Thursday, February 26, 2009

Levocetirizine


Levocetirizine (as levocetirizine dihydrochloride) is a third generation non-sedative antihistamine, developed from the second generation antihistamine cetirizine. Chemically, levocetirizine is the active enantiomer of cetirizine. It is the R-enantiomer of the cetirizine racemate. Levocetirizine works by blocking histamine receptors. It does not prevent the actual release of histamine from mast cells, but prevents it binding to its receptors. This in turn prevents the release of other allergy chemicals and increased blood supply to the area, and provides relief from the typical symptoms of hayfever.
It is claimed to be more effective and with fewer side effects than the second generation drugs; however, this claim is not clearly supported by the available clinical literature.

Latest research shows levocetirizine reduces asthma attacks by 70% in children.[2]

Montelukast


Montelukast (trade name Singulair) is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies.[1] It is usually administered orally. Montelukast is a CysLT1 antagonist; that is it blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation.
Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific focus of operation, it does not interact with other allergy medications such as theophylline.
Another leukotriene receptor antagonist is zafirlukast (Accolate), taken once daily. Zileuton (Zyflo), an asthma drug taken four times per day, blocks leukotriene synthesis by inhibiting 5-lipoxygenase, an enzyme of the eicosanoid synthesis pathway.
The Mont in Montelukast stands for Montreal, the place where Merck developed the drug [2]

Schering-Plough and Merck have sought permission to market a combined tablet with loratadine (Claritin) and montelukast (Singulair), as many patients combine the two themselves. However, the FDA has found no benefit from a combined pill for seasonal allergies over taking the two drugs in combination[5], and on April 25, 2008, issued a "not approvable" letter for the combination.[6]

Fexofenadine


Fexofenadine hydrochloride (brand names include Allegra, Telfast and Fastofen) is an antihistamine drug used in the treatment of hayfever and similar allergy symptoms. It was developed as a successor of and alternative to terfenadine (brand names include Triludan and Seldane), an antihistamine with potentially serious contraindications. Fexofenadine, like other second and third-generation antihistamines, does not readily cross the blood-brain barrier, and so causes less drowsiness than first-generation histamine-receptor antagonists. It works by being an antagonist to the H1 receptor.[1]
It has been described as both second-generation[2] and third-generation.[3]


In controlled clinical studies there were no interactions with other drugs that significantly affected the safety or effectiveness of fexofenadine.[citation needed]

Loratadine


Loratadine is a drug used to treat allergies, and marketed for its non-sedating properties. It is marketed by Schering-Plough and Shionogi in Japan under several trade names such as Claritin, Claritin-D, Claritine, Clarityn, Clarityne or Fristamin depending on the market; by Cadila as Lorfast; by Lek as Lomilan or Flonidan; by Sandoz as Symphoral; by Ranbaxy as Roletra; by Pliva as Rinolan; by Teva as AllergyX; by Wyeth as Alavert; and by Pharma International as Tidilor[1]. It is also available as a generic. In a version marketed as Claritin-D or Clarinase, loratadine is combined with pseudoephedrine, a decongestant; this makes it somewhat useful for colds as well as allergies, but adds potential side-effects of insomnia, nervousness and anxiety.
It is considered a second generation agent.[2]

Loratadine is available as tablets, oral suspension and syrup, and also in combination with pseudoephedrine.
Also available are quick-dissolving tablets, which are marketed as being faster to get into one's circulatory system but which require special handling to avoid degrading in the package.

Hydroxyzine


Hydroxyzine (pronounced /haɪˈdrɒksɨziːn/) is a first-generation antihistamine, of the piperazine class that is an H1 receptor antagonist. It was synthesised in the early 1950s and the medicinal formulation of this drug was announced in the 04 August 1956 issue of Chemistry Week. It is used primarily as an antihistamine for the treatment of itches and irritations, an antiemetic for the reduction of nausea, as a weak analgesic by itself and as an opioid potentiator, and as an anxiolytic '''for the treatment of anxiety'''.[1]
Its most common formulation is 25 mg small white, capsule-shaped and scored tablets of the hydrochloride salt made by UCB in the Netherlands. In the United States, a nearly-spherical dark green tablet is the most-commonly encountered version of it, with 25 and 100 mg capsules being available as well as a series of colour-coded round tablets from Mallinkrodt (25 mg white, 50 mg orange, 100 mg blue). Hydroxyzine preparations usually require a doctor's prescription as do other potent antihistamines in many countries whereas some countries allow hydroxyzine and all or most other antihistamines to be sold over the counter.

Cetirizine


Cetirizine hydrochloride (pronounced /sɛˈtɪrɨziːn/), an antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. The structural similarity of cetirizine to hydroxyzine, and its derivation from piperazine, attribute similar adverse reactions and properties to other piperazine derivatives.
Formerly prescription-only in the US and Canada, cetirizine is now available over the counter in both countries as Zyrtec and Reactine respectively. In Australia Zyrtec is available over the counter in pharmacies and in the UK cetirizine can be sold in any outlet and is often available in supermarkets.

Cetirizine crosses the blood-brain barrier only slightly, eliminating the sedative side-effect common with older antihistamines; however it still causes mild drowsiness.[1]

Sunday, February 22, 2009

Clobazam


Clobazam, (marketed under the brand names Frisium and Urbanol), is a drug which is a benzodiazepine derivative. It has been marketed as an anxiolytic since 1975[2] and an anticonvulsant since 1984.[3]

As of 2005, clobazam (Frisium) is approved in Canada for adjunctive use in tonic-clonic, complex partial, and myoclonic seizures.[14] Clobazam (Urbanyl[15]) is approved for adjunctive therapy in complex partial seizures[16] certain types of status epilepticus, specifically the myoclonic, myoclonic-absent, simple partial, complex partial, and tonic varieties,[17] and non-status absence seizures.[18] It is also approved for treatment of anxiety. In India, clobazam (Frisium, Aventis Pharma India, Ltd.) is approved for use as an adjunctive therapy in epilepsy and in acute and chronic anxiety.[19] In Japan, clobazam (Mystan[5]) is approved for adjunctive therapy in treatment-resistant epilepsy featuring complex partial seizures.[20] In New Zealand, clobazam is marketed as Frisium[21] In the United Kingdom clobazam (Frisium) is approved for short-term (2-4 weeks) relief of acute anxiety in patients who have not responded to other drugs, with or without insomnia and without uncontrolled clinical depression.[22]

Bromazepam


Bromazepam (marketed under brand names Brazepam, Bromaze, Lexotan, Lectopam)[1] is a potent benzodiazepine derivative drug, developed in 1970s.[2][3] It has mainly anxiolytic and at higher doses also sedative, hypnotic and skeletal muscle relaxant properties.[4]

Bromazepam shares with other benzodiazepines the risk of abuse, misuse, psychological dependence and/or physical dependence.[13][14] A withdrawal study demonstrated both psychological dependence and physical dependence on bromazepam including marked rebound anxiety after 4 weeks chronic use. Those whose dose was gradually reduced experienced no withdrawal.[15]
Patients treated with bromazepam for generalised anxiety disorder were found to experience withdrawal symptoms such as a worsening of anxiety, as well as the development of physical withdrawal symptoms when abruptly withdrawn from bromazepam.[16][17] Abrupt or over rapid withdrawal from bromazepam after chronic use even at therapeutic prescribed doses may lead to a severe withdrawal syndrome including status epilepticus and a condition resembling delerium tremens.[18][19][20]

Alprazolam


Alprazolam, also known under the trade names Xanax, Xanor and Niravam, is a short-acting drug of the benzodiazepine class used to treat moderate to severe anxiety disorders, panic attacks, and as an adjunctive treatment for anxiety associated with moderate depression. It is also available in an extended release form, Xanax XR. Both forms are now available generically. Alprazolam possesses anxiolytic, sedative, hypnotic, amnesic, anticonvulsant and muscle relaxant properties.[3]
Alprazolam is a potentially addictive drug and long term use of alprazolam may cause a physical dependence to develop and benzodiazepine withdrawal syndrome to appear during discontinuation. In the USA, alprazolam is the most commonly misused benzodiazepine and is a schedule IV controlled drug.[4]

Alprazolam was first synthesized by Upjohn (now a part of Pfizer). It is covered under U.S. Patent 3,987,052 , which was filed on October 29, 1969, granted on October 19, 1976 and expired in September 1993. Alprazolam was released in 1981.[5][6] The first approved indication was panic disorder. Upjohn took this direction at the behest of a young psychiatrist David Sheehan. Sheehan's suggestion was to use the confusion DSM-III created in the classification of anxiety disorders (a distinction had just been made in DSM-III between generalized anxiety disorder (GAD) and panic disorder). Panic disorder was, at that point, perceived to be rare and treatable only with tricyclic antidepressants; benzodiazepines were thought to be ineffective

Friday, February 20, 2009

Lorazepam


Lorazepam (also known in English speaking countries under the following brand names Ativan, Lorapam, Novo-Lorazem, Nu-Loraz, Temesta and Tranqipamor)[4] is a benzodiazepine drug with short to medium duration of action. It has all five intrinsic benzodiazepine effects: anxiolytic, amnesic, sedative/hypnotic, anticonvulsant and muscle relaxant.[5] It is a powerful anxiolytic and since its introduction in 1977, lorazepam's principal use has been in treating the symptom of anxiety. It is a unique benzodiazepine insofar as it has also found use as an adjunct antiemetic in chemotherapy. Among benzodiazepines, lorazepam has a relatively high addictive potential.[6]
Lorazepam has relatively potent anxiolytic effects and its best known indication is the short-term management of severe anxiety. It is less useful in panic disorder.[7]
Lorazepam has strong sedative/hypnotic effects, and the duration of clinical effects from a single dose makes it an appropriate choice for the short term treatment of insomnia, particularly in the presence of severe anxiety. Withdrawal symptoms, including rebound insomnia and rebound anxiety, may occur after only 7 days' administration of lorazepam.[8]

Sodium valproate


Sodium valproate (INN) or valproate sodium (USAN) is the sodium salt of valproic acid and is an anticonvulsant used in the treatment of epilepsy and bipolar disorder, as well as other psychiatric conditions requiring the administration of a mood stabilizer. The intravenous formulations are used when oral administration is not possible.

All antiepilepic medications have been shown to be associated with higher risks of fetal abnormalities (mostly for spina bifida) since at least 1983 with the risks being related to the strength of medication used and use of more than one drug.[1][2] Valproate has also been recognised as sometimes causing a specific facial changes ("facial phenotype") termed "fetal valproate syndrome".[3] Sodium valproate has been associated with the rare condition Paroxysmal tonic upgaze of childhood from childhood exposure(Epileptic Disord. 2007 Sep;9(3):332-6) and also fetal exposure (This condition resolved after discontinuing valproate therapy. Ouvrier-Billson syndrome (J Child Neurol. 1988 Jul;3(3):177-80) is the name used for this condition, to honor the discoverer.

Fluoxetine



Fluoxetine hydrochloride (trade names Prozac, Fontex, Ladose, Sarafem, Solax, Lovan) is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. Fluoxetine is approved for the treatment of major depression (including pediatric depression), obsessive-compulsive disorder (in both adult and pediatric populations), bulimia nervosa, anorexia nervosa, panic disorder and premenstrual dysphoric disorder.[1] Despite the availability of newer agents, it remains extremely popular. Over 22.2 million prescriptions for generic formulations of fluoxetine were filled in the United States in 2007, making it the third most prescribed antidepressant.[2]

Olanzapine


Olanzapine (Zyprexa, Zyprexa Zydis, Zalasta, Zolafren, Olzapin, or in combination with fluoxetine Symbyax) is an atypical antipsychotic, approved by the FDA for the treatment of: schizophrenia on September 6, 1996;[1] depressive episodes associated with bipolar disorder, as part of the Symbyax formulation, on December 24, 2003;[2] acute manic episodes and maintenance treatment in bipolar disorder on January 14, 2004.[3] Off-label uses are listed below.
The olanzapine formulations are manufactured and marketed by the pharmaceutical company Eli Lilly and Company, whose patent for olanzapine proper expires in 2011.
Olanzapine is available as a tablet in strengths of 2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg and 20 mg and orally disintegrating wafers (known as Zydis), which dissolve on the tongue, in strengths of 5 mg, 10 mg, 15 mg and 20 mg. It is also available as a rapid-acting intramuscular injection for short-term acute use.

Monday, February 16, 2009

Risperidone


Risperidone (pronounced Ris-PEE-rǐ-dōne and sold under the trade name Risperdal in the Netherlands, United States, Canada, the United Kingdom, Portugal and several other countries, Risperdal or Ridal in New Zealand, Sizodon or Riscalin in India, Rispolept in Eastern Europe, and Belivon, or Rispen elsewhere) is an atypical antipsychotic developed by Janssen-Cilag.

Risperidone was approved by the United States Food and Drug Administration (FDA) in 1993[1] for the treatment of schizophrenia. On August 22, 2007, Risperdal was approved as the only drug agent available for treatment of schizophrenia in youth ages 13–18; it was also approved that same day for treatment of bipolar disorder in youth and children ages 10–18, joining lithium. Risperidone contains the functional groups of benzisoxazole and piperidine as part of its molecular structure. In 2003 the FDA approved risperidone for the short-term treatment of the mixed and manic states associated with bipolar disorder. In 2006 the FDA approved risperidone for the treatment of irritability in children and adolescents with autism.

Wednesday, February 11, 2009

Citalopram


Citalopram is an antidepressant drug used to treat major depression associated with mood disorders. It is also used on occasion in the treatment of body dysmorphic disorder and anxiety.
Citalopram belongs to a class of drugs known as selective serotonin reuptake inhibitors (SSRIs). It is sold under the brand-names Celexa (U.S. and Canada, Forest Laboratories, Inc.), Cipramil (Australia, Brazil, Finland, Germany, Ireland, Sweden, United Kingdom), Citrol, Seropram, Talam (Europe and Australia), Citabax, Citaxin (Poland), Citalec (Slovakia), Recital (Israel, Thrima Inc. for Unipharm Ltd.), Zetalo (India), Celapram, Ciazil (Australia, New Zealand), Zentius (South America, Roemmers), Ciprapine (Ireland), Cilift (South Africa), Citox (Mexico),Citopam , and Cipram (Denmark, H. Lundbeck A/S).

Escitalopram


Escitalopram (trade names Lexapro, Cipralex) is the pure (S) enantiomer of racemic citalopram and is a selective serotonin reuptake inhibitor (SSRI). Escitalopram is used in the treatment of depression and anxiety.
According to a meta-analysis of 12 new-generation antidepressants, escitalopram and sertraline are the best in terms of efficacy and acceptability in the acute-phase treatment of adults with unipolar major depression. Reboxetine was significantly worse.[1][2]

Paroxetine


Paroxetine (trade names Seroxat, Paxil) is a selective serotonin reuptake inhibitor (SSRI) antidepressant. It was released in 1992 by the pharmaceutical company GlaxoSmithKline. It is used to treat major depression, obsessive-compulsive, panic and social anxiety disorders in adult outpatients.
The efficacy of paroxetine for depression is comparable to that of older tricyclic antidepressants with fewer side effects.[1][2] Differences with newer antidepressants are subtler and mostly confined to side effects. It shares the common side effects and contraindications of other SSRIs, with high rates of nausea, somnolence, and sexual side effects. Unlike two other popular SSRI antidepressants fluoxetine and sertraline, paroxetine is associated with a clinically significant weight gain[3] and statistically significant increase in the risk of suicidal tendencies in both adults[4] and children.[5] Stopping paroxetine may result in a discontinuation syndrome.

Topiramate


Topiramate (brand name Topamax) is an anticonvulsant drug produced by Ortho-McNeil Neurologics and Noramco, Inc., both being divisions of Johnson & Johnson. Generic versions are available in Canada and were FDA approved in September 2006. Mylan Pharmaceuticals was recently granted final approval for generic topiramate 25, 100, and 200 mg tablets and sprinkle capsules by the FDA for sale in the US. 50 mg tablets were granted tentative approval. [1] The only patent left for topiramate in the U.S. is for pediatric use; this patent will expire on February 28, 2009. [2] It was discovered in 1979 by Drs. Bruce E. Maryanoff and Joseph F. Gardocki during their research work at McNeil Pharmaceutical.[3][4][5]

Glibenclamide



Glibenclamide (INN), also known as glyburide (USAN), is an anti-diabetic drug in a class of medications known as sulfonylureas,
It is sold in doses of 1.25 mg, 2.5 mg and 5 mg, under the trade names Diabeta, Glynase and Micronase in the United States and Daonil, Semi-Daonil and Euglucon in the United Kingdom.
It is also sold in combination with metformin under the trade name Glucovance.


It is used in the treatment of type II diabetes. As of 2007[update], it is one of only two oral anti-diabetics in the World Health Organization Model List of Essential Medicines (the other being metformin).[1] As of 2003, in the United States, it was the most popular sulfonyurea.[2]
Additionally, recent research shows that glyburide improves outcome in animal stroke models by preventing brain swelling. A retrospective study showed that in type 2 diabetic patients already taking glyburide there was improved NIH stroke scale scores on discharge compared to diabetic patients not taking glyburide.

Metformin


Metformin (INN; trade names Glucophage, Riomet, Fortamet, Glumetza, Obimet, Dianben, Diabex, Diaformin, and others) (IPA: /mɛtˈfɔrmɪn/) is an oral anti-diabetic drug from the biguanide class. It is the first-line drug for the treatment of type 2 diabetes, particularly in overweight and obese people and those with normal kidney function,[1][2][3] and evidence suggests it may be the best choice for people with heart failure.[4] Metformin is the most popular anti-diabetic drug in the United States and one of the most prescribed drugs in the country overall, with nearly 35 million prescriptions filled in 2006 for generic metformin alone.[5] It is also used in the treatment of polycystic ovary syndrome.
When prescribed appropriately, metformin causes few adverse effects—the most common is gastrointestinal upset—and, unlike many other anti-diabetic drugs, does not cause hypoglycemia if used alone. It also helps reduce LDL cholesterol and triglyceride levels, and may aid weight loss. As of 2008[update], metformin is one of only two oral anti-diabetics in the World Health Organization Model List of Essential Medicines (the other being glibenclamide).[6]

Pioglitazone


Pioglitazone is a prescription drug of the class thiazolidinedione (TZD) with hypoglycemic (antihyperglycemic, antidiabetic) action. Pioglitazone is marketed as trademarks Actos in the USA, Glustin in Europe and Zactos in Mexico by the pharmaceutical company Takeda.

Pioglitazone is used for the treatment of diabetes mellitus type 2 (previously known as non-insulin-dependent diabetes mellitus, NIDDM) in monotherapy and in combination with sulfonylurea, metformin, or insulin. Pioglitazone has also been used to treat non-alcoholic steatohepatitis (fatty liver), but this use is presently considered experimental.[5]

Glimepiride


Glimepiride is a medium-to-long acting sulfonylurea anti-diabetic drug. It is marketed as Amaryl by Sanofi-Aventis and as DIAPRIDE by Micro Labs Ltd. Glimepiride is the first third-generation sulfonylurea, and is very potent.
It is sometimes classified as third-generation,[1] and sometimes classified as second-generation.[2]

Glimepiride

Glimepiride is a medium-to-long acting sulfonylurea anti-diabetic drug. It is marketed as Amaryl by Sanofi-Aventis and as DIAPRIDE by Micro Labs Ltd. Glimepiride is the first third-generation sulfonylurea, and is very potent.
It is sometimes classified as third-generation,[1] and sometimes classified as second-generation.[2]


Amaryl is an oral diabetes medicine that helps control blood sugar levels. This medication helps your body respond better to insulin produced by your pancreas.
Amaryl is used together with diet and exercise to treat type 2 (non-insulin dependent) diabetes. Other diabetes medicines are sometimes used in combination with this medicine if needed.

Clopidogrel


Clopidogrel is an oral antiplatelet agent used in treatment of coronary artery disease, peripheral vascular disease, and cerebrovascular disease. It is marketed by Bristol-Myers Squibb and Sanofi-Aventis under the trade names Iscover and Plavix respectively, by Sun Pharmaceuticals under the trade name Clopilet and by Ranbaxy Laboratories under the trade name Ceruvin. It works by blocking a receptor called P2Y12. Adverse effects include hemorrhage.

PLAVIX (clopidogrel bisulfate) is a prescription medicine that when taken daily can help reduce your risk of having a future heart attack or stroke. It is recommended for people who have suffered from a recent heart attack or recent stroke, or who have been diagnosed with peripheral artery disease, or P.A.D.—poor circulation in the legs that may cause pain during exercise, such as walking, and may be relieved by rest.*

Simvastatin


Simvastatin (INN) (pronounced /ˈsɪmvəstætɨn/), (marketed under the trade names Zocor, Simvastatin, Simlup, Simcard and others) is a hypolipidemic drug belonging to the class of pharmaceuticals called "statins". It is used to control hypercholesterolemia (elevated cholesterol levels) and to prevent cardiovascular disease. Simvastatin is a synthetic derivate of a fermentation product of Aspergillus terreus.

Atorvastatin


Atorvastatin (INN) (pronounced /əˌtɔrvəˈstætən/) (Lipitor, Pfizer), is a member of the drug class known as statins, used for lowering blood cholesterol. It also stabilizes plaque and prevents strokes through anti-inflammatory and other mechanisms.
Atorvastatin inhibits HMG-CoA reductase, the rate-determining enzyme located in hepatic tissue that produces mevalonate, a small molecule used in the synthesis of cholesterol and other mevalonate derivatives. This lowers the amount of cholesterol produced which in turn lowers the total amount of LDL cholesterol.
Atorvastatin was first synthesized in 1985 by Bruce Roth while working at Warner-Lambert Company (now Pfizer).
With 2006 sales of US$12.9 billion, Lipitor is the largest selling drug in the world.[1]
Lipitor is not the only statin; there are several other statins on the market.[2][3]