Koact 1000

KOACT 1000: White colored capsule shaped film coated tablets, debossed with 'A' on one side and with a score line in between '6' and '5' on the other side. (See table.)

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Excipients/Inactive Ingredients: Cellulose Microcrystalline, Purified Water, Sodium Starch Glycolate, Silica Colloidal anhydrous, Magnesium Stearate, Opadry white, Isopropyl alcohol and Methylene chloride.

Pharmacology: Pharmacodynamics: Resistance to many antibiotics is caused by bacterial enzymes which destroy the antibiotic before it can act on the pathogen. The clavulanate in KOACT anticipates this defense mechanism by blocking the β-lactamase enzymes, thus rendering the organisms susceptible to amoxicillin's rapid bactericidal effect.
KOACT is an antibiotic agent of broad spectrum.
KOACT is bactericidal to a wide range of organisms including: Gram-positive: Aerobes: Bacillus anthracis*, Enterococcus faecalis*, Streptococcus pneumoniae, Streptococcus viridans, Staphylococcus aureus*, Staphylococci*.
Anaerobes: Clostridium species, Peptococcus species, Peptostreptococcus.
Gram-negative: Aerobes: Escherichia coli*, Haemophilus influenzae*, Klebsiella species*, Moraxella catarrhalis* (Branhamella catarrhalis), Neisseria gonorrhoeae*, Neisseria meningitidis*, Proteus mirabilis*, Proteus vulgaris*.
Anaerobes: Bacteroides species* including B. fragilis.
* Some members of these species of bacteria produce β-lactamase, rendering them insensitive to amoxicillin alone.
Pharmacokinetics: The pharmacokinetics of the two components of KOACT are closely matched. Peak serum levels of both occur about one hour after oral administration. Absorption of KOACT is optimized at the start of a meal. Both clavulanate and amoxicillin have low levels of serum binding (18% and 25%); about 70% remains free in the serum.

KOACT is an antibiotic agent with a notably broad spectrum of activity against bacteria which are sensitive to amoxicillin and non-sensitive to amoxicillin due to the β-lactamase inhibitory action of clavulanate in the formula.
KOACT oral preparations are indicated for short-term treatment of bacterial infections caused by amoxicillin resistant β-lactamase-producing strains or when amoxicillin alone is not effective, at the following sites: Upper Respiratory Tract Infections (including ENT): e.g. sinusitis, otitis media.
Lower Respiratory Tract Infections: e.g. acute exacerbations of chronic bronchitis, bronchopneumonia.
Genito-urinary Tract Infections: e.g. cystitis.
Skin and Soft Tissue Infections: e.g. cellulitis caused by E. coli, Klebsiella and Enterobacter spp.
Mixed infections caused by amoxicillin-susceptible organisms in conjunction with Co-amoxiclav-susceptible β-lactamase-producing organisms may be treated with KOACT.

Adults: The usual adult dose is one tablet of KOACT 625 every 12 hours or one tablet of KOACT 375 every 8 hours.
For more severe infections, the dose should be one tablet of KOACT 1000 every 12 hours or one tablet of KOACT 625 every 8 hours, 7-10 days continuously.
Patients with impaired renal function: Do not generally require a reduction in dose unless the impairment is severe.
Severely impaired patients with a glomerular filtration rate of <30 mL/min. should not receive the 1000 mg tablet.
Patients with a glomerular filtration rate of 10 to 30 mL/min. should receive 375 mg or 625 mg two times a day or every 12 hours, depending on the severity of the infection.
Patients with a less than 10 mL/min glomerular filtration rate should receive not more than 375 mg two times a day or every 12 hours, if higher dose is necessary, it should be under consideration of the physician.
Hemodialysis patients should receive 625 mg or 375 mg every 24 hours, depending on severity of the infection. They should receive an additional dose both during and at the end of dialysis.
Hepatically Impaired patients: Use of KOACT is not recommended unless considered essential by the physician, and hepatic function monitored at regular intervals.
Pediatric Patients: Pediatric patients weighing 40 kg or more, or age over 12 years should be dosed according to the adult recommendations.
Dosage in renal impairment: Dosage reductions are similar to that of adult recommendation.
Dosage in hepatic impairment: Use of KOACT is not recommended unless considered essential by the physician, and hepatic function monitored at regular intervals. There are, as yet, insufficient data on which to base a dosage recommendation.
Administration: To minimize the potential gastrointestinal intolerance, administer at the start of a meal. The absorption of KOACT is optimized when taken at the start of a meal.
Treatment should not be extended beyond 14 days without review.

Symptoms: Gastrointestinal symptoms and disturbance of the fluid and electrolyte balances may be evident. Amoxicillin crystalluria, in some cases leading to renal failure, has been observed.
Treatment: They may be treated symptomatically with attention to the water/electrolyte balance. KOACT can be removed from the circulation by hemodialysis.

KOACT is contraindicated in patients with a history of hypersensitivity to co-amoxiclav or to β-lactams e.g. penicillins and cephalosporins.
KOACT is contraindicated in patients with a previous history of Co-amoxiclav-associated jaundice/hepatic dysfunction.

Thai FDA mandatory warnings: Do not use in patients with known hypersensitivity to this medicine.
This medicine may cause a serious hypersensitivity reaction which can be fatal.
In case of erythema rash, irritation or edema occur, discontinue this medicine and consult a physician.
In case of rash or flu-like symptoms, discontinue this medicine and immediately consult a physician.
In case of the following occurs such as fever, rash, bullae, exfoliation of skin and other mucous membrane e.g. in the mouth, throat, nose, genitalia and conjunctivitis, discontinue this medicine and consult a physician since this may be Stevens-Johnson syndrome.

Before initiating therapy with KOACT, careful enquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins, or other allergens. Because serious and occasionally fatal hypersensitivity (anaphylactoid) reactions have been reported in patients with a history of hypersensitivity to penicillin.
This drug may cause cholestatic jaundice or rise of hepatic enzyme (cause hepatic dysfunction), which may be severe, but is usually reversible. Symptoms may not become apparent for up to 6 weeks after treatment has ceased.
Prolonged use of this drug may also occasionally result in overgrowth of non-susceptible organisms.
KOACT should be used carefully when anticoagulants are prescribed concomitantly because this drug increases the effect of warfarin in prolongation of prothrombin time.
Patients with evidence of hepatic dysfunction, KOACT should not be used in patients unless considered essential by the physician, and hepatic function should be monitored at regular intervals.
Patients with renal impairment, KOACT dosage should be adjusted according to creatinine clearance.
Patients with reduced urine output, crystalluria has been observed very rarely, predominately with parenteral therapy. During the administration of high doses of amoxicillin, it is advisable to maintain adequate fluid intake in order to reduce the possibility of amoxicillin crystalluria.
Effects on ability to drive and use machines: Adverse effects on ability to drive and operate machinery have not been observed.

Use in pregnancy: Use of this drug should be avoided in pregnancy, especially during the first trimester, unless considered essential by the physician.
Use in lactation: KOACT may be administered during the period of lactation. With the exception of the risk of sensitisation, associated with the excretion of trace quantities in breast milk.

The following convention has been used for the classification of frequency: Very common: ≥1/10; Common: ≥1/100 and ≤1/10; Uncommon: ≥1/1,000 and ≤1/100; Rare ≥1/10,000 and ≤1/1,000; Very rare: ≤1/10,000.
Infections and infestations: Common: Mucocutaneous candidiasis.
Blood and Lymphatic system disorders: Rare: Reversible leucopenia (including neutropenia) and thrombocytopenia.
Very rare: Reversible Agranulocytosis and hemolytic anemia, Prolongation of bleeding time and prothrombin time.
Immune system disorders: Very Rare: Angioneurotic oedema, anaphylaxis, serum sickness-like syndrome, hypersensitivity vasculitis.
Nervous system disorders: Rare: Dizziness, headache.
Very rare: Reversible hyperactivity and convulsions. Convulsions may occur in patients with impaired renal function or in those receiving high doses.
Gastrointestinal disorders: Adults: Very common: Diarrhea.
Common: Nausea, vomiting.
Children: Common: Diarrhea, nausea, vomiting.
Nausea is more often associated with higher oral dosages. If gastrointestinal reactions are evident, they may be reduced by taking KOACT at the start of meals.
Rare: Indigestion.
Very rare: Antibiotic-associated colitis (including pseudomembranous colitis and hemorrhagic colitis).
Superficial tooth discoloration has been reported very rarely.
Hepatobiliary disorders: Rare: A moderate rise in hepatic enzyme, AST and/or ALT.
Very rare: Hepatitis and cholestatic jaundice.
Hepatic events have been reported predominantly in males and elderly patients.
Signs and symptoms usually occur during treatment or until several weeks after treatment has ceased. These are usually reversible. Hepatic events may be severe and very rarely, deaths occurs. These have almost always occurred in patients with serious underlying disease or taking concomitant medications known to have the potential for hepatic effects.
Skin and subcutaneous tissue disorders: Rare: Erythema multiforme Skin rashes, pruritus, urticaria.
Very rare: Stevens-Johnson syndrome, toxic epidermal necrolysis, bullous exfoliative dermatitis, acute generalized exanthematous pustulosis (AGEP). If any hypersensitivity dermatitis reaction occurs, treatment should be discontinued and consult the physicians.
Renal and urinary disorders: Very rare: Interstitial nephritis, crystalluria.

Concomitant use of probenecid is not recommended. Probenecid decreases the renal tubular secretion of amoxicillin. Concomitant use with KOACT may result in increased and prolonged blood level of amoxicillin but not of clavulanate.
Concomitant use of allopurinol during treatment with amoxicillin can increase the likelihood of allergic skin reactions. There are no data on the concomitant use of Co-amoxiclav and allopurinol.
KOACT may reduce the efficacy of oral contraceptives and patients should be recommended to use other contraceptive method such as use of condom.

Store in a dry place at or below 30°C. Protect from moisture.
Shelf-life: 24 months.

Antibacterial Combinations

J01CR02 - amoxicillin and beta-lactamase inhibitor ; Belongs to the class of penicillin combinations, including beta-lactamase inhibitors. Used in the systemic treatment of infections.

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