Atenolol + Amiloride + Hydrochlorothiazide Pharmacology

Atenolol + Amiloride + Hydrochlorothiazide

About Atenolol + Amiloride + Hydrochlorothiazide
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Mechanism of Action of Atenolol + Amiloride + Hydrochlorothiazide
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Pharmacokinets of Atenolol + Amiloride + Hydrochlorothiazide
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Onset of Action for Atenolol + Amiloride + Hydrochlorothiazide
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Duration of Action for Atenolol + Amiloride + Hydrochlorothiazide
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Half Life of Atenolol + Amiloride + Hydrochlorothiazide
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Side Effects of Atenolol + Amiloride + Hydrochlorothiazide
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Contra-indications of Atenolol + Amiloride + Hydrochlorothiazide
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Special Precautions while taking Atenolol + Amiloride + Hydrochlorothiazide
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Pregnancy Related Information
Contraindicated; Atenolol, Amiloride and Hydrochlorothiazide are contraindicated in pregnancy. So the combination generic is contraindicated in pregnancy.
Old Age Related Information
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Breast Feeding Related Information
Breast feeding: Contraindicated; since Atenolol, Amiloride and Hydrochlorothiazide are contraindicated in lactation. So the combination generic is contraindicated in breast feeding.
Children Related Information
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Indications for Atenolol + Amiloride + Hydrochlorothiazide
It is a combination of beta blocker -Atenolol, thiazide diuretic- hydrochlorothiazide and potassium sparing diuretic Amiloride.
1.Hypertension
Interactions for Atenolol + Amiloride + Hydrochlorothiazide
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Typical Dosage for Atenolol + Amiloride + Hydrochlorothiazide
1 tablet / day and if needed dose can be increased to 2 tablet / day.
Schedule of Atenolol + Amiloride + Hydrochlorothiazide
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Storage Requirements for Atenolol + Amiloride + Hydrochlorothiazide
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Effects of Missed Dosage of Atenolol + Amiloride + Hydrochlorothiazide
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Effects of Overdose of Atenolol + Amiloride + Hydrochlorothiazide
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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

Amiloride

About Amiloride
Potassium-Sparing Diuretic , a pyrazine-carbonyl-guanidine, Diuretic, Antihypertensive.
Mechanism of Action of Amiloride
Amiloride 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 Amiloride
Absorption: 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 Amiloride
2hours
Duration of Action for Amiloride
24 hours.
Half Life of Amiloride
6 to 9 hours
Side Effects of Amiloride
1.Headache
2.Orthostatic hypotension
3.Confusion
4.Nausea
5.Diarrhoea
6.Anorexia
7.Weakness
8.Hyperkalemia
9.Hyponatremia
10.Aplastic anaemia
11.Neutropenia
12.Impotence
13.Altered liver function tests
14.Altered kidney function tests
15.Gastro intestinal disturbances
16.Constipation
17.Dyspnoea
18.Rashes
19.Ototoxicity
Contra-indications of Amiloride
1.Hypersensitivity to the drug
2.Renal impairment
3.Hyper kalemia
4.Along with other potassium sparing diuretics
5.Anuria
6.Diabetic nephropathy.
Special Precautions while taking Amiloride
1.Hepatic impairment
2.Diabetes mellitus
3.Along with other diuretics


Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Contraindicated.
Children Related Information
Contraindicated
Indications for Amiloride
1.Adjunctive in treatment of Hypertension
2.Edema associated with heart failure with potassium conservation
3.Edema where potassium conservation is needed.
4.Liddle`s syndrome
Interactions for Amiloride
Lithium: Increaes serum lithium levels and toxicity.
Ace inhibitors: Increased risk of potassium retention.
Digoxin: Increased renal clearance of digoxin.

Typical Dosage for Amiloride
5mg 1 to 2 times daily. Increased to 10mg 1 to 2 times if required.
Schedule of Amiloride
H
Storage Requirements for Amiloride
Store 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 Amiloride
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 Amiloride
Treatment 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.

Hydrochlorothiazide

About Hydrochlorothiazide
Thiazide derivatibve, Diuretic.
Mechanism of Action of Hydrochlorothiazide
It 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 Hydrochlorothiazide
Absorption: It is absorbed after oral administration.
Metabolism: It is not metabolized in the body.
Excretion: Excreted unchanged in urine.

Onset of Action for Hydrochlorothiazide
1 to 3 hours
Duration of Action for Hydrochlorothiazide
12 to 16 hours
Half Life of Hydrochlorothiazide
5 to 15 hours
Side Effects of Hydrochlorothiazide
1. 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 Hydrochlorothiazide
1. 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 Hydrochlorothiazide
1. 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 Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
May be used
Indications for Hydrochlorothiazide
1. 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 Hydrochlorothiazide
Cholestyramine & 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 Hydrochlorothiazide
Adults:
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 Hydrochlorothiazide
G
Storage Requirements for Hydrochlorothiazide
Store at room temperature in a well closed container and protected from light.
Effects of Missed Dosage of Hydrochlorothiazide
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 Hydrochlorothiazide
Treatment 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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