Widecillin

Amoxicillin, or with trihydrate.

Each cap, dry syrup and vial contains amoxicillin as amoxicillin trihydrate.
Each sachet contains amoxicillin as base.
Amoxicillin trihydrate is (6-R)-6-[α-D-(4-hydroxylphenyl)glycylamino]penicillin trihydrate.

Pharmacology: Widecillin is a new derivative of 6-aminopenicillanic acid. It is a bactericidal antibiotic which is effective against the same range of organisms as ampicillin and has a similar mode of action.
Microbiology: Antibacterial Activity: Widecillin shows antibacterial activity against gram-positive and gram-negative bacteria. The MICs of Widecillin against the major infectious microorganisms are shown in Table 1.


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Pharmacokinetics: Widecillin is well absorbed from the gastrointestinal tract and is absorbed more rapidly and completely than ampicillin independently of the presence of food in the alimentary canal. The concentration of Widecillin in the blood is twice higher than the same dose of ampicillin.
Absorption and Excretion: In normal adults, preprandial oral administration of 125 or 250 mg (potency) of Widecillin produces a mean peak blood concentration of 2.6 or 5.3 mcg/mL, respectively after 2 hrs. This decreases gradually thereafter and is 0.15 or 0.3 mcg/mL after 6 hrs.
The urinary-recovery rate within 6 hrs after administration is 54% or 60.2%, respectively. In normal adults, postprandial oral administration of 500 mg (potency) of amoxicillin produces a mean peak blood concentration of 7.4 mcg/mL after 3 hrs. This level is the same as the 7.6 mcg/mL attained following preprandial dosing.
Tissue Concentration: Oral administration of 100 mg (potency) amoxicillin to rats produces the following tissue concentrations after 1 hr: 64.2 mcg/g in the kidney, 62.6 mcg/g in the liver, 15.9 mcg/mL in the blood, 10.7 mcg/g in SC soft tissue, 8.1 mcg/g in the lung and 7 mcg/g in the spleen.
Toxicology: LD₅₀ (mg/kg): See Table 2.


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Treatment of the following infections due to amoxicillin-susceptible strains of Escherichia coli, Proteus sp (especially Proteus mirabilis), Haemophilus influenzae, Neisseria gonorrhoeae, Streptococcus haemolyticus, Enterococcus, Streptococcus pneumoniae, Staphylococcus sp and Treponema pallidum, Salmonella sp: Bacterial endocarditis. Folliculitis, pyoderma, impetigo, furuncle, carbuncle, acne, abscess, phlegmon, atheroma, felon, decubitus. Mastitis, lymphadenitis, osteomyelitis, periostitis. Tonsillitis, pharyngitis, bronchitis, pneumonia, cholangitis, cholecystitis, acute pancreatitis. Pyelonephritis, cystitis, urethritis, prostatitis, epididymitis, adnexitis, intrauterine infection, parametritis, pelveoperitonitis, gonorrhoea, syphilis. Scarlet fever, typhoid, paratyphoid. Blepharitis, dacryocystitis, stye. Otofuruncle, nose furuncle, otitis media. Alveolar pyorrhea, acute jaw inflammation, maxillary paradentitis, pericoronitis, alveolar ostitis. Secondary infections after wounds, postoperative infections.

Adults: 250-500 mg (potency) 3-4 times daily.
Children: 20-40 mg (potency)/kg/day in 3-4 equally divided doses.
The dosage may be adjusted according to the patient's age and the severity of the infection.
Typhoid and Paratyphoid: Adults: 4 g (potency) daily in divided doses for 14-21 days.
Children: 100 mg (potency)/kg/day in divided doses for 14-21 days.
Administration: Widecillin cap/dry syrup/sachet may be taken with meals for better absorption and to reduce gastrointestinal discomfort.

Known hypersensitivity to penicillin. Infectious mononucleosis.

It is necessary that the patient's history be taken to predict adverse reactions eg, shock symptoms.
Widecillin should not be used in patients suffering from shock symptoms due to previous administration of amoxicillin for infectious mononucleosis.
Widecillin should be given under close clinical observation to: Patients who have a past history of hypersensitivity to penicillins or cephems (cephalosporins and cephamycins).
Patients who themselves, or whose parents or siblings, have a constitution susceptible to allergic reactions eg, bronchial asthma, eruption and urticaria.
Patients with severely impaired renal function. Since a high blood concentration is maintained, Widecillin should be administered at sufficient intervals.
Superinfections, especially in the gastrointestinal tract, have been noted, particularly when large doses were given or therapy was prolonged.

Shock: Rarely, shock symptoms may occur, so sufficient observation is needed. When such symptoms as discomfort, a strange feeling in the oral cavity, wheeze, vertigo, defecation, tinnitus, etc occur, administration should be discontinued.
Hypersensitivity: If hypersensitivity symptoms eg, fever, eruption and urticaria appear, administration should be stopped.
Blood: Rarely, eosinophilia, granulocytopenia and anemia may develop.
Liver: Rarely, a rise in SGOT may develop.
Digestive Tract: Rarely, pseudomembranous colitis eg, severe colitis accompanied by fever, abdominal pain, leukocytosis and violent diarrhea develops. When such symptoms as abdominal pain and frequent diarrhea occur, administration should be discontinued and suitable countermeasures be taken. Occasionally, diarrhea, nausea and anorexia develops.
Microbial Substitution: Rarely, stomatitis and colitis according to microbial substitution develops because of Candida sp and nonsensitive Klebsiella sp. When such symptoms occur, administration should be discontinued and suitable countermeasures should be taken.
Avitaminosis: Rarely, diseases of vitamin K (prothrombinopenia, hemorrhagic tendency, etc) and of vitamin B (glossitis, stomatitis, anorexia, neuritis, etc) may occur. These are likely to occur in the case of administration to patients who are aged, emaciated or unable to ingest sufficient amounts of food.

Allopurinol increases incidence of skin rashes. Reduces effectiveness of oral contraceptives. Probenecid retards renal excretion.

Store at a temperature not exceeding 30°C in airtight containers.

Penicillins

J01CA04 - amoxicillin ; Belongs to the class of penicillins with extended spectrum. Used in the systemic treatment of infections.

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