Ibutin
Ibutin Uses, Dosage, Side Effects, Food Interaction and all others data.
Ibutin is a non-selective inhibitor of cyclooxygenase, an enzyme invovled in prostaglandin synthesis via the arachidonic acid pathway. Its pharmacological effects are believed to be due to inhibition cylooxygenase-2 (COX-2) which decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever and swelling. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation. Inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration. Ibutin is administered as a racemic mixture. The R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo. The S-enantiomer is believed to be the more pharmacologically active enantiomer.
Ibutin has multiple actions in different inflammatory pathways involved in acute and chronic inflammation. The main effects reported in ibuprofen are related to the control of pain, fever and acute inflammation by the inhibition of the synthesis of prostanoids by COX-1 and COX-2. Pain relief is attributed to peripheral affected regions and central nervous system effects in the pain transmission mediated by the dorsal horn and higher spinothalamic tract. Some reports have tried to link the pain regulation with a possible enhancement on the synthesis of endogenous cannabinoids and action on the NMDA receptors. The effect on pain has been shown to be related to the cortically evoked potentials.
The antipyretic effect is reported to be linked to the effect on the prostanoid synthesis due to the fact that the prostanoids are the main signaling mediator of pyresis in the hypothalamic-preoptic region.
The use of ibuprofen in dental procedures is attributed to the local inhibition of prostanoid production as well as to anti-oedemic activity and an increase of plasma beta-endorphins. Some reports have suggested a rapid local reduction of the expression of COX-2 in dental pulp derived by the administration of ibuprofen.
| Trade Name | Ibutin |
| Availability | Rx and/or OTC |
| Generic | Ibuprofen |
| Ibuprofen Other Names | Ibuprofen, Ibuprofene, Ibuprofeno, Ibuprofenum, Ibuprophen |
| Related Drugs | Humira, Buprenex, aspirin, prednisone, acetaminophen, tramadol, meloxicam, duloxetine, cyclobenzaprine, Paracetamol |
| Type | |
| Formula | C13H18O2 |
| Weight | Average: 206.2808 Monoisotopic: 206.13067982 |
| Protein binding | Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml. |
| Groups | Approved |
| Therapeutic Class | Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs) |
| Manufacturer | |
| Available Country | Taiwan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ibutin is used
- For the treatment of sign and symptoms of rheumatoid arthritis, ankylosing spondylitis, osteoarthritis and other non-rheumatoid arthropathies,
- For the treatment of non-articular rheumatic conditions, such as frozen shoulder, bursitis, tendinitis, tenosynovitis and low back pain,
- For the treatment of soft tissue injuries such as sprain, strain and post operative pain
- For the treatment of dysmenorrhoea,
- For the treatment of dental pain.
- For the treatment of cold & fever.
Ibutin is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Common Cold, Cystic Fibrosis (CF), Fever, Gastric Ulcer, Gouty Arthritis, Headache, Insomnia, Juvenile Idiopathic Arthritis (JIA), Menstrual Distress (Dysmenorrhea), Migraine, Mild pain, Nasal Congestion, Osteoarthritis (OA), Pain, Pain, Acute, Pain, Inflammatory, Patent Ductus Arteriosus (PDA), Pericarditis, Primary Dysmenorrhoea, Rheumatoid Arthritis, Severe Pain, Sinus pressure, Mild to moderate pain, Minor aches and pains, Moderate Pain
How Ibutin works
The exact mechanism of action of ibuprofen is unknown. However, ibuprofen is considered an NSAID and thus it is a non-selective inhibitor of cyclooxygenase, which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway.
Ibutin is a non-selective COX inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration.
Dosage
Ibutin dosage
Oral Administrations-
For Children:
- 20 mg per kg body weight daily in divided doses. In children weighing less than 30 kg the total daily dosage should not exceed 500 mg. If gastrointestinal disturbances occur Ibutinshould be given with food or milk.
- 1-2 years: 1/2 tea spoonful (2.5 ml) 3-4 times daily;
- 3-7 years: 1 tea spoonful (5 ml) 3-4 times daily;
- 8-12 years: 2 tea spoonful (10 ml) 3-4 times daily. Ibutinis not recommended for children under 1 year.
For adult:
- For arthritic pain: The dosage range is from 0.9 to 2.4 g per day. The usual dose is 400 mg, 3-4 times per day, preferably after food. The dose may be raised to a maximum of 2.4 g daily depending on the severity of symptom at the time of initiating drug therapy or as patients fail to respond. After a satisfactory response has been achieved the patients dose should be reviewed and adjusted as required and tapered gradually.
- For mild to moderate pain: 400 mg 6 hourly or as demanded by the condition.
- For dysmenorrhoea: 400 mg every 4 hours or as demanded by the condition.
Topical Administrations-
Pain and inflammation associated with musculoskeletal and joint disorder: As 5% cream, foam, gel, spray soln or 10% gel: Apply onto affected area.
Side Effects
Usually Ibutin has a low incidence of side effects. The most frequent side effects are gastrointestinal disturbances. Peptic ulceration and gastrointestinal bleeding have occasionally been reported. Other side effects include headache, dizziness, nervousness, skin rash, pruritus, drowsiness, insomnia, blurred vision and other ocular reactions, hypersensitivity reaction, abnormal liver function test, impairment of renal function, agranulocytosis and thrombocytopenia.
Toxicity
The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinnitus, CNS depression, convulsions and seizures. May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).
The reported LD50 of ibuprofen is of 636 mg/kg in rat, 740 mg/kg in mouse and 495 mg/kg in guinea pig.
Precaution
Ibutin should be given with caution to patients with bleeding disorders, cardiovascular diseases, peptic ulceration or a history of such ulceration and in those who are receiving coumarin anticoagulants and in patients with renal or hepatic impairment.
Interaction
Increased risk of GI bleeding with warfarin, corticosteroids, SSRIs and aspirin. May reduce the natriuretic effects of diuretics. Reduced antihypertensive effect of ACE inhibitors and angiotensin II receptor antagonists. May increase toxicity of lithium and methotrexate. Increased nephrotoxicity with ciclosporin and tacrolimus.
Food Interaction
- Avoid alcohol.
- Take with food. Food reduces irritation.
Ibutin Alcohol interaction
[Moderate] GENERALLY AVOID:
The concurrent use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may lead to gastrointestinal (GI) blood loss.
The mechanism may be due to a combined local effect as well as inhibition of prostaglandins leading to decreased integrity of the GI lining.
Patients should be counseled on this potential interaction and advised to refrain from alcohol consumption while taking aspirin or NSAIDs.
Ibutin Hypertension interaction
[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).
Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.
Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.
Hypertension interaction[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.
NSAIDs should be used with caution in patients with hypertension.
Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.
Ibutin Drug Interaction
Moderate: duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acidsUnknown: diphenhydramine, diphenhydramine, pregabalin, pregabalin, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, alprazolam, alprazolam, cetirizine, cetirizine
Ibutin Disease Interaction
Major: asthma, fluid retention, GI toxicity, rash, renal toxicities, thrombosisModerate: PKU, anemia, heart failure, hepatotoxicity, hyperkalemia, hypertension, platelet aggregation inhibition
Volume of Distribution
The apparent volume of distribution of ibuprofen is of 0.1 L/kg.
Elimination Route
It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.
When orally administered, the absorption of ibuprofen in adults is very rapidly done in the upper GI tract. The average Cmax, Tmax and AUC ranges around 20 mcg/ml, 2 h and 70 mcg.h/ml. These parameters can vary depending on the enantiomer form, route, and dose of administration.
Half Life
The serum half-life of ibuprofen is 1.2-2 hours. In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4 hours.
Clearance
The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.
Elimination Route
Ibutin is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose. The biliary excretion of unchanged drug and active phase II metabolites represents 1% of the administered dose.
In summary, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not impaired by old age or the presence of renal impairment.
Pregnancy & Breastfeeding use
Ibutin is not recommended during pregnancy or for use in nursing mothers.
Contraindication
Ibutin should not be given to patients with hypersensitivity to lbuprofen and to individuals who show nasal polyps, angioedema, bronchospastic reactivity to aspirin or other non-steroidal anti-inflammatory drug. Ibutin is contraindicated in patients with active or previous peptic ulceration & gastro-intestinal ulceration or bleeding.
Acute Overdose
Gastric lavage, correction of blood electrolytes (if necessary). There is no specific antidote for Ibutin
Storage Condition
Keep in a cool & dry place. Keep out of the reach of children.
Innovators Monograph
You find simplified version here Ibutin
Ibutin contains Ibuprofen see full prescribing information from innovator Ibutin Monograph, Ibutin MSDS, Ibutin FDA label
FAQ
What is Ibutin used for?
Ibutin is a nonsteroidal anti-inflammatory drug (NSAID). It works by reducing hormones that cause inflammation and pain in the body. Ibutin is used to reduce fever and treat pain or inflammation caused by many conditions such as headache, toothache, back pain, arthritis, menstrual cramps, or minor injury.
What are the bad side effects of Ibutin?
The most common side effects of Ibutin are:
- headache.
- dizziness.
- drowsiness, fatigue and restless sleep.
- thirst and sweating.
- tingling or numbness in hands and feet.
- ringing in the ears.
- blurred vision and eye irritation.
- fluid retention and ankle swelling.
How many 400 mg Ibutin can I take?
It's important to read the enclosed leaflet carefully before using Ibutin tablets. For adults, the recommended dose is one 400mg tablet every four to six hours (up to three or four times a day). To prevent longer term side effects, the lowest effective dose and duration should be used to control your symptoms.
Can Ibutin keep me awake at night?
Aspirin and Ibutin disrupted sleep in comparison to placebo by increasing the number of awakenings and percentage of time spent in stage wake, and by decreasing sleep efficiency.
Is Ibutin a fever reducer?
It is classified as a pain reliever (analgesic) and fever reducer (antipyretic). Ibutin is often known by its given name, but you may also know it as Advil or Motrin. It is classified as a nonsteroidal anti-inflammatory drug (NSAID).
Can I lie down after taking ibuprofen?
Take Ibutin by mouth, usually every 4 to 6 hours with a full glass of water (8 ounces/240 milliliters) unless your doctor directs you otherwise. Do not lie down for at least 10 minutes after taking Ibutin. If you have stomach upset while taking this medication, take it with food, milk, or an antacid.
Does Ibutin raise blood pressure?
This may cause your blood pressure to rise even higher, putting greater stress on your heart and kidneys. NSAIDs can also raise your risk for heart attack or stroke, especially in higher doses. Common NSAIDs that can raise blood pressure include: Ibuprofen (Ibutin)
Is Ibutin a sedative?
Ibutin p.m. is a combination medication that contains ibuprofen and diphenhydramine, which is the active ingredient in Benadryl, an antihistamine taken for allergies. Diphenhydramine is sedating, so Ibutin p.m. is probably helping you get to sleep.
Which is better for fever acetaminophen or Ibutin?
A few studies have suggested Ibutin (ibuprofen) may be better than acetaminophen in helping to treat fevers over 102 – 103 F, while acetaminophen may be better for children who are also having stomach pain or upset, because Ibutin can sometimes irritate the stomach.
How do I know if Ibutin is working?
When Ibutin begins to work, you'll typically start to notice a decrease in pain or fever. The anti-inflammatory effects of Ibutin usually take longer — sometimes a week or more. Ibutin levels in your bloodstream are estimated to be at their maximum level after 1 to 2 hours
How much does Ibutin raise your blood pressure?
While celecoxib and naproxen produced either a slight decrease (celecoxib) or a relatively small increase (naproxen) in blood pressure, Ibutin was associated with a significant increase in ambulatory systolic blood pressure of more than 3 mmHg.
Who should not take Ibutin?
You should use Ibutin with caution if you're aged 65 or over, breastfeeding, or have:
- asthma.
- kidney or liver problems.
- lupus.
- Crohn's disease or ulcerative colitis.
- previously had any bleeding in your stomach.
- high blood pressure (hypertension)
- narrowing of the arteries (peripheral arterial disease)
Why should you eat when taking Ibutin?
It reduces stomach acid and increases mucus production. When Ibutin is taken in large doses or for a long time, less prostaglandin is produced. This can increase stomach acid and irritate the stomach lining, causing problems.
Can I drink after taking Ibutin?
Alcohol can also intensify the side effects of some medications. This second interaction is what can happen when you mix Ibutin and alcohol. In most cases, consuming a small amount of alcohol while taking Ibutin is not harmful.
Is Ibutin bad for your liver?
Nonprescription pain relievers such as acetaminophen (Tylenol, others), aspirin, Ibutin (Advil, Motrin IB, others) and naproxen (Aleve, others) can damage your liver, especially if taken frequently or combined with alcohol.
Is Ibutin an antidepressant?
Ibutin decreased the total immobility time during FST and TST and decreased cerebral PGE2 and NO levels, which was comparable to fluoxetine's effect. This would suggest that Ibutin might have an antidepressant effect through inhibition of PGE2 and NO production.
What happens when you take Ibutin on an empty stomach?
"Taking ibuprofen on an empty stomach may cause irritation of the stomach lining and bleeding ulcers," said South Florida-based cardiologist Dr. Adam Splaver of Nanohealth Associates.
Is Ibutin a painkiller?
Ibutin is an everyday painkiller for a range of aches and pains, including back pain, period pain, toothache. It also treats inflammation such as strains and sprains, and pain from arthritis. It's available as tablets and capsules, and as a syrup that you swallow.
What Ibutin does to the body?
Ibutin works by blocking the production of prostaglandins, substances that the body releases in response to illness and injury. Prostaglandins cause pain and swelling, or inflammation. They are released in the brain, and they can also cause fever. Ibutin's painkilling effects begin soon after taking a dose.
Should I take Ibutin for lower back pain?
If back pain keeps you from normal daily activities, your doctor can help by recommending or prescribing pain medications. Over-the-counter painkillers such as Tylenol, aspirin, or NSAIDs -- such as ketoprofen, ibuprofen (Advil, Motrin), and naproxen (Aleve) -- can be helpful.
Can I take Ibutin for back pain?
NSAIDs are often the go-to drugs for back pain relief. They can be purchased over the counter (or, in higher doses, by prescription) and include ibuprofen (Advil) and naproxen (Aleve). NSAIDs help reduce pain, swelling, and inflammation in muscles and around damaged spinal discs or arthritic joints.
