Losartan potassium + Atenolol Pharmacology

Losartan potassium + Atenolol

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

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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