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- Pharmacology For Atenolol + Amiloride + Hydrochlorothiazide
Atenolol + Amiloride + Hydrochlorothiazide Pharmacology
Atenolol + Amiloride + HydrochlorothiazideAbout Atenolol + Amiloride + HydrochlorothiazideN/AMechanism of Action of Atenolol + Amiloride + HydrochlorothiazideN/APharmacokinets of Atenolol + Amiloride + HydrochlorothiazideN/AOnset of Action for Atenolol + Amiloride + HydrochlorothiazideN/ADuration of Action for Atenolol + Amiloride + HydrochlorothiazideN/AHalf Life of Atenolol + Amiloride + HydrochlorothiazideN/ASide Effects of Atenolol + Amiloride + HydrochlorothiazideN/AContra-indications of Atenolol + Amiloride + HydrochlorothiazideN/ASpecial Precautions while taking Atenolol + Amiloride + HydrochlorothiazideN/APregnancy Related InformationContraindicated; Atenolol, Amiloride and Hydrochlorothiazide are contraindicated in pregnancy. So the combination generic is contraindicated in pregnancy.Old Age Related InformationN/ABreast Feeding Related InformationBreast feeding: Contraindicated; since Atenolol, Amiloride and Hydrochlorothiazide are contraindicated in lactation. So the combination generic is contraindicated in breast feeding.Children Related InformationN/AIndications for Atenolol + Amiloride + HydrochlorothiazideIt is a combination of beta blocker -Atenolol, thiazide diuretic- hydrochlorothiazide and potassium sparing diuretic Amiloride.
Interactions for Atenolol + Amiloride + HydrochlorothiazideN/ATypical Dosage for Atenolol + Amiloride + Hydrochlorothiazide1 tablet / day and if needed dose can be increased to 2 tablet / day.Schedule of Atenolol + Amiloride + HydrochlorothiazideN/AStorage Requirements for Atenolol + Amiloride + HydrochlorothiazideN/AEffects of Missed Dosage of Atenolol + Amiloride + HydrochlorothiazideN/AEffects of Overdose of Atenolol + Amiloride + HydrochlorothiazideN/A
AtenololAbout 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
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
Special Precautions while taking Atenolol1.Congestive heart failure
4.The drug should be gradually withdraw with caution
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Atenolol1.Hypertension
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 absorption
AmilorideAbout AmiloridePotassium-Sparing Diuretic , a pyrazine-carbonyl-guanidine, Diuretic, Antihypertensive.Mechanism of Action of AmilorideAmiloride is a guanidine derivative which exerts its diuretic action by interacting with renal epithelial Na+ channels in distal tubules and collecting duct and prevents sodium reabsorption. It prevents potassium lose. It also increases chloride, bicarbonate, and water excretion and decreases H+ excretion. The drug augment the natriuretic and anti hypertensive response of other drugs. It is used in the management of edema associated with congestive heart failure, hepatic cirrhosis and idiopathic edema. It is used mainly in combination with other drugs in the management of hypertension and to correct hypokalemia caused by other diuretic drugs.Pharmacokinets of AmilorideAbsorption: Orally absorbed up to 50%. Food decreases absorption. Distribution: Widely distributed extravascularly. Metabolism: It is not metabolized in the body. Excretion: Excreted mainly through urine.
Onset of Action for Amiloride2hoursDuration of Action for Amiloride24 hours.Half Life of Amiloride6 to 9 hoursSide Effects of Amiloride1.Headache
13.Altered liver function tests
14.Altered kidney function tests
15.Gastro intestinal disturbances
Contra-indications of Amiloride1.Hypersensitivity to the drug
4.Along with other potassium sparing diuretics
Special Precautions while taking Amiloride1.Hepatic impairment
3.Along with other diuretics
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with caution.Breast Feeding Related InformationContraindicated.Children Related InformationContraindicatedIndications for Amiloride1.Adjunctive in treatment of Hypertension
2.Edema associated with heart failure with potassium conservation
3.Edema where potassium conservation is needed.
Interactions for AmilorideLithium: Increaes serum lithium levels and toxicity.
Ace inhibitors: Increased risk of potassium retention.
Digoxin: Increased renal clearance of digoxin.
Typical Dosage for Amiloride5mg 1 to 2 times daily. Increased to 10mg 1 to 2 times if required.Schedule of AmilorideHStorage Requirements for AmilorideStore in a well closed container at a temperature range of 15 to 30 degree C. Protects from light, moisture and freezing.Effects of Missed Dosage of AmilorideTake 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 AmilorideTreatment is supportive and symptomatic. Drug is removed by induced emesis or gastric lavage. Monitor & support serum electrolyte level and blood acidosis. To reduce potassium levels administer I.V. sodium bicarbonate or glucose with insulin. Potassium levels can be also lowered by cation exchange resins like sodium polystyrene sulfonate given orally or as retention enema.
HydrochlorothiazideAbout 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
4. Tingling fingers
5. Dry mouth
14. Elevated levels of glucose, calcium and lipids
15. Gastro intestinal disturbances
17. Electrolyte imbalance
24. Muscle cramps
26. Blood dyscrasias
Contra-indications of Hydrochlorothiazide1. Hyper uricaemia
2. Hyper calcaemia
3. Renal impairment
4. Hepatic impairment
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
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.
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.
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.
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.
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