Thursday, July 25, 2013


Nifedipine is a dihydropyridine calcium channel blocker. Its main uses are as an antianginal (especially in Prinzmetal's angina) and antihypertensive, although a large number of other indications have recently been found for this agent, such as Raynaud's phenomenon, premature labor, and painful spasms of the esophagus such as in cancer and tetanus patients. It is also commonly used for the small subset of pulmonary hypertension patients whose symptoms respond to calcium channel blockers.

3,5-dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate


The recommended starting dose for immediate-release nifedipine capsules is 10 mg, taken 3 times daily. With the extended-release version, the recommended starting nifedipine dosage is 30 to 60 mg, taken once daily. Nifedipine rapidly lowers blood pressure, and patients are commonly warned they may feel dizzy or faint after taking the first few doses. Tachycardia (fast heart rate) may occur as a reaction. These problems are much less frequent in the sustained-release preparations of nifedipine (such as Adalat OROS). A more novel release system is GITS (Gastro-Intestinal Therapeutic System), which - according to Bayer - provides 24-hour continuous release through an osmotic push system. Recent trials with GITS include INSIGHT (for blood pressure) and ACTION (for angina).
Extended release formulations of nifedipine should be taken on an empty stomach, and patients are warned not to consume anything containing grapefruit or grapefruit juice, as they raise blood nifedipine levels. There are several possible mechanisms, including the lowering of CYP3A4 activity.

The approved uses for are the long-term treatment of hypertension (high blood pressure) and angina pectoris. In hypertension, recent clinical guidelines generally favour diuretics and ACE inhibitors, although calcium channel antagonists, along with thiazide diuretics, are still favoured as primary treatment for over 55's and black patients.
Sublingual nifedipine has previously been used in hypertensive emergencies. This was found to be dangerous, and has been abandoned. Sublingual nifedipine causes blood-pressure lowering through peripheral vasodilation. It can cause an uncontrollable decrease in blood pressure, reflex tachycardia, and a steal phenomenon in certain vascular beds. There have been multiple reports in the medical literature of serious adverse effects with sublingual nifedipine, including cerebral ischemia/infarction, myocardial infarction, complete heart block, and death. As a result of this, the FDA reviewed all data regarding the safety and efficacy of sublingual nifedipine for hypertensive emergencies in 1995, and concluded that the practice should be abandoned because it was neither safe nor efficacious. An exception to the avoidance of this practice is in the use of nifedipine in the treatment of hypertension associated with autonomic dysreflexia in spinal cord injury.

A number of persons have developed toxicity due to acute overdosage with nifedipine, either accidentally or intentionally, and via either oral or parenteral administration. The adverse effects include lethargy, bradycardia, marked hypotension and loss of consciousness. The drug may be quantitated in blood or plasma to confirm a diagnosis of poisoning in hospitalized patients or to assist in a medicolegal death investigation. Analytical methods usually involve gas or liquid chromatography and specimen concentrations are usually in the 100-1000 μg/L range.


ADALAT ORS CAP                               BAYER
ANGIBLOCK CAP                                 ALKEM
CALBLOC                                            UNISERCH
CALCIGARD                              TORRENT
CARDULES CAP                        NICHOLAS
DEPICOR CAP                            MERCK
DEPICOR SR CAP                       MERCK
DEPIN CAP                                 Zydus cadila
NICARDIA CAP                            J.B.Chemichels
Nicardia retard                           ,,
NEFEDINE TAB                            Nicolas piramal
Nifelat cap                                   Cipla
Niferil tab                                     usv

Tuesday, July 23, 2013


Nebivolol is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and, in Europe, also for left ventricular failure. It is highly cardioselective under certain circumstances
Nebivolol slows down the activity of your heart by stopping messages sent by some nerves to your heart. It does this by blocking tiny areas (called beta-adrenergic receptors) where the messages are received by your heart. Nebivolol also relaxes (widens) some blood vessels. These two things together allow the pressure of blood within your blood vessels to be reduced and make it easier for your heart to pump blood around your body. This is of benefit in hypertension (where your blood pressure is too high), and in heart failure (which is a condition where the pumping action of your heart is reduced).
In the US, Nebivolol (nebivolol systemic) is a member of the drug class cardioselective beta blockers and is used to treat High Blood Pressure and Mitral Valve Prolapse.


Beta blockers help patients with cardiovascular disease by blocking β receptors, while many of the side-effects of these medications are caused by their blockade of β2 receptors. For this reason, beta blockers that selectively block β1 receptors (termed cardioselective or β1-selective beta blockers) produce fewer adverse effects (for instance, bronchoconstriction) than those drugs that non-selectively block both β1 and β2 receptors. Nebilovol has been marketed by Cipla Ltd under brand name Nebicip; by Forest Laboratories under the name Bystolic; by Micro Labs under the brand name Nebilong; ; and by Menarini under the names Hypoloc, Lobivon, Nebilet, Nebilox, Nobiten, and Temerit. In a laboratory experiment conducted on biopsied heart tissue, nebivolol proved to be the most β1-selective of the β-blockers tested, being approximately 3.5 times more β1-selective than bisoprolol. However, the drug's receptor selectivity in humans is more complex and depends on the drug dose and the genetic profile of the patient taking the medication. The drug is highly cardioselective at 5 mg. However, at doses above 10 mg, nebivolol loses its cardioselectivity and blocks both β1 and β2 receptors. (While the recommended starting dose of nebivolol is 5 mg, sufficient control of blood pressure may require doses up to 40 mg). Furthermore, nebivolol is also not cardioselective when taken by patients with a genetic makeup that makes them "poor metabolizers" of nebivolol (and other drugs) or with CYP2D6 inhibitors. As many as 1 in 10 Whites and even more Blacks are poor CYP2D6 metabolizers and therefore might benefit less from nebivolol's cardioselectivity although currently there are no directly comparable studies

Before taking nebivolol
Some medicines are not suitable for people with certain conditions, and sometimes a medicine may only be used if extra care is taken. For these reasons, before you start taking nebivolol it is important that your doctor or pharmacist knows:

If you are pregnant, trying for a baby or breast-feeding.
If you have liver or kidney problems.
If you have low blood pressure or poor circulation.
If you have asthma or breathing difficulties.
If you have diabetes.
If you have psoriasis (a skin problem).
If you have myasthenia gravis (a condition causing muscle weakness).
If you have been told you have a slow heartbeat or heart block (a slow and irregular heartbeat).
If you have been told you have Prinzmetal's angina (chest pain caused by spasms of the heart's blood vessels).
If you have phaeochromocytoma (a tumour on your adrenal gland).
If you are taking other medicines, including those available to buy without a prescription, herbal and complementary medicines.
If you have ever had an allergic reaction to a medicine, or if you have ever had any other severe allergic reaction.


ASIVOL        -           AS PHARMA
BIPINOR            -    ACI  (Bangladesh)
BYSTOLIC          -    Forest (United States)
EBIVOL              -    Actavis Group (Poland)
ENDOLOL          -     Heto       India
EZOCEM            -    OZONE Laboratories        -   Poland, Romania
LOVISPES        -      Specifar SA           Slovenia, Teva, Poland
NEBEST           -    USV               -    India
Nebeta                Abdi Ibrahim, Georgia
Nebicard        Biofarm, Poland;         Hexal, Latvia;        Sandoz, Lithuania;      Torrent, India;     Torrent  -      Vietnam
Nebicard-H             (Nebivolol and Hydrochlorothiazide)           Torrent   -    India
Nebicard-SM       (Nebivolol and Levamlodipine)        Torrent  -  India
Nebicard-V      (Nebivolol and Valsartan)       Torrent  -   India
Nebilet        Adcock Ingram Pharmaceuticals -  South Africa;          Berlin-Chemie  -   Georgia;                Berlin-Chemie -  Tunisia;            Biotoscana -  Peru;                  Menarini -  Costa Rica;                         Menarini  -  Dominican Republic;                      Menarini  -    Honduras;              Menarini  -  Nicaragua;   Menarini  -   Panama;       Menarini  -   El Salvador;                 Menarini Laboratorios  -   Guatemala
Nebilet Plus     (Nebivolol and Hydrochlorothiazide (pediatric))       Berlin-Chemie  -   Georgia
Nebilong       Micro Carsyon  - India
Nebilong-H    (Nebivolol and Hydrochlorothiazide)         Micro Carsyon  -  India
Nebimac      -   Macleods  -   India
Nebimac-H    (Nebivolol and Hydrochlorothiazide)       Macleods  -   India
Nebinad        Farma-Projekt   -  Poland
Nebinex         Glenmark   -  India
Nebinex-AM     (Nebivolol and Amlodipine)         Glenmark  -   India
Nebinorm      Medicament  -   Romania
Nebipil           Alkem  -  India
Nebipril-SA   (Nebivolol and Levamlodipine)      Alkem   -   India
Nebispes      Galex  -   Poland;                Galex  -   Slovenia;        Nycomed  -   Latvia;        Pharmanova -Serbia
Nebistar                Lupin  -  India
Nebistar-SA        (Nebivolol and Levamlodipine)          Lupin  -  India
Nebiten       Anthus  -  India
Nebiten-H     (Nebivolol and Hydrochlorothiazide)               Anthus  -   India
NebivoLek            Sandoz  -    Poland
Nebivolol Actavis         Actavis  -   Romania
Nebivolol AL            Aliud   -  Germany
Nebivolol EG       Eurogenerics  -   Luxembourg
Nebivolol Hexal           1A Pharma  -   Poland;       Hexal  -   Luxembourg
Nebivolol Mylan        Generics  -  Slovenia
Nebivolol Pliva          Pliva   -  Poland
Nebivolol Teva            Teva   -  Romania
Nebivor           Orion  -   Poland
Neblotensol           Gerot-Lannach  -  Romania
Nedal     Polfa Warszawa  -   Poland
Nemirostad         STADA     Lithuania
Nemont        Norameda  - Lithuania
Nerose         Norameda  -  Lithuania
Nevol            Medley  -   India
Nevol-H(Nebivolol and Hydrochlorothiazide)          Medley  -   India
Niavas         Ranbaxy   -   India
Niavas-D(Nebivolol and Hydrochlorothiazide)                     Ranbaxy  -   India
Nobiten           Menarini   -   Luxembourg
Nobizide(Nebivolol and Hydrochlorothiazide)      Menarini International-L      -    Italy
Nolet                 Antibiotice    -   Romania
Nonblon             Aversi     -  Georgia
Nonblon H   (Nebivolol and Hydrochlorothiazide)          Aversi  -   Georgia
Nubeta         Abbott  -   India
Nubeta-H      (Nebivolol and Hydrochlorothiazide)       Abbott  -   India
Nubeta-SM       (Nebivolol and Levamlodipine)     Abbott   -   India
X-Pressol          Labormed Pharma  Romania
Zenebi         FDC    India
Zinebi        FDC  -   India
Anfibol      Drugtech   Chile
Betalol       East West   India
Betalol-H     (Nebivolol and Hydrochlorothiazide)         East West  -   India
Bivol       Specifar  -  Greece
Bravylol      -   Tchaikapharma  -  Bulgaria
Conébilox       (Nebivolol and Hydrochlorothiazide)         Negma  -  France
Ezocem    S.C. Labormed Pharma   -   Czech Republic
Hypoloc      Berlin-Chemie   -   Germany;             Menarini  -   Austria;                   Menarini -  Denmark;   Menarini   -  Finland;                  Menarini    -   Greece;             Menarini  -   Luxembourg;                  Menarini   -      Netherlands
Lobibeta       Alet Pharmaceuticals   -   Greece
Lobivon Plus    (Nebivolol and Hydrochlorothiazide)           Menarini  -  Spain   
Lobivon       Berlin-Chemie   -  Germany;              Menarini  -  Spain;                Menarini     -   Greece; Menarini   -   Italy;                   Menarini    Netherlands
Nabila       Tecnofarma  -  Chile
Nebalex      Specifar   -   Bulgaria
Nebest-H      (Nebivolol and Hydrochlorothiazide)       USV  -   India
Nebicar           OEP Phils   -   Philippines
Nebicard       Medicamenta  -   Bulgaria;       Sandoz-  Estonia;        Torrent  -   Myanmar;                    Torrent  -  Philippines
Nebicor        Adipharm -  Bulgaria
Nebicur        Kleva     Greece
Nebilan      G.L. Pharma  -   Bulgaria;                 Lannacher  -   Austria
Nebilet plus  (Nebivolol and Hydrochlorothiazide)     Menarini  -   Lithuania;    Menarini  -  Latvia;    Menarini  -   Malta
A. Menarini  -   United Kingdom;     Berlin Chemie  -   Bosnia & Herzegowina;        Berlin-Chemie, Bulgaria;     Berlin-Chemie, Czech Republic;             Berlin-Chemie -  Germany;            Berlin-Chemie  -   Croatia (Hrvatska);    Berlin-Chemie  - Hungary;              Berlin-Chemie -  Poland;                Berlin-Chemie, Romania;         Berlin-Chemie, Serbia;          Berlin-Chemie   -   Slovakia;                   Biotoscana, Colombia; CSL, Australia; ITF – Labomed   Chile;       Leti  -   Venezuela;      Menarini, Argentina; Menarini, Switzerland; Menarini, Estonia; Menarini  -  Ireland;       Menarini  -  Lithuania;      Menarini  -   Latvia;      Menarini  -  Malta;       Menarini  -   Netherlands; Menarini, Portugal; Menarini, Singapore; Menarini, Slovenia;      Menarini, Thailand
Nebilet Plus (Nebivolol and Hydrochlorothiazide)        Berlin-Chemie, Bulgaria; Menarini, Estonia
Nebilet plus(Nebivolol and Hydrochlorothiazide)          Menarini, Switzerland
Nebiloc      Menarini, Netherlands
Nebilostad      STADA, Netherlands
Nebilox       Berlin-Chemie, Germany; GlaxoSmithKline, Italy
Nébilox       Negma, France
Nebinorm          Glenmark, Lithuania; Medicamenta, Czech Republic
Nebiphar          Teva, Estonia; Teva, Lithuania; Teva, Latvia
Nebirod        Sopharma, Bulgaria
Nebisam     Specifar, Lithuania; Specifar, Latvia
Nebiscal              +pharma, Czech Republic
Nebiscop        Specifar, Estonia; Specifar, Lithuania; Specifar, Latvia
Nebispes        Galex, Czech Republic; Nycomed, Lithuania; Specifar, Estonia
Nebiten                  G.L. Pharma, Estonia; G.L. Pharma, Lithuania; Lannacher Heilmittel, Latvia
Nebitrix      Glenmark, Bulgaria; Glenmark, Czech Republic
Nebivolol - 1 A Pharma               1A Pharma, Germany
Nebivolol +pharma                    +pharma, Czech Republic
Nebivolol 1A Pharma        1A Pharma, Estonia; 1A Pharma, Lithuania
Nebivolol AAA                     AAA-Pharma, Germany
Nebivolol AbZ        AbZ-Pharma, Germany
Nebivolol Actavis       Actavis, Switzerland; Actavis, Bulgaria; Actavis, Estonia; Actavis, United Kingdom; Actavis, Lithuania; Actavis, Latvia; Actavis, Malta; Actavis, Netherlands
Nébivolol Actavis      Actavis, France
Nebivolol Apotex       Apotex, Spain; Apotex Europe, Netherlands
Nébivolol Arrow        Arrow, France
Nebivolol Axapharm      Axapharm, Switzerland
Nébivolol Biogaran    Biogaran, France
Nebivolol CF       Centrafarm, Netherlands
Nebivolol Cinfa         Cinfa, Spain
Nébivolol CristerS     CristerS, France
Nebivolol Dival       Dival Classics, Netherlands
Nebivolol Edigen       Germed, Spain
Nébivolol EG     EG Labo, France
Nébivolol Evolugen       Evolupharm, France
Nebivolol G.L.         G.L. Pharma, Austria
Nebivolol Generis       Generis, Portugal
Nebivolol Glenmark       Glenmark, Netherlands
Nebivolol Heumann        Heumann, Germany
Nebivolol HEXAL          Hexal, Germany
Nébivolol Isomed           Teva Santé, France
Nebivolol Labesfal                     Labesfal, Portugal
Nebivolol Mylan                  Mylan, Spain; Mylan, Netherlands
Nébivolol Mylan                   Mylan, France
Nebivolol Normon              Normon, Spain
Nebivolol Orion                  Orion, Estonia; Orion, Lithuania; Orion, Latvia
Nebivolol PCH         Pharmachemie, Netherlands
Nebivolol Pensa                Pensa Pharma, Spain
Nebivolol Pliva      Pliva, Croatia (Hrvatska); Pliva, Hungary
Nebivolol Portfarma         Portfarma, Estonia; Portfarma, Lithuania; Portfarma, Latvia
Nébivolol Qualimed           Qualimed, France
Nébivolol Ranbaxy             Ranbaxy, France
Nebivolol Ratio                      Ratiopharm, Spain
Nebivolol Ratiopharm               Ratiopharm, Spain
Nébivolol Ratiopharm               Ratiopharm, France
Nebivolol Sandoz           Sandoz, Bulgaria; Sandoz, Switzerland; Sandoz, Czech Republic; Sandoz, Germany; Sandoz, United Kingdom; Sandoz, Netherlands; Sandoz Farmaceutica, Spain
Nébivolol Sandoz            Sandoz, France
Nebivolol Spirig                Spirig HealthCare, Switzerland
Nebivolol STADA                       STADA, Germany
Nebivolol Streuli                      Streuli Pharma, Switzerland
Nebivolol Teva             Teva, Bulgaria
Nébivolol Teva              Teva Santé, France
Nebivolol Tevagen                       Teva, Spain
Nebivolol Torrent                  Torrent Pharma, Lithuania
Nebivolol Winthrop                Winthrop Pharmaceuticals, United Kingdom
Nébivolol Winthrop                 Sanofi-Aventis, France
Nebivolol Zentiva                   Sanofi Aventis, Spain
Nébivolol Zydus                    Zydus, France
Nebivolol/Alapis Bulgaria            Alapis, Bulgaria
Nebivolol-1A Pharma                        1A Pharma, Latvia
Nebivolol-Acino                      Acino, Germany
Nebivolol-aconitum             Aconitum, Lithuania
Nebivolol-Actavis             Actavis, Germany
Nebivolol-CT                      CT Arzneimittel, Germany
Nebivolol-Mepha          Mepha, Switzerland
Nebivololo Actavis         Actavis Italy, Italy
Nebivololo Alter              Alter, Italy
Nebivololo Angenerico                  Angenerico, Italy
Nebivololo Doc Generici         DOC Generici, Italy
Nebivololo Dr Reddy's             Dr Reddy's, Italy
Nebivololo EG               EG, Italy
Nebivololo Mylan                Mylan, Italy
Nebivololo Pensa                 Pensa Pharma, Italy
Nebivololo Ranbaxy          Ranbaxy Italia, Italy
Nebivololo Ratiopharm        Ratiopharm Italia, Italy
Nebivololo Sandoz                 Sandoz, Italy
Nebivololo Teva                     Teva Italia, Italy
Nebivololo Winthrop             Winthrop Ph.Italia, Italy
Nebivolol-ratiopharm             Merckle, Bulgaria;              Merckle, Estonia;           Ratiopharm, Germany; Ratiopharm, Latvia
Nebivolol-Tchaikapharma          Tchaikapharma, Bulgaria
Nebivolol-Teva                         Teva, Germany;           Teva, Estonia;       Teva, Lithuania;          Teva, Latvia; Teva Pharma, Switzerland
Nebizita                       Specifar, Bulgaria
Nemirostad                STADA, Estonia; STADA, Latvia
Nexivol                       Abdi Ibrahim, Turkey
Nibel                        Belupo, Croatia (Hrvatska)
Nobiten                  Menarini, Belgium
Nomexor               Menarini, Austria
Nomexor plus HCT(Nebivolol and Hydrochlorothiazide)     Menarini, Austria
Noviblock     Medicamerc, Greece
Pertium       Saval, Chile
Silostar Plus(Nebivolol and Hydrochlorothiazide)          Uriach-Aquilea, Spain
Silostar                     Uriach-Aquilea, Spain
Temerit                    Menarini, France
TemeritDuo(Nebivolol and Hydrochlorothiazide)        Menarini, France
Vasoxen          I.E. Ulagay, Turkey
Volone             Farmal, Croatia (Hrvatska)

Monday, July 15, 2013


Metoprolol is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension. The active substance metoprolol is employed either as metoprolol succinate or metoprolol tartrate . The tartrate is an immediate-release and the succinate is an extended-release formulation.
Metoprolol is used to treat angina (chest pain) and hypertension (high blood pressure). It is also used to treat or prevent heart attack.

Hypertension,angina(chest pain),acute myocardial infarction,supraventricular tachycardia,ventricular tachycardia,congestive heart failure and for prevention of migrain headaches
Treatment of heart failure.
Vasovagal syncope
Adjunct in treatment of hyperthyroidism
Long QT syndrome, especially for patients with asthma, as metoprolol's β1 selectivity tends to interfere less with asthma drugs which are often β2-adrenergic receptor-agonist drugs
Due to its selectivity in blocking the beta1 receptors in the heart, metoprolol is also prescribed for off-label use in performance anxiety, social anxiety disorder, and other anxiety disorders.

Important information about metoprolol
You should not use metoprolol if you have a serious heart problem (heart block, sick sinus syndrome, slow heart rate), severe circulation problems, severe heart failure, or a history of slow heart beats that caused fainting.
Before taking metoprolol
You should not use this medication if you are allergic to metoprolol, or other beta-blockers (atenolol, carvedilol, labetalol, nadolol, nebivolol, propranolol, sotalol, and others), or if you have:
a serious heart problem such as heart block, sick sinus syndrome, or slow heart rate;
severe circulation problems;
severe heart failure (that required you to be in the hospital); or
history of slow heart beats that have caused you to faint.
To make sure metoprolol is safe for you, tell your doctor if you have:
asthma, chronic obstructive pulmonary disease (COPD), sleep apnea, or other breathing disorder;
diabetes (taking metoprolol may make it harder for you to tell when you have low blood sugar);
liver disease;
congestive heart failure;
problems with circulation (such as Raynaud's syndrome);
a thyroid disorder; or
pheochromocytoma (tumor of the adrenal gland).
FDA pregnancy category C. It is not known whether metoprolol will harm an unborn baby. Tell your doctor right away if you become pregnant while using this medication.

Metoprolol can pass into breast milk and may harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Do not give this medication to anyone under 18 years old without medical advice.

What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.
What should I avoid while taking metoprolol?
Metoprolol may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.
Drinking alcohol can increase certain side effects of metoprolol.

Metoprolol side effects
Get emergency medical help if you have any of these signs of an allergic reaction to metoprolol: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Call your doctor at once if you have:
very slow heartbeats;
a light-headed feeling, like you might pass out;
shortness of breath (even with mild exertion), swelling, rapid weight gain; or
cold feeling in your hands and feet.
Common metoprolol side effects may include:
dizziness, tired feeling;
confusion, memory problems;
nightmares, trouble sleeping;
diarrhea; or
mild itching or rash.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Metoprolol Dosing Information
Usual Adult Dose of Metoprolol for Angina Pectoris Prophylaxis:
Initial dose: 100 mg orally in 1 or 2 divided doses.
Maintenance dose: 100 to 450 mg/day.
Extended release may be used at the same total daily dose given once a day.

Usual Adult Dose for Hypertension:

Initial dose: 100 mg orally in 1 or 2 divided doses.
Maintenance dose: 100 to 450 mg/day.
Extended release may be used at the same total daily dose given once a day.

Usual Adult Dose for Supraventricular Tachycardia:
Initial dose: 100 mg orally in 1 or 2 divided doses.
Maintenance dose: 100 to 450 mg/day.
Extended release may be used at the same total daily dose given once a day.

Usual Adult Dose of Metoprolol for Angina Pectoris:
Initial dose: 100 mg orally in 1 or 2 divided doses.
Maintenance dose: 100 to 400 mg/day.
Extended release may be used at the same total daily dose given once a day.

Usual Adult Dose for Myocardial Infarction:
Early treatment:
IV: 3 bolus injections of 5 mg given at 2 minute intervals.
Oral: In patients who tolerate the full IV dose (15 mg), metoprolol tablets, 50 mg every 6 hours, should be initiated 15 minutes after the last IV dose and continued for 48 hours. Maintenance dose: 100 mg orally twice a day.
Patients who appear not to tolerate the full IV dose should be started on metoprolol tablets at 25 mg or 50 mg every 6 hours 15 minutes after the last intravenous dose or as soon as their clinical condition allows.

Late treatment:
Oral: 100 mg orally twice a day.
Patients with contraindications to treatment during the early phase of suspected or definite myocardial infarction, patients who appear not to tolerate the full early treatment, and patients in whom the physician wishes to delay therapy for any other reason should be started on metoprolol tablets as soon as their clinical condition allows.

Usual Adult Dose for Congestive Heart Failure:
Initial dose: 25 mg once daily (of the XL formulation) for two weeks in patients with NYHA class II heart failure and 12.5 mg once daily (of the XL formulation) in patients with more severe heart failure.
Maintenance dose: This dosage should then be doubled every two weeks to the highest dosage level tolerated or up to 200 mg.
If transient worsening of heart failure occurs, it may be treated with increased doses of diuretics, and it may also be necessary to lower the dose or temporarily discontinue treatment. The dose should not be increased until symptoms of worsening heart failure stabilize.
Initial difficulty with titration should not preclude later attempts to institute therapy. If heart failure patients experience symptomatic bradycardia, the dose should be reduced.

Usual Pediatric Dose of Metoprolol for Hypertension:
Immediate release:
1 to 17 years:
Initial dose: 1 to 2 mg/kg/day, administered in 2 divided doses. Dosage should be adjusted based on patient response.
Maximum dose: 6 mg/kg/day (less than or equal to 200 mg/day)

Extended release:
6 to 16 years:
Initial dose: 1 mg/kg orally once daily (not to exceed 50 mg once daily). The minimum available dose is one half of the 25 mg tablet.
Maintenance dose: Dosage should be adjusted according to blood pressure response. Doses above 2 mg/kg (or in excess of 200 mg) once daily have not been studied.

What other drugs will affect metoprolol?
Tell your doctor about all medicines you use, and those you start or stop using during your treatment with metoprolol, especially:
an antidepressant--bupropion, clomipramine, desipramine, duloxetine, fluoxetine, fluvoxamine, paroxetine, sertraline;
an ergot medicine--dihydroergotamine, ergonovine, ergotamine, methylergonovine;
heart or blood pressure medications--amlodipine, clonidine, digoxin, diltiazem, dipyridamole, hydralazine, methyldopa, nifedipine, quinidine, reserpine, verapamil, and others;
an MAO inhibitor--isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, tranylcypromine; or
medicine to treat mental illness--chlorpromazine, fluphenazine haloperidol, thioridazine.
This list is not complete. Other drugs may interact with metoprolol, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.



Sunday, July 14, 2013


Metolazone is a thiazide-like diuretic marketed under the brand names Zytanix from Zydus Cadila, Zaroxolyn, and Mykrox. It is primarily used to treat congestive heart failure and high blood pressure. Metolazone indirectly decreases the amount of water reabsorbed into the bloodstream by the kidney, so that blood volume decreases and urine volume increases. This lowers blood pressure and prevents excess fluid accumulation in heart failure. Metolazone is sometimes used together with loop diuretics such as furosemide or bumetanide, but these highly effective combinations can lead to dehydration and electrolyte abnormalities.


One of the primary uses of metolazone is for treating oedema (fluid retention) associated with congestive heart failure (CHF). In mild heart failure, metolazone or another diuretic may be used alone, or combined with other diuretics for moderate or severe heart failure. In addition to preventing fluid buildup, the use of metolazone may allow the patient to relax the amount of sodium restriction that is required. Although most thiazide diuretics lose their effectiveness in renal failure, metolazone remains active even when the glomerular filtration rate (GFR) is below 30–40 mL/min (moderate renal failure). This gives it a considerable advantage over other thiazide diuretics, since renal and heart failure often coexist and contribute to fluid retention.
Metolazone may also be used in renal (kidney) disease, such as chronic renal failure or the nephrotic syndrome. Chronic renal failure causes excess fluid retention that is often treated with diet adjustments and diuretics Metolazone may be combined with other diuretics (typically loop diuretics) to treat diuretic resistance in CHF, chronic renal failure, and nephrotic syndrome. Metolazone and a loop diuretic will synergistically enhance diuresis over the use of either agent alone. Using this combination, diuretic effects will occur at two different segments of the nephron; namely, the loop diuretic will act at the loop of Henle, and metolazone will act at the distal convoluted tubule. Metolazone is frequently prescribed in addition to the loop diuretic. Metolazone may be used for edema caused by liver cirrhosis as well.
The other major use of metolazone is in treating hypertension (high blood pressure). Thiazide diuretics, though usually not metolazone, are very often used alone as first-line treatment for mild hypertension. They are also used in combination with other drugs for difficult-to-treat or more severe hypertension. "The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure" (JNC 7) recommends thiazide diuretics as the initial medication for treatment of hypertension. Hydrochlorothiazide is by far the most commonly used, as it is both better-studied and cheaper (about four times) than metolazone, although as mentioned above metolazone is used in patients with moderate renal failure.

The primary target of all thiazide diuretics, including metolazone, is the distal convoluted tubule, part of the nephron in the kidney, where they inhibit the sodium-chloride symporter.
In the kidney, blood is filtered into the lumen, or open space, of the nephron tubule. Whatever remains in the tubule will travel to the bladder as urine and eventually be excreted. The cells lining the tubule modify the fluid inside, absorbing some material and excreting others. One side of the cell (the apical side) faces the lumen; the opposite side (the basolateral side) faces the interstitial space near blood vessels. The other sides are tightly joined to neighboring cells.
As with other regions, tubule cells in the distal convoluted tubule possess the ATP-powered sodium-potassium antiporter (Na+/K+-ATPase), which uses energy from ATP to transfer three sodium ions out from the basolateral surface (toward blood vessels) while simultaneously transferring two potassium ions in. The distal convoluted tubule cells also possess a sodium-chloride symporter on the apical side, which passively allows one sodium ion and one chloride ion to diffuse together in from the lumen (where urine is forming) into the cell interior. As sodium is pumped out of the cell by the ATPase, its intracellular concentration falls, and additional sodium begins to diffuse in from the tubule lumen as replacement. The symporter requires chloride to be transported in as well. Water passively follows to maintain isotonicity; excess chloride and potassium passively diffuse out the cell through basolateral channels into the interstitial space, and water accompanies them. The water and chloride, as well as the sodium pumped out by the ATPase, will be absorbed into the bloodstream.
Metolazone and the other thiazide diuretics inhibit the function of the sodium-chloride symporter, preventing sodium and chloride, and therefore water too, from leaving the lumen to enter the tubule cell. As a result, water remains in the lumen and is excreted as urine, instead of being reabsorbed into the bloodstream. Since most of the sodium in the lumen has already been reabsorbed by the time the filtrate reaches the distal convoluted tubule, thiazide diuretics have limited effects on water balance and on electrolyte levels. Nevertheless, they can be associated with low sodium levels, volume depletion, and low blood pressure, among other adverse effects.


 Diurem  CIPLA
MELA    RPG Lifescience
MEMTOZ - CENTAUR Laboratories
METORAL   -  Dr Reddy Laboratories
METOZ    -  CENTAUR Pharmaceuticals
ZYTANIX  -  Zydus cadila
METOLACTONE  - Centaur Pharmaceuticals


Methyldopa (L-α-Methyl-3,4-dihydroxyphenylalanine; Aldomet, Aldoril, Dopamet, Dopegyt, etc.) is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive. Its use is now mostly deprecated following the introduction of alternative safer classes of agents. However, it continues to have a role in otherwise difficult to treat hypertension and gestational hypertension (also known as pregnancy-induced hypertension (PIH)).

Methyldopa is used in the clinical treatment of the following disorders:
Hypertension (or high blood pressure)
Gestational hypertension (or pregnancy-induced hypertension) and pre-eclampsia

(S)-2-amino-3-(3,4-dihydroxyphenyl)-2-methyl-propanoic acid

Methyldopa has a dual mechanism of action:
It is a competitive inhibitor of the enzyme DOPA decarboxylase, also known as aromatic L-amino acid decarboxylase, which converts L-DOPA into dopamine. Dopamine is a precursor for norepinephrine (noradrenaline) and subsequently epinephrine (adrenaline). This inhibition results in reduced dopaminergic and adrenergic neurotransmission in the peripheral nervous system. This effect may lower blood pressure and cause central nervous system effects such as depression, anxiety, apathy, anhedonia, and parkinsonism.
It is converted to α-methylnorepinephrine by dopamine beta-hydroxylase (DBH). α-methylnorepinephrine is an agonist of presynaptic central nervous system α2-adrenergic receptors. Activation of these receptors in the brainstem appears to inhibit sympathetic nervous system output and lower blood pressure. This is also the mechanism of action of clonidine.

Methyldopa exhibits variable absorption from the gastrointestinal tract. It is metabolized in the liver and intestines and is excreted in urine.

Methyldopa is capable of inducing a number of adverse side effects, which range from mild to severe. Nevertheless, they are generally mild when the dose is less than 1 gram per day.[1] Side effects may include:
Depression and/or even suicidal ideation, as well as nightmares
Apathy and/or anhedonia, as well as dysphoria
Anxiety, especially of the social anxiety variant
Decreased alertness, awareness, and wakefulness
Impaired attention, focus, and concentration
Decreased desire, drive, and motivation
Fatigue or lethargy and/or malaise or lassitude
Sedation or drowsiness and/or somnolence or sleepiness
Agitation or restlessness
Cognitive and memory impairment
Derealization and/or depersonalization, as well as mild psychosis
Sexual dysfunction including impaired libido, desire, and drive
Dizziness, lightheadedness, or vertigo
Miosis or pupil constriction
Xerostomia or dry mouth
Gastrointestinal disturbances such as diarrhea and/or constipation
Headache or migraine
Myalgia or muscle aches, arthralgia or joint pain, and/or paresthesia ("pins and needles")
Restless legs syndrome (RLS)
Parkinsonian symptoms such as muscle tremors, rigidity, hypokinesia, and/or balance or postural instability
Akathisia, ataxia, dyskinesia as well as even tardive dyskinesia, and/or dystonia
Bell's palsy or facial paralysis
Sexual dysfunction consisting of impaired erectile dysfunction and/or anorgasmia
Hyperprolactinemia or excess prolactin, gynecomastia/breast enlargement in males, and/or amenorrhoea or absence of menstrual cycles in females
Bradycardia or decreased heart rate
Hypotension or decreased blood pressure (though this may also be considered a therapeutic benefit)
Orthostatic hypotension (also known as postural hypotension)
Hepatitis, hepatotoxicity, or liver dysfunction or damage
Pancreatitis or inflammation of the pancreas
Haemolytic anaemia or deficiency in red blood cells (RBCs)
Myelotoxicity or bone marrow suppression, potentially leading to thrombocytopenia or blood platelet deficiency and/or leukopenia or white blood cell (WBC) deficiency
Hypersensitivity such as lupus erythematosus, myocarditis, and/or pericarditis
Lichenoid reactions such as skin lesions and/or rashes

Alphadopa    Wokhardt  (Merind)