What is the mechanism of action of pseudoephedrine?
Mechanism of action/Effect: Pseudoephedrine acts on alpha-adrenergic receptors in the mucosa of the respiratory tract, producing vasoconstriction. The medication shrinks swollen nasal mucous membranes; reduces tissue hyperemia, edema, and nasal congestion; and increases nasal airway patency.
What are the effects of pseudoephedrine?
Side effects from typical pseudoephedrine use can include:
- Urinary retention
- Insomnia
- Nervousness or anxiety
- Dizziness
- Excitability
What conditions does pseudoephedrine treat?
Pseudoephedrineis used for the temporary relief of stuffy nose and sinuspain/pressure caused by infection (such as the common cold, flu) or other breathing illnesses (such as hay fever, allergies, bronchitis). Pseudoephedrine is a decongestant(sympathomimetic).
Does pseudoephedrine cause loss of appetite?
Pseudoephedrine Side Effects. Pseudoephedrine has several side effects that can cause weight loss. They include loss of appetite, upset stomach, stomach pain, nausea, vomiting, headaches and dizziness. Other possible side effects include dry mouth, thirst, fatigue, sore throat, insomnia and nervousness.
What is the function of pseudoephedrine?
Pseudoephedrine is used to relieve nasal congestion caused by colds, allergies, and hay fever. It is also used to temporarily relieve sinus congestion and pressure.
How does pseudoephedrine work in the brain?
It causes vasoconstriction by stimulating primarily alpha-adrenergic receptors. It also has weak activity at beta-adrenergic receptors. It is chemically related to ephedrine, but with less central nervous system activity (fewer effects on the brain).
Is pseudoephedrine an agonist or antagonist?
Pseudoephedrine is an α-adrenergic agonist that is readily absorbed from the gastrointestinal tract with a short onset of action and has a half-life of about 5–8h (Kanfer et al., 1993).
What are three 3 teaching points for the pseudoephedrine?
Do not crush, chew, or break an extended-release tablet. Swallow it whole. You may need to shake the oral suspension (liquid) well just before you measure a dose. Measure liquid medicine with the dosing syringe provided, or with a special dose-measuring spoon or medicine cup.
Does pseudoephedrine release serotonin?
Pseudoephedrine is also an inhibitor of norepinephrine, dopamine, and serotonin transporters. The sympathomimetic effects of pseudoephedrine include an increase in mean arterial pressure, heart rate, and chronotropic response of the right atria.
Does pseudoephedrine release dopamine?
Consequently, it was suggested that the action of pseudoephedrine is mediated via dopamine release and it's activation of D1 dopamine receptors.
What's the difference between antihistamine and pseudoephedrine?
Benadryl and Sudafed belong to different drug classes. Benadryl is an antihistamine and Sudafed is a decongestant. Benadryl and Sudafed are available in generic form and over-the-counter (OTC).
Is pseudoephedrine an antihistamine?
It is available over-the-counter and as generic loratadine/pseudoephedrine. DESLORATADINE; PSEUDOEPHEDRINE is a combination of an antihistamine and a decongestant. This medicine is used to treat the symptoms of allergies. It reduces congestion, sneezing, runny nose, and itching.
What control is pseudoephedrine?
Pseudoephedrine is a medication that works as a nasal decongestant. It helps to relieve the symptoms of respiratory allergies, sinusitis and the common cold. It is an over-the-counter drug, not a controlled substance.
What should you not take with pseudoephedrine?
Avoid taking MAO inhibitors (isocarboxazid, linezolid, metaxalone, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, safinamide, selegiline, tranylcypromine) during treatment with this medication. Most MAO inhibitors should also not be taken for two weeks before treatment with this medication.
Why is pseudoephedrine so good?
Good question. Pseudoephedrine belongs to a group of medicines that act as decongestants by constricting small blood vessels in the nasal passages. Thus, less inflammation and congestion as the sinus tissue settles down a bit. It may improve thinking by improving breathing and sleep.
Is pseudoephedrine a strong stimulant?
It acts as a stimulant. This causes some people to begin to abuse it in order to be awake and get a rush of energy. It's true that pseudoephedrine is a stimulant. But, medically, it is commonly used to shrink mucous membranes that often become inflamed due to allergies or a cold.
Why does pseudoephedrine help me focus?
Due to its central nervous system (CNS) stimulant properties and structural similarity to amphetamine, it is also used for non-medical purposes. The substance is taken as an appetite reducer, an agent which eliminates drowsiness and fatigue, to improve concentration and as a doping agent.
Why does pseudoephedrine help with ADHD?
Roy Fontenot, staff pharmacist at the Neighborhood Walmart on Highland Road, said while Adderall and other ADHD medications target certain receptors in the brain that increase concentration, pseudoephedrine targets different receptors, and the body reacts to it the same way as it does adrenaline.
Is pseudoephedrine a neurotransmitter?
Pseudoephedrine displaces norepinephrine from storage vesicles in presynaptic neurones, thereby releasing norepinephrine into the neuronal synapses where it stimulates primarily alpha-adrenergic receptors....4.1.11H NMR Spectra.Spectra ID1821pH10.005 more rows
Does pseudoephedrine help ADHD?
I can say that pseudoephedrine is unlikely to have any significant benefit in adult ADHD. I think she would benefit from seeing a provider to find the right diagnosis and treatment for her nasal complaints and to determine whether she does have ADHD or another condition requiring treatment.
What are the effects of pseudoephedrine?
The sympathomimetic effects of pseudoephedrine include an increase in mean arterial pressure, heart rate, and chronotropic response of the right atria. 5 Pseudoephedrine is also a partial agonist of the anococcygeal muscle. 5 Pseudoephedrine also inhibits NF-kappa-B, NFAT, and AP-1. 10
What is pseudoephedrine used for?
Pseudoephedrine is an alpha and beta adrenergic agonist used to treat nasal and sinus congestion, as well as allergic rhinitis. Pseudoephedrine: Uses, Interactions, Mechanism of Action | DrugBank Online. Online.
How much pseudoephedrine is in urine?
55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine. 13
What is the apparent volume of distribution of pseudoephedrin?
The apparent volume of distribution of pseudoephedrin is 2.6-3.3L/kg. 11
Does pseudoephedrine increase hypertension?
Pseudoephedrine may decrease the sedative and stimulatory activities of Orphenadrine. Oxaprozin. The risk or severity of hypertension can be increased when Pseudoephedrine is combined with Oxaprozin. Oxatomide. Pseudoephedrine may decrease the sedative and stimulatory activities of Oxatomide.
Can pseudoephedrine be combined with etafedrine?
The risk or severity of hypertension can be increased when Pseudoephedrine is combined with Etafedrine. Ethosuximide. Pseudoephedrine can cause a decrease in the absorption of Ethosuximide resulting in a reduced serum concentration and potentially a decrease in efficacy. Etilefrine.
Is pseudoephedrine a metabolite?
Pseudoephedrine is <1% N-demethylated to an inactive metabolite. 16, 17 The majority of pseudoephedrine is eliminated unmetabolized in the urine. 16, 17
How is pseudoephedrine quantified?
Pseudoephedrine may be quantified in blood, plasma, or urine to monitor any possible performance-enhancing use by athletes, confirm a diagnosis of poisoning, or to assist in a medicolegal death investigation. Many commercial immunoassay screening tests directed at the amphetamines cross-react appreciably with pseudoephedrine, but chromatographic techniques can easily distinguish pseudoephedrine from other phenethylamine derivatives. Blood or plasma pseudoephedrine concentrations are typically in the 50–300 µg/l range in persons taking the drug therapeutically, 500–3000 µg/l in people with substance use disorder involving pseudoephedrine, or poisoned patients and 10–70 mg/l in cases of acute fatal overdose.
What are the side effects of pseudoephedrine?
Common adverse drug reactions (ADRs) associated with pseudoephedrine therapy include central nervous system stimulation, insomnia, nervousness, excitability, dizziness and anxiety. Infrequent ADRs include tachycardia or palpitations. Rarely, pseudoephedrine therapy may be associated with mydriasis (dilated pupils), hallucinations, arrhythmias, hypertension, seizures and ischemic colitis; as well as severe skin reactions known as recurrent pseudo-scarlatina, systemic contact dermatitis, and nonpigmenting fixed drug eruption. Pseudoephedrine, particularly when combined with other drugs including narcotics, may also play a role in the precipitation of episodes of paranoid psychosis. It has also been reported that pseudoephedrine, among other sympathomimetic agents, may be associated with the occurrence of stroke.
How much pseudoephedrine can you buy in a month?
30-day (not monthly) sales limit—must not exceed 7.5 grams of pseudoephedrine base if sold by mail order or "mobile retail vendor". 30-day purchase limit—must not exceed 9 grams of pseudoephedrine base. (A misdemeanor possession offense under 21 U.S.C. § 844a for the person who buys it.)
Why was pseudoephedrine discontinued?
Pseudoephedrine was withdrawn from sale in 1989 due to concerns about adverse cardiac side effects.
What is PSE in medicine?
Pseudoephedrine ( PSE) is a sympathomimetic drug of the phenethylamine and amphetamine chemical classes. It may be used as a nasal/sinus decongestant, as a stimulant, or as a wakefulness-promoting agent in higher doses.
What is PSE drug?
Pseudoephedrine. Pseudoephedrine ( PSE) is a sympathomimetic drug of the phenethylamine and amphetamine chemical classes. It may be used as a nasal/sinus decongestant, as a stimulant, or as a wakefulness-promoting agent in higher doses.
When was pseudoephedrine illegal?
On November 23, 2007, the use and trade of pseudoephedrine in Mexico was made illicit, as it was argued that it was extremely popular as a precursor in the synthesis of methamphetamine.
How is pseudoephedrine metabolized?
Pseudoephedrine is incompletely metabolized (less than 1%) in the liver by N-demethylation to an inactive metabolite. The drug and its metabolite are excreted in urine; 55-96% of a dose is excreted unchanged.
Where does pseudoephedrine come from?
Although pseudoephedrine occurs naturally as an alkaloid in certain plant species (for example, as a constituent of extracts from the ephedra species, also known as Ma Huang, in which it occurs together with other isomers of ephedrine ), the majority of pseudoephedrine produced for commercial use is derived from yeast fermentation of dextrose in the presence of benzaldehyde. In this process, specialized strains of yeast (typically a variety of Candida utilis or Saccharomyces cerevisiae) are added to large vats containing water, dextrose and the enzyme pyruvate decarboxylase (such as found in beets and other plants, inter alia). After the yeast has begun fermenting the dextrose, the benzaldehyde is added to the vats, and in this environment the yeast convert the precursor ingredients to L- phenylacetylcarbinol. /L- phenylacetylcarbinol / is then chemically converted to pseudoephedrine via reductive amination.
How to store pseudoephedrine?
Pseudoephedrine hydrochloride preparation should generally be stored at 15-30 °C; freezing of the oral solution should be avoided. Pseudoephedrine hydrochloride tablets and extended release capsules should be stored in tight containers and oral solution in tight, light-resistant containers. Pseudoephedrine sulfate extended release tablets should be protected from light and stored in well-closed containers at 2-30 °C.
How long does pseudoephedrine stay in your system?
The elimination half-life of pseudoephedrine ranges from 3-6 or 9-16 hours when urinary pH is 5 or 8, respectively, while when urinary pH is 5.8, the elimination half-life of the drug ranges from 5-8 hours. In one study in children 6-12 years of age, the elimination half-life of pseudoephedrine averaged about 3 hours when urinary pH was 6.5.
What is the elimination half life of pseudoephedrine?
The mean elimination half life of pseudoephedrine is 6.0h.
How much pseudoephedrine is in urine?
55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine.
What is the meth epidemic?
The act bans over-the-counter sales of cold medicines that contain the ingredient pseudoephedrine, which is commonly used to make methamphetamine. The sale of cold medicine containing pseudoephedrine is limited to behind the counter. The amount of pseudoephedrine that an individual can purchase each month is limited and individuals are required to present photo identification to purchase products containing pseudoephedrine. In addition, stores are required to keep personal information about purchasers for at least two years.
What is the mechanism of action of pseudoephedrine?
MECHANISM OF ACTION. Pseudoephedrine is a sympathomimetic drug belonging to the phenethylamine and amphetamine chemical classes. Its principal mechanism of action depends on its effects on the adrenergic receptor system, causing vasoconstriction. Pseudoephedrine hydrochloride and its sulfate salts are found in an abundance ...
What are the side effects of pseudoephedrine?
Some adverse effects of pseudoephedrine that typically do not need medical attention and that may subside during use include nervousness, restlessness, and trouble sleeping. Less common are dysuria, syncope, tachycardia, palpitations, headache, nausea and vomiting, trembling, and weakness. 3. DISEASE INTERACTIONS.
How long does pseudoephedrine stay in your system?
A small amount is metabolized in the liver and also excreted in the urine. The half-life of pseudoephedrine is between 5 and 8 hours, though the more acidic the urine, the lower the half-life. 10
When was pseudoephedrine first used?
Pseudoephedrine: Uses, Indications, and Adverse Effects. Pseudoephedrine has been around since the 1920s. Pseudoephedrine has been around since the 1920s. Although the drug occurs naturally in certain plants (eg, ma huang), the majority that is produced derives from yeast fermentation of dextrose in the presence of benzaldehyde.
Where does pseudoephedrine come from?
Although the drug occurs naturally in certain plants (eg, ma huang), the majority that is produced derives from yeast fermentation of dextrose in the presence of benzaldehyde. Pharmaceutical manufacturers in China and India produce the bulk of commercially available pseudoephedrine.
Is pseudoephedrine safe for type 2 diabetes?
Pseudoephedrine is contraindicated in patients with type 2 diabetes, as it may increase glucose levels. 4 Patients with glaucoma or a predisposition for glaucoma should not use pseudoephedrine because of its vasoconstrictive qualities. 4 The same is true for prostatic hypertrophy 4. Pseudoephedrine may worsen the following conditions: cardiovascular disease, severe or uncontrolled hypertension, severe coronary artery disease, ischemic heart disease, and hyperthyroidism. 4
Is pseudoephedrine available for the general public?
Since the implementation of the Combat Methamphetamine Epidemic Act, it has been difficult to obtain pseudoephedrine for the general public, but the methamphetamine epidemic has just continued to grow. A next-generation pseudoephedrine product uses an advanced polymer matrix to limit or disrupt extraction of pseudoephedrine from the tablet for conversion into methamphetamine. 13
What is pseudoephedrine used for?
Dilated blood vessels can cause nasal congestion (stuffy nose). 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.
What antidepressants interact with pseudoephedrine?
an antidepressant such as amitriptyline (Elavil, Vanatrip, Limbitrol), doxepin (Sinequan), nortriptyline (Pamelor), and others. This list is not complete and other drugs may interact with pseudoephedrine. Tell your doctor about all medications you use.
How to know if you are allergic to pseudoephedrine?
Get emergency medical help if you have any of these signs of an allergic reaction to pseudoephedrine: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using pseudoephedrine and call your doctor at once if you have a serious side effect such as: 1 fast, pounding, or uneven heartbeat; 2 severe dizziness or anxiety; 3 easy bruising or bleeding, unusual weakness, fever, chills, body aches, flu symptoms; or 4 dangerously high blood pressure (severe headache, blurred vision, ringing in your ears, anxiety, confusion, chest pain, trouble breathing, uneven heart rate, seizure).
How long can you take pseudoephedrine?
Do not take pseudoephedrine for longer than 7 days in a row . Talk with your doctor if your symptoms do not improve after 7 days of treatment, or if you have a fever with a headache, cough, or skin rash. If you need surgery, tell the surgeon ahead of time that you are using pseudoephedrine.
Can you take pseudoephedrine and decongestant together?
Ask a doctor or pharmacist before using any other cough or cold medicine. Pseudoephedrine or other decongestants are contained in many combination medicines. Taking certain products together can cause you to get too much of a certain drug. Check the label to see if a medicine contains pseudoephedrine or a decongestant. Do not use pseudoephedrine if you have used a MAO inhibitor such as furazolidone (Furoxone), isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam, Zelapar), or tranylcypromine (Parnate) in the last 14 days. A dangerous drug interaction could occur, leading to serious side effects.
Can you give a child pseudoephedrine?
Do not give pseudoephedrine to a child younger than 4 years old. 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. Take this medicine with a full glass of water.
Can you take pseudoephedrine for longer than recommended?
Use pseudoephedrine exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Cold medicine is usually taken only for a short time until your symptoms clear up.
Overview
Mechanism of action
Pseudoephedrine is a sympathomimetic amine. Its principal mechanism of action relies on its direct action on the adrenergic receptor system. The vasoconstriction that pseudoephedrine produces is believed to be principally an α-adrenergic receptor response.
Pseudoephedrine acts on α- and β2-adrenergic receptors, to cause vasoconstriction and relaxation of smooth muscle in the bronchi, respectively. α-Adrenergic receptors are located on t…
Medical uses
Pseudoephedrine is a stimulant, but it is well known for shrinking swollen nasal mucous membranes, so it is often used as a decongestant. It reduces tissue hyperemia, edema, and nasal congestion commonly associated with colds or allergies. 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 pseudoep…
Adverse effects
Common adverse drug reactions (ADRs) associated with pseudoephedrine therapy include central nervous system stimulation, insomnia, nervousness, excitability, dizziness and anxiety. Infrequent ADRs include tachycardia or palpitations. Rarely, pseudoephedrine therapy may be associated with mydriasis (dilated pupils), hallucinations, arrhythmias, hypertension, seizures and ischemic colitis; as well as severe skin reactions known as recurrent pseudo-scarlatina, systemic contact dermat…
Interactions
Concomitant or recent (previous fourteen days) monoamine oxidase inhibitor use can lead to hypertensive reactions, including hypertensive crises.
The antihypertensive effects of methyldopa, mecamylamine, reserpine and veratrum alkaloids may be reduced by sympathomimetics. Beta-adrenergic antagonists may also interact with sympathomimetics. Increase of ectopic pacemaker activity can occur when pseudoephedrine is …
Other uses
There have been reports of off-label uses of pseudoephedrine for its stimulant properties. Long-distance truck drivers and athletes, for example, have reportedly used pseudoephedrine as a stimulant to increase their state of alertness/awareness.
A study has also found that pseudoephedrine can reduce milk production in breastfeeding women.
Chemistry
Pseudoephedrine is a diastereomer of ephedrine and is readily reduced into methamphetamine or oxidized into methcathinone.
The dextrorotary (+)- or d- enantiomer is (1S,2S)-pseudoephedrine, whereas the levorotating (−)- or l- form is (1R,2R)-pseudoephedrine.
In the outdated D/L system (+)-pseudoephedrine is also referred to as L-pseudo…
Society and culture
The following is a list of consumer medicines that either contain pseudoephedrine or have switched to a less-regulated alternative such as phenylephrine.
• Actifed (made by GlaxoSmithKline) — contains 60 mg pseudoephedrine and 2.5 mg triprolidine in certain countries.