Drug Interaction:
Potentiation with alcohol,other CNS depressants and MAOIs.
Diazepam may produce respiratory and cardiac collapse.
May precipatate withdrawal in narcotic addits.
Buphrenophine transdermal patch-
MAOIs-
Buphrenorphine should not be used concomittantly with MAOIs or in patients who have received MAOIs within the previous two weeks
Ketoconazole-
A drug interaction study with CYP3A4 inhibitor - ketoconazole did not produce any clinically
increases in mean Cmax or total AUC buphrenorphine exposure, following buphrenorphine
patch with ketoconazole as compared to buphrenorphine patch alone.
Buphrenorphine patch and enzyme inducers eg. phenobarbital, carbamazepine, phenytion and rifampicin-
could lead to increased clearance which might result in reduced efficacy
General anesthetics eg halothane-
Reduction in blood flow induced by genearal anesthtics eg halothane and medicinal products may resullt in a decreased tate ofhepatic elimination of buphrenorphine
Benzodiazepines-
Buphrenorphine patch should be used cautiously. This combintion with benzodiazepines
can potentiate espiratory depression of central origin with risk of death
Other CNS depressants , other opiod derivatives(analgesics and antitissues containing eg morphine, dextromethorphan or noscopine)-
These combinations increase the CNS depressant activity
Indication:
U.S FDA APPROVED DRUGS FROM 01-01-08 TO 31-12-08
Drug name Indication Date of Approval
249. Buprenorphine 02-12-08
+ Naloxone (2mg/0.4mg + 0.5/0.1mg) tablets
(Addl.Lower stgth)
Aminoketone group - Bupropion
U.S FDA APPROVED DRUGS DURING 2004
225. FDC of Buprenorphin 2mg + 19-08-2004
Nalaxone (0.5mg) For Opioid Dependency
Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
1.Buphrenorphine + Naloxone (2mg/0.4mg+ 0.5+1mg) 02-12-2008
tablets
Addl.lower stgth
As approved
2. Buphrenophine transdermal patch having an 03-09-2009
area of 6.25cm,125cm,and 25cm contains-
Buphrenorphine 5mg/10mg/20mg having
release rate of 5mcg,10mcg. 20mcg
buphrenorphine ( over a period of 7 days)
For the treatment of severe opioid responsive pain conditions
whch are responding to non-opioid analgesics for hospital
supply only
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Buoropion Hcl CNS Glaxo-Wellcome 18-08-2004
FIXED DOSE COMBINATIONS APPROVED BY DCG(I)
FROM JANUARY 1961 TILL NOVEMBER 2014
Name of Drug Indication Date of Approval
1.Buphrenorphine 0.4mg+ 04-06-2005
Noloxone 0.1mg sublingual tablet
For opiod dependence
2.Buphrenorphine + 02-12-2008
Naloxone 0.2mg/0.4mg + 0.5/0.1mg tablet
For opiod dependence
3.Buphrenorphine HCL eq.to Buphrenorphine 2mg+ 01-08-2004
Naloxone Hcl eq.to Naloxone 0.5mg sublingual tablet
For opioid depencdence
Propxyphene -Narcotic Analgesics- information also applies to Dextropropoxyphene
Dextropopoxyphene, Buprenorphine, butorphanol, codiene, hydrocodiene, hydromorphone,levorphanol, meperidine, methadone, morphine, nalbuphrine, opium injection,oxycodone, oxymorphone, pentozocaine, propoxyphene
Refer Dextroprpoxyphene-
Adverse Reaction:
Rare respiratory failure(post operative).
Sedation,nausea,vertigo,
Hypotension,miosis,headache,
Hypoventilation,respiratory or CNS depression,
Tachycardia,bradycardia,pruritus,
Urinary retention,conjuntivitis,
Coma, psychosis.
Contra-Indications:
Severe respiratory disease.
Special precautions:
Opoid agonists,pregnancy,hepatic/renal disease.
Buprenorphine -Transdermal Patch
Contraindications-
1.Patients with hypersensitivity to the active substance or any of the exceipients
2.The treatment of opiod dependence and narcotic withderawal
3.Conditions in which the respiratory centre and function are severely impaired or
become so.
4.Patients who are recieving MAO inhibitors or who have taken them within the last two
weeks
5. Patients suffering from myastenia gravis
6.Patients suffering from delirium temens
Warnings and precautions-
1. Buprenorphine patch should be used with particular caution in patients with convulsive
disorders , head injury, shock, a reduced level of consciousness of uncertain origin,
intracranial lesions or inceased intracranial pressure or in patients with severe hepatic
impairment.
2. Significant respiratory depression has been asociated with buphrenophine , particularly
by the intravenous route
3. A number of deaths have occured when addicts have intravenously abused buphrenophine usually with bezodiazepines concocomittantly.
4. Additional overdose deaths due to ethanol and benzodiazepines in combination with
buphrenorphine have been reported
5. Buphrenorphine patch is not recommended for analgesia in immediate post-operative
period or in other situations characterised by a narrow therapeutic index or rapidly varying
analgesic requirement
Effects of ability to drive or use machines-
Buphrenorphine has a major influence on the ability to drive and use machines, even when used according to instructions. Buphrenorphine patch may affect the patients reactions to such an extent that road safety and inability of operate machinery may be impaired. This applies in the beginning of the treatment and in conjunction with other centrally acting substances including alcohol, tranquillers, sedatives and hypnotics.
In patients who are affected such as treetment, iniiation or titration to a higher dose, these patients should not drive or use machines, nor for at least 24 hours after the patch has been removed
Pregnancy- There are no data from the use of buphrenorphine patch in pregnant women.
Potential risk for humans is unknown.
Towards the end of pregnancy high dose of buphrenorphine may induce respiratory depression in the neonate even after short period of administration.Long term administration of buphrenorpine during the last three months of pregnancy may cause withdrawal symtoms in neonate
Therefore the use of buphrenorphine during pregnancy should be avoided
Dosages/ Overdosage Etc:
Indications:
Acute moderate to severe pain
Dosage:
Patients more than 13 years of age -0.3mg IM slowly every 6 hrs as needed .
Storage: Avoid excessive heat (more than 40C) and light.
Patient Information:
PROPOXYPHENE- NARCOTIC ANALGESIS- INFORMATION ALSO APPLIES TO DEXTROPROPOXYPHENE, BUPRENORPHINE, BUTORPHANOL, CODIENE, HYDROCODONE, HYDROMORPHONE, LEVORPHANOL, MEPERIDINE, METHADONE, MORPHINE, NALBUPHINE, OPIUM INJECTION, OXYCODONE, OXYMORPHONE, PENTOZOCINE, PROPOXYPHENE
Refer Dextroprpoxyphene-
1.May cause dizziness or drowsiness,observe caution while driving or performing tasks requiring alertness.
2. Do not exceed the prescribed dose. Avoid alcohol and benzodiapines.
Pharmacology/ Pharmacokinetics:
Pharmacology:
Buphrenorphine is a semisynthetic centrally acting opoid analgesic derived from thebine; a 0.3mg dose is approximately equivalent to 10mg of morphine in analgesic effect. It exerts its analgesic action via high affinity binding of CNS opiate receptors.
Pharmacokinetics:
Onset of analgesic action occurs 15 minutes after IM injection,peak in about 1 hour,and persists for upto 6 hours. When given IV,the time of onset and peak is shortened.
Interaction with Food:
Place under the tongue and swallow to dissolve completely.
Pregnancy and lactation:
Pregnancy:
Effects not clearly established. Use only if potential benefits outweigh the potential hazards to the fetus.
Lactation:
Not known if buphrenmorphine is excreted in breast milk. Excercise caution when administering to a nursing mother.
Children:
Safety and and efficacy not been established.
