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- Pharmacology For Losartan Potassium + Atenolol + Hydrochlorothiazide
Losartan Potassium + Atenolol + Hydrochlorothiazide Pharmacology
Losartan Potassium + Atenolol + Hydrochlorothiazide
About Losartan Potassium + Atenolol + HydrochlorothiazideN/AMechanism of Action of Losartan Potassium + Atenolol + HydrochlorothiazideN/APharmacokinets of Losartan Potassium + Atenolol + HydrochlorothiazideN/AOnset of Action for Losartan Potassium + Atenolol + HydrochlorothiazideN/ADuration of Action for Losartan Potassium + Atenolol + HydrochlorothiazideN/AHalf Life of Losartan Potassium + Atenolol + HydrochlorothiazideN/ASide Effects of Losartan Potassium + Atenolol + HydrochlorothiazideN/AContra-indications of Losartan Potassium + Atenolol + HydrochlorothiazideN/ASpecial Precautions while taking Losartan Potassium + Atenolol + HydrochlorothiazideN/APregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Losartan Potassium + Atenolol + HydrochlorothiazideHypertensionInteractions for Losartan Potassium + Atenolol + HydrochlorothiazideN/ATypical Dosage for Losartan Potassium + Atenolol + HydrochlorothiazideN/ASchedule of Losartan Potassium + Atenolol + HydrochlorothiazideN/AStorage Requirements for Losartan Potassium + Atenolol + HydrochlorothiazideN/AEffects of Missed Dosage of Losartan Potassium + Atenolol + HydrochlorothiazideN/AEffects of Overdose of Losartan Potassium + Atenolol + HydrochlorothiazideN/ALosartan Potassium
About Losartan PotassiumAn angiotensin II receptor antagonist, Antihypertensive.Mechanism of Action of Losartan PotassiumIt 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 PotassiumAbsorption: 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 Potassium1 hourDuration of Action for Losartan PotassiumN/AHalf Life of Losartan Potassium2 hours
Half life of active metabolite: 6 to 9 hours
Side Effects of Losartan Potassium1. 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 Potassium1. Hypersensitivity to the drugSpecial Precautions while taking Losartan Potassium1.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 InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Losartan Potassium1. HypertensionInteractions for Losartan PotassiumDiuretics, 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 Potassium25 to 50mg once daily. Gradually increases up to 100mg once daily or as two divided doses.Schedule of Losartan PotassiumHStorage Requirements for Losartan PotassiumStore 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 PotassiumTake 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 PotassiumTreatment is supportive and symptomatic.Atenolol
About AtenololCardioselective Beta(Beta1 )-adrenergic blocking agent, Antihypertensive,anti anginal.Mechanism of Action of AtenololAtenolol 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 AtenololAbsorption: 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 Atenolol1hourDuration of Action for AtenololBelow 1dayHalf Life of Atenolol6 - 7 hoursSide Effects of Atenolol1.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 Atenolol1.Hypersensitivity to the drug
2.Second or third degree heart block
3.Heart failure
4.Cardiogenic shock
5.Sinus bradycardia
Special Precautions while taking Atenolol1.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 InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Atenolol1.Hypertension
2. Angina
3.Myocardial infarction
4.Migraine prophylaxisInteractions for AtenololAlcohol, 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 AtenololHypertension: 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 AtenololHStorage Requirements for AtenololStore at room temperature and protect from heat, moisture, and direct sunlightEffects of Missed Dosage of AtenololTake 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 AtenololTreatment is supportive and symptomatic. After ingestion empty the stomach by induced emesis or gastric lavage. Administer activated charcoal to reduce absorptionHydrochlorothiazide
About HydrochlorothiazideThiazide derivatibve, Diuretic.Mechanism of Action of HydrochlorothiazideIt is thiazide diuretic which exerts its action by acting at site-3(central dilating segment of early distal tubule). It binds to Na+Cl- symporter and inhibits Na+Cl- symport at the luminal membrane. It has additional carbonic anhydrase inhibitory actions in proximal tubules. It increases natriuresis, kaliuresis and diuresis. It decreases Ca2+ excretion and increases Mg2+excretion. It also has minor carbonic anhydrase inhibitory action. It also causes direct arteriolar vasodilatation and decreases total peripheral resistance. The antihypertensive actions of the drug may be attributable to depletion of sodium and subsequent reduction in plasma volume and a decrease in peripheral resistance. Decrease in peripheral resistance is due to either the loss of sodium from the arteriolar wall or a direct action on the vascular bed. It is an effective drug in edema associated with congestive heart failure.
Vertigo: Diuretics are used in vertigo in assumption that vertigo is due to endolymphatic hydrops. They reduce labyrinthine fluid pressure
Pharmacokinets of HydrochlorothiazideAbsorption: It is absorbed after oral administration.
Metabolism: It is not metabolized in the body.
Excretion: Excreted unchanged in urine.
Onset of Action for Hydrochlorothiazide1 to 3 hoursDuration of Action for Hydrochlorothiazide12 to 16 hoursHalf Life of Hydrochlorothiazide5 to 15 hoursSide Effects of Hydrochlorothiazide1. Dizziness
2. Blurred vision
3. Confusion
4. Tingling fingers
5. Dry mouth
6. Nausea
7. Diarrhoea
8. Constipation
9. Vomiting
10. Weakness
11. Hypokalaemia
12. Hyponatraemia
13. Hyperuricaemia
14. Elevated levels of glucose, calcium and lipids
15. Gastro intestinal disturbances
16. Polyuria
17. Electrolyte imbalance
18. Jaundice
19. Rashes
20. Photosensitivity
21. Fever
22. Itching
23. Myalgia
24. Muscle cramps
25. Arthralgia
26. Blood dyscrasias
27. Ototoxicity
Contra-indications of Hydrochlorothiazide1. Hyper uricaemia
2. Hyper calcaemia
3. Renal impairment
4. Hepatic impairment
5. Anuria
6. Hypersensitivity to the drug
7. Hyper sensitivity to sulfonamides
8. Fluid and electrolyte imbalance
Special Precautions while taking Hydrochlorothiazide1. Gout
2. Diabetes mellitus
3. Renal impairment
4. Hepatic impairment
5. Monitor and correct Fluid and electrolyte imbalance
6. Hyper parathyroidism
7. Cirrhosis
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationMay be usedIndications for Hydrochlorothiazide1. Hypertension
2. Oedema associated with heart failure
3. Oedema due to renal and hepatic diseases
4. Diabetes insipidus
5. Idiopathic hypercalciurea.
6. Vertigo
Interactions for HydrochlorothiazideCholestyramine & Colestipol: decrease absorption of hydrochlorothiazide.
Diazoxide: Additive action - may cause hyperglycemia, hyperuricaemia and hypotension.
Digitalis: Diuretics induced hypokalaemia may precipitate digitalis toxicity.
Lithium: Hydrochlorothiazide potentiates therapeutic and toxic effects by increasing its renal excretion.
Frusemide: Synergy leading to profound diuresis and greater than predicted electrolyte loss.
Non-depolarizing muscle relaxants: Diuretics induced hypokalaemia enhances efficacy.
Sulfonylureas: Efficacy decreased due to hydrochlorothiazide induced glucose intolerance.
Chlorpropamide: Hypokalaemia.
Propantheline: Bioavailability of hydrochlorothiazide increased.
Metoclopramide: Bioavailability of hydrochlorothiazide decreased.
NSAIDs: Natriuretic effect of hydrochlorothiazide decreased.
Typical Dosage for HydrochlorothiazideAdults:
Hypertension: 25mg once daily or in divided doses. Increased to 50mg if required; depending up on the patient`s response.
Children: 1mg/kg single daily dose.
Oedema:
Adults:
Starts with 25 to 50mg. Increased the dose until desired response is obtained.
Maximum dose: 200mg/day
Maintenance dosage: 25 to 100mg daily or on alternate days.
Children: 1mg/kg single daily dose or 1 to 3mg/kg/day in two divided doses
Schedule of HydrochlorothiazideGStorage Requirements for HydrochlorothiazideStore at room temperature in a well closed container and protected from light.Effects of Missed Dosage of HydrochlorothiazideTake 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 HydrochlorothiazideTreatment is supportive and symptomatic. Remove drug from the body by induced emesis and gastric lavage. Monitor and assist respiratory, cardiovascular, and renal function as indicated. Monitor and support fluid and electrolyte balance.Home Delivery for Losartan Potassium + Atenolol + Hydrochlorothiazide in Your City
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