Tuesday, April 28, 2009

Telmisartan


Telmisartan (INN) (pronounced /tɛlmɪˈsɑrtən/) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. It is marketed under the trade names Pritor or Kinzal (Bayer Schering Pharma), Micardis (Boehringer Ingelheim), Telma (Glenmark Pharma), Telday (Torrent Pharmaceuticals) and Teleact D by (Ranbaxy).
Mode of action
Telmisartan ( Teli marketed by cadila pharma) is an Angiotensin Receptor Blocker (ARB) that shows high affinity for the angiotensin II type 1 (AT1) receptors, has a long duration of action, and has the longest half-life of any ARB. [1][2]
In addition to blocking the Renin-Angiotensin System (RAS), telmisartan acts as a selective modulator of Peroxisome Proliferator-Activated Receptor-gamma (PPAR-γ), a central regulator of insulin and glucose metabolism. It is believed that telmisartan’s dual mode of action may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease (CVD). [2]
Telmisartan has binding affinity 3000 times with AT-2 receptor than AT-1 receptor.Telmisartan is also having maximum half life in sartans - 24 Hrs.

Indication
Telmisartan is indicated in the treatment of essential hypertension. [1]

Candesartan


Candesartan (rINN) (pronounced /ˌkændɨˈsɑrtən/) is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. The prodrug candesartan cilexetil is marketed by AstraZeneca and Takeda Pharmaceuticals, commonly under the trade names Blopress, Atacand, Amias, and Ratacand.

As with all angiotensin II receptor antagonists, candesartan is indicated for the treatment of hypertension. Results from the CHARM study in the early 2000s demonstrated the morbidity and mortality reduction benefits of candesartan therapy in congestive heart failure.[1] Thus, while ACE inhibitors are still considered first-line therapy in heart failure, candesartan can be used in combination with an ACE to achieve improved mortality and morbidity vs. an ACE alone and additionally is an alternative in patients intolerant of ACE inhibitor therapy.

Clopidogrel


Clopidogrel is an oral antiplatelet agent (thienopyridine class) to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease. It is marketed by Bristol-Myers Squibb and Sanofi-Aventis under the trade name Plavix, by Sun Pharmaceuticals under the trade name Clopilet, by Ranbaxy Laboratories under the trade name Ceruvin. It works by irreversibly inhibiting a receptor called P2Y12. Adverse effects include hemorrhage.

Adverse effects
Serious adverse drug reactions associated with clopidogrel therapy include:Severe neutropenia (Incidence: 1/2,000)Thrombotic thrombocytopenic purpura (TTP) (Incidence: 4/1,000,000 patients treated)[citation needed]Hemorrhage - The incidence of hemorrhage may be increased by the co-administration of aspirin.[9] Gastrointestinal Hemorrhage (Incidence: 2.0%)Cerebral Hemorrhage (Incidence: 0.1 to 0.4%)Use of non-steroidal anti-inflammatory drugs is discouraged in those taking clopidogrel due to increased risk of digestive tract hemorrhage

Captopril


Captopril (rINN) (pronounced /ˈkæptəprɪl/) is an angiotensin-converting enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and some types of congestive heart failure. Captopril was the first ACE inhibitor developed and was considered a breakthrough both because of its novel mechanism of action and also because of the revolutionary development process. Captopril is commonly marketed by Bristol-Myers Squibb under the trade name Capoten.
Adverse effects

Cough is the most common long-term adverse drug reaction associated with captopril therapy, as it is with all the ACE inhibitors. Hypotension is also a possible adverse effect, if the dose is too high. Hyperkalemia is possible, due to ACE inhibition reducing aldosterone production. Captopril can also be the cause of glomerulonephritis. It is even known to cause a condition called acute generalized exanthematous pustulosis.[citation needed]

Isosorbide mononitrate


Isosorbide mononitrate is a drug used principally in the treatment of angina pectoris[1] and acts by dilating the blood vessels so as to reduce the blood pressure. It is sold by AstraZeneca under the trade name Imdur.

Isosorbide mononitrate is used for the prophylactic treatment of angina pectoris; that is, it is taken in order to prevent or at least reduce the occurrence of angina. Research on Isosorbide mononitrate as a cervical ripener to reduce time at hospital to birth is supportive.[2]

Side effects

The adverse reactions which follow have been reported in studies with isosorbide mononitrate:
Very common: Headache predominates (up to 30%) necessitating withdrawal of 2 to 3 % of patients, but the incidence reduces rapidly as treatment continues .
Common: Tiredness, sleep disturbances (6%) and gastrointestinal disturbances (6%) have been reported during clinical trials with isosorbide mononitrate modified release tablets, but at a frequency no greater than for placebo. Hypotension (4 to 5%), poor appetite (2.5%), nausea (1%).
Adverse effects associated with the clinical use of the drug are as expected with all nitrate preparations. They occur mainly in the early stages of treatment.
Hypotension (4%) with symptoms such as dizziness and nausea (1%) have been reported. These symptoms generally disappear during long-term treatment.
Other reactions that have been reported with isosorbide mononitrate modified release tablets include tachycardia, vomiting, diarrhoea, vertigo and heartburn.

Propranolol


Propranolol (INN) is a non-selective beta blocker mainly used in the treatment of hypertension. It was the first successful beta blocker developed. It is the only drug proven effective for the prophylaxis of migraines in children. Propranolol is available in generic form as propranolol hydrochloride, as well as an AstraZeneca and Wyeth product under the trade names Inderal, Inderal LA, Avlocardyl (also available in prolonged absorption form named "Avlocardyl Retard"), Deralin, Dociton, Inderalici, InnoPran XL, Sumial (depending on marketplace and release rate).

Propranolol is rapidly and completely absorbed, with peak plasma levels achieved approximately 1–3 hours after ingestion. Co-administration with food appears to enhance bioavailability. Despite complete absorption, propranolol has a variable bioavailability due to extensive first-pass metabolism. Hepatic impairment will therefore increase its bioavailability. The main metabolite 4-hydroxypropranolol, with a longer half-life (5.2–7.5 hours) than the parent compound (3–4 hours), is also pharmacologically active.
Propranolol is a highly lipophilic drug achieving high concentrations in the brain. The duration of action of a single oral dose is longer than the half-life and may be up to 12 hours, if the single dose is high enough (e.g., 80 mg). Effective plasma concentrations are between 10–100 ng/mL.
Toxic levels are associated with plasma concentrations above 2000 ng/ml.

Monday, April 27, 2009

Aspirin

Aspirin (USAN), also known as acetylsalicylic acid (pronounced /əˌsɛtɪlsælɪˌsɪlɪk ˈæsɪd/, abbreviated ASA), is a salicylate drug, often used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication.
Aspirin also has an antiplatelet, or "anti-coagulate", effect by inhibiting thromboxane prostaglandins, which under normal circumstances bind platelet molecules together to repair damaged blood vessels. This is why aspirin is used in long-term, low doses to prevent heart attacks, strokes, and blood clot formation in people at high risk for developing blood clots.[1] It has also been established that low doses of aspirin may be given immediately after a heart attack to reduce the risk of another heart attack or of the death of cardiac tissue.[2][3]
The main undesirable side effects of aspirin are gastrointestinal ulcers, stomach bleeding, and tinnitus, especially in higher doses. In children and adolescents, aspirin is no longer used to control flu-like symptoms or the symptoms of chickenpox or other viral illnesses, due to the risk of Reye's syndrome.[4]
Aspirin was the first discovered member of the class of drugs known as non-steroidal anti-inflammatory drugs (NSAIDs), not all of which are salicylates, although they all have similar effects and most have inhibition of the enzyme cyclooxygenase as their mechanism of action. Today, aspirin is one of the most widely used medications in the world, with an estimated 40,000 metric tons of it being consumed each year.[5] In countries where Aspirin is a registered trademark owned by Bayer, the generic term is acetylsalicylic acid (ASA).[6][7]