Pseudoephedrine

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Pseudoephedrine
Legal Status
US Law-yellow.png Prescription Only in OR and MS
Law-green.png Restricted OTC in all other states
UK Law-green.png Restricted OTC
Canada
Drug Information
FDA Classification Drug
Class Stimulant
Wakefulness Promoting
Anorectic
Vasoconstrictor
Onset of Action 30-60 minutes (instant release)
Duration of Action As a stimulant:
2-4 hours (instant release)
4-8 hours (extended release)
Addiction Risk Addiction-green.png Low
Brand names Sudafed
Nexafed

Pseudoephedrine, known better by its brand name Sudafed, is a drug with stimulant properties sold as a decongestant.

It should be noted that the newer formulations of on-the-shelf Sudafed, Sudafed PE, contain phenylephrine, not "real" pseudoephedrine.

Background[edit]

Pseudoephedrine is found naturally in the Ephedra plant, and has been used in traditional Chinese medicine for at least 2,000 years.

Legality and Availability[edit]

United States[edit]

Pseudoephedrine is available by prescription only in Oregon and Mississippi, and without a prescription in all other states.

Pseudoephedrine is legal and over-the-counter in the United States and elsewhere, but is restricted because it can be used to manufacture meth. Buying pseudoephedrine typically requires one to sign a logbook and/or scan their state ID. Sales are limited to 3.6 grams per day, and 7.5 grams per month.[1] Purchasing greater amounts constitutes probable cause for law enforcement to investigate.

It must be noted that Sudafed-branded products are often available for sale on store shelves or online retailers. However, these products do NOT contain pseudoephedrine. After pseudoephedrine was restricted circa 2005, it was replaced with phenylephrine in mass-market unrestricted brands. Typically, these brands include the name "PE". For instance, "Sudafed" with real pseudoephedrine is still sold behind the counter, while "Sudafed PE" is sold on shelves, at convenience stores, online, etc.

Generic pseudoephedrine is cheap, usually around $7 for 24 120mg XR tablets ($2.43 per gram), and as low as $4.60 for 96 30mg IR tablets at Costco Pharmacy ($1.60 per gram). Thus a typical dose of 120mg to 240mg instant release costs only $0.20 to $0.40, making it competitive with other legal and illegal stimulants such as caffeine.

Some U.S. pharmacies are now selling Nexafed, which is pseudoephedrine mixed with an inactive ingredient that makes methamphetamine manufacturing more difficult.

Athletic Organizations[edit]

Pseudoephedrine is banned by the International Olympic Committee.[2]

The NCAA allows the use of pseudoephedrine, despite considering it a stimulant.[3]

Official Uses[edit]

Officially, pseudoephedrine is only a decongestant.[4] It is a much better decongestant than phenylephrine (Sudafed PE), which has often failed to be demonstrably better than placebo.

Unofficial Uses[edit]

Stimulant[edit]

Pseudoephedrine, despite the official position of the FDA and pharmaceutical companies, is an effective stimulant. It is a member of the amphetamine class, and acts on dopamine and adrenergic systems in the CNS.[5]

Pseudoephedrine can be used in the place of stronger stimulants like Adderall, and can even be considered equivalent to drugs like Adderall, to a point.

Time-release tablets[edit]

12-Hour preparations of pseudoephedrine are sold widely, and include doses higher than those in instant-release versions.

When used as a stimulant, time-release formulations can provide the stimulant and wakefulness-promoting effects over a longer period of time, although some individuals report a very slow rate of onset (2-3 hours or more) with this method.

Modifications

The time-release mechanism can be defeated by crushing up the pill and putting the powder in an empty capsule, usually obtained by purchasing a cheap vitamin and emptying out the capsule. Alternatively, this can be accomplished more crudely by putting the time-release pill in your mouth, crushing it with your teeth, then quickly drinking water and swallowing it.

Mixing pseudoephedrine with water or a beverage is not recommended, simply because it has a very bitter taste that is difficult to mask.

Wakefulness-promoting agent[edit]

Pseudoephedrine is also an effective wakefulness-promoting medicine, potentially more effective than caffeine in many individuals.

Appetite Suppressant[edit]

Pseudoepehdrine, being an amphetamine, increases metabolism and decreases appetite, possibly due to its dopaminergic effects.

Dosage[edit]

The official recommended dose of pseudoephedrine for nasal congestion is 60 mg instant release, 120 mg for a 12-hour extended release, and 240 mg for a 24-hour extended release.[6] 24-hour extended release products, however, carry the risk of restlessness and insomnia overnight.

Pharmacology[edit]

Pseudoephedrine inhibits the sodium-dependent norepinephrine, serotonin, and dopamine transporters, leading to an increased concentration of norepinephrine, serotonin, and dopamine.

It acts as an agonist at the Alpha-1A, Alpha-2A adrenergic receptors, and a partial agonist at the Beta-1 and Beta-2 receptors.

This profile is similar to that of drugs officially recognized as stimulants by the FDA and other organizations.

References[edit]

  1. http://www.namsdl.org/library/80BA8CEC-1C23-D4F9-74BBEEA9C03FDF52/ page 2
  2. https://en.wikipedia.org/wiki/List_of_drugs_banned_from_the_Olympics
  3. http://www.ncaa.org/2015-16-ncaa-banned-drugs
  4. http://reference.medscape.com/drug/sudafed-nexafed-pseudoephedrine-343412]
  5. http://www.drugbank.ca/drugs/DB00852#targets
  6. http://reference.medscape.com/drug/sudafed-nexafed-pseudoephedrine-343412