No-spa pills 40mg №24

No shpa.
International non-proprietary name: Drotaverine.
Dosage Form: pills.
Composition
1 pill contains:
active ingredient: drotaverine hydrochloride - 40 mg;
excipients: Magnesium stearate - 3 mg, talc - 4 mg, povidone - 6 mg,
Corn starch - 35 mg, lactose monohydrate - 52 mg.
Description
Round biconvex pills of yellow with greenish or orangish
a touch of color, with spa engraving on one side.
Pharmacotherapeutic group: antispasmodic.
ATX code: A03A D02.
Pharmacological properties
Pharmacodynamics
Drotaverine is an isoquinoline derivative that exhibits
powerful antispasmodic effect on smooth muscles due to inhibition
phosphodiesterase enzyme (PDE). The enzyme phosphodiesterase is necessary for
hydrolysis of cyclic adenosine monophosphate (cAMP) to adenosine monophosphate
(AMP). Inhibition of the phosphodiesterase enzyme leads to an increase in
cAMP concentrations that trigger the following cascade reaction: high
cAMP concentrations activate cAMP dependent kinase phosphorylation
light chains of myosin (MLCM). Phosphorylation of MLCC leads to a decrease in
its affinity for the Ca2 + calmodulin complex, resulting in
inactivated form of MLCK supports muscle relaxation. cAMP
in addition, it affects the cytosolic concentration of the Ca2 + ion due to
stimulate Ca2 + transport to the extracellular space and
sarcoplasmic reticulum. This decreasing Ca2 + ion concentration
Drotaverine effect through cAMP explains the antagonistic effect of Drotaverine
in relation to Ca2 +.
In vitro, Drotaverine inhibits PDE IV isoenzyme without inhibition.
PDE III and PDE V isoenzymes V. Therefore, the effectiveness of Drotaverine depends on
concentration of PDE IV in tissues, the content of which in different tissues varies.
PDE IV is most important in suppressing the contractile activity of smooth
musculature, and therefore the selective inhibition of PDE IV may be
useful for the treatment of hyperkinetic dyskinesias and various diseases,
accompanied by a spastic condition of the gastrointestinal tract.
Hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs, mainly
way, with the help of PDE III isoenzyme, which explains the fact that when
high antispasmodic activity in Drotaverine, no serious
side effects from the heart and blood vessels and pronounced effects in
respect of the cardiovascular system.
Drotaverine is effective for smooth muscle spasms of both neurogenic and
muscular origin. Regardless of the type of vegetative innervation
Drotaverine relaxes the smooth muscles of the gastrointestinal tract,
biliary tract, urogenital system.
Pharmacokinetics
Absorption
After oral administration, drotaverine is rapidly and completely absorbed. After
65% of the accepted dose enters the systemic circulation in the systemic circulation
Drotaverine. The maximum plasma concentration (Cmax) is achieved through
45-60 minutes.
Distribution
In vitro, Drotaverine has a high binding to plasma proteins (95-98%), especially with
albumin, γ and β-globumin.
Drotaverine is evenly distributed through the tissues, penetrates the smooth muscle
cells Does not penetrate the blood-brain barrier. Drotaverine and / or its
metabolites may slightly penetrate the placental barrier.
Metabolism
In humans, drotaverine is almost completely metabolized in the liver by O-
deethylation. Its metabolites are rapidly conjugated with glucuronic acid.
The main metabolite is 4’-deethyldrotaverine, in addition to which
6-desethyldrotaverine and 4'-deethyldrotaveraldine were identified.
Removal
In humans, for the evaluation of pharmacokinetics, drotaverine was used
two-chamber mathematical model. The final half-life
plasma radioactivity was 16 hours.
Within 72 hours, drotaverine is almost completely eliminated from the body.
More than 50% of drotaverine is excreted by the kidneys and about 30% through the gastrointestinal
intestinal tract (excretion in bile). Drotaverine is mainly excreted.
in the form of metabolites, unchanged drotaverine in the urine is not detected.
Indications for use
Spasms of smooth muscles in diseases of the biliary tract:
cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis,
papillitis.
Spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis,
pyelitis, cystitis, spasms of the bladder.
As an adjunct therapy
With spasms of smooth muscles of the gastrointestinal tract: ulcerative
stomach and duodenal diseases, gastritis, cardia cramps and
pylorus, enteritis, colitis, spastic colitis with constipation and syndrome
irritable bowel with flatulence after exclusion of diseases,
manifested by the syndrome of "acute abdomen" (appendicitis, peritonitis,
ulcer perforation, acute pancreatitis, etc.).
With tension headaches.
With dysmenorrhea.
Contraindications
Hypersensitivity to the active substance or to any of
excipients of the drug.
Severe hepatic or renal failure.
Severe heart failure (low cardiac output syndrome).
Children's age up to 6 years.
Lactation period (no clinical data).
Rare hereditary intolerance to galactose, lactase deficiency and syndrome
glucose-galactose malabsorption (due to the presence of
lactose).
Carefully
- With arterial hypotension.
- In children (lack of clinical experience).
- In pregnant women (see section "Pregnancy and lactation").
Pregnancy and lactation period
As shown by reproductive studies in animals and retrospective data
on the clinical use of drotaverine, the use of drotaverine in the period
pregnancy had no teratogenic or embryotoxic effects.
Despite this, when using the drug during pregnancy should
to correlate the potential benefits to the mother and the possible risk to the fetus.
Due to the lack of necessary clinical data, during lactation
appoint is not recommended.
Dosage and administration
Adults
Usually the average daily dose in adults is 120-240 mg (daily dose
divided into 2-3 receptions). The maximum single dose is 80 mg. Maximum
the daily dose is 240 mg.
Children
Clinical studies using drotaverine involving children are not
was carried out.
In the case of the appointment of drotaverine children:
- for children from 6 to 12 years old, the maximum daily dose is 80 mg,
divided into 2 steps.
- for children over 12 years old, the maximum daily dose is 160 mg,
divided into 2-4 receptions.
Duration of treatment without consulting a doctor
When taking the drug without consulting a doctor recommended
the duration of the drug is usually 1-2 days. If within
this period, pain does not decrease, the patient should refer to
the doctor to clarify the diagnosis and, if necessary, change therapy. In cases
when Drotaverine is used as adjuvant therapy,
the duration of treatment without consulting a doctor may be longer (2-3
days).
Evaluation Method
If the patient can easily self-diagnose the symptoms of his
diseases, as they are well known to him, then the effectiveness
treatment, namely the disappearance of pain, is also easily measurable by the patient. AT
If within a few hours after taking the maximum single dose
there is a moderate decrease in pain or no decrease in pain, or
if the pain does not significantly decrease after taking the maximum daily dose,
It is recommended to consult a doctor.
Side effect
The adverse reactions observed in clinical
studies, divided by organ systems, indicating their frequency
occurrences in accordance with the following gradations: very frequent (≥ 10%),
frequent (≥1%, 10); infrequent (≥0.1%, 1%); rare (≥0.01%, 0.1%) and very rare,
including individual messages (0.01%), unknown frequency (according to available
data frequency can not be determined).
Since the cardiovascular system
Rare - increased heart rate, lowering blood pressure.
The nervous system
Rare - headache, dizziness, insomnia.
From the gastrointestinal tract
Rare - nausea, constipation.
The immune system
Rare - allergic reactions (angioedema, urticaria, rash, itching)
(see section "Contraindications").
Overdose
Data overdose of the drug is not available.
In case of overdose, patients should be under medical care.
observation, and if necessary, they should be symptomatic and
treatment aimed at maintaining the basic functions of the body, including
artificial induction of vomiting or gastric lavage.
Interaction with other drugs
With levodopa
Phosphodiesterase inhibitors like papaverine reduce
antiparkinsonic action of levodopa. When prescribing Drotaverine
simultaneously with levodopa, stiffness and tremor may be increased.
With other antispasmodic drugs, including m-anticholinergics
Mutual enhancement of antispasmodic action.
Drugs significantly binding to plasma proteins (more than 80%)
Drotaverine significantly binds to plasma proteins, predominantly
albumin, γ- and β-globulins (see the Pharmacokinetics section).
There are no data on the interaction of drotaverine with drugs, significantly
bound to plasma proteins, however there is a hypothetical
the possibility of their interaction with drotaverine at the level of communication with protein
(displacement of one of the drugs by the other due to protein and an increase in
the concentration of the free fraction in the blood of the drug with a less strong bond with
protein), which hypothetically may increase the risk of
pharmacodynamic and / or toxic side effects of this drug.
special instructions
No-shpa® 40 mg pills contain 52 mg of lactose. It may cause gastrointestinal
intestinal complaints in persons suffering from lactose intolerance. This form
unacceptable for patients suffering from lactose deficiency, galactosemia or
syndrome of impaired absorption of glucose / galactose (see section
"Contraindications").
Influence on ability to drive a car and other mechanisms
When administered in therapeutic doses, drotaverine has no effect on
ability to drive and perform jobs that require increased
attention. If any side effects occur, the question of driving
transport and working with mechanisms requires individual consideration.
In case of dizziness after taking the drug, it should be avoided.
engaging in potentially hazardous activities such as
car and work with mechanisms.
Release form
Tablets 40 mg.
On 6, 10 or 20 pills in the PVC / Aluminum blister.
On 1, 2, 4 or 5 blisters on 6 pills with the application instruction in cardboard
a pack.
On 3 blisters on 10 pills with the application instruction in a cardboard pack.
On 1 blister on 20 pills with the application instruction in a cardboard pack.
On 10 pills in the Aluminum / Aluminum blister card (it is laminated by polymer).
On 2 blisters with the application instruction in a cardboard pack.
On 60 pills in a bottle from polypropylene with a polyethylene stopper,
equipped with a piece dispenser.
On 1 bottle with the application instruction in a cardboard pack.
On 100 pills in a bottle from polypropylene with a polyethylene stopper.
On 1 bottle with the application instruction in a cardboard pack.
Shelf life
For pills in blisters Aluminum / Aluminum: 5 years.
For pills in PVC / Aluminum blister packs: 3 years.
For pills in vials: 5 years.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
For pills in blisters Aluminum / Aluminum: store at a temperature not higher than
30 ° C.
For pills in PVC / Aluminum blisters: Store at temperatures not higher than 25 ° C.
For pills in bottles: store in a dark place at a temperature
from 15 C to 25 C.
Keep out of the reach of children.
Pharmacy sales terms
Over the counter.
Manufacturer
Hinoin Pharmaceutical and Chemical Products CJSC, Hungary
st. Levai, 5, 2112 Veresegynház, Hungary.