#trimethoprim

Common Brand Names: Bactrim, Septra

Therapeutic Class: A diaminopyrimidine/sulfonamide combination antibacterial agent

Common Injectable Dosage Forms: Injection: 16 mg/mL of trimethoprim and 80 mg/mL of sulfamethoxazole in vials and ampoules

Dosage Ranges:

Dosage of this combination is always expressed in milligrams of trimethoprim.

The usual adult IV dose for severe infections is 8-10 mg/kg daily administered in 2-4 equally divided doses every 6,8, or 12 hours. The maximum daily dose is 960 mg with duration of therapy based on severity of infection and susceptibility of organisms.

For treatment of pneumocystis pneumonia in children older than 2 months of age up to adults, the IV dosage is 15-20 mg/kg daily given in 3-4 equally divided doses every 6-8 hours. The minimum duration of therapy in AIDS patients is usually 21 days.

Dosage reductions may be necessary in patients with renal dysfunction.

Administration and Stability: The concentrate for injection (16 mg TMP/mL) must be diluted before injection with 5 mL of concentrate added to 125 mL of D5W (only recommended solution) and administered over 60-90 minutes. If fluid intake by the patient is a concern, the diluent volume may be reduced to 75 mL of D5W. Stable for 6 hours at room temperature in 125 mL diluent, 4 hours in 100 mL, and 2 hours in 75 mL diluent. pH 9.5-10.5

Pharmacology/Pharmacokinetics: This combination is usually bactericidal in nature by acting to inhibit sequential enzymes in the folic acid pathway which, in turn, prevents bacterial replication. The spectrum of antibacterial action includes many Gram-positive aerobic bacteria (including S. pneumoniae and many strains of S. aureus), Gram-negative bacteria (including most Enterobacteriaceae but not P. aeruginosa), and the protozoan Pneumocystis carinii. Following administration, the drugs distribute to most body tissues and fluids including the CSF. The drugs are both metabolized in the liver and excreted primarily via the urine. Half-life elimination is 6-17 hours, time to peak is 1-4 hours.

Drug and Lab Interactions: Sulfamethoxazole/trimethoprim may increase toxicity of methotrexate and procainamide, as well as increase levels of amiodarone, fluoxetine, glimepiride, glipizide, phenytoin, warfarin, and sertraline.

Contraindications/Precautions: Contraindicated in patients with documented megaloblastic anemia secondary to folate deficiency, known hypersensitivity to other sulfonamide-type agents, and patients with creatinine clearances of less than 15 mL/minute. Caution should be exercised in use with patients who have known renal or hepatic dysfunction. Use with caution in patients with known G6PD deficiency. Pregnancy Category C/D.

Monitoring Parameters: CBC, serum potassium, creatinine, and BUN

Adverse Effects: Reported effects include blood dyscrasias (pancytopenia, thrombocytopenia, anemia, leukopenia), hypoglycemia, diarrhea, pseudomembranous colitis, skin rash, and Stevens-Johnson syndrome. In AIDS patients, toxicity has been reported including a syndrome manifested by fever, malaise, nausea, and headache.

Brand Name: Bactrim, Septra

Generic Available

Common Dosage Forms:

Tablets, regular strength: 80 mg trimethoprim with 400 mg sulfamethoxazole

Tablets, double strength: 160 mg trimethoprim with 800 mg sulfamethoxazole

Suspension: 40 mg/5 mL trimethoprim with 200 mg/5 mL sulfamethoxazole

Injection: 80 mg/5 mL trimethoprim with 400 mg/5 mL sulfamethoxazole

FDA Indications/Dosages:

Urinary tract infections due to susceptible strains of E. coli, Klebsiella-Enterobacter, P. mirabilis, P. vulgaris, and P. morganii; shigellosis due to susceptible strains of S. flexneri or S. sonnei; and acute exacerbations of chronic bronchitis in adults: 160 mg trimethoprim/800 mg sulfamethoxazole every 12 hours for 10-14 days, or 5 days for shigellosis. For children, use 8 mg/kg trimethoprim and 40 mg/kg sulfamethoxazole/day in two divided doses every 12 hours for 10 days, or 5 days for shigellosis.

Acute otitis media in children due to susceptible strains of H. influenzae or S. pneumoniae: 8 mg/kg trimethoprim and 40 mg/kg sulfamethoxazole/day in two divided doses every 12 hours for 10 days.

Pneumocystis carinii pneumonitis (PCP): 20 mg/kg trimethoprim or 100 mg/kg sulfamethoxazole/day in equally divided doses every 6 hours for 14 days. (Children’s dose is the same.)

Prophylaxis against PCP in individuals who are immunosuppressed and considered to be at increased risk: 160 mg trimethoprim/800 mg sulfamethoxazole given orally every 24 hours. In children, 75 mg/m^2 trimethoprim (375 mg/m^2 sulfamethoxazole) twice a day for 3 days. The total dose should not exceed 320 mg trimethoprim/1600 mg sulfamethoxazole.

Treatment of traveler’s diarrhea in adults: One double strength tablet every 12 hours for 5 days.

Pharmacology/Pharmacokinetics: Trimethoprim blocks the production of tetrahydrofolic acid by inhibiting the enzyme dihydrofolate reductase. It is weakly bound to plasma proteins (44%). Sulfamethoxazole inhibits bacterial synthesis of dihydrofolic acid by competitive antagonism of para-aminobenzoic acid (PABA). It is 70% bound to plasma proteins. Steady state plasma levels of both drugs occur in 3 days. Metabolism occurs in the liver and excretion in the urine.

Drug Interactions: May decrease effects of cyclosporine. May increase the serum levels of procainamide and hydantoins. May increase the effects of anticoagulants and sulfonylureas.

Contraindications/Precautions: Contraindicated in infants less than 2 months of age, during pregnancy, in nursing mothers, in patients allergic to sulfa drugs, and in patients with megaloblastic anemia due to folate deficiency. Use with caution in patients with impaired renal or hepatic function. Pregnancy Category D.

Adverse Effects: Increased sensitivity to sunlight, Stevens-Johnson Syndrome, nausea, vomiting, DIARRHEA, anorexia, and RASH.

Colorimetric Determination of Stability Constant of Trimethoprim Cu II Complex at Different Temperatures by Continuous Variation Method

by O. V. Ikpeazu | I. E. Otuokere | K. K. Igwe "Colorimetric Determination of Stability Constant of Trimethoprim-Cu(II) Complex at Different Temperatures by Continuous Variation Method"

Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-4 | Issue-5 , August 2020,

URL: https://www.ijtsrd.com/papers/ijtsrd31849.pdf

Paper Url :https://www.ijtsrd.com/chemistry/biochemistry/31849/colorimetric-determination-of-stability-constant-of-trimethoprimcuii-complex-at-different-temperatures-by-continuous-variation-method/o-v-ikpeazu

callforpaperinternationaljournal, ugclistofjournals, bestinternationaljournal

New Post has been published on http://pharmapedia.pw/2016/11/21/septazole-suspension-tablets-forte-tablets-sulfamethoxazole-trimethoprim-antibacterial-for-urinary-tract-infections-and-acute-otitis-media/

Septazole suspension , tablets , forte tablets | sulfamethoxazole + trimethoprim - antibacterial for urinary tract infections and acute otitis media

Composition :

Active ingredients : 

Septazole tablets each tablet contains : sulfamethoxazole   400 mg  ,  trimethoprim   80 mg

Septazole fort tab each tablets contains :

sulfamethoxazole   800 mg  ,  trimethoprim   160 mg

Septazole suspension each 5 ml contains  :

sulfamethoxazole   200 mg  ,  trimethoprim   40 mg

Inactive Ingredients: SeptazoIe Tablets : Maize ,starch, P.V P 25 & Magnesoum stearate Septazole Forte Tablets : Maize Starch, P.VP 25, Explotab & Magnesium stearate Septazole suecensen : Sucrose. Carboxymethyloenulose Sodium, Veegum HV. Sorbitol solution 70% , Saccharin Sodium, Methylparaben , Propylparaben, Geranine & Anethole.

Pharmaceutical form :

Suspeosion , Tablets

Pharmacological action :

sulfamethoxazole inhibits bacterial synthesis of dihydrofolic acid by competing with para aminobenzoic acid , trimethoprim blocks the production of tetrahydrofolic acid from dihydrofolic acid by binding to and reversibly inhibiting the required enzyme , dihydrofolate reductase . thus septazole blocks two consecutive steps in the biosynthesis of nucleic acids and proteins essential to many bacteria in vitro studies have shown that bacterial resistance develops more slowly with septazole than with either trimethoprim or sulfamethoxazole alone .

Pharmacokinetics :

Septazole is rapidly absorbed following oral administration. Both sulfamethoxazole and trimethoprim exist in the blood a, unbound, protein-bound, and metabolized forms Peak blood levels for the individual components occur 1 to 4 hours after 0fltI administration. The mean serum half-lives of sulfamethoxazole and trimethoprim are 10 and 8to 10 hours. respectively Bofh tinethopnm and slfamelhoxazole distnbute to sputum. vaginal fluid, and middle ear fluid, trimethoprim also distributes to bronchial secretions and both pass the placental and are excreted in human milk excretion of septazole is primarily by the kinneys

Indications :

– urinary Tract Infections :For the treatment of urinary tract  , infections due 10 suspension strains of the following organisms Escherichia coli. klebsiella species Enterobacter species, morganella morganii, Proteus mirabills. and Proteus vulgans – Acute otitis media :For the lreatment of acute otrtil media in pediatric patlenta due 10 susceptible strams of Streptococcus pneumoniae or haemophilus influenzae – travelers diarrhea in adults : for the treatment of travelers diarrhea duo to susceptible strains of enterotoxigenic e coil                   – shigellosis : for the treatment of enteritis caused by susceptible strains of shigella flexneri and shigella sonnei when antibacterial therapy is indicated                                                                                  -pneumocystis carinii pneumonia : for the treatment of documented pneumocystis carinii pneumonia and for prophylaxis against pneumocystis carinii pneumonia in individuals who are immunosuppressed and considered to be at an increased risk of developing pneumocystis carinii pneumonia

Dosage & Administration:

1 – Urinary tract infectlona and ahlgellosis in adults and l)«liatrle patienta, and ilCute otitis media in pediatrk: patienta: Adulta : One Septarole Forte tablet or two Septazole tablets, or four teaspoonfuls (20 ml) Sepgzole ,u’pe1lsiol”l ev8fY 12 hours fOf 1010 14 days. An idenllClll daily dosage is used for 5 days in the treatment of shigellosis                                                                                    Pediatric patients : use for children under 3 years under medical supervision only Not recommended for Infanta less than two months except for treatment or prophylaxis of pneumocystis pneumonia 8 mg / kg trimethoprim and 40mg/kg sulfamethourole per 24 hours given in two divided doses every 12 hours for 10 days an identical daily dosage is used for 5 days in the treatment of shigellosis                 – pediatric patients : two months of age or older                                    – for patients with impaired renal function : when renal function is impaired areduced dosage should be employed using the follwing tab – adults and pediatric patients : 15 to 20 mg/kg trimethoprim and 75 to 100 mg/kg sulfamethoxazole per 24 hours givin in equally doses every 6 hours for 14 to 21 days – Prophylaxis: Adults: The recommended dosage for prophylaxis in adults is one septatole fort tablet daily

Contraindications:

1- patients with aknwn hypersensitivity to trimethoprim or sulfonamides 2- patients with documented megaloblastic anemia due to folate deficiency 3- Pregnant patients at term and in nursing mothers because sulfonamides pass the placenta and are excreted in the milk and may cause kernicterus 4 – Pediatric patients leas than 2 months of age

Side Effects:

The most common adverse effects are gastrointestinal disturbances (nausea. vomiting, and anorexia) and allergic skin reactions (Such as rash and unlcafia) Hematologic: Agranulocytosis , aplastic anemia, thrombocytopenia, leukopenia ,neutropenia , hemolytic anemia, megaloblastic  anemia Gastrointestinal : stomatitis  , glossitis , nausea , emesis , abdominal pain , diarrhea , anorexia                                                              Genitourinary : Renal failure , interstitial nephritis  , bun and serum creatinine evevation , toxic nephrosis with oliguria , anuria , and crystalluria Psyehlatric: Hallucmations, depression , apathy , nervousness

Drug interactions:

is elderly patients coneurrently receiving certain diuretics , ,primanly thiazides ,an increased incidenee of thrombocytopenia with purpura has been reported. ithas been reported that Seplazole may prolong the proIhlombin time 1(1 patients who are receIVIng the anticoagulant warfltfln this interaction should be kept in mind when Septarole is given to patients alleady on anticoagulant therapy. and the coagulallOfl !me should be reassessed septazole may I(Ihibrt the hepatic metaboIiIm of phenytoin SeptuoIe gr.oen at a cornrnon clinical 00SItge. lI”ICfeased Itle phenyto.’l half-life by 39% and decreased \he phenytoin metabolic clearance rate by 27%. when adnwmstenng these drugs one should be alert for possible  excessive phenytoin effect.

Pregnancy and Lactation:

septazole is contraindicated in pregnant patients at term and IrIIlUfSIIlg mothers, because ,ulfonamldes pass the placenta and are excreted in the milk and may cause kernicterus

Precautions & Warnings:

-It is not recommended for use in diabetic patients -Sulfonamides Including sulfonamrde – contalrttng products suctl as trJnelhopnm , sutfarnethoxazoie should be discontinued at the first appearance of skin rash or any sign of adverse reaction. -Cough. shortness of breath and pulmonary infiltrates are hypersensitivity reecuone of the respiratory tract that have been reported in assoeaton with sulfonamidetreatrnent, The sulfooamides should not be used for the tfeatmenl of group A beta-hemoiytic streptococcal inlelmns In 8fl esdbtishad inlection. !hey will not wadicate the Treatment with antibaclunal agents alhml the normall are 0f the colon and may permit overgrowth of ciostndia.

Package & Storage:

Packing: Carton box contains 2 or 20 or 100 strips in 10 tablets of septazole Carton box contain ,2 or 20 or 100 strips x 10 tablets of Septazole Forte Carton box contains an ember glass bottle of 100 ml (for local market) & 120 or 125 ml (for export & tenders) of Septazole suspension

Storage : Seplazole suspension Store in temperature not ellceedang 30 C alrtight containers away from light

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