Medaxone

Medaxone 1 g powder for injection is almost white or yellowish crystalline powder.
The active substance is ceftriaxone. Medaxone 1 g powder for injection contains 1 g ceftriaxone as ceftriaxone sodium. There are no other excipients.

Pharmacology: Pharmacodynamics: Ceftriaxone inhibits bacterial cell wall synthesis following attachment to penicillin binding proteins (PBPs). This results in the interruption of cell wall (peptidoglycan) biosynthesis, which leads to bacterial cell lysis and death.
Pharmacokinetics: Absorption: After intravenous bolus administration of ceftriaxone 500 mg and 1 g, mean peak plasma ceftriaxone levels are approximately 120 and 200 mg/L respectively. After intravenous infusion of ceftriaxone 500 mg, 1 g and 2 g, the plasma ceftriaxone levels are approximately 80, 150 and 250 mg/L respectively. Following intramuscular injection, mean peak plasma ceftriaxone levels are approximately half those observed after intravenous administration of an equivalent dose. The maximum plasma concentration after a single intramuscular dose of 1 g is about 81 mg/L and is reached in 2-3 hours after administration. The area under the plasma concentration-time curve after intramuscular administration is equivalent to that after intravenous administration of an equivalent dose.
Distribution: The volume of distribution of ceftriaxone is 7-12 L. Concentrations well above the minimal inhibitory concentrations of most relevant pathogens are detectable in tissue including lung, heart, biliary tract/liver, tonsil, middle ear and nasal mucosa, bone, and in cerebrospinal, pleural, prostatic and synovial fluids. An 8-15% increase in mean peak plasma concentration (Cmax) is seen on repeated administration; steady state is reached in most cases within 48-72 hours depending on the route of administration.
Penetration into particular tissues: Ceftriaxone penetrates the meninges. Penetration is greatest when the meninges are inflamed. Mean peak ceftriaxone concentrations in CSF in patients with bacterial meningitis are reported to be up to 25% of plasma levels compared to 2% of plasma levels in patients with uninflamed meninges. Peak ceftriaxone concentrations in CSF are reached approximately 4-6 hours after intravenous injection. Ceftriaxone crosses the placental barrier and is excreted in the breast milk at low concentrations.
Protein binding: Ceftriaxone is reversibly bound to albumin. Plasma protein binding is about 95% at plasma concentrations below 100 mg/L. Binding is saturable and the bound portion decreases with rising concentration (up to 85% at a plasma concentration of 300 mg/L).
Biotransformation: Ceftriaxone is not metabolised systemically; but is converted to inactive metabolites by the gut flora.
Elimination: Plasma clearance of total ceftriaxone (bound and unbound) is 10-22 mL/min. Renal clearance is 5-12 mL/min. 50-60% of ceftriaxone is excreted unchanged in the urine, primarily by glomerular filtration, while 40-50% is excreted unchanged in the bile. The elimination half-life of total ceftriaxone in adults is about 8 hours.

Medaxone is used to treat infections of the brain (meningitis), the lungs, the middle ear, the abdomen and abdominal wall (peritonitis), the urinary tract and kidneys, the bones and joints, the skin or soft tissues, the blood, the heart.
It can be given: to treat specific sexually transmitted infections (gonorrhoea and syphilis).
To treat patients with low white blood cell counts (neutropenia) who have fever due to bacterial infection.
To treat infections of the chest in adults with chronic bronchitis.
To treat Lyme disease (caused by tick bites) in adults and children including newborn babies from 15 days of age.
To prevent infections during surgery.

Medaxone is usually given by a doctor or nurse. It can be given as a drip (intravenous infusion) or as an injection directly into a vein or into a muscle. Medaxone is made up by the doctor, pharmacist or nurse and will not be mixed with or given to the patient at the same time as calcium-containing injections.
The usual dose: The doctor will decide the correct dose of Medaxone for the patient. The dose will depend on the severity and type of infection; whether the patient is on any other antibiotics; the weight and age; how well the kidneys and liver are working. The number of days or weeks that the patient is given Medaxone depends on what sort of infection the patient has.
Adults, older people and children aged 12 years and over with a body weight greater than or equal to 50 kilograms (kg): 1 to 2 g once a day depending on the severity and type of infection. If the patient has a severe infection, the doctor will give a higher dose (up to 4 g once a day). If the daily dose is higher than 2 g, the patient may receive it as a single dose once a day or as two separate doses.
Newborn babies, infants and children aged 15 days to 12 years with a body weight of less than 50 kg: 50-80 mg Medaxone for each kg of the child's body weight once a day depending on the severity and type of infection. If the patient has a severe infection, the doctor will give a higher dose up to 100 mg for each kg of body weight to a maximum of 4 g once a day. If the daily dose is higher than 2 g, the patient may receive it as a single dose once a day or as two separate doses.
Children with a body weight of 50 kg or more should be given the usual adult dose.
Newborn babies (0-14 days): 20-50 mg Medaxone for each kg of the child's body weight once a day depending on the severity and type of infection.
The maximum daily dose is not to be more than 50 mg for each kg of the baby's weight.
People with liver and kidney problems: The patient may be given a different dose to the usual dose. The doctor will decide how much Medaxone the patient will need and will check closely depending on the severity of the liver and kidney disease.

If the patient accidentally receives more than the prescribed dose, contact a doctor or nearest hospital straight away.

The patient must not be given Medaxone if: The patient is allergic to ceftriaxone or any of the other ingredients of this medicine.
The patient has had a sudden or severe allergic reaction to penicillin or similar antibiotics (such as cephalosporins, carbapenems or monobactams). The signs include sudden swelling of the throat or face which might make it difficult to breath or swallow, sudden swelling of the hands, feet and ankles, and a severe rash that develops quickly.
The patient is allergic to lidocaine and is to be given Medaxone as an injection into a muscle.
Medaxone must not be given to babies if: The baby is premature.
The baby is newborn (up to 28 days of age) and has certain blood problems or jaundice (yellowing of the skin or the whites of the eyes) or is to be given a product that contains calcium into their vein.

Talk to a doctor or pharmacist or nurse before the patient is given Medaxone if: The patient has recently received or is about to receive products that contain calcium.
The patient has recently had diarrhoea after having an antibiotic medicine. The patient has ever had problems with the gut, in particular colitis (inflammation of the bowel).
The patient has liver or kidney problems.
The patient has gall stones or kidney stones.
The patient has other illnesses, such as haemolytic anaemia (a reduction in the red blood cells that may make the skin pale yellow and cause weakness or breathlessness).
The patient is on a low sodium diet.
If the patient needs a blood or urine test: If the patient is given Medaxone for a long time, the patient may need to have regular blood tests. Medaxone can affect the results of urine tests for sugar and a blood test known as the Coombs test. If the patient is having tests: Tell the person taking the sample that the patient has been given Medaxone.
Use in Children: Talk to a doctor or pharmacist or nurse before the child is administered Medaxone if: The patient has recently been given or is to be given a product that contains calcium into their vein.

If the patient is pregnant or breast-feeding, is may be pregnant or is planning to have a baby, ask a doctor for advice before taking this medicine. The doctor will consider the benefit of treating the patient with Medaxone against the risk to the baby.

Like all medicines, this medicine can cause side effects, although not everybody gets them. The following side effects may happen with this medicine: Severe allergic reactions (not known, frequency cannot be estimated from the available data): If the patient has a severe allergic reaction, tell a doctor straight away. The signs may include: Sudden swelling of the face, throat, lips or mouth. This can make it difficult to breathe or swallow.
Sudden swelling of the hands, feet and ankles.
Severe skin rashes (not known, frequency cannot be estimated from the available data): If the patient gets a severe skin rash, tell a doctor straight away. The signs may include: A severe rash that develops quickly, with blisters or peeling of the skin and possibly blisters in the mouth (Stevens-Johnson syndrome and toxic epidermal necrolysis which are also known as SJS and TEN).
A combination of any of the following symptoms: widespread rash, high body temperature, liver enzyme elevations, blood abnormalities (eosinophilia), enlarged lymph nodes and other body organs involvement (Drug Reaction with Eosinophilia and Systemic Symptoms which is also known as DRESS or drug hypersensitivity syndrome).
Jarisch-Herxheimer reaction which causes fever, chills, headache, muscle pain, and skin rash that is usually self-limiting. This occurs shortly after starting ceftriaxone treatment for infections with spirochete such as Lyme disease.
Other possible side effects: Common (may affect up to 1 in 10 people): Abnormalities with the white blood cells (such as a decrease of leucocytes and an increase of eosinophils) and platelets (decrease of thrombocytes); Loose stools or diarrhoea; Changes in the results of blood tests for liver functions; Rash.
Uncommon (may affect up to 1 in 100 people): Fungal infections (for example, thrush); A decrease in the number of white blood cells (granulocytopenia); Reduction in number of red blood cells (anaemia); Problems with the way the blood clots. The signs may include bruising easily and pain and swelling of the joints; Headache; Dizziness; Feeling sick or being sick; Pruritis (itching); Pain or a burning feeling along the vein where Medaxone has been given. Pain where the injection was given; A high temperature (fever); Abnormal kidney function test (blood creatinine increased).
Rare (may affect up to 1 in 1,000 people): Inflammation of the large bowel (colon). The signs include diarrhoea, usually with blood and mucus, stomach pain and fever; Difficulty in breathing (bronchospasm); A lumpy rash (hives) that may cover a lot of the body, feeling itchy and swelling; Blood or sugar in the urine; Oedema (fluid build-up); Shivering.
Treatment with ceftriaxone, particularly in elderly patients with serious kidney or nervous system problems may rarely cause decreased consciousness, abnormal movements, agitation and convulsions.
Not known (Frequency cannot be estimated from the available data): A secondary infection that may not respond to the antibiotic previously prescribed; Form of anaemia where red blood cells are destroyed (haemolytic anaemia); Severe decrease in white blood cells (agranulocytosis); Convulsions; Vertigo (spinning sensation); Inflammation of the pancreas (pancreatitis). The signs include severe pain in the stomach which spreads to the back; Inflammation of the mucus lining of the mouth (stomatitis); Inflammation of the tongue (glossitis). The signs include swelling, redness and soreness of the tongue; Problems with the gallbladder, which may cause pain, feeling sick and being sick; A neurological condition that may occur in neonates with severe jaundice (kernicterus); Kidney problems caused by deposits of calcium ceftriaxone. There may be pain when passing water (urine) or low output of urine; A false positive result in a Coombs' test (a test for some blood problems); A false positive result for galactosaemia (an abnormal build up of the sugar galactose); Medaxone may interfere with some types of blood glucose tests - please check with the doctor.

Tell the doctor or pharmacist if the patient is taking, has recently taken or might take any other medicines. In particular, tell the doctor or pharmacist if the patient is taking any of the following medicines: A type of antibiotic called an aminoglycoside.
An antibiotic called chloramphenicol (used to treat infections, particularly of the eyes).

Instruction and Special Precautions for Handling disposal: Concentrations for the intravenous injection: 100 mg/mL, Concentrations for the intravenous infusion: 50 mg/mL.
Reconstitution for injection: Reconstitution should be carried out under suitable conditions and with appropriate precautions to prevent microbial contamination. It is recommended that freshly prepared solutions be used; the solutions retain satisfactory potency for six hours at a temperature not exceeding 25°C, and up to twenty four hours at 2 to 8°C. Following reconstitution, a pale yellow to amber solution is produced.
Intramuscular injection: Reconstitution uses Lignocaine hydrochloride 1.06% injection; 1 g should be reconstituted using 3.5 mL of lignocaine hydrochloride 1.06% injection. Administration is by deep intramuscular injection. If the dosage exceeds 1 g, the dose should be divided equally and administered at more than one injection site. Solutions reconstituted in lignocaine should not be administered intravenously.
Intravenous injection: Reconstitution uses Water for Injection; 1 g should be dissolved in 10 mL of water. Administration is by slow intravenous injection over two to four minutes.
Intravenous infusion: 2 g of ceftriaxone should be dissolved in 40 mL of one of the following calcium-free solutions; Glucose Intravenous Infusion 5% or 10%, Sodium Chloride Intravenous Infusion, Sodium Chloride and Glucose Intravenous Infusion (0.45% sodium chloride and 2.5% Glucose), Dextran 6% in Glucose Injection 5%, isotonic hydroxyethylstarch 6-10% infusions. The infusion should be administered over at least 30 minutes.
Diluents containing calcium (e.g. Ringer's solution or Hartmann's solution), should not be used to reconstitute ceftriaxone vials or to further dilute a reconstituted vial for IV administration because a precipitate can form. Precipitation of ceftriaxone-calcium can also occur when ceftriaxone is mixed with calcium-containing solutions in the same IV administration line. Therefore, ceftriaxone and calcium-containing solutions must not be mixed or administered simultaneously.
Reconstitution should be carried out under suitable aseptic precautions. Following reconstitution the solution should be visually examined for any foreign particulate matter and discarded if any is observed. It is recommended that reconstituted solution is used immediately following preparation. The solutions retain satisfactory potency for six hours at a temperature not exceeding 25°C, and up to twenty four hours at 2 to 8°C. Medaxone vials are for single use only, any remaining suspension/solution should be discarded.

Powder for injection: Store at a temperature not exceeding 30°C.
Reconstituted solution: It is recommended that reconstituted solutions be used immediately. The product does not contain any antimicrobial preservative agent. If not used immediately, in-use storage times and conditions are the responsibility of the user.
When the powder has been mixed with liquid, which will be done by the nurse or doctor, it is best used straight away. If this is not possible, it can be kept for 6 hours at 25°C and 24 hours at 2°C-8°C.

Cephalosporins

J01DD04 - ceftriaxone ; Belongs to the class of third-generation cephalosporins. Used in the systemic treatment of infections.

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