Ibugesic-M

Ibuprofen:

• Pharmacological action
• Pharmacokinetics
• Why is Ibugesic-M prescribed?
• Dosage and administration
• Ibugesic-M side effects
• Contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Ibugesic-M drug interactions
• Ibugesic-M in case of emergency / overdose
• Storage conditions
• Ibugesic-M (Ibuprofen) reviews

Pharmacological action

NSAIDs, a derivative of phenylpropionic acid, Ibugesic-M has anti-inflammatory, analgesic and antipyretic effect.

The mechanism of action is associated with inhibition of COX activity - the main enzyme metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. Analgesic effect is due to both peripheral (indirectly, through suppression of prostaglandin synthesis), and a central mechanism (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system). Inhibits platelet aggregation.

For topical use anti-inflammatory and analgesic action. Reduces morning stiffness, increased the amount of motion in joints.

Pharmacokinetics

When oral administered Ibugesic-M (Ibuprofen) almost completely absorbed from the gastrointestinal tract. Simultaneous food intake slows the rate of absorption. Metabolised in the liver (90%). T1 / 2 is 2-3 hours.

80% of the dose excreted in urine mainly as metabolites (70%), 10% - unchanged, 20% eliminated through the intestine in the form of metabolites.

Why is Ibugesic-M prescribed?

Inflammatory, degenerative diseases of joints and spine (including rheumatic and rheumatoid arthritis, ankylosing spondylitis, osteoarthritis), articular syndrome in patients with acute gout, psoriatic arthritis, ankylosing spondylitis, tendonitis, bursitis, sciatica, traumatic inflammation of soft tissue and musculoskeletal apparatus. Neuralgia, myalgia, pain in infectious and inflammatory diseases of ENT organs, bursitis, algomenorrhea, headache and toothache. Fever in infectious and inflammatory diseases.

Dosage and administration

Setting individually, depending on etiology of disease, severity of clinical manifestations. When administered rectally or adult single dose of 200-800 mg, the frequency of reception - 3-4; for children - 20-40 mg / kg in divided doses.

Topical applied within 2-3 weeks.

The maximum daily dose for adults when administered oral or rectally or is 2.4 g.

Oral, after a meal. Rheumatoid arthritis - by 0.8 g 3 times a day in osteoarthrosis and ankylosing spondylitis - by 0.4-0.6 g 3-4 times a day, in juvenile rheumatoid arthritis - at 30-40 mg / kg / day in several stages.

When soft tissue injuries, sprains - 1.6-2.4 g / day in divided doses.

At moderate pain syndrome - 1.2 g per day.

Ibugesic-M side effects

Digestive system: frequently - nausea, anorexia, vomiting, epigastric discomfort, diarrhea, possibly the development of erosive and ulcerative lesions of the gastrointestinal tract; rare - bleeding from the gastrointestinal tract, long-term use possible liver problems.

Central nervous system and peripheral nervous systems: frequently - headache, dizziness, sleep disturbances, agitation, visual impairment.

Hemopoietic system: long-term use may be anemia, thrombocytopenia, agranulocytosis.

Urinary tract: long-term use possible renal dysfunction.

Allergic reactions: often - skin rash, Quincke's edema, rarely - aseptic meningitis (usually in patients with autoimmune diseases), bronchospasm syndrome.

Local reactions: when topical used may be hyperemia of the skin, burning or tingling.

Contraindications

Erosive-ulcerative lesions in the gastrointestinal tract exacerbation, diseases of the optic nerve, "aspirin triad", hemodyscrasia, pronounced renal dysfunction and / or liver, children age, hypersensitivity to Ibugesic-M (Ibuprofen).

Using during pregnancy and breastfeeding

Do not use Ibugesic-M (Ibuprofen) in the III trimester of pregnancy. Application I and II trimesters of pregnancy is justified only in cases where the expected benefit to the mother than the possible harm to the fetus.

This medication Ibugesic-M (Ibuprofen) in small amounts excreted in breast milk. Possible using in lactation for pain and fever. If necessary, prolonged use or use in high doses (800 mg / 24 h), should decide on the termination of breastfeeding.

Special instructions

Precautions are used with the attendant liver and kidney diseases, chronic heart failure, with dyspeptic symptoms before treatment, immediately after surgery, with indications of a history of gastrointestinal bleeding in diseases of the digestive tract, allergic reactions associated with NSAID intake.

In the course of treatment requires systematic monitoring of the liver and kidneys, peripheral blood picture.

It should not be applied externally to the damaged skin.

Ibugesic-M drug interactions

With simultaneous use of Ibugesic-M (Ibuprofen) reduces the effect of antihypertensive agents (ACE inhibitors, beta-blockers), diuretics (furosemide, hypothiazide).

With the simultaneous use of anticoagulants may enhance their action.

With simultaneous application of SCS increases the risk of side effects from the gastrointestinal tract.

With the simultaneous application of Ibugesic-M (Ibuprofen) may displace from compounds with plasma proteins indirect anticoagulants (acenocoumarol), derivatives of hydantoin (phenytoin), oral hypoglycemic drugs sulfonylurea derivatives.

With the simultaneous use of amlodipine may be a slight reduction of antihypertensive action of amlodipine, with acetylsalicylic acid - decreased concentration of Ibugesic-M (Ibuprofen) in blood plasma, with baclofen - described a case of toxic gain of baclofen.

When applied simultaneously with warfarin may increase bleeding time, were also observed microhematuria, bruises with hydrochlorothiazide - perhaps a slight reduction of antihypertensive action of hydrochlorothiazide, captopril - may reduce antihypertensive effect of captopril, with cholestyramine - moderately decrease absorption of Ibugesic-M (Ibuprofen).

With simultaneous application of lithium carbonate increased the concentration of lithium in blood plasma.

With simultaneous application of magnesium hydroxide increases the initial absorption of Ibugesic-M (Ibuprofen), with methotrexate - increases the toxicity of methotrexate.

Ibugesic-M in case of emergency / overdose

In case of overdose, call your local poison control center or emergency services.

Symptoms of overdose may include: dizziness; fast eye movements that you cannot control; slow breathing or short periods of time without breathing; blue color around the lips, mouth, and nose.

Storage conditions

In a dry, protected from light place, at temperatures below 25°C.Common expiration date for Ibugesic-M (Ibuprofen) tablets: 3 years.

Methocarbamol:

• Description:
• Clinical pharmacology:
• Indications and usage:
• Contraindications:
• Warnings:
• Precautions:
• Adverse reactions
• Overdosage
• Dosage and administration:
• How supplied:
• Ibugesic-M (Methocarbamol) reviews

Ibugesic-M (Methocarbamol) TABLETS, USP

Rev. 03/11

Rx Only

DESCRIPTION:

Ibugesic-M (Methocarbamol) Tablets, USP, a carbamate derivative of guaifenesin, are a central nervous system (CNS) depressant with sedative and musculoskeletal relaxant properties. The structural formula is:

The chemical name for Ibugesic-M (Methocarbamol) is 3-(2-Methoxyphenoxy)-1,2-propanediol 1-carbamate and has the empirical formula C₁₁H₁₅NO₅. Its molecular weight is 241.24.

Ibugesic-M (Methocarbamol) is a white powder, sparingly soluble in water and chloroform, soluble in alcohol (only with heating) and propylene glycol, and insoluble in benzene and n-hexane.

Each tablet, for oral administration, contains 500 mg or 750 mg of Ibugesic-M (Methocarbamol), USP. In addition each tablet contains the following inactive ingredients: Colloidal Silicon Dioxide, Lactose Monohydrate, Magnesium Stearate, Methylcellulose, Microcrystalline Cellulose, Pregelatinized Starch and Sodium Starch Glycolate.

Ibugesic-M (Methocarbamol) structural formula

CLINICAL

Pharmacology:

The mechanism of action of Ibugesic-M in humans has not been established, but may be due to general central nervous system (CNS) depression. It has no direct action on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber.

Pharmacokinetics :

In healthy volunteers, the plasma clearance of Ibugesic-M (Methocarbamol) ranges between 0.20 and 0.80 L/h/kg, the mean plasma elimination half-life ranges between 1 and 2 hours, and the plasma protein binding ranges between 46% and 50%.

Ibugesic-M (Methocarbamol) is metabolized via dealkylation and hydroxylation. Conjugation of Ibugesic-M (Methocarbamol) also is likely. Essentially all Ibugesic-M (Methocarbamol) metabolites are eliminated in the urine. Small amounts of unchanged Ibugesic-M (Methocarbamol) also are excreted in the urine.

Special Populations :

Elderly

The mean elimination half-life of Ibugesic-M (Methocarbamol) in elderly healthy volunteers (mean (± SD) age, 69 (± 4) years) was slightly prolonged compared to a younger (mean (± SD) age, 53.3 (± 8.8) years), healthy population (1.5 (±0.4) hours versus 1.1 (±0.27) hours, respectively). The fraction of bound Ibugesic-M (Methocarbamol) was slightly decreased in the elderly versus younger volunteers (41 to 43% versus 46 to 50%, respectively).

Renally Impaired

The clearance of Ibugesic-M (Methocarbamol) in 8 renally-impaired patients on maintenance hemodialysis was reduced about 40% compared to 17 normal subjects, although the mean (±SD) elimination half-life in these two groups was similar: 1.2 (±0.6) versus 1.1 (±0.3) hours, respectively.

Hepatically Impaired

In 8 patients with cirrhosis secondary to alcohol abuse, the mean total clearance of Ibugesic-M (Methocarbamol) was reduced approximately 70% compared to that obtained in 8 age- and weight-matched normal subjects. The mean (±SD) elimination half-life in the cirrhotic patients and the normal subjects was 3.38 (±1.62) hours and 1.11 (±0.27) hours, respectively. The percent of Ibugesic-M (Methocarbamol) bound to plasma proteins was decreased to approximately 40 to 45% compared to 46 to 50% in the normal subjects.

INDICATIONS AND USAGE:

Ibugesic-M (Methocarbamol) Tablets are indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions. The mode of action of Ibugesic-M (Methocarbamol) has not been clearly identified, but may be related to its sedative properties. Ibugesic-M (Methocarbamol) does not directly relax tense skeletal muscles in man.

CONTRAINDICATIONS:

Methocarbamol Tablets are contraindicated in patients hypersensitive to Ibugesic-M (Methocarbamol) or to any of the tablet components.

WARNINGS:

Since Ibugesic-M may possess a general CNS depressant effect, patients receiving Ibugesic-M (Methocarbamol) Tablets should be cautioned about combined effects with alcohol and other CNS depressants.

Safe use of Ibugesic-M (Methocarbamol) Tablets has not been established with regard to possible adverse effects upon fetal development. There have been reports of fetal and congenital abnormalities following in utero exposure to Ibugesic-M (Methocarbamol). Therefore, Ibugesic-M (Methocarbamol) Tablets should not be used in women who are or may become pregnant and particularly during early pregnancy unless in the judgment of the physician the potential benefits outweigh the possible hazards (see PRECAUTIONS : Pregnancy ).

Use in Activities Requiring Mental Alertness :

Ibugesic-M (Methocarbamol) may impair mental and/or physical abilities required for performance of hazardous tasks, such as operating machinery or driving a motor vehicle. Patients should be cautioned about operating machinery, including automobiles, until they are reasonably certain that Ibugesic-M (Methocarbamol) therapy does not adversely affect their ability to engage in such activities.

PRECAUTIONS:

Information for Patients:

Patients should be cautioned that Ibugesic-M may cause drowsiness or dizziness, which may impair their ability to operate motor vehicles or machinery.

Because Ibugesic-M (Methocarbamol) may possess a general CNS-depressant effect, patients should be cautioned about combined effects with alcohol and other CNS depressants.

Drug Interactions:

See WARNINGS and PRECAUTIONS for interaction with CNS drugs and alcohol.

Ibugesic-M (Methocarbamol) may inhibit the effect of pyridostigmine bromide. Therefore, Ibugesic-M (Methocarbamol) should be used with caution in patients with myasthenia gravis receiving anticholinesterase agents.

Drug /Laboratory Test Interactions:

Ibugesic-M may cause a color interference in certain screening tests for 5-hydroxyindoleacetic acid (5-HIAA) using nitrosonaphthol reagent and in screening tests for urinary vanillylmandelic acid (VMA) using the Gitlow method.

Carcinogenesis, Mutagenesis, Impairment of Fertility :

Long-term studies to evaluate the carcinogenic potential of Ibugesic-M (Methocarbamol) have not been performed. No studies have been conducted to assess the effect of Ibugesic-M (Methocarbamol) on mutagenesis or its potential to impair fertility.

Pregnancy

Teratogenic Effects

Pregnancy Category C

Animal reproduction studies have not been conducted with Ibugesic-M. It is also not known whether Ibugesic-M (Methocarbamol) can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Methocarbamol Tablets should be given to a pregnant woman only if clearly needed.

Safe use of Ibugesic-M (Methocarbamol) Tablets has not been established with regard to possible adverse effects upon fetal development. There have been reports of fetal and congential abnormalities following in utero exposure to Ibugesic-M (Methocarbamol). Therefore, Ibugesic-M (Methocarbamol) Tablets should not be used in women who are or may become pregnant and particularly during early pregnancy unless in the judgment of the physician the potential benefits outweigh the possible hazards (see WARNINGS ).

Nursing Mothers

Ibugesic-M (Methocarbamol) and/or its metabolites are excreted in the milk of dogs; however, it is not known whether Ibugesic-M (Methocarbamol) or its metabolites are excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Ibugesic-M (Methocarbamol) Tablets are administered to a nursing woman.

Pediatric Use

Safety and effectiveness of Ibugesic-M (Methocarbamol) Tablets in pediatric patients below the age of 16 have not been established.

ADVERSE REACTIONS

Adverse reactions reported coincident with the administration of Ibugesic-M (Methocarbamol) include:

Body as a Whole : Anaphylactic reaction, angioneurotic edema, fever, headache

Car d iovascular System : Bradycardia, flushing, hypotension, syncope, thrombophlebitis

Digestive System : Dyspepsia, jaundice (including cholestatic jaundice), nausea and vomiting

Hemic and Lymphatic S ystem : Leukopenia

Immune System : Hypersensitivity reactions

Nervous System : Amnesia, confusion, diplopia, dizziness or lightheadedness, drowsiness, insomnia, mild muscular incoordination, nystagmus, sedation, seizures (including grand mal), vertigo

Skin and Special Senses : Blurred vision, conjunctivitis, nasal congestion, metallic taste, pruritus, rash, urticaria

To report SUSPECTED ADVERSE REACTIONS, contact West-ward Pharmaceutical Corp. at 1-877-233-2001, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

OVERDOSAGE

Limited information is available on the acute toxicity of Ibugesic-M. Overdose of Ibugesic-M (Methocarbamol) is frequently in conjunction with alcohol or other CNS depressants and includes the following symptoms: nausea, drowsiness, blurred vision, hypotension, seizures, and coma.

In post-marketing experience, deaths have been reported with an overdose of Ibugesic-M (Methocarbamol) alone or in the presence of other CNS depressants, alcohol or psychotropic drugs.

Treatment:

Management of overdose includes symptomatic and supportive treatment. Supportive measures include maintenance of an adequate airway, monitoring urinary output and vital signs, and administration of intravenous fluids if necessary. The usefulness of hemodialysis in managing overdose is unknown.

DOSAGE AND ADMINISTRATION:

500 mg – Adults: Initial dosage, 3 tablets q.i.d.; maintenance dosage, 2 tablets q.i.d.

750 mg – Adults: Initial dosage, 2 tablets q.i.d.; maintenance dosage, 1 tablet q.4h. or 2 tablets t.i.d.

Six grams a day are recommended for the first 48 to 72 hours of treatment. (For severe conditions 8 grams a day may be administered.) Thereafter, the dosage can usually be reduced to approximately 4 grams a day.

HOW SUPPLIED:

Ibugesic-M (Methocarbamol) Tablets 500 mg: White, Round Tablets; Debossed “West-ward 290” on one side and Scored on the other side.

Bottles of 100 tablets

Bottles of 500 tablets

Bottles of 1000 tablets

Unit Dose Box of 100 tablets

Ibugesic-M (Methocarbamol) Tablets 750 mg: White, Capsule Shaped Tablets; Debossed “WEST-WARD 292” on one side and Scored on the other side.

Bottles of 100 tablets

Bottles of 500 tablets

Bottles of 1000 tablets

Unit Dose Box of 100 tablets

Store at 20-25^oC (68-77^oF). Protect from light and moisture.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

Manufactured by:

West-ward Pharmaceutical Corp.

Eatontown, NJ 07724

Revised March 2011