GREENLIFE

PHARMACEUTICALS LTD

.
 LOFNAC SUPPOSITORY
Diclofenac Sodium 100mg

THE ALTERNATIVE ROUTE

 DEFINITION

 The term suppository comes from the latin word

which means ‘to place under’.

 Suppositories are solid dosage forms intended for

administration of medicine into body orifices.
 TYPES OF SUPPOSITORIES

There are 3 types of suppositories

 Rectal
 Vagina
 Urethral
 SUPPOSITORY BASE

 This could be classified into 2 types

 (1) Fatty bases

-Cocoa butter
-Synthetic triglycerides (cocoa butter
-substitutes hydrogenated vegetable oils) e.g
witepsol
 Contd

 (2) Water soluble and water miscible bases.

 -Glycerinated gelatin
 -Polyethylene glycol bases (PEG)
 THE FORMULATION

 The medicament is incorporated into a base that

melts or dissolves at the body temperature.
 Suppository base composition plays an important
role in both the rate and extent of release of
medications.
 In the poly ethylene glycol base with the structure
below
 .

 HOCH2(CH2-0-CH2)Nch20h
 There is rapid release of the drug
 Faster dissolution
 It absorbs water.
 It can be stored without refrigeration.
 Dissolution time for polyethylene glycol Suppository
is 15-30 mins
 CHARACTERISTICS OF AN IDEAL
SUPPOSITORY

 It should be non-toxic.
 It should be physically stable i.e, during storage
and manufacture
 It should be non-irritating
 It should be chemically inert i.e, no colour change
 Dissolve or disperse in rectal fluids
 It should have high viscosity when dissolved ie,
doesn’t leak from rectum or vagina
 It should be
hygroscopic
 It should be
convenient to handle
 It should not bind
with other molecules
found inside the
rectum
) PHYSIOLOGY OF ABSORPTION

 The rectum is highly vascularised

 It consists of three main veins
Inferior haemorrhoidal vein
Middle haemorrhoidal vein
Superior haemorrhoidal vein
THE RECTUM
The blood supply to the ano-
rectal region.
 .

 The middle and inferior veins have more blood

capillaries
 When a suppository is inserted into the rectum, it is
absorbed by the middle and inferior veins and
transported via the ileum directly into the systemic
circulation thereby bypassing the portal vein and
first pass metabolism does not occur
 .

 When inserting, do not insert too deep into the

rectum as the drug will be absorbed by the superior
veins, then to the portal vein.
 The drug then passes through first pass metabolism.
 PHARMACOKINETICS OF PEG

 Plasma concentrations obtained with PEG is greater

than that with cocoa butter, therefore PEG enhances
the bioavailability of the drug than cocoa butter.
 ADVANTAGES OF SUPPOSITORIES

 Effective in cases of nausea and vomiting with oral

medication
 Protect drug from harsh GI conditions
 Portal circulation is bypassed, thereby side effect is
reduced
 Oral intake is restricted before surgery,
suppository comes in useful
 Self administration
 Alternative route for drugs that are not palatable or
have bitter taste
 LOFNAC SUPPOSITORY

 LOFNAC SUPPOSITORIES (diclofenac sodium

100mg). A non-steroidal anti inflammatory agent
used in management of pains, joint stiffness and
inflammation
 LOFNAC SUPPOSITORY

Early post-operative relief of pain and shivering using

diclofenac suppository versus intravenous pethidine
in spinal anesthesia.

Ali Janpour Ebrahim et al( 2014): Journal of Anaesthesiology Clinical

Pharmacology, vol 30: iss 2 Pg243-247
 ABSTRACT

Background: Pain and shivering are two challenging

components in the post operative period. Many
drugs were used for prevention and treatment of
them. The aim of this study was to compare the
effects of prophylactic prescription of diclofenac
suppository versus intravenous (IV) pethidine in
spinal anesthesia
 METHOD

 A multi-centered,prospective, double-blinded,
randomized clinical trial was conducted with a total
of 180 patient scheduled for surgery under spinal
anesthesia which include 60 patient in three groups.
 Patient were randomly allocated to receive 100mg
diclofenac sodium suppository or 30mg IV Pethidine
or placebo
 METHOD

 Categorical and continuous variables were analyzed

by Chi-square, t-test, Mann-Whiteney and ANOVA
or Kruskal-Wallis test
 RESULTS

 There was no statistical difference with regard to

patient characteristics and hemodynamics indices
among the 3 groups. 15%, 16.65% and 40% in
diclofenac, pethidine and control group respectively
reported pain.
 Prutitis was repetitive in pethidine group and was
statistically significant (p=0.0036)
 CONCLUSION

A single dose of sodium diclofenac suppository

can provide satisfactory analgesia immediately
after surgery and decrease shivering without
remarkable complications.
 This investigation highlights the role of pre-
operative administration of a single dose of rectal
diclofenac as a sole analgesic for early post
operative period.
 Dosage and application
• One suppository should be inserted daily into
the rectum.

APPLICATIONS
• Clean the area around the rectum.
• Position the patient flat on back or on one side,
with anal exposed.
 Dosage and Application Cont

• Remove wrapper by holding the suppository upright

and carefully peel the wrapper.
 LOFNAC SUPPOSITORY

• Gently insert well into the rectum. Use fingertips to

complete insertion.

• Note: Avoid excessive handling as suppository melts

at body temperature.
 LOFNAC SUPPOSITORY

Indications
• Post surgical pains
• Rhematoid Arthritis
• Osteoarthritis
• Dysmenorrea
• Ankylosing spondylitis
• Pains and inflammation after injuries or minor
surgeries.
 LOFNAC SUPPOSITORY.

Contra-indications:
• Hypersensitivity to Diclofenac sodium
• Gastric and/or duodenal ulcers
 WHY YOU SHOULD PRSCRIBE
SUPPOSITORIES

 Useful when patient cannot swallow e.g in

unconscious patients, E.N.T patients and emergency
cases
 Absorption is rapid
 Drugs avoid first pass metabolism in the liver
 Effective in cases of nausea and vomiting especially
after surgery
 Reduce the pain of giving injection
 .

 THANK YOU