Amoxycillin + Probenecid Pharmacology

Amoxycillin + Probenecid

About Amoxycillin + Probenecid
N/A
Mechanism of Action of Amoxycillin + Probenecid
N/A
Pharmacokinets of Amoxycillin + Probenecid
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Onset of Action for Amoxycillin + Probenecid
N/A
Duration of Action for Amoxycillin + Probenecid
N/A
Half Life of Amoxycillin + Probenecid
N/A
Side Effects of Amoxycillin + Probenecid
N/A
Contra-indications of Amoxycillin + Probenecid
N/A
Special Precautions while taking Amoxycillin + Probenecid
N/A
Pregnancy Related Information
Contraindicated; since Probenicid is contraindicated in pregnancy
Old Age Related Information
N/A
Breast Feeding Related Information
Use with caution
Children Related Information
N/A
Indications for Amoxycillin + Probenecid
1. Urinary tract infections
2. Respiratory tract infections
3. Surgical prophylaxis
Interactions for Amoxycillin + Probenecid
N/A
Typical Dosage for Amoxycillin + Probenecid
1 - 2 tablets 2 times a day
Amoxycillin 250 mg + Probenicid 250 mg 12 hourly in a day or
Amoxycillin 500 mg + Probenicid 500 mg 12 hourly in a day depending on the severity of infection

Schedule of Amoxycillin + Probenecid
N/A
Storage Requirements for Amoxycillin + Probenecid
N/A
Effects of Missed Dosage of Amoxycillin + Probenecid
N/A
Effects of Overdose of Amoxycillin + Probenecid
N/A

Amoxycillin

About Amoxycillin
Semisynthetic Broad spectrum beta-lactam antibiotic, An aminopenicillin Derivative.
Mechanism of Action of Amoxycillin
Amoxycillin 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. Amoxycillin is active against gram positive and gram negative bacteria except penicillinase producing once.
Pharmacokinets of Amoxycillin
Absorption .It is well absorbed after oral administration. Distribution: It is very widely distributed in the body .Metabolism: In significant metabolism. Excretion: It is excreted mainly through urine and small amount excreted
in breast milk
Onset of Action for Amoxycillin
60 -120 minutes
Duration of Action for Amoxycillin
6-8 hours
Half Life of Amoxycillin
60 minutes
Side Effects of Amoxycillin
1.Aaphylaxis
2. Vomiting
3.Diarrhoea
4 Nausea
5.Rash
6.Urticaria
7.Thrombocytopenia
8.Nephritis
9.Seizure
10.Super infections.
Contra-indications of Amoxycillin
Hypersensitivity to Amoxicillin and other Penicillins.
Special Precautions while taking Amoxycillin
1.Mononucleosis
2.Lymphatic leukaemia
3.HIV infections
4.Hepatic impairment
5.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
Use with caution
Indications for Amoxycillin
1Urinary 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.Biliarytract infections
12.Bronchitis
13.Salmonellosis
14.Typhoid
15.Gastroenteritis
16.Chlamydia infection
17.Paratyphoid fever
18.Dental infections
Interactions for Amoxycillin
Oral contraceptives: Efficacy reduced, may cause breakthrough bleeding or pregnancy.
Erythromycin, Tetracycline: Reduce efficacy.
Typical Dosage for Amoxycillin
ADULT: 250 - 500 mg three to four times daily.
In severe infections dose can be increased to 3 - 6 g daily depending on the severity of infection.
CHILDREN:125 - 250 mg three to four times a day depending on the severity of infection.
Schedule of Amoxycillin
H
Storage Requirements for Amoxycillin
It should store at temperature below 25 degree C. Keep away from moisture and heat. Keep out of the reach of children.
Effects of Missed Dosage of Amoxycillin
Take the dose as soon as noticed and if it is the time to the next dose then skip the missed dose
Effects of Overdose of Amoxycillin
Give supportive measures and symptomatic treatment. If the patient is conscious induce emesis or gastric lavage followed by charcoal administration. Haemodialysis can be done if needed.

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.

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