Substitution of phenylephrine for pseudoephedrine as a nasal decongeststant.

An illogical way to control methamphetamine abuse PE

PE is a poor substitute for PDE as an orally administered decongestant as it is extensively metabolized in the gut and its efficacy as a decongestant is unproven. the efficacy of PE as a nasal decongestant has received little attention in the literature. PE differs chemically from adrenaline only in the absence of one hydroxyl group from the benzene ring. PE contains a single chiral carbon atom and thus exists as an enantiomeric pair of stereoismers. It is used commercially as the (-)-enantiomer [10] as PE hydrochloride.PE is a relatively selective a1 agonist. It has weak a2 adrenoceptor agonist activity and low b agonist activity. after oral administration PE is subject to extensive presystemic metabolism by monoamine oxidase in the gut wall [10, 13]. As a consequence of metabolism, systemic bioavailability of PE is only around 40% [13]. Only about 3% of an oral dose of PE is excreted unchanged in the urine [10]. When administered intravenously, PE causes an increase in arterial blood pressure and bradycardia [16] and may also cause coronary vasospasm. The threshold dosage of PE administered orally in man for

any effects on the cardiovascular system is about 50 mg and at this dose PE causes a decline in heart rate and a slight increase in arterial blood pressure PE is a potent vasoconstrictor agent because of its direct a agonist activity, The tolerability of PE as an oral nasal decongestant is likely to be due to its poor access to the systemic circulation rather than to its pharmacological profile. The 1976 FDA monograph on OTC cold and cough products reports that PE is an effective nasal decongestant on the basis of reports on in-house studies on PE provided by representatives of pharmaceutical companies [18]. On the basis of these in-house studies, the FDAapproved PE as an effective nasal decongestant. This decision by the FDAon the efficacy of PE was questioned by a comment to the FDA in 1985, which stated that the unpublished studies split evenly between mild successes and total failures; in addition, the comment questioned the oral bioavailability of PE and recommended that the FDA should not accept PE as an oral decongestant [19] The standard pharmaceutical textbooks provide informationabout the efficacy of PE as a vasoconstrictor used during surgery to counteract hypotension, and as eye drops to dilate the pupil, but provide no information about the efficacy of PE as a nasal decongestant [11, 21]. However, the efficacy of phenylephrine formulated as a topical nasal decongestant nasal spray (0.250.5% w/v) is supported by several studies [2224]. The only study involving an oral dose of PE reported that 10 mg PE was no more effective than placebo as a nasal decongestant [17] (the study also reported a similar lack of effect for PDE), As with all sympathomimetics, PE and PDE should not be taken by patients suffering from hypertension, hyperthyroidism or heart disease because of the vasoconstrictor effects of the medicines. Similarly, patients suffering from Raynauds syndrome or taking medicines that inhibit monoamine oxidase (MAO) should consult their doctor before taking PE. PE and PDE may cause retention of urine in patients with prostate problems.

The Effects of Phenylpropanolamine on Zucker Rats Selected for Fat Food Preference PP In low-fat preferring animals, phenylpropanolamine decreased carbohydrate, protein,

and total caloric intake, had no significant effect of spontaneous activity, and increased serotonin and 5-hydroxyindole acetic acid levels in the PVN. It was found that in high-fat preferring animals, phenylpropanolamine significantly decreased spontaneous open-field activity, decreased only carbohydrate caloric intake, and increased serotonin and 5HIAA levels in the paraventricular nucleus (PVN).

Adrenergic agonist The main effect of 1 stimulation ( with agonist such as phenylephrine) is vasoconstriction. Local application of a vasoconstrictor to the nasal passages decreases blood flow locally and decreases secretions, thus acting as a nasal decongestant. Phenylpropanolamine has also been used as an appetite suppressant.

Adrenoceptor Agonists Are a large group of drugs whose diverse pharmacologic effects make them valuable in the treatment of a wide spectrum of clinical conditions. Agonists exert their effects on multiple organ systems, Phenylephrine Pharmacologic effect: Vasoconstriction, increased blood pressure, mydriasis Clinical Use: Nasal and ocular decongestion, mydriasis, maintenance of blood pressure and treatment of shock. Mechanisms and effects Causes smooth muscle contraction, to contraction of the iris dilator muscle and dilation of the pupil(myriasis).

Indications: -nasal decongestant in patients with viral rhinitis -used with allergic rhinitis

In patients with allergic conjunctivitis an inflammatory of the eyes associated with hay fever or other allergies, phenylephrine can be used as a topical ocular decongestant. The ocular preparation of phenylephrine is also used to induce mydriasis. -given IV to treat forms hypotension and shock caused by decreased peripheral vascular resistance.