Archive for the ‘Pharmacology’ Category
Sunday, March 23rd, 2008
PDE5 is a dimeric enzyme that is composed of two identical 100 kD proteins. There are four known isoforms of PDE5 ( PDE5A 1-4 ) ACC . No : NM - 03343I : these isoforms are products of a single gene and are formed by alternative splicing of mRNA . The enzymatic characteris- tics of [...]
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Sunday, March 23rd, 2008
Sildenafil is a competitive and reversible inhibitor of cGMP hydrolysis by the catalytic site of PDE5 . Sildenafil is an analog of cGMP , the PDE5 substrate , but PDE5 has - 1000-fold higher affinity for sildenafil than for cGMP. The purine ring of cGMP is mimicked by similar components in sildenafil , and this [...]
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Sunday, March 23rd, 2008
In all cells , the level of cGMP is primarily determined by the relative rates of cGMP synthesis by the GCs and its breakdown by PDEs. An imbal- ance between the synthesis ( e . g ., decreased release of nitric oxide due to penile nerve deterioration or endothelial cell damage ) and breakdown of [...]
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Sunday, March 23rd, 2008
Sharron H . Francis and Jackie D . Corkin
Light Hall Room 702 , Department of Molecular Physiology & Biophysics , Vanderbilt University School of Medicine , Nashville , TN 37232-0615 , ( ISA Introduction The roles of cAMP ( cyclic AMP ) and cGMP ( cyclic GMP ) in regulating myr- iad physiological and pathophysiological [...]
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Sunday, March 23rd, 2008
This is a book about real people . The men and women who pass through my office share intimate details of their lives that would otherwise never see the light of day were it not for this book . Nat- urally , names and details have been changed in order to preserve privacy , and […]
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Tuesday, March 4th, 2008
Tadalafil is a highly selective PDE5 inhibitor that is safe and efficacious
for the treatment of ED. Clinical evidence generally demonstrates
the favorable safety and efficacy profiles of the PDE5 inhibitors in most
patient populations, including men with stable ischemic heart disease
and those receiving therapy with antihypertensive agents (other than
a-blockers). These general properties also hold true for tadalafil, [...]
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Sunday, March 2nd, 2008
Although tadalafil, like other PDE5 inhibitors, is a vasodilator that may
augment the blood pressure-lowering effects of antihypertensive agents,
recent data show that tadalafil is safe in patients receiving two or more
concomitant antihypertensive agents. According to an analysis of
data from six placebo-controlled phase III studies of interactions between
tadalafil and commonly prescribed antihypertensive agents, a comparison
of patients receiving [...]
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Sunday, March 2nd, 2008
Another potential drug interaction exists between PDE5 inhibitors and
a blockers. In a drug-interaction study, when 20 mg of tadalafil was administered
to healthy subjects taking doxazosin (8 mg daily), an a1-adrenergic
blocker, there was a significant augmentation of the blood pressure-lowering effect of doxazosin. When 20 mg of tadalafil was administered to healthy
subjects taking 0.4-mg once-daily tamsulosin, [...]
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Sunday, March 2nd, 2008
Like other PDE5 inhibitors, clinical pharmacology studies show that
tadalafil (5–20 mg) potentiates the hypotensive effect of nitrates. This is thought to result from the combined effects of nitrates and tadalafil on the
NO-cGMP pathway. Therefore, administration of tadalafil to patients who
are using any form of organic nitrates, either regularly or intermittently, is
contraindicated.
Results of a recent placebo-controlled [...]
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Sunday, March 2nd, 2008
The long-term safety of tadalafil has been assessed in 1173 patients
enrolled in an ongoing, international, open-label study. Of the patients
enrolled, most (870) had been exposed to 10 or 20 mg of tadalafil daily
for at least 1 yr, with 991 being exposed to these dosages for more than
6 mo. Adverse events experienced by patients in the [...]
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