What is dicloxylin and what is it for ? We usually hear the name of this drug, which has a great and diverse utility. Here we tell you all the details.
Index
What is Dicloxylin?
Dicloxacillin is a narrow-spectrum β-lactam antibiotic of the penicillin class. It is used to treat infections caused by susceptible (non-resistant) gram-positive bacteria. It is active against beta-lactamase producing organisms such as Staphylococcus aureus, which would otherwise be resistant to most penicillins. Dicloxacillin is available under a variety of trade names including Diclocyl (BMS).
Medical uses
Dicloxacillin is used to treat mild to moderate staph infections. To decrease the development of resistance, dicloxacillin is recommended to treat infections that can be caused by bacteria that generate beta-lactamases.
Dicloxacillin is similar in pharmacokinetics, antibacterial activity, and indications to flucloxacillin, and the two agents are considered interchangeable. It is believed to have a lower incidence of serious hepatic adverse effects than flucloxacillin, but a higher incidence of renal adverse effects.
Dicloxacillin is used to treat infections caused by susceptible bacteria. Specific approved indications include:
- Staphylococcal skin infections and cellulitis, including impetigo, external otitis, folliculitis, boils, carbuncles, and mastitis
- Pneumonia (attached)
- Osteomyelitis, septic arthritis, throat infections, strep
- Septicemia
- Empirical treatment for endocarditis
- Surgical prophylaxis
How do you get it?
Dicloxacillin is commercially available as the sodium salt, dicloxacillin sodium, in capsules and as a powder for reconstitution.
Contraindications
Dicloxacillin should not be rejected in those who have a history of having been affected by allergies (hypersensitivity / anaphylactic reaction) to any penicillin.
Adverse effects
Common adverse reactions (ADRs) associated with the use of dicloxacillin include: diarrhea, nausea, rash, hives, pain and swelling at the injection site, superinfection (including candidiasis), allergy, and transient increases in liver enzymes and bilirubin.
Rarely, cholestatic jaundice (also known as cholestatic hepatitis) has been associated with dicloxacillin therapy. The reaction can occur up to several weeks after treatment has stopped, and takes weeks to resolve. The estimated incidence is 1 in 15,000 exposures, with more appearing in people over 55, women, and people with treatment for more than 2 weeks.
It should be used with caution and controlled in the elderly, particularly with intravenous administration, due to the risk of thrombophlebitis.
Interactions
Dicloxacillin has potential interactions with the following medications:
Warfarin
Methotrexate
Tetracyclines
Endurance
Although dicloxacillin is insensitive to beta-lactamases, some organisms have developed resistance to other narrow-spectrum beta-lactam antibiotics, including methicillin. Such organisms include methicillin-resistant Staphylococcus aureus (MRSA).
Mechanism of action
Like other β-lactam antibiotics, dicloxacillin works by inhibiting the synthesis of bacterial cell walls. It inhibits the cross-linking between the linear peptidoglycan polymer chains that constitute a major component of the cell wall of Gram-positive bacteria.
Medicinal chemistry
Dicloxacillin is insensitive to beta-lactamase enzymes (also known as penicillinases). The presence of the isoxazolyl group in the side chain of the penicillin nucleus facilitates resistance to β-lactamase, since they are relatively intolerant to steric hindrance of the side chain. Thus, it is capable of binding to penicillin-binding proteins (PBPs) and inhibiting peptidoglycan cross-linking, but it is not bound or inactivated by β-lactamase.
To reduce the development of drug resistant bacteria and maintain the effectiveness of USP Dicloxacillin Sodium Capsules and other antibacterial drugs, USP Dicloxacillin Sodium Capsules should only be used to treat or prevent infections.
Dicloxacillin: Description
Dicloxacillin sodium USP is a semi-synthetic antibiotic substance that resists destruction by the enzyme penicillinase (beta-lactamase). It is monosodium (2S, 5R, 6R) -6- [3- (2,6-dichlorophenyl) -5-methyl-4-isoxazolecarboxamido] -3,3-dimethyl-7-oxo-4-thia-1-azabicyclo [ 3.2.0] heptane-2-carboxylate monohydrate.
Dicloxacillin is administered orally with a powder for reconstitution or a capsule. Structurally, Dicloxacillin sodium USP can be represented as follows:
Capsule and printed components: Gelatin, Lacquer, Sodium Lauryl Sulfate, Sorbitan Monolaurate, Black Iron Oxide, Titanium Dioxide, Propylene Glycol. Penicillinase-resistant penicillins exert a bactericidal action against penicillin-susceptible microorganisms during the state of active multiplication. All penicillins inhibit bacterial cell wall biosynthesis.
Antibacterial activity
Dicloxacillin sodium has been shown to be active against most isolates of the following microorganisms, both in vitro and in clinical infections, as described in the section on indications and uses for this well-recognized drug.
Susceptibility test methods
The susceptibility of staphylococcal isolates to dicloxacillin can be inferred by analyzing penicillin and oxacillin or cefoxitin. For staphylococcal isolates, penicillin susceptibility implies susceptibility to other beta-lactam agents, and penicillin resistance implies resistance to penicillinase-labile penicillins. Resistance to oxacillin (or cefoxitin) implies resistance to all other beta-lactam agents except newer agents such as methicillin-resistant Staphylococcus aureus. Routine testing of dicloxacillin is not recommended.
Pharmacokinetics
Methicillin sodium is easily destroyed by heartburn and must be administered by intramuscular or intravenous injection. The isoxazolyl penicillins (cloxacillin, dicloxacillin, and oxacillin) and nafcillin are more resistant to acids and can be administered orally.
Absorption of isoxazolyl penicillins after oral administration is rapid but incomplete; peak blood levels are reached in 1 to 1.5 hours. In one study, after ingestion of a single 500 mg oral dose, peak serum concentrations ranged from 5 to 7 micrograms / milliliter for oxacillin, 7.5 to 14.4 mcg / ml for cloxacillin, and 10 to 17 mcg / ml for Dicloxacillin.
Oral absorption of cloxacillin, dicloxacillin, oxacillin, and nafcillin is delayed when the drugs are given after meals.
Once absorbed, penicillinase-resistant penicillins bind to serum protein, primarily albumin. The degree of protein binding reported varies with the study method and the investigator.
Penicillinase-resistant penicillins vary in the extent to which they are distributed in body fluids. At normal doses, negligible concentrations are found in cerebrospinal fluid and aqueous humor. All drugs in this class are found in therapeutic concentrations in the pleural, bile, and amniotic fluids.
Penicillinase-resistant penicillins are excreted rapidly as an unchanged drug in the urine with glomerular filtration and by active tubular secretion. The elimination half-life for Dicloxacillin is approximately 0.7 hours. Non-renal elimination includes hepatic inactivation and excretion in the bile.
Indications and use of dicloxacillin
To reduce the development of drug resistant bacteria and maintain the effectiveness of USP Dicloxacillin Sodium Capsules and other antibacterial drugs, USP Dicloxacillin Sodium Capsules should only be used to treat or prevent infections possibly caused by susceptible bacteria. When culture and susceptibility information is available, taking this into account when choosing or changing antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empirical selection of therapy.
Dr. Samantha Robson ( CRN: 0510146-5) is a nutritionist and website content reviewer related to her area of expertise. With a postgraduate degree in Nutrition from The University of Arizona, she is a specialist in Sports Nutrition from Oxford University and is also a member of the International Society of Sports Nutrition.