Download S04.OTC.Hemorrhoids

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Hemorrhoids
 Hemorrhoids 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
 The dentate line delineates where nerve fibers end.
 Above this line, this area is relatively insensitive to
pain.
 Below the dentate line, the anal canal and anus are
extremely sensitive.
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 Hemorrhoids that form above the boundary between
the rectum and anus (anorectal junction) are called
internal hemorrhoids.
 Those that form below the anorectal junction are
called external hemorrhoids.
 Both internal and external hemorrhoids may remain
in the anus or protrude outside the anus.
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The Liver and Hemorrhoids
 By Looking at the venous return for the external and
internal hemorrhoidal veins, the following is observed:
 External – pours into the systemic circulation
 Internal - pours into portal veins
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Frequency. United States:
 Prevalence of symptomatic hemorrhoids is estimated at 4.4% in the general
population.
Race
 Patients presenting with hemorrhoidal disease are more frequently Caucasian, from
higher socioeconomic status, and from rural areas.
Sex
 No predilection is known, although men are more likely to seek
treatment. However, pregnancy causes physiologic changes that predispose women
to developing symptomatic hemorrhoids. As the gravid uterus expands, it
compresses the inferior vena cava, causing decreased venous return and distal
engorgement.
Age
 External hemorrhoids occur more commonly in young and middle-aged adults than
in older adults. The prevalence of hemorrhoids increases with age, with a peak in
persons aged 45-65 years.
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Etiology
 Most common cause - constipation
 Prolonged straining
 Pregnancy
 Heredity
 Increased intra-abdominal pressure
 Aging (due to thinning of supportive tissue)
 Chronic diarrhea.
 Obesity
 Colon Cancer
 Rectal Surgery
 Rectal intercourse
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Generalized Symptoms
 Painless bleeding. Most common symptom. Blood is bright
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red
Mucosal protrusion
Discharge
Soiled underwear - due to prolapse
Sensation of incomplete evacuation
Pain
Discomfort, pruritis, burning sensation.
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Symptoms - external hemorrhoids
 External hemorrhoids, because they lie under the
skin are usually very painful
 Result in tender blue swelling at the anal verge due
to thrombosis of a vein in the external plexus need not be associated with enlargement of the
internal veins
 Spasm often occurs since the thrombus usually lies
at the level of the sphincteric muscles
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Conditions that mimic hemorrhoids
 Anal abscess
 Cryptitis
 Anal fissure
 Inflammatory bowel disease
 Rectal polyps
 Colorectal cancers
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June 22, 2011 — The US Food and Drug
Administration (FDA) has approved
nitroglycerin ointment 0.4% (Rectiv,
ProStrakan Group) for the treatment of
moderate to severe pain associated with
chronic anal fissures
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Classification
 Most clinicians use the grading system proposed by Banov et al in 1985,
which classifies internal hemorrhoids by their degree of prolapse into the
anal canal. This system both correlates with symptoms and guides
therapeutic approaches.
Grade I hemorrhoids project into the anal canal and often bleed but do
not prolapse.
Grade II hemorrhoids may protrude beyond the anal verge with straining
or defecating but reduce spontaneously when straining ceases.
Grade III hemorrhoids protrude spontaneously or with straining and
require manual reduction.
Grade IV hemorrhoids chronically prolapse and cannot be reduced. They
usually contain both internal and external components and may present
with acute thrombosis or strangulation.
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Treatment
For 1st and 2nd grades:
 Reduce straining
 Correction of constipation
 Epsom salt baths
 OTC hemorrhoidal ointments, creams, foams and
suppositories
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 For higher-grade internal hemorrhoids
 Hemorrhoidal banding
 Surgical hemorrhoidectomy
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OTC medications
 Analgesics and local anesthetics
 Astringents
 Protectants
 Vasoconstrictors
 Keratolytics
 Hydrocortisone
 Wound healing agents
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 Astringents
Astringents reduce the swelling of the affected
tissues by shrinking them. They also act to
decrease mucous and other secretions. This
way, astringents reduce hemorrhoidal
symptoms like inflammation, burning, and
itching. However, they do not relive pain.
 Calamine, witch hazel (hamamelis water), and
zinc oxide are the most commonly used
astringents for hemroid treatment.
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Astringents
Allantoin,
Bismuth
oxide,
Bismuth
subgallate, Peru balsam, Zinc oxide.
MOA:
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astringents coagulate protein in skin and
mucous membrane cells to form a superficial
protective layer. By reducing secretion &
intracellular contents from damaged cells, they
help to relieve local irritation and
inflammation
2. Some astringents like zinc oxide and bismuth salts
also provide a mechanical protective barrier on the
surface of damaged skin. According to the FDA, such
barriers in order to be effective should constitute at
least 50% of the dosage unit
3. Peru balsam has additional mild antiseptic
properties.
 Protectants
Protectants are a type of over the counter hemorrhoid
medications that reduces inflammation by forming a
protective barrier over the skin and mucous membrane.
Protectants also prevent stratum corneum (topmost skin
layer) from losing water.
 A number of protectants are employed in over the counter
hemorrhoidal medication, e.g. aluminum hydroxide (in gel
form), glycerin (water solution), cocoa butter, mineral oil,
kaolin, and petrolatum etc.
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 Vasoconstrictors
Vasoconstrictors are a group of over the counter
hemorrhoid medications that work to 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, and discomfort of the affected tissues.
Vasoconstrictors are not usually recommended for
people with blood pressure problems and heart diseases
because the chemical agents in these products can raise
blood pressure and cause abnormal heartbeat along
with a range of other side effects.
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 Local Anesthetics
By blocking the nerves from conducting messages
of pain, burning, itching, and irritation, local
anesthetics provide temporary relief from these
hemorrhoid symptoms.
 Local anesthetics are mostly used for external
hemorrhoids only and include such chemical
agents as Benzocaine, Benzyl alcohol, Dibucaine,
and Lidocaine.
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Local Anaesthetics
 Benzocaine, Cinchocaine & Lidocaine
 MOA: Reversibly block stimulation of pain
receptors & sensory nerve fibers in & around area of
application
 All LA used in hemorrhoidal preparations are weak
basic amines: aromatic lipophilic group joined to
the hydrophilic amino group by a linking ester or
amide moiety
 They reach their site of action by penetrating the
lipophilic nerve structure in their lipid-soluble
unchanged form, but exert their anaesthetic action
in the ionised form
Local Anaesthetics
 All compounds used in haemorrhoidal
preparations, except for benzocaine, are HCL
salts converted to the un-ionized base at tissue
pH;
 Benzocaine is used in the free base form;
 Compounds with high lipid solubility tend to be
more potent & have faster onset & longer duration
of action than those with low lipid solubility
Local Anaesthetics
 LA are less effective on inflamed than on normal
tissue as the pH of inflamed tissue is lower,
resulting in higher degree of ionization Less
penetration;
 Generally, amide type anaesthetics are more
potent & produce less sensitization than ester-type
compounds
 In haemorrhoids, LA are used to relieve pain,
burning & itching;
Local Anaesthetics
 Use should be restricted to perianal region & lower
anal canal, they shouldn’t be used in the rectum
WHY?
 Because there is little sensory tissue there & and
anesthetics can be rapidly absorbed through the
rectal mucosa to cause potentially toxic systemic
effects;
 Use should be restricted to 5-7 days, as skin
sensitization & systemic allergic reactions are
possible with prolonged use;
Local Anaesthetics
Benzaocaine
 Used in concentration of 5-10% and frequency of
application of up to 6 times daily
 It is an ester type LA allergic reactions &
sensitization have been reported frequently
Cinchocaine
 Potent & long-acting amide type compound
 Used in 0.5-1.0% in haemorrhoidal preparations
 It has less sensitizing potential than Benzocaine
Local Anaesthetics
Lidocaine (Lignocaine)
 The most widely used LA in Haemorrhoidal
preparations
 An amide-type compound with a relatively long
duration of action
 Although it is poorly absorbed through the
skin, it may be rapidly & almost completely
absorbed through mucus membranes & broken
skin causing systemic toxicity
 However, most OTC formulations contain low
conc are safe
 Keratolytics
Keratolytics are yet another type of over the counter
hemroid medication. Keratolytics act to dissolve
skin flakes and scales (peel off the skin), which
enables the affected tissues to better absorb other
topical medication for hemorrhoids.
 This way, Keratolytics reduce itching and irritation
associated with the condition. Examples of
Keratolytics include Alcloxa and Resorcinol.
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Lidocaine ointment 5% (Lidoderm, Dermaflex): Indicated for PAIN & ITCHING
 Decreases permeability to sodium ions in neuronal membranes, resulting in
inhibition of depolarization, blocking transmission of nerve impulses.
Dosing
 Adult
 Apply to affected area prn
 Pediatric
 Apply as in adults
Interactions
 None reported
Contraindications
 Documented hypersensitivity
Precautions
 Pregnancy
 B - Fetal risk not confirmed in studies in humans but has been shown in some
studies in animals.
 For external or mucous membrane use only; do not use in eyes.
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Hamamelis water (Witch Hazel)
 Mild astringent prepared from twigs of Hamamelis virginiana,
used to temporarily relieve itching of hemorrhoids.
Dosing
 Adult
 Apply locally up to 6 times/d or following a bowel movement
 Pediatric
 Not established
Interactions
 None reported
Contraindications
 Documented hypersensitivity
Precautions
 Pregnancy: A - Fetal risk not revealed in controlled studies in
humans
 For external use only; avoid contact with eyes; discontinue
treatment if condition worsens
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Procedures to treat
haemorrhoids
 Injection of haemorroids with sclerosing agent.
This does not require a general anesthetic and can
be done in outpatient clinic or doctor’s room
 Rubber band ligation- this stops the blood flow
to the haemorrhoids causing the tissue to die and
the haemorroids will fall off
 Haemorrhoidectomy- surgical excision of the
haemorrhoid under general anesthetic and is
performed while inpatient at hospital
Administration & Dosage
Forms
 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
 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 selftreatment of haemorrhoids
Product Recommendations
 For mild cases- a compound preparation
containing a local anesthetic & astringent or skin
protective constituents
 For cases with additional inflammation and
irritation- a preparation containing
hydrocortisone
 For underlying constipation-short term
treatment with a stimulant laxative, followed by an
increase in fiber and fluid in the diet or regular use
of bulk laxative
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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The combination of diosmin 1350 mg plus hesperidin 150
mg twice daily for 4 days followed by diosmin 900 mg and
hesperidin 100 mg twice daily for 3 days seems to
significantly improve signs and symptoms of internal
hemorrhoids.
The combination can stop acute bleeding in up to 92% of
patients after 4 days of treatment. It can also reduce
symptoms such as anal discomfort, pain, discharge, and
local lesions.
Subjective symptoms can be relieved within 2 days of
treatment. The combination also seems to reduce the
duration and intensity of hemorrhoidal flare-ups
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 Some clinicians use diosmin in lower doses and in
combination with bulk laxatives instead of hesperidin.
Diosmin 600 mg three times daily for 4 days, then 300
mg twice daily for 10 more days plus the bulk laxative
psyllium 11 grams daily does seem to slightly help after
4 days of treatment.
 However, this combination does not seem to be as
effective as the higher dose of diosmin plus hesperidin
combination. Maintenance use of diosmin 450 mg plus
hesperidin 50 mg twice daily for 3 months in patients
following acute treatment for internal hemorrhoids
seems to significantly decrease the relapse rate.
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