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Dicloxacillin
Allopathy
Prescription Required
DCGI (Drugs Controller General of India)
Schedule H
Dicloxacillin belongs to the pharmacological class of Beta-Lactam Antibiotics.
Dicloxacillin has been approved to relieve symptoms and also for the treatment and maintenance of mastitis, lactational, prosthetic joint infection, skin and soft tissue infection, septic arthritis, and osteomyelitis (Pediatric).
Dicloxacillin is rapidly but incompletely absorbed from the gastrointestinal tract. The absorption of Dicloxacillin is reduced with food. The Bioavailability of Dicloxacillin is 49-76%. The Time to achieve the peak plasma concentration of Dicloxacillin is found to be 1-1.5 hours. Dicloxacillin is distributed in bone, body tissues, and body fluids. The Volume of distribution of Dicloxacillin is found to be 5.99 L. Dicloxacillin is found to be partially metabolized into active and inactive metabolites. The excretion of Dicloxacillin is mainly via urine which is 31-65%, as an unchanged drug and active metabolite and to a lesser extent through feces.
The common side effects involving the use of Dicloxacillin are nausea, vomiting, headache, diarrhea, headache, upset stomach, etc.
Dicloxacillin is available in the form of Tablets.
Dicloxacillin is approved in the U.S., U.K., Germany, Japan, Malaysia, India, and China.
Dicloxacillin belongs to the pharmacological class of Beta-Lactam Antibiotics.
Dicloxacillin is the pivaloyloxymethyl ester of mecillinam. It interferes with the bacterial cell wall with its high specificity against the penicillin-binding protein 2 (PBP-2), making it different from other penicillins.
Dicloxacillin has been approved to relieve symptoms and for treating and maintaining mastitis, lactational, prosthetic joint infection, skin and soft tissue infection, septic arthritis, and osteomyelitis (Pediatric).
Elimination, the half-life of Dicloxacillin, is approximately 0.7 hours.
Dicloxacillin is available in the form of tablets.
Dicloxacillin can be used in the following treatment:
- Mastitis, lactational
- Prosthetic joint infection
- Skin and soft tissue infection
- Septic arthritis, osteomyelitis (Pediatric)
Dicloxacillin can help to relieve symptoms and also for the treatment and maintenance of mastitis, lactational, prosthetic joint infection, skin and soft tissue infection, septic arthritis, and osteomyelitis (Pediatric).
Dicloxacillin is approved for use in the following clinical indications:
- Mastitis, lactational
- Prosthetic joint infection
- Skin and soft tissue infection
- Septic arthritis, osteomyelitis (Pediatric)
Mastitis, lactational
500mg three to four times a day for a period of 10 to 14 days
Prosthetic joint infection
500mg three to four times a day for a period of 10 to 14 days
Skin and soft tissue infection
500mg three to four times a day for a period of 10 to 14 days
Septic arthritis, osteomyelitis (Pediatric)
Oral: 25 mg/kg/dose every 6 hours; maximum dose: 500 mg/dose
Dicloxacillin is available in the form of 500mg tablets.
Tablets
- Dosage Adjustments in Pediatric Patients:
Children and Adolescents Oral: 3 to 6.25 mg/kg/dose every 6 hours; maximum dose: 250 mg/dose.
Avoid high-acid foods like citrus fruits and juices like orange and grapefruit, soda, and chocolates.
Alcohol intake might lead to nausea, vomiting, and headache.
Multivitamins and antacids contain minerals, primarily magnesium, calcium, aluminum, iron, or zinc, which bind to the antibiotic and refrain it from working. Spacing them at least for 2 hours after Dicloxacillin administration is recommended.
Dicloxacillin may is contraindicated under the following conditions:
- Patients with known hypersensitivity to Penicillin and cephalosporins.
The physician should closely monitor the patients and keep pharmacovigilance as follows:
Sensitivity
Serious as well as occasionally fatal hypersensitivity (anaphylactoid) reactions have been reported in patients receiving penicillin. The reactions are more likely to occur in persons with a history of sensitivity to multiple allergens. Before therapy with Dicloxacillin, a careful inquiry should be made with the patients concerning previous hypersensitivity reactions to penicillins, cephalosporins/ other allergens. If an allergic reaction occurs, the administration of Dicloxacillin should be discontinued and also appropriate therapy instituted. The possibility of superinfections with mycotic or the bacterial pathogens should be kept in mind during the therapy. If superinfections, usually involving Pseudomonas or Candida, or hypersensitivity reactions occur, the Dicloxacillin should be discontinued and/or appropriate therapy instituted.
Susceptibility/Resistance Development of Drug-Resistant Bacteria
Prescribing Dicloxacillin in the absence of a proven or strongly suspected bacterial infection which is unlikely to provide benefit to the patient and risks the development of drug-resistant bacteria.
Alcohol Warning
Usage of alcohol should be avoided while on Dicloxacillin medication, as alcohol can worsen the effects of any underlying disease condition, including conditions such as dizziness, blurred vision, etc.
Breast Feeding Warning
It was found that at therapeutic doses of Dicloxacillin, no effects on breastfed newborns/infants are anticipated. Dicloxacillin can be used during breastfeeding.
Pregnancy Warning
Category B
The clinical data on pregnant women, which is more than 1000 pregnancy outcomes, indicates that there is no malformation nor feto/neonatal toxicity of Dicloxacillin. Dicloxacillin can be used in pregnancy if clinically needed.
Food Warning
No sufficient scientific evidence is traceable regarding the use and safety of Dicloxacillin in concurrent use with any particular food.
The adverse reactions related to Dicloxacillin can be categorized as follows:
- Abdominal pain
- Discomfort
- Diarrhea
- Flatulence
- Stomatitis
- Bacterial or fungal superinfection, which including pseudomembranous colitis and C. difficile-associated diarrhea caused due to prolonged use.
- Eosinophilia
- Agranulocytosis
- Neutropenia
- Hemolytic anemia
- Leucopenia
- Thrombocytopenia
- Nausea
- Vomiting
- Black or hairy tongue
- Serum sickness-like reaction
- Increased liver enzymes
- Haematuria
- Interstitial nephritis
- Rash
- Urticaria
- Pruritus
- Anaphylactic shock with the collapse
The clinically relevant drug interactions of Dicloxacillin are briefly summarized here:
- Simultaneous administration of the drug probenecid reduces the excretion of penicillins and hence increases the blood level of the antibiotic.
- The bactericidal effect of penicillins can be hindered by concurrent administration of products with bacteriostatic effects, for instance, erythromycin and tetracyclines.
The following are the side effects involving Dicloxacillin:
- Abdominal pain
- Discomfort
- Diarrhea
- Flatulence
- Stomatitis
- Bacterial or fungal superinfection, which including pseudomembranous colitis and C. difficile-associated diarrhea caused due to prolonged use.
- Eosinophilia
- Agranulocytosis
- Neutropenia
- Hemolytic anemia
- Leucopenia
- Thrombocytopenia
- Nausea
- Vomiting
- Black or hairy tongue
- Serum sickness-like reaction
- Increased liver enzymes
- Haematuria
- Interstitial nephritis
- Rash
- Urticaria
- Pruritus
- Anaphylactic shock with the collapse
- Pregnancy
Category B
The clinical data on pregnant women, which is more than 1000 pregnancy outcomes, indicates that there is no malformation nor feto/neonatal toxicity of Dicloxacillin. Dicloxacillin can be used in pregnancy if clinically needed.
- Lactation
It was found that at therapeutic doses of Dicloxacillin, no effects on breastfed newborns/infants are anticipated. Dicloxacillin can be used during breastfeeding. Although it is advised that caution be exercised when administering Dicloxacillin to patients who are breastfeeding, penicillins are considered compatible with breastfeeding when used in the usual recommended doses (WHO 2002).
Physicians should be knowledgeable and vigilant about the treatment and identification of overdosage of Dicloxacillin.
There is no experience of overdosage with Dicloxacillin (Dicloxacillin hydrochloride) tablets. However, excessive doses of Dicloxacillin are likely to induce nausea, vomiting, abdominal pain, and diarrhea.
Pharmacodynamics
Dicloxacillin is said to be a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. Dicloxacillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Dicloxacillin results from the inhibition of cell wall synthesis as well as is mediated through Dicloxacillin binding to penicillin-binding proteins (PBPs).
Pharmacokinetics
- Absorption: Dicloxacillin is rapidly but incompletely absorbed from the gastrointestinal tract. Absorption is reduced with food. Bioavailability of Dicloxacillin achieved is 49-76%. Time to peak plasma concentration: 1-1.5 hours.
- Distribution: Dicloxacillin is distributed in bone, body tissues, and body fluids. Low CSF penetration. It Crosses the placenta; it enters breast milk. The Volume of distribution is 5.99 L. The Plasma protein binding achieved is 95-99%, mainly to albumin.
- Metabolism: Dicloxacillin is partially metabolized into active and inactive metabolites.
- Excretion: The excretion of Dicloxacillin is mainly via urine which is 31-65%, as an unchanged drug and active metabolite and to a lesser extent through feces.
- Smith AL, Meeks CA, Koup JR, Opheim KE, Weber A, Vishwanathan CT. Dicloxacillin absorption and elimination in children. Dev Pharmacol Ther. 1990;14(1):35-44.
- Nauta EH, Mattie H. Dicloxacillin and cloxacillin: pharmacokinetics in healthy and hemodialysis subjects. Clin Pharm and Ther. 1976;20(1): 98-108.
- Muysson M, Datta P, Rewers-Felkins K, Baker T, Hale TW. Transfer of Dicloxacillin into human milk. Breastfeed Med. Published online July 15, 2020. doi:10.1089/bfm.2020.0156
- https://www.mims.com/philippines/drug/info/dicloxacillin?mtype=generic
- https://go.drugbank.com/drugs/DB00485
- https://www.accessdata.fda.gov/drugsatfda_docs/psg/Dicloxacillin_cap_62286_RC6-05.pdf
- https://medlineplus.gov/druginfo/meds/a685017.html#:~:text=Dicloxacillin is used to treat,flu, or other viral infections.
- https://www.webmd.com/drugs/2/drug-10328/dicloxacillin-oral/details