Flucamed Intravenous Infusion

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by Wisdom Support Desk

(Fluconazole 2mg/ml)

Composition:

Flucamed Intravenous infusion contains 2mg fluconazole in 1ml solution.

Clinical Pharmacology:

Fluconazole, a member of the triazole class of antifungal agents, is a potent and selective inhibitor of fungal enzymes necessary for the synthesis of ergosterol. Fluconazole is highly specific for fungal cytochrome P-450 dependent enzyme. Fluconazole has shown some effectiveness against Aspergillus flavus, Aspergillus fumigatus, Blastomyces dermatitidis, and Coccidioides immitis in laboratory mice. Peak action achieved in 1 to 2 hours; half- life extends for 30 hours.

Initial double dose results in steady-state plasma concentration by day 2 when given intravenously. Fluconazole penetrates into all body fluids in similar and effective coancentrations and remains constant with daily single-dose administration 80% excreted as unchanged drug through the kidneys. Secreted in breast milk.

Indications:

  • Oropharyngeal and esophageal candidis is.
  • Serious systemic candidal infections, including peritonitis and pneumonia. May be an appropriate and less toxic alternative to amphotericin B.
  • Cryptococcal meningitis, including suppressive therapy to prevent relapse.
  • Prevention of candidiasis in bone marrow transplant patients.

Contraindications:

Fluconazole in Flucamed® should not be used in patient with known hypersensitivity to Fluconazole ot to related azole compounds.

Interactions:

  • Hepatotoxicity increased if used concurrently with ketoconazole.
  • Fluconazole inhibits metabolism and increases serum levels of cyclosporine, phenytoin and theophyllines:careful monitoring of their plasma levels is required.
  • Potentiates oral hypoglycemic agents e.g glipzide, glyburide and tolbutamide; monitor blood glucose levels. In all of these situations dose reductions of the above drugs may be indicated.
  • Risk of cardiac arrhythmias increased with cisapride, pimozide and quinidine, concurrent use not recommended.
  • Fluconazole plasma concentrations and effectiveness may be decreased by anticonvulsants (e.g phenytoin, carbamazepine and antimycobacterial agents (e.g, isoniazid may result in treatment failure.

Warnings/ Precaution

-For intravenous use only do not give intramuscular

– Use caution in patients with preexisting liver disease.

Pregnancy and Lactation

-Safety for use in pregnancy and breast feeding not established.

-Use in pregnancy only if potential benefits out weigh risk to fetus.

-Use in nursing mothers is not recommended.

Adverse Reactions:

More frequent in HIV- Infected patients

Abdominal pain, agranulocytosis, allergic reactions, diarrhea, dizziness, dry mouth, exfoliative skin disorders, headache, hepatic reactions, increased appetite, increased sweating, nausea, pallor, rash, taste perversion, thrombocytopenia, framor and vomiting.

Symptoms of overdosage and antidote

Overdose: Cyanosis, decreased motility, decreased respirations, lacrimation, loss of balance, salivation, urinary incontinence.

Most will be treated symptomatically.

A 3-hours dialysis session will decrease plasma levels by 50%. Treat anaphylaxis or resuscitate if indicated.

Dosage and administration:

Intravenous dose has been used for a maximum of 14 days. Plasma levels are similar with intravenous or oral, so oral dose can replace intravenous dose at anytime.

  • Orophageal candidiasis: Initial dose of 299mg followed by 100mg/day for a minimum of 14 days.
  • Esophageal candidiasis: initial dose of 200mg following by 100mg/day for a minimum of 21 days and for at least 2 weeks after symptoms subside. Up to 400mg /24hr may be used.
  • Urinary tract or peritoneal candidiasis: 50 to 200mg/day.
  • Systemic (disseminated) candidiasis: Initial dose of 400mg followed by 200mg/day for a minimum of 28 days and for at least 2 weeks after symptoms subside.
  • Treatment of acute cryptococcal meningitis: Initial dose of 400mg followed by 200mg/day for a minimum of 10 to 12 weeks after cerebrospinal fluid culture becomes negative. Another source suggests a loading dose of 4000mg twice a day   

For 2 days followed by 400mg/day

For the same duration.

  • Suppression of cryptococcal meningitis:

200mg/day. Usually required in pateients with Aids to prevent relapse.

  • Prevention of candidiasis in bone marrow transplant. 40mg/day. If severe neutropenia (less than 500/mm3) is expected, begin Fluconazole pprophylaxis several days ahead of expected neutropenia. Continue for 7 days after neutrophils reach 1000/mm3.

Paediatric Dose

Ages 6 months to 13 years:

10mg/kg as a loading dose. Maintain with 3 to 6 mg/kg/day. Begin 24 hours after loading dose.

Dosing guidelines specific for each indication:

-Oropharyngeal candidiasis: Initial dose of 6mg/kg of body weight followed by 3 mg/kg/day for a minimum of 14 days.

-Esophageal candidiasis: Initial dose of 6mg/kg of body weight followed by 3 mg/kg/day for a minimum of 12 days and for at least 2 weeks after symptoms subside. Up to 12mg/kg has been used. –System candidiasis: 6 to 12 mg/kg/day foa aminimum of 28 days and for at least 2 weeks after symptoms subside.

-Treatment of acute cryptococcal meningitis: Initial dose of 12mg/kg of body weight followed by 6mg/kg/day for a minimum of 10 to 12 weeks after cerebrospinal fluid culture becomes negative.

-Suppression of cryptococcal meningitis: 6 mg/kg/day

Neonatal Dose

-2 weeks to 3 months of age with meningitis or septicemia: 5 to 6mg/kg/day oral or by intravenous infusion over 1 hour, or 10mg/kg as a loading dose followed by 5mg/kg.

-Birth to a 2 weeks of age with meningitis or septicemia: one source suggests using paediatric doses and extending the intervals to once every 72 hours. Another source suggests 6 mg/kg/day with a reduction to 3 mg/kg in neonates with reduced renal function.

A third source suggests a loading dose of 6 to 12 mg/kg and breaks maintenance doses down to post conceptual or postnatal age and adjusts both dose and intervals. The younger the neonate, the higher the maintenance dose and the longer the internal. Premature infants younger than 29 weeks post conception  receive 5 to 6mg/kg every  48 to 72 hours. Beginning  at 30 weeks post conception, neonates receive a maintenancedose of 3 to 6 mg/kg at intervals of 24 to 48 hours  (48-hour interval is for neonates 30 to 36 weeks post conception and full-term infants less than 1 week of age).

Dose adjustments:

-In all adult situations the infecting organism and response to therapy may justify increased doses up to 400mg daily.

– Reduce each dose by 50% in patients with a creatinine clearance at or less than 50ml/min.

-Give one recommended dose after each dialysis in patients receiving regular dialysis.

Presentation:

Storage:

Store at room temperature

Manufactured by:

Drugfield Pharmaceuticals Limited

Lynson Chemical Avenue

Km 38 Lagos Abeokuta Expressway

Sango –Ota

Ogun State.

Metrodine® Intravenous Infusion

(Metronidazole BP 0.5% w/v).

Composition:

Metrodine® Intravenous Infusion Contains 500mg Metronidazole in 100ml solution.

Clinical Pharmacology:

Metronidazole has antiprotozoal and antibacterial actions and is effective against Trichomonas vaginallis and other protozoa including Entamoeba histolytica and Gardia lambila and against anaerobic bacteria.

Widely distributed in therapeutic levels to all body fluid (including abscesses). Levels are directly proportional to dose gicen. Onset of action is prompt and last about 8 hours. Crosses placental and blood-brain barriers. Excreted in urine, some infeces. Secreted in breast milk.

Indications:

-The prevention of postoperative infections due to anaerobic bacteria, particularly species of Bacteroides and anaerobic streptococci.

-The treatment of septicaemia, bacteraemia, peritonitis, brain abscess, necrotising pneumonia, Osteomyelitis, Pueperal sepsis, pelvis abscess, pelvic cellulites and psot operative wound infections from which pathogenic anaerobes have been isolated.

Contraindications:

Hypersensitivity to metronidazole or nitromidazole derivatives; first trimester of pregnancy.

Interactions:

-Patients should be advised to avoid alcohol, alcohol containing preparations for at least 3 days after taking any dose of metronidazole because of the possibility of a disulfiram-like (antabuse effect) reaction.

-Patients receiving phenobarbitone metabolise metronidazole at a much great rate than norma, reducing the half-life to approximately 3 hours.

– Bactericidal action of metronidazole may be negated by bacteriostatic antibiotics (e.g Chloramphenicol, erythromycin and tetracyclines).

-Cimetidine may increase Metronidazole serum levels.

-Metronidazole may decrease metabolism and increase anticoagulant effects of warfarin.

-Metronidazole may increase lithium levels and cause toxicity.

Warning/Precautions

-In Patents undergoing haemodialysis metronidazole and metabolites are efficiently removed during an eight hour period of dialysis.

– Metronidazole should be used with caution in patients with active disease of the central nervous system.

– Metronidazole infusion may be diluted with appropriate volumes of normal saline, dextrose-saline, dextrose 5%w/v of potassium chloride infusions (20 and 40mm /Litres).

Pregnancy and Lactation

There is inadequate evidence of the safety of metronidazole in pregnancy. Metronidazole should not therefore be given during pregnancy or during lactation unless the physician considers it essential; In these circumstances the short, high-dosage regimens are not recommended.

Adverse reactions: Serious adverse reactions occur rarely with standard recommended regimens. During internsive and /or prolonged metronidazole therapy. A few instances of peripheral neuropathy or transient epileptiform seizures have been reported. In most cases neuropathy disappeared after treatment was stopped or when dosage was reduced.

Drowsiness, dizziness, headaches, ataxia, skin rashes, pruritus, inco-ordination of movement, darkening of urine (due to metronidazole metabolite) myalgia and arthralgia have been reported but very rarely.

Symptoms of overdose and antidote

Treatment will be symptomatic and supportive. Discontnue metronidazole with onset of seizures or signs of peripheral neuropathy (e.g numbness or an extremity): benefit/risk of therapy must be considered with onset of convulsions or peripheral neuropathy. Rapidly removed by hemodialyis. Treat anaphylaxis and resuscitate as necessary.

Dosage and administration

Adult Dose

Anaerobic infections: Begin with an initial loading dose of 15mg/kg of body weight. Follow with 7.5mg/kg (up to g/dose) in 6 hours and every 6 hours thereafter for 7 to 10 days or longer if indicated.

Do not exceed 4g in 24 hours

Complicated intrabdominal infections: 50mg every 6 hours given in combination with ciprofloxacin 400mg every 12 hours.

Prevent post operative infection in contaminated or potentially contaminated colorectal surgery: 15mg/kg infused over 30 to 60 minutes and completed 1 hour before surgery. Follow with 7.5mg/kg in 6 hours and in 12 hours. If Bacteroides fragilis is the suspected or confirmed organism, an alternative regimens is to give a 1,500mg dose at the beginning of surgery to ensure adequate metronidazole levels. Amebiasis: 500 to 750mg every 8 hours for 5 to 10 days.

Paediatric Dose

Safety for use in infants and children not established, but is used for anaerobic infections.

Anaerobic infections: children & infants more than 7 days of age: An initial loading dose of 15mg/kg. Follow with 7.5mg/kg every 6 or 8 hours. Preterm infants: same as preterm except begin maintenance   dose (7.5mg/kg) 24 hours after loading dose.

Dose Adjustments:

Reduce dose in hepatic disease and in the elderly.

Increase intervals in neonates.

Reduce dose in hepatic disease and in the elderly.

Increase intervals in neonates.

Presentation:-