So just what IS restless leg syndrome? I've always thought it was just stress manifesting itself in the middle of the night and a brief stroll around the bedroom or a good stretch and it goes away. Apparently, it's way more prevalent in the U.S. and several new drugs for treatment have recently been approved by the FDA. Now for a medical definition:
Restless legs syndrome (RLS) is a neurological disorder characterized by unpleasant sensations in the legs and an uncontrollable urge to move when at rest in an effort to relieve these feelings. RLS sensations are often described by people as burning, creeping, tugging, or like insects crawling inside the legs. Often called paresthesias (abnormal sensations) or dysesthesias (unpleasant abnormal sensations), the sensations range in severity from uncomfortable to irritating to painful.
The most distinctive or unusual aspect of the condition is that lying down and trying to relax activates the symptoms. As a result, most people with RLS have difficulty falling asleep and staying asleep. Left untreated, the condition causes exhaustion and daytime fatigue. Many people with RLS report that their job, personal relations, and activities of daily living are strongly affected as a result of their exhaustion. They are often unable to concentrate, have impaired memory, or fail to accomplish daily tasks.
Current treatment involves dopamine agonist treatment. One such drug is Requip, drug name ropinirole. In 2005, requip became the only drug approved by the U.S. Food and Drug Administration specifically for the treatment of moderate to severe RLS. The drug was first approved in 1997 for patients with Parkinson’s disease. Requip stimulates D2 and D3 type dopamine receptors, to stimulate motor neuron firing (activity-or signaling). The specific mechanism of action for the indication of both Parkinson's and RLS are unknown.
The side effects of ropinirole are interesting to say the least. It has been reported that dopamine receptor agonists stimulate compulsive gambling ( NEUROLOGY 2007;68:301–303). Three subjects were followed from either never gambled or 1-2 visits to a casino to visiting a casino 3-4 times a week and losing up to several hundred thousand dollars. One possible mechanism of action is the stimulation of D3 receptors, the highest concentration of which is found in the mesolimbic pathways [in the brain, centers for controlling the following functions] implicated in motivation, emotion, and reward behaviors, which could lead to the development of pathologic
gambling.
I can understand the "reward" part of the gamble--USC 2nd half football games the last 2 years have paid rents. Just goes to show how pharmacological manipulation of brain function can have drastic effects.
Wednesday, September 19, 2007
Coming tomorrow....Dopamine agonists and getting down on some ACTION!
a tease:
Compulsive gambling with extreme losses -- in two cases, greater than $100,000 -- by people without a prior history of gambling problems has been linked to a class of drugs commonly used to treat the neurological disorder restless legs syndrome (RLS). A new Mayo Clinic study is the first to describe this compulsive gambling in RLS patients who are being treated with medications that stimulate dopamine receptors in the brain.
Mechanism of action and my interpretation tomorrow (later today).....
Compulsive gambling with extreme losses -- in two cases, greater than $100,000 -- by people without a prior history of gambling problems has been linked to a class of drugs commonly used to treat the neurological disorder restless legs syndrome (RLS). A new Mayo Clinic study is the first to describe this compulsive gambling in RLS patients who are being treated with medications that stimulate dopamine receptors in the brain.
Mechanism of action and my interpretation tomorrow (later today).....
Wednesday, May 23, 2007
Researchers are reporting a potential "cure" for hepatitis C,
Use of the drug peginterferon, either alone or in combination with the drug ribavirin, reduced levels of the virus to undetectable levels for up to seven years, the researchers said.
"This paper strongly suggests, for the first time, that hepatitis C is a curable disease," said lead researcher Dr. Mitchell Shiffman, a professor at Virginia Commonwealth University School of Medicine and chief of hepatology and medical director of the school's Liver Transplant Program. "After treatment, 99.6 percent of the patients remained virus undetectable for over five years," he added.
In the study, 997 patients with hepatitis C or with both hepatitis C and
HIV' were treated with either Pegasys (peginterferon alfa-2a) alone or in tandem with ribavirin. Shiffman's team then monitored blood levels of hepatitis C once a year for an average of 4.1 years, and as long as seven years.
The researchers found that 99 percent of patients with hepatitis C who were treated successfully with peginterferon alone, or in combination with ribavirin, had no detectable virus up to seven years later.
"This is the first long-term study that confirms what we believed for many years that these individuals are truly cured of hepatitis C," Shiffman said.
The remaining eight patients tested positive for hepatitis C at an average of two years after treatment. There was no pattern to the patients as far as age, gender or hepatitis C genotype. It isn't known whether these patients had a relapse or were re-infected with the virus, the researchers noted.
The findings were to be presented Monday at the 38th annual Digestive Disease Week conference, in Washington, D.C.
Hepatitis C is a blood-borne infectious disease of the liver and is one of the most important causes of chronic liver disease in the United States. An estimated 4.1 million Americans have been infected with hepatitis C, and 3.2 million are chronically infected. The number of new infections each year declined from an average of 240,000 in the 1980s to about 26,000 in 2004, the latest year for which statistics are available. The number of hepatitis C-related deaths could increase to 38,000 a year by the year 2010, surpassing annual HIV deaths, according to the U.S. Centers for Disease Control and Prevention.
The virus is usually spread through contact with infected blood and blood products. Blood transfusions and the use of shared, unsterilized, or poorly sterilized needles, syringes and injection equipment have been the main routes of transmission in the United States, according to the National Institutes of Health.
Most people who have hepatitis C don't know they have it, Shiffman said. "Of those who have been diagnosed, only about 25 percent have received treatment, because of the side effects of treatment," he said. "The reason why you should treat it is because you can cure hepatitis C, and we finally have the data to definitively document it."
Dr. Eugene Schiff, chief of the division of hepatology and professor of medicine at the University of Miami Miller School of Medicine, agrees that most cases of hepatitis C can be cured.
"In contrast to hepatitis B or HIV, this virus can be totally eradicated and cured," he said.
But, many patients find the side effects of treatment off-putting. Those side effects can include fever and chills, Shiff said. "You feel pretty lousy. After treatment starts, you feel worse the day after your shot, but it tapers off over the course of the week," he said. "Along with that anxiety, irritability and depression can develop. And we are quick to use antidepressants to allow these people to stay on the medication."
Additional side effects include a drop in the production of white blood cells and anemia. Often patients are giving additional drugs to combat these conditions, Shiff said.
Treatments can go on for as many as 72 weeks, depending on the reaction to therapy Shiff said. "Some people are reluctant to get treatment, because they heard that the treatment isn't so pleasant," he said. "But they should come out and get treatment."
Schiff noted that new antiviral drugs to treat hepatitis C are being tested. "It is hoped that these new antivirals will be more effective and have less severe side effects and may even be used without peginterferon alfa-2a or ribavirin," he said.
UMMM--Going to have to call BS on this one. The authors must be in dire need of NIH funding to be making such bold observations. The fact IS, that >60% of patients of HCV infection are already resistant to both therapies. This data is not anything new in the HCV field. The "new" drugs that are being investigated beyond PEG-interferon and nucleoside polymerase inhibitors are very promising however. TLR agonists are coming of age as potent immune stimulators as well as combination cytokine therapy.
"This paper strongly suggests, for the first time, that hepatitis C is a curable disease," said lead researcher Dr. Mitchell Shiffman, a professor at Virginia Commonwealth University School of Medicine and chief of hepatology and medical director of the school's Liver Transplant Program. "After treatment, 99.6 percent of the patients remained virus undetectable for over five years," he added.
In the study, 997 patients with hepatitis C or with both hepatitis C and
HIV' were treated with either Pegasys (peginterferon alfa-2a) alone or in tandem with ribavirin. Shiffman's team then monitored blood levels of hepatitis C once a year for an average of 4.1 years, and as long as seven years.
The researchers found that 99 percent of patients with hepatitis C who were treated successfully with peginterferon alone, or in combination with ribavirin, had no detectable virus up to seven years later.
"This is the first long-term study that confirms what we believed for many years that these individuals are truly cured of hepatitis C," Shiffman said.
The remaining eight patients tested positive for hepatitis C at an average of two years after treatment. There was no pattern to the patients as far as age, gender or hepatitis C genotype. It isn't known whether these patients had a relapse or were re-infected with the virus, the researchers noted.
The findings were to be presented Monday at the 38th annual Digestive Disease Week conference, in Washington, D.C.
Hepatitis C is a blood-borne infectious disease of the liver and is one of the most important causes of chronic liver disease in the United States. An estimated 4.1 million Americans have been infected with hepatitis C, and 3.2 million are chronically infected. The number of new infections each year declined from an average of 240,000 in the 1980s to about 26,000 in 2004, the latest year for which statistics are available. The number of hepatitis C-related deaths could increase to 38,000 a year by the year 2010, surpassing annual HIV deaths, according to the U.S. Centers for Disease Control and Prevention.
The virus is usually spread through contact with infected blood and blood products. Blood transfusions and the use of shared, unsterilized, or poorly sterilized needles, syringes and injection equipment have been the main routes of transmission in the United States, according to the National Institutes of Health.
Most people who have hepatitis C don't know they have it, Shiffman said. "Of those who have been diagnosed, only about 25 percent have received treatment, because of the side effects of treatment," he said. "The reason why you should treat it is because you can cure hepatitis C, and we finally have the data to definitively document it."
Dr. Eugene Schiff, chief of the division of hepatology and professor of medicine at the University of Miami Miller School of Medicine, agrees that most cases of hepatitis C can be cured.
"In contrast to hepatitis B or HIV, this virus can be totally eradicated and cured," he said.
But, many patients find the side effects of treatment off-putting. Those side effects can include fever and chills, Shiff said. "You feel pretty lousy. After treatment starts, you feel worse the day after your shot, but it tapers off over the course of the week," he said. "Along with that anxiety, irritability and depression can develop. And we are quick to use antidepressants to allow these people to stay on the medication."
Additional side effects include a drop in the production of white blood cells and anemia. Often patients are giving additional drugs to combat these conditions, Shiff said.
Treatments can go on for as many as 72 weeks, depending on the reaction to therapy Shiff said. "Some people are reluctant to get treatment, because they heard that the treatment isn't so pleasant," he said. "But they should come out and get treatment."
Schiff noted that new antiviral drugs to treat hepatitis C are being tested. "It is hoped that these new antivirals will be more effective and have less severe side effects and may even be used without peginterferon alfa-2a or ribavirin," he said.
UMMM--Going to have to call BS on this one. The authors must be in dire need of NIH funding to be making such bold observations. The fact IS, that >60% of patients of HCV infection are already resistant to both therapies. This data is not anything new in the HCV field. The "new" drugs that are being investigated beyond PEG-interferon and nucleoside polymerase inhibitors are very promising however. TLR agonists are coming of age as potent immune stimulators as well as combination cytokine therapy.
Monday, May 21, 2007
FDA Issues Safety Alert on Diabetes Drug
Diabetes Drug Avandia Raises Risk of Heart Attack, Study Suggests; FDA Issues Safety Alert
The widely prescribed diabetes drug Avandia is linked to a greater risk of heart attack and possibly death, a new scientific analysis revealed, and the U.S. government issued a safety alert Monday.
The Food and Drug Administration urged diabetics taking the pill to talk to their doctors, but stopped short of forcing a sharper warning label on the drug sold by GlaxoSmithKline PLC of London.
More than 6 million people worldwide have taken the drug since it came on the market eight years ago. Pooled results of dozens of studies revealed a 43 percent higher risk of heart attack, according to the review published by the New England Journal of Medicine.
Experts said the overall risk was small and cautioned people not to stop taking the drug on their own but to talk to their doctors.
The company downplayed the report of heart risks, saying the analysis by Dr. Steven Nissen and statistician Kathy Wolski at the Cleveland Clinic is not definitive scientific proof. In a conference call Monday, Dr. Lawson McCartney who leads Glaxo's diabetes drug development, said the company is not seeing "anything like" the problems reported in the medical journal.
"We remain very confident in the safety and of course in the efficacy of Avandia as an important diabetic medicine," McCartney said.
The government will take no immediate action on a label change or other measures regarding the drug, said Dr. Robert J. Meyer of the FDA's Center for Drug Evaluation and Research.
Some data suggests "that there is a potentially significant increase in the risk" but there also is risk if patients switch drugs or do not keep their blood-sugar under control, an FDA statement says.
FDA officials acknowledged that Glaxo submitted information last August indicating some increased risk from the drug but that other studies were contradictory. However, several members of Congress expressed alarm and said they would hold hearings on the safety issues.
Avandia is used to treat Type 2 diabetes, the most common form of the disease, which is linked to obesity and afflicts 18 million Americans and 200 million people worldwide. This form of diabetes occurs when the body does not make enough insulin or cannot effectively use what it manages to produce.
Avandia helps sensitize the body to insulin and was considered a breakthrough medication for blood-sugar control.
Worried patients should not quit Avandia on their own and should discuss concerns with their doctors, wrote Drs. Bruce Psaty and Curt Furberg in an editorial in the New England Journal. Psaty is with the University of Washington in Seattle and Furberg is with Wake Forest University.
However, to the extent that the new analysis shows valid risks, the drug "represents a major failure of the drug-use and drug-approval processes in the United States," they said.
When the drug was approved, "evidence was at best mixed" on its benefit, wrote the two doctors. Both have been frequent critics of the FDA's failure to spot dangers in the drug approval process and its conduct in the case involving Vioxx. The popular arthritis medicine sold by Merck & Co. was taken off the market in 2004 when heart problems came to light after it had been taken by millions of people
Several experts said Avandia was another example of the FDA failing to detect a safety problem early enough.
Glaxo's shares trading in the United States fell $3.85, or 6.6 percent, to $53.89 in afternoon trading.
The report on the diabetes drug's risks follow Glaxo's $2.5 million settlement of a lawsuit filed by former New York Attorney General Eliot Spitzer over the release of data on the safety and effectiveness of its drugs. Spitzer, now New York governor, accused Glaxo of fraudulently withholding some results of studies that had examined the safety of prescribing the antidepressant Paxil to children.
The widely prescribed diabetes drug Avandia is linked to a greater risk of heart attack and possibly death, a new scientific analysis revealed, and the U.S. government issued a safety alert Monday.
The Food and Drug Administration urged diabetics taking the pill to talk to their doctors, but stopped short of forcing a sharper warning label on the drug sold by GlaxoSmithKline PLC of London.
More than 6 million people worldwide have taken the drug since it came on the market eight years ago. Pooled results of dozens of studies revealed a 43 percent higher risk of heart attack, according to the review published by the New England Journal of Medicine.
Experts said the overall risk was small and cautioned people not to stop taking the drug on their own but to talk to their doctors.
The company downplayed the report of heart risks, saying the analysis by Dr. Steven Nissen and statistician Kathy Wolski at the Cleveland Clinic is not definitive scientific proof. In a conference call Monday, Dr. Lawson McCartney who leads Glaxo's diabetes drug development, said the company is not seeing "anything like" the problems reported in the medical journal.
"We remain very confident in the safety and of course in the efficacy of Avandia as an important diabetic medicine," McCartney said.
The government will take no immediate action on a label change or other measures regarding the drug, said Dr. Robert J. Meyer of the FDA's Center for Drug Evaluation and Research.
Some data suggests "that there is a potentially significant increase in the risk" but there also is risk if patients switch drugs or do not keep their blood-sugar under control, an FDA statement says.
FDA officials acknowledged that Glaxo submitted information last August indicating some increased risk from the drug but that other studies were contradictory. However, several members of Congress expressed alarm and said they would hold hearings on the safety issues.
Avandia is used to treat Type 2 diabetes, the most common form of the disease, which is linked to obesity and afflicts 18 million Americans and 200 million people worldwide. This form of diabetes occurs when the body does not make enough insulin or cannot effectively use what it manages to produce.
Avandia helps sensitize the body to insulin and was considered a breakthrough medication for blood-sugar control.
Worried patients should not quit Avandia on their own and should discuss concerns with their doctors, wrote Drs. Bruce Psaty and Curt Furberg in an editorial in the New England Journal. Psaty is with the University of Washington in Seattle and Furberg is with Wake Forest University.
However, to the extent that the new analysis shows valid risks, the drug "represents a major failure of the drug-use and drug-approval processes in the United States," they said.
When the drug was approved, "evidence was at best mixed" on its benefit, wrote the two doctors. Both have been frequent critics of the FDA's failure to spot dangers in the drug approval process and its conduct in the case involving Vioxx. The popular arthritis medicine sold by Merck & Co. was taken off the market in 2004 when heart problems came to light after it had been taken by millions of people
Several experts said Avandia was another example of the FDA failing to detect a safety problem early enough.
Glaxo's shares trading in the United States fell $3.85, or 6.6 percent, to $53.89 in afternoon trading.
The report on the diabetes drug's risks follow Glaxo's $2.5 million settlement of a lawsuit filed by former New York Attorney General Eliot Spitzer over the release of data on the safety and effectiveness of its drugs. Spitzer, now New York governor, accused Glaxo of fraudulently withholding some results of studies that had examined the safety of prescribing the antidepressant Paxil to children.
Wednesday, May 16, 2007
Thursday, April 5, 2007
US aims to tighten rules on direct-to-consumer drug ads
With a new Congress controlled by the Democratic Party, the US biotech industry might be facing tighter restrictions on direct-to-consumer (DTC) advertising. This spring, Congress is set to debate measures that include a two-year moratorium on advertising for newly approved products and higher user fees for extra Food and Drug Administration (FDA) staff to monitor television, print and radio advertisements.
The US and New Zealand are the only countries that allow DTC drug advertising, and such ads pumped $4.5 billion into the US media economy in 2006, up from $2.8 billion in 2002, according to the drug and biotech industries.
However, over the past several years—and after the spectacular safety failure in 2004 of a heavily advertised and top-selling drug, the COX-2 inhibitor Vioxx (rofecoxib)—calls have grown louder for more government control.
"The ads have limited educational value and may oversell the benefits of drugs in ways that might conflict with promoting...health," says Dominick Frosch, assistant professor of medicine at the University of California, Los Angeles (UCLA). In the January/February issue of the Annals of Family Medicine, Frosch and colleagues published an analysis of television drug ads, concluding that 95% of analyzed ads appealed to emotion and none mentioned lifestyle changes as an alternative to a pill.
The US and New Zealand are the only countries that allow DTC drug advertising, and such ads pumped $4.5 billion into the US media economy in 2006, up from $2.8 billion in 2002, according to the drug and biotech industries.
However, over the past several years—and after the spectacular safety failure in 2004 of a heavily advertised and top-selling drug, the COX-2 inhibitor Vioxx (rofecoxib)—calls have grown louder for more government control.
"The ads have limited educational value and may oversell the benefits of drugs in ways that might conflict with promoting...health," says Dominick Frosch, assistant professor of medicine at the University of California, Los Angeles (UCLA). In the January/February issue of the Annals of Family Medicine, Frosch and colleagues published an analysis of television drug ads, concluding that 95% of analyzed ads appealed to emotion and none mentioned lifestyle changes as an alternative to a pill.
Riding a bike in the desert: Flomax
Every male mammal will eventually present with symptoms of an enlarged prostate. Non cancerous prostate enlargement is termed benign prostatic hyperplasia (BPH) and is a common chronic disease, with the incidence of BPH increasing with age.
This enlargement causes partial blockage of the urethra which impedes urinary output and and may lead to obstructive and irritative symptoms. It is caused by enlarged cells and cells that grow to compensate the enlarged cells within the prostate. The growing cells are called smooth muscle cells and have specific receptors on their cell surface that can regulate their rigidness, such that when these receptors are inhibited, they relax. This results in increased flow.
Flomax blocks these receptors and causes increased urinary flow by relaxing enlarged/proliferating smooth muscle cells within the prostate.
This enlargement causes partial blockage of the urethra which impedes urinary output and and may lead to obstructive and irritative symptoms. It is caused by enlarged cells and cells that grow to compensate the enlarged cells within the prostate. The growing cells are called smooth muscle cells and have specific receptors on their cell surface that can regulate their rigidness, such that when these receptors are inhibited, they relax. This results in increased flow.
Flomax blocks these receptors and causes increased urinary flow by relaxing enlarged/proliferating smooth muscle cells within the prostate.
Wednesday, April 4, 2007
In the news today: Combo migraine drug beat single drug therapy
An experimental drug that combines two commonly used treatments helped quell migraine symptoms better than either one alone, a new U.S. study released Tuesday suggested.
The research, published in this week's Journal of the American Medical Association, tested experimental drug combination Trexima against either drug used alone.
Pozen Inc. is developing Trexima with British drugmaker GlaxoSmithKline's. The drug combines Glaxo's popular migraine drug Imitrex -- known generically as sumatriptan -- with the older painkiller naproxen sodium.
The drug combo attacks different pathways in the brain believed to contribute to migraines, which affect more than 28 million people in the United States. Migraine symptoms include throbbing headache pain, nausea, vomiting and sensitivity to light and sound.
The multibillion-dollar market for prescription migraine drugs is dominated by a class know as triptans, of which Glaxo's Imitrex is the most widely used.
Source: CNN
Something like this can get fast tracked by the FDA and in patient use in a very short time. If you suffer from migraines, this is good news.
The research, published in this week's Journal of the American Medical Association, tested experimental drug combination Trexima against either drug used alone.
Pozen Inc. is developing Trexima with British drugmaker GlaxoSmithKline's. The drug combines Glaxo's popular migraine drug Imitrex -- known generically as sumatriptan -- with the older painkiller naproxen sodium.
The drug combo attacks different pathways in the brain believed to contribute to migraines, which affect more than 28 million people in the United States. Migraine symptoms include throbbing headache pain, nausea, vomiting and sensitivity to light and sound.
The multibillion-dollar market for prescription migraine drugs is dominated by a class know as triptans, of which Glaxo's Imitrex is the most widely used.
Source: CNN
Something like this can get fast tracked by the FDA and in patient use in a very short time. If you suffer from migraines, this is good news.
Tuesday, April 3, 2007
I'm getting sick of seeing Dr. Jarvick
I've posted lipitor but here's a reference to that post.
see thursday march 1st...
Flomax coming shortly.......
see thursday march 1st...
Flomax coming shortly.......
Monday, April 2, 2007
Is chemotherapy right for you? Ask about Neulasta
This ad just amazes me. "ask your doctor if chemotherapy is right for you" is basically what this says. Just how many people even know anything about their disease except what they are told and even those dont know what drugs they are getting or how they work. Rant over.
Back to Neulasta. What is it indicated for and how does it work so we can all understand?
Neulasta is a genetically engineered human protein [it's grown in the laboratory] that is the exact same as a protein in our body call G-CSF, for granulocyte colony stimulating factor. Simply, it's a cocktail of growth factors that tells specific cells of your immune system to grow. These cells are the body's primary defense system against opportunistic infections that often occur in chemotherapy patients. This is important since most chemotherapy is not specific to cancer cells in the body. It simply kills all cells, leaving a person suspect to infection; thus how the drug protects and helps a person.
Back to Neulasta. What is it indicated for and how does it work so we can all understand?
Neulasta is a genetically engineered human protein [it's grown in the laboratory] that is the exact same as a protein in our body call G-CSF, for granulocyte colony stimulating factor. Simply, it's a cocktail of growth factors that tells specific cells of your immune system to grow. These cells are the body's primary defense system against opportunistic infections that often occur in chemotherapy patients. This is important since most chemotherapy is not specific to cancer cells in the body. It simply kills all cells, leaving a person suspect to infection; thus how the drug protects and helps a person.
Monday, March 26, 2007
New drug posts coming soon...
I''m on vacation and internet access is limited--check back this afternoon, thanks!!!
Friday, March 16, 2007
It's my 10th day...Prilosec OTC
Marketed as the first 24 hour heartburn relief with one pill a day.
How does it work and how is it different from Nexium?
Prilosec OTC (omeprazole) is a delayed-release 20mg tablet, taken once a day (every 24 hours) for 14 days before eating. It is in the same class of drugs as Nexium, that is, it's a proton pump inhibitor, which stops acid secretion in the stomach. Gastric cells called parietal cells make acid and pump it into the lumen of the stomach. Prilosec works to slow down or stop the pump action. For more details, check out my post on Nexium.
AstraZeneca Pharmaceuticals makes Prilosec and Nexium.
How does it work and how is it different from Nexium?
Prilosec OTC (omeprazole) is a delayed-release 20mg tablet, taken once a day (every 24 hours) for 14 days before eating. It is in the same class of drugs as Nexium, that is, it's a proton pump inhibitor, which stops acid secretion in the stomach. Gastric cells called parietal cells make acid and pump it into the lumen of the stomach. Prilosec works to slow down or stop the pump action. For more details, check out my post on Nexium.
AstraZeneca Pharmaceuticals makes Prilosec and Nexium.
Tuesday, March 13, 2007
Allergy Season is HERE! So how does Claritin work?
Claritin (drug name loratadine) is an antihistamine used mainly for seasonal allergies. It is a long acting tricyclic antihistamine with selective peripheral histamine H1 receptor antagonistic activity. What the heck does that mean?
We all know antihistamines.....they block the histamine released from immune cells in your body and the syptoms of allergies go away. Histamine receptors on cells have various types. Claritin works on the H-1 type of histamine receptor. It is what is termed and H1 antagonist. An antagonist means that it binds to a specific receptor and turns it off. This means that claritin binds to this specific receptor, mainly in the periphery, eg. not in the brain thus it doesn't make you sleepy. Now that these receptors are blocked, the mast cells can't release histamine and you feel better.
I can go into greater detail if there is interest.
We all know antihistamines.....they block the histamine released from immune cells in your body and the syptoms of allergies go away. Histamine receptors on cells have various types. Claritin works on the H-1 type of histamine receptor. It is what is termed and H1 antagonist. An antagonist means that it binds to a specific receptor and turns it off. This means that claritin binds to this specific receptor, mainly in the periphery, eg. not in the brain thus it doesn't make you sleepy. Now that these receptors are blocked, the mast cells can't release histamine and you feel better.
I can go into greater detail if there is interest.
Friday, March 9, 2007
Do you have the purple pill? Nexium
Nexium is a drug that is heavily advertised in just about any medium found. I've always noticed that most of the time, they always say something about the purple pill but fail to even tell you what it treats (much less it's mechanism of action).
Nexium (esomeprazole magnesium) is indicated for the treatment of heartburn and acid reflux disease. This is when the acid in your stomach backs up into the lining of the esophagus. Nexium works by inhibiting the proton pumps in the stomach that make the acid to digest food. Protons are pumped in which drops the pH (as anybody with a fish tank, acidity breaks down proteins) and makes acid to degrade the food you eat. By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity. This effect is dose-related up to a daily dose of 20 to 40 mg and leads to inhibition of gastric acid secretion.
In certain cases, nexium is given in combination with an antibiotic such as amoxicillin to clear any persistent bacterial contaminants in the stomach.
Nexium is well tolerated and does not interact with many drugs, but does inhibit gastric acid secretion therefore may slow the absorption of other medications.
Nexium (esomeprazole magnesium) is indicated for the treatment of heartburn and acid reflux disease. This is when the acid in your stomach backs up into the lining of the esophagus. Nexium works by inhibiting the proton pumps in the stomach that make the acid to digest food. Protons are pumped in which drops the pH (as anybody with a fish tank, acidity breaks down proteins) and makes acid to degrade the food you eat. By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity. This effect is dose-related up to a daily dose of 20 to 40 mg and leads to inhibition of gastric acid secretion.
In certain cases, nexium is given in combination with an antibiotic such as amoxicillin to clear any persistent bacterial contaminants in the stomach.
Nexium is well tolerated and does not interact with many drugs, but does inhibit gastric acid secretion therefore may slow the absorption of other medications.
Monday, March 5, 2007
Mr. Beaver is missing you......Rozerem
Rozerem is the first prescription insomnia medication with a novel therapeutic mechanism of action in 35 years. Rozerem is the first and only prescription sleep medication that has shown no evidence of abuse and dependence and, as a result, has not been designated as a controlled substance by the U.S. Drug Enforcement Administration (DEA). With the exception of ROZEREM, all other prescription medications indicated for insomnia are classified as Schedule IV controlled substances by the DEA.
Rozerem works by specifically binding to receptors in the brain called MT1 and MT2 (melatonin receptors). Melatonin is released in a cycle that corresponds to sleep (night). Activation of the MT1 and MT2 receptors in the brain stops an alerting signal, which is thought to facilitate the onset of sleep. It does not act like other sleep drugs, which act through benzonbiazpine receptors. The MT1/2 receptors control many physiological functions other than sleep, such as blood pressure and immune cell signaling.
Rozerem is made by Takeda Pharmaceuticals
Rozerem works by specifically binding to receptors in the brain called MT1 and MT2 (melatonin receptors). Melatonin is released in a cycle that corresponds to sleep (night). Activation of the MT1 and MT2 receptors in the brain stops an alerting signal, which is thought to facilitate the onset of sleep. It does not act like other sleep drugs, which act through benzonbiazpine receptors. The MT1/2 receptors control many physiological functions other than sleep, such as blood pressure and immune cell signaling.
Rozerem is made by Takeda Pharmaceuticals
Saturday, March 3, 2007
Zestril---How are you treating your high blood pressure?
I've seen a lot of ads for this hypertension medication. So what is it?
It's generic name is lisinopril. I actually take this medication, so before taking it I did extensive research to understand how it is manipulating my body. Here's what I know.
Lisinopril is in a class of drugs called ACE inhibitors, ACE being angiotensin converting enzyme. Angiotensin is a peptide that exerts it's function in the kidney through a system called angiotensin-renin loop. Basically, this system is the body's way of controlling smooth muscle relaxation within blood vessels. Angiotensin is converted to angiotensin II in the kidney which then acts on blood vessels to constrict. When the blood vessels are constricted, it's harder for blood to be pumped through, thus raising blood pressure. These drugs stop the converstion of ANG to ANG II, thus allowing relaxation of the vessels.
The following is a list of the ACE inhibitors that are available in the United States:
captopril (Capoten), benazepril (Lotensin), enalapril (Vasotec), lisinopril (Prinivil, Zestril) fosinopril (Monopril), ramipril (Altace), perindopril (Aceon), quinapril (Accupril), moexipril (Univasc), and trandolapril (Mavik). These drugs have few drug interactions and are well tolerated (few side effects).
It's generic name is lisinopril. I actually take this medication, so before taking it I did extensive research to understand how it is manipulating my body. Here's what I know.
Lisinopril is in a class of drugs called ACE inhibitors, ACE being angiotensin converting enzyme. Angiotensin is a peptide that exerts it's function in the kidney through a system called angiotensin-renin loop. Basically, this system is the body's way of controlling smooth muscle relaxation within blood vessels. Angiotensin is converted to angiotensin II in the kidney which then acts on blood vessels to constrict. When the blood vessels are constricted, it's harder for blood to be pumped through, thus raising blood pressure. These drugs stop the converstion of ANG to ANG II, thus allowing relaxation of the vessels.
The following is a list of the ACE inhibitors that are available in the United States:
captopril (Capoten), benazepril (Lotensin), enalapril (Vasotec), lisinopril (Prinivil, Zestril) fosinopril (Monopril), ramipril (Altace), perindopril (Aceon), quinapril (Accupril), moexipril (Univasc), and trandolapril (Mavik). These drugs have few drug interactions and are well tolerated (few side effects).
Thursday, March 1, 2007
Caduet--for high blood pressure and cholesterol
Caduet is a dual anti hypertension/cholesterol medicine combined into one pill. It's generic name(s) are amlodipine and atorvastatin or Norvasc/lipitor.
Atorvastatin is a statin drug, [see below post] as you remember blocks the production of cholesterol by inhibiting a specific enzyme.
Amlodipine is a calcium channel blocker; ( calcium is very important in the contraction of muscles, therefore if the channels [specific areas of cells that the calcium ions use to enter the cell] are blocked, the muscle cell cannot contract and thus relaxes. This in turn allows unrestricted blood flow and lowers blood pressure.
Atorvastatin is a statin drug, [see below post] as you remember blocks the production of cholesterol by inhibiting a specific enzyme.
Amlodipine is a calcium channel blocker; ( calcium is very important in the contraction of muscles, therefore if the channels [specific areas of cells that the calcium ions use to enter the cell] are blocked, the muscle cell cannot contract and thus relaxes. This in turn allows unrestricted blood flow and lowers blood pressure.
2 tubs in a field: Cialis
We've all seen the bathtub commercial for Cialis. What is it?
It's drug name is tadalafil. It is (obviously) indicated for erectile dysfunction. But how does it work?
Tadalafil relaxes muscles within the penis. This allows increased blood flow into the penis, necessary to achieve and maintain an erection. Specifically, it inhibits a very specific enzyme, phosphodiesterase type 5, enhancing effects of nitric oxide-activated increases in cGMP. Nitric oxide is a very key part of the way this drug works. Nitric oxide (NO) has many, manyin the body. Each revelation adds to nitric oxide's already lengthy resume in controlling the circulation of the blood, and regulating activities of the brain, lungs, liver, kidneys, stomach, gut, genitals and other organs. It thereby, influences erection by dilating muscles within the penis, allowing adequate blood flow resulting in erection.
It's drug name is tadalafil. It is (obviously) indicated for erectile dysfunction. But how does it work?
Tadalafil relaxes muscles within the penis. This allows increased blood flow into the penis, necessary to achieve and maintain an erection. Specifically, it inhibits a very specific enzyme, phosphodiesterase type 5, enhancing effects of nitric oxide-activated increases in cGMP. Nitric oxide is a very key part of the way this drug works. Nitric oxide (NO) has many, manyin the body. Each revelation adds to nitric oxide's already lengthy resume in controlling the circulation of the blood, and regulating activities of the brain, lungs, liver, kidneys, stomach, gut, genitals and other organs. It thereby, influences erection by dilating muscles within the penis, allowing adequate blood flow resulting in erection.
A lot of ads about : Lipitor
otherwise known as atorvastatin, known as a "statin" drug. The statin drugs inhibit an enzyme in the synthesis of fatty acids. Generallly, these drugs induce an increase in receptors in the body that bind LDL cholesterol and help the body (liver) extract LDL from the blood. Because the pattern of cholesterol production happens at night, this class of drugs should be given in the evening as a single dose.
Side Effects:
Women should not take these drugs if they are pregnant, lactating or likely to become pregnant. The most common complaints are constipation and a bloating sensation, both easity relieved with increased dietary fiber consumption.
Side Effects:
Women should not take these drugs if they are pregnant, lactating or likely to become pregnant. The most common complaints are constipation and a bloating sensation, both easity relieved with increased dietary fiber consumption.
Welcome! What is this site about?
As everyone knows, there are a ton of drug advertisements in just about any media source. And I have noticed, many (and more everyday) don't even bother to reveal what the drug is even prescribed for----The "Purple Pill" comes to mind. And I love the ads that say "Ask your Doctor if XXXX is right for you". I like to joke and reword it for some of the more obscure ads for drugs like chemotherapy: Ask your Dr. if knee replacement is right for you--LOL.
So my intent here is to try to explain what the ad is actually trying to sell and a brief summary of the drug, its classification and how it generally works [mechanism of action]; but in a way that non-scientifically trained people can understand.
So what about me? I am a research scientist currently working full time in the biotech/pharmaceutical industry. I have laboratory research experience in both academia 13 years and biotech 4 years. My research topics have include diverse fields as immunology, cancer, biochemistry and cell biology and my favorite--pharmacology. So let's get the ball rolling and learn something today!
So my intent here is to try to explain what the ad is actually trying to sell and a brief summary of the drug, its classification and how it generally works [mechanism of action]; but in a way that non-scientifically trained people can understand.
So what about me? I am a research scientist currently working full time in the biotech/pharmaceutical industry. I have laboratory research experience in both academia 13 years and biotech 4 years. My research topics have include diverse fields as immunology, cancer, biochemistry and cell biology and my favorite--pharmacology. So let's get the ball rolling and learn something today!
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