Saturday, April 26, 2014

Telmisartan

Telmisartan is an angiotensin II receptor antagonist (angiotensin receptor blocker, ARB) used in the management of hypertension. It is marketed under the trade names, Telsartan,Telmiget, etc..

MICARDIS is a non-peptide angiotensin II receptor (type AT1) antagonist.

Telmisartan is chemically described as 4'-[(1,4'-dimethyl-2'-propyl [2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid. Its empirical formula is C33H30N4O2, its molecular weight is 514.63, and its structural formula is:



Telmisartan is a white to slightly yellowish solid. It is practically insoluble in water and in the pH range of 3 to 9, sparingly soluble in strong acid (except insoluble in hydrochloric acid), and soluble in strong base.

MICARDIS is available as tablets for oral administration, containing 20 mg, 40 mg or 80 mg of telmisartan. The tablets contain the following inactive ingredients: sodium hydroxide, meglumine, povidone, sorbitol, and magnesium stearate. MICARDIS tablets are hygroscopic and require protection from moisture.


What are the possible side effects of telmisartan (Micardis)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

In rare cases, telmisartan can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure. Call your doctor right away if you have muscle pain, tenderness, or weakness especially if you also have fever, nausea or vomiting, and dark colored urine.

Call your doctor at once if you have any other serious side effects, such as:

feeling like you might pass...
Read All Potential Side Effects and See Pictures of Micardis »

What are the precautions when taking telmisartan (Micardis)?

Before taking telmisartan, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease (such as renal artery stenosis), liver disease, bile duct blockage, high blood levels of potassium in the blood (hyperkalemia), loss of too much body water and/or minerals (volume depletion, dehydration).

This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.


BRANDS
Adcom Tablet 40 mg            Intel Pharmaceuticals
Arbitel Tablet                     Micro Labs Ltd (Cardicare)
Arbitel (40 mg) Tablet        Micro Labs Ltd (Cardicare)
Astel Tablet                       AS Pharma
Astel (40 mg)Tablet             AS Pharma
Cortel Tablet                            Corona Laboratories  
Cortel (40 mg) Tablet           Corona Laboratories
Cortel (80 mg) Tablet        Corona Laboratories
Cresar (20 mg) Tablet        Cipla Limited  
Cresar (40 mg) Tablet        Cipla Limited  
Cresar (80 mg) Tablet     Cipla Limited
Etela Tablet                     Venus Remedies
Hytel Tablet                     East West Pharma
Hytel (40 mg)Tablet   East West Pharma
Hytel (80 mg)Tablet   East West Pharma
Lovetel FC Tablet         Q Check Speciality Care
Micartel Tablet         Ind-Chemie Health Specialities Pvt Ltd.
Micartel (40 mg)Tablet Ind-Chemie Health Specialities Pvt Ltd.
Mytel Tablet              Rhine Biogenics Pvt Ltd


PRICE LIST

Ozotel (40Mg)
(10 Tablets in Tablet)
Ozone Pharmaceuticals Ltd
Rs. 2/Tablet

Ozotel Am Tab 10`S
(10 Tablet in Tablet)
Ozone Pharmaceuticals Ltd
Rs. 2/Tablet

Telmikind (40 Mg)
(10 Tablets in Tablet)
Mankind Pharma
Rs. 2.15/Tablet

Telmikind-(40mg)
(10 Tablets in Tablet)
Mankind Pharma
Rs. 2.58/Tablet

Temsan (40Mg)
(10 Tablets in Tablet)
Emcure Pharmaceuticals Ltd
Rs. 2.75/Tablet

Xstan (40Mg)
(10 Tablets in Tablet)
Blue Cross Laboratories Ltd
Rs. 2.80/Tablet

Telsartan Activ (40 Mg)
(30 Tablets in Tablet)
Dr Reddy Laboratories Ltd
Rs. 2.97/Tablet

Newtel (40 Mg)
(14 Tablets in Tablet)
Systopic Laboratories Pvt Ltd
Rs. 3.35/Tablet

Zitelmi (40 Mg)
(10 Tablets in Tablet)
FDC Limited
Rs. 3.38/Tablet

Cortel (40 Mg)
(10 Tablets in Tablet)
Aarush (Corona Remedies Pvt Ltd)
Rs. 3.50/Tablet

Sodium Nitroprusside


Sodium nitroprusside is primarily used as a vasodilator. In this role it is abbreviated SNP, and it has tradenames like Nitropress. It acts as a drug by releasing nitric oxide; it belongs to the class of NO-releasing drugs as a result. This drug is used as a vasodilator to reduce blood pressure. Sodium nitroprusside is also used as an analytical reagent for the detection of methyl ketones, and for the detection of amines that are often found in illicit drugs.


Sodium nitroprusside is an inorganic compound with the formula Na2[Fe(CN)5NO], usually encountered as the dihydrate, Na2[Fe(CN)5NO]·2H2O. This red-colored sodium salt dissolves in water ethanol to give solutions containing the free complex dianion [Fe(CN)5NO]2−.

USE 
Sodium nitroprusside is primarily used as a vasodilator. It was first used in human medicine in 1928. By 1955, data on its safety during short-term use in patients with severe hypertension had become available. Despite this, due to difficulties in its chemical preparation, it was not until 1974 that it was finally approved by the US FDA for the treatment of severe hypertension. By 1993 its popularity had grown such that total sales in the US had totalled $2 million USD.
NITROPRESS  (Sodium Nitroprusside Injection) is not suitable for direct injection. The solution must be further diluted in sterile 5% dextrose injection before infusion.
NITROPRESS (nitroprusside sodium) can cause precipitous decreases in blood pressure . In patients not properly monitored, these decreases can lead to irreversible ischemic injuries or death. Sodium nitroprusside should be used only when available equipment and personnel allow blood pressure to be continuously monitored.
Except when used briefly or at low ( < 2 mcg/kg/min) infusion rates, sodium nitroprusside gives rise to important quantities of cyanide ion, which can reach toxic, potentially lethal levels . The usual dose rate is 0.5-10 mcg/kg/min, but infusion at the maximum dose rate should never last more than 10 minutes. If blood pressure has not been adequately controlled after 10 minutes of infusion at the maximum rate, administration of sodium nitroprusside should be terminated immediately.
Although acid-base balance and venous oxygen concentration should be monitored and may indicate cyanide toxicity, these laboratory tests provide imperfect guidance.
This package insert should be thoroughly reviewed before administration of NITROPRESS (nitroprusside sodium) .

Sodium nitroprusside has potent vasodilating effects in arterioles and venules (arterioles more than venuols, but this selectivity is much less marked than that of nitroglycerin) as a result of its breakdown to nitric oxide (NO). It is intravenously infused in cases of acute hypertensive crises. Its therapeutic effects are usually seen within a few minutes.

Nitric oxide reduces both total peripheral resistance as well as venous return, thus decreasing both preload and afterload. For this reason, it can be used in severe congestive heart failure where this combination of effects can act to increase cardiac output. In situations where cardiac output is normal, the effect is to reduce blood pressure. It is sometimes also used to induce hypotension (in order to reduce bleeding) for surgical procedures (for which it is also FDA, TGA and MHRA labelled).

This compound has also been successfully used as a treatment for: aortic valve stenosis, erythromelalgia, oesophageal varices, severe pyrexia (fever), lactic acidosis, myocardial infarction, neuroleptic malignant syndrome, pulmonary hypertension, respiratory distress syndrome in the newborn, shock, cerebral vasospasm, ergot toxicity, ventricular septal defects.





BRANDS
Nipress inj        -  Samarth Pharma
Niside  inj        -  Shree Ganesh Rubber & Chemicals Co
Nitroplus 50mg inj -  Neon Laboratories Ltd
Pruside inj        -  Troikaa Parenterals Pvt. Ltd.
Sonide inj         -  Gufic Limited

DOSE

Dilution to proper strength for infusion: Depending on the desired concentration, the solution containing 50 mg of NITROPRESS (nitroprusside sodium) must be further diluted in 250-1000 mL of sterile 5% dextrose injection. The diluted solution should be protected from light, using the supplied opaque sleeve, aluminum foil, or other opaque material. It is not necessary to cover the infusion drip chamber or the tubing.

Verification of the chemical integrity of the product: Sodium nitroprusside solution can be inactivated by reactions with trace contaminants. The products of these reactions are often blue, green, or red, much brighter than the faint brownish color of unreacted NITROPRESS (nitroprusside sodium) . Discolored solutions, or solutions in which particulate matter is visible, should not be used. If properly protected from light, the freshly diluted solution is stable for 24 hours.

No other drugs should be administered in the same solution with sodium nitroprusside.

Avoidance of excessive hypotension: While the average effective rate in adults and children is about 3 mcg/kg/min, some patients will become dangerously hypotensive when they receive NITROPRESS at this rate. Infusion of sodium nitroprusside should therefore be started at a very low rate (0.3 mcg/kg/min), with upward titration every few minutes until the desired effect is achieved or the maximum recommended infusion rate (10 mcg/kg/min) has been reached.

Because sodium nitroprusside's hypotensive effect is very rapid in onset and in dissipation, small variations in infusion rate can lead to wide, undesirable variations in blood pressure. Sodium nitroprusside should not be infused through ordinary I.V. apparatus, regulated only by gravity and mechanical clamps. Only an infusion pump, preferably a volumetric pump, should be used.

Because sodium nitroprusside can induce essentially unlimited blood-pressure reduction, the blood pressure of a patient receiving this drug must be continuously monitored, using either a continually reinflated sphygmomanometer or (preferably) an intra-arterial pressure sensor. Special caution should be used in elderly patients, since they may be more sensitive to the hypotensive effects of the drug.

When sodium nitroprusside is used in the treatment of acute congestive heart failure, titration of the infusion rate must be guided by the results of invasive hemodynamic monitoring with simultaneous monitoring of urine output. Sodium nitroprusside can be titrated by increasing the infusion rate until:

measured cardiac output is no longer increasing,
systemic blood pressure cannot be further reduced without compromising the perfusion of vital organs, or
the maximum recommended infusion rate has been reached, whichever comes earliest. Specific hemodynamic goals must be tailored to the clinical situation, but improvements in cardiac output and left ventricular filling pressure must not be purchased at the price of undue hypotension and consequent hypoperfusion.
The table below shows the infusion rates corresponding to the recommended initial and maximal doses (0.3 mcg/kg/min and 10 mcg/kg/min, respectively) for both adults and children of various weights. Some of the listed infusion rates are so slow or so rapid as to be impractical, and these practicalities must be considered when the concentration to be used is selected. Note that when the concentration used in a given patient is changed, the tubing is still filled with a solution at the previous concentration.

Avoidance of cyanide toxicity: As described in CLINICAL PHARMACOLOGY above, when more than 500 mcg/kg of sodium nitroprusside is administered faster than 2 mcg/kg/min, cyanide is generated faster than the unaided patient can eliminate it. Administration of sodium thiosulfate has been shown to increase the rate of cyanide processing, reducing the hazard of cyanide toxicity. Although toxic reactions to sodium thiosulfate have not been reported, the co-infusion regimen has not been extensively studied, and it cannot be recommended without reservation. In one study, sodium thiosulfate appeared to potentiate the hypotensive effects of sodium nitroprusside.

Co-infusions of sodium thiosulfate have been administered at rates of 5-10 times that of sodium nitroprusside. Care must be taken to avoid the indiscriminate use of prolonged or high doses of sodium nitroprusside with sodium thiosulfate as this may result in thiocyanate toxicity and hypovolemia. Incautious administration of sodium nitroprusside must still be avoided, and all of the precautions concerning sodium nitroprusside administration must still be observed.
Sonide inj         -  Gufic Limited


Infusion Rates (mL/hour) to Achieve Initial (0.3 mcg/kg/min) and Maximal (10 mcg/kg/min) Dosing of NITROPRESS (nitroprusside sodium) 
VOLUME
NITROPRESS (NITROPRUSSIDE SODIUM)
CONCENTRATION
250 ML
50 MG
200 MCG/ML
500 ML
50 MG
100 MCG/ML
1000 ML
50 MG
50 MCG/ML
PTWEIGHT
KGLBSINITMAXINITMAXINITMAX
10221302604120
204426041207240
3066390518011360
40884120724014480
501105150930018600
6013251801136022720
7015462101342025840
8017672401448029960
90198827016540321080
100220930018600361200
Consideration of methemoglobinemia and thiocyanate toxicity: Rare patients receiving more than 10 mg/kg of sodium nitroprusside will develop methemoglobinemia; other patients, especially those with impaired renal function, will predictably develop thiocyanate toxicity after prolonged, rapid infusions. In accordance with the descriptions in ADVERSE REACTIONS above, patients with suggestive findings should be tested for these toxicities.
WARNING: Do not use flexible container in series connections.

PRICE LIST

Sonide (50 Mg)
(1 Unit in Injection)
Gufic Chem Pvt Ltd
Rs. 45/Injection

Niside (50 Mg)
(1 Unit in Injection)
Shree Ganesh Pharmaceuticals
Rs. 120/Injection

Pruside (50 Mg)
(1 Unit in Injection)
Troikaa Pharmaceuticals Ltd
Rs. 140/Injection

Nitroplus (50 Mg)
(1 Unit in Injection)
Neon Laboratories Ltd
Rs. 144/Injection

Nitoside (50Mg)
(1 Unit in Injection)
Neon Laboratories Ltd
Rs. 144/Injection

Nipress (50 Mg)
(1 Unit in Injection)
Samarth Life Sciences Pvt. Ltd
Rs. 157/Injection


Sunday, April 20, 2014

RAMIPRIL

Ramipril is an angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.

USE

Hypertension;
Congestive heart failure;
Following heart attack in patients with clinical evidence of heart failure;
Susceptible patients over 55 years: prevention of heart attack, stroke, cardiovascular death or need of revascularization procedures.
Diabetic nephropathy (kidney damage due to diabetes) with microalbuminuria (protein in the urine); in low doses it is used as a prophylaxis for developing nephropathy and related secondary cardiovascular events.

DOSING: The usual dose of ramipril for hypertension is 2.5-20 mg a day as a single dose or two divided doses. Patients taking diuretics or who have reduced kidney function may require lower doses. Heart failure is initially treated with 1.25-2.5 mg twice daily then titrated up to 10 mg once daily or 5 mg twice daily. The dose for preventing heart attacks and strokes is 2.5-10 mg daily.


IUPAC Name     -  (2S,3aS,6aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-octahydrocyclopenta[b]pyrrole-2-carboxylic acid


STORAGE: Tablets and capsules should be stored at room temperature between 15 C to 30 C (59 F to 86 F).

CONTRA INDICATIONS  -  Renovascular disease (impaired blood flow in the kidneys), severe renal impairment (especially in patients with one kidney or with bilateral renal artery stenosis), volume-depleted patients, history of angioedema while on an ACE inhibitor, pregnancy, hypotension.


ADVERSE EFFECTS  -
low blood sugar (in patients taking medication for diabetes), causing sweating or shakiness
dry cough
dizziness and light-headedness due to low blood pressure
tiredness and fatigue, especially in the early stages
mouth dryness in the early stages
nausea, vomiting, diarrhea (persistent in rare cases)
fainting
change in amount of urine
signs of infection (e.g., fever, chills, persistent sore throat)
yellowing of eyes or skin, dark urine
stomach or abdominal pain
neutropenia (low white blood cells)
impotence (erectile dysfunction)
Serious allergic reactions to this drug are unlikely, but immediate medical attention must be sought if they occur. Symptoms of a serious allergic reaction include, but are not limited to a rash or swelling of the face, mouth, tongue, or throat.

In extreme cases, ramipril may lead to potentially fatal liver problems.


MECHANISM OF ACTION  -
ACE inhibitors, as the name suggests, inhibit the actions of angiotensin converting enzyme (ACE), thereby lowering the production of angiotensin II and also decreasing the breakdown of bradykinin. The decrease in angiotensin II results in relaxation of arteriole smooth muscle leading to a decrease in total peripheral resistance, reducing blood pressure as the blood is pumped through widened vessels. Its effect on bradykinin is responsible for the dry cough side effect.

Ramipril, a prodrug or precursor drug, is converted to the active metabolite (metabolic product) ramiprilat by liver esterase enzymes.[4] Ramiprilat is mostly excreted by the kidneys. The half-life of ramiprilat is variable (3–16 hours), and is prolonged by heart and liver failure, as well as kidney failure.

DRUG INTERACTIONS: The use of ACE inhibitors with potassium supplements, salt substitutes or diuretics (for example, spironolactone [Aldactone] that increase potassium in the blood may lead to excessive potassium levels. Potassium levels should be monitored whenever ACE inhibitors are used in combination with these drugs.


PATENT -
The compound was protected by U.S. Patent 5,061,722 which was assigned to Aventis on 29 October 1991. The patent was scheduled to expire on 29 October 2008. On 11 September 2007, in an appeal by the Indian company Lupin Ltd., the United States Court of Appeals for the Federal Circuit reversed a district court trial verdict and found that Aventis's patent on ramipril was invalid for "obviousness" - opening this medicine to generic manufacturers.

Ramipril is marketed in India under the brand names of Cardace, Zigpril, Ramistar and Zorem.

BRANDS
Artere Tabet                  Valiant Healthcare Limited
Artere (5 mg) Tabet         Alchemist Lifesciences Ltd.
Cardace Tabet              Alcare David Ltd.
Cardiopril Cap                Dr. Reddy s Laboratories
Conram Tabet              Concertina Pharma Pvt. Ltd
Cordimil Cap                Ind - Swift
Corpril Cap                     Ranbaxy
Dexace (10 mg) Tabet     Dexter Laboratories Pvt. Ltd.
Ecator (10 mg) Tabet       Torrent Labs (P) Ltd.
G -Pril Tabet               Hinglaj Labs of India
Gopril (10 mg)Tabet         CMG Biotech
GR Pace (10 mg)Tabet     G R Laboratories Pvt. Ltd.
Hopace Tab                 Micro Labs Ltd (Cardicare)
Hoperam(1.25mg)Tabet   Zinnia Life Sciences
Kepry Tabet                 Cadex Laboratories
Megapril Tabet                 Biomax
Misry Tabet                 Biocin Healthcare
Nexrami Tabet               Nexus Biotech
Panpril -5 Tabet               Panvik Pharmaceuticals
Polypril (10mg)Tabet       Druto Laboratories
Preface Tabet               Centaur Pharmaceuticals Pvt.Ltd.
Proace (2.5mg)Tabet       Alembic Chemical Works Co Ltd
Race (1.25mg)Tablet       Alkem Laboratories Ltd
Ramace (10mg)Cap         Astra Zeneca Pharma India Limited
Ramcor 5 Cap                 IPCA Laboratories (Innova Division)
Ramey Cap                Cadila Pharmaceuticals (Recon Healthcare)
Rami -Ten tab                Twilight Merchantiles (P) Ltd.
Ramic (1.25 mg)Tab        D.R.John & Lab
Ramicard tab                Intra Labs India Pvt Ltd
Ramichek (1.25mg)tab    Indoco Remedies Ltd
Ramihart (2.5mg)Tab       Mankind Pharmaceuticals Pvt. Ltd.
Ramil (1.25 mg) Tab        Aurobindo Pharma Ltd. (Argus)
Ramipres (10 mg) Tab     Cipla Limited
Ramipro Cap                 Emcure Pharmaceuticals
Ramiril Cap                     Micro Labs
Ramistar (10 mg)Cap      Lupin Laboratories Ltd.
Rampril (10 mg)Cap       Themis Medicare Ltd.
Ramsho (1.25 mg)Tab    Aamorb Pharmaceuticals Pvt Ltd (Xeena)
Rebeat (5 mg) Tab          Le Renon Healthcare Pvt.Ltd
Rigapril (10mg) Tab        Quadriga Biotech Pvt Ltd
RL Tab 1.25                   Sunij Pharma Pvt Ltd
Saface Tab               Morepen Laboratories Ltd.
Servace Cap               Bal Pharma (Servetus Division)
Topril Cap                     Torrent Pharmaceuticals
Variace (1.25mg) Tab    Win-Medicare Limited


PRICELIST

Odipril Hg (5 Mg) (10 Capsules in Capsule) Blue Cross Laboratories Ltd Rs. 3/Capsule Servace (5 Mg) (10 Capsules in Capsule) Servetus (Bal Pharma Limited) Rs. 3.75/Capsule Ziram (5 Mg) (10 Capsules in Capsule) FDC Limited Rs. 3.83/Capsule Ramihart (5 Mg) (7 Capsule in Capsule) Mankind Pharma Rs. 3.86/Capsule Ramm (5 Mg) (10 Capsules in Capsule) Finecure Pharmaceuticals Ltd Rs. 4.20/Capsule Rl (5 Mg) (10 Capsules in Capsule) Sunij Pharma Pvt Ltd Rs. 4.40/Capsule Acepril (5 Mg) (10 Capsules in Capsule) Sain Medicaments Pvt. Ltd Rs. 4.96/Capsule Ramidil (5 Mg) (10 Capsules in Capsule) Vazokare (Medley Pharmaceuticals Limited) Rs. 5.30/Capsule R Pril (5 Mg) (10 Capsules in Capsule) Biochem Pharmaceutical Industrial Ltd Rs. 5.40/Capsule Rampril (5 Mg) (10 Capsules in Capsule) Themis Pharmaceuticals Limited Rs. 5.60/Capsule