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Hemorrhoidal Products
Hemorrhoids
Hemorrhoids (piles) are dilated, twisted
(varicose) veins located in the wall of the
rectum and anus.
 Hemorrhoids occur when the veins in the
rectum or anus become enlarged; they may
eventually bleed.
 Hemorrhoids may also become inflamed or
may develop a blood clot (thrombus).
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Anatomy & Physiology
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The perianal area (about 7 cm in diameter) is the
portion of the skin & buttocks immediately
surrounding the anus
This area is very sensitive to pain and is moist &
occluded
The anal canal (about 4 cm long) is the channel
connecting the rectum with the outside of the body
It contains sensory nerve endings & pressure
receptors
Anatomy & Physiology
Two powerful sphincters encircle the anal
canal. The external one is a voluntary
muscle. The internal sphincter is an
involuntary muscle
 The point at the mid-upper anal canal at
which the skin lining changes to mucous
membrane is the dentate (anorectal) line.
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Anatomy & Physiology
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The rectum is 12-15 cm long. It is highly
vascularized and does not contain sensory fibers.
Like anal canal, however, it does contain pressure
receptors
Substances absorbed through the rectal mucous
membranes may enter systemic circulation
without passing through the liver
The rectal pH ranges from neutral to basic,
determining the extent to which the substances in
the rectum are absorbed
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Hemorrhoids that form above the boundary
between the rectum and anus (anorectal
junction) are called internal hemorrhoids.
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Those that form below the anorectal junction
are called external hemorrhoids.
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Both internal and external hemorrhoids may
remain in the anus or protrude outside the
anus.
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Haemorrhoids
Haemorrhoids
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Haemorrhoids are common & estimated to affect 5%
of the adult population at some time
Males>females
Peak between 45-70 years old
Increased incidence during pregnancy
Embarrassment over the site of the lesion & the need
for rectal examination may deter some patients from
seeking medical attention as early as they might for
other conditions
It is important for pharmacists to have a sound
knowledge of the symptoms & to know when
Factors Implicated in Etiology
of Hemorrhoids
Erect posture
 Pregnancy
 Prolonged standing or sitting
 Lack of dietary fiber
 Heavy lifting with straining
 Constipation
 Diarrhea
 Heredity (conflicting data)
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Treatment
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Most cases of haemorrhoids can be managed by:
local symptomatic treatment, plus use of laxatives
where necessary & dietary adjustment
Most products contain a combination of
ingredients
As is the case with OTC medicines, there is little
objective evidence of their effectiveness
Self-care of hemorrhoids
Nonpharmacological treatment
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Diet rich in fiber & bulk (gradual ↑to 25-30 g of
fiber or fiber supplement such as psyllium or
methylcellulose)
Avoiding prolonged sitting on the toilet (> 10
min)
Good perianal hygiene + Sitz baths (Homework)
Avoiding lifting heavy subjects
Avoiding irritating food & beverages (e.g.,
caffeine)
Avoiding aspirin & NSAIDs (↑ bleeding)
Homework: guidelines for
applying & inserting rectal
products
1. Local Anaesthetics
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Relieve itching, irritation, burning, dyscomfort &
pain
Benzocaine, Benzyl alcohol, Diclonine HCl,
Dybucaine, Lidocaine, Pramoxine HCl,
Tetracaine
Benzocaine is ester LA allergic reactions & have
been reported frequently can switch to pramoxine
Use should be restricted to perianal region & lower
anal canal, they shouldn’t be used in rectum WHY?
Because there is little sensory tissue there &
anesthetics can be rapidly absorbed through rectal
1. Local Anaesthetics
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Toxic systemic effects involve CV & CNS
Accidental ingestion in children → lethargy,
convulsions & cardiorespiratory arrest → all
products containing LA should be kept away from
children
Preparations of LA must carry warning that
allergy can occur
LA may produce burning & itching which is
undistinguishable from anorectal symptoms being
treated
2. Vasoconstrictors
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reduce swelling by causing the blood vessels to constrict.
They also have a slightly anesthetic effect on the blood
vessels. These enable vasoconstrictors to provide relief
from itching, irritation, & discomfort of the affected
tissues.
Ephedrine, epinephrine & phenylephrine (the latter has
minimal cardiovascular & CNS ADRs)
Vasoconstrictors should be taken only after physician
advice by people with HTN, DM, heart, prostate & thyroid
disease & those receiving antiHTN, antidepressants &
cadriac medications
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3. Protectants
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reduce inflammation by forming a protective barrier over
the skin and mucous membrane.
Protectants also prevent stratum corneum (topmost skin
layer) from losing water.
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4. Astringents
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Calamine, Zinc oxide (externally & internally)
Witch Hazel (only externally)
Astringents act by:
coagulate protein in skin & mucous membrane
cells to form superficial protective layer.
By reducing secretion & intracellular contents
from damaged cells, they help to relieve local
irritation & inflammation
Approved for temporary relief of itching, burning
& irritation
5. Keratolytics
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Cause desquamation & debridement (peel off the
skin), which enables the affected tissues to better
absorb other topical medication for hemorrhoids.
Keratolytics reduce itching and irritation
associated with the condition.
Intrarectal use is not justified & may be harmful
(mucosa does not contain keratin layer!)
Examples are Alcloxa & Resorcinol.
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5. Keratolytics
6.Analgesics/anesthetics/antipruritics
7. Topical corticosteroids
Hydrocortisone
 Acts as vasoconstrictor & antipruritic
 Max. concentration is 1% in ointments,
 Onset is slow (up to 12 hrs) but the duration is
longest compared to other agents
 May mask symptoms of bacterial or fungal
infections
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Anti-inflammatories
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Haemorrhoidal preparations containing
corticosteroids should never be used:
in patients < 18 years old
during pregnancy
during lactation
Should never be used for more than 7 days
It is advised to recommend such products only in
severe cases of haemorrhoids and after consultation
of a doctor
Products in Jordanian Market
Lupinus Albus ,
Vateria Indica ,
Mentha Piperita ,
Aloe Vera
Lupinus Albus
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Proctoheal ointment
Fluocinolone Acetonide , Lidocaine Hydrochloride, 0.1
mg/g, 20 mg/g
Why Fluocinolone???
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Lidocaine , Tribenoside, 2 %, 5 %
Tribenoside: Vasoprotectant
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Diosmin & Flavonid Expressed In Hespiridin
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3 tab BID for 4 days followed by 2 tab. BID for 3 days
seems to significantly improve signs & symptoms of
internal hemorrhoids.
can stop acute bleeding in up to 92% of patients after 4
days of treatment.
can also reduce symptoms such as anal discomfort, pain,
discharge, & local lesions.
subjective symptoms can be relieved within 2 days of
treatment.
also seems to reduce duration & intensity of
hemorrhoidal flare-ups
Maintenance use of 1 tab. BID for 3 months for internal
hemorrhoids seems to significantly decrease relapse rate
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Administration & Dosage Forms
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The recommended treatment regimen for most
preparations is twice daily, morning & evening and
after each bowel movement;
Products containing hydrocortisone should not be
used more than 3-4 times in 24 hours
The bases of all products are likely to contribute an
additional emollient and soothing effect, and the
lubricating effect of suppositories may ease straining
at stool
Administration & Dosage Forms
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However, suppositories may slip into the rectum and
melt there, bypassing the anal areas where the
medication is needed and increasing the possibility
of systemic absorption of local anesthetics &
hydrocortisone;
This possibility is increased if the patient is lying
down
Thus, creams and ointments are generally considered
preferable to suppositories for self-treatment of
haemorrhoids
Product selection points
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Although little evidence of the effectiveness of
haemorrhoidal preparations, most have been
available & used with apparent satisfaction for
many years
The bases of the products may themselves have a
soothing effect
Products containing local aesthetics and
constituents with mechanical protective or
astringent properties should be used first