Drugs CotrimStada forte have composition Trimethoprim and Sulfarmethoxazole, indications for Urinary tract infections, Gastrointestinal tract infections, Respiratory tract infections, Acute treatment of otitis media …
OpeCipro 500mg is indicated for severe infections Gastrointestinal tract infections, urinary tract
COMPOSITION
Each tablet contatas.
Trimethoprim 160 mg
Sulfarmethoxazole 800 mg
Excipierntsq.s 1 tablet (Maize starch, povidone K30. croscarmeflose sodium, sodium starch alveolate, magnesium stearate)
DESCRIPTION
White oval-shaped tablet, fracture line on both sides, engraved with ‘STADA’ on one side and “A12” on the other side
PHARMACODYNAMICS
Cotrim Stada forte (co-trimoxazole) is a synergistic fixed combination of sulfamethoxazole and trimethoprim (co-trimoxazole). in the proportion of 5 parts of sulfamethoxazole to 1 part of trimethoprim; both are synthetic folate-antagonist anti-infectives Co-trimoxazole acts by sequentially inhibiting enzymes of the folic acid pathway; sulfamethoxazole inhibits the formation of dihydrorolic acid from p-aminobenzoic acid and, by inhibiting dlhydrofolate reductase, trimethoprim inhibits the formation of tetrahydrofolicacid from dihydrofolicacid. By inhibiting synthesis of tetrahydrofblic add, tho metabolically active form of folic add. co- trimoxazole inhibits bacterial thymidine synthesis.
Sequential inhibltion by co-trimoxazole of two steps in the folic acid pathway appears to be responsible for the antibacterial synergism of the trimethoprim-sulfamethoxazole combination. Susceptibility of organisms to trimethoprim usually is more critical to the efficacy of co-trimoxazole than is susceptibility to sulfamethoxazole. Many organisms that are resistant to sulfamethoxazole but susceptible or only moderately susceptible to trimethoprim will show synergistic antibacterial response to co-trimoxazble.
PHARMACOKINETICS
CotrimStada forte ( Co-trimoxazole ) is rapidly and well absorbed from the Gl tract. Peak serum concentrations of 1 – 2 mcg/ml of trimethopnrn and 40-60 mcg/ml of unbound sulfamethoxazole are reached 1-4 hours after a single oral dose of co-trimoxazole containing 160 mg of trimethoprim and 800 mg of sulfamethoxazole.
CotrimStada forte ( Co-trimoxazole ) is widely distributed into body tissues and fluids, induding sputum, aqueous humor, middle ear fluid, prostatic fluid, vaginal fluid, bile, and CSF; trimethoprim also distributes into bronchial secretions. Trimethoprim has a larger volume of distribution than does sulfamethoxazole. Trimethoprim is approximately 44% and sulfamethoxazole is approximately 70% bound to plasma proteins. Co-trimoxazole readily crosses the placenta, is distributed into milk.
CotrimStada forte ( Co-trimoxazole ) is metabolized In the liver. Trimethoprim and sulfamethoxazole have serum half-lives of approximately 6-11 and 10-13 hours, respectively, in adults with normal renal function. Approximately 50 – 60% of a trimethoprim and 45 – 70% of a sulfamethoxazole oral dose are excreted in urine within 24 hours. Approximately 80% of the amount of trimethoprim and 20% of the amount of sulfamethoxazole recovered in urine are unchanged drug. Only small amounts of trimethoprim are excreted in feces via biliary elimination,
INDICATIONS
– Urinary tract infections:
+ Acute uncomplicated urinary tract infections.
+ Chronic or recurrent urinary tract infections.
+ Prostatitis.
– Respiratory tract infections: Treatment of acute exacerbations of chronic bronchitis.
– Gastrointestinal tract infections:
+ Shigella infections,
+ Travelers’ diarrhea.
– Acute treatment of otitis media.
– Treatment of cholera when tetracyclines are contraindicated or when the infection is caused by tetracycline-resistant Vibrio choierae.
– Treatment of Pneumocystisjiroveci (formerly Pneumocystis cerinil) pneumonia.
– Prophylaxis of Toxoplasmosis, treatment of Nocardiosis.
DOSAGE AND ADMINISTRATION
CotrimStada forte is administered orally with some food or drink to minimize the possibility of Gl disturbances,
Adults
– Urinary tract infections:
– Acute uncomplicated urinaiy tract infections: 1 tablet every 12 hours for 10 days or 2 tablets as a single dose for 3 – 7 days.
– Chronic or recurrent urinary tract infections (UTIs): 1 tablet every 12 hours for 10 -14 days.
– Prostatitis: 1 tablet every 12 hours for 3 – 6 months.
– Respiratory tract infections:
+ Treatment of acute exacerbations of chronic bronchitis caused by susceptible strains of Streptococcus pneumonia or Haemophilus influenzae: 1 tablet every 12 hours for 10 -14 days. + Pharyngitis caused by S. pyogenes; Co-trimoxazole should not be used.
– Gastrointestinal tract infections:
– Shigella infections caused by S. flexnerior S. sonnei: 1 tablet every 12 hours for 5 days.
+ Travellers’diarrhea caused by enterotoxigenic E. coll: 1 tablet every 12 hours for 3-5 days.
– Acute treatment of otitis media: 1 tablet every 12 hours for 10 days.
– Cholera: 1 tablet twice daily for 3 days, in conjunction with fluid and electrolyte replacement.
– Pneumocystis carinii pneumonia (PCP):
– Treatment: 120 mg/kg (20 mg sulfamethoxazole plus 100 mg trimethoprim) daily given in 2 – 4 divided doses for 14 – 21 days.
– For both primary and secondary prevention of Pneumocystis carinii pneumonia in HIV- infected adults and adolescents: 1 tablet once daily 3 consecutive days.
– Prophylaxis of Toxoplasmosis, treatment of Nocardiosis: 1 tablet daily for 14-21 days.
Children
8 mg/kg of trimethoprim plus 40 mg/kg of sulfamethoxazole given in 2 divided doses every 12 hours
Patients with renal Impairment
The following recommendations for adults and children over 12 years of aoe are based on creatinine clearance (CC):
+ CC above 30 ml/minute: The standard dose.
+ CC 15 to 30 ml/minute: Half the standard dose.
+ CC below 15 ml/minute: Not recommended.
CONTRAINDICATIONS
Patients with known hypersensitivity to sulfamethoxazole or trimethopnrn or any components of the drug.
Patients with marked hepatic damage.
Patients with severe renal impairment when renal function status cannot be monitored or creatinine clearances less than 15 ml/minute
Patients with documented megaloblastic anemia secondary to folate deficiency.
Pregnancy and lactation.
Infants younger than 2 months of age
PRECAUTIONS
– CotrimStada forte ( Co-trimoxazole ) should be used with caution in patients with impaired renal function, possible Mate deficiency (e g.. genatric individuals, chronic alcoholics, patients anticonvulsants, malnourished patients, those with malabsorption syndrome) with severe allergy or bronchial asthma, or with glucose-6-phosphate-dehydrogenase deficiency
– Patients receiving co-trimoxazole should be cautioned to maintain adequate fluid intake to prevent crystalluria and stone formation.
– Regular blood counts and urinalyses and renal-function tests should be earned out in patients receiving prolonged treatment with co-trimoxazoie
– Elderly patients may be more susceptible to adverse effects.
DRUG INTERACTIONS
Warfarin: Co-trimoxazole may prolong the prothrombin time (PTj of patients receiving concomitant warfarin by inhibiting metabolic clearance of warfann.
Phenytoin: Co-trimoxazole inhibits the metabolism of phenytoin
Methotrexate- Since sulfonamides can displace methotrexate from plasma protein-binding sites resulting in increased free methotrexate concentrations
Cyclosporine: Marked but reversible nephrotoxicity has boon reported m renal transplant recipients receiving co-tnmoxazble together with cydosponne
Digoxin: Increases in serum digoxin concentrations can occur in patients receiving co- trimoxazole; this interaction is more likely to occur in geriatoc patients
Indomelhactn: Increases in plasma sulfamethoxazole concentration may occur in patients receiving indomethadn.
Pyrimethamine: Megaloblastic anemia has been reported «n patients receiving and pyrimethamine dosages exceeding 25 mg weekly (for malana prophylaxis)
Antidepressant: Co-trlmoxazole may decrease tho efficacy of tho antidepressant of trtcydic antidepressants.
Amantadine: Toxic delirium has been reported when administration of eo-tnmoxazoie and amantadine.
PREGNANCY AND LACTATION
Pregnancy
Because co-trimoxazole crosses the placenta and may interfere with folic aod metabolism, toe drug should be used during pregnancy only when the potential benefits justify tho possible risks to tho fetus. Because sulfonamides may cause kemicterus in neonates, use of co-tnmoxazoie In pregnant women is contraindicated.
Lactation
CotrimStada forte ( Co-trimoxazole ) is distributed into milk. Because sulfonamides may cause kermclerus in intents younger than 2 months of age, a decision should be made whether to discontinue nursing or co- trimoxazole or to use an alternative drug, taking into account toe importance of o-tnmoxazote to the woman.
ADVERSE REACTIONS
Common: Nausea, vomiting, anorexia and diarrhea
– Hypersensitivity reactions:
+ Common: Fever, reactions Involving the skin may indude rashes, pruritus. photosensitivity reactions, exfoliative dermatitis and erythema.
+ Severe: Potentially fatal, skin reactions including toxic epidermal necroiysrs and the Stevens-Johnson syndrome.
Other: Dermatitis, systemic lupus erythematosus, particularly exacerbation of pre-existing disease.
– Nephrotoxic reactions- Interstitial nephritis and tubular necrosis Lumbar pain naematuna, oliguria, anuria may also occur.
– Blood disorders: Agranulocytosis, aplastic anaemia, thrombocytopenia eucopenia. hypoprothrombinaemia and eosinophilia.
– Disturbancesofliverenzymevaluesand cholestatic jaundice,
– Rarely: Cyanosis due to methaemoglobmaemia, acute haemolytic anaemia
OVERDOSAGE
Symptoms
Nausea, vomiting, diarrhea, mental depression, confusion, facta! swelling, headache bone marrow depression, and slight elevations of serum aminotransferases (transaminases)
Treatment
In acute overdosage with oral co-trimoxazole, the stomach should be emptied mmed«aie:v by inducing emesis or by lavage. Supportive and symptomatic treatment snovc be -aieteta Patients should be monitored with blood counts and other appropriate laboratory studies e.g serum electrolyte concentrations). Hemodialysis may remove only moderate amounts of tho drug; peritoneal dialysis is not effective in enhancing tho elimination of co-tnmexazeie
STORAGE : Store in a well-closed container, in a dry place Do not store above 300 C
SHELF-LIFE : 60 months from the date of manufactunng.
PACKAGING:
Blisterof 10 tablets Box of 2blisters.
Blister of 10 tablets Box of 10 bisters
Bottle of 100 tablets. Box of 1 bottle
SPECIFICATION: Manufacturer’s specification.
