Heracillin

Heracillin Uses, Dosage, Side Effects, Food Interaction and all others data.

Heracillin inhibits the 3rd and last step of bacterial cell wall synthesis by binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall. It is active against penicillinase-producing and non-penicillinase-producing staphylococci.

Heracillin is isoxazolyl penicillin which combined the properties of resistance to hydrolysis by penicillinase, gastric acid stability and activity against gram-positive bacteria. Heracillin is a bactericidal antibiotic that is particularly useful against penicillinase-producing staphylococci. Heracillin kills bacterial cellwall, thus interfering with peptidoglycan synthesis. Peptidoglycan is a heteropolymeric structure that provides the cell wall with its mechanical stability. The final stage of peptidoglycan synthesis involves the completion of the cross-linking with the terminal glycine residue of the pentaglycin bridge linking to the fourth residue of the pentapeptide (D-alanine). The transpeptidase enzyme that performs this step is inhibited by Heracillin. As a result the bacterial cellwall is weakened, the cell swells and then ruptures. Heracillin resists the action of bacterial penicillinase probably because of the steric hindrance induced by the acyl side chain which prevents the opening of the β- lactam ring.

Heracillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Heracillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Heracillin results from the inhibition of cell wall synthesis and is mediated through flucloxacillin binding to penicillin binding proteins (PBPs). Heracillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.

Trade Name Heracillin
Generic Flucloxacillin
Flucloxacillin Other Names Floxacillin, Flucloxacilina, Flucloxacillin, Flucloxacilline, Flucloxacillinum
Type
Formula C19H17ClFN3O5S
Weight Average: 453.872
Monoisotopic: 453.056147271
Groups Approved, Investigational
Therapeutic Class Penicillinase-resistant penicillins
Manufacturer
Available Country Denmark, Iceland, Sweden
Last Updated: September 19, 2023 at 7:00 am
Heracillin
Heracillin

Uses

Heracillin is used for the treatment of infections due to Gram-positive organisms, including infections caused by β-lactamase producing staphylococci.

Skin and Soft Tissue Infections: Boils, abscesses, carbuncles, furunculosis,infected wounds, infected burns, protection of skin grafts, otitis media and externa, impetigo.

Infected Skin Conditions: Ulcer, eczema and acne.

Respiratory Tract Infections: Pneumonia, lung abscess, empyema, sinusitis,pharyngitis, tonsillitis, quinsy.

Other infections caused by Heracillin-sensitive organisms such as osteomyelitis, enteritis, endocarditis, urinary tract infection, meningitis, septicaemia.

Heracillin is also used for use as a prophylactic agent during major surgical procedures where appropriate, for example, cardiothoracic and orthopaedic surgery

Heracillin is also used to associated treatment for these conditions: Susceptible infections

How Heracillin works

By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, flucloxacillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that flucloxacillin interferes with an autolysin inhibitor.

Dosage

Heracillin dosage

Oral administration:

Adult or Elderly:

  • Usual dosage: 250 mg four times daily. In severe infections, dosage should be doubled.
  • In osteomyelitis and endocarditis: up to 8 gm daily, in divided doses 6 to 8 hourly.
  • In case of secondary bacterial infection in chicken pox: Heracillin 500 mg six hourly should be prescribed.

Children:

  • Usual dosage: 2-10 years: half of the adult dose. Under 2 years: quarter of the adult dose.

Parenteral administration:

Adult or Elderly:

  • Intramuscular Injection: 250 mg four times daily.
  • Intravenous Injection: 250 mg-1 g four times daily by slow injection over 3 to 4 minutes or by intravenous infusion.
  • All systemic doses may be doubled in severe infections: doses up to 8 g daily have been suggested for endocarditis or osteomyelitis.

Children:

  • Usual dosage: 2-10 years : half of the adult dose. Under 2 years : quarter of the adult dose.

Doses should be administered half an hour before meals.

Heracillin has been used in other routes in conjunction with systemic therapy. It has been administered in a dose of 250 mg to 500 mg daily by intraarticular injection, dissolved if necessary in a 0.5% solution of lignocaine hydrochloride, and by intrapleural injection in a dose of 250 mg daily. Using powder for injection, 125 mg-250 mg has been dissolved in 3 ml of sterile water and inhaled by nebuliser four times daily.

Side Effects

There have been some common side effects of GIT such as nausea, vomiting, diarrhoea, dyspepsia and other minor gastrointestinal disturbances. Besides these rashes, urticaria, purpura, fever, interstitial nephritis, hepatitis and cholestatic jaundice have been reported

Precaution

Patient with spirochaete infections (e.g. syphilis, leptospirosis), history of hypersensitivity to β-lactam antibiotics. Newborn infants. Hepatic or renal impairment. Pregnancy and lactation.

Interaction

The administration of probenecid with Heracillin results in higher serum peak concentrations and prolongs the time that therapeutic concentrations of Heracillin are achieved in serum. Physical incompatibility and/or loss of activity of Heracillin in solution has been reported when given with gentamycin sulphate, streptomycin sulphate, vitamin mixtures. Heracillin should not be added to intravenous lipids, blood products and protein hydrolysates or other proteinaceous fluids.

Food Interaction

  • Take on an empty stomach.

Elimination Route

Bioavailability is 50–70% following oral administration.

Half Life

0.75–1 hour

Pregnancy & Breastfeeding use

The use of Heracillin in pregnancy should be reserved for cases considered essential by the clinician. Use of the drug in the second and third trimesters may result in the sensitisation of the fetus. During lactation, trace quantities of penicillins can be detected in breast milk.

Contraindication

Heracillin is contraindicated for those who have hypersensitivity to penicillins.

Special Warning

Dose adjustment in renal impairment : As common with other penicillins, Heracillin usage in patients with renal impairment does not usually require dosage reduction. However, in the presence of severe renal failure (creatinine clearance < 10 ml/min) a reduction in dose or an extension of dose interval should be considered. Heracillin is not significantly removed by dialysis and hence no supplementary dosages need to be administered either during or at the end of the dialysis period.

Acute Overdose

Symptoms: Neurotoxicity (e.g. convulsions, encephalopathy), GI effects (e.g. nausea, vomiting, diarrhoea), blood disorders (e.g. neutropenia, haemolytic anaemia, prolongation of bleeding time, defective platelet function), electrolyte disturbances.

Management: Symptomatic treatment.

Storage Condition

Store below 25° C. Reconstituted solution: Store between 2-8°C.

Innovators Monograph

You find simplified version here Heracillin

Heracillin contains Flucloxacillin see full prescribing information from innovator Heracillin Monograph, Heracillin MSDS, Heracillin FDA label

FAQ

What is Heracillin used for?

Heracillin is an antibiotic used to treat skin infections, external ear infections, infections of leg ulcers, diabetic foot infections, and infection of bone. It may be used together with other medications to treat pneumonia, and endocarditis.

How safe is Heracillin?

It is normally very well tolerated but can be more likely than other antibiotics to cause heartburn. 

How does Heracillin work?

Heracillin works by interfering with the formation of the bacterial cell walls.

What are the common side effects of Heracillin?

The most common side effects are feeling sick (nausea) and diarrhoea. You can drink alcohol while taking Heracillin. You can take Heracillin during pregnancy or while you're breastfeeding.

Is Heracillin safe during pregnancy?

It is safe to take Heracillin during pregnancy.

Is Heracillin safe during breastfeeding?

It is safe to take Heracillin while breastfeeding. Information shows that only tiny amounts of Heracillin get into breast milk, which would not be expected to cause any side effects in your baby.

Can I drink alcohol with Heracillin?

Yes, you can drink alcohol while taking Heracillin.

How quickly does Heracillin take to work?

This means at least 30 to 60 minutes before a meal or snack, or at least 2 hours after. For most infections, you should start to feel better within a few days.

Can I take Heracillin on an empty stomach?

Heracillin is best taken on an empty stomach, one hour before eating food. This is because your body may absorb less Heracillin after a meal, making it less effective.

What is the half life of Heracillin?

The elimination half-life of Heracillin is in the order of 53 minutes.

How often can I take Heracillin?

The usual dose of Heracillin is 250mg to 500mg, taken 4 times a day.

Can I take Heracillin long term?

Keep taking Heracillin until you finish the pack, or for as long as your doctor recommends. Do not stop taking Heracillin, even if you feel better after a few days, unless advised by your doctor. Your infection may not clear completely if you stop taking your medicine too soon.

What happen If I stop taking Heracillin?

Do not stop taking Heracillin, even if you feel better after a few days, unless advised by your doctor. If you do not complete the full course prescribed by your doctor, the infection may not clear completely or your symptoms may return.

What happens if I miss a dose?

If you miss a dose, take it as soon as you remember. However, if it's almost time for your next dose, plan to skip the missed dose and take your next dose as scheduled. Never double up on a dose. If you'd like more information about an antibiotic you've been prescribed, talk with your doctor or pharmacist.

What happens if I overdose?

Symptoms of an overdose may include nausea, vomiting and diarrhoea. If you take too much (overdose) Immediately telephone your doctor or the Poisons Information Centre for advice, or go to Accident and Emergency at the nearest hospital, if you think that you or anyone else may have taken too much FLOPEN. Do this even if there are no signs of discomfort or poisoning.

Who should not take Heracillin?

You have pale poo with dark pee, and the whites of your eyes or skin turn yellow (this may be less obvious on black or brown skin) – this can be a sign of liver problems. you get bruising or discoloured skin. you have joint or muscle pain that starts happening after 2 days of taking the medicine.

Can Heracillin affect my kidneys?

Heracillin can injure the kidneys as well as the liver. Both interstitial nephritis and hepatitis are listed as very rare undesirable effects in the Heracillin data sheets.

Can Heracillin affects my liver?

Heracillin is now established as an important cause of cholestatic liver disease.

*** Taking medicines without doctor's advice can cause long-term problems.
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