Amopidine

Uses

Amoxicillin is used for the treatment of the following bacterial infections when caused by susceptible organisms:

• Respiratory tract, ENT infections: Acute and chronic bronchitis, pneumonia, otitis media, sinusitis, tonsillitis, pharyngitis & laryngitis, lobar & bronchopneumonia, chronic bronchial sepsis.
• Urinary tract infections: Pyelonephritis, cystitis and urethritis.
• Obstetric & gynaecological infections: Bacteriuria in pregnancy, septic abortion, intra-abdominal sepsis and puerperal sepsis.
• Gastro-intestinal infections: Typhoid and paratyphoid.
• Skin & soft tissue infections: Cellulitis, infected wounds and abscesses.
• Generalized infections: Septicemia, bacterial endocarditis, meningitis, peritonitis and osteomyelitis.
• Venereal infections: Gonorrhea and syphilis. Amoxicillin may also be used as prophylactic cover for patients at risk of developing endocarditis when undergoing dental surgery.

Sulbactam is an beta-lactamase inhibitor antibiotic combined with other antibiotics to treat a variety of susceptible bacterial infections.

Sulbactam is currently available in combination products with ampicillin. Within this formulation it is indicated for the treatment of infections due to susceptible strains of the designated microorganisms in the conditions listed below. Skin and Skin Structure Infections caused by beta-lactamase producing strains of Staphylococcus aureus, Escherichia coli, Klebsiella spp. (including K. pneumoniae), Proteus mirabilis, Bacteroides fragilis, Enterobacter spp., and Acinetobacter calcoaceticus. Intra-Abdominal Infections caused by beta-lactamase producing strains of Escherichia coli, Klebsiella spp. (including K. pneumoniae), Bacteroides spp. (including B. fragilis), and Enterobacter spp. Gynecological Infections caused by beta-lactamase producing strains of Escherichia coli, and Bacteroides spp. (including B. fragilis).

Amopidine is also used to associated treatment for these conditions: Acute Bacterial Sinusitis (ABS), Acute Otitis Media, Acute Otitis Media (AOM), Bacterial Infections, Community Acquired Pneumonia (CAP), Duodenal ulcer caused by helicobacter pylori, Genitourinary infections, Helicobacter Pylori Infection, Lower Respiratory Tract Infection (LRTI), Peptic Ulcer With H. Pylori Infection, Sinusitis, Skin and Subcutaneous Tissue Bacterial Infections, Urinary Tract Infection, Acute, uncomplicated Gonorrhea, Ear, nose, and throat infectionsAnimal bite, Bacterial Infections, Bacterial Infections caused by Beta lactamase producing bacteria, Bacterial Sinusitis, Bites, Human, Catheter Related Infections, Community Acquired Pneumonia (CAP), Gynaecological infection, Infective Endocarditis, Intra-Abdominal Infections, Nosocomial Pneumonia, Postoperative Infections, Postoperative Wound Infection, Skin and Subcutaneous Tissue Bacterial Infections, Complicated Bacterial Infections caused by Beta lactamase producing bacteria, Moderate Bacterial Infections, Severe Bacterial Infections

How Amopidine works

Amoxicillin competitively inhibits penicillin-binding protein 1 and other high molecular weight penicillin binding proteins. Penicillin bind proteins are responsible for glycosyltransferase and transpeptidase reactions that lead to cross-linking of D-alanine and D-aspartic acid in bacterial cell walls. Without the action of penicillin binding proteins, bacteria upregulate autolytic enzymes and are unable to build and repair the cell wall, leading to bacteriocidal action.

Sulbactam is an irreversible inhibitor of β-lactamase; by binding and inhibiting β-lactamase produced by bacterial cells, sulbactam is thereby able to prevent it from reducing antibiotic activity. Although sulbactam alone possesses little useful antibacterial activity, except against the Neisseriaceae, whole organism studies have shown that sulbactam restores ampicillin activity against beta-lactamase producing strains. In particular, sulbactam has good inhibitory activity against the clinically important plasmid mediated beta-lactamases most frequently responsible for transferred drug resistance. The presence of sulbactam in formulations with ampicillin effectively extends the antibacterial spectrum of ampicillin to include many bacteria normally resistant to it and to other beta-lactam antibacterials. Thus, products with ampicillin + sulbactam possess the properties of a broad-spectrum antibacterial and a beta-lactamase inhibitor.

Dosage

Amopidine dosage

Ear/Nose/ThroatInfection (Mild to Moderate):

• Adult:500 mg every 12 hours or 250 mg every 8 hours
• Children:25 mg/kg/day in divided doses every 12 hours or 20 mg/kg/day in divided doses every 8 hours

Ear/Nose/ThroatInfection (Severe):

• Adult: 875 mg every 12 hours or 500 mg every 8 hours
• Children: 45 mg/kg/day in divided doses every 12 hours or 40 mg/kg/day in divided doses every 8 hours

Lower respiratory tractInfection (Mild/ Moderate/Severe):

• Adult: 875 mg every 12 hours or 500 mg every 8 hours
• Children: 45 mg/kg/day in divided doses every 12 hours or 40 mg/kg/day in divided doses every 8 hours

Skin/skin structureInfection (Mild/Moderate):

• Adult: 500 mg every 12 hours or 250 mg every 8 hours
• Children: 25 mg/kg/day in divided doses every 12 hours or 20 mg/kg/day in divided doses every 8 hours

Skin/skin structureInfection (Severe):

• Adult: 875 mg every 12 hours or 500 mg every 8 hours
• Children: 45 mg/kg/day in divided doses every 12 hours or 40 mg/kg/day in divided doses every 8 hours

Genitourinary tractInfection (Mild/ Moderate):

• Adult: 500 mg every 12 hours or 250 mg every 8 hours
• Children: 25 mg/kg/day in divided doses every 12 hours or 20 mg/kg/day in divided doses every 8 hours

Genitourinary tractInfection (Severe):

• Adult: 875 mg every 12 hours or 500 mg every 8 hours
• Children: 45 mg/kg/day in divided doses every 12 hours or 40 mg/kg/day in divided doses every 8 hours

Gonorrhea, Acute, uncomplicated ano-genital, and urethral infections in males and females:

• Adult: 3 g as single oral dose
• Prepubertal children: 50 mg/Kg/Amoxycillin, combined with 25 mg/kg Probenecid as a single dose. Since Probenecid is contraindicated in children under 2 years, do not use this regimen in these cases.

Suspension: Shake the bottle well before adding water. Then add 12 tea spoonful (60 ml) of boiled and cooled water to the bottle and shake well to make 100 ml suspension.

Amoxycillin 500 mg Injection:

• Intramuscular : Add 2.5 ml water for injection to Amoxycillin 500 mg injection vial.
• Intravenous : Dissolve Amoxycillin 500 mg injection in 10 ml water for injection.

Side Effects

Side effects are mild, rare and infrequent. As with other penicillins, it may induce diarrhea, indigestion or skin rashes that usually stop during treatment and rarely calls for discontinuation of therapy.

Toxicity

Patients experiencing an overdose may present with hematuria, oliguria, abdominal pain, acute renal failure, vomiting, diarrhea, rash, hyperactivity, and drowsiness. Treat overdose with symptomatic and supportive treatment, which may include emesis or hemodialysis.

Precaution

In renal impairment, the excretion of antibiotic will be delayed and depending on the degree of impairment it may be necessary to reduce the total daily dose.

Interaction

The simultaneous use of Amoxicillin and an oral contraceptive might cause breakthrough bleeding or pregnancy on rare occasions. Concurrent administration of probenecid delays the excretion of Amoxicillin.

Volume of Distribution

The central volume of distribution of amoxicillin is 27.7L.

Penetration of both ampicillin and sulbactam into cerebrospinal fluid in the presence of inflamed meninges has been demonstrated after IV administration.

Elimination Route

Amoxicillin is approximately 60% bioavailable. A 250mg dose of oral amoxicillin reaches a C_max 3.93±1.13mg/L with a T_max 1.31±0.33h and an AUC of 27.29±4.72mg*h/L. A 875mg dose of oral amoxicillin reaches a C_max 11.21±3.42mg/L with a T_max 1.52±0.40h and an AUC of 55.04±12.68mg*h/L.

Peak serum concentrations are reached almost immediately following a 15-minute intravenous infusion of sulbactam + ampicillin. Mean peak serum levels for sulbactam range from 48 to 88 mcg/mL following intravenous administration of 2000 mg of ampicillin plus 1000 mg sulbactam. After an intramuscular injection of 1000 mg ampicillin plus 500 mg sulbactam, peak sulbactam serum levels ranging from 6 to 24 mcg/mL are attained.

Half Life

The half life of amoxicillin is 61.3 minutes.

~1 hr

Clearance

The mean clearance of amoxicillin is 21.3L/h.

Elimination Route

125mg to 1g doses of amoxicillin are 70-78% eliminated in the urine after 6 hours.

Approximately 75 to 85% of both ampicillin and sulbactam are excreted unchanged in the urine during the first 8 hours after administration.

Pregnancy & Breastfeeding use

Because of its lack of teratogenicity, Amoxicillin can beused safely throughout pregnancy at the normal adult dose. The small amount of Amoxicillin secreted in maternal milk rarely causes problem in the infant. It can therefore be used safely during lactation in most instances.

Contraindication

Amoxicillin is contraindicated for patients hypersensitive to penicillin, infectious mononucleosis, neonatal period or babies born of mothers hypersensitive to penicillin

Acute Overdose

If encountered, gastro-intestinal symptoms and disturbance of the fluid and electrolyte balance may be evident. They may be treated symptomatically and supportive with attention to the water/ electrolyte balance. In the absence of an adequate fluid intake and urinary output, crystalluria is a possibility and the antibiotic may be removed from the circulation by haemodialysis. Oral administration can cause gastro intestinal symptoms such as transient diarrhoea, nausea and colic which are dose related and a result of local irritation not toxicity.

Storage Condition

Store in a cool & dry place protected from light. Amoxicillin suspension and drops should be freshly prepared, stored in a cool dry place preferably in a refrigerator. Reconstituted suspension and drops should be used within 5 days if kept at room temperature or within 7 days if kept in a refrigerator.

Innovators Monograph

You find simplified version here Amopidine