Triamterene + Frusemide Pharmacology

Triamterene + Frusemide

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

About Triamterene
A potassium-sparing diuretic, Diuretic,Antioedema, Adjunctive in therapy of hypertension.
Mechanism of Action of Triamterene
Triamterene exerts its diuretic action by interacting with renal epithelial Na+ channels in distal tubules and collecting duct and prevent sodium reabsorption. It prevents potassium and magnesium loses. It also increases chloride, bicarbonate, and water excretion. The drug augment the natriuretic and anti hypertensive response of other diuretic drugs. It is used in the management of edema associated with congestive heart failure, hepatic cirrhosis with ascites, nephrotic syndrome, 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 Triamterene
Absorption: Rapidly but incompleately absorbed orally, Distribution: It is distributed in a protein bound form, Metabolism: It metabolized in to an active metabolite in the body,
Excretion: Excreted through urine.
Onset of Action for Triamterene
2 to4hours
Duration of Action for Triamterene
12 to 16 hours
Half Life of Triamterene
100 to 150minutes
Side Effects of Triamterene
1.Headache
2.Dizziness
3.Nausea
4.Diarrhoea
5.Vomiting
6.Dry mouth
7.Weakness
8.Hyper kalemia
9.Hyponatremia
10.Thrombocytopenia
11.Agranulocytosis
12.Photosensitivity
13.Reduce glucose tolerance
14.Altered liver function tests
15.Altered kidney function tests
16.Gastro intestinal disturbances
17.Interstitial nephritis
18.Kidney stones
19.Rashes
20.Ototoxicity
Contra-indications of Triamterene
1.Hypersensitivity to the drug
2.Renal impairment
3.Hyper kalemia
4.Along with other potassium sparing diuretics
5.Anuria
6.Hepatic impairment

Special Precautions while taking Triamterene
1.Gout
2.Diabetes mellitus
3.Deliberate individuals

Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Triamterene
1.Oedema
2.Liddle`s syndrome
3.Adjunctive in therapy of hypertension

Interactions for Triamterene
Amantadine: Triamterene increases the toxic effects of Amantadine.
ACE inhibitors: May result in significant hyperkalaemia.
Indomethacin: May produce unexpectedly high incidence of nephrotoxicity.
Potassium preparations: May result in hyperkalaemia, possibly with cardiac arrhythmias or cardiac arrest, particularly in those with impaired renal function.
Lab tests: Since both triamterene and quinidine have similar fluorescene spectra, triamterene will interfere with fluoroscent measurement of Quinidine serum levels.
Typical Dosage for Triamterene
100 to 250mg/day in divided doses.
Children: 2mg/kg two times daily. Take after break fast & lunch. Reduce the dosage after one week in to alternate days.
Schedule of Triamterene
H
Storage Requirements for Triamterene
Store at controlled room temperature at a range of 20 to 25 degree C. in a well closed container and protects from light.




Effects of Missed Dosage of Triamterene
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 Triamterene
Treatment is supportive and symptomatic. Remove drug from the body by induced emesis and gastric lavage. Monitor and support electrolyte balance and blood acidosis. Reduce serum potassium with I.V. sodium bicarbonate or glucose with insulin. Potassium level is also reduced by a cation exchange resins like sodium polystyrene sulfonate given orally or as retention enema.

Frusemide

About Frusemide
A high ceiling loop diuretic, Symporter inhibitor,anthranilic acid derivative, Diuretic ,antiedema ,antihypertensive.
Mechanism of Action of Frusemide
Furosemide is a high ceiling loop diuretic which exerts it`s diuretic action by acting at site-2(thick ascending loop of Henle). It binds to Na+K+2Cl- co transporter and inhibits Na+K+2Cl- co transport in luminal membrane of thick ascending loop of Henle. It inhibits sodium and chloride re absorption and promotes excretion of sodium, water, chloride, potassium, calcium, and magnesium. It abolishes cortico-medullary osmotic gradient and blocks positive as well as negative free water clearance. It also has weak carbonic anhydrase inhibitory action.
It increase local prostaglandin synthesis and increases systemic venous capacitance and decreases left ventricular filling pressure. This causes relief in left ventricular failure and pulmonary edema. It causes renal and peripheral vasodilatation and decrease in peripheral resistance. It is preferred in the initial treatment of congestive heart failure for rapid mobilization of oedema fluid.
Vertigo: Diuretics are used in vertigo in assumption that vertigo is due to endolymphatic hydrops. They reduce labyrinthine fluid pressure.

Pharmacokinets of Frusemide
Absorption: Absorbed orally about 60%.
Distribution: It is widely distributed in a plasma protein bound form and crosses placenta. Metabolism: It is partly metabolized by glucuronide conjugation.
Excretion: Excreted as unchanged drug mainly through urine. Some drug is excreted through faeces
Onset of Action for Frusemide
Oral: 20 to 40 minutes
I.V.: 2 to 5 minutes
I.M.: 10 to 20 minutes
Duration of Action for Frusemide
Oral: 6 to 8hours
I.V.: 2 hours
Half Life of Frusemide
30 to 120 minutes
Side Effects of Frusemide
1. Dizziness
2. Headache
3. Diarrhoea
4. Anorexia
5. Nausea
6. Polyurea
7. Vomiting
8. Constipation
9. Frequent urination
10. Nocturea
11. Altered renal function tests
12. Weakness
13. Altered liver function tests
14. Dry mouth
15. Hypo calcaemia
16. Hypo kalaemia
17. Hypo natraemia
18. Transient deafness
19. Gastro intestinal disturbances
20. Visual impairment
21. Muscle cramps
22. Decreased tolerance to carbohydrates
23. Hyper uricaemia.
24. Electrolyte imbalance
25. Orthostatic hypotension
26. Aplastic anaemia
27. Agranulocytosis
28. Paraesthesia
29.Ototoxicity


Contra-indications of Frusemide
1. Hypo natraemia
2. Hypo kalaemia
3. Hypo volaemia
4. Hypotension
5. Hepatic coma
6. Hypersensitivity to the drug
7. Anuric renal failure

Special Precautions while taking Frusemide
1. Hepatic impairment
2. Renal impairment
3. Gout
4. Diabetes mellitus
5. Hypersensitivity to Sulfonamides
6. Fluid and electrolyte imbalance
7. Long term purgatives
8. Hepatic cirrhosis
9. Chronic Diarrhoea and dehydration.

Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Frusemide
1. Hypertension
2. Oedema associated with heart failure
3. Oedema due to renal and hepatic diseases
4. Acute pulmonary Oedema
5. Cerebral Oedema
6. Refractory Oedema
7. Hypercalcaemia
8. Oliguria
9. Forced diuresis in drug over dosage.
10. Vertigo

Interactions for Frusemide
Anticoagulants: Activity of anticoagulants may be enhanced.
Aminoglycoside antibiotics: Frusemide increases potential for ototoxicity.
Cisplatin: Frusemide increases potential for ototoxicity.
Digitalis glycosides: Diuretics induced potassium loss may precipitate digitalis toxicity, increased frequency of cardiac arrhythmias.
NSAIDs: Effect of frusemide reduced.
Lithium: Therapeutic and toxic effects of lithium increased.
Metolazone: Profound diuresis and greater than predicted electrolyte loss related to the ability of metolazone to block proximal tubular sodium reabsorption useful in patients refractory to frusemide.
Non-depolarizing muscle relaxants: Action of succinylcholine & tubocurarine potentiated by low doses reversed by high doses.
Food: Efficacy reduced when administered with food.
Propranolol: Plasma propranolol level may be increased.
Clofibrate: Increased diuretic responses.
Hydantoins: May decrease the diuretic effects.
Typical Dosage for Frusemide
Oral:
Oedema: 40mg in the morning. Increased if required; based on patient`s response up to 80mg.
Maintenance dosage: 20 to 40mg daily or on alternate days.
Maximum dose: 600mg/day.
Children: 3mg/kg/day.
I.V.:
Adult: 20 to 50mg as slow I.V. or I.M. injection. Increased by 20mg every 2hours. Higher I.V. doses must be infused
Children: 0.5 to 1.5mg/kg/day.
Maximum child dose: 20mg/day.
Oliguria: 250mg/day. Gradually increased; by 250mg at every 4 to 6 hours.
Maximum dose: 2gm
Hypertension: 40mg orally twice daily. Adjust the dosage according to patient`s response.
Hypercalcaemia: 120mg orally/day or 80 to 100mg I.V. every 1 to 2 hours
Acute pulmonary Oedema:
Adults: 40mg slow I.V. injection. Then 80mg within 1hour if required.
Children: 1mg/kg I.V.or I.M. Every 2 hours until desired response is gained.
Maximum dose: 6mg/kg/day.

Schedule of Frusemide
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Storage Requirements for Frusemide
Store at controlled room temperature at a range of 15 to 30 degree C. in a well closed container and protects from light.
Effects of Missed Dosage of Frusemide
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 Frusemide
Treatment is supportive and symptomatic. Monitor and support fluid and electrolyte balance by replacing fluids and electrolytes.

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