Ampicillin + Probenecid Pharmacology
Ampicillin + Probenecid
1.Gonorrhoea
2.Neurosyphilis infections
Ampicillin 250 mg + Probenecid 250 mg twice daily or
Ampicillin 500 mg + Probenecid 500 mg twice daily depending on the severity of infection.
Ampicillin
2.Vomiting
3.Diarrhoea
4.Anaphylaxis
5.Rash
6.Urticaria
7.Thrombocytopenia
8.Nephritis
9.Seizure.
2.Lymphatic leukaemia
3.HIV infections
4.Renal impairment
2.Gonorrhoea
3. Meningitis
4.SABE
5. Respiratory tract infections
6.Septicemia
7.Soft tissue infections
8.Otitis media
9.Sinusitis
10.Tetanus
11.Biliary tract nfections
12.Bronchitis
13.Salmonellosis
14.Typhoid
15.Gastroenteritis
16.Cholecystitis
17.Paratyphoid fever
Allopurinol: Increases risk of ampicillin induced skin rash.
Beta blockers: Oral penicillin like ampicillin may reduce bio-availability of atenolol. Also they may potentiate anaphylatic reactions with penicillin.
Probenecid: Increases blood levels.
Erythromycin, Tetracycline: Reduce efficacy.
Clavulinic Acid: Synergy.
Food: Interferes with absorption.
Bacterial infections: 250 - 500 mg four times a day depending on the severity of infection
Typhoid and paratyphoid fever: 1 - 2 g four times daily
CHILDREN
Bacterial infections: 125 - 250 mg four times a day depending on the severity of infection
.
Probenecid
Antibiotic therapy adjunct: Probenecid is a competitive inhibitor of the secretion of weak organic acids such as Penicillins and some of the cephalosporin antibiotics, at the proximal and distal renal tubules. It thereby increases blood concentrations of these antibiotics, increases their elimination half-life, and prolongs their duration of action
Distribution: Probenecid is widely distributed throughout the body
Metabolism: It is metabolised to active metabolite in the liver
Excretion: Probenecid and its active metabolites are excreted mainly in the urine. Probenecid is actively reabsorbed.
2. Vomiting
3. Headache
4. Dizziness
5. Anorexia
6. Sore gums
7. Urinary frequency
8. Renal colic
9. Nephrotic syndrome
10. Anaemia
11. Dermatitis
12. Pruritis
13. Flushing
14. Fever
2. Uric acid kidney stones
3. Blood dyscrasias
4. Acute gout
2. Peptic ulcer
Below 2 years: contraindicated
NEONATES: contraindicated
2. Gouty arthritis
3. Along with antibiotics (Stimulate the action of some antibiotics)
Allopurinol: Co-administration may increase uric acid lowering effect.
Barbiturate: Efficacy of thiopentone enhanced.
Benzodiazepines: More rapid or more prolonged benzodiazepine effect may occur.
Clofibrate: Increase in serum concentration of clofibric acid may occur.
Dapsone: Increased accumulation of dapsone may occur.
Methotrexate: Enhanced efficacy & toxicity of methotrexate.
NSAIDs: Increased plasma levels and toxicity of NSAID.
Penicillamine: Efficacy of penicillamine attenuated.
Sulfonylureas: Increased half-life of sulfonylureas.
Zidovudine: Bioavailability of zidovudine increased.
Salicylates: May result in inhibition of uricosuric effect.
Lab. Tests: False diagnosis of glycosuria. False high determination of theophylline by using Schack and Waxler technique. Probenecid may inhibit renal clearance of phenoelulonphtha-lein (PSP), 17 ketosteroids and sulfo-bromophthalein (BSP).
Gout: Initial dose: 500mg / day in 2 divided doses for 1 week followed by 1g /day if needed dosage can be increased by 500 mg/day every 1 month up to 2- 3 g/day.
Adjunct to penicillin or cephalosporin therapy: 2 g / day in 4 divided doses.
Gonorrhoea, uncomplicated: 1 g (as a single dose) 30 min before IM Penicillin and along with oral penicillin.
Neurosyphilis: 2g / day in 4 divided doses with penicillin G procaine aqueous
Pelvic inflammatory disease: 1 g (as a single dose) along with Cefoxitin,
Children:
Adjunct to penicillin or cephalosporin therapy: Pediatric, 2-14 years, initial: 25 mg/kg /day followed by 40mg/kg/day in 4 divided doses.
For children 50 kg or more: give adult dosage
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