Valsartan + Hydrochlorothiazide Pharmacology

Valsartan + Hydrochlorothiazide

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

About Valsartan
Angiotensin II receptor antagonist, Antihypertensive.
Mechanism of Action of Valsartan
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 Valsartan
Absorption: Absorbed orally, bioavailability is about 25%.
Distribution: It is distributed in to the body in a protein bound form.
Metabolism: About 20% of the drug undergoes metabolism.
Excretion: Excreted mainly through faeces and rest is excreted through urine.
Onset of Action for Valsartan
2 hours
Duration of Action for Valsartan
24 hours
Half Life of Valsartan
6 hours
Side Effects of Valsartan
1. Dizziness
2. Headache
3. Coughing
4. Edema
5. Nausea
6. Abdominal pain
7. Diarrhoea
8. Pharyngitis
9. Rhinitis
10. Sinusitis
11. Upper respiratory tract infections
12. Weakness
13. Arthralgia
14. Neutropenia
15. Fetopathic
16. Precipitate renal failure in renal artery stenosis and in insufficient renal blood flow
17. Rashes
18. Hyperkalemia

Contra-indications of Valsartan
1. Hypersensitivity to the drug
Special Precautions while taking Valsartan
1.Renal impairment: Use with caution in renal impairment. Precipitate renal failure in renal artery stenosis, and in insufficient renal blood flow.
2.Hepatic impairment: Use with caution in hepatic impairment and dosage adjustment is required.
3.Heart failure
4.Aortic or mitral valve stenosis
5.Obstructive cardiomyopathy
6. Use cautiously in volume depleted and salt depleted individuals
7. Patient should be cautiously involve in driving or operating heavy machinery during therapy
8. Avoid alcohol or use with caution during therapy
9. Use with caution in hyperkalemia and along with potassium sparing diuretics


Pregnancy Related Information
Contraindicated.
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
Indications for Valsartan
1. Hypertension
Interactions for Valsartan
Potassium-sparing diuretics (e.g., Spironolactone, Triamterene, Amiloride), Potassium supplements, or Salt substitutes containing potassium: Concomitant use of Valsartan with these drugs will result in hyperkalaemia and in heart failure patients it increases serum creatinine.
Typical Dosage for Valsartan
Starts with 80mg once daily. Increase the dosage after 2 to 4 weeks intervals depending upon the patient`s response to 160mg once daily or two divided doses or a diuretic should be added if required. Further increase in dosage is depending up on patient`s response.
Maximum dose: 320mg/day.

Schedule of Valsartan
H
Storage Requirements for Valsartan
Store at room temperature at a range of 15 to 30 degree C. protects from direct heat and light and store in a tightly closed container.
Effects of Missed Dosage of Valsartan
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 Valsartan
Treatment is supportive and symptomatic. If hypotension occur kept patient in supine position and if required give I.V. infusion of normal saline.

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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