Pharmacological operation: Drotaverine hydrochloride belongs
to spasmolytics of isochinoline derivative which contributes the relaxation of
smooth muscle, inhibition of phosphodiestherase enzyme, its intracellular
accumulation, increase of CAMF concentration and myosine kinasa via
inactivation of light chains.
Spasmolytic action of
drotaverine doesn't depend on vegetative innervation character, it has the same
spsmolytic action on gastrointestinal, billiary, urogenital and smooth
musculature of vascular system.
Because of vasodilatative
effect, it improves provision of tissues with blood. It is not characterized
withteratogenic andembriotoxic action.
Pharmacocynetics: Thepreparation
is absorbed rapidly and fully form gastrointestinal tract. Bioavailability is
almost 100%. T1/2 is 12 hour.
It distributes equally in tissues and compasses to smooth muscle cells.
Drotaverine bind to plasma proteins. Drotaverine is excreted mainly by kidneys.
Indications:
·Smooth muscles spasm, which is associated with
diseases of billiary tract; cholecystitis, cholangitis, pericholencystitis,
cholecystolithiasis, cholangiolithiasis, papillitis.
·Spasm of the urination system smooth muscles:
nephrolithiasis, urethrolithiasis, pyelitis, cystitis, urinary bladder
tenesmus.
·Spasm of gastrointestinal smooth muscle: gastric
and duodenum ulcer diseases, gastritis, enteritis, colitis,colitis due to
constipation and the colitis proceeding with meteorism;
·During obstetrics-gynecology:painful
menstruation,during pregnancy forthe decrease of uterus tonus, in case of
danger of abortion.
Contraindications:
·Increased sensitivity toward the components of
the preparation.
·During insufficiency of liver, kidneys and
heart.
Side effects:
Rarely may be occurred: nausea,
constipation, headache, dizziness, tachicardia, decrease of arterial pressure.
In patients with increased
sensitivity to lactic sugar constipation may occurred.
Application and
dosage rule:
In adults: Daily dose is 40-120 mg, 3-6 tablets a day, which should
be taken2-3 times a day. Single does
for adults is 40-80 mg (1-2 tablets).
In children until 12 years
preparation is prescribed by a doctor.
In children up to 6 years:
Recommended dose is 80-200 mg, 2-5 tablets a day, which should be taken 2-5
times a day.Single dose for children
above 6 years old is 40 mg (1tablet).
For children from 1 to 6
years: recommended daily dose is 40-120
mg, 1-3 tablets a day, which should be taken 2-3 times a day. Single dose for
children from 1 to 6 years is 20-40 mg (1/2 - 1 tablet);
Interaction with
other preparations: Usagethe preparation
withantiparkinson medication – Levodopa
decreasesits’ efficiency.
Pregnancy and lactation period: Due to the lack of safety and toxicity data about the
preparation, usage ,,Neospan” is
permitted after estimation expected benefit for mother and potential risk for the fetus.
Influence of vehicle and mechanisms management:In therapeutic doses the preparation doesn’t
influence on concentration ability.
Overdose: In case of
overdose antrioventricular block, heart stop and respiratory centre paralisys
occures. Specific antidote does’t exists.
In case of overdose
application of the preparation should be stopped and symptomatic treatment
should be carried. While antrioventricular block atropine and isoprenaline is
applied in vien, in case heart stop atropine or adrenaline in vien and
cardiostimulation is recommended,in
case respiratory centre paralisys artificial ventilation of lung should be carried.
Package:
Primary packing: 10
tabletsin blister.
Secondary packing: 6 blisters
in a cardboard box.
Shelf-life: 5 years.
In
case of visual defects and expiry of validity date, the preparation can not be
used.
Storage
conditions:
Store not more than 25ºC temperature in a dark, dry place and keep away from
children.
Issue:
III group of a pharmaceutical product(issued without a doctor's prescription).
