Dioxel

Diosmin + Hesperidin

Dioxel
450 mg/50 mg Film-Coated Tablet
Venotonic / Vasculoprotective
FORMULATION
Each film-coated tablet contains:
Micronized purified flavonoid fraction ……………....................................……. 500 mg
(Equivalent to 450 mg diosmin + 50 mg hesperidin)

PHARMACOLOGIC CATEGORY
Venotonic / Vasculoprotective

PRODUCT DESCRIPTION
Brown, film-coated, elliptical, biconvex tablet, plain on both sides
CLINICAL PHARMACOLOGY
PHARMACODYNAMICS
Micronized purified flavonoid fraction (MPFF) is an oral phlebotropic and vascular
protective agent consisting of 90% diosmin and 10% hesperidin. It increases venous
tone, improves lymphatic drainage and protects the microcirculation from inflammatory
processes and apoptosis. By decreasing the expression of some endothelial adhesion
molecules, MPFF inhibits the activation, migration and adhesion of leukocytes at the
capillary level. This leads to a reduction in the release of inflammatory mediators such
as oxygen-free radicals, prostaglandins and thromboxane resulting in a decrease in
capillary hyperpermeability.
PHARMACOKINETICS
Diosmin is rapidly transformed in the intestine by intestinal flora and absorbed as its
aglycone, diosmetin, after oral administration.
A study compared the absorption of a single oral dose of radiolabelled MPFF [500 mg
tablets containing trace amounts (about 25 nCi) of 14C-diosmin] with that of
nonmicronized diosmin in 12 healthy male volunteers. Results showed that about half
of an oral 500 mg dose of radiolabelled MPFF was absorbed within 48 hours of
administration. Since unabsorbed diosmin was not excreted in the urine, absorption
was evaluated based on the urinary elimination of radioactivity. Reduction in the
particle size of diosmin led to a significant increase in absorption; mean
gastrointestinal absorption of micronized 14C-diosmin was significantly greater than
with nonmicronized 14C-diosmin (57.9 vs. 32.7% during 0 to 168 hours postdose;
p=0.004).
The time to peak plasma concentration of diosmetin is 1 hour and plasma

concentrations decrease slowly after 2 hours; diosmetin is still detectable after 48
hours. The mean volume of distribution of diosmetin is 62.1 liters.
Diosmetin is rapidly and extensively degraded to phenolic acids or their glycine

conjugate derivates, which are eliminated in the urine. The predominant metabolite in
man is 3-hydroxy-phenylpropionic acid which is mainly eliminated in its conjugated
form. Metabolites found in smaller amounts include other phenolic acids
corresponding to 3-hydroxy-4-methoxybenzoic acid, 3-methoxy-4-
hydroxyphenylacetic acid and 3,4-dihydroxybenzoic acid. It is possible that
unidentified metabolites may be responsible for the pharmacological activity of
diosmin.
Elimination of micronized diosmin is relatively rapid with » 34% of the radiolabelled

dose of 14C-diosmin excreted in the urine and feces over the first 24 hours and » 86%
over the first 48 hours. Unmetabolized diosmin and diosmetin are not excreted in the
urine. The cumulative excretion of the dose in the urine and feces was 100%. About
half of the dose was eliminated in the feces as unchanged diosmin and diosmetin.
INDICATIONS
· Treatment of symptoms related to venolymphatic insufficiency (heavy legs, pain,
early morning restless cramps)
· Treatment of functional symptoms related to acute hemorrhoidal attack
DOSAGE AND ADMINISTRATION

R E C OMME NDE D OR A L DOS E
INDIC AT I ON (S hould be taken at midday and evening,
with meals )
Venolymphatic ins uffic ienc y 1 tablet twice a day
3 tablets twice a day for the firs t 4 days ,
A c ute hemorrhoidal attac k then 2 tablets twice a day for the next
3 days
Or, as pres c ribed by a phys ic ian
CONTRAINDICATIONS
· Hypersensitivity to any component of the product
WARNINGS AND PRECAUTIONS

Venolymphatic insufficiency
· The most effective way of giving this treatment is in combination with a healthy
lifestyle such as diet and exercise.
· Avoid exposure to sun, heat, excessive standing and being overweight.
· Walking and wearing special support stockings stimulate blood circulation.
Acute hemorrhoidal attack

· This medicine is no substitute for the specific treatment of other anal disorders.
· The treatment must be short-term. If the symptoms do not disappear within 15 days,
ask your doctor for advice; proctological examination should be performed and the
treatment reviewed.
INTERACTIONS WITH OTHER MEDICAMENTS

There are no known drug interactions with this medicine.
Tell your physician about other medicines you are taking.
STATEMENT ON USAGE FOR HIGH RISK GROUPS

Pregnancy:Inform your physician if you become pregnant while taking this medicine.
Experimental studies in animals have not demonstrated any teratogenic effect. To

date, there have been no reports of adverse effects in humans.
Lactation: Due to lack of information, breastfeeding should be avoided during

treatment.
UNDESIRABLE EFFECTS
Autonomic: Anxiety, cramps, drowsiness, feeling of discomfort, headache, hypotension,
insomnia, palpitation, tiredness, vertigo
Gastrointestinal: Abdominal pain, diarrhea, dyspepsia, epigastric pain, gastric
discomfort, nausea, vomiting
OVERDOSE ANDTREATMENT
No overdosage has been reported.
STORE AT TEMPERATURES NOT EXCEEDING 30ºC.
CAUTION: Foods, Drugs, Devices, and Cosmetics Act prohibits dispensing without
prescription.
Availability : Alu/Clear PVC Blister Pack by 10's; box of 30's
Manufactured by Amherst Laboratories, Inc.

UNILAB Pharma Campus, Barangay Mamplasan
Biñan, Laguna, Philippines
Distributed by United Laboratories, Inc.
66 United St., Mandaluyong City, Philippines
Under authority by BIOMEDIS, INC.
6/F Dynavision Bldg., 108 Rada St., Legaspi Village
Makati City, Philippines

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Diosmin + Hesperidin

The time to peak plasma concentration of diosmetin is 1 hour and plasma

Diosmetin is rapidly and extensively degraded to phenolic acids or their glycine

Elimination of micronized diosmin is relatively rapid with » 34% of the radiolabelled

DOSAGE AND ADMINISTRATION

WARNINGS AND PRECAUTIONS

Acute hemorrhoidal attack

INTERACTIONS WITH OTHER MEDICAMENTS

Tell your physician about other medicines you are taking.

STATEMENT ON USAGE FOR HIGH RISK GROUPS

Experimental studies in animals have not demonstrated any teratogenic effect. To

Lactation: Due to lack of information, breastfeeding should be avoided during

STORE AT TEMPERATURES NOT EXCEEDING 30ºC.

Availability : Alu/Clear PVC Blister Pack by 10's; box of 30's

Manufactured by Amherst Laboratories, Inc.

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