Archive for September, 2007

Lipitor.

Thursday, September 27th, 2007

Atorvastatin Calcium Tablets (Lipitor) to Reduce Risk for MI in

Canada

On April 24, Health Canada approved an expanded indication for atorvastatin calcium (Lipitor tablets, Pfizer Canada, Inc), allowing its use to reduce the risk for myocardial infarction in adult patients without clinically evident coronary heart disease (CHD) but having risk factors for the condition such as prior myocardial infarction (MI).

The approval was based in part on data from the Treating to New Targets (TNT trial), in which the effect of 80 mg/day of atorvastatin on the reduction of cardiovascular (CV) events was assessed in 10,001 patients (94% white, 81% men, 38% aged ≥ 65 years) with clinically evident CHD. The patients had received a run-in regimen of atorvastatin, 10 mg/day, for 8 weeks, which lowered their mean low-density lipoprotein (LDL) cholesterol level from 152 to 98 mg/dL.

Patients were randomized to continue with the 10-mg/day dose or to receive 80 mg/day for a median duration of 4.9 years. At the end of the study, those in the high- vs the low-dose group had a significantly lower mean LDL cholesterol level (77 vs 101 mg/dL).

Results showed that the time to first occurrence of major CV events was significantly lower in patients receiving atorvastatin 80 vs 10 mg/day (8.7% vs 10.9%), representing a 2.2% absolute risk reduction and 22% relative risk reduction. Overall risk reduction was not affected by age or sex.

Further analysis revealed that the reduction was driven by significant decreases in the rate for nonfatal, nonprocedure-related MI (hazard ratio, [HR], 0.78; 95% CI, 0.66 - 0.93) and fatal/nonfatal stroke (HR, 0.75; 95% CI, 0.59 - 0.96), but not CHD death (HR, 0.80; 95% CI, 0.61 - 1.03) or resuscitated cardiac arrest (HR, 0.96; 95% CI, 0.56 - 1.67).

Although the overall frequency of treatment-related adverse events was similar between groups, patients receiving 80 mg vs 10 mg of atorvastatin daily were more likely to have serious adverse events (1.8% vs 1.4%) and to discontinue therapy due to adverse events (9.9% vs 8.1%) during the 4.9-year period. The rate for persistent transaminase elevations (≥ 3 times the upper limit of normal) was 1.3% in the 80-mg/day group vs 0.2% in patients receiving 10 mg/day of atorvastatin.

The expanded indication was previously approved by the US Food and Drug Administration (FDA). Other FDA-approved uses for atorvastatin include its adjunctive use with diet to treat certain dyslipidemias; to reduce the risk for MI, stroke, revascularization procedures, and angina in patients without CHD but having multiple risk factors for the condition; to reduce the risk for MI and stroke in patients with diabetes mellitus and no clinically evident CHD but having multiple risk factors for the condition; and to reduce the risk for nonfatal MI, fatal/nonfatal stroke, revascularization procedures, congestive heart failure hospitalization, and angina in patients with clinically evident CHD.

In Canada, atorvastatin was previously approved for adjunctive use with diet and lifestyle measures to treat certain dyslipidemias; to reduce the risk for MI in adult hypertensive patients without clinically evident CHD but at least 3 additional risk factors (eg, age, smoking, and type 2 diabetes); and to reduce the risk for MI and stroke in adult patients with type 2 diabetes mellitus and hypertension without clinically evident CHD but with other risk factors such as age, albuminuria, or smoking.

Imitrex.

Tuesday, September 25th, 2007

Why is this drug prescribed: Imitrex is prescribed for the treatment of a migraine attack with or without the presence of an aura (visual disturbances, usually sensations of halos or flickering lights, which precede an attack). The injectable form is also used to relieve cluster headache attacks. (Cluster headaches come on in waves, then disappear for long periods of time. They are limited to one side of the head, and occur mainly in men.) Imitrex cuts headaches short. It will not reduce the number of attacks you experience.

Most important fact about this drug: Imitrex should be used only to treat an acute, classic migraine attack or a cluster headache. It should not be used for certain unusual types of migraine.

How should you take this medication: Imitrex should be taken as soon as your symptoms appear, but may be used at any time during an attack. It is available in three forms: injection, tablets, and nasal spray. Imitrex injection is administered just below the skin with an autoinjector (self-injection device). Choose a site where the skin is thick enough to take the full length of the needle (1/4 inch). Avoid injecting Imitrex into a muscle or a vein. Your doctor should instruct you on how to use the autoinjector and how to dispose of the empty syringes. You should also read the instruction pamphlet that comes with the medication. You can take a second injection if your headache returns; however, never take more than 2 injections within 24 hours, and be sure to wait 1 hour between doses. Imitrex tablets should be swallowed whole, with liquid. If you have had no relief 2 hours after taking Imitrex Tablets, you may take a second dose of up to 100 milligrams, if your doctor advises it. If the headache returns, you may take additional doses at intervals of at least 2 hours. You should not take more than 300 milligrams in one day. If your headache returns after you have had an Imitrex Injection, you may take single Imitrex Tablets, at intervals of at least 2 hours, up to a maximum of 200 milligrams in a day. Imitrex nasal spray is packaged in single-dose bottles containing either 5 or 20 milligrams of the drug. The usual dosage is a single spray in one nostril. If the headache returns, you may repeat the dose once after 2 hours. Do not take more than 40 milligrams a day. –If you miss a dose… Imitrex is not for regular use. Take it only during an attack. –Storage instructions… Store Imitrex away from heat and light, at room temperature, in the case provided. If your medication has expired (the expiration date is printed on the treatment pack), throw it away as instructed, but keep the autoinjector. If your doctor decides to stop your treatment, do not keep any leftover medicine unless your doctor tells you to. Throw away your medicine as instructed.

Amaryl.

Friday, September 21st, 2007

Amaryl is an oral medication used to treat type 2 (non-insulin-dependent) diabetes when diet and exercise alone fail to control abnormally high levels of blood sugar. Like other diabetes drugs classified as sulfonylureas, Amaryl lowers blood sugar by stimulating the pancreas to produce more insulin. Amaryl is often prescribed along with the insulin-boosting drug Glucophage. It may also be used in conjunction with insulin and other diabetes drugs. 

Always remember that Amaryl is an aid to, not a substitute for, good diet and exercise. Failure to follow a sound diet and exercise plan may diminish the results of Amaryl and can lead to serious complications such as dangerously high or low blood sugar levels. Remember, too, that Amaryl is not an oral form of insulin, and cannot be used in place of insulin. 

Do not take more or less of this medication than directed by your doctor. Amaryl should be taken with breakfast or the first main meal.

If you miss a dose… 

Take it as soon as you remember. If it is almost time for the next dose, skip the one you missed and go back to your regular schedule. Do not take 2 doses at the same time. 

Storage instructions… 

Amaryl should be stored at room temperature in a well-closed container. 

Side effects cannot be anticipated. If any develop or change in intensity, tell your doctor as soon as possible. Only your doctor can determine if it is safe for you to continue taking Amaryl. 

More common side effects may include:
Anemia and other blood disorders, blurred vision, diarrhea, dizziness, headache, itching, liver problems and jaundice, muscle weakness, nausea, sensitivity to light, skin rash and eruptions, stomach and intestinal pain, vomiting

 Amaryl, like all oral antidiabetics, can result in hypoglycemia (low blood sugar). The risk of hypoglycemia can be increased by missed meals, alcohol, fever, injury, infection, surgery, excessive exercise, and the addition of other medications such as Glucophage or insulin. To avoid hypoglycemia, closely follow the dietary and exercise regimen suggested by your doctor. 

Avoid Amaryl if you have ever had an allergic reaction to it. 

Do not take Amaryl to correct diabetic ketoacidosis (a life-threatening medical emergency caused by insufficient insulin and marked by excessive thirst, nausea, fatigue, and fruity breath). This condition should be treated with insulin. 

It’s possible that drugs such as Amaryl may lead to more heart problems than diet treatment alone, or treatment with diet and insulin. If you have a heart condition, you may want to discuss this with your doctor. 

When taking Amaryl, you should check your blood and urine regularly for abnormally high sugar (glucose) levels. The effectiveness of any oral antidiabetic, including Amaryl, may decrease with time. This may occur because of either a diminished responsiveness to the medication or a worsening of the diabetes. 

Even people with well-controlled diabetes may find that stress such as injury, infection, surgery, or fever triggers a loss of control. If this happens, your doctor may recommend that you add insulin to your treatment with Amaryl or that you temporarily stop taking Amaryl and use insulin instead.

Mevacor.

Thursday, September 20th, 2007

MEVACOR (Lovastatin) is a cholesterol lowering agent isolated from a strain of Aspergillus terreus. After oral ingestion, lovastatin, which is an inactive lactone, is hydrolyzed to the corresponding Beta-hydroxacid form. This is a principal metabolite and an inhibitor of 3-hydroxy-3- menthylglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, which is an early and rate limiting step in the biosynthesis of cholesterol.  The involvement of low-density lipoprotein (LDL) cholesterol in atherogenesis has been well- documented in clinical and pathological studies, as well as in many animal experiments. Epidemiological studies have established that (high density lipoprotein) cholesterol are both risk factors for coronary heart disease. The Lipid Research Clinics Coronary Primary Prevention Trial (LRC-CPPT), coordinated by the National Institutes of Health (NIH) studied men aged 35-59 with total cholesterol levels 265mg/dL (6.8 mmol/L) or greater and triglyceride levels not more than 300 mg/dL (3.4 mmol/L). This seven-year, double-blind, placebo-controlled study demonstrated that lowering LDL cholesterol with diet and cholestyamine decreased the combined rate of coronary heart disease death plus non-fatal myocardial infarction.  

MEVACOR has been shown to reduce both normal and elevated LDL cholesterol concentrations. LDL is formed from VDL and is catabolized predominantly by the high affinity LDL receptor. The mechanism of the LDL-lowering effect of MEVACOR may involve both reduction of VLDL cholesterol concentration, and induction of the LDL receptor; leading to reduced production and/or increased catabolism of LDL cholesterol. Apolipoprotein B also falls substantially during treatment with MEVACOR. Since each LDL particle contains one molecule of apolipoprotein B, and since little apolipoprotein B is found in other lipoproteins, this strongly suggests that MEVACOR does not merely cause cholesterol to be lost from LDL, but also reduces the concentration of circulating LDL particles. In addition, MEVACOR can produce increases of variable magnitude in HDL cholesterol, and modestly reduces VLDL cholesterol and plasma triglycerides (see Tables I-IV under Clinical Studies). The effects of MEVACOR or Lp(a) fibrinogen, and certain other independant biochemical risk markers for coronary heart disease are unknown.  

MEVACOR is a specific inhibitor of HMG-CoA to mevalonate. The conversation of HMG-CoA to mevalonate is an early step in the biosynthetic pathway for cholesterol.
Lovastatin is a lactone which is readily hydrolyzed in vivo to the corresponding B-hydroxyacid, a potent inhibitor of HMG-CoA reductase. Inhibition of HMG-CoA reductase is the basis for an assay in pharmacokinetic studies of the B-hydroxyacid metabolites (active inhibitors) and, following base hydrolysis, active plus latent inhibitors (total inhibitors) in plasma following administration of lovastatin.

 Following an oral dose of 14C-labeled lovastatin in man, 10% of the dose was excreted in urine and 83% in feces. The latter represents absorbed drug equivalents excreted in bile, as well as any unabsorbed drug. Plasma concentrations of total radio activity (lovastatin plus 14C- metabolites) peaked at 2 hours and declined rapidly to about 10% of peak by 24 hours postdose. Absorption of lovastatin, estimated relative to an intravenous reference dose, in each of four animal species tested, averaged about 30% of an oral dose. In animal studies, after oral dosing, lovastatin had high selectivity for the liver, where it achieved substantially higher concentrations than in nontarget tissues. Lovastatin undergoes extensive first-pass extraction in the liver, its primary site of action, with subsequent excretion of drug equivalents in the bile. As a consequence of hepatic extraction of lavastatin, the availability of drug to the general circulation is low and variable. In a single dose study in four hypercholesterolemic patients, it was estimated that less than 5% of an oral dose of lovastatin reaches the general circulation as active inhibitors. Following administration of lovastatin tablets the coefficient of varation, based on between-subject variability, was approximately 40% for the area under the curve (AUC) of total inhibitory activity in the general circulation.  

Both lovastatin and its B-hydroxyacid metabolite are highly bound (95%) to human plasma proteins. Animal studies demonstrated that lovastatin crosses the blood-brain and placental barriers.  

The major active metabolites present in human plasma are the B-hydroxyacid of lovastatin, its 6- hydroxy derivative, and two additional metabolites. Peak plasma concentrations of both active and total inhibitors were attained within 2 to 4 hours of dose administration. While the recommended therapeutic dose range is 10 to 80 mg/day, linearity of inhibitory activity in the general circulation was established by a single dose study employing lovastatin tablet-dosages from 60 to as high as 120 mg. With a once-a-day dosing regimen, plasma concentrations of total inhibitors over a dosing interval achieved a steady state between the second and third days of therapy and were about 1.5 times those following a single dose. When lovastatin was given under fasting condition, plasma concentrations of total inhibitors were on average about two- thirds those found when lovastatin was administered immediately after a standard test meal.  

In a study of patients with severe insufficiency (creatinine clearance 10-30 mL/min) , the plasma concentrations of total inhibitors after a single dose of lovastatin were approximately two-fold higher than those in healthy volunteers.
MEVACOR has been shown to be highly effective in reducing total LDL cholesterol in the heterozygous familial and non-familial forms of primary hypercholesterolemia and in mixed hyperlipidemia. A marked response was seen within 2 weeks, and the maximum therapeutic response occurred within 4-6 weeks. The response was maintained during continuation of therapy. Single daily doses given in the evening were more effective than the same dose given in the morning, perhaps because cholesterol is synthesized mainly at night. In multicenter, double-blind studies in patients with familial or non-familial hypercholesterolemia, MEVACOR administered in doses ranging from 10 mg q.p.m. to 40 mg b.i.d. was compared to placebo. MEVACOR consistently and significantly decreased total plasma cholesterol (TOTAL- C), LDL cholesterol (LDL-C), total cholesterol/HDL cholesterol (TOTAL-C/HDL) ratio and LDL cholesterol/HDL-C) ratio. In addition, MEVACOR produced increases of variable magnitude in HDL cholesterol (HDL-C), and modestly decreased VLDL cholesterol (VLDL-C) and plasma triglycerides (TRIG).
(see Tables I through IV for dose response results).

Fosamax.

Wednesday, September 19th, 2007

Fosamax is indicated for treatment and prevention of osteoporosis in postmenopausal women. For the treatment of osteoporosis, Fosamax increases bone mass and reduces the incidence of fractures, including those of the hip and spine. It is also indicated for the prevention of osteoporosis, treatment to increase bone mass in men with osteoporosis, treatment of glucocorticoid. It is used to treat induced osteoporosis in men and women receiving glucocorticoids in a daily dosage equivalent to 7.5 mg or greater of prednisone and who have low bone mineral density, treatment of Paget’s disease of bone in men and women.

   Fosamax comes as a tablet to take by mouth. It should be taken once a day in the morning on an empty stomach. Fosamax should be taken with a full glass (6-8 ounces) of plain water. Wait at least 30 minutes after taking Fosamax before you eat, drink, or take other medications. Do not take Fosamax with mineral water, coffee, orange juice, milk, or other dairy products. Do not suck or chew the tablet; swallow the tablet whole. Do not lie down for at least 30 minutes after taking Fosamax. Standing or sitting upright helps you get the full dose and decreases heartburn or the risk of injury to your esophagus.

  Before taking Fosamax, tell your doctor if you have a problem swallowing, such as a narrowing of the esophagus; have esophageal ulcers or an esophageal disease; have a condition that causes low levels of calcium in the body; have kidney disease; have stomach ulcers or other stomach or digestive problems; or are unable to stand or sit upright for at least 30 minutes. You may not be able to take Fosamax, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above. Fosamax is in the FDA pregnancy category C. This means that it is not known whether Fosamax will be harmful to an unborn baby. Do not take Fosamax without first talking to your doctor if you are pregnant or could become pregnant during treatment. It is not known whether Fosamax passes into breast milk. Do not take Fosamax without first talking to your doctor if you are breast-feeding a baby.

   If you take Fosamax every day and you miss a dose, skip that dose and take the next regularly scheduled dose the following day. Missing one dose will not affect your treatment. Do not take two tablets at the same time. If you take a Fosamax once a week and you miss a dose, take the missed dose on the morning after you remember. Do not take two tablets on the same day. Return to taking one tablet once a week, as originally scheduled on your chosen day. 

Stop taking Fosamax if you experience any of the following serious side effects: an allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives); Seek emergency or talk to your doctor if you have difficulty or pain when swallowing; chest pain; pain or burning under the ribs or in the back; or new or worsening heartburn. Other, less serious side effects may be more likely to occur. Continue to take Fosamax and talk to your doctor if you experience abdominal discomfort; stomach upset, nausea, vomiting, diarrhea, or constipation; headache; muscle, bone, or joint soreness or aches; eye pain; a rash; or an altered sense of taste. Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

Kamagra.

Monday, September 17th, 2007

ED or Erectile Dysfunction is quite common with men, which had led chemists and druggists to come up with various medical remedies to it. The good news is that this sexual dysfunction or impotence is curable. Of all medication available in the stores today, Kamagra has made a distinctive mark as an effective answer to the treatment of ED.

Kamagra or Sildenafil Citrate (its generic name) is one of its kind, being the first significant oral medication for ED, which is widely popular now. It is same as the 100mg Viagra. Only the color is different. It is found in two forms tablet and jelly. The interesting trivia surrounding Kamagra is that it was originally prepared to improve blood flow into the heart and soothe cardiovascular problems. But it proved more effective in boosting sexual abilities and the erection of the penis. Thereafter, Kamagra was approved by FDD and it gripped the market as a surefire remedy for ED.


It’s meant for oral ingestion and is manufactured in pills of 25mg, 50mg and 100mg. It is recommended that you should take this medicine in an empty stomach about an hour before intercourse. In full stomach, the efficiency is considerably reduced. This tablet is absorbed into your blood approximately 30 to 60 minutes after the intake and start acting on your system by inhibiting the enzyme PDE5 (phosphodiesterase type) found in penis. This enzyme is the main deterrent for proper erection as it restricts the relaxation of the penis muscles. Kamagra, when fully absorbed, inhibits PDE5 and thereby relaxes the muscles to allow healthy erection. But you need not worry if you don’t indulge in any sexual activity after its consumption. It will be automatically eliminated out of your body.

Like all pills, even this has its side effects; but with Kamagra, the fallouts are mild and short-lived. Congestion, diarrhea, headaches, urinary tract infections, facial flushing, etc. are some of its side effects. However, the effectiveness of this oral medicine Kamagra has been tested over the years and across all age groups. Kamagra-treated patients have shown 80% improvement in terms of erection, penetration and maintaining the erection over a longer period of time.

However, it is important to remember that Kamagra should not be consumed just because you haven’t had an intercourse for a long time. In such a case, it is always advised to consult a medical practitioner. Also, Kamagra is not provided without a prescription and even if you have ordered it online, your medical profile is reviewed before the delivery.

Adalat.

Friday, September 14th, 2007

Adalat GITS reduces cardiovascular risk by reducing blood pressure and improving endothelial function. It should be used in the context of a comprehensive plan to reduce cardiovascular risk in a wide range of patients with hypertension - with or without additional risk factors. 

Take exactly as directed by your physician and follow the instructions in the product leaflet. Swallow whole. Do not break, crush, or chew before swallowing. Avoid drinking grapefruit juice while taking this medicine. 

If you miss a dose of this medicine, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.  

Possible side effects associated with use of Adalat include dizziness, lightheadedness, headache, weakness, constipation, flushing, nausea, or heartburn. If any of the symptoms listed above persist or are especially bothersome, consult your physician. More serious side effects are also possible. Consult your physician as soon as possible if you experience tender, bleeding, or swollen gums; irregular pulse; shortness of breath; or swelling of the feet or hands. 

The effect of Adalat on you may change if you are using certain other drugs at the same time or if you have certain medical conditions. Tell your physician about all prescription and over-the-counter medicine that you are taking. You may require special supervision if you are taking cimetidine or intravenous (iv) calcium. 

Tell your physician about any other medical conditions, especially narrowing of the intestines (stricture), allergies, pregnancy, or breast-feeding. Adalat treatment is not recommended if you have a history of low blood pressure. Do not quit using Adalat without first consulting your physician. Adalat may make you dizzy. Do not drive or perform any other activity that require alertness until you know how Adalat affects you. Before you begin taking any new medicine, either prescription or over-the-counter, consult your physician. Take good care of your gums while you are using Adalat. Carefully brush and floss your teeth. For women: if you plan on becoming pregnant, discuss with your physician the benefits and risks of using this medicine during pregnancy. If overdose is suspected, seek emergency medical help.

Cialis.

Thursday, September 13th, 2007

Let love happen when the moment is right. Cialis helps you consummate passion play when a real moment turns into the right moment. You need not to worry about the time limit as cialis facilitate you to enjoy a spontaneous love reaction although you have 36 hours to calm down and take your time.

Cialis is the only erectile dysfunction prescription medicine that has been clinically proven to not only work fast, but also up to 36 hours and that is the maximum time being offered by an erectile dysfunction drug. And believe us Cialis is one and only appropriate partner for romance and relaxation to come back into your life. This single drug can initiate work as soon as after 16 minutes and remnants effective for up to 36 hours.

 Now what is erectile dysfunction or impotence? It’s also known as sexual dysfunction. In this condition of sexual dysfunction a man cannot get, or keep, a hard erect penis needed for proper sexual activity or sexual intercourse. Men facing such diseases should seek medical attention.

 Cialis is an oral drug to cure Erectile Dysfunction problems. Proper investigation should be made before you take cialis. But consider the thing that it does not protect you and your partner from sexually transmitted diseases.

 Cialis is emerging a popular erectile dysfunction drug during this time. Lilly the maker of cialis drug is planning to launch its once daily version. This new version of cialis can be taken all the time, which abolish the need to plan sex within a limited timeframe. More over this new cialis version has been aimed at men who await sexual activity at least twice a week. First of all in such circumstances, nitrates should still only be administered under close medical supervision with appropriate hemodynamic monitoring, therefore, patients who experience anginal chest pain after taking cialis pills should seek immediate medical attention.

 Cialis pills is only for men with ed, therefore Cialis pills is not for women or children, and Cialis pills must be used only under a healthcare professional’s care.

 However, physicians should advise patients to stop use of all inhibitors, including cialis pills, and seek medical attention in the event of a sudden loss of vision in one or both eyes, then such an event may be a sign of non-arteritic anterior ischemic optic neuropathy, a cause of decreased vision, including permanent loss of vision that has been reported rarely postmarketing in temporal association with the use of all inhibitors.

Viagra.

Wednesday, September 12th, 2007

Viagra, an oral therapy for erectile dysfunction, is the citrate salt of sildenafil, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). 

The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. NO then activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation in the corpus cavernosum and allowing inflow of blood. Sildenafil has no direct relaxant effect on isolated human corpus cavernosum, but enhances the effect of nitric oxide (NO) by inhibiting phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP in the corpus cavernosum. When sexual stimulation causes local release of NO, inhibition of PDE5 by sildenafil causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum. Sildenafil at recommended doses has no effect in the absence of sexual stimulation. 

Studies in vitro have shown that sildenafil is selective for PDE5. Its effect is more potent on PDE5 than on other known phosphodiesterases (10-fold for PDE6, >80-fold for PDE1, >700-fold for PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11). The approximately 4,000-fold selectivity for PDE5 versus PDE3 is important because PDE3 is involved in control of cardiac contractility. Sildenafil is only about 10-fold as potent for PDE5 compared to PDE6, an enzyme found in the retina which is involved in the phototransduction pathway of the retina. This lower selectivity is thought to be the basis for abnormalities related to color vision observed with higher doses or plasma levels (see Pharmacodynamics). 

In addition to human corpus cavernosum smooth muscle, PDE5 is also found in lower concentrations in other tissues including platelets, vascular and visceral smooth muscle, and skeletal muscle. The inhibition of PDE5 in these tissues by sildenafil may be the basis for the enhanced platelet antiaggregatory activity of nitric oxide observed in vitro, an inhibition of platelet thrombus formation in vivo and peripheral arterial-venous dilatation in vivo.

Ultram.

Tuesday, September 11th, 2007

Ultram is a type of narcotic-like oral pain reliever that is often prescribed to treat low back pain. Ultram (tramadol) was approved by the FDA in 1998 and acts centrally (in the brain) to modulate the sensation of pain; it has no anti-inflammatory effect, however. Its mechanism of action is similar to acetaminophen (e.g. Tylenol), but Ultram is a stronger pain reliever than acetaminophen and has a weak narcotic effect.While Ultram is technically a narcotic or opioid pain medication, it is different from typical narcotics in that patients do not build up a tolerance with extended usage and there is a very low incidence of addiction. With other narcotics there is a general tendency to escalate the dosage of the medicine with time and a chance of addiction.
Ultram is prescribed to control moderate to moderately severe low back pain or chronic pain, or as an intermediary step between over-the-counter pain relievers such as Tylenol or ibuprofen and narcotic pain killers. Other indications for the pain reliever Ultram may include:

       To treat postoperative pain, especially in patients who do not want or need stronger narcotics like Vicodin,  Percocet or Oxycontin, but for whom Tylenol is not strong enough.

 

       To control pain that flares up from time to time, although it is recommended that the cause be evaluated to determine if other treatment (such as physical therapy) might minimize the pain flares.

 The regularly prescribed dose is one or two 50mg tablets every four to six hours, not to exceed eight pills a day. Exceeding the prescribed dose may lead to potentially serious complications, such as respiratory depression or seizures.

 As with all pain medications, Ultram has several potential side effects and risks. Several of the more common risks include:Drug interactions. Care should be taken if the patient is also taking antidepressant medications, as a combination of Ultram and antidepressant medications can lead to seizures. Alcohol. Ultram should also not be taken in conjunction with alcohol, tranquilizers, or narcotics because the effects are additive and it may impair mental and physical function. Specifically, Ultram and alcohol are both respiratory depressants, so breathing may be significantly impaired if Ultram and alcohol are combined. Pregnancy risk. Ultram should not be taken by women who may be pregnant.

Tolerance. Ultram is not well tolerated by everyone, and some people report feeling “spacey” or “unusual” while on the medication.

 History of addiction. Patients who have been addicted to other narcotics or alcohol should not take Ultram.