Losartan potassium + Perindopril Pharmacology

Losartan potassium + Perindopril

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

Perindopril

About Perindopril
A long-acting Dicarboxylate-containing ACE inhibitor, Antihypertensive.
Mechanism of Action of Perindopril
It is a prodrug and converted in to active Perindoprilat; which is a long acting 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. 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. The drug restores the reduced elastic properties of arteries and heart in hypertensive individuals. 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 Perindopril
Absorption: Well absorbed orally, Distribution: It is distributed in to the body, Metabolism: Metabolized in the body in to active metabolite, Perindoprilat; and other inactive metabolites Excretion: Excreted mainly through urine.
Onset of Action for Perindopril
60minutes
Duration of Action for Perindopril
24 hour
Half Life of Perindopril
N/A
Side Effects of Perindopril
1.Cough
2.Angioedema
3.Chest pain
4.Hyperkalemia
5.Rashes
6.Urticaria
7.Swelling of lips, mouth, nose, and larynx
8.Fetopathic in later half of pregnancy
9.Headache
10.Dizziness
11.Depression
12.Sleep disturbances
13.Diarrhoea
14.Anorexia
15.Nausea
16.Vomiting
17.Fatigue
18.Decreased haemoglobin count
19.Infections
20.Elevated liver enzymes
21.Acute renal failure is precipitated in renal artery stenosis


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

Special Precautions while taking Perindopril
1.Renal impairment
2.Hepatic impairment
3.Ischaemic heart disease
4.Severe heart failure
5.Collagen vascular diseases
6.Angioedema
7.Cerebrovascular diseases
8.Lower dosage is needed for elderly

Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
Indications for Perindopril
1.Hypertension
2.Congestive heart failure
Interactions for Perindopril
Nitrates, Diuretics, Beta-blockers, Anti-depressants, Alcohol, Calcium channel blockers: Enhanced hypotensive effect.
Potassium sparing diuretics: Hyperkalaemia.
Sex hormones: Oestrogens and combined oral contraceptives antagonise hypotensive effect.
Typical Dosage for Perindopril
Starts with 4mg; orally once daily. Increases the dose to 8mg once daily or in two divided doses; after one month of therapy depending on patient`s response.
Maximum dose: 16mg/day
In CHF patients starts the dosage with 2mg once daily dosage and gradually increases at 1 to2 weeks` intervals to 4mg or further increase in dose depends up on patient`s response.

Schedule of Perindopril
H
Storage Requirements for Perindopril
Store at a temperature range of 15 to 30 degree C. in a well closed container and protect from light and moisture.

Effects of Missed Dosage of Perindopril
N/A
Effects of Overdose of Perindopril
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 to treat hypotension. Treat dehydration and maintain electrolyte balance.

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