Lexmodine may be available in the countries listed below.
Ingredient matches for Lexmodine
Famotidine
Famotidine is reported as an ingredient of Lexmodine in the following countries:
- Indonesia
International Drug Name Search
Thursday, September 29, 2016
Wednesday, September 28, 2016
Lexin
Lexin may be available in the countries listed below.
Ingredient matches for Lexin
Carbamazepine
Carbamazepine is reported as an ingredient of Lexin in the following countries:
- Japan
Cefalexin
Cefalexin is reported as an ingredient of Lexin in the following countries:
- Argentina
- Ethiopia
- Peru
Cefalexin monohydrate (a derivative of Cefalexin) is reported as an ingredient of Lexin in the following countries:
- Bahrain
- Iraq
- Jordan
- Kuwait
- Oman
- Saudi Arabia
- Syria
- United Arab Emirates
- Yemen
International Drug Name Search
Inflaflur
Inflaflur may be available in the countries listed below.
Ingredient matches for Inflaflur
Flurbiprofen
Flurbiprofen sodium salt (a derivative of Flurbiprofen) is reported as an ingredient of Inflaflur in the following countries:
- Greece
International Drug Name Search
Doxorubicine
Doxorubicine may be available in the countries listed below.
Ingredient matches for Doxorubicine
Doxorubicin
Doxorubicine (DCF) is known as Doxorubicin in the US.
International Drug Name Search
Glossary
| DCF | Dénomination Commune Française |
Click for further information on drug naming conventions and International Nonproprietary Names.
Lisinopril Jaba
Lisinopril Jaba may be available in the countries listed below.
Ingredient matches for Lisinopril Jaba
Lisinopril
Lisinopril dihydrate (a derivative of Lisinopril) is reported as an ingredient of Lisinopril Jaba in the following countries:
- Portugal
International Drug Name Search
Penicillinum procainicum L
Penicillinum procainicum L may be available in the countries listed below.
Ingredient matches for Penicillinum procainicum L
Benzylpenicillin
Benzylpenicillin procaine (a derivative of Benzylpenicillin) is reported as an ingredient of Penicillinum procainicum L in the following countries:
- Poland
International Drug Name Search
Sominex Tablets (Actavis UK Ltd)
1. Name Of The Medicinal Product
Sominex
2. Qualitative And Quantitative Composition
Promethazine hydrochloride EP 20mg/tab
3. Pharmaceutical Form
Tablet
4. Clinical Particulars
4.1 Therapeutic Indications
As a night-time sleep aid, for the correction of temporary disturbances of sleep pattern where there is difficulty in going to sleep or staying asleep, caused for example by specific dislocation of normal routine.
4.2 Posology And Method Of Administration
Oral
For bedtime use only.
Adults: one tablet at bedtime. May be taken up to one hour after going to bed when sleep is difficult to achieve.
Not to be given to children under the age of 16 years except on medical advice.
Elderly: the normal adult dose may be taken.
4.3 Contraindications
Known hypersensitivity to promethazine or phenothiazines. Patients taking MAOIs or within 14 days of taking MAOIs. Patients with any form of CNS depression.
4.4 Special Warnings And Precautions For Use
Cause drowsiness. Do not drive or operate machinery.
Not to be used for more than 7 days without medical advice.
Concomitant use of alcohol should be avoided.
In patients with asthma or other respiratory disorders (eg bronchitis or bronchiectasis), glaucoma, epilepsy, urinary retention, prostatic hypertrophy, hepatic or renal impairment, cardiovascular problems or pyloroduodenal obstruction the product should only be taken after consulting a doctor.
This product should be used with caution in patients with seizure disorders or in patients receiving medication which may affect the seizure threshold because of risk of convulsions.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Promethazine hydrochloride may potentiate the action of alcohol and other centrally acting depressants such as sedatives (barbiturates), opiod analgesics, antipsychotics, anticonvulsants, hypnotics and anxiolytics. MAOIs may enhance the antimuscarinic effects of antihistamines.
Antihistamines have an added antimuscarinic effect with other antimuscarinic drugs such as atropine and tricyclic antidepressants. Promethazine may interfere with immunologic urine pregnancy tests to produce false positive or negative results.
Promethazine hydrochloride should be discontinued at least 72 hours before the start of skin tests as it may inhibit the cutaneous histamine response thus producing false negative results.
4.6 Pregnancy And Lactation
The advice of a doctor should be sought before use.
4.7 Effects On Ability To Drive And Use Machines
This product causes drowsiness. Do not drive or operate machinery.
4.8 Undesirable Effects
Blood and lymphatic system disorders
Agranulocytosis, leucopenia, thrombocytopenia. Blood dycrasias occur rarely.
Psychiatric disorders
Sedation, paradoxical reactions such as hyperexcitability and abnormal movements, drowsiness, confusion, disorientation, restlessness, insomnia.
Nervous system disorders
Convulsive seizures, headache, psychomotor impairment, antimuscarinic effects (dry mouth, blurred vision, urinary retention). Dizziness, tremor and extrapyramidal effects are rare side effects.
Eye disorders
Angle closure glaucoma occurs rarely.
Ear and labyrinth disorders
Tinnitus.
Heart rate and rhythm disorders
Palpitations, arrhythmias.
Vascular disorders
Hypotension.
Respiratory, thoracic and mediastinal disorders
Nasal stuffiness. Bronchospasm occurs rarely.
Gastrointestinal disorders
Nausea, vomiting.
Hepatobiliary disorders
Jaundice occurs rarely.
Skin and subcutaneous tissue disorders
Photosensitivity. Angioedema and rashes occur rarely.
General disorders and administration site conditions
Anaphylaxis occurs rarely.
The elderly are particularly susceptible to the anticholinergic effects and confusion due to promethazine.
4.9 Overdose
Common features include:
nausea, vomiting, flushing, dilated pupils, dry mouth and tongue, hot dry skin, fever, sinus tachycardia, hypertension, ataxia, nystagmus, drowsiness, delirium, agitation and visual hallucinations.
Uncommon systemic features include:
myoclonic jerking, coma, convulsions, cardiac conduction abnormalities and dysrhythmias, cardiovascular collapse, paralytic ileus, urinary retention and cardiorespiratory depression.
Patients who have been unconscious may be hypothermic.
In cases of unintentional exposure:
Children may also experience combinations of excitation, ataxia, incoordination, athetosis and hallucinations.
Treatment:
Gastric lavage or activated charcoal is only recommended if the patient presents within 1 hour of ingestion of a potentially toxic amount.
Treatment is otherwise supportive with attention to maintenance of adequate respiratory and circulatory status. Convulsions should be treated with diazepam or other suitable anticonvulsants.
Forced diuresis, haemodialysis and haemoperfusion are of no value
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Promethazine hydrochloride – sedative. The drug is an antihistamine with anticholinergic activity.
5.2 Pharmacokinetic Properties
Promethazine hydrochloride is readily absorbed from the gastrointestinal tract, but undergoes extensive first pass metabolism in the liver. With only 25% of the oral dose reaching the systemic circulation unchanged. After oral therapy therapeutic effects are identifiable at 15-30 minutes and peak plasma concentrations at 2 to 3 hours. Estimates of terminal half-life in blood plasma have been quoted as 4-6 hours. It is extensively plasma protein bound. It is eliminated mainly as metabolites, predominantly by the faecal (via biliary) route, with <1% of the parent compound and CA 10% as the sulphoxide metabolite being excreted in the urine over a 72 hour period.
5.3 Preclinical Safety Data
None stated.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Lactose, maize starch, croscarmellose sodium, magnesium stearate.
6.2 Incompatibilities
None known.
6.3 Shelf Life
60 months unopened.
6.4 Special Precautions For Storage
None.
6.5 Nature And Contents Of Container
Opaque blister strip of polyvinylchloride/polyvinylidine chloride. Backed with aluminium foil. Each strip contains 8 tablets. One or two strips are packed into each cardboard carton.
6.6 Special Precautions For Disposal And Other Handling
None.
7. Marketing Authorisation Holder
Actavis Group PTC ehf
Reykjavíkurvegi 76-78
220 Hafnarfjordur
Iceland.
8. Marketing Authorisation Number(S)
PL 30306/0080
9. Date Of First Authorisation/Renewal Of The Authorisation
6th September 2002
10. Date Of Revision Of The Text
16/09/2010
11 DOSIMETRY (IF APPLICABLE)
Not Applicable
12 INSTRUCTIONS FOR PREPARATION OF RADIOPHARMACEUTICALS (IF APPLICABLE)
Not Applicable
Levothroid
In the US, Levothroid (levothyroxine systemic) is a member of the drug class thyroid drugs and is used to treat Hashimoto's disease, Hypothyroidism - After Thyroid Removal, Myxedema Coma, Thyroid Suppression Test, TSH Suppression and Underactive Thyroid.
US matches:
- Levothroid
Ingredient matches for Levothroid
Levothyroxine
Levothyroxine sodium salt (a derivative of Levothyroxine) is reported as an ingredient of Levothroid in the following countries:
- Spain
- United States
International Drug Name Search
Pannocort
Pannocort may be available in the countries listed below.
Ingredient matches for Pannocort
Hydrocortisone
Hydrocortisone 21-acetate (a derivative of Hydrocortisone) is reported as an ingredient of Pannocort in the following countries:
- Belgium
- Luxembourg
International Drug Name Search
Luprostiol
In some countries, this medicine may only be approved for veterinary use.
Scheme
Rec.INN
CAS registry number (Chemical Abstracts Service)
0067110-79-6
Chemical Formula
C21-H29-Cl-O6-S
Molecular Weight
444
Therapeutic Categories
Oxytocic
Prostaglandin analogue
Chemical Name
5-Heptenoic acid, 7-[2-[[3-(3-chlorophenoxy)-2-hydroxypropyl]thio]-3,5-dihydroxycyclopentyl]-, [1α(Z),2ß(R*),3α,5α]-(±)-
Foreign Names
- Luprostiolum (Latin)
- Luprostiol (German)
- Luprostiol (French)
- Luprostiol (Spanish)
Generic Names
- Luprostiol (OS: BAN)
- EMD 34 946 (IS: Merck)
- Prostianol (IS)
Brand Names
- Equestrolin (veterinary use)
Intervet, United States - Prosolvin (veterinary use)
Intervet, United Kingdom; Intervet, Ireland; Intervet, Italy; Intervet, Netherlands; Intervet, Sweden; Intervet, United States; Intervet, South Africa; Organon Vet, Portugal; Virbac, Switzerland; Virbac, France; Virbac, New Zealand; Virbac, South Africa - Prostapar (veterinary use)
Intervet, United Kingdom; Intervet, Netherlands; Intervet Schering-Plough Animal Health, Portugal
International Drug Name Search
Glossary
| BAN | British Approved Name |
| IS | Inofficial Synonym |
| OS | Official Synonym |
| Rec.INN | Recommended International Nonproprietary Name (World Health Organization) |
Click for further information on drug naming conventions and International Nonproprietary Names.
Oestro Tabs Plus cyclic
Oestro Tabs Plus cyclic may be available in the countries listed below.
Ingredient matches for Oestro Tabs Plus cyclic
Estradiol
Estradiol hemihydrate (a derivative of Estradiol) is reported as an ingredient of Oestro Tabs Plus cyclic in the following countries:
- Switzerland
Medroxyprogesterone
Medroxyprogesterone 17α-acetate (a derivative of Medroxyprogesterone) is reported as an ingredient of Oestro Tabs Plus cyclic in the following countries:
- Switzerland
International Drug Name Search
Tuesday, September 27, 2016
Levox
Levox may be available in the countries listed below.
Ingredient matches for Levox
Levofloxacin
Levofloxacin is reported as an ingredient of Levox in the following countries:
- Bangladesh
- Philippines
International Drug Name Search
Lumidol
Lumidol may be available in the countries listed below.
Ingredient matches for Lumidol
Tramadol
Tramadol is reported as an ingredient of Lumidol in the following countries:
- Bosnia & Herzegowina
Tramadol hydrochloride (a derivative of Tramadol) is reported as an ingredient of Lumidol in the following countries:
- Croatia (Hrvatska)
International Drug Name Search
Adrenalina Galenica
Adrenalina Galenica may be available in the countries listed below.
Ingredient matches for Adrenalina Galenica
Epinephrine
Epinephrine is reported as an ingredient of Adrenalina Galenica in the following countries:
- Italy
International Drug Name Search
Lexinor
Lexinor may be available in the countries listed below.
Ingredient matches for Lexinor
Norfloxacin
Norfloxacin is reported as an ingredient of Lexinor in the following countries:
- Philippines
- Thailand
International Drug Name Search
Sulfachlorpyridazine Sodium
Sulfachlorpyridazine Sodium may be available in the countries listed below.
Ingredient matches for Sulfachlorpyridazine Sodium
Sulfachlorpyridazine
Sulfachlorpyridazine Sodium (BAN) is also known as Sulfachlorpyridazine (Rec.INN)
International Drug Name Search
Glossary
| BAN | British Approved Name |
| Rec.INN | Recommended International Nonproprietary Name (World Health Organization) |
Click for further information on drug naming conventions and International Nonproprietary Names.
Lexmox
Lexmox may be available in the countries listed below.
Ingredient matches for Lexmox
Amoxicillin
Amoxicillin is reported as an ingredient of Lexmox in the following countries:
- India
International Drug Name Search
Goritel
Goritel may be available in the countries listed below.
Ingredient matches for Goritel
Amlodipine
Amlodipine besilate (a derivative of Amlodipine) is reported as an ingredient of Goritel in the following countries:
- Ecuador
International Drug Name Search
Secnizol ratio
Secnizol ratio may be available in the countries listed below.
Ingredient matches for Secnizol ratio
Secnidazole
Secnidazole is reported as an ingredient of Secnizol ratio in the following countries:
- Dominican Republic
International Drug Name Search
Monday, September 26, 2016
Lumirelax
Lumirelax may be available in the countries listed below.
Ingredient matches for Lumirelax
Methocarbamol
Methocarbamol is reported as an ingredient of Lumirelax in the following countries:
- France
International Drug Name Search
Platin
Platin may be available in the countries listed below.
Ingredient matches for Platin
Fluoxetine
Fluoxetine hydrochloride (a derivative of Fluoxetine) is reported as an ingredient of Platin in the following countries:
- India
International Drug Name Search
Lunvon
Lunvon may be available in the countries listed below.
Ingredient matches for Lunvon
Bromhexine
Bromhexine hydrochloride (a derivative of Bromhexine) is reported as an ingredient of Lunvon in the following countries:
- Japan
International Drug Name Search
Lextrasa
Lextrasa may be available in the countries listed below.
Ingredient matches for Lextrasa
Mesalazine
Mesalazine is reported as an ingredient of Lextrasa in the following countries:
- Italy
International Drug Name Search
Terbinafin-ratiopharm
Terbinafin-ratiopharm may be available in the countries listed below.
Ingredient matches for Terbinafin-ratiopharm
Terbinafine
Terbinafine hydrochloride (a derivative of Terbinafine) is reported as an ingredient of Terbinafin-ratiopharm in the following countries:
- Austria
- Denmark
- Finland
- Germany
- Hungary
- Sweden
International Drug Name Search
Lipiget
Lipiget may be available in the countries listed below.
Ingredient matches for Lipiget
Atorvastatin
Atorvastatin is reported as an ingredient of Lipiget in the following countries:
- Vietnam
International Drug Name Search
Friday, September 23, 2016
Levotuss
Levotuss may be available in the countries listed below.
Ingredient matches for Levotuss
Levodropropizine
Levodropropizine is reported as an ingredient of Levotuss in the following countries:
- Belgium
- Greece
- Italy
- Malta
- Portugal
- Spain
International Drug Name Search
Irzaim
Irzaim may be available in the countries listed below.
Ingredient matches for Irzaim
Serrapeptase
Serrapeptase is reported as an ingredient of Irzaim in the following countries:
- Japan
International Drug Name Search
Lumisteron
Lumisteron may be available in the countries listed below.
Ingredient matches for Lumisteron
Hyaluronic Acid
Hyaluronic Acid sodium salt (a derivative of Hyaluronic Acid) is reported as an ingredient of Lumisteron in the following countries:
- Japan
International Drug Name Search
Linvas
Linvas may be available in the countries listed below.
Ingredient matches for Linvas
Lisinopril
Lisinopril is reported as an ingredient of Linvas in the following countries:
- India
International Drug Name Search
Lunex
Lunex may be available in the countries listed below.
Ingredient matches for Lunex
Tranexamic Acid
Tranexamic Acid is reported as an ingredient of Lunex in the following countries:
- Indonesia
International Drug Name Search
Lévoglutamide
Lévoglutamide may be available in the countries listed below.
Ingredient matches for Lévoglutamide
Glutamine
Lévoglutamide (DCF) is known as Glutamine in the US.
International Drug Name Search
Glossary
| DCF | Dénomination Commune Française |
Click for further information on drug naming conventions and International Nonproprietary Names.
Lumiracoxib
Scheme
Rec.INN
ATC (Anatomical Therapeutic Chemical Classification)
M01AH06
CAS registry number (Chemical Abstracts Service)
0220991-20-8
Chemical Formula
C15-H13-Cl-F-N-O2
Molecular Weight
293
Therapeutic Categories
Analgesic, antipyretic and anti-inflammatory agent
Non-steroidal anti-inflammatory drug, NSAID
Cyclo-oxygenase 2 (COX-2) inhibitor
Chemical Names
[2-[(2-Chloro-6-fluorophenyl)amino]-5-methylphenyl]acetic acid (WHO)
2-[2-(2-Chlor-6-fluorphenylamino)-5-methylphenyl]essigsäure (IUPAC)
Benzeneacetic acid, 2-[(2-chloro-6-fluorophenyl)amino]-5-methyl- (USAN)
Foreign Names
- Lumiracoxibum (Latin)
- Lumiracoxib (German)
- Lumiracoxib (French)
- Lumiracoxib (Spanish)
Generic Names
- Lumiracoxib (OS: USAN, BAN)
- COX-189 (IS: Novartis)
- Prexige (IS)
Brand Names
- Prexige
Novartis, Argentina; Novartis, Brazil; Novartis, Chile; Novartis, Ecuador; Novartis, Estonia; Novartis, Georgia; Novartis, Lithuania; Novartis, Latvia; Novartis, Mexico; Novartis, Philippines; Novartis, Thailand
International Drug Name Search
Glossary
| BAN | British Approved Name |
| IUPAC | International Union of Pure and Applied Chemistry |
| IS | Inofficial Synonym |
| OS | Official Synonym |
| Rec.INN | Recommended International Nonproprietary Name (World Health Organization) |
| USAN | United States Adopted Name |
| WHO | World Health Organization |
Click for further information on drug naming conventions and International Nonproprietary Names.
Luinesin
Luinesin may be available in the countries listed below.
Ingredient matches for Luinesin
Gentamicin
Gentamicin sulfate (a derivative of Gentamicin) is reported as an ingredient of Luinesin in the following countries:
- Japan
International Drug Name Search
Thursday, September 22, 2016
Celebrex
Generic Name: Celecoxib
Class: Cyclooxygenase-2 (COX-2) Inhibitors
Chemical Name: 4-[5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
CAS Number: 184007-95-2
- Cardiovascular Risk
Possible increased risk of serious (sometimes fatal) cardiovascular thrombotic events (e.g., MI, stroke).1 Risk may increase with duration of use.1 Individuals with cardiovascular disease or risk factors for cardiovascular disease may be at increased risk.1 (See Cardiovascular Effects under Cautions.)
Contraindicated for the treatment of pain in the setting of CABG surgery.1
- GI Risk
Increased risk of serious (sometimes fatal) GI events (e.g., bleeding, ulceration, perforation of the stomach or intestine).1 Serious GI events can occur at any time and may not be preceded by warning signs and symptoms.1 Geriatric individuals are at greater risk for serious GI events.1 (See GI Effects under Cautions.)
Introduction
NSAIA1 2 3 4 5 8 11 41 that is a selective inhibitor of cycloogenase-2 (COX-2);1 2 8 diaryl-substituted pyrazole derivative containing a sulfonamide substituent.1 2 3 4 5 8 11 41
Uses for Celebrex
Consider potential benefits and risks of celecoxib therapy as well as alternative therapies before initiating therapy with the drug.1 Use lowest effective dosage and shortest duration of therapy consistent with the patient's treatment goals.1
Osteoarthritis
Symptomatic treatment of osteoarthritis.1 2 3 28 29 64 Effect comparable to that of prototypical NSAIAs (naproxen).1 2 3 28 29 64
Lower incidence of endoscopically confirmed GI ulcer and serious adverse GI effects than prototypical NSAIAs.1 28 29 33 79
Rheumatoid Arthritis in Adults
Symptomatic treatment of rheumatoid arthritis in adults.1 2 3 9 10 21 23 24 28 65 66 99 Effect comparable to that of prototypical NSAIAs (naproxen, diclofenac).1 2 3 9 10 21 23 24 28 65 66 99
Lower incidence of endoscopically confirmed GI ulcer and serious adverse GI effects than prototypical NSAIAs.1 3 9 10 21 23 24 28 33 65 66 79
Juvenile Arthritis
Symptomatic management of pauciarticular course, polyarticular course, or systemic onset juvenile rheumatoid arthritis in children ≥2 years of age.1 Effect comparable to that of naproxen.1
Ankylosing Spondylitis
Management of the signs and symptoms of ankylosing spondylitis.1 132
Colorectal Polyps
Reduction of the number of adenomatous colorectal polyps (colorectal adenomas) in adults with familial adenomatous polyposis (FAP); used as an adjunct to usual care.1 60 Not known whether celecoxib reduces the risk of colorectal, duodenal, or other FAP-related cancers.1
Has been investigated for the prevention of colorectal adenomas in patients without a history of FAP†.149 150 Use of celecoxib reduces the risk of recurrent colorectal adenomas;149 150 not known whether celecoxib reduces the risk of colorectal cancer.149 150 Routine use not recommended because of the potential for serious cardiovascular events.149
Pain
Management of acute pain, including postoperative (e.g., dental, orthopedic) pain, in adults.1 8 42 43
Dysmenorrhea
Symptomatic management of primary dysmenorrhea in adults.1 2
Cardiovascular Risk Reduction
Not a substitute for aspirin in the prevention of adverse cardiovascular events (MI).1 (See Cardiovascular Effects under Cautions.)
Celebrex Dosage and Administration
General
Consider potential benefits and risks of celecoxib therapy as well as alternative therapies before initiating therapy with the drug.1
Administration
Oral Administration
Administer orally once or twice daily for osteoarthritis or ankylosing spondylitis; administer twice daily for rheumatoid arthritis, juvenile arthritis, colorectal polyps, pain, or dysmenorrhea.1 2
Administer dosages up to 200 mg twice daily without regard to meals; administer higher dosages (400 mg twice daily) with food.1
For patients who have difficulty swallowing capsules, the capsule may be opened and the contents sprinkled onto a level teaspoonful of applesauce at room temperature or cooler, and the mixture swallowed immediately with water.1
Dosage
To minimize the potential risk of adverse cardiovascular and/or GI events, use lowest effective dosage and shortest duration of therapy consistent with the patient's treatment goals.1
Attempt to titrate to the lowest effective dosage in adults with arthritis.1
Pediatric Patients
Juvenile Arthritis
Oral
Children ≥2 years of age weighing 10–25 kg: 50 mg twice daily.1
Children ≥2 years of age weighing >25 kg: 100 mg twice daily.1
Adults
Osteoarthritis
Oral
200 mg daily as a single dose or in 2 equally divided doses.1 2 3
No additional benefit from dosages >200 mg daily.1
Rheumatoid Arthritis in Adults
Oral
100–200 mg twice daily.1 78
No additional benefit from higher dosages (400 mg twice daily).1
Ankylosing Spondylitis
Oral
Initially, 200 mg daily as a single dose or in 2 equally divided doses.1 If no response observed after 6 weeks, increase to 400 mg daily.1 If no response observed after 400 mg daily for 6 weeks, response is unlikely; consider alternative therapies.1
Colorectal Polyps
Oral
400 mg twice daily.1 60
Pain
Oral
400 mg initially as a single dose, followed by an additional dose of 200 mg, if necessary, on the first day.1 For continued relief, 200 mg twice daily as needed.1
Dysmenorrhea
Oral
400 mg initially as a single dose, followed by an additional dose of 200 mg, if necessary, on the first day.1 For continued relief, 200 mg twice daily as needed.1
Special Populations
Hepatic Impairment
Reduce dosage by 50% in patients with moderate hepatic impairment; not recommended in patients with severe impairment.1
Geriatric Patients
Dosage adjustment based solely on age is not necessary; initiate at lowest recommended dosage in geriatric patients weighing <50 kg.1
Cautions for Celebrex
Contraindications
Known hypersensitivity to celecoxib, sulfonamides, or any ingredient in the formulation.1
History of asthma, urticaria, or other sensitivity reaction precipitated by aspirin or other NSAIAs.1
Treatment of perioperative pain in the setting of CABG surgery.1
Warnings/Precautions
Warnings
Cardiovascular Effects
Selective COX-2 inhibitors have been associated with increased risk of cardiovascular events (e.g., MI, stroke) in certain situations.1 103 104 113 116 122 123 129 130 131 134 137 138 139 140 141 146 147 148 Several prototypical NSAIAs also have been associated with increased risk of cardiovascular events.146 147 148 Current evidence suggests that use of celecoxib at dosages >200 mg daily is associated with increased cardiovascular risk, while the potential risk is less clear at dosages of ≤200 mg daily.146 148 157 158
Short-term use to relieve acute pain, especially at low dosages, does not appear to be associated with increased risk of serious cardiovascular events (except immediately following CABG surgery).133
Not known whether long-term use in children is associated with increased cardiovascular risk.1
Use celecoxib with caution and careful monitoring (e.g., monitor for development of cardiovascular events).1 102 112 Until more data are available, a selective COX-2 inhibitor remains an appropriate choice for patients at low cardiovascular risk who have had serious GI events, especially while receiving a prototypical NSAIA.112 121 128 145 May be prudent to avoid use of selective COX-2 inhibitors in patients who have or are at risk for cardiovascular disease.112 121 124 128 142 143
No consistent evidence that concomitant use of low-dose aspirin mitigates the increased risk of serious adverse cardiovascular events associated with NSAIAs.1 103 133 134 135 139 141 (See Specific Drugs under Interactions.)
Hypertension and worsening of preexisting hypertension reported; either event may contribute to the increased incidence of cardiovascular events.1 Use with caution in patients with hypertension; monitor BP.1 Impaired response to certain diuretics may occur.1 (See Specific Drugs under Interactions.)
Fluid retention and edema reported.1 Caution in patients with fluid retention or heart failure.1
GI Effects
Serious GI toxicity (e.g., bleeding, ulceration, perforation) can occur with or without warning symptoms; increased risk in those with a history of GI bleeding or ulceration, geriatric patients, smokers, those with alcohol dependence, and those in poor general health.1
Lower risk of GI ulceration than prototypical NSAIAs.1 2 3 9 21 22 24 28 29 33 38 65 66
Renal Effects
Adverse renal effects similar to those of prototypical NSAIAs.1 2 58 59
Direct renal injury, including renal papillary necrosis, reported in patients receiving long-term NSAIA therapy.1
Potential for overt renal decompensation.1 Increased risk of renal toxicity in patients with renal or hepatic impairment or heart failure, in patients with volume depletion, in geriatric patients, and in those receiving a diuretic, ACE inhibitor, or angiotensin II receptor antagonist.1 46 153 (See Renal Impairment under Cautions.)
FAP
Celecoxib not shown to reduce risk of GI cancer or need for prophylactic colectomy or other FAP-related surgery in patients with FAP; usual care (i.e., endoscopic surveillance, prophylactic colectomy, other FAP-related surgery) should not be altered.1
Sensitivity Reactions
Hypersensitivity Reactions
Anaphylactoid reactions (e.g., anaphylaxis, angioedema) reported.1
Immediate medical intervention and discontinuance for anaphylaxis.1
Avoid in patients with aspirin triad (aspirin sensitivity, asthma, nasal polyps); caution in patients with asthma.1
Dermatologic Reactions
Serious skin reactions (e.g., exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) reported; can occur without warning and in patients without a history of sulfonamide sensitivity.1 144 Discontinue at first appearance of rash or any other sign of hypersensitivity (blisters, fever, pruritus).1
General Precautions
Hepatic Effects
Severe reactions including jaundice, fatal fulminant hepatitis, liver necrosis, and hepatic failure (sometimes fatal) reported rarely with NSAIAs.1
Elevations of serum ALT or AST reported.1
Monitor for symptoms and/or signs suggesting liver dysfunction; monitor abnormal liver function test results.1 Discontinue if signs or symptoms of liver disease or systemic manifestations (e.g., eosinophilia, rash) occur.1
Hematologic Effects
Anemia reported rarely.1 Determine hemoglobin concentration or hematocrit in patients receiving long-term therapy if signs or symptoms of anemia occur.1
No effect on platelet counts, prothrombin time, or partial thromboplastin time; usual dosages do not affect platelet aggregation.1
Modest increases in aPTT reported in children with systemic onset juvenile rheumatoid arthritis (active systemic disease not present); risk of disseminated intravascular coagulation.1 Use with caution and monitor coagulation tests in these children.1
CYP2D6 Phenotype
Potential for increased plasma celecoxib concentrations in patients with poor metabolizer phenotype of CYP2D6; use with caution in patients with known or suspected poor metabolizer phenotype.1
Prescribing and Dispensing Precautions
Ensure accuracy of prescription; similarity in spelling of Celebrex (celecoxib), Celexa (citalopram hydrobromide), and Cerebyx (fosphenytoin sodium) may result in errors.34
Other Precautions
Not a substitute for corticosteroid therapy; not effective in the management of adrenal insufficiency.1
May mask certain signs of infection.1
Obtain CBC and chemistry profile periodically during long-term use.1
Specific Populations
Pregnancy
Category C.1 Avoid use in third trimester because of possible premature closure of the ductus arteriosus.1
Lactation
Distributed into milk in rats; not known whether distributed into milk in humans.1 Discontinue nursing or the drug.1
Pediatric Use
Safety and efficacy in children 2–17 years of age with pauciarticular course, polyarticular course, or systemic onset juvenile rheumatoid arthritis supported by evidence from an active-controlled clinical study.1 Safety and efficacy not established in children <2 years of age, those weighing <10 kg, or children with active systemic disease.1 Not studied beyond 6 months.1
Children with systemic onset juvenile rheumatoid arthritis: Risk of abnormal coagulation test results; modest prolongation of aPTT reported.1 Risk of disseminated intravascular coagulation.1 Use with caution in these children; monitor coagulation tests.1
Geriatric Use
Efficacy similar to that in younger adults.1 However, fatal adverse GI effects and acute renal failure reported more frequently in geriatric patients than younger adults.1
Hepatic Impairment
Use not recommended in patients with severe hepatic impairment.1
Reduced dosage recommended in patients with moderate hepatic impairment.1 (See Hepatic Impairment under Dosage and Administration.)
Renal Impairment
Use with caution in patients with renal disease.1 No experience in patients with advanced renal disease; use not recommended in such patients; close monitoring of renal function advised if used.1
Common Adverse Effects
Adults: Abdominal pain, diarrhea, dyspepsia, headache, nausea, sinusitis, upper respiratory tract infection.1
Children: Headache, fever, abdominal pain, cough, nasopharyngitis, nausea, arthralgia, diarrhea, vomiting.1
Interactions for Celebrex
Metabolized by CYP2C9.77
Inhibits CYP2D6; does not inhibit CYP2C9, CYP2C19, or CYP3A4.1
Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes
Potential pharmacokinetic interaction (increased plasma celecoxib concentrations) with drugs that inhibit CYP2C9.1 Caution is advised.1
Potential pharmacokinetic interaction (increased plasma concentrations of CYP2D6 substrate) with drugs metabolized by CYP2D6.1 3 6 44
Specific Drugs
Drug | Interaction | Comments |
|---|---|---|
ACE inhibitors | Reduced BP response to ACE inhibitor1 | Monitor BP1 |
Angiotensin II receptor antagonists | Reduced BP response to angiotensin II receptor antagonists153 | Monitor BP153 |
Antacids (magnesium- or aluminum-containing) | Decreased plasma concentration and AUC of celecoxib1 50 | Not considered clinically important1 50 |
Aspirin | Increased risk of GI ulceration and other complications1 33 79 No consistent evidence that low-dose aspirin mitigates the increased risk of serious cardiovascular events associated with NSAIAs1 103 133 134 139 141 | |
Diuretics (furosemide, thiazides) | Reduced natriuretic effects1 | |
Fluconazole | Increased plasma celecoxib concentrations1 | Initiate celecoxib at lowest recommended dosage1 |
Glyburide | Pharmacokinetic interaction unlikely1 | |
Ketoconazole | Pharmacokinetic interaction unlikely1 | |
Lithium | Increased plasma lithium concentrations1 | Monitor for lithium toxicity when initiating or discontinuing celecoxib1 |
Methotrexate | Pharmacokinetics of methotrexate not altered1 | |
Phenytoin | Pharmacokinetic interaction unlikely1 | |
Tolbutamide | Pharmacokinetic interaction unlikely1 | |
Warfarin | Reports of bleeding complications and increases in PT in some (mainly geriatric) patients1 56 57 | Monitor anticoagulant activity, especially when initiating or changing celecoxib therapy1 56 57 |
Celebrex Pharmacokinetics
Absorption
Bioavailability
Well absorbed following oral administration; peak plasma concentration usually attained within 3 hours in fasting individuals.1 2 23
Onset
Single doses provide pain relief within 60 minutes.1
Food
Bioavailability increased 10–20% and time to reach peak plasma concentration delayed 1–2 hours when 200-mg capsule is administered with a high-fat meal.1 2 Administration of dosages of 400 mg twice daily with food improves absorption.1
Administration as mixture in applesauce does not alter AUC, peak plasma concentration, or time to peak plasma concentration.1
Special Populations
In geriatric patients, peak plasma concentration and AUC increased by 40 and 50%, respectively.1 2
In patients with mild or moderate hepatic impairment, AUC increased by 40 or 180%, respectively.1 2
In patients with chronic renal impairment (GFR 35–60 mL/minute), AUC decreased by 40%; pharmacokinetics not studied in patients with severe renal impairment.1 2
Distribution
Extent
Not well characterized.1
Plasma Protein Binding
97% (principally albumin; α1-acid glycoprotein to a lesser extent).1 2 23
Elimination
Metabolism
Metabolized in the liver to inactive metabolites, mainly by CYP2C9.1 2 23
Elimination Route
Excreted in urine and feces principally as metabolites.1 2 23
Pediatric patients: Oral clearance increases in less-than-proportional manner with increasing weight; clearance predicted to be 40 or 24% lower in pediatric patients weighing 10 or 25 kg, respectively, than in a 70-kg adult.1
Half-life
11 hours under fasting conditions.1
Stability
Storage
Oral
Capsules
25°C (may be exposed to 15–30°C).1
Mixture of capsule contents in applesauce is stable for 6 hours when refrigerated.1
ActionsActions
Selective inhibitor of COX-2.1 2 3 4 5 7 8 10 48 52 53
Related structurally and pharmacologically to rofecoxib and valdecoxib (COX-2 inhibitors no longer commercially available in the US); differs structurally and, to some extent, pharmacologically from prototypical NSAIAs, which inhibit COX-1 and COX-2.1 2 3 4 5 8 11 41 52
Anti-inflammatory, analgesic, and antipyretic actions; no effect on platelets at usual therapeutic doses; may reduce risk of colon cancer.1 2 3 9 15 20 38 53 60 61 75 76 77
Lower risk of GI ulceration than prototypical NSAIAs.1 2 3 9 21 22 24 28 29 33 38 65 66
Advice to Patients
Importance of reading the medication guide for NSAIAs that is provided each time the drug is dispensed.1
Risk of serious cardiovascular events with long-term use.1
Risk of GI bleeding and ulceration.1
Risk of serious skin reactions.1 Risk of anaphylactoid and other sensitivity reactions.1
Risk of hepatotoxicity.1
Not a substitute for aspirin in the prevention of adverse cardiovascular events.1
Importance of notifying clinician if signs and symptoms of a cardiovascular event (chest pain, dyspnea, weakness, slurred speech) occur.1
Importance of notifying clinician if signs and symptoms of GI ulceration or bleeding, unexplained weight gain, or edema develops.1
Importance of discontinuing celecoxib and contacting clinician if rash or other signs of hypersensitivity (blisters, fever, pruritus) develop.1 Importance of seeking immediate medical attention if an anaphylactic reaction occurs.1
Importance of discontinuing therapy and contacting clinician immediately if signs and symptoms of hepatotoxicity (nausea, fatigue, lethargy, pruritus, jaundice, upper right quadrant tenderness, flu-like symptoms) occur.1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 Importance of avoiding celecoxib use in late pregnancy (third trimester).1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1
For patients with FAP, importance of continuing usual care.1
Importance of informing patients of other important precautionary information. (See Cautions.)1
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral | Capsules | 50 mg | Celebrex (with povidone) | Pfizer |
100 mg | Celebrex (with povidone) | Pfizer | ||
200 mg | Celebrex (with povidone) | Pfizer | ||
400mg | Celebrex (with povidone) | Pfizer |
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
CeleBREX 100MG Capsules (PFIZER U.S.): 30/$90.99 or 90/$249.97
CeleBREX 200MG Capsules (PFIZER U.S.): 30/$140.99 or 90/$404.97
CeleBREX 400MG Capsules (PFIZER U.S.): 30/$208.98 or 90/$601.98
Disclaimer
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions May 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
References
1. Pfizer. Celebrex (celecoxib) capsules prescribing information. New York, NY; 2006 Dec.
2. G.D. Searle & Co. Celebrex (celecoxib) formulary information. Skokie, IL; 1999 Feb 8.
3. Anon. Celecoxib for arthritis. Med Lett Drugs Ther. 1999; 41:11-2. [PubMed 9949762]
4. Gierse JK, McDonald JJ, Hauser SD et al. A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors. J Biol Chem. 1996; 271:15810-4. [PubMed 8663121]
5. Seibert K, Zhang Y, Leahy K et al. Pharmacological and biochemical demonstration of the role of cyclooxygenase 2 in inflammation and pain. Proc Natl Acad Sci USA. 1994; 91:12013-7. [PubMed 7991575]
6. Funck-Brentano C, Thomas G, Jacqz-Aigrain E et al. Polymorphism of dextromethorphan metabolism: relationships between phenotype, genotype and response to the administration of encainide in humans. J Pharmacol Exp Ther. 1992; 263:780-6. [PubMed 1432700]
7. McAdam BF, Catella-Lawson F, Mardini IA et al. Systemic biosynthesis of prostacyclin by cyclooxygenase (COX)-2: the human pharmacology of a selective inhibitor of COX-2. Proc Natl Acad Sci USA. 1999; 96:272-7. [PubMed 9874808]
8. Hawkey CJ. COX-2 inhibitors. Lancet. 1999; 353:307-14. [IDIS 418284] [PubMed 9929039]
9. Simon LS, Lanza FL, Lipsky PE et al. Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase 2 inhibitor: efficacy and safety in two placebo-controlled trials in osteoarthritis and rheumatoid arthritis, and studies of gastrointestinal and platelet effects. Arthritis Rheum. 1998; 41:1591-602. [IDIS 411265] [PubMed 9751091]
10. Lipsky PE, Isakson PC. Outcome of specific COX-2 inhibition in rheumatoid arthritis. J Rheumatol. 1997; 24(Suppl 49):9-14. [PubMed 9002004]
11. Penning TD, Talley JJ, Bertenshaw SR et al. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (SC-58635, celecoxib). J Med Chem. 1997; 40:1347-65. [PubMed 9135032]
12. Markind JE (G. D. Searle, Skokie, Ill): Personal communication; 1999 May 7.
13. G.D. Searle. Response to Wall Street Journal article regarding Celebrex. Skokie, Ill; 1999 Apr 20. Press release from website (http://www.searlehealthnet.com/pr/042099.htm).
14. Anon. Searle responds to Journal report on Celebrex side effects. Skokie, Ill; 1999 Apr 22. Press release from website (http://www.pslgroup.com:80/dg/f8f2e.htm).
15. Kawamori T, Rao CV, Seibert K et al. Chemopreventive activity of celecoxib, a specific cyclooxygenase-2 inhibitor, against colon carcinogenesis. Cancer Res. 1998; 58:409-12. [PubMed 9458081]
16. McAdam BF, Kapoor S, Catella-Lawson F et al. Selective inhibition of monocyte COX-2 vs platelet COX-1 in humans. Circulation. 1997; 96(Suppl):I-557.
17. Crofford LJ, Wilder RL, Ristimäki AP et al. Cyclooxygenase-1 and -2 expression in rheumatoid synovial tissues: effects of interleukin-1β, phorbol ester, and corticosteroids. J Clin Invest. 1994; 93:1095-101. [PubMed 8132748]
18. Lane NE. Pain management in osteoarthritis: the role of COX-2 inhibitors. J Rheumatol. 1997; 24(Suppl 49):20-4. [PubMed 9002006]
19. DeWitt DL, Bhattacharyya D, Lecomte M et al. The differential susceptibility of prostaglandin endoperoxide H synthases-1 and -2 to nonsteroidal anti-inflammatory drugs: aspirin derivatives as selective inhibitors. Med Chem Res. 1995; 5:325-43.
20. Mengle-Gaw L, Hubbard RC, Karim A et al. A study of the platelet effects of SC-58635, a novel COX-2-selective inhibitor. Arthritis Rheum. 1997; 40:S93.
21. Geis GS, Hubbard R, Callison D et al. Safety and efficacy of celecoxib, a specific COX-2 inhibitor, in patients with rheumatoid arthritis. Arthritis Rheum. 1998; 41:S364.
22. Hubbard RC, Koepp R, Yu SS et al. Pilot efficacy of SC-58635, a COX-2-selective inhibitor, in rheumatoid arthritis. Arthritis Rheum. 1997; 40:S51.
23. Karim A, Tolbert D, Burton E et al. SC-58635 (celecoxib): a highly selective inhibitor of cyclooxygenase-2, disposition kinetics in man and identification of its major CYP450 isozyme in its biotransformation. Pharm Res. 1997; 14(Suppl):S617.
24. Geis GS, Stead H, Morant S et al. Efficacy and safety of celecoxib, a specific COX-2 inhibitor, in patients with rheumatoid arthritis. Arthritis Rheum. 1998; 41:S316.
25. Felson DT, Anderson JJ, Boers M et al. American College of Rheumatology preliminary definition of improvement in rheumatoid arthritis. Arthritis Rheum. 1995; 38:727-35. [PubMed 7779114]
26. Felson DT, Anderson JJ, Boers M et al. The American College of Rheumatology preliminary core set of disease activity measures for rheumatoid arthritis clinical trials. Arthritis Rheum. 1993; 36:729-40. [PubMed 8507213]
27. Felson DT, Anderson JJ, Lange MLM et al. Should improvement in rheumatoid arthritis clinical trials be defined as fifty percent or seventy percent improvement in core set measures, rather than twenty percent? Arthritis Rheum. 1998; 41:1564-70. (IDIS 411264)
28. Hubbard RC, Geis GS, Callison DA et al. Efficacy and safety of celecoxib, a specific COX-2 inhibitor, in osteoarthritis (OA) and rheumatoid (RA). J Rheumatol. 1998; 25(Suppl 52):6. [PubMed 9458195]
29. Hubbard R, Geis GS, Woods E et al. Efficacy, tolerability, and safety of celecoxib, a specific COX-2 inhibitor, in osteoarthritis. Arthritis Rheum. 1998; 41:S196.
30. American College of Rheumatology Subcommittee on Rheumatoid Arthritis Guidelines. Guidelines for the management of rheumatoid arthritis: 2002 update. Arthritis Rheum. 2002; 46:328-46. [IDIS 476480] [PubMed 11840435]
31. Lane NE, Thompson JM. Management of osteoarthritis in the primary-care setting: an evidence-based approach to treatment. Am J Med. 1997; 103(Suppl 6A):25-30S. [IDIS 390389] [PubMed 9236482]
32. Altman RD, Hochberg MC, Moskowitz RW et al. Recommendations for the medical management of osteoarthritis of the hip and knee. Arthritis Rheum. 2000; 43:1905-15. [IDIS 453740] [PubMed 11014340]
33. Silverstein FE, Faich G, Goldstein JL et al. Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumtoid arthritis. The CLASS study: a randomized controlled trial. JAMA. 2000; 284:1247-55. [IDIS 453422] [PubMed 10979111]
34. Sharpe R. Monsanto, FDA are trying to overcome confusion over name of arthritis drug. Wall St J. 1999 Apr 15.
35. Anon. Celebrex wins “unclear” advantage from FDA: backhanded ok for GI safety. F-D-C Rep. 1999; Jan 4:33-4.
36. Lithium interactions. In: Hansten PD, Horn JR. Drug interactions analysis and management. Vancouver, WA: Applied Therapeutics, Inc; 1997:223, 327, 332, 358, 367-369, 371.
37. Smith CJ, Zhang Y, Koboldt CM et al. Pharmacological analysis of cyclooxygenase-1 in inflammation. Proc Natl Acad Sci USA. 1998; 95:13313-8. [PubMed 9789085]
38. Cryer B, Dubois A. The advent of highly selective inhibitors of cyclooxygenase—a review. Prostaglandins Lipid Mediators. 1998; 56:341-61.
39. Anderson GD, Hauser SD, McGarity KL et al. Selective inhibition of cyclooxygenase (COX)-2 reverses inflammation and expression of COX-2 and interleukin 6 in rat adjuvant arthritis. J Clin Invest. 1996; 97:2672-9. [PubMed 8647962]
40. Riendeau D, Charleson S, Cromlish W et al. Comparison of the cyclooxygenase-1 inhibitory properties of nonsteroidal anti-inflammatory drugs (NSAIDs) and selective COX-2 inhibitors, using sensitive microsomal and platelet assays. Can J Physiol Pharmacol. 1997; 75:1088-95. [PubMed 9365818]
41. Kurumbail RG, Stevens AM, Gierse JK et al. Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents. Nature. 1996; 384:644-8. [PubMed 8967954]
42. Hubbard RC, Mehlisch DR et al. SC-58635, a highly selective inhibitor of COX-2, is an effective analgesic in an acute post surgical pain model. J Invest Med. 1996; 44:293A.
43. Mehlisch DR, Hubbard RC, Isakson P et al. Analgesic efficacy and plasma levels of a highly selective inhibitor of COX-2 (SC-58635; SC) in patients with post-surgical dental pain. Clin Pharmacol Ther. 1997; 61:195.
44. Michalets EL. Update: clinically significant cytochrome P-450 drug interactions. Pharmacotherapy. 1998; 18:84-112. [IDIS 398636] [PubMed 9469685]
45. Angiotensin-converting enzyme inhibitor interactions: nonsteroidal anti-inflammatory drugs (NSAIDSs). In: Hansten PD, Horn JR. Drug interactions and updates. Vancouver, WA: Applied Therapeutics, Inc; 1993:131-2.
46. Novartis Pharmaceuticals. Diovan (valsartan) capsules prescribing information (dated 1997 Apr). In: Physicians’ desk reference. 53rd ed. Montvale, NJ: Medical Economics Company Inc; 1999:2013-5.
47. Lanza FL, Rack MF, Callison DA et al. A pilot endoscopic study of the gastroduodenal effects of SC-58635, a novel COX-2 selective inhibitor. Gastroenterology. 1997; 112:A194.
48. Simon LS. Role and regulation of cyclooxygenase-2 during inflammation. Am J Med. 1999; 106:37S-42. [IDIS 430024] [PubMed 10390126]
49. Geis GS. Update on clinical developments with celecoxib, a new specific COX-2 inhibitor: what can we expec
Propofabb
Propofabb may be available in the countries listed below.
Ingredient matches for Propofabb
Propofol
Propofol is reported as an ingredient of Propofabb in the following countries:
- Luxembourg
International Drug Name Search
Pyrazinamide
Pyrazinamide, the pyrazine analogue of nicotinamide, is an antituberculous agent. It is a white crystalline powder, stable at room temperature, and sparingly soluble in water. Pyrazinamide has the following structural formula:
C5H5N3O M.W.123.11
Each Pyrazinamide tablet for oral administration contains 500 mg of Pyrazinamide and the following inactive ingredients: dibasic calcium phosphate (dihydrate), colloidal silicon dioxide, croscarmellose sodium, microcrystalline cellulose, and stearic acid.
CLINICAL PHARMACOLOGY:
Pyrazinamide is well absorbed from the GI tract and attains peak plasma concentrations within 2 hours. Plasma concentrations generally range from 30 to 50 mcg/mL with doses of 20 to 25 mg/kg. It is widely distributed in body tissues and fluids including the liver, lungs and cerebrospinal fluid (CSF). The CSF concentration is approximately equal to concurrent steady-state plasma concentrations in patients with inflamed meninges.1 Pyrazinamide is approximately 10% bound to plasma proteins.2 The half-life (t 1/2) of Pyrazinamide is 9 to 10 hours in patients with normal renal and hepatic function. The plasma half-life may be prolonged in patients with impaired renal or hepatic function. Pyrazinamide is hydrolyzed in the liver to its major active metabolite, pyrazinoic acid. Pyrazinoic acid is hydroxylated to the main excretory product, 5-hydroxypyrazinoic acid.3
Approximately 70% of an oral dose is excreted in the urine, mainly by glomerular filtration within 24 hours.3
Pyrazinamide may be bacteriostatic or bactericidal against Mycobacterium tuberculosis depending on the concentration of the drug attained at the site of infection. The mechanism of action is unknown. In vitro and in vivo the drug is active only at a slightly acidic pH.
INDICATIONS AND USAGE:
Pyrazinamide is indicated for the initial treatment of active tuberculosis in adults and children when combined with other antituberculous agents. (The current recommendation of the CDC for drugsusceptible disease is to use a six-month regimen for initial treatment of active tuberculosis, consisting of isoniazid, rifampin and Pyrazinamide given for 2 months, followed by isoniazid and rifampin for 4 months.*4)
(Patients with drug-resistant disease should be treated with regimens individualized to their situation. Pyrazinamide frequently will be an important component of such therapy.)
(In patients with concomitant HIV infection, the physician should be aware of current recommendation of CDC. It is possible these patients may require a longer course of treatment)
It is also indicated after treatment failure with other primary drugs in any form of active tuberculosis.
Pyrazinamide should only be used in conjunction with other effective antituberculous agents.
*See recommendations of Center for Disease Control (CDC) and American Thoracic Society for complete regimen and dosage recommendations.4
CONTRAINDICATIONS:
Pyrazinamide is contraindicated in persons:
- with severe hepatic damage.
- who have shown hypersensitivity to it.
- with acute gout.
WARNINGS:
Patients started on Pyrazinamide should have baseline serum uric acid and liver function determinations. Those patients with preexisting liver disease or those at increased risk for drug related hepatitis (e.g., alcohol abusers) should be followed closely.
Pyrazinamide should be discontinued and not be resumed if signs of hepatocellular damage or hyperuricemia accompanied by an acute gouty arthritis appear.
PRECAUTIONS:
General:
Pyrazinamide inhibits renal excretion of urates, frequently resulting in hyperuricemia which is usually asymptomatic. If hyperuricemia is accompanied by acute gouty arthritis, Pyrazinamide should be discontinued.
Pyrazinamide should be used with caution in patients with a history of diabetes mellitus, as management may be more difficult.
Primary resistance of M. tuberculosis to Pyrazinamide is uncommon. In cases with known or suspected drug resistance, in vitro susceptibility tests with recent cultures of M. tuberculosis against Pyrazinamide and the usual primary drugs should be performed. There are few reliable in vitro tests for Pyrazinamide resistance. A reference laboratory capable of performing these studies must be employed.
Information for Patients:
Patients should be instructed to notify their physicians promptly if they experience any of the following: fever, loss of appetite, malaise, nausea and vomiting, darkened urine, yellowish discoloration of the skin and eyes, pain or swelling of the joints.
Compliance with the full course of therapy must be emphasized, and the importance of not missing any doses must be stressed.
Laboratory Tests:
Baseline liver function studies [especially ALT (SGPT), AST (SGOT) determinations] and uric acid levels should be determined prior to therapy. Appropriate laboratory testing should be performed at periodic intervals and if any clinical signs of symptoms occur during therapy.
Drug/Laboratory Test Interactions:
Pyrazinamide has been reported to interfere with ACETEST® and KETOSTIX® urine tests to produce a pink-brown color.5
Carcinogenesis, Mutagenesis, Impairment of Fertility:6,7,8
In lifetime bioassays in rats and mice, Pyrazinamide was administered in the diet at concentrations of up to 10,000 ppm. This resulted in estimated daily doses for the mouse of 2 g/kg, or 40 times the maximum human dose, and for the rat of 0.5 g/kg, or 10 times the maximum human dose. Pyrazinamide was not carcinogenic in rats or male mice and no conclusion was possible for female mice due to insufficient numbers of surviving control mice.
Pyrazinamide was not mutagenic in the Ames bacterial test, but induced chromosomal aberrations in human lymphocyte cell cultures.
Pregnancy:
Teratogenic Effects-Pregnancy Category C
Animal reproduction studies have not been conducted with Pyrazinamide. It is also not known whether Pyrazinamide can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Pyrazinamide should be given to a pregnant woman only if clearly needed.
Nursing Mothers:
Pyrazinamide has been found in small amounts in breast milk. Therefore, it is advised that Pyrazinamide be used with caution in nursing mothers taking into account the risk-benefit of this therapy.9
Usage in Children:
Pyrazinamide regimens employed in adults are probably equally effective in children.4,10,11 Pyrazinamide appears to be well tolerated in children.
Geriatric Use:12
Clinical studies of Pyrazinamide did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic or renal function, and of concomitant disease or other drug therapy.
It does not appear that patients with impaired renal function require a reduction in dose. It may be prudent to select doses at the low end of the dosing range, however.13
ADVERSE REACTIONS:
General:
Fever, porphyria and dysuria have rarely been reported. Gout (see PRECAUTIONS:).
Gastrointestinal:
The principal adverse effect is a hepatic reaction (see WARNINGS:). Hepatotoxicity appears to be dose related, and may appear at any time during therapy. GI disturbances including nausea, vomiting and anorexia have also been reported.
Hematologic and Lymphatic:
Thrombocytopenia and sideroblastic anemia with erythroid hyperplasia, vacuolation of erythrocytes and increased serum iron concentration have occurred rarely with this drug. Adverse effects on blood clotting mechanisms have also been rarely reported.
Other:
Mild arthralgia and myalgia have been reported frequently. Hypersensitivity reactions including rashes, urticaria, and pruritis have been reported. Fever, acne, photosensitivity, porphyria, dysuria and interstitial nephritis have been reported rarely.
OVERDOSAGE:
Overdosage experience is limited. In one case report of overdose, abnormal liver function tests developed. These spontaneously reverted to normal when the drug was stopped. Clinical monitoring and supportive therapy should be employed. Pyrazinamide is dialyzable.13
DOSAGE AND ADMINISTRATION:
Pyrazinamide should always be administered with other effective antituberculous drugs. It is administered for the initial 2 months of a 6-month or longer treatment regimen for drug-susceptible patients. Patients who are known or suspected to have drug-resistant disease should be treated with regimens individualized to their situation.
Pyrazinamide frequently will be an important component of such therapy.
Patients with concomitant HIV infection may require longer courses of therapy. Physicians treating such patients should be alert to any revised recommendations from CDC for this group of patients.
Usual dose: Pyrazinamide is administered orally, 15 to 30 mg/kg once daily. Older regimens employed 3 or 4 divided doses daily, but most current recommendations are for once a day. Three grams per day should not be exceeded. The CDC recommendations do not exceed 2 g per day when given as a daily regimen (see table).
Alternatively, a twice weekly dosing regimen (50 to 75 mg/kg twice weekly based on lean body weight) has been developed to promote patient compliance with a regimen on an outpatient basis. In studies evaluation the twice weekly regimen, doses of Pyrazinamide in excess of 3 g twice weekly have been administered. This exceeds the recommended maximum 3 g/daily dose. However, an increased incidence of adverse reactions has not been reported.
This table is taken from the CDC-American Thoracic Society joint recommendations.4
| Definition of abbreviations: PO = perorally; IM = intramuscularly. | ||
| ||
| Daily Dose* | ||
| Drug | Children | Adults |
| Isoniazid | 10 to 20 mg/kg PO or IM | 5 mg/kg PO or IM |
| Rifampin | 10 to 20 mg/kg PO | 10 mg/kg PO |
| Pyrazinamide | 15 to 30 mg/kg PO | 15 to 30 mg/kg PO |
| Streptomycin | 20 to 40 mg/kg IM | 15 mg/kg† IM |
| Ethambutol | 15 to 25 mg/kg PO | 15 to 25 mg/kg PO |
| |
| Maximal Daily Dose in Children and Adults | |
| Drug | |
| Isoniazid | 300 mg |
| Rifampin | 600 mg |
| Pyrazinamide | 2 g |
| Streptomycin | 1 g* |
| Ethambutol | 2.5 g |
| Definition of abbreviations: PO = perorally; IM = intramuscularly. | ||
| Twice Weekly Dose | ||
| Drug | Children | Adults |
| Isoniazid | 20 to 40 mg/kg Max. 900 mg | 15 mg/kg Max. 900 mg |
| Rifampin | 10 to 20 mg/kg Max. 600 mg | 10 mg/kg Max. 600 mg |
| Pyrazinamide | 50 to 70 mg/kg | 50 to 70 mg/kg |
| Streptomycin | 25 to 30 mg/kg IM | 25 to 30 mg/kg IM |
| Ethambutol | 50 mg/kg | 50 mg/kg |
HOW SUPPLIED:
Pyrazinamide Tablets USP contain Pyrazinamide 500 mg. They are supplied as white, round, scored tablets, debossed "EFF/12" on one side, in containers of 60 tablets, NDC #55806-012-02, in containers of 90 tablets, NDC #55806-012-08, in containers of 100 tablets, NDC #55806-012-03, in containers of 500 tablets, NDC #55806-012-04, and in hospital unit-dose cartons of 100 tablets (10 strips of 10 tablets per strip), NDC #55806-012-21.
Storage:
Store in a well-closed container at controlled room temperature 15°-30°C (59°-86°F).
Dispense in a well-closed container with a child resistant closure.
CAUTION: Federal law prohibits dispensing without prescription.
Marketed by:
EFFCON LABORATORIES, INC.
Marietta, GA 30065-1509
Manufactured by:
MIKART, INC.,
Atlanta, GA 30318
Rev. 8/94
Code 590A00
REFERENCES:
- Drug Information, American Hospital Formulary Service. American Society of Hospital Pharmacists. Bethesda, Md. 1991.
- USPDI, Drug Information for the Health Care Professional. United States Pharmacopeial Convention, Inc. Rockville, Md. 1991: 1 B : 2226-2227.
- Goodman-Gilman A, Rall TW, Nies AS, Taylor P. The Pharmacological Basis of Therapeutics, ed 8. New York, Pergamon Press. 1990; 1154.
- Treatment of tuberculosis and tuberculosis infection in adults and children. Am Rev Respir Dis. 1986 ; 134 : 363-368.
- Reynolds JEF, Parfitt K, Parsons AV, Sweetman SC. Martindale The Extra Pharmacopoeia, ed 29. London, The Pharmaceutical Press. 1989; 569-570.
- Bioassay of Pyrazinamide for possible carcinogenicity. National Cancer Institute Carcinogenesis Technical Report Series No. 48, 1978.
- Zerger E, Anderson B, Haworth S, Lawlor T, Mortelmans K, Speck W. Salmonella mutagenicity tests: III. Results from the testing of 255 chemicals. Environ Mutagen. 1987; 9 (Suppl 9) : 1109.
- Roman IC, Georgian L. Cytogenetic effects of some antituberculosis drugs in vitro. Mutation Research. 1977; 48: 215- 224.
- Holdiness M. Antituberculosis drugs and breast-feeding. Arch Intern Med. 1984; 144: 1888.
- Turcios N, Evans H. Preventing and managing tuberculosis in children. J Resp Dis. 1989; 10 (6) (Jun): 23.
- Starke JR. Multidrug therapy for tuberculosis in children. Pediatr Infec Dis J. 1990; 9: 785793.
- Specific requirements on content and format of labeling for human prescription drugs; proposed addition of "geriatric use" subsection in the labeling. Federal Register. 1990; 55 (212) (Nov 1): 46134-46137.
- Stamathakis G, Montes C, Trouvin JH, et al. Pyrazinamide and pyrazinoic acid pharmacokinetics in patients with chronic renal failure. Clinical Nephrology. 1988 ; 30 : 230-234.
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Revised: 08/2006MIKART, INC.
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