Pseudoephedrine, its salts, optical isomers, and
salts of optical isomers
CAS number : 90-82-4
Formula : C10H15NO
Mol. Weight : 165.23
Melting Point:182 - 186 C
Solubility: Soluble (soluble in alcohol) RESIDUE Complies
Risk Codes:R20/21/22;R36/37/38 Details
Appearance:White fine powder
Synonyms: Isoephedrine, trans-Ephedrine, PSEUDOEPHEDRINE,
Sudafed, d-Pseudoephedrine, d-Isoephedrine, Psi-ephedrine,
Psi-ephedrin, d-psi-Ephedrine, Besan, (+)-Pseudoephedrine, L(+)-psi-Ephedrine,
(+)-threo-Ephedrine, (+)-psi-Ephedrine, L-(+)-Pseudoephedrine,
Pseudoephedrine (D), ()-psi-Ephedrine, ()-Pseudoephedrine, ( )-Pseudoephedrine,
is a sympathomimetic amine commonly used as a decongestant. The salts
pseudoephedrine hydrochloride and pseudoephedrine sulfate are found in
many over-the-counter preparations either as single-ingredient
preparations, or more commonly in combination with antihistamines,
paracetamol (acetaminophen) and/or ibuprofen. Sudafed is a trademark for
a common brand which contains pseudoephedrine hydrochloride, though
Sudafed PE does not. Cirrus contains pseudoephedrine in conjunction with
cetirizine (an antihistamine).
Unlike antihistamines, which relieve multiple allergic symptoms by
acting as antagonists at histamine receptors, pseudoephedrine primarily
relieves nasal congestion commonly associated with colds or allergies.
The advantage of oral pseudoephedrine over topical nasal preparations,
such as oxymetazoline, is that it does not cause rebound congestion
(rhinitis medicamentosa); however, it is more likely to cause adverse
effects including hypertension.
Pseudoephedrine is being phased out as an over-the-counter drug in some
countries and replaced by less effective alternative decongestants such
as phenylephrine, due to pseudoephedrine's use as an ingredient in the
manufacture of methamphetamine.
Metabolism hepatic (10–30%)
Half life 9–16 hours
Excretion 70-90% renal
Pseudoephedrine is a decongestant that shrinks blood vessels in the
nasal passages. Dilated blood vessels can cause nasal congestion (stuffy
Pseudoephedrine is used to treat nasal and sinus congestion, or
congestion of the tubes that drain fluid from your inner ears, called
the eustachian (yoo-STAY-shun) tubes.
Important information about pseudoephedrine
Always ask a doctor before giving a cough or cold medicine to a child.
Death can occur from the misuse of cough and cold medicines in very
young children. Do not use any other over-the-counter cough or cold
medication without first asking your doctor or pharmacist. If you take
certain products together you may accidentally take too much of a
certain drug. Read the label of any other medicine you are using to see
if it contains pseudoephedrine. Do not use a cough or cold medicine if
you have used an MAO inhibitor such as isocarboxazid (Marplan),
phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam),
or tranylcypromine (Parnate) within the past 14 days. Serious,
life-threatening side effects can occur if you take cough or cold
medicine before the MAO inhibitor has cleared from your body.
Pseudoephedrineis a sympathomimetic amine commonly used as a
decongestant. The salts pseudoephedrine hydrochloride and
pseudoephedrine sulfate are found in many over-the-counter preparations
either as single-ingredient preparations, or more commonly in
combination with antihistamines, paracetamol (acetaminophen) and/or
ibuprofen. Sudafed is a trademark for a common brand which contains
pseudoephedrine hydrochloride, though Sudafed PE does not. Cirrus
contains Pseudoephedrine in conjunction with Cetirizine (an
antihistamine).The advantage of oral pseudoephedrine over topical nasal
preparations, such as oxymetazoline, is that it does not cause rebound
congestion (rhinitis medicamentosa); however, it is more likely to cause
adverse effects including hypertension.
Pseudoephedrine is indicated for the treatment of:
* nasal congestion
* sinus congestion
* Eustachian tube congestion.
Mechanism of action
Pseudoephedrine is a sympathomimetic amine—that is, its principal
mechanism of action relies on its indirect action on the adrenergic
receptor system. While it may have weak agonist activity at α- and
β-adrenergic receptors, the principal mechanism is to cause the release
of endogenous norepinephrine (noradrenaline) from storage vesicles in
presynaptic neurons. The displaced noradrenaline is released into the
neuronal synapse where it is free to activate the aforementioned
postsynaptic adrenergic receptors.
These adrenergic receptors are located on the muscles lining the walls
of blood vessels. When activated by pseudoephedrine, the muscles
contract, causing the blood vessels to constrict (vasoconstriction).
These constricted blood vessels now allow less fluid to leave the blood
vessels and enter the nose, throat and sinus linings, which results in
decreased inflammation of nasal membranes as well as decreased mucus
production. Thus, by constriction of blood vessels, mainly those located
in the nasal passages, pseudoephedrine causes a decrease in the symptoms
of nasal congestion.
The vasoconstriction that pseudoephedrine produces is believed to be
principally an α-adrenergic receptor response. While all sympathomimetic
amines, to some extent, have decongestant action, pseudoephedrine shows
greater selectivity for the nasal mucosa and a lower affinity for
central nervous system (CNS) adrenergic-receptors than other
Vasoconstriction in the nasal mucosa shrinks swollen nasal mucous
membranes, reduces tissue hyperemia, edema, and nasal congestion. Other
beneficial effects may include increasing the drainage of sinus
secretions, and opening of obstructed Eustachian tubes. The same
vasoconstriction action can also result in hypertension, which is a
noted side effect of pseudoephedrine.
Precautions and contraindications
It is recommended that pseudoephedrine not be used in patients with:
diabetes mellitus, cardiovascular disease, hypertension, prostatic
hypertrophy, hyperthyroidism, closed angle glaucoma and/or pregnancy
Since nasal congestion is considered to be a relatively minor ailment,
alternatives are preferred in patients with these conditions.
Appropriate alternatives may include topical decongestants or saline
sprays/instillations, depending on the patient's condition.
Contraindications for the use of pseudoephedrine include: concomitant or
recent (previous fourteen days) monoamine oxidase inhibitor (MAOI), or
serotonin-specific reuptake inhibitor (SSRI) therapy , severe or
uncontrolled hypertension, and/or severe coronary artery disease.
People with bipolar disorder should use care when taking pseudoephedrine,
as it can cause insomnia and thus trigger a manic episode.
Pseudoephedrine is a phenethylamine, and a diastereomer of
ephedrine.Pseudoephedrine is the International Nonproprietary Name (INN)
of the (1S,2S)- diastereomer of ephedrine (which has 1R,2S-
configuration). Other names are (+)-pseudoephedrine and D-pseudoephedrine
These API/ chemicals are designated as
those that are used in the manufacture of the controlled substances and
are important to the manufacture of the substances. For any (Control
Substance) products Import and Export *** subjected to your country
government laws /control substance ACT.
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