Thursday, March 26, 2009

Sibutramine




Sibutramine (trade name Meridia in the U.S. and Canada, Reductil in Europe and most other countries), usually as sibutramine hydrochloride monohydrate, is an orally administered agent for the treatment of obesity, as an appetite suppressant. It is a centrally-acting serotonin-norepinephrine reuptake inhibitor structurally related to amphetamines,[1] although its mechanism of action is distinct.[2]
Sibutramine is manufactured by Abbott Laboratories. It is classified as a Schedule IV controlled substance in the United States, despite having an extremely low-potential for abuse(due to the lack of dopamine effects).


Frequently encountered side effects are: dry mouth, paradoxically increased appetite, nausea, strange taste in the mouth, upset stomach, constipation, trouble sleeping, dizziness, drowsiness, menstrual cramps/pain, headache, flushing, or joint/muscle pain.
Sibutramine can substantially increase blood pressure and pulse in some patients. Therefore all patients treated with sibutramine should have regular monitoring of blood pressure and pulse.
The following side effects are infrequent but serious and require immediate medical attention: cardiac arrhythmias, paresthesia, mental/mood changes (e.g., excitement, restlessness, confusion, depression, rare thoughts of suicide).
Symptoms that require urgent medical attention are seizures, problems urinating, abnormal bruising or bleeding, melena, hematemesis, jaundice, fever and rigors, chest pain, hemiplegia, abnormal vision, dyspnea and edema.
Currently, no case of pulmonary hypertension has been noted, although related compounds (such as Fen-Phen) have shown this rare but clinically significant problem.

Metronidazole




Metronidazole (INN) (pronounced /mɛtrəˈnaɪdəzoʊl/) is a nitroimidazole anti-infective medication used mainly in the treatment of infections caused by susceptible organisms, particularly anaerobic bacteria and protozoa. It is marketed by Pfizer under the trade name Flagyl in the US, while Sanofi-Aventis markets metronidazole globally under the same tradename, Flagyl, and also by various generic manufacturers, who sell it at a lower price.
Metronidazole is also used as a gel preparation in the treatment of the dermatological conditions such as rosacea (Rozex and MetroGel by Galderma) and fungating tumours (Anabact, Cambridge Healthcare Supplies).




Latest paper studying Metronidazole found "Metronidazole therapy before 32 weeks was associated with an increased risk of preterm birth", possibly as a result of "changes in the vaginal flora... seen with vaginal clindamycin or oral metronidazole therapy." [4]
Metronidazole has also been used in women to prevent preterm birth associated with bacterial vaginosis, amongst other risk factors including the presence of cervicovaginal fetal fibronectin (fFN). A randomised controlled trial demonstrated that metronidazole was ineffective in preventing preterm delivery in high-risk pregnant women and, conversely, the incidence of preterm delivery was actually higher in women treated with metronidazole.[5]
Lamont has argued that Metronidazole is not the right antibiotic to administer in these circumstances and was often administered too late to be of use. Clindamycin administered early in the second trimester to women who test positive for bacterial vaginosis seems to be more effective.[6]

Sunday, March 22, 2009

Gaviscon


Gaviscon is a non-prescription medication for the treatment of heartburn and GERD/(also known as GORD) (acid reflux). It is produced and distributed in the UK by Reckitt Benckiser and by GlaxoSmithKline in the US and Canada.
Gaviscon is taken to treat heartburn, similar to other antacids. Gaviscon is based on a mixture of the buffering agents and neutralizers calcium carbonate and sodium bicarbonate, the laxative magnesium carbonate and the gelling agents alginic acid and aluminium hydroxide. When taken by mouth the combination of the alginic acid and bicarbonate creates a barrier which prevents stomach acid from refluxing back up into the esophagus.
If reflux occurs, this protective barrier is the first to contact the esophageal mucosa, in lieu of gastric contents.
The Gaviscon infant variant for infants (≥ 1 years) and young children contains only the gelling agents sodium alginate and magnesium alginate. It is used to help stabilize the stomach contents and reduce reflux and regurgitation, but is not an antacid.

Lactulose


Lactulose (IPA: ˈlæktjʊləʊz) is a synthetic sugar used in the treatment of constipation[1] and hepatic encephalopathy, a complication of liver disease. It is a disaccharide (double-sugar) formed from one molecule each of the simple sugars (monosaccharides) fructose and galactose. The commercial syrup used for treatment of constipation is dyed yellow-orange. It is produced commercially by isomerization of lactose.

In the treatment of chronic constipation[2], the metabolites of lactulose draw water into the bowel, causing a cathartic effect through osmotic action. Unlike other laxatives that are recommended for temporary relief, lactulose can be taken daily for decades. [1] It is safe for people of all ages, except for those in a very small percentage of the population that are galactose intolerant. Dosage may have to be adjusted over time to produce the desired effect.

Phloroglucinol

Phloroglucinol is the organic compound that is used in the synthesis. This molecule exists in two forms, or tautomers, 1,3,5-trihydroxybenzene, which has phenol-like, and 1,3,5--cyclohexanetrione, which has ketone-like character. These two tautomers are in equilibrium. Phloroglucinol is a useful intermediate because it is polyfunctional.
From water, phloroglucinol crystallizes as the dihydrate, which has a melting point of 116-117 °C, but the anhydrous form melts much higher, at 218-220 °C. It does not boil intact, but it does sublime.

Meclizine


Meclizine (proposed INN is meclozine) is an antihistamine considered to be an antiemetic.[1] It is sold under the brand names of Bonine, Bonamine, Antivert and Postafen and is most commonly used to inhibit nausea and vomiting. Emesafene is a combination of meclizine (1/3rd) and pyridoxine (2/3rd). An alternative to dimenhydrinate (Dramamine), meclizine is considered to be equally effective, but with reduced side effects. Note that in Canada, Antivert (no longer available) was a combination of meclizine and nicotinic acid.
Meclizine is a first-generation antihistamine of the piperazine class. It differs from the protoype of this class, cyclizine, primarily in having a 12-hour duration of action.[citation needed] Meclizine is less anticholinergic than many other antihistamines and other agents used for their anti-emetic and anti-pruritic effects.[citation needed]Along with the aforementioned efficacy against nausea and itching, meclizine also shares the anxiolytic, analgesic-sparing (potentiating), sedative, and other effects of its chemical relatives cyclizine and hydroxyzine to varying extents.[citation needed] Related to this is the reported ability of meclizine to potentiate the anti-spasmodic, anti-diarrhoeal, and other effects of diphenoxylate, loperamide, and difenoxin.[citation needed]

Domperidone


Domperidone (trade names Motilium, Motillium, Motinorm and Costi) is an antidopaminergic drug, developed by Janssen Pharmaceutica, and used orally, rectally or intravenously, generally to suppress nausea and vomiting. It has also been used to stimulate lactation.

Domperidone is used, together with metoclopramide, cyclizine, and 5HT3 receptor antagonists (such as granisetron) in the treatment of nausea and vomiting.
Domperidone has also been found effective in the treatment of gastroparesis,[2] a stomach motility condition, and for paediatric Gastroesophageal reflux (infant vomiting).

There is some evidence that domperidone has antiemetic activity.[7]
Domperidone is a first choice anti-emetic in most countries,[citation needed] together with metoclopramide. It is however not approved for prescription in the US. Although it has never been officially approved for use in the United States, domperidone is sometimes purchased from pharmacies in other countries for this purpose.

Loperamide


Loperamide, a synthetic piperidine derivative,[3] is a drug effective against diarrhea resulting from gastroenteritis or inflammatory bowel disease. In most countries it is available generically and under brand names such as Lopex, Imodium, Dimor and Pepto Diarrhea Control. It was discovered at Janssen Pharmaceutica in 1969.

Loperamide is an opioid receptor agonist and acts on the μ-opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids.
It works by decreasing the activity of the myenteric plexus, which decreases the motility of the circular and longitudinal smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.[4]
Loperamide molecules do not cross the blood-brain barrier in significant amounts, and, thus, it has no analgesic properties. Any that do cross the blood-brain barrier are quickly exported from the brain by P-glycoprotein (Pgp), also known as multidrug resistance protein (MDR1). Tolerance in response to long-term use has not been reported.
However, loperamide can cause physical dependence. Symptoms of opiate withdrawal have been observed in patients abruptly discontinuing long-term therapy with loperamide. For this reason, the drug was briefly classified as a Schedule V controlled substance upon its introduction.[citation needed]

Mebendazole


Mebendazole or MBZ, marketed as Ovex, Vermox, Antiox, is a benzimidazole drug that is used to treat infestations by worms including pinworms, roundworms, tapeworms, hookworms, and whipworms.

Oral dosage is 100 mg per dose, two doses per day, for three days. This regime is repeated two weeks later if the infection has not cleared up. The dosage may differ depending on which type of worm someone is infected with.

sylimarine


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Pantoprazole


Pantoprazole (Sold as Pantotab; Pantopan; Protium; Protonix; Pantozol; Pantor; Pantoloc; Astropan; Controloc; Pantecta; Inipomp; Ulcepraz) is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease. Initial treatment is generally of eight weeks' duration, after which another eight week course of treatment may be considered if necessary. It can be used as a maintenance therapy for long term use after initial response is obtained. This medication may affect the results of certain lab tests (e.g. false positive urine screen for tetrahydrocannabinal-THC). It is recommended you make sure laboratory personnel and your doctor know you are using this drug. The active ingredient in PROTONIX (pantoprazole sodium) Delayed-Release Tablets is a substituted benzimidazole , sodium 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)methyl] sulfinyl]-1 H -benzimidazole sesquihydrate, a compound that inhibits gastric acid secretion.

Pantoprazole is metabolized in the liver by the cytochrome P450 system. Metabolism mainly consists of demethylation by CYP2C19 followed by sulfation. Another metabolic pathway is oxidation by CYP3A4. Pantoprazole metabolites are not thought to have any pharmacological significance. Pantoprazole is relatively free of drug interactions, however it may alter the absorption of other medications that depend on the amount of acid in the stomach, such as ketoconazole or digoxin.

Tuesday, March 17, 2009

Mebeverine


Mebeverine HCI is a musculotropic antispasmodic drug without atropic side-effects whose major therapeutic role is in the treatment of irritable bowel syndrome. It is also indicated for treatment of gastrointestinal spasm secondary to organic disorder. It was first registered in 1965 and manufacture by rameda Pharmaceuticals.
Mebeverine HCI presented in tablets (100mg) tablet

Mebeverine is an antimuscarinic. Mebeverine HCI belongs to a group of compounds called musculotropic antispasmodics. These compounds act directly on the gut muscles at the cellular level to relax them. Mebeverine is also an inhibitor of calcium-depot replenishment. Therefore, mebeverine has dual mode of action which normalizes the small bowel motility

Ranitidine


Ranitidine hydrochloride (INN) (pronounced /rəˈnɪtɨdiːn/) is a histamine H2-receptor antagonist that inhibits stomach acid production. It is commonly used in treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD). Ranitidine is also used alongside fexofenadine and other antihistamines for the treatment of skin conditions such as hives. Ranitidine is currently marketed under the brand name Zantac by GlaxoSmithKline and other brand names by various pharmaceutical companies.

Ranitidine increases absorption and decreases excretion of amphetamines. Ranitidine can also be taken separately with amphetamines based in sulphate (amphetamine sulphate) to increase its central effects and half-life.[2]
Ranitidine increases oral absorption of triazolam in both young and older people. This effect is likely caused by elevation of gastrointestinal pH, allowing for greater absorption of acid-labile triazolam. Ranitidine-Coadministration of ranitidine increased the maximum plasma concentration of triazolam by 30%, increased the area under the concentration curve by 27%, and increased half-life by 3.3%. Caution is recommended during coadministration with triazolam. Thus this co-administration can lead to an overdose of triazolam which can lead to somnolence, confusion, impaired coordination, coma and death.

Esomeprazole


Esomeprazole (pronounced /ɛsoʊˈmɛprəzoʊl/) is a proton pump inhibitor (brand names Sompraz, Zoleri, Nexium, Lucen, Esopral; Axagon in Italy, Nexiam in Belgium) developed and marketed by AstraZeneca which is used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and Zollinger-Ellison syndrome. Esomeprazole is the S-enantiomer of omeprazole (marketed as Losec/Prilosec), and AstraZeneca claims improved efficacy of this single enantiomer product over the racemic mixture of omeprazole. However, this greater efficacy has been disputed, with some claiming it offers no benefit from its older form. (see below). Esomeprazole was the third biggest selling pharmaceutical drug in the world for 2005, totaling US$ 5.7 billion in sales.[citation needed]

Esomeprazole is combined with the antibiotics clarithromycin and amoxicillin (or metronidazole) in the 7-day eradication triple therapy for Helicobacter pylori. Infection by H. pylori is the causative factor in the majority of peptic and duodenal ulcers.

Omeprazole


Omeprazole (INN) (pronounced /owˈmejprəzowl/) is a proton pump inhibitor used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and Zollinger-Ellison syndrome. It was first marketed in the US in 1989 by AstraZeneca as the magnesium salt omeprazole magnesium under the brand names Losec and Prilosec, and is now also available from generic manufacturers under various brand names. Omeprazole is one of the most widely prescribed drugs internationally and is available over the counter in some countries.

As with all proton pump inhibitors, omeprazole is generally well tolerated. Some of the most frequent side effects of omeprazole (experienced by over 1% of those taking the drug) are headache, diarrhea, abdominal pain, nausea, dizziness, trouble awakening and sleep deprivation, although in clinical trials the incidence of these effects with omeprazole was mostly comparable to that found with placebo.[2]
Proton pump inhibitors may be associated with a greater risk of hip fractures [3], clostridium difficile diarrhea[4] and heart problems, including cardiac arrest.

Patients who are taking Plavix in combination with proton pump inhibiting drugs may be at a greater risk of stroke or heart attack

Wednesday, March 11, 2009

Tramadol


Tramadol (INN) (pronounced /ˈtræmədɒl/) is a CNS depressant and analgesic, used for treating moderate to severe pain. It is a synthetic agent, and it appears to have actions at the μ-opioid receptor as well as the noradrenergic and serotonergic systems.[1][2][3] Tramadol was developed by the German pharmaceutical company Grünenthal GmbH in the late 1970s and marketed under the trade name Tramal.[4] Grünenthal has also cross licensed the drug to many other pharmaceutical companies that market it under various names such as MEDTRAP(NEOMED) Ultram and ULTRAM® ER. Tramadol's chemical structure is quite different from those of opiates. The closest chemical relative of tramadol in clinical use is tapentadol, which is a member of the same chemical class as tramadol and also developed by Grünethal.

Tramadol is in FDA pregnancy category C; animal studies have shown its use to be dangerous during pregnancy and human studies are lacking. Therefore, the drug should not be taken by women who are pregnant unless "the potential benefits outweigh the risks".[24]
Tramadol causes serious or fatal[citation needed] side effects in a newborn, including neonatal withdrawal syndrome, if the mother uses the medication during pregnancy or labor. Use of tramadol by nursing mothers is not recommended by the manufacturer because the drug passes into breast milk.[24] However, the absolute dose excreted in milk is quite low, and tramadol is generally considered to be acceptable for use in breastfeeding mothers.[25]

Celecoxib


Celecoxib (INN) (pronounced /sɛlɨˈkɒksɪb/) is a non-steroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis. It is marketed by Pfizer. It has the brand name Celebrex and Celebra (in other countries) for arthritis and Onsenal for polyps. Celecoxib is available by prescription in capsule form.

Celecoxib is licensed for use in osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce the number of colon and rectal polyps in patients with familial adenomatous polyposis. It was originally intended to relieve pain while minimizing the gastrointestinal adverse effects usually seen with conventional NSAIDs. In practice, its primary indication is in patients who need regular and long term pain relief: there is probably no advantage to using celecoxib for short term or acute pain relief over conventional NSAIDs. In addition, the pain relief offered by celecoxib is similar to that offered by paracetamol.[1]

Pregabalin


Pregabalin (INN) (pronounced /prɨˈgæbəlɨn/) is an anticonvulsant drug used for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults.[1] It has also been found effective for generalized anxiety disorder and is (as of 2007) approved for this use in Europe.[1] It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade name Lyrica.
Recent studies have shown that pregabalin is effective at treating chronic pain in disorders such as fibromyalgia[2] and spinal cord injury.[3] In June 2007, pregabalin became the first medication approved by the U.S. Food and Drug Administration specifically for the treatment of fibromyalgia.[4]
It is considered to have a low potential for abuse, and a limited dependence liability if misused, and is thus classified as a Schedule V drug in the U.S.[5]

Nerve Pain after Herpes, Diabetic Complication causing Injury to some Body Nerves, Additional Medication to Treat Partial Seizures, Disorder characterized by Stiff, Tender & Painful Muscles. Lyrica Oral may also be used to treat Neuropathic Pain. This medication is used to treat pain caused by nerve damage due to diabetes and shingles (herpes zoster) infection. It is also used to treat pain in people with fibromyalgia. It is also used with other medications to treat certain types of seizures (partial onset seizures).
Pregabalin is indicated for:
Treatment of neuropathic pain from diabetic neuropathy or post herpetic neuralgia. There is not enough data to state that it should be used in all neuropathic pain.
Adjunctive therapy in adults with partial seizures with or without secondary generalization
Fibromyalgia pain
Generalized anxiety disorder (approved in the European Union).[8]

Monday, March 9, 2009

Raloxifene


Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women. It was announced on April 17, 2006, that raloxifene is as effective as tamoxifen in reducing the incidence of breast cancer in certain high risk groups of females, [1] though with a reduced risk of thromboembolic events and cataracts in patients taking raloxifene versus those taking tamoxifen.[1] On September 14, 2007, the U.S. Food and Drug Administration announced approval of raloxifene for reducing the risk of invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer.[2]
There has been criticism in the mainstream oncology press of the way that information about the drug was released.[3] There has been some confusion in the lay media about the meaning of the trial results. There is no specific clinical evidence for the use of raloxifene in the adjuvant treatment of breast cancer over established drugs such as tamoxifen or anastrozole.[citation needed]

Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women, for reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate.

Gabapentin


Gabapentin (brand name Neurontin) is a GABA analogue. It was originally developed for the treatment of epilepsy, and currently, gabapentin is widely used to relieve pain, especially neuropathic pain.
Gabapentin was initially synthesized to mimic the chemical structure of the neurotransmitter gamma-aminobutyric acid (GABA), but is not believed to act on the same brain receptors.
Its exact mechanism of action is unknown, but its therapeutic action on neuropathic pain is thought to involve voltage-gated N-type calcium ion channels. It is thought to bind to the α2δ subunit (1 and 2)[2] of the voltage-dependent calcium channel in the central nervous system.[3]

Gabapentin should not be discontinued abruptly after long term use. Abrupt or over rapid withdrawal may provoke a withdrawal syndrome similar to alcohol or benzodiazepine withdrawal. Gradual reduction over a period of weeks or months helps minimise or prevents the withdrawal syndrome.[17]

Tizanidine

Tizanidine (brandnames Zanaflex, Sirdalud) is a drug which is used as a muscle relaxant. It is a centrally acting α-2 adrenergic agonist. It is used to treat the spasms, cramping, and tightness of muscles caused by medical problems such as multiple sclerosis, spastic diplegia, back pain, or certain other injuries to the spine or central nervous system. It is also prescribed off-label as a sleep aid, seizure inhibitor, and for some symptoms of fibromyalgia[1].
Tizanidine may cause hypotension so caution is advised when it is used in patients who have a history of orthostatic hypotension.
Tizanidine can come in tablets with "cor 138" on one side and 2 scores on the back that create an X, or R179 on one side and a single score through the middle of the back, or a white oval pill with R180 on one side and 2 scores on the back that create an X. It's also found as a circular white pill with the number 503 on one side and X-scored on the back[2].
It is supplied as 2 and 4 mg tablets for oral administration, and in gel cap form in doses of 2mg, 4mg, and 6mg.
The tablets are composed of the active ingredient, tizanidine hydrochloride (2.288 mg equivalent to 2 mg tizanidine base and 4.576 mg equivalent to 4 mg tizanidine base), and the inactive ingredients, silicon dioxide colloidal, stearic acid, microcrystalline cellulose and anhydrous lactose.

Thursday, March 5, 2009

Flurbiprofen


Flurbiprofen is a member of the phenylalkanoic acid derivative family of non-steroidal anti-inflammatory drugs (NSAIDs) used to treat the inflammation and pain of arthritis. It is known by the following tradenames: Ansaid, marketed by Pfizer, and Froben, by Abbott. Flurbiprofen is also used as an active ingredient in some kinds of throat lozenges.
The single enantiomer of racemate flurbiprofen, tarenflurbil (R-flurbiprofen), is currently in clinical trials for the treatment of metastatic prostate cancer.

Naproxen


Naproxen (INN) (pronounced /nəˈprɒksən/) is a non-steroidal anti-inflammatory drug (NSAID) commonly used for the reduction of moderate to severe pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes. Naproxen and naproxen sodium are marketed under various trade names including: Xenobid, Aleve, Anaprox, Miranax, Naprogesic, Naprosyn, Naprelan, Proxen, Synflex.
Naproxen was originally marketed as the prescription drug Naprosyn in 1976, and naproxen sodium was first marketed under the trade name Anaprox in 1980. It remains a prescription-only drug in much of the world. The U.S. Food and Drug Administration (FDA) approved the use of naproxen sodium as an over-the-counter (OTC) drug in 1994, where OTC preparations are sold under the trade name Aleve. In Australia, small packets of lower-strength preparations of naproxen sodium are Schedule 2 Pharmacy Medicines. In the UK, 250mg tablets of naproxen were approved for OTC sale under the brand name Feminax Ultra in 2008, for the treatment of primary dysmenorrhoea in women aged 15 to 50.[1]

Diclofenac


Diclofenac (marketed as Flector patch, Voltaren, Voltarol, Diclon, Dicloflex Difen, Difene, Cataflam, Pennsaid, Panamor, Rhumalgan, Modifenac, Abitren, Olfen, Voveran, Arthrotec, Dedolor, Deflamat, Vetagesic and Zolterol, with various drug dose combinations) is a non-steroidal anti-inflammatory drug (NSAID) taken to reduce inflammation and as an analgesic reducing pain in conditions such as arthritis or acute injury. It can also be used to reduce menstrual pain, dysmenorrhea. The name is derived from its chemical name: 2-(2,6-dichloranilino) phenylacetic acid
In the United Kingdom, India, and the United States, it may be supplied as either the sodium or potassium salt, in China most often as the sodium salt, while in some other countries only as the potassium salt. Diclofenac is available as a generic drug in a number of formulations. Over the counter (OTC) use is approved in some countries for minor aches and pains and fever associated with common infections.
Diclofenac is used for musculoskeletal complaints, especially arthritis (rheumatoid arthritis, osteoarthritis, spondylarthritis, ankylosing spondylitis), gout attacks, and pain management in case of kidney stones and gallstones. An additional indication is the treatment of acute migraines. Diclofenac is used commonly to treat mild to moderate post-operative or post-traumatic pain, particularly when inflammation is also present, and is effective against menstrual pain.

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