Enalapril + Amlodipine Pharmacology

Enalapril + Amlodipine

About Enalapril + Amlodipine
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Mechanism of Action of Enalapril + Amlodipine
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Pharmacokinets of Enalapril + Amlodipine
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Onset of Action for Enalapril + Amlodipine
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Duration of Action for Enalapril + Amlodipine
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Half Life of Enalapril + Amlodipine
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Side Effects of Enalapril + Amlodipine
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Contra-indications of Enalapril + Amlodipine
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Special Precautions while taking Enalapril + Amlodipine
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Pregnancy Related Information
Contraindicated since Enalapril and Amlodipine are contraindicated during pregnancy
Old Age Related Information
N/A
Breast Feeding Related Information
Use with caution since Enalapril and Amlodipine are used with caution in pregnancy
Children Related Information
N/A
Indications for Enalapril + Amlodipine
1.Refractory hypertension
2.Hypertension co-existing with congestive cardiac failure
Interactions for Enalapril + Amlodipine
N/A
Typical Dosage for Enalapril + Amlodipine
Adult: one tablet once daily. Then gradually increase the dose according to response.
Following combinations are available in the market.
Enalapril: 2.5mg + Amlodipine: 2.5mg or
Enalapril: 2.5mg + Amlodipine: 5mg or
Enalapril: 5mg + Amlodipine: 5mg.
Schedule of Enalapril + Amlodipine
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Storage Requirements for Enalapril + Amlodipine
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Effects of Missed Dosage of Enalapril + Amlodipine
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Effects of Overdose of Enalapril + Amlodipine
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Enalapril

About Enalapril
Angiotensin converting enzyme (ACE) inhibitor, Antihypertensive.
Mechanism of Action of Enalapril
It is a prodrug and converted in to active Enalaprilat; which is an angiotensin converting enzyme inhibitor prevents the conversion of angiotensin-1 to angiotensin-2 and abolishes the pressor actions of angiotensin. It decreases aldosterone secretion, sodium and water retention, and total peripheral resistance, leads to fall in BP. The arterioles dilate and the compliance of larger arteries is increased. Both systolic and diastolic BP is lowered. It has no effect on cardiac output and cardiovascular reflexes. And there is little dilatation of capacitance vessels; so postural hypotension is not a problem. The drug does not compromise renal, cerebral, and coronary blood flow. The drug also increases plasma kinin levels and potentiate the hypotensive action of exogenously administered bradykinin. It is used for treatment of systolic heart failure, because it improves symptoms, decrease mortality and reduce ventricular hypertrophy. It reduces both preload and after load and thus increasing cardiac out put in patients with heart failure.
Pharmacokinets of Enalapril
Absorption: Absorbed orally up to60%
Distribution: Widely distributed, but poor brain penetration.
Metabolism: Metabolized in to active metabolite Enalaprilat
Excretion: Excreted mainly through urine and a small amount is excreted through faeces
Onset of Action for Enalapril
1 hour
Duration of Action for Enalapril
24 hour
Half Life of Enalapril
11 hours
Side Effects of Enalapril
1. Cough
2. Angioedema
3. Hypotension
4. Bradycardia
5. Hyperkalemia
6. Rashes
7. Urticaria
8. Swelling of lips, mouth, nose and larynx
9. Fetopathic in later half of pregnancy
10. Headache
11. Diarrhoea
12. Fatigue
13. Dizziness
14. Nausea
15. Acute renal failure is precipitated in renal artery stenosis
16. Transient increase in liver enzymes.

Contra-indications of Enalapril
1. Hypersensitivity to the drug
2. Renal artery stenosis
3. Aortic stenosis
4. Coarctation of aorta

Special Precautions while taking Enalapril
1. Renal impairment
2. Patient at high risk of cardiogenic shock, severe heart failure etc
3. Anaesthesia and surgery
4. Stops diuretics 2 to 3days before Enalapril therapy
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 Enalapril
1. Hypertension
2. Congestive heart failure
3. Left ventricular dysfunction

Interactions for Enalapril
Antacids: Decrease effeciency of Captopril.
Indomethacin: Reduces hypotensive effect.
Digoxin: Increases plasma digoxin levels.
Potassium preparations & potassium sparing diuretics: Hyperkalaemia and increased risk of renal failure.
Lithium: Toxicity due to increased serum concentration of lithium.
Immunosuppressive Drugs : Increased risk of bone marrow depression.
Antidepressants, diuretics, Beta-blockers, Nitrates, Dopaminergics, Calcium channel blockers, Phenothiazines: Enhance hypotensive effect.
Morphine: Enhanced analgesic effect and respiratory depression.
Typical Dosage for Enalapril
Adult:
5mg once daily. Increases the dose to 10 to 20mg once daily or as two divided doses depending on patient`s response if required.
Maximum dose: 40mg/day
In patient on diuretic therapy & In CHF patients starts the dosage with 2.5mg once daily dosage and increases to usual dosage.
Left ventricular dysfunction: Starts with 2.5mg orally twice daily. Increases the dosage up to 20mg/day in two divided doses.
Children : 0.1 to 0.5mg/kg/day once daily or in divided doses as suspension of crushed tablets.
Schedule of Enalapril
H
Storage Requirements for Enalapril
Store at room temperature in a well closed container and protect from moisture.
Effects of Missed Dosage of Enalapril
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose.Do not double the dose.
Effects of Overdose of Enalapril
Treatment is supportive and symptomatic. To remove drug from the body perform induced emesis and gastric lavage. Administer activated charcoal to reduce absorption. In severe cases haemodialysis is considered if required. Treatment includes I.V. infusion of normal saline solution.

Amlodipine

About Amlodipine
Calcium Channel Blocker, Anti hypertensive,anti angina.
Mechanism of Action of Amlodipine
Amlodipine is a second generation dihydropyridine Ca channel blocker. It exerts it`s antihypertensive, antianginal actions through blocking the influx of Ca 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. They do not compromise haemodynamics and cerebral and renal perfusion.
Pharmacokinets of Amlodipine
Absorption: Well absorbed orally, Distribution: Widely distributed in a protein bound form, Metabolism: Metabolized in liver, but there is no active metabolite.
Onset of Action for Amlodipine
Slow
Duration of Action for Amlodipine
24 hours
Half Life of Amlodipine
N/A
Side Effects of Amlodipine
1.Palpitation
2.Flushing
3.Nausea
4.Vomiting
5.Abdominal pain
6.Edema
7.Headache
8.Dizziness
9.Paresthesia
10.Light headedness
11.Fatigue
12.Aggravates myocardial ischaemia
13.Rashes
Contra-indications of Amlodipine
1.Heart failure
2.Aortic stenosis
3.Hypersensitivity to the drug
4.Unstable angina
5.Hepatic impairment
6.Along with other anti hypertensive drugs.
Special Precautions while taking Amlodipine
1.Cardiovascular disorders: Use cautiously in cardiovascular disorders because it aggravates myocardial ischaemia.
2.Sick sinus syndrome
3.Renal impairment
4.Use cautiously along with other antihypertensive drugs,
Pregnancy Related Information
Contraindicated.
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution.
Children Related Information
Contraindicated
Indications for Amlodipine
1.Hypertension
2.Prinzmetal`s angina
3.Stable angina
Interactions for Amlodipine
ACE inhibitors, Thiazide diuretics: Potentiates effect of these drugs.
Beta Blockers: Best avoided, especially by those with impaired LV function due to depressant effect on myocardial contractibility or AV conduction.
Fentanyl: Severe hypotension or increased fluid volume requirements.
Typical Dosage for Amlodipine
5 mg once daily.
Maximum dose: 10mg/day
Prinzmetal`s angina and Stable angina:
5 to 10mg once daily.
Hypertension: 2.5 to 5mg once daily. Dose may increase up to 10mg once daily as required by the individual needs.
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Schedule of Amlodipine
H
Storage Requirements for Amlodipine
Store at room temperature below 30 degree C. Protect from moisture and light.

Effects of Missed Dosage of Amlodipine
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 Amlodipine
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.

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