Losartan potassium + Enalapril Pharmacology

Losartan potassium + Enalapril

About Losartan potassium + Enalapril
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Mechanism of Action of Losartan potassium + Enalapril
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Pharmacokinets of Losartan potassium + Enalapril
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Onset of Action for Losartan potassium + Enalapril
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Duration of Action for Losartan potassium + Enalapril
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Half Life of Losartan potassium + Enalapril
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Side Effects of Losartan potassium + Enalapril
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Contra-indications of Losartan potassium + Enalapril
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Special Precautions while taking Losartan potassium + Enalapril
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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 Losartan potassium + Enalapril
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Interactions for Losartan potassium + Enalapril
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Typical Dosage for Losartan potassium + Enalapril
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Schedule of Losartan potassium + Enalapril
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Storage Requirements for Losartan potassium + Enalapril
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Effects of Missed Dosage of Losartan potassium + Enalapril
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Effects of Overdose of Losartan potassium + Enalapril
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Losartan Potassium

About Losartan Potassium
An angiotensin II receptor antagonist, Antihypertensive.
Mechanism of Action of Losartan Potassium
It is a competitive antagonist of angiotensin-2 at AT-1 receptor. It decreases peripheral resistance and lowers BP in hypertensive individuals. It blocks all overt actions of angiotensin-2 such as: - 1. Vasoconstriction, 2. Central & Peripheral sympathetic stimulus, 3. Release of aldosterone and adrenaline, 4. Salt and water reabsorption, 5. Central actions like thirst, vasopressin release, and growth promoting actions on heart and blood vessels.
Pharmacokinets of Losartan Potassium
Absorption: Well absorbed orally, but bioavailability is about 33% due to first pass metabolism.
Distribution: Distributed in to the body in a protein bound form, but there is no brain penetration.
Metabolism: Metabolized in the liver in to active carboxylic acid metabolite and other metabolites.
Excretion: Excreted through faeces and urine.
Onset of Action for Losartan Potassium
1 hour
Duration of Action for Losartan Potassium
N/A
Half Life of Losartan Potassium
2 hours
Half life of active metabolite: 6 to 9 hours
Side Effects of Losartan Potassium
1. Hypotension
2. Hyperkalemia
3. Headache
4. Breathlessness
5. Chest pain
6. Sore throat
7. Infections
8. Weakness
9. Dizziness
10. Elevated liver enzyme levels
11. Myalgia
12. Fetopathic
13. Precipitate renal failure in renal artery stenosis, and in insufficient renal blood flow
14. Rashes
15. Insomnia
16. Nightmares
Contra-indications of Losartan Potassium
1. Hypersensitivity to the drug
Special Precautions while taking Losartan Potassium
1.Hepatic impairment
2.Renal impairment
3.Heart failure
4.Volume depleted individuals
5.Monitor serum potassium levels and avoid use along with potassium sparing diuretics
6. Avoid driving or operating heavy machinery during therapy
7. Avoid alcohol use during therapy
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
Indications for Losartan Potassium
1. Hypertension
Interactions for Losartan Potassium
Diuretics, other antihypertensives: Potentiate the hypotensive effect of losartan.
Potassium sparing diuretics, potassium suppliments: Risk of hyperkalaemia.
NSAIDs: May blunt hypotensive effect of losartan.
Cytochrome P450 inhibitors like ketoconazole: Increase in AUC of losartan by 18 % but has no effect on its active metabolite.
Phenobarbital: Results in 20% reduction in AUC of losartan and its active metabolite.
Typical Dosage for Losartan Potassium
25 to 50mg once daily. Gradually increases up to 100mg once daily or as two divided doses.
Schedule of Losartan Potassium
H
Storage Requirements for Losartan Potassium
Store at room temperature at a range of 15 to 30 degree C. protect from moisture and store in a tightly closed container.
Effects of Missed Dosage of Losartan Potassium
Take the missed dose as soon as remember; if it is the time of next dose then skip the missed dose and take the regular dose.
Effects of Overdose of Losartan Potassium
Treatment is supportive and symptomatic.

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.

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