Aleve-d Sinus & Cold
Aleve-d Sinus & Cold Uses, Dosage, Side Effects, Food Interaction and all others data.
Naproxen, a propionic acid derivative, is a prototypical NSAID. It reversibly inhibits the cyclooxygenase-1 and -2 (COX-1 and -2) enzymes, thus resulting in reduced synthesis of prostaglandin precursors. It can inhibit platelet aggregation, has anti-inflammatory, analgesic and antipyretic actions.
Naproxen is an established non-selective NSAID and is useful as an analgesic, anti-inflammatory and antipyretic. Similar to other NSAIDs, the pharmacological activity of naproxen can be attributed to the inhibition of cyclo-oxygenase, which in turn reduces prostaglandin synthesis in various tissues and fluids including the synovial fluid, gastric mucosa, and the blood.
Although naproxen is an effective analgesic, it can have unintended deleterious effects in the patient. For instance, naproxen can adversely affect blood pressure control. A study found that use of naproxen induced an increase in blood pressure, although the increase was not as significant as that found with ibuprofen use.
Further, studies have found that the risk of upper gastrointestinal bleeding is on average four-fold higher for individuals taking NSAIDs. Other factors that increase the risk of upper gastrointestinal bleeding include concurrent use of corticosteroids or anticoagulants, and a history of gastrointestinal ulcers.
Pseudoephedrine is structurally related to ephedrine but exerts a weaker effect on the sympathetic nervous system. Both drugs naturally occur in in ephedra plant which have a history of use in traditional Eastern medicine and were first researched in the west in 1889. The decongestant effect of pseudoephedrine was described in dogs in 1927.
Pseudoephedrine causes vasoconstriction which leads to a decongestant effect. It has a short duration of action unless formulated as an extended release product. Patients should be counselled regarding the risk of central nervous system stimulation.
| Trade Name | Aleve-d Sinus & Cold |
| Generic | Naproxen + pseudoephedrine |
| Weight | 220mg + 120mg, |
| Type | Oral Tablet, Extended Release |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Naproxen is used for the relief of symptoms of rheumatoid arthritis, both of acute flares and long term management of the disease. It is also used in the diseases of rheumatoid osteoarthritis (degenerative arthritis), ankylosing spondylitis, juvenile rheumatoid arthritis, tendinitis, brusitis, acute gout, acute musculoskeletal disorders (such as sprains, direct trauma and fibrositis), migraine and dysmenorrhoea.
Pseudoephedrine is an alpha and beta adrenergic agonist used to treat nasal and sinus congestion, as well as allergic rhinitis.
Pseudoephedrine is a sympathomimetic amine used for its decongestant activity.
Aleve-d Sinus & Cold is also used to associated treatment for these conditions: Acute Gouty Arthritis, Acute Migraine, Ankylosing Spondylitis (AS), Arthritis, Backache, Bursitis, Extra-Articular Rheumatism, Fever, Flu caused by Influenza, Headache, Juvenile Idiopathic Arthritis (JIA), Menstrual Distress (Dysmenorrhea), Migraine, Muscle Spasms, Nasal Congestion, Osteoarthritis (OA), Pain, Post-traumatic pain, Postoperative pain, Primary Dysmenorrhoea, Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile, Seasonal Allergic Rhinitis, Sinusitis, Tendinitis, ToothacheAllergic Rhinitis (AR), Allergies, Common Cold, Common Cold Associated With Cough, Common Cold/Flu, Cough, Cough caused by Common Cold, Eye allergy, Fever, Flu caused by Influenza, Headache, Irritative cough, Nasal Allergies, Nasal Congestion, Nasal Congestion caused by Common Cold, Pain, Perennial Allergy, Priapism, Respiratory Allergy, Rhinorrhoea, Seasonal Allergic Rhinitis, Seasonal Allergies, Sinus Congestion, Sinusitis, Sneezing, Sore Throat, Symptoms of Acute Bronchitis Accompanied by Coughing, Throat irritation, Upper Respiratory Tract Infection, Upper respiratory tract congestion, Upper respiratory tract signs and symptoms, Dry cough, Minor aches and pains, Sinus pain, Watery itchy eyes, Airway secretion clearance therapy
How Aleve-d Sinus & Cold works
As with other non-selective NSAIDs, naproxen exerts it's clinical effects by blocking COX-1 and COX-2 enzymes leading to decreased prostaglandin synthesis. Although both enzymes contribute to prostaglandin production, they have unique functional differences. The COX-1 enzymes is constitutively active and can be found in normal tissues such as the stomach lining, while the COX-2 enzyme is inducible and produces prostaglandins that mediate pain, fever and inflammation. The COX-2 enzyme mediates the desired antipyretic, analgesic and anti-inflammatory properties offered by Naproxen, while undesired adverse effects such as gastrointestinal upset and renal toxicities are linked to the COX-1 enzyme.
Pseudoephedrine acts mainly as an agonist of alpha adrenergic receptors and less strongly as an agonist of beta adrenergic receptors.[A10896] This agonism of adrenergic receptors produces vasoconstriction which is used as a decongestant and as a treatment of priapism. 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. Pseudoephedrine is also a partial agonist of the anococcygeal muscle. Pseudoephedrine also inhibits NF-kappa-B, NFAT, and AP-1.
Dosage
Aleve-d Sinus & Cold dosage
Tablet & Suppository (Adult)-
- Rheumatic disorders:The usual initial dose of naproxen is 250 mg twice daily adjusted to 500 mg to 1000 mg daily in 2 divided doses.
- Juvenile arthritis: A dose of 10 mg/kg body weight daily in 2 divided doses is used for children over 5 years of age.
- Acute gout: An initial dose of 750 mg followed by 250 mg every 8 hours.
- Dysmenorrhoea: 500 mg may be given initially followed by 250 mg in every 6-8 hours.
Syrup (Children over 5 years)-
- In juvenile arthritis: The usual dosage of Naproxen is 10 mg/kg/day taken in two doses at 12-hour intervals is recommended.
Gel:Naproxen gel is to be applied 2-6 times a day as required and is not recommended for use in children.
Side Effects
Gastro-intestinal discomfort: nausea, diarrhoea and occasionally bleeding and ulceration.
Hypersensitivity reactions: notably with bronchospasm, rashes and angioedema.
CNS side effect: drowsiness, headache, fluid retention, vertigo, hearing disturbances such as tinnitus, photosensitivity.
A few instances of jaundice, impairment of renal function, thrombocytopenia, and agranulocytosis have been reported.
Toxicity
Although the over-the-counter (OTC) availability of naproxen provides convenience to patients, it also increases the likelihood of overdose. Thankfully, the extent of overdose is typically mild with adverse effects normally limited to drowsiness, lethargy, epigastric pain, nausea and vomiting. Although there is no antidote for naproxen overdose, symptoms will typically subside with appropriate supportive care.
Naproxen is classified as Category B during the first 2 trimesters of pregnancy, and as Category D during the third trimester. Naproxen is contraindicated in the 3rd trimester since it increases the risk of premature closure of the fetal ductus arteriosus and should be avoided in pregnant women starting at 30 weeks gestation.
The oral LD50 of pseudoephedrine is 2206mg/kg in rats and 726mg/kg in mice.
Patients experiencing an overdose of pseudoephedrine may present with giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty urinating, muscle weakness, muscle tension, anxiety, restlessness, insomnia, toxic psychosis, cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure. Treat overdose with symptomatic and supportive treatment including removal of unabsorbed drug.
Precaution
Naproxen should be used with caution in patients with cardiac, hepatic and renal impairment, coagulation defect, and previous history of gastro-intestinal ulceration. The drug is contraindicated in patients with a history of hypersensitivity to aspirin or any other NSAID - which includes those in whom attacks of asthma, angioedema, urticaria or rhinitis have been precipitated by aspirin or any other NSAID.
Interaction
Antacid: The absorption of naproxen can be altered by antacids.
Aspirin: Plasma concentration of Naproxen can be reduced when aspirin is given concomitantly, this appeared to be due to increased exeretion of naproxen.
Diuretics: Naproxen diminish the effect of frusemide.
Probenecid: It increase the plasma concentration of Naproxen.
Volume of Distribution
Naproxen has a volume of distribution of 0.16 L/kg.
The apparent volume of distribution of pseudoephedrin is 2.6-3.3L/kg.
Elimination Route
Naproxen is available as a free acid and sodium salt. At comparable doses, (naproxen 500 mg = naproxen sodium 550 mg) they differ slightly in their rates of absorption, but otherwise they are therapeutically and pharmacologically equivalent. Naproxen sodium achieves a peak plasma concentration after 1 hour, while peak plasma concentration is observed after 2 hours with naproxen (free acid). There are no differences between the 2 forms in the post-absorption phase pharmacokinetics. The difference in initial absorption should be considered when treating acute pain, since naproxen sodium may offer a quicker onset of action.
The mean Cmax for the various formulations (immediate release, enteric coated, controlled release etc.) of naproxen are comparable and range from 94 mcg/mL to 97.4 mcg/mL. In one pharmacokinetic study, the mean Tmax of naproxen 500 mg (immediate release) given every 12 hours over 5 days was 3 hours, compared to a mean Tmax of 5 hours for Naprelan 1000 mg (controlled release) given every 24 hours over 5 days. In this same study, the AUC0-24hr was 1446mcgxhr/mL for naproxen immediate release and 1448 mcgxhr/mL for the controlled release formulation. A separate study comparing the pharmacokinetics of Naprosyn tablets and EC-Naprosyn observed the following values: Tmax and AUC0-12hrs of EC-Naprosyn were 4 hours and 845 mcgxhr/mL respectively, and Tmax and AUC0-12hrs values of Naprosyn were 1.9 hours and 767 mcgxhr/mL respectively.
When given in combination with sumatriptan the Cmax of naproxen is roughly 36% lower compared to naproxen sodium 550 mg tablets, and the median Tmax is 5 hours.
Based on the AUC and Cmax of naproxen, Vimovo (naproxen/esomeprazole combination product) and enteric-coated naproxen may be considered bioequivalent.
Overall, naproxen is rapidly and completely absorbed when administered orally and rectally. Food may contribute to a delay in the absorption of orally administered naproxen, but will not affect the extent of absorption.
A 240mg oral dose of pseudoephedrine reaches a Cmax of 246.3±10.5ng/mL fed and 272.5±13.4ng/mL fasted, with a Tmax of 6.60±1.38h fed and 11.87±0.72h fasted, with an AUC of 6862.0±334.1ng*h/mL fed and 7535.1±333.0ng*h/mL fasted.
Half Life
The elimination half-life of naproxen is reported to be 12-17 hours.
The mean elimination half life of pseudoephedrine is 6.0h.
Clearance
Naproxen is cleared at a rate of 0.13 mL/min/kg.
A 60mg oral dose of pseudoephedrine has a clearance of 5.9±1.7mL/min/kg.
Elimination Route
After oral administration, about 95% of naproxen and it's metabolites can be recovered in the urine with 66-92% recovered as conjugated metabolite and less than 1% recovered as naproxen or desmethylnaproxen. Less than 5% of naproxen is excreted in the feces.
55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine.
Pregnancy & Breastfeeding use
There are no well controlled studies in pregnant women. The drug should not be used during pregnancy unless clearly needed. Because of the possible adverse effects of prostaglandin inhibiting drugs on neonates, use in nursing mothers must be avoided.
Contraindication
Naproxen suppository in contraindicated in children under 12 years of age. The suppository is contraindicated also in patients with any inflammatory lesions of rectum or anus and in patients with recent history of rectal or anal bleeding.
Acute Overdose
Significant overdosage of the drug may be characterized by drowsiness, heartburn, indigestion, and nausea or vomiting. It is not known what dose of the drug would be life threatening.
Storage Condition
Tablet: Protect from light and store below 30° C temperature in a dry place.
Suppository: Store below 25°C temperature.
Gel: Store in a cool and dry place protected from light.
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