Thrive – Interesting Facts

Brand/Commercial Names
Nicotine

Uses
Thrive lozenges can help you stop smoking by reducing withdrawal symptoms and nicotine cravings. Using Thrive lozenges can enable you to reduce the daily number of cigarettes smoked to ease the transition into a smoke-free lifestyle. Although smoking cessation is preferable, THRIVE lozenges can also be used in cases when you need to temporarily refrain from smoking, for example, in smoke-free areas, airplanes, etc. or in other situations when you wish to avoid smoking. Product effectiveness is directly related to your motivation to stop smoking.

Active Ingredient(s)

Nicotine (as nicotine bitartrade dihydrate)

Chemically and Mechanistically Related Drugs

Nicotex, Nicorette, Nicoderm, Nicogum, Nicotinell, Thrive and Commit Lozenge

Pediatric Use
Do not give this medication to anyone under 18 years old without medical advice.

Use in the Elderly
In elderly patients, failure to thrive describes a state of decline that is multifactorial and may be caused by chronic concurrent diseases and functional impairments. Manifestations of this condition include weight loss, decreased appetite, poor nutrition, and inactivity. Four syndromes are prevalent and predictive of adverse outcomes in patients with failure to thrive: impaired physical function, malnutrition, depression, and cognitive impairment.

Interesting Fact(s)
Thrive® Lozenges dissolve quickly in your mouth, releasing controlled amounts of nicotine into your body for relief of your cravings and withdrawal symptoms. One lozenge should be placed in the mouth and allowed to dissolve. Move the lozenge occasionally from one side of the mouth to the other. Repeat until the lozenge is completely dissolved (about 10 minutes).
The Nicotine transdermal patch may burn your skin if you wear the patch during an MRI (magnetic resonance imaging). Remove the patch before undergoing such a test.

Nicotine as Therapy
There’s a cheap, common, and mostly safe drug, in daily use for centuries by hundreds of millions of people that only lately has been investigated for its therapeutic potential for a long list of common ills. The list includes Alzheimer disease, Parkinson disease, depression and anxiety, schizophrenia, attention deficit hyperactivity disorder (ADHD), and even pain and obesity. Why has interest in this potential cure-all been slow to develop? One reason: in its current forms the drug offers pharmaceutical companies no possibility of substantial profit. Another, perhaps more important: the drug is reviled as the world’s most addictive.
Nicotine is an alkaloid in the tobacco plant Nicotiana tabacum, which was smoked or chewed in the Americas for thousands of years before European invaders also succumbed to its pleasures and shipped it back to the Old World.

Nicotine and the Brain
People with depressive-spectrum disorders, schizophrenia, and adult ADHD tend to smoke heavily, which suggested to researchers that nicotine may soothe their symptoms. Common to all these disorders is a failure of attention, an inability to concentrate. Nicotine helps.
Smokers also have lower rates of neurodegenerative disorders, and nicotine improves cognitive and motor functioning in people with Alzheimer disease and Parkinson disease.
Some researchers is heading the first study ever to examine the efficacy and safety of nicotine patches for treating mild cognitive impairment, thought to be a precursor of Alzheimer disease. The researchers hope to see a positive effect on attention and learning. They also heads two studies of nicotinic stimulation in ADHD, using the patch, nicotine blockers, and some novel drugs that activate nicotine receptors.

Nicotine and Pain
Two much newer topics of academic research are nicotine’s potential for pain relief and for treating obesity. Nicotine itself has provided modest pain relief in animal studies.
Meanwhile, nicotine is also being investigated as an analgesic in humans.
The nice thing about nicotine and drugs like nicotine is that they have opposite side effects to anesthetics. Instead of being respiratory depressants, they are respiratory stimulants. Instead of being sedating, they increase alertness.

Nicotine and Weight Gain
Nicotine may be the most effective drug around for weight control. As ex-smokers know, to their rue, one of the worst things about quitting cigarettes is putting on pounds—as much as 10% of body weight.
Ming Li and his colleagues at the University of Texas in San Antonio, Texas, are studying nicotine’s effects on weight. In the weight study, nicotine-treated rats not only lost weight, they lost about 20% of their body fat compared to saline-treated controls. The researchers suggest that, among its other effects, nicotine alters fat storage.

Nicotine’s Future
Developing new drugs that selectively target specific subtypes of nicotine receptors is an expensive proposition. And therein lies a question. Will nicotine-based therapy consist mostly of costly new drugs from the pharmaceutical industry? Or can less expensive nicotine products like the patch, chewing gum, and nasal spray—which are generally intended for smoking cessation but widely available, usually without prescription—find their way into the world’s medicine cabinets?
Yet much of the work to date showing nicotine’s effectiveness on a huge range of disorders has involved products available at any drugstore and intended to help people quit smoking. Newhouse is using patches for mild cognitive impairment. Flood has demonstrated pain relief with nasal spray and will use patches in her next study. And Role feels that gum hasn’t been adequately explored for its therapeutic potential. Nicotine gum, she notes, is a better imitator of smoking than the patch because it delivers brief hits rather than a steady supply. But Role also points out that nicotine has its serious problems—addictive potential, cardiovascular damage, and (especially when delivered through the mucosa) cancer.

Ritalin – Interesting Facts

Brand/Commercial Names
Methylphenidate, Concerta®, Metadate CD®, Metadate ER®, Methylin®, Methylin ER ®, Quillivant XR®, Ritalin®, Ritalin® LA, Ritalin® SR

Uses
Ritalin is used as part of a treatment program to control symptoms of attention deficit hyperactivity disorder (ADHD; more difficulty focusing, controlling actions, and remaining still or quiet than other people who are the same age) in adults and children. Ritalin is also used to treat narcolepsy (a sleep disorder that causes excessive daytime sleepiness and sudden attacks of sleep). Ritalin is in a class of medications called central nervous system (CNS) stimulants. It works by changing the amounts of certain natural substances in the brain.

Active Ingredient(s)
Ritalin tablets contain the active ingredient methylphenidate hydrochloride, which is a type of medicine called a stimulant.

Chemically and Mechanistically Related Drugs
There are two main kinds of attention deficit hyperactivity disorder ADHD medications: stimulants and non-stimulants.
Stimulants include Concerta, Ritalin LA, Focalin XR, Metadate CD, Daytrana, Adderall, and Vyvanse. They come as a liquid, pill, capsule, and even a patch. Stimulants work very quickly, and people with ADHD may see an improvement right away.
Non-stimulants work a little differently in the brain than stimulants. They may take longer to work, but they work better than stimulants for some people. Non-stimulants include atomoxetine (Strattera), extended release guanfacine (Intuniv), extended release clonidine (Kapvay), and certain antidepressants (such as Wellbutrin).

Pediatric Use
The American Academy of Pediatrics (AAP) recommends that behavioral therapy be used as the first-line treatment for preschoolers, and that methylphenidate, better known as Ritalin or Concerta, be prescribed only after behavior management therapies have been tried without success.

Use in the Elderly
Depressive symptoms, apathy, and fatigue are common symptoms among medically ill older adults and patients with advanced disease, and are associated with morbidity and mortality. Methylphenidate has been used to treat these symptoms because of its rapid effect.

Worldwide Sales
Methylphenidate U.S. retail sales in 2013 was $1,383,814,000

Interesting Fact(s)
In the US, Delaware, Virginia and Michigan rank as the top three states for Ritalin use, and most of the prescriptions are for elementary and middle school age children. Doctors in these states prescribe at least 33 grams for every 1,000 residents, 56 percent more than the national average, according to figures compiled by the Federal Drug Enforcement Agency.

Future Developments
During the past few years considerable debate has arisen within academic journals with respect to the use of smart drugs or cognitive enhancement pharmaceuticals. Some studies seek to examine the foundations of this cognitive enhancement debate using the example of methylphenidate use among college students.
The argument taken is that much of the enhancement debate rests upon inflated assumptions about the ability of such drugs to enhance and over-estimations of either the size of the current market for such drugs or the rise in popularity as drugs for enhancing cognitive abilities. Some studies overview empirical evidence that methylphenidate has the ability to significantly improve cognitive abilities in healthy individuals, and examine whether the presumed uptake of the drug is either as socially significant as implied or growing to the extent that it requires urgent regulatory attention. In addition, those studies review the evidence of side-effects for the use of methylphenidate which may be an influential factor in whether an individual decides to use such drugs. The primary conclusions are that neither drug efficacy, nor the benefit-to-risk balance, nor indicators of current or growing demand provide sufficient evidence that methylphenidate is a suitable example of a cognitive enhancer with mass appeal.

Prozac – Interesting Facts

Brand/Commercial Names
Fluoxetine, Prozac® Weekly, Rapiflux®, Sarafem®, Selfemra®

Uses
Fluoxetine (Prozac) is used to treat depression, obsessive-compulsive disorder (bothersome thoughts that won’t go away and the need to perform certain actions over and over), some eating disorders, and panic attacks (sudden, unexpected attacks of extreme fear and worry about these attacks). Fluoxetine (Sarafem) is used to relieve the symptoms of premenstrual dysphoric disorder, including mood swings, irritability, bloating, and breast tenderness. Fluoxetine is in a class of medications called selective serotonin reuptake inhibitors (SSRIs). It works by increasing the amount of serotonin, a natural substance in the brain that helps maintain mental balance.

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Active Ingredient(s)

fluoxetine hydrochloride

Chemically and Mechanistically Related Drugs

Beginning in the 1950s, scientists developed a number of synthetic drugs for the treatment of depression, which represented a major step forward at the time.
The Tricyclics
The tricyclic drugs (Tofranil, (Elavil, Limbitrol, Endep, Norpramin, Adapin, Sinequan, Pamelor, Aventyl ) were the first antidepressant medications. They dominated the market for more than twenty years, and are still used today, though less frequently. They work by desensitizing a receptor in the neuron that absorbs the neurotransmitters norepinephrine and dopamine into the cells. This results in higher levels of these two chemicals in the synapse, and consequent improvements in mood.
A serious problem with the tricyclics is their level of side effects, particularly in patients over age sixty-five.
The Monoamine Oxidase Inhibitors
The monoamine oxidase inhibitors (Nardil, Parnate), or MAOIs, have a different mechanism of action than the other antidepressants. They work by reducing the quantity of the enzyme MAO within the synapse.
While the MAOIs have fewer side effects than the tricyclic drugs, they can still cause problems in some individuals.
The Selective Serotonin Re-Uptake Inhibitors
Prozac (fluoxetine hydrochloride) was the first selective serotonin re-uptake inhibitor, or SSRI, put on the market. Prozac’s success has spawned other SSRIs, including Zoloft (sertraline hydrochloride) and Paxil (paroxetine hydrochloride).
Prozac and the other SSRIs can exact a high price for their benefits. Prozac is considered better than the older drugs because “only” 17 percent of the people who try it have to stop because of negative experiences, compared with nearly a third (31 percent) of the patients taking the tricyclic drugs. Zoloft and Paxil are similar to Prozac in terms of their side effects.
Wellbutrin
Wellbutrin (bupropion hydrochloride) seems to boost norepinephrine function, with no impact on serotonin levels. The main difficulty with this drug is its association with seizures.
Desyrel
Desyrel (trazodone hydrochloride) works on the serotonin system. Rather than being used for its antidepressant effects, it is most often prescribed along with Prozac because the drowsiness Desyrel induces counteracts Prozac’s tendency to produce insomnia.
Effexor
Effexor (venlafaxine hydrochloride) is chemically similar to an antidepressant compound in chocolate known as phenylethylamine (PEA), sometimes associated with the “love effect.” It is likely that PEA raises the level of endorphins in the brain, which creates a sense of well-being. The tradition of giving chocolates on Valentine’s Day reflects our intuitive knowledge of this effect.

As of April 2, 2010, fluoxetine is one of four antidepressant drugs that the FAA allows pilots to take. The others are sertraline (Zoloft), citalopram (Celexa), and escitalopram (Lexapro).

Pediatric Use
In the US, a survey of drug companies found that between 1995 and 1999, use of Prozac-like drugs for children aged seven to 12 increased by 151 per cent, and in those aged under six by 580 per cent. In 2004, children aged five and under were America’s fastest-growing segment of the non-adult population using antidepressants. ‘Selective mutism’ (fear of speaking in social situations) is one affliction common in preschoolers and has been treated with Prozac.
A small number of children, teenagers, and young adults (up to 24 years of age) who took antidepressants (‘mood elevators’) such as fluoxetine during clinical studies became suicidal (thinking about harming or killing oneself or planning or trying to do so). Children, teenagers, and young adults who take antidepressants to treat depression or other mental illnesses may be more likely to become suicidal than children, teenagers, and young adults who do not take antidepressants to treat these conditions. However, experts are not sure about how great this risk is and how much it should be considered in deciding whether a child or teenager should take an antidepressant.

Use in the Elderly
Fluoxetine is generally not recommended for use in the elderly because of its long half-life and prolonged side effects.

Worldwide Sales
Roughly 19.49 million prescriptions for this drug were filled in 2009, 24.4 million in 2010, and the number increased to over 24.5 million prescriptions in 2011. Prozac was considered the very first SSRI (Selective Serotonin Reuptake Inhibitors) medication to hit the market and was approved in 1987. It is widely regarded as the most popular antidepressant and some would consider “Prozac" to antidepressants as “Coke" is to soda. In addition to being approved for major depression, it is also used for OCD, eating disorders, and trichotillomania.

Interesting Fact(s)
You’ve probably heard about all the prescription meds in our water supply. Turns out Prozac in public waters makes shrimp act nutty—and not in a good way.

Seems that the active ingredient in antidepressants like Prozac boosts serotonin in the shrimps’ nervous system and make them wiggle away from safe, dark waters toward the light, where they’re more likely to be devoured by predators.

And because researchers don’t think Prozac has the same mood-elevating effect in shrimp as it does in people, the crustaceans don’t even get to die happy.
Future Developments
Prozac, an antidepressant that revolutionized the medical landscape, can cause birth defects if taken during pregnancy and can increase suicidal thoughts and behavior in children and young adults. Patients have targeted Eli Lilly & Co., drug manufacturer, with numerous Prozac lawsuits, claiming the company didn’t properly warn them about the drug’s dangerous side effects.
Eli Lilly paid more than $50 million by 2000 to settle dozens of lawsuits related to Prozac. The drug remains on the market, although the FDA now requires it to carry a black-box label warning stating that it may increase suicidal thoughts or behavior in young people. So far, the company has refused to admit liability in birth defect cases.

Myonal – Interesting Facts

Brand/Commercial Names
Eperisone, Expose

Uses
Myonal acts by relaxing both skeletal muscles and vascular smooth muscles, and demonstrates a variety of effects such as reduction of myotonia, improvement of circulation, and suppression of the pain reflex. The drug inhibits the vicious circle of myotonia by decreasing pain, ischaemia, and hypertonia in skeletal muscles, thus alleviating stiffness and spasticity, and facilitating muscle movement.
Myonal also improves dizziness and tinnitus associated with cerebrovasculardisorders or cervical spondylosis.

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Active Ingredient(s)
Eperisone HCl

Chemically and Mechanistically Related Drugs
Inaperisone, Silperisone, Tolperisone

Pediatric Use
Safety in children has not been established (insufficient clinical experience).

Use in the Elderly
Since the elderly often have a physiological hypofunction, it is advisable to take measures, such as reduction in dosage under careful supervision.

Interesting Fact(s)
Study of Myonal versus tizanidine for treatment of chronic low back pain.
AIM:
Many therapies exist for treatment of chronic low-back pain (LBP) including the use of muscle relaxant and analgesic drugs. The aim of this study was to compare efficacy and tolerability of Myonal and tizanidine in combination treatment with tramadol in chronic LBP.
RESULTS:
Both associations assumed for one month, have shown effective for LBP at rest and with effort. Myonal /tramadol, reducing discontinuation and allowing a better adherence to the therapy, may be considered a viable option for the treatment of chronic LBP.

Future Developments
Myonal suffers from a very low bioavailability when taken orally, as a result of high first pass intestinal metabolism; a transdermal patch containing Myonal is currently in development in South Korea. This has shown promise, with the antispasmodic effect lasting over 24 hours, compared to one to two hours following oral administration.
Myonal is also under investigation as an antihypertensive agent, with promising results from trials on beagles.

Modafinil – Interesting Facts

Brand/Commercial Names
Provigil

Uses

Modafinil is used to treat excessive sleepiness caused by narcolepsy (a condition that causes excessive daytime sleepiness) or shift work sleep disorder (sleepiness during scheduled waking hours and difficulty falling asleep or staying asleep during scheduled sleeping hours in people who work at night or on rotating shifts). Modafinil is also used along with breathing devices or other treatments to prevent excessive sleepiness caused by obstructive sleep apnea/hypopnea syndrome (OSAHS; a sleep disorder in which the patient briefly stops breathing or breathes shallowly many times during sleep and therefore doesn’t get enough restful sleep). Modafinil is in a class of medications called wakefulness promoting agents. It works by changing the amounts of certain natural substances in the area of the brain that controls sleep and wakefulness.

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Active Ingredient(s)
modafinil

Chemically and Mechanistically Related Drugs
Adrafinil
Adrafinil or Modafinil to give you more energy and vitality, you might be curious as to what the main differences between these smart drugs are. These are two of the most popular cognitive enhancement drugs available today with considerable benefits recorded for speed of cognition, memory, productivity and general alertness.
The original clinical purpose of Adrafinil was to help those who have sleep problems.
Many users also seem to experience a higher level of energy from this supplement. This is most likely due to the fact that it works by increasing the presence of the neurotransmitter Hypocretin. This brain chemical actually controls how alert and awake a person will feel.
Mood is also generally improved while using Adrafinil. This is caused by an increase in the levels of Dopamine and Serotonin within the brain.
Adrafinil is also capable of stimulating Glutamate receptors in the brain. As Glutamate receptors are stimulated and their pathways activated, this supplement increases memory and may also improve the speed of recall.
Ritalin
Ritalin is a controlled substance under the Misuse of Drugs act, the spokesperson says. Possession of it without a prescription is illegal and it is a Class B drug.

Pediatric Use
Provigil is not approved for use in children for any medical condition. It is not known if Provigil is safe or effective in children under 17 years of age.

Use in the Elderly
Although appropriate studies on the relationship of age to the effects of Modafinil have not been performed in the geriatric population, geriatric-specific problems are not expected to limit the usefulness of Modafinil in the elderly. However, elderly patients may have a slower removal of this medicine from the body, which may require an adjustment in the dose for patients receiving Modafinil.

Worldwide Sales
Q3 2013 sales: $176,996,000

Interesting Fact(s)
Modafinil is a stimulant in the same vein as caffeine and adenosine, but the difference in how it works the brain means it doesn’t have the same side-effects that the others do.
The way caffeine and Adenosine work is that they block certain receptors in the brain that react to dopamine, which makes it slow down. This means, for example, that coffee does not give you energy, but rather, doesn’t let the brain realize it needs more energy. This is why people crash after caffeine. The effect goes away and all the tiredness catches up to you. Modafinil doesn’t have that problem.
No one really knows how it works yet, but it seems that instead of blocking the brain’s Dopamine processing, it just slows production of Dopamine. On top of that, it also prevents the re-uptake of another neurotransmitter called noradrenaline, which triggers sleep.
The end result, and one of the most mysterious, is that Modafinil doesn’t trigger sleep debt. People who stay awake for a day or two on Modafinil don’t report a need to catch up on sleep after the effect wears off. They can sleep the normal amount!

Ketamine – Interesting Facts

Brand/Commercial Names
Ketalar®, Ketaject®, Ketaset®, Vetalar®;

Uses
Ketamine is an anesthetic medication. Ketamine is used to put you to sleep for surgery and to prevent pain and discomfort during certain medical tests or procedures.
Primarily used in veterinary applications as a tranquilizer.
Recreationally used as a psychedelic and for its dissociative effects.
Psychological: Decreased awareness of general environment, sedation, dream-like state, vivid dreams, feelings of invulnerability, increased distractibility, disorientation, and subjects are generally uncommunicative. Intense hallucinations, impaired thought processes, out-of-body experiences, and changes in perception about body, surroundings, time and sounds. Delirium and hallucinations can be experienced after awakening from anesthesia.
Physiological: Anesthesia, cataplexy, immobility, tachycardia, increased blood pressure, nystagmus, hypersalivation, increased urinary output, profound insensitivity to pain, amnesia, slurred speech, and lack of coordination.

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Active Ingredient(s)
Ketamine hydrochloride

Chemically and Mechanistically Related Drugs
Lanicemine (a drug originally developed to treat epilepsy that targets the same brain receptors as ketamine), Tiletamine and Phencyclidine (PCP)

Pediatric and Elderly Use
Occasionally used as a short-acting general anesthetic for children and elderly patients.

Worldwide Sales
A huge seizure of ketamine and a law change in India, the major supplier globally of the drug, are being blamed for a ‘ketamine drought’. Dozens of factories in the Indian states of Maharashtra, Andhra Pradesh, and Gujarat manufacture tonnes of ketamine annually for the legitimate international medical and veterinary markets. But many illegal outfits also operate and sell the chemicals to narcotraffickers worldwide.
The U.S. general anesthesia market (drugs such as propofol, midazolam & diazepam, fospropofol disodium, sodium pentothal, ketamine, methohexital sodium, pentobarbital, etomidate and fentanyl) was valued at $2 billion in 2011 and is poised to grow at a CAGR of approximately 4% to reach $2.3 billion by 2015.

Interesting Fact(s)
Ketamine has a reputation as an illicit party drug due to its hallucinogenic effects. But in a handful of ketamine clinics around the country, people who weren’t helped by standard treatments are getting a series of infusions to ease their depression.
In tests, almost 70 percent of people who responded negatively to ordinary antidepressants improved within hours of taking the ketamine. Because around 40 percent of depressed people don’t respond to medication, this could be a huge help. And many others only respond after many months or years of trying different treatments.
The drug has also been used in emergency rooms for curbing suicidal thoughts, making it a potential lifesaver. But it hasn’t been thoroughly studied for long-term safety and effectiveness, and the FDA hasn’t approved it to treat depression.
Ketamine was widely employed as a field anaesthetic by the US Army during the Vietnam War.

Future Developments
Ketamine has been in the market for the past 41 years. There are four major players of ketamine in the U.S. market. JHP Pharmaceuticals is the only company which offers a branded generic of ketamine – ketalar. Ketalar is expected to maintain its position in the market in the coming five years but with a decreasing share in the market, due to high cost compared to the generic counterparts.

Diprospan – Interesting Facts

Brand/Commercial Names
Celestone Soluspan

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Uses
Diprospan Injectable Suspension is indicated for the treatment of acute and chronic disorders that respond to corticosteroids. The corticosteroid hormone therapy is an adjunct and not replace conventional therapy.
The primary or secondary adrenocortical insufficiency may be treated with Diprospan Suspension for injection, but should be supplemented with mineralocorticosteroides.

Diprospan Injectable Suspension is recommended for:
– Intramuscular injection in conditions responsive to systemic corticosteroids.
– injection directly into soft tissues, such therapy when indicated.
– intra and periarticular injection in arthritic disorders.
– intralesional injections in various dermatological conditions.
– local injection in certain inflammatory and cystic disorders of the foot.

Contraindications
Diprospan Suspension for injection is contraindicated in patients with systemic fungal infections in those with sensitivity reactions to betamethasone, other corticosteroids, or any component of this product.

Active Ingredient(s)
Betamethasone 17α,21-dipropionate and 21-(disodium phosphate)

Chemically and mechanistically related drugs
Hyaluronic acid, Tenoxicam

Pediatric Use
The efficacy and safety of corticosteroids in the pediatric population are based on the well-established course of effect of corticosteroids, which is similar in pediatric and adult populations. Published studies provide evidence of efficacy and safety in pediatric patients for the treatment of nephrotic syndrome (>2 years of age), and aggressive lymphomas and leukemias (>1 month of age). Other indications for pediatric use of corticosteroids, eg, severe asthma and wheezing, are based on adequate and well-controlled trials conducted in adults, on the premises that the course of the diseases and their pathophysiology are considered to be substantially similar in both populations.

Use in the Elderly
No overall differences in safety or effectiveness were observed between elderly subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and young patients, but greater sensitivity of some older individuals cannot be ruled out.

Interesting Fact(s)
A comparative study on the impact of intra-articular injections of hyaluronic acid, tenoxicam and betametazon on the relief of t joint disorder complaints.
OBJECTIVE
The aim of this study was to compare the efficacy of intra-articular injections of three different agents with well-known anti-inflammatory properties.
CONCLUSION
Study found that hyaluronic acid produced better pain relief scores when compared to the other anti-inflammatory agents studied. The main disadvantage of hyaluronic acid is its relatively higher cost. Additionally it does not have a reimbursement status by state or private health insurance systems in Turkey. Despite the lower VAS scores, intra-articular tenoxicam and Diprospan may be assessed as more economic alternatives to intra-articular hyaluronic acid injections.

Azithromycin – Interesting Facts

Brand/Commercial Names
Zithromax®, Zithromax® Single Dose Packets, Zithromax® Tri-Paks®, Zithromax® Z-Paks®, Zmax®

Uses
Azithromycin is used to treat certain bacterial infections, such as bronchitis; pneumonia; sexually transmitted diseases (STD); and infections of the ears, lungs, sinuses, skin, throat, and reproductive organs. Azithromycin also is used to treat or prevent disseminated Mycobacterium avium complex (MAC) infection [a type of lung infection that often affects people with human immunodeficiency virus (HIV).
Azithromycin is in a class of medications called macrolide antibiotics. It works by stopping the growth of bacteria. Antibiotics will not kill viruses that can cause colds, flu, or other infections.
Azithromycin is also used sometimes to treat H. pylori infection, travelers’ diarrhea, and other gastrointestinal infections, Legionnaires’ disease (a type of lung infection), pertussis (whooping cough; a serious infection that can cause severe coughing), and babesiosis (an infectious disease carried by ticks). It is also used to prevent heart infection in people having dental or other procedures, and to prevent STD in victims of sexual assault. Talk to your doctor about the possible risks of using this medication for your condition.

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Active Ingredient(s)
Azithromycin

Chemically and Mechanistically Related Drugs
Minocycline
Azithromycin is at least as effective as Minocycline in the treatment of facial comedonic and papulopustular acne.
Cefadroxil (Duricef)
Azithromycin may be somewhat more effective and better tolerated than Cefadroxil for treating uncomplicated skin and skin structure infections.
Cefdinir (Omnicef)
Cefdinir and Azithromycin have comparable effectiveness in the treatment of acute otitis media

Pediatric Use
Azithromycin has become a frequent choice for many common pediatric infections, including otitis media and pharyngitis. It appears to be as effective as traditional therapies, and offers the advantage of a shorter treatment course. Research continues with this drug, as new dosing regimens are proposed and additional patient populations are studied.

Use in the Elderly

Azithromycin (Zithromax and Zmax) poses the risk for a potentially fatal irregular heart rhythm, which therefore warrants careful screening of patients for this drug.
Patients at risk for this azithromycin-induced arrhythmia include those who already have a prolonged QT interval, low blood levels of potassium or magnesium, and an abnormally slow heart rate, or who take drugs to treat arrhythmias. Elderly patients and patients with cardiac disease also may be more susceptible to the arrhythmogenic effects of the antibiotic.

Worldwide Sales
Azithromycin is one of the world best-selling antibiotics.
Zithromax – Pfizer’s branded version of Azithromycin – was one of the bestselling branded antibiotics in the United States and worldwide, with total sales peaking at US$ 2 billion in 2005 before starting to decline with the loss of patent protection in 2006 and resulting generics competition. However, the strong and proven Zithromax brand name has helped keep market share losses in check.

Interesting Fact(s)
Azithromycin “pros” and “cons”
Advantages:
• Excellent efficacy. Many scientific studies have shown that azithromycin is better or equally effective compared to other antibiotics.
• Low potential for drug interactions. Azithromycin, unlike the majority of macrolides, does not bind to cytochrome P-450 in the liver, resulting in low potential for drug to drug interaction.
• Low rate of side effects. Side effects with azithromycin are mild to moderate, mostly gastrointestinal.
• Sustained antimicrobial activity. Azithromycin reaches high and sustained tissue concentrations that results in sustained antimicrobial activity.
• Active against intracellular bacteria (Chlamydia pneumoniae, Chlamydia trachomatis, Mycoplasma pneumoniae, Legionella spp.). Since azithromycin is a weak base, it easily penetrates the cell membrane and stays within the cell.
• Targeted activity at the site of infection. Because of the transport with white blood cells, azithromycin possesses a unique property – targeted activity at the site of infection. In infected tissues, azithromycin achieves high and sustained therapeutic concentrations that last five to seven days after the last dose.
• Suitable choice for empirical therapy. Since azithromycin has a good activity against the most common pathogens it is used as a choice for empirical therapy.
• Good compliance: short once daily dosing regimen. Azithromycin’s short dosing regimen is convenient and improves patient compliance. For the majority of infections, azithromycin is administered once daily for three days. In the treatment of sexually transmitted diseases, azithromycin is administered as a single dose.
• Active against most respiratory tract infections. Betalactams lack activity against atypical pathogens. Among macrolides, azithromycin shows the best activity against H. influenzae.
Disadvantages:
• Food reduces absorption rate of azithromycin capsules. Capsules should not be mixed with or taken with food, however tablets may be taken without regard to food.
• In 2013, the U.S. FDA sent out a communication stating that azithromycin may cause irregular heartbeats. However, in the study19 (published in the New England Journal of Medicine on May 2013) azithromycin use was not linked with an increased risk of death from cardiovascular (heart) causes in a general population of young and middle-aged adults.

Future Developments
Treatment guidelines increasingly recommend that certain antibiotics, particularly the macrolide azithromycin, no longer be used to treat many common infections. Inappropriate use has led to widespread antibiotic resistance and is contributing to the emergence of super bugs.
At least one prominent emergency medicine expert suggests that the drug not be used at all. The Canadian Pediatric Society strongly recommended that azithromycin not be used to treat acute pharyngitis, otitis media, or community-acquired pneumonia.

Aspirin – Interesting Facts

Brand/Commercial Names
Acuprin®, Anacin® Aspirin Regimen, Ascriptin®, Aspergum®, Aspidrox®, Aspir-Mox®, Aspirtab®, Aspir-trin®, Bayer® Aspirin, Bufferin®, Buffex®, Easprin®, Ecotrin®, Empirin®, Entaprin®, Entercote®, Fasprin®, Genacote®, Gennin-FC®, Genprin®, Halfprin®, Magnaprin®, Miniprin®, Minitabs®, Ridiprin®, Sloprin®, Uni-Buff®, Uni-Tren®, Valomag®, Zorprin®

Uses
Prescription Aspirin is used to relieve the symptoms of rheumatoid arthritis (arthritis caused by swelling of the lining of the joints), osteoarthritis (arthritis caused by breakdown of the lining of the joints), systemic lupus erythematosus (condition in which the immune system attacks the joints and organs and causes pain and swelling) and certain other rheumatologic conditions (conditions in which the immune system attacks parts of the body).
Nonprescription Aspirin is used to reduce fever and to relieve mild to moderate pain from headaches, menstrual periods, arthritis, colds, toothaches, and muscle aches. Nonprescription aspirin is also used to prevent heart attacks in people who have had a heart attack in the past or who have angina (chest pain that occurs when the heart does not get enough oxygen), to reduce the risk of death in people who are experiencing or who have recently experienced a heart attack, to prevent ischemic strokes (strokes that occur when a blood clot blocks the flow of blood to the brain) or mini-strokes (strokes that occur when the flow of blood to the brain is blocked for a short time) in people who have had this type of stroke or mini-stroke in the past.
Aspirin will not prevent hemorrhagic strokes (strokes caused by bleeding in the brain).
Aspirin is in a group of medications called salicylates. It works by stopping the production of certain natural substances that cause fever, pain, swelling, and blood clots.
Aspirin is also available in combination with other medications such as antacids, pain relievers, and cough and cold medications. This monograph only includes information about the use of aspirin alone. If you are taking a combination product, read the information on the package or prescription label or ask your doctor or pharmacist for more information.

ASA 325 MG Oral Tablet
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Active Ingredient(s)
The active ingredient of Aspirin – Salicylic acid – was first discovered from the bark of the willow tree in 1763. Extracts of willow were traditionally used in folk medicine and as early as 400 BC the Greek physician Hippocrates recommended a brew made from willow leaves to treat labor pains.
Acetyl salicylic acid is a synthetic derivative of a compound salicin.

Chemically and Mechanistically Related Drugs
Advil, Aleve, Alka-Seltzer Products, Anacin Products, Ascriptin with Codeine, Arthritis Strength Bufferin, ASA, ASA Enseals, Ascriptin, Aspergurn, Bayer Aspirin Products, Bufferin Aspirin, Cama, Carisoprodol Compound, Congespirin Chewables, Cope, Darvon Compound, Diurex, Doan’s Pills, Dristan, Ecotrin Products, Enteric Coated Aspirin, Empirin, Empirin with Codeine, Equagesic, Excedrin Products, Fiorinol, Fiorinol with Codeine, lbuprofen Products, LortabASA, Medipren, Methocarbomol with ASDA, Midol, Momentum, Norgesic, Nuprin, Pamprin IB, Pepto Bismol, Percodan, Propox/phene Compound, Quiet World Tabs, Robaxisol, St. Joseph Aspirin, Sine-Off Sinus Medication, Soma Compound, Trisesic

Pediatric Use
Consult your doctor before giving this drug to a child younger than 12 years.
Aspirin has been linked with Reye’s syndrome, so use caution when giving aspirin to children or teenagers. Though aspirin is approved for use in children older than age 2, children and teenagers recovering from chickenpox or flu-like symptoms should never take aspirin.

Use in the Elderly
Older age could be a strong risk factor for bleeding from aspirin use. Even low-dose aspirin could increase the risk of bleeding in the gut.

Worldwide Sales
Aspirin is one of the most widely used medications in the world, with an estimated 40,000 tons of it being consumed each year.

Interesting Fact(s)
Aspirin was first synthesized by Felix Hoffmann, a chemist with the German company Bayer in 1897.
Bayer AG is a German company best known for their development of aspirin, yet for as famous as they are, few people know the dark history Bayer has. First founded in 1863 by Friedrich Bayer after discovering aspirin, Bayer AG would go on to become one of the largest chemical and pharmaceutical companies in the world.
The company grew until they were purchased by IG Farben, another German chemical company. IG Farben used intense slave labor in their factories, most notably at Mauthausen-Gusen concentration camp, and during the Nazi regime had few human rights restrictions to follow. In fact, IG Farben produced 42.5% of the chemical used in the gas chambers of various concentration camps in Germany.
When they purchased Bayer they continued to use human test subjects, and many of the chemicals that were being tested, both to help and hurt humans, were tested on human subjects. Bayer became known for this practice and by the end of the war the Bayer executive, Fritz ter Meer, was arrested and imprisoned for crimes against humanity.

Future Developments
Aspirin use after coronary or cerebral thrombosis is virtually mandatory, unless there are signs of intolerance. A ‘loading dose’ of soluble aspirin should be given on first contact with a patient who may be suffering from myocardial infarction. Patients considered to be at increased risk of a vascular event should also be advised to carry their own aspirin and, if they experience sudden severe chest pain, to chew and swallow a 300 mg tablet or a soluble preparation immediately. The current phase of the aspirin story is, however, not over, and its possible value in a variety of conditions, including dementia and certain cancers, seems likely to ensure that it will long continue to play a remarkable part in clinical practice.
Studies indicate that prolonged use of aspirin may play a role in reducing the risk of colorectal cancer. Emerging evidence from other studies being conducted in Boston and elsewhere suggest that aspirin also may reduce the risk of breast cancer or prevent recurrence or death from breast cancer in women with a history of the disease.

Amoxicillin – Interesting Facts

Brand/Commercial Names
Amoxycillin, Amoxil®, Amoxil® Pediatric Drops, Dispermox®, Larotid® Suspension, Moxtag®, Polymox® Suspension, Trimox®, Trimox® Pediatric Drops, Wymox®

Uses
Amoxicillin is used to treat certain infections caused by bacteria, such as pneumonia; bronchitis; gonorrhea; and infections of the ears, nose, throat, urinary tract, and skin. It is also used in combination with other medications to eliminate H. pylori, a bacteria that causes ulcers. Amoxicillin is in a class of medications called penicillin-like antibiotics. It works by stopping the growth of bacteria. Antibiotics will not work for colds, flu, and other viral infections.

Chemically and Mechanistically Related Drugs
Amoxicillin Clavulanate (Augmentin)
Recent Italian study found that skin reactions occur more frequently with amoxicillin than with amoxicillin/clavulanic acid. The incidence of gastrointestinal, hepatic and haematological side effects is significantly higher for amoxicillin/clavulanic acid. Also, Amoxicillin/clavulanic acid seems to be associated with a higher risk of Stevens-Johnson syndrome, purpura and hepatitis than amoxicillin alone.
Clarithromycin (Biaxin)
Clarithromycin and Amoxicillin appears to have comparable effectiveness in the treatment of sinusitis.
In a randomized clinical trial the success rates of Clarithromycin and Amoxicillin in the treatment of patients with acute maxillary sinusitis were comparable. A clinical (based on direct observation of the patient) success rate of 91% and a roentgenographic success rate of 78% were achieved in the clarithromycin group; comparable results for the Amoxicillin group were 89% and 92%, respectively. Differences between the two groups were not statistically significant. Both drugs caused mild gastrointestinal side effects. Dropout rates were low in both groups: 3% for clarithromycin and 4% for amoxicillin.
Cefuroxime axetil (Ceftin)
Both Amoxicillin and Cefuroxime axetil are safe and effective for Lyme disease.
Both Amoxicillin and Cefuroxime are similarly effective in the improvement of bronchitis symptoms. However, Amoxicillin therapy results in a significantly higher relapse rates.
Minocycline
Minocycline may be somewhat more effective than Amoxicillin in the treatment of acute bacterial sinusitis.
Doxycycline
Doxycycline and Amoxicillin are equally effective for treating chlamydial and nonchlamydial cervicitis.

Pediatric Use
Children >3 months: Children weighing ≥88 pounds should follow the recommended adult dosing schedule. Children weighing <88 pounds will have their dosage determined by their weight. Children ≤3 months: The maximum recommended dose is 30 mg per 2.2 pounds of body weight every 12 hours. History
Amoxicillin was discovered by scientists at Beecham Research Laboratories in 1972. In the US it is marketed by GlaxoSmithKline (the inheritor company) under the original trade name Amoxil.
The narrow spectrum of antimicrobial activity of the penicillins, led to the search for derivatives of penicillin which could treat a wider range of infections. The first important step forward was the development of ampicillin. Ampicillin had a broader spectrum of activity than either of the original penicillins and allowed doctors to treat a broader range of both Gram-positive and Gram-negative infections.
Further developments led to amoxicillin, with improved duration of action. It differs structurally from ampicillin merely by having an additional hydroxyl group on the benzene ring. The main difference between ampicillin and amoxicillin is that amoxicillin is slightly more lipid soluble. As a result, amoxicillin may kill bacteria slightly quicker.

Worldwide Sales
2011 sales: $2.41 billion

Interesting Fact(s)
The results of a 20-year study published in the BMJ finds that 1 in 10 of all antibiotic prescriptions fail to treat the infection. This marks an increase in the number of antibiotic failures, which is continuing to rise.
Both primary care clinicians and members of the public typically regard antibiotic resistance as a problem that largely affects patients in hospital.
Overall antibiotic failures rose from 13.9% in 1991 to 15.4% in 2012. Antibiotics prescribed to treat bronchitis, pneumonia and other lower respiratory tract infections were found to be the least successful, showing an increased failure rate of 35%.
Throughout the study period, the treatment failure rates for the commonly prescribed antibiotics Amoxicillin, Penicillin and Flucloxacillin remained below 20%.

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