FENTANYL BUCCAL
TABLETS
Learning objective :
1. Physicochemical properties of
fentanyl
2. Pharmacology properties of
fentanyl
3. Dosage form of fentanyl that
available in the market
4. Advantage and disadvantage of
buccal tablet
5. Formulation of fentanyl buccal
tablet
Physicochemical
properties of fentanyl
• Molecular Formula: C22H28N2O
• Molecular Weigh: 336.5 g/mol
• Physical properties: Solid, White crystalline
powder, bitter taste
• Log P : 3.9
• Solubility in water (200mg/L at 25 Celsius)
• Soluble in methanol; slightly soluble in
chloroform -Fentanyl citrate
• Chemical structure: monocarboxylic acid
amide resulting from the formal
condensation of the aryl amino group of Nphenyl-1-(2-phenylethyl)piperidin-4-amine
with propanoic acid It is a member of
piperidines, an anilide and a
monocarboxylic acid amide.
•
Pharmacology
properties of fentanyl
Mechanism of action
•
Fentanyl binds to opioid
receptors,(mu opioid receptor)
which are coupled to G-proteins.
•
Activation of opioid receptors
causes GTP to be exchanged for
GDP on the G-proteins
•
inhibit adenylate cyclase,
reducing in concentrations of
cAMP.
•
decreases presynaptic calcium
ion
•
The exchange of GTP for GDP
results in hyperpolarization of
the cell
•
Increase potassium efflux (
postsynaptic hyperpolarization)
•
inhibition of nerve activity.
•
Reduced the pain in patient
• Fentora Buccal Tablet is an
opioid agonist.
USES & INDICATION OF
FENTORA (FENTANYL)
BUCCAL TABLET
•
It is indicated for the
management of
breakthrough pain in cancer
patients 18 years of age and
older.
-
Already receiving and
tolerant to around- the-clock
opioid
-
therapy for their underlying
persistent cancer pain.
-
Around the clock opioid
therapy
-
regular administration
of doses for the opioid drug.
- Patients who
are taking, for
one week or longer, aroundthe-clock medicine consisting
of:
i.
How to know that
patient already
tolerant?
At least 60 mg of oral
morphine per day
ii. At least 25 mcg per hour
of transdermal fentanyl
iii. At least 30 mg of oral
oxycodone per day
iv. At least 8 mg of oral
hydromorphone per day
v. At least 25 mg oral
oxymorphone per day
vi. At least 60 mg of oral
hydrocodone per day
vii. An equianalgesic dose of
another opioid daily for a
week or longer.
Patients must remain on
around-the-clock opioids
while taking FENTORA.
DOSE OF FENTORA
BUCCAL TABLET
•
The initial dose of Fentora buccal
tablet is always 100 mcg with the
only exception for patients already
using ACTIQ (oral transmucosal
fentanyl citrate)
•
If the breakthrough pain episode is
not relieved after 30 minutes,
patients may take only one
additional dose using the same
strength for that episode.
•
Maximum of two doses of Fentora
for any episode of breakthrough
pain.
•
Patient must wait at least 4 hours
before treating another episode of
breakthrough pain with Fentora.
•
Fentora Buccal Tablets dose and
strength that available:
100 mcg, 200 mcg, 400 mcg, 600 mcg,
and 800 mcg
SIDE EFFECT OF FENTANYL
BUCCAL TABLET
Common side effects of Fentora:
- Nausea
- Vomiting
- Constipation
- Light headedness
- Drowsiness
Serious side effects of Fentora :
- mental/mood changes
(agitation, confusion, hallucinations)
- severe stomach / abdominal pain
- difficulty urinating
Dosage form of
fentanyl that available
in the market
Troche/lozenge
(Actiq)
•
•
•
•
•
•
200mcg
400mcg
600mcg
800mcg
1200mcg
1600mcg
Tablet/sublingual
(Abstral)
•
•
•
•
•
•
100mcg
200mcg
300mcg
400mcg
600mcg
800mcg
Buccal tablet
(Fentora)
•
•
•
•
•
100mcg
200mcg
400mcg
600mcg
800mcg
Sublingual spray
(Subsys)
•
•
•
•
•
100mcg/spray
200mcg/spray
400mcg/spray
600mcg/spray
800mcg/spray
Soluble film
(Onsolis)
•
•
•
•
•
200mcg
400mcg
600mcg
800mcg
1200mcg
Reason use
fentanyl buccal
tablet
Advantage and disadvantage of
buccal tablet
Advantages
Disadvantages
•
•
•
•
•
•
•
•
•
Mesenteric circulation is by passed
No loss of drug ( by first pass effect)
Higher bioavailability and onset of
action ( than oral)
Rapid absorption due to high
vascularization
Reduce side effects due to low dose
and high efficiency
Fast dissolution and disintegration
without water or chewing action.
Improved drug compliance
pH of mouth is neutral so drug will
be stable
•
•
•
•
Interferes with eating, drinking, and
talking
Not for unconscious patient
If any is swallowed that portion must
be treated as an oral dose and
subjected to 1st pass effect
Only small dose can be
accommodated
Patient should not smoke while taking
the medication as smoking cause
vasoconstriction of BV and will
decrease the absorption of drug.
Formulation
of fentanyl
buccal tablet
References
• drugbank.ca/drugs/DB00813#BE00007
70
• rxlist.com/fentora-side-effects-drugcenter.htm
• https://pubchem.ncbi.nlm.nih.gov/co
mpound/Fentanyl