Thursday, February 8, 2007

Phentermine

GENERIC NAME: phentermine
BRAND NAMES: Adipex-P, Obenix, Oby-Trim

DRUG CLASS AND MECHANISM: Phentermine is in a class of drugs called anorectics which decrease appetite by possibly changing brain levels of serotonin. Phentermine is a nervous system stimulator like the amphetamines, causing stimulation, elevation of blood pressure, and faster heart rates.

Obesity is usually defined as being 20% over ideal weight with resultant increase in certain diseases including high cholesterol levels, heart disease, high blood pressure, gallbladder disease, type II diabetes mellitus, hardening of the arteries, and degenerative arthritis. Weight loss decreases blood pressure, cholesterol levels, and improves diabetes control.

PRESCRIPTION: yes

GENERIC AVAILABLE: yes

PREPARATIONS: Tablets: 30mg, 37.5mg.

STORAGE: Phentermine should be stored in a tight container at room temperature.

PRESCRIBED FOR: Phentermine is usually used as a short- term drug along with diet and behavior modification to treat obesity. Recently, it has been combined with diet and fenfluramine (Pondimin) and used over longer terms in selected obesity patients (P & P diets) with some favorable long-term modest weight loss.

DOSING: Phentermine should be taken after breakfast; evening doses should be avoided because of secondary insomnia.

DRUG INTERACTIONS: Phentermine should not be taken by patients with glaucoma, hyperthyroidism, or a history of drug abuse or psychotic illnesses. Phentermine is not recommended in patients with high blood pressure that is not well controlled. Patients on phentermine should have their blood pressure closely followed. Insulin requirements may change in patients on phentermine; alcohol can cause a drug interaction. Abrupt stoppage of the drug can cause withdrawal with fatigue and depression. Phentermine is potentially addicting. Phentermine is not recommended for patients with symptomatic heart disease including rhythm problems.

SIDE EFFECTS: Side effects include diarrhea, dry mouth, constipation, an unpleasant taste, hives, impotence, palpitations, high blood pressure, and fast heart rates. Central nervous system side effects include overstimulation, insomnia, restlessness, tremor, and dizziness.

Wednesday, January 17, 2007

Viagra - Sildenafil


What is Viagra?


• Viagra relaxes muscles and increases blood flow to particular areas of the body.
• Sildenafil under the name Viagra is used to treat erectile dysfunction (impotence) in men. Another brand of sildenafil is Revatio, which is used to treat pulmonary arterial hypertension and improve exercise capacity in men and women.
• Viagra may also be used for purposes other than those listed here.

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History

Sildenafil (compound UK-92,480) was synthesized by a group of pharmaceutical chemists working at Pfizer's Sandwich, Kent research facility. It was initially studied for use in hypertension (high blood pressure) and angina pectoris (a form of ischaemic cardiovascular disease). Phase I clinical trials under the direction of Ian Osterloh suggested that the drug had little effect on angina, but that it could induce marked penile erections.[1][2] Pfizer therefore decided to market it for erectile dysfunction, rather than for angina. 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 pill approved to treat erectile dysfunction in the United States, and offered for sale in the United States later that year.[3] It soon became a great success: annual sales of Viagra in the period 1999–2001 exceeded $1 billion.

The British press portrayed Peter Dunn and Albert Wood as the inventors of the drug, a claim which Pfizer disputes.[4] Their names are on the manufacturing patent application drug, but Pfizer claims this is only for convenience.

Viagra is available as blue pills with a characteristic shape

Even though sildenafil is only available by prescription from a doctor, it was advertised directly to consumers on US TV (famously being endorsed by Bob Dole and Football star Pele). Numerous sites on the Internet offer Viagra for sale after an "online consultation", a mere web questionnaire. The "Viagra" name has become so well known that many fake aphrodisiacs now call themselves "herbal Viagra" or are presented as blue tablets imitating the shape and colour of Pfizer's product. Viagra is also informally known as "Vitamin V", "the Blue Pill", as well as various other nicknames.

Pfizer's worldwide patents on sildenafil citrate will expire in 2011–2013. The UK patent held by Pfizer on the use of PDE5 inhibitors (see below) as treatment of impotence was invalidated in 2000 because of obviousness; this decision was upheld on appeal in 2002.

Mechanism of action

Part of the physiological process of erection involves the parasympathetic nervous system causing the release of nitric oxide (NO) in the corpus cavernosum of the penis. NO binds to the receptors of the enzyme guanylate cyclase which results in increased levels of cyclic guanosine monophosphate (cGMP), leading to smooth muscle relaxation (vasodilation) in the corpus cavernosum, resulting in increased inflow of blood and an erection.

Sildenafil is a potent and selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum. The molecular structure of sildenafil is similar to that of cGMP and acts as a competitive binding agent of PDE5 in the corpus cavernosum, resulting in more cGMP and better erections. Without sexual stimulation, and therefore lack of activation of the NO/cGMP system, sildenafil should not cause an erection. Other drugs that operate by the same mechanism include tadalafil (Cialis®) and vardenafil (Levitra®).

Sildenafil is metabolised by hepatic enzymes and excreted by both the liver and kidneys. If taken with a high-fat meal, there may be a delay in absorption of sildenafil and the peak effect might be reduced slightly as the plasma concentration will be lowered.

Dosage and price

As with all prescription drugs, proper dosage is at the discretion of a licensed medical doctor. The dose of sildenafil is 25 mg to 100 mg taken once per day between 30 minutes and 4 hours prior to sexual intercourse.

It is usually recommended to start with a dosage of 50 mg and then lower or raise the dosage as appropriate. The drug is sold in three dosages (25, 50, and 100 mg), all three costing about US$10 per pill. Name-brand Viagra sildenafil is not scored and a fairly hard coating makes it more difficult to accurately cut the pills in half, even with a pill cutter.

Contraindications

Contraindications include:
When taking nitric oxide donors, organic nitrites and nitrates, such as glyceryl trinitrate, sodium nitroprusside, amyl nitrite ("poppers")[5]
In men for whom sexual intercourse is inadvisable due to cardiovascular risk factors
Severe hepatic impairment (decreased liver function)
Severe impairment in renal function
Hypotension (low blood pressure)
Recent stroke or heart attack
Hereditary degenerative retinal disorders (including genetic disorders of retinal phosphodiesterases)

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Cialis - Tadalafil

What is Cialis?

Cialis relaxes muscles and increases blood flow to particular areas of the body.
Cialis is used to treat erectile dysfunction (impotence).
Cialis may also be used for purposes other than those listed in this medication guide.



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Cialis drug history


The history of Cialis cannot be discussed without mentioning Pfizer's drug, Viagra. The FDA's approval on March 27, 1998, led this prescription drug, Viagra, to a ground breaking success in just the first year of introduction as Pfizer sold drugs worth over a billion dollars. However, things changed considerably for the giant of erectile dysfunction drugs when the FDA also approved Levitra in August 19, 2003, and Cialis in November 21, 2003. In 1993 the drug company Icos began studying IC351, which is a PDE5 enzyme inhibitor, and this is basically the process through which the erectile dysfunction drugs work. In 1994, Pfizer scientists discovered that Sildenafil Citrate, which is a white crystalline powder that temporarily normalizes erectile function of the penis by blocking an enzyme known to inhibit the production of a chemical that causes erections, caused the heart patients that were participating in a clinical study of a heart medicine to have erections. Although the scientists were not testing the chemical compound IC351 for erectile dysfunction, the compound seemed to have a side effect which could potentially be worth millions, if not billions of dollars. Soon Icos received its very first patent in 1994 on IC351, and the clinical trials of phase I took place in 1995. In 1997, phase II clinical studies began and Icos performed its first study on patients with erectile dysfunction. Phase II lasted about two years, and after that phase III began.

In 1998, ICOS Corporation, and Eli Lilly and Company, commercialized the drug for erectile dysfunction, and two years later they filed a new drug application with the U.S. Food and Drug Administration for IC351; the only difference was that this time they decided to call the drug, Cialis. In May of 2002, Icos and Eli Lilly and Company reported to the American Urological Association that the phase III tests show that Cialis works for up to 36 hours, and one year later Icos and Eli Lilly and Company received the U.S. FDA's approval for Cialis. One advantage that Cialis has over Viagra is that tadalafil has an half-life of 17.5 hours[1] (and thus Cialis is advertised to work for up to 36 hours) as compared to 4 hours half-life for sildenafil (Viagra).

Tadalafil is a drug used to treat male erectile dysfunction (impotence). It was developed by the biotechnology firm ICOS and marketed worldwide by Eli Lilly and Company under the brand name Cialis.

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Levitra - Vardenafil (Erection)


Important Safety and Dosing Information

LEVITRA is a prescription medicine that is used to treat erectile dysfunction (ED). Men taking nitrate drugs, often used to control chest pain (also known as angina), should not take LEVITRA. Such combinations could cause blood pressure to drop to an unsafe level.



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What is Levitra?
• Levitra relaxes muscles and increases blood flow to particular areas of the body.
• Levitra is used to treat erectile dysfunction (impotence).
• Levitra may also be used for purposes other than those listed in this medication guide.

History

Vardenafil was co-marketed by Bayer Pharmaceuticals and (GSK) under the trade name Levitra. As of 2005, the co-promotion rights of GSK on Levitra have been "transferred back" to Bayer in many markets outside of the United States. In Italy, Bayer markets the product as Levitra and GSK markets the product as Vivanza. Due to European Union trade rules, parallel imports may result in the Vivanza branded packs being seen alongside Levitra packs in pharmacies in other EU member states.

As with all ED drugs, there is a rare risk of an erection lasting longer than four hours. To avoid long-term injury, seek immediate medical attention. LEVITRA does not protect against sexually transmitted diseases. In rare instances, men taking PDE5 inhibitors (oral erectile dysfunction medicine, including LEVITRA) reported a sudden decrease or loss of vision in one or both eyes. It is not possible to determine whether these events are related directly to these medicines or to other factors. If you experience sudden decrease or loss of vision, stop taking PDE5 inhibitors, including LEVITRA, and call a doctor right away.


Discuss your medical conditions, including heart problems, and medications, including alpha blockers prescribed for prostate problems or high blood pressure, with your doctor to ensure LEVITRA is right for you and that you are healthy enough for sexual activity.


The starting dose of LEVITRA is 10 mg taken no more than once per day. Your doctor will decide the dose that is right for you. In patients taking alpha blockers, your doctor may start you on a lower dose of LEVITRA. In patients taking certain medications such as ritonavir, indinavir, ketoconazole, itraconazole, and erythromycin, lower doses of LEVITRA are recommended, and time between doses of LEVITRA may need to be extended.


In clinical trials, the most commonly reported side effects were headache, flushing, and stuffy or runny nose. LEVITRA is available in 2.5-mg, 5-mg, 10-mg, and 20-mg tablets.


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