Ampicillin + Probenecid Pharmacology

Ampicillin + Probenecid

About Ampicillin + Probenecid
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Mechanism of Action of Ampicillin + Probenecid
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Pharmacokinets of Ampicillin + Probenecid
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Onset of Action for Ampicillin + Probenecid
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Duration of Action for Ampicillin + Probenecid
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Half Life of Ampicillin + Probenecid
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Side Effects of Ampicillin + Probenecid
N/A
Contra-indications of Ampicillin + Probenecid
N/A
Special Precautions while taking Ampicillin + Probenecid
N/A
Pregnancy Related Information
Use with caution
Old Age Related Information
N/A
Breast Feeding Related Information
Use with caution
Children Related Information
N/A
Indications for Ampicillin + Probenecid
Probenecid is used with Penicillin for the purpose of delaying the excretion of Penicillin. Higher dose of Probenecid are used as an adjunct to prolong Penicillin concentrations.
1.Gonorrhoea
2.Neurosyphilis infections
Interactions for Ampicillin + Probenecid
N/A
Typical Dosage for Ampicillin + Probenecid
1 tablet to be taken every 12 hours for 7 - 10days.
Ampicillin 250 mg + Probenecid 250 mg twice daily or
Ampicillin 500 mg + Probenecid 500 mg twice daily depending on the severity of infection.
Schedule of Ampicillin + Probenecid
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Storage Requirements for Ampicillin + Probenecid
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Effects of Missed Dosage of Ampicillin + Probenecid
N/A
Effects of Overdose of Ampicillin + Probenecid
N/A

Ampicillin

About Ampicillin
Semisynthetic Broad spectrum beta-lactam antibiotic, Aminobenzylpenicillin Antibiotic
Mechanism of Action of Ampicillin
Ampicillin is a bactericidal drug. It is a Beta lactum antibiotic. It binds to the Penicillin binding protein in the cell wall of bacteria and inhibits the enzyme transpeptidase which is responsible for the transpeptidation reaction in peptidoglycan synthesis. It also activates the endogenous enzyme which degrades the peptidoglycan.These results in inhibition of protein synthesis and there by cell wall synthesis. Ampicillin is active against both gram positive and gram negative organism.
Pharmacokinets of Ampicillin
Absorption .It is readily but incompletely absorbed after oral administration. Distribution: It is very widely distributed in the body .Metabolism: It does not undergo metabolism. Excretion: It is excreted mainly through bile and small amount excreted through urine and breast milk.
Onset of Action for Ampicillin
30 minutes
Duration of Action for Ampicillin
6 - 8 hours
Half Life of Ampicillin
90 minutes
Side Effects of Ampicillin
1.Nausea
2.Vomiting
3.Diarrhoea
4.Anaphylaxis
5.Rash
6.Urticaria
7.Thrombocytopenia
8.Nephritis
9.Seizure.
Contra-indications of Ampicillin
1.Hypersensitivity to Penicillin
Special Precautions while taking Ampicillin
1.Mononucleosis
2.Lymphatic leukaemia
3.HIV infections
4.Renal impairment
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
N/A
Indications for Ampicillin
1.Urinary tract infections
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
Interactions for Ampicillin
Oral contraceptives: Efficacy reduced, may cause breakthrough bleeding or pregnancy.
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.
Typical Dosage for Ampicillin
ADULT
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
.
Schedule of Ampicillin
H
Storage Requirements for Ampicillin
Store the drug at 15 - 30 degree C in a tightly closed container. Keep out of the reach of children
Effects of Missed Dosage of Ampicillin
Take the missed dose as soon as noticed. If it is the time for next dose then skip the missed dose and continue the regular schedule. Do not double the dose.
Effects of Overdose of Ampicillin
Give supportive measures and symptomatic treatment. Absorption of the drug can be reduced by administration of activated charcoal.

Probenecid

About Probenecid
Uricosuric, Antigout .
Mechanism of Action of Probenecid
Probenecid is a uricosuric agent. It increases the uric acid excretion by inhibiting the tubular reabsorption of uric acid and results in a decreased serum level of uric acid.
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
Pharmacokinets of Probenecid
Absorption: It is completely absorbed after oral administration.
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.
Onset of Action for Probenecid
Within 60 minutes
Duration of Action for Probenecid
1 day
Half Life of Probenecid
3 - 12 hours
Side Effects of Probenecid
1. Nausea
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

Contra-indications of Probenecid
1. Hypersensitivity to Probenecid
2. Uric acid kidney stones
3. Blood dyscrasias
4. Acute gout
Special Precautions while taking Probenecid
1. Renal impairment
2. Peptic ulcer
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
Below 2 years: contraindicated
NEONATES: contraindicated
Indications for Probenecid
1. Gout
2. Gouty arthritis
3. Along with antibiotics (Stimulate the action of some antibiotics)
Interactions for Probenecid
Acyclovir: Increased bioavailability of acyclovir may occur.
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).






Typical Dosage for Probenecid
Adult:
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
Schedule of Probenecid
N/A
Storage Requirements for Probenecid
Store at room temperature. Protect from heat and light. Keep out of the reach of children
Effects of Missed Dosage of Probenecid
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Probenecid
Give supportive measures and symptomatic treatment. Drug can be removed from the body by inducing emesis and by gastric lavage. Seizure can be controlled by intravenous administration of Phenobarbital and Phenytoin.

Home Delivery for Ampicillin + Probenecid in Your City

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