: Interferes with Glucose or insulin tolerence tests.
Typical Dosage for Atenolol
Hypertension: Starts with 50mg single dose then gradually increases at weekly intervals to 100mg/day once daily based on patient`s response.
Children: 1 to 1.3 mg/kg/day once daily or as two divided doses
Angina: Starts with 50mg single dose orally, and then gradually increases to 100mg/day based on patient`s response at one week intervals
Maximum dose: 200mg/day
Myocardial infarction: 5mg I.V. over 5minuts twice daily at 10minuts intervals. Then after 10minuts starts oral therapy with 50mg dose. Then 50mg at 12th hour. And increases to 100mg/day once daily or in two divided doses up to 9days
Migraine prophylaxis: 50 - 150mg / day in divided doses
Schedule of Atenolol
H
Storage Requirements for Atenolol
Store at room temperature and protect from heat, moisture, and direct sunlight
Effects of Missed Dosage of Atenolol
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Atenolol
Treatment is supportive and symptomatic. After ingestion empty the stomach by induced emesis or gastric lavage. Administer activated charcoal to reduce absorption

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