Ampiral^® (Ampicillin)

Description

Ampiral^® is a semisynthetic antibiotic, with a broad spectrum of bactericidal activity.

Clinical pharmacology

Ampiral^® is similar to Amoxicillin in its bactericidal action against susceptible organisms during the stage of active multiplication. It acts through the inhibition of biosynthesis of cell wall mucopeptide. Ampiral^® has been shown to be active against most strains of the following microorganisms.

Antibacterial activity

Aerobic Gram-Positive Microorganisms:

Enterococcus faecalis Staphylococcus spp. * ((beta)-lactamase-negative strains only) ,Streptococci,Streptococcus pneumoniae Streptococcus spp. ((alpha) - and (beta)-hemolytic strains only) *, Bacillus anthracis, Listeria monocytogenes

Aerobic Gram-Negative Microorganisms:

Escherichia coli ((beta)-lactamase-negative strains only) Haemophilus influenzae ((beta)-lactamase-negative strains only) Neisseria gonorrhoeae, Neisseria meningitides, Salmonella sp. Shigella sp., Proteus mirabilis

Anaerobic

Clostridium sp., peptococcus sp.

Pharmacokinetics

Oral absorption  rapidly

Presystemic metabolism ----

Plasma half – life range 61.3 min

Volume of distribution 0.291.kg^-1

Plasma protein binding ~ 20%

Indication

1- Genitourinary tract infections

2- Respiratory tract infections

3- GI tract infections

4- Meningitis

Contraindication

Ampiral^® is contraindicated for patients known to have hypersensitivity to any of the penicillins.

Precaution

· The possibility of superinfections with mycotic or bacterial pathogens should be kept in mind during therapy. If superinfections occur, Ampicillin should be discontinued and appropriate therapy instituted.

· Prescribing Ampiral ^Òin the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.

· Ampiral^® should only be used to treat bacterial infections. They don’t treat viral infections (e.g. the common cold).

· As with any potent drug, periodic assessment of renal, hepatic, and hematopoietic function should be made during prolonged therapy.

Pregnancy

Pregnancy category B.

Studies in animals given doses several times the human dose have revealed no evidence of adverse effects in the fetus

Breast feeding

Ampiral^® is secreted in human milk. Caution should be exercised when Ampiral^® is administered to a nursing mother.

Dosage

Adults and children weight over 20 kg

· GI AND GU infections- for GU or GI tract infections other than gonorrhea in men and women , the usual dose is 500 mg 4 times a day in equally spaced doses; severe or chronic infections may required larger doses.

· Gonorrhea- For the treatment of gonorrhea in both men and women, a single oral dose of 3.5 grams of Ampicillin administered simultaneously with 1 gram of Probenecid is recommended. Physicians are cautioned to use no less than the above recommended dosage for the treatment of gonorrhea.

Follow up cultures should be obtained from the original sites of infection 7 to 14 days after therapy.

Respiratory tract infections- the usual dose is 250 mg 4 times a day in equally spaced doses

Usual adult prescribing limits:

4 grams a day

Usual pediatric dose

· Antibacterial-

Infants and children up to 20 kg of body weight. A product of suitable strength is not available for infants and children up to 20 kg of body weight

Patient consultation

· Consult with your physician if you have sensitivity to Penicillin, Cephalosporins , or any other medications

· Tell your doctor if you have allergies, asthma, fever, hives, severe diarrhea, shortness of breath, wheezing ,sore throat, nausea, vomiting , unusual bleeding or

· If you missed a dose, take it as soon as possible, don't take if it is almost time for next dose, don’t double dose.

· Continue medicine for full time of treatment.

· Check with your physician if condition does not improve or worsens.

Warning

Before initiating therapy with Ampiral^®, careful inquiry should be made concerning previous

· hypersensitivity reactions to penicillins, cephalosporins, or other allergens. If an allergic reaction occurs, Ampiral^® should be discontinued and appropriate therapy instituted.

· Pseudomembranous colitis has been reported with nearly all antibacterial agents, including Ampicillin, and may range in severity from mild to life threatening. It is important to consider this diagnosis in patients who present with diarrhea subsequent to the administration of antibacterial agents.

Interaction

· Concurrent use Allopurinol with Ampiral^® may significantly increase the possibility of skin rash, especially in hyperuricemic patients.

· Probenecid decreases the renal tubular secretion of Ampiral^®. Concurrent use of Ampicillin and Probenecid may result in increased and prolonged blood levels of Ampicillin.

· Chloramphenicol, macrolides, sulfonamides, and tetracyclines may interfere with the bactericidal effects of penicillin in the treatment of meningitis or in other situations in which a rapid bactericidal effect is necessary.

· Ampiral^®, reduced oral contraceptive effectiveness in women taking Ampicillin

· Concurrent use Methotrexate with Ampiral^® has resulted in decreased clearance of Methotrexate and in Methotrexate toxicity

· Ampiral may reduce the bioavailability Atenolol. Case reports indicated that beta blockers may potentiate anaphylactic reactions of penicillin.

· Laboratory value alteration

High urine concentrations of Ampicillin may result in false-positive reactions when testing for the presence of glucose in urine using clinitest®, benedict's solution or fehling's solution. Since this effect may also occur with amoxicillin, it is recommended that glucose tests based on enzymatic glucose oxidase reactions (such as clinistix®) be used.

· Following administration of Ampicillin to pregnant women, a transient decrease in plasma concentration of total conjugated estriol, estriol-glucuronide, conjugated estrone, and estradiol has been noted.

Adverse reactions

Those indicating need for medical attention

Incidence less frequent

Allergic reactions, specifically anaphylaxis (fast or irregular breathing; puffiness or swelling around face; shortness of breath; sudden, severe decrease in blood pressure); serum sickness-like reactions (skin rash; joint pain; fever), skin rash, hives, or itching,

Incidence rare

Clostridium difficile colitis(severe abdominal or stomach cramps and pain ; abdominal tenderness; watery and severe diarrhea, which may also be bloody; fever), hepatotoxicity (fever, nausea, and vomiting, yellow eyes or skin) ,interstitial nephritis(fever, possibly deceased urine output; skin rash);leucopenia or neutropenia( sore throat and fever ); mental disturbances ( anxiety, confusion, agitation or combativeness, depression, seizures, hallucinations, expressed fear of impending death), seizures

Those indicating need for medical attention only if they continue or are bothersome

Incidence more frequent

Gastrointestinal reactions (mild diarrhea, nausea or vomiting), headache, oral candidiasis ( sore mouth or tongue, white patches in mouth and / or on tongue), vaginal candidiasis ( vaginal itching and discharge)

Overdose

Specific treatment- Hemodialysis may aid in the removal of penicillins from the blood.

Supportive care- Since there is no specific antidote; treatment of penicillin overdose should be symptomatic and supportive. Patients in whom intentional overdose is known or suspected should be referred for psychiatric consultation.

Storage and stability condition

· Store at room temperature.

· After constitution, discard unused portion after 7 days if kept at room temperature or after 14 days if refrigerated.

· Keep bottles tightly closed.

· Keep out of the reach of children.

Packaging

Each bottele contains 250 or 125 mg / 5 ml of Ampicillin as the trihydrate when reconstituted.