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PROPECIA [Finasteride] an Overview             

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PROPECIA [Finasteride], one of the newest medications for the treatment of androgenic alopecia and is a product of Merck & Co. Before commenting on the drug, a few lines on what is androgenic alopecia.

Androgenic alopecia is a hereditary disorder due to excessive conversion of testosterone to dihydrotestosterone in the scalp skin in genetically susceptible men and women. The dihydrotestosterone causes shrinking of the local terminal hair follicles to miniaturized hair follicles. The plasma levels of testosterone are appropriate for the sex. The onset of androgenic alopecia in both the sexes is early in life, often in teens. The miniaturized hair of various lengths and diameters are the hallmark of this condition.

PROPECIA [Finasteride] is a 5-alpha reductase inhibitor. 5-alpha reductase is an enzyme that converts testosterone to dihydrotestosterone. The recognition potential value of PROPECIA [Finasteride] in the treatment of androgenic alopecia was based upon the observation that men congenitally deficient in 5-alpha reductase had low levels of dihydrotestosterone and did not develop male pattern baldness or prostate enlargement. In contrast, balding areas of the scalp have increased levels of dihydrotestosterone and smaller hair follicles than do non-balding areas There are two types of 5-alpha reductase: - Type 1: This is found in the sebaceous glands [These glands secrete a substance called sebum] - Type 2: This is found in the hair follicles.

PROPECIA [Finasteride] is a type 2 class of 5-alpha reductase inhibitor and it suppresses both, the serum and the tissue levels of dihydrotestosterone.

PROPECIA [Finasteride] – 1 mg per day, has been shown to increase hair growth in up to 80% of men when given over a 2 year period. This drug is taken orally, 1mg per day. PROPECIA [Finasteride] increases the hair counts in both the vertex of the scalp and the frontal area of the scalp. The response to PROPECIA [Finasteride] is better in the frontal region of the scalp, which has a higher level of 5-alpha reductase than in the occipital region which has higher levels of aromatase. Increased hair growth can be observed as early as 3 months into treatment.

PROPECIA [Finasteride] is approved for use only in men. It is not sure if it is of any benefit to women, though doctors say that it can be tried in postmenopausal women. On December 22, 1997, the FDA approved PROPECIA [Finasteride] to treat male pattern hair loss. It is a FDA pregnancy category X drug. This means that PROPECIA [Finasteride] is known to cause birth defects in an unborn baby. Pregnant women should not touch broken tablets because of the potential for genital abnormalities in male fetuses, since it is widely believed that some absorption can take place through skin. No birth defects have e seen in female fetuses It is not known whether PROPECIA [Finasteride] passes into breast milk, and thus should not be taken during the lactation period. Male partners on PROPECIA [Finasteride] should use a protective device like condom while having intercourse since it may pass through semen, though Merck says that it is not an issue of concern. Side effects of PROPECIA [Finasteride] include: - Decreased libido - Erectile dysfunction - Ejaculation disorder - Decreased ejaculate volume - Depression These effects are seen in less than 2% of patients. Apart from the above stated there can be chances of gynaecomastia [enlarged male breasts]. However this condition is drug dependant and subsides on withdrawing the drug. Before starting this drug check if there is any of the following are present: - Liver disease or abnormal liver enzyme test - Bladder muscle disorder - Prostate cancer - Urethral stricture - Difficulty in micturation

The treatment with PROPECIA [Finasteride] must be continued or new hair growth will be lost.

Finasteride is also known to decrease the levels of serum prostate-specific antigen [PSA] which is used in prostrate cancer screening. It is used as a treatment in benign prostatic hyperplasia (BPH) in low doses, and prostate cancer in higher doses.

 

 

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XENICAL                      

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Xenical [Orlistat] marketed by Roche Labs is a drug designed to treat obesity.
Its primary is preventing the absorption of fats from the human diet, this leads to decrease in calorific intake.
In plain language it blocks some of the fat that we eat thereby keeping it from being absorbed by the body.

Xenical is used together with a reduced-calorie diet and weight maintenance to treat obesity in people with certain risk factors (such as diabetes mellitus, high blood pressure, and atherosclerosis, family history of stroke, heart attack, and high serum cholesterol and serum triglycerides.

But why do we need to keep obesity in check? Here’s the reason why.
Obesity is one of the leading causes of diabetes mellitus and hypertension in the world. The situation is so grim that, heart attack, which once used to be seen only in aged people [>50 years] is now commonly seen in people as young as 20-25years.
Obesity has not even spared our children who just can’t seem to get enough of the fast food culture.
Combine this with the stressful life and it becomes a deadly cocktail. Our sedentary lifestyle makes matters worse.

Observational epidemiologic studies have established a relationship between obesity and visceral fat and the risks for cardiovascular disease, type 2 diabetes, and certain forms of cancer, gallstones, certain respiratory disorders, and an increase in overall mortality. This suggests that weight loss, if maintained, may produce health benefits for obese patients who have or are at risk of developing weight-related co morbidities. The long-term effects of Xenical [Orlistat] on morbidity and mortality associated with obesity have not been established.
Obesity/Body Mass Index [BMI] can be calculated by the following formula: kg/m2
The normal range is 17.99 to 24.99. Above 30 is termed as obese and more than 40 is termed as morbid obesity.

The effects of Xenical [Orlistat] on weight loss and maintenance and related co-morbidities like type 2 diabetes mellitus, lipids and blood pressure were assessed in a study called the XENDOS, a 4 year study. The XENDOS study found a 37% reduction in the incidence of Type II Diabetes Mellitus, a significant difference
In one-year clinical trials carried out on humans, between 35.5% and 54.8% of subjects a 5% or greater decrease in body mass was achieved, although not all of this mass was necessarily fat. Between 16.4% and 24.8% achieved at least a 10% decrease in body mass. After discontinuation of Xenical [Orlistat], a majority of the subjects showed weight gain of up to 35% of the total weight they had lost.

Xenical [Orlistat], chemically a tetrahydrolipstatin is a saturated derivative of lipostatin which is a potent inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. But lipostatin is an unstable and complex compound, thus Xenical [Orlistat] which is a simple and stable compound was developed as an antiobesity drug.
Xenical [Orlistat] reversibly inhibits lipases, an enzyme that breaks down the triglycerides in the gastro-intestinal tract, especially in the lumen of the stomach and small intestine. It forms a covalent bond with the active serine residue site of gastric and pancreatic lipases. The inactivated enzymes thus cannot hydrolyze the dietary fat which is in the form of triglycerides. Meaning, the pancreatic and gastric lipases cannot hydrolyze the triglycerides from the fat in the diet into simpler monoglycerides and free fatty acids [FFAs].These unabsorbed triglycerides are then excreted in the stools in an undigested form. The resulting calorie deficit may lead to weight control.

Xenical [Orlistat] is metabolized mainly in the gastro-intestinal tract

Side effects and Contraindications:
The most common side effect of Xenical [Orlistat] is altered bowel movement habits. This is usually experienced during the initial weeks of treatment; though this may be seen throughout the regimen in rare cases. This is supported by the XENDOS study which found that of the 91% of subjects who suffered from gastrointestinal side effects in the first year only 36% had the gastrointestinal adverse effects during their fourth year of taking Xenical [Orlistat]. In case the side effects are severe then this should be immediately brought to the notice of the prescribing physician.
• Steatorrhea i.e. oily, loose stools seen as oily spotting on underwear or on clothing
• Feacal incontinence- urgent need to have a bowel movement along with flatus
• increased number of bowel movements
• difficulty controlling bowel movements
• gas with oily spotting
• loose stools
• oily or fatty stools
• pain or discomfort in the rectum/anus
• irregular menstrual periods
• headache
• anxiety
• hives
• rash
• itching
• difficulty breathing or swallowing
• severe or continuous abdominal pain
• Cold or flu-like syndrome.

Contraindications:
- Hypersensitivity to Xenical [Orlistat]
- Reduced gall bladder function
- Chronic Malabsorption syndrome
- Pregnancy [FDA Pregnancy category B drug] and lactation. Can be prescribed to the pediatric age group of elder than 10 years.

Precaution:
- Impaired liver profile
- Impaired pancreatic profile
- Obstructed bile duct
- History of hyperoxaluria, calcium oxalte nephrolithiasis
- Obesity due to any organic cause like hypothyroidism
- Any eating disorder like anorexia or bulimia
- If taking any other weight loss drug

Drug interactions:
- Amiodarone [antiarrhythimic]
- Cyclosporine
- Digoxin
- Warfarin

Special information:
Since Xenical [Orlistat] inhibits the body’s absorption of beta carotene and certain fat soluble vitamins, multivitamin supplements should be taken daily. This multivitamin can be taken 2 hours before or after having food. It can also be taken during midnight or in the morning.
Avoid fat rich food and prefer foodstuffs which are likely to contain less than 30% fat.

The recommended dose of XENICAL [Orlistat] is one 120-mg capsule three times a day with each main meal containing fat.during or up to 1 hour after the meal.

 

 

 

 

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Acomplia (Rimonabant), marketed by Sanofi-Aventis is a selective CB1 endocannabinoid receptor antagonist indicated for the treatment of obesity.

Its mechanism of action is to block the endogenous cannabinoid binding to neuronal CB1 receptors.

 

What is endocannabinoid system?

The endocannabinoid system is in the part of the brain that regulates metabolism, energy levels and appetite.

With reference to the above drug, endocannabinoid receptors on activation will increase the appetite. Hence, drugs like Acomplia (Rimonabant) will block this endocannabinoid receptor, eventually leading to a decrease in the appetite. It is the most advanced endocannabinoid receptor antagonist in clinical development and offers a novel therapeutic approach to appetite control and weight reduction

 

So what is obesity?

Obesity medically is defined on the basis of Body Mass Index which is the individual's body weight divided by the square of their height in kg/m². So, a BMI of 18.5 to 25 may indicate optimal weight; a BMI lower than 18.5 suggests the person is underweight while a number above 25 may indicate the person is overweight; a BMI below 17.5 may indicate the person has anorexia or a related disorder; a number above 30 suggests the person is obese (over 40, morbidly obese).

So technically speaking, those with their body mass index of 30 and above tend to fall in the high risk zone. It arises from the accumulation of excess fat in the body from over consumption of fatty foods and is now one of the most common nutritional disorders in the world.

Latest studies have corroborated the fact that obesity is a silent killer. It is associated with cardiovascular disease, especially angina and myocardial infarction, atherosclerosis and arteriosclerosis leading to cerebrovascular accidents/ strokes.

They also cause joint pains and are also associated with certain cancers like that of the breast or of the colon. The proportion of obese individuals in the developed countries has reached epidemic proportions. To put this picture in a better perspective, statistics show that one in five of all Americans are obese and one in three overweight.

In the presence of diabetes mellitus it forms a deadly combination and is termed as diabetisity. It shows more predilections to Type 2 diabetes mellitus

Various therapeutic strategies have been explored, including:

• Serotonin and nor adrenaline reuptake inhibitors (anorectic agents)
• Lipase inhibitors
• ß 3-adrenoreceptor agonists
• Leptin agonists
• Melanocortin-3 agonists

All these strategies have shown some amount of success.

Usually, after having cannabis these drug addicts suffer from extreme hunger pangs which these smokers refer to as ‘munchies’. This lead to the belief that cannabinoid is associated with hunger pangs and if this receptor is suppressed it will lead to decreased appetite which is what precisely the manufacturers of Acomplia (Rimonabant) Sanofi-Aventis did.

Rimonabant] prevents the endogenous cannabinoid binding to CB1 receptors in nerve cells. These CB1 receptors, when activated, stimulate appetite. Hence this drug blocks the activation of these CB1 receptors and thus reduces appetite.

 

Side Effects

1.     Nausea and vomiting------------------------------------------------------------- Nausea, vomiting and other gastrointestinal disorders were relatively common side effects of taking Acomplia.

2. Disorders of the nervous system------------------------------------------------ this category includes headaches, faintness and feeling dizzy.
3. Psychiatric Disorders------------------------------------------------------------- Including mood swings, anxiety, depression, irritability, sleep disorders and other similar disorders. The current advice is that you should not take this drug if you suffer from mental health problems. The drug is not suitable for those with continuing major depressive illness and/or antidepressive treatment.

 

Contraindications:

1. Any hypersensitivity to the drug or any of its ingredients.
2. Presence of liver damage.
3. Impaired renal function
4. Age more than 75 years and less than 16 years
5. Pregnant and lactating women.
6. In patients with lactose intolerance since it Acomplia contains lactose
7. It should only be used with caution in combination with CYP3A4 inhibitors, such as ketoconazole, ritonavir, Clarithromycin and related drugs.
8. It is not to be prescribed in patients with untreated psychiatric disease.

Acomplia [Rimonabant] taken for up to two years in conjunction with diet and exercise produces greater weight loss than the placebo, although most of the weight loss occurs in the first year.

 

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Kamagra (Generic Viagra) [sildenafil citrate], manufactured by Ajanta Pharma, Ltd, this drug is the first cyclic guanosine monophosphate [cGMP] specific phosphodiesterase type 5 enzyme inhibitor. This enzyme helps in regulating the blood circulation in the penile tissue. This leads to better penile erection.

Kamagra (Generic Viagra) is primarily indicated in the treatment of impotence [erectile dysfunction]

 

The compound sildenafil was synthesized in Pfizer’s research lab in Kent, England. Believe it or not, sildenafil was actually being studied for the treatment of hypertension and angina pectoris. Angina pectoris, or chest pain, caused by an insufficient supply of oxygen and decreased blood flow to the heart muscle. Angina is frequently the first sign of ischemic heart disease. However, during the phase 1 clinical trials, it was found that instead of having a remarkable action on angina, this drug was very effective in inducing penile erections, the main pathology behind erectile dysfunction.

The drug was patented in 1996, approved for use in erectile dysfunction by the Food and Drug Administration on March 27, 1998, becoming the first oral treatment approved to treat erectile dysfunction in the United States

Needless to say, this drug has become a household hit.

 

Erectile dysfunction:

Erectile dysfunction (ED) is defined as the inability of a man to achieve or maintain an erection sufficient for his sexual needs or the needs of his partner

Erection of the penis during coitus or otherwise is a result of increase in the blood flow of the arteries of the penis and simultaneous relaxation of the smooth muscle of corpora cavernosum. This whole process is due to the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP in turn, relaxes smooth muscle and resulting in an increase in the blood flow to the corpus cavernosum.

In erectile dysfunction, enough blood does not flow in the arteries of the penis to cause a sufficient erection.

Causes of erectile dysfunction:

With reduced libido:

-          hypogonadism

-          depression

With intact libido:

-          psychological problems, including anxiety

-          vascular insufficiency [atheroma]

-          neuropathic [diabetes mellitus, alcohol excess, multiple sclerosis]

-          drugs [beta blockers, thiazide diuretics]

An organic cause can be found out in about 50% of the cases of erectile dysfunction; the rest are either psychogenic in origin or are due to a psychiatric illness such as depression which requires appropriate drug treatment. Systemic diseases like chronic liver or kidney diseases and drug addiction are important causes and should be looked for. In case of any psychogenic problem, even the partner should be actively involved in the counseling therapy

The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum of the penile tissue during sexual stimulation. Nitric oxide 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. Kamagra (Generic Viagra) [sildenafil citrate] 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 nitric oxide, 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.

There are many types of PDE, each having varied function. The plus point of Kamagra (Generic Viagra) [sildenafil citrate] is that it is PDE 5 selective, though it can also act on the other types of PDE. In fact higher doses or plasma levels of the drug is thought to be associated with defects in color vision due to its action on PDE 6.Kamagra (Generic Viagra) [sildenafil citrate] has a 4,000-fold selectivity for PDE5 versus PDE3, which is concerned with cardiac contractility.

 

Indications:

-          Erectile dysfunction. This is the main indication whereas for the indications given below, sildenafil is not in the first line treatment regimen.

-          pulmonary arterial hypertension

-          prevention of high altitude pulmonary edema associated with altitude sickness

-          treatment of benign prostatic hypertrophy [BPH]-associated lower urinary tract symptoms [LUTS]

Indications under investigation:

-          Relieving female sexual dysfunction. Several studies have indicated the drug may be effective in improving libido and arousal in women taking selective serotonin uptake inhibitors (SSRIs)

-          Treatment of infertility. Women who have had repeated failures with in vitro fertilization (IVF) due to poor development of the endometrium [tissue that lines the uterus] may benefit from treatment with vaginal suppositories containing sildenafil.

-          Esophageal motility dysfunction (achalasia), since it can enhance nitric oxide production.

 

Contraindications:

 -  patients on nitric oxide drugs since sildenafil potentiate the hypotensive effects of  nitrates, and its administration to patients who are using organic nitrates, either regularly and/or intermittently, in any form is therefore contraindicated.

 - There is a degree of cardiac risk associated with sexual activity, especially in elderly people above the age of 60 years. There is increase incidence of mortality and morbidity with KAMAGRA (GENERIC VIAGRA) [sildenafil]

    - Severe hepatic impairment (decreased liver function)

    - Severe impairment in renal function

    - Hypotension (low blood pressure)

    - History of stroke or heart attack

    - Hereditary degenerative retinal disorders (including genetic disorders of retinal phosphodiesterases)

Side effects:

The most commonly reported side effects of KAMAGRA (GENERIC VIAGRA) are headache, flushing of the face, upset stomach, and nasal congestion.

Other less common side effects include, but are not limited to:

• vision problems, including sensitivity to light, blurred vision, and a color tinge to vision
• urinary tract infection
• diarrhea
• dizziness
• rash

Dosage:

Administered in the dose of 50 mg one hour before the intended sexual activity. Based on effectiveness and toleration, it can be increased to 100 mg or decreased to 25 mg.

 

 

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INTRODUCTION

Advancements in the field of science have a tremendous effect in the lifestyle of people around the world. The things which we were only conceiving in our minds a long time ago came into reality after years of research and testing of the greatest minds of every century. The pursuit for the elixir of life has become a race for most developed countries so a lot of them are investing a lot of money, time and effort just to bring quality life in every household around the globe, most especially to those who can afford.

 

With these evident realities at hand, it is undoubtedly a fact that aside from the prolonging of life span, production of goods which are luxurious and would give immediate satisfaction is also being held as a primary consideration. In medical science, one such thing that has brought so much change in the lifestyle of people is the manufacture of Viagra, a drug that has been popular among people of all ages and races for adding more color to one of the basic needs of humanity---sex.

 

BRIEF HISTORY

It is safe to remember that Viagra is not for everybody. Originally, Viagra was developed by Pfizer as a drug to help men who were suffering from chest pain. However, sildenafil citrate, the active ingredient of Viagra, as a heart medication did not show progress of attaining its purpose and studies were stopped in 1992. Yet, based on published information about some properties contained in sildenafil citrate, Pfizer researchers began to look at it as a treatment for erectile dysfunction. Erectile dysfunction can also be termed as impotence or the difficulty to have an erection or maintaining it among males. Re-evaluation for its effect on the ability of men with ED to engage in sexual activity, and the ability to achieve and maintain erection sufficient for satisfactory sexual activity was taken.

 

Later, the clinical trials conducted by the researchers found Viagra to be so effective that the FDA approved it only six months after submission, and without consulting an advisory committee of outside experts because there were no troubling questions and no significant side effects. In furtherance to its primary uses, Viagra is being tested against pulmonary hypertension in children and infertility in women.

 

HOW IT WORKS

Basically Viagra’s appearance is bluish, diamond-shaped tablets with 25mg, 50mg, or 100mg strengths embossed on one side, denoting tablet strength. It works by dilating blood vessels throughout the body, allowing blood to flow more readily to the heart, lungs and other organs. Moreover, Viagra relaxes smooth muscle contractions in the penis. Around 70 percent of men using it reported some improvement in achieving and maintaining an erection. Effects normally begin within 30 minutes and last about 4 hours.

 

Since Viagra is only for those who have erectile dysfunctions, the drug must be taken orally once a day, one hour before the sexual activity. Viagra is not meant to be taken regularly for a prolonged period. Just take it when you need it.

 

An important thing to remember also is, you should not take Viagra if you are using nitrate drugs to control angina pain because the combination of the nitrate drugs and Viagra can lower your blood pressure dangerously putting your life in danger. The combinations of drugs are life-threatening for you. If it gives you an allergic reaction, do not use it again. Also, if you have severe heart problems where sexual activity can be a danger to your life, do not take Viagra.

 

AFTER EFFECTS

Side effects of using Viagra include headache, flushed skin, and anxiety. Its serious risks can include distorted vision and priapism -- a painful, prolonged erection that may require medical intervention. Historically, 69 deaths were linked to Viagra during its first three months on the market so the U.S. Food and Drug Administration issued a warning against using it with amyl nitrate ("poppers"), nitroglycerin, and nitrous oxide since each dilates blood vessels, thus, a dangerous drop in blood pressure can result, leading to possible heart attack or stroke.

 

ADDICTIVE?

Probably yes. Firstly, men who take Viagra to obtain even greater pleasure from their sex life become so much used to the drug that they find their love life uninteresting without the use of Viagra, as compared to earlier. Secondly, to some men, the effect of Viagra may decrease with time hence these men are less likely to have a non Viagra erection as compared to earlier when they did not take Viagra. Moreover, some men with no performance problems except psychologically may take even far larger doses of the drug to satisfy their own perception of a satisfactory sexual performance.

 

CONCLUSION

With the facts given, the question now is, “Is it for you?” Think it over. Never rush.

 

 

 

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