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موارد مصرف:

 درمان فشار خون

درمان نارسايي قلبي NYHA (New York Heart Association) Class II-IV

كاهش مرگ و مير قلبي عروقي در بيماران پايدار از نظر باليني و داراي اختلال عملكرد يا نارسايي بطن چپ ناشي از سكته قلبي 

نفروپاتي ديابتينارسايي قلبي دياستوليك  

نفروپاتي پروتئينوريك غير ديابتي

جلوگيري از فيبريلاسيون دهليزي راجعه

موارد مهمتر براي تجويز دارو:

والسارتان يك مهار كننده گيرنده آنژيوتانسين 2 مي باشد.

نحوه تجويز و مقدار مصرف:    

در افراد مسن، بيماران داراي اختلال عملكرد كليوي خفيف تا متوسط و بيماران داراي نارسايي كبدي خفيف تا متوسط نيازي به تنظيم دوز اوليه وجود ندارد.

در بيماران داراي نقص شديد عملكرد كبد يا كليه، به تنظيم دوز والسارتان بايد دقت شود.

اين دارو بدون غذا يا همراه با آن مي تواند مصرف شود.در بيماران داراي نارسايي قلبي، به كاهش دوز داروهاي ديورتيك مورد مصرف همزمان بايد دقت شود.

در هنگام تجويز پس از سكته قلبي، در صورت وقوع فشار خون پايين سمپتوماتيك يا نقص عملكرد كليوي، بايد به كاهش دادن دوز دارو توجه شود.

هشدار مصرف دربارداري:

بلافاصله هنگامي كه باردار بودن تشخيص داده شد، مصرف والسارتان بايد قطع شود، زيرا داروهايي كه مستقيما روي سيستم رنين-آنژيوتانسين اثر مي كنند، مي تواند باعث آسيب و حتي مرگ جنين در حال رشد شوند.

موارد منع مصرف:

هيچ مورد خاصي وجود ندارد.

هشدارها و احتياطات:

-         جنين و نوزاد نبايد در معرض اين دارو باشند

-         به علائم و نشانه هاي وقوع فشار خون پايين بايد توجه شود

-         در بيماران داراي نقص عملكرد كبدي يا كليوي بايد با احتياط مصرف شود.

عوارض ناخواسته و با شيوع بيشتر:

-         در تجويز براي درمان فشار خون: سردرد، سرگيجه، عفونت ويروسي، خستگي و درد شكم

-         در تجويز در نارسايي قلبي:  سرگيجه، فشار خون پايين، اسهال، درد مفاصل، درد پشت، خستگي و هايپركالمي

-         در تجويز پس از حمله قلبي: عوارض شايعتري كه باعث قطع درمان توسط بيمار مي شود شامل: فشار خون پايين، سرفه و افزايش كراتينين خون

تداخلات دارويي:

مدرهاي نگهدارنده پتاسيم، مكملهاي پتاسيمي يا نمكهاي جايگزين مي توانند باعث افزايش پتاسيم خون و در بيماران داراي نارسايي قلبي باعث افزايش كراتينين سرم شوند.

مصرف در جمعيتهاي خاص:

-         مادراني كه به نوزاد شير مي دهند: دادن شير مادر به نوزاد و يا مصرف دارو بايد قطع شود.

-         اطفال: فعلا اطلاعات در مورد اثربخشي و امنيت مصرف دارو شامل اطفال بين 6 تا 16 سال مي شود.

-         سالمندان: رويهم رفته تفاوتي در اثر بخشي و امنيت دارو در مقايسه با بيماران جوانتر وجود ندارد ولي نمي توان حساس بودن بيشتر بعضي از افراد سالمند را رد كرد.     

تاريخ بازنگري: نوامبر 2007

Generic Name: VALSARTAN

Category: Antihypertensive¹

Composition:  Each scored F.C. Tablet contains: Valsartan 80,160 mg

Actions and Pharmacokinetics:

Valsartan is a nonpeptide angiotensin II antagonist that selectively blocks the binding of angiotensin II to the AT 1 receptor in tissues such as vascular smooth muscle and the adrenal gland. Angiotensin II stimulates the adrenal cortex to synthesize and secrete aldosterone, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle.

Absorption: Absolute bioavailability for the capsule formulation is approximately 25% (range, 10 to 35%).Protein binding: Very high (95%), mainly to albumin. Half-life: approximately6 hours. Elimination: Approximately 6 hours. Renal: 13%, Fecal: 83%. ¹

Indications:

Hypertension: Valsartan is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.

Heart Failure: Valsartan is indicated for the treatment of heart failure (NYHA class II-IV).

Post-Myocardial Infarction: In clinically stable patients with left ventricular failure or left ventricular dysfunction following myocardial infarction, valsartan is indicated to reduce cardiovascular mortality.²

Contraindications:

Valsartan is contraindicated in patients who are hypersensitive to any component of this product.² and also in angioedema, lactating Mother, pregnancy. ³

Drug interactions:

As with other drugs that block angiotensin II or its effects, concomitant use of potassium sparing diuretics (e.g. spironolactone, triamterene, amiloride), potassium supplements, or salt substitutes containing potassium may lead to increases in serum potassium and in heart failure patients to increases in serum creatinine.²

Combinations containing following medications, depending on the amount present, may interact with this medication.

>> Diuretics (may have additive hypertensive effects).

>>Lithium salts (may reduce lithium clearance; monitor serum lithium levels).

>>Warfarin (may cause an increase (12%) in prothrombin time (PT); activated partial thromboplastin time is unaffected).¹

Warnings:

When pregnancy is detected, valsartan should be discontinued as soon as possible.

Excessive hypotension was rarely seen (0.1%) in patients with uncomplicated hypertension treated with valsartan alone. In patients with an activated renin-angiotensin system, such as volume- and/or salt-depleted patients receiving high doses of diuretics, symptomatic hypotension may occur. This condition should be corrected prior to administration of valsartan, or the treatment should start under close medical supervision.

Caution should be observed when initiating therapy in patients with heart failure or post-myocardial infarction patients. Patients with heart failure or post-myocardial infarction patients given valsartan commonly have some reduction in blood pressure, but discontinuation of therapy because of continuing symptomatic hypotension usually is not necessary when dosing instructions are followed.²

Precautions:

The pharmacokinetics of valsartan have not been investigated in patients <18 years of age.²

Impaired Hepatic Function: As the majority of valsartan is eliminated in the bile, patients with mild-to-moderate hepatic impairment, including patients with biliary obstructive disorders, showed lower valsartan clearance (higher AUCs). Care should be exercised in administering valsartan to these patients.

Impaired Renal Function: In studies of ACE inhibitors in hypertensive patients with unilateral or bilateral renal artery stenosis, increases in serum creatinine or blood urea nitrogen have been reported. In a 4-day trial of valsartan in 12 hypertensive patients with unilateral renal artery stenosis, no significant increases in serum creatinine or blood urea nitrogen were observed. There has been no long-term use of valsartan in patients with unilateral or bilateral renal artery stenosis, but an effect similar to that seen with ACE inhibitors should be anticipated.

      As a consequence of inhibiting the renin-angiotensin-aldosterone system, changes in renal function may be anticipated in susceptible individuals. In patients with severe heart failure whose renal function may depend on the activity of the renin-angiotensin-aldosterone system, treatment with angiotensin-converting enzyme inhibitors and angiotensin receptor antagonists has been associated with oliguria and/or progressive azotemia and (rarely) with acute renal failure and/or death. Similar outcomes have been reported with valsartan.

      Some patients with heart failure have developed increases in blood urea nitrogen, serum creatinine, and potassium. These effects are usually minor and transient, and they are more likely to occur in patients with pre-existing renal impairment. Dosage reduction and/or discontinuation of the diuretic and/or valsartan may be required. In the Valsartan Heart Failure Trial, in which 93% of patients were on concomitant ACE inhibitors, treatment was discontinued for elevations in creatinine or potassium (total of 1.0% on valsartan vs. 0.2% on placebo). In the Valsartan in Acute Myocardial Infarction Trial (VALIANT), discontinuations due to various types of renal dysfunction occurred in 1.1% of valsartan-treated patients and 0.8% of captopril-treated patients. Evaluation of patients with heart failure or post-myocardial infarction should always include assessment of renal function.²

Pregnancy:

When used in pregnancy, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, valsartan should be discontinued as soon as possible.²

Breast-Feeding:

It is not known whether valsartan is excreted in human milk. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.²

Adverse Effects:

Those indicating need for medical attention: Incidence rare: Angioedema (sudden trouble in swallowing or breathing;   swelling of face, mouth, hands, or feet;   hoarseness); hypotension (dizziness, lightheadedness, or fainting; neutropenia.

Those indicating need for medical attention only if they continue or are bothersome: Incidence less frequent Abdominal pain; arthralgia (pain, swelling, or redness in joints;   muscle pain or stiffness; difficulty in moving); back pain; coughing; diarrhea; dizziness; fatigue  ; headache; upper respiratory tract infection; viral infection.¹

Other less frequent or rare adverse effects: Nausea, Renal Disease, Abnormal Hepatic Function Tests, Blurred Vision, Fainting, Hyperkalemia, Rhabdomyolysis, Vertigo. ³

Administration and Dosage:

Hypertension: The recommended starting dose of valsartan is 80 mg or 160 mg once daily when used as monotherapy in patients who are not volume-depleted. Patients requiring greater reductions may be started at the higher dose. valsartan may be used over a dose range of 80 mg to 320 mg daily, administered once a day. The antihypertensive effect is substantially present within 2 weeks and maximal reduction is generally attained after 4 weeks. If additional antihypertensive effect is required over the starting dose range, the dose may be increased to a maximum of 320 mg or a diuretic may be added. Addition of a diuretic has a greater effect than dose increases beyond 80 mg. Care should be exercised with dosing of valsartan in patients with hepatic or severe renal impairment.

Valsartan may be administered with or without food and with other antihypertensive agents.

Heart Failure: The recommended starting dose of valsartan is 40 mg twice daily. Uptitration to 80 mg and 160 mg twice daily should be done to the highest dose, as tolerated by the patient. Consideration should be given to reducing the dose of concomitant diuretics. The maximum daily dose administered in clinical trials is 320 mg in divided doses.

Post-Myocardial Infarction: Valsartan may be initiated as early as 12 hours after a myocardial infarction. The recommended starting dose of valsartan is 20 mg twice daily. Patients may be uptitrated within 7 days to 40 mg twice daily, with subsequent titrations to a target maintenance dose of 160 mg twice daily, as tolerated by the patient. If symptomatic hypotension or renal dysfunction occurs, consideration should be given to a dosage reduction. Valsartan may be given with other standard post-myocardial infarction treatment, including thrombolytics, aspirin, beta-blockers, and statins. ²

Storage: Store in 30°C.² Protect from moisture and heat. Store in tight container.¹

How Supplied: Box of 5 blisters of 20 scored F.C. tablets.

References:

1-       USP DI 2005

2-       FDA Approval Labeling for Valsartan. Revised: 09/2006

3-       Medscape

4-       Novartis Pharmaceuticals Corporation. Diovan (Valsartan) safety information. 2007