Drug Interaction:
Drug Interactions - summary
+ Posaconazole
Cimetidine
Avoid concomittant use unless the benefit outweighs the risk
Phenytoin
Perform frequent monitoring of phenytoin conc. and consider
dose reduction of phenytoin during coadmin.
Ribabutin
Avoid concomittant use unless the benefit outweighs the risk.
If coadmin. is reqd. frequent monitoring of complete cell counts
Posaconazole +
Benzodiazepine metabolised by CYP3A4 eg. midolazam
Perform frequent monitoring for adverse reactions and consider
dose reduction of benzodiazepines during co-admin.
Cal Channel blockrs metabolised through CYP3A4 eg. felodipine
frequent monitoring for adverse reactions and toxicity related
to cal. channel blockrs. is recommended
Dose reduction of cal. channel blockrs may be needed
CYP3A4 substrate eg. astemizole, cisapride, halofantrine,pimozide,
quinidine , terfanadine
Coadmin. is contraindicated
Ergot alkaloids eg. ergotamine, dihydroergotamine
Coadmin. is contraindicated
HMG- CoA reductase inhibitors metabolized by CYP3A4 eg, atorvastatin
it is recommended that dose reduction of statins be considered
during coadmin.
Immunosuppressants eg. cyclosporine,tacrolimus
Reduce the dose of cylcosporine and tacrolimus by three fourths
of the original dose respy. Perform frequent clinical monitoring of
cyclosporine, tacrolimus, sirolimus , whole blood conc. therapy is
initiated and disconitinued
Vinca alkaloids eg. vincristine,vinblastine
Consider dosage adjustment of the vinca alkaloids
Indication:
Oropharyngeal candidiasis Prophylaxis of invasive fungal infections
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Posaconazole Antibiotics& Schering-Plough 26-08-2014
Antifungals
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
Posaconazole Oral suspension 18-07-2009
40mg/ml
For the treatment of orpharyngeal candidiasis, including orophyngeal
candidiasis and refractory to Itraconazole and Fluconazole for prophylaxis
of invasive aspergillus and Canida infections in patients, 13 years of age
and older, who are at risk of developing these infections due to being severely
immunocompromised, such as hemopoetietic stem cell transplant (HSCT)
receipants wth graft -versus -host disease (GVHD) or those with Haemotologic
Malignancies with prolonged neutropenia from Chemotherapy
Adverse Reaction:
Cardiovascular - hypertension 18%, hypotension 14%, tachycardia 12%
CNS - anxiety 9%, dizziness 11%, fatigue 17%, headche 28%, insomnia 17%, weakness 8%
Dermatilogic - pruritus 11%, rash 19%
GI- abdominal pain 27%, anorexia 15%, constipation 21%, diarrhea 42%, dyspepsia 10%,
nausea 38%, vomiting 29%
GU - vaginal haemorrhage 10%
Haemotological- anemia 25%, febrile neutropenia 20%, neutropenia 23%, petechie 11%, thrombocytopenia 29%
Hepatic - bilirubinemia 10%
Metabolic/nutrional - hyperglycaemia 11%, hypocalcemia 9%, hypokalemia 30%, hypomagnesemia 18%,
Musculoskeletal - arthlagia 11% , back pain 10%, musculoskeletal pain 16%, rigors 20%,
Respiratory - coughing 24%, dyspnea 20%, epistaxis 14%, pharyngitis 12%,
upper respiratory tract infection 7%
Miscellaneous- bacteremia 18%, edema, legs 9%, fever 45%, herpes simplex 15%
Contra-Indications:
Hypersensitivity to active substance.
Coadmin with ergot alkaloids,
Coadmin with CYP3A4 substrates, terfenafdine, astemizole, cisapride, pimozide, halofantrine or quinidine because this may result in increased conc. leading to QTc elongation and rare occurance of torsedes de points
Warnings-
Hepatic toxicity-- seen primarily in subjects receiving poaconazole 800mg daily ( 400mg twice daily) or 200mg 4 times daily
Instances- mild to moderate elevation in ALT, AST , alkaline phosphatase- rarely required drug discontinuation
Cardiac effects- administer posaconazole with caution to patients with potentially proarrhythmic conditions, do not administer with drugs that are known to prolong QTc elongation. Make rigourous attempts to correct [potassium, magnesiumm, and calccium before starting posaconazole
Hypersensitivity - use with caution when prescribing to patients with hypersensitivity to
other azoles
Pregnancy- Use posaconazole in pregnancy to patients onlynif the potential benefits justifies the potential risk to fetus
Lactation- Do not prescribe posaconazole to breast feeding mothers unless the benefit cearly outweighs the potential risk to infant
Children- Safety and efficacy in children younger than 13 years of age have not been established
Dosages/ Overdosage Etc:
Oropharyngeal candidiasis Prophylaxis of invasive fungal infections
Dosage-
400mg twice daily Invasive fungal infections- 200mg 3 times daily
Patient Information:
1. Advice patients to take each dose of posaconazole oral suspension with a full meal or liquid nutrional supplement in order to to enhance absorption
2. Inform hypsician, if they develop severe diarrhea, or vomiting becuase these conditions may change blood levels of posaconazole.
3. Inform physician, it they are taking or planning to take other drugs because certain drugs can change blood levels
Interaction with Food:
In order to ensure attainment of adequate plasma concentrations administering posaconazole with food or a nutrional supplement is recommended
Pregnancy and lactation:
Pregnancy-
Use posaconazole in pregnancy to patients onlynif the potential benefits justifies the potential risk to fetus
Lactation-
Do not prescribe posaconazole to breast feeding mothers unless the benefit cearly outweighs the potential risk to infant
Children-
Safety and efficacy in children younger than 13 years of age have not been established
Manufacturer Details