NIFEDIPINE

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

DOSE

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.

USES

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.

OVERDOSAGE

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.

BRANDS

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

NEBIVOLOL

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.

1-(6-fluorochroman-2-yl)-{[2-(6-fluorochroman-2-yl)-2-hydroxy-ethyl]amino}ethanol

PHARMACOLOGY

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.

BRANDS

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

Nebilet

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)

METOPROLOL

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.

(RS)-1-(Isopropylamino)-3-[4-(2-methoxyethyl)phenoxy]propan-2-ol

USE

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:

bupropion;

prazosin;

terbinafine;

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.

BRANDS

BETALOC       ASTRAZENICA

LOPRESOR      NOVARTIS

MEPOL         TARUS LABORATORIES

MET XL        AJANTHA

METAPRO       MICRO

METOLAR       CIPLA

METOLAR XR

METPURE XL    EMCURE

METOLAZONE

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.

7-chloro-2-methyl-4-oxo-3-o-tolyl-1,2,3,4-tetrahydroquinazoline-6-sulfonamide

USE
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.


MECHANISM OF ACTION
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.



BRANDS

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

METHYLDOPA

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)).

INDICATION
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


PHARMACOLOGY
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.

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



SIDE EFFECTS
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:
Psychological
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
Physiological
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
Pallor



BRANDS
Alphadopa    Wokhardt  (Merind)
aldomet
METHYL DOPA  UNICURE (INDIA
ALDOPAM TAB   NEON LABS
DOPAGYT TAB    THEMIS PHARMA
EMDOPA TAB     IDPL
GYNAPRES TAB    MANKIND
SEMBRINA TAB    SANOFI AVENTIS

DIABETIC KETO ACIDOSIS

HYPOGLYCEMIA SYMPTOMS